Assay Detail
Functional
CHEMBL1811339
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CRF-1 receptor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of N-(1-ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98-2): an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 8.48 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL498311 | — | — | 1 | 9.70 |
| CHEMBL432800 | — | — | 1 | 9.05 |
| CHEMBL44698 | — | — | 1 | 8.70 |
| CHEMBL1628268 | — | — | 1 | 8.70 |
| CHEMBL45281 | — | — | 1 | 8.70 |
| CHEMBL309138 | — | — | 1 | 8.52 |
| CHEMBL9946 | CP-154526 | — | 1 | 8.52 |
| CHEMBL188907 | — | — | 1 | 8.40 |
| CHEMBL497653 | — | — | 1 | 8.05 |
| CHEMBL398531 | — | — | 1 | 7.96 |
| CHEMBL1806727 | — | — | 1 | 6.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL498311 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL432800 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL44698 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1628268 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL45281 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL309138 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL9946 | CP-154526 | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL188907 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL497653 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL398531 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL1806727 | — | Ki | = | 103.0 | nM | 6.99 |