Assay Detail
Binding
CHEMBL1009319
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Inhibition of ERBb2 by HTRF assay
23
Total Activities
23
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
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 |
|---|---|---|---|
| IC50 | 23 | 7.40 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 9.00 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 8.70 |
| CHEMBL1201179 | LAPATINIB DITOSYLATE | 4.0 | 1 | 8.30 |
| CHEMBL461426 | — | — | 1 | 7.80 |
| CHEMBL466586 | — | — | 1 | 7.70 |
| CHEMBL466174 | — | — | 1 | 7.70 |
| CHEMBL499534 | — | — | 1 | 7.70 |
| CHEMBL504034 | — | — | 1 | 7.50 |
| CHEMBL461869 | — | — | 1 | 7.50 |
| CHEMBL450109 | — | — | 1 | 7.50 |
| CHEMBL517585 | — | — | 1 | 7.50 |
| CHEMBL466412 | GSK-238063A | — | 1 | 7.40 |
| CHEMBL447365 | — | — | 1 | 7.40 |
| CHEMBL512076 | GSK-192082A | — | 1 | 7.37 |
| CHEMBL466175 | — | — | 1 | 7.20 |
| CHEMBL450396 | — | — | 1 | 7.20 |
| CHEMBL466615 | — | — | 1 | 7.20 |
| CHEMBL466614 | — | — | 1 | 7.20 |
| CHEMBL517123 | GSK-182497A | — | 1 | 7.17 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 7.10 |
| CHEMBL507329 | GW869810X | — | 1 | 7.08 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.57 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL180022 | NERATINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1201179 | LAPATINIB DITOSYLATE | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL461426 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL466586 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL466174 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL499534 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL504034 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL461869 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL450109 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL517585 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL466412 | GSK-238063A | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL447365 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL512076 | GSK-192082A | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL466175 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL450396 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL466615 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL466614 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL517123 | GSK-182497A | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL31965 | CANERTINIB | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL507329 | GW869810X | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL939 | GEFITINIB | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 3500.0 | nM | 5.46 |