Assay Detail
Binding
CHEMBL884694
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity against calcitonin gene related peptide receptor (1 uM) in marmoset tissue homogenates using [125I]CGRP as radioligand after 180 minutes of incubation at pH 7.40
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Callithrix |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Calcitonin gene-related peptide type 1 receptor (CHEMBL3798) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of human calcitonin gene-related peptide (CGRP) receptor antagonists. 1. Potent and selective small molecule CGRP antagonists. 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-l-lysyl]-4-(4-pyridinyl)piperazine: the first CGRP antagonist for clinical trials in acute migraine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 9.40 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL197529 | — | — | 1 | 10.22 |
| CHEMBL382469 | — | — | 1 | 8.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL197529 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL382469 | — | IC50 | = | 2.7 | nM | 8.57 |