Assay Detail
Binding
CHEMBL2400791
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CGRP receptor
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migraine through intranasal delivery.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 10.42 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL207197 | OLCEGEPANT | 2.0 | 1 | 11.00 |
| CHEMBL450668 | — | — | 1 | 10.89 |
| CHEMBL1910936 | MK3207 | 2.0 | 1 | 10.68 |
| CHEMBL236593 | TELCAGEPANT | 3.0 | 1 | 9.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL207197 | OLCEGEPANT | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL450668 | — | Ki | = | 0.013 | nM | 10.89 |
| CHEMBL1910936 | MK3207 | Ki | = | 0.021 | nM | 10.68 |
| CHEMBL236593 | TELCAGEPANT | Ki | = | 0.77 | nM | 9.11 |