Assay Detail
Binding
CHEMBL855513
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Inhibition of human c-Src in NIH3T3 cells
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 42 | 7.36 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 8.57 |
| CHEMBL217463 | — | — | 1 | 8.52 |
| CHEMBL217464 | — | — | 1 | 8.40 |
| CHEMBL436968 | — | — | 1 | 8.30 |
| CHEMBL170984 | — | — | 1 | 8.30 |
| CHEMBL385723 | — | — | 1 | 8.30 |
| CHEMBL385563 | — | — | 1 | 8.22 |
| CHEMBL216105 | — | — | 1 | 8.22 |
| CHEMBL213762 | — | — | 1 | 8.15 |
| CHEMBL217091 | — | — | 1 | 8.02 |
| CHEMBL426161 | AZM-475271 | 2.0 | 1 | 8.00 |
| CHEMBL214665 | — | — | 1 | 8.00 |
| CHEMBL216369 | — | — | 1 | 7.82 |
| CHEMBL217493 | — | — | 1 | 7.70 |
| CHEMBL200217 | — | — | 1 | 7.70 |
| CHEMBL386996 | — | — | 1 | 7.70 |
| CHEMBL385240 | — | — | 1 | 7.52 |
| CHEMBL214893 | — | — | 1 | 7.40 |
| CHEMBL381206 | — | — | 1 | 7.40 |
| CHEMBL215682 | — | — | 1 | 7.26 |
| CHEMBL214894 | — | — | 1 | 7.19 |
| CHEMBL387093 | — | — | 1 | 7.12 |
| CHEMBL385958 | — | — | 1 | 7.10 |
| CHEMBL266188 | — | — | 1 | 7.07 |
| CHEMBL263947 | — | — | 1 | 7.00 |
| CHEMBL384031 | — | — | 1 | 7.00 |
| CHEMBL215087 | — | — | 1 | 6.96 |
| CHEMBL384260 | — | — | 1 | 6.82 |
| CHEMBL275513 | — | — | 1 | 6.64 |
| CHEMBL216586 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL217092 | SARACATINIB | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL217463 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL217464 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL436968 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL170984 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL385723 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL385563 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL216105 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL213762 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL217091 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL426161 | AZM-475271 | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL214665 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL216369 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL386996 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL200217 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL217493 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL385240 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL214893 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL381206 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL215682 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL214894 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL387093 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL385958 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL266188 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL263947 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL384031 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL215087 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL384260 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL275513 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL216586 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL386584 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL385533 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL439182 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL217977 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL262721 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL426148 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL217088 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL217090 | — | IC50 | < | 4.0 | nM | - |
| CHEMBL262371 | — | IC50 | < | 4.0 | nM | - |
| CHEMBL216703 | — | IC50 | < | 4.0 | nM | - |
| CHEMBL216693 | — | IC50 | < | 4.0 | nM | - |
| CHEMBL214376 | — | IC50 | < | 4.0 | nM | - |