Assay Detail
Binding
CHEMBL764536
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In vitro for platelet activating factor receptor antagonist activity in a binding assay using washed whole dog platelets.
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Canis lupus familiaris |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.94 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34461 | — | — | 1 | 8.10 |
| CHEMBL442259 | — | — | 1 | 8.00 |
| CHEMBL430919 | — | — | 1 | 8.00 |
| CHEMBL286217 | — | — | 1 | 8.00 |
| CHEMBL32475 | — | — | 1 | 7.70 |
| CHEMBL287465 | — | — | 1 | 7.70 |
| CHEMBL289463 | — | — | 1 | 7.70 |
| CHEMBL32942 | — | — | 1 | 7.52 |
| CHEMBL432850 | — | — | 1 | 7.46 |
| CHEMBL284079 | — | — | 1 | 7.22 |
| CHEMBL286229 | — | — | 1 | 7.10 |
| CHEMBL369194 | — | — | 1 | 7.00 |
| CHEMBL286762 | — | — | 1 | 6.96 |
| CHEMBL32389 | — | — | 1 | 6.92 |
| CHEMBL286557 | — | — | 1 | 6.75 |
| CHEMBL32327 | — | — | 1 | 6.75 |
| CHEMBL280164 | APAFANT | 2.0 | 1 | 6.70 |
| CHEMBL285035 | — | — | 1 | 6.60 |
| CHEMBL32479 | BROTIZOLAM | 4.0 | 1 | 6.52 |
| CHEMBL33857 | — | — | 1 | 6.52 |
| CHEMBL20359 | — | — | 1 | 6.43 |
| CHEMBL284280 | — | — | 1 | 6.42 |
| CHEMBL286337 | — | — | 1 | 6.40 |
| CHEMBL32932 | — | — | 1 | 6.40 |
| CHEMBL34796 | — | — | 1 | 6.38 |
| CHEMBL285199 | — | — | 1 | 6.38 |
| CHEMBL285067 | — | — | 1 | 6.35 |
| CHEMBL32767 | — | — | 1 | 6.19 |
| CHEMBL32303 | — | — | 1 | 6.00 |
| CHEMBL33217 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34461 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL442259 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL430919 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL286217 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL32475 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL287465 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL289463 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL32942 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL432850 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL284079 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL286229 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL369194 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL286762 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL32389 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL286557 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL32327 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL280164 | APAFANT | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL285035 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL32479 | BROTIZOLAM | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL33857 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL20359 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL284280 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL286337 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL32932 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL34796 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL285199 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL285067 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL32767 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL32303 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL33217 | — | IC50 | = | 1000.0 | nM | 6.00 |