Reaction Details |
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Target | Transient receptor potential cation channel subfamily V member 4 |
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Ligand | BDBM50505543 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1823163 (CHEMBL4322927) |
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IC50 | 3.8±n/a nM |
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Citation | Brooks, CA; Barton, LS; Behm, DJ; Brnardic, EJ; Costell, MH; Holt, DA; Jolivette, LJ; Matthews, JM; McAtee, JJ; McCleland, BW; Patterson, JR; Pero, JE; Rivero, RA; Roethke, TJ; Sanchez, RM; Shenje, R; Terrell, LR; Lawhorn, BG Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4). J Med Chem62:9270-9280 (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 |
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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BDBM50505543 |
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n/a |
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Name | BDBM50505543 |
Synonyms: | CHEMBL4454801 |
Type | Small organic molecule |
Emp. Form. | C19H16FN3O5S |
Mol. Mass. | 417.411 |
SMILES | OC[C@]1(O)CN(C[C@@H]1Oc1ccc(C#N)c(F)c1)S(=O)(=O)c1ccccc1C#N |r| |
Structure |
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