Assay Detail
Binding
CHEMBL995931
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Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BHK |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gastric inhibitory polypeptide receptor (CHEMBL4383) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Human glucagon receptor antagonists with thiazole cores. A novel series with superior pharmacokinetic properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.37 | 6.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL491920 | — | — | 1 | 6.68 |
| CHEMBL455323 | — | — | 1 | 6.54 |
| CHEMBL523847 | — | — | 1 | 6.53 |
| CHEMBL448561 | — | — | 1 | 6.50 |
| CHEMBL492813 | — | — | 1 | 6.41 |
| CHEMBL451288 | — | — | 1 | 6.41 |
| CHEMBL471580 | — | — | 1 | 6.39 |
| CHEMBL519776 | — | — | 1 | 6.34 |
| CHEMBL501628 | — | — | 1 | 6.32 |
| CHEMBL492605 | — | — | 1 | 6.29 |
| CHEMBL446821 | — | — | 1 | 6.11 |
| CHEMBL470729 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL491920 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL455323 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL523847 | — | IC50 | = | 293.0 | nM | 6.53 |
| CHEMBL448561 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL492813 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL451288 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL471580 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL519776 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL501628 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL492605 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL446821 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL470729 | — | IC50 | = | 1100.0 | nM | 5.96 |