Assay Detail
Binding
CHEMBL2040006
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Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Calcitonin gene-related peptide type 1 receptor (CHEMBL4755) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.79 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2035981 | — | — | 1 | 8.47 |
| CHEMBL1910936 | MK3207 | 2.0 | 1 | 8.00 |
| CHEMBL2035985 | — | — | 1 | 7.89 |
| CHEMBL2035983 | — | — | 1 | 7.77 |
| CHEMBL2035984 | — | — | 1 | 7.75 |
| CHEMBL2035982 | — | — | 1 | 7.42 |
| CHEMBL2035986 | — | — | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2035981 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL1910936 | MK3207 | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2035985 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2035983 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL2035984 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2035982 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL2035986 | — | Ki | = | 60.0 | nM | 7.22 |