Assay Detail
Binding
CHEMBL1924801
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Inhibition of human N-terminus peptide (DYKDDDD)-tagged EGFR expressed in baculovirus infected insect cells using [gamma-32P]ATP as substrate after 60 mins by scintillation counting
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 7.31 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1923009 | — | — | 1 | 8.24 |
| CHEMBL1923022 | — | — | 1 | 8.14 |
| CHEMBL1923000 | — | — | 1 | 8.11 |
| CHEMBL1923003 | — | — | 1 | 8.04 |
| CHEMBL1923006 | — | — | 1 | 8.02 |
| CHEMBL1923019 | — | — | 1 | 8.00 |
| CHEMBL1923010 | — | — | 1 | 7.82 |
| CHEMBL1923020 | — | — | 1 | 7.82 |
| CHEMBL1923001 | — | — | 1 | 7.75 |
| CHEMBL1922999 | — | — | 1 | 7.70 |
| CHEMBL1923013 | — | — | 1 | 7.66 |
| CHEMBL1614725 | TAK-285 | 1.0 | 1 | 7.64 |
| CHEMBL1923004 | — | — | 1 | 7.57 |
| CHEMBL1922900 | — | — | 1 | 7.57 |
| CHEMBL1923015 | — | — | 1 | 7.51 |
| CHEMBL1923012 | — | — | 1 | 7.48 |
| CHEMBL1923007 | — | — | 1 | 7.47 |
| CHEMBL1923021 | — | — | 1 | 7.46 |
| CHEMBL1921812 | — | — | 1 | 7.46 |
| CHEMBL1923017 | — | — | 1 | 7.42 |
| CHEMBL1923016 | — | — | 1 | 7.40 |
| CHEMBL1923014 | — | — | 1 | 7.36 |
| CHEMBL1923011 | — | — | 1 | 7.31 |
| CHEMBL1923005 | — | — | 1 | 7.30 |
| CHEMBL1922901 | — | — | 1 | 7.29 |
| CHEMBL1922898 | — | — | 1 | 7.21 |
| CHEMBL1922905 | — | — | 1 | 7.17 |
| CHEMBL1923008 | — | — | 1 | 6.96 |
| CHEMBL1922897 | — | — | 1 | 6.96 |
| CHEMBL1922904 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1923009 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL1923022 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL1923000 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL1923003 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL1923006 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL1923019 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1923010 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1923020 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1923001 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1922999 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1923013 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1614725 | TAK-285 | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1923004 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1922900 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1923015 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1923012 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1923007 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1923021 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1921812 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1923017 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL1923016 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1923014 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL1923011 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL1923005 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1922901 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL1922898 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL1922905 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL1923008 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1922897 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1922904 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1922899 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1922902 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1922906 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1922998 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1923018 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1921813 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL1614726 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL1922903 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL1923002 | — | IC50 | = | 1900.0 | nM | 5.72 |