Assay Detail
Binding
CHEMBL867719
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Inhibition of Akt1 using 10 uM ATP
46
Total Activities
46
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
Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 6.08 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.82 |
| CHEMBL203624 | — | — | 1 | 8.01 |
| CHEMBL383541 | — | — | 1 | 7.85 |
| CHEMBL203384 | — | — | 1 | 7.72 |
| CHEMBL379914 | — | — | 1 | 7.64 |
| CHEMBL203275 | — | — | 1 | 7.16 |
| CHEMBL381703 | — | — | 1 | 7.10 |
| CHEMBL381075 | — | — | 1 | 6.92 |
| CHEMBL206183 | — | — | 1 | 6.85 |
| CHEMBL381328 | — | — | 1 | 6.84 |
| CHEMBL381610 | — | — | 1 | 6.83 |
| CHEMBL382914 | — | — | 1 | 6.79 |
| CHEMBL202787 | — | — | 1 | 6.75 |
| CHEMBL203329 | — | — | 1 | 6.70 |
| CHEMBL205415 | — | — | 1 | 6.56 |
| CHEMBL206198 | — | — | 1 | 6.56 |
| CHEMBL383254 | — | — | 1 | 6.55 |
| CHEMBL205410 | — | — | 1 | 6.50 |
| CHEMBL205871 | — | — | 1 | 6.49 |
| CHEMBL381808 | — | — | 1 | 6.44 |
| CHEMBL204012 | — | — | 1 | 6.30 |
| CHEMBL383527 | — | — | 1 | 6.17 |
| CHEMBL203673 | — | — | 1 | 6.16 |
| CHEMBL202937 | — | — | 1 | 6.12 |
| CHEMBL203685 | — | — | 1 | 6.06 |
| CHEMBL202893 | — | — | 1 | 5.96 |
| CHEMBL377294 | — | — | 1 | 5.57 |
| CHEMBL381260 | — | — | 1 | 5.51 |
| CHEMBL205514 | — | — | 1 | 5.50 |
| CHEMBL206708 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL203624 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL383541 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL203384 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL379914 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL203275 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL381703 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL381075 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL206183 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL381328 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL381610 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL382914 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL202787 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL203329 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL206198 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL205415 | — | IC50 | = | 278.0 | nM | 6.56 |
| CHEMBL383254 | — | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL205410 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL205871 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL381808 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL204012 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL383527 | — | IC50 | = | 668.0 | nM | 6.17 |
| CHEMBL203673 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL202937 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL203685 | — | IC50 | = | 875.0 | nM | 6.06 |
| CHEMBL202893 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL377294 | — | IC50 | = | 2670.0 | nM | 5.57 |
| CHEMBL381260 | — | IC50 | = | 3110.0 | nM | 5.51 |
| CHEMBL205514 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL206708 | — | IC50 | = | 3340.0 | nM | 5.48 |
| CHEMBL206236 | — | IC50 | = | 4040.0 | nM | 5.39 |
| CHEMBL206382 | — | IC50 | = | 5080.0 | nM | 5.29 |
| CHEMBL419932 | — | IC50 | = | 5290.0 | nM | 5.28 |
| CHEMBL203483 | — | IC50 | = | 6350.0 | nM | 5.20 |
| CHEMBL378823 | — | IC50 | = | 6450.0 | nM | 5.19 |
| CHEMBL203434 | — | IC50 | = | 6760.0 | nM | 5.17 |
| CHEMBL381829 | — | IC50 | = | 8020.0 | nM | 5.10 |
| CHEMBL204213 | — | IC50 | = | 10870.0 | nM | 4.96 |
| CHEMBL205820 | — | IC50 | = | 14710.0 | nM | 4.83 |
| CHEMBL204059 | — | IC50 | = | 19320.0 | nM | 4.71 |
| CHEMBL206654 | — | IC50 | = | 23270.0 | nM | 4.63 |
| CHEMBL380958 | — | IC50 | = | 24010.0 | nM | 4.62 |
| CHEMBL205645 | — | IC50 | = | 23910.0 | nM | 4.62 |
| CHEMBL206328 | — | IC50 | = | 32250.0 | nM | 4.49 |
| CHEMBL203004 | — | IC50 | = | 43010.0 | nM | 4.37 |
| CHEMBL205836 | — | IC50 | > | 50000.0 | nM | - |