Assay Detail
Binding
CHEMBL2427158
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NCI-H1975 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.63 | 8.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2426278 | — | — | 1 | 8.25 |
| CHEMBL2426277 | — | — | 1 | 7.72 |
| CHEMBL2426282 | — | — | 1 | 7.66 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 7.64 |
| CHEMBL1229592 | — | — | 1 | 7.64 |
| CHEMBL2426286 | — | — | 1 | 7.48 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | 7.38 |
| CHEMBL2426287 | — | — | 1 | 7.28 |
| CHEMBL2426279 | — | — | 1 | 7.17 |
| CHEMBL2424676 | — | — | 1 | 7.15 |
| CHEMBL2426281 | — | — | 1 | 7.09 |
| CHEMBL2426288 | — | — | 1 | 7.02 |
| CHEMBL2426290 | — | — | 1 | 6.66 |
| CHEMBL2426289 | — | — | 1 | 6.60 |
| CHEMBL2426377 | — | — | 1 | 6.54 |
| CHEMBL2426280 | — | — | 1 | 6.11 |
| CHEMBL2426284 | — | — | 1 | 5.68 |
| CHEMBL2426248 | — | — | 1 | 5.64 |
| CHEMBL2426285 | — | — | 1 | 5.55 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.48 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 5.12 |
| CHEMBL2426283 | — | — | 1 | 4.89 |
| CHEMBL2426378 | — | — | 1 | 4.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2426278 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL2426277 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2426282 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1229592 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2426286 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2426287 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL2426279 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL2424676 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL2426281 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL2426288 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL2426290 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2426289 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2426377 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2426280 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL2426284 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2426248 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL2426285 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL939 | GEFITINIB | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL2426283 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL2426378 | — | IC50 | = | 15200.0 | nM | 4.82 |