Reaction Details |
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Target | Transient receptor potential cation channel subfamily V member 1 |
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Ligand | BDBM50336136 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_718134 (CHEMBL1671587) |
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IC50 | 43±n/a nM |
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Citation | Palin, R; Abernethy, L; Ansari, N; Cameron, K; Clarkson, T; Dempster, M; Dunn, D; Easson, AM; Edwards, D; Maclean, J; Everett, K; Feilden, H; Ho, KK; Kultgen, S; Littlewood, P; McArthur, D; McGregor, D; McLuskey, H; Neagu, I; Neale, S; Nisbet, LA; Ohlmeyer, M; Pham, Q; Ratcliffe, P; Rong, Y; Roughton, A; Sammons, M; Swanson, R; Tracey, H; Walker, G Structure-activity studies of a novel series of isoxazole-3-carboxamide derivatives as TRPV1 antagonists. Bioorg Med Chem Lett21:892-8 (2011) [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 |
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) |
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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BDBM50336136 |
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n/a |
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Name | BDBM50336136 |
Synonyms: | 4-chloro-N-(tetrahydro-2H-pyran-4-yl)-5-(4-(trifluoromethyl)phenyl)isoxazole-3-carboxamide | CHEMBL1669525 |
Type | Small organic molecule |
Emp. Form. | C16H14ClF3N2O3 |
Mol. Mass. | 374.742 |
SMILES | FC(F)(F)c1ccc(cc1)-c1onc(C(=O)NC2CCOCC2)c1Cl |
Structure |
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