Assay Detail
Functional
CHEMBL1106147
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Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum
15
Total Activities
15
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
Identification of potent, highly constrained CGRP receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.69 | 9.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL512773 | — | — | 1 | 9.21 |
| CHEMBL1089433 | — | — | 1 | 8.89 |
| CHEMBL1092208 | — | — | 1 | 8.82 |
| CHEMBL1092882 | — | — | 1 | 8.60 |
| CHEMBL1092837 | — | — | 1 | 8.39 |
| CHEMBL453643 | — | — | 1 | 8.27 |
| CHEMBL1092838 | — | — | 1 | 8.19 |
| CHEMBL1090848 | — | — | 1 | 7.85 |
| CHEMBL1090841 | — | — | 1 | 7.37 |
| CHEMBL1089772 | — | — | 1 | 7.36 |
| CHEMBL1090847 | — | — | 1 | 7.09 |
| CHEMBL1090515 | — | — | 1 | 7.02 |
| CHEMBL223156 | — | — | 1 | 6.28 |
| CHEMBL1090846 | — | — | 1 | 6.07 |
| CHEMBL1092883 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL512773 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL1089433 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL1092208 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1092882 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL1092837 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL453643 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL1092838 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL1090848 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1090841 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1089772 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL1090847 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL1090515 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL223156 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL1090846 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL1092883 | — | IC50 | = | 1200.0 | nM | 5.92 |