Assay Detail
Binding
CHEMBL4612974
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]telcagepant from recombinant human CLR/RAMP1 expressed in Sf21 insect cell membranes measured after 60 mins by microbeta scintillation counting method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| 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
Structure-Based Drug Discovery of <i>N</i>-((<i>R</i>)-3-(7-Methyl-1<i>H</i>-indazol-5-yl)-1-oxo-1-(((<i>S</i>)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2'-oxo-1',2'-dihydrospiro[piperidine-4,4'-pyrido[2,3-<i>d</i>][1,3]oxazine]-1-carboxamide (HTL22562): A Calcitonin Gene-Related Peptide Receptor Antagonist for Acute Treatment of Migraine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 10.34 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4638112 | — | — | 1 | 10.70 |
| CHEMBL4638938 | — | — | 1 | 10.60 |
| CHEMBL207197 | OLCEGEPANT | 2.0 | 1 | 10.50 |
| CHEMBL4635331 | HTL-0022562 | 1.0 | 1 | 10.50 |
| CHEMBL4635521 | — | — | 1 | 10.40 |
| CHEMBL4640887 | — | — | 1 | 10.20 |
| CHEMBL4642755 | — | — | 1 | 10.10 |
| CHEMBL4649523 | — | — | 1 | 10.10 |
| CHEMBL4636143 | — | — | 1 | 10.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4638112 | — | Ki | = | 0.01995 | nM | 10.70 |
| CHEMBL4638938 | — | Ki | = | 0.02512 | nM | 10.60 |
| CHEMBL207197 | OLCEGEPANT | Ki | = | 0.03162 | nM | 10.50 |
| CHEMBL4635331 | HTL-0022562 | Ki | = | 0.03162 | nM | 10.50 |
| CHEMBL4635521 | — | Ki | = | 0.03981 | nM | 10.40 |
| CHEMBL4640887 | — | Ki | = | 0.0631 | nM | 10.20 |
| CHEMBL4642755 | — | Ki | = | 0.07943 | nM | 10.10 |
| CHEMBL4649523 | — | Ki | = | 0.07943 | nM | 10.10 |
| CHEMBL4636143 | — | Ki | = | 0.1 | nM | 10.00 |