Assay Detail
Binding
CHEMBL3854864
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Irreversible inhibition of GST-tagged ERBB2 (unknown origin) (Ile-675 to Val-1256 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA
57
Total Activities
57
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 |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 57 | 7.10 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3968417 | — | — | 1 | 8.70 |
| CHEMBL3959248 | — | — | 1 | 8.40 |
| CHEMBL3890186 | — | — | 1 | 8.30 |
| CHEMBL3962365 | — | — | 1 | 8.00 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | 3.0 | 1 | 7.96 |
| CHEMBL3969056 | — | — | 1 | 7.96 |
| CHEMBL3932176 | — | — | 1 | 7.92 |
| CHEMBL3930506 | — | — | 1 | 7.85 |
| CHEMBL3967962 | — | — | 1 | 7.77 |
| CHEMBL3942228 | — | — | 1 | 7.72 |
| CHEMBL3970330 | — | — | 1 | 7.72 |
| CHEMBL3941823 | — | — | 1 | 7.72 |
| CHEMBL3923228 | — | — | 1 | 7.72 |
| CHEMBL3939985 | — | — | 1 | 7.70 |
| CHEMBL3921129 | — | — | 1 | 7.64 |
| CHEMBL3907533 | — | — | 1 | 7.57 |
| CHEMBL3890751 | — | — | 1 | 7.52 |
| CHEMBL3950966 | — | — | 1 | 7.52 |
| CHEMBL3950549 | — | — | 1 | 7.50 |
| CHEMBL3958006 | — | — | 1 | 7.46 |
| CHEMBL3899132 | — | — | 1 | 7.42 |
| CHEMBL3981551 | — | — | 1 | 7.38 |
| CHEMBL3986103 | — | — | 1 | 7.35 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | 7.34 |
| CHEMBL3904257 | — | — | 1 | 7.28 |
| CHEMBL3949347 | — | — | 1 | 7.21 |
| CHEMBL3948267 | — | — | 1 | 7.21 |
| CHEMBL3958482 | — | — | 1 | 7.14 |
| CHEMBL3921555 | — | — | 1 | 7.05 |
| CHEMBL3977504 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3968417 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3959248 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3890186 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3962365 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3969056 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3932176 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3930506 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3967962 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3942228 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3970330 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3941823 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3923228 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3939985 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3921129 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3907533 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3890751 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3950966 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3950549 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3958006 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3899132 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3981551 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3986103 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3904257 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3949347 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3948267 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3958482 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3921555 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3977504 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3933895 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3896779 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL3977326 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL3914227 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL3948084 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL3957416 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL3971413 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL3977926 | — | IC50 | = | 278.0 | nM | 6.56 |
| CHEMBL3936505 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3981041 | — | IC50 | = | 286.0 | nM | 6.54 |
| CHEMBL939 | GEFITINIB | IC50 | = | 343.0 | nM | 6.46 |
| CHEMBL3934034 | — | IC50 | = | 404.0 | nM | 6.39 |
| CHEMBL3930316 | — | IC50 | = | 406.0 | nM | 6.39 |
| CHEMBL3930965 | — | IC50 | = | 413.0 | nM | 6.38 |
| CHEMBL3943512 | — | IC50 | = | 419.0 | nM | 6.38 |
| CHEMBL3961532 | — | IC50 | = | 458.0 | nM | 6.34 |
| CHEMBL3957801 | — | IC50 | = | 509.0 | nM | 6.29 |
| CHEMBL3904205 | — | IC50 | = | 556.0 | nM | 6.25 |
| CHEMBL3968839 | — | IC50 | = | 642.0 | nM | 6.19 |
| CHEMBL3964380 | — | IC50 | = | 782.0 | nM | 6.11 |