AR231453 [Ligand Id: 5653] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL461384 |
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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 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay | F | 5.52 | pEC50 | 3000 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 2383-2387 [PMID:24751443] |
| ChEMBL | Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay | F | 6.15 | pEC50 | 700 | nM | EC50 | Eur J Med Chem (2016) 124: 103-116 [PMID:27560285] |
| ChEMBL | Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay | F | 6.19 | pEC50 | 640 | nM | EC50 | Eur J Med Chem (2020) 188: 112017-112017 [PMID:31926470] |
| GtoPdb | - | - | 8.2 | pEC50 | - | - | - | Endocrinology (2007) 148: 2601-9 [PMID:17289847] |
| ChEMBL | Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay | F | 8.22 | pEC50 | 6 | nM | EC50 | Bioorg Med Chem (2021) 35: 116071-116071 [PMID:33611013] |
| ChEMBL | Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay | B | 8.32 | pEC50 | 4.78 | nM | EC50 | Bioorg Med Chem Lett (2019) 29: 126707-126707 [PMID:31630858] |
| ChEMBL | Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation | F | 9.17 | pEC50 | 0.68 | nM | EC50 | J Med Chem (2008) 51: 5172-5175 [PMID:18698756] |
| ChEMBL | Agonist activity at human GPR119 by melanophore assay | F | 9.19 | pEC50 | 0.65 | nM | EC50 | 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]
