Assay Detail
Binding
CHEMBL4038754
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Inhibition of recombinant human PTP1B (1 to 322 residues) expressed in Escherichia coli using pNPP as substrate incubated for 10 mins measured for 30 mins by spectrometric analysis
18
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Tyrosine-protein phosphatase non-receptor type 1 (CHEMBL335) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Competitive protein tyrosine phosphatase 1B (PTP1B) inhibitors, prenylated caged xanthones from Garcinia hanburyi and their inhibitory mechanism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.39 | 6.33 |
| Inhibition | 8 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL555017 | GAMBOGIC ACID | — | 2 | 6.33 |
| CHEMBL4095800 | — | — | 2 | 6.13 |
| CHEMBL4069859 | — | — | 2 | 6.03 |
| CHEMBL2205166 | GAMBOGENIC ACID | — | 2 | 5.46 |
| CHEMBL4090412 | — | — | 2 | 5.35 |
| CHEMBL4068566 | — | — | 2 | 5.33 |
| CHEMBL4059800 | — | — | 2 | 4.89 |
| CHEMBL169 | URSOLIC ACID | 2.0 | 1 | 4.81 |
| CHEMBL4068458 | — | — | 2 | 4.15 |
| CHEMBL4088075 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL555017 | GAMBOGIC ACID | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4095800 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4069859 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL2205166 | GAMBOGENIC ACID | IC50 | = | 3470.0 | nM | 5.46 |
| CHEMBL4090412 | — | IC50 | = | 4440.0 | nM | 5.35 |
| CHEMBL4068566 | — | IC50 | = | 4690.0 | nM | 5.33 |
| CHEMBL4059800 | — | IC50 | = | 12790.0 | nM | 4.89 |
| CHEMBL169 | URSOLIC ACID | IC50 | = | 15500.0 | nM | 4.81 |
| CHEMBL4068458 | — | IC50 | = | 70250.0 | nM | 4.15 |
| CHEMBL4059800 | — | Inhibition | - | % | - | |
| CHEMBL4068458 | — | Inhibition | - | % | - | |
| CHEMBL4095800 | — | Inhibition | - | % | - | |
| CHEMBL2205166 | GAMBOGENIC ACID | Inhibition | - | % | - | |
| CHEMBL4069859 | — | Inhibition | - | % | - | |
| CHEMBL4068566 | — | Inhibition | - | % | - | |
| CHEMBL4090412 | — | Inhibition | - | % | - | |
| CHEMBL555017 | GAMBOGIC ACID | Inhibition | - | % | - | |
| CHEMBL4088075 | — | IC50 | > | 200000.0 | nM | - |