Assay Detail
Binding
CHEMBL3750741
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PGES-1 in human A549 cell microsomes using PGH2 as substrate assessed as suppression of interleukin-1beta-stimulated PGE2 production incubated for 15 mins post interleukin-1beta challenge for 72 hrs by RP-HPLC analysis
11
Total Activities
11
Compounds Tested
1
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 |
Publication
Hit-to-lead optimization of phenylsulfonyl hydrazides for a potent suppressor of PGE2 production: Synthesis, biological activity, and molecular docking study.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.81 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3746729 | — | — | 1 | 7.16 |
| CHEMBL29097 | — | — | 1 | 5.70 |
| CHEMBL3746644 | — | — | 1 | 5.21 |
| CHEMBL3746332 | — | — | 1 | 5.18 |
| CHEMBL3747740 | — | — | 1 | - |
| CHEMBL3746705 | — | — | 1 | - |
| CHEMBL3746542 | — | — | 1 | - |
| CHEMBL3746507 | — | — | 1 | - |
| CHEMBL3746498 | — | — | 1 | - |
| CHEMBL3747473 | — | — | 1 | - |
| CHEMBL3747438 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3746729 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL29097 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3746644 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL3746332 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL3747740 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3746705 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3746542 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3746507 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3746498 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3747473 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3747438 | — | IC50 | > | 10000.0 | nM | - |