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Assay Detail

CHEMBL5152978

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

Functional
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 48 hrs by AlamarBlue-based assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-29
Confidence 1 — Organism
Curated By Autocuration

Target

HT-29 (CHEMBL384)
Type CELL-LINE
Organism Homo sapiens

Publication

Bis-aryl-α,β-unsaturated ketone (ABK) chaperonin inhibitors exhibit selective cytotoxicity to colorectal cancer cells that correlates with levels of aberrant HSP60 in the cytosol.
Chitre S, Ray AM, Stevens M, Doud EH, Liechty H, Washburn A, Tepper K, Sivinski J, O'Hagan HM, Georgiadis MM, Chapman E, Johnson SM.
Bioorg Med Chem (2022) 75 : 117072 -117072
PubMed 36356534 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 4.75 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5177265 1 5.70
CHEMBL5178695 1 5.60
CHEMBL3115912 1 5.46
CHEMBL5209316 1 5.41
CHEMBL3115914 1 5.09
CHEMBL187926 1 4.89
CHEMBL7976 CHALCONE 1 4.85
CHEMBL34398 4'-METHOXYCHALCONE 1 4.64
CHEMBL1927391 1 4.55
CHEMBL5170692 1 4.55
CHEMBL276473 4'-HYDROXYCHALCONE 1 4.52
CHEMBL105496 4-METHOXY CHALCONE 1 4.50
CHEMBL463017 1 4.46
CHEMBL5202538 1 4.44
CHEMBL7747 4-HYDROXYCHALCONE 1 4.41
CHEMBL3115924 1 4.30
CHEMBL5185585 1 4.12
CHEMBL1578953 1 4.06
CHEMBL207313 1 -
CHEMBL5185073 1 -
CHEMBL490512 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5177265 EC50 = 2000.0 nM 5.70
CHEMBL5178695 EC50 = 2500.0 nM 5.60
CHEMBL3115912 EC50 = 3500.0 nM 5.46
CHEMBL5209316 EC50 = 3900.0 nM 5.41
CHEMBL3115914 EC50 = 8200.0 nM 5.09
CHEMBL187926 EC50 = 13000.0 nM 4.89
CHEMBL7976 CHALCONE EC50 = 14000.0 nM 4.85
CHEMBL34398 4'-METHOXYCHALCONE EC50 = 23000.0 nM 4.64
CHEMBL1927391 EC50 = 28000.0 nM 4.55
CHEMBL5170692 EC50 = 28000.0 nM 4.55
CHEMBL276473 4'-HYDROXYCHALCONE EC50 = 30000.0 nM 4.52
CHEMBL105496 4-METHOXY CHALCONE EC50 = 32000.0 nM 4.50
CHEMBL463017 EC50 = 35000.0 nM 4.46
CHEMBL5202538 EC50 = 36000.0 nM 4.44
CHEMBL7747 4-HYDROXYCHALCONE EC50 = 39000.0 nM 4.41
CHEMBL3115924 EC50 = 50000.0 nM 4.30
CHEMBL5185585 EC50 = 76000.0 nM 4.12
CHEMBL1578953 EC50 = 88000.0 nM 4.06
CHEMBL207313 EC50 > 100000.0 nM -
CHEMBL5185073 EC50 > 100000.0 nM -
CHEMBL490512 EC50 > 100000.0 nM -