Assay Detail
Functional
CHEMBL862515
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGF stimulated human erbB1 autophosphorylation in NIH3T3 cells
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NIH3T3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 8.08 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | 3.0 | 1 | 8.77 |
| CHEMBL203661 | — | — | 1 | 8.74 |
| CHEMBL203599 | — | — | 1 | 8.72 |
| CHEMBL91867 | — | — | 1 | 8.60 |
| CHEMBL203644 | — | — | 1 | 8.60 |
| CHEMBL437890 | — | — | 1 | 8.57 |
| CHEMBL202360 | — | — | 1 | 8.57 |
| CHEMBL205059 | — | — | 1 | 8.37 |
| CHEMBL202424 | — | — | 1 | 8.35 |
| CHEMBL382073 | — | — | 1 | 8.35 |
| CHEMBL204638 | — | — | 1 | 8.35 |
| CHEMBL373207 | — | — | 1 | 8.17 |
| CHEMBL203645 | — | — | 1 | 8.02 |
| CHEMBL202398 | — | — | 1 | 7.96 |
| CHEMBL380669 | — | — | 1 | 7.96 |
| CHEMBL204085 | — | — | 1 | 7.92 |
| CHEMBL202556 | — | — | 1 | 7.85 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.84 |
| CHEMBL378144 | — | — | 1 | 7.82 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.71 |
| CHEMBL202411 | — | — | 1 | 7.60 |
| CHEMBL202621 | — | — | 1 | 7.51 |
| CHEMBL202425 | — | — | 1 | 7.32 |
| CHEMBL202421 | — | — | 1 | 7.31 |
| CHEMBL383499 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL203661 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL203599 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL91867 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL203644 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL437890 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL202360 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL205059 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL202424 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL382073 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL204638 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL373207 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL203645 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL202398 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL380669 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL204085 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL202556 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL939 | GEFITINIB | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL378144 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL202411 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL202621 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL202425 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL202421 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL383499 | — | IC50 | = | 73.0 | nM | 7.14 |