Assay Detail
Binding
CHEMBL3887976
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PIM Kinase Binding Activity Assay: PIM-1, PIM-2, and PIM-3 enzymes were generated as fusion proteins expressed in bacteria and purified by IMAC column chromatography (Sun, X., Chiu, J. F., and He, Q. Y. (2005) Expert Rev. Proteomics, 2:649-657). A fluorescent-labeled Pim-specific peptide substrate, was custom synthesized by American Peptide Company (Sunnyvale, Calif.). Reaction Buffer contained 10 mM HEPES, pH 7.2, 10 mM MgCl2, 0.01% Tween 20, 2 mM DTT. Termination Buffer contained 190 mM HEPES, pH 7.2, 0.015% Brij-35, 0.2% Coating Reagent 3 (Caliper Life Sciences, Hopkinton, Mass.), 20 mM EDTA. Separation Buffer contained 100 mM HEPES, pH 7.2, 0.015% Brij-35, 0.1% Coating Reagent 3, 1:200 Coating Reagent 8 (Caliper Life Sciences, Hopkinton, Mass.), 10 mM EDTA and 5% DMSO.
412
Total Activities
405
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase pim-1 (CHEMBL2147) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Pyrazolo[3,4-c]pyridine compounds and methods of use
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 412 | 9.09 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3972110 | — | — | 1 | 11.00 |
| CHEMBL3634783 | — | — | 1 | 11.00 |
| CHEMBL3894581 | — | — | 1 | 11.00 |
| CHEMBL3634760 | — | — | 1 | 10.89 |
| CHEMBL3949620 | — | — | 1 | 10.89 |
| CHEMBL3922596 | — | — | 1 | 10.85 |
| CHEMBL4115489 | — | — | 1 | 10.85 |
| CHEMBL3925594 | — | — | 1 | 10.85 |
| CHEMBL3967523 | — | — | 1 | 10.82 |
| CHEMBL3634769 | — | — | 1 | 10.82 |
| CHEMBL3971218 | — | — | 1 | 10.80 |
| CHEMBL3910119 | — | — | 2 | 10.80 |
| CHEMBL3946733 | — | — | 1 | 10.77 |
| CHEMBL3893927 | — | — | 1 | 10.72 |
| CHEMBL3978766 | — | — | 1 | 10.72 |
| CHEMBL4113655 | — | — | 1 | 10.70 |
| CHEMBL3972403 | — | — | 1 | 10.70 |
| CHEMBL3895582 | — | — | 1 | 10.70 |
| CHEMBL3905023 | — | — | 1 | 10.68 |
| CHEMBL3634772 | — | — | 1 | 10.68 |
| CHEMBL3899964 | — | — | 1 | 10.68 |
| CHEMBL3962485 | — | — | 1 | 10.66 |
| CHEMBL3634771 | — | — | 1 | 10.66 |
| CHEMBL3940007 | — | — | 1 | 10.66 |
| CHEMBL3897509 | — | — | 1 | 10.66 |
| CHEMBL3890600 | — | — | 1 | 10.64 |
| CHEMBL3970485 | — | — | 1 | 10.62 |
| CHEMBL3903449 | — | — | 1 | 10.60 |
| CHEMBL4112372 | — | — | 1 | 10.60 |
| CHEMBL3892821 | — | — | 1 | 10.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3972110 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL3634783 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL3894581 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL3949620 | — | Ki | = | 0.013 | nM | 10.89 |
| CHEMBL3634760 | — | Ki | = | 0.013 | nM | 10.89 |
| CHEMBL3925594 | — | Ki | = | 0.014 | nM | 10.85 |
| CHEMBL4115489 | — | Ki | = | 0.014 | nM | 10.85 |
| CHEMBL3922596 | — | Ki | = | 0.014 | nM | 10.85 |
| CHEMBL3634769 | — | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL3967523 | — | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL3910119 | — | Ki | = | 0.016 | nM | 10.80 |
| CHEMBL3971218 | — | Ki | = | 0.016 | nM | 10.80 |
| CHEMBL3946733 | — | Ki | = | 0.017 | nM | 10.77 |
| CHEMBL3893927 | — | Ki | = | 0.019 | nM | 10.72 |
| CHEMBL3978766 | — | Ki | = | 0.019 | nM | 10.72 |
| CHEMBL3972403 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL3895582 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL4113655 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL3899964 | — | Ki | = | 0.021 | nM | 10.68 |
| CHEMBL3634772 | — | Ki | = | 0.021 | nM | 10.68 |
| CHEMBL3905023 | — | Ki | = | 0.021 | nM | 10.68 |
| CHEMBL3897509 | — | Ki | = | 0.022 | nM | 10.66 |
| CHEMBL3940007 | — | Ki | = | 0.022 | nM | 10.66 |
| CHEMBL3634771 | — | Ki | = | 0.022 | nM | 10.66 |
| CHEMBL3962485 | — | Ki | = | 0.022 | nM | 10.66 |
| CHEMBL3890600 | — | Ki | = | 0.023 | nM | 10.64 |
| CHEMBL3970485 | — | Ki | = | 0.024 | nM | 10.62 |
| CHEMBL3892821 | — | Ki | = | 0.025 | nM | 10.60 |
| CHEMBL4112372 | — | Ki | = | 0.025 | nM | 10.60 |
| CHEMBL3903449 | — | Ki | = | 0.025 | nM | 10.60 |
| CHEMBL4107084 | — | Ki | = | 0.026 | nM | 10.59 |
| CHEMBL4111907 | — | Ki | = | 0.026 | nM | 10.59 |
| CHEMBL3948781 | — | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL3918555 | — | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL3902873 | — | Ki | = | 0.0268 | nM | 10.57 |
| CHEMBL4108413 | — | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL4114430 | — | Ki | = | 0.028 | nM | 10.55 |
| CHEMBL3933509 | — | Ki | = | 0.028 | nM | 10.55 |
| CHEMBL4114499 | — | Ki | = | 0.028 | nM | 10.55 |
| CHEMBL3902989 | — | Ki | = | 0.029 | nM | 10.54 |
| CHEMBL3932937 | — | Ki | = | 0.029 | nM | 10.54 |
| CHEMBL3895992 | — | Ki | = | 0.029 | nM | 10.54 |
| CHEMBL3926542 | — | Ki | = | 0.029 | nM | 10.54 |
| CHEMBL3908352 | — | Ki | = | 0.0294 | nM | 10.53 |
| CHEMBL4111381 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL4107359 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL4115471 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL3918702 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL4107502 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL3927435 | — | Ki | = | 0.03 | nM | 10.52 |