Reaction Details |
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Target | Transient receptor potential cation channel subfamily V member 1 |
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Ligand | BDBM20498 |
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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 | 16±n/a nM |
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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 |
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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BDBM20498 |
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BDBM10852 |
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Name | BDBM20498 |
Synonyms: | 1-(2-bromophenyl)-3-[(3R)-1-(3-fluorophenyl)pyrrolidin-3-yl]urea | pyrrolidine urea analogue, 9 |
Type | Small organic molecule |
Emp. Form. | C17H17BrFN3O |
Mol. Mass. | 378.239 |
SMILES | Fc1cccc(c1)N1CC[C@H](C1)NC(=O)Nc1ccccc1Br |r| |
Structure |
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