Assay Detail
Binding
CHEMBL2189067
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human kidney glutaminase (124 to 669) using L-[3H]-glutamine as substrate after 45 mins by GLS assay
27
Total Activities
27
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 pharmacological evaluation of bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide 3 (BPTES) analogs as glutaminase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 5.06 | 5.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2177749 | — | — | 1 | 5.85 |
| CHEMBL2178396 | — | — | 1 | 5.72 |
| CHEMBL2177740 | — | — | 1 | 5.58 |
| CHEMBL2178393 | — | — | 1 | 5.57 |
| CHEMBL2177757 | — | — | 1 | 5.48 |
| CHEMBL2177748 | — | — | 1 | 5.42 |
| CHEMBL2177739 | — | — | 1 | 5.35 |
| CHEMBL2177744 | — | — | 1 | 5.34 |
| CHEMBL2177753 | — | — | 1 | 5.28 |
| CHEMBL2178398 | — | — | 1 | 5.14 |
| CHEMBL2177746 | — | — | 1 | 5.09 |
| CHEMBL2177747 | — | — | 1 | 5.00 |
| CHEMBL2177752 | — | — | 1 | 4.96 |
| CHEMBL2177741 | — | — | 1 | 4.92 |
| CHEMBL2178395 | — | — | 1 | 4.82 |
| CHEMBL2177738 | — | — | 1 | 4.66 |
| CHEMBL2177751 | — | — | 1 | 4.58 |
| CHEMBL2177755 | — | — | 1 | 4.32 |
| CHEMBL2178394 | — | — | 1 | 4.21 |
| CHEMBL2177758 | — | — | 1 | 4.00 |
| CHEMBL2177742 | — | — | 1 | - |
| CHEMBL2177743 | — | — | 1 | - |
| CHEMBL2178397 | — | — | 1 | - |
| CHEMBL2177745 | — | — | 1 | - |
| CHEMBL2177750 | — | — | 1 | - |
| CHEMBL2177754 | — | — | 1 | - |
| CHEMBL2177756 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2177749 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2178396 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2177740 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL2178393 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL2177757 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL2177748 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL2177739 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL2177744 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL2177753 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL2178398 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL2177746 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL2177747 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2177752 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2177741 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2178395 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2177738 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2177751 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL2177755 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL2178394 | — | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL2177758 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL2177742 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2177743 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2178397 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2177745 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2177750 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2177754 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2177756 | — | IC50 | > | 100000.0 | nM | - |