Assay Detail
Binding
CHEMBL829792
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
43
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | IMR-32 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis, structure-activity relationships, and anxiolytic activity of 7-aryl-6,7-dihydroimidazoimidazole corticotropin-releasing factor 1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 43 | 6.74 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45281 | — | — | 2 | 8.70 |
| CHEMBL9946 | CP-154526 | — | 2 | 8.57 |
| CHEMBL362815 | — | — | 1 | 7.62 |
| CHEMBL182482 | — | — | 1 | 7.58 |
| CHEMBL359936 | — | — | 1 | 7.39 |
| CHEMBL359832 | — | — | 1 | 7.39 |
| CHEMBL359956 | — | — | 1 | 7.38 |
| CHEMBL369341 | — | — | 1 | 7.21 |
| CHEMBL181227 | — | — | 1 | 7.20 |
| CHEMBL178165 | — | — | 1 | 7.17 |
| CHEMBL433768 | — | — | 1 | 7.14 |
| CHEMBL183824 | — | — | 1 | 7.12 |
| CHEMBL368879 | — | — | 1 | 7.03 |
| CHEMBL181283 | — | — | 1 | 7.03 |
| CHEMBL368041 | — | — | 1 | 7.00 |
| CHEMBL182278 | — | — | 1 | 6.90 |
| CHEMBL180178 | — | — | 1 | 6.66 |
| CHEMBL183639 | — | — | 1 | 6.66 |
| CHEMBL183348 | — | — | 1 | 6.66 |
| CHEMBL181053 | — | — | 1 | 6.57 |
| CHEMBL180613 | — | — | 1 | 6.57 |
| CHEMBL178617 | — | — | 1 | 6.54 |
| CHEMBL181287 | — | — | 1 | 6.21 |
| CHEMBL181823 | — | — | 1 | 6.19 |
| CHEMBL359499 | — | — | 1 | 6.18 |
| CHEMBL368245 | — | — | 1 | 6.13 |
| CHEMBL179499 | — | — | 1 | 6.11 |
| CHEMBL182624 | — | — | 1 | 5.81 |
| CHEMBL180610 | — | — | 1 | 5.52 |
| CHEMBL181002 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL45281 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL9946 | CP-154526 | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL9946 | CP-154526 | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL45281 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL362815 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL182482 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL359832 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL359936 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL359956 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL369341 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL181227 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL178165 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL433768 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL183824 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL368879 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL181283 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL368041 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL182278 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL183348 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL183639 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL180178 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL181053 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL180613 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL178617 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL181287 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL181823 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL359499 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL368245 | — | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL179499 | — | Ki | = | 770.0 | nM | 6.11 |
| CHEMBL182624 | — | Ki | = | 1559.0 | nM | 5.81 |
| CHEMBL181002 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL180610 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL180284 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL181989 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL362799 | — | Ki | = | 6600.0 | nM | 5.18 |
| CHEMBL179985 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL182585 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL361194 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL181797 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL180137 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL179790 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL183163 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL178577 | — | Ki | > | 10000.0 | nM | - |