Assay Detail
Binding
CHEMBL2344596
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR in human A431 cells assessed as inhibition of EGF-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A-431 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 17 | 5.26 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL306315 | — | — | 1 | 8.22 |
| CHEMBL2337373 | — | — | 1 | 6.83 |
| CHEMBL29197 | — | — | 1 | 6.70 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 5.92 |
| CHEMBL2337371 | — | — | 1 | 4.51 |
| CHEMBL2337368 | — | — | 1 | 4.41 |
| CHEMBL2337364 | — | — | 1 | 4.41 |
| CHEMBL2337362 | — | — | 1 | 4.38 |
| CHEMBL2337369 | — | — | 1 | 4.23 |
| CHEMBL2337363 | — | — | 1 | 4.20 |
| CHEMBL2337366 | — | — | 1 | 4.08 |
| CHEMBL2337367 | — | — | 1 | - |
| CHEMBL2337374 | — | — | 1 | - |
| CHEMBL2337365 | — | — | 1 | - |
| CHEMBL2337370 | — | — | 1 | - |
| CHEMBL2337372 | — | — | 1 | - |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL306315 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2337373 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL29197 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2337371 | — | IC50 | = | 30800.0 | nM | 4.51 |
| CHEMBL2337368 | — | IC50 | = | 39200.0 | nM | 4.41 |
| CHEMBL2337364 | — | IC50 | = | 38900.0 | nM | 4.41 |
| CHEMBL2337362 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL2337369 | — | IC50 | = | 58700.0 | nM | 4.23 |
| CHEMBL2337363 | — | IC50 | = | 63600.0 | nM | 4.20 |
| CHEMBL2337366 | — | IC50 | = | 82900.0 | nM | 4.08 |
| CHEMBL2337367 | — | IC50 | = | 114700.0 | nM | - |
| CHEMBL2337374 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2337365 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2337370 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2337372 | — | IC50 | = | 130500.0 | nM | - |
| CHEMBL535 | SUNITINIB | IC50 | = | 172100.0 | nM | - |