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 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]