TPMPA [Ligand Id: 4328] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL397209 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GABAA receptor ρ1 subunit/GABA receptor rho-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3561] [GtoPdb: 420] [UniProtKB: P24046] | ||||||||
| ChEMBL | Antagonist activity at human recombinant GABAc rho-1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique | F | 5.65 | pIC50 | 2220 | nM | IC50 | ACS Med Chem Lett (2011) 2: 11-16 [PMID:24900248] |
| ChEMBL | Antagonist activity at GABAC rho1 receptor (unknown origin) | B | 5.65 | pIC50 | 2220 | nM | IC50 | ACS Med Chem Lett (2013) 4: 402-407 [PMID:24900684] |
| GABAA receptor ρ2 subunit/GABA receptor rho-2 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2375] [GtoPdb: 421] [UniProtKB: P28476] | ||||||||
| ChEMBL | Antagonist activity at human recombinant GABAc rho-2 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique | F | 4.66 | pIC50 | 22090 | nM | IC50 | ACS Med Chem Lett (2011) 2: 11-16 [PMID:24900248] |
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]
