GLPG1837 [Ligand Id: 12735] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4075348
  • CFTR/Cystic fibrosis transmembrane conductance regulator in Human [ChEMBL: CHEMBL4051] [GtoPdb: 707] [UniProtKB: P13569]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CFTR/Cystic fibrosis transmembrane conductance regulator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4051] [GtoPdb: 707] [UniProtKB: P13569]
ChEMBL Potentiation of CFTR G551D mutant (unknown origin) expressed in HEK293 cells incubated for 10 mins in presence of forskolin measured for 2 mins by YFP halide assay B 6.47 pEC50 339 nM EC50 J Med Chem (2018) 61: 1425-1435 [PMID:29148763]
ChEMBL Potentiation of CFTR G551D mutant in primary HBE cells assessed as increase in channel conductivity measured every 2 mins for 20 mins by TECC assay B 6.74 pEC50 181 nM EC50 J Med Chem (2018) 61: 1425-1435 [PMID:29148763]
ChEMBL Potentiation of CFTR F508del mutant (unknown origin) expressed in human CFBE41o cells incubated for 10 mins in presence of forskolin measured for 7 secs by YFP halide assay B 8.52 pEC50 3 nM EC50 J Med Chem (2018) 61: 1425-1435 [PMID:29148763]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG by manual patch clamp method B 4.48 pEC50 >33000 nM EC50 J Med Chem (2018) 61: 1425-1435 [PMID:29148763]

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]