| Reaction Details |
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 | Report a problem with these data |
| Target | Transient receptor potential cation channel subfamily V member 4 |
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| Ligand | BDBM50502626 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1808132 (CHEMBL4307491) |
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| IC50 | 1.5±n/a nM |
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| Citation |  Brooks, CA; Barton, LS; Behm, DJ; Eidam, HS; Fox, RM; Hammond, M; Hoang, TH; Holt, DA; Hilfiker, MA; Lawhorn, BG; Patterson, JR; Stoy, P; Roethke, TJ; Ye, G; Zhao, S; Thorneloe, KS; Goodman, KB; Cheung, M Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4). ACS Med Chem Lett10:1228-1233 (2019) [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 |
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| Synonyms: | TRPV4 | TRPV4_HUMAN | Transient receptor potential cation channel subfamily V member 4 (TRPV4) | VRL2 | VROAC |
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| Type: | Enzyme |
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| Mol. Mass.: | 98290.10 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q9HBA0 |
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| Residue: | 871 |
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| Sequence: | MADSSEGPRAGPGEVAELPGDESGTPGGEAFPLSSLANLFEGEDGSLSPSPADASRPAGP
GDGRPNLRMKFQGAFRKGVPNPIDLLESTLYESSVVPGPKKAPMDSLFDYGTYRHHSSDN
KRWRKKIIEKQPQSPKAPAPQPPPILKVFNRPILFDIVSRGSTADLDGLLPFLLTHKKRL
TDEEFREPSTGKTCLPKALLNLSNGRNDTIPVLLDIAERTGNMREFINSPFRDIYYRGQT
ALHIAIERRCKHYVELLVAQGADVHAQARGRFFQPKDEGGYFYFGELPLSLAACTNQPHI
VNYLTENPHKKADMRRQDSRGNTVLHALVAIADNTRENTKFVTKMYDLLLLKCARLFPDS
NLEAVLNNDGLSPLMMAAKTGKIGIFQHIIRREVTDEDTRHLSRKFKDWAYGPVYSSLYD
LSSLDTCGEEASVLEILVYNSKIENRHEMLAVEPINELLRDKWRKFGAVSFYINVVSYLC
AMVIFTLTAYYQPLEGTPPYPYRTTVDYLRLAGEVITLFTGVLFFFTNIKDLFMKKCPGV
NSLFIDGSFQLLYFIYSVLVIVSAALYLAGIEAYLAVMVFALVLGWMNALYFTRGLKLTG
TYSIMIQKILFKDLFRFLLVYLLFMIGYASALVSLLNPCANMKVCNEDQTNCTVPTYPSC
RDSETFSTFLLDLFKLTIGMGDLEMLSSTKYPVVFIILLVTYIILTFVLLLNMLIALMGE
TVGQVSKESKHIWKLQWATTILDIERSFPVFLRKAFRSGEMVTVGKSSDGTPDRRWCFRV
DEVNWSHWNQNLGIINEDPGKNETYQYYGFSHTVGRLRRDRWSSVVPRVVELNKNSNPDE
VVVPLDSMGNPRCDGHQQGYPRKWRTDDAPL
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| BDBM50502626 |
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| n/a |
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| Name | BDBM50502626 |
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| Synonyms: | CHEMBL4536058 |
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| Type | Small organic molecule |
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| Emp. Form. | C25H26N6O2 |
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| Mol. Mass. | 442.5129 |
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| SMILES | C[C@]1(Cn2cnc3ccc(cc23)C#N)CCC[C@@]2(CN(C(=O)O2)c2cnc(cn2)C2CC2)C1 |r| |
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| Structure | 
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