Assay Detail
Binding
CHEMBL3591004
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [Phe13, [125I]Tyr19]-MCH from human MCHR1 E4Q/A5T double mutant expressed in HEK293 cell membranes after 90 mins by scintillation counting analysis
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 |
|---|---|---|---|
| Ki | 22 | 8.16 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3589138 | — | — | 1 | 9.38 |
| CHEMBL3589147 | — | — | 1 | 9.15 |
| CHEMBL3589149 | — | — | 1 | 9.10 |
| CHEMBL3589145 | — | — | 1 | 9.02 |
| CHEMBL214957 | — | — | 1 | 9.00 |
| CHEMBL3589146 | — | — | 1 | 8.89 |
| CHEMBL3589148 | — | — | 1 | 8.68 |
| CHEMBL3589144 | — | — | 1 | 8.64 |
| CHEMBL3589151 | — | — | 1 | 8.57 |
| CHEMBL3589150 | — | — | 1 | 8.19 |
| CHEMBL3589152 | — | — | 1 | 8.15 |
| CHEMBL3589154 | — | — | 1 | 8.10 |
| CHEMBL3589135 | — | — | 1 | 8.10 |
| CHEMBL3589136 | — | — | 1 | 8.05 |
| CHEMBL3589153 | — | — | 1 | 7.96 |
| CHEMBL3589134 | — | — | 1 | 7.89 |
| CHEMBL3589142 | — | — | 1 | 7.47 |
| CHEMBL3589141 | — | — | 1 | 7.39 |
| CHEMBL3589137 | — | — | 1 | 7.36 |
| CHEMBL3589140 | — | — | 1 | 6.97 |
| CHEMBL3589143 | — | — | 1 | 6.95 |
| CHEMBL3589139 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3589138 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL3589147 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3589149 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3589145 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL214957 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3589146 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3589148 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3589144 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL3589151 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL3589150 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL3589152 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL3589154 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL3589135 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL3589136 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3589153 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3589134 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL3589142 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL3589141 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL3589137 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL3589140 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL3589143 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL3589139 | — | Ki | = | 334.0 | nM | 6.48 |