fexofenadine [Ligand Id: 4819] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL914 (Allegra, Fexofenadina, Fexofenadine)
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG channel B 4.64 pKi 23000 nM Ki J Med Chem (2015) 58: 2584-2608 [PMID:25494650]
ChEMBL Inhibition of human ERG in L929 cells at 10 uM by whole cell patch-clamp assay B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2009) 19: 5043-5047 [PMID:19660947]
ChEMBL Inhibition of human ERG expressed in HEK293 cells by whole cell patch clamp method B 4.19 pIC50 65000 nM IC50 J Med Chem (2009) 52: 1630-1638 [PMID:19260734]
ChEMBL Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1 B 4.64 pIC50 23000 nM IC50 Bioorg Med Chem Lett (2003) 13: 1829-1835 [PMID:12729675]
ChEMBL Inhibition of human Erg expressed in HEK293 cells assessed as rubidium efflux after 4 hrs by atomic absorbance spectrometric analysis B 4.64 pIC50 23000 nM IC50 Bioorg Med Chem Lett (2012) 22: 3781-3785 [PMID:22542010]
ChEMBL Inhibition of human ERG potassium channel in HEK293 cells by patch clamp assay B 4.64 pIC50 23000 nM IC50 Bioorg Med Chem Lett (2006) 16: 5507-5512 [PMID:16931010]
ChEMBL Inhibition of human ERG B 4.64 pIC50 22908.68 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 F 4.67 pIC50 21570 nM IC50 J Med Chem (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Inhibition of human ERG in MCF7 cells B 4.67 pIC50 21379.62 nM IC50 Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state F 4.67 pIC50 21379.62 nM IC50 Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL Inhibition of human ERG in L929 cells by whole cell patch-clamp assay B 7 pIC50 >100 nM IC50 Bioorg Med Chem Lett (2009) 19: 5043-5047 [PMID:19660947]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting B 7.57 pKi 27 nM Ki Bioorg Med Chem Lett (2009) 19: 5043-5047 [PMID:19660947]
GtoPdb - - 7.57 pKi 27 nM Ki Bioorg Med Chem Lett (2009) 19: 5043-7 [PMID:19660947]
ChEMBL Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting B 7.11 pIC50 78 nM IC50 Bioorg Med Chem Lett (2009) 19: 2766-2771 [PMID:19362477]
ChEMBL Inhibition of histamine H1 receptor B 7.11 pIC50 78 nM IC50 Bioorg Med Chem Lett (2009) 19: 2766-2771 [PMID:19362477]
ChEMBL Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting B 7.11 pIC50 78 nM IC50 Bioorg Med Chem (2011) 19: 3005-3021 [PMID:21470866]
ChEMBL Inhibition of histamine H1 receptor (unknown origin) B 7.82 pIC50 15 nM IC50 J Med Chem (2015) 58: 2584-2608 [PMID:25494650]

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]