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

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ChEMBL ligand: CHEMBL6 (Imbrilon, Ledmecin, Rimacid, Indomethacin, Indolar, Indocin, Indocid Ret, Indolar SR, Flexin-75 Continus, Indocin SR, Indoptol, Indoflex, Slo-Indo, Pardelprin MR, Indoderm, Maximet Sr, Tivorbex, Indotard MR 75, Indomax-25, Flexin-50 Continus, Rheumacin LA, Artracin, Indo-Paed, Flexin-25 Continus, Indometacin, Artracin Sr, Berlind 75 Ret, Indometacin Farnesil, NSC-77541, Indomod, Indo-Lemmon, Indomax-75 Sr, Mobilan, Indocid-R)
  • Aldo-keto reductase family 1 member C1 in Human [ChEMBL: CHEMBL5905] [UniProtKB: Q04828]
  • This target only has 1 pki data point
1 CHEMBL6_lig_chart_1 Aldo-keto reductase family 1 member C1 Human
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  • Aldo-keto reductase family 1 member C2 in Human [ChEMBL: CHEMBL5847] [UniProtKB: P52895]
  • This target only has 1 pki data point
2 CHEMBL6_lig_chart_2 Aldo-keto reductase family 1 member C2 Human
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  • AKR1C3/Aldo-keto-reductase family 1 member C3 in Human [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
  • This target only has 1 pki data point
3 CHEMBL6_lig_chart_3 Aldo-keto-reductase family 1 member C3 Human
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  • Aldo-keto reductase family 1 member C4 in Human [ChEMBL: CHEMBL4999] [UniProtKB: P17516]
  • This target only has 0 pki data point
4 CHEMBL6_lig_chart_4 Aldo-keto reductase family 1 member C4 Human
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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]
  • This target only has 0 pki data point
5 CHEMBL6_lig_chart_5 Aldose reductase HumanBovineRat
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  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
  • This target only has 0 pki data point
6 CHEMBL6_lig_chart_6 Androgen Receptor Human
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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]
  • This target only has 0 pki data point
7 CHEMBL6_lig_chart_7 Arachidonate 5-lipoxygenase HumanRat
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  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
  • This target only has 1 pki data point
8 CHEMBL6_lig_chart_8 Cannabinoid CB1 receptor Human
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
  • This target only has 1 pki data point
9 CHEMBL6_lig_chart_9 Cannabinoid CB2 receptor Human
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10 CHEMBL6_lig_chart_10 Cyclooxygenase-1 HumanBovineSheepMouseRat
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11 CHEMBL6_lig_chart_11 Cyclooxygenase-2 HumanSheepMouseRat
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  • Cytochrome c oxidase subunit 2 in Human [ChEMBL: CHEMBL6174] [UniProtKB: P00403]
  • This target only has 0 pki data point
12 CHEMBL6_lig_chart_12 Cytochrome c oxidase subunit 2 Human
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  • cPLA2-4C/Cytosolic phospholipase A2 gamma in Human [ChEMBL: CHEMBL4834] [GtoPdb: 1426] [UniProtKB: Q9UP65]
  • This target only has 0 pki data point
13 CHEMBL6_lig_chart_13 Cytosolic phospholipase A2 gamma Human
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  • Dehydrogenase/reductase SDR family member 9 in Human [ChEMBL: CHEMBL5974] [UniProtKB: Q9BPW9]
  • This target only has 0 pki data point
14 CHEMBL6_lig_chart_14 Dehydrogenase/reductase SDR family member 9 Human
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
  • This target only has 0 pki data point
15 CHEMBL6_lig_chart_15 Epidermal growth factor receptor erbB1 Human
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  • epoxide hydrolase 2/Epoxide hydratase in Human [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
  • This target only has 0 pki data point
16 CHEMBL6_lig_chart_16 Epoxide hydratase Human
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17 CHEMBL6_lig_chart_17 Glyoxalase I Human
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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]
18 CHEMBL6_lig_chart_18 G protein-coupled receptor 44 HumanMouse
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  • Interleukin-8 in Human [ChEMBL: CHEMBL2157] [UniProtKB: P10145]
  • This target only has 0 pki data point
19 CHEMBL6_lig_chart_19 Interleukin-8 Human
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  • ABCC1/Multidrug resistance-associated protein 1 in Human [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527]
  • This target only has 0 pki data point
20 CHEMBL6_lig_chart_20 Multidrug resistance-associated protein 1 Human
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  • Inducible NOS/Nitric oxide synthase, inducible in Mouse [ChEMBL: CHEMBL3464] [GtoPdb: 1250] [UniProtKB: P29477]
  • This target only has 0 pki data point
21 CHEMBL6_lig_chart_21 Nitric oxide synthase, inducible Mouse
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
  • This target only has 0 pki data point
22 CHEMBL6_lig_chart_22 Peroxisome proliferator-activated receptor gamma Human
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  • ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
  • This target only has 0 pki data point
23 CHEMBL6_lig_chart_23 P-glycoprotein 1 Human
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  • mPGES1/Prostaglandin E synthase in Human [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684]
  • This target only has 0 pki data point
24 CHEMBL6_lig_chart_24 Prostaglandin E synthase Human
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  • L-PGDS/Prostaglandin-H2 D-isomerase in Mouse [ChEMBL: CHEMBL4334] [GtoPdb: 1380] [UniProtKB: O09114]
  • This target only has 0 pki data point
25 CHEMBL6_lig_chart_25 Prostaglandin-H2 D-isomerase Mouse
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  • DP1 receptor/Prostanoid DP receptor in Mouse [ChEMBL: CHEMBL3933] [GtoPdb: 338] [UniProtKB: P70263]
26 CHEMBL6_lig_chart_26 Prostanoid DP receptor Mouse
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  • EP1 receptor/Prostanoid EP1 receptor in Mouse [ChEMBL: CHEMBL2181] [GtoPdb: 340] [UniProtKB: P35375]
27 CHEMBL6_lig_chart_27 Prostanoid EP1 receptor Mouse
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  • EP2 receptor/Prostanoid EP2 receptor in Mouse [ChEMBL: CHEMBL2488] [GtoPdb: 341] [UniProtKB: Q62053]
28 CHEMBL6_lig_chart_28 Prostanoid EP2 receptor Mouse
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  • EP3 receptor/Prostanoid EP3 receptor in Mouse [ChEMBL: CHEMBL4336] [GtoPdb: 342] [UniProtKB: P30557]
29 CHEMBL6_lig_chart_29 Prostanoid EP3 receptor Mouse
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  • EP4 receptor/Prostanoid EP4 receptor in Mouse [ChEMBL: CHEMBL2489] [GtoPdb: 343] [UniProtKB: P32240]
30 CHEMBL6_lig_chart_30 Prostanoid EP4 receptor Mouse
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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]
31 CHEMBL6_lig_chart_31 Solute carrier family 22 member 6 HumanRat
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  • Organic anion transporter 3/Solute carrier family 22 member 8 in Human [ChEMBL: CHEMBL1641348] [GtoPdb: 1027] [UniProtKB: Q8TCC7]
  • This target only has 1 pki data point
32 CHEMBL6_lig_chart_32 Solute carrier family 22 member 8 Human
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  • CYP5A1/Thromboxane-A synthase in Human [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557]
  • This target only has 0 pki data point
33 CHEMBL6_lig_chart_33 Thromboxane-A synthase Human
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  • GPR17/Uracil nucleotide/cysteinyl leukotriene receptor in Human [ChEMBL: CHEMBL1075162] [GtoPdb: 88] [UniProtKB: Q13304]
  • This target only has 0 pki data point
34 CHEMBL6_lig_chart_34 Uracil nucleotide/cysteinyl leukotriene receptor Human
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  • Proton-coupled folate transporter in Human [GtoPdb: 1213] [UniProtKB: Q96NT5]
  • This target only has 0 pki data point
35 CHEMBL6_lig_chart_35 Proton-coupled folate transporter Human
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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 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 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 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