Assay Detail
Binding
CHEMBL830138
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Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
24
Total Activities
24
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 tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.30 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL191090 | — | — | 1 | 8.96 |
| CHEMBL190845 | — | — | 1 | 8.70 |
| CHEMBL296641 | ANTALARMIN | — | 1 | 8.51 |
| CHEMBL188907 | — | — | 1 | 8.35 |
| CHEMBL190488 | — | — | 1 | 8.29 |
| CHEMBL364680 | — | — | 1 | 8.10 |
| CHEMBL365260 | — | — | 1 | 7.92 |
| CHEMBL189780 | — | — | 1 | 7.77 |
| CHEMBL190881 | — | — | 1 | 7.70 |
| CHEMBL371348 | — | — | 1 | 7.64 |
| CHEMBL191395 | — | — | 1 | 7.36 |
| CHEMBL414664 | — | — | 1 | 7.24 |
| CHEMBL364892 | — | — | 1 | 7.22 |
| CHEMBL361242 | — | — | 1 | 6.89 |
| CHEMBL364938 | — | — | 1 | 6.85 |
| CHEMBL190757 | — | — | 1 | 6.82 |
| CHEMBL364037 | — | — | 1 | 6.77 |
| CHEMBL190037 | — | — | 1 | 6.72 |
| CHEMBL190262 | — | — | 1 | 6.70 |
| CHEMBL191188 | — | — | 1 | 6.34 |
| CHEMBL190661 | — | — | 1 | 6.04 |
| CHEMBL363152 | — | — | 1 | 6.00 |
| CHEMBL365745 | — | — | 1 | 5.06 |
| CHEMBL365973 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL191090 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL190845 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL296641 | ANTALARMIN | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL188907 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL190488 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL364680 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL365260 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL189780 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL190881 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL371348 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL191395 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL414664 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL364892 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL361242 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL364938 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL190757 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL364037 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL190037 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL190262 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL191188 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL190661 | — | Ki | = | 920.0 | nM | 6.04 |
| CHEMBL363152 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL365745 | — | Ki | = | 8800.0 | nM | 5.06 |
| CHEMBL365973 | — | Ki | > | 10000.0 | nM | - |