Assay Detail
Binding
CHEMBL4714146
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FAP (unknown origin) using AMC substrate by fluorometric assay
50
Total Activities
50
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 BR102910 as a selective fibroblast activation protein (FAP) inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 50 | 7.43 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4762591 | — | — | 1 | 9.00 |
| CHEMBL4786982 | — | — | 1 | 8.70 |
| CHEMBL3233842 | — | — | 1 | 8.48 |
| CHEMBL4750058 | — | — | 1 | 8.40 |
| CHEMBL4758299 | — | — | 1 | 8.30 |
| CHEMBL4780357 | — | — | 1 | 8.30 |
| CHEMBL4747575 | — | — | 1 | 8.15 |
| CHEMBL4789965 | — | — | 1 | 8.05 |
| CHEMBL4776967 | — | — | 1 | 7.96 |
| CHEMBL4753316 | — | — | 1 | 7.92 |
| CHEMBL4799823 | — | — | 1 | 7.85 |
| CHEMBL4746868 | — | — | 1 | 7.80 |
| CHEMBL4791505 | — | — | 1 | 7.72 |
| CHEMBL4759201 | — | — | 1 | 7.70 |
| CHEMBL4797479 | — | — | 1 | 7.70 |
| CHEMBL4781018 | — | — | 1 | 7.68 |
| CHEMBL4789754 | — | — | 1 | 7.68 |
| CHEMBL4744633 | — | — | 1 | 7.66 |
| CHEMBL4742308 | — | — | 1 | 7.64 |
| CHEMBL4748680 | — | — | 1 | 7.62 |
| CHEMBL2333026 | — | — | 1 | 7.60 |
| CHEMBL4762306 | — | — | 1 | 7.60 |
| CHEMBL4748328 | — | — | 1 | 7.58 |
| CHEMBL4761499 | — | — | 1 | 7.55 |
| CHEMBL4755802 | — | — | 1 | 7.46 |
| CHEMBL4754490 | — | — | 1 | 7.46 |
| CHEMBL4779526 | — | — | 1 | 7.43 |
| CHEMBL4748332 | — | — | 1 | 7.33 |
| CHEMBL4751873 | — | — | 1 | 7.30 |
| CHEMBL4743736 | — | — | 1 | 7.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4762591 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4786982 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3233842 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4750058 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4758299 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4780357 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4747575 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4789965 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4776967 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4753316 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4799823 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4746868 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4791505 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4759201 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4797479 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4781018 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4789754 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4744633 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4742308 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4748680 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2333026 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4762306 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4748328 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4761499 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4754490 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4755802 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4779526 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4748332 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4751873 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4743736 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4792518 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4785892 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4762435 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL67279 | TALABOSTAT | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4758377 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4740030 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4800379 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4797809 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4799547 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4751194 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4746891 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL4743815 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL4757491 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL4799063 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL4747683 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4748662 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4755107 | — | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL4795188 | — | IC50 | = | 446.0 | nM | 6.35 |
| CHEMBL4758296 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4782931 | — | IC50 | = | 795.0 | nM | 6.10 |