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 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]
