Assay Detail
Binding
CHEMBL1009324
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Inhibition of ERBb2 by DELFIA assay
12
Total Activities
12
Compounds Tested
2
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
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 7.24 | 8.00 |
| IC50 | 3 | 7.77 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL512076 | GSK-192082A | — | 1 | 8.00 |
| CHEMBL517123 | GSK-182497A | — | 1 | 8.00 |
| CHEMBL466174 | — | — | 1 | 8.00 |
| CHEMBL466175 | — | — | 1 | 7.70 |
| CHEMBL466412 | GSK-238063A | — | 1 | 7.52 |
| CHEMBL507329 | GW869810X | — | 1 | 7.30 |
| CHEMBL461869 | — | — | 1 | 7.30 |
| CHEMBL450109 | — | — | 1 | 7.30 |
| CHEMBL450396 | — | — | 1 | 6.92 |
| CHEMBL466614 | — | — | 1 | 6.89 |
| CHEMBL447365 | — | — | 1 | 6.89 |
| CHEMBL466615 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL512076 | GSK-192082A | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL517123 | GSK-182497A | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL466174 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL466175 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL466412 | GSK-238063A | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL507329 | GW869810X | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL461869 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL450109 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL450396 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL466614 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL447365 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL466615 | — | EC50 | = | 220.0 | nM | 6.66 |