Assay Detail
Functional
CHEMBL2433982
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CGRP receptor expressed in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SK-N-MC |
| 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
Preparation of imidazoles as potent calcitonin gene-related peptide (CGRP) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 9.01 | 10.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL450668 | — | — | 1 | 10.59 |
| CHEMBL2430167 | — | — | 1 | 10.11 |
| CHEMBL2430169 | — | — | 1 | 9.89 |
| CHEMBL2430177 | — | — | 1 | 9.72 |
| CHEMBL2430166 | — | — | 1 | 9.66 |
| CHEMBL2430165 | — | — | 1 | 9.59 |
| CHEMBL2430174 | — | — | 1 | 9.43 |
| CHEMBL2430178 | — | — | 1 | 9.41 |
| CHEMBL2430176 | — | — | 1 | 9.41 |
| CHEMBL2430170 | — | — | 1 | 9.38 |
| CHEMBL2430179 | — | — | 1 | 9.20 |
| CHEMBL2430185 | — | — | 1 | 9.11 |
| CHEMBL2430168 | — | — | 1 | 9.08 |
| CHEMBL2430182 | — | — | 1 | 9.06 |
| CHEMBL2430180 | — | — | 1 | 9.01 |
| CHEMBL2430171 | — | — | 1 | 8.80 |
| CHEMBL2430164 | — | — | 1 | 8.77 |
| CHEMBL2430181 | — | — | 1 | 8.72 |
| CHEMBL2430163 | — | — | 1 | 8.54 |
| CHEMBL2430184 | — | — | 1 | 8.32 |
| CHEMBL2430172 | — | — | 1 | 8.32 |
| CHEMBL2430173 | — | — | 1 | 8.13 |
| CHEMBL2430183 | — | — | 1 | 7.01 |
| CHEMBL2430175 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL450668 | — | IC50 | = | 0.026 | nM | 10.59 |
| CHEMBL2430167 | — | IC50 | = | 0.078 | nM | 10.11 |
| CHEMBL2430169 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL2430177 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL2430166 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL2430165 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL2430174 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL2430178 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL2430176 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL2430170 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL2430179 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL2430185 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL2430168 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL2430182 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL2430180 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL2430171 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2430164 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2430181 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL2430163 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL2430184 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL2430172 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL2430173 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL2430183 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL2430175 | — | IC50 | = | 120.0 | nM | 6.92 |