Assay Detail
Binding
CHEMBL911961
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Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cells
20
Total Activities
20
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 | Expert |
Target
Calcitonin gene-related peptide type 1 receptor (CHEMBL3798) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.37 | 8.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL374064 | — | — | 1 | 8.17 |
| CHEMBL375533 | — | — | 1 | 8.06 |
| CHEMBL220146 | — | — | 1 | 8.02 |
| CHEMBL374251 | — | — | 1 | 8.00 |
| CHEMBL223756 | — | — | 1 | 7.92 |
| CHEMBL220715 | — | — | 1 | 7.82 |
| CHEMBL375224 | — | — | 1 | 7.77 |
| CHEMBL220101 | — | — | 1 | 7.70 |
| CHEMBL223156 | — | — | 1 | 7.68 |
| CHEMBL376292 | — | — | 1 | 7.60 |
| CHEMBL374666 | — | — | 1 | 7.54 |
| CHEMBL221009 | — | — | 1 | 7.37 |
| CHEMBL219782 | — | — | 1 | 7.32 |
| CHEMBL385322 | — | — | 1 | 7.11 |
| CHEMBL219721 | — | — | 1 | 7.06 |
| CHEMBL221160 | — | — | 1 | 6.99 |
| CHEMBL223805 | — | — | 1 | 6.55 |
| CHEMBL220336 | — | — | 1 | 6.51 |
| CHEMBL376263 | — | — | 1 | 6.22 |
| CHEMBL222198 | — | — | 1 | 5.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL374064 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL375533 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL220146 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL374251 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL223756 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL220715 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL375224 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL220101 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL223156 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL376292 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL374666 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL221009 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL219782 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL385322 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL219721 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL221160 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL223805 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL220336 | — | Ki | = | 309.0 | nM | 6.51 |
| CHEMBL376263 | — | Ki | = | 607.0 | nM | 6.22 |
| CHEMBL222198 | — | Ki | = | 1050.0 | nM | 5.98 |