Reaction Details |
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Target | Sodium channel protein type 10 subunit alpha |
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Ligand | BDBM50329218 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_675096 (CHEMBL1272887) |
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IC50 | 280±n/a nM |
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Citation | Kort, ME; Atkinson, RN; Thomas, JB; Drizin, I; Johnson, MS; Secrest, MA; Gregg, RJ; Scanio, MJ; Shi, L; Hakeem, AH; Matulenko, MA; Chapman, ML; Krambis, MJ; Liu, D; Shieh, CC; Zhang, X; Simler, G; Mikusa, JP; Zhong, C; Joshi, S; Honore, P; Roeloffs, R; Werness, S; Antonio, B; Marsh, KC; Faltynek, CR; Krafte, DS; Jarvis, MF; Marron, BE Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. Bioorg Med Chem Lett20:6812-5 (2010) [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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BDBM50329218 |
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n/a |
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Name | BDBM50329218 |
Synonyms: | CHEMBL1271105 | N-(3,5-dimethylphenyl)-5-(4-(trifluoromethoxy)phenyl)-1,2,4-thiadiazole-3-carboxamide |
Type | Small organic molecule |
Emp. Form. | C18H14F3N3O2S |
Mol. Mass. | 393.383 |
SMILES | Cc1cc(C)cc(NC(=O)c2nsc(n2)-c2ccc(OC(F)(F)F)cc2)c1 |
Structure |
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