Reaction Details
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Transient receptor potential cation channel subfamily V member 1
Ligand
BDBM20381
Substrate
BDBM10852
Meas. Tech.
Ca2+ Influx Functional Assay for the Determination of in Vitro Activity.
EC50
35.3±n/a 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:
BDBM20381
Synonyms:
1-({4-[(1R,5S)-8-azabicyclo[3.2.1]octan-8-yl]-2-(propan-2-yl)phenyl}methyl)-3-1H-indazol-4-ylurea | Indazole Analogue, 75
Type:
Small organic molecule
Emp. Form.:
C25H31N5O
Mol. Mass.:
417.5465
SMILES:
CC(C)c1cc(ccc1CNC(=O)Nc1cccc2[nH]ncc12)N1[C@H]2CC[C@@H]1CCC2 |r,THB:5:23:29.28.30:25.26|
Structure:
Substrate