Assay Detail
Binding
CHEMBL2212266
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Inhibition of human recombinant GLO1 expressed in Escherichia coli BL21 assessed as decrease in reduced glutathione level after 1 hr by Ellman's method
18
Total Activities
18
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 |
Publication
Design and evaluation of azaindole-substituted N-hydroxypyridones as glyoxalase I inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.34 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2203964 | — | — | 1 | 7.96 |
| CHEMBL2203978 | — | — | 1 | 7.85 |
| CHEMBL2203976 | — | — | 1 | 7.40 |
| CHEMBL2203975 | — | — | 1 | 6.60 |
| CHEMBL2203963 | — | — | 1 | 6.58 |
| CHEMBL2203974 | — | — | 1 | 6.55 |
| CHEMBL2203966 | — | — | 1 | 6.52 |
| CHEMBL2203965 | — | — | 1 | 6.52 |
| CHEMBL2203977 | — | — | 1 | 6.32 |
| CHEMBL2203967 | — | — | 1 | 6.29 |
| CHEMBL218644 | — | — | 1 | 5.92 |
| CHEMBL1624076 | — | — | 1 | 5.92 |
| CHEMBL2203968 | — | — | 1 | 5.82 |
| CHEMBL2203970 | — | — | 1 | 5.09 |
| CHEMBL2203971 | — | — | 1 | 5.08 |
| CHEMBL2203969 | — | — | 1 | 5.08 |
| CHEMBL2203973 | — | — | 1 | - |
| CHEMBL2203972 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2203964 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2203978 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2203976 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2203975 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2203963 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2203974 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2203966 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2203965 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2203977 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL2203967 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL218644 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1624076 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL2203968 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL2203970 | — | IC50 | = | 8130.0 | nM | 5.09 |
| CHEMBL2203971 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL2203969 | — | IC50 | = | 8280.0 | nM | 5.08 |
| CHEMBL2203973 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2203972 | — | IC50 | > | 10000.0 | nM | - |