Assay Detail
Functional
CHEMBL2183195
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Cytotoxicity against human NCI-H1975 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 | NCI-H1975 |
| 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 | 5.72 | 6.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2178352 | — | — | 1 | 6.44 |
| CHEMBL2178353 | — | — | 1 | 6.41 |
| CHEMBL2178365 | — | — | 1 | 6.41 |
| CHEMBL2178363 | — | — | 1 | 6.25 |
| CHEMBL2178362 | — | — | 1 | 6.19 |
| CHEMBL2178351 | — | — | 1 | 6.02 |
| CHEMBL2178361 | — | — | 1 | 6.01 |
| CHEMBL2178364 | — | — | 1 | 5.99 |
| CHEMBL2178367 | — | — | 1 | 5.95 |
| CHEMBL2178360 | — | — | 1 | 5.92 |
| CHEMBL2178354 | — | — | 1 | 5.74 |
| CHEMBL2178355 | — | — | 1 | 5.72 |
| CHEMBL2178366 | — | — | 1 | 5.68 |
| CHEMBL2178348 | — | — | 1 | 5.67 |
| CHEMBL2178346 | — | — | 1 | 5.59 |
| CHEMBL2178358 | — | — | 1 | 5.55 |
| CHEMBL2178350 | — | — | 1 | 5.54 |
| CHEMBL2178347 | — | — | 1 | 5.40 |
| CHEMBL2178349 | — | — | 1 | 5.22 |
| CHEMBL2178356 | — | — | 1 | 5.04 |
| CHEMBL2178357 | — | — | 1 | 5.01 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.00 |
| CHEMBL2178368 | — | — | 1 | 4.74 |
| CHEMBL2178359 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2178352 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL2178353 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL2178365 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL2178363 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL2178362 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL2178351 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL2178361 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL2178364 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL2178367 | — | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL2178360 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL2178354 | — | IC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL2178355 | — | IC50 | = | 1910.0 | nM | 5.72 |
| CHEMBL2178366 | — | IC50 | = | 2090.0 | nM | 5.68 |
| CHEMBL2178348 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL2178346 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL2178358 | — | IC50 | = | 2810.0 | nM | 5.55 |
| CHEMBL2178350 | — | IC50 | = | 2860.0 | nM | 5.54 |
| CHEMBL2178347 | — | IC50 | = | 4010.0 | nM | 5.40 |
| CHEMBL2178349 | — | IC50 | = | 6060.0 | nM | 5.22 |
| CHEMBL2178356 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL2178357 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL939 | GEFITINIB | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2178368 | — | IC50 | = | 18060.0 | nM | 4.74 |
| CHEMBL2178359 | — | IC50 | > | 10000.0 | nM | - |