Assay Detail
Functional
CHEMBL908628
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Calcitonin gene-related peptide type 1 receptor (CHEMBL3798) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: optimization of the 4-substituted piperidine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.56 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL385454 | — | — | 1 | 8.29 |
| CHEMBL215499 | — | — | 1 | 7.85 |
| CHEMBL424864 | — | — | 1 | 7.47 |
| CHEMBL383872 | — | — | 1 | 7.43 |
| CHEMBL214507 | — | — | 1 | 7.34 |
| CHEMBL408093 | — | — | 1 | 7.31 |
| CHEMBL386757 | — | — | 1 | 7.13 |
| CHEMBL215325 | — | — | 1 | 7.07 |
| CHEMBL213976 | — | — | 1 | 7.00 |
| CHEMBL384799 | — | — | 1 | 7.00 |
| CHEMBL215274 | — | — | 1 | 6.97 |
| CHEMBL384408 | — | — | 1 | 6.81 |
| CHEMBL214800 | — | — | 1 | 6.71 |
| CHEMBL405544 | — | — | 1 | 6.66 |
| CHEMBL427743 | — | — | 1 | 6.65 |
| CHEMBL211931 | — | — | 1 | 6.54 |
| CHEMBL214873 | — | — | 1 | 6.43 |
| CHEMBL384539 | — | — | 1 | 6.43 |
| CHEMBL437718 | — | — | 1 | 6.37 |
| CHEMBL379548 | — | — | 1 | 6.37 |
| CHEMBL386701 | — | — | 1 | 6.35 |
| CHEMBL386204 | — | — | 1 | 6.35 |
| CHEMBL212942 | — | — | 1 | 6.21 |
| CHEMBL377252 | — | — | 1 | 6.20 |
| CHEMBL213670 | — | — | 1 | 6.17 |
| CHEMBL405543 | — | — | 1 | 6.15 |
| CHEMBL214904 | — | — | 1 | 6.10 |
| CHEMBL214829 | — | — | 1 | 6.09 |
| CHEMBL214845 | — | — | 1 | 6.00 |
| CHEMBL386113 | — | — | 1 | 5.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL385454 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL215499 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL424864 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL383872 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL214507 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL408093 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL386757 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL215325 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL213976 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL384799 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL215274 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL384408 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL214800 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL405544 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL427743 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL211931 | — | IC50 | = | 286.0 | nM | 6.54 |
| CHEMBL214873 | — | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL384539 | — | IC50 | = | 369.0 | nM | 6.43 |
| CHEMBL437718 | — | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL379548 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL386701 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL386204 | — | IC50 | = | 446.0 | nM | 6.35 |
| CHEMBL212942 | — | IC50 | = | 616.0 | nM | 6.21 |
| CHEMBL377252 | — | IC50 | = | 627.0 | nM | 6.20 |
| CHEMBL213670 | — | IC50 | = | 672.0 | nM | 6.17 |
| CHEMBL405543 | — | IC50 | = | 715.0 | nM | 6.15 |
| CHEMBL214904 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL214829 | — | IC50 | = | 804.0 | nM | 6.09 |
| CHEMBL214845 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL386113 | — | IC50 | = | 1135.0 | nM | 5.95 |
| CHEMBL415453 | — | IC50 | = | 1381.0 | nM | 5.86 |
| CHEMBL426142 | — | IC50 | = | 1396.0 | nM | 5.86 |
| CHEMBL384723 | — | IC50 | = | 1398.0 | nM | 5.85 |
| CHEMBL381798 | — | IC50 | = | 1583.0 | nM | 5.80 |
| CHEMBL215424 | — | IC50 | = | 1837.0 | nM | 5.74 |
| CHEMBL425807 | — | IC50 | = | 3100.0 | nM | 5.51 |