Reaction Details
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Target
Histone deacetylase
Ligand
BDBM25142
Substrate
pfHDAC-1 Substrate
Meas. Tech.
pfHDAC-1 Enzyme Assay
pH
7.5±n/a
Temperature
296.15±n/a K
IC50
1±0.1 nM
Km
30000±2000 nM
kcat
0.19±0.01 1/sec
Citation
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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:
BDBM25142
Synonyms:
(3S,6S,9S,15aR)-9-[(2R)-butan-2-yl]-6-[(1-methoxy-1H-indol-3-yl)methyl]-3-(6-oxooctyl)-tetradecahydro-1H-pyrido[1,2-a][,,,]cyclododecane-1,4,7,10-tetrone | Apicidin
Type:
Small organic molecule
Emp. Form.:
C34H49N5O6
Mol. Mass.:
623.7828
SMILES:
CCC(C)[C@@H]1NC(=O)[C@H](Cc2cn(OC)c3ccccc23)NC(=O)[C@H](CCCCCC(=O)CC)NC(=O)[C@H]2CCCCN2C1=O |r|
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