Assay Detail
Binding
CHEMBL5737541
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Biochemical EGFR Inhibition Assays (100 mM ATP): 5 μL of EGFR enzyme form in assay buffer (50 mM HEPES pH 7.3, 10 mM MgCl2, 1 mM EGTA, 0.01% Tween 20, 2 mM DTT) are dispensed into columns 1-23, than 5 μL of ATP and ULight-poly-GT substrate (PerkinElmer; TRF0100-M) mix in assay buffer is added to all wells (final assay concentration of the ULight-poly-GT substrate 200 nM). Each of the different EGFR enzyme form assays is available at high ATP levels (final assay concentration 100 μM). After 90 minutes incubation at room temperature 5 μL EDTA (final assay concentration 50 mM) and LANCE Eu-anti-P-Tyr (PT66) antibody (PerkinElmer, AD0069) (final assay concentration 6 nM) mix are added to stop the reaction and start the binding of the antibody. After additional 60 minutes incubation at room temperature the signal is measured in a PerkinElmer Envision HTS Multilabel Reader using the TR-FRET LANCE Ultra specs of PerkinElmer (used wavelengths: excitation 320 nm, emission 1 665 nm, emission 2 615 nm). Each plate contains 16 wells of a negative control (diluted DMSO instead of test compound; w EGFR enzyme form; column 23) and 16 wells of a positive control (diluted DMSO instead of test compound; w/o EGFR enzyme form; column 24). Negative and positive control values are used for normalization and IC50 values are calculated and analysed using a 4 parametric logistic model.
180
Total Activities
60
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Benzimidazole compounds and derivatives as EGFR inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 60 | 7.32 | 8.52 |
| kon | 60 | - | - |
| k_off | 60 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5994478 | — | — | 3 | 8.52 |
| CHEMBL6055515 | — | — | 3 | 8.52 |
| CHEMBL5984171 | — | — | 3 | 8.43 |
| CHEMBL5968167 | — | — | 3 | 8.38 |
| CHEMBL5998385 | — | — | 3 | 8.24 |
| CHEMBL6029813 | — | — | 3 | 8.24 |
| CHEMBL5932830 | — | — | 3 | 8.06 |
| CHEMBL5810396 | — | — | 3 | 7.99 |
| CHEMBL5790363 | — | — | 3 | 7.99 |
| CHEMBL5914292 | — | — | 3 | 7.99 |
| CHEMBL5825830 | — | — | 3 | 7.98 |
| CHEMBL5755984 | — | — | 3 | 7.95 |
| CHEMBL4532034 | — | — | 3 | 7.92 |
| CHEMBL5786240 | — | — | 3 | 7.86 |
| CHEMBL5902827 | — | — | 3 | 7.76 |
| CHEMBL6021978 | — | — | 3 | 7.73 |
| CHEMBL5976089 | — | — | 3 | 7.72 |
| CHEMBL5864704 | — | — | 3 | 7.61 |
| CHEMBL5809520 | — | — | 3 | 7.59 |
| CHEMBL5994405 | — | — | 3 | 7.56 |
| CHEMBL5772994 | — | — | 3 | 7.56 |
| CHEMBL6043073 | — | — | 3 | 7.50 |
| CHEMBL5954592 | — | — | 3 | 7.46 |
| CHEMBL6056421 | — | — | 3 | 7.46 |
| CHEMBL5897403 | — | — | 3 | 7.42 |
| CHEMBL5195167 | — | — | 3 | 7.40 |
| CHEMBL5959712 | — | — | 3 | 7.40 |
| CHEMBL6007714 | — | — | 3 | 7.34 |
| CHEMBL5840868 | — | — | 3 | 7.21 |
| CHEMBL5893361 | — | — | 3 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6055515 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5994478 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5984171 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5968167 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL6029813 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL5998385 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5932830 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL5914292 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL5790363 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL5810396 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL5825830 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL5755984 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL4532034 | — | IC50 | = | 11.9 | nM | 7.92 |
| CHEMBL5786240 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL5902827 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL6021978 | — | IC50 | = | 18.6 | nM | 7.73 |
| CHEMBL5976089 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5864704 | — | IC50 | = | 24.3 | nM | 7.61 |
| CHEMBL5809520 | — | IC50 | = | 25.5 | nM | 7.59 |
| CHEMBL5772994 | — | IC50 | = | 27.7 | nM | 7.56 |
| CHEMBL5994405 | — | IC50 | = | 27.7 | nM | 7.56 |
| CHEMBL6043073 | — | IC50 | = | 31.6 | nM | 7.50 |
| CHEMBL6056421 | — | IC50 | = | 34.5 | nM | 7.46 |
| CHEMBL5954592 | — | IC50 | = | 34.8 | nM | 7.46 |
| CHEMBL5897403 | — | IC50 | = | 38.5 | nM | 7.42 |
| CHEMBL5959712 | — | IC50 | = | 39.6 | nM | 7.40 |
| CHEMBL5195167 | — | IC50 | = | 40.1 | nM | 7.40 |
| CHEMBL6007714 | — | IC50 | = | 45.7 | nM | 7.34 |
| CHEMBL5840868 | — | IC50 | = | 61.7 | nM | 7.21 |
| CHEMBL5893361 | — | IC50 | = | 64.6 | nM | 7.19 |
| CHEMBL5960825 | — | IC50 | = | 67.4 | nM | 7.17 |
| CHEMBL5872035 | — | IC50 | = | 76.5 | nM | 7.12 |
| CHEMBL6015235 | — | IC50 | = | 78.2 | nM | 7.11 |
| CHEMBL5865007 | — | IC50 | = | 79.3 | nM | 7.10 |
| CHEMBL5891448 | — | IC50 | = | 86.9 | nM | 7.06 |
| CHEMBL5829030 | — | IC50 | = | 91.6 | nM | 7.04 |
| CHEMBL5865099 | — | IC50 | = | 94.1 | nM | 7.03 |
| CHEMBL5963945 | — | IC50 | = | 94.6 | nM | 7.02 |
| CHEMBL5911542 | — | IC50 | = | 95.2 | nM | 7.02 |
| CHEMBL5932930 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL5861020 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL5832255 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5985978 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5783119 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL5925024 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL5784511 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL5834325 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL5945119 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL6048747 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL5750984 | — | IC50 | = | 178.0 | nM | 6.75 |