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TargetTransient receptor potential cation channel subfamily V member 1/2/4
LigandBDBM20321
Substrate/Competitorn/a
Meas. Tech.ChEMBL_177039 (CHEMBL779560)
IC50 37±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 Lett14:1693-6 (2004) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Transient receptor potential cation channel subfamily V member 1/2/4
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:
MTSASSPPAFRLETSDGDEEGNAEVNKGKQEPPPMESPFQREDRNSSPQIKVNLNFIKRP
PKNTSAPSQQEPDRFDRDRLFSVVSRGVPEELTGLLEYLRWNSKYLTDSAYTEGSTGKTC
LMKAVLNLQDGVNACIMPLLQIDKDSGNPKLLVNAQCTDEFYQGHSALHIAIEKRSLQCV
KLLVENGADVHLRACGRFFQKHQGTCFYFGELPLSLAACTKQWDVVTYLLENPHQPASLE
ATDSLGNTVLHALVMIADNSPENSALVIHMYDGLLQMGARLCPTVQLEEISNHQGLTPLK
LAAKEGKIEIFRHILQREFSGPYQPLSRKFTEWCYGPVRVSLYDLSSVDSWEKNSVLEII
AFHCKSPNRHRMVVLEPLNKLLQEKWDRLVSRFFFNFACYLVYMFIFTVVAYHQPSLDQP
AIPSSKATFGESMLLLGHILILLGGIYLLLGQLWYFWRRRLFIWISFMDSYFEILFLLQA
LLTVLSQVLRFMETEWYLPLLVLSLVLGWLNLLYYTRGFQHTGIYSVMIQKVILRDLLRF
LLVYLVFLFGFAVALVSLSREARSPKAPEDNNSTVTEQPTVGQEEEPAPYRSILDASLEL
FKFTIGMGELAFQEQLRFRGVVLLLLLAYVLLTYVLLLNMLIALMSETVNHVADNSWSIW
KLQKAISVLEMENGYWWCRRKKHREGRLLKVGTRGDGTPDERWCFRVEEVNWAAWEKTLP
TLSEDPSGPGITGNKKNPTSKPGKNSASEEDHLPLQVLQSP
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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:
MEQRASLDSEESESPPQENSCLDPPDRDPNCKPPPVKPHIFTTRSRTRLFGKGDSEEASP
LDCPYEEGGLASCPIITVSSVLTIQRPGDGPASVRPSSQDSVSAGEKPPRLYDRRSIFDA
VAQSNCQELESLLPFLQRSKKRLTDSEFKDPETGKTCLLKAMLNLHNGQNDTIALLLDVA
RKTDSLKQFVNASYTDSYYKGQTALHIAIERRNMTLVTLLVENGADVQAAANGDFFKKTK
GRPGFYFGELPLSLAACTNQLAIVKFLLQNSWQPADISARDSVGNTVLHALVEVADNTVD
NTKFVTSMYNEILILGAKLHPTLKLEEITNRKGLTPLALAASSGKIGVLAYILQREIHEP
ECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLNR
LLQDKWDRFVKRIFYFNFFVYCLYMIIFTAAAYYRPVEGLPPYKLKNTVGDYFRVTGEIL
SVSGGVYFFFRGIQYFLQRRPSLKSLFVDSYSEILFFVQSLFMLVSVVLYFSQRKEYVAS
MVFSLAMGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYLVFLFGFSTAVVTLIE
DGKNNSLPMESTPHKCRGSACKPGNSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVFI
ILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKAF
RSGKLLQVGFTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRSG
RVSGRNWKNFALVPLLRDASTRDRHATQQEEVQLKHYTGSLKPEDAEVFKDSMVPGEK
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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:
MADPGDGPRAAPGDVAEPPGDESGTSGGEAFPLSSLANLFEGEEGSSSLSPVDASRPAGP
GDGRPNLRMKFQGAFRKGVPNPIDLLESTLYESSVVPGPKKAPMDSLFDYGTYRHHPSDN
KRWRRKVVEKQPQSPKAPAPQPPPILKVFNRPILFDIVSRGSTADLDGLLSYLLTHKKRL
TDEEFREPSTGKTCLPKALLNLSNGRNDTIPVLLDIAERTGNMREFINSPFRDIYYRGQT
ALHIAIERRCKHYVELLVAQGADVHAQARGRFFQPKDEGGYFYFGELPLSLAACTNQPHI
VNYLTENPHKKADMRRQDSRGNTVLHALVAIADNTRENTKFVTKMYDLLLLKCSRLFPDS
NLETVLNNDGLSPLMMAAKTGKIGVFQHIIRREVTDEDTRHLSRKFKDWAYGPVYSSLYD
LSSLDTCGEEVSVLEILVYNSKIENRHEMLAVEPINELLRDKWRKFGAVSFYINVVSYLC
AMVIFTLTAYYQPLEGTPPYPYRTTVDYLRLAGEVITLLTGVLFFFTSIKDLFMKKCPGV
NSLFVDGSFQLLYFIYSVLVVVSAALYLAGIEAYLAVMVFALVLGWMNALYFTRGLKLTG
TYSIMIQKILFKDLFRFLLVYLLFMIGYASALVTLLNPCTNMKVCNEDQSNCTVPSYPAC
RDSETFSAFLLDLFKLTIGMGDLEMLSSAKYPVVFILLLVTYIILTFVLLLNMLIALMGE
TVGQVSKESKHIWKLQWATTILDIERSFPVFLRKAFRSGEMVTVGKSSDGTPDRRWCFRV
DEVNWSHWNQNLGIINEDPGKSEIYQYYGFSHTMGRLRRDRWSSVVPRVVELNKNSGTDE
VVVPLDNLGNPNCDGHQQGYAPKWRAEDAPL
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BDBM20321
n/a
NameBDBM20321
Synonyms:3-[(4-tert-butylphenyl)methyl]-1-[(3-fluoro-4-methanesulfonamidophenyl)methyl]thiourea | CHEMBL388824 | JYL1421 | thiourea analogue, 2
TypeSmall organic molecule
Emp. Form.C20H26FN3O2S2
Mol. Mass.423.568
SMILESCC(C)(C)c1ccc(CNC(=S)NCc2ccc(NS(C)(=O)=O)c(F)c2)cc1
Structure
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