Reaction Details
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Transient receptor potential cation channel subfamily V member 1
Ligand
BDBM20345
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
3.8±0.5 nM
Citation
Perner, RJ; DiDomenico, S; Koenig, JR; Gomtsyan, A; Bayburt, EK; Schmidt, RG; Drizin, I; Zheng, GZ; Turner, SC; Jinkerson, T; Brown, BS; Keddy, RG; Lukin, K; McDonald, HA; Honore, P; Mikusa, J; Marsh, KC; Wetter, JM; George, KS; Jarvis, MF; Faltynek, CR; Lee, CH In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists. J Med Chem 50:3651-60 (2007) [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:
BDBM20345
Synonyms:
3-{[4-(azepan-1-yl)phenyl]methyl}-1-(3-methylisoquinolin-5-yl)urea | Isoquinoline Analogue, 39
Type:
Small organic molecule
Emp. Form.:
C24H28N4O
Mol. Mass.:
388.5053
SMILES:
Cc1cc2c(NC(=O)NCc3ccc(cc3)N3CCCCCC3)cccc2cn1
Structure:
Substrate