Assay Detail
Binding
CHEMBL4769103
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His6-tagged AMPK alpha1 using ULight CRBtide as substrate incubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET assay
21
Total Activities
21
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
5'-AMP-activated protein kinase catalytic subunit alpha-1 (CHEMBL4045) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.66 | 7.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4794096 | — | — | 1 | 7.03 |
| CHEMBL4781578 | — | — | 1 | 6.97 |
| CHEMBL13976 | — | — | 1 | 6.87 |
| CHEMBL4796639 | — | — | 1 | 6.86 |
| CHEMBL4788980 | — | — | 1 | 6.82 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.80 |
| CHEMBL4788376 | — | — | 1 | 6.79 |
| CHEMBL4800500 | — | — | 1 | 6.76 |
| CHEMBL3542344 | — | — | 1 | 6.75 |
| CHEMBL4795330 | — | — | 1 | 6.74 |
| CHEMBL4792246 | — | — | 1 | 6.69 |
| CHEMBL4782796 | — | — | 1 | 6.68 |
| CHEMBL4799580 | — | — | 1 | 6.66 |
| CHEMBL4786972 | — | — | 1 | 6.66 |
| CHEMBL4779166 | — | — | 1 | 6.62 |
| CHEMBL275117 | — | — | 1 | 6.61 |
| CHEMBL4781062 | — | — | 1 | 6.53 |
| CHEMBL4785831 | — | — | 1 | 6.46 |
| CHEMBL3542333 | — | — | 1 | 6.41 |
| CHEMBL4799631 | — | — | 1 | 6.38 |
| CHEMBL4779730 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4794096 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4781578 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL13976 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4796639 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL4788980 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL535 | SUNITINIB | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL4788376 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL4800500 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL3542344 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4795330 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL4792246 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL4782796 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL4799580 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL4786972 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL4779166 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL275117 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL4781062 | — | IC50 | = | 296.0 | nM | 6.53 |
| CHEMBL4785831 | — | IC50 | = | 348.0 | nM | 6.46 |
| CHEMBL3542333 | — | IC50 | = | 393.0 | nM | 6.41 |
| CHEMBL4799631 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL4779730 | — | IC50 | = | 2100.0 | nM | 5.68 |