Reaction Details |
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Target | Transient receptor potential cation channel subfamily V member 4 |
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Ligand | BDBM50192809 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1613868 (CHEMBL3855668) |
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IC50 | 2.1±n/a nM |
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Citation | Tsuno, N; Yukimasa, A; Yoshida, O; Suzuki, S; Nakai, H; Ogawa, T; Fujiu, M; Takaya, K; Nozu, A; Yamaguchi, H; Matsuda, H; Funaki, S; Nishimura, Y; Ito, T; Nagamatsu, D; Asaki, T; Horita, N; Yamamoto, M; Hinata, M; Soga, M; Imai, M; Morioka, Y; Kanemasa, T; Sakaguchi, G; Iso, Y Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 2. Bioorg Med Chem Lett26:4936-4941 (2016) [PubMed] Article |
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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 4 |
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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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BDBM50192809 |
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n/a |
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Name | BDBM50192809 |
Synonyms: | CHEMBL3941914 |
Type | Small organic molecule |
Emp. Form. | C25H23F3N8OS2 |
Mol. Mass. | 572.628 |
SMILES | Cc1nc(C)c(s1)-c1csc(Nc2ccc(cn2)C(=O)N2C3CCC2CN(C3)c2ncc(cn2)C(F)(F)F)n1 |
Structure |
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