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

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ChEMBL ligand: CHEMBL914 (Fexofenadine, Allegra)
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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 27:

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]