Reaction Details Report a problem with these data
Target
Transient receptor potential cation channel subfamily V member 1
Ligand
BDBM244979
Substrate
n/a
Meas. Tech.
Functional Assay
Temperature
310.15±n/a K
IC50
10±n/a nM
Comments
extracted
Citation
 Allison, BD; Branstetter, BJ; Breitenbucher, JG; Hack, MD; Hawryluk, NA; Lebsack, AD; McClure, KJ; Merit, JE Tetrahydro-pyrimidoazepines as modulators of TRPV1 US Patent  US9422293 Publication Date 8/23/2016 
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:
BDBM244979
Synonyms:
US9422293, 214
Type:
Small organic molecule
Emp. Form.:
C27H28F6N6O
Mol. Mass.:
566.5412
SMILES:
COC1CCCN(C1)c1nc2CCN(CCc2c(Nc2ccc(cc2)C(F)(F)F)n1)c1ncccc1C(F)(F)F
Structure:
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