Assay Detail
Binding
CHEMBL3854874
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Irreversible inhibition of human recombinant GST-tagged JAK3 expressed in baculovirus infected Sf9 insect cells assessed as reduction in polyglutamic acid-tyrosine phosphorylation after 30 mins by ELISA
40
Total Activities
40
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 | 40 | 5.31 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3930506 | — | — | 1 | 6.10 |
| CHEMBL3981551 | — | — | 1 | 5.91 |
| CHEMBL3958006 | — | — | 1 | 5.77 |
| CHEMBL3921555 | — | — | 1 | 5.62 |
| CHEMBL3904257 | — | — | 1 | 5.46 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | 5.45 |
| CHEMBL3939985 | — | — | 1 | 5.43 |
| CHEMBL3890751 | — | — | 1 | 5.42 |
| CHEMBL3890186 | — | — | 1 | 5.32 |
| CHEMBL3923228 | — | — | 1 | 5.30 |
| CHEMBL3896779 | — | — | 1 | 5.22 |
| CHEMBL3962365 | — | — | 1 | 5.19 |
| CHEMBL3932176 | — | — | 1 | 5.16 |
| CHEMBL3941823 | — | — | 1 | 5.16 |
| CHEMBL3958482 | — | — | 1 | 5.15 |
| CHEMBL3942228 | — | — | 1 | 5.15 |
| CHEMBL3959248 | — | — | 1 | 5.15 |
| CHEMBL3949347 | — | — | 1 | 5.13 |
| CHEMBL3950549 | — | — | 1 | 5.13 |
| CHEMBL3948267 | — | — | 1 | 5.12 |
| CHEMBL3914227 | — | — | 1 | 5.12 |
| CHEMBL3977504 | — | — | 1 | 5.10 |
| CHEMBL3950966 | — | — | 1 | 5.09 |
| CHEMBL3921129 | — | — | 1 | 5.06 |
| CHEMBL3971413 | — | — | 1 | 5.05 |
| CHEMBL3899132 | — | — | 1 | - |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | - |
| CHEMBL3907533 | — | — | 1 | - |
| CHEMBL3921446 | — | — | 1 | - |
| CHEMBL3967962 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3930506 | — | IC50 | = | 793.0 | nM | 6.10 |
| CHEMBL3981551 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL3958006 | — | IC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL3921555 | — | IC50 | = | 2420.0 | nM | 5.62 |
| CHEMBL3904257 | — | IC50 | = | 3490.0 | nM | 5.46 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | IC50 | = | 3570.0 | nM | 5.45 |
| CHEMBL3939985 | — | IC50 | = | 3690.0 | nM | 5.43 |
| CHEMBL3890751 | — | IC50 | = | 3790.0 | nM | 5.42 |
| CHEMBL3890186 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL3923228 | — | IC50 | = | 4960.0 | nM | 5.30 |
| CHEMBL3896779 | — | IC50 | = | 5970.0 | nM | 5.22 |
| CHEMBL3962365 | — | IC50 | = | 6450.0 | nM | 5.19 |
| CHEMBL3932176 | — | IC50 | = | 6880.0 | nM | 5.16 |
| CHEMBL3941823 | — | IC50 | = | 6940.0 | nM | 5.16 |
| CHEMBL3959248 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL3958482 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL3942228 | — | IC50 | = | 7150.0 | nM | 5.15 |
| CHEMBL3949347 | — | IC50 | = | 7440.0 | nM | 5.13 |
| CHEMBL3950549 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL3914227 | — | IC50 | = | 7670.0 | nM | 5.12 |
| CHEMBL3948267 | — | IC50 | = | 7620.0 | nM | 5.12 |
| CHEMBL3977504 | — | IC50 | = | 8010.0 | nM | 5.10 |
| CHEMBL3950966 | — | IC50 | = | 8150.0 | nM | 5.09 |
| CHEMBL3921129 | — | IC50 | = | 8750.0 | nM | 5.06 |
| CHEMBL3971413 | — | IC50 | = | 8880.0 | nM | 5.05 |
| CHEMBL3957416 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3936505 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3968417 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3922922 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3977926 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3930965 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3933895 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3986103 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3970330 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3969056 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3967962 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3921446 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3907533 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL939 | GEFITINIB | IC50 | > | 1000.0 | nM | - |
| CHEMBL3899132 | — | IC50 | > | 10000.0 | nM | - |