Assay Detail
Binding
CHEMBL3854865
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Irreversible inhibition of GST-tagged ERBB4 (unknown origin) (Gly-259 to Gly-690 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA
67
Total Activities
67
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-4 (CHEMBL3009) ↗| 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 | 67 | 7.55 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3959248 | — | — | 1 | 9.00 |
| CHEMBL3896779 | — | — | 1 | 8.70 |
| CHEMBL3890186 | — | — | 1 | 8.70 |
| CHEMBL3932176 | — | — | 1 | 8.52 |
| CHEMBL3986103 | — | — | 1 | 8.52 |
| CHEMBL3949347 | — | — | 1 | 8.52 |
| CHEMBL3977504 | — | — | 1 | 8.52 |
| CHEMBL3958482 | — | — | 1 | 8.52 |
| CHEMBL3970330 | — | — | 1 | 8.52 |
| CHEMBL3981551 | — | — | 1 | 8.52 |
| CHEMBL3967962 | — | — | 1 | 8.40 |
| CHEMBL3962365 | — | — | 1 | 8.40 |
| CHEMBL3942228 | — | — | 1 | 8.40 |
| CHEMBL3923228 | — | — | 1 | 8.40 |
| CHEMBL3971413 | — | — | 1 | 8.40 |
| CHEMBL3969056 | — | — | 1 | 8.40 |
| CHEMBL3921129 | — | — | 1 | 8.40 |
| CHEMBL3941823 | — | — | 1 | 8.40 |
| CHEMBL3948267 | — | — | 1 | 8.40 |
| CHEMBL3904257 | — | — | 1 | 8.30 |
| CHEMBL3914227 | — | — | 1 | 8.30 |
| CHEMBL3950966 | — | — | 1 | 8.22 |
| CHEMBL3907533 | — | — | 1 | 8.22 |
| CHEMBL3930506 | — | — | 1 | 8.15 |
| CHEMBL3899132 | — | — | 1 | 8.00 |
| CHEMBL3939985 | — | — | 1 | 8.00 |
| CHEMBL3890751 | — | — | 1 | 7.96 |
| CHEMBL3930965 | — | — | 1 | 7.89 |
| CHEMBL3919183 | — | — | 1 | 7.82 |
| CHEMBL3948084 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3959248 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3896779 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3890186 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3932176 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3986103 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3949347 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3977504 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3958482 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3970330 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3981551 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3969056 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3962365 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3942228 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3923228 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3967962 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3971413 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3921129 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3941823 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3948267 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3904257 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3914227 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3950966 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3907533 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3930506 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3939985 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3899132 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3890751 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3930965 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3919183 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3948084 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3957416 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3964380 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3933895 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3968417 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3936505 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3977326 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3916644 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3977926 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3958006 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3943512 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3981041 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL3944095 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3972605 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL3904205 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3950549 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3921446 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL3922922 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL3968839 | — | IC50 | = | 95.0 | nM | 7.02 |