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ChEMBL ligand: CHEMBL1008 (Bepadin, Bepridil, Vascor) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Anthrax lethal factor in Bacillus anthracis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4372] [UniProtKB: P15917] | ||||||||
ChEMBL | Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability after 24 hrs by WST1 dye reduction assay | B | 5.32 | pIC50 | 4800 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 2403-2411 [PMID:17485504] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Displacement of [3H]Astemizole from hERG expressed in HEK293 cells at 10 uM | B | 6.35 | pKi | 444 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 5303-5308 [PMID:16908150] |
ChEMBL | Displacement of [3H]dofetilide from hERG expressed in HEK293 cells by SPA | B | 6.54 | pKi | 291 | nM | Ki | J Med Chem (2007) 50: 2931-2941 [PMID:17536794] |
ChEMBL | Binding affinity at hERG expressed in HEK293 cells by fluorescence polarization assay | B | 6.74 | pKi | 184 | nM | Ki | J Med Chem (2007) 50: 2931-2941 [PMID:17536794] |
ChEMBL | Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay | B | 5.85 | pIC50 | 1400 | nM | IC50 | J Med Chem (2020) 63: 5734-5751 [PMID:32392053] |
ChEMBL | K+ channel blocking activity in COS-7 African green monkey kidney derived cells expressing HERG Kv11.1 | F | 6.26 | pIC50 | 550 | nM | IC50 | J Med Chem (2002) 45: 3844-3853 [PMID:12190308] |
ChEMBL | Inhibition of human Potassium channel HERG expressed in mammalian cells | B | 6.26 | pIC50 | 549.54 | 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 | 6.26 | pIC50 | 549.54 | nM | IC50 | Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342] |
ChEMBL | Inhibition of human ERG in MCF7 cells | B | 6.26 | pIC50 | 549.54 | 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 | 6.26 | pIC50 | 549.54 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831] |
ChEMBL | Inhibitory concentration against potassium channel HERG | B | 6.26 | pIC50 | 549.54 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
ChEMBL | Inhibitory concentration against IKr potassium channel | B | 6.37 | pIC50 | 430 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4771-4777 [PMID:15324906] |
ChEMBL | Inhibition of hERG K channel | F | 7.48 | pIC50 | 33 | nM | IC50 | Cardiovasc Res (2011) 91: 53-61 [PMID:21300721] |
ChEMBL | Inhibition of human ERG | B | 7.64 | pIC50 | 22.91 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antimalarial activity against Plasmodium falciparum | F | 5.6 | pIC50 | 2500 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 2403-2411 [PMID:17485504] |
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
ChEMBL | Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA | F | 5.43 | pIC50 | 3700 | nM | IC50 | Cardiovasc Res (2011) 91: 53-61 [PMID:21300721] |
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505] | ||||||||
ChEMBL | Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes | F | 5.59 | pIC50 | 2600 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
ChEMBL | Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in guinea pig atrial myocytes | F | 5.81 | pIC50 | 1550 | nM | IC50 | IC50 data for the L-type calcium channel extracted from a set of literature articles |
ChEMBL | Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes | F | 6.3 | pIC50 | 500 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
ChEMBL | Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes | F | 6.68 | pIC50 | 211 | nM | IC50 | Cardiovasc Res (2011) 91: 53-61 [PMID:21300721] |
ChEMBL | Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes | F | 6.68 | pIC50 | 211 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936] | ||||||||
ChEMBL | Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit | F | 5.85 | pIC50 | 1400 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
Voltage-gated L-type calcium channel alpha-1C subunit in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2830] [UniProtKB: P15381] | ||||||||
ChEMBL | Inhibition of [3H]nitrendipine binding to calcium channels in Rabbit cardiac muscle. | B | 4.66 | pIC50 | 22000 | nM | IC50 | J Med Chem (1988) 31: 2221-2227 [PMID:3184128] |
KNa1.1 in Rat [GtoPdb: 385] [UniProtKB: Q9Z258] | ||||||||
GtoPdb | - | - | 6 | pIC50 | - | - | - | Neuropharmacology (2006) 51: 896-906 [PMID:16876206] |
Kv7.4 in Human [GtoPdb: 563] [UniProtKB: P56696] | ||||||||
GtoPdb | - | - | 5 | pIC50 | - | - | - | Am J Physiol, Cell Physiol (2001) 280: C859-66 [PMID:11245603] |
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]