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 | GPCR PRESTO-Tango dose-response in agonist mode with target: GPR119 | F | 5.84 | pEC50 | 1444.63 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 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 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]
