Assay Detail
Binding
CHEMBL972348
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Displacement of [125I]GLP1 from human GLP1R expressed in CHOK1 cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.96 | 9.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL414357 | EXENATIDE | 4.0 | 1 | 9.18 |
| CHEMBL525934 | — | — | 1 | 8.96 |
| CHEMBL499930 | — | — | 1 | 8.77 |
| CHEMBL499133 | — | — | 1 | 8.72 |
| CHEMBL524907 | — | — | 1 | 8.68 |
| CHEMBL527077 | — | — | 1 | 8.57 |
| CHEMBL526685 | — | — | 1 | 8.55 |
| CHEMBL499370 | — | — | 1 | 8.54 |
| CHEMBL499208 | — | — | 1 | 8.44 |
| CHEMBL507645 | — | — | 1 | 8.21 |
| CHEMBL526730 | — | — | 1 | 8.19 |
| CHEMBL500447 | — | — | 1 | 7.80 |
| CHEMBL507190 | — | — | 1 | 7.77 |
| CHEMBL524538 | — | — | 1 | 7.58 |
| CHEMBL525956 | — | — | 1 | 7.22 |
| CHEMBL526684 | — | — | 1 | 7.19 |
| CHEMBL526893 | — | — | 1 | 6.68 |
| CHEMBL505224 | — | — | 1 | 6.54 |
| CHEMBL468769 | — | — | 1 | 5.70 |
| CHEMBL504759 | — | — | 1 | - |
| CHEMBL504234 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL414357 | EXENATIDE | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL525934 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL499930 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL499133 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL524907 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL527077 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL526685 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL499370 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL499208 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL507645 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL526730 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL500447 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL507190 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL524538 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL525956 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL526684 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL526893 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL505224 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL468769 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL504759 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL504234 | — | IC50 | > | 500.0 | nM | - |