Assay Detail
Functional
CHEMBL1060869
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.83 | 9.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL512773 | — | — | 1 | 9.21 |
| CHEMBL562069 | — | — | 1 | 8.70 |
| CHEMBL564487 | ISOMER A | — | 1 | 8.19 |
| CHEMBL564088 | EPIMER A | — | 2 | 8.09 |
| CHEMBL236593 | TELCAGEPANT | 3.0 | 1 | 7.96 |
| CHEMBL1162991 | — | — | 1 | 7.89 |
| CHEMBL549503 | ISOMER A | — | 1 | 7.64 |
| CHEMBL564466 | — | — | 1 | 7.43 |
| CHEMBL563727 | — | — | 1 | 7.17 |
| CHEMBL556703 | — | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL512773 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL562069 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL564487 | ISOMER A | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL564088 | EPIMER A | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL236593 | TELCAGEPANT | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1162991 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL549503 | ISOMER A | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL564088 | EPIMER A | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL564466 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL563727 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL556703 | — | IC50 | = | 530.0 | nM | 6.28 |