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Target
Transient receptor potential cation channel subfamily V member 1
Ligand
BDBM50056386
Substrate
n/a
Meas. Tech.
ChEMBL_1451403 (CHEMBL3363963)
IC50
10.0±n/a nM
Citation
 Voight, EA; Gomtsyan, AR; Daanen, JF; Perner, RJ; Schmidt, RG; Bayburt, EK; DiDomenico, S; McDonald, HA; Puttfarcken, PS; Chen, J; Neelands, TR; Bianchi, BR; Han, P; Reilly, RM; Franklin, PH; Segreti, JA; Nelson, RA; Su, Z; King, AJ; Polakowski, JS; Baker, SJ; Gauvin, DM; Lewis, LR; Mikusa, JP; Joshi, SK; Faltynek, CR; Kym, PR; Kort, ME Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy. J Med Chem 57:7412-24 (2014) [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:
Human
Description:
Q8NER1
Residue:
839
Sequence:
MKKWSSTDLGAAADPLQKDTCPDPLDGDPNSRPPPAKPQLSTAKSRTRLFGKGDSEEAFPVDCPHEEGELDSCPTITVSPVITIQRPGDGPTGARLLSQDSVAASTEKTLRLYDRRSIFEAVAQNNCQDLESLLLFLQKSKKHLTDNEFKDPETGKTCLLKAMLNLHDGQNTTIPLLLEIARQTDSLKELVNASYTDSYYKGQTALHIAIERRNMALVTLLVENGADVQAAAHGDFFKKTKGRPGFYFGELPLSLAACTNQLGIVKFLLQNSWQTADISARDSVGNTVLHALVEVADNTADNTKFVTSMYNEILMLGAKLHPTLKLEELTNKKGMTPLALAAGTGKIGVLAYILQREIQEPECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLNRLLQDKWDRFVKRIFYFNFLVYCLYMIIFTMAAYYRPVDGLPPFKMEKTGDYFRVTGEILSVLGGVYFFFRGIQYFLQRRPSMKTLFVDSYSEMLFFLQSLFMLATVVLYFSHLKEYVASMVFSLALGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYIVFLFGFSTAVVTLIEDGKNDSLPSESTSHRWRGPACRPPDSSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVFIILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKAFRSGKLLQVGYTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRSSRVSGRHWKNFALVPLLREASARDRQSAQPEEVYLRQFSGSLKPEDAEVFKSPAASGEK
  
Inhibitor
Name:
BDBM50056386
Synonyms:
CHEMBL3325460
Type:
Small organic molecule
Emp. Form.:
C23H22F3N3O2
Mol. Mass.:
429.4349
SMILES:
Cc1cc2c(NC(=O)N[C@@H]3CC(C)(C)Oc4cc(ccc34)C(F)(F)F)cccc2cn1 |r|
Structure:
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