Assay Detail
Binding
CHEMBL3705594
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinase Assay: Recombinant human PDK1 enzyme (aa 52-556) linked at its N-terminal end to His6 is isolated from baculovirus-infected insect cells. Purified enzyme may be obtained for example from the University of Dundee, Scotland. The following components are combined in a well of a 96-well round-based dish (Greiner bio-one, No. 650101): 1. 15 uL of compound to be tested in varying concentrations (e.g. starting at 10 uM, and diluted in steps of 1:5) in APT buffer (50 mM Tris/Cl pH7.5; 0.05% beta -mercaptoethanol; 10 mM Mg-acetate; 0.0166% Tween 20; 3.33% DMSO) 2. 15 uL His6-PDK1 (aa 52-556) 3.33 ng/well) and PDKtide (KTFCGTPEYLAPEVRRE PRILSEEEQEMFRDFDYIADWC), synthesised by Pepceuticals Limited, Nottingham, United Kingdom; 25 uM final concentration); His6-PDK1 and PDKtide are together diluted accordingly in assay buffer (50 mM tris pH 7.5, 0.05% beta -mercaptoethanol, 10 mM Mg-acetate); PDKtide is present in this mixture as an 83.3 uM solution.
96
Total Activities
94
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
3-phosphoinositide-dependent protein kinase 1 (CHEMBL2534) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
1H-imidazo[4,5-c]quinolines
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 96 | 7.94 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3644732 | — | — | 1 | 9.00 |
| CHEMBL3644712 | — | — | 1 | 9.00 |
| CHEMBL3644710 | — | — | 1 | 9.00 |
| CHEMBL3644758 | — | — | 1 | 9.00 |
| CHEMBL3644741 | — | — | 1 | 9.00 |
| CHEMBL3644750 | — | — | 1 | 9.00 |
| CHEMBL3644753 | — | — | 1 | 9.00 |
| CHEMBL3644700 | — | — | 1 | 9.00 |
| CHEMBL3644680 | — | — | 1 | 9.00 |
| CHEMBL3644697 | — | — | 1 | 8.70 |
| CHEMBL3639436 | — | — | 1 | 8.70 |
| CHEMBL3644759 | — | — | 1 | 8.70 |
| CHEMBL3644689 | — | — | 1 | 8.70 |
| CHEMBL3644683 | — | — | 1 | 8.70 |
| CHEMBL3644755 | — | — | 1 | 8.70 |
| CHEMBL3644695 | — | — | 1 | 8.70 |
| CHEMBL3644703 | — | — | 1 | 8.70 |
| CHEMBL3644704 | — | — | 3 | 8.70 |
| CHEMBL3644713 | — | — | 1 | 8.70 |
| CHEMBL3644733 | — | — | 1 | 8.70 |
| CHEMBL3644729 | — | — | 1 | 8.70 |
| CHEMBL3644722 | — | — | 1 | 8.70 |
| CHEMBL3644724 | — | — | 1 | 8.52 |
| CHEMBL3644754 | — | — | 1 | 8.52 |
| CHEMBL3644751 | — | — | 1 | 8.52 |
| CHEMBL3644699 | — | — | 1 | 8.40 |
| CHEMBL3644752 | — | — | 1 | 8.40 |
| CHEMBL3644681 | — | — | 1 | 8.40 |
| CHEMBL3644682 | — | — | 1 | 8.40 |
| CHEMBL3644736 | — | — | 1 | 8.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3644700 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3644758 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3644680 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3644732 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3644712 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3644741 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3644753 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3644750 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3644710 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3644703 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644697 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644695 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644683 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644689 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3639436 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644759 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644755 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644729 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644704 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644713 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644704 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644704 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644722 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644733 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3644751 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3644754 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3644724 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3644752 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3644681 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3644682 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3644736 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3644699 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3644748 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3644706 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3644757 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3644708 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3644709 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3644761 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3644698 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3647298 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3644726 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3644749 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3644727 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3644734 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3644693 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3644696 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3644723 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3644760 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3647295 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3644691 | — | IC50 | = | 9.0 | nM | 8.05 |