Assay Detail
Binding
CHEMBL680917
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-acetyl-L-aspartyl-[3H]L-glutamate binding to glutamate carboxypeptidase II (GCP II)
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.12 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL47009 | — | — | 1 | 9.52 |
| CHEMBL303352 | — | — | 1 | 7.05 |
| CHEMBL292562 | — | — | 1 | 6.24 |
| CHEMBL60317 | — | — | 1 | 5.96 |
| CHEMBL58232 | — | — | 1 | 5.92 |
| CHEMBL294565 | — | — | 1 | 5.85 |
| CHEMBL302413 | — | — | 1 | 5.85 |
| CHEMBL304885 | — | — | 1 | 5.58 |
| CHEMBL61067 | — | — | 1 | 5.58 |
| CHEMBL61832 | — | — | 1 | 5.51 |
| CHEMBL60941 | — | — | 1 | 5.22 |
| CHEMBL61882 | — | — | 1 | 5.19 |
| CHEMBL417214 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL47009 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL303352 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL292562 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL60317 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL58232 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL294565 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL302413 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL304885 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL61067 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL61832 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL60941 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL61882 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL417214 | — | IC50 | > | 10000.0 | nM | - |