Assay Detail
Binding
CHEMBL839639
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
36
Total Activities
36
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 |
|---|---|---|---|
| Ki | 36 | 8.12 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL364987 | — | — | 1 | 8.89 |
| CHEMBL65078 | — | — | 1 | 8.80 |
| CHEMBL366155 | — | — | 1 | 8.66 |
| CHEMBL186033 | — | — | 1 | 8.64 |
| CHEMBL361509 | — | — | 1 | 8.62 |
| CHEMBL185705 | — | — | 1 | 8.62 |
| CHEMBL185858 | — | — | 1 | 8.60 |
| CHEMBL183845 | — | — | 1 | 8.59 |
| CHEMBL189821 | — | — | 1 | 8.59 |
| CHEMBL188566 | — | — | 1 | 8.54 |
| CHEMBL121896 | — | — | 1 | 8.47 |
| CHEMBL186592 | — | — | 1 | 8.47 |
| CHEMBL309138 | — | — | 1 | 8.46 |
| CHEMBL188844 | — | — | 1 | 8.38 |
| CHEMBL360851 | — | — | 1 | 8.38 |
| CHEMBL188609 | — | — | 1 | 8.32 |
| CHEMBL365841 | — | — | 1 | 8.28 |
| CHEMBL187039 | — | — | 1 | 8.28 |
| CHEMBL444614 | — | — | 1 | 8.25 |
| CHEMBL361670 | — | — | 1 | 8.19 |
| CHEMBL359784 | — | — | 1 | 8.14 |
| CHEMBL184752 | — | — | 1 | 8.06 |
| CHEMBL183148 | — | — | 1 | 8.04 |
| CHEMBL186992 | — | — | 1 | 8.03 |
| CHEMBL184850 | — | — | 1 | 8.00 |
| CHEMBL366096 | — | — | 1 | 7.96 |
| CHEMBL189754 | — | — | 1 | 7.89 |
| CHEMBL363269 | — | — | 1 | 7.82 |
| CHEMBL426260 | — | — | 1 | 7.77 |
| CHEMBL364828 | — | — | 1 | 7.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL364987 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL65078 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL366155 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL186033 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL361509 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL185705 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL185858 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL183845 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL189821 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL188566 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL121896 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL186592 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL309138 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL188844 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL360851 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL188609 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL365841 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL187039 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL444614 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL361670 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL359784 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL184752 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL183148 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL186992 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL184850 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL366096 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL189754 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL363269 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL426260 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL364828 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL362305 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL364214 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL184740 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL182595 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL364168 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL184284 | — | Ki | = | 260.0 | nM | 6.58 |