Reaction Details |
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Target | Transient receptor potential cation channel subfamily V member 1 |
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Ligand | BDBM50418973 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_759395 (CHEMBL1810633) |
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IC50 | 19.95±n/a nM |
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Citation | Ratcliffe, P; Abernethy, L; Ansari, N; Cameron, K; Clarkson, T; Dempster, M; Dunn, D; Easson, AM; Edwards, D; Everett, K; Feilden, H; Ho, KK; Kultgen, S; Littlewood, P; Maclean, J; McArthur, D; McGregor, D; McLuskey, H; Neagu, I; Nimz, O; Nisbet, LA; Ohlmeyer, M; Palin, R; Pham, Q; Rong, Y; Roughton, A; Sammons, M; Swanson, R; Tracey, H; Walker, G Discovery of potent, soluble and orally active TRPV1 antagonists. Structure-activity relationships of a series of isoxazoles. Bioorg Med Chem Lett21:4652-7 (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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BDBM50418973 |
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n/a |
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Name | BDBM50418973 |
Synonyms: | CHEMBL1807958 |
Type | Small organic molecule |
Emp. Form. | C17H18F4N2O3 |
Mol. Mass. | 374.33 |
SMILES | CC(C)[C@H](C)NC(=O)c1noc(c1CO)-c1ccc(c(F)c1)C(F)(F)F |r| |
Structure |
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