Assay Detail
Functional
CHEMBL1015394
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity at human CGRP receptor expressed in HEK293 cells coexpressing RAMP1 assessed as inhibition of CGRP-induced cAMP production
17
Total Activities
16
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
The discovery of highly potent CGRP receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 8.13 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL512773 | — | — | 1 | 9.55 |
| CHEMBL466192 | — | — | 2 | 9.06 |
| CHEMBL517467 | — | — | 1 | 9.06 |
| CHEMBL518422 | — | — | 1 | 8.80 |
| CHEMBL464078 | — | — | 1 | 8.60 |
| CHEMBL463880 | — | — | 1 | 8.28 |
| CHEMBL464079 | — | — | 1 | 8.24 |
| CHEMBL465934 | — | — | 1 | 8.07 |
| CHEMBL482178 | — | — | 1 | 8.00 |
| CHEMBL519421 | — | — | 1 | 7.92 |
| CHEMBL520778 | — | — | 1 | 7.57 |
| CHEMBL1162991 | — | — | 1 | 7.51 |
| CHEMBL408093 | — | — | 1 | 7.31 |
| CHEMBL480999 | — | — | 1 | 7.24 |
| CHEMBL220101 | — | — | 1 | 7.21 |
| CHEMBL223156 | — | — | 1 | 7.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL512773 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL466192 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL517467 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL518422 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL466192 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL464078 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL463880 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL464079 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL465934 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL482178 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL519421 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL520778 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1162991 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL408093 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL480999 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL220101 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL223156 | — | IC50 | = | 78.0 | nM | 7.11 |