Assay Detail
Functional
CHEMBL866622
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
40
Total Activities
37
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Melanin-concentrating hormone receptor 1 (CHEMBL344) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 7.54 | 8.77 |
| Kb | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL212256 | — | — | 1 | 8.77 |
| CHEMBL364871 | — | — | 2 | 8.60 |
| CHEMBL209109 | — | — | 2 | 8.46 |
| CHEMBL209993 | — | — | 1 | 8.44 |
| CHEMBL211672 | — | — | 1 | 8.41 |
| CHEMBL377843 | — | — | 1 | 8.32 |
| CHEMBL209103 | — | — | 1 | 8.14 |
| CHEMBL268938 | — | — | 1 | 8.00 |
| CHEMBL377372 | — | — | 1 | 7.99 |
| CHEMBL429895 | — | — | 1 | 7.99 |
| CHEMBL211820 | — | — | 2 | 7.82 |
| CHEMBL209754 | — | — | 1 | 7.82 |
| CHEMBL211069 | — | — | 1 | 7.81 |
| CHEMBL377864 | — | — | 1 | 7.70 |
| CHEMBL211615 | — | — | 1 | 7.66 |
| CHEMBL378310 | — | — | 1 | 7.58 |
| CHEMBL208573 | — | — | 1 | 7.51 |
| CHEMBL211511 | — | — | 1 | 7.51 |
| CHEMBL208931 | — | — | 1 | 7.50 |
| CHEMBL208827 | — | — | 1 | 7.43 |
| CHEMBL209123 | — | — | 1 | 7.39 |
| CHEMBL208635 | — | — | 1 | 7.36 |
| CHEMBL211492 | — | — | 1 | 7.35 |
| CHEMBL211956 | — | — | 1 | 7.28 |
| CHEMBL212573 | — | — | 1 | 7.19 |
| CHEMBL208688 | — | — | 1 | 7.17 |
| CHEMBL378242 | — | — | 1 | 7.15 |
| CHEMBL377270 | — | — | 1 | 7.11 |
| CHEMBL424697 | — | — | 1 | 7.06 |
| CHEMBL379802 | — | — | 1 | 7.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL212256 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL364871 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL209109 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL209993 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL211672 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL377843 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL209103 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL268938 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL377372 | — | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL429895 | — | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL209754 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL211820 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL211069 | — | Ki | = | 15.5 | nM | 7.81 |
| CHEMBL377864 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL211615 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL378310 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL211511 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL208573 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL208931 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL208827 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL209123 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL208635 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL211492 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL211956 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL212573 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL208688 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL378242 | — | Ki | = | 71.4 | nM | 7.15 |
| CHEMBL377270 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL424697 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL379802 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL209590 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL379521 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL378261 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL212254 | — | Ki | = | 133.0 | nM | 6.88 |
| CHEMBL211232 | — | Ki | = | 174.0 | nM | 6.76 |
| CHEMBL379060 | — | Ki | = | 221.0 | nM | 6.66 |
| CHEMBL384449 | — | Ki | = | 464.0 | nM | 6.33 |
| CHEMBL209109 | — | Kb | = | 25.0 | nM | - |
| CHEMBL211820 | — | Kb | = | 70.0 | nM | - |
| CHEMBL364871 | — | Kb | = | 3.1 | nM | - |