| 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 | BDBM20554 |
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| Substrate/Competitor | BDBM10852 |
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| Meas. Tech. | Capsaicin Antagonist Assay |
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| pH | 7.4±n/a |
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| Temperature | 295.15±n/a K |
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| IC50 | 0.8±0.28 nM |
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| Citation |  Doherty, EM; Fotsch, C; Bannon, AW; Bo, Y; Chen, N; Dominguez, C; Falsey, J; Gavva, NR; Katon, J; Nixey, T; Ognyanov, VI; Pettus, L; Rzasa, RM; Stec, M; Surapaneni, S; Tamir, R; Zhu, J; Treanor, JJ; Norman, MH Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. J Med Chem50:3515-27 (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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| BDBM20554 |
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| BDBM10852 |
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| Name | BDBM20554 |
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| Synonyms: | 3-amino-5-({6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl}oxy)-1,2-dihydroquinoxalin-2-one | 4-Oxopyrimidine, 32 | CHEMBL375681 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H12F3N5O2 |
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| Mol. Mass. | 399.3261 |
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| SMILES | Nc1nc2c(Oc3cc(ncn3)-c3ccc(cc3)C(F)(F)F)cccc2[nH]c1=O |
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| Structure | 
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