Assay Detail
Binding
CHEMBL886902
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Displacement of [125I]MCH from MCHR1 expressed in IMR32 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | IMR-32 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Melanin-concentrating hormone receptor 1 (CHEMBL344) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.62 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL246258 | — | — | 1 | 8.70 |
| CHEMBL214021 | — | — | 1 | 8.52 |
| CHEMBL248297 | — | — | 1 | 8.52 |
| CHEMBL245844 | — | — | 1 | 8.40 |
| CHEMBL394639 | — | — | 1 | 7.82 |
| CHEMBL246050 | — | — | 1 | 7.77 |
| CHEMBL248296 | — | — | 1 | 7.70 |
| CHEMBL246464 | — | — | 1 | 7.64 |
| CHEMBL214768 | — | — | 1 | 7.62 |
| CHEMBL246259 | — | — | 1 | 7.58 |
| CHEMBL245846 | — | — | 1 | 7.54 |
| CHEMBL245642 | — | — | 1 | 7.51 |
| CHEMBL247891 | — | — | 1 | 7.29 |
| CHEMBL247689 | — | — | 1 | 7.19 |
| CHEMBL246051 | — | — | 1 | 7.07 |
| CHEMBL247688 | — | — | 1 | 6.78 |
| CHEMBL248295 | — | — | 1 | 5.82 |
| CHEMBL247690 | — | — | 1 | - |
| CHEMBL247283 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL246258 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL214021 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL248297 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL245844 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL394639 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL246050 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL248296 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL246464 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL214768 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL246259 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL245846 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL245642 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL247891 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL247689 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL246051 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL247688 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL248295 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL247690 | — | IC50 | - | — | - | |
| CHEMBL247283 | — | IC50 | > | 2000.0 | nM | - |