Assay Detail
Binding
CHEMBL828240
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and structure--activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.10 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL65078 | — | — | 1 | 7.54 |
| CHEMBL187039 | — | — | 1 | 7.40 |
| CHEMBL444614 | — | — | 1 | 7.30 |
| CHEMBL309138 | — | — | 1 | 7.30 |
| CHEMBL121896 | — | — | 1 | 7.12 |
| CHEMBL188844 | — | — | 1 | 6.96 |
| CHEMBL184850 | — | — | 1 | 6.80 |
| CHEMBL183148 | — | — | 1 | 6.75 |
| CHEMBL366155 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL65078 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL187039 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL444614 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL309138 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL121896 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL188844 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL184850 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL183148 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL366155 | — | IC50 | = | 190.0 | nM | 6.72 |