Assay Detail
Binding
CHEMBL5737797
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro AKT1 Kinase Assay: Following addition of compound or control to the assay plate, 6p1 peptide mix containing 3 μM substrate (5-FAM-GRPRTSSFAEG-CONH2; CRB) and 40 μM ATP in Kinase base buffer (100 mM Hepes pH 7.5, 0.015% Brij-35) and 6p1 enzyme mix containing 8 nM AKT1/PKBα active enzyme (Upstate Biotechnology, Cat No. 14-276), 8 mM DTT and 20 mM MgCl2 in kinase base buffer was added. All buffers were made up with 18MΩ water. The plates were sealed and incubated at room temperature for 50 minutes. The reaction was stopped by the addition of 10 μl stop buffer (100 mM Hepes pH 7.5, 0.015% Brij-35 solution, 0.1% coating reagent #3, 40 mM EDTA, 5% DMSO) to each well (N.B. plates can be frozen after stopping and read later).
231
Total Activities
77
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
RAC-alpha serine/threonine-protein kinase (CHEMBL4282) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Protein kinase B inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 77 | 7.96 | 8.92 |
| kon | 77 | - | - |
| k_off | 77 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6061476 | — | — | 3 | 8.92 |
| CHEMBL5798563 | — | — | 3 | 8.89 |
| CHEMBL2325992 | — | — | 3 | 8.70 |
| CHEMBL5948798 | — | — | 3 | 8.66 |
| CHEMBL5804752 | — | — | 3 | 8.59 |
| CHEMBL5818600 | — | — | 3 | 8.57 |
| CHEMBL5782008 | — | — | 3 | 8.55 |
| CHEMBL2325993 | — | — | 3 | 8.54 |
| CHEMBL5762410 | — | — | 3 | 8.52 |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 3 | 8.49 |
| CHEMBL6064010 | — | — | 3 | 8.48 |
| CHEMBL5962920 | — | — | 3 | 8.47 |
| CHEMBL2325994 | — | — | 3 | 8.44 |
| CHEMBL2325729 | — | — | 3 | 8.43 |
| CHEMBL2325743 | — | — | 3 | 8.42 |
| CHEMBL2325728 | — | — | 3 | 8.41 |
| CHEMBL5767632 | — | — | 3 | 8.40 |
| CHEMBL5849470 | — | — | 3 | 8.38 |
| CHEMBL2325738 | — | — | 3 | 8.38 |
| CHEMBL5909930 | — | — | 3 | 8.37 |
| CHEMBL5998995 | — | — | 3 | 8.35 |
| CHEMBL5914656 | — | — | 3 | 8.35 |
| CHEMBL2325996 | — | — | 3 | 8.30 |
| CHEMBL2325983 | — | — | 3 | 8.30 |
| CHEMBL5828090 | — | — | 3 | 8.27 |
| CHEMBL2325995 | — | — | 3 | 8.25 |
| CHEMBL5779455 | — | — | 3 | 8.25 |
| CHEMBL2325739 | — | — | 3 | 8.21 |
| CHEMBL6008744 | — | — | 3 | 8.20 |
| CHEMBL5788486 | — | — | 3 | 8.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6061476 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5798563 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2325992 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5948798 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5804752 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5818600 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5782008 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL2325993 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5762410 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2325741 | CAPIVASERTIB | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL6064010 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5962920 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL2325994 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL2325729 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL2325743 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL2325728 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5767632 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2325738 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5849470 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5909930 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5914656 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL5998995 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL2325996 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2325983 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5828090 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL2325995 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL5779455 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL2325739 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5788486 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL6008744 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL2325734 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5977643 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL2325982 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL2325736 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL2325737 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL5780547 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL2325997 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL5804316 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL2325987 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL5865809 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL2325740 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL5758529 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL5783615 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL6032267 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2325733 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5956984 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL6026023 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5967812 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5786800 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5849633 | — | IC50 | = | 14.0 | nM | 7.85 |