| Reaction Details |
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 | Report a problem with these data |
| Target | Histone deacetylase 4 [653-1084,H976Y] |
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| Ligand | BDBM25164 |
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| Substrate/Competitor | BDBM25143 |
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| Meas. Tech. | HDAC Activity Assay |
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| Temperature | 298.15±n/a K |
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| IC50 | 370±n/a nM |
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| Comments | extracted |
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| Citation |  Jones, P; Bottomley, MJ; Carfí, A; Cecchetti, O; Ferrigno, F; Lo Surdo, P; Ontoria, JM; Rowley, M; Scarpelli, R; Schultz-Fademrecht, C; Steinkühler, C 2-Trifluoroacetylthiophenes, a novel series of potent and selective class II histone deacetylase inhibitors. Bioorg Med Chem Lett18:3456-61 (2008) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Histone deacetylase 4 [653-1084,H976Y] |
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| Name: | Histone deacetylase 4 [653-1084,H976Y] |
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| Synonyms: | HDAC4 | HDAC4_HUMAN | Histone Deacetylase 4 (HDAC4) Mutant (H976Y) | Histone deacetylase 4 gain of function (GOF) mutant | KIAA0288 |
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| Type: | Catalytic domain |
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| Mol. Mass.: | 46476.72 |
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| Organism: | Homo sapiens (Human) |
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| Description: | His-tagged HDAC4 GOF(gain of function, H976Y) catalytic domains (T653-L1084) was expressed in E.coli and purified by Nickel-Chelation affinity chromatography and anion exchange (MonoQ) chromatography. |
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| Residue: | 432 |
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| Sequence: | TTGLVYDTLMLKHQCTCGSSSSHPEHAGRIQSIWSRLQETGLRGKCECIRGRKATLEELQ
TVHSEAHTLLYGTNPLNRQKLDSKKLLGSLASVFVRLPCGGVGVDSDTIWNEVHSAGAAR
LAVGCVVELVFKVATGELKNGFAVVRPPGHHAEESTPMGFCYFNSVAVAAKLLQQRLSVS
KILIVDWDVHHGNGTQQAFYSDPSVLYMSLHRYDDGNFFPGSGAPDEVGTGPGVGFNVNM
AFTGGLDPPMGDAEYLAAFRTVVMPIASEFAPDVVLVSSGFDAVEGHPTPLGGYNLSARC
FGYLTKQLMGLAGGRIVLALEGGYDLTAICDASEACVSALLGNELDPLPEKVLQQRPNAN
AVRSMEKVMEIHSKYWRCLQRTTSTAGRSLIEAQTCENEEAETVTAMASLSVGVKPAEKR
PDEEPMEEEPPL
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| BDBM25164 |
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| BDBM25143 |
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| Name | BDBM25164 |
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| Synonyms: | 2,2,2-trifluoro-1-[5-({3-phenyl-5H,6H,7H,8H-imidazo[1,2-a]pyrazin-7-yl}carbonyl)thiophen-2-yl]ethan-1-one | CHEMBL496094 | thiophene derivative, 3j |
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| Type | Small organic molecule |
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| Emp. Form. | C19H14F3N3O2S |
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| Mol. Mass. | 405.394 |
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| SMILES | FC(F)(F)C(=O)c1ccc(s1)C(=O)N1CCn2c(C1)ncc2-c1ccccc1 |
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| Structure | 
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