Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T45993 | Target Info | |||
| Target Name | Calcium channel unspecific (CaC) | ||||
| Target Type | Successful Target | ||||
| Gene Name | NO-GeName | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Voltage-gated L-type calcium channel (L-CaC) | Successful Target | ||||
| UniProt ID | CAC1C_HUMAN; CAC1D_HUMAN; CAC1F_HUMAN; CAC1S_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Synonyms |
L-type voltage-dependent Ca(2+) channel; L-type Ca2+ channel; L-type Ca(2+) channel
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| Representative Drug(s) | Nisoldipine | Drug Info | IC50 = 0.015 nM | Click to Show More | [1] | |
| 2 | Bepridil | Drug Info | IC50 = 1000 nM | [5] | ||
| 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) | Bepridil | Drug Info | IC50 = 22.91 nM | [2] | ||
| Co-Target Name | S-mephenytoin 4-hydroxylase (CYP2C9) | Successful Target | ||||
| UniProt ID | CP2C9_HUMAN | |||||
| Gene Name | CYP2C9 | |||||
| Synonyms |
Cytochrome P450 PB-1; Cytochrome P450 MP-8; Cytochrome P450 MP-4; Cytochrome P450 2C9; Cytochrome P-450MP; Cholesterol 25-hydroxylase; CYPIIC9; CYP2C10; (S)-limonene 7-monooxygenase; (S)-limonene 6-monooxygenase; (R)-limonene 6-monooxygenase
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| Representative Drug(s) | Nicardipine | Drug Info | Ki = 280 nM | [3] | ||
| Co-Target Name | Multidrug resistance protein 1 (ABCB1) | Clinical trial Target | ||||
| UniProt ID | MDR1_HUMAN | |||||
| Gene Name | ABCB1 | |||||
| Synonyms |
PGY1; P-glycoprotein 1; MDR1; CD243 antigen; CD243; ATP-binding cassette sub-family B member 1
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| Representative Drug(s) | Nicardipine | Drug Info | IC50 = 950 nM | [4] | ||
| 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) | Nicardipine | Drug Info | IC50 = 380 nM | [6] | ||
| Co-Target Name | Cytochrome P450 2C19 (CYP2C19) | Co-Target | ||||
| UniProt ID | CP2CJ_HUMAN | |||||
| Gene Name | CYP2C19 | |||||
| Synonyms |
Fenbendazole monooxygenase (4'-hydroxylating); (R)-limonene 6-monooxygenase; (S)-limonene 6-monooxygenase; (S)-limonene 7-monooxygenase; CYPIIC17; CYPIIC19; Cytochrome P450-11A; Cytochrome P450-254C; Mephenytoin 4-hydroxylase
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| Representative Drug(s) | Bepridil | Drug Info | IC50 < 100 nM | Click to Show More | [7] | |
| 2 | Nicardipine | Drug Info | IC50 = 560 nM | [6] | ||
| 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) | Bepridil | Drug Info | IC50 = 840 nM | [8] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Crystal structures and pharmacologic activities of 1,4-dihydropyridine calcium channel antagonists of the isobutyl methyl 2,6-dimethyl-4-(substituted phenyl)-1,4-dihydropyridine-3,5-dicarboxylate (nisoldipine) series. J Med Chem. 1988 Feb;31(2):300-5. | ||||
| REF 2 | Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. Eur J Med Chem. 2011 Feb;46(2):618-30. | ||||
| REF 3 | Conformer- and alignment-independent model for predicting structurally diverse competitive CYP2C9 inhibitors. J Med Chem. 2004 Feb 12;47(4):907-14. | ||||
| REF 4 | 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 5 | MICE models: superior to the HERG model in predicting Torsade de Pointes. Sci Rep. 2013;3:2100. | ||||
| REF 6 | Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors. Drug Metab Dispos. 2013 Jan;41(1):60-71. | ||||
| REF 7 | Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. Drug Metab Dispos. 2012 May;40(5):943-51. | ||||
| REF 8 | [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. | ||||
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