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TargetVanilloid receptor
LigandBDBM20291
Substrate/CompetitorBDBM20285
Meas. Tech.Competition Binding Assay and Inhibition of Ca2+ Uptake Assay
pH7.4±n/a
Temperature310.15±n/a K
Ki 3.6±1.2 nM
EC50 12.3±4.7 nM
Citation Ryu HJin MKKim SYChoi HKKang SUKang DWLee JPearce LVPavlyukovets VAMorgan MATran RToth ALundberg DJBlumberg PM Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-Benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues. J Med Chem 51:57-67 (2008) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
Vanilloid receptor
Name:Vanilloid receptor
Synonyms:Capsaicin receptor | OTRPC1 | Transient receptor potential cation channel subfamily V member 1 (TRPV1) | Vanilloid Receptor 1 (TRPV1, VR1) | Vanilloid VR1 | Vanilloid receptor 1 (VRI/TRPV1) | Vanilloid receptor type 1-like | Vanilloid receptor type 1-like (TrpV1/Vr1) | osm-9-like TRP channel 1
Type:Transient Receptor
Mol. Mass.:94956.12
Organism:Rattus norvegicus (rat)
Description:O35433
Residue:838
Sequence:
MEQRASLDSEESESPPQENSCLDPPDRDPNCKPPPVKPHIFTTRSRTRLFGKGDSEEASP
LDCPYEEGGLASCPIITVSSVLTIQRPGDGPASVRPSSQDSVSAGEKPPRLYDRRSIFDA
VAQSNCQELESLLPFLQRSKKRLTDSEFKDPETGKTCLLKAMLNLHNGQNDTIALLLDVA
RKTDSLKQFVNASYTDSYYKGQTALHIAIERRNMTLVTLLVENGADVQAAANGDFFKKTK
GRPGFYFGELPLSLAACTNQLAIVKFLLQNSWQPADISARDSVGNTVLHALVEVADNTVD
NTKFVTSMYNEILILGAKLHPTLKLEEITNRKGLTPLALAASSGKIGVLAYILQREIHEP
ECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLNR
LLQDKWDRFVKRIFYFNFFVYCLYMIIFTAAAYYRPVEGLPPYKLKNTVGDYFRVTGEIL
SVSGGVYFFFRGIQYFLQRRPSLKSLFVDSYSEILFFVQSLFMLVSVVLYFSQRKEYVAS
MVFSLAMGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYLVFLFGFSTAVVTLIE
DGKNNSLPMESTPHKCRGSACKPGNSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVFI
ILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKAF
RSGKLLQVGFTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRSG
RVSGRNWKNFALVPLLRDASTRDRHATQQEEVQLKHYTGSLKPEDAEVFKDSMVPGEK
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BDBM20291
BDBM20285
NameBDBM20291
Synonyms:2-[(4-tert-butylphenyl)methyl]-3-[2-(3-chloro-4-methanesulfonamidophenyl)propanamido]propyl 2,2-dimethylpropanoate | alpha-methyl amide analogue, 11
TypeSmall organic molecule
Emp. Form.C29H41ClN2O5S
Mol. Mass.565.164
SMILESCC(C(=O)NCC(COC(=O)C(C)(C)C)Cc1ccc(cc1)C(C)(C)C)c1ccc(NS(C)(=O)=O)c(Cl)c1
Structure
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