Assay Detail
Binding
CHEMBL5152973
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Inhibition of human mitochondrial HSP60 expressed in Escherichia coli Rosetta 2 (DE3) cells/human mitochondrial HSP10 expressed in Escherichia coli Rosetta 2 (DE3) pLysS cells assessed as inhibition of GroEL/ES-mediated dMDH refolding by reporter analysis
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Subcellular | Mitochondria |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 4.99 | 5.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5178695 | — | — | 1 | 5.66 |
| CHEMBL5209316 | — | — | 1 | 5.64 |
| CHEMBL3115912 | — | — | 1 | 5.60 |
| CHEMBL5170692 | — | — | 1 | 5.33 |
| CHEMBL5202538 | — | — | 1 | 5.23 |
| CHEMBL3115914 | — | — | 1 | 5.21 |
| CHEMBL5177265 | — | — | 1 | 5.11 |
| CHEMBL7976 | CHALCONE | — | 1 | 5.07 |
| CHEMBL1927391 | — | — | 1 | 5.01 |
| CHEMBL3115924 | — | — | 1 | 4.92 |
| CHEMBL187926 | — | — | 1 | 4.85 |
| CHEMBL34398 | 4'-METHOXYCHALCONE | — | 1 | 4.80 |
| CHEMBL5185585 | — | — | 1 | 4.70 |
| CHEMBL7747 | 4-HYDROXYCHALCONE | — | 1 | 4.68 |
| CHEMBL276473 | 4'-HYDROXYCHALCONE | — | 1 | 4.68 |
| CHEMBL105496 | 4-METHOXY CHALCONE | — | 1 | 4.66 |
| CHEMBL463017 | — | — | 1 | 4.37 |
| CHEMBL1578953 | — | — | 1 | 4.36 |
| CHEMBL207313 | — | — | 1 | - |
| CHEMBL5185073 | — | — | 1 | - |
| CHEMBL490512 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5178695 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5209316 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3115912 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5170692 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL5202538 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL3115914 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL5177265 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL7976 | CHALCONE | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL1927391 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL3115924 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL187926 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL34398 | 4'-METHOXYCHALCONE | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL5185585 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL7747 | 4-HYDROXYCHALCONE | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL276473 | 4'-HYDROXYCHALCONE | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL105496 | 4-METHOXY CHALCONE | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL463017 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL1578953 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL207313 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5185073 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL490512 | — | IC50 | > | 100000.0 | nM | - |