Assay Detail
Binding
CHEMBL5165817
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Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) by ELISA
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.45 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5185864 | — | — | 1 | 8.82 |
| CHEMBL5180778 | — | — | 1 | 8.80 |
| CHEMBL5206683 | — | — | 1 | 8.38 |
| CHEMBL5176897 | — | — | 1 | 8.37 |
| CHEMBL5205581 | — | — | 1 | 8.21 |
| CHEMBL5185922 | — | — | 1 | 7.84 |
| CHEMBL5188272 | — | — | 1 | 7.72 |
| CHEMBL5172251 | — | — | 1 | 7.66 |
| CHEMBL5193609 | — | — | 1 | 7.63 |
| CHEMBL5197952 | — | — | 1 | 7.55 |
| CHEMBL5209545 | — | — | 1 | 7.51 |
| CHEMBL5181684 | — | — | 1 | 7.49 |
| CHEMBL5198314 | — | — | 1 | 7.46 |
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 7.42 |
| CHEMBL5194174 | — | — | 1 | 7.38 |
| CHEMBL5179214 | — | — | 1 | 7.25 |
| CHEMBL5170653 | — | — | 1 | 7.24 |
| CHEMBL5207083 | — | — | 1 | 7.11 |
| CHEMBL5201250 | — | — | 1 | 7.05 |
| CHEMBL5172338 | — | — | 1 | 6.91 |
| CHEMBL5181437 | — | — | 1 | 6.85 |
| CHEMBL5188281 | — | — | 1 | 6.84 |
| CHEMBL5169943 | — | — | 1 | 6.78 |
| CHEMBL5200598 | — | — | 1 | 6.65 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.33 |
| CHEMBL5179495 | — | — | 1 | 6.32 |
| CHEMBL5170303 | — | — | 1 | - |
| CHEMBL5201287 | — | — | 1 | - |
| CHEMBL5185999 | — | — | 1 | - |
| CHEMBL5195358 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5185864 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5180778 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5206683 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5176897 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5205581 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL5185922 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL5188272 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5172251 | — | IC50 | = | 21.8 | nM | 7.66 |
| CHEMBL5193609 | — | IC50 | = | 23.6 | nM | 7.63 |
| CHEMBL5197952 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5209545 | — | IC50 | = | 30.8 | nM | 7.51 |
| CHEMBL5181684 | — | IC50 | = | 32.1 | nM | 7.49 |
| CHEMBL5198314 | — | IC50 | = | 34.8 | nM | 7.46 |
| CHEMBL3545311 | BRIGATINIB | IC50 | = | 37.6 | nM | 7.42 |
| CHEMBL5194174 | — | IC50 | = | 41.9 | nM | 7.38 |
| CHEMBL5179214 | — | IC50 | = | 56.4 | nM | 7.25 |
| CHEMBL5170653 | — | IC50 | = | 57.8 | nM | 7.24 |
| CHEMBL5207083 | — | IC50 | = | 77.8 | nM | 7.11 |
| CHEMBL5201250 | — | IC50 | = | 89.9 | nM | 7.05 |
| CHEMBL5172338 | — | IC50 | = | 124.5 | nM | 6.91 |
| CHEMBL5181437 | — | IC50 | = | 141.9 | nM | 6.85 |
| CHEMBL5188281 | — | IC50 | = | 145.3 | nM | 6.84 |
| CHEMBL5169943 | — | IC50 | = | 164.9 | nM | 6.78 |
| CHEMBL5200598 | — | IC50 | = | 222.3 | nM | 6.65 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 465.4 | nM | 6.33 |
| CHEMBL5179495 | — | IC50 | = | 477.7 | nM | 6.32 |
| CHEMBL5170303 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5201287 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5185999 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5195358 | — | IC50 | > | 1000.0 | nM | - |