Assay Detail
Binding
CHEMBL2172850
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Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and biological evaluation of a novel class of dual microsomal prostaglandin E2 synthase-1/5-lipoxygenase inhibitors based on 2-[(4,6-diphenethoxypyrimidin-2-yl)thio]hexanoic acid.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 5.58 | 6.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1173376 | — | — | 1 | 6.05 |
| CHEMBL1172016 | — | — | 1 | 6.05 |
| CHEMBL2170363 | — | — | 1 | 5.96 |
| CHEMBL461883 | — | — | 1 | 5.92 |
| CHEMBL1171851 | — | — | 1 | 5.92 |
| CHEMBL1819397 | — | — | 1 | 5.82 |
| CHEMBL1170264 | — | — | 1 | 5.72 |
| CHEMBL1172003 | — | — | 1 | 5.70 |
| CHEMBL1172019 | — | — | 1 | 5.66 |
| CHEMBL1819396 | — | — | 1 | 5.62 |
| CHEMBL1171834 | — | — | 1 | 5.62 |
| CHEMBL1819390 | — | — | 1 | 5.62 |
| CHEMBL29097 | — | — | 1 | 5.62 |
| CHEMBL1819394 | — | — | 1 | 5.57 |
| CHEMBL1819391 | — | — | 1 | 5.55 |
| CHEMBL1817687 | — | — | 1 | 5.47 |
| CHEMBL1819398 | — | — | 1 | 5.47 |
| CHEMBL1819478 | — | — | 1 | 5.46 |
| CHEMBL1171652 | — | — | 1 | 5.43 |
| CHEMBL1172222 | — | — | 1 | 5.42 |
| CHEMBL1819393 | — | — | 1 | 5.41 |
| CHEMBL1819392 | — | — | 1 | 5.34 |
| CHEMBL1171831 | — | — | 1 | 5.23 |
| CHEMBL1171832 | — | — | 1 | 5.19 |
| CHEMBL1173499 | — | — | 1 | 5.14 |
| CHEMBL1172001 | — | — | 1 | 5.02 |
| CHEMBL1172000 | — | — | 1 | - |
| CHEMBL518507 | — | — | 1 | - |
| CHEMBL1170852 | — | — | 1 | - |
| CHEMBL1173121 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1173376 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL1172016 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2170363 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL461883 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1171851 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1819397 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1170264 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1172003 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1172019 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1171834 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL29097 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1819390 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1819396 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1819394 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1819391 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL1817687 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1819398 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1819478 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL1171652 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL1172222 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL1819393 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL1819392 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL1171831 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL1171832 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL1173499 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL1172001 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL314360 | — | IC50 | - | — | - | |
| CHEMBL1819480 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1819479 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1819395 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1172002 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1171833 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1173121 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1170852 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL518507 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1172000 | — | IC50 | > | 10000.0 | nM | - |