Assay Detail
Binding
CHEMBL3239282
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Inhibition of recombinant human PREP purified from Escherichia coli using Z-Gly-Pro-p-nitroanilide as substrate by spectrophotometry
60
Total Activities
60
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
Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 60 | 5.30 | 7.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3233847 | — | — | 1 | 7.95 |
| CHEMBL3233540 | — | — | 1 | 7.36 |
| CHEMBL3233840 | — | — | 1 | 6.54 |
| CHEMBL3233834 | — | — | 1 | 6.30 |
| CHEMBL3233848 | — | — | 1 | 6.11 |
| CHEMBL2385281 | — | — | 1 | 6.07 |
| CHEMBL67279 | TALABOSTAT | 3.0 | 1 | 6.01 |
| CHEMBL2333026 | — | — | 1 | 6.00 |
| CHEMBL3233839 | — | — | 1 | 5.89 |
| CHEMBL3233546 | — | — | 1 | 5.70 |
| CHEMBL3233561 | — | — | 1 | 5.70 |
| CHEMBL3233837 | — | — | 1 | 5.69 |
| CHEMBL3233543 | — | — | 1 | 5.58 |
| CHEMBL3233572 | — | — | 1 | 5.57 |
| CHEMBL3233833 | — | — | 1 | 5.47 |
| CHEMBL3233571 | — | — | 1 | 5.25 |
| CHEMBL3233539 | — | — | 1 | 5.24 |
| CHEMBL3233562 | — | — | 1 | 5.23 |
| CHEMBL3233545 | — | — | 1 | 5.20 |
| CHEMBL3233564 | — | — | 1 | 5.18 |
| CHEMBL3233555 | — | — | 1 | 5.17 |
| CHEMBL3233568 | — | — | 1 | 5.14 |
| CHEMBL3233556 | — | — | 1 | 5.14 |
| CHEMBL3233843 | — | — | 1 | 5.08 |
| CHEMBL3233838 | — | — | 1 | 5.06 |
| CHEMBL3233544 | — | — | 1 | 5.05 |
| CHEMBL3233553 | — | — | 1 | 5.05 |
| CHEMBL3233835 | — | — | 1 | 5.04 |
| CHEMBL3233844 | — | — | 1 | 5.03 |
| CHEMBL3233554 | — | — | 1 | 4.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3233847 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL3233540 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3233840 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3233834 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3233848 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL2385281 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL67279 | TALABOSTAT | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL2333026 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL3233839 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL3233546 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3233561 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3233837 | — | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL3233543 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3233572 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3233833 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3233571 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL3233539 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL3233562 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL3233545 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL3233564 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL3233555 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL3233568 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL3233556 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL3233843 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL3233838 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL3233544 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL3233553 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL3233835 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL3233844 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL3233554 | — | IC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL3233559 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL3233569 | — | IC50 | = | 13700.0 | nM | 4.86 |
| CHEMBL3233558 | — | IC50 | = | 14200.0 | nM | 4.85 |
| CHEMBL3233845 | — | IC50 | = | 16800.0 | nM | 4.78 |
| CHEMBL3233836 | — | IC50 | = | 19400.0 | nM | 4.71 |
| CHEMBL3233567 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL3233575 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL3233542 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL3233560 | — | IC50 | = | 29100.0 | nM | 4.54 |
| CHEMBL3233557 | — | IC50 | = | 33700.0 | nM | 4.47 |
| CHEMBL3233563 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL3233541 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL3233570 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL3233549 | — | IC50 | = | 67000.0 | nM | 4.17 |
| CHEMBL3233842 | — | IC50 | > | 1800.0 | nM | - |
| CHEMBL2385300 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL1243153 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL237500 | LINAGLIPTIN | IC50 | > | 100000.0 | nM | - |
| CHEMBL3233841 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3233574 | — | IC50 | > | 100000.0 | nM | - |