tecalcet [Ligand Id: 718] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL292376 (Tecalcet)
  • CaS receptor/Calcium sensing receptor in Human [ChEMBL: CHEMBL1878] [GtoPdb: 54] [UniProtKB: P41180]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CaS receptor/Calcium sensing receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1878] [GtoPdb: 54] [UniProtKB: P41180]
GtoPdb - - 6.5 pKd - - - Proc Natl Acad Sci USA (1998) 95: 4040-5 [PMID:9520489]
ChEMBL Activity at human CaSR expressed in HEK293 cells assessed as calcium release by FLIPR assay B 6.71 pEC50 194 nM EC50 J. Med. Chem. (2009) 52: 6535-6538 [PMID:19835382]
ChEMBL Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay B 7.1 pEC50 80 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 2451-2454 [PMID:23465611]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]