Reaction Details |
| Report a problem with these data |
Target | Sodium channel protein type 10 subunit alpha |
---|
Ligand | BDBM50329209 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_675099 (CHEMBL1272890) |
---|
IC50 | 45±n/a nM |
---|
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 |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Sodium channel protein type 10 subunit alpha |
---|
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
|
|
|
BDBM50329209 |
---|
n/a |
---|
Name | BDBM50329209 |
Synonyms: | 5-(4-chlorophenyl)-N-(2-(piperidin-1-yl)benzyl)nicotinamide | CHEMBL1269990 |
Type | Small organic molecule |
Emp. Form. | C24H24ClN3O |
Mol. Mass. | 405.92 |
SMILES | Clc1ccc(cc1)-c1cncc(c1)C(=O)NCc1ccccc1N1CCCCC1 |
Structure |
|