Assay Detail
Binding
CHEMBL1686143
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Inhibition of EGFR 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 |
Publication
Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.89 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 9.00 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 9.00 |
| CHEMBL1683967 | — | — | 1 | 8.52 |
| CHEMBL1683974 | — | — | 1 | 8.05 |
| CHEMBL1201179 | LAPATINIB DITOSYLATE | 4.0 | 1 | 8.00 |
| CHEMBL1683973 | — | — | 1 | 7.96 |
| CHEMBL1683970 | — | — | 1 | 7.89 |
| CHEMBL1683955 | — | — | 1 | 7.77 |
| CHEMBL1683965 | — | — | 1 | 7.75 |
| CHEMBL1683968 | — | — | 1 | 7.72 |
| CHEMBL1683963 | — | — | 1 | 7.55 |
| CHEMBL1683961 | — | — | 1 | 7.47 |
| CHEMBL1683972 | — | — | 1 | 7.42 |
| CHEMBL1683959 | — | — | 1 | 7.19 |
| CHEMBL1683958 | — | — | 1 | 7.17 |
| CHEMBL1683966 | — | — | 1 | 6.94 |
| CHEMBL1683964 | — | — | 1 | 6.92 |
| CHEMBL1683969 | — | — | 1 | 6.81 |
| CHEMBL1683962 | — | — | 1 | 6.62 |
| CHEMBL1683975 | — | — | 1 | 6.57 |
| CHEMBL1683960 | — | — | 1 | 6.23 |
| CHEMBL1683956 | — | — | 1 | 6.19 |
| CHEMBL205652 | — | — | 1 | 6.04 |
| CHEMBL1683949 | — | — | 1 | 5.96 |
| CHEMBL1683950 | — | — | 1 | 5.92 |
| CHEMBL1683971 | — | — | 1 | 5.38 |
| CHEMBL1683954 | — | — | 1 | 5.00 |
| CHEMBL1683957 | — | — | 1 | 4.70 |
| CHEMBL1683952 | — | — | 1 | 4.66 |
| CHEMBL1683951 | — | — | 1 | 4.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1683967 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1683974 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1201179 | LAPATINIB DITOSYLATE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1683973 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1683970 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1683955 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1683965 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1683968 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1683963 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1683961 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1683972 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL1683959 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1683958 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL1683966 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL1683964 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1683969 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL1683962 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1683975 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1683960 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL1683956 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL205652 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL1683949 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1683950 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1683971 | — | IC50 | = | 4130.0 | nM | 5.38 |
| CHEMBL1683954 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1683957 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL1683952 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL1683951 | — | IC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL1683953 | — | IC50 | > | 100000.0 | nM | - |