Reaction Details |
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Target | Sodium channel protein type 10 subunit alpha |
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Ligand | BDBM50330948 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_684073 (CHEMBL1286450) |
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IC50 | 19±n/a nM |
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Citation | Scanio, MJ; Shi, L; Drizin, I; Gregg, RJ; Atkinson, RN; Thomas, JB; Johnson, MS; Chapman, ML; Liu, D; Krambis, MJ; Liu, Y; Shieh, CC; Zhang, X; Simler, GH; Joshi, S; Honore, P; Marsh, KC; Knox, A; Werness, S; Antonio, B; Krafte, DS; Jarvis, MF; Faltynek, CR; Marron, BE; Kort, ME Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain. Bioorg Med Chem18:7816-25 (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_RAT | Scn10a | Sns | Sodium Channel | Sodium channel protein type X alpha subunit | Voltage-gated sodium channel subunit alpha Nav1.8 |
Type: | Enzyme |
Mol. Mass.: | 219724.17 |
Organism: | Rattus norvegicus (Rat) |
Description: | Q62968 |
Residue: | 1956 |
Sequence: | MELPFASVGTTNFRRFTPESLAEIEKQIAAHRAAKKARTKHRGQEDKGEKPRPQLDLKAC
NQLPKFYGELPAELVGEPLEDLDPFYSTHRTFMVLNKSRTISRFSATWALWLFSPFNLIR
RTAIKVSVHSWFSIFITITILVNCVCMTRTDLPEKVEYVFTVIYTFEALIKILARGFCLN
EFTYLRDPWNWLDFSVITLAYVGAAIDLRGISGLRTFRVLRALKTVSVIPGLKVIVGALI
HSVRKLADVTILTVFCLSVFALVGLQLFKGNLKNKCIRNGTDPHKADNLSSEMAEYIFIK
PGTTDPLLCGNGSDAGHCPGGYVCLKTPDNPDFNYTSFDSFAWAFLSLFRLMTQDSWERL
YQQTLRASGKMYMVFFVLVIFLGSFYLVNLILAVVTMAYEEQSQATIAEIEAKEKKFQEA
LEVLQKEQEVLAALGIDTTSLQSHSGSPLASKNANERRPRVKSRVSEGSTDDNRSPQSDP
YNQRRMSFLGLSSGRRRASHGSVFHFRAPSQDISFPDGITDDGVFHGDQESRRGSILLGR
GAGQTGPLPRSPLPQSPNPGRRHGEEGQLGVPTGELTAGAPEGPALDTTGQKSFLSAGYL
NEPFRAQRAMSVVSIMTSVIEELEESKLKCPPCLISFAQKYLIWECCPKWRKFKMALFEL
VTDPFAELTITLCIVVNTVFMAMEHYPMTDAFDAMLQAGNIVFTVFFTMEMAFKIIAFDP
YYYFQKKWNIFDCVIVTVSLLELSASKKGSLSVLRTFRLLRVFKLAKSWPTLNTLIKIIG
NSVGALGNLTFILAIIVFIFALVGKQLLSEDYGCRKDGVSVWNGEKLRWHMCDFFHSFLV
VFRILCGEWIENMWVCMEVSQKSICLILFLTVMVLGNLVVLNLFIALLLNSFSADNLTAP
EDDGEVNNLQLALARIQVLGHRASRAIASYISSHCRFRWPKVETQLGMKPPLTSSEAKNH
IATDAVSAAVGNLTKPALSSPKENHGDFITDPNVWVSVPIAEGESDLDELEEDMEQASQS
SWQEEDPKGQQEQLPQVQKCENHQAARSPASMMSSEDLAPYLGESWKRKDSPQVPAEGVD
DTSSSEGSTVDCPDPEEILRKIPELADDLDEPDDCFTEGCTRRCPCCNVNTSKSPWATGW
QVRKTCYRIVEHSWFESFIIFMILLSSGALAFEDNYLEEKPRVKSVLEYTDRVFTFIFVF
EMLLKWVAYGFKKYFTNAWCWLDFLIVNISLTSLIAKILEYSDVASIKALRTLRALRPLR
ALSRFEGMRVVVDALVGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFSKCVDTRNNPFS
NVNSTMVNNKSECHNQNSTGHFFWVNVKVNFDNVAMGYLALLQVATFKGWMDIMYAAVDS
GEINSQPNWENNLYMYLYFVVFIIFGGFFTLNLFVGVIIDNFNQQKKKLGGQDIFMTEEQ
KKYYNAMKKLGSKKPQKPIPRPLNKYQGFVFDIVTRQAFDIIIMVLICLNMITMMVETDE
QGEEKTKVLGRINQFFVAVFTGECVMKMFALRQYYFTNGWNVFDFIVVILSIGSLLFSAI
LKSLENYFSPTLFRVIRLARIGRILRLIRAAKGIRTLLFALMMSLPALFNIGLLLFLVMF
IYSIFGMASFANVVDEAGIDDMFNFKTFGNSMLCLFQITTSAGWDGLLSPILNTGPPYCD
PNLPNSNGSRGNCGSPAVGIIFFTTYIIISFLIVVNMYIAVILENFNVATEESTEPLSED
DFDMFYETWEKFDPEATQFIAFSALSDFADTLSGPLRIPKPNQNILIQMDLPLVPGDKIH
CLDILFAFTKNVLGESGELDSLKTNMEEKFMATNLSKASYEPIATTLRWKQEDLSATVIQ
KAYRSYMLHRSLTLSNTLHVPRAEEDGVSLPGEGYVTFMANSGLPDKSETASATSFPPSY
DSVTRGLSDRANINPSSSMQNEDEVAAKEGNSPGPQ
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BDBM50330948 |
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n/a |
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Name | BDBM50330948 |
Synonyms: | CHEMBL1277959 | N-(2-Methylbenzyl)-6-(4-ethoxyphenyl)-pyrazine-2-carboxamide |
Type | Small organic molecule |
Emp. Form. | C21H21N3O2 |
Mol. Mass. | 347.4103 |
SMILES | CCOc1ccc(cc1)-c1cncc(n1)C(=O)NCc1ccccc1C |
Structure |
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