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ChEMBL ligand: CHEMBL914 (Allegra, Fexofenadine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]