encenicline [Ligand Id: 6926] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2151572 (Encenicline, Evp-6124, EVP-6124, MT-4666, MT4666) |
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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 | Displacement of [3H]epibatidine form human alpha7 nAchR expressed in HEK293 cells | B | 8 | pKi | 9.98 | nM | Ki | J Med Chem (2012) 55: 9793-9809 [PMID:23126648] |
| ChEMBL | Binding affinity to human alpha7 nAchR | B | 8.37 | pKi | 4.3 | nM | Ki | J Med Chem (2011) 54: 7943-7961 [PMID:21919481] |
| GtoPdb | - | - | 8.37 | pKi | 4.3 | nM | Ki |
Drugs R D (2004) 5: 102-7 [PMID:15293871]; J Med Chem (2011) 54: 7943-61 [PMID:21919481] |
| ChEMBL | Partial agonist activity at human alpha7 nAChR expressed in Xenopus laevis oocytes by voltage clamp electrophysiological method | B | 6.41 | pEC50 | 390 | nM | EC50 | Eur J Med Chem (2018) 160: 37-48 [PMID:30317024] |
| ChEMBL | Agonist activity at human alpha7 nAChR expressed in xenopus oocytes preincubated for 10 mins followed by acetylcholine addition by patch clamp electrophysiological assay | B | 6.47 | pEC50 | 340 | nM | EC50 | Eur J Med Chem (2016) 115: 94-108 [PMID:26994846] |
| ChEMBL | Agonist activity at human alpha7 nAChR expressed in Xenopus laevis oocytes assessed as induction of channel current at -90 mV holding potential by two-electrode voltage clamp method | B | 6.6 | pEC50 | 250 | nM | EC50 | Eur J Med Chem (2019) 182: 111618-111618 [PMID:31434041] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | Binding affinity to 5HT3 receptor | B | 6.52 | pIC50 | 299 | nM | IC50 | J Med Chem (2011) 54: 7943-7961 [PMID:21919481] |
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]
