Assay Detail
Functional
CHEMBL874202
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human epidermal growth factor receptor-2 (HER-2) autophosphorylation
83
Total Activities
83
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL179363 | — | — | 1 | 8.10 |
| CHEMBL360519 | — | — | 1 | 8.00 |
| CHEMBL367492 | — | — | 1 | 7.89 |
| CHEMBL179652 | — | — | 1 | 7.82 |
| CHEMBL178573 | — | — | 1 | 7.75 |
| CHEMBL359629 | — | — | 1 | 7.70 |
| CHEMBL180415 | — | — | 1 | 7.62 |
| CHEMBL179164 | — | — | 1 | 7.60 |
| CHEMBL360958 | — | — | 1 | 7.60 |
| CHEMBL361343 | — | — | 1 | 7.57 |
| CHEMBL179052 | — | — | 1 | 7.55 |
| CHEMBL179123 | — | — | 1 | 7.55 |
| CHEMBL175557 | — | — | 1 | 7.54 |
| CHEMBL178654 | HKI-357 | 1.0 | 1 | 7.48 |
| CHEMBL179726 | — | — | 1 | 7.41 |
| CHEMBL368702 | — | — | 1 | 7.40 |
| CHEMBL362232 | — | — | 1 | 7.36 |
| CHEMBL362824 | — | — | 1 | 7.24 |
| CHEMBL178312 | — | — | 1 | 7.23 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 7.23 |
| CHEMBL175556 | — | — | 1 | 7.23 |
| CHEMBL179969 | — | — | 1 | 7.21 |
| CHEMBL176199 | — | — | 1 | 7.21 |
| CHEMBL175513 | — | — | 1 | 7.19 |
| CHEMBL359630 | — | — | 1 | 7.16 |
| CHEMBL360979 | — | — | 1 | 7.13 |
| CHEMBL180227 | — | — | 1 | 7.12 |
| CHEMBL434720 | — | — | 1 | 7.12 |
| CHEMBL360662 | — | — | 1 | 7.12 |
| CHEMBL180516 | — | — | 1 | 7.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL179363 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL360519 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL367492 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL179652 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL178573 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL359629 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL180415 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL179164 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL360958 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL361343 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL179052 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL179123 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL175557 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL178654 | HKI-357 | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL179726 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL368702 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL362232 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL362824 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL178312 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL180022 | NERATINIB | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL175556 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL179969 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL176199 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL175513 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL359630 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL360979 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL434720 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL360662 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL180227 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL180516 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL360028 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL179572 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL179766 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL179607 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL179577 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL369088 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL426051 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL179659 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL180175 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL179527 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL362611 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL178958 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL178144 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL180018 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL359660 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL368234 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL179310 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL175492 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL179313 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL178199 | — | IC50 | = | 281.0 | nM | 6.55 |