Assay Detail
Binding
CHEMBL908288
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Displacement of [125I]MCH from MCHr1 expressed in IMR32 cells
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 7.29 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL277531 | — | — | 1 | 8.70 |
| CHEMBL217442 | — | — | 1 | 8.70 |
| CHEMBL387178 | — | — | 1 | 8.70 |
| CHEMBL204828 | — | — | 1 | 8.52 |
| CHEMBL387418 | — | — | 1 | 8.52 |
| CHEMBL214021 | — | — | 1 | 8.52 |
| CHEMBL217789 | — | — | 1 | 8.30 |
| CHEMBL206081 | — | — | 1 | 7.96 |
| CHEMBL216225 | — | — | 1 | 7.92 |
| CHEMBL217593 | — | — | 1 | 7.89 |
| CHEMBL217105 | — | — | 1 | 7.66 |
| CHEMBL214768 | — | — | 1 | 7.62 |
| CHEMBL386021 | — | — | 1 | 7.62 |
| CHEMBL217400 | — | — | 1 | 7.51 |
| CHEMBL217706 | — | — | 1 | 7.50 |
| CHEMBL384487 | — | — | 1 | 7.41 |
| CHEMBL387417 | — | — | 1 | 7.33 |
| CHEMBL387309 | — | — | 1 | 7.28 |
| CHEMBL217707 | — | — | 1 | 7.24 |
| CHEMBL214377 | — | — | 1 | 7.23 |
| CHEMBL213761 | — | — | 1 | 7.22 |
| CHEMBL214731 | — | — | 1 | 7.19 |
| CHEMBL213715 | — | — | 1 | 7.19 |
| CHEMBL214767 | — | — | 1 | 7.18 |
| CHEMBL425448 | — | — | 1 | 7.14 |
| CHEMBL2113245 | — | — | 1 | 7.12 |
| CHEMBL214413 | — | — | 1 | 7.04 |
| CHEMBL441542 | — | — | 1 | 7.00 |
| CHEMBL387219 | — | — | 1 | 6.88 |
| CHEMBL214278 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL277531 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL387178 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL217442 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL204828 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL387418 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL214021 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL217789 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL206081 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL216225 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL217593 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL217105 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL214768 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL386021 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL217400 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL217706 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL384487 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL387417 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL387309 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL217707 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL214377 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL213761 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL214731 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL213715 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL214767 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL425448 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2113245 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL214413 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL441542 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL387219 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL214278 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL402868 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL217925 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL216577 | — | IC50 | = | 351.0 | nM | 6.46 |
| CHEMBL213658 | — | IC50 | = | 393.0 | nM | 6.41 |
| CHEMBL214075 | — | IC50 | = | 427.0 | nM | 6.37 |
| CHEMBL216777 | — | IC50 | = | 566.0 | nM | 6.25 |
| CHEMBL216133 | — | IC50 | = | 734.0 | nM | 6.13 |
| CHEMBL384458 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL215631 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL216680 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL216456 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL214766 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL425435 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL217857 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL216190 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL214679 | — | IC50 | > | 700.0 | nM | - |