Assay Detail
Binding
CHEMBL768487
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Displacement of [3H]PAF from PAF receptor of human platelet membranes
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
(+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a potent dual 5-lipoxygenase inhibitor and platelet-activating factor receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.55 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113725 | — | — | 1 | 8.70 |
| CHEMBL299944 | — | — | 1 | 8.22 |
| CHEMBL2113720 | — | — | 1 | 8.00 |
| CHEMBL2113727 | — | — | 1 | 7.70 |
| CHEMBL2113723 | — | — | 1 | 7.68 |
| CHEMBL2113722 | — | — | 1 | 7.66 |
| CHEMBL2113721 | — | — | 1 | 7.64 |
| CHEMBL2113733 | — | — | 1 | 7.60 |
| CHEMBL59051 | — | — | 1 | 7.48 |
| CHEMBL2113726 | — | — | 1 | 7.42 |
| CHEMBL2113730 | — | — | 1 | 7.41 |
| CHEMBL2113724 | — | — | 1 | 7.35 |
| CHEMBL280164 | APAFANT | 2.0 | 1 | 7.03 |
| CHEMBL2113731 | — | — | 1 | 6.78 |
| CHEMBL2113732 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113725 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL299944 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2113720 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2113727 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2113723 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2113722 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2113721 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2113733 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL59051 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2113726 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2113730 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2113724 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL280164 | APAFANT | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL2113731 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL2113732 | — | IC50 | = | 285.0 | nM | 6.54 |