Assay Detail
Binding
CHEMBL5732719
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: The degree of inhibition activity for PTP1B was investigated by using 2 mM p-nitrophenyl phosphate (p-NPP) as a substrate to measure the dephosphorylation degree. First, PTP1B diluted with distilled water was reacted with 2 mM p-nitrophenyl phosphate {p-NPP, 0.1 M NaCl, 1 mM EDTA, 50 mM citrate pH 6.0, and 1 mM dithiothreitol (DTT)} and Compound 1 at various concentrations at 30° C. for 30 minutes, and then the reaction was terminated with a 1 N-sodium hydroxide (NaOH) solution. The absorbance of the samples thus prepared was measured to confirm the inhibition degree (IC50: The half maximal inhibitory concentration) for PTP1B activity according to the concentration of Compound 1.
33
Total Activities
9
Compounds Tested
3
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
Pyranochromenyl phenol derivative, and pharmaceutical composition for treating metabolic syndrome or inflammatory disease
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.27 | 5.92 |
| kon | 11 | - | - |
| k_off | 11 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6004394 | — | — | 3 | 5.92 |
| CHEMBL5912516 | — | — | 6 | 5.72 |
| CHEMBL5776864 | — | — | 3 | 5.64 |
| CHEMBL5811295 | — | — | 3 | 5.55 |
| CHEMBL5875339 | — | — | 3 | 5.54 |
| CHEMBL5978005 | — | — | 3 | 5.47 |
| CHEMBL5946660 | — | — | 3 | 5.19 |
| CHEMBL5848347 | — | — | 3 | 5.16 |
| CHEMBL480477 | GLABRIDIN | — | 6 | 4.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6004394 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5912516 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL5776864 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5811295 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL5875339 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5978005 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL5946660 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL5848347 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL5912516 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL480477 | GLABRIDIN | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL480477 | GLABRIDIN | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL5946660 | — | k_off | = | - | s-1 | - |
| CHEMBL5811295 | — | k_off | = | - | s-1 | - |
| CHEMBL5811295 | — | kon | = | - | — | - |
| CHEMBL5875339 | — | k_off | = | - | s-1 | - |
| CHEMBL5875339 | — | kon | = | - | — | - |
| CHEMBL5848347 | — | k_off | = | - | s-1 | - |
| CHEMBL5848347 | — | kon | = | - | — | - |
| CHEMBL480477 | GLABRIDIN | k_off | = | - | s-1 | - |
| CHEMBL480477 | GLABRIDIN | kon | = | - | — | - |
| CHEMBL480477 | GLABRIDIN | k_off | = | - | s-1 | - |
| CHEMBL480477 | GLABRIDIN | kon | = | - | — | - |
| CHEMBL5912516 | — | kon | = | - | — | - |
| CHEMBL5912516 | — | k_off | = | - | s-1 | - |
| CHEMBL5776864 | — | k_off | = | - | s-1 | - |
| CHEMBL5776864 | — | kon | = | - | — | - |
| CHEMBL6004394 | — | k_off | = | - | s-1 | - |
| CHEMBL6004394 | — | kon | = | - | — | - |
| CHEMBL5946660 | — | kon | = | - | — | - |
| CHEMBL5978005 | — | kon | = | - | — | - |
| CHEMBL5912516 | — | k_off | = | - | s-1 | - |
| CHEMBL5912516 | — | kon | = | - | — | - |
| CHEMBL5978005 | — | k_off | = | - | s-1 | - |