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Assay Detail

CHEMBL4606150

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

Binding
Inhibition of human recombinant HDAC1 pre-incubated for 30 mins before Ac-Leu- Gly-Lys(Ac)-AMC substrate addition and measured after 90 mins by fluorescence based assay
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Achiral Derivatives of Hydroxamate AR-42 Potently Inhibit Class I HDAC Enzymes and Cancer Cell Proliferation.
Tng J, Lim J, Wu KC, Lucke AJ, Xu W, Reid RC, Fairlie DP.
J Med Chem (2020) 63 : 5956 -5971
PubMed 32383881 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 7.63 9.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4642874 1 9.14
CHEMBL4632569 1 9.03
CHEMBL4634521 1 8.70
CHEMBL4639966 1 8.70
CHEMBL4640304 1 8.70
CHEMBL4640415 1 8.70
CHEMBL4640356 1 8.52
CHEMBL4633137 1 8.52
CHEMBL4636523 1 8.52
CHEMBL4636734 1 8.40
CHEMBL4640407 1 8.40
CHEMBL4646011 1 8.40
CHEMBL4640593 1 8.30
CHEMBL4647467 1 8.30
CHEMBL4646613 1 8.30
CHEMBL4646320 1 8.22
CHEMBL4646451 1 8.22
CHEMBL4647859 1 8.15
CHEMBL4633570 1 8.10
CHEMBL4648856 1 8.10
CHEMBL4646610 1 8.05
CHEMBL4643094 1 8.05
CHEMBL4644988 1 8.00
CHEMBL4646807 1 8.00
CHEMBL4636298 1 8.00
CHEMBL4646862 1 7.96
CHEMBL4633692 1 7.92
CHEMBL4646185 1 7.92
CHEMBL4639928 1 7.92
CHEMBL4634357 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4642874 IC50 = 0.72 nM 9.14
CHEMBL4632569 IC50 = 0.94 nM 9.03
CHEMBL4639966 IC50 = 2.0 nM 8.70
CHEMBL4640304 IC50 = 2.0 nM 8.70
CHEMBL4640415 IC50 = 2.0 nM 8.70
CHEMBL4634521 IC50 = 2.0 nM 8.70
CHEMBL4640356 IC50 = 3.0 nM 8.52
CHEMBL4633137 IC50 = 3.0 nM 8.52
CHEMBL4636523 IC50 = 3.0 nM 8.52
CHEMBL4636734 IC50 = 4.0 nM 8.40
CHEMBL4640407 IC50 = 4.0 nM 8.40
CHEMBL4646011 IC50 = 4.0 nM 8.40
CHEMBL4646613 IC50 = 5.0 nM 8.30
CHEMBL4647467 IC50 = 5.0 nM 8.30
CHEMBL4640593 IC50 = 5.0 nM 8.30
CHEMBL4646320 IC50 = 6.0 nM 8.22
CHEMBL4646451 IC50 = 6.0 nM 8.22
CHEMBL4647859 IC50 = 7.0 nM 8.15
CHEMBL4633570 IC50 = 8.0 nM 8.10
CHEMBL4648856 IC50 = 8.0 nM 8.10
CHEMBL4646610 IC50 = 9.0 nM 8.05
CHEMBL4643094 IC50 = 9.0 nM 8.05
CHEMBL4644988 IC50 = 10.0 nM 8.00
CHEMBL4646807 IC50 = 10.0 nM 8.00
CHEMBL4636298 IC50 = 10.0 nM 8.00
CHEMBL4646862 IC50 = 11.0 nM 7.96
CHEMBL4646185 IC50 = 12.0 nM 7.92
CHEMBL4639928 IC50 = 12.0 nM 7.92
CHEMBL4633692 IC50 = 12.0 nM 7.92
CHEMBL4634357 IC50 = 15.0 nM 7.82
CHEMBL4643555 IC50 = 15.0 nM 7.82
CHEMBL4646512 IC50 = 16.0 nM 7.80
CHEMBL4633594 IC50 = 22.0 nM 7.66
CHEMBL4642831 IC50 = 22.0 nM 7.66
CHEMBL4633012 IC50 = 23.0 nM 7.64
CHEMBL191091 IC50 = 25.0 nM 7.60
CHEMBL4639790 IC50 = 28.0 nM 7.55
CHEMBL4645602 IC50 = 28.0 nM 7.55
CHEMBL4633750 IC50 = 29.0 nM 7.54
CHEMBL4634503 IC50 = 31.0 nM 7.51
CHEMBL4632914 IC50 = 41.0 nM 7.39
CHEMBL4642153 IC50 = 42.0 nM 7.38
CHEMBL4648635 IC50 = 42.0 nM 7.38
CHEMBL4644709 IC50 = 43.0 nM 7.37
CHEMBL4633075 IC50 = 43.0 nM 7.37
CHEMBL4647881 IC50 = 63.0 nM 7.20
CHEMBL356824 IC50 = 75.0 nM 7.12
CHEMBL4646653 IC50 = 93.0 nM 7.03
CHEMBL4643485 IC50 = 132.0 nM 6.88
CHEMBL190727 IC50 = 218.0 nM 6.66