bepridil [Ligand Id: 2337] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1008 (Bepadin, Bepridil, Vascor)
  • Anthrax lethal factor in Bacillus anthracis [ChEMBL: CHEMBL4372] [UniProtKB: P15917]
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
  • Voltage-gated L-type calcium channel alpha-1C subunit in Rabbit [ChEMBL: CHEMBL2830] [UniProtKB: P15381]
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  • KNa1.1 in Rat [GtoPdb: 385] [UniProtKB: Q9Z258]
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  • Kv7.4 in Human [GtoPdb: 563] [UniProtKB: P56696]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]