Assay Detail
Binding
CHEMBL2346129
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Inhibition of human FAP using Z-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence 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
Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.31 | 9.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2333025 | — | — | 1 | 9.33 |
| CHEMBL2333023 | — | — | 1 | 8.96 |
| CHEMBL1243373 | — | — | 1 | 8.64 |
| CHEMBL2333030 | — | — | 1 | 8.47 |
| CHEMBL2332619 | — | — | 1 | 8.19 |
| CHEMBL2332618 | — | — | 1 | 8.03 |
| CHEMBL67279 | TALABOSTAT | 3.0 | 1 | 7.92 |
| CHEMBL2333029 | — | — | 1 | 7.82 |
| CHEMBL2332617 | — | — | 1 | 7.80 |
| CHEMBL2333026 | — | — | 1 | 7.44 |
| CHEMBL67089 | — | — | 1 | 7.28 |
| CHEMBL2333027 | — | — | 1 | 7.27 |
| CHEMBL2332622 | — | — | 1 | 7.19 |
| CHEMBL387050 | — | — | 1 | 7.03 |
| CHEMBL2332620 | — | — | 1 | 6.92 |
| CHEMBL2332621 | — | — | 1 | 6.46 |
| CHEMBL2333028 | — | — | 1 | 6.30 |
| CHEMBL2332624 | — | — | 1 | 5.96 |
| CHEMBL2332623 | — | — | 1 | 5.89 |
| CHEMBL387462 | — | — | 1 | 5.54 |
| CHEMBL2333022 | — | — | 1 | 5.03 |
| CHEMBL2333024 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2333025 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL2333023 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1243373 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2333030 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL2332619 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL2332618 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL67279 | TALABOSTAT | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2333029 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2332617 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2333026 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL67089 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL2333027 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2332622 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL387050 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL2332620 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2332621 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL2333028 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2332624 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2332623 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL387462 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL2333022 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL2333024 | — | IC50 | > | 100000.0 | nM | - |