Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T84316 Target Info
Target Name Voltage-gated calcium channel alpha-2/delta-1 (CACNA2D1)
Synonyms
Voltage-gated calcium channel subunit alpha-2/delta-1; Voltage-dependent calcium channel subunit delta-1; Voltage-dependent calcium channel subunit alpha-2-1; MHS3; CCHL2A; CACNL2A; CACNA2D1
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Target Type Successful Target
Gene Name CACNA2D1
Biochemical Class Voltage-gated ion channel
UniProt ID
CA2D1_HUMAN
Co-Targets of This Target  Top
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) Diltiazem Drug Info IC50 = 100 nM [1]
Co-Target Name Voltage-gated calcium channel alpha Cav1.1 (CACNA1S) Literature-reported Target
UniProt ID CAC1S_HUMAN
Gene Name CACNA1S
Synonyms
Voltage-gated calcium channel subunit alpha Cav1.1; Voltage-dependent L-type calcium channel subunit alpha-1S; Calcium channel, L type, alpha-1 polypeptide, isoform 3, skeletal muscle; CACNL1A3; CACN1; CACH1
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Representative Drug(s) Diltiazem Drug Info Ki = 380 nM [2]
Co-Target Name Potassium channel subfamily K member 2 (KCNK2) Co-Target
UniProt ID KCNK2_HUMAN
Gene Name KCNK2
Synonyms
Outward rectifying potassium channel protein TREK-1; TREK-1 K(+) channel subunit; Two pore domain potassium channel TREK-1; Two pore potassium channel TPKC1
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Representative Drug(s) Amlodipine Drug Info IC50 = 400 nM [3]
References  Top
REF 1 Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. Drug Metab Dispos. 2012 Jul;40(7):1429-40
REF 2 (cis)-3-methyl-1,5-benzothiazepine-4-ones: potent analogs of the calcium channel blocker diltiazen. Bioorg Med Chem Lett. 1993 Dec;3(12):2797-800.
REF 3 Ion channels as therapeutic targets: a drug discovery perspective. J Med Chem. 2013 Feb 14;56(3):593-624.

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