cerlapirdine [Ligand Id: 7356] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL2103880 (Cerlapirdina, Cerlapirdine, PF-05212365, Sam-531, SAM-531, SAM-531 FREE BASE, WAY-262,531, WAY-262531)
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells B 8.89 pKi 1.3 nM Ki J Med Chem (2014) 57: 7160-7181 [PMID:24850589]
ChEMBL Antagonist activity at 5-HT6 receptor (unknown origin) B 8.89 pKi 1.3 nM Ki J Med Chem (2017) 60: 1843-1859 [PMID:28212021]
ChEMBL Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constant B 8.89 pKi 1.3 nM Ki Bioorg Med Chem Lett (2021) 49: 128275-128275 [PMID:34311086]
GtoPdb - - 8.89 pKi 1.3 nM Ki Alzheimers Dement (2010) 6: S548-S549

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]