E4031 [Ligand Id: 2605] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL327980 (E-4031)
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  • Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259]
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  • Kv11.2 in Rat [GtoPdb: 573] [UniProtKB: O54853]
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  • Kv11.3 in Rat [GtoPdb: 574] [UniProtKB: O54852]
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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 tracer Red binding to human ERG expressed in membranes after 3 hrs by fluorescence polarization assay B 6.52 pIC50 <300 nM IC50 J Med Chem (2019) 62: 4638-4655 [PMID:30998358]
ChEMBL Inhibition of human ERG expressed in cell membranes after 4 hrs by fluorescence polarization assay B 7.15 pIC50 70 nM IC50 Bioorg. Med. Chem. (2016) 24: 2954-2963 [PMID:27229618]
ChEMBL Inhibition of human ERG expressed in HEK293 cells by patch clamp assay B 7.57 pIC50 27 nM IC50 J Med Chem (2020) 63: 4506-4516 [PMID:32298114]
ChEMBL Inhibition of human ERG incubated for 3 hrs by competitive fluorescence tracer binding based assay B 7.62 pIC50 24.2 nM IC50 Eur J Med Chem (2021) 224: 113674-113674 [PMID:34237622]
ChEMBL Inhibition of human ERG expressed in CHOK1 cells assessed as inhibition of tail current after 5 mins by automated whole-cell patch clamp assay B 7.62 pIC50 24 nM IC50 Eur. J. Med. Chem. (2016) 117: 256-268 [PMID:27105029]
ChEMBL Inhibition of human ERG channel in HEK293 cells by voltage-clamp method B 7.64 pIC50 22.91 nM IC50 Eur. J. Med. Chem. (2008) 43: 2479-2488 [PMID:18262683]
ChEMBL Inhibition of human ERG incubated for 4 hrs by competitive fluorescence tracer binding based assay B 7.68 pIC50 21 nM IC50 Eur J Med Chem (2019) 183: 111684-111684 [PMID:31520926]
ChEMBL Inhibitory concentration against IKr potassium channel B 7.7 pIC50 20 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 4771-4777 [PMID:15324906]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 7.7 pIC50 19.95 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 7.7 pIC50 19.95 nM IC50 Bioorg. Med. Chem. (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibitory concentration against potassium channel HERG B 7.7 pIC50 19.95 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human ERG B 7.92 pIC50 12.02 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
GtoPdb - - 8.1 pIC50 7.7 nM IC50 Biophys J (1998) 74: 230-41 [PMID:9449325]
ChEMBL Inhibition of fluorescently labeled tracer binding to human ERG by competitive binding assay B 8.11 pIC50 7.82 nM IC50 Eur J Med Chem (2019) 175: 107-113 [PMID:31077996]
ChEMBL Inhibition of human ERG in MCF7 cells B 8.11 pIC50 7.76 nM IC50 Eur. J. Med. Chem. (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 F 8.11 pIC50 7.7 nM IC50 J. Med. Chem. (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Inhibition of human ERG by fluorescently labeled tracer binding method B 8.92 pIC50 1.2 nM IC50 J Med Chem (2017) 60: 9205-9221 [PMID:29091425]
ChEMBL Inhibition of human ERG assessed as reduction of tail current B 7.6 pEC50 25 nM EC50 Eur. J. Med. Chem. (2015) 101: 627-639 [PMID:26204510]
Kv11.1 in Rat [GtoPdb: 572] [UniProtKB: O08962]
GtoPdb - - 7 pKd - - - J Neurosci (1997) 17: 9423-32 [PMID:9390998]
Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259]
GtoPdb - - 6.4 pIC50 - - - Br J Pharmacol (2003) 138: 161-71 [PMID:12522086]
Kv11.2 in Rat [GtoPdb: 573] [UniProtKB: O54853]
GtoPdb - - 6.9 pKd - - - J Neurosci (1997) 17: 9423-32 [PMID:9390998]
Kv11.3 in Rat [GtoPdb: 574] [UniProtKB: O54852]
GtoPdb - - 6.7 pKd - - - J Neurosci (1997) 17: 9423-32 [PMID:9390998]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]