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, Indometacina, Indometacine, 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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  • xanthine dehydrogenase/Xanthine dehydrogenase in Human [ChEMBL: CHEMBL1929] [GtoPdb: 2646] [UniProtKB: P47989]
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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 AKR1C3 (unknown origin) B 5.13 pIC50 7350 nM IC50 J Med Chem (2021) 64: 1786-1815 [PMID:33569941]
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 (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 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 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-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 B 5.92 pIC50 1200 nM IC50 J Nat Prod (1998) 61: 347-350 [PMID:9544564]
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 COX-1 (unknown origin) using arachidonic acid as substrate and measured by fluorometric assay B 6.33 pIC50 463.1 nM IC50 Eur J Med Chem (2022) 241: 114597-114597 [PMID:35931005]
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 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 Inhibition of COX1 B 6.6 pIC50 250 nM IC50 Bioorg Med Chem Lett (2009) 19: 3271-3274 [PMID:19427206]
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 human recombinant COX-I measured after 50 mins B 6.66 pIC50 220 nM IC50 Eur J Med Chem (2018) 151: 628-685 [PMID:29656203]
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 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 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 Inhibition of COX1 in human whole blood B 6.7 pIC50 200 nM IC50 Bioorg Med Chem (2010) 18: 3910-3924 [PMID:20451397]
ChEMBL Inhibition of COX-1 (unknown origin) at 40 uM relative to control B 6.7 pIC50 200 nM IC50 Eur J Med Chem (2020) 200: 112438-112438 [PMID:32485533]
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 COX-1 (unknown origin) using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 2 mins by ELISA method B 7 pIC50 100 nM IC50 Eur J Med Chem (2023) 250: 115180-115180 [PMID:36796297]
ChEMBL Inhibition of COX1 B 7 pIC50 100 nM IC50 J Med Chem (2008) 51: 2400-2411 [PMID:18363350]
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 Inhibition of COX1 (unknown origin) B 7 pIC50 100 nM IC50 J Med Chem (2021) 64: 1786-1815 [PMID:33569941]
ChEMBL Inhibition of COX1 (unknown origin) B 7 pIC50 100 nM IC50 Med Chem Res (2012) 21: 3491-3498
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 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 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 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 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 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 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 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 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 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 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 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 ACS Med Chem Lett (2011) 2: 353-357 [PMID:24900317]
ChEMBL Inhibition of COX1 B 8 pIC50 10 nM IC50 J Nat Prod (2005) 68: 985-991 [PMID:16038536]
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]
ChEMBL Inhibition of COX1 (unknown origin) B 9.85 pIC50 0.14 nM IC50 RSC Med Chem (2024) 15: 788-808 [PMID:38516587]
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 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 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 COX-1 by EIA method B 6.29 pIC50 510 nM IC50 Eur J Med Chem (2020) 200: 112438-112438 [PMID:32485533]
ChEMBL Inhibition of sheep COX-1 B 6.3 pIC50 500 nM IC50 Eur J Med Chem (2023) 256: 115443-115443 [PMID:37182334]
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 ovine COX-1 B 6.54 pIC50 290 nM IC50 RSC Med Chem (2022) 13: 1150-1196 [PMID:36325400]
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 full-length ovine COX-1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetry B 6.7 pIC50 200 nM IC50 Bioorg Med Chem (2022) 57: 116633-116633 [PMID:35134642]
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 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 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 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 by enzyme immuno assay B 7 pIC50 100 nM IC50 Bioorg Med Chem (2007) 15: 4767-4774 [PMID:17509888]
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 B 7 pIC50 100 nM IC50 J Med Chem (2012) 55: 688-696 [PMID:22148253]
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 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 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 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 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 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 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 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 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 Inhibition of ovine COX1 B 7.2 pIC50 63 nM IC50 Eur J Med Chem (2013) 65: 51-59 [PMID:23693150]
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 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 (2010) 20: 1787-1791 [PMID:20129783]
ChEMBL Inhibition of ovine COX1 B 7.3 pIC50 50 nM IC50 Bioorg Med Chem Lett (2008) 18: 85-89 [PMID:18061444]
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 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 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 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 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 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 after 5 mins B 8.22 pIC50 6 nM IC50 J Med Chem (2010) 53: 4691-4700 [PMID:20503989]
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 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 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 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 COX-2 (unknown origin) at 5 uM by colorimetric method B 4.94 pIC50 11360 nM IC50 Eur J Med Chem (2020) 200: 112438-112438 [PMID:32485533]
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 by enzyme immuno assay B 5.16 pIC50 6900 nM IC50 Bioorg Med Chem Lett (2012) 22: 2154-2159 [PMID:22361134]
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 B 5.21 pIC50 6200 nM IC50 Eur J Med Chem (2020) 200: 112438-112438 [PMID:32485533]
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 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 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]
ChEMBL Inhibition of human recombinant COX-II measured after 50 mins B 5.58 pIC50 2640 nM IC50 Eur J Med Chem (2018) 151: 628-685 [PMID:29656203]
GtoPdb - - 5.58 pIC50 2630 nM IC50 Eur J Med Chem (2017) 141: 306-321 [PMID:29031075]
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 Inhibition of COX-2 (unknown origin) at 0.5 uM by colorimetric assay B 5.58 pIC50 2630 nM IC50 Eur J Med Chem (2020) 200: 112438-112438 [PMID:32485533]
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 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 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 recombinant human COX-2 B 5.79 pIC50 1610 nM IC50 Eur J Med Chem (2023) 256: 115443-115443 [PMID:37182334]
ChEMBL Inhibition of COX-2 (unknown origin) B 5.79 pIC50 1610 nM IC50 Eur J Med Chem (2023) 256: 115443-115443 [PMID:37182334]
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 COX-2 (unknown origin) using arachidonic acid as substrate and measured by fluorometric assay B 5.86 pIC50 1393 nM IC50 Eur J Med Chem (2022) 241: 114597-114597 [PMID:35931005]
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 5.92 pIC50 1200 nM IC50 Bioorg Med Chem Lett (2015) 25: 2931-2936 [PMID:26048794]
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-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 (unknown origin) B 5.93 pIC50 1170 nM IC50 Med Chem Res (2012) 21: 3491-3498
ChEMBL Inhibition of human COX-2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetry B 5.96 pIC50 1100 nM IC50 Bioorg Med Chem (2022) 57: 116633-116633 [PMID:35134642]
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 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 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 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 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 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 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 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 DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) B 6.08 pIC50 840 nM IC50 DrugMatrix in vitro pharmacology data
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 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 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 (unknown origin) B 6.21 pIC50 610 nM IC50 J Med Chem (2021) 64: 1786-1815 [PMID:33569941]
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 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 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 COX-2 (unknown origin) B 6.3 pIC50 500 nM IC50 Eur J Med Chem (2023) 256: 115443-115443 [PMID:37182334]
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 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 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 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 Inhibition of COX2 in human whole blood B 6.3 pIC50 500 nM IC50 Bioorg Med Chem (2010) 18: 3910-3924 [PMID:20451397]
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 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 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 COX-2 (unknown origin) assessed as inhibition at 15 uM B 6.31 pIC50 490 nM IC50 Eur J Med Chem (2020) 200: 112438-112438 [PMID:32485533]
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 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 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 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 COX-2 (unknown origin) B 7.1 pIC50 80 nM IC50 J Med Chem (2022) 65: 13436-13451 [PMID:36170566]
ChEMBL Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 2 mins by ELISA method B 7.1 pIC50 80 nM IC50 Eur J Med Chem (2023) 250: 115180-115180 [PMID:36796297]
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 human COX-2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA B 7.35 pIC50 45 nM IC50 RSC Med Chem (2022) 13: 471-496 [PMID:35685617]
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 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 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 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 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 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 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 Inhibition of human recombinant COX2 after 5 mins B 8 pIC50 10 nM IC50 J Med Chem (2010) 53: 4691-4700 [PMID:20503989]
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 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 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 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]
ChEMBL Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate preincubated for 15 mins followed by substrate addition by colorimetric assay B 9.85 pIC50 0.14 nM IC50 RSC Med Chem (2024) 15: 788-808 [PMID:38516587]
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 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 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 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 COX-2 B 5.44 pIC50 3650 nM IC50 RSC Med Chem (2022) 13: 1150-1196 [PMID:36325400]
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]
ChEMBL Inhibition of ovine COX-2 colorimetric enzyme immunoassay B 7.06 pIC50 87 nM IC50 RSC Med Chem (2022) 13: 471-496 [PMID:35685617]
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 (2017)
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]
xanthine dehydrogenase/Xanthine dehydrogenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1929] [GtoPdb: 2646] [UniProtKB: P47989]
ChEMBL Inhibition of XO (unknown origin) using xanthine as substrate assessed as decrease in uric acid level measured after 3 mins by spectrophotometric analysis B 4.07 pIC50 86000 nM IC50 RSC Med Chem (2023) 14: 2155-2191 [PMID:37974965]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]