ChEMBL ligand: CHEMBL571 (19583RP, Actron, Actron ketoprofen, Alrheumat, Aneol, Axorid, Capisten, Fenoket 200, Hydratropic acid, m-benzoyl-, IDEA-033, Iso-k, Jomethid xl, Ketocid 200, Ketonal, Ketoprofen, Ketorin, Ketotard 200 xl, Ketovail, Ketozip 200 xl, Larafen, Larafen cr, Nexcede, NSC-758144, Orudis, Orudis 100, Orudis kt, Oruvail, Oruvail 100, Oruvail 150, Oruvail 200, Oruvail im, Powergel, R.P. 19,583, R.P. 19583, RP-19583, (rs)-ketoprofen, RU-4733, Sector, Tiloket, Tiloket cr, Valket 200 retard)
COX-1 /Cyclooxygenase-1 in Human [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219] Cyclooxygenase-1 in Sheep [ChEMBL: CHEMBL2949] [UniProtKB: P05979] There should be some charts here, you may need to enable JavaScript!
COX-2 /Cyclooxygenase-2 in Human [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] Cyclooxygenase-2 in Sheep [ChEMBL: CHEMBL4102] [UniProtKB: P79208] There should be some charts here, you may need to enable JavaScript!
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
Organic anion transporter 2/Solute carrier family 22 member 7 in Rat [ChEMBL: CHEMBL2073671] [GtoPdb: 1026] [UniProtKB: Q5RLM2] There should be some charts here, you may need to enable JavaScript!
SMCT1 in Human [GtoPdb: 922] [UniProtKB: Q8N695] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
GtoPdb	Inhibition of COX1 in human whole blood.	-	6.48	pIC50	330	nM	IC50	Bioorg Med Chem Lett (2008) 18: 4655-7 [PMID:18667313]
ChEMBL	Inhibition of COX1 in human whole blood	B	6.48	pIC50	330	nM	IC50	Bioorg Med Chem Lett (2008) 18: 4655-4657 [PMID:18667313]
ChEMBL	DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)	B	7.85	pIC50	14	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	In vitro inhibition of cyclooxygenase-1 via inhibition of TXB2 generation in the presence of 1 uM arachidonic acid in human platelet	F	8.7	pIC50	2	nM	IC50	Bioorg Med Chem Lett (2002) 12: 533-537 [PMID:11844666]
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979]
ChEMBL	Inhibition of purified ovine COX1 pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay	B	6.1	pIC50	800	nM	IC50	ACS Med Chem Lett (2014) 5: 983-988 [PMID:25221653]
ChEMBL	Inhibition of Ovine COX-1 preincubated for 15 mins by fluorescence analysis	B	7.17	pIC50	67	nM	IC50	ACS Med Chem Lett (2015) 6: 1086-1090 [PMID:26487917]
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL	Inhibition of human recombinant COX2 pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay	B	5.42	pIC50	3800	nM	IC50	ACS Med Chem Lett (2014) 5: 983-988 [PMID:25221653]
ChEMBL	DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid)	B	6.11	pIC50	785	nM	IC50	DrugMatrix in vitro pharmacology data
GtoPdb	Inhibition of COX2 in human whole blood.	-	6.16	pIC50	690	nM	IC50	Bioorg Med Chem Lett (2008) 18: 4655-7 [PMID:18667313]
ChEMBL	Inhibition of COX2 in human whole blood	B	6.16	pIC50	690	nM	IC50	Bioorg Med Chem Lett (2008) 18: 4655-4657 [PMID:18667313]
ChEMBL	Inhibition of recombinant human COX-2 preincubated for 15 mins by fluorescence analysis	B	7.21	pIC50	61	nM	IC50	ACS Med Chem Lett (2015) 6: 1086-1090 [PMID:26487917]
ChEMBL	In vitro inhibition of PGE-2 generation by LPS-stimulated monocytes isolated from human blood.	F	7.59	pIC50	26	nM	IC50	Bioorg Med Chem Lett (2002) 12: 533-537 [PMID:11844666]
Cyclooxygenase-2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4102] [UniProtKB: P79208]
ChEMBL	Inhibition of ovine COX2 assessed as reduction in PGH2 production by enzyme immunoassay	B	6.74	pIC50	180	nM	IC50	Bioorg Med Chem (2018) 26: 4113-4126 [PMID:29980364]
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]
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 6-Carboxyfluorescein uptake in OAT1-expressing CHO cells	F	5.85	pIC50	1400	nM	IC50	Anal Biochem (2000) 283: 49-55 [PMID:10929807]
ChEMBL	TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells	F	5.89	pIC50	1300	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 MTX uptake in Xenopus laevis oocytes	F	6.3	pIC50	500	nM	IC50	Eur J Pharmacol (2000) 409: 31-36 [PMID:11099697]
Organic anion transporter 2/Solute carrier family 22 member 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073671] [GtoPdb: 1026] [UniProtKB: Q5RLM2]
ChEMBL	TP_TRANSPORTER: inhibition of Salicylate uptake in Oat2-expressing LLC PK1 cells	F	5.74	pKi	1840	nM	Ki	Jpn Pharmacol Ther (2001) 29: S101-S104
SMCT1 in Human [GtoPdb: 922] [UniProtKB: Q8N695]
GtoPdb	-	-	3.92	pIC50	119000	nM	IC50	Pharm Res (2006) 23: 1209-16 [PMID:16729224]

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]