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Assay Detail

CHEMBL821898

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Binding
Inhibitory activity against histone deacetylase (HDAC) derived from partially purified extracts of human HeLa cells
32
Total Activities
32
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 1.
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 : 107 -111
PubMed 11206438 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.55 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1793811 1 9.70
CHEMBL1793822 1 9.52
CHEMBL1793816 1 9.40
CHEMBL1793823 1 9.00
CHEMBL1793810 1 9.00
CHEMBL1793947 1 9.00
CHEMBL1793938 1 8.70
CHEMBL1793945 1 8.52
CHEMBL1793941 1 8.30
CHEMBL1793937 1 8.22
CHEMBL1793819 1 8.15
CHEMBL1793827 1 7.82
CHEMBL1793820 1 7.75
CHEMBL1793824 1 7.52
CHEMBL1793825 1 7.41
CHEMBL1793813 1 7.22
CHEMBL1793807 1 7.21
CHEMBL1793944 1 7.14
CHEMBL1793936 1 7.13
CHEMBL1793826 1 6.96
CHEMBL1793939 1 6.96
CHEMBL1793808 1 6.84
CHEMBL1793818 1 6.75
CHEMBL1793946 1 6.63
CHEMBL1793828 1 6.55
CHEMBL1793940 1 6.49
CHEMBL1793809 1 6.35
CHEMBL1793942 1 6.16
CHEMBL1793821 1 6.07
CHEMBL1793806 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1793811 IC50 = 0.2 nM 9.70
CHEMBL1793822 IC50 = 0.3 nM 9.52
CHEMBL1793816 IC50 = 0.4 nM 9.40
CHEMBL1793823 IC50 = 1.0 nM 9.00
CHEMBL1793810 IC50 = 1.0 nM 9.00
CHEMBL1793947 IC50 = 1.0 nM 9.00
CHEMBL1793938 IC50 = 2.0 nM 8.70
CHEMBL1793945 IC50 = 3.0 nM 8.52
CHEMBL1793941 IC50 = 5.0 nM 8.30
CHEMBL1793937 IC50 = 6.0 nM 8.22
CHEMBL1793819 IC50 = 7.0 nM 8.15
CHEMBL1793827 IC50 = 15.0 nM 7.82
CHEMBL1793820 IC50 = 18.0 nM 7.75
CHEMBL1793824 IC50 = 30.0 nM 7.52
CHEMBL1793825 IC50 = 39.0 nM 7.41
CHEMBL1793813 IC50 = 60.0 nM 7.22
CHEMBL1793807 IC50 = 61.0 nM 7.21
CHEMBL1793944 IC50 = 73.0 nM 7.14
CHEMBL1793936 IC50 = 74.0 nM 7.13
CHEMBL1793826 IC50 = 110.0 nM 6.96
CHEMBL1793939 IC50 = 110.0 nM 6.96
CHEMBL1793808 IC50 = 144.0 nM 6.84
CHEMBL1793818 IC50 = 180.0 nM 6.75
CHEMBL1793946 IC50 = 235.0 nM 6.63
CHEMBL1793828 IC50 = 282.0 nM 6.55
CHEMBL1793940 IC50 = 326.0 nM 6.49
CHEMBL1793809 IC50 = 450.0 nM 6.35
CHEMBL1793942 IC50 = 700.0 nM 6.16
CHEMBL1793821 IC50 = 848.0 nM 6.07
CHEMBL1793806 IC50 = 1450.0 nM 5.84
CHEMBL1793817 IC50 = 2000.0 nM 5.70
CHEMBL1793812 IC50 < 0.1 nM -