Assay Detail
Binding
CHEMBL5735192
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinase Activity Inhibition Assay: Inhibition of ASK1 kinase activity was determined radiometrically using 33P substrate incorporation (Reaction Biology Corp., Malvern, Pa.). Briefly, recombinant human ASK1 protein, 20 μM substrate (myelin basic protein (MBP)), and compound (diluted from DMSO stock to give 1% final DMSO) were incubated in Base Reaction buffer (20 mM Hepes (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, 1% DMSO) at room temperature for 20 minutes. The reaction was initiated by addition of 10 μM 33P-ATP (specific activity 10 μCi/4l). The reaction was then allowed to proceed for 2 hours at room temperature. Upon reaction termination, the mixture was spotted on P81 exchange paper and kinase activity by incorporation of 33P into MBP substrate was detected by filter-binding method.
276
Total Activities
90
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Mitogen-activated protein kinase kinase kinase 5 (CHEMBL5285) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
ASK1 isoindolin-1-one inhibitors and methods of use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 92 | 8.22 | 9.52 |
| kon | 92 | - | - |
| k_off | 92 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5787727 | — | — | 3 | 9.52 |
| CHEMBL5946199 | — | — | 3 | 9.15 |
| CHEMBL5967167 | — | — | 3 | 8.80 |
| CHEMBL5795972 | — | — | 3 | 8.80 |
| CHEMBL5841486 | — | — | 3 | 8.74 |
| CHEMBL5746635 | — | — | 3 | 8.72 |
| CHEMBL5985747 | — | — | 3 | 8.68 |
| CHEMBL5879519 | — | — | 3 | 8.60 |
| CHEMBL6060824 | — | — | 3 | 8.59 |
| CHEMBL6057773 | — | — | 3 | 8.55 |
| CHEMBL5775165 | — | — | 3 | 8.55 |
| CHEMBL5865443 | — | — | 3 | 8.49 |
| CHEMBL6022506 | — | — | 3 | 8.48 |
| CHEMBL5862012 | — | — | 6 | 8.48 |
| CHEMBL6019733 | — | — | 3 | 8.47 |
| CHEMBL5886893 | — | — | 3 | 8.46 |
| CHEMBL5895853 | — | — | 3 | 8.44 |
| CHEMBL5771353 | — | — | 3 | 8.41 |
| CHEMBL5782592 | — | — | 3 | 8.40 |
| CHEMBL5819333 | — | — | 3 | 8.39 |
| CHEMBL5868776 | — | — | 3 | 8.37 |
| CHEMBL6058001 | — | — | 3 | 8.37 |
| CHEMBL5914977 | — | — | 3 | 8.37 |
| CHEMBL5804541 | — | — | 3 | 8.36 |
| CHEMBL5750805 | — | — | 3 | 8.34 |
| CHEMBL5908319 | — | — | 3 | 8.34 |
| CHEMBL6049786 | — | — | 3 | 8.34 |
| CHEMBL5876473 | — | — | 3 | 8.33 |
| CHEMBL5906116 | — | — | 3 | 8.33 |
| CHEMBL5939633 | — | — | 3 | 8.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5787727 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5946199 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5795972 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5967167 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5841486 | — | IC50 | = | 1.83 | nM | 8.74 |
| CHEMBL5746635 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5985747 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5879519 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL6060824 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5775165 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL6057773 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5865443 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL6022506 | — | IC50 | = | 3.28 | nM | 8.48 |
| CHEMBL5862012 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL6019733 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5886893 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5895853 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5771353 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5782592 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5819333 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL6058001 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5914977 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5868776 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5804541 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL6049786 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5908319 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5750805 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5939633 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5876473 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5906116 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5857821 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL5794733 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL5758560 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL6010208 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL5787566 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL6041520 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL6029058 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL5808077 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL5987742 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL5780163 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5765172 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL5932507 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5963745 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5909721 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5792360 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL6041862 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL5880765 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5862012 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5976849 | — | IC50 | = | 5.44 | nM | 8.26 |
| CHEMBL6031940 | — | IC50 | = | 5.52 | nM | 8.26 |