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Target
Transient receptor potential cation channel subfamily V member 1
Ligand
BDBM50253983
Substrate
n/a
Meas. Tech.
ChEMBL_559247 (CHEMBL1014666)
IC50
12±n/a nM
Citation
 Lebsack, AD; Branstetter, BJ; Hack, MD; Xiao, W; Peterson, ML; Nasser, N; Maher, MP; Ao, H; Bhattacharya, A; Kansagara, M; Scott, BP; Luo, L; Rynberg, R; Rizzolio, M; Chaplan, SR; Wickenden, AD; Guy 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 | 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:
MKKWSSTDLGAAADPLQKDTCPDPLDGDPNSRPPPAKPQLSTAKSRTRLFGKGDSEEAFPVDCPHEEGELDSCPTITVSPVITIQRPGDGPTGARLLSQDSVAASTEKTLRLYDRRSIFEAVAQNNCQDLESLLLFLQKSKKHLTDNEFKDPETGKTCLLKAMLNLHDGQNTTIPLLLEIARQTDSLKELVNASYTDSYYKGQTALHIAIERRNMALVTLLVENGADVQAAAHGDFFKKTKGRPGFYFGELPLSLAACTNQLGIVKFLLQNSWQTADISARDSVGNTVLHALVEVADNTADNTKFVTSMYNEILMLGAKLHPTLKLEELTNKKGMTPLALAAGTGKIGVLAYILQREIQEPECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLNRLLQDKWDRFVKRIFYFNFLVYCLYMIIFTMAAYYRPVDGLPPFKMEKTGDYFRVTGEILSVLGGVYFFFRGIQYFLQRRPSMKTLFVDSYSEMLFFLQSLFMLATVVLYFSHLKEYVASMVFSLALGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYIVFLFGFSTAVVTLIEDGKNDSLPSESTSHRWRGPACRPPDSSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVFIILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKAFRSGKLLQVGYTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRSSRVSGRHWKNFALVPLLREASARDRQSAQPEEVYLRQFSGSLKPEDAEVFKSPAASGEK
  
Inhibitor
Name:
BDBM50253983
Synonyms:
CHEMBL462688 | N2-(2,6-dichlorophenyl)-5-(pyrrolidin-1-yl)-N7-(4-(trifluoromethyl)phenyl)thiazolo[5,4-d]pyrimidine-2,7-diamine
Type:
Small organic molecule
Emp. Form.:
C22H17Cl2F3N6S
Mol. Mass.:
525.377
SMILES:
FC(F)(F)c1ccc(Nc2nc(nc3sc(Nc4c(Cl)cccc4Cl)nc23)N2CCCC2)cc1
Structure:
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