Assay Detail
Binding
CHEMBL655828
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Binding affinity against [125I]-hCalcitonin gene-related peptide type receptor binding sites in guinea pig atrium membrane
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cardiac atrium |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Calcitonin gene-related peptide type 1 receptor (CHEMBL3798) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-activity study of hCGRP8-37, a calcitonin gene-related peptide receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.22 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2369459 | — | — | 1 | 8.70 |
| CHEMBL2369463 | — | — | 1 | 8.64 |
| CHEMBL525571 | — | — | 1 | 8.64 |
| CHEMBL2369454 | — | — | 1 | 8.52 |
| CHEMBL2369458 | — | — | 1 | 8.16 |
| CHEMBL2369452 | — | — | 1 | 8.05 |
| CHEMBL2369457 | — | — | 1 | 7.95 |
| CHEMBL2369464 | — | — | 1 | 7.70 |
| CHEMBL2369465 | — | — | 1 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2369459 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2369463 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL525571 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2369454 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2369458 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL2369452 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2369457 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL2369464 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL2369465 | — | IC50 | = | 25.0 | nM | 7.60 |