Assay Detail
Binding
CHEMBL2156338
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant GCP2 using N-acetyl-L-aspartyl-[3H]-L-glutamate as substrate by microplate assay
22
Total Activities
22
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, synthesis, and pharmacological evaluation of glutamate carboxypeptidase II (GCPII) inhibitors based on thioalkylbenzoic acid scaffolds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.99 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2152556 | — | — | 1 | 8.70 |
| CHEMBL2152561 | — | — | 1 | 8.70 |
| CHEMBL2152562 | — | — | 1 | 8.15 |
| CHEMBL382398 | — | — | 1 | 7.82 |
| CHEMBL2152557 | — | — | 1 | 7.80 |
| CHEMBL1287900 | — | — | 1 | 7.66 |
| CHEMBL2152437 | — | — | 1 | 7.42 |
| CHEMBL2152555 | — | — | 1 | 7.39 |
| CHEMBL2152438 | — | — | 1 | 7.28 |
| CHEMBL2152565 | — | — | 1 | 7.16 |
| CHEMBL303352 | — | — | 1 | 7.05 |
| CHEMBL2152564 | — | — | 1 | 6.85 |
| CHEMBL2152566 | — | — | 1 | 6.70 |
| CHEMBL2152563 | — | — | 1 | 6.70 |
| CHEMBL2152560 | — | — | 1 | 6.64 |
| CHEMBL2152436 | — | — | 1 | 6.47 |
| CHEMBL2152439 | — | — | 1 | 6.38 |
| CHEMBL2152558 | — | — | 1 | 6.03 |
| CHEMBL2152434 | — | — | 1 | 5.89 |
| CHEMBL2152559 | — | — | 1 | 5.85 |
| CHEMBL294565 | — | — | 1 | 5.85 |
| CHEMBL2152435 | — | — | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2152556 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2152561 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2152562 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL382398 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2152557 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1287900 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2152437 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2152555 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2152438 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL2152565 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL303352 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2152564 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2152566 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2152563 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2152560 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2152436 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL2152439 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2152558 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL2152434 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2152559 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL294565 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2152435 | — | IC50 | = | 5700.0 | nM | 5.24 |