Assay Detail
Functional
CHEMBL834295
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Inhibition of human A431 cell proliferation
83
Total Activities
83
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A-431 |
| 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 | 6.65 | 8.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL179274 | — | — | 1 | 8.16 |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | 8.00 |
| CHEMBL175556 | — | — | 1 | 7.43 |
| CHEMBL178144 | — | — | 1 | 7.37 |
| CHEMBL179577 | — | — | 1 | 7.32 |
| CHEMBL360662 | — | — | 1 | 7.28 |
| CHEMBL179659 | — | — | 1 | 7.28 |
| CHEMBL180018 | — | — | 1 | 7.28 |
| CHEMBL179313 | — | — | 1 | 7.25 |
| CHEMBL362824 | — | — | 1 | 7.20 |
| CHEMBL180415 | — | — | 1 | 7.16 |
| CHEMBL179527 | — | — | 1 | 7.15 |
| CHEMBL361343 | — | — | 1 | 7.14 |
| CHEMBL426051 | — | — | 1 | 7.11 |
| CHEMBL360979 | — | — | 1 | 7.09 |
| CHEMBL179726 | — | — | 1 | 7.08 |
| CHEMBL179652 | — | — | 1 | 7.08 |
| CHEMBL360933 | — | — | 1 | 7.07 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 7.07 |
| CHEMBL176199 | — | — | 1 | 7.05 |
| CHEMBL362611 | — | — | 1 | 7.04 |
| CHEMBL179633 | — | — | 1 | 7.00 |
| CHEMBL180227 | — | — | 1 | 7.00 |
| CHEMBL180516 | — | — | 1 | 6.99 |
| CHEMBL424959 | — | — | 1 | 6.97 |
| CHEMBL434720 | — | — | 1 | 6.97 |
| CHEMBL360754 | — | — | 1 | 6.96 |
| CHEMBL175726 | — | — | 1 | 6.94 |
| CHEMBL178654 | HKI-357 | 1.0 | 1 | 6.92 |
| CHEMBL360519 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL179274 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL607707 | PELITINIB | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL175556 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL178144 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL179577 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL360662 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL179659 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL180018 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL179313 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL362824 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL180415 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL179527 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL361343 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL426051 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL360979 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL179726 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL179652 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL360933 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL180022 | NERATINIB | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL176199 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL362611 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL179633 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL180227 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL180516 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL434720 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL424959 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL360754 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL175726 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL178654 | HKI-357 | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL360519 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL178312 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL175557 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL175840 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL180175 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL360211 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL369299 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL179363 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL427315 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL179607 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL179123 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL369088 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL368702 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL178958 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL179766 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL179164 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL175933 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL360028 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL359660 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL179310 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL360958 | — | IC50 | = | 244.0 | nM | 6.61 |