Assay Detail
Binding
CHEMBL4052479
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST-tagged EGFR L858R mutant cytoplasmic domain expressed in baculovirus expression system preincubated for 20 mins followed by addition of [33P]-ATP measured after 2 hrs by filter-binding method
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.19 | 8.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4090582 | — | — | 1 | 8.13 |
| CHEMBL4072874 | — | — | 1 | 8.11 |
| CHEMBL4070454 | — | — | 1 | 7.95 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.94 |
| CHEMBL4100759 | — | — | 1 | 7.89 |
| CHEMBL4066951 | — | — | 1 | 7.81 |
| CHEMBL4077917 | — | — | 1 | 7.73 |
| CHEMBL4097627 | — | — | 1 | 7.63 |
| CHEMBL2179119 | — | — | 1 | 7.62 |
| CHEMBL4088971 | — | — | 1 | 7.61 |
| CHEMBL4094438 | — | — | 1 | 7.49 |
| CHEMBL4102179 | — | — | 1 | 7.47 |
| CHEMBL2179128 | — | — | 1 | 6.99 |
| CHEMBL4078920 | — | — | 1 | 6.59 |
| CHEMBL4077228 | — | — | 1 | 6.55 |
| CHEMBL4069229 | — | — | 1 | 6.53 |
| CHEMBL4064224 | — | — | 1 | 6.34 |
| CHEMBL2179124 | — | — | 1 | 6.20 |
| CHEMBL4071494 | — | — | 1 | 5.89 |
| CHEMBL4062617 | — | — | 1 | 5.41 |
| CHEMBL4061829 | — | — | 1 | - |
| CHEMBL4089892 | — | — | 1 | - |
| CHEMBL4085781 | — | — | 1 | - |
| CHEMBL4071827 | — | — | 1 | - |
| CHEMBL4097718 | — | — | 1 | - |
| CHEMBL4092011 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4090582 | — | IC50 | = | 7.41 | nM | 8.13 |
| CHEMBL4072874 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4070454 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL4100759 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4066951 | — | IC50 | = | 15.4 | nM | 7.81 |
| CHEMBL4077917 | — | IC50 | = | 18.7 | nM | 7.73 |
| CHEMBL4097627 | — | IC50 | = | 23.6 | nM | 7.63 |
| CHEMBL2179119 | — | IC50 | = | 24.1 | nM | 7.62 |
| CHEMBL4088971 | — | IC50 | = | 24.4 | nM | 7.61 |
| CHEMBL4094438 | — | IC50 | = | 32.1 | nM | 7.49 |
| CHEMBL4102179 | — | IC50 | = | 34.2 | nM | 7.47 |
| CHEMBL2179128 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4078920 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL4077228 | — | IC50 | = | 279.0 | nM | 6.55 |
| CHEMBL4069229 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL4064224 | — | IC50 | = | 459.0 | nM | 6.34 |
| CHEMBL2179124 | — | IC50 | = | 631.0 | nM | 6.20 |
| CHEMBL4071494 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4062617 | — | IC50 | = | 3920.0 | nM | 5.41 |
| CHEMBL4061829 | — | IC50 | < | 0.3 | nM | - |
| CHEMBL4089892 | — | IC50 | < | 0.3 | nM | - |
| CHEMBL4085781 | — | IC50 | - | — | - | |
| CHEMBL4071827 | — | IC50 | < | 0.3 | nM | - |
| CHEMBL4097718 | — | IC50 | - | — | - | |
| CHEMBL4092011 | — | IC50 | - | — | - |