Assay Detail
Binding
CHEMBL3761675
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Inhibition of mPGES1 in LPS-induced human whole blood assessed as suppression of PGE2 response after 20 to 24 hrs by LC-MS/MS analysis
38
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.08 | 7.92 |
| IC80 | 19 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3342693 | — | — | 2 | 7.92 |
| CHEMBL3758924 | — | — | 2 | 7.54 |
| CHEMBL3759288 | — | — | 2 | 7.04 |
| CHEMBL3758953 | — | — | 2 | 6.47 |
| CHEMBL3758222 | — | — | 2 | 6.43 |
| CHEMBL2152710 | — | — | 2 | 6.22 |
| CHEMBL412099 | — | — | 2 | 6.17 |
| CHEMBL2152712 | LY-3031207 | 1.0 | 2 | 6.13 |
| CHEMBL2152711 | — | — | 2 | 6.10 |
| CHEMBL3758186 | — | — | 2 | 6.07 |
| CHEMBL3758743 | — | — | 2 | 5.84 |
| CHEMBL3759737 | — | — | 2 | 5.67 |
| CHEMBL3759709 | — | — | 2 | 5.61 |
| CHEMBL3760103 | — | — | 2 | 5.34 |
| CHEMBL3758980 | — | — | 2 | 5.02 |
| CHEMBL3760032 | — | — | 2 | 4.98 |
| CHEMBL3759119 | — | — | 2 | 4.89 |
| CHEMBL3758879 | — | — | 2 | - |
| CHEMBL3758663 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3342693 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3758924 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3759288 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL3758953 | — | IC50 | = | 338.0 | nM | 6.47 |
| CHEMBL3758222 | — | IC50 | = | 374.0 | nM | 6.43 |
| CHEMBL2152710 | — | IC50 | = | 607.0 | nM | 6.22 |
| CHEMBL412099 | — | IC50 | = | 676.0 | nM | 6.17 |
| CHEMBL2152712 | LY-3031207 | IC50 | = | 744.0 | nM | 6.13 |
| CHEMBL2152711 | — | IC50 | = | 792.0 | nM | 6.10 |
| CHEMBL3758186 | — | IC50 | = | 853.0 | nM | 6.07 |
| CHEMBL3758743 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL3759737 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL3759709 | — | IC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL3760103 | — | IC50 | = | 4610.0 | nM | 5.34 |
| CHEMBL3758980 | — | IC50 | = | 9530.0 | nM | 5.02 |
| CHEMBL3760032 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL3759119 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL3758663 | — | IC50 | - | — | - | |
| CHEMBL3758879 | — | IC50 | - | — | - | |
| CHEMBL3758663 | — | IC80 | - | — | - | |
| CHEMBL3758953 | — | IC80 | = | 994.0 | nM | - |
| CHEMBL3758924 | — | IC80 | = | 146.0 | nM | - |
| CHEMBL3759288 | — | IC80 | = | 480.0 | nM | - |
| CHEMBL3342693 | — | IC80 | = | 69.0 | nM | - |
| CHEMBL3758222 | — | IC80 | = | 991.0 | nM | - |
| CHEMBL3758879 | — | IC80 | - | — | - | |
| CHEMBL3760103 | — | IC80 | = | 31.0 | uM | - |
| CHEMBL3758980 | — | IC80 | = | 57.4 | uM | - |
| CHEMBL3759119 | — | IC80 | = | 132.0 | uM | - |
| CHEMBL2152711 | — | IC80 | = | 8.8 | uM | - |
| CHEMBL3758186 | — | IC80 | = | 9.37 | uM | - |
| CHEMBL2152712 | LY-3031207 | IC80 | = | 2.44 | uM | - |
| CHEMBL412099 | — | IC80 | = | 3.65 | uM | - |
| CHEMBL3758743 | — | IC80 | = | 33.7 | uM | - |
| CHEMBL3759737 | — | IC80 | = | 10.5 | uM | - |
| CHEMBL3760032 | — | IC80 | = | 21.1 | uM | - |
| CHEMBL3759709 | — | IC80 | = | 9.08 | uM | - |
| CHEMBL2152710 | — | IC80 | = | 2.39 | uM | - |