| 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 | BDBM20387 |
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| Substrate/Competitor | BDBM10852 |
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| Meas. Tech. | Ca2+ Influx Functional Assay for the Determination of in Vitro Activity. |
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| pH | 7.4±n/a |
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| Temperature | 295.15±n/a K |
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| EC50 | 147±21 nM |
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| Citation |  Gomtsyan, A; Bayburt, EK; Keddy, R; Turner, SC; Jinkerson, TK; Didomenico, S; Perner, RJ; Koenig, JR; Drizin, I; McDonald, HA; Surowy, CS; Honore, P; Mikusa, J; Marsh, KC; Wetter, JM; Faltynek, CR; Lee, CH Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model. Bioorg Med Chem Lett17:3894-9 (2007) [PubMed] Article |
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| More Info.: | Get all data from this article, 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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| BDBM20387 |
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| BDBM10852 |
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| Name | BDBM20387 |
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| Synonyms: | 3-isoquinolin-5-yl-1-{phenyl[4-(trifluoromethyl)phenyl]methyl}urea | isoquinoline antagonist, 5e |
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| Type | Small organic molecule |
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| Emp. Form. | C24H18F3N3O |
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| Mol. Mass. | 421.4144 |
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| SMILES | FC(F)(F)c1ccc(cc1)C(NC(=O)Nc1cccc2cnccc12)c1ccccc1 |
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| Structure | 
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