Assay Detail
Binding
CHEMBL2344595
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDGFRbeta in human SF539 cells assessed as inhibition of PDGFR-BB-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SF-539 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Platelet-derived growth factor receptor beta (CHEMBL1913) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological activity of 5-chloro-N⁴-substituted phenyl-9H-pyrimido[4,5-b]indole-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 4.57 | 5.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL328710 | — | — | 1 | 5.43 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 4.91 |
| CHEMBL2337366 | — | — | 1 | 4.30 |
| CHEMBL2337367 | — | — | 1 | 4.15 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 4.08 |
| CHEMBL2337372 | — | — | 1 | - |
| CHEMBL2337371 | — | — | 1 | - |
| CHEMBL2337370 | — | — | 1 | - |
| CHEMBL2337369 | — | — | 1 | - |
| CHEMBL2337368 | — | — | 1 | - |
| CHEMBL2337365 | — | — | 1 | - |
| CHEMBL2337364 | — | — | 1 | - |
| CHEMBL2337363 | — | — | 1 | - |
| CHEMBL2337362 | — | — | 1 | - |
| CHEMBL2337374 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL328710 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL2337366 | — | IC50 | = | 50500.0 | nM | 4.30 |
| CHEMBL2337367 | — | IC50 | = | 70600.0 | nM | 4.15 |
| CHEMBL535 | SUNITINIB | IC50 | = | 83100.0 | nM | 4.08 |
| CHEMBL2337372 | — | IC50 | = | 196200.0 | nM | - |
| CHEMBL2337371 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2337370 | — | IC50 | = | 170800.0 | nM | - |
| CHEMBL2337369 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2337368 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2337365 | — | IC50 | = | 172200.0 | nM | - |
| CHEMBL2337364 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2337363 | — | IC50 | = | 196200.0 | nM | - |
| CHEMBL2337362 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2337374 | — | IC50 | > | 200000.0 | nM | - |