Assay Detail
Binding
CHEMBL4197224
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Inhibition of wild type EGFR L858R/T790M double mutant (unknown origin) using Poly (Glu, Tyr) as substrate after 40 mins by kinase-Glo luminescence assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.48 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 8.62 |
| CHEMBL4203016 | — | — | 1 | 7.63 |
| CHEMBL4215076 | — | — | 1 | 7.54 |
| CHEMBL4215080 | — | — | 1 | 7.52 |
| CHEMBL4209019 | — | — | 1 | 7.47 |
| CHEMBL4206166 | — | — | 1 | 7.36 |
| CHEMBL4206716 | — | — | 1 | 7.35 |
| CHEMBL4206288 | — | — | 1 | 7.27 |
| CHEMBL4217992 | — | — | 1 | 7.24 |
| CHEMBL4212884 | — | — | 1 | 7.18 |
| CHEMBL4209801 | — | — | 1 | 7.07 |
| CHEMBL4208673 | — | — | 1 | - |
| CHEMBL4204983 | — | — | 1 | - |
| CHEMBL4203001 | — | — | 1 | - |
| CHEMBL4204139 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4203016 | — | IC50 | = | 23.2 | nM | 7.63 |
| CHEMBL4215076 | — | IC50 | = | 28.8 | nM | 7.54 |
| CHEMBL4215080 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4209019 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4206166 | — | IC50 | = | 44.1 | nM | 7.36 |
| CHEMBL4206716 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4206288 | — | IC50 | = | 53.2 | nM | 7.27 |
| CHEMBL4217992 | — | IC50 | = | 57.7 | nM | 7.24 |
| CHEMBL4212884 | — | IC50 | = | 65.6 | nM | 7.18 |
| CHEMBL4209801 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4208673 | — | IC50 | - | — | - | |
| CHEMBL4204983 | — | IC50 | - | — | - | |
| CHEMBL4203001 | — | IC50 | - | — | - | |
| CHEMBL4204139 | — | IC50 | - | — | - |