Assay Detail
Functional
CHEMBL674641
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of tyrosine phosphorylation by full length Epidermal growth factor receptor from human A431 carcinoma cells.
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | A-431 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Tyrosine kinase inhibitors. 7. 7-Amino-4-(phenylamino)- and 7-amino-4-[(phenylmethyl)amino]pyrido[4,3-d]pyrimidines: a new class of inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 5.92 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL52076 | — | — | 1 | 8.00 |
| CHEMBL125810 | — | — | 1 | 7.82 |
| CHEMBL331792 | — | — | 1 | 7.40 |
| CHEMBL124673 | — | — | 1 | 7.40 |
| CHEMBL123322 | — | — | 1 | 7.16 |
| CHEMBL338625 | — | — | 1 | 7.05 |
| CHEMBL124528 | — | — | 1 | 6.92 |
| CHEMBL334173 | — | — | 1 | 6.89 |
| CHEMBL332846 | — | — | 1 | 6.64 |
| CHEMBL122132 | — | — | 1 | 6.62 |
| CHEMBL122534 | — | — | 1 | 6.60 |
| CHEMBL125550 | — | — | 1 | 6.58 |
| CHEMBL300083 | — | — | 1 | 6.24 |
| CHEMBL128001 | — | — | 1 | 6.17 |
| CHEMBL340438 | — | — | 1 | 6.08 |
| CHEMBL121708 | — | — | 1 | 6.00 |
| CHEMBL338662 | — | — | 1 | 5.90 |
| CHEMBL124617 | — | — | 1 | 5.81 |
| CHEMBL331307 | — | — | 1 | 5.78 |
| CHEMBL125331 | — | — | 1 | 5.75 |
| CHEMBL124533 | — | — | 1 | 5.71 |
| CHEMBL125949 | — | — | 1 | 5.61 |
| CHEMBL332173 | — | — | 1 | 5.54 |
| CHEMBL126101 | — | — | 1 | 5.43 |
| CHEMBL125035 | — | — | 1 | 5.37 |
| CHEMBL339684 | — | — | 1 | 5.33 |
| CHEMBL341053 | — | — | 1 | 5.31 |
| CHEMBL124618 | — | — | 1 | 5.28 |
| CHEMBL333272 | — | — | 1 | 5.23 |
| CHEMBL333041 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL52076 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL125810 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL124673 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL331792 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL123322 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL338625 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL124528 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL334173 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL332846 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL122132 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL122534 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL125550 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL300083 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL128001 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL340438 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL121708 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL338662 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL124617 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL331307 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL125331 | — | IC50 | = | 1790.0 | nM | 5.75 |
| CHEMBL124533 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL125949 | — | IC50 | = | 2460.0 | nM | 5.61 |
| CHEMBL332173 | — | IC50 | = | 2870.0 | nM | 5.54 |
| CHEMBL126101 | — | IC50 | = | 3710.0 | nM | 5.43 |
| CHEMBL125035 | — | IC50 | = | 4250.0 | nM | 5.37 |
| CHEMBL339684 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL341053 | — | IC50 | = | 4860.0 | nM | 5.31 |
| CHEMBL124618 | — | IC50 | = | 5250.0 | nM | 5.28 |
| CHEMBL333272 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL333041 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL123676 | — | IC50 | = | 10100.0 | nM | 5.00 |
| CHEMBL126062 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL332879 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL333045 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL333115 | — | IC50 | = | 65000.0 | nM | 4.19 |
| CHEMBL123523 | — | IC50 | = | 69000.0 | nM | 4.16 |
| CHEMBL121709 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL125995 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL122168 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL127763 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL121984 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL126097 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL419601 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL122081 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL125983 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL124836 | — | IC50 | > | 10000.0 | nM | - |