Assay Detail
Binding
CHEMBL5730262
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinase-Glo Assay: These assays are set up in duplicate 50 ul volumes in white, flat bottom 96 well plates. Inhibitors are added to the solution of 1× kinase buffer, 10 uM ATP, 100 uM Pim-1-specific substrate, 50 ng of active Pim-1 enzyme, and water in serial dilutions ranging from micromolar to nanomolar concentrations. This solution is incubated at 30 degrees Celsius at 360 rpm for two hours. Following the incubation, 50 ul of Kinase-Glo reagent is added to each well, including all positive and negative control wells, and incubated at room temperature for 15 minutes. The plate is then read by the Luminoskan Ascent instrument and the results displayed with the Ascent Software version 2.6.
312
Total Activities
103
Compounds Tested
3
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
Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 104 | 7.11 | 9.00 |
| kon | 104 | - | - |
| k_off | 104 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3975308 | NUVISERTIB | 2.0 | 3 | 9.00 |
| CHEMBL3928943 | — | — | 3 | 8.70 |
| CHEMBL3938841 | — | — | 3 | 8.40 |
| CHEMBL3973281 | — | — | 3 | 8.40 |
| CHEMBL3947323 | — | — | 3 | 8.40 |
| CHEMBL3979144 | — | — | 3 | 8.30 |
| CHEMBL3355542 | — | — | 3 | 8.30 |
| CHEMBL3964407 | — | — | 3 | 8.15 |
| CHEMBL3929683 | — | — | 3 | 8.15 |
| CHEMBL3936197 | — | — | 3 | 8.10 |
| CHEMBL3976594 | — | — | 3 | 8.10 |
| CHEMBL3917577 | — | — | 3 | 8.05 |
| CHEMBL3935594 | — | — | 3 | 8.00 |
| CHEMBL3951241 | — | — | 3 | 7.92 |
| CHEMBL3895053 | — | — | 3 | 7.89 |
| CHEMBL3891871 | — | — | 3 | 7.89 |
| CHEMBL3965204 | — | — | 3 | 7.89 |
| CHEMBL3914589 | — | — | 3 | 7.85 |
| CHEMBL3935431 | — | — | 3 | 7.85 |
| CHEMBL3976705 | — | — | 3 | 7.80 |
| CHEMBL3952816 | — | — | 3 | 7.80 |
| CHEMBL3915263 | — | — | 3 | 7.77 |
| CHEMBL3355552 | — | — | 3 | 7.77 |
| CHEMBL3920771 | — | — | 3 | 7.75 |
| CHEMBL3941934 | — | — | 3 | 7.75 |
| CHEMBL3943090 | — | — | 3 | 7.72 |
| CHEMBL3930875 | — | — | 3 | 7.64 |
| CHEMBL3355987 | — | — | 3 | 7.64 |
| CHEMBL3355557 | — | — | 6 | 7.62 |
| CHEMBL3355550 | — | — | 3 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3975308 | NUVISERTIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3928943 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3947323 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3938841 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3973281 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3355542 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3979144 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3929683 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3964407 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3976594 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3936197 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3917577 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3935594 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3951241 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3965204 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3891871 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3895053 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3914589 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3935431 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3952816 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3976705 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3355552 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3915263 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3941934 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3920771 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3943090 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3930875 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3355987 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3355557 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3355557 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3355550 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3355544 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3953965 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3929768 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3927091 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3959607 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3965060 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3962567 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4107503 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4113689 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3961837 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3945649 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3355541 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3922142 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL426658 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3918006 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3961500 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3355551 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3914508 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3976290 | — | IC50 | = | 58.0 | nM | 7.24 |