Assay Detail
Functional
CHEMBL760189
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Platelet-activating factor receptor (CHEMBL5136) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Novel antagonists of platelet-activating factor. 2. Synthesis and structure-activity relationships of potent and long-acting heterofused [1,5]benzodiazepine and [1,4]diazepine derivatives of 2-methyl-1-phenylimidazo[4,5-c]pyridine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 8.38 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119660 | — | — | 1 | 9.52 |
| CHEMBL420527 | — | — | 1 | 9.40 |
| CHEMBL119371 | — | — | 1 | 9.30 |
| CHEMBL324121 | — | — | 1 | 9.22 |
| CHEMBL327034 | — | — | 1 | 9.22 |
| CHEMBL119659 | — | — | 1 | 9.15 |
| CHEMBL119417 | — | — | 1 | 9.10 |
| CHEMBL431664 | — | — | 1 | 9.00 |
| CHEMBL177351 | — | — | 1 | 8.92 |
| CHEMBL119317 | — | — | 1 | 8.89 |
| CHEMBL117733 | — | — | 1 | 8.89 |
| CHEMBL431470 | — | — | 1 | 8.85 |
| CHEMBL333780 | — | — | 1 | 8.82 |
| CHEMBL119439 | — | — | 1 | 8.77 |
| CHEMBL118813 | — | — | 1 | 8.64 |
| CHEMBL116938 | — | — | 1 | 8.62 |
| CHEMBL119425 | — | — | 1 | 8.62 |
| CHEMBL119763 | — | — | 1 | 8.60 |
| CHEMBL120515 | — | — | 1 | 8.57 |
| CHEMBL118672 | — | — | 1 | 8.49 |
| CHEMBL118793 | — | — | 1 | 8.46 |
| CHEMBL118511 | — | — | 1 | 8.46 |
| CHEMBL118780 | — | — | 1 | 8.40 |
| CHEMBL119452 | — | — | 1 | 8.40 |
| CHEMBL331124 | — | — | 1 | 8.40 |
| CHEMBL29067 | — | — | 1 | 8.37 |
| CHEMBL432832 | — | — | 1 | 8.30 |
| CHEMBL332448 | — | — | 1 | 8.28 |
| CHEMBL332455 | — | — | 1 | 8.25 |
| CHEMBL118247 | — | — | 1 | 8.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119660 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL420527 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL119371 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL324121 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL327034 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL119659 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL119417 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL431664 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL177351 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL119317 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL117733 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL431470 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL333780 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL119439 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL118813 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL116938 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL119425 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL119763 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL120515 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL118672 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL118511 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL118793 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL118780 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL119452 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL331124 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL29067 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL432832 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL332448 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL332455 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL118247 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL331567 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL420697 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL116325 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL118302 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL118840 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL324154 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL325928 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL120322 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL331512 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL332542 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL118182 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL325439 | BEPAFANT | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL325700 | — | IC50 | = | 130.0 | nM | 6.89 |