Assay Detail
Binding
CHEMBL4407340
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Akt1 expressed in Escherichia coli using STK Substrate 2-biotin as substrate incubated for 1 hr by HTRF assay
78
Total Activities
78
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 of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 78 | 7.62 | 9.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4441825 | — | — | 1 | 9.01 |
| CHEMBL4440965 | — | — | 1 | 8.86 |
| CHEMBL4554668 | — | — | 1 | 8.85 |
| CHEMBL4447967 | — | — | 1 | 8.71 |
| CHEMBL4552655 | — | — | 1 | 8.60 |
| CHEMBL4460525 | — | — | 1 | 8.60 |
| CHEMBL4451765 | — | — | 1 | 8.59 |
| CHEMBL4475923 | — | — | 1 | 8.58 |
| CHEMBL4517950 | — | — | 1 | 8.56 |
| CHEMBL4445510 | — | — | 1 | 8.54 |
| CHEMBL4457064 | — | — | 1 | 8.52 |
| CHEMBL4593086 | — | — | 1 | 8.50 |
| CHEMBL4438877 | — | — | 1 | 8.49 |
| CHEMBL4567295 | — | — | 1 | 8.48 |
| CHEMBL4441416 | — | — | 1 | 8.48 |
| CHEMBL4531735 | — | — | 1 | 8.47 |
| CHEMBL4590906 | — | — | 1 | 8.47 |
| CHEMBL4470606 | — | — | 1 | 8.42 |
| CHEMBL4589576 | — | — | 1 | 8.40 |
| CHEMBL4519793 | — | — | 1 | 8.35 |
| CHEMBL3137336 | UPROSERTIB | 2.0 | 1 | 8.33 |
| CHEMBL4529738 | — | — | 1 | 8.29 |
| CHEMBL4524940 | — | — | 1 | 8.25 |
| CHEMBL4518523 | — | — | 1 | 8.22 |
| CHEMBL4546392 | — | — | 1 | 8.19 |
| CHEMBL4465572 | — | — | 1 | 8.19 |
| CHEMBL4568343 | — | — | 1 | 8.15 |
| CHEMBL4536780 | — | — | 1 | 8.14 |
| CHEMBL4585120 | — | — | 1 | 8.10 |
| CHEMBL4447158 | — | — | 1 | 8.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4441825 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL4440965 | — | IC50 | = | 1.37 | nM | 8.86 |
| CHEMBL4554668 | — | IC50 | = | 1.41 | nM | 8.85 |
| CHEMBL4447967 | — | IC50 | = | 1.94 | nM | 8.71 |
| CHEMBL4552655 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4460525 | — | IC50 | = | 2.49 | nM | 8.60 |
| CHEMBL4451765 | — | IC50 | = | 2.56 | nM | 8.59 |
| CHEMBL4475923 | — | IC50 | = | 2.64 | nM | 8.58 |
| CHEMBL4517950 | — | IC50 | = | 2.74 | nM | 8.56 |
| CHEMBL4445510 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4457064 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4593086 | — | IC50 | = | 3.13 | nM | 8.50 |
| CHEMBL4438877 | — | IC50 | = | 3.24 | nM | 8.49 |
| CHEMBL4567295 | — | IC50 | = | 3.31 | nM | 8.48 |
| CHEMBL4441416 | — | IC50 | = | 3.29 | nM | 8.48 |
| CHEMBL4531735 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4590906 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4470606 | — | IC50 | = | 3.79 | nM | 8.42 |
| CHEMBL4589576 | — | IC50 | = | 3.95 | nM | 8.40 |
| CHEMBL4519793 | — | IC50 | = | 4.47 | nM | 8.35 |
| CHEMBL3137336 | UPROSERTIB | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4529738 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4524940 | — | IC50 | = | 5.65 | nM | 8.25 |
| CHEMBL4518523 | — | IC50 | = | 5.99 | nM | 8.22 |
| CHEMBL4465572 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4546392 | — | IC50 | = | 6.41 | nM | 8.19 |
| CHEMBL4568343 | — | IC50 | = | 7.01 | nM | 8.15 |
| CHEMBL4536780 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4585120 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4447158 | — | IC50 | = | 7.98 | nM | 8.10 |
| CHEMBL4450403 | — | IC50 | = | 8.78 | nM | 8.06 |
| CHEMBL4591854 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4467439 | — | IC50 | = | 10.44 | nM | 7.98 |
| CHEMBL4449509 | — | IC50 | = | 12.41 | nM | 7.91 |
| CHEMBL4450141 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL4554683 | — | IC50 | = | 17.3 | nM | 7.76 |
| CHEMBL4443488 | — | IC50 | = | 17.3 | nM | 7.76 |
| CHEMBL4471578 | — | IC50 | = | 17.6 | nM | 7.75 |
| CHEMBL4460756 | — | IC50 | = | 21.6 | nM | 7.67 |
| CHEMBL2325741 | CAPIVASERTIB | IC50 | = | 25.43 | nM | 7.59 |
| CHEMBL4574492 | — | IC50 | = | 27.3 | nM | 7.56 |
| CHEMBL4518386 | — | IC50 | = | 29.4 | nM | 7.53 |
| CHEMBL4439720 | — | IC50 | = | 29.8 | nM | 7.53 |
| CHEMBL4578995 | — | IC50 | = | 31.2 | nM | 7.51 |
| CHEMBL4465905 | — | IC50 | = | 35.6 | nM | 7.45 |
| CHEMBL4583911 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4540052 | — | IC50 | = | 50.3 | nM | 7.30 |
| CHEMBL4533641 | — | IC50 | = | 51.2 | nM | 7.29 |
| CHEMBL4528834 | — | IC50 | = | 57.7 | nM | 7.24 |
| CHEMBL3805228 | — | IC50 | = | 61.0 | nM | 7.21 |