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 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]
