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ChEMBL ligand: CHEMBL850 (AT-4140, CI-978, NSC-759641, Spara, Sparfloxacin, Zagam) |
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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 | DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) | B | 4.41 | pKi | 38619.4 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) | B | 4.33 | pIC50 | 47138.4 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity to human ERG S624A tetrameric mutant expressed in HEK293 cells assessed as inhibition of tail current measured upon repolarization to -40 mV by patch clamp method | B | 4.33 | pIC50 | 46900 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3848-3851 [PMID:23711922] |
ChEMBL | K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 | F | 4.46 | pIC50 | 34400 | nM | IC50 | J Med Chem (2002) 45: 3844-3853 [PMID:12190308] |
ChEMBL | Binding affinity to human ERG F656A tandem dimeric mutant expressed in HEK293 cells assessed as inhibition of tail current measured upon repolarization to -120 mV by patch clamp method | B | 4.47 | pIC50 | 33600 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3848-3851 [PMID:23711922] |
ChEMBL | Inhibition of human ERG in MCF7 cells | B | 4.58 | pIC50 | 26302.68 | 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 | 4.58 | pIC50 | 26302.68 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831] |
ChEMBL | Binding affinity to wild type human ERG expressed in HEK293 cells assessed as inhibition of tail current measured upon repolarization to -40 mV by patch clamp method | B | 4.66 | pIC50 | 21700 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3848-3851 [PMID:23711922] |
ChEMBL | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | B | 4.74 | pIC50 | 18197.01 | nM | IC50 | Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342] |
ChEMBL | Inhibitory concentration against potassium channel HERG | B | 4.74 | pIC50 | 18197.01 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
ChEMBL | Inhibition of human Potassium channel HERG expressed in mammalian cells | B | 4.74 | pIC50 | 18197.01 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512] |
ChEMBL | Inhibition of human ERG current by patch clamp assay | B | 4.74 | pIC50 | 18000 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3848-3851 [PMID:23711922] |
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]