Reaction Details |
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Target | Transient receptor potential cation channel subfamily V member 1 |
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Ligand | BDBM20557 |
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Substrate/Competitor | BDBM10852 |
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Meas. Tech. | Capsaicin Antagonist Assay |
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IC50 | 0.9±n/a 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 |
Synonyms: | Capsaicin receptor | OTRPC1 | TRPV1_RAT | Transient receptor potential cation channel subfamily V member 1 (TRPV1) | Trpv1 | Vanilloid Receptor 1 (TRPV1, VR1) | Vanilloid VR1 | Vanilloid receptor | Vanilloid receptor 1 (VRI/TRPV1) | Vanilloid receptor type 1-like | Vanilloid receptor type 1-like (TrpV1/Vr1) | Vr1 | Vr1l | osm-9-like TRP channel 1 |
Type: | Transient Receptor |
Mol. Mass.: | 94956.12 |
Organism: | Rattus norvegicus (rat) |
Description: | O35433 |
Residue: | 838 |
Sequence: | MEQRASLDSEESESPPQENSCLDPPDRDPNCKPPPVKPHIFTTRSRTRLFGKGDSEEASP
LDCPYEEGGLASCPIITVSSVLTIQRPGDGPASVRPSSQDSVSAGEKPPRLYDRRSIFDA
VAQSNCQELESLLPFLQRSKKRLTDSEFKDPETGKTCLLKAMLNLHNGQNDTIALLLDVA
RKTDSLKQFVNASYTDSYYKGQTALHIAIERRNMTLVTLLVENGADVQAAANGDFFKKTK
GRPGFYFGELPLSLAACTNQLAIVKFLLQNSWQPADISARDSVGNTVLHALVEVADNTVD
NTKFVTSMYNEILILGAKLHPTLKLEEITNRKGLTPLALAASSGKIGVLAYILQREIHEP
ECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLNR
LLQDKWDRFVKRIFYFNFFVYCLYMIIFTAAAYYRPVEGLPPYKLKNTVGDYFRVTGEIL
SVSGGVYFFFRGIQYFLQRRPSLKSLFVDSYSEILFFVQSLFMLVSVVLYFSQRKEYVAS
MVFSLAMGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYLVFLFGFSTAVVTLIE
DGKNNSLPMESTPHKCRGSACKPGNSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVFI
ILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKAF
RSGKLLQVGFTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRSG
RVSGRNWKNFALVPLLRDASTRDRHATQQEEVQLKHYTGSLKPEDAEVFKDSMVPGEK
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BDBM20557 |
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BDBM10852 |
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Name | BDBM20557 |
Synonyms: | AMG 517 | CHEMBL229430 | JMC503515 Compound 23 | N-[4-({6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl}oxy)-1,3-benzothiazol-2-yl]acetamide | US8796328, A | US8802711, H |
Type | Small organic molecule |
Emp. Form. | C20H13F3N4O2S |
Mol. Mass. | 430.403 |
SMILES | CC(=O)Nc1nc2c(Oc3cc(ncn3)-c3ccc(cc3)C(F)(F)F)cccc2s1 |
Structure |
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