pirlindole [Ligand Id: 6638] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL32350 (Pirazidol, Pirlindol, 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 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]
