tenidap [Ligand Id: 2395] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1908355 (CP-66,248, CP-66248, Tenidap)
  • 5-LOX/Arachidonate 5-lipoxygenase in Rat [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
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  • Kir2.3 in Human [GtoPdb: 432] [UniProtKB: P48050]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-LOX/Arachidonate 5-lipoxygenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
ChEMBL In vitro inhibition of 5-lipoxygenase pathway in rat basophilic leukemia (RBL-1) cells B 5.05 pIC50 9000 nM IC50 J Med Chem (1990) 33: 2019-2024 [PMID:2113951]
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 7.26 pIC50 55 nM IC50 DrugMatrix in vitro pharmacology data
Cyclooxygenase-1 in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3334] [UniProtKB: O97554]
ChEMBL Inhibition of COX-1 in rabbit peripheral venous blood assessed as formation of 12-hydroxyheptadecatrienoic acid after 24 hrs by HPLC in presence of calcium ionophore A23187 B 5.59 pIC50 2560 nM IC50 Bioorg Med Chem Lett (2010) 20: 7349-7353 [PMID:21055929]
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) B 6.57 pIC50 267 nM IC50 DrugMatrix in vitro pharmacology data
CYP1A2/Cytochrome P450 1A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3356] [GtoPdb: 1319] [UniProtKB: P05177]
ChEMBL DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 6 pIC50 1000 nM IC50 DrugMatrix in vitro pharmacology data
CYP2C9/Cytochrome P450 2C9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3397] [GtoPdb: 1326] [UniProtKB: P11712]
ChEMBL DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 6.15 pIC50 700 nM IC50 DrugMatrix in vitro pharmacology data
Prostaglandin G/H synthase 2 in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293198] [UniProtKB: O02768]
ChEMBL Inhibition of COX-2 in rabbit peripheral venous blood assessed as formation of 12-hydroxyheptadecatrienoic acid after 24 hrs in by HPLC presence of calcium ionophore A23188 and lipopolysaccharide B 5.08 pIC50 8400 nM IC50 Bioorg Med Chem Lett (2010) 20: 7349-7353 [PMID:21055929]
Kir2.3 in Human [GtoPdb: 432] [UniProtKB: P48050]
GtoPdb - - 6.4 pEC50 - - - Eur J Pharmacol (2002) 435: 153-60 [PMID:11821021]

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]