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Assay Detail

CHEMBL4737686

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Binding
Inhibition of recombinant human HDAC7 using Ac-LGK(TFA)-AMC as substrate pre-incubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay
23
Total Activities
23
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 7 (CHEMBL2716)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

HDAC7 Inhibition by Phenacetyl and Phenylbenzoyl Hydroxamates.
Mak JYW,Wu KC,Gupta PK,Barbero S,McLaughlin MG,Lucke AJ,Tng J,Lim J,Loh Z,Sweet MJ,Reid RC,Liu L,Fairlie DP
J Med Chem (2021) 64 : 2186 -2204
PubMed 33570940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.49 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4761013 1 7.92
CHEMBL4748500 1 7.92
CHEMBL4799406 1 7.62
CHEMBL4751615 1 7.57
CHEMBL4776127 1 7.51
CHEMBL4762512 1 7.31
CHEMBL4776962 1 7.12
CHEMBL4752663 1 6.85
CHEMBL4784844 1 6.66
CHEMBL4759268 1 6.44
CHEMBL191482 AR-42 2.0 1 6.37
CHEMBL4776825 1 6.21
CHEMBL4751174 1 6.05
CHEMBL4792528 1 6.02
CHEMBL4760192 1 5.96
CHEMBL4748151 1 5.96
CHEMBL4747652 1 5.89
CHEMBL4758506 1 5.85
CHEMBL4741326 1 5.77
CHEMBL4740957 1 5.72
CHEMBL98 VORINOSTAT 4.0 1 5.02
CHEMBL4763919 1 4.96
CHEMBL356769 TUBACIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4761013 IC50 = 12.0 nM 7.92
CHEMBL4748500 IC50 = 12.0 nM 7.92
CHEMBL4799406 IC50 = 24.0 nM 7.62
CHEMBL4751615 IC50 = 27.0 nM 7.57
CHEMBL4776127 IC50 = 31.0 nM 7.51
CHEMBL4762512 IC50 = 49.0 nM 7.31
CHEMBL4776962 IC50 = 76.0 nM 7.12
CHEMBL4752663 IC50 = 140.0 nM 6.85
CHEMBL4784844 IC50 = 220.0 nM 6.66
CHEMBL4759268 IC50 = 360.0 nM 6.44
CHEMBL191482 AR-42 IC50 = 430.0 nM 6.37
CHEMBL4776825 IC50 = 620.0 nM 6.21
CHEMBL4751174 IC50 = 890.0 nM 6.05
CHEMBL4792528 IC50 = 950.0 nM 6.02
CHEMBL4760192 IC50 = 1100.0 nM 5.96
CHEMBL4748151 IC50 = 1100.0 nM 5.96
CHEMBL4747652 IC50 = 1300.0 nM 5.89
CHEMBL4758506 IC50 = 1400.0 nM 5.85
CHEMBL4741326 IC50 = 1700.0 nM 5.77
CHEMBL4740957 IC50 = 1900.0 nM 5.72
CHEMBL98 VORINOSTAT IC50 = 9600.0 nM 5.02
CHEMBL4763919 IC50 = 11000.0 nM 4.96
CHEMBL356769 TUBACIN IC50 - -