Assay Detail
Functional
CHEMBL765153
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration tested in vitro to inhibit PAF-induced maximum aggregation (PAF-Antagonistic activity) by 50%.
87
Total Activities
87
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
(Pyridylcyanomethyl)piperazines as orally active PAF antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 87 | 6.41 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3216197 | — | — | 1 | 8.72 |
| CHEMBL338940 | — | — | 1 | 8.57 |
| CHEMBL133742 | — | — | 1 | 8.12 |
| CHEMBL545771 | — | — | 1 | 8.04 |
| CHEMBL317193 | — | — | 1 | 8.00 |
| CHEMBL335113 | — | — | 1 | 8.00 |
| CHEMBL3216401 | — | — | 1 | 7.96 |
| CHEMBL335432 | — | — | 1 | 7.82 |
| CHEMBL101245 | — | — | 1 | 7.70 |
| CHEMBL103753 | — | — | 1 | 7.68 |
| CHEMBL336612 | — | — | 1 | 7.68 |
| CHEMBL3216182 | — | — | 1 | 7.68 |
| CHEMBL340544 | — | — | 1 | 7.68 |
| CHEMBL335853 | — | — | 1 | 7.64 |
| CHEMBL132852 | — | — | 1 | 7.62 |
| CHEMBL134123 | — | — | 1 | 7.62 |
| CHEMBL134143 | — | — | 1 | 7.58 |
| CHEMBL3217088 | — | — | 1 | 7.58 |
| CHEMBL544607 | — | — | 1 | 7.50 |
| CHEMBL336816 | — | — | 1 | 7.44 |
| CHEMBL554463 | — | — | 1 | 7.44 |
| CHEMBL555567 | — | — | 1 | 7.44 |
| CHEMBL545773 | — | — | 1 | 7.30 |
| CHEMBL3216867 | — | — | 1 | 7.29 |
| CHEMBL103801 | — | — | 1 | 7.28 |
| CHEMBL133457 | — | — | 1 | 7.26 |
| CHEMBL545072 | — | — | 1 | 7.22 |
| CHEMBL423524 | — | — | 1 | 7.12 |
| CHEMBL552805 | — | — | 1 | 7.07 |
| CHEMBL3216628 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3216197 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL338940 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL133742 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL545771 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL317193 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL335113 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3216401 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL335432 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL101245 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL103753 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL336612 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3216182 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL340544 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL335853 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL134123 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL132852 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL134143 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3217088 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL544607 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL336816 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL554463 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL555567 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL545773 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3216867 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL103801 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL133457 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL545072 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL423524 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL552805 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL3216628 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL280164 | APAFANT | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL134094 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL335176 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL543420 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL335044 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL545306 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL130034 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL133921 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3217094 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL335556 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL131597 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3215746 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL559013 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL133425 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL3215980 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL1203313 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL131690 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL542731 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL340989 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL132636 | — | IC50 | = | 720.0 | nM | 6.14 |