Assay Detail
Binding
CHEMBL830013
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL4649) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 8.29 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL187073 | — | — | 1 | 9.52 |
| CHEMBL186203 | — | — | 1 | 9.31 |
| CHEMBL188464 | — | — | 1 | 9.30 |
| CHEMBL186252 | — | — | 1 | 9.15 |
| CHEMBL186097 | — | — | 1 | 9.09 |
| CHEMBL189089 | — | — | 1 | 9.04 |
| CHEMBL364883 | — | — | 1 | 9.04 |
| CHEMBL186241 | — | — | 1 | 8.92 |
| CHEMBL363654 | — | — | 1 | 8.82 |
| CHEMBL189196 | — | — | 1 | 8.74 |
| CHEMBL187987 | — | — | 1 | 8.66 |
| CHEMBL186517 | — | — | 1 | 8.59 |
| CHEMBL187410 | — | — | 1 | 8.48 |
| CHEMBL188858 | — | — | 1 | 8.39 |
| CHEMBL188861 | — | — | 1 | 8.38 |
| CHEMBL185648 | — | — | 1 | 8.15 |
| CHEMBL433592 | — | — | 1 | 8.00 |
| CHEMBL425542 | — | — | 1 | 7.75 |
| CHEMBL361296 | — | — | 1 | 7.31 |
| CHEMBL365868 | — | — | 1 | 7.17 |
| CHEMBL365511 | — | — | 1 | 7.04 |
| CHEMBL188112 | — | — | 1 | 6.90 |
| CHEMBL185736 | — | — | 1 | 6.70 |
| CHEMBL365488 | — | — | 1 | 6.52 |
| CHEMBL188001 | — | — | 1 | - |
| CHEMBL185963 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL187073 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL186203 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL188464 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL186252 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL186097 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL189089 | — | IC50 | = | 0.92 | nM | 9.04 |
| CHEMBL364883 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL186241 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL363654 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL189196 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL187987 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL186517 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL187410 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL188858 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL188861 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL185648 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL433592 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL425542 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL361296 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL365868 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL365511 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL188112 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL185736 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL365488 | — | IC50 | = | 305.0 | nM | 6.52 |
| CHEMBL188001 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL185963 | — | IC50 | > | 1000.0 | nM | - |