Assay Detail
Functional
CHEMBL1037057
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
31
Total Activities
31
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Melanin-concentrating hormone receptor 1 (CHEMBL344) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.79 | 9.30 |
| Kd | 1 | 9.24 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214957 | — | — | 1 | 9.30 |
| CHEMBL185271 | SNAP-7941 | — | 1 | 9.24 |
| CHEMBL578049 | — | — | 1 | 8.70 |
| CHEMBL568208 | — | — | 1 | 8.64 |
| CHEMBL578166 | — | — | 1 | 8.60 |
| CHEMBL567993 | — | — | 1 | 8.54 |
| CHEMBL569204 | — | — | 1 | 8.40 |
| CHEMBL568400 | — | — | 1 | 8.32 |
| CHEMBL566075 | — | — | 1 | 8.30 |
| CHEMBL178707 | — | — | 1 | 8.26 |
| CHEMBL565551 | — | — | 1 | 8.22 |
| CHEMBL568663 | — | — | 1 | 8.19 |
| CHEMBL182150 | — | — | 1 | 8.14 |
| CHEMBL567950 | — | — | 1 | 8.12 |
| CHEMBL583014 | — | — | 1 | 8.10 |
| CHEMBL568162 | — | — | 1 | 8.02 |
| CHEMBL577912 | — | — | 1 | 8.00 |
| CHEMBL578170 | — | — | 1 | 7.89 |
| CHEMBL567791 | — | — | 1 | 7.80 |
| CHEMBL568664 | — | — | 1 | 7.60 |
| CHEMBL577913 | — | — | 1 | 7.58 |
| CHEMBL568649 | — | — | 1 | 7.34 |
| CHEMBL568209 | — | — | 1 | 7.24 |
| CHEMBL568604 | — | — | 1 | 7.19 |
| CHEMBL576665 | — | — | 1 | 7.09 |
| CHEMBL577714 | — | — | 1 | 7.00 |
| CHEMBL577904 | — | — | 1 | 6.92 |
| CHEMBL577259 | — | — | 1 | 6.70 |
| CHEMBL568458 | — | — | 1 | 6.68 |
| CHEMBL578784 | — | — | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214957 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL185271 | SNAP-7941 | Kd | = | 0.5754 | nM | 9.24 |
| CHEMBL578049 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL568208 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL578166 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL567993 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL569204 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL568400 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL566075 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL178707 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL565551 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL568663 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL182150 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL567950 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL583014 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL568162 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL577912 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL578170 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL567791 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL568664 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL577913 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL568649 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL568209 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL568604 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL576665 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL577714 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL577904 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL577259 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL568458 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL578784 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL568183 | — | IC50 | = | 600.0 | nM | 6.22 |