indomethacin [Ligand Id: 1909] activity data from GtoPdb and ChEMBL

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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)
  • Aldo-keto reductase family 1 member C1 in Human [ChEMBL: CHEMBL5905] [UniProtKB: Q04828]
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  • Aldo-keto reductase family 1 member C2 in Human [ChEMBL: CHEMBL5847] [UniProtKB: P52895]
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  • AKR1C3/Aldo-keto-reductase family 1 member C3 in Human [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
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  • Aldo-keto reductase family 1 member C4 in Human [ChEMBL: CHEMBL4999] [UniProtKB: P17516]
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  • aldo-keto reductase family 1 member B/Aldose reductase in Human [ChEMBL: CHEMBL1900] [GtoPdb: 2768] [UniProtKB: P15121]
  • Aldose reductase in Bovine [ChEMBL: CHEMBL3081] [UniProtKB: P16116]
  • aldo-keto reductase family 1 member B/Aldose reductase in Rat [ChEMBL: CHEMBL2622] [GtoPdb: 2768] [UniProtKB: P07943]
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  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
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  • 5-LOX/Arachidonate 5-lipoxygenase in Human [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
  • 5-LOX/Arachidonate 5-lipoxygenase in Rat [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
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  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
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  • Cytochrome c oxidase subunit 2 in Human [ChEMBL: CHEMBL6174] [UniProtKB: P00403]
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  • cPLA2-4C/Cytosolic phospholipase A2 gamma in Human [ChEMBL: CHEMBL4834] [GtoPdb: 1426] [UniProtKB: Q9UP65]
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  • Dehydrogenase/reductase SDR family member 9 in Human [ChEMBL: CHEMBL5974] [UniProtKB: Q9BPW9]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • epoxide hydrolase 2/Epoxide hydratase in Human [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
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  • DP2 receptor/G protein-coupled receptor 44 in Human [ChEMBL: CHEMBL5071] [GtoPdb: 339] [UniProtKB: Q9Y5Y4]
  • DP2 receptor in Mouse [GtoPdb: 339] [UniProtKB: Q9Z2J6]
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  • ABCC1/Multidrug resistance-associated protein 1 in Human [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527]
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  • Inducible NOS/Nitric oxide synthase, inducible in Mouse [ChEMBL: CHEMBL3464] [GtoPdb: 1250] [UniProtKB: P29477]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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  • L-PGDS/Prostaglandin-H2 D-isomerase in Mouse [ChEMBL: CHEMBL4334] [GtoPdb: 1380] [UniProtKB: O09114]
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  • DP1 receptor/Prostanoid DP receptor in Mouse [ChEMBL: CHEMBL3933] [GtoPdb: 338] [UniProtKB: P70263]
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  • EP1 receptor/Prostanoid EP1 receptor in Mouse [ChEMBL: CHEMBL2181] [GtoPdb: 340] [UniProtKB: P35375]
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  • EP2 receptor/Prostanoid EP2 receptor in Mouse [ChEMBL: CHEMBL2488] [GtoPdb: 341] [UniProtKB: Q62053]
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  • EP3 receptor/Prostanoid EP3 receptor in Mouse [ChEMBL: CHEMBL4336] [GtoPdb: 342] [UniProtKB: P30557]
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  • EP4 receptor/Prostanoid EP4 receptor in Mouse [ChEMBL: CHEMBL2489] [GtoPdb: 343] [UniProtKB: P32240]
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  • Organic anion transporter 1/Solute carrier family 22 member 6 in Human [ChEMBL: CHEMBL1641347] [GtoPdb: 1025] [UniProtKB: Q4U2R8]
  • Organic anion transporter 1/Solute carrier family 22 member 6 in Rat [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956]
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  • Organic anion transporter 3/Solute carrier family 22 member 8 in Human [ChEMBL: CHEMBL1641348] [GtoPdb: 1027] [UniProtKB: Q8TCC7]
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  • GPR17/Uracil nucleotide/cysteinyl leukotriene receptor in Human [ChEMBL: CHEMBL1075162] [GtoPdb: 88] [UniProtKB: Q13304]
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  • Proton-coupled folate transporter in Human [GtoPdb: 1213] [UniProtKB: Q96NT5]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]