Assay Detail
Binding
CHEMBL664985
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebellum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL4649) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 7.89 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL115836 | 5-Chloro-N-cyclopropylmethyl-N'-(2,6-dichloro-4-tributylstannanyl-phenyl)-2-methyl-N-propyl-pyrimidine-4,6-diamine | — | 1 | 8.52 |
| CHEMBL325577 | — | — | 1 | 7.85 |
| CHEMBL113333 | — | — | 1 | 7.68 |
| CHEMBL45281 | — | — | 1 | 7.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL115836 | 5-Chloro-N-cyclopropylmethyl-N'-(2,6-dichloro-4-tributylstannanyl-phenyl)-2-methyl-N-propyl-pyrimidine-4,6-diamine | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL325577 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL113333 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL45281 | — | Ki | = | 31.0 | nM | 7.51 |