Assay Detail
Binding
CHEMBL828835
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Ltk- |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Rational design, synthesis, and structure-activity relationships of aryltriazoles as novel corticotropin-releasing factor-1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 39 | 7.36 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45281 | — | — | 1 | 8.70 |
| CHEMBL2094063 | — | — | 1 | 8.57 |
| CHEMBL3085414 | — | — | 1 | 8.40 |
| CHEMBL2094043 | — | — | 1 | 8.28 |
| CHEMBL2093962 | — | — | 1 | 8.24 |
| CHEMBL3085416 | — | — | 1 | 8.20 |
| CHEMBL178836 | — | — | 1 | 8.17 |
| CHEMBL426419 | — | — | 1 | 8.16 |
| CHEMBL362453 | — | — | 1 | 8.14 |
| CHEMBL2094044 | — | — | 1 | 8.05 |
| CHEMBL110609 | — | — | 1 | 8.04 |
| CHEMBL3085415 | — | — | 1 | 7.93 |
| CHEMBL178735 | — | — | 1 | 7.92 |
| CHEMBL359863 | — | — | 1 | 7.85 |
| CHEMBL178117 | — | — | 1 | 7.85 |
| CHEMBL3085418 | — | — | 1 | 7.79 |
| CHEMBL3085417 | — | — | 1 | 7.66 |
| CHEMBL179540 | — | — | 1 | 7.62 |
| CHEMBL433940 | — | — | 1 | 7.58 |
| CHEMBL107786 | — | — | 1 | 7.55 |
| CHEMBL362847 | — | — | 1 | 7.34 |
| CHEMBL2093960 | — | — | 1 | 7.34 |
| CHEMBL2093961 | — | — | 1 | 7.29 |
| CHEMBL175902 | — | — | 1 | 7.21 |
| CHEMBL106972 | — | — | 1 | 7.10 |
| CHEMBL194877 | — | — | 1 | 7.08 |
| CHEMBL179647 | — | — | 1 | 6.92 |
| CHEMBL178346 | — | — | 1 | 6.82 |
| CHEMBL178667 | — | — | 1 | 6.55 |
| CHEMBL2094064 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL45281 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2094063 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL3085414 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2094043 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL2093962 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL3085416 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL178836 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL426419 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL362453 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL2094044 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL110609 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL3085415 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL178735 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL359863 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL178117 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3085418 | — | Ki | = | 16.3 | nM | 7.79 |
| CHEMBL3085417 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL179540 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL433940 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL107786 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL2093960 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL362847 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL2093961 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL175902 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL106972 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL194877 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL179647 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL178346 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL178667 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL2094064 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL2093959 | — | Ki | = | 428.0 | nM | 6.37 |
| CHEMBL178618 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL367789 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL178702 | — | Ki | = | 910.0 | nM | 6.04 |
| CHEMBL178725 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL431067 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL175536 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL180381 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL321389 | — | Ki | > | 10000.0 | nM | - |