PNU-120596 [Ligand Id: 3991] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL257591 (PNU-120596) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544] | ||||||||
| ChEMBL | Positive allosteric modulation at human alpha7 nACHR expressed in Xenopus oocyte assessed as potentiation of 200 uM ACh-induced current at holding potential of -80 mV by electrophysiology | B | 5.42 | pEC50 | 3800 | nM | EC50 | Eur J Med Chem (2014) 86: 724-739 [PMID:25232969] |
| ChEMBL | Activity at human alpha-7 nACh receptor expressed in Xenopus laevis oocyte assessed as increase in acetylcholine-induced current | B | 5.82 | pEC50 | 1500 | nM | EC50 | J Med Chem (2008) 51: 701-712 [PMID:18198823] |
| ChEMBL | Positive allosteric modulation of human alpha7 nAChR expressed in Xenopus laevis oocytes assessed as increase in Ach-induced current at -90 mV membrane potential by two electrode voltage-clamp assay | B | 6.66 | pEC50 | 220 | nM | EC50 | J Med Chem (2021) 64: 12379-12396 [PMID:34374537] |
| ChEMBL | Positive allosteric modulator activity at human alpha7 nAChR expressed in rat GH4C1 assessed as calcium mobilization by FLIPR assay | B | 6.8 | pEC50 | 158.49 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 4561-4565 [PMID:20591663] |
ChEMBL data shown on this page come from version 35:
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]
