Assay Detail
Binding
CHEMBL2389863
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition
37
Total Activities
35
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.41 | 8.21 |
| Ki | 2 | 8.46 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2385281 | — | — | 2 | 8.52 |
| CHEMBL2385300 | — | — | 2 | 8.39 |
| CHEMBL2385273 | — | — | 1 | 8.21 |
| CHEMBL2385272 | — | — | 1 | 8.15 |
| CHEMBL2385271 | — | — | 1 | 8.04 |
| CHEMBL2385299 | — | — | 1 | 8.00 |
| CHEMBL2385270 | — | — | 1 | 7.99 |
| CHEMBL2385302 | — | — | 1 | 7.92 |
| CHEMBL2385301 | — | — | 1 | 7.85 |
| CHEMBL67279 | TALABOSTAT | 3.0 | 1 | 7.16 |
| CHEMBL2385278 | — | — | 1 | 6.97 |
| CHEMBL2385279 | — | — | 1 | 6.80 |
| CHEMBL2385298 | — | — | 1 | 6.80 |
| CHEMBL2385274 | — | — | 1 | 6.72 |
| CHEMBL237500 | LINAGLIPTIN | 4.0 | 1 | 6.43 |
| CHEMBL2385275 | — | — | 1 | 6.43 |
| CHEMBL2385277 | — | — | 1 | 6.38 |
| CHEMBL2385293 | — | — | 1 | 6.17 |
| CHEMBL2385297 | — | — | 1 | 6.11 |
| CHEMBL2385295 | — | — | 1 | 6.00 |
| CHEMBL2385291 | — | — | 1 | 5.68 |
| CHEMBL2385280 | — | — | 1 | 5.66 |
| CHEMBL2385282 | — | — | 1 | 5.44 |
| CHEMBL2385276 | — | — | 1 | 5.32 |
| CHEMBL2385294 | — | — | 1 | 5.23 |
| CHEMBL2385286 | — | — | 1 | 5.07 |
| CHEMBL2385285 | — | — | 1 | 5.03 |
| CHEMBL2385290 | — | — | 1 | 4.93 |
| CHEMBL2385284 | — | — | 1 | 4.85 |
| CHEMBL2385283 | — | — | 1 | 4.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2385281 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2385300 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL2385273 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL2385272 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL2385271 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL2385299 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL2385281 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL2385270 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL2385300 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2385302 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2385301 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL67279 | TALABOSTAT | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2385278 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL2385279 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL2385298 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2385274 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2385275 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL237500 | LINAGLIPTIN | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL2385277 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2385293 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL2385297 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL2385295 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2385291 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2385280 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL2385282 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL2385276 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL2385294 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL2385286 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL2385285 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL2385290 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL2385284 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL2385283 | — | IC50 | = | 15400.0 | nM | 4.81 |
| CHEMBL2385289 | — | IC50 | = | 17600.0 | nM | 4.75 |
| CHEMBL2385292 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL2385288 | — | IC50 | > | 12500.0 | nM | - |
| CHEMBL2385287 | — | IC50 | > | 12500.0 | nM | - |
| CHEMBL2385296 | — | IC50 | > | 10000.0 | nM | - |