Assay Detail
Binding
CHEMBL1772121
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-CGRP from human recombinant CGRP receptor
30
Total Activities
30
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
Orally bioavailable imidazoazepanes as calcitonin gene-related peptide (CGRP) receptor antagonists: discovery of MK-2918.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 9.32 | 10.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1770729 | — | — | 1 | 10.44 |
| CHEMBL1770728 | — | — | 1 | 10.41 |
| CHEMBL1770715 | — | — | 1 | 10.40 |
| CHEMBL1770726 | — | — | 1 | 10.30 |
| CHEMBL1770724 | — | — | 1 | 10.30 |
| CHEMBL1770720 | — | — | 1 | 10.15 |
| CHEMBL1770557 | — | — | 1 | 9.85 |
| CHEMBL1770723 | — | — | 1 | 9.85 |
| CHEMBL1770727 | — | — | 1 | 9.80 |
| CHEMBL1770722 | — | — | 1 | 9.72 |
| CHEMBL1770725 | — | — | 1 | 9.54 |
| CHEMBL1770714 | — | — | 1 | 9.42 |
| CHEMBL1770719 | — | — | 1 | 9.40 |
| CHEMBL1770721 | — | — | 1 | 9.32 |
| CHEMBL1770718 | — | — | 1 | 9.21 |
| CHEMBL1770716 | — | — | 1 | 9.21 |
| CHEMBL1770717 | — | — | 1 | 9.20 |
| CHEMBL1770568 | — | — | 1 | 9.16 |
| CHEMBL236593 | TELCAGEPANT | 3.0 | 1 | 9.10 |
| CHEMBL1770556 | — | — | 1 | 9.00 |
| CHEMBL1770567 | — | — | 1 | 8.96 |
| CHEMBL1770566 | — | — | 1 | 8.96 |
| CHEMBL1770562 | — | — | 1 | 8.66 |
| CHEMBL1770563 | — | — | 1 | 8.60 |
| CHEMBL1770565 | — | — | 1 | 8.55 |
| CHEMBL1770558 | — | — | 1 | 8.51 |
| CHEMBL1770560 | — | — | 1 | 8.49 |
| CHEMBL1770559 | — | — | 1 | 8.41 |
| CHEMBL1770561 | — | — | 1 | 8.40 |
| CHEMBL1770564 | — | — | 1 | 8.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1770729 | — | Ki | = | 0.036 | nM | 10.44 |
| CHEMBL1770728 | — | Ki | = | 0.039 | nM | 10.41 |
| CHEMBL1770715 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL1770726 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL1770724 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL1770720 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL1770557 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL1770723 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL1770727 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL1770722 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL1770725 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL1770714 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL1770719 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL1770721 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL1770718 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL1770716 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL1770717 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL1770568 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL236593 | TELCAGEPANT | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL1770556 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1770567 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1770566 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1770562 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL1770563 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL1770565 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL1770558 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL1770560 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL1770559 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL1770561 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL1770564 | — | Ki | = | 5.7 | nM | 8.24 |