Reaction Details
Report a problem with these data
Report a problem with these dataTarget
Transient receptor potential cation channel subfamily V member 1
Ligand
BDBM20435
Substrate
BDBM10852
Meas. Tech.
Ca2+ Influx Functional Assay for the Determination of in Vitro Activity.
pH
7.4±n/a
Temperature
295.15±n/a K
EC50
1470±140 nM
Citation
Drizin, I; Gomtsyan, A; Bayburt, EK; Schmidt, RG; Zheng, GZ; Perner, RJ; DiDomenico, S; Koenig, JR; Turner, SC; Jinkerson, TK; Brown, BS; Keddy, RG; McDonald, HA; Honore, P; Wismer, CT; Marsh, KC; Wetter, JM; Polakowski, JS; Segreti, JA; Jarvis, MF; Faltynek, CR; Lee, CH Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists. Bioorg Med Chem 14:4740-9 (2006) [PubMed] Article More Info.:
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:
BDBM20435
Synonyms:
1-[(4-bromophenyl)methyl]-3-(2,3-dimethyl-1H-indol-4-yl)urea | heterocyclic urea, 34
Type:
Small organic molecule
Emp. Form.:
C18H18BrN3O
Mol. Mass.:
372.259
SMILES:
Cc1[nH]c2cccc(NC(=O)NCc3ccc(Br)cc3)c2c1C
Structure:
Substrate