Assay Detail
Functional
CHEMBL1037909
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimising metabolic stability in lipophilic chemical space: the identification of a metabolically stable pyrazolopyrimidine CRF-1 receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.82 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL576049 | — | — | 1 | 8.05 |
| CHEMBL568606 | — | — | 1 | 7.89 |
| CHEMBL568685 | — | — | 1 | 7.77 |
| CHEMBL569666 | — | — | 1 | 7.50 |
| CHEMBL566279 | — | — | 1 | 7.46 |
| CHEMBL565442 | — | — | 1 | 7.38 |
| CHEMBL568665 | — | — | 1 | 7.37 |
| CHEMBL583237 | — | — | 1 | 7.13 |
| CHEMBL566073 | — | — | 1 | 7.12 |
| CHEMBL568188 | — | — | 1 | 7.08 |
| CHEMBL576664 | — | — | 1 | 7.07 |
| CHEMBL567164 | — | — | 1 | 7.00 |
| CHEMBL567383 | — | — | 1 | 6.93 |
| CHEMBL566938 | — | — | 1 | 6.91 |
| CHEMBL566910 | — | — | 1 | 6.89 |
| CHEMBL568656 | — | — | 1 | 6.88 |
| CHEMBL577239 | — | — | 1 | 6.87 |
| CHEMBL584472 | — | — | 1 | 6.74 |
| CHEMBL583005 | — | — | 1 | 6.71 |
| CHEMBL566912 | — | — | 1 | 6.68 |
| CHEMBL567538 | — | — | 1 | 6.56 |
| CHEMBL567741 | — | — | 1 | 6.40 |
| CHEMBL569202 | — | — | 1 | 6.24 |
| CHEMBL576639 | — | — | 1 | 6.24 |
| CHEMBL568397 | — | — | 1 | 6.21 |
| CHEMBL583223 | — | — | 1 | 6.20 |
| CHEMBL568607 | — | — | 1 | 6.00 |
| CHEMBL566939 | — | — | 1 | 5.95 |
| CHEMBL566911 | — | — | 1 | 5.85 |
| CHEMBL567382 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL576049 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL568606 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL568685 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL569666 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL566279 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL565442 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL568665 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL583237 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL566073 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL568188 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL576664 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL567164 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL567383 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL566938 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL566910 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL568656 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL577239 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL584472 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL583005 | — | Ki | = | 193.0 | nM | 6.71 |
| CHEMBL566912 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL567538 | — | Ki | = | 275.0 | nM | 6.56 |
| CHEMBL567741 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL569202 | — | Ki | = | 574.0 | nM | 6.24 |
| CHEMBL576639 | — | Ki | = | 577.0 | nM | 6.24 |
| CHEMBL568397 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL583223 | — | Ki | = | 632.0 | nM | 6.20 |
| CHEMBL568607 | — | Ki | = | 996.0 | nM | 6.00 |
| CHEMBL566939 | — | Ki | = | 1130.0 | nM | 5.95 |
| CHEMBL566911 | — | Ki | = | 1409.0 | nM | 5.85 |
| CHEMBL567382 | — | Ki | = | 2500.0 | nM | 5.60 |