Assay Detail
Binding
CHEMBL5737540
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Biochemical EGFR Inhibition Assays (5 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 low ATP (final assay concentration 5 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.
249
Total Activities
80
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 | 83 | 8.48 | 9.52 |
| kon | 83 | - | - |
| k_off | 83 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5832595 | — | — | 3 | 9.52 |
| CHEMBL6029813 | — | — | 3 | 9.40 |
| CHEMBL5969707 | — | — | 3 | 9.40 |
| CHEMBL5755058 | — | — | 3 | 9.40 |
| CHEMBL5993712 | — | — | 3 | 9.30 |
| CHEMBL5932830 | — | — | 3 | 9.30 |
| CHEMBL6023158 | — | — | 3 | 9.22 |
| CHEMBL5790363 | — | — | 3 | 9.22 |
| CHEMBL5756022 | — | — | 3 | 9.15 |
| CHEMBL5843126 | — | — | 6 | 9.15 |
| CHEMBL5788210 | — | — | 3 | 9.15 |
| CHEMBL5914292 | — | — | 3 | 9.15 |
| CHEMBL6043073 | — | — | 6 | 9.10 |
| CHEMBL6027769 | — | — | 3 | 9.10 |
| CHEMBL5825830 | — | — | 3 | 9.10 |
| CHEMBL5920247 | — | — | 3 | 9.05 |
| CHEMBL6020978 | — | — | 3 | 9.05 |
| CHEMBL5786240 | — | — | 3 | 9.00 |
| CHEMBL6057405 | — | — | 3 | 9.00 |
| CHEMBL5800758 | — | — | 3 | 8.92 |
| CHEMBL5887634 | — | — | 3 | 8.85 |
| CHEMBL5969655 | — | — | 3 | 8.82 |
| CHEMBL5959712 | — | — | 3 | 8.82 |
| CHEMBL5195167 | — | — | 3 | 8.80 |
| CHEMBL5749996 | — | — | 3 | 8.77 |
| CHEMBL6057006 | — | — | 3 | 8.77 |
| CHEMBL5828125 | — | — | 3 | 8.74 |
| CHEMBL6007714 | — | — | 3 | 8.74 |
| CHEMBL5985978 | — | — | 3 | 8.72 |
| CHEMBL5893361 | — | — | 3 | 8.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5832595 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5969707 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5755058 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL6029813 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5993712 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5932830 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL6023158 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5790363 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5756022 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5843126 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5788210 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5914292 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5843126 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL6027769 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL6043073 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL6043073 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5825830 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL6020978 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5920247 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL6057405 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5786240 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5800758 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5887634 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5959712 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5969655 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5195167 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5749996 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL6057006 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5828125 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL6007714 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5985978 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5893361 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5838821 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5948958 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL6025269 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5996878 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL6060232 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5782254 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5880562 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5944318 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5863443 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5770970 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5861063 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5861063 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5998521 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL6001037 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5783119 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5785378 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5894059 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5905751 | — | IC50 | = | 4.3 | nM | 8.37 |