Assay Detail
Functional
CHEMBL4220183
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Agonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gastric inhibitory polypeptide receptor (CHEMBL4383) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of peptide-based polyagonists for treatment of diabetes and obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 8.70 | 9.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4226634 | — | — | 1 | 9.88 |
| CHEMBL4227180 | — | — | 1 | 9.09 |
| CHEMBL4225594 | — | — | 1 | 9.06 |
| CHEMBL4224968 | — | — | 1 | 8.96 |
| CHEMBL4225795 | — | — | 1 | 8.78 |
| CHEMBL4226185 | — | — | 1 | 8.78 |
| CHEMBL4224701 | — | — | 1 | 8.69 |
| CHEMBL4226514 | — | — | 1 | 8.66 |
| CHEMBL4225340 | — | — | 1 | 8.57 |
| CHEMBL4229251 | — | — | 1 | 8.45 |
| CHEMBL4227861 | — | — | 1 | 8.26 |
| CHEMBL4226451 | — | — | 1 | 8.23 |
| CHEMBL4226613 | — | — | 1 | 8.20 |
| CHEMBL4227045 | — | — | 1 | 8.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4226634 | — | EC50 | = | 0.133 | nM | 9.88 |
| CHEMBL4227180 | — | EC50 | = | 0.812 | nM | 9.09 |
| CHEMBL4225594 | — | EC50 | = | 0.867 | nM | 9.06 |
| CHEMBL4224968 | — | EC50 | = | 1.103 | nM | 8.96 |
| CHEMBL4225795 | — | EC50 | = | 1.654 | nM | 8.78 |
| CHEMBL4226185 | — | EC50 | = | 1.646 | nM | 8.78 |
| CHEMBL4224701 | — | EC50 | = | 2.032 | nM | 8.69 |
| CHEMBL4226514 | — | EC50 | = | 2.194 | nM | 8.66 |
| CHEMBL4225340 | — | EC50 | = | 2.691 | nM | 8.57 |
| CHEMBL4229251 | — | EC50 | = | 3.545 | nM | 8.45 |
| CHEMBL4227861 | — | EC50 | = | 5.53 | nM | 8.26 |
| CHEMBL4226451 | — | EC50 | = | 5.828 | nM | 8.23 |
| CHEMBL4226613 | — | EC50 | = | 6.258 | nM | 8.20 |
| CHEMBL4227045 | — | EC50 | = | 6.26 | nM | 8.20 |