Assay Detail
Binding
CHEMBL1686142
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Inhibition of HER2 by homogeneous time-resolved fluorescence assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.31 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201179 | LAPATINIB DITOSYLATE | 4.0 | 1 | 8.05 |
| CHEMBL1683967 | — | — | 1 | 7.72 |
| CHEMBL1683974 | — | — | 1 | 7.44 |
| CHEMBL1683972 | — | — | 1 | 7.16 |
| CHEMBL1683968 | — | — | 1 | 7.15 |
| CHEMBL1683970 | — | — | 1 | 7.13 |
| CHEMBL1683965 | — | — | 1 | 7.11 |
| CHEMBL1683963 | — | — | 1 | 7.09 |
| CHEMBL1683973 | — | — | 1 | 7.02 |
| CHEMBL1683969 | — | — | 1 | 6.99 |
| CHEMBL1683955 | — | — | 1 | 6.85 |
| CHEMBL1683961 | — | — | 1 | 6.82 |
| CHEMBL1683964 | — | — | 1 | 6.72 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 6.62 |
| CHEMBL1683966 | — | — | 1 | 6.50 |
| CHEMBL1683962 | — | — | 1 | 6.36 |
| CHEMBL1683958 | — | — | 1 | 6.13 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.12 |
| CHEMBL1683975 | — | — | 1 | 6.09 |
| CHEMBL1683959 | — | — | 1 | 5.75 |
| CHEMBL1683956 | — | — | 1 | 5.54 |
| CHEMBL1683960 | — | — | 1 | 5.43 |
| CHEMBL1683971 | — | — | 1 | 5.27 |
| CHEMBL1683950 | — | — | 1 | 5.20 |
| CHEMBL1683949 | — | — | 1 | 5.19 |
| CHEMBL205652 | — | — | 1 | 4.60 |
| CHEMBL1683952 | — | — | 1 | 4.44 |
| CHEMBL1683957 | — | — | 1 | 4.19 |
| CHEMBL1683954 | — | — | 1 | - |
| CHEMBL1683953 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201179 | LAPATINIB DITOSYLATE | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1683967 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1683974 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1683972 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1683968 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL1683970 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL1683965 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL1683963 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL1683973 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL1683969 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL1683955 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1683961 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1683964 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL939 | GEFITINIB | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1683966 | — | IC50 | = | 318.0 | nM | 6.50 |
| CHEMBL1683962 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1683958 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL1683975 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL1683959 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1683956 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL1683960 | — | IC50 | = | 3750.0 | nM | 5.43 |
| CHEMBL1683971 | — | IC50 | = | 5380.0 | nM | 5.27 |
| CHEMBL1683950 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL1683949 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL205652 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL1683952 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL1683957 | — | IC50 | = | 65000.0 | nM | 4.19 |
| CHEMBL1683954 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1683953 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1683951 | — | IC50 | > | 100000.0 | nM | - |