Assay Detail
Binding
CHEMBL4013171
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His-tagged KGA (L123 to L669 residues) expressed in Escherichia coli BL21(DE3)pLysS using glutamine substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by glutamate dehydrogenase coupled enzyme assay
17
Total Activities
17
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 |
Target
Glutaminase kidney isoform, mitochondrial (CHEMBL2146302) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, Synthesis, and Evaluation of Thiazolidine-2,4-dione Derivatives as a Novel Class of Glutaminase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.90 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4082885 | — | — | 1 | 7.46 |
| CHEMBL4072390 | — | — | 1 | 7.41 |
| CHEMBL4090687 | — | — | 1 | 7.35 |
| CHEMBL4061000 | — | — | 1 | 7.32 |
| CHEMBL4080388 | — | — | 1 | 7.30 |
| CHEMBL4099331 | — | — | 1 | 7.27 |
| CHEMBL4087349 | — | — | 1 | 7.25 |
| CHEMBL4074218 | — | — | 1 | 7.24 |
| CHEMBL4065595 | — | — | 1 | 7.23 |
| CHEMBL4065936 | — | — | 1 | 7.18 |
| CHEMBL2177757 | — | — | 1 | 7.09 |
| CHEMBL4098413 | — | — | 1 | 6.99 |
| CHEMBL4069677 | — | — | 1 | 6.61 |
| CHEMBL4087025 | — | — | 1 | 6.61 |
| CHEMBL4100814 | — | — | 1 | 6.12 |
| CHEMBL4070276 | — | — | 1 | 5.51 |
| CHEMBL4074051 | — | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4082885 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4072390 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4090687 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4061000 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4080388 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4099331 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4087349 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4074218 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4065595 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4065936 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2177757 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4098413 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4069677 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL4087025 | — | IC50 | = | 247.0 | nM | 6.61 |
| CHEMBL4100814 | — | IC50 | = | 754.0 | nM | 6.12 |
| CHEMBL4070276 | — | IC50 | = | 3097.0 | nM | 5.51 |
| CHEMBL4074051 | — | IC50 | = | 4896.0 | nM | 5.31 |