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Assay Detail

CHEMBL5046020

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

Functional
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 48 hrs by cell-titer glo assay
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-116 (CHEMBL394)
Type CELL-LINE
Organism Homo sapiens

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
EC50 4 5.22 5.37
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5073757 1 5.37
CHEMBL5084955 1 5.28
CHEMBL5077287 1 5.14
CHEMBL235191 TACEDINALINE 3.0 1 5.08
CHEMBL5077743 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5073757 EC50 = 4300.0 nM 5.37
CHEMBL5084955 EC50 = 5200.0 nM 5.28
CHEMBL5077287 EC50 = 7300.0 nM 5.14
CHEMBL235191 TACEDINALINE EC50 = 8400.0 nM 5.08
CHEMBL5077743 Activity - -