Assay Detail
Binding
CHEMBL1958783
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Growth hormone secretagogue receptor type 1 (CHEMBL4616) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substituted azaquinazolinones as modulators of GHSr-1a for the treatment of type II diabetes and obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 9.20 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1956994 | — | — | 1 | 11.00 |
| CHEMBL1956993 | — | — | 1 | 11.00 |
| CHEMBL1957010 | — | — | 1 | 10.30 |
| CHEMBL1957001 | — | — | 1 | 10.00 |
| CHEMBL1956990 | — | — | 1 | 9.80 |
| CHEMBL1956991 | — | — | 1 | 9.70 |
| CHEMBL1956999 | — | — | 1 | 9.70 |
| CHEMBL1957007 | — | — | 1 | 9.59 |
| CHEMBL1957009 | — | — | 1 | 9.57 |
| CHEMBL1957000 | — | — | 1 | 9.52 |
| CHEMBL1956997 | — | — | 1 | 9.40 |
| CHEMBL1957003 | — | — | 1 | 9.30 |
| CHEMBL1957005 | — | — | 1 | 9.22 |
| CHEMBL1956992 | — | — | 1 | 9.05 |
| CHEMBL1957006 | — | — | 1 | 8.82 |
| CHEMBL1956987 | — | — | 1 | 8.77 |
| CHEMBL1957008 | — | — | 1 | 8.72 |
| CHEMBL1956988 | — | — | 1 | 8.70 |
| CHEMBL1956996 | — | — | 1 | 8.59 |
| CHEMBL1956995 | — | — | 1 | 8.51 |
| CHEMBL1957004 | — | — | 1 | 8.51 |
| CHEMBL1956998 | — | — | 1 | 8.47 |
| CHEMBL243001 | — | — | 1 | 8.40 |
| CHEMBL1957011 | — | — | 1 | 8.30 |
| CHEMBL1957002 | — | — | 1 | 8.18 |
| CHEMBL1956989 | — | — | 1 | 8.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1956994 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL1956993 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL1957010 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL1957001 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL1956990 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL1956991 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL1956999 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL1957007 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL1957009 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL1957000 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL1956997 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL1957003 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL1957005 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1956992 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL1957006 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1956987 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL1957008 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL1956988 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1956996 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL1956995 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL1957004 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL1956998 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL243001 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL1957011 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1957002 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL1956989 | — | Ki | = | 6.7 | nM | 8.17 |