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Assay Detail

CHEMBL1016194

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

Functional
Antimalarial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Confidence 1 — Organism
Curated By Autocuration

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
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 7.28 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL491254 1 7.82
CHEMBL99 TRICHOSTATIN 1.0 1 7.80
CHEMBL447806 1 7.70
CHEMBL483254 PANOBINOSTAT 4.0 1 7.68
CHEMBL307765 1 7.66
CHEMBL490230 1 7.62
CHEMBL489218 1 7.52
CHEMBL430060 APICIDIN 1 7.48
CHEMBL491253 1 7.46
CHEMBL523640 1 7.33
CHEMBL490228 1 7.30
CHEMBL489010 1 7.28
CHEMBL490032 1 7.24
CHEMBL519035 1 7.23
CHEMBL446605 1 7.17
CHEMBL508866 1 7.00
CHEMBL485506 1 6.85
CHEMBL98 VORINOSTAT 4.0 1 6.68
CHEMBL491452 1 6.54
CHEMBL489011 1 6.30
CHEMBL490229 1 -
CHEMBL86537 SPLITOMICIN 1 -
CHEMBL27759 ENTINOSTAT 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL491254 IC50 = 15.0 nM 7.82
CHEMBL99 TRICHOSTATIN IC50 = 16.0 nM 7.80
CHEMBL447806 IC50 = 20.0 nM 7.70
CHEMBL483254 PANOBINOSTAT IC50 = 21.0 nM 7.68
CHEMBL307765 IC50 = 22.0 nM 7.66
CHEMBL490230 IC50 = 24.0 nM 7.62
CHEMBL489218 IC50 = 30.0 nM 7.52
CHEMBL430060 APICIDIN IC50 = 33.0 nM 7.48
CHEMBL491253 IC50 = 35.0 nM 7.46
CHEMBL523640 IC50 = 47.0 nM 7.33
CHEMBL490228 IC50 = 50.0 nM 7.30
CHEMBL489010 IC50 = 53.0 nM 7.28
CHEMBL490032 IC50 = 57.0 nM 7.24
CHEMBL519035 IC50 = 59.0 nM 7.23
CHEMBL446605 IC50 = 68.0 nM 7.17
CHEMBL508866 IC50 = 99.0 nM 7.00
CHEMBL485506 IC50 = 142.0 nM 6.85
CHEMBL98 VORINOSTAT IC50 = 210.0 nM 6.68
CHEMBL491452 IC50 = 288.0 nM 6.54
CHEMBL489011 IC50 = 498.0 nM 6.30
CHEMBL490229 IC50 > 500.0 nM -
CHEMBL86537 SPLITOMICIN IC50 > 10000.0 nM -
CHEMBL27759 ENTINOSTAT IC50 > 10000.0 nM -