Assay Detail
Functional
CHEMBL833864
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human SKBr3 cell proliferation
83
Total Activities
83
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SK-BR-3 |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 83 | 7.85 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL179313 | — | — | 1 | 9.40 |
| CHEMBL179123 | — | — | 1 | 8.96 |
| CHEMBL179363 | — | — | 1 | 8.92 |
| CHEMBL360662 | — | — | 1 | 8.89 |
| CHEMBL180175 | — | — | 1 | 8.89 |
| CHEMBL179652 | — | — | 1 | 8.85 |
| CHEMBL179572 | — | — | 1 | 8.82 |
| CHEMBL369299 | — | — | 1 | 8.80 |
| CHEMBL362611 | — | — | 1 | 8.77 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 8.74 |
| CHEMBL179527 | — | — | 1 | 8.72 |
| CHEMBL179577 | — | — | 1 | 8.70 |
| CHEMBL175840 | — | — | 1 | 8.68 |
| CHEMBL362232 | — | — | 1 | 8.66 |
| CHEMBL179274 | — | — | 1 | 8.64 |
| CHEMBL178654 | HKI-357 | 1.0 | 1 | 8.60 |
| CHEMBL434720 | — | — | 1 | 8.57 |
| CHEMBL369088 | — | — | 1 | 8.57 |
| CHEMBL179923 | — | — | 1 | 8.55 |
| CHEMBL360519 | — | — | 1 | 8.54 |
| CHEMBL360211 | — | — | 1 | 8.49 |
| CHEMBL362824 | — | — | 1 | 8.49 |
| CHEMBL178290 | — | — | 1 | 8.48 |
| CHEMBL426051 | — | — | 1 | 8.48 |
| CHEMBL360028 | — | — | 1 | 8.48 |
| CHEMBL180227 | — | — | 1 | 8.47 |
| CHEMBL176199 | — | — | 1 | 8.43 |
| CHEMBL179726 | — | — | 1 | 8.42 |
| CHEMBL180018 | — | — | 1 | 8.41 |
| CHEMBL360958 | — | — | 1 | 8.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL179313 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL179123 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL179363 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL360662 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL180175 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL179652 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL179572 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL369299 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL362611 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL180022 | NERATINIB | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL179527 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL179577 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL175840 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL362232 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL179274 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL178654 | HKI-357 | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL434720 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL369088 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL179923 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL360519 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL360211 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL362824 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL178290 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL426051 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL360028 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL180227 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL176199 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL179726 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL180018 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL360958 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL179052 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL361343 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL360979 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL178312 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL178144 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL440935 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL360754 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL179607 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL175726 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL180516 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL367492 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL180415 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL424959 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL175556 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL360780 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL175513 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL359629 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL179659 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL427315 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL179164 | — | IC50 | = | 15.0 | nM | 7.82 |