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Assay Detail

CHEMBL5045992

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

Binding
Inhibition of HDAC2-CoREST-LSD1 (unknown origin) using Boc- (Ac)Lys-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by fluorescent assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Optimization of Class I Histone Deacetylase PROTACs Reveals that HDAC1/2 Degradation is Critical to Induce Apoptosis and Cell Arrest in Cancer Cells.
Smalley JP, Baker IM, Pytel WA, Lin LY, Bowman KJ, Schwabe JWR, Cowley SM, Hodgkinson JT.
J Med Chem (2022) 65 : 5642 -5659
PubMed 35293758 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.75 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5077287 1 6.44
CHEMBL235191 TACEDINALINE 3.0 1 6.21
CHEMBL5084955 1 6.09
CHEMBL5077743 1 5.46
CHEMBL5080755 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5077287 IC50 = 360.0 nM 6.44
CHEMBL235191 TACEDINALINE IC50 = 620.0 nM 6.21
CHEMBL5084955 IC50 = 820.0 nM 6.09
CHEMBL5077743 IC50 = 3460.0 nM 5.46
CHEMBL5080755 IC50 = 28380.0 nM 4.55