Target
Histone deacetylase 1
Ligand
BDBM25237
Substrate
Fluor de Lys-H4-AcK16
Meas. Tech.
HDAC Activity Assay
pH
8±n/a
Temperature
295.15±n/a K
IC50
10±n/a nM
Citation
 Andrews, DMGibson, KMGraham, MAMatusiak, ZSRoberts, CAStokes, ESBrady, MCChresta, CM Design and campaign synthesis of pyridine-based histone deacetylase inhibitors. Bioorg Med Chem Lett 18:2525-9 (2008) [PubMed]  Article 
Target
Name:
Histone deacetylase 1
Synonyms:
Cereblon/Histone deacetylase 1 | HD1 | HDAC1 | HDAC1_HUMAN | Histone deacetylase 1 (HDAC1) | Human HDAC1 | RPD3L1
Type:
Enzyme
Mol. Mass.:
55090.27
Organism:
Homo sapiens (Human)
Description:
Q13547
Residue:
482
Sequence:
MAQTQGTRRKVCYYYDGDVGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKANAEEMTKYHSDDYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVASAVKLNKQQTDIAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNYPLRDGIDDESYEAIFKPVMSKVMEMFQPSAVVLQCGSDSLSGDRLGCFNLTIKGHAKCVEFVKSFNLPMLMLGGGGYTIRNVARCWTYETAVALDTEIPNELPYNDYFEYFGPDFKLHISPSNMTNQNTNEYLEKIKQRLFENLRMLPHAPGVQMQAIPEDAIPEESGDEDEDDPDKRISICSSDKRIACEEEFSDSEEEGEGGRKNSSNFKKAKRVKTEDEKEKDPEEKKEVTEEEKTKEEKPEAKGVKEEVKLA
  
Inhibitor
Name:
BDBM25237
Synonyms:
N-(2-aminophenyl)-4-{3-cyano-5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl}benzamide | aminomethylpyridine-based compound, 14b
Type:
Small organic molecule
Emp. Form.:
C26H28N6O
Mol. Mass.:
440.5401
SMILES:
CCN1CCN(Cc2cnc(-c3ccc(cc3)C(=O)Nc3ccccc3N)c(c2)C#N)CC1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Fluor de Lys-H4-AcK16
Synonyms:
Biomol KI-174 | acetylated histone H4 lysine-16
Type:
fluorogenic, acetylated peptide substrate
Mol. Mass.:
1841.13
Organism:
n/a
Description:
It is based on residues from histone H4 (12-16).
Residue:
17
Sequence:
LYSGLYGLYALALYSAC