Assay Detail
Binding
CHEMBL4681994
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST-tagged MAP4K4 catalytic domain (1 to 328 residues) expressed in baculovirus expression system pre-incubated for 30 mins before Ser/Thr 07 peptide substrate and 10 uM ATP addition and further incubated for 90 mins by Z'-lyte assay
42
Total Activities
42
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 |
Target
Mitogen-activated protein kinase kinase kinase kinase 4 (CHEMBL6166) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2-Aminopyridine-Based Mitogen-Activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4) Inhibitors: Assessment of Mechanism-Based Safety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 8.14 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4746566 | — | — | 1 | 9.40 |
| CHEMBL4787152 | — | — | 1 | 9.22 |
| CHEMBL4759743 | — | — | 1 | 9.00 |
| CHEMBL4750540 | — | — | 1 | 8.89 |
| CHEMBL4783711 | — | — | 1 | 8.85 |
| CHEMBL4781045 | — | — | 1 | 8.85 |
| CHEMBL4779507 | — | — | 1 | 8.70 |
| CHEMBL4740167 | — | — | 1 | 8.70 |
| CHEMBL4787142 | — | — | 1 | 8.70 |
| CHEMBL4745446 | — | — | 1 | 8.68 |
| CHEMBL4751017 | — | — | 1 | 8.62 |
| CHEMBL4757082 | — | — | 1 | 8.62 |
| CHEMBL4777705 | — | — | 1 | 8.54 |
| CHEMBL4800212 | — | — | 1 | 8.46 |
| CHEMBL4788172 | — | — | 1 | 8.46 |
| CHEMBL4760299 | — | — | 1 | 8.46 |
| CHEMBL3754515 | — | — | 1 | 8.43 |
| CHEMBL4790042 | — | — | 1 | 8.40 |
| CHEMBL3753424 | — | — | 1 | 8.39 |
| CHEMBL4778859 | — | — | 1 | 8.34 |
| CHEMBL4780690 | — | — | 1 | 8.25 |
| CHEMBL4741486 | — | — | 1 | 8.22 |
| CHEMBL4780287 | — | — | 1 | 8.19 |
| CHEMBL4753817 | — | — | 1 | 8.14 |
| CHEMBL4740781 | — | — | 1 | 8.12 |
| CHEMBL4757382 | — | — | 1 | 8.12 |
| CHEMBL4756318 | — | — | 1 | 8.10 |
| CHEMBL4793121 | — | — | 1 | 8.09 |
| CHEMBL4787865 | — | — | 1 | 7.96 |
| CHEMBL4756492 | — | — | 1 | 7.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4746566 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4787152 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4759743 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4750540 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4783711 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4781045 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4779507 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4740167 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4787142 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4745446 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4751017 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4757082 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4777705 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4760299 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4788172 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4800212 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3754515 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4790042 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3753424 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4778859 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4780690 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4741486 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4780287 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4753817 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4740781 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4757382 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4756318 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4793121 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL4787865 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4756492 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4797557 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4788138 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4790014 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3754123 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4750571 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4799332 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4750380 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4749078 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3753371 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4743812 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL4741143 | — | IC50 | = | 1426.0 | nM | 5.85 |
| CHEMBL4764356 | — | IC50 | = | 1421.0 | nM | 5.85 |