Assay Detail
Binding
CHEMBL663559
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | IMR-32 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
3-Aryl pyrazolo[4,3-d]pyrimidine derivatives: Nonpeptide CRF-1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 7.74 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL67484 | — | — | 1 | 9.00 |
| CHEMBL303380 | — | — | 1 | 8.70 |
| CHEMBL293228 | — | — | 1 | 8.70 |
| CHEMBL9946 | CP-154526 | — | 1 | 8.57 |
| CHEMBL66054 | — | — | 1 | 8.52 |
| CHEMBL66275 | — | — | 1 | 8.52 |
| CHEMBL304335 | — | — | 1 | 8.52 |
| CHEMBL304272 | — | — | 1 | 8.52 |
| CHEMBL302742 | — | — | 1 | 8.40 |
| CHEMBL309138 | — | — | 1 | 8.30 |
| CHEMBL293469 | — | — | 1 | 8.00 |
| CHEMBL68076 | — | — | 1 | 7.96 |
| CHEMBL304059 | — | — | 1 | 7.82 |
| CHEMBL66719 | — | — | 1 | 7.80 |
| CHEMBL66492 | — | — | 1 | 7.80 |
| CHEMBL69968 | — | — | 1 | 7.77 |
| CHEMBL66831 | — | — | 1 | 7.70 |
| CHEMBL303272 | — | — | 1 | 7.62 |
| CHEMBL302589 | — | — | 1 | 7.60 |
| CHEMBL68697 | — | — | 1 | 7.54 |
| CHEMBL417039 | — | — | 1 | 7.42 |
| CHEMBL67483 | — | — | 1 | 7.21 |
| CHEMBL68303 | — | — | 1 | 6.95 |
| CHEMBL67646 | — | — | 1 | 6.94 |
| CHEMBL303639 | — | — | 1 | 6.84 |
| CHEMBL66631 | — | — | 1 | 6.76 |
| CHEMBL66052 | — | — | 1 | 6.72 |
| CHEMBL66671 | — | — | 1 | 6.25 |
| CHEMBL67360 | — | — | 1 | 6.12 |
| CHEMBL306866 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL67484 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL303380 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL293228 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL9946 | CP-154526 | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL66054 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL66275 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL304335 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL304272 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL302742 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL309138 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL293469 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL68076 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL304059 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL66719 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL66492 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL69968 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL66831 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL303272 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL302589 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL68697 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL417039 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL67483 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL68303 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL67646 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL303639 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL66631 | — | Ki | = | 174.0 | nM | 6.76 |
| CHEMBL66052 | — | Ki | = | 192.0 | nM | 6.72 |
| CHEMBL66671 | — | Ki | = | 561.0 | nM | 6.25 |
| CHEMBL67360 | — | Ki | = | 765.0 | nM | 6.12 |
| CHEMBL306866 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL304048 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL66010 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL302037 | — | Ki | > | 5000.0 | nM | - |