Assay Detail
Functional
CHEMBL1004155
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human cloned CGRP receptor expressed in mouse E10 cells assessed as inhibition of CGRP-induced cAMP production
13
Total Activities
13
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 | Autocuration |
Target
Calcitonin gene-related peptide type 1 receptor (CHEMBL3798) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 10.29 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL452966 | — | — | 1 | 11.00 |
| CHEMBL508453 | — | — | 1 | 10.96 |
| CHEMBL508215 | — | — | 1 | 10.77 |
| CHEMBL447297 | — | — | 1 | 10.70 |
| CHEMBL451164 | — | — | 1 | 10.66 |
| CHEMBL501603 | — | — | 1 | 10.36 |
| CHEMBL499488 | — | — | 1 | 10.28 |
| CHEMBL452686 | — | — | 1 | 10.24 |
| CHEMBL508349 | — | — | 1 | 10.20 |
| CHEMBL502243 | — | — | 1 | 10.17 |
| CHEMBL507893 | — | — | 1 | 9.89 |
| CHEMBL499810 | — | — | 1 | 9.74 |
| CHEMBL500384 | — | — | 1 | 8.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL452966 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL508453 | — | IC50 | = | 0.011 | nM | 10.96 |
| CHEMBL508215 | — | IC50 | = | 0.017 | nM | 10.77 |
| CHEMBL447297 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL451164 | — | IC50 | = | 0.022 | nM | 10.66 |
| CHEMBL501603 | — | IC50 | = | 0.044 | nM | 10.36 |
| CHEMBL499488 | — | IC50 | = | 0.053 | nM | 10.28 |
| CHEMBL452686 | — | IC50 | = | 0.057 | nM | 10.24 |
| CHEMBL508349 | — | IC50 | = | 0.063 | nM | 10.20 |
| CHEMBL502243 | — | IC50 | = | 0.068 | nM | 10.17 |
| CHEMBL507893 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL499810 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL500384 | — | IC50 | = | 1.8 | nM | 8.74 |