Target Information
Target General Infomation | |||||
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Target ID |
T12119
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Former ID |
TTDS00503
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Target Name |
Voltage-gated sodium channel subunit alpha Nav1.7
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Gene Name |
SCN9A
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Synonyms |
Neuroendocrine sodium channel; Peripheral sodium channel 1; Sodium channel proteintype 9 subunit alpha; Sodium channel proteintype IX subunit alpha; hNE-Na; SCN9A
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Target Type |
Clinical Trial
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Disease | Asthma [ICD10: J45] | ||||
Chronic pain [ICD9: 338.2,780; ICD10: R52.1-R52.2, G89] | |||||
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 channelthrough which na+ ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-sensitive na+ channel isoform. Plays a role in pain mechanisms, especially in the development of inflammatory pain.
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BioChemical Class |
Voltage-gated ion channel
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Target Validation |
T12119
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UniProt ID | |||||
Sequence |
MAMLPPPGPQSFVHFTKQSLALIEQRIAERKSKEPKEEKKDDDEEAPKPSSDLEAGKQLP
FIYGDIPPGMVSEPLEDLDPYYADKKTFIVLNKGKTIFRFNATPALYMLSPFSPLRRISI KILVHSLFSMLIMCTILTNCIFMTMNNPPDWTKNVEYTFTGIYTFESLVKILARGFCVGE FTFLRDPWNWLDFVVIVFAYLTEFVNLGNVSALRTFRVLRALKTISVIPGLKTIVGALIQ SVKKLSDVMILTVFCLSVFALIGLQLFMGNLKHKCFRNSLENNETLESIMNTLESEEDFR KYFYYLEGSKDALLCGFSTDSGQCPEGYTCVKIGRNPDYGYTSFDTFSWAFLALFRLMTQ DYWENLYQQTLRAAGKTYMIFFVVVIFLGSFYLINLILAVVAMAYEEQNQANIEEAKQKE LEFQQMLDRLKKEQEEAEAIAAAAAEYTSIRRSRIMGLSESSSETSKLSSKSAKERRNRR KKKNQKKLSSGEEKGDAEKLSKSESEDSIRRKSFHLGVEGHRRAHEKRLSTPNQSPLSIR GSLFSARRSSRTSLFSFKGRGRDIGSETEFADDEHSIFGDNESRRGSLFVPHRPQERRSS NISQASRSPPMLPVNGKMHSAVDCNGVVSLVDGRSALMLPNGQLLPEVIIDKATSDDSGT TNQIHKKRRCSSYLLSEDMLNDPNLRQRAMSRASILTNTVEELEESRQKCPPWWYRFAHK FLIWNCSPYWIKFKKCIYFIVMDPFVDLAITICIVLNTLFMAMEHHPMTEEFKNVLAIGN LVFTGIFAAEMVLKLIAMDPYEYFQVGWNIFDSLIVTLSLVELFLADVEGLSVLRSFRLL RVFKLAKSWPTLNMLIKIIGNSVGALGNLTLVLAIIVFIFAVVGMQLFGKSYKECVCKIN DDCTLPRWHMNDFFHSFLIVFRVLCGEWIETMWDCMEVAGQAMCLIVYMMVMVIGNLVVL NLFLALLLSSFSSDNLTAIEEDPDANNLQIAVTRIKKGINYVKQTLREFILKAFSKKPKI SREIRQAEDLNTKKENYISNHTLAEMSKGHNFLKEKDKISGFGSSVDKHLMEDSDGQSFI HNPSLTVTVPIAPGESDLENMNAEELSSDSDSEYSKVRLNRSSSSECSTVDNPLPGEGEE AEAEPMNSDEPEACFTDGCVWRFSCCQVNIESGKGKIWWNIRKTCYKIVEHSWFESFIVL MILLSSGALAFEDIYIERKKTIKIILEYADKIFTYIFILEMLLKWIAYGYKTYFTNAWCW LDFLIVDVSLVTLVANTLGYSDLGPIKSLRTLRALRPLRALSRFEGMRVVVNALIGAIPS IMNVLLVCLIFWLIFSIMGVNLFAGKFYECINTTDGSRFPASQVPNRSECFALMNVSQNV RWKNLKVNFDNVGLGYLSLLQVATFKGWTIIMYAAVDSVNVDKQPKYEYSLYMYIYFVVF IIFGSFFTLNLFIGVIIDNFNQQKKKLGGQDIFMTEEQKKYYNAMKKLGSKKPQKPIPRP GNKIQGCIFDLVTNQAFDISIMVLICLNMVTMMVEKEGQSQHMTEVLYWINVVFIILFTG ECVLKLISLRHYYFTVGWNIFDFVVVIISIVGMFLADLIETYFVSPTLFRVIRLARIGRI LRLVKGAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYAIFGMSNFAYVKKEDGINDMFN FETFGNSMICLFQITTSAGWDGLLAPILNSKPPDCDPKKVHPGSSVEGDCGNPSVGIFYF VSYIIISFLVVVNMYIAVILENFSVATEESTEPLSEDDFEMFYEVWEKFDPDATQFIEFS KLSDFAAALDPPLLIAKPNKVQLIAMDLPMVSGDRIHCLDILFAFTKRVLGESGEMDSLR SQMEERFMSANPSKVSYEPITTTLKRKQEDVSATVIQRAYRRYRLRQNVKNISSIYIKDG DRDDDLLNKKDMAFDNVNENSSPEKTDATSSTTSPPSYDSVTKPDKEKYEQDRTEKEDKG KDSKESKK |
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Drugs and Mode of Action | |||||
Drug(s) | PF-05089771 | Drug Info | Phase 2 | Chronic pain | [523792] |
XEN-402 | Drug Info | Phase 2 | Pain | [523154] | |
PF-05186462 | Drug Info | Phase 1 | Pain | [523119] | |
PF-05241328 | Drug Info | Phase 1 | Pain | [523119] | |
RG7893 | Drug Info | Phase 1 | Pain | [549579] | |
Corus 1030 | Drug Info | Discontinued in Phase 2 | Asthma | [547604] | |
SIPATRIGINE | Drug Info | Discontinued in Phase 2 | Neurological disease | [545614] | |
V-102862 | Drug Info | Discontinued in Phase 1 | Discovery agent | [546691] | |
Inhibitor | 4-(2'-(trifluoromethoxy)biphenyl-3-yl)oxazole | Drug Info | [531103] | ||
4-(2'-(trifluoromethoxy)biphenyl-3-yl)thiazole | Drug Info | [531103] | |||
4-(2'-(trifluoromethyl)biphenyl-3-yl)oxazole | Drug Info | [531103] | |||
PF-05186462 | Drug Info | [548599] | |||
PF-05241328 | Drug Info | [532897] | |||
RG7893 | Drug Info | [549580], [551871] | |||
SIPATRIGINE | Drug Info | [530055] | |||
V-102862 | Drug Info | [531103] | |||
XEN-402 | Drug Info | [531677] | |||
XEN-907 | Drug Info | [543884] | |||
Activator | batrachotoxin | Drug Info | [543884] | ||
veratridine | Drug Info | [543884] | |||
Modulator | Corus 1030 | Drug Info | [527078] | ||
Inhibitor (gating inhibitor) | N-Me-aminopyrimidinone 9 | Drug Info | [531752] | ||
Blocker | PF-05089771 | Drug Info | [533324] | ||
Blocker (channel blocker) | pyrrolopyrimidine 48 | Drug Info | [531793] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
Pathways | |||||
Reactome | Interaction between L1 and Ankyrins | ||||
References | |||||
Ref 523119 | ClinicalTrials.gov (NCT01165736) To Calculate the Pharmacokinetics (Concentration of Compound in and Rate of Excretion From the Blood) Following a Very Low Dose of Compound Which Will Not Have Any Pharmacological Activity. U.S. National Institutes of Health. | ||||
Ref 523154 | ClinicalTrials.gov (NCT01195636) A Crossover Study to Evaluate the Safety, Tolerability and Efficacy of XPF-002 in Subjects With Postherpetic Neuralgia (PHN). U.S. National Institutes of Health. | ||||
Ref 523792 | ClinicalTrials.gov (NCT01529346) Efficacy Of PF-05089771 In Treating Postoperative Dental Pain. U.S. National Institutes of Health. | ||||
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 546691 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009655) | ||||
Ref 527078 | Differential modulation of Nav1.7 and Nav1.8 peripheral nerve sodium channels by the local anesthetic lidocaine. Br J Pharmacol. 2004 Jun;142(3):576-84. Epub 2004 May 17. | ||||
Ref 530055 | J Med Chem. 2009 May 14;52(9):2694-707.Oxadiazolylindazole sodium channel modulators are neuroprotective toward hippocampal neurones. | ||||
Ref 531103 | Bioorg Med Chem Lett. 2010 Sep 15;20(18):5536-40. Epub 2010 Jul 21.Substituted biaryl oxazoles, imidazoles, and thiazoles as sodium channel blockers. | ||||
Ref 531677 | Treatment of Na(v)1.7-mediated pain in inherited erythromelalgia using a novel sodium channel blocker. Pain. 2012 Jan;153(1):80-5. | ||||
Ref 531752 | Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1055-60. | ||||
Ref 531793 | Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Na(v)1.7 antagonists. Bioorg Med Chem Lett. 2012 Mar 1;22(5):2052-62. | ||||
Ref 532897 | Recent progress in sodium channel modulators for pain. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3690-9. | ||||
Ref 543884 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 584). | ||||
Ref 548599 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026875) |
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