Assay Detail
Binding
CHEMBL1037787
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Frontal cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL4649) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
A strategy to minimize reactive metabolite formation: discovery of (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a potent, orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.91 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL583153 | — | — | 1 | 9.68 |
| CHEMBL574852 | — | — | 1 | 9.62 |
| CHEMBL584343 | — | — | 1 | 9.55 |
| CHEMBL583387 | — | — | 1 | 9.52 |
| CHEMBL572589 | — | — | 1 | 9.30 |
| CHEMBL574853 | — | — | 1 | 9.09 |
| CHEMBL573978 | — | — | 1 | 9.07 |
| CHEMBL575491 | — | — | 1 | 8.96 |
| CHEMBL576589 | — | — | 1 | 8.85 |
| CHEMBL574436 | — | — | 1 | 8.82 |
| CHEMBL573748 | — | — | 1 | 8.82 |
| CHEMBL572588 | — | — | 1 | 8.80 |
| CHEMBL573976 | — | — | 1 | 8.77 |
| CHEMBL573284 | — | — | 1 | 8.00 |
| CHEMBL578838 | — | — | 1 | 7.92 |
| CHEMBL575510 | — | — | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL583153 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL574852 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL584343 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL583387 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL572589 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL574853 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL573978 | — | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL575491 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL576589 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL574436 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL573748 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL572588 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL573976 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL573284 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL578838 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL575510 | — | IC50 | = | 14.0 | nM | 7.85 |