compound 58 [PMID: 21273063] [Ligand Id: 5748] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1771100
  • GPR119/Glucose-dependent insulinotropic receptor in Human [ChEMBL: CHEMBL5652] [GtoPdb: 126] [UniProtKB: Q8TDV5]
  • GPR119/Glucose-dependent insulinotropic receptor in Mouse [ChEMBL: CHEMBL5263] [GtoPdb: 126] [UniProtKB: Q7TQP3]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GPR119/Glucose-dependent insulinotropic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5652] [GtoPdb: 126] [UniProtKB: Q8TDV5]
ChEMBL Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay F 8.4 pEC50 4 nM EC50 Bioorg Med Chem Lett (2011) 21: 2665-2669 [PMID:21273063]
GtoPdb - - 8.4 pEC50 4 nM EC50 Bioorg Med Chem Lett (2011) 21: 2665-9 [PMID:21273063]
GPR119/Glucose-dependent insulinotropic receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5263] [GtoPdb: 126] [UniProtKB: Q7TQP3]
ChEMBL Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay F 8.4 pEC50 4 nM EC50 Bioorg Med Chem Lett (2011) 21: 2665-2669 [PMID:21273063]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG by patch clamp technique B 4.72 pIC50 19000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2665-2669 [PMID:21273063]

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]