Reaction Details |
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Target | Transient receptor potential cation channel subfamily V member 1 |
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Ligand | BDBM50188650 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_364425 (CHEMBL870233) |
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IC50 | 0.9±n/a nM |
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Citation | Ognyanov, VI; Balan, C; Bannon, AW; Bo, Y; Dominguez, C; Fotsch, C; Gore, VK; Klionsky, L; Ma, VV; Qian, YX; Tamir, R; Wang, X; Xi, N; Xu, S; Zhu, D; Gavva, NR; Treanor, JJ; Norman, MH Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles. J Med Chem49:3719-42 (2006) [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 | 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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BDBM50188650 |
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n/a |
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Name | BDBM50188650 |
Synonyms: | (R,S)-1-(5-chloro-6-((R)-3-methyl-4-(6-(trifluoromethyl)-4-(3,4,5-trifluorophenyl)-1H-benzo[d]imidazol-2-yl)piperazin-1-yl)pyridin-3-yl)ethane-1,2-diol | 1-(5-chloro-6-((R)-3-methyl-4-(6-(trifluoromethyl)-4-(3,4,5-trifluorophenyl)-1H-benzo[d]imidazol-2-yl)piperazin-1-yl)pyridin-3-yl)ethane-1,2-diol | CHEMBL209569 |
Type | Small organic molecule |
Emp. Form. | C26H22ClF6N5O2 |
Mol. Mass. | 585.929 |
SMILES | C[C@@H]1CN(CCN1c1nc2c(cc(cc2[nH]1)C(F)(F)F)-c1cc(F)c(F)c(F)c1)c1ncc(cc1Cl)C(O)CO |
Structure |
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