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ChEMBL ligand: CHEMBL6 (Aconip, Artracin, Artracin sr, Berlind 75 ret, Durametacin, Flexin-25 continus, Flexin-50 continus, Flexin-75 continus, Imbrilon, Indocid-r, Indocid ret, Indocin, Indocin sr, Indoderm, Indoflex, Indolar, Indolar sr, Indo-lemmon, Indomax-25, Indomax-75 sr, Indometacin, Indometacin farnesil, Indometacinum, Indomethacin, Indomod, Indo-paed, Indoptol, Indotard mr 75, Ledmecin, Maximet sr, Mobilan, NSC-757061, NSC-77541, Pardelprin mr, Reumacide, Rheumacin la, Rimacid, Slo-indo, Tivorbex) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Aldo-keto reductase family 1 member C1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5905] [UniProtKB: Q04828] | ||||||||
ChEMBL | Discontinuous Radiometric Assay: Compounds may be evaluated as selective reversible inhibitors of AKR1C3 by screening them against homogeneous recombinant AKR1C1-AKR1C4 expressed in E. coli. In each case, a discontinuous radiometric assay may be used to monitor the inhibition of progesterone reduction (20-ketosteroid reduction) catalyzed by AKR1C1, the inhibition of Δ4-AD reduction (17-ketosteroid reduction) catalyzed by AKR1C3, and the inhibition of 5α-DHT reduction (3-ketosteroid reduction) catalyzed by AKR1C2 and AKR1C4 (by measuring the formation of 20α-hydroxyprogesterone, testosterone or 3α-androstanediol by radiochromatography). Secondary screens of the compounds of interest include: (a) a full-screen against all nine human recombinant AKR enzymes to ensure there are no-intended off-target effects (in this context AKR1B10 (retinal reductase; SEQ ID NO:5) has been shown to be potently inhibited by N-phenylanthranilates) (Endo et al., 2010, Biol. Pharm. Bull. 33:886-90); (b) a screen against COX-1 and COX-2 to reaffirm that compounds do not act as NSAIDs; and (c) an expanded screen against other nuclear receptors (especially other steroid hormone receptors). | B | 4 | pKi | >100000 | nM | Ki | US-9271961-B2. Bifunctional AKR1C3 inhibitors/androgen receptor modulators and methods of use thereof (2016) |
ChEMBL | Inhibition of human recombinant N-terminal His6-tagged AKR1C1 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 7746-7758 [PMID:22877157] |
Aldo-keto reductase family 1 member C2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5847] [UniProtKB: P52895] | ||||||||
ChEMBL | Discontinuous Radiometric Assay: Compounds may be evaluated as selective reversible inhibitors of AKR1C3 by screening them against homogeneous recombinant AKR1C1-AKR1C4 expressed in E. coli. In each case, a discontinuous radiometric assay may be used to monitor the inhibition of progesterone reduction (20-ketosteroid reduction) catalyzed by AKR1C1, the inhibition of Δ4-AD reduction (17-ketosteroid reduction) catalyzed by AKR1C3, and the inhibition of 5α-DHT reduction (3-ketosteroid reduction) catalyzed by AKR1C2 and AKR1C4 (by measuring the formation of 20α-hydroxyprogesterone, testosterone or 3α-androstanediol by radiochromatography). Secondary screens of the compounds of interest include: (a) a full-screen against all nine human recombinant AKR enzymes to ensure there are no-intended off-target effects (in this context AKR1B10 (retinal reductase; SEQ ID NO:5) has been shown to be potently inhibited by N-phenylanthranilates) (Endo et al., 2010, Biol. Pharm. Bull. 33:886-90); (b) a screen against COX-1 and COX-2 to reaffirm that compounds do not act as NSAIDs; and (c) an expanded screen against other nuclear receptors (especially other steroid hormone receptors). | B | 4 | pKi | >100000 | nM | Ki | US-9271961-B2. Bifunctional AKR1C3 inhibitors/androgen receptor modulators and methods of use thereof (2016) |
ChEMBL | Inhibition of human recombinant N-terminal His6-tagged AKR1C2 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 7746-7758 [PMID:22877157] |
ChEMBL | Inhibition of human recombinant AKR1C2 expressed in Escherichia coli using S-tetralol as substrate by fluorometry | B | 4.12 | pIC50 | 75000 | nM | IC50 | J Nat Prod (2012) 75: 716-721 [PMID:22506594] |
ChEMBL | Inhibition of human recombinant AKR1C2-mediated NADP+-dependent oxidation of S-(+)-1,2,3,4-tetrahydro-1-naphthol | B | 4.44 | pIC50 | 36530 | nM | IC50 | J Med Chem (2013) 56: 2429-2446 [PMID:23432095] |
AKR1C3/Aldo-keto-reductase family 1 member C3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330] | ||||||||
ChEMBL | Discontinuous Radiometric Assay: Compounds may be evaluated as selective reversible inhibitors of AKR1C3 by screening them against homogeneous recombinant AKR1C1-AKR1C4 expressed in E. coli. In each case, a discontinuous radiometric assay may be used to monitor the inhibition of progesterone reduction (20-ketosteroid reduction) catalyzed by AKR1C1, the inhibition of Δ4-AD reduction (17-ketosteroid reduction) catalyzed by AKR1C3, and the inhibition of 5α-DHT reduction (3-ketosteroid reduction) catalyzed by AKR1C2 and AKR1C4 (by measuring the formation of 20α-hydroxyprogesterone, testosterone or 3α-androstanediol by radiochromatography). Secondary screens of the compounds of interest include: (a) a full-screen against all nine human recombinant AKR enzymes to ensure there are no-intended off-target effects (in this context AKR1B10 (retinal reductase; SEQ ID NO:5) has been shown to be potently inhibited by N-phenylanthranilates) (Endo et al., 2010, Biol. Pharm. Bull. 33:886-90); (b) a screen against COX-1 and COX-2 to reaffirm that compounds do not act as NSAIDs; and (c) an expanded screen against other nuclear receptors (especially other steroid hormone receptors). | B | 5.09 | pKi | 8200 | nM | Ki | US-9271961-B2. Bifunctional AKR1C3 inhibitors/androgen receptor modulators and methods of use thereof (2016) |
ChEMBL | Inhibition of N-terminal GST-tagged recombinant human AKR1C3 His5Gln mutant expressed in Escherichia coli BL21 (DE) Codon Plus RP cells assessed as reduction in NADPH production | B | 5.13 | pIC50 | 7350 | nM | IC50 | ACS Med Chem Lett (2019) 10: 437-443 [PMID:30996776] |
ChEMBL | Inhibition of N-terminal His-tagged human AKR1C3 (1 to 323 residues) expressed in Escherichia coli using 4-adione as substrate in presence of NADPH by fluorescence method | B | 5.14 | pIC50 | 7260 | nM | IC50 | J Med Chem (2020) 63: 11305-11329 [PMID:32463235] |
ChEMBL | Inhibition of human recombinant AKR1C3 expressed in Escherichia coli JM109 cells using S-tetralol as substrate by fluorometry | B | 5.39 | pIC50 | 4100 | nM | IC50 | J Nat Prod (2012) 75: 716-721 [PMID:22506594] |
ChEMBL | Inhibition of AKR1C3 using 9,10-phenanthroquinone as substrate | B | 5.64 | pIC50 | 2300 | nM | IC50 | J Med Chem (2012) 55: 7746-7758 [PMID:22877157] |
ChEMBL | Inhibition of AKR1C3 (unknown origin) using 9,10-phenanthrenequinone as substrate | B | 5.64 | pIC50 | 2300 | nM | IC50 | J Med Chem (2020) 63: 11305-11329 [PMID:32463235] |
ChEMBL | Inhibition of human recombinant N-terminal His6-tagged AKR1C3 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis | B | 6.14 | pIC50 | 730 | nM | IC50 | J Med Chem (2012) 55: 7746-7758 [PMID:22877157] |
ChEMBL | Inhibition of human recombinant AKR1C3-mediated NADP+-dependent oxidation of S-(+)-1,2,3,4-tetrahydro-1-naphthol | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2013) 56: 2429-2446 [PMID:23432095] |
Aldo-keto reductase family 1 member C4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4999] [UniProtKB: P17516] | ||||||||
ChEMBL | Inhibition of human recombinant N-terminal His6-tagged AKR1C4 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 7746-7758 [PMID:22877157] |
ChEMBL | Inhibition of human recombinant GST-tagged AKR1C4 expressed in Escherichia coli using S-tetralol as substrate by fluorometry | B | 4.27 | pIC50 | 54000 | nM | IC50 | J Nat Prod (2012) 75: 716-721 [PMID:22506594] |
aldo-keto reductase family 1 member B/Aldose reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1900] [GtoPdb: 2768] [UniProtKB: P15121] | ||||||||
ChEMBL | In vitro inhibition of rabbit lens aldose reductase. | B | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (1986) 29: 2347-2351 [PMID:3097317] |
Aldose reductase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3081] [UniProtKB: P16116] | ||||||||
ChEMBL | Inhibition of Aldose reductase (AR) | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (2001) 44: 1718-1728 [PMID:11356107] |
aldo-keto reductase family 1 member B/Aldose reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2622] [GtoPdb: 2768] [UniProtKB: P07943] | ||||||||
ChEMBL | DRUGMATRIX: Aldose Reductase enzyme inhibition (substrate: DL-Glyceraldehyde) | B | 5.44 | pIC50 | 3631 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
ChEMBL | Agonist activity at androgen receptor (unknown origin) expressed in HeLa cells co-expressing PSA-(ARE)4-Luc13 assessed as induction of DHT-induced luciferase activity after 20 mins by luciferase reporter gene assay | B | 9.85 | pEC50 | 0.14 | nM | EC50 | J Med Chem (2013) 56: 2429-2446 [PMID:23432095] |
5-LOX/Arachidonate 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917] | ||||||||
ChEMBL | Inhibitory activity against 5-lipoxygenase in Human whole blood (HWBL) stimulated with calcium ionophore (A23187) and LTB4 measured by enzyme immunoassay | F | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (1997) 40: 819-824 [PMID:9057869] |
5-LOX/Arachidonate 5-lipoxygenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527] | ||||||||
ChEMBL | Compound was evaluated for its inhibitory activity against 5-LO (5-lipoxygenase) in intact RBL-1 cell line assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 705-708 |
ChEMBL | Tested for inhibition of 5-Lipoxygenase (ARBL) in calcium-stimulated rat basophilic leukemia cells(RBL-1) | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 1655-1660 |
ChEMBL | Inhibition of 5-lipoxygenase in intact RBL-1 cell line | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1990) 33: 2070-2072 [PMID:2115586] |
ChEMBL | Inhibitory activity against 5-lipoxygenase of RBL-1 cell line | B | 4.6 | pIC50 | >25000 | nM | IC50 | J Med Chem (1992) 35: 3148-3155 [PMID:1507204] |
ChEMBL | Inhibition of 5-lipoxygenase in rat RBL-1 cells | B | 4.7 | pIC50 | >>20000 | nM | IC50 | J Med Chem (1990) 33: 1163-1170 [PMID:2319562] |
ChEMBL | Inhibitory activity against 5-lipoxygenase catalysis (5-LO) in sonicated rat basophilic leukemia cell lysate | F | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1997) 40: 819-824 [PMID:9057869] |
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
ChEMBL | Evaluated for binding affinity against recombinant human central cannabinoid receptor 1 | B | 4.7 | pKi | >20000 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 2263-2268 |
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
ChEMBL | Evaluated for binding affinity against recombinant human peripheral cannabinoid receptor 2 | B | 4.7 | pKi | >20000 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 2263-2268 |
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219] | ||||||||
ChEMBL | Binding affinity to COX1 (unknown origin) | B | 6.6 | pKd | 253 | nM | Kd | Med Chem Res (2012) 21: 3491-3498 |
ChEMBL | Inhibition of COX1 (unknown origin) | B | 4.9 | pIC50 | 12500 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 2931-2936 [PMID:26048794] |
ChEMBL | Inhibitory concentration against human recombinant Prostaglandin G/H synthase 1 cloned and expressed in baculovirus (Sf9) | B | 4.91 | pIC50 | 12400 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 1325-1328 [PMID:11392547] |
ChEMBL | Inhibition of COX1 in human platelet microsomes assessed as reduction in formation of oxidized TMPD using arachidonic acid as substrate preincubated for 3 to 5 mins followed by arachidonic acid addition measured for 25 secs by spectrophotometric assay | B | 4.92 | pIC50 | 12160 | nM | IC50 | ACS Med Chem Lett (2018) 9: 1045-1050 [PMID:30344915] |
ChEMBL | Inhibition of COX1 in human whole blood assessed as inhibition of 12-hydroxyheptadecatrienoic acid production by HPLC method | B | 5.22 | pIC50 | 6000 | nM | IC50 | Bioorg Med Chem (2010) 18: 3910-3924 [PMID:20451397] |
ChEMBL | Inhibition of COX1 | B | 5.25 | pIC50 | 5600 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2558-2560 [PMID:17346963] |
ChEMBL | Inhibition of COX1 by scintillation proximity assay | B | 5.41 | pIC50 | 3900 | nM | IC50 | J Nat Prod (2002) 65: 1517-1521 [PMID:12444669] |
ChEMBL | Inhibition of COX1 (unknown origin) | B | 5.41 | pIC50 | 3870 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1017-1025 [PMID:28089698] |
ChEMBL | Inhibition of human COX1 using arachidonic acid as substrate incubated for 2 mins by ELISA method | B | 5.81 | pIC50 | 1560 | nM | IC50 | Eur J Med Chem (2020) 185: 111780-111780 [PMID:31655429] |
ChEMBL | Inhibition of COX1-catalyzed prostaglandin biosynthesis 10 mins of preincubation | B | 5.85 | pIC50 | 1400 | nM | IC50 | J Nat Prod (1998) 61: 1212-1215 [PMID:9784154] |
ChEMBL | Inhibition of COX1-mediated PGD2 formation in LPS-stimulated human monocytes preincubated for 15 mins before arachidonic acid substrate addition measured after 30 mins by UPLC-MS/MS analysis | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2014) 57: 5638-5648 [PMID:24920381] |
ChEMBL | Inhibition of COX1 | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Nat Prod (1998) 61: 347-350 [PMID:9544564] |
ChEMBL | Inhibition of COX1-mediated PGF2alpha formation in LPS-stimulated human monocytes preincubated for 15 mins before arachidonic acid substrate addition measured after 30 mins by UPLC-MS/MS analysis | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2014) 57: 5638-5648 [PMID:24920381] |
ChEMBL | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2007) 50: 6367-6382 [PMID:17994684] |
ChEMBL | Inhibition of human platelets COX1 after 2 mins | B | 6.59 | pIC50 | 260 | nM | IC50 | Eur J Med Chem (2010) 45: 6027-6038 [PMID:20970223] |
ChEMBL | Inhibition of human COX1 using [14C]arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by TLC | B | 6.59 | pIC50 | 260 | nM | IC50 | Bioorg Med Chem (2018) 26: 3731-3762 [PMID:30017112] |
ChEMBL | Inhibition of human platelet COX1 | B | 6.59 | pIC50 | 260 | nM | IC50 | Eur J Med Chem (2008) 43: 456-463 [PMID:17532544] |
GtoPdb | - | - | 6.59 | pIC50 | 260 | nM | IC50 | Eur J Med Chem (2017) 141: 306-321 [PMID:29031075] |
ChEMBL | Inhibition of COX1 | B | 6.6 | pIC50 | 250 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3271-3274 [PMID:19427206] |
ChEMBL | Inhibitory activity against prostaglandin G/H synthase 1 | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2000) 43: 214-223 [PMID:10649977] |
ChEMBL | Inhibitory effect on Prostaglandin G/H synthase 1 activity was evaluated in human whole blood as TXB2 production | F | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2002) 45: 1402-1411 [PMID:11906281] |
ChEMBL | Inhibition of COX1 in human whole blood | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem (2010) 18: 3910-3924 [PMID:20451397] |
ChEMBL | Tested for inhibition against Prostaglandin G/H synthase 1 | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (1994) 37: 3878-3881 [PMID:7966148] |
ChEMBL | In vitro inhibitory potency against U-937 microsomal COX-1 | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684] |
ChEMBL | In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 1 | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1773-1778 [PMID:10406640] |
ChEMBL | Inhibitory activity against Prostaglandin G/H synthase 1 in human whole blood | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2207-2212 [PMID:10465547] |
ChEMBL | Biochemical index for Prostaglandin G/H synthase 1 measured as, thromboxane 2 (TXB2) levels following blood coagulation | B | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 1745-1748 [PMID:10937738] |
ChEMBL | Inhibitory potency against Prostaglandin G/H synthase 1 in human whole blood assay | B | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1201-1203 [PMID:14980665] |
ChEMBL | Inhibition of COX1 | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1612-1616 [PMID:21345672] |
ChEMBL | Inhibition of Prostaglandin G/H synthase 1 in human whole blood (HWB) assay | B | 6.8 | pIC50 | 160 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1715-1720 [PMID:10397507] |
ChEMBL | Inhibition of human Prostaglandin G/H synthase 1 | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2002) 45: 1511-1517 [PMID:11906292] |
ChEMBL | In vitro inhibitory activity towards human platelet recombinant Prostaglandin G/H synthase 1 | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 65-68 [PMID:11738574] |
ChEMBL | Inhibition of COX1 | B | 6.92 | pIC50 | 120 | nM | IC50 | ACS Med Chem Lett (2011) 2: 353-357 [PMID:24900317] |
ChEMBL | Inhibitory activity against recombinant human prostaglandin G/H synthase 1 | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1201-1203 [PMID:14980665] |
ChEMBL | Inhibition of COX1 (unknown origin) | B | 7 | pIC50 | 100 | nM | IC50 | Med Chem Res (2012) 21: 3491-3498 |
ChEMBL | In vitro inhibitory activity against constitutive form of human recombinant Prostaglandin G/H synthase 1 | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 867-872 |
ChEMBL | In vitro inhibitory activity against human recombinant prostaglandin G/H synthase 1. | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (1996) 39: 1846-1856 [PMID:8627608] |
ChEMBL | Inhibition of COX1 | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2008) 51: 2400-2411 [PMID:18363350] |
ChEMBL | Concentration required to inhibit human prostaglandin G/H synthase 1 (COX-1) by 50% | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (1997) 40: 1634-1647 [PMID:9171873] |
ChEMBL | In vitro inhibition of prostaglandin G/H synthase 1. | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (1995) 38: 4570-4578 [PMID:7473585] |
ChEMBL | Inhibitory activity against Prostaglandin G/H synthase 1 | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2000) 43: 3168-3185 [PMID:10956225] |
ChEMBL | Inhibition of COX1-mediated 12-HHT production in human platelet after 5 mins by HPLC analysis | B | 7.15 | pIC50 | 70 | nM | IC50 | Eur J Med Chem (2011) 46: 5021-5033 [PMID:21868137] |
ChEMBL | Inhibition of human COX1 | B | 7.29 | pIC50 | 51 | nM | IC50 | J Med Chem (2020) 63: 12873-12886 [PMID:33079544] |
ChEMBL | Inhibition of COX1 | B | 7.3 | pIC50 | 50 | nM | IC50 | Eur J Med Chem (2010) 45: 4058-4064 [PMID:20576329] |
ChEMBL | Inhibition of COX1 | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2012) 55: 2287-2300 [PMID:22263894] |
ChEMBL | Inhibition of human platelet COX1 using arachidonic acid as substrate preincubated for 15 mins before arachidonic acid addition measured after 15 mins | B | 7.36 | pIC50 | 44 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4307-4309 [PMID:22652053] |
ChEMBL | Inhibition of COX1-mediated PGH2 production by enzyme immunoassay | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem (2009) 17: 5044-5053 [PMID:19540763] |
ChEMBL | Inhibition of PGE-2 production in arachidonic acid-stimulated CHO cells expressing human Prostaglandin G/H synthase 1 | B | 7.41 | pIC50 | 39 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 2677-2682 |
ChEMBL | Inhibition of human platelet COX1 by EIA assay | B | 7.44 | pIC50 | 36 | nM | IC50 | J Nat Prod (2007) 70: 859-862 [PMID:17378609] |
ChEMBL | Inhibition of human platelets COX1 assessed as PGE2 production using arachidonic acid as substrate preincubated for 15 mins measured after 15 mins by EIA | B | 7.47 | pIC50 | 33.8 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4888-4890 [PMID:21752640] |
ChEMBL | Inhibition of human platelet COX1 assessed as effect on prostaglandin E2 production by ELISA | B | 7.55 | pIC50 | 28.2 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 459-461 [PMID:19056264] |
ChEMBL | In vitro inhibitory activity against human whole cells Prostaglandin G/H synthase 1 | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1773-1778 [PMID:10406640] |
ChEMBL | Inhibition of Prostaglandin G/H synthase 1 was measured by the inhibition of PGE-2 produced by microsomes from U937 cells incubated in low concentration of arachidonic acid | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2777-2782 [PMID:9873621] |
ChEMBL | Inhibition of COX1 (unknown origin)-mediated oxidation of N,N,N,Ntetramethyl-1,4-phenylenediamine using arachidonic acid as substrate by colorimetric assay | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2013) 56: 2429-2446 [PMID:23432095] |
ChEMBL | Inhibition of COX-1 in U-937 (human lymphoma) cell microsomes. | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3187-3192 [PMID:10576685] |
ChEMBL | Tested in vitro for the ability to inhibit Prostaglandin G/H synthase 1 in chinese hamster ovary (CHO) cells | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 57-62 |
ChEMBL | In vitro inhibitory potency against human COX-1 in stably transfected chinese hamster ovary (CHO) cells | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684] |
ChEMBL | In vitro inhibition of the production of PGE-2 in arachidonic acid stimulated chinese hamster ovary (CHO) cells transfected with human cyclooxygenase-1 | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 47-52 |
ChEMBL | DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) | B | 7.82 | pIC50 | 15 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibition activity against recombinant human Prostaglandin G/H synthase 1 | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (1997) 40: 819-824 [PMID:9057869] |
ChEMBL | Inhibition of COX1 | B | 8 | pIC50 | 10 | nM | IC50 | J Nat Prod (2005) 68: 985-991 [PMID:16038536] |
ChEMBL | Inhibition of COX1 | B | 8 | pIC50 | 10 | nM | IC50 | ACS Med Chem Lett (2011) 2: 353-357 [PMID:24900317] |
ChEMBL | IC50 value against Prostaglandin G/H synthase 1 of human platelet rich plasma | B | 8.09 | pIC50 | 8.2 | nM | IC50 | J Med Chem (1999) 42: 1161-1169 [PMID:10197960] |
ChEMBL | IC50 against Prostaglandin G/H synthase 1 from human platelet rich plasma | B | 8.09 | pIC50 | 8.2 | nM | IC50 | J Med Chem (1999) 42: 1151-1160 [PMID:10197959] |
ChEMBL | Inhibition of COX1 | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2007) 50: 1425-1441 [PMID:17341061] |
ChEMBL | Inhibition of COX1 assessed as TBX2 production in human whole blood | F | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4440-4443 [PMID:16814546] |
ChEMBL | Inhibition of arachidonic acid induced TXB2 generation in isolated human platelets (Prostaglandin G/H synthase 1 cell assay) | F | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2002) 45: 1402-1411 [PMID:11906281] |
ChEMBL | Inhibition of Prostaglandin G/H synthase 1 in U-937 cells from human histiocytic lymphoma | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2001) 44: 350-361 [PMID:11462976] |
ChEMBL | In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2003) 46: 3463-3475 [PMID:12877584] |
Cyclooxygenase-1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2860] [UniProtKB: O62664] | ||||||||
ChEMBL | Inhibition of bovine seminal microsomal COX1 assessed as PGE2 production | B | 5.48 | pIC50 | 3300 | nM | IC50 | J Nat Prod (1998) 61: 2-7 [PMID:9461646] |
ChEMBL | Inhibition of bovine seminal microsomal COX1 assessed as PGE2 production preincubated for 10 mins | B | 5.85 | pIC50 | 1400 | nM | IC50 | J Nat Prod (1998) 61: 2-7 [PMID:9461646] |
ChEMBL | Inhibition of bovine COX1-mediated prostaglandin biosynthesis using [1-14C]arachidonic acid | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Nat Prod (2001) 64: 745-749 [PMID:11421736] |
ChEMBL | Inhibition of bovine seminal vesicle microsomal COX1-mediated prostaglandin production | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Nat Prod (1998) 61: 8-12 [PMID:9461647] |
ChEMBL | Inhibition of bovine COX1 assessed as inhibition of calcium ionophore A23187-induced 12-hydroxyheptadecatrienoic acid formation by reverse-phase HPLC analysis | B | 8.39 | pIC50 | 4.1 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 5031-5034 [PMID:22749420] |
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979] | ||||||||
ChEMBL | Inhibition of ovine COX1 pre-incubated before addition of [1-14C]arachidonic acid | B | 5.1 | pKi | 7900 | nM | Ki | J Biol Chem (2007) 282: 16379-16390 [PMID:17434872] |
ChEMBL | Inhibition of ovine COX1 | B | 5.05 | pIC50 | 9000 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5324-5329 [PMID:25444084] |
ChEMBL | Inhibition of ovine COX1 by oxidized TMPD detection based colorimetric assay | B | 5.43 | pIC50 | 3740 | nM | IC50 | Eur J Med Chem (2015) 101: 81-95 [PMID:26117820] |
ChEMBL | Inhibition of ram seminal vesicle COX1 assessed as PGE2 production by enzyme immunoassay | B | 5.68 | pIC50 | 2100 | nM | IC50 | J Nat Prod (2011) 74: 1779-1786 [PMID:21800856] |
ChEMBL | Inhibitory activity against Prostaglandin G/H synthase 1 isolated from ram (sheep) seminal vesicle | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (1998) 41: 420-427 [PMID:9484493] |
ChEMBL | Inhibition of COX1 in ram seminal vesicle microsomes assessed as reduction of PGE2 formation | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Nat Prod (2000) 63: 403-405 [PMID:10757731] |
ChEMBL | Inhibition of ovine COX1 | B | 5.85 | pIC50 | 1400 | nM | IC50 | J Nat Prod (2006) 69: 887-890 [PMID:16792405] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay | B | 5.94 | pIC50 | 1140 | nM | IC50 | Eur J Med Chem (2017) 127: 10-21 [PMID:28038322] |
ChEMBL | Inhibition of ram seminal vesicle COX1 assessed as PGE2 level by EIA | B | 5.96 | pIC50 | 1090 | nM | IC50 | Bioorg Med Chem (2010) 18: 2809-2815 [PMID:20236826] |
ChEMBL | Inhibition of COX1 in ram seminal vesicle by enzyme immunoassay | B | 6.05 | pIC50 | 900 | nM | IC50 | Bioorg Med Chem (2009) 17: 4459-4465 [PMID:19481465] |
ChEMBL | Inhibition of ovine COX-1 using arachidonic acid after 5 mins by colorimetric method | B | 6.1 | pIC50 | 790 | nM | IC50 | Bioorg Med Chem (2015) 23: 6807-6814 [PMID:26455657] |
ChEMBL | Inhibition of ovine COX-1 assessed as reduction in oxidation of TMPD using arachidonic acid as substrate preincubated for 5 mins followed by substrate and TMPD addition measured after 5 mins by colorimetric assay | B | 6.15 | pIC50 | 710 | nM | IC50 | Bioorg Med Chem (2017) 25: 665-676 [PMID:27916468] |
ChEMBL | Inhibition of ovine COX1 assessed as inhibition of PGF2alpha production from PGH2 by enzyme immuno assay | B | 6.17 | pIC50 | 680 | nM | IC50 | Eur J Med Chem (2012) 57: 59-64 [PMID:23047224] |
ChEMBL | Inhibition of ovine recombinant COX-1 using PGH2 as substrate incubated for 10 mins prior to arachidonic acid addition measured after 2 mins by EIA | B | 6.19 | pIC50 | 650 | nM | IC50 | Bioorg Med Chem (2015) 23: 2518-2528 [PMID:25868745] |
ChEMBL | Inhibition of sheep placental COX2 by liquid scintillation counter | B | 6.22 | pIC50 | 600 | nM | IC50 | J Nat Prod (2005) 68: 69-73 [PMID:15679320] |
ChEMBL | Inhibition of ovine COX1 assessed as prostaglandin F2alpha level | B | 6.22 | pIC50 | 600 | nM | IC50 | Eur J Med Chem (2014) 77: 155-165 [PMID:24631895] |
ChEMBL | Tested for inhibitory activity against Prostaglandin G/H synthase 1 from ovine | B | 6.51 | pIC50 | 310 | nM | IC50 | J Med Chem (1995) 38: 3895-3901 [PMID:7562922] |
ChEMBL | Inhibition of ram seminal vesicle COX-1 assessed as PGE2 production from arachidonic acid after 20 mins enzyme immunoassay | B | 6.52 | pIC50 | 300 | nM | IC50 | J Nat Prod (2011) 74: 614-619 [PMID:21319773] |
ChEMBL | Inhibition of sheep COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by UV-visible spectrophotometric method | B | 6.6 | pIC50 | 250 | nM | IC50 | Eur J Med Chem (2020) 186: 111863-111863 [PMID:31740050] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid substrate assessed as PGE2 production ELISA method after 2 mins | B | 6.68 | pIC50 | 210 | nM | IC50 | Bioorg Med Chem (2014) 22: 4151-4161 [PMID:24938495] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate assessed as production of PGF2alpha preincubated for 10 mins followed by substrate addition measured after 2 mins by EIA in presence of stannous chloride | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem (2013) 21: 4581-4590 [PMID:23769654] |
ChEMBL | Inhibition of ovine COX1 assessed as reduction in PGF2alpha formation incubated for 18 hrs by enzyme immunoassay | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4638-4642 [PMID:25219899] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 10 mins before substrate addition measured after 5 mins by EIA | B | 6.74 | pIC50 | 180 | nM | IC50 | Eur J Med Chem (2014) 80: 47-56 [PMID:24763362] |
ChEMBL | Inhibition of ovine COX1 after 5 mins by microplate reader assay | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 121-124 [PMID:21144750] |
ChEMBL | Inhibition of ovine COX-1 by enzyme immuno assay | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 2154-2159 [PMID:22361134] |
ChEMBL | Inhibition of ovine COX-1 | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2011) 54: 1356-1364 [PMID:21280601] |
ChEMBL | Inhibition of ovine COX1 by colorimetric assay | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2012) 55: 8152-8163 [PMID:22916727] |
ChEMBL | Inhibition of Ovine COX-1 preincubated for 15 mins by fluorescence analysis | B | 6.96 | pIC50 | 110 | nM | IC50 | ACS Med Chem Lett (2015) 6: 1086-1090 [PMID:26487917] |
ChEMBL | Inhibition of ovine COX1 | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2012) 55: 688-696 [PMID:22148253] |
ChEMBL | Inhibition of COX1 from ram seminal vesicles by liquid scintillation counter | B | 7 | pIC50 | 100 | nM | IC50 | J Nat Prod (2005) 68: 69-73 [PMID:15679320] |
ChEMBL | Inhibition of ovine COX1 by enzyme immunoassay | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3014-3018 [PMID:19419861] |
ChEMBL | Inhibition of ovine COX1 by enzyme immuno assay | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem (2007) 15: 4767-4774 [PMID:17509888] |
ChEMBL | In vitro inhibitory concentration against COX-1 enzyme | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2005) 48: 4061-4067 [PMID:15943479] |
ChEMBL | Inhibition of ovine COX1 assessed as reduction in PGF2alpha production by ELISA | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2017) 139: 936-946 [PMID:28881288] |
ChEMBL | Inhibition of ovine COX1 by peroxidase activity-based colorimetric assay | B | 7 | pIC50 | 99 | nM | IC50 | Eur J Med Chem (2014) 74: 606-618 [PMID:24531199] |
ChEMBL | Inhibition of ovine COX-1 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2021) 64: 9550-9566 [PMID:34137625] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by spectrophotometry | B | 7.1 | pIC50 | 80 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 77-82 [PMID:24332492] |
ChEMBL | Inhibition of ovine COX-1 assessed as PGF2alpha formation using arachidonic acid as substrate pretreated with compound for 20 mins prior to substrate addition by spectrophotometric analysis | B | 7.1 | pIC50 | 80 | nM | IC50 | Eur J Med Chem (2015) 97: 104-123 [PMID:25956953] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins followed by substrate addition and measured after 2 mins by EIA assay | B | 7.1 | pIC50 | 80 | nM | IC50 | Bioorg Med Chem (2020) 28: 115246-115246 [PMID:31843462] |
ChEMBL | Inhibition of ovine COX-1 assessed as decrease in prostaglandin production using arachidonic acid as substrate incubated with enzyme for 10 mins prior to substrate challenge by enzyme immunoassay | B | 7.1 | pIC50 | 80 | nM | IC50 | Eur J Med Chem (2014) 77: 185-192 [PMID:24631898] |
ChEMBL | Inhibition of ovine COX1 by enzyme immunoassay | B | 7.16 | pIC50 | 69 | nM | IC50 | Eur J Med Chem (2009) 44: 1830-1837 [PMID:19084295] |
ChEMBL | Inhibition of sheep COX1 by enzyme immunoassay | B | 7.16 | pIC50 | 69 | nM | IC50 | Bioorg Med Chem (2010) 18: 6367-6376 [PMID:20692174] |
ChEMBL | In vitro inhibitory activity against prostaglandin G/H synthase 1 from the microsomal fraction of ram seminal vesicles | B | 7.17 | pIC50 | 67 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1683-1688 [PMID:15026050] |
ChEMBL | In vitro inhibition against Prostaglandin G/H synthase 1 from ram seminal vesicles | B | 7.17 | pIC50 | 67 | nM | IC50 | J Med Chem (2003) 46: 3975-3984 [PMID:12954051] |
ChEMBL | Inhibition of ovine COX1 | B | 7.2 | pIC50 | 63 | nM | IC50 | Eur J Med Chem (2013) 65: 51-59 [PMID:23693150] |
ChEMBL | In vitro inhibitory activity against ovine Prostaglandin G/H synthase 1 (44 nM) using [14C]AA (50 uM) was determined | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2000) 43: 2860-2870 [PMID:10956194] |
ChEMBL | Inhibition of ovine COX1 by discontinuous radioactive TLC assay | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2013) 56: 2429-2446 [PMID:23432095] |
ChEMBL | Inhibition of ram seminal vesicle COX1 assessed as conversion of [14C]-arachidonic acid to [14C]-prostaglandins preincubated for 20 mins by thin-layer chromatography analysis | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem (2011) 19: 3242-3248 [PMID:21524587] |
ChEMBL | Inhibition of ovine COX1 | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 85-89 [PMID:18061444] |
ChEMBL | Inhibition concentration against Prostaglandin G/H synthase 1 | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1315-1318 [PMID:11965379] |
ChEMBL | Inhibition of ovine COX1 | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 1787-1791 [PMID:20129783] |
ChEMBL | Inhibition of ovine COX-1 by EIA method | B | 7.39 | pIC50 | 41 | nM | IC50 | Eur J Med Chem (2019) 183: 111693-111693 [PMID:31539778] |
ChEMBL | Inhibition of ovine COX1 by colorimetric analysis | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2020) 200: 112439-112439 [PMID:32485532] |
ChEMBL | Inhibition of ovine COX1 assessed as reduction in PGH2 formation by measuring PGF2alpha by colorimetric assay | B | 7.41 | pIC50 | 39 | nM | IC50 | Bioorg Med Chem (2017) 25: 5637-5651 [PMID:28916158] |
ChEMBL | Inhibition of ovine COX1 catalytic activity using arachidonic acid as substrate pre-incubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA method | B | 7.41 | pIC50 | 39 | nM | IC50 | Eur J Med Chem (2019) 167: 562-582 [PMID:30818268] |
ChEMBL | Inhibition of ovine COX -1 by colorimetric inhibitor screening assay kit method | B | 7.41 | pIC50 | 39 | nM | IC50 | Eur J Med Chem (2019) 167: 161-186 [PMID:30771604] |
ChEMBL | Inhibition of ovine COX1 assessed as reduction in PGF2alpha production using arachidonic acid as substrate by colorimetric method | B | 7.41 | pIC50 | 39 | nM | IC50 | Eur J Med Chem (2018) 144: 635-650 [PMID:29289887] |
ChEMBL | Inhibition of ovine COX1 | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem (2007) 15: 1014-1021 [PMID:17079150] |
ChEMBL | Inhibition of wild type ovine COX1 expressed in ram seminal vesicles using [1-14C]-arachidonic acid as substrate incubated for 17 mins at 25 degC followed by 3 mins at 37 degC prior to substrate addition measured after 30 secs by thin layer chromatographic analysis | B | 7.57 | pIC50 | 27 | nM | IC50 | ACS Med Chem Lett (2013) 4: 486-490 [PMID:23687559] |
ChEMBL | IC50 value against ovine Prostaglandin G/H synthase 1 | B | 7.91 | pIC50 | 12.2 | nM | IC50 | J Med Chem (1999) 42: 1161-1169 [PMID:10197960] |
ChEMBL | IC50 against ovine Prostaglandin G/H synthase 1 | B | 7.91 | pIC50 | 12.2 | nM | IC50 | J Med Chem (1999) 42: 1151-1160 [PMID:10197959] |
ChEMBL | Inhibition of ovine COX-1 using arachidonic acid as substrate by fluorescence assay | B | 7.92 | pIC50 | 12 | nM | IC50 | Eur J Med Chem (2021) 224: 113682-113682 [PMID:34245948] |
ChEMBL | Inhibition of ovine COX1 by colorimetric assay | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2012) 55: 8152-8163 [PMID:22916727] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 1 min prior to substrate addition measured for 25 secs by TMPD-based chromogenic assay | B | 8.17 | pIC50 | 6.7 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6745-6749 [PMID:23010270] |
ChEMBL | Inhibition of ovine COX1 after 5 mins | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2010) 53: 4691-4700 [PMID:20503989] |
ChEMBL | Inhibition of ovine COX-1 assessed as residual activity by measuring formation of 12-HHT from arachidonic acid by HPLC analysis | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem (2011) 19: 5372-5382 [PMID:21873070] |
ChEMBL | Inhibition of ovine COX1 | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4440-4443 [PMID:16814546] |
COX-1 /Cyclooxygenase-1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2649] [GtoPdb: 1375] [UniProtKB: P22437] | ||||||||
ChEMBL | In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2005) 48: 3428-3432 [PMID:15857149] |
COX-1 /Cyclooxygenase-1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4042] [GtoPdb: 1375] [UniProtKB: Q63921] | ||||||||
ChEMBL | In vitro inhibitory concentration against rat prostaglandin G/H synthase 1 | B | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2687-2690 [PMID:11591502] |
ChEMBL | Inhibition of Prostaglandin G/H synthase 1 using whole cell assay | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 725-730 |
ChEMBL | In vitro inhibition of Prostaglandin G/H synthase 1 | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 731-736 |
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] | ||||||||
ChEMBL | Binding affinity to COX2 (unknown origin) | B | 7.04 | pKd | 92 | nM | Kd | Med Chem Res (2012) 21: 3491-3498 |
ChEMBL | Binding affinity to wild type human COX2 expressed in insect cells using [1-14C]-arachidonic acid as substrate | B | 5.82 | pKi | 1500 | nM | Ki | ACS Med Chem Lett (2013) 4: 486-490 [PMID:23687559] |
ChEMBL | Inhibition of COX2 | B | 4.11 | pIC50 | 77100 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2558-2560 [PMID:17346963] |
ChEMBL | Inhibition of human COX2 using arachidonic acid as substrate incubated for 2 mins by ELISA method | B | 4.16 | pIC50 | 68450 | nM | IC50 | Eur J Med Chem (2020) 185: 111780-111780 [PMID:31655429] |
ChEMBL | Inhibition of human recombinant COX2 expressed in baculovirus infected SF21 cell | B | 4.45 | pIC50 | 35200 | nM | IC50 | Eur J Med Chem (2010) 45: 6135-6138 [PMID:20974503] |
ChEMBL | Inhibition of human COX2 expressed in baculovirus infected sf21 cells assessed as reduction in formation of oxidized TMPD using arachidonic acid as substrate preincubated for 3 to 5 mins followed by arachidonic acid addition measured for 25 secs by spectrophotometric assay | B | 4.45 | pIC50 | 35200 | nM | IC50 | ACS Med Chem Lett (2018) 9: 1045-1050 [PMID:30344915] |
ChEMBL | Inhibition of human recombinant COX-2 using PGH2 as substrate incubated for 10 mins prior to arachidonic acid addition measured after 2 mins by EIA | B | 4.53 | pIC50 | 29600 | nM | IC50 | Bioorg Med Chem (2015) 23: 2518-2528 [PMID:25868745] |
ChEMBL | Inhibition of COX2 | B | 4.7 | pIC50 | 20000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 353-357 [PMID:24900317] |
ChEMBL | Inhibition of human recombinant COX2 assessed as prostaglandin F2alpha level | B | 4.73 | pIC50 | 18500 | nM | IC50 | Eur J Med Chem (2014) 77: 155-165 [PMID:24631895] |
ChEMBL | Inhibition of human recombinant COX2 assessed as inhibition of PGF2alpha production from PGH2 by enzyme immunoassay | B | 4.74 | pIC50 | 18300 | nM | IC50 | Eur J Med Chem (2012) 57: 59-64 [PMID:23047224] |
ChEMBL | Inhibition of COX2 | B | 4.74 | pIC50 | 18000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 353-357 [PMID:24900317] |
ChEMBL | Inhibition of human recombinant COX-2 after 2 mins by fluorescence assay | B | 4.77 | pIC50 | 17000 | nM | IC50 | J Med Chem (2011) 54: 3037-3050 [PMID:21434686] |
ChEMBL | Inhibition of human recombinant COX-2 assessed as reduction in oxidation of TMPD using arachidonic acid as substrate preincubated for 5 mins followed by substrate and TMPD addition measured after 5 mins by colorimetric assay | B | 4.96 | pIC50 | 11070 | nM | IC50 | Bioorg Med Chem (2017) 25: 665-676 [PMID:27916468] |
ChEMBL | Inhibition of COX2 | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (2008) 51: 2400-2411 [PMID:18363350] |
ChEMBL | Inhibition of COX2 (unknown origin) | B | 5.09 | pIC50 | 8130 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1017-1025 [PMID:28089698] |
ChEMBL | In vitro inhibitory activity against human recombinant prostaglandin G/H synthase 2 expressed in sf-9 cells infected with baculovirus | B | 5.11 | pIC50 | 7810 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1683-1688 [PMID:15026050] |
ChEMBL | In vitro inhibition against human Prostaglandin G/H synthase 2 | B | 5.11 | pIC50 | 7800 | nM | IC50 | J Med Chem (2003) 46: 3975-3984 [PMID:12954051] |
ChEMBL | Inhibition of human COX2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay | B | 5.14 | pIC50 | 7240 | nM | IC50 | Eur J Med Chem (2017) 127: 10-21 [PMID:28038322] |
ChEMBL | Inhibition of human recombinant COX-2 | B | 5.16 | pIC50 | 6900 | nM | IC50 | J Med Chem (2011) 54: 1356-1364 [PMID:21280601] |
ChEMBL | Inhibition of human recombinant COX-2 by enzyme immuno assay | B | 5.16 | pIC50 | 6900 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 2154-2159 [PMID:22361134] |
ChEMBL | IC50 against recombinant human Prostaglandin G/H synthase 2 | B | 5.24 | pIC50 | 5800 | nM | IC50 | J Med Chem (1999) 42: 1151-1160 [PMID:10197959] |
ChEMBL | Inhibition of recombinant human prostaglandin G/H synthase 2 (COX-2) | B | 5.24 | pIC50 | 5800 | nM | IC50 | J Med Chem (1999) 42: 1161-1169 [PMID:10197960] |
ChEMBL | Inhibition of human recombinant COX2 | B | 5.24 | pIC50 | 5800 | nM | IC50 | J Nat Prod (2006) 69: 887-890 [PMID:16792405] |
ChEMBL | Inhibition of human recombinant COX2 | B | 5.24 | pIC50 | 5700 | nM | IC50 | J Med Chem (2012) 55: 688-696 [PMID:22148253] |
ChEMBL | Inhibition of COX2 | B | 5.41 | pIC50 | 3900 | nM | IC50 | J Nat Prod (2005) 68: 985-991 [PMID:16038536] |
ChEMBL | Inhibition of human recombinant COX2 using arachidonic acid substrate assessed as PGE2 production ELISA method after 2 mins | B | 5.49 | pIC50 | 3240 | nM | IC50 | Bioorg Med Chem (2014) 22: 4151-4161 [PMID:24938495] |
GtoPdb | - | - | 5.58 | pIC50 | 2630 | nM | IC50 | Eur J Med Chem (2017) 141: 306-321 [PMID:29031075] |
ChEMBL | Inhibition of human recombinant COX2 after 45 mins | B | 5.58 | pIC50 | 2630 | nM | IC50 | Eur J Med Chem (2010) 45: 6027-6038 [PMID:20970223] |
ChEMBL | Inhibition of human recombinant COX2 | B | 5.58 | pIC50 | 2630 | nM | IC50 | Eur J Med Chem (2008) 43: 456-463 [PMID:17532544] |
ChEMBL | Inhibition of human COX2 using [14C]arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 45 mins by TLC | B | 5.58 | pIC50 | 2630 | nM | IC50 | Bioorg Med Chem (2018) 26: 3731-3762 [PMID:30017112] |
ChEMBL | Inhibition of human COX-2 using [14C]-arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 45 mins by thin layer chromatographic method | B | 5.58 | pIC50 | 2630 | nM | IC50 | Eur J Med Chem (2017) 141: 306-321 [PMID:29031075] |
ChEMBL | In vitro inhibitory activity towards human recombinant Prostaglandin G/H synthase 2 enzyme | B | 5.62 | pIC50 | 2400 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 65-68 [PMID:11738574] |
ChEMBL | Inhibition of human Prostaglandin G/H synthase 2 | B | 5.62 | pIC50 | 2380 | nM | IC50 | J Med Chem (2002) 45: 1511-1517 [PMID:11906292] |
ChEMBL | Inhibition of human recombinant COX-2 assessed as PGE2 production from arachidonic acid after 20 mins enzyme immunoassay | B | 5.72 | pIC50 | 1900 | nM | IC50 | J Nat Prod (2011) 74: 614-619 [PMID:21319773] |
ChEMBL | Inhibition of human COX-2 using arachidonic acid as substrate incubated for 5 mins by fluorescence-based assay | B | 5.83 | pIC50 | 1466 | nM | IC50 | Eur J Med Chem (2019) 180: 41-50 [PMID:31299586] |
ChEMBL | Inhibition of COX2-mediated PGF2alpha formation in LPS-stimulated human monocytes preincubated for 15 mins before arachidonic acid substrate addition measured after 30 mins by UPLC-MS/MS analysis | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2014) 57: 5638-5648 [PMID:24920381] |
ChEMBL | Inhibition of COX2-mediated PGD2 formation in LPS-stimulated human monocytes preincubated for 15 mins before arachidonic acid substrate addition measured after 30 mins by UPLC-MS/MS analysis | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2014) 57: 5638-5648 [PMID:24920381] |
ChEMBL | Inhibition of COX2 (unknown origin) | B | 5.92 | pIC50 | 1200 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 2931-2936 [PMID:26048794] |
ChEMBL | Tested for inhibition against Prostaglandin G/H synthase 2 | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (1994) 37: 3878-3881 [PMID:7966148] |
ChEMBL | Inhibition of COX2 (unknown origin) | B | 5.93 | pIC50 | 1170 | nM | IC50 | Med Chem Res (2012) 21: 3491-3498 |
ChEMBL | Inhibition of human COX2 pre-incubated for 10 mins before arachidonic acid addition and measured after 2 mins by EIA method | B | 6.02 | pIC50 | 960 | nM | IC50 | J Med Chem (2018) 61: 7929-7941 [PMID:30095904] |
ChEMBL | Inhibition of human COX-2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA | B | 6.02 | pIC50 | 960 | nM | IC50 | J Med Chem (2021) 64: 9550-9566 [PMID:34137625] |
ChEMBL | Inhibition of human recombinant COX-2 assessed as PGF2 alpha formation using arachidonic acid as substrate pretreated with compound for 20 mins prior to substrate addition by spectrophotometric analysis | B | 6.02 | pIC50 | 960 | nM | IC50 | Eur J Med Chem (2015) 97: 104-123 [PMID:25956953] |
ChEMBL | Inhibition of human recombinant COX2 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by spectrophotometry | B | 6.02 | pIC50 | 960 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 77-82 [PMID:24332492] |
ChEMBL | Inhibition of human recombinant COX-2 assessed as decrease in prostaglandin production using arachidonic acid as substrate incubated with enzyme for 10 mins prior to substrate challenge by enzyme immunoassay | B | 6.02 | pIC50 | 960 | nM | IC50 | Eur J Med Chem (2014) 77: 185-192 [PMID:24631898] |
ChEMBL | Inhibition of recombinant human COX-2 assessed as reduction in prostaglandin production preincubated for 10 mins followed by arachidonic acid addition and measured after 2 mins by EIA method | B | 6.02 | pIC50 | 960 | nM | IC50 | J Med Chem (2019) 62: 6363-6376 [PMID:31244108] |
ChEMBL | Inhibition of human COX2 using arachidonic acid as substrate incubated for 10 mins followed by substrate addition and measured after 2 mins by EIA assay | B | 6.02 | pIC50 | 960 | nM | IC50 | Bioorg Med Chem (2020) 28: 115246-115246 [PMID:31843462] |
ChEMBL | Inhibition of human COX2 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA | B | 6.04 | pIC50 | 920 | nM | IC50 | Eur J Med Chem (2020) 189: 112066-112066 [PMID:31982653] |
ChEMBL | In vitro inhibitory activity against human recombinant prostaglandin G/H synthase 2 | B | 6.05 | pIC50 | 900 | nM | IC50 | J Med Chem (1996) 39: 1846-1856 [PMID:8627608] |
ChEMBL | Inhibitory activity against Prostaglandin G/H synthase 2 | B | 6.05 | pIC50 | 900 | nM | IC50 | J Med Chem (2000) 43: 3168-3185 [PMID:10956225] |
ChEMBL | In vitro inhibition of prostaglandin G/H synthase 2 (COX-2). | B | 6.05 | pIC50 | 900 | nM | IC50 | J Med Chem (1995) 38: 4570-4578 [PMID:7473585] |
ChEMBL | In vitro inhibitory activity against inducible form of human recombinant Prostaglandin G/H synthase 1 | B | 6.05 | pIC50 | 900 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 867-872 |
ChEMBL | Concentration required to inhibit human Prostaglandin G/H synthase 2 (COX-2) by 50% | B | 6.05 | pIC50 | 900 | nM | IC50 | J Med Chem (1997) 40: 1634-1647 [PMID:9171873] |
ChEMBL | DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) | B | 6.08 | pIC50 | 840 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (66 nM) using [14C]AA (50 uM) was determined | B | 6.12 | pIC50 | 750 | nM | IC50 | J Med Chem (2000) 43: 2860-2870 [PMID:10956194] |
ChEMBL | Inhibition of human COX2 expressed in SF-9 insect cells assessed as conversion of [14C]-arachidonic acid to [14C]-prostaglandins preincubated for 20 mins by thin-layer chromatography analysis | B | 6.12 | pIC50 | 750 | nM | IC50 | Bioorg Med Chem (2011) 19: 3242-3248 [PMID:21524587] |
ChEMBL | Inhibition of COX2 | B | 6.12 | pIC50 | 750 | nM | IC50 | J Med Chem (2012) 55: 2287-2300 [PMID:22263894] |
ChEMBL | Inhibitory activity against recombinant human Prostaglandin G/H synthase 2 | B | 6.14 | pIC50 | 730 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1201-1203 [PMID:14980665] |
ChEMBL | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production | B | 6.15 | pIC50 | 700 | nM | IC50 | J Med Chem (2007) 50: 6367-6382 [PMID:17994684] |
ChEMBL | Inhibition of COX2 | B | 6.17 | pIC50 | 670 | nM | IC50 | Eur J Med Chem (2010) 45: 4058-4064 [PMID:20576329] |
ChEMBL | In vitro percent inhibition of Prostaglandin G/H synthase 2 (COX-2) in human whole blood was determined | B | 6.19 | pIC50 | 640 | nM | IC50 | J Med Chem (2003) 46: 3463-3475 [PMID:12877584] |
ChEMBL | Inhibitory effect on Prostaglandin G/H synthase 2 activity was evaluated in human whole blood as LPS-induced PGE-2 generation | F | 6.2 | pIC50 | 630 | nM | IC50 | J Med Chem (2002) 45: 1402-1411 [PMID:11906281] |
ChEMBL | Inhibition of COX2-mediated PGH2 production by enzyme immunoassay | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem (2009) 17: 5044-5053 [PMID:19540763] |
ChEMBL | Inhibition activity against recombinant human Prostaglandin G/H synthase 2 | B | 6.25 | pIC50 | 560 | nM | IC50 | J Med Chem (1997) 40: 819-824 [PMID:9057869] |
ChEMBL | Inhibition of human recombinant COX-2 by EIA method | B | 6.29 | pIC50 | 510 | nM | IC50 | Eur J Med Chem (2019) 183: 111693-111693 [PMID:31539778] |
ChEMBL | Inhibition of Prostaglandin G/H synthase 2 in human whole blood (HWB) assay | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1715-1720 [PMID:10397507] |
ChEMBL | Inhibitory potency against PGE-2 production in the human whole blood (HWB COX-2) assay | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3187-3192 [PMID:10576685] |
ChEMBL | In vitro inhibitory potency against human COX-2 (HWB COX-2) by whole blood assay | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684] |
ChEMBL | In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 2 | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1773-1778 [PMID:10406640] |
ChEMBL | Inhibition of Prostaglandin G/H synthase 2 was measured by the inhibition of PGE-2 produced by lipopolysaccharide-challenged HWB | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2777-2782 [PMID:9873621] |
ChEMBL | Inhibition of COX2 in human whole blood assessed as inhibition of 12-hydroxyheptadecatrienoic acid production by HPLC method | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem (2010) 18: 3910-3924 [PMID:20451397] |
ChEMBL | Inhibition of COX2 in human whole blood | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem (2010) 18: 3910-3924 [PMID:20451397] |
ChEMBL | Inhibition of COX2 in human whole blood assessed as inhibition of LPS-induced PGE2 synthesis up to 24 hrs by radioimmunoassay | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 5031-5034 [PMID:22749420] |
ChEMBL | Inhibition of human recombinant COX2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem (2020) 28: 115403-115403 [PMID:32127262] |
ChEMBL | Inhibition of recombinant human COX2 assessed as reduction in PGF2alpha production using arachidonic acid as substrate by colorimetric method | B | 6.31 | pIC50 | 490 | nM | IC50 | Eur J Med Chem (2018) 144: 635-650 [PMID:29289887] |
ChEMBL | Inhibition of human recombinant COX2 by colorimetric analysis | B | 6.31 | pIC50 | 490 | nM | IC50 | Eur J Med Chem (2020) 200: 112439-112439 [PMID:32485532] |
ChEMBL | Inhibition of human recombinant COX2 catalytic activity using arachidonic acid as substrate pre-incubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA method | B | 6.31 | pIC50 | 490 | nM | IC50 | Eur J Med Chem (2019) 167: 562-582 [PMID:30818268] |
ChEMBL | Inhibition of human recombinant COX2 assessed as reduction in PGH2 formation by measuring PGF2alpha by colorimetric assay | B | 6.31 | pIC50 | 490 | nM | IC50 | Bioorg Med Chem (2017) 25: 5637-5651 [PMID:28916158] |
ChEMBL | In vivo ability to inhibit Prostaglandin G/H synthase 2 in human whole blood assay | B | 6.34 | pIC50 | 460 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 57-62 |
ChEMBL | Inhibitory potency against cyclooxygenase-2 in human whole blood assay | B | 6.36 | pIC50 | 440 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1201-1203 [PMID:14980665] |
ChEMBL | Biochemical index for Prostaglandin G/H synthase 2 measured as, PGE-2 levels in lipopolysaccharide (LPS)-challenged human whole blood | B | 6.39 | pIC50 | 410 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 1745-1748 [PMID:10937738] |
ChEMBL | Inhibition of recombinant human COX-2 preincubated for 15 mins by fluorescence analysis | B | 6.39 | pIC50 | 410 | nM | IC50 | ACS Med Chem Lett (2015) 6: 1086-1090 [PMID:26487917] |
ChEMBL | Inhibition of Prostaglandin G/H synthase 2 in human whole blood | B | 6.4 | pIC50 | 400 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2207-2212 [PMID:10465547] |
ChEMBL | Inhibitory activity against prostaglandin G/H synthase 2 | B | 6.66 | pIC50 | 220 | nM | IC50 | J Med Chem (2000) 43: 214-223 [PMID:10649977] |
ChEMBL | Inhibition of Prostaglandin G/H synthase 2 in CHO whole cell assay | B | 6.7 | pIC50 | <200 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1715-1720 [PMID:10397507] |
ChEMBL | Inhibition of wild type human COX2 expressed in insect cells using [1-14C]-arachidonic acid as substrate incubated for 17 mins at 25 degC followed by 3 mins at 37 degC prior to substrate addition measured after 30 secs by thin layer chromatographic analysis | B | 6.74 | pIC50 | 180 | nM | IC50 | ACS Med Chem Lett (2013) 4: 486-490 [PMID:23687559] |
ChEMBL | Inhibition of human recombinant COX-2 using arachidonic acid as substrate by fluorescence assay | B | 7.09 | pIC50 | 82 | nM | IC50 | Eur J Med Chem (2021) 224: 113682-113682 [PMID:34245948] |
ChEMBL | Inhibition of human COX2 assessed as reduction in PGF2alpha production using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition by ELISA | B | 7.17 | pIC50 | 67.72 | nM | IC50 | Eur J Med Chem (2019) 171: 25-37 [PMID:30904755] |
ChEMBL | Inhibition of PGE-2 production by arachidonic acid-stimulated CHO cells expressing human Prostaglandin G/H synthase 2 | B | 7.31 | pIC50 | 49 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 2677-2682 |
ChEMBL | Inhibition of human recombinant COX2 expressed in insect cells using arachidonic acid as substrate incubated for 1 min prior to substrate addition measured for 25 secs by TMPD-based chromogenic assay | B | 7.32 | pIC50 | 48 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6745-6749 [PMID:23010270] |
ChEMBL | Inhibition of COX2 | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3271-3274 [PMID:19427206] |
ChEMBL | Inhibition of COX2 assessed as LPS-stimulated PGE2 production in human whole blood leukocyte | F | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4440-4443 [PMID:16814546] |
ChEMBL | In vitro inhibitory activity against human whole cells (CHO) Prostaglandin G/H synthase 2 | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1773-1778 [PMID:10406640] |
ChEMBL | Inhibitory concentration against human recombinant Prostaglandin G/H synthase 2 cloned and expressed in baculovirus (Sf9) | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 1325-1328 [PMID:11392547] |
ChEMBL | In vitro inhibition of PGE-2 produced by arachidonic acid-stimulated CHO cells stably expressing human Prostaglandin G/H synthase 2 | B | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2777-2782 [PMID:9873621] |
ChEMBL | In vitro inhibition of the production of PGE-2 in arachidonic acid stimulated chinese hamster ovary (CHO) cells transfected with human cyclooxygenase-2 | B | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 47-52 |
ChEMBL | Inhibition of PGE-2 production in CHO cells expressing human COX-2. | B | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3187-3192 [PMID:10576685] |
ChEMBL | Tested in vitro for the ability to inhibit Prostaglandin G/H synthase 2 in chinese hamster ovary (CHO) cells | B | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 57-62 |
ChEMBL | In vitro inhibitory potency against human COX-2 in stably transfected chinese hamster ovary (CHO) cells | B | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684] |
ChEMBL | Inhibition of human recombinant COX-2 assessed as residual activity by measuring formation of 12-HHT from arachidonic acid by HPLC analysis | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2011) 19: 5372-5382 [PMID:21873070] |
ChEMBL | Inhibition of COX2 | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2007) 50: 1425-1441 [PMID:17341061] |
ChEMBL | Inhibition of human recombinant COX2 after 5 mins | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2010) 53: 4691-4700 [PMID:20503989] |
ChEMBL | In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (COX-2) in 143982 cells | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2003) 46: 3463-3475 [PMID:12877584] |
ChEMBL | Inhibition of Prostaglandin G/H synthase 2 in 143.98.2 from human osteosarcoma cells | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2001) 44: 350-361 [PMID:11462976] |
ChEMBL | Inhibition of PGE-2 generation in LPS-stimulated human monocytes (Prostaglandin G/H synthase 2 cell assay) | F | 8.23 | pIC50 | 5.9 | nM | IC50 | J Med Chem (2002) 45: 1402-1411 [PMID:11906281] |
Cyclooxygenase-2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4102] [UniProtKB: P79208] | ||||||||
ChEMBL | Competitive inhibition of ovine COX2 using arachidonic acid substrate by Ellman's spectrophotometric assay based Lineweaver-Burk double reciprocal plot | B | 5.01 | pKi | 9860 | nM | Ki | Eur J Med Chem (2015) 101: 81-95 [PMID:26117820] |
ChEMBL | Inhibition of ovine COX2 using arachidonic acid as substrate preincubated for 10 mins before substrate addition measured after 5 mins by EIA | B | 4.52 | pIC50 | >30000 | nM | IC50 | Eur J Med Chem (2014) 80: 47-56 [PMID:24763362] |
ChEMBL | Inhibition of ovine COX2 using arachidonic acid as substrate assessed as production of PGF2alpha preincubated for 10 mins followed by substrate addition measured after 2 mins by EIA in presence of stannous chloride | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem (2013) 21: 4581-4590 [PMID:23769654] |
ChEMBL | Inhibition of ovine COX2 by colorimetric assay | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2012) 55: 8152-8163 [PMID:22916727] |
ChEMBL | Inhibition of ovine COX2 by colorimetric assay | B | 4.74 | pIC50 | 18000 | nM | IC50 | J Med Chem (2012) 55: 8152-8163 [PMID:22916727] |
ChEMBL | Inhibition of ovine COX-2 using arachidonic acid after 5 mins by colorimetric method | B | 4.93 | pIC50 | 11800 | nM | IC50 | Bioorg Med Chem (2015) 23: 6807-6814 [PMID:26455657] |
ChEMBL | Inhibition of ovine COX-2 assessed as appearance of oxidized TMPD level by EIA method | B | 4.94 | pIC50 | 11360 | nM | IC50 | Eur J Med Chem (2016) 123: 803-813 [PMID:27541263] |
ChEMBL | Inhibition of ovine COX2 after 5 mins by microplate reader assay | B | 5 | pIC50 | 10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 121-124 [PMID:21144750] |
ChEMBL | Inhibition of ovine COX2 | B | 5.11 | pIC50 | 7700 | nM | IC50 | Bioorg Med Chem (2007) 15: 1014-1021 [PMID:17079150] |
ChEMBL | Inhibition of ovine COX2 by enzyme immuno assay | B | 5.24 | pIC50 | 5700 | nM | IC50 | Bioorg Med Chem (2007) 15: 4767-4774 [PMID:17509888] |
ChEMBL | Inhibition of ovine COX2 by enzyme immunoassay | B | 5.24 | pIC50 | 5700 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3014-3018 [PMID:19419861] |
ChEMBL | Inhibition of ovine COX2 by enzyme immunoassay | B | 5.24 | pIC50 | 5700 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 5776-5780 [PMID:20727750] |
ChEMBL | In vitro inhibitory concentration against COX-2 enzyme | B | 5.24 | pIC50 | 5700 | nM | IC50 | J Med Chem (2005) 48: 4061-4067 [PMID:15943479] |
ChEMBL | Inhibition of ovine COX2 by peroxidase activity-based colorimetric assay | B | 5.38 | pIC50 | 4200 | nM | IC50 | Eur J Med Chem (2014) 74: 606-618 [PMID:24531199] |
ChEMBL | Inhibition of ovine COX2 by oxidized TMPD detection based colorimetric assay | B | 5.41 | pIC50 | 3930 | nM | IC50 | Eur J Med Chem (2015) 101: 81-95 [PMID:26117820] |
ChEMBL | Inhibition of ovine COX2 by colorimetric assay | B | 5.44 | pIC50 | 3670 | nM | IC50 | Eur J Med Chem (2019) 162: 435-447 [PMID:30469039] |
ChEMBL | Inhibition of ovine COX2 | B | 5.51 | pIC50 | 3100 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5324-5329 [PMID:25444084] |
ChEMBL | Inhibitory activity against Prostaglandin G/H synthase 2 obtained from sheep placenta | B | 5.62 | pIC50 | 2400 | nM | IC50 | J Med Chem (1998) 41: 420-427 [PMID:9484493] |
ChEMBL | Inhibition of ovine COX2 assessed as reduction in PGH2 production by enzyme immunoassay | B | 6.05 | pIC50 | 900 | nM | IC50 | Bioorg Med Chem (2018) 26: 4113-4126 [PMID:29980364] |
ChEMBL | Inhibition of ovine COX2 | B | 6.12 | pIC50 | 750 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 85-89 [PMID:18061444] |
ChEMBL | Inhibition of sheep COX2 by enzyme immunoassay | B | 6.27 | pIC50 | 537 | nM | IC50 | Bioorg Med Chem (2010) 18: 6367-6376 [PMID:20692174] |
ChEMBL | Inhibition of ovine COX2 by enzyme immunoassay | B | 6.27 | pIC50 | 537 | nM | IC50 | Eur J Med Chem (2009) 44: 1830-1837 [PMID:19084295] |
ChEMBL | Inhibition of ovine COX -2 by colorimetric inhibitor screening assay kit method | B | 6.31 | pIC50 | 490 | nM | IC50 | Eur J Med Chem (2019) 167: 161-186 [PMID:30771604] |
ChEMBL | Inhibition of ovine COX2 | B | 6.32 | pIC50 | 480 | nM | IC50 | Eur J Med Chem (2013) 65: 51-59 [PMID:23693150] |
ChEMBL | Inhibition of ovine COX2 | B | 6.47 | pIC50 | 340 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4440-4443 [PMID:16814546] |
COX-2 /Cyclooxygenase-2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4321] [GtoPdb: 1376] [UniProtKB: Q05769] | ||||||||
ChEMBL | Inhibition of COX2-mediated PGE2 production in LPS-stimulated mouse RAW 264.7 cells after 24 hrs by ELISA | B | 4.81 | pIC50 | 15370 | nM | IC50 | J Med Chem (2011) 54: 2060-2068 [PMID:21381754] |
ChEMBL | Inhibition of mouse COX2 | B | 6.12 | pIC50 | 750 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 1787-1791 [PMID:20129783] |
ChEMBL | Inhibition concentration against Prostaglandin G/H synthase 2 | B | 6.68 | pIC50 | 210 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1315-1318 [PMID:11965379] |
ChEMBL | Inhibition of wild type mouse COX2 by discontinuous radioactive TLC assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2013) 56: 2429-2446 [PMID:23432095] |
ChEMBL | Inhibition of wild type mouse COX2 expressed in insect cells using [1-14C]-arachidonic acid as substrate incubated for 17 mins at 25 degC followed by 3 mins at 37 degC prior to substrate addition measured after 30 secs by thin layer chromatographic analysis | B | 6.9 | pIC50 | 127 | nM | IC50 | ACS Med Chem Lett (2013) 4: 486-490 [PMID:23687559] |
ChEMBL | Inhibition of mouse COX2 | B | 7.17 | pIC50 | 68 | nM | IC50 | Bioorg Med Chem (2010) 18: 2204-2218 [PMID:20188577] |
ChEMBL | In vitro inhibitory activity against Prostaglandin G/H synthase 2 in murine J774 cells | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2005) 48: 3428-3432 [PMID:15857149] |
ChEMBL | IC50 value was determined against Prostaglandin G/H synthase 2 of J7744A.1 cell lines. | B | 8.19 | pIC50 | 6.4 | nM | IC50 | J Med Chem (1999) 42: 1151-1160 [PMID:10197959] |
ChEMBL | IC50 value against Prostaglandin G/H synthase 2 of murine J774A.1 cell line | B | 8.19 | pIC50 | 6.4 | nM | IC50 | J Med Chem (1999) 42: 1161-1169 [PMID:10197960] |
COX-2 /Cyclooxygenase-2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2977] [GtoPdb: 1376] [UniProtKB: P35355] | ||||||||
ChEMBL | In vitro inhibitory concentration against rat Prostaglandin G/H synthase 2 | B | 6.66 | pIC50 | 220 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2687-2690 [PMID:11591502] |
ChEMBL | Inhibition of Prostaglandin G/H synthase 2 | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 725-730 |
ChEMBL | In vitro inhibition of Prostaglandin G/H synthase 2 | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 731-736 |
Cytochrome c oxidase subunit 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6174] [UniProtKB: P00403] | ||||||||
ChEMBL | Inhibition of human COX2 assessed as reduction in PGF2alpha production by ELISA | B | 6.21 | pIC50 | 610 | nM | IC50 | Eur J Med Chem (2017) 139: 936-946 [PMID:28881288] |
ChEMBL | Inhibition of recombinant human COX2 expressed in baculovirus infected Sf21 cells using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by UV-visible spectrophotometric method | B | 7.15 | pIC50 | 70 | nM | IC50 | Eur J Med Chem (2020) 186: 111863-111863 [PMID:31740050] |
cPLA2-4C/Cytosolic phospholipase A2 gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4834] [GtoPdb: 1426] [UniProtKB: Q9UP65] | ||||||||
ChEMBL | Concentration required to inhibit human Cytosolic phospholipase A2 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 587-590 [PMID:11229777] |
Dehydrogenase/reductase SDR family member 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5974] [UniProtKB: Q9BPW9] | ||||||||
ChEMBL | Inhibition of 3alphaHSD | B | 4.85 | pIC50 | 14000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2558-2560 [PMID:17346963] |
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
ChEMBL | Inhibition of EGFR (unknown origin) using tyrosine 4 as substrate by fluorescence analysis | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2015) 6: 1086-1090 [PMID:26487917] |
epoxide hydrolase 2/Epoxide hydratase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913] | ||||||||
ChEMBL | Inhibition of human recombinant soluble epoxide hydrolase after 10 mins by fluorescent-based assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2011) 54: 3037-3050 [PMID:21434686] |
Glyoxalase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2424] [UniProtKB: Q04760] | ||||||||
ChEMBL | Inhibition of human glyoxalase 1 | B | 4.61 | pKi | 24400 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4243-4247 [PMID:21689932] |
ChEMBL | Inhibition of human recombinant His-tagged glyoxalase 1 expressed in Escherichia coli BL21 (DE3) preincubated for 20 mins by Dixon plot analysis | B | 4.62 | pKi | 24000 | nM | Ki | Bioorg Med Chem (2011) 19: 1189-1196 [PMID:21237663] |
ChEMBL | Inhibition of glyoxalase 1 | B | 4.74 | pKi | 18100 | nM | Ki | Bioorg Med Chem (2011) 19: 1189-1196 [PMID:21237663] |
DP2 receptor/G protein-coupled receptor 44 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5071] [GtoPdb: 339] [UniProtKB: Q9Y5Y4] | ||||||||
ChEMBL | Binding affinity towards human CRTH2 receptor expressed in CHO cells; range 25 nM to 8 uM | B | 5.1 | pKi | 8000 | nM | Ki | J Med Chem (2005) 48: 6174-6177 [PMID:16190744] |
ChEMBL | In vitro binding affinity (agonistic) towards human CRTH2 receptor expressed in CHO cells; range 15 to 25 nM | B | 7.3 | pKi | 50 | nM | Ki | J Med Chem (2005) 48: 6174-6177 [PMID:16190744] |
GtoPdb | - | - | 7.7 | pKi | - | - | - |
Br J Pharmacol (2002) 137: 1163-72 [PMID:12466225]; Eur J Pharmacol (2005) 524: 30-7 [PMID:16256979] |
ChEMBL | Partial antagonist activity at CRTH2 in human eosinophils assessed as inhibition of PGD2-induced shape change by FACS analysis | F | 6.41 | pEC50 | 389 | nM | EC50 | J Med Chem (2012) 55: 2915-2931 [PMID:22224640] |
DP2 receptor in Mouse [GtoPdb: 339] [UniProtKB: Q9Z2J6] | ||||||||
GtoPdb | - | - | 6 | pKi | - | - | - |
J Pharmacol Exp Ther (2003) 306: 463-70 [PMID:12721327]; J Biol Chem (2005) 280: 32442-32451 [PMID:16030019] |
Interleukin-8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2157] [UniProtKB: P10145] | ||||||||
ChEMBL | Inhibition of CXCL8-induced chemotaxis in human polymorphonuclear leukocyte pretreated for 15 mins measured after 4 hrs by cell migration assay | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4026-4030 [PMID:19560921] |
ABCC1/Multidrug resistance-associated protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527] | ||||||||
ChEMBL | Inhibition of MRP1 expressed in human 2008 cells assessed as calcein AM accumulation by cell based assay | B | 4.9 | pIC50 | 12600 | nM | IC50 | Bioorg Med Chem (2011) 19: 2090-2102 [PMID:21354800] |
ChEMBL | Inhibition of human MRP1 in human 2008 cells | B | 4.92 | pIC50 | 12000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4761-4763 [PMID:18707884] |
Nicotinate phosphoribosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523354] [UniProtKB: Q6XQN6] | ||||||||
ChEMBL | Inhibition of NAPRT (unknown origin) | B | 9.82 | pKi | 0.15 | nM | Ki | WO-2017162840-A1. Sensitization of cancer cells to nampt inhibitors by nicotinic acid phosphoribosyltransferase neutralization (null) |
Inducible NOS/Nitric oxide synthase, inducible in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3464] [GtoPdb: 1250] [UniProtKB: P29477] | ||||||||
ChEMBL | Inhibition of iNOS in LPS-stimulated mouse RAW 264.7 cells after 2 hrs by fluorescence plate reader analysis | B | 4.31 | pIC50 | 48890 | nM | IC50 | J Med Chem (2011) 54: 2060-2068 [PMID:21381754] |
ChEMBL | Inhibition of iNOS in LPS-stimulated mouse RAW 264.7 cells preincubated for 1 hr followed by LPS-stimulation and measured after 6 hrs by fluorescence based assay | B | 4.6 | pIC50 | 24890 | nM | IC50 | J Med Chem (2019) 62: 4013-4031 [PMID:30925056] |
ChEMBL | Inhibition of iNOS-mediated nitric oxide production in LPS-stimulated mouse RAW 264.7 cells treated 2 hrs before LPS challenge measured after 18 hrs by Griess reaction method | B | 4.63 | pIC50 | 23470 | nM | IC50 | J Med Chem (2011) 54: 2060-2068 [PMID:21381754] |
ChEMBL | Inhibition of iNOS in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production for 2 hrs by DAF-FMDA dye based fluorometric assay | B | 4.7 | pIC50 | 20000 | nM | IC50 | Eur J Med Chem (2012) 54: 272-280 [PMID:22633833] |
ChEMBL | Inhibition of iNOS in LPS-stimulated mouse RAW264.7 cells using L-Arginine substrate incubated for 2 hrs by fluorescence spectrometry | B | 5.35 | pIC50 | 4500 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 2429-2433 [PMID:25881822] |
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
GtoPdb | - | - | 7.38 | pKd | - | - | - |
Eur J Pharmacol (2001) 417: 77-89 [PMID:11301062]; J Biol Chem (1997) 272: 3406-10 [PMID:9013583] |
ChEMBL | Activation of GAL4 fused human PPARgamma ligand binding domain transfected in african green monkey CV1 cells by CAT reporter assay | B | 4.3 | pEC50 | 50000 | nM | EC50 | J Nat Prod (2006) 69: 547-552 [PMID:16643023] |
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
ChEMBL | Inhibition of human recombinant P-glycoprotein after 40 mins by Pgp-Glo assay | B | 4.49 | pIC50 | 32000 | nM | IC50 | J Med Chem (2012) 55: 8152-8163 [PMID:22916727] |
ChEMBL | Inhibition of human recombinant P-glycoprotein after 40 mins by Pgp-Glo assay | B | 4.55 | pIC50 | 28000 | nM | IC50 | J Med Chem (2012) 55: 8152-8163 [PMID:22916727] |
mPGES1/Prostaglandin E synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684] | ||||||||
ChEMBL | Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as inhibition of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis | B | 4.39 | pIC50 | 40600 | nM | IC50 | J Med Chem (2012) 55: 8958-8962 [PMID:22992107] |
L-PGDS/Prostaglandin-H2 D-isomerase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4334] [GtoPdb: 1380] [UniProtKB: O09114] | ||||||||
ChEMBL | Concentration required to inhibit 50% activity of prostaglandin synthetase was determined in vitro in mouse brain microsomes | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (1991) 34: 1099-1110 [PMID:1900533] |
DP1 receptor/Prostanoid DP receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3933] [GtoPdb: 338] [UniProtKB: P70263] | ||||||||
ChEMBL | Binding affinity for mouse Prostanoid DP receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4557-4562 [PMID:15357992] |
ChEMBL | Displacement of [3H]-PGD2 from mouse DP receptor expressed in CHO cells after 20 mins by liquid scintillation counting | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2011) 19: 4574-4588 [PMID:21737285] |
ChEMBL | Inhibition of mouse Prostanoid DP receptor | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4557-4562 [PMID:15357992] |
EP1 receptor/Prostanoid EP1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2181] [GtoPdb: 340] [UniProtKB: P35375] | ||||||||
ChEMBL | Binding affinity for mouse Prostanoid EP1 receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4557-4562 [PMID:15357992] |
ChEMBL | Displacement of [3H]-PGE2 from mouse EP1 receptor expressed in CHO cells after 20 mins by liquid scintillation counting | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2011) 19: 4574-4588 [PMID:21737285] |
EP2 receptor/Prostanoid EP2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2488] [GtoPdb: 341] [UniProtKB: Q62053] | ||||||||
ChEMBL | Binding affinity for mouse Prostanoid EP2 receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4557-4562 [PMID:15357992] |
ChEMBL | Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2011) 19: 4574-4588 [PMID:21737285] |
EP3 receptor/Prostanoid EP3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4336] [GtoPdb: 342] [UniProtKB: P30557] | ||||||||
ChEMBL | Binding affinity for mouse Prostanoid EP3 receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4557-4562 [PMID:15357992] |
ChEMBL | Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2011) 19: 4574-4588 [PMID:21737285] |
EP4 receptor/Prostanoid EP4 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2489] [GtoPdb: 343] [UniProtKB: P32240] | ||||||||
ChEMBL | Binding affinity for mouse Prostanoid EP4 receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4557-4562 [PMID:15357992] |
ChEMBL | Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counting | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2011) 19: 4574-4588 [PMID:21737285] |
Organic anion transporter 1/Solute carrier family 22 member 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641347] [GtoPdb: 1025] [UniProtKB: Q4U2R8] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells | F | 5.52 | pIC50 | 3000 | nM | IC50 | J Pharmacol Exp Ther (2000) 295: 10-15 [PMID:10991954] |
Organic anion transporter 1/Solute carrier family 22 member 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of PAH uptake in Xenopus laevis oocytes | F | 5 | pKi | 10000 | nM | Ki | Mol Pharmacol (1999) 55: 847-854 [PMID:10220563] |
ChEMBL | TP_TRANSPORTER: inhibition of MTX uptake in Xenopus laevis oocytes | F | 5.38 | pKi | 4200 | nM | Ki | Eur J Pharmacol (2000) 409: 31-36 [PMID:11099697] |
Organic anion transporter 3/Solute carrier family 22 member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641348] [GtoPdb: 1027] [UniProtKB: Q8TCC7] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of MTX uptake in OAT3-expressing S2 cells | F | 5.23 | pKi | 5950 | nM | Ki | J Pharmacol Exp Ther (2002) 302: 666-671 [PMID:12130730] |
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557] | ||||||||
ChEMBL | Inhibitory activity against thromboxane A2 synthetase | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1985) 28: 1427-1432 [PMID:3930740] |
ChEMBL | Inhibitory activity to inhibit Inophore-induced arachidonic acid metabolism (inhibition of TXB2 formation) in rat | F | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (1989) 32: 1842-1860 [PMID:2547071] |
GPR17/Uracil nucleotide/cysteinyl leukotriene receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075162] [GtoPdb: 88] [UniProtKB: Q13304] | ||||||||
ChEMBL | Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay | F | 4.54 | pIC50 | 28800 | nM | IC50 | J Med Chem (2018) 61: 8136-8154 [PMID:30048589] |
ChEMBL | Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of ATP-induced intracellular calcium influx preincubated for 20 mins followed by ATP addition measured at 0.4 secs interval for 60 times by Oregon Green BAPTA-1/AM dye-based fluorescence assay | F | 4.54 | pIC50 | 28800 | nM | IC50 | Eur J Med Chem (2020) 186: 111789-111789 [PMID:31727469] |
Proton-coupled folate transporter in Human [GtoPdb: 1213] [UniProtKB: Q96NT5] | ||||||||
GtoPdb | - | - | 3.7 | pIC50 | 200000 | nM | IC50 | Cell (2006) 127: 917-28 [PMID:17129779] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]