| 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 | BDBM20504 |
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| Substrate/Competitor | BDBM10852 |
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| Meas. Tech. | FLIPR (Fluorescence Imaging Plate Reader)-Based Ca2+ Assay |
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| pH | 7.2±n/a |
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| Temperature | 298.15±n/a K |
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| EC50 | 32±n/a nM |
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| Comments | The compound solubility = 0.4 mg/mL in simulated gastric fluid. Electrophysiological assay showed the compound was potent antagonist versus the multiple chemical and physical modes of TRPV1 activation (namely capsaicin, acid and noxious heat). |
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| Citation |  Rami, HK; Thompson, M; Stemp, G; Fell, S; Jerman, JC; Stevens, AJ; Smart, D; Sargent, B; Sanderson, D; Randall, AD; Gunthorpe, MJ; Davis, JB Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development. Bioorg Med Chem Lett16:3287-91 (2006) [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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| BDBM20504 |
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| BDBM10852 |
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| Name | BDBM20504 |
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| Synonyms: | 1-(2-bromophenyl)-3-[(3R)-1-[5-(trifluoromethyl)pyridin-2-yl]pyrrolidin-3-yl]urea | BMCL163287 Compound 15 | SB-705498 |
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| Type | Small organic molecule |
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| Emp. Form. | C17H16BrF3N4O |
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| Mol. Mass. | 429.234 |
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| SMILES | FC(F)(F)c1ccc(nc1)N1CC[C@H](C1)NC(=O)Nc1ccccc1Br |r| |
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| Structure | 
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