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Assay Detail

CHEMBL5130698

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

Binding
Inhibition of recombinant HDAC5 (unknown origin) using Boc-Lys(TFA)-AMC as substrate by fluorescence based plate reader assay
10
Total Activities
10
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 5 (CHEMBL2563)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Developing HDAC4-Selective Protein Degraders To Investigate the Role of HDAC4 in Huntington's Disease Pathology.
Macabuag N, Esmieu W, Breccia P, Jarvis R, Blackaby W, Lazari O, Urbonas L, Eznarriaga M, Williams R, Strijbosch A, Van de Bospoort R, Matthews K, Clissold C, Ladduwahetty T, Vater H, Heaphy P, Stafford DG, Wang HJ, Mangette JE, McAllister G, Beaumont V, Vogt TF, Wilkinson HA, Doherty EM, Dominguez C.
J Med Chem (2022) 65 : 12445 -12459
PubMed 36098485 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.94 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3692671 1 8.30
CHEMBL4456445 1 7.22
CHEMBL5172806 1 6.85
CHEMBL5208515 1 6.82
CHEMBL5194487 1 6.64
CHEMBL5199458 1 6.60
CHEMBL5181194 1 6.58
CHEMBL5202426 1 6.51
CHEMBL5191938 1 -
CHEMBL5206361 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3692671 IC50 = 5.0 nM 8.30
CHEMBL4456445 IC50 = 60.0 nM 7.22
CHEMBL5172806 IC50 = 140.0 nM 6.85
CHEMBL5208515 IC50 = 150.0 nM 6.82
CHEMBL5194487 IC50 = 230.0 nM 6.64
CHEMBL5199458 IC50 = 250.0 nM 6.60
CHEMBL5181194 IC50 = 260.0 nM 6.58
CHEMBL5202426 IC50 = 310.0 nM 6.51
CHEMBL5191938 IC50 - -
CHEMBL5206361 IC50 - -