Assay Detail
Binding
CHEMBL3420871
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mPGES1 in IL-1beta stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 synthase activity after 15 mins using PGH2 substrate by RP-HPLC method
50
Total Activities
50
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Macrophage-expressed gene 1 protein (CHEMBL3414409) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel series of benzoquinones with high potency against 5-lipoxygenase in human polymorphonuclear leukocytes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 48 | 5.60 | 6.68 |
| Activity | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221137 | EMBELIN | — | 1 | 6.68 |
| CHEMBL221598 | — | — | 1 | 6.10 |
| CHEMBL462801 | Rapanone | — | 1 | 6.05 |
| CHEMBL3416163 | — | — | 1 | 6.00 |
| CHEMBL3416165 | — | — | 1 | 5.80 |
| CHEMBL3416348 | — | — | 1 | 5.75 |
| CHEMBL462998 | — | — | 1 | 5.68 |
| CHEMBL29097 | — | — | 1 | 5.66 |
| CHEMBL3416164 | — | — | 1 | 5.51 |
| CHEMBL3416349 | — | — | 1 | 5.36 |
| CHEMBL3416347 | — | — | 1 | 5.33 |
| CHEMBL3416173 | — | — | 1 | 5.24 |
| CHEMBL2269075 | Sorgoleone-364 | — | 1 | 5.21 |
| CHEMBL3416350 | — | — | 1 | 5.14 |
| CHEMBL471270 | 5-O-METHYLEMBELIN | — | 1 | 5.04 |
| CHEMBL3416174 | — | — | 1 | 5.03 |
| CHEMBL3416356 | — | — | 1 | - |
| CHEMBL3416179 | — | — | 1 | - |
| CHEMBL37141 | — | — | 1 | - |
| CHEMBL3416365 | — | — | 1 | - |
| CHEMBL3416364 | — | — | 1 | - |
| CHEMBL3416351 | — | — | 1 | - |
| CHEMBL3416352 | — | — | 1 | - |
| CHEMBL3416353 | — | — | 1 | - |
| CHEMBL3416354 | — | — | 1 | - |
| CHEMBL3416355 | — | — | 1 | - |
| CHEMBL3416361 | — | — | 1 | - |
| CHEMBL3416357 | — | — | 1 | - |
| CHEMBL3416358 | — | — | 1 | - |
| CHEMBL3416359 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221137 | EMBELIN | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL221598 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL462801 | Rapanone | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3416163 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3416165 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3416348 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL462998 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL29097 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3416164 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3416349 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL3416347 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL3416173 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL2269075 | Sorgoleone-364 | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL3416350 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL471270 | 5-O-METHYLEMBELIN | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL3416174 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL2228912 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3263323 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416166 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416167 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416168 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416169 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416170 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416171 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416172 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2296071 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416175 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416176 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416177 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416178 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416162 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416180 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2228913 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416354 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416356 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416179 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL37141 | — | Activity | - | — | - | |
| CHEMBL3416365 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416364 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416351 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416352 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416353 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416360 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416355 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416361 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416357 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416358 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416359 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416363 | — | Activity | - | — | - | |
| CHEMBL3416362 | — | IC50 | > | 10000.0 | nM | - |