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 F 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 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]