zelatriazin (TAK-041) [Ligand Id: 11685] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4779773 (Tak-041, Zelatriazin, Zelatriazina, Zelatriazine) |
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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 (2019) |
| 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 (2019) |
| 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 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]
