Assay Detail
Binding
CHEMBL663521
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2, 4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: a potent, orally bioavailable CRF(1) receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.77 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL341820 | — | — | 1 | 9.40 |
| CHEMBL344223 | — | — | 1 | 9.22 |
| CHEMBL140894 | — | — | 1 | 9.15 |
| CHEMBL336678 | — | — | 1 | 8.96 |
| CHEMBL337768 | — | — | 1 | 8.92 |
| CHEMBL140143 | — | — | 1 | 8.92 |
| CHEMBL475903 | — | — | 1 | 8.80 |
| CHEMBL138154 | — | — | 1 | 8.80 |
| CHEMBL141085 | — | — | 1 | 8.80 |
| CHEMBL44698 | — | — | 1 | 8.77 |
| CHEMBL141084 | — | — | 1 | 8.74 |
| CHEMBL138155 | — | — | 1 | 8.72 |
| CHEMBL141692 | — | — | 1 | 8.21 |
| CHEMBL334935 | — | — | 1 | 7.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL341820 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL344223 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL140894 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL336678 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL337768 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL140143 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL475903 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL138154 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL141085 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL44698 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL141084 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL138155 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL141692 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL334935 | — | Ki | = | 44.5 | nM | 7.35 |