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TargetTransient receptor potential cation channel subfamily V member 1
LigandBDBM20467
Substrate/CompetitorBDBM20458
Meas. Tech.Radioligand Binding Assay and Antagonist Ca2+ Influx Functional Assay
pH7.4±n/a
Temperature298.15±n/a K
Ki 112±22 nM
EC50 34±5 nM
Citation Bianchi, BREl Kouhen, RNeelands, TRLee, CHGomtsyan, ARaja, SNVaidyanathan, SNSurber, BMcDonald, HASurowy, CSFaltynek, CRMoreland, RBJarvis, MFPuttfarcken, PS [3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor. J Pharmacol Exp Ther323:285-93 (2007) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   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 | 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) | TrpV1 | 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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BDBM20467
NameBDBM20467
Synonyms:3-[(1S)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-1-isoquinolin-5-ylurea | A-778316
TypeSmall organic molecule
Emp. Form.C23H25N3O
Mol. Mass.359.4641
SMILESCC(C)(C)c1ccc2[C@H](CCc2c1)NC(=O)Nc1cccc2cnccc12 |r|
Structure
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BDBM20458
NameBDBM20458
Synonyms:1-[(1R)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-3-isoquinolin-5-ylurea | 3-[(1R)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-1-isoquinolin-5-ylurea | A-778317 | Radiolabeled A-778317 | [3H] A-778317
TypeSmall organic molecule
Emp. Form.C23H25N3O
Mol. Mass.359.4641
SMILESCC(C)(C)c1ccc2[C@@H](CCc2c1)NC(=O)Nc1cccc2cnccc12 |r|
Structure
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