Assay Detail
Functional
CHEMBL1958784
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Antagonist activity at mouse GSH-R1a receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced calcium mobilization after 5 mins by FLIPR assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 |
|---|---|---|---|
| IC50 | 28 | 7.30 | 8.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1957010 | — | — | 1 | 8.93 |
| CHEMBL1956991 | — | — | 1 | 8.70 |
| CHEMBL1956994 | — | — | 1 | 8.64 |
| CHEMBL1956993 | — | — | 1 | 8.57 |
| CHEMBL253126 | — | — | 1 | 8.25 |
| CHEMBL1957007 | — | — | 1 | 8.24 |
| CHEMBL1957006 | — | — | 1 | 7.78 |
| CHEMBL1956992 | — | — | 1 | 7.72 |
| CHEMBL1956990 | — | — | 1 | 7.58 |
| CHEMBL1957001 | — | — | 1 | 7.54 |
| CHEMBL1956997 | — | — | 1 | 7.42 |
| CHEMBL1957011 | — | — | 1 | 7.29 |
| CHEMBL1957009 | — | — | 1 | 7.10 |
| CHEMBL1957000 | — | — | 1 | 7.06 |
| CHEMBL1957005 | — | — | 1 | 6.99 |
| CHEMBL1956995 | — | — | 1 | 6.93 |
| CHEMBL1956996 | — | — | 1 | 6.88 |
| CHEMBL1956987 | — | — | 1 | 6.88 |
| CHEMBL1957003 | — | — | 1 | 6.86 |
| CHEMBL1957008 | — | — | 1 | 6.85 |
| CHEMBL243001 | — | — | 1 | 6.85 |
| CHEMBL1956999 | — | — | 1 | 6.84 |
| CHEMBL1956988 | — | — | 1 | 6.73 |
| CHEMBL211265 | — | — | 1 | 6.73 |
| CHEMBL1956989 | — | — | 1 | 6.45 |
| CHEMBL1956998 | — | — | 1 | 6.40 |
| CHEMBL1957004 | — | — | 1 | 6.23 |
| CHEMBL1957002 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1957010 | — | IC50 | = | 1.17 | nM | 8.93 |
| CHEMBL1956991 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1956994 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL1956993 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL253126 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL1957007 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL1957006 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL1956992 | — | IC50 | = | 19.2 | nM | 7.72 |
| CHEMBL1956990 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1957001 | — | IC50 | = | 29.2 | nM | 7.54 |
| CHEMBL1956997 | — | IC50 | = | 37.7 | nM | 7.42 |
| CHEMBL1957011 | — | IC50 | = | 51.8 | nM | 7.29 |
| CHEMBL1957009 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1957000 | — | IC50 | = | 86.5 | nM | 7.06 |
| CHEMBL1957005 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL1956995 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL1956996 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL1956987 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL1957003 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL1957008 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL243001 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL1956999 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL1956988 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL211265 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL1956989 | — | IC50 | = | 357.0 | nM | 6.45 |
| CHEMBL1956998 | — | IC50 | = | 399.0 | nM | 6.40 |
| CHEMBL1957004 | — | IC50 | = | 587.0 | nM | 6.23 |
| CHEMBL1957002 | — | IC50 | = | 1440.0 | nM | 5.84 |