Assay Detail
Binding
CHEMBL655824
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Binding affinity against [125I]-hCalcitonin gene-related peptide type alpha receptor binding sites in rat brain membrane
9
Total Activities
9
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 | Expert |
Target
Calcitonin gene-related peptide type 1 receptor (CHEMBL4755) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity study of hCGRP8-37, a calcitonin gene-related peptide receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.21 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL525571 | — | — | 1 | 9.22 |
| CHEMBL2369463 | — | — | 1 | 9.05 |
| CHEMBL2369459 | — | — | 1 | 8.62 |
| CHEMBL2369458 | — | — | 1 | 8.17 |
| CHEMBL2369452 | — | — | 1 | 8.00 |
| CHEMBL2369454 | — | — | 1 | 7.96 |
| CHEMBL2369464 | — | — | 1 | 7.75 |
| CHEMBL2369457 | — | — | 1 | 7.66 |
| CHEMBL2369465 | — | — | 1 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL525571 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL2369463 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL2369459 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2369458 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL2369452 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2369454 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2369464 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL2369457 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2369465 | — | IC50 | = | 33.0 | nM | 7.48 |