Assay Detail
Binding
CHEMBL3887297
Review assay metadata, readout intent, target linkage, and publication context from the same page.
AKT Enzyme Assay: A TTP Mosquito liquid handling instrument is used to place 125 nl of the appropriate concentration of inhibitor in 100% DMSO (for a dose response curve calculation) into each well of a 384-well plate. To this reaction components are added to a final volume of 12.5 .mu.l: 0.1 ng/.mu.l His-AKT (Full Length), (Invitrogen, Part # P2999, Lot #641228C). 160 uM ATP (Fluka, 02055) 1 mM DTT (Sigma, D0632) 1 mM MgCl2 (Sigma, M1028) 1 .mu.M substrate peptide (sequence FITC-AHA-GRPRTSSFAEG-NH2), synthesized by Tufts Peptide Synthesis service. 100 mM HEPES pH 7.5 (Calbiochem, 391338)0.015% Brij-35 (Sigma, B4184)The reaction is incubated for 90 min at 25 C, and then stopped by the addition of 70 .mu.l of Stop buffer (100 mM HEPES pH 7.5, 0.015% Brij-35, 10 mM EDTA (Sigma, E7889)).The plate is read on a Caliper LC 3000 in an Off-Chip mobility shift assay format, using the following parameters for a 12-sipper chip: screening pressure -2.3 psi, upstream voltage -500, and downstream voltage -3000.
372
Total Activities
371
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
RAC-alpha serine/threonine-protein kinase (CHEMBL4282) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Imidazole amines as modulators of kinase activity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 372 | 7.50 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3899716 | — | — | 1 | 10.00 |
| CHEMBL3966806 | — | — | 1 | 9.82 |
| CHEMBL3936990 | — | — | 1 | 9.52 |
| CHEMBL3906990 | — | — | 1 | 9.40 |
| CHEMBL3943127 | — | — | 1 | 9.28 |
| CHEMBL3980521 | — | — | 1 | 9.15 |
| CHEMBL3927358 | — | — | 1 | 9.15 |
| CHEMBL3986943 | — | — | 1 | 9.10 |
| CHEMBL3960355 | — | — | 1 | 9.10 |
| CHEMBL3971598 | — | — | 1 | 9.05 |
| CHEMBL3919089 | — | — | 1 | 9.00 |
| CHEMBL3941283 | — | — | 1 | 9.00 |
| CHEMBL3966203 | — | — | 1 | 8.89 |
| CHEMBL3954981 | — | — | 1 | 8.85 |
| CHEMBL3890352 | — | — | 1 | 8.85 |
| CHEMBL3948454 | — | — | 1 | 8.85 |
| CHEMBL3899490 | — | — | 1 | 8.82 |
| CHEMBL3967010 | — | — | 1 | 8.82 |
| CHEMBL3894849 | — | — | 1 | 8.82 |
| CHEMBL3912471 | — | — | 1 | 8.82 |
| CHEMBL3941451 | — | — | 1 | 8.80 |
| CHEMBL3983282 | — | — | 1 | 8.80 |
| CHEMBL3949795 | — | — | 1 | 8.77 |
| CHEMBL3944201 | — | — | 1 | 8.77 |
| CHEMBL3948085 | — | — | 1 | 8.77 |
| CHEMBL3969016 | — | — | 1 | 8.77 |
| CHEMBL3980219 | — | — | 1 | 8.74 |
| CHEMBL3940867 | — | — | 1 | 8.72 |
| CHEMBL3965271 | — | — | 1 | 8.72 |
| CHEMBL3984164 | — | — | 1 | 8.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3899716 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3966806 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL3936990 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3906990 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3943127 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL3927358 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3980521 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3960355 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3986943 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3971598 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3919089 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3941283 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3966203 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3948454 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3954981 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3890352 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3912471 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3899490 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3894849 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3967010 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3941451 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3983282 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3948085 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3944201 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3969016 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3949795 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3980219 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3895898 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3965271 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3984164 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3940867 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3961056 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3904291 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3910789 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3916178 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3928772 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3891980 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3986793 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3977147 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3981085 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3903522 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3967750 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3972479 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3927877 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3894578 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3912769 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3938454 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3933597 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3896910 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3919834 | — | IC50 | = | 2.5 | nM | 8.60 |