Target
Transient receptor potential cation channel subfamily V member 1/2/4
Ligand
BDBM50305278
Substrate
n/a
Meas. Tech.
ChEMBL_177039 (CHEMBL779560)
IC50
4000±n/a nM
Citation
 Park, HGChoi, JYChoi, SHPark, MKLee, JSuh, YGCho, HOh, UKim, HDJoo, YHKim, SYPark, YHJeong, YSChoi, JKKim, JKJew, SS N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands. Bioorg Med Chem Lett 14:1693-6 (2004) [PubMed]  Article 
Target
Name:
Transient receptor potential cation channel subfamily V member 1/2/4
Synonyms:
Vanilloid receptor
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 177578
Components:
This complex has 3 components.
Component 1
Name:
Transient receptor potential cation channel subfamily V member 2
Synonyms:
Sac2b | TRPV2_RAT | Transient receptor potential cation channel subfamily V member 2 | Trpv2 | Vanilloid receptor | Vrl1
Type:
PROTEIN
Mol. Mass.:
86707.60
Organism:
Rattus norvegicus
Description:
ChEMBL_768011
Residue:
761
Sequence:
MTSASSPPAFRLETSDGDEEGNAEVNKGKQEPPPMESPFQREDRNSSPQIKVNLNFIKRPPKNTSAPSQQEPDRFDRDRLFSVVSRGVPEELTGLLEYLRWNSKYLTDSAYTEGSTGKTCLMKAVLNLQDGVNACIMPLLQIDKDSGNPKLLVNAQCTDEFYQGHSALHIAIEKRSLQCVKLLVENGADVHLRACGRFFQKHQGTCFYFGELPLSLAACTKQWDVVTYLLENPHQPASLEATDSLGNTVLHALVMIADNSPENSALVIHMYDGLLQMGARLCPTVQLEEISNHQGLTPLKLAAKEGKIEIFRHILQREFSGPYQPLSRKFTEWCYGPVRVSLYDLSSVDSWEKNSVLEIIAFHCKSPNRHRMVVLEPLNKLLQEKWDRLVSRFFFNFACYLVYMFIFTVVAYHQPSLDQPAIPSSKATFGESMLLLGHILILLGGIYLLLGQLWYFWRRRLFIWISFMDSYFEILFLLQALLTVLSQVLRFMETEWYLPLLVLSLVLGWLNLLYYTRGFQHTGIYSVMIQKVILRDLLRFLLVYLVFLFGFAVALVSLSREARSPKAPEDNNSTVTEQPTVGQEEEPAPYRSILDASLELFKFTIGMGELAFQEQLRFRGVVLLLLLAYVLLTYVLLLNMLIALMSETVNHVADNSWSIWKLQKAISVLEMENGYWWCRRKKHREGRLLKVGTRGDGTPDERWCFRVEEVNWAAWEKTLPTLSEDPSGPGITGNKKNPTSKPGKNSASEEDHLPLQVLQSP
  
Component 2
Name:
Transient receptor potential cation channel subfamily V member 1
Synonyms:
Capsaicin receptor | OTRPC1 | TRPV1_RAT | Transient receptor potential cation channel subfamily V member 1 (TRPV1) | Trpv1 | Vanilloid Receptor 1 (TRPV1, VR1) | Vanilloid VR1 | Vanilloid receptor | Vanilloid receptor 1 (VRI/TRPV1) | Vanilloid receptor type 1-like | Vanilloid receptor type 1-like (TrpV1/Vr1) | Vr1 | Vr1l | osm-9-like TRP channel 1
Type:
Transient Receptor
Mol. Mass.:
94956.12
Organism:
Rattus norvegicus (rat)
Description:
O35433
Residue:
838
Sequence:
MEQRASLDSEESESPPQENSCLDPPDRDPNCKPPPVKPHIFTTRSRTRLFGKGDSEEASPLDCPYEEGGLASCPIITVSSVLTIQRPGDGPASVRPSSQDSVSAGEKPPRLYDRRSIFDAVAQSNCQELESLLPFLQRSKKRLTDSEFKDPETGKTCLLKAMLNLHNGQNDTIALLLDVARKTDSLKQFVNASYTDSYYKGQTALHIAIERRNMTLVTLLVENGADVQAAANGDFFKKTKGRPGFYFGELPLSLAACTNQLAIVKFLLQNSWQPADISARDSVGNTVLHALVEVADNTVDNTKFVTSMYNEILILGAKLHPTLKLEEITNRKGLTPLALAASSGKIGVLAYILQREIHEPECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLNRLLQDKWDRFVKRIFYFNFFVYCLYMIIFTAAAYYRPVEGLPPYKLKNTVGDYFRVTGEILSVSGGVYFFFRGIQYFLQRRPSLKSLFVDSYSEILFFVQSLFMLVSVVLYFSQRKEYVASMVFSLAMGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYLVFLFGFSTAVVTLIEDGKNNSLPMESTPHKCRGSACKPGNSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVFIILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKAFRSGKLLQVGFTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRSGRVSGRNWKNFALVPLLRDASTRDRHATQQEEVQLKHYTGSLKPEDAEVFKDSMVPGEK
  
Component 3
Name:
Transient receptor potential cation channel subfamily V member 4
Synonyms:
TRPV4_RAT | Trpv4 | Vanilloid receptor | Vroac
Type:
PROTEIN
Mol. Mass.:
98016.72
Organism:
Rattus norvegicus
Description:
ChEMBL_1514408
Residue:
871
Sequence:
MADPGDGPRAAPGDVAEPPGDESGTSGGEAFPLSSLANLFEGEEGSSSLSPVDASRPAGPGDGRPNLRMKFQGAFRKGVPNPIDLLESTLYESSVVPGPKKAPMDSLFDYGTYRHHPSDNKRWRRKVVEKQPQSPKAPAPQPPPILKVFNRPILFDIVSRGSTADLDGLLSYLLTHKKRLTDEEFREPSTGKTCLPKALLNLSNGRNDTIPVLLDIAERTGNMREFINSPFRDIYYRGQTALHIAIERRCKHYVELLVAQGADVHAQARGRFFQPKDEGGYFYFGELPLSLAACTNQPHIVNYLTENPHKKADMRRQDSRGNTVLHALVAIADNTRENTKFVTKMYDLLLLKCSRLFPDSNLETVLNNDGLSPLMMAAKTGKIGVFQHIIRREVTDEDTRHLSRKFKDWAYGPVYSSLYDLSSLDTCGEEVSVLEILVYNSKIENRHEMLAVEPINELLRDKWRKFGAVSFYINVVSYLCAMVIFTLTAYYQPLEGTPPYPYRTTVDYLRLAGEVITLLTGVLFFFTSIKDLFMKKCPGVNSLFVDGSFQLLYFIYSVLVVVSAALYLAGIEAYLAVMVFALVLGWMNALYFTRGLKLTGTYSIMIQKILFKDLFRFLLVYLLFMIGYASALVTLLNPCTNMKVCNEDQSNCTVPSYPACRDSETFSAFLLDLFKLTIGMGDLEMLSSAKYPVVFILLLVTYIILTFVLLLNMLIALMGETVGQVSKESKHIWKLQWATTILDIERSFPVFLRKAFRSGEMVTVGKSSDGTPDRRWCFRVDEVNWSHWNQNLGIINEDPGKSEIYQYYGFSHTMGRLRRDRWSSVVPRVVELNKNSGTDEVVVPLDNLGNPNCDGHQQGYAPKWRAEDAPL
  
Inhibitor
Name:
BDBM50305278
Synonyms:
CHEMBL595069 | iodoresiniferatoxin
Type:
Small organic molecule
Emp. Form.:
C37H39IO9
Mol. Mass.:
754.6046
SMILES:
COc1cc(CC(=O)OCC2=C[C@H]3[C@H]4O[C@]5(Cc6ccccc6)O[C@]4(C[C@@H](C)[C@]3(O5)[C@@H]3C=C(C)C(=O)[C@@]3(O)C2)C(C)=C)cc(I)c1O |r,t:10,35,TLB:16:15:12:25.26.24,THB:23:15:12:25.26.24|
Structure:
Search PDB for entries with ligand similarity: