Assay Detail
Binding
CHEMBL4725975
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Agonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method
40
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of BMS-986235/LAR-1219: A Potent Formyl Peptide Receptor 2 (FPR2) Selective Agonist for the Prevention of Heart Failure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 40 | 6.53 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4744094 | — | — | 2 | 8.41 |
| CHEMBL4743917 | — | — | 1 | 8.05 |
| CHEMBL4744835 | — | — | 1 | 7.77 |
| CHEMBL4793557 | — | — | 1 | 7.54 |
| CHEMBL4776349 | — | — | 1 | 7.40 |
| CHEMBL4755590 | — | — | 1 | 7.14 |
| CHEMBL4751168 | — | — | 1 | 7.14 |
| CHEMBL4743084 | — | — | 1 | 7.12 |
| CHEMBL4740375 | — | — | 2 | 7.09 |
| CHEMBL4745044 | — | — | 1 | 7.07 |
| CHEMBL4761554 | — | — | 1 | 7.02 |
| CHEMBL4793814 | — | — | 1 | 7.00 |
| CHEMBL4758920 | — | — | 1 | 6.92 |
| CHEMBL4753713 | — | — | 1 | 6.72 |
| CHEMBL4781596 | — | — | 1 | 6.55 |
| CHEMBL4778725 | — | — | 1 | 6.54 |
| CHEMBL4742149 | — | — | 1 | 6.46 |
| CHEMBL4743133 | — | — | 1 | 6.39 |
| CHEMBL4762030 | — | — | 1 | 6.09 |
| CHEMBL4793603 | — | — | 1 | 6.04 |
| CHEMBL4790836 | — | — | 1 | 6.00 |
| CHEMBL4789579 | — | — | 1 | 6.00 |
| CHEMBL4760897 | — | — | 1 | 5.92 |
| CHEMBL4783963 | — | — | 1 | 5.82 |
| CHEMBL4763824 | — | — | 1 | 5.77 |
| CHEMBL4781488 | — | — | 1 | 5.72 |
| CHEMBL4784510 | BMS-986235 | 1.0 | 1 | 5.55 |
| CHEMBL4749577 | — | — | 1 | 5.52 |
| CHEMBL4763673 | — | — | 1 | 5.50 |
| CHEMBL4792002 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4744094 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4743917 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4744835 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4793557 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4744094 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4776349 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4755590 | — | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4751168 | — | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4743084 | — | EC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4740375 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4745044 | — | EC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4761554 | — | EC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4793814 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4758920 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4753713 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4781596 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4778725 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4742149 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4743133 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4762030 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4793603 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4740375 | — | EC50 | = | 950.0 | nM | 6.02 |
| CHEMBL4790836 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4789579 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4760897 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4783963 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4763824 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4781488 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4784510 | BMS-986235 | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4749577 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4763673 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4792002 | — | EC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL4758129 | — | EC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL4797598 | — | EC50 | - | — | - | |
| CHEMBL4756320 | — | EC50 | - | — | - | |
| CHEMBL4784400 | — | EC50 | < | 10.0 | nM | - |
| CHEMBL4756217 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4790245 | — | EC50 | - | — | - | |
| CHEMBL4778312 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4796468 | — | EC50 | > | 10000.0 | nM | - |