Reaction Details |
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Target | Transient receptor potential cation channel subfamily V member 1 |
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Ligand | BDBM50332850 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_696915 (CHEMBL1639431) |
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IC50 | 15±n/a nM |
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Citation | Lebsack, AD; Rech, JC; Branstetter, BJ; Hawryluk, NA; Merit, JE; Allison, B; Rynberg, R; Buma, J; Rizzolio, M; Swanson, N; Ao, H; Maher, MP; Herrmann, M; Freedman, J; Scott, BP; Luo, L; Bhattacharya, A; Wang, Q; Chaplan, SR; Wickenden, AD; Breitenbucher, JG 1,2-diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines as TRPV1 antagonists with improved properties. Bioorg Med Chem Lett20:7142-6 (2010) [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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BDBM50332850 |
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n/a |
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Name | BDBM50332850 |
Synonyms: | 2-(4-cyclopentylpiperazin-1-yl)-N-(4-(trifluoromethyl)phenyl)-7-(3-(trifluoromethyl)pyridin-2-yl)-6,7,8,9-tetrahydro-5H-pyrimido[5,4-d]azepin-4-amine | CHEMBL1630303 |
Type | Small organic molecule |
Emp. Form. | C30H33F6N7 |
Mol. Mass. | 605.6203 |
SMILES | FC(F)(F)c1ccc(Nc2nc(nc3CCN(CCc23)c2ncccc2C(F)(F)F)N2CCN(CC2)C2CCCC2)cc1 |
Structure |
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