Assay Detail
Binding
CHEMBL1000504
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [I125]CGRP from human CGRP receptor in SK-N-MC cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-N-MC |
| 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
Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and efficient intranasal exposure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 10.19 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL454791 | — | — | 1 | 11.00 |
| CHEMBL450668 | — | — | 1 | 10.89 |
| CHEMBL454751 | — | — | 1 | 9.59 |
| CHEMBL466555 | — | — | 1 | 9.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL454791 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL450668 | — | Ki | = | 0.0128 | nM | 10.89 |
| CHEMBL454751 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL466555 | — | Ki | = | 0.55 | nM | 9.26 |