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TargetTransient receptor potential cation channel subfamily V member 1
LigandBDBM20378
Substrate/CompetitorBDBM10852
Meas. Tech.Ca2+ Influx Functional Assay for the Determination of in Vitro Activity.
EC50 29.0±n/a nM
Citation Perner, RJDiDomenico, SKoenig, JRGomtsyan, ABayburt, EKSchmidt, RGDrizin, IZheng, GZTurner, SCJinkerson, TBrown, BSKeddy, RGLukin, KMcDonald, HAHonore, PMikusa, JMarsh, KCWetter, JMGeorge, KSJarvis, MFFaltynek, CRLee, CH In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists. J Med Chem50:3651-60 (2007) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Transient receptor potential cation channel subfamily V member 1
Name:Transient receptor potential cation channel subfamily V member 1
Synonyms:Capsaicin receptor | OTRPC1 | Osm-9-like TRP channel 1 | TRPV1 | TRPV1_HUMAN | Transient receptor potential cation channel subfamily V member 1 | Transient receptor potential cation channel subfamily V member 1 (TRPV1) | Transient receptor potential cation channel subfamily V member 1 (VR1/TRPV1) | Transient receptor potential cation channel subfamily V member 1(TRPV1) | VR1 | Vanilloid VR1 | Vanilloid receptor | Vanilloid receptor 1 | Vanilloid receptor 1 (TrpV1/Vr1) | Vanilloid receptor 1 (VRI/TRPV1)
Type:Protein
Mol. Mass.:94960.75
Organism:Homo sapiens (Human)
Description:Q8NER1
Residue:839
Sequence:
MKKWSSTDLGAAADPLQKDTCPDPLDGDPNSRPPPAKPQLSTAKSRTRLFGKGDSEEAFP
VDCPHEEGELDSCPTITVSPVITIQRPGDGPTGARLLSQDSVAASTEKTLRLYDRRSIFE
AVAQNNCQDLESLLLFLQKSKKHLTDNEFKDPETGKTCLLKAMLNLHDGQNTTIPLLLEI
ARQTDSLKELVNASYTDSYYKGQTALHIAIERRNMALVTLLVENGADVQAAAHGDFFKKT
KGRPGFYFGELPLSLAACTNQLGIVKFLLQNSWQTADISARDSVGNTVLHALVEVADNTA
DNTKFVTSMYNEILMLGAKLHPTLKLEELTNKKGMTPLALAAGTGKIGVLAYILQREIQE
PECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLN
RLLQDKWDRFVKRIFYFNFLVYCLYMIIFTMAAYYRPVDGLPPFKMEKTGDYFRVTGEIL
SVLGGVYFFFRGIQYFLQRRPSMKTLFVDSYSEMLFFLQSLFMLATVVLYFSHLKEYVAS
MVFSLALGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYIVFLFGFSTAVVTLIE
DGKNDSLPSESTSHRWRGPACRPPDSSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVF
IILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKA
FRSGKLLQVGYTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRS
SRVSGRHWKNFALVPLLREASARDRQSAQPEEVYLRQFSGSLKPEDAEVFKSPAASGEK
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BDBM20378
BDBM10852
NameBDBM20378
Synonyms:1-({4-[(1R,5S)-8-azabicyclo[3.2.1]octan-8-yl]-2-methylphenyl}methyl)-3-1H-indazol-4-ylurea | Indazole Analogue, 72
TypeSmall organic molecule
Emp. Form.C23H27N5O
Mol. Mass.389.4934
SMILESCc1cc(ccc1CNC(=O)Nc1cccc2[nH]ncc12)N1[C@H]2CC[C@@H]1CCC2 |r,THB:3:21:27.26.28:23.24|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: