Assay Detail
Binding
CHEMBL4681995
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Inhibition of MAP4K4 in human GripTite 293 MSR cells assessed as reduction in TRAF2 Ser/Thr phosphorylation incubated for 1.5 hrs by ELISA
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 41 | 6.11 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4787142 | — | — | 1 | 7.00 |
| CHEMBL4783711 | — | — | 1 | 6.99 |
| CHEMBL4778859 | — | — | 1 | 6.83 |
| CHEMBL3754515 | — | — | 1 | 6.80 |
| CHEMBL4750540 | — | — | 1 | 6.71 |
| CHEMBL4746566 | — | — | 1 | 6.65 |
| CHEMBL4760299 | — | — | 1 | 6.64 |
| CHEMBL4788172 | — | — | 1 | 6.61 |
| CHEMBL4757082 | — | — | 1 | 6.56 |
| CHEMBL4777705 | — | — | 1 | 6.48 |
| CHEMBL4800212 | — | — | 1 | 6.42 |
| CHEMBL4781045 | — | — | 1 | 6.39 |
| CHEMBL3754123 | — | — | 1 | 6.33 |
| CHEMBL4780287 | — | — | 1 | 6.33 |
| CHEMBL4787152 | — | — | 1 | 6.33 |
| CHEMBL4741486 | — | — | 1 | 6.31 |
| CHEMBL4740167 | — | — | 1 | 6.25 |
| CHEMBL4793121 | — | — | 1 | 6.22 |
| CHEMBL4759743 | — | — | 1 | 6.08 |
| CHEMBL4751017 | — | — | 1 | 6.03 |
| CHEMBL4757382 | — | — | 1 | 5.99 |
| CHEMBL4740781 | — | — | 1 | 5.99 |
| CHEMBL4750571 | — | — | 1 | 5.98 |
| CHEMBL3753371 | — | — | 1 | 5.95 |
| CHEMBL3753424 | — | — | 1 | 5.93 |
| CHEMBL4797557 | — | — | 1 | 5.88 |
| CHEMBL4780690 | — | — | 1 | 5.80 |
| CHEMBL4788138 | — | — | 1 | 5.77 |
| CHEMBL4787865 | — | — | 1 | 5.73 |
| CHEMBL4745446 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4787142 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4783711 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL4778859 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL3754515 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4750540 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL4746566 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL4760299 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL4788172 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL4757082 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL4777705 | — | IC50 | = | 331.0 | nM | 6.48 |
| CHEMBL4800212 | — | IC50 | = | 377.0 | nM | 6.42 |
| CHEMBL4781045 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL3754123 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4780287 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4787152 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL4741486 | — | IC50 | = | 491.0 | nM | 6.31 |
| CHEMBL4740167 | — | IC50 | = | 564.0 | nM | 6.25 |
| CHEMBL4793121 | — | IC50 | = | 602.0 | nM | 6.22 |
| CHEMBL4759743 | — | IC50 | = | 842.0 | nM | 6.08 |
| CHEMBL4751017 | — | IC50 | = | 935.0 | nM | 6.03 |
| CHEMBL4757382 | — | IC50 | = | 1019.0 | nM | 5.99 |
| CHEMBL4740781 | — | IC50 | = | 1019.0 | nM | 5.99 |
| CHEMBL4750571 | — | IC50 | = | 1052.0 | nM | 5.98 |
| CHEMBL3753371 | — | IC50 | = | 1121.0 | nM | 5.95 |
| CHEMBL3753424 | — | IC50 | = | 1182.0 | nM | 5.93 |
| CHEMBL4797557 | — | IC50 | = | 1308.0 | nM | 5.88 |
| CHEMBL4780690 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL4788138 | — | IC50 | = | 1692.0 | nM | 5.77 |
| CHEMBL4787865 | — | IC50 | = | 1852.0 | nM | 5.73 |
| CHEMBL4745446 | — | IC50 | = | 2018.0 | nM | 5.70 |
| CHEMBL4799332 | — | IC50 | = | 3148.0 | nM | 5.50 |
| CHEMBL4753817 | — | IC50 | = | 3391.0 | nM | 5.47 |
| CHEMBL4756492 | — | IC50 | = | 4006.0 | nM | 5.40 |
| CHEMBL4764356 | — | IC50 | = | 4699.0 | nM | 5.33 |
| CHEMBL4790042 | — | IC50 | = | 5388.0 | nM | 5.27 |
| CHEMBL4779507 | — | IC50 | = | 5574.0 | nM | 5.25 |
| CHEMBL4756318 | — | IC50 | = | 8728.0 | nM | 5.06 |
| CHEMBL4750380 | — | IC50 | > | 8500.0 | nM | - |
| CHEMBL4790014 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4743812 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4749078 | — | IC50 | > | 10000.0 | nM | - |