Assay Detail
Binding
CHEMBL663518
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Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | EBNA |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
4-Aryl-2-anilinopyrimidines as corticotropin-releasing hormone (CRH) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 7.59 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10125 | — | — | 1 | 8.62 |
| CHEMBL274578 | — | — | 1 | 8.60 |
| CHEMBL9946 | CP-154526 | — | 1 | 8.57 |
| CHEMBL10175 | — | — | 1 | 8.51 |
| CHEMBL436978 | — | — | 1 | 8.34 |
| CHEMBL10373 | — | — | 1 | 8.24 |
| CHEMBL266617 | — | — | 1 | 8.24 |
| CHEMBL276184 | — | — | 1 | 8.11 |
| CHEMBL10189 | — | — | 1 | 8.08 |
| CHEMBL276599 | — | — | 1 | 8.07 |
| CHEMBL10203 | — | — | 1 | 8.05 |
| CHEMBL10473 | — | — | 1 | 8.04 |
| CHEMBL10015 | — | — | 1 | 8.03 |
| CHEMBL10208 | — | — | 1 | 8.00 |
| CHEMBL276716 | — | — | 1 | 7.95 |
| CHEMBL10249 | — | — | 1 | 7.87 |
| CHEMBL10698 | — | — | 1 | 7.86 |
| CHEMBL9975 | — | — | 1 | 7.76 |
| CHEMBL268043 | — | — | 1 | 7.74 |
| CHEMBL275738 | — | — | 1 | 7.69 |
| CHEMBL274081 | — | — | 1 | 7.63 |
| CHEMBL10237 | — | — | 1 | 7.62 |
| CHEMBL9956 | — | — | 1 | 7.60 |
| CHEMBL10526 | — | — | 1 | 7.26 |
| CHEMBL9794 | — | — | 1 | 7.11 |
| CHEMBL10032 | — | — | 1 | 7.07 |
| CHEMBL10150 | — | — | 1 | 6.96 |
| CHEMBL416882 | — | — | 1 | 6.65 |
| CHEMBL274579 | — | — | 1 | 6.64 |
| CHEMBL273745 | — | — | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10125 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL274578 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL9946 | CP-154526 | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL10175 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL436978 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL10373 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL266617 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL276184 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL10189 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL276599 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL10203 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL10473 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL10015 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL10208 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL276716 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL10249 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL10698 | — | Ki | = | 13.9 | nM | 7.86 |
| CHEMBL9975 | — | Ki | = | 17.4 | nM | 7.76 |
| CHEMBL268043 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL275738 | — | Ki | = | 20.6 | nM | 7.69 |
| CHEMBL274081 | — | Ki | = | 23.4 | nM | 7.63 |
| CHEMBL10237 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL9956 | — | Ki | = | 24.9 | nM | 7.60 |
| CHEMBL10526 | — | Ki | = | 54.8 | nM | 7.26 |
| CHEMBL9794 | — | Ki | = | 78.2 | nM | 7.11 |
| CHEMBL10032 | — | Ki | = | 84.6 | nM | 7.07 |
| CHEMBL10150 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL416882 | — | Ki | = | 222.0 | nM | 6.65 |
| CHEMBL274579 | — | Ki | = | 229.0 | nM | 6.64 |
| CHEMBL273745 | — | Ki | = | 369.0 | nM | 6.43 |
| CHEMBL10464 | — | Ki | = | 662.0 | nM | 6.18 |
| CHEMBL9795 | — | Ki | = | 2359.0 | nM | 5.63 |
| CHEMBL274439 | — | Ki | = | 3536.0 | nM | 5.45 |
| CHEMBL269174 | — | Ki | - | nM | - | |
| CHEMBL9589 | — | Ki | - | nM | - | |
| CHEMBL276411 | — | Ki | - | nM | - |