Assay Detail
Binding
CHEMBL1246389
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Inhibition of human recombinant FAP expressed in Hi5 insect cells
33
Total Activities
33
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
Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.81 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1243373 | — | — | 1 | 7.72 |
| CHEMBL1243126 | — | — | 1 | 7.70 |
| CHEMBL1243153 | — | — | 1 | 7.66 |
| CHEMBL1243184 | — | — | 1 | 7.51 |
| CHEMBL1243372 | — | — | 1 | 7.27 |
| CHEMBL1242940 | — | — | 1 | 7.23 |
| CHEMBL1243127 | — | — | 1 | 7.20 |
| CHEMBL1242939 | — | — | 1 | 7.18 |
| CHEMBL1243091 | — | — | 1 | 7.14 |
| CHEMBL1243402 | — | — | 1 | 7.10 |
| CHEMBL1242967 | — | — | 1 | 7.06 |
| CHEMBL1242966 | — | — | 1 | 6.96 |
| CHEMBL387050 | — | — | 1 | 6.92 |
| CHEMBL1243061 | — | — | 1 | 6.70 |
| CHEMBL1243403 | — | — | 1 | 6.68 |
| CHEMBL1242993 | — | — | 1 | 6.60 |
| CHEMBL1243028 | — | — | 1 | 6.29 |
| CHEMBL1243374 | — | — | 1 | 6.21 |
| CHEMBL1242994 | — | — | 1 | 6.19 |
| CHEMBL1243092 | — | — | 1 | 6.14 |
| CHEMBL1243060 | — | — | 1 | 5.50 |
| CHEMBL1243027 | — | — | 1 | 4.82 |
| CHEMBL1243248 | — | — | 1 | - |
| CHEMBL1243183 | — | — | 1 | - |
| CHEMBL1243215 | — | — | 1 | - |
| CHEMBL1243216 | — | — | 1 | - |
| CHEMBL1422 | SITAGLIPTIN | 4.0 | 1 | - |
| CHEMBL1243154 | — | — | 1 | - |
| CHEMBL1243093 | — | — | 1 | - |
| CHEMBL362018 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1243373 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1243126 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1243153 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1243184 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1243372 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1242940 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1243127 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL1242939 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1243091 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL1243402 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL1242967 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL1242966 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL387050 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1243061 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1243403 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1242993 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1243028 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL1243374 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL1242994 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL1243092 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL1243060 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1243027 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL1243248 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL1243183 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1243215 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1243216 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1422 | SITAGLIPTIN | IC50 | > | 100000.0 | nM | - |
| CHEMBL1243154 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL1243093 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL362018 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL397070 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL98762 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL142703 | VILDAGLIPTIN | IC50 | > | 100000.0 | nM | - |