Assay Detail
Binding
CHEMBL5736794
Review assay metadata, readout intent, target linkage, and publication context from the same page.
ERK2 In vitro Inhibition Assay: Activity of ERK2 enzyme (Life Technologies) was determined using a time-resolved fluorescence format measuring the phosphorylation of a truncated version of Activating transcription factor 2 labelled with green fluorescent protein (ATF2-GFP) (Life Technologies). Assay reactions containing 50 mM Tris pH 7.5, 10 mM MgC2, 1 mM EGTA, 0.01% Triton X-100, 1 mM DTT, 2.5% DMSO, 0.4 μM ATF2-GFP, 20 μM ATP and 0.25 nM ERK2 were set up in the presence of compound and allowed to proceed for 30 min at room temperature. Reactions were then stopped using TR-FRET dilution buffer (Life Technologies), 25 mM EDTA and 2 nM Tb-Anti-pATF2 (Thr71) (Life Technologies). After a further incubation period of at least 30 minutes, fluorescence was read on a Pherastar reader (Lanthascreen optic module; excitation 340 nm, emission 520 nm (channel A), 495 nm (channel B)). The ratio between A and B counts was used to calculate signal. IC50 values were calculated using a sigmoidal dose response equation (Prism GraphPad software, La Jolla, Calif., USA).In the assays using ERK2, the compounds of Examples 125, 127, 162, 181, 183, 289, 299, 310 and 939 have IC50 values in the range from 1 μM to 10 μM, provide at least 50% inhibition of the activity at a concentration of 10 μM in the assay against ERK2 or would be expected to provide at least 50% inhibition of the activity at a concentration of 10 μM (based on the level of inhibition of the activity at concentrations of 3 μM) in the assay against ERK2.
2769
Total Activities
899
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Benzolactam compounds as protein kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 923 | 7.84 | 8.96 |
| kon | 923 | - | - |
| k_off | 923 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4871302 | — | — | 3 | 8.96 |
| CHEMBL4849148 | — | — | 3 | 8.92 |
| CHEMBL5952643 | — | — | 9 | 8.89 |
| CHEMBL4847212 | — | — | 3 | 8.89 |
| CHEMBL5930683 | — | — | 3 | 8.89 |
| CHEMBL5883529 | — | — | 3 | 8.85 |
| CHEMBL5875401 | — | — | 3 | 8.85 |
| CHEMBL5776683 | — | — | 6 | 8.82 |
| CHEMBL6019688 | — | — | 3 | 8.82 |
| CHEMBL5812423 | — | — | 3 | 8.82 |
| CHEMBL5886204 | — | — | 3 | 8.82 |
| CHEMBL6034338 | — | — | 3 | 8.82 |
| CHEMBL5822851 | — | — | 3 | 8.80 |
| CHEMBL5923573 | — | — | 3 | 8.80 |
| CHEMBL5746376 | — | — | 3 | 8.80 |
| CHEMBL5760842 | — | — | 3 | 8.80 |
| CHEMBL5774206 | — | — | 3 | 8.80 |
| CHEMBL5860427 | — | — | 3 | 8.80 |
| CHEMBL6046631 | — | — | 3 | 8.80 |
| CHEMBL5979676 | — | — | 3 | 8.77 |
| CHEMBL5965263 | — | — | 3 | 8.77 |
| CHEMBL5905526 | — | — | 3 | 8.77 |
| CHEMBL5918274 | — | — | 3 | 8.77 |
| CHEMBL5903955 | — | — | 3 | 8.77 |
| CHEMBL5857382 | — | — | 3 | 8.77 |
| CHEMBL5788880 | — | — | 3 | 8.77 |
| CHEMBL5803384 | — | — | 3 | 8.77 |
| CHEMBL5788403 | — | — | 3 | 8.77 |
| CHEMBL5900929 | — | — | 3 | 8.77 |
| CHEMBL5823208 | — | — | 3 | 8.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4871302 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4849148 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5952643 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4847212 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5930683 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5875401 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5883529 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5812423 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL6019688 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5776683 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5886204 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL6034338 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5822851 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5774206 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5760842 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5746376 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5860427 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL6046631 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5923573 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5965263 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5788880 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5903955 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5803384 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5900929 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5776683 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5788403 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5905526 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5857382 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5979676 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5918274 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4857389 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5823208 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL6064867 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5961403 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5768700 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5929439 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5933836 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5813710 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5929791 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4865318 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5754931 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5958179 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5860624 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL6001381 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5907157 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5783614 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5888852 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5961659 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5999598 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5796891 | — | IC50 | = | 2.0 | nM | 8.70 |