Assay Detail
Binding
CHEMBL4132766
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST tagged human PDGFRbeta (557 to 1106 end residues) cytoplasmic domain expressed in baculovirus expression system preincubated for 10 mins followed by fluorescein amidite-labelled peptide substrate addition measured after 1 hr by mobility shift assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Platelet-derived growth factor receptor beta (CHEMBL1913) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel methyl indolinone-6-carboxylates containing an indole moiety as angiokinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.27 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 8.46 |
| CHEMBL4165429 | — | — | 1 | 7.66 |
| CHEMBL4173078 | — | — | 1 | 7.46 |
| CHEMBL4161991 | — | — | 1 | 7.41 |
| CHEMBL4166696 | — | — | 1 | 7.36 |
| CHEMBL4169257 | — | — | 1 | 7.34 |
| CHEMBL4162400 | — | — | 1 | 7.31 |
| CHEMBL4164318 | — | — | 1 | 7.22 |
| CHEMBL4177112 | — | — | 1 | 7.21 |
| CHEMBL4172205 | — | — | 1 | 7.19 |
| CHEMBL4165850 | — | — | 1 | 7.04 |
| CHEMBL4173756 | — | — | 1 | 7.03 |
| CHEMBL4173817 | — | — | 1 | 6.93 |
| CHEMBL4176458 | — | — | 1 | 6.87 |
| CHEMBL4161351 | — | — | 1 | 6.62 |
| CHEMBL4165827 | — | — | 1 | - |
| CHEMBL4176039 | — | — | 1 | - |
| CHEMBL4163106 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL502835 | NINTEDANIB | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4165429 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4173078 | — | IC50 | = | 34.3 | nM | 7.46 |
| CHEMBL4161991 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4166696 | — | IC50 | = | 44.2 | nM | 7.36 |
| CHEMBL4169257 | — | IC50 | = | 45.5 | nM | 7.34 |
| CHEMBL4162400 | — | IC50 | = | 49.2 | nM | 7.31 |
| CHEMBL4164318 | — | IC50 | = | 60.7 | nM | 7.22 |
| CHEMBL4177112 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4172205 | — | IC50 | = | 64.6 | nM | 7.19 |
| CHEMBL4165850 | — | IC50 | = | 91.7 | nM | 7.04 |
| CHEMBL4173756 | — | IC50 | = | 92.7 | nM | 7.03 |
| CHEMBL4173817 | — | IC50 | = | 116.2 | nM | 6.93 |
| CHEMBL4176458 | — | IC50 | = | 135.1 | nM | 6.87 |
| CHEMBL4161351 | — | IC50 | = | 241.6 | nM | 6.62 |
| CHEMBL4165827 | — | IC50 | - | — | - | |
| CHEMBL4176039 | — | IC50 | - | — | - | |
| CHEMBL4163106 | — | IC50 | > | 500.0 | nM | - |