Assay Detail
Binding
CHEMBL1015393
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]hCGRP from human CGRP receptor expressed in HEK293 cells coexpressing RAMP1
28
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 28 | 7.83 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL512773 | — | — | 1 | 10.40 |
| CHEMBL517467 | — | — | 1 | 9.68 |
| CHEMBL466192 | — | — | 2 | 9.64 |
| CHEMBL518422 | — | — | 1 | 9.21 |
| CHEMBL464078 | — | — | 1 | 9.06 |
| CHEMBL463880 | — | — | 1 | 8.92 |
| CHEMBL464079 | — | — | 1 | 8.77 |
| CHEMBL519421 | — | — | 1 | 8.77 |
| CHEMBL465934 | — | — | 1 | 8.64 |
| CHEMBL473445 | — | — | 1 | 8.43 |
| CHEMBL1162991 | — | — | 1 | 8.15 |
| CHEMBL520778 | — | — | 1 | 7.89 |
| CHEMBL482178 | — | — | 1 | 7.80 |
| CHEMBL223156 | — | — | 1 | 7.70 |
| CHEMBL220101 | — | — | 1 | 7.70 |
| CHEMBL408093 | — | — | 1 | 7.66 |
| CHEMBL518236 | — | — | 1 | 7.47 |
| CHEMBL480999 | — | — | 1 | 7.46 |
| CHEMBL464263 | — | — | 1 | 7.02 |
| CHEMBL472829 | — | — | 1 | 6.89 |
| CHEMBL465279 | — | — | 1 | 6.64 |
| CHEMBL465280 | — | — | 1 | 6.57 |
| CHEMBL515087 | — | — | 1 | 6.28 |
| CHEMBL213976 | — | — | 1 | 6.28 |
| CHEMBL381798 | — | — | 1 | 5.66 |
| CHEMBL481382 | — | — | 1 | 5.58 |
| CHEMBL464264 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL512773 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL517467 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL466192 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL466192 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL518422 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL464078 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL463880 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL464079 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL519421 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL465934 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL473445 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL1162991 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL520778 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL482178 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL220101 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL223156 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL408093 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL518236 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL480999 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL464263 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL472829 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL465279 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL465280 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL515087 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL213976 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL381798 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL481382 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL464264 | — | Ki | = | 2700.0 | nM | 5.57 |