Assay Detail
Binding
CHEMBL2040005
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Displacement of [125I]CGRP from human recombinant CALCRL/RAMP1 receptor expressed in HEK293 cells after 3 hrs
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 (CHEMBL2107838) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 10.46 | 10.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2035984 | — | — | 1 | 10.85 |
| CHEMBL2035985 | — | — | 1 | 10.80 |
| CHEMBL1910936 | MK3207 | 2.0 | 1 | 10.66 |
| CHEMBL2035982 | — | — | 1 | 10.55 |
| CHEMBL2035981 | — | — | 1 | 10.40 |
| CHEMBL2035983 | — | — | 1 | 10.33 |
| CHEMBL2035986 | — | — | 1 | 9.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2035984 | — | Ki | = | 0.014 | nM | 10.85 |
| CHEMBL2035985 | — | Ki | = | 0.016 | nM | 10.80 |
| CHEMBL1910936 | MK3207 | Ki | = | 0.022 | nM | 10.66 |
| CHEMBL2035982 | — | Ki | = | 0.028 | nM | 10.55 |
| CHEMBL2035981 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL2035983 | — | Ki | = | 0.047 | nM | 10.33 |
| CHEMBL2035986 | — | Ki | = | 0.25 | nM | 9.60 |