Assay Detail
Binding
CHEMBL664982
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membrane
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL4649) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.39 | 8.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9946 | CP-154526 | — | 1 | 8.26 |
| CHEMBL300935 | — | — | 1 | 8.12 |
| CHEMBL296977 | — | — | 1 | 6.96 |
| CHEMBL49217 | — | — | 1 | 6.21 |
| CHEMBL300278 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9946 | CP-154526 | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL300935 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL296977 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL49217 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL300278 | — | IC50 | > | 10000.0 | nM | - |