Reaction Details |
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Target | Transient receptor potential cation channel subfamily V member 1 |
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Ligand | BDBM20322 |
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Substrate/Competitor | BDBM20285 |
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Meas. Tech. | Competition Binding Assay and Inhibition of Ca2+ Uptake Assay |
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pH | 7.4±n/a |
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Temperature | 310.15±n/a K |
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Ki | 54±11 nM |
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EC50 | 9.2±2.9 nM |
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Citation | Chung, JU; Kim, SY; Lim, JO; Choi, HK; Kang, SU; Yoon, HS; Ryu, H; Kang, DW; Lee, J; Kang, B; Choi, S; Toth, A; Pearce, LV; Pavlyukovets, VA; Lundberg, DJ; Blumberg, PM Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists. Bioorg Med Chem15:6043-53 (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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BDBM20322 |
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BDBM20285 |
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Name | BDBM20322 |
Synonyms: | 3-[(4-tert-butylphenyl)methyl]-1-[1-(3-fluoro-4-methanesulfonamidophenyl)ethyl]thiourea | thiourea analogue, 11 |
Type | Small organic molecule |
Emp. Form. | C21H28FN3O2S2 |
Mol. Mass. | 437.594 |
SMILES | CC(NC(=S)NCc1ccc(cc1)C(C)(C)C)c1ccc(NS(C)(=O)=O)c(F)c1 |
Structure |
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