Reaction Details |
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Target | Sodium channel protein type 10 subunit alpha |
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Ligand | BDBM50371252 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_460715 (CHEMBL926786) |
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IC50 | 1700±n/a nM |
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Citation | Kort, ME; Drizin, I; Gregg, RJ; Scanio, MJ; Shi, L; Gross, MF; Atkinson, RN; Johnson, MS; Pacofsky, GJ; Thomas, JB; Carroll, WA; Krambis, MJ; Liu, D; Shieh, CC; Zhang, X; Hernandez, G; Mikusa, JP; Zhong, C; Joshi, S; Honore, P; Roeloffs, R; Marsh, KC; Murray, BP; Liu, J; Werness, S; Faltynek, CR; Krafte, DS; Jarvis, MF; Chapman, ML; Marron, BE Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. J Med Chem51:407-16 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Sodium channel protein type 10 subunit alpha |
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Name: | Sodium channel protein type 10 subunit alpha |
Synonyms: | SCNAA_MOUSE | Scn10a | Sns | Sodium channel protein type 10 subunit alpha | Sodium channel protein type X alpha subunit |
Type: | PROTEIN |
Mol. Mass.: | 220545.77 |
Organism: | Mus musculus |
Description: | ChEMBL_675096 |
Residue: | 1958 |
Sequence: | MEFPFGSVGTTNFRRFTPESLAEIEKQIAAHRAAKKGRPKQRGQKDKSEKPRPQLDLKAC
NQLPRFYGELPAELVGEPLEDLDPFYSTHRTFIVLDKSRTISRFSATWALWLFSPFNLIR
RTAIKVSVHSWFSIFITVTILVNCVCMTRTDLPEKLEYAFTVVYTFEALIKILARGFCLN
EFTYLRDPWNWLDFSVITLAYVGAAIDLRGISGLRTFRVLRALKTVSVIPGLKVIVGALI
HSVRKLADVTILTVFCLSVFALVGLQLFKGNLKNKCIKNGTDPHKADNLSSEMAGDIFIK
PGTTDPLLCGNGSDAGHCPNDYVCRKTSDNPDFNYTSFDSFAWAFLSLFRLMTQDSWERL
YQQTLRASGKMYMVFFVLVIFLGSFYLVNLILAVVTMAYEEQSQATIAEIEAKEKKFKEA
LEVLQKEQEVLAALGIDTTSLYSHNGSPLAPKNANERRPRVKSRMSEGSTDDNRSLQSDP
YNQRRMSFLGLSSGRRRASHSSVFHFRAPSQDVSFPDGILDDGVFHGDQESRRSSILLGR
GAGQAGPLPRSPLPQSPNPGPRRGEEGQRGVPTGELATGAPEGPALDAAGQKNFLSADYL
NEPFRAQRAMSVVSIMTSVIEELEESKLKCPPCLISLAQKYLIWECCPKWKKFKMVLFEL
VTDPFAELTITLCIVVNTVFMAMEHYPMTDAFDAMLQAGNIVFTVFFTMEMAFKIIAFDP
YYYFQKKWNIFDCVIVTVSLLELSTSKKGSLSVLRTFRLLRVFKLAKSWPTLNMLIKIIG
NSVGALGNLTFILAIIVFIFALVGKQLLSENYGCRRDGISVWNGERLRWHMCDFFHSFLV
VFRILCGEWIENMWVCMEVSQDYICLTLFLTVMVLGNLVVLNLFIALLLNSFSADNLTAP
EDDGEVNNLQVALARIQVFGHRASRAITSYIRSHCRLRWPKVETQLGMKPPLTSCKAENH
IATDAVNAAVGNLAKPALGGPKENHGDFITDPNVWVSVPIAEGESDLDELEEDVEHASQS
SWQEESPKGQQELLQQVQKCEDHQAARSPPSGMSSEDLAPYLGERWQREESPRVPAEGVD
DTSSSEGSTVDCPDPEEILRKIPELAEELDEPDDCFPEGCTRRCPCCKVNTSKFPWATGW
QVRKTCYRIVEHSWFESFIIFMILLSSGALAFEDNYLEEKPRVKSVLEYTDRVFTFIFVF
EMLLKWVAYGFKKYFTNAWCWLDFLIVNISLTSLIAKILEYSDVASIKALRTLRALRPLR
ALSRFEGMRVVVDALVGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFSRCVDTRSNPFS
VVNSTFVTNKSDCYNQNNTGHFFWVNVKVNFDNVAMGYLALLQVATFKGWMDIMYAAVDS
RDINSQPNWEESLYMYLYFVVFIIFGGFFTLNLFVGVIIDNFNQQKKKLGGQDIFMTEEQ
KKYYNAMKKLGSKKPQKPIPRPLNKYQGFVFDIVTRQAFDIIIMALICLNMITMMVETDN
QSEEKTKVLGRINQFFVAVFTGECVMKMFALRQYYFTNGWNVFDFIVVILSISSLLFSAI
LSSLESYFSPTLLRVIRLARIGRILRLIRAAKGIRTLLFALMMSLPALFNIGLLLFLVMF
IYSIFGMASFANVIDEAGIDDMFNFKTFGNSMLCLFQITTSAGWDGLLSPILNTGPPYCD
PNRPNSNGSKGNCGSPAVGILFFTTYIIISFLIVVNMYIAVILENFNVATEESTEPLSED
DFDMFYETWEKFDPEATQFIAFSALSDFADTLSGPLRIPKPNQNILIQMDLPLVPGDKIH
CLDILFAFTKNVLGESGELDSLKTNMEEKFMATNLSKASYEPIATTLRCKQEDISATIIQ
KAYRNYMLQRSLMLSNPLHVPRAEEDGVSLPREGYVTFMANDNGGLPDKSETASATSFPP
SYDSVTRGLSDRANISTSSSMQNEDEVTAKEGKSPGPQ
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BDBM50371252 |
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n/a |
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Name | BDBM50371252 |
Synonyms: | CHEMBL400769 |
Type | Small organic molecule |
Emp. Form. | C19H13ClN2O2 |
Mol. Mass. | 336.772 |
SMILES | Clc1ccc(cc1)-c1ccc(o1)C(=O)Nc1cccc(CC#N)c1 |
Structure |
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