APD668 [Ligand Id: 12151] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1775179 (JNJ-28630368) |
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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 human HEK293 cells assessed as increase in adenylate cyclase activation | F | 7.64 | pEC50 | 23 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 3134-3141 [PMID:21444206] |
| ChEMBL | Agonist activity at human GPR119 by melanophore assay | F | 8.57 | pEC50 | 2.7 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 3134-3141 [PMID:21444206] |
| GtoPdb | Determined in a melanophore assay (Xenopus oocytes expressing GPR119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion. | - | 8.57 | pEC50 | 2.7 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 3134-41 [PMID:21444206] |
| GPR119/Glucose-dependent insulinotropic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5262] [GtoPdb: 126] [UniProtKB: Q7TQN8] | ||||||||
| GtoPdb | Determined in a melanophore assay (Xenopus oocytes expressing rGpr119) that reveals receptor-mediated Gs activation as intracellular pigment dispresion. | - | 7.48 | pEC50 | 33 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 3134-41 [PMID:21444206] |
| ChEMBL | Agonist activity at rat GPR119 by melanophore assay | F | 7.48 | pEC50 | 33 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 3134-3141 [PMID:21444206] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG by patch clamp assay | B | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3134-3141 [PMID:21444206] |
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]
