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Assay Detail

CHEMBL1960758

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

Binding
Inhibition of HDAC expressed in human HeLa cells after 1 hr by fluorescence analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Histone deacetylase (CHEMBL2093865)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei.
Kelly JM, Taylor MC, Horn D, Loza E, Kalvinsh I, Björkling F.
Bioorg Med Chem Lett (2012) 22 : 1886 -1890
PubMed 22326398 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.31 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1958429 1 8.00
CHEMBL1958439 1 7.89
CHEMBL453755 1 7.70
CHEMBL1958436 1 7.70
CHEMBL1958433 1 7.66
CHEMBL1958434 1 7.66
CHEMBL1958437 1 7.66
CHEMBL272847 1 7.64
CHEMBL490018 1 7.58
CHEMBL1958430 1 7.55
CHEMBL1955942 1 7.54
CHEMBL1958438 1 7.38
CHEMBL1958440 1 7.32
CHEMBL1958428 1 7.17
CHEMBL1958422 1 7.08
CHEMBL1958424 1 6.91
CHEMBL1958432 1 6.88
CHEMBL1958423 1 6.83
CHEMBL1958425 1 6.73
CHEMBL1958427 1 6.72
CHEMBL1958431 1 6.67
CHEMBL1958435 1 6.57
CHEMBL1958426 1 -
CHEMBL1955943 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1958429 IC50 = 10.0 nM 8.00
CHEMBL1958439 IC50 = 13.0 nM 7.89
CHEMBL453755 IC50 = 20.0 nM 7.70
CHEMBL1958436 IC50 = 20.0 nM 7.70
CHEMBL1958433 IC50 = 22.0 nM 7.66
CHEMBL1958434 IC50 = 22.0 nM 7.66
CHEMBL1958437 IC50 = 22.0 nM 7.66
CHEMBL272847 IC50 = 23.0 nM 7.64
CHEMBL490018 IC50 = 26.0 nM 7.58
CHEMBL1958430 IC50 = 28.0 nM 7.55
CHEMBL1955942 IC50 = 29.0 nM 7.54
CHEMBL1958438 IC50 = 42.0 nM 7.38
CHEMBL1958440 IC50 = 48.0 nM 7.32
CHEMBL1958428 IC50 = 68.0 nM 7.17
CHEMBL1958422 IC50 = 84.0 nM 7.08
CHEMBL1958424 IC50 = 123.0 nM 6.91
CHEMBL1958432 IC50 = 132.0 nM 6.88
CHEMBL1958423 IC50 = 149.0 nM 6.83
CHEMBL1958425 IC50 = 187.0 nM 6.73
CHEMBL1958427 IC50 = 191.0 nM 6.72
CHEMBL1958431 IC50 = 212.0 nM 6.67
CHEMBL1958435 IC50 = 269.0 nM 6.57
CHEMBL1958426 IC50 - -
CHEMBL1955943 IC50 - -