Assay Detail
Binding
CHEMBL1771950
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Inhibition of recombinant cytosolic PLA2alpha assessed as inhibition of cleavage of soluble fluorogenic substrate
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design of novel and potent cPLA2α inhibitors containing an α-methyl-2-ketothiazole as a metabolically stable serine trap.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.19 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1770456 | — | — | 1 | 7.40 |
| CHEMBL29838 | — | — | 1 | 7.10 |
| CHEMBL1770258 | — | — | 1 | 7.10 |
| CHEMBL1770450 | — | — | 1 | 7.10 |
| CHEMBL1770257 | — | — | 1 | 6.85 |
| CHEMBL1770465 | — | — | 1 | 6.70 |
| CHEMBL1770457 | — | — | 1 | 6.70 |
| CHEMBL1770453 | — | — | 1 | 6.62 |
| CHEMBL1770452 | — | — | 1 | 6.55 |
| CHEMBL1770455 | — | — | 1 | 6.52 |
| CHEMBL1770447 | — | — | 1 | 6.52 |
| CHEMBL1770448 | — | — | 1 | 6.30 |
| CHEMBL1770462 | — | — | 1 | 6.16 |
| CHEMBL1770250 | — | — | 1 | 6.00 |
| CHEMBL1770254 | — | — | 1 | 6.00 |
| CHEMBL1770463 | — | — | 1 | 5.82 |
| CHEMBL1770451 | — | — | 1 | 5.70 |
| CHEMBL1770255 | — | — | 1 | 5.57 |
| CHEMBL1770454 | — | — | 1 | 5.52 |
| CHEMBL1770461 | — | — | 1 | 5.44 |
| CHEMBL1770449 | — | — | 1 | 5.37 |
| CHEMBL1770460 | — | — | 1 | 5.36 |
| CHEMBL1770458 | — | — | 1 | 5.17 |
| CHEMBL1770459 | — | — | 1 | 5.10 |
| CHEMBL1770446 | — | — | 1 | - |
| CHEMBL1770256 | — | — | 1 | - |
| CHEMBL1770253 | — | — | 1 | - |
| CHEMBL1770252 | — | — | 1 | - |
| CHEMBL1770464 | — | — | 1 | - |
| CHEMBL1770251 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1770456 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL29838 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1770258 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1770450 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1770257 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1770465 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1770457 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1770453 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1770452 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1770455 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1770447 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1770448 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1770462 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1770250 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1770254 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1770463 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1770451 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1770255 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1770454 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1770461 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL1770449 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL1770460 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL1770458 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL1770459 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL1770446 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1770256 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1770253 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1770252 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1770464 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1770251 | — | IC50 | > | 10000.0 | nM | - |