Assay Detail
Binding
CHEMBL1914005
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of RPTPgamma expressed in Escherichia coli BL21 (DE3) assessed as reduction in dephosphorylation of Z'-Lyte phospho-Tyr 1 peptide preincubated for 20 mins by FRET assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Receptor-type tyrosine-protein phosphatase gamma (CHEMBL4905) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Small molecule receptor protein tyrosine phosphatase γ (RPTPγ) ligands that inhibit phosphatase activity via perturbation of the tryptophan-proline-aspartate (WPD) loop.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 5.17 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1910889 | — | — | 1 | 6.30 |
| CHEMBL1910968 | — | — | 1 | 5.89 |
| CHEMBL1403981 | — | — | 1 | 5.58 |
| CHEMBL1910886 | — | — | 1 | 5.48 |
| CHEMBL1910887 | — | — | 1 | 5.47 |
| CHEMBL1910882 | — | — | 1 | 5.47 |
| CHEMBL1910888 | — | — | 1 | 5.42 |
| CHEMBL1910966 | — | — | 1 | 5.40 |
| CHEMBL1910962 | — | — | 1 | 5.27 |
| CHEMBL1910967 | — | — | 1 | 5.24 |
| CHEMBL1910963 | — | — | 1 | 5.24 |
| CHEMBL1910965 | — | — | 1 | 5.00 |
| CHEMBL1910879 | — | — | 1 | 4.70 |
| CHEMBL1910964 | — | — | 1 | 4.11 |
| CHEMBL1910878 | — | — | 1 | 4.10 |
| CHEMBL1910877 | — | — | 1 | 4.10 |
| CHEMBL1910969 | — | — | 1 | - |
| CHEMBL1910885 | — | — | 1 | - |
| CHEMBL1910884 | — | — | 1 | - |
| CHEMBL1910883 | — | — | 1 | - |
| CHEMBL1910881 | — | — | 1 | - |
| CHEMBL1910880 | — | — | 1 | - |
| CHEMBL1910876 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1910889 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1910968 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1403981 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1910886 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL1910887 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1910882 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1910888 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL1910966 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL1910962 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL1910967 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL1910963 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL1910965 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1910879 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL1910964 | — | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL1910878 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL1910877 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL1910969 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1910885 | — | IC50 | > | 120000.0 | nM | - |
| CHEMBL1910884 | — | IC50 | > | 120000.0 | nM | - |
| CHEMBL1910883 | — | IC50 | > | 120000.0 | nM | - |
| CHEMBL1910881 | — | IC50 | > | 120000.0 | nM | - |
| CHEMBL1910880 | — | IC50 | = | 110000.0 | nM | - |
| CHEMBL1910876 | — | IC50 | > | 120000.0 | nM | - |