Assay Detail
Functional
CHEMBL832411
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | IMR-32 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Melanin-concentrating hormone receptor 1 (CHEMBL344) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of 2-(4-benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.55 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL179501 | — | — | 1 | 7.96 |
| CHEMBL360142 | — | — | 1 | 7.15 |
| CHEMBL178259 | — | — | 1 | 6.54 |
| CHEMBL179091 | — | — | 1 | 6.06 |
| CHEMBL2096766 | — | — | 1 | 5.83 |
| CHEMBL176081 | — | — | 1 | 5.74 |
| CHEMBL360896 | — | — | 1 | - |
| CHEMBL178989 | — | — | 1 | - |
| CHEMBL180168 | — | — | 1 | - |
| CHEMBL179606 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL179501 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL360142 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL178259 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL179091 | — | IC50 | = | 874.0 | nM | 6.06 |
| CHEMBL2096766 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL176081 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL360896 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL178989 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL180168 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL179606 | — | IC50 | > | 10000.0 | nM | - |