Assay Detail
Functional
CHEMBL855536
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against mouse NIH3T3 cell line transfected with c-SRC
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NIH3T3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Proto-oncogene tyrosine-protein kinase Src (CHEMBL267) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.54 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL217463 | — | — | 1 | 7.40 |
| CHEMBL436968 | — | — | 1 | 7.30 |
| CHEMBL216693 | — | — | 1 | 7.30 |
| CHEMBL214376 | — | — | 1 | 7.30 |
| CHEMBL217090 | — | — | 1 | 7.19 |
| CHEMBL217464 | — | — | 1 | 7.16 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 7.12 |
| CHEMBL216105 | — | — | 1 | 7.10 |
| CHEMBL216703 | — | — | 1 | 7.00 |
| CHEMBL213762 | — | — | 1 | 7.00 |
| CHEMBL217091 | — | — | 1 | 6.82 |
| CHEMBL385563 | — | — | 1 | 6.82 |
| CHEMBL214665 | — | — | 1 | 6.82 |
| CHEMBL381206 | — | — | 1 | 6.75 |
| CHEMBL200217 | — | — | 1 | 6.70 |
| CHEMBL386996 | — | — | 1 | 6.70 |
| CHEMBL262371 | — | — | 1 | 6.66 |
| CHEMBL214893 | — | — | 1 | 6.52 |
| CHEMBL385240 | — | — | 1 | 6.30 |
| CHEMBL426161 | AZM-475271 | 2.0 | 1 | 6.28 |
| CHEMBL215682 | — | — | 1 | 6.22 |
| CHEMBL387093 | — | — | 1 | 6.20 |
| CHEMBL217493 | — | — | 1 | 6.12 |
| CHEMBL385958 | — | — | 1 | 6.10 |
| CHEMBL384031 | — | — | 1 | 6.00 |
| CHEMBL266188 | — | — | 1 | 5.96 |
| CHEMBL217977 | — | — | 1 | 5.52 |
| CHEMBL426148 | — | — | 1 | 5.41 |
| CHEMBL384260 | — | — | 1 | 5.35 |
| CHEMBL262721 | — | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL217463 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL436968 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL214376 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL216693 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL217090 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL217464 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL217092 | SARACATINIB | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL216105 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL216703 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL213762 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL217091 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL385563 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL214665 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL381206 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL386996 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL200217 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL262371 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL214893 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL385240 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL426161 | AZM-475271 | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL215682 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL387093 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL217493 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL385958 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL384031 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL266188 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL217977 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL426148 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL384260 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL262721 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL263947 | — | IC50 | - | — | - | |
| CHEMBL386584 | — | IC50 | - | — | - | |
| CHEMBL439182 | — | IC50 | - | — | - | |
| CHEMBL385533 | — | IC50 | - | — | - | |
| CHEMBL275513 | — | IC50 | - | — | - |