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Assay Detail

CHEMBL907491

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

Binding
Inhibition of human HDAC1 expressed in domain of SMRT
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design of novel histone deacetylase inhibitors.
Siliphaivanh P, Harrington P, Witter DJ, Otte K, Tempest P, Kattar S, Kral AM, Fleming JC, Deshmukh SV, Harsch A, Secrist PJ, Miller TA.
Bioorg Med Chem Lett (2007) 17 : 4619 -4624
PubMed 17555962 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.93 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL250946 1 8.30
CHEMBL400919 1 7.68
CHEMBL251145 1 7.47
CHEMBL251337 1 7.46
CHEMBL251144 1 7.44
CHEMBL400920 1 7.35
CHEMBL398950 1 7.33
CHEMBL251338 1 7.33
CHEMBL251756 1 7.32
CHEMBL251336 1 7.25
CHEMBL251146 1 7.20
CHEMBL251757 1 7.03
CHEMBL400921 1 6.99
CHEMBL251544 1 6.71
CHEMBL398333 1 6.70
CHEMBL248718 1 6.70
CHEMBL248909 1 6.70
CHEMBL251546 1 6.64
CHEMBL249284 1 6.15
CHEMBL251545 1 5.14
CHEMBL16300 BENZOHYDROXAMATE 1 4.70
CHEMBL734 ACETOHYDROXAMIC ACID 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL250946 IC50 = 5.0 nM 8.30
CHEMBL400919 IC50 = 21.0 nM 7.68
CHEMBL251145 IC50 = 34.0 nM 7.47
CHEMBL251337 IC50 = 35.0 nM 7.46
CHEMBL251144 IC50 = 36.0 nM 7.44
CHEMBL400920 IC50 = 45.0 nM 7.35
CHEMBL398950 IC50 = 47.0 nM 7.33
CHEMBL251338 IC50 = 47.0 nM 7.33
CHEMBL251756 IC50 = 48.0 nM 7.32
CHEMBL251336 IC50 = 56.0 nM 7.25
CHEMBL251146 IC50 = 63.0 nM 7.20
CHEMBL251757 IC50 = 94.0 nM 7.03
CHEMBL400921 IC50 = 103.0 nM 6.99
CHEMBL251544 IC50 = 196.0 nM 6.71
CHEMBL398333 IC50 = 199.0 nM 6.70
CHEMBL248718 IC50 = 198.0 nM 6.70
CHEMBL248909 IC50 = 200.0 nM 6.70
CHEMBL251546 IC50 = 229.0 nM 6.64
CHEMBL249284 IC50 = 715.0 nM 6.15
CHEMBL251545 IC50 = 7195.0 nM 5.14
CHEMBL16300 BENZOHYDROXAMATE IC50 = 20000.0 nM 4.70
CHEMBL734 ACETOHYDROXAMIC ACID IC50 = 625000.0 nM -