Assay Detail
Functional
CHEMBL5610153
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at MCHR1 (unknown origin) using MCH peptide as substrate assessed as decrease in Ca2+ influx incubated for 140 mins by FLIPR assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Melanin-concentrating hormone receptor 1 (CHEMBL344) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Exploring monocyclic core: Discovery of pyrrol-2-one derivatives as a new series of potent MCHR1 antagonists with in vivo efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.25 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5613587 | — | — | 1 | 8.15 |
| CHEMBL5614297 | — | — | 1 | 8.05 |
| CHEMBL5612007 | — | — | 1 | 7.92 |
| CHEMBL5613768 | — | — | 1 | 7.85 |
| CHEMBL5613208 | — | — | 1 | 7.82 |
| CHEMBL5612395 | — | — | 1 | 7.72 |
| CHEMBL5611933 | — | — | 1 | 7.68 |
| CHEMBL5612296 | — | — | 1 | 7.68 |
| CHEMBL5614124 | — | — | 1 | 7.66 |
| CHEMBL5613259 | — | — | 1 | 7.54 |
| CHEMBL5613243 | — | — | 1 | 7.33 |
| CHEMBL5613278 | — | — | 1 | 7.19 |
| CHEMBL5614007 | — | — | 1 | 7.16 |
| CHEMBL5613131 | — | — | 1 | 7.15 |
| CHEMBL5612188 | — | — | 1 | 6.97 |
| CHEMBL5613960 | — | — | 1 | 6.97 |
| CHEMBL5612410 | — | — | 1 | 6.78 |
| CHEMBL5612906 | — | — | 1 | 6.69 |
| CHEMBL5614058 | — | — | 1 | 6.55 |
| CHEMBL5613133 | — | — | 1 | 6.52 |
| CHEMBL5612929 | — | — | 1 | 6.42 |
| CHEMBL5611987 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5613587 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5614297 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5612007 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5613768 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5613208 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5612395 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5611933 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5612296 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5614124 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5613259 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5613243 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5613278 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5614007 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL5613131 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5612188 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL5613960 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL5612410 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL5612906 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL5614058 | — | IC50 | = | 279.0 | nM | 6.55 |
| CHEMBL5613133 | — | IC50 | = | 299.0 | nM | 6.52 |
| CHEMBL5612929 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5611987 | — | IC50 | = | 2427.0 | nM | 5.62 |