Assay Detail
Binding
CHEMBL866916
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]CGRP from human cloned CLR/RAMP1 receptor expressed in E10 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | E10 |
| 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
Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 6.16 | 7.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL424864 | — | — | 1 | 7.36 |
| CHEMBL381710 | — | — | 1 | 7.21 |
| CHEMBL381585 | — | — | 1 | 7.08 |
| CHEMBL211052 | — | — | 1 | 6.05 |
| CHEMBL380514 | — | — | 1 | 5.97 |
| CHEMBL207186 | — | — | 1 | 5.66 |
| CHEMBL381798 | — | — | 1 | 5.62 |
| CHEMBL208148 | — | — | 1 | 5.37 |
| CHEMBL379686 | — | — | 1 | 5.08 |
| CHEMBL207197 | OLCEGEPANT | 2.0 | 1 | - |
| CHEMBL206149 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL424864 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL381710 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL381585 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL211052 | — | Ki | = | 897.0 | nM | 6.05 |
| CHEMBL380514 | — | Ki | = | 1060.0 | nM | 5.97 |
| CHEMBL207186 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL381798 | — | Ki | = | 2370.0 | nM | 5.62 |
| CHEMBL208148 | — | Ki | = | 4250.0 | nM | 5.37 |
| CHEMBL379686 | — | Ki | = | 8400.0 | nM | 5.08 |
| CHEMBL207197 | OLCEGEPANT | Ki | = | 0.005 | nM | - |
| CHEMBL206149 | — | Ki | > | 13000.0 | nM | - |