Assay Detail
Binding
CHEMBL3854867
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Irreversible inhibition of full length human ERBB1 autophosphorylation transfected in EGF-stimulated mouse NIH/3T3 cells incubated for 2 hrs followed by stimulation with EGF for 10 mins
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NIH/3T3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 7.92 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3968417 | — | — | 1 | 9.00 |
| CHEMBL3930506 | — | — | 1 | 8.70 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | 3.0 | 1 | 8.70 |
| CHEMBL3958006 | — | — | 1 | 8.70 |
| CHEMBL3932176 | — | — | 1 | 8.70 |
| CHEMBL3942228 | — | — | 1 | 8.70 |
| CHEMBL3948267 | — | — | 1 | 8.52 |
| CHEMBL3923228 | — | — | 1 | 8.52 |
| CHEMBL3949347 | — | — | 1 | 8.52 |
| CHEMBL3907533 | — | — | 1 | 8.40 |
| CHEMBL3959248 | — | — | 1 | 8.30 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | 8.22 |
| CHEMBL3950966 | — | — | 1 | 8.15 |
| CHEMBL3890186 | — | — | 1 | 8.10 |
| CHEMBL3896779 | — | — | 1 | 8.10 |
| CHEMBL3921129 | — | — | 1 | 8.10 |
| CHEMBL3950549 | — | — | 1 | 8.05 |
| CHEMBL3921555 | — | — | 1 | 8.05 |
| CHEMBL3967962 | — | — | 1 | 8.00 |
| CHEMBL3969056 | — | — | 1 | 8.00 |
| CHEMBL3939985 | — | — | 1 | 8.00 |
| CHEMBL3981551 | — | — | 1 | 7.96 |
| CHEMBL3977926 | — | — | 1 | 7.92 |
| CHEMBL3977504 | — | — | 1 | 7.85 |
| CHEMBL3957416 | — | — | 1 | 7.85 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.85 |
| CHEMBL3958482 | — | — | 1 | 7.80 |
| CHEMBL3899132 | — | — | 1 | 7.80 |
| CHEMBL3904257 | — | — | 1 | 7.80 |
| CHEMBL3941823 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3968417 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3930506 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3942228 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3932176 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3958006 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3948267 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3923228 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3949347 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3907533 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3959248 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3950966 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3921129 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3890186 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3896779 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3950549 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3921555 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3967962 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3969056 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3939985 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3981551 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3977926 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3957416 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL939 | GEFITINIB | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3977504 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3958482 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3899132 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3904257 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3941823 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3962365 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3957801 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3914227 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3946232 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3970330 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3930965 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3933895 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3890751 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3986103 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3922922 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3974571 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3918330 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3921446 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3936505 | — | IC50 | = | 390.0 | nM | 6.41 |