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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 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]