Assay Detail
Functional
CHEMBL1046105
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Calcitonin gene-related peptide type 1 receptor (CHEMBL3798) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: development of novel spiropiperidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.73 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL236593 | TELCAGEPANT | 3.0 | 1 | 8.70 |
| CHEMBL570746 | — | — | 1 | 8.57 |
| CHEMBL571203 | — | — | 1 | 8.48 |
| CHEMBL570531 | — | — | 1 | 7.96 |
| CHEMBL570748 | — | — | 1 | 7.89 |
| CHEMBL577110 | — | — | 1 | 7.64 |
| CHEMBL570793 | — | — | 1 | 7.36 |
| CHEMBL572114 | — | — | 1 | 7.26 |
| CHEMBL571459 | — | — | 1 | 7.22 |
| CHEMBL577957 | — | — | 1 | 7.03 |
| CHEMBL577320 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL236593 | TELCAGEPANT | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL570746 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL571203 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL570531 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL570748 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL577110 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL570793 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL572114 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL571459 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL577957 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL577320 | — | IC50 | = | 120.0 | nM | 6.92 |