Assay Detail
Binding
CHEMBL1106145
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1
22
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 22 | 8.34 | 10.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1092882 | — | — | 1 | 10.64 |
| CHEMBL512773 | — | — | 1 | 10.40 |
| CHEMBL1092208 | — | — | 1 | 10.14 |
| CHEMBL1089433 | — | — | 1 | 9.92 |
| CHEMBL1090848 | — | — | 1 | 9.52 |
| CHEMBL1090515 | — | — | 1 | 9.39 |
| CHEMBL453643 | — | — | 1 | 9.29 |
| CHEMBL1092838 | — | — | 1 | 9.28 |
| CHEMBL1092837 | — | — | 1 | 9.26 |
| CHEMBL1089772 | — | — | 1 | 8.89 |
| CHEMBL1090847 | — | — | 1 | 8.85 |
| CHEMBL1090841 | — | — | 1 | 8.82 |
| CHEMBL1092883 | — | — | 1 | 8.52 |
| CHEMBL1090846 | — | — | 1 | 8.05 |
| CHEMBL1091903 | — | — | 1 | 7.77 |
| CHEMBL223156 | — | — | 1 | 7.70 |
| CHEMBL1093189 | — | — | 1 | 7.26 |
| CHEMBL1089207 | — | — | 1 | 6.73 |
| CHEMBL1089497 | — | — | 2 | 6.50 |
| CHEMBL1089496 | — | — | 1 | 6.14 |
| CHEMBL1088906 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1092882 | — | Ki | = | 0.023 | nM | 10.64 |
| CHEMBL512773 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL1092208 | — | Ki | = | 0.072 | nM | 10.14 |
| CHEMBL1089433 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL1090848 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL1090515 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL453643 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL1092838 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL1092837 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL1089772 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL1090847 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL1090841 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1092883 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL1090846 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL1091903 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL223156 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1093189 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL1089207 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL1089497 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL1089496 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL1088906 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL1089497 | — | Ki | = | 6600.0 | nM | 5.18 |