Assay Detail
Binding
CHEMBL4409780
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
15
Total Activities
15
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 | Autocuration |
Target
Glucose-dependent insulinotropic receptor (CHEMBL5652) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
One-pot synthesis of novel tert-butyl-4-substituted phenyl-1H-1,2,3-triazolo piperazine/piperidine carboxylates, potential GPR119 agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 8.12 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4439483 | — | — | 1 | 8.51 |
| CHEMBL4578862 | — | — | 1 | 8.45 |
| CHEMBL4475130 | — | — | 1 | 8.44 |
| CHEMBL4435207 | — | — | 1 | 8.38 |
| CHEMBL461384 | — | — | 1 | 8.32 |
| CHEMBL4457078 | — | — | 1 | 8.15 |
| CHEMBL4521163 | — | — | 1 | 8.09 |
| CHEMBL4445174 | — | — | 1 | 8.06 |
| CHEMBL4591642 | — | — | 1 | 7.98 |
| CHEMBL4473081 | — | — | 1 | 7.95 |
| CHEMBL4456666 | — | — | 1 | 7.91 |
| CHEMBL4461803 | — | — | 1 | 7.91 |
| CHEMBL4461083 | — | — | 1 | 7.91 |
| CHEMBL4464713 | — | — | 1 | 7.87 |
| CHEMBL4454792 | — | — | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4439483 | — | EC50 | = | 3.12 | nM | 8.51 |
| CHEMBL4578862 | — | EC50 | = | 3.59 | nM | 8.45 |
| CHEMBL4475130 | — | EC50 | = | 3.67 | nM | 8.44 |
| CHEMBL4435207 | — | EC50 | = | 4.21 | nM | 8.38 |
| CHEMBL461384 | — | EC50 | = | 4.78 | nM | 8.32 |
| CHEMBL4457078 | — | EC50 | = | 7.12 | nM | 8.15 |
| CHEMBL4521163 | — | EC50 | = | 8.17 | nM | 8.09 |
| CHEMBL4445174 | — | EC50 | = | 8.78 | nM | 8.06 |
| CHEMBL4591642 | — | EC50 | = | 10.43 | nM | 7.98 |
| CHEMBL4473081 | — | EC50 | = | 11.12 | nM | 7.95 |
| CHEMBL4456666 | — | EC50 | = | 12.34 | nM | 7.91 |
| CHEMBL4461803 | — | EC50 | = | 12.43 | nM | 7.91 |
| CHEMBL4461083 | — | EC50 | = | 12.31 | nM | 7.91 |
| CHEMBL4464713 | — | EC50 | = | 13.56 | nM | 7.87 |
| CHEMBL4454792 | — | EC50 | = | 13.98 | nM | 7.85 |