Reaction Details |
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Target | Transient receptor potential cation channel subfamily V member 4 |
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Ligand | BDBM50195064 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1617390 (CHEMBL3859459) |
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IC50 | >10000±n/a nM |
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Citation | Tsuno, N; Yukimasa, A; Yoshida, O; Ichihashi, Y; Inoue, T; Ueno, T; Yamaguchi, H; Matsuda, H; Funaki, S; Yamanada, N; Tanimura, M; Nagamatsu, D; Nishimura, Y; Ito, T; Soga, M; Horita, N; Yamamoto, M; Hinata, 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 1. Bioorg Med Chem Lett26:4930-4935 (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 | TRPV4_HUMAN | Transient receptor potential cation channel subfamily V member 4 (TRPV4) | VRL2 | VROAC |
Type: | Enzyme |
Mol. Mass.: | 98290.10 |
Organism: | Homo sapiens (Human) |
Description: | Q9HBA0 |
Residue: | 871 |
Sequence: | MADSSEGPRAGPGEVAELPGDESGTPGGEAFPLSSLANLFEGEDGSLSPSPADASRPAGP
GDGRPNLRMKFQGAFRKGVPNPIDLLESTLYESSVVPGPKKAPMDSLFDYGTYRHHSSDN
KRWRKKIIEKQPQSPKAPAPQPPPILKVFNRPILFDIVSRGSTADLDGLLPFLLTHKKRL
TDEEFREPSTGKTCLPKALLNLSNGRNDTIPVLLDIAERTGNMREFINSPFRDIYYRGQT
ALHIAIERRCKHYVELLVAQGADVHAQARGRFFQPKDEGGYFYFGELPLSLAACTNQPHI
VNYLTENPHKKADMRRQDSRGNTVLHALVAIADNTRENTKFVTKMYDLLLLKCARLFPDS
NLEAVLNNDGLSPLMMAAKTGKIGIFQHIIRREVTDEDTRHLSRKFKDWAYGPVYSSLYD
LSSLDTCGEEASVLEILVYNSKIENRHEMLAVEPINELLRDKWRKFGAVSFYINVVSYLC
AMVIFTLTAYYQPLEGTPPYPYRTTVDYLRLAGEVITLFTGVLFFFTNIKDLFMKKCPGV
NSLFIDGSFQLLYFIYSVLVIVSAALYLAGIEAYLAVMVFALVLGWMNALYFTRGLKLTG
TYSIMIQKILFKDLFRFLLVYLLFMIGYASALVSLLNPCANMKVCNEDQTNCTVPTYPSC
RDSETFSTFLLDLFKLTIGMGDLEMLSSTKYPVVFIILLVTYIILTFVLLLNMLIALMGE
TVGQVSKESKHIWKLQWATTILDIERSFPVFLRKAFRSGEMVTVGKSSDGTPDRRWCFRV
DEVNWSHWNQNLGIINEDPGKNETYQYYGFSHTVGRLRRDRWSSVVPRVVELNKNSNPDE
VVVPLDSMGNPRCDGHQQGYPRKWRTDDAPL
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BDBM50195064 |
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n/a |
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Name | BDBM50195064 |
Synonyms: | CHEMBL3951293 |
Type | Small organic molecule |
Emp. Form. | C14H12N4O2S2 |
Mol. Mass. | 332.401 |
SMILES | Cc1nc(C)c(s1)-c1csc(Nc2ccc(cn2)C(O)=O)n1 |
Structure |
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