Reaction Details |
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Target | Transient receptor potential cation channel subfamily V member 4 |
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Ligand | BDBM50450507 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1742691 (CHEMBL4158441) |
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IC50 | 1000±n/a nM |
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Citation | Brnardic, EJ; Ye, G; Brooks, C; Donatelli, C; Barton, L; McAtee, J; Sanchez, RM; Shu, A; Erhard, K; Terrell, L; Graczyk-Millbrandt, G; He, Y; Costell, MH; Behm, DJ; Roethke, T; Stoy, P; Holt, DA; Lawhorn, BG Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4). J Med Chem61:9738-9755 (2018) [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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BDBM50450507 |
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n/a |
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Name | BDBM50450507 |
Synonyms: | CHEMBL4175922 |
Type | Small organic molecule |
Emp. Form. | C18H15Cl2FN2O4S |
Mol. Mass. | 445.292 |
SMILES | O[C@@H]1CN(C[C@H]1COc1ccc(C#N)c(F)c1)S(=O)(=O)c1ccc(Cl)cc1Cl |r| |
Structure |
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