Assay Detail
Binding
CHEMBL1038652
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Inhibition of PTP1B
22
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Tyrosine-protein phosphatase non-receptor type 1 (CHEMBL335) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Thiazolidinedione derivatives as PTP1B inhibitors with antihyperglycemic and antiobesity effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 4.93 | 5.85 |
| Ki | 1 | 5.68 | 5.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL184041 | ERTIPROTAFIB | 2.0 | 1 | 5.85 |
| CHEMBL574813 | — | — | 2 | 5.68 |
| CHEMBL575025 | — | — | 1 | 5.30 |
| CHEMBL572574 | — | — | 1 | 5.22 |
| CHEMBL572800 | — | — | 1 | 5.10 |
| CHEMBL572582 | — | — | 1 | 5.10 |
| CHEMBL572814 | — | — | 1 | 5.10 |
| CHEMBL575043 | — | — | 1 | 5.10 |
| CHEMBL574377 | — | — | 1 | 5.05 |
| CHEMBL362497 | — | — | 1 | 5.05 |
| CHEMBL573469 | — | — | 1 | 4.96 |
| CHEMBL576191 | — | — | 1 | 4.85 |
| CHEMBL582941 | — | — | 1 | 4.82 |
| CHEMBL575024 | — | — | 1 | 4.82 |
| CHEMBL426796 | — | — | 1 | 4.80 |
| CHEMBL574814 | — | — | 1 | 4.64 |
| CHEMBL408 | TROGLITAZONE | 4.0 | 1 | 4.26 |
| CHEMBL315736 | — | — | 1 | 4.19 |
| CHEMBL582968 | — | — | 1 | 4.17 |
| CHEMBL595 | PIOGLITAZONE | 4.0 | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL184041 | ERTIPROTAFIB | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL574813 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL575025 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL574813 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL572574 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL575043 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL572814 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL572582 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL572800 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL362497 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL574377 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL573469 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL576191 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL582941 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL575024 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL426796 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL574814 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL408 | TROGLITAZONE | IC50 | = | 55000.0 | nM | 4.26 |
| CHEMBL315736 | — | IC50 | = | 64000.0 | nM | 4.19 |
| CHEMBL582968 | — | IC50 | = | 68000.0 | nM | 4.17 |
| CHEMBL595 | PIOGLITAZONE | IC50 | = | 220000.0 | nM | - |
| CHEMBL121 | ROSIGLITAZONE | IC50 | = | 400000.0 | nM | - |