Assay Detail
Binding
CHEMBL950399
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Inhibition of ErbB2 kinase
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.25 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL497804 | — | — | 1 | 7.96 |
| CHEMBL496174 | — | — | 1 | 7.89 |
| CHEMBL466586 | — | — | 1 | 7.70 |
| CHEMBL495734 | — | — | 1 | 7.42 |
| CHEMBL500115 | — | — | 1 | 7.40 |
| CHEMBL512076 | GSK-192082A | — | 1 | 7.37 |
| CHEMBL495979 | — | — | 1 | 7.27 |
| CHEMBL517123 | GSK-182497A | — | 1 | 7.17 |
| CHEMBL525805 | — | — | 1 | 7.11 |
| CHEMBL507329 | GW869810X | — | 1 | 7.08 |
| CHEMBL495733 | — | — | 1 | 7.06 |
| CHEMBL501705 | — | — | 1 | 7.06 |
| CHEMBL500381 | — | — | 1 | 7.05 |
| CHEMBL497184 | — | — | 1 | 7.01 |
| CHEMBL523573 | — | — | 1 | 6.96 |
| CHEMBL497803 | — | — | 1 | 6.92 |
| CHEMBL500640 | — | — | 1 | 6.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL497804 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL496174 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL466586 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL495734 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL500115 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL512076 | GSK-192082A | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL495979 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL517123 | GSK-182497A | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL525805 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL507329 | GW869810X | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL495733 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL501705 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL500381 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL497184 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL523573 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL497803 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL500640 | — | IC50 | = | 135.0 | nM | 6.87 |