Assay Detail
Binding
CHEMBL862611
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Akt1 at 10 uM ATP
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
RAC-alpha serine/threonine-protein kinase (CHEMBL4282) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 5.82 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL383264 | — | — | 1 | 8.89 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.82 |
| CHEMBL383541 | — | — | 1 | 7.85 |
| CHEMBL381187 | — | — | 1 | 7.58 |
| CHEMBL207496 | — | — | 1 | 6.72 |
| CHEMBL206732 | — | — | 1 | 6.68 |
| CHEMBL206208 | — | — | 1 | 6.68 |
| CHEMBL381785 | — | — | 1 | 6.64 |
| CHEMBL208199 | — | — | 1 | 6.58 |
| CHEMBL205994 | — | — | 1 | 6.57 |
| CHEMBL206819 | — | — | 1 | 6.52 |
| CHEMBL203673 | — | — | 1 | 6.16 |
| CHEMBL378589 | — | — | 1 | 5.95 |
| CHEMBL268054 | — | — | 1 | 5.87 |
| CHEMBL206746 | — | — | 1 | 5.86 |
| CHEMBL439340 | — | — | 1 | 5.84 |
| CHEMBL382397 | — | — | 1 | 5.81 |
| CHEMBL427388 | — | — | 1 | 5.74 |
| CHEMBL208499 | — | — | 1 | 5.70 |
| CHEMBL207671 | — | — | 1 | 5.67 |
| CHEMBL205781 | — | — | 1 | 5.66 |
| CHEMBL208406 | — | — | 1 | 5.57 |
| CHEMBL383223 | — | — | 1 | 5.54 |
| CHEMBL202972 | — | — | 1 | 5.43 |
| CHEMBL380542 | — | — | 1 | 5.21 |
| CHEMBL206179 | — | — | 1 | 5.16 |
| CHEMBL382379 | — | — | 1 | 5.16 |
| CHEMBL205324 | — | — | 1 | 5.15 |
| CHEMBL426126 | — | — | 1 | 5.03 |
| CHEMBL207530 | — | — | 1 | 5.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL383264 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL383541 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL381187 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL207496 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL206732 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL206208 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL381785 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL208199 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL205994 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL206819 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL203673 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL378589 | — | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL268054 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL206746 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL439340 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL382397 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL427388 | — | IC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL208499 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL207671 | — | IC50 | = | 2160.0 | nM | 5.67 |
| CHEMBL205781 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL208406 | — | IC50 | = | 2710.0 | nM | 5.57 |
| CHEMBL383223 | — | IC50 | = | 2860.0 | nM | 5.54 |
| CHEMBL202972 | — | IC50 | = | 3670.0 | nM | 5.43 |
| CHEMBL380542 | — | IC50 | = | 6230.0 | nM | 5.21 |
| CHEMBL206179 | — | IC50 | = | 6940.0 | nM | 5.16 |
| CHEMBL382379 | — | IC50 | = | 6970.0 | nM | 5.16 |
| CHEMBL205324 | — | IC50 | = | 7090.0 | nM | 5.15 |
| CHEMBL207530 | — | IC50 | = | 9350.0 | nM | 5.03 |
| CHEMBL426126 | — | IC50 | = | 9310.0 | nM | 5.03 |
| CHEMBL377771 | — | IC50 | = | 9870.0 | nM | 5.01 |
| CHEMBL205422 | — | IC50 | = | 12030.0 | nM | 4.92 |
| CHEMBL207031 | — | IC50 | = | 14330.0 | nM | 4.84 |
| CHEMBL207699 | — | IC50 | = | 18830.0 | nM | 4.72 |
| CHEMBL205349 | — | IC50 | = | 25200.0 | nM | 4.60 |
| CHEMBL414861 | — | IC50 | = | 31950.0 | nM | 4.50 |
| CHEMBL204892 | — | IC50 | = | 31280.0 | nM | 4.50 |
| CHEMBL383702 | — | IC50 | = | 33010.0 | nM | 4.48 |
| CHEMBL206581 | — | IC50 | = | 33160.0 | nM | 4.48 |