zelatriazin (TAK-041) [Ligand Id: 11685] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4779773 (Tak-041) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GPR139/Probable G-protein coupled receptor 139 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3632455] [GtoPdb: 130] [UniProtKB: Q6DWJ6] | ||||||||
| GtoPdb | Radioligand competition binding assay using membranes isolated from CHO-T-REx cells that stably express the hGPR139 | - | 6.92 | pKi | 119 | nM | Ki | J Med Chem (2021) 64: 11527-11542 [PMID:34260228] |
| ChEMBL | Displacement of (S)-N-(1-(2-[3H]-4-methoxyphenyl)propan-2-yl)-2-(2,3-dimethyl-7-oxothieno[2,3-d]pyridazin-6(7H)-yl)acetamide, from human GPR139 expressed in CHO-TRex membranes incubated for 20 mins by scintillation counting assay | B | 6.92 | pKi | 119 | nM | Ki | EP-3221298-B1. 4-oxo-3,4-dihydro-1,2,3-benzotriazine derivatives as modulators of gpr139 (null) |
| ChEMBL | Displacement of (S)-N-(1-(2-[3H]-4-methoxyphenyl)propan-2-yl)-2-(2,3-dimethyl-7-oxothieno[2,3-d]pyridazin-6(7H)-yl)acetamide from human GPR139 expressed in CHO-TRex membranes incubated for 20 mins by scintillation counting assay | B | 6.92 | pKi | 119 | nM | Ki | J Med Chem (2021) 64: 11527-11542 [PMID:34260228] |
| ChEMBL | Agonist activity at human GPR139 expressed in CHO-TRex cells assessed as stimulation of calcium signalling incubated for 15 mins by FLIPR assay | F | 7.66 | pEC50 | 22 | nM | EC50 | EP-3221298-B1. 4-oxo-3,4-dihydro-1,2,3-benzotriazine derivatives as modulators of gpr139 (null) |
| ChEMBL | Agonist activity at human GPR139 expressed in CHO-TRex cells assessed as stimulation of calcium signalling incubated for 15 mins by FLIPR assay | F | 7.66 | pEC50 | 22 | nM | EC50 | J Med Chem (2021) 64: 11527-11542 [PMID:34260228] |
| GtoPdb | Agonist-induced in vitro calcium mobilization assay, using CHO-T-REx cells stably expressing hGPR139 | - | 7.66 | pEC50 | 22 | nM | EC50 | J Med Chem (2021) 64: 11527-11542 [PMID:34260228] |
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]
