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Assay Detail

CHEMBL1016193

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Cell Type S2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase (CHEMBL5541)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.
Patel V, Mazitschek R, Coleman B, Nguyen C, Urgaonkar S, Cortese J, Barker RH, Greenberg E, Tang W, Bradner JE, Schreiber SL, Duraisingh MT, Wirth DF, Clardy J.
J Med Chem (2009) 52 : 2185 -2187
PubMed 19317450 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.49 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 9.22
CHEMBL430060 APICIDIN 1 9.00
CHEMBL483254 PANOBINOSTAT 4.0 1 8.74
CHEMBL490032 1 7.82
CHEMBL519035 1 7.70
CHEMBL490229 1 7.66
CHEMBL307765 1 7.44
CHEMBL491254 1 7.43
CHEMBL490230 1 7.43
CHEMBL447806 1 7.39
CHEMBL490228 1 7.37
CHEMBL446605 1 7.35
CHEMBL491253 1 7.31
CHEMBL508866 1 7.23
CHEMBL523640 1 7.23
CHEMBL489011 1 7.23
CHEMBL98 VORINOSTAT 4.0 1 7.23
CHEMBL491452 1 7.05
CHEMBL489218 1 7.05
CHEMBL489010 1 6.97
CHEMBL485506 1 6.96
CHEMBL27759 ENTINOSTAT 3.0 1 6.03
CHEMBL86537 SPLITOMICIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN IC50 = 0.6 nM 9.22
CHEMBL430060 APICIDIN IC50 = 1.0 nM 9.00
CHEMBL483254 PANOBINOSTAT IC50 = 1.8 nM 8.74
CHEMBL490032 IC50 = 15.0 nM 7.82
CHEMBL519035 IC50 = 20.0 nM 7.70
CHEMBL490229 IC50 = 22.0 nM 7.66
CHEMBL307765 IC50 = 36.0 nM 7.44
CHEMBL491254 IC50 = 37.0 nM 7.43
CHEMBL490230 IC50 = 37.0 nM 7.43
CHEMBL447806 IC50 = 41.0 nM 7.39
CHEMBL490228 IC50 = 43.0 nM 7.37
CHEMBL446605 IC50 = 45.0 nM 7.35
CHEMBL491253 IC50 = 49.0 nM 7.31
CHEMBL508866 IC50 = 59.0 nM 7.23
CHEMBL523640 IC50 = 59.0 nM 7.23
CHEMBL489011 IC50 = 59.0 nM 7.23
CHEMBL98 VORINOSTAT IC50 = 59.0 nM 7.23
CHEMBL491452 IC50 = 90.0 nM 7.05
CHEMBL489218 IC50 = 89.0 nM 7.05
CHEMBL489010 IC50 = 106.0 nM 6.97
CHEMBL485506 IC50 = 110.0 nM 6.96
CHEMBL27759 ENTINOSTAT IC50 = 940.0 nM 6.03
CHEMBL86537 SPLITOMICIN IC50 > 10000.0 nM -