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Assay Detail

CHEMBL857631

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Binding
Inhibitory activity against histone deacetylase (HDAC) enzyme derived from partially purified extracts of human HeLa cells using [3H]11 as radioligand
17
Total Activities
17
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

Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 2.
Colletti SL, Myers RW, Darkin-Rattray SJ, Gurnett AM, Dulski PM, Galuska S, Allocco JJ, Ayer MB, Li C, Lim J, Crumley TM, Cannova C, Schmatz DM, Wyvratt MJ, Fisher MH, Meinke PT.
Bioorg Med Chem Lett (2001) 11 : 113 -117
PubMed 11206439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.71 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1793991 1 9.70
CHEMBL1793985 1 9.70
CHEMBL430060 APICIDIN 1 9.00
CHEMBL1793992 1 8.89
CHEMBL1793989 1 8.70
CHEMBL1793984 1 8.40
CHEMBL1793982 1 7.89
CHEMBL1793990 1 7.82
CHEMBL1793974 1 7.47
CHEMBL1793983 1 7.17
CHEMBL1793973 1 7.07
CHEMBL1793968 1 7.04
CHEMBL1793969 1 6.59
CHEMBL1793972 1 6.48
CHEMBL1793978 1 6.38
CHEMBL279636 1 6.37
CHEMBL1793981 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1793991 IC50 = 0.2 nM 9.70
CHEMBL1793985 IC50 = 0.2 nM 9.70
CHEMBL430060 APICIDIN IC50 = 1.0 nM 9.00
CHEMBL1793992 IC50 = 1.3 nM 8.89
CHEMBL1793989 IC50 = 2.0 nM 8.70
CHEMBL1793984 IC50 = 4.0 nM 8.40
CHEMBL1793982 IC50 = 13.0 nM 7.89
CHEMBL1793990 IC50 = 15.0 nM 7.82
CHEMBL1793974 IC50 = 34.0 nM 7.47
CHEMBL1793983 IC50 = 67.0 nM 7.17
CHEMBL1793973 IC50 = 86.0 nM 7.07
CHEMBL1793968 IC50 = 91.0 nM 7.04
CHEMBL1793969 IC50 = 257.0 nM 6.59
CHEMBL1793972 IC50 = 330.0 nM 6.48
CHEMBL1793978 IC50 = 419.0 nM 6.38
CHEMBL279636 IC50 = 430.0 nM 6.37
CHEMBL1793981 IC50 = 444.0 nM 6.35