Assay Detail
Binding
CHEMBL4052480
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST-tagged EGFR L858R/T790M double 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 | 6.54 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 9.42 |
| CHEMBL4071827 | — | — | 1 | 8.82 |
| CHEMBL4089892 | — | — | 1 | 8.08 |
| CHEMBL4061829 | — | — | 1 | 7.90 |
| CHEMBL4064224 | — | — | 1 | 7.17 |
| CHEMBL4072874 | — | — | 1 | 6.95 |
| CHEMBL4100759 | — | — | 1 | 6.58 |
| CHEMBL4090582 | — | — | 1 | 6.43 |
| CHEMBL4066951 | — | — | 1 | 6.19 |
| CHEMBL4070454 | — | — | 1 | 6.18 |
| CHEMBL4102179 | — | — | 1 | 6.17 |
| CHEMBL4097627 | — | — | 1 | 6.15 |
| CHEMBL4088971 | — | — | 1 | 6.05 |
| CHEMBL2179119 | — | — | 1 | 6.04 |
| CHEMBL4094438 | — | — | 1 | 6.04 |
| CHEMBL4077917 | — | — | 1 | 6.01 |
| CHEMBL2179128 | — | — | 1 | 5.84 |
| CHEMBL4069229 | — | — | 1 | 5.73 |
| CHEMBL4071494 | — | — | 1 | 5.48 |
| CHEMBL4077228 | — | — | 1 | 5.23 |
| CHEMBL4062617 | — | — | 1 | 4.95 |
| CHEMBL2179124 | — | — | 1 | - |
| CHEMBL4085781 | — | — | 1 | - |
| CHEMBL4078920 | — | — | 1 | - |
| CHEMBL4097718 | — | — | 1 | - |
| CHEMBL4092011 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL4071827 | — | IC50 | = | 1.52 | nM | 8.82 |
| CHEMBL4089892 | — | IC50 | = | 8.39 | nM | 8.08 |
| CHEMBL4061829 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL4064224 | — | IC50 | = | 67.9 | nM | 7.17 |
| CHEMBL4072874 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4100759 | — | IC50 | = | 263.0 | nM | 6.58 |
| CHEMBL4090582 | — | IC50 | = | 368.0 | nM | 6.43 |
| CHEMBL4066951 | — | IC50 | = | 651.0 | nM | 6.19 |
| CHEMBL4070454 | — | IC50 | = | 658.0 | nM | 6.18 |
| CHEMBL4102179 | — | IC50 | = | 683.0 | nM | 6.17 |
| CHEMBL4097627 | — | IC50 | = | 706.0 | nM | 6.15 |
| CHEMBL4088971 | — | IC50 | = | 893.0 | nM | 6.05 |
| CHEMBL2179119 | — | IC50 | = | 916.0 | nM | 6.04 |
| CHEMBL4094438 | — | IC50 | = | 908.0 | nM | 6.04 |
| CHEMBL4077917 | — | IC50 | = | 987.0 | nM | 6.01 |
| CHEMBL2179128 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL4069229 | — | IC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL4071494 | — | IC50 | = | 3310.0 | nM | 5.48 |
| CHEMBL4077228 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4062617 | — | IC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL2179124 | — | IC50 | - | — | - | |
| CHEMBL4085781 | — | IC50 | - | — | - | |
| CHEMBL4078920 | — | IC50 | - | — | - | |
| CHEMBL4097718 | — | IC50 | - | — | - | |
| CHEMBL4092011 | — | IC50 | - | — | - |