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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]