Assay Detail
Binding
CHEMBL663558
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Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Rapid microscale synthesis, a new method for lead optimization using robotics and solution phase chemistry: application to the synthesis and optimization of corticotropin-releasing factor1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 5.95 | 7.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL306618 | — | — | 1 | 7.24 |
| CHEMBL77391 | — | — | 1 | 6.94 |
| CHEMBL308544 | — | — | 1 | 6.89 |
| CHEMBL419636 | — | — | 1 | 6.31 |
| CHEMBL307419 | — | — | 1 | 6.31 |
| CHEMBL305671 | — | — | 1 | 5.98 |
| CHEMBL78035 | — | — | 1 | 5.98 |
| CHEMBL307871 | — | — | 1 | 5.83 |
| CHEMBL78271 | — | — | 1 | 5.77 |
| CHEMBL137434 | — | — | 1 | 5.77 |
| CHEMBL77527 | — | — | 1 | 5.68 |
| CHEMBL136519 | — | — | 1 | 5.24 |
| CHEMBL136828 | — | — | 1 | 5.10 |
| CHEMBL343073 | — | — | 1 | 4.26 |
| CHEMBL343704 | — | — | 1 | - |
| CHEMBL343343 | — | — | 1 | - |
| CHEMBL137122 | — | — | 1 | - |
| CHEMBL137666 | — | — | 1 | - |
| CHEMBL137610 | — | — | 1 | - |
| CHEMBL78203 | — | — | 1 | - |
| CHEMBL337096 | — | — | 1 | - |
| CHEMBL138597 | — | — | 1 | - |
| CHEMBL138124 | — | — | 1 | - |
| CHEMBL343958 | — | — | 1 | - |
| CHEMBL136596 | — | — | 1 | - |
| CHEMBL135615 | — | — | 1 | - |
| CHEMBL137291 | — | — | 1 | - |
| CHEMBL137123 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL306618 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL77391 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL308544 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL419636 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL307419 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL305671 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL78035 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL307871 | — | Ki | = | 1470.0 | nM | 5.83 |
| CHEMBL78271 | — | Ki | = | 1690.0 | nM | 5.77 |
| CHEMBL137434 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL77527 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL136519 | — | Ki | = | 5700.0 | nM | 5.24 |
| CHEMBL136828 | — | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL343073 | — | Ki | = | 55000.0 | nM | 4.26 |
| CHEMBL343704 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL343343 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL137122 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL137666 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL137610 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL78203 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL337096 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL138597 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL138124 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL343958 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL136596 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL135615 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL137291 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL137123 | — | Ki | > | 10000.0 | nM | - |