| Reaction Details |
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 | Report a problem with these data |
| Target | Transient receptor potential cation channel subfamily V member 1 |
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| Ligand | BDBM20334 |
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| Substrate/Competitor | BDBM20458 |
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| Meas. Tech. | Radioligand Binding Assay and Antagonist Ca2+ Influx Functional Assay |
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| pH | 7.4±n/a |
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| Temperature | 298.15±n/a K |
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| Ki | 47±n/a nM |
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| EC50 | 11±1.5 nM |
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| Citation |  Bianchi, BR; El Kouhen, R; Neelands, TR; Lee, CH; Gomtsyan, A; Raja, SN; Vaidyanathan, SN; Surber, B; McDonald, HA; Surowy, CS; Faltynek, CR; Moreland, RB; Jarvis, MF; Puttfarcken, 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 |
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| More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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| Transient receptor potential cation channel subfamily V member 1 |
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| Name: | Transient receptor potential cation channel subfamily V member 1 |
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| 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) |
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| Type: | Protein |
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| Mol. Mass.: | 94960.75 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q8NER1 |
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| Residue: | 839 |
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| Sequence: | MKKWSSTDLGAAADPLQKDTCPDPLDGDPNSRPPPAKPQLSTAKSRTRLFGKGDSEEAFP
VDCPHEEGELDSCPTITVSPVITIQRPGDGPTGARLLSQDSVAASTEKTLRLYDRRSIFE
AVAQNNCQDLESLLLFLQKSKKHLTDNEFKDPETGKTCLLKAMLNLHDGQNTTIPLLLEI
ARQTDSLKELVNASYTDSYYKGQTALHIAIERRNMALVTLLVENGADVQAAAHGDFFKKT
KGRPGFYFGELPLSLAACTNQLGIVKFLLQNSWQTADISARDSVGNTVLHALVEVADNTA
DNTKFVTSMYNEILMLGAKLHPTLKLEELTNKKGMTPLALAAGTGKIGVLAYILQREIQE
PECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLN
RLLQDKWDRFVKRIFYFNFLVYCLYMIIFTMAAYYRPVDGLPPFKMEKTGDYFRVTGEIL
SVLGGVYFFFRGIQYFLQRRPSMKTLFVDSYSEMLFFLQSLFMLATVVLYFSHLKEYVAS
MVFSLALGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYIVFLFGFSTAVVTLIE
DGKNDSLPSESTSHRWRGPACRPPDSSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVF
IILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKA
FRSGKLLQVGYTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRS
SRVSGRHWKNFALVPLLREASARDRQSAQPEEVYLRQFSGSLKPEDAEVFKSPAASGEK
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| BDBM20334 |
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| BDBM20458 |
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| Name | BDBM20334 |
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| Synonyms: | 1-Isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea | 1-isoquinolin-5-yl-3-{[4-(trifluoromethyl)phenyl]methyl}urea | A-425619 | CHEMBL104028 | JMC48744 Compound 14a |
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| Type | Small organic molecule |
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| Emp. Form. | C18H14F3N3O |
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| Mol. Mass. | 345.3185 |
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| SMILES | FC(F)(F)c1ccc(CNC(=O)Nc2cccc3cnccc23)cc1 |
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| Structure | 
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