Assay Detail
Functional
CHEMBL899872
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | E10 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Calcitonin gene-related peptide type 1 receptor (CHEMBL3798) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.53 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL392636 | — | — | 1 | 8.70 |
| CHEMBL237662 | — | — | 1 | 8.52 |
| CHEMBL392634 | — | — | 1 | 8.52 |
| CHEMBL392730 | — | — | 1 | 8.30 |
| CHEMBL238276 | — | — | 1 | 8.22 |
| CHEMBL438120 | — | — | 1 | 8.10 |
| CHEMBL415263 | — | — | 1 | 8.10 |
| CHEMBL392937 | — | — | 1 | 8.00 |
| CHEMBL392635 | — | — | 1 | 8.00 |
| CHEMBL236593 | TELCAGEPANT | 3.0 | 1 | 7.96 |
| CHEMBL237849 | — | — | 1 | 7.82 |
| CHEMBL237663 | — | — | 1 | 7.68 |
| CHEMBL237664 | — | — | 1 | 7.66 |
| CHEMBL237661 | — | — | 1 | 7.66 |
| CHEMBL236590 | — | — | 1 | 7.64 |
| CHEMBL237848 | — | — | 1 | 7.52 |
| CHEMBL239630 | — | — | 1 | 6.92 |
| CHEMBL391660 | — | — | 1 | 6.60 |
| CHEMBL241118 | — | — | 1 | 6.60 |
| CHEMBL398575 | — | — | 1 | 6.47 |
| CHEMBL240904 | — | — | 1 | 6.21 |
| CHEMBL429803 | — | — | 1 | 6.16 |
| CHEMBL240686 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL392636 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL237662 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL392634 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL392730 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL238276 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL438120 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL415263 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL392937 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL392635 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL236593 | TELCAGEPANT | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL237849 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL237663 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL237664 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL237661 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL236590 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL237848 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL239630 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL391660 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL241118 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL398575 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL240904 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL429803 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL240686 | — | IC50 | = | 1800.0 | nM | 5.75 |