Assay Detail
Binding
CHEMBL3801876
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Frontal cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL4649) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and evaluation of carbamate and aryl ether substituted pyrazinones as corticotropin releasing factor-1 (CRF₁) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 8.47 | 9.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL574852 | — | — | 1 | 9.54 |
| CHEMBL3799870 | — | — | 1 | 9.13 |
| CHEMBL44698 | — | — | 1 | 8.92 |
| CHEMBL3797830 | — | — | 1 | 8.92 |
| CHEMBL3799337 | — | — | 1 | 8.89 |
| CHEMBL3797992 | — | — | 1 | 8.82 |
| CHEMBL3798885 | — | — | 1 | 8.82 |
| CHEMBL3799452 | — | — | 1 | 8.82 |
| CHEMBL3800497 | — | — | 1 | 8.82 |
| CHEMBL574436 | — | — | 1 | 8.82 |
| CHEMBL3799036 | — | — | 1 | 8.80 |
| CHEMBL3798004 | — | — | 1 | 8.80 |
| CHEMBL3800413 | — | — | 1 | 8.77 |
| CHEMBL3799825 | — | — | 1 | 8.77 |
| CHEMBL3799784 | — | — | 1 | 8.72 |
| CHEMBL3799560 | — | — | 1 | 8.33 |
| CHEMBL3797551 | — | — | 1 | 8.31 |
| CHEMBL3797368 | — | — | 1 | 8.28 |
| CHEMBL3800125 | — | — | 1 | 8.28 |
| CHEMBL3799801 | — | — | 1 | 8.17 |
| CHEMBL3799211 | — | — | 1 | 8.17 |
| CHEMBL3797955 | — | — | 1 | 8.11 |
| CHEMBL3798497 | — | — | 1 | 8.04 |
| CHEMBL3800523 | — | — | 1 | 8.00 |
| CHEMBL3799417 | — | — | 1 | 8.00 |
| CHEMBL3800035 | — | — | 1 | 7.85 |
| CHEMBL3800457 | — | — | 1 | 7.17 |
| CHEMBL3799741 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL574852 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL3799870 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL44698 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3797830 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3799337 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3797992 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3798885 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3799452 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3800497 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL574436 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3799036 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3798004 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3800413 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3799825 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3799784 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3799560 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3797551 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3797368 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3800125 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3799801 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL3799211 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL3797955 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL3798497 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL3800523 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3799417 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3800035 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3800457 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3799741 | — | IC50 | = | 88.0 | nM | 7.06 |