Assay Detail
Binding
CHEMBL3854863
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Irreversible inhibition of GST-tagged ERBB1 (unknown origin) (Met-668 to Ala-1211 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA
75
Total Activities
75
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 | 75 | 7.28 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3930316 | — | — | 1 | 8.70 |
| CHEMBL3950549 | — | — | 1 | 8.70 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | 3.0 | 1 | 8.70 |
| CHEMBL3968417 | — | — | 1 | 8.70 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 8.52 |
| CHEMBL3963723 | — | — | 1 | 8.22 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | 8.22 |
| CHEMBL3932176 | — | — | 1 | 8.22 |
| CHEMBL3923228 | — | — | 1 | 8.15 |
| CHEMBL3959248 | — | — | 1 | 8.15 |
| CHEMBL3946232 | — | — | 1 | 8.15 |
| CHEMBL3942228 | — | — | 1 | 8.10 |
| CHEMBL3957801 | — | — | 1 | 8.05 |
| CHEMBL3890186 | — | — | 1 | 8.00 |
| CHEMBL3958006 | — | — | 1 | 7.92 |
| CHEMBL3930506 | — | — | 1 | 7.85 |
| CHEMBL3950966 | — | — | 1 | 7.82 |
| CHEMBL3970330 | — | — | 1 | 7.80 |
| CHEMBL3941823 | — | — | 1 | 7.77 |
| CHEMBL3948084 | — | — | 1 | 7.77 |
| CHEMBL3921555 | — | — | 1 | 7.72 |
| CHEMBL3977326 | — | — | 1 | 7.68 |
| CHEMBL3986103 | — | — | 1 | 7.68 |
| CHEMBL3974571 | — | — | 1 | 7.68 |
| CHEMBL3918330 | — | — | 1 | 7.66 |
| CHEMBL3939985 | — | — | 1 | 7.64 |
| CHEMBL3921129 | — | — | 1 | 7.64 |
| CHEMBL3981551 | — | — | 1 | 7.60 |
| CHEMBL3907533 | — | — | 1 | 7.58 |
| CHEMBL3934034 | — | — | 1 | 7.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3930316 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3968417 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3950549 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL939 | GEFITINIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3963723 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3932176 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3923228 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3959248 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3946232 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3942228 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3957801 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3890186 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3958006 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3930506 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3950966 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3970330 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3941823 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3948084 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3921555 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3977326 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3986103 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3974571 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3918330 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3939985 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3921129 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3981551 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3907533 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3934034 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3890751 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3904257 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3899132 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3949347 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3948267 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3962365 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3968839 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3970738 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3943512 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3961532 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3957416 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3971413 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3914227 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3921347 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3936505 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3973028 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL3964380 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL3919183 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL3977926 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL3925158 | — | IC50 | = | 116.0 | nM | 6.94 |