Assay Detail
Binding
CHEMBL3707623
Review assay metadata, readout intent, target linkage, and publication context from the same page.
HTRF Assay: The ability of compounds to inhibit the activity of JAK1, JAK2, JAK3, and Tyk2 was measured using a recombinant purified GST-tagged catalytic domain for each enzyme (Invitrogen JAK1 #M4290, JAK2 #M4290, JAK3 #M4290, Tyk2 #M4290) in an HTRF format biochemical assay. The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 mL of diluted compounds in DMSO were dispensed into the wells of a dry 384-well Black plate (Greiner #781076) using a Labcyte Echo 555 acoustic dispenser. Subsequent reagent additions employed an Agilent Bravo. Next, 18 uL of 1.11x enzyme and 1.11x substrate in 1x assay buffer (Invitrogen kinase buffer #PV3189, 2 mM DTT, 0.05% BSA) were added to the wells and shaken and then preincubated for 30 minutes at ambient temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction.
596
Total Activities
561
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 |
Publication
Cycloalkylnitrile pyrazole carboxamides as janus kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 596 | 7.59 | 9.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3699558 | — | — | 1 | 9.18 |
| CHEMBL3699521 | — | — | 1 | 9.10 |
| CHEMBL3702904 | — | — | 1 | 9.05 |
| CHEMBL3647859 | — | — | 1 | 9.02 |
| CHEMBL3702907 | — | — | 1 | 9.02 |
| CHEMBL3702903 | — | — | 1 | 9.00 |
| CHEMBL3702910 | — | — | 1 | 9.00 |
| CHEMBL3647845 | — | — | 1 | 9.00 |
| CHEMBL3702889 | — | — | 1 | 9.00 |
| CHEMBL3702920 | — | — | 1 | 9.00 |
| CHEMBL3702919 | — | — | 1 | 9.00 |
| CHEMBL3702887 | — | — | 1 | 9.00 |
| CHEMBL3647728 | — | — | 1 | 9.00 |
| CHEMBL3702914 | — | — | 1 | 9.00 |
| CHEMBL3647736 | — | — | 1 | 9.00 |
| CHEMBL3699531 | — | — | 1 | 9.00 |
| CHEMBL3703042 | — | — | 1 | 9.00 |
| CHEMBL3647923 | — | — | 2 | 9.00 |
| CHEMBL3702905 | — | — | 1 | 9.00 |
| CHEMBL3647858 | — | — | 1 | 8.70 |
| CHEMBL3699528 | — | — | 1 | 8.70 |
| CHEMBL3699499 | — | — | 2 | 8.70 |
| CHEMBL3647835 | — | — | 2 | 8.70 |
| CHEMBL3647922 | — | — | 2 | 8.70 |
| CHEMBL3647918 | — | — | 1 | 8.70 |
| CHEMBL3647751 | — | — | 1 | 8.70 |
| CHEMBL3702886 | — | — | 1 | 8.70 |
| CHEMBL3647856 | — | — | 1 | 8.70 |
| CHEMBL3702883 | — | — | 1 | 8.70 |
| CHEMBL3702947 | — | — | 1 | 8.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3699558 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL3699521 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL3702904 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3702907 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL3647859 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL3702910 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3702903 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3702889 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3699531 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3647728 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3702920 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3647923 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3647845 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3702905 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3702914 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3647736 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3703042 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3702919 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3702887 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3702953 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3702947 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3702883 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3702886 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3699551 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3699537 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3699528 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3647919 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3647751 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3647858 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3647856 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3699499 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3647861 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3647918 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3647922 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3702902 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3702908 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3702912 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3647835 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3703048 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3647727 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3699538 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3647835 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3699500 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3699530 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3702957 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3647771 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3647852 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3702951 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3647924 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3703051 | — | IC50 | = | 3.0 | nM | 8.52 |