Assay Detail
Functional
CHEMBL2183196
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity against human HCC827 cells incubated for 72 hrs by MTT assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCC827 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.47 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2178346 | — | — | 1 | 11.00 |
| CHEMBL2178351 | — | — | 1 | 10.00 |
| CHEMBL2178360 | — | — | 1 | 9.33 |
| CHEMBL2178356 | — | — | 1 | 9.18 |
| CHEMBL2178364 | — | — | 1 | 9.14 |
| CHEMBL2178355 | — | — | 1 | 9.00 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 8.82 |
| CHEMBL2178354 | — | — | 1 | 8.77 |
| CHEMBL2178366 | — | — | 1 | 8.66 |
| CHEMBL2178367 | — | — | 1 | 8.64 |
| CHEMBL2178359 | — | — | 1 | 8.57 |
| CHEMBL2178358 | — | — | 1 | 8.55 |
| CHEMBL2178348 | — | — | 1 | 7.82 |
| CHEMBL2178350 | — | — | 1 | 7.75 |
| CHEMBL2178349 | — | — | 1 | 7.62 |
| CHEMBL2178357 | — | — | 1 | 7.50 |
| CHEMBL2178368 | — | — | 1 | 6.63 |
| CHEMBL2178347 | — | — | 1 | 5.54 |
| CHEMBL2178361 | — | — | 1 | - |
| CHEMBL2178362 | — | — | 1 | - |
| CHEMBL2178363 | — | — | 1 | - |
| CHEMBL2178365 | — | — | 1 | - |
| CHEMBL2178353 | — | — | 1 | - |
| CHEMBL2178352 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2178346 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL2178351 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL2178360 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL2178356 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL2178364 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL2178355 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL939 | GEFITINIB | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2178354 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2178366 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL2178367 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2178359 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL2178358 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL2178348 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2178350 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2178349 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2178357 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2178368 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL2178347 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL2178361 | — | IC50 | < | 0.01 | nM | - |
| CHEMBL2178362 | — | IC50 | < | 0.01 | nM | - |
| CHEMBL2178363 | — | IC50 | < | 0.01 | nM | - |
| CHEMBL2178365 | — | IC50 | < | 0.01 | nM | - |
| CHEMBL2178353 | — | IC50 | < | 0.01 | nM | - |
| CHEMBL2178352 | — | IC50 | < | 0.01 | nM | - |