Assay Detail
Functional
CHEMBL998537
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Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 6.32 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL525577 | — | — | 1 | 8.41 |
| CHEMBL450593 | — | — | 1 | 6.68 |
| CHEMBL513374 | — | — | 1 | 6.62 |
| CHEMBL501895 | — | — | 1 | 6.46 |
| CHEMBL527650 | — | — | 1 | 6.42 |
| CHEMBL469313 | — | — | 1 | 6.29 |
| CHEMBL471016 | — | — | 1 | 6.24 |
| CHEMBL488400 | — | — | 1 | 5.80 |
| CHEMBL892 | UFIPRAZOLE | 2.0 | 1 | 5.41 |
| CHEMBL1503 | OMEPRAZOLE | 4.0 | 1 | 4.85 |
| CHEMBL488600 | — | — | 1 | - |
| CHEMBL486340 | — | — | 1 | - |
| CHEMBL470373 | — | — | 1 | - |
| CHEMBL508987 | — | — | 1 | - |
| CHEMBL469314 | — | — | 1 | - |
| CHEMBL512159 | — | — | 1 | - |
| CHEMBL470807 | — | — | 1 | - |
| CHEMBL470169 | — | — | 1 | - |
| CHEMBL469758 | — | — | 1 | - |
| CHEMBL502335 | — | — | 1 | - |
| CHEMBL449415 | — | — | 1 | - |
| CHEMBL530558 | — | — | 1 | - |
| CHEMBL470806 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL525577 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL450593 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL513374 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL501895 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL527650 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL469313 | — | EC50 | = | 510.0 | nM | 6.29 |
| CHEMBL471016 | — | EC50 | = | 570.0 | nM | 6.24 |
| CHEMBL488400 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL892 | UFIPRAZOLE | EC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL1503 | OMEPRAZOLE | EC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL488600 | — | EC50 | > | 32000.0 | nM | - |
| CHEMBL486340 | — | EC50 | > | 32000.0 | nM | - |
| CHEMBL470373 | — | EC50 | > | 32000.0 | nM | - |
| CHEMBL508987 | — | EC50 | > | 32000.0 | nM | - |
| CHEMBL469314 | — | EC50 | > | 32000.0 | nM | - |
| CHEMBL512159 | — | EC50 | > | 32000.0 | nM | - |
| CHEMBL470807 | — | EC50 | > | 32000.0 | nM | - |
| CHEMBL470169 | — | EC50 | > | 32000.0 | nM | - |
| CHEMBL469758 | — | EC50 | > | 32000.0 | nM | - |
| CHEMBL502335 | — | EC50 | > | 32000.0 | nM | - |
| CHEMBL449415 | — | EC50 | > | 32000.0 | nM | - |
| CHEMBL530558 | — | EC50 | > | 32000.0 | nM | - |
| CHEMBL470806 | — | EC50 | > | 32000.0 | nM | - |