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ChEMBL ligand: CHEMBL327980 (E-4031) |
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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 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 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]