Assay Detail
Binding
CHEMBL664974
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In vitro affinity for CysLT1 receptors on guinea pig lung membranes, measured by displacement of [3H]LTD4.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Lung |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and structure-activity relationships of carboxyflavones as structurally rigid CysLT1 (LTD4) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 23 | 6.67 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL416769 | — | — | 1 | 7.96 |
| CHEMBL33729 | — | — | 1 | 7.92 |
| CHEMBL34835 | — | — | 1 | 7.89 |
| CHEMBL32136 | — | — | 1 | 7.77 |
| CHEMBL33871 | — | — | 1 | 7.77 |
| CHEMBL284624 | — | — | 1 | 7.77 |
| CHEMBL32138 | — | — | 1 | 7.51 |
| CHEMBL287559 | — | — | 1 | 7.10 |
| CHEMBL34740 | — | — | 1 | 7.00 |
| CHEMBL284730 | — | — | 1 | 6.90 |
| CHEMBL33331 | — | — | 1 | 6.68 |
| CHEMBL32764 | — | — | 1 | 6.57 |
| CHEMBL33607 | — | — | 1 | 6.51 |
| CHEMBL285994 | — | — | 1 | 6.42 |
| CHEMBL33329 | — | — | 1 | 6.39 |
| CHEMBL34507 | — | — | 1 | 6.30 |
| CHEMBL33294 | — | — | 1 | 6.28 |
| CHEMBL417135 | — | — | 1 | 5.96 |
| CHEMBL34177 | — | — | 1 | 5.95 |
| CHEMBL33276 | — | — | 1 | 5.76 |
| CHEMBL32944 | — | — | 1 | 5.76 |
| CHEMBL33228 | — | — | 1 | 4.96 |
| CHEMBL286797 | — | — | 1 | 4.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL416769 | — | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL33729 | — | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL34835 | — | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL32136 | — | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL33871 | — | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL284624 | — | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL32138 | — | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL287559 | — | Kd | = | 79.0 | nM | 7.10 |
| CHEMBL34740 | — | Kd | = | 101.0 | nM | 7.00 |
| CHEMBL284730 | — | Kd | = | 127.0 | nM | 6.90 |
| CHEMBL33331 | — | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL32764 | — | Kd | = | 270.0 | nM | 6.57 |
| CHEMBL33607 | — | Kd | = | 307.0 | nM | 6.51 |
| CHEMBL285994 | — | Kd | = | 382.0 | nM | 6.42 |
| CHEMBL33329 | — | Kd | = | 408.0 | nM | 6.39 |
| CHEMBL34507 | — | Kd | = | 504.0 | nM | 6.30 |
| CHEMBL33294 | — | Kd | = | 526.0 | nM | 6.28 |
| CHEMBL417135 | — | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL34177 | — | Kd | = | 1130.0 | nM | 5.95 |
| CHEMBL33276 | — | Kd | = | 1750.0 | nM | 5.76 |
| CHEMBL32944 | — | Kd | = | 1730.0 | nM | 5.76 |
| CHEMBL33228 | — | Kd | = | 11000.0 | nM | 4.96 |
| CHEMBL286797 | — | Kd | = | 55000.0 | nM | 4.26 |