Target Information
Target General Infomation | |||||
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Target ID |
T76937
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Former ID |
TTDR01255
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Target Name |
Voltage-gated sodium channel subunit alpha Nav1.3
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Gene Name |
SCN3A
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Synonyms |
KIAA1356; NAC3; Sodium channel protein type 3 subunit alpha; Sodium channel protein type III subunit alpha; Sodium channel protein, brain III subunit alpha; Voltage-gated sodium channel subtype III; SCN3A
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Target Type |
Successful
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Disease | Angina pectoris [ICD9: 413; ICD10: I20] | ||||
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Function |
Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na+ ions may pass in accordance with their electrochemical gradient.
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BioChemical Class |
Sodium channel
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Target Validation |
T76937
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UniProt ID | |||||
Sequence |
MAQALLVPPGPESFRLFTRESLAAIEKRAAEEKAKKPKKEQDNDDENKPKPNSDLEAGKN
LPFIYGDIPPEMVSEPLEDLDPYYINKKTFIVMNKGKAIFRFSATSALYILTPLNPVRKI AIKILVHSLFSMLIMCTILTNCVFMTLSNPPDWTKNVEYTFTGIYTFESLIKILARGFCL EDFTFLRDPWNWLDFSVIVMAYVTEFVSLGNVSALRTFRVLRALKTISVIPGLKTIVGAL IQSVKKLSDVMILTVFCLSVFALIGLQLFMGNLRNKCLQWPPSDSAFETNTTSYFNGTMD SNGTFVNVTMSTFNWKDYIGDDSHFYVLDGQKDPLLCGNGSDAGQCPEGYICVKAGRNPN YGYTSFDTFSWAFLSLFRLMTQDYWENLYQLTLRAAGKTYMIFFVLVIFLGSFYLVNLIL AVVAMAYEEQNQATLEEAEQKEAEFQQMLEQLKKQQEEAQAVAAASAASRDFSGIGGLGE LLESSSEASKLSSKSAKEWRNRRKKRRQREHLEGNNKGERDSFPKSESEDSVKRSSFLFS MDGNRLTSDKKFCSPHQSLLSIRGSLFSPRRNSKTSIFSFRGRAKDVGSENDFADDEHST FEDSESRRDSLFVPHRHGERRNSNVSQASMSSRMVPGLPANGKMHSTVDCNGVVSLVGGP SALTSPTGQLPPEGTTTETEVRKRRLSSYQISMEMLEDSSGRQRAVSIASILTNTMEELE ESRQKCPPCWYRFANVFLIWDCCDAWLKVKHLVNLIVMDPFVDLAITICIVLNTLFMAME HYPMTEQFSSVLTVGNLVFTGIFTAEMVLKIIAMDPYYYFQEGWNIFDGIIVSLSLMELG LSNVEGLSVLRSFRLLRVFKLAKSWPTLNMLIKIIGNSVGALGNLTLVLAIIVFIFAVVG MQLFGKSYKECVCKINDDCTLPRWHMNDFFHSFLIVFRVLCGEWIETMWDCMEVAGQTMC LIVFMLVMVIGNLVVLNLFLALLLSSFSSDNLAATDDDNEMNNLQIAVGRMQKGIDYVKN KMRECFQKAFFRKPKVIEIHEGNKIDSCMSNNTGIEISKELNYLRDGNGTTSGVGTGSSV EKYVIDENDYMSFINNPSLTVTVPIAVGESDFENLNTEEFSSESELEESKEKLNATSSSE GSTVDVVLPREGEQAETEPEEDLKPEACFTEGCIKKFPFCQVSTEEGKGKIWWNLRKTCY SIVEHNWFETFIVFMILLSSGALAFEDIYIEQRKTIKTMLEYADKVFTYIFILEMLLKWV AYGFQTYFTNAWCWLDFLIVDVSLVSLVANALGYSELGAIKSLRTLRALRPLRALSRFEG MRVVVNALVGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFYHCVNMTTGNMFDISDVNN LSDCQALGKQARWKNVKVNFDNVGAGYLALLQVATFKGWMDIMYAAVDSRDVKLQPVYEE NLYMYLYFVIFIIFGSFFTLNLFIGVIIDNFNQQKKKFGGQDIFMTEEQKKYYNAMKKLG SKKPQKPIPRPANKFQGMVFDFVTRQVFDISIMILICLNMVTMMVETDDQGKYMTLVLSR INLVFIVLFTGEFVLKLVSLRHYYFTIGWNIFDFVVVILSIVGMFLAEMIEKYFVSPTLF RVIRLARIGRILRLIKGAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYAIFGMSNFAYV KKEAGIDDMFNFETFGNSMICLFQITTSAGWDGLLAPILNSAPPDCDPDTIHPGSSVKGD CGNPSVGIFFFVSYIIISFLVVVNMYIAVILENFSVATEESAEPLSEDDFEMFYEVWEKF DPDATQFIEFSKLSDFAAALDPPLLIAKPNKVQLIAMDLPMVSGDRIHCLDILFAFTKRV LGESGEMDALRIQMEDRFMASNPSKVSYEPITTTLKRKQEEVSAAIIQRNFRCYLLKQRL KNISSNYNKEAIKGRIDLPIKQDMIIDKLNGNSTPEKTDGSSSTTSPPSYDSVTKPDKEK FEKDKPEKESKGKEVRENQK |
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Structure |
1BYY
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Drugs and Mode of Action | |||||
Inhibitor | 2-(1-Pentyl-hexyl)-4-phenyl-1H-imidazole | Drug Info | [527102] | ||
2-Hexyl-4-(4-isobutyl-phenyl)-1H-imidazole | Drug Info | [527102] | |||
2-Hydroxy-2-phenyl-nonanoic acid amide | Drug Info | [525483] | |||
4-Biphenyl-4-yl-2-(1-pentyl-hexyl)-1H-imidazole | Drug Info | [527102] | |||
4-Biphenyl-4-yl-2-(1-propyl-butyl)-1H-imidazole | Drug Info | [527102] | |||
4-Biphenyl-4-yl-2-cyclohexylmethyl-1H-imidazole | Drug Info | [527102] | |||
4-Biphenyl-4-yl-2-hexyl-1H-imidazole | Drug Info | [527102] | |||
4-Biphenyl-4-yl-2-methyl-1H-imidazole | Drug Info | [527102] | |||
5-Ethyl-3-methyl-5-phenyl-oxazolidine-2,4-dione | Drug Info | [533048] | |||
5-Heptyl-5-phenyl-imidazolidine-2,4-dione | Drug Info | [525483] | |||
5-Hexyl-5-phenyl-imidazolidine-2,4-dione | Drug Info | [525483] | |||
5-Nonyl-5-phenyl-imidazolidine-2,4-dione | Drug Info | [525483] | |||
BW-202W92 | Drug Info | [530055] | |||
CCNCSSKWCRDHSRCC | Drug Info | [529000] | |||
L-741742 | Drug Info | [525540] | |||
LIDOFLAZINE | Drug Info | [533974] | |||
PD-85639 | Drug Info | [533974] | |||
SIPATRIGINE | Drug Info | [526398] | |||
U-92032 | Drug Info | [525864] | |||
Activator | batrachotoxin | Drug Info | [543881] | ||
veratridine | Drug Info | [543881] | |||
Antagonist | RQ-00203066 | Drug Info | [543881] | ||
Pathways | |||||
Reactome | Interaction between L1 and Ankyrins | ||||
References | |||||
Ref 545294 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002730) | ||||
Ref 545614 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003904) | ||||
Ref 525483 | J Med Chem. 1999 May 6;42(9):1537-45.Comparative molecular field analysis of hydantoin binding to the neuronal voltage-dependent sodium channel. | ||||
Ref 525540 | J Med Chem. 1999 Jul 15;42(14):2706-15.1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels. | ||||
Ref 525864 | J Med Chem. 2000 Sep 7;43(18):3372-6.Discovery of (2S)-1-(4-amino-2,3,5- trimethylphenoxy)-3-[4-[4-(4- fluorobenzyl)phenyl]-1-piperazinyl]-2-propanol dimethanesulfonate (SUN N8075): a dual Na(+) and Ca(2+) channel blocker with antioxidant activity. | ||||
Ref 526398 | J Med Chem. 2002 Aug 15;45(17):3755-64.Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke. | ||||
Ref 527102 | Bioorg Med Chem Lett. 2004 Jul 5;14(13):3521-3.2-Alkyl-4-arylimidazoles: structurally novel sodium channel modulators. | ||||
Ref 529000 | J Biol Chem. 2007 Oct 19;282(42):30699-706. Epub 2007 Aug 27.Structure/function characterization of micro-conotoxin KIIIA, an analgesic, nearly irreversible blocker of mammalian neuronal sodium channels. | ||||
Ref 530055 | J Med Chem. 2009 May 14;52(9):2694-707.Oxadiazolylindazole sodium channel modulators are neuroprotective toward hippocampal neurones. | ||||
Ref 533048 | J Med Chem. 1989 Jul;32(7):1577-80.Sodium channel binding and anticonvulsant activities for the enantiomers of a bicyclic 2,4-oxazolidinedione and monocyclic models. |
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