Assay Detail
Binding
CHEMBL2167614
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
10
Total Activities
10
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 | Autocuration |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL4649) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 8.46 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL559437 | — | — | 1 | 9.59 |
| CHEMBL2165202 | — | — | 1 | 9.17 |
| CHEMBL550685 | — | — | 1 | 9.06 |
| CHEMBL2165196 | — | — | 1 | 8.62 |
| CHEMBL2165195 | — | — | 1 | 8.39 |
| CHEMBL2165201 | — | — | 1 | 8.37 |
| CHEMBL2165197 | — | — | 1 | 8.30 |
| CHEMBL2165198 | — | — | 1 | 8.27 |
| CHEMBL2165200 | — | — | 1 | 8.11 |
| CHEMBL2165199 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL559437 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL2165202 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL550685 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL2165196 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2165195 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL2165201 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL2165197 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2165198 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL2165200 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL2165199 | — | IC50 | = | 210.0 | nM | 6.68 |