Target
Transient receptor potential cation channel subfamily V member 1
Ligand
BDBM50254079
Substrate
n/a
Meas. Tech.
ChEMBL_559248 (CHEMBL1014667)
IC50
11±n/a nM
Citation
 Lebsack, ADBranstetter, BJHack, MDXiao, WPeterson, MLNasser, NMaher, MPAo, HBhattacharya, AKansagara, MScott, BPLuo, LRynberg, RRizzolio, MChaplan, SRWickenden, ADGuy Breitenbucher, J Identification and synthesis of 2,7-diamino-thiazolo[5,4-d]pyrimidine derivatives as TRPV1 antagonists. Bioorg Med Chem Lett 19:40-6 (2008) [PubMed]  Article 
Target
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:
MEQRASLDSEESESPPQENSCLDPPDRDPNCKPPPVKPHIFTTRSRTRLFGKGDSEEASPLDCPYEEGGLASCPIITVSSVLTIQRPGDGPASVRPSSQDSVSAGEKPPRLYDRRSIFDAVAQSNCQELESLLPFLQRSKKRLTDSEFKDPETGKTCLLKAMLNLHNGQNDTIALLLDVARKTDSLKQFVNASYTDSYYKGQTALHIAIERRNMTLVTLLVENGADVQAAANGDFFKKTKGRPGFYFGELPLSLAACTNQLAIVKFLLQNSWQPADISARDSVGNTVLHALVEVADNTVDNTKFVTSMYNEILILGAKLHPTLKLEEITNRKGLTPLALAASSGKIGVLAYILQREIHEPECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLNRLLQDKWDRFVKRIFYFNFFVYCLYMIIFTAAAYYRPVEGLPPYKLKNTVGDYFRVTGEILSVSGGVYFFFRGIQYFLQRRPSLKSLFVDSYSEILFFVQSLFMLVSVVLYFSQRKEYVASMVFSLAMGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYLVFLFGFSTAVVTLIEDGKNNSLPMESTPHKCRGSACKPGNSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVFIILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKAFRSGKLLQVGFTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRSGRVSGRNWKNFALVPLLRDASTRDRHATQQEEVQLKHYTGSLKPEDAEVFKDSMVPGEK
  
Inhibitor
Name:
BDBM50254079
Synonyms:
CHEMBL459320 | N2-(2,6-dichlorophenyl)-N5-(2-morpholinoethyl)-N7-(4-(trifluoromethyl)phenyl)thiazolo[5,4-d]pyrimidine-2,5,7-triamine
Type:
Small organic molecule
Emp. Form.:
C24H22Cl2F3N7OS
Mol. Mass.:
584.444
SMILES:
FC(F)(F)c1ccc(Nc2nc(NCCN3CCOCC3)nc3sc(Nc4c(Cl)cccc4Cl)nc23)cc1
Structure:
Search PDB for entries with ligand similarity: