Assay Detail
Binding
CHEMBL861463
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against PDGFRbeta kinase
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Platelet-derived growth factor receptor beta (CHEMBL1913) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.17 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL200735 | — | — | 1 | 8.52 |
| CHEMBL120077 | — | — | 1 | 8.38 |
| CHEMBL120862 | — | — | 1 | 8.30 |
| CHEMBL432219 | — | — | 1 | 8.05 |
| CHEMBL120634 | — | — | 1 | 8.00 |
| CHEMBL331760 | — | — | 1 | 7.92 |
| CHEMBL121161 | — | — | 1 | 7.77 |
| CHEMBL371949 | — | — | 1 | 7.75 |
| CHEMBL332375 | — | — | 1 | 7.48 |
| CHEMBL184948 | — | — | 1 | 7.42 |
| CHEMBL371910 | — | — | 1 | 7.27 |
| CHEMBL200774 | — | — | 1 | 6.96 |
| CHEMBL122528 | — | — | 1 | 6.86 |
| CHEMBL200726 | — | — | 1 | 6.66 |
| CHEMBL262249 | — | — | 1 | 6.51 |
| CHEMBL175596 | — | — | 1 | 6.50 |
| CHEMBL119910 | — | — | 1 | 6.39 |
| CHEMBL425751 | — | — | 1 | 6.18 |
| CHEMBL198642 | — | — | 1 | 5.27 |
| CHEMBL382735 | — | — | 1 | 5.21 |
| CHEMBL185391 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL200735 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL120077 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL120862 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL432219 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL120634 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL331760 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL121161 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL371949 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL332375 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL184948 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL371910 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL200774 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL122528 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL200726 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL262249 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL175596 | — | IC50 | = | 317.0 | nM | 6.50 |
| CHEMBL119910 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL425751 | — | IC50 | = | 659.0 | nM | 6.18 |
| CHEMBL198642 | — | IC50 | = | 5420.0 | nM | 5.27 |
| CHEMBL382735 | — | IC50 | = | 6220.0 | nM | 5.21 |
| CHEMBL185391 | — | IC50 | > | 800.0 | nM | - |