Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T54644 Target Info
Target Name Voltage-gated calcium channel alpha Cav3.2 (CACNA1H)
Synonyms
Voltage-gated calcium channel subunit alpha Cav3.2; Voltage-dependent T-type calcium channel subunit alpha-1H; Low-voltage-activated calcium channel alpha1 3.2 subunit
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Target Type Successful Target
Gene Name CACNA1H
Biochemical Class Voltage-gated ion channel
UniProt ID
CAC1H_HUMAN
Co-Targets of This Target  Top
Co-Target Name Debrisoquine 4-hydroxylase (CYP2D6) Successful Target
UniProt ID CP2D6_HUMAN
Gene Name CYP2D6
Synonyms
P450-DB1; Cytochrome P450-DB1; Cytochrome P450 2D6; CYPIID6; CYP2DL1
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Representative Drug(s) Mibefradil Drug Info IC50 = 63 nM [1]
Co-Target Name Voltage-gated calcium channel alpha Cav3.1 (CACNA1G) Successful Target
UniProt ID CAC1G_HUMAN
Gene Name CACNA1G
Synonyms
Voltage-gated calcium channel alpha subunit Cav3.1; Voltage-dependent T-type calcium channel; NBR13; Cav3.1c; CACNA1G
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Representative Drug(s) Mibefradil Drug Info IC50 = 64 nM [2]
Co-Target Name Voltage-gated potassium channel Kv11.1 (KCNH2) Successful Target
UniProt ID KCNH2_HUMAN
Gene Name KCNH2
Synonyms
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
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Representative Drug(s) Mibefradil Drug Info Ki = 190 nM [3]
Co-Target Name Voltage-gated calcium channel alpha Cav1.2 (CACNA1C) Successful Target
UniProt ID CAC1C_HUMAN
Gene Name CACNA1C
Synonyms
Voltage-gated calcium channel subunit alpha Cav1.2; Voltage-dependent L-type calcium channel subunit alpha-1C; Calcium channel, L type, alpha-1 polypeptide, isoform 1, cardiac muscle; CCHL1A1; CACNL1A1; CACN2; CACH2
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Representative Drug(s) Mibefradil Drug Info IC50 = 202 nM [4]
Co-Target Name Voltage-gated calcium channel alpha Cav2.2 (CACNA1B) Successful Target
UniProt ID CAC1B_HUMAN
Gene Name CACNA1B
Synonyms
Voltage-gated calcium channel alpha subunit Cav2.2; Voltage-dependent N-type calcium channel alpha-1B subunit; N-type Ca2+ channel; Calcium channel, L type, alpha-1 polypeptide isoform 5; CACNA1B; Brain calcium channel III; BIII
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Representative Drug(s) Mibefradil Drug Info IC50 = 416 nM [5]
Co-Target Name Voltage-gated sodium channel alpha Nav1.5 (SCN5A) Successful Target
UniProt ID SCN5A_HUMAN
Gene Name SCN5A
Synonyms
Voltage-gated sodium channel subunit alpha Nav1.5; Sodium channel protein type V subunit alpha; Sodium channel protein type 5 subunit alpha; Sodium channel protein cardiac muscle subunit alpha; HH1
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Representative Drug(s) Mibefradil Drug Info IC50 = 500 nM [2]
Co-Target Name Albendazole monooxygenase (CYP3A4) Clinical trial Target
UniProt ID CP3A4_HUMAN
Gene Name CYP3A4
Synonyms
Taurochenodeoxycholate 6-alpha-hydroxylase; Quinine 3-monooxygenase; P450-PCN1; Nifedipine oxidase; NF-25; HLp; Cytochrome P450-PCN1; Cytochrome P450 NF-25; Cytochrome P450 HLp; Cytochrome P450 3A4; Cytochrome P450 3A3; CYPIIIA4; CYPIIIA3; CYP3A3; Albendazole sulfoxidase; Albendazole monooxygenase (sulfoxide-forming); 1,8-cineole 2-exo-monooxygenase
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Representative Drug(s) Mibefradil Drug Info IC50 = 130 nM [6]
Co-Target Name Voltage-gated sodium channel alpha Nav1.7 (SCN9A) Clinical trial Target
UniProt ID SCN9A_HUMAN
Gene Name SCN9A
Synonyms
hNE-Na; Voltage-gated sodium channel subunit alpha Nav1.7; Sodium channel proteintype IX subunit alpha; Sodium channel proteintype 9 subunit alpha; Sodium channel protein type IX subunit alpha; Sodium channel protein type 9 subunit alpha; Peripheral sodium channel 1; PN1; Neuroendocrine sodium channel; NENA
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Representative Drug(s) Mibefradil Drug Info IC50 = 500 nM [2]
Co-Target Name Voltage-gated calcium channel alpha Cav3.3 (CACNA1I) Literature-reported Target
UniProt ID CAC1I_HUMAN
Gene Name CACNA1I
Synonyms
Voltage-gated calcium channel subunit alpha Cav3.3; Voltage-dependent T-type calcium channel subunit alpha-1I; KIAA1120; Ca(v)3.3
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Representative Drug(s) Mibefradil Drug Info IC50 = 126 nM [7]
Co-Target Name Cytochrome P450 2J2 (CYP2J2) Co-Target
UniProt ID CP2J2_HUMAN
Gene Name CYP2J2
Synonyms
Albendazole monooxygenase (hydroxylating); Albendazole monooxygenase (sulfoxide-forming); Arachidonic acid epoxygenase; Hydroperoxy icosatetraenoate isomerase; CYPIIJ2
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Representative Drug(s) Flunarizine Drug Info Ki = 100 nM [8]
Co-Target Name Brain sodium channel alpha (Types I, II, III) Co-Target
UniProt ID SCN1A_HUMAN; SCN2A_HUMAN; SCN3A_HUMAN
Gene Name SCN1A; SCN2A; SCN3A
Representative Drug(s) Flunarizine Drug Info IC50 = 600 nM [9]
Co-Target Name Sodium channel alpha subunit Co-Target
UniProt ID SCN1A_HUMAN; SCN2A_HUMAN; SCN3A_HUMAN; SCN4A_HUMAN; SCN5A_HUMAN; SCN7A_HUMAN; SCN8A_HUMAN; SCN9A_HUMAN; SCNAA_HUMAN; SCNBA_HUMAN
Gene Name NO-GeName
Representative Drug(s) Mibefradil Drug Info IC50 = 980 nM [10]
References  Top
REF 1 Discovery of N-[[1-[2-(tert-butylcarbamoylamino)ethyl]-4-(hydroxymethyl)-4-piperidyl]methyl]-3,5-dichloro-benzamide as a selective T-type calcium channel (Cav3.2) inhibitor. Bioorg Med Chem Lett. 2013 Jan 1;23(1):119-24.
REF 2 Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies. J Med Chem. 2017 Dec 14;60(23):9769-9789.
REF 3 Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel. J Med Chem. 2007 Jun 28;50(13):2931-41.
REF 4 Discovery of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers. Bioorg Med Chem Lett. 2015 Sep 15;25(18):3941-6.
REF 5 Design, syntheses, and SAR of 2,8-diazaspiro[4.5]decanones as T-type calcium channel antagonists. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6375-8.
REF 6 Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25.
REF 7 Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels. J Med Chem. 2008 Oct 23;51(20):6471-7.
REF 8 Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors. Drug Metab Dispos. 2013 Jan;41(1):60-71.
REF 9 [3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs. J Med Chem. 1985 Mar;28(3):381-8.
REF 10 Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk. Cardiovasc Res. 2011 Jul 1;91(1):53-61.

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