Assay Detail
Binding
CHEMBL2187635
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive inhibition of wild-type full-length amino-terminal polyhistidine-tagged human Akt1 expressed in recombinant baculovirus system using fluorescence labeled substrate after 60 mins by fluorescence polarization assay in presence of ATP
31
Total Activities
31
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
RAC-alpha serine/threonine-protein kinase (CHEMBL4282) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 8.01 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2177378 | — | — | 1 | 8.70 |
| CHEMBL2177387 | — | — | 1 | 8.70 |
| CHEMBL2177361 | — | — | 1 | 8.52 |
| CHEMBL2177388 | — | — | 1 | 8.52 |
| CHEMBL2177379 | — | — | 1 | 8.52 |
| CHEMBL2177368 | — | — | 1 | 8.52 |
| CHEMBL2177372 | — | — | 1 | 8.52 |
| CHEMBL2178597 | — | — | 1 | 8.52 |
| CHEMBL2177381 | — | — | 1 | 8.40 |
| CHEMBL2177367 | — | — | 1 | 8.30 |
| CHEMBL2177366 | — | — | 1 | 8.30 |
| CHEMBL2177390 | IPATASERTIB | 3.0 | 1 | 8.30 |
| CHEMBL2177374 | — | — | 1 | 8.30 |
| CHEMBL2177363 | — | — | 1 | 8.22 |
| CHEMBL2178598 | — | — | 1 | 8.22 |
| CHEMBL2177385 | — | — | 1 | 8.22 |
| CHEMBL2177377 | — | — | 1 | 8.10 |
| CHEMBL2177369 | — | — | 1 | 8.05 |
| CHEMBL2177364 | — | — | 1 | 8.05 |
| CHEMBL2177375 | — | — | 1 | 7.92 |
| CHEMBL2177382 | — | — | 1 | 7.92 |
| CHEMBL2177371 | — | — | 1 | 7.92 |
| CHEMBL2177362 | — | — | 1 | 7.92 |
| CHEMBL2177370 | — | — | 1 | 7.92 |
| CHEMBL2177365 | — | — | 1 | 7.75 |
| CHEMBL2177373 | — | — | 1 | 7.62 |
| CHEMBL2177380 | — | — | 1 | 7.17 |
| CHEMBL2177389 | — | — | 1 | 7.09 |
| CHEMBL2177376 | — | — | 1 | 6.04 |
| CHEMBL2177383 | — | — | 1 | 5.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2177378 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2177387 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2177361 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2177388 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2177379 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2177368 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2177372 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2178597 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2177381 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2177367 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2177366 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2177390 | IPATASERTIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2177374 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2177363 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2177385 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2178598 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2177377 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2177369 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2177364 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2177362 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2177370 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2177371 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2177382 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2177375 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2177365 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2177373 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2177380 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL2177389 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL2177376 | — | IC50 | = | 902.0 | nM | 6.04 |
| CHEMBL2177383 | — | IC50 | = | 1169.0 | nM | 5.93 |
| CHEMBL2177386 | — | IC50 | > | 2000.0 | nM | - |