Target
Histone deacetylase
Ligand
BDBM29589
Substrate
pfHDAC-1 Substrate
Meas. Tech.
pfHDAC-1 Enzyme Assay
pH
7.5±n/a
Temperature
296.15±n/a K
IC50
1.8±0.2 nM
Km
30000±2000 nM
kcat
0.19±0.01 1/sec
Citation
 Patel, VMazitschek, RColeman, BNguyen, CUrgaonkar, SCortese, JBarker, RHGreenberg, ETang, WBradner, JESchreiber, SLDuraisingh, MTWirth, DFClardy, J Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum. J Med Chem 52:2185-7 (2009) [PubMed]  Article 
Target
Name:
Histone deacetylase
Synonyms:
Histone Deacetylase (pfHDAC-1)
Type:
Enzyme
Mol. Mass.:
51371.91
Organism:
Plasmodium falciparum (isolate 3D7)
Description:
Assays were performed using recombinant pfHDAC-1 expressed and purified from S2 insect cells.
Residue:
449
Sequence:
MSNRKKVAYFHDPDIGSYYYGAGHPMKPQRIRMTHSLIVSYNLYKYMEVYRPHKSDVNELTLFHDYEYIDFLSSISLENYREFTYQLKRFNVGEATDCPVFDGLFQFQQSCAGASIDGASKLNHHCADICVNWSGGLHHAKMSEASGFCYINDIVLGILELLKYHARVMYIDIDVHHGDGVEEAFYVTHRVMTVSFHKFGDYFPGTGDITDVGVNHGKYYSVNVPLNDGMTDDAFVDLFKVVIDKCVQTYRPGAIIIQCGADSLTGDRLGRFNLTIKGHARCVEHVRSYNIPLLVLGGGGYTIRNVSRCWAYETGVVLNKHHEMPDQISLNDYYDYYAPDFQLHLQPSNIPNYNSPEHLSRIKMKIAENLRHIEHAPGVQFSYVPPDFFNSDIDDESDKNQYELKDDSGGGRAPGTRAKEHSTTHHLRRKNYDDDFFDLSDRDQSIVPY
  
Inhibitor
Name:
BDBM29589
Synonyms:
Faridak | LBH-589 | LBH-589B | Panobinostat | US10722597, Compound Panobinostat
Type:
Small organic molecule
Emp. Form.:
C21H23N3O2
Mol. Mass.:
349.4262
SMILES:
Cc1[nH]c2ccccc2c1CCNCc1ccc(\C=C\C(=O)NO)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
pfHDAC-1 Substrate
Synonyms:
n/a
Type:
fluorogenic, acetylated peptide
Mol. Mass.:
1609.93
Organism:
n/a
Description:
n/a
Residue:
15
Sequence:
ACLEGLYLYSACAMC