Assay Detail
Functional
CHEMBL3591192
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
5
Total Activities
5
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
Melanin-concentrating hormone receptor 1 (CHEMBL344) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.75 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3589154 | — | — | 1 | 7.89 |
| CHEMBL214957 | — | — | 1 | 7.80 |
| CHEMBL3589145 | — | — | 1 | 6.62 |
| CHEMBL3589135 | — | — | 1 | 5.93 |
| CHEMBL3589138 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3589154 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL214957 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3589145 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL3589135 | — | IC50 | = | 1173.0 | nM | 5.93 |
| CHEMBL3589138 | — | IC50 | = | 3057.0 | nM | 5.51 |