Assay Detail
Functional
CHEMBL5126027
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human MRGPRX2 expressed in HEK293 cells co-expressing mouse Galpha15 assessed as inhibition of Cortistatin-14 induced Ca2+ mobilization preincubated for 30 mins followed by Cortistatin-14 addition by FLIPRtetra-calcium mobilization assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Mas-related G-protein coupled receptor member X2 (CHEMBL5849) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel MRGX2 Antagonists for Treating Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.60 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5184300 | — | — | 1 | 8.60 |
| CHEMBL5182351 | — | — | 1 | - |
| CHEMBL5204738 | — | — | 1 | - |
| CHEMBL5205680 | — | — | 1 | - |
| CHEMBL5205183 | — | — | 1 | - |
| CHEMBL5191640 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5184300 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL5182351 | — | IC50 | <= | 10.0 | nM | - |
| CHEMBL5204738 | — | IC50 | <= | 10.0 | nM | - |
| CHEMBL5205680 | — | IC50 | <= | 10.0 | nM | - |
| CHEMBL5205183 | — | IC50 | <= | 10.0 | nM | - |
| CHEMBL5191640 | — | IC50 | <= | 10.0 | nM | - |