Assay Detail
Binding
CHEMBL3606405
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay
38
Total Activities
38
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
Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.11 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 8.52 |
| CHEMBL3604937 | — | — | 1 | 7.16 |
| CHEMBL3604912 | — | — | 1 | 7.00 |
| CHEMBL3604941 | — | — | 1 | 6.70 |
| CHEMBL3604940 | — | — | 1 | 6.52 |
| CHEMBL3604917 | — | — | 1 | 6.52 |
| CHEMBL3604915 | — | — | 1 | 6.40 |
| CHEMBL3604921 | — | — | 1 | 6.30 |
| CHEMBL3604927 | — | — | 1 | 6.22 |
| CHEMBL3604925 | — | — | 1 | 6.16 |
| CHEMBL3604939 | — | — | 1 | 6.16 |
| CHEMBL3604931 | — | — | 1 | 6.05 |
| CHEMBL3604928 | — | — | 1 | 6.05 |
| CHEMBL3604911 | — | — | 1 | 5.96 |
| CHEMBL3604930 | — | — | 1 | 5.85 |
| CHEMBL3604936 | — | — | 1 | 5.82 |
| CHEMBL3604926 | — | — | 1 | 5.80 |
| CHEMBL3604933 | — | — | 1 | 5.72 |
| CHEMBL3604920 | — | — | 1 | 5.68 |
| CHEMBL3604910 | — | — | 1 | 5.66 |
| CHEMBL1232944 | — | — | 1 | 5.66 |
| CHEMBL3604922 | — | — | 1 | 5.62 |
| CHEMBL3604919 | — | — | 1 | 5.60 |
| CHEMBL3604942 | — | — | 1 | 5.31 |
| CHEMBL3604929 | — | — | 1 | 5.31 |
| CHEMBL3604938 | — | — | 1 | 5.07 |
| CHEMBL3604932 | — | — | 1 | - |
| CHEMBL3604934 | — | — | 1 | - |
| CHEMBL3604935 | — | — | 1 | - |
| CHEMBL3604924 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545308 | ROCILETINIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3604937 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3604912 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3604941 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3604940 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3604917 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3604915 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3604921 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3604927 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3604925 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3604939 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3604931 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3604928 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3604911 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3604930 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3604936 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3604926 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3604933 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3604920 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3604910 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1232944 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3604922 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3604919 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3604942 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL3604929 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL3604938 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL1229592 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL939 | GEFITINIB | IC50 | = | 100.0 | nM | - |
| CHEMBL3604913 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3604943 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3604914 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3604916 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3604918 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3604923 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3604924 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3604935 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3604934 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3604932 | — | IC50 | > | 10000.0 | nM | - |