Assay Detail
Binding
CHEMBL664958
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor(1) (CRF(1)) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.86 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL63989 | — | — | 1 | 7.96 |
| CHEMBL65484 | — | — | 1 | 7.82 |
| CHEMBL61954 | — | — | 1 | 7.82 |
| CHEMBL293627 | — | — | 1 | 7.72 |
| CHEMBL63029 | — | — | 1 | 7.31 |
| CHEMBL66249 | — | — | 1 | 7.20 |
| CHEMBL63457 | — | — | 1 | 7.20 |
| CHEMBL291828 | — | — | 1 | 7.00 |
| CHEMBL291657 | CRINECERFONT | 4.0 | 1 | 6.62 |
| CHEMBL291419 | — | — | 1 | 6.62 |
| CHEMBL302396 | — | — | 1 | 6.60 |
| CHEMBL305354 | — | — | 1 | 6.34 |
| CHEMBL417033 | — | — | 1 | 6.16 |
| CHEMBL63585 | — | — | 1 | 6.07 |
| CHEMBL305583 | — | — | 1 | 5.70 |
| CHEMBL65979 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL63989 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL65484 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL61954 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL293627 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL63029 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL66249 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL63457 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL291828 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL291657 | CRINECERFONT | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL291419 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL302396 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL305354 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL417033 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL63585 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL305583 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL65979 | — | Ki | = | 2200.0 | nM | 5.66 |