Assay Detail
Binding
CHEMBL1060867
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1
11
Total Activities
10
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 | Intermediate |
Target
Calcitonin gene-related peptide type 1 receptor (CHEMBL3798) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 9.23 | 10.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL512773 | — | — | 1 | 10.41 |
| CHEMBL562069 | — | — | 1 | 9.92 |
| CHEMBL1162991 | — | — | 1 | 9.64 |
| CHEMBL564487 | ISOMER A | — | 1 | 9.55 |
| CHEMBL564088 | EPIMER A | — | 2 | 9.46 |
| CHEMBL236593 | TELCAGEPANT | 3.0 | 1 | 9.10 |
| CHEMBL549503 | ISOMER A | — | 1 | 8.96 |
| CHEMBL563727 | — | — | 1 | 8.85 |
| CHEMBL564466 | — | — | 1 | 8.66 |
| CHEMBL556703 | — | — | 1 | 8.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL512773 | — | Ki | = | 0.039 | nM | 10.41 |
| CHEMBL562069 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL1162991 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL564487 | ISOMER A | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL564088 | EPIMER A | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL236593 | TELCAGEPANT | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL549503 | ISOMER A | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL564088 | EPIMER A | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL563727 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL564466 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL556703 | — | Ki | = | 9.7 | nM | 8.01 |