mibefradil
A benzimidazoyl-substituted tetraline that selectively binds and inhibits CALCIUM CHANNELS, T-TYPE.
Ligand Summary
UNII: 27B90X776A
PubChem: 60663
Guide to Pharmacology: 2522
ChEMBL: CHEMBL45816
DrugCentral: 1797
LyCHI: KY2KDTUWSUYM
Target Activities
CACNA1G
Voltage-dependent T-type calcium channel subunit alpha-1G
22 Activities
Items per page:
1 – 10 of 22
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 7.19 | J Med Chem, (2017) 60:23:9769 | ||||
IC50 | 6.7 | Bioorg. Med. Chem., (2011) 19:18:5628 | ||||
IC50 | 6.25 | Bioorg. Med. Chem. Lett., (2013) 23:24:6656 | ||||
IC50 | 6.25 | Bioorg. Med. Chem. Lett., (2014) 24:6:1565 | ||||
IC50 | 6.08 | Bioorg. Med. Chem. Lett., (2004) 14:13:3379 | ||||
IC50 | 6.08 | Bioorg. Med. Chem., (2007) 15:2:1091 | ||||
IC50 | 6.08 | Bioorg. Med. Chem. Lett., (2010) 20:14:4219 | ||||
IC50 | 6.08 | Bioorg. Med. Chem. Lett., (2013) 23:6:1887 | ||||
IC50 | 6.07 | Bioorg. Med. Chem. Lett., (2010) 20:14:4219 | ||||
IC50 | 6 | Bioorg. Med. Chem., (2010) 18:16:5938 | ||||
KCNH2
Potassium voltage-gated channel subfamily H member 2
19 Activities
Items per page:
1 – 10 of 19
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
Ki | 6.72 | J. Med. Chem., (2007) 50:13:2931 | ||||
Ki | 6.45 | J. Med. Chem., (2007) 50:13:2931 | ||||
IC50 | 6.24 | J Med Chem, (2017) 60:23:9769 | ||||
IC50 | 6.09 | J. Med. Chem., (2008) 51:20:6471 | ||||
IC50 | 5.89 | Bioorg. Med. Chem. Lett., (2015) 25:18:3941 | ||||
IC50 | 5.87 | Bioorg. Med. Chem. Lett., (2011) 21:19:5910 | ||||
IC50 | 5.87 | Bioorg Med Chem Lett, (2019) 29:10:1168 | ||||
IC50 | 5.85 | Bioorg. Med. Chem. Lett., (2004) 14:18:4771 | ||||
IC50 | 5.85 | Bioorg. Med. Chem. Lett., (2010) 20:9:2705 | ||||
IC50 | 5.85 | Bioorg. Med. Chem. Lett., (2011) 21:1:215 | ||||
CACNA1H
Voltage-dependent T-type calcium channel subunit alpha-1H
7 Activities
Items per page:
1 – 7 of 7
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 7.5 | Bioorg. Med. Chem. Lett., (2010) 20:22:6375 | ||||
IC50 | 6.89 | Bioorg. Med. Chem. Lett., (2008) 18:2:474 | ||||
IC50 | 6.89 | J Med Chem, (2017) 60:23:9769 | ||||
IC50 | 6.74 | Bioorg. Med. Chem. Lett., (2015) 25:18:3941 | ||||
IC50 | 6 | Bioorg. Med. Chem., (2010) 18:16:5938 | ||||
IC50 | 6 | Bioorg. Med. Chem. Lett., (2013) 23:1:119 | ||||
IC50 | 6.6 | BLOCKER | ||||
CYP3A4
Cytochrome P450 3A4
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 6.89 | J. Med. Chem., (2003) 46:9:1716 | ||||
Ki | 6.55 | Drug Metab. Dispos., (2011) 39:7:1188 | ||||
IC50 | 6.52 | J. Med. Chem., (2012) 55:11:4896 | ||||
AC50 | 6.5 | None, None:None:None | ||||
IC50 | 6.33 | Drug Metab. Dispos., (2013) 41:1:60 | ||||
CACNA1I
Voltage-dependent T-type calcium channel subunit alpha-1I
4 Activities
Items per page:
1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 5.8 | |||||
IC50 | 6.9 | J. Med. Chem., (2008) 51:20:6471 | ||||
IC50 | 6.89 | J Med Chem, (2017) 60:23:9769 | ||||
IC50 | 6 | Bioorg. Med. Chem., (2010) 18:16:5938 | ||||
CACNA1C
Voltage-dependent L-type calcium channel subunit alpha-1C
3 Activities
CYP2D6
Cytochrome P450 2D6
3 Activities
CACNA1B
Voltage-dependent N-type calcium channel subunit alpha-1B
2 Activities
CACNA1A
Voltage-dependent P/Q-type calcium channel subunit alpha-1A
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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- | 6.5 | |||||
CACNA1E
Voltage-dependent R-type calcium channel subunit alpha-1E
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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- | 6.4 | |||||
SCN5A
Sodium channel protein type 5 subunit alpha
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 6.3 | J Med Chem, (2017) 60:23:9769 | ||||
SCN9A
Sodium channel protein type 9 subunit alpha
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 6.3 | J Med Chem, (2017) 60:23:9769 | ||||