Assay Detail
Binding
CHEMBL2019336
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant PTP1B expressed in Escherichia coli using para-nitrophenyl phosphate as substrate preincubated for 30 mins followed by substrate addition measured by fluorescence analysis
22
Total Activities
22
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
Discovery of novel and potent heterocyclic carboxylic acid derivatives as protein tyrosine phosphatase 1B inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 5.65 | 6.52 |
| IC50 | 1 | 6.92 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8758 | — | — | 1 | 6.92 |
| CHEMBL2017853 | — | — | 1 | 6.52 |
| CHEMBL2017852 | — | — | 1 | 6.40 |
| CHEMBL2017855 | — | — | 1 | 6.30 |
| CHEMBL2017854 | — | — | 1 | 6.30 |
| CHEMBL2017850 | — | — | 1 | 6.22 |
| CHEMBL2017848 | — | — | 1 | 6.10 |
| CHEMBL2017836 | — | — | 1 | 5.96 |
| CHEMBL2017840 | — | — | 1 | 5.92 |
| CHEMBL2017847 | — | — | 1 | 5.85 |
| CHEMBL2017846 | — | — | 1 | 5.82 |
| CHEMBL2017849 | — | — | 1 | 5.75 |
| CHEMBL2017845 | — | — | 1 | 5.62 |
| CHEMBL2017841 | — | — | 1 | 5.54 |
| CHEMBL2017851 | — | — | 1 | 5.40 |
| CHEMBL2017843 | — | — | 1 | 5.29 |
| CHEMBL117869 | — | — | 1 | 5.16 |
| CHEMBL2017842 | — | — | 1 | 5.11 |
| CHEMBL2017839 | — | — | 1 | 5.11 |
| CHEMBL2017838 | — | — | 1 | 5.11 |
| CHEMBL2017837 | — | — | 1 | 4.79 |
| CHEMBL2017844 | — | — | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8758 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2017853 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL2017852 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL2017855 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL2017854 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL2017850 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL2017848 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL2017836 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL2017840 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL2017847 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL2017846 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL2017849 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL2017845 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL2017841 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL2017851 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL2017843 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL117869 | — | Ki | = | 6900.0 | nM | 5.16 |
| CHEMBL2017842 | — | Ki | = | 7700.0 | nM | 5.11 |
| CHEMBL2017839 | — | Ki | = | 7800.0 | nM | 5.11 |
| CHEMBL2017838 | — | Ki | = | 7800.0 | nM | 5.11 |
| CHEMBL2017837 | — | Ki | = | 16300.0 | nM | 4.79 |
| CHEMBL2017844 | — | Ki | = | 40000.0 | nM | 4.40 |