Assay Detail
Binding
CHEMBL832373
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Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Melanin-concentrating hormone receptor 1 (CHEMBL344) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.27 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL360081 | — | — | 1 | 8.70 |
| CHEMBL182150 | — | — | 1 | 8.47 |
| CHEMBL179878 | — | — | 1 | 8.35 |
| CHEMBL180962 | — | — | 1 | 8.34 |
| CHEMBL181466 | — | — | 1 | 8.31 |
| CHEMBL362400 | — | — | 1 | 8.30 |
| CHEMBL359510 | — | — | 1 | 8.23 |
| CHEMBL181383 | — | — | 1 | 8.17 |
| CHEMBL361442 | — | — | 1 | 8.03 |
| CHEMBL362193 | — | — | 1 | 8.02 |
| CHEMBL181099 | — | — | 1 | 8.00 |
| CHEMBL181632 | — | — | 1 | 7.82 |
| CHEMBL178084 | — | — | 1 | 7.46 |
| CHEMBL360159 | — | — | 1 | 7.42 |
| CHEMBL181393 | — | — | 1 | 7.10 |
| CHEMBL180003 | — | — | 1 | 7.08 |
| CHEMBL181217 | — | — | 1 | 6.85 |
| CHEMBL537846 | — | — | 1 | 6.80 |
| CHEMBL181184 | — | — | 1 | 6.80 |
| CHEMBL367359 | — | — | 1 | 6.77 |
| CHEMBL360671 | — | — | 1 | 6.60 |
| CHEMBL360876 | — | — | 1 | 6.50 |
| CHEMBL360117 | — | — | 1 | 6.02 |
| CHEMBL181251 | — | — | 1 | 5.92 |
| CHEMBL367355 | — | — | 1 | 5.82 |
| CHEMBL182235 | — | — | 1 | 5.25 |
| CHEMBL181727 | — | — | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL360081 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL182150 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL179878 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL180962 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL181466 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL362400 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL359510 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL181383 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL361442 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL362193 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL181099 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL181632 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL178084 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL360159 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL181393 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL180003 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL181217 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL537846 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL181184 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL367359 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL360671 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL360876 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL360117 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL181251 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL367355 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL182235 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL181727 | — | IC50 | = | 5800.0 | nM | 5.24 |