| 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 | BDBM20464 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_312923 (CHEMBL874818) |
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| IC50 | 0.420000±n/a nM |
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| Citation |  Doherty, EM; Fotsch, C; Bo, Y; Chakrabarti, PP; Chen, N; Gavva, N; Han, N; Kelly, MG; Kincaid, J; Klionsky, L; Liu, Q; Ognyanov, VI; Tamir, R; Wang, X; Zhu, J; Norman, MH; Treanor, JJ Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides. J Med Chem48:71-90 (2005) [PubMed] Article |
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| More Info.: | Get all data from this article, 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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| BDBM20464 |
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| n/a |
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| Name | BDBM20464 |
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| Synonyms: | (2E)-3-[2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl]-N-(quinolin-7-yl)prop-2-enamide | AMG6880 | CHEMBL190874 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H21F3N4O |
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| Mol. Mass. | 426.4342 |
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| SMILES | FC(F)(F)c1ccc(\C=C\C(=O)Nc2ccc3cccnc3c2)c(n1)N1CCCCC1 |
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| Structure | 
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