Reaction Details |
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Target | Transient receptor potential cation channel subfamily V member 4 |
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Ligand | BDBM50521996 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1885908 (CHEMBL4387490) |
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IC50 | 1.1±n/a nM |
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Citation | Sami, Y; Morita, M; Kubota, H; Hirabayashi, R; Seo, R; Nakagawa, N Discovery of a novel orally active TRPV4 inhibitor: Part 1. Optimization from an HTS hit. Bioorg Med Chem27:3775-3787 (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_RAT | Trpv4 | Vanilloid receptor | Vroac |
Type: | PROTEIN |
Mol. Mass.: | 98016.72 |
Organism: | Rattus norvegicus |
Description: | ChEMBL_1514408 |
Residue: | 871 |
Sequence: | MADPGDGPRAAPGDVAEPPGDESGTSGGEAFPLSSLANLFEGEEGSSSLSPVDASRPAGP
GDGRPNLRMKFQGAFRKGVPNPIDLLESTLYESSVVPGPKKAPMDSLFDYGTYRHHPSDN
KRWRRKVVEKQPQSPKAPAPQPPPILKVFNRPILFDIVSRGSTADLDGLLSYLLTHKKRL
TDEEFREPSTGKTCLPKALLNLSNGRNDTIPVLLDIAERTGNMREFINSPFRDIYYRGQT
ALHIAIERRCKHYVELLVAQGADVHAQARGRFFQPKDEGGYFYFGELPLSLAACTNQPHI
VNYLTENPHKKADMRRQDSRGNTVLHALVAIADNTRENTKFVTKMYDLLLLKCSRLFPDS
NLETVLNNDGLSPLMMAAKTGKIGVFQHIIRREVTDEDTRHLSRKFKDWAYGPVYSSLYD
LSSLDTCGEEVSVLEILVYNSKIENRHEMLAVEPINELLRDKWRKFGAVSFYINVVSYLC
AMVIFTLTAYYQPLEGTPPYPYRTTVDYLRLAGEVITLLTGVLFFFTSIKDLFMKKCPGV
NSLFVDGSFQLLYFIYSVLVVVSAALYLAGIEAYLAVMVFALVLGWMNALYFTRGLKLTG
TYSIMIQKILFKDLFRFLLVYLLFMIGYASALVTLLNPCTNMKVCNEDQSNCTVPSYPAC
RDSETFSAFLLDLFKLTIGMGDLEMLSSAKYPVVFILLLVTYIILTFVLLLNMLIALMGE
TVGQVSKESKHIWKLQWATTILDIERSFPVFLRKAFRSGEMVTVGKSSDGTPDRRWCFRV
DEVNWSHWNQNLGIINEDPGKSEIYQYYGFSHTMGRLRRDRWSSVVPRVVELNKNSGTDE
VVVPLDNLGNPNCDGHQQGYAPKWRAEDAPL
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BDBM50521996 |
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n/a |
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Name | BDBM50521996 |
Synonyms: | CHEMBL4459940 |
Type | Small organic molecule |
Emp. Form. | C25H32Cl2FN5OS |
Mol. Mass. | 540.524 |
SMILES | Cl.Cl.Cc1c(cnn1-c1ccc(F)cc1)C(=O)Nc1nc(C2CCC2)c(CCN2CCCCC2)s1 |
Structure |
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