Assay Detail
Binding
CHEMBL665735
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
13
Total Activities
13
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
Design and synthesis of a series of non-peptide high-affinity human corticotropin-releasing factor1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.67 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45281 | — | — | 1 | 8.77 |
| CHEMBL305900 | — | — | 1 | 8.70 |
| CHEMBL306482 | — | — | 1 | 8.64 |
| CHEMBL75859 | — | — | 1 | 8.60 |
| CHEMBL77716 | — | — | 1 | 8.42 |
| CHEMBL77006 | — | — | 1 | 7.52 |
| CHEMBL306618 | — | — | 1 | 7.24 |
| CHEMBL140175 | — | — | 1 | 7.16 |
| CHEMBL344805 | — | — | 1 | 6.82 |
| CHEMBL134475 | — | — | 1 | 6.60 |
| CHEMBL80806 | — | — | 1 | 5.86 |
| CHEMBL138687 | — | — | 1 | - |
| CHEMBL136593 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL45281 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL305900 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL306482 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL75859 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL77716 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL77006 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL306618 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL140175 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL344805 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL134475 | — | Ki | = | 253.0 | nM | 6.60 |
| CHEMBL80806 | — | Ki | = | 1390.0 | nM | 5.86 |
| CHEMBL138687 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL136593 | — | Ki | > | 10000.0 | nM | - |