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TargetTransient receptor potential cation channel subfamily V member 1
LigandBDBM20285
Substrate/CompetitorBDBM20458
Meas. Tech.Radioligand Binding Assay and Agonist Ca2+ Influx Functional Assay
pH7.4±n/a
Temperature298.15±n/a K
Ki 65±36 nM
EC50 24±16 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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BDBM20285
NameBDBM20285
Synonyms:Resiniferatoxin | [(1R,2R,6R,10S,11R,15R,17R)-13-benzyl-6-hydroxy-4,17-dimethyl-5-oxo-15-(prop-1-en-2-yl)-12,14,18-trioxapentacyclo[11.4.1.0^{1,10}.0^{2,6}.0^{11,15}]octadeca-3,8-dien-8-yl]methyl 2-(4-hydroxy-3-methoxyphenyl)acetate
TypeSmall organic molecule
Emp. Form.C37H40O9
Mol. Mass.628.7081
SMILES[H][C@]12OC3(Cc4ccccc4)O[C@]1(C[C@@H](C)[C@]1(O3)[C@]3([H])C=C(C)C(=O)[C@@]3(O)CC(COC(=O)Cc3ccc(O)c(OC)c3)=C[C@@]21[H])C(C)=C |c:47,t:23,TLB:11:3:12.14.13:44,THB:4:3:12.14.13:44|
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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