Reaction Details |
| Report a problem with these data |
Target | Histone deacetylase 4 [653-1084,H976Y] |
---|
Ligand | BDBM25159 |
---|
Substrate/Competitor | BDBM25143 |
---|
Meas. Tech. | HDAC Activity Assay |
---|
Temperature | 298.15±n/a K |
---|
IC50 | 280±n/a nM |
---|
Comments | extracted |
---|
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 |
---|
More Info.: | Get all data from this article, Solution Info, Assay Method |
---|
|
Histone deacetylase 4 [653-1084,H976Y] |
---|
Name: | Histone deacetylase 4 [653-1084,H976Y] |
Synonyms: | HDAC4 | HDAC4_HUMAN | Histone Deacetylase 4 (HDAC4) Mutant (H976Y) | Histone deacetylase 4 gain of function (GOF) mutant | KIAA0288 |
Type: | Catalytic domain |
Mol. Mass.: | 46476.72 |
Organism: | Homo sapiens (Human) |
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. |
Residue: | 432 |
Sequence: | TTGLVYDTLMLKHQCTCGSSSSHPEHAGRIQSIWSRLQETGLRGKCECIRGRKATLEELQ
TVHSEAHTLLYGTNPLNRQKLDSKKLLGSLASVFVRLPCGGVGVDSDTIWNEVHSAGAAR
LAVGCVVELVFKVATGELKNGFAVVRPPGHHAEESTPMGFCYFNSVAVAAKLLQQRLSVS
KILIVDWDVHHGNGTQQAFYSDPSVLYMSLHRYDDGNFFPGSGAPDEVGTGPGVGFNVNM
AFTGGLDPPMGDAEYLAAFRTVVMPIASEFAPDVVLVSSGFDAVEGHPTPLGGYNLSARC
FGYLTKQLMGLAGGRIVLALEGGYDLTAICDASEACVSALLGNELDPLPEKVLQQRPNAN
AVRSMEKVMEIHSKYWRCLQRTTSTAGRSLIEAQTCENEEAETVTAMASLSVGVKPAEKR
PDEEPMEEEPPL
|
|
|
BDBM25159 |
---|
BDBM25143 |
---|
Name | BDBM25159 |
Synonyms: | CHEMBL462208 | N-[(1S)-1-phenylethyl]-5-(2,2,2-trifluoroacetyl)thiophene-2-carboxamide | thiophene derivative, 3e |
Type | Small organic molecule |
Emp. Form. | C15H12F3NO2S |
Mol. Mass. | 327.321 |
SMILES | C[C@H](NC(=O)c1ccc(s1)C(=O)C(F)(F)F)c1ccccc1 |r| |
Structure |
|