Reaction Details |
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Target | Transient receptor potential cation channel subfamily V member 4 |
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Ligand | BDBM50192821 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1699600 (CHEMBL4050582) |
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IC50 | 29±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; Yamanada, N; Tanimura, M; Nagamatsu, D; Asaki, T; Horita, N; Yamamoto, M; Hinata, M; Soga, M; Imai, M; Morioka, Y; Kanemasa, T; Sakaguchi, G; Iso, Y Pharmacological evaluation of novel (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives as TRPV4 antagonists for the treatment of pain. Bioorg Med Chem25:2177-2190 (2017) [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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BDBM50192821 |
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n/a |
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Name | BDBM50192821 |
Synonyms: | CHEMBL2133556 |
Type | Small organic molecule |
Emp. Form. | C26H28F3N3O2 |
Mol. Mass. | 471.5146 |
SMILES | Cc1c(cc(-c2ccccc2)n1CCCN1CCOCC1)C(=O)Nc1cccc(c1)C(F)(F)F |
Structure |
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