pirlindole [Ligand Id: 6638] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL32350 (Pirazidol, Pirlindole) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14] | ||||||||
| ChEMBL | Antagonist activity against Gamma-aminobutyric acid A (GABA-A) receptor | F | 4.92 | pEC50 | 12000 | nM | EC50 | J Med Chem (2000) 43: 1427-1447 [PMID:10780899] |
| TEA domain transcription factor 1/Transcriptional enhancer factor TEF-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3334416] [GtoPdb: 3240] [UniProtKB: P28347] | ||||||||
| ChEMBL | Binding affinity to TEAD1 (194 to 411 residues) (unknown origin) by ITC assay | B | 4.92 | pKd | 12000 | nM | Kd | J Med Chem (2019) 62: 1291-1305 [PMID:30640473] |
| ChEMBL | Inhibition of Gal4-fused TEAD1 (unknown origin) interaction with YAP expressed in human HeLa cells assessed as basal transcriptional activity level after 6 hrs by nanoluciferase reporter gene assay | B | 4.4 | pIC50 | 40000 | nM | IC50 | J Med Chem (2019) 62: 1291-1305 [PMID:30640473] |
| TEA domain transcription factor 4/Transcriptional enhancer factor TEF-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295828] [GtoPdb: 3243] [UniProtKB: Q15561] | ||||||||
| ChEMBL | Inhibition of Gal4-fused TEAD4 (unknown origin) interaction with YAP expressed in human HeLa cells assessed as basal transcriptional activity level after 6 hrs by nanoluciferase reporter gene assay | B | 4.44 | pIC50 | 36000 | nM | IC50 | J Med Chem (2019) 62: 1291-1305 [PMID:30640473] |
| TEA domain transcription factor 2/Transcriptional enhancer factor TEF-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523301] [GtoPdb: 3241] [UniProtKB: Q15562] | ||||||||
| ChEMBL | Inhibition of Gal4-fused TEAD2 (unknown origin) interaction with YAP expressed in human HeLa cells assessed as basal transcriptional activity level after 6 hrs by nanoluciferase reporter gene assay | B | 4.48 | pIC50 | 33000 | nM | IC50 | J Med Chem (2019) 62: 1291-1305 [PMID:30640473] |
| TEA domain transcription factor 3/Transcriptional enhancer factor TEF-5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523435] [GtoPdb: 3242] [UniProtKB: Q99594] | ||||||||
| ChEMBL | Inhibition of Gal4-fused TEAD3 (unknown origin) interaction with YAP expressed in human HeLa cells assessed as basal transcriptional activity level after 6 hrs by nanoluciferase reporter gene assay | B | 4.36 | pIC50 | 44000 | nM | IC50 | J Med Chem (2019) 62: 1291-1305 [PMID:30640473] |
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]
