Assay Detail
Binding
CHEMBL4714732
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full-length His-tagged TAK1-TAB1 fusion protein (437 to 504 residues) expressed in baculovirus expression system using fluorescein-MAP2K1 as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins in presence of ATP by lanthascreen TR-FRET assay
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of 2,4-1H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 6.05 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4796239 | — | — | 1 | 8.70 |
| CHEMBL4752978 | — | — | 1 | 8.30 |
| CHEMBL2408611 | — | — | 1 | 8.00 |
| CHEMBL3823738 | — | — | 1 | 7.52 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.41 |
| CHEMBL4795442 | — | — | 1 | 6.52 |
| CHEMBL4786426 | — | — | 1 | 6.52 |
| CHEMBL4799816 | — | — | 1 | 6.30 |
| CHEMBL4743586 | — | — | 1 | 6.05 |
| CHEMBL4793594 | — | — | 1 | 6.05 |
| CHEMBL4753680 | — | — | 1 | 6.00 |
| CHEMBL4784347 | — | — | 1 | 5.92 |
| CHEMBL4754286 | — | — | 1 | 5.92 |
| CHEMBL4787765 | — | — | 1 | 5.89 |
| CHEMBL4748960 | — | — | 1 | 5.77 |
| CHEMBL4742800 | — | — | 1 | 5.75 |
| CHEMBL4787363 | — | — | 1 | 5.75 |
| CHEMBL4764405 | — | — | 1 | 5.64 |
| CHEMBL4760000 | — | — | 1 | 5.58 |
| CHEMBL4790917 | — | — | 1 | 5.58 |
| CHEMBL4779445 | — | — | 1 | 5.55 |
| CHEMBL4742896 | — | — | 1 | 5.54 |
| CHEMBL4758712 | — | — | 1 | 5.50 |
| CHEMBL4740886 | — | — | 1 | 5.47 |
| CHEMBL4776433 | — | — | 1 | 5.47 |
| CHEMBL4785659 | — | — | 1 | 5.46 |
| CHEMBL4760703 | — | — | 1 | 5.35 |
| CHEMBL4785897 | — | — | 1 | 5.24 |
| CHEMBL4758714 | — | — | 1 | 4.58 |
| CHEMBL4750042 | — | — | 1 | 4.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4796239 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4752978 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2408611 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3823738 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4795442 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4786426 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4799816 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4743586 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4793594 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4753680 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4754286 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4784347 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4787765 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4748960 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4742800 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4787363 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4764405 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4760000 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4790917 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4779445 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4742896 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4758712 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4776433 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4740886 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4785659 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4760703 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4785897 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4758714 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4750042 | — | IC50 | = | 59000.0 | nM | 4.23 |
| CHEMBL4792942 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4746806 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4763165 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4777281 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4751348 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4763783 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4778091 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4763081 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4762449 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4746405 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4789883 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4781976 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4785563 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4741059 | — | IC50 | > | 10000.0 | nM | - |