Assay Detail
Binding
CHEMBL3428080
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 6-His-N-terminal tagged human PTP1B expressed in Escherichia coli BL21 (DE3) cells assessed as pNP formation using pNPP as substrate incubated for 15 mins prior to substrate addition by plate reader analysis
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BL21-DE3 |
| 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
Is RK-682 a promiscuous enzyme inhibitor? Synthesis and in vitro evaluation of protein tyrosine phosphatase inhibition of racemic RK-682 and analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.77 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3427126 | — | — | 1 | 6.52 |
| CHEMBL110642 | — | — | 1 | 6.40 |
| CHEMBL3427125 | — | — | 1 | 6.40 |
| CHEMBL3427124 | — | — | 1 | 6.40 |
| CHEMBL3427127 | — | — | 1 | 6.30 |
| CHEMBL3427132 | — | — | 1 | 6.22 |
| CHEMBL233760 | — | — | 1 | 6.16 |
| CHEMBL3427224 | — | — | 1 | 6.10 |
| CHEMBL3427137 | — | — | 1 | 6.10 |
| CHEMBL3427131 | — | — | 1 | 6.00 |
| CHEMBL3427223 | — | — | 1 | 5.96 |
| CHEMBL3427129 | — | — | 1 | 5.25 |
| CHEMBL3427128 | — | — | 1 | 5.09 |
| CHEMBL3427130 | — | — | 1 | 4.81 |
| CHEMBL3427133 | — | — | 1 | 4.54 |
| CHEMBL3427134 | — | — | 1 | 4.14 |
| CHEMBL3427135 | — | — | 1 | - |
| CHEMBL3427136 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3427126 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL110642 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3427125 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3427124 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3427127 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3427132 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL233760 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3427224 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3427137 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3427131 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3427223 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3427129 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL3427128 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL3427130 | — | IC50 | = | 15600.0 | nM | 4.81 |
| CHEMBL3427133 | — | IC50 | = | 28700.0 | nM | 4.54 |
| CHEMBL3427134 | — | IC50 | = | 72700.0 | nM | 4.14 |
| CHEMBL3427135 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3427136 | — | IC50 | > | 100000.0 | nM | - |