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Assay Detail

CHEMBL5043884

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

Binding
Inhibition of human recombinant HDAC1 using Boc-Lys(acetyl)-AMC substrate incubated for 2 hrs by fluorescence based assay
24
Total Activities
24
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

Potent Hydrazide-Based HDAC Inhibitors with a Superior Pharmacokinetic Profile for Efficient Treatment of Acute Myeloid Leukemia In Vivo.
Jiang Y, Xu J, Yue K, Huang C, Qin M, Chi D, Yu Q, Zhu Y, Hou X, Xu T, Li M, Chou CJ, Li X.
J Med Chem (2022) 65 : 285 -302
PubMed 34942071 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.03 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5083249 1 8.52
CHEMBL5078985 1 8.45
CHEMBL5087431 1 8.42
CHEMBL5086141 1 8.41
CHEMBL5080511 1 8.33
CHEMBL4597954 1 8.29
CHEMBL5093099 1 8.13
CHEMBL5083475 1 8.11
CHEMBL5084347 1 8.10
CHEMBL5093836 1 8.09
CHEMBL5086924 1 8.06
CHEMBL5089712 1 8.05
CHEMBL5084847 1 8.01
CHEMBL5073909 1 7.97
CHEMBL5081353 1 7.95
CHEMBL5089744 1 7.93
CHEMBL4526892 1 7.93
CHEMBL5089258 1 7.89
CHEMBL5087971 1 7.86
CHEMBL5073024 1 7.86
CHEMBL5074837 1 7.79
CHEMBL5075150 1 7.77
CHEMBL5075425 1 7.68
CHEMBL5076715 1 7.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5083249 IC50 = 3.01 nM 8.52
CHEMBL5078985 IC50 = 3.52 nM 8.45
CHEMBL5087431 IC50 = 3.79 nM 8.42
CHEMBL5086141 IC50 = 3.91 nM 8.41
CHEMBL5080511 IC50 = 4.66 nM 8.33
CHEMBL4597954 IC50 = 5.17 nM 8.29
CHEMBL5093099 IC50 = 7.4 nM 8.13
CHEMBL5083475 IC50 = 7.85 nM 8.11
CHEMBL5084347 IC50 = 7.98 nM 8.10
CHEMBL5093836 IC50 = 8.22 nM 8.09
CHEMBL5086924 IC50 = 8.8 nM 8.06
CHEMBL5089712 IC50 = 8.91 nM 8.05
CHEMBL5084847 IC50 = 9.73 nM 8.01
CHEMBL5073909 IC50 = 10.73 nM 7.97
CHEMBL5081353 IC50 = 11.28 nM 7.95
CHEMBL5089744 IC50 = 11.71 nM 7.93
CHEMBL4526892 IC50 = 11.81 nM 7.93
CHEMBL5089258 IC50 = 12.93 nM 7.89
CHEMBL5087971 IC50 = 13.76 nM 7.86
CHEMBL5073024 IC50 = 13.7 nM 7.86
CHEMBL5074837 IC50 = 16.15 nM 7.79
CHEMBL5075150 IC50 = 17.1 nM 7.77
CHEMBL5075425 IC50 = 20.76 nM 7.68
CHEMBL5076715 IC50 = 58.31 nM 7.23