Assay Detail
Binding
CHEMBL4624682
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-87MG ATCC |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A cell-based fluorescent assay for FAP inhibitor discovery.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.68 | 7.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3233842 | — | — | 1 | 7.26 |
| CHEMBL67279 | TALABOSTAT | 3.0 | 1 | 6.65 |
| CHEMBL4640030 | — | — | 1 | 6.18 |
| CHEMBL4647532 | — | — | 1 | 5.82 |
| CHEMBL142703 | VILDAGLIPTIN | 4.0 | 1 | 4.10 |
| CHEMBL1422 | SITAGLIPTIN | 4.0 | 1 | 4.07 |
| CHEMBL376359 | ALOGLIPTIN | 4.0 | 1 | - |
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3233842 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL67279 | TALABOSTAT | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL4640030 | — | IC50 | = | 663.0 | nM | 6.18 |
| CHEMBL4647532 | — | IC50 | = | 1504.0 | nM | 5.82 |
| CHEMBL142703 | VILDAGLIPTIN | IC50 | = | 79760.0 | nM | 4.10 |
| CHEMBL1422 | SITAGLIPTIN | IC50 | = | 85340.0 | nM | 4.07 |
| CHEMBL376359 | ALOGLIPTIN | IC50 | = | 1470000.0 | nM | - |
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | IC50 | = | 1720000.0 | nM | - |