Reaction Details |
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Target | Transient receptor potential cation channel subfamily V member 1/2/4 |
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Ligand | BDBM20284 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_177578 (CHEMBL783653) |
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IC50 | 590±n/a nM |
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Citation | Suh, YG; Lee, YS; Min, KH; Park, OH; Seung, HS; Kim, HD; Park, HG; Choi, J; Lee, J; Kang, SW; Oh, UT; Koo, JY; Joo, YH; Kim, SY; Kim, JK; Park, YH Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects. Bioorg Med Chem Lett13:4389-93 (2003) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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Transient receptor potential cation channel subfamily V member 1/2/4 |
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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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BDBM20284 |
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n/a |
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Name | BDBM20284 |
Synonyms: | CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorophenyl)ethyl]-7,8-dihydroxy-1,3,4,5-tetrahydro-2-benzazepine-2-carbothioamide | N-[2-(4-chlorophenyl)ethyl]-7,8-dihydroxy-2,3,4,5-tetrahydro-1H-2-benzazepine-2-carbothioamide |
Type | Small organic molecule |
Emp. Form. | C19H21ClN2O2S |
Mol. Mass. | 376.9 |
SMILES | Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1 |
Structure |
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