Assay Detail
Binding
CHEMBL3888428
Review assay metadata, readout intent, target linkage, and publication context from the same page.
HTRF Biochemical Assay: The reactions employed a common peptide substrate, LCB-EQEDEPEGDYFEWLW-NH2 (in-house). The basic assay protocol is as follows: First, 250 nL 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 room temperature to allow compound binding to equilibrate. After equilibration, 2 uL of 10xATP in 1x assay buffer was added to initiate the kinase reaction and the plates were shaken and then incubated at room temperature for 120 minutes. At the end of the incubation, 20 uL of 2x stop buffer (streptavidin-Dylight 650 (Thermo #84547B/100 mL), Eu-tagged pY20 antibody (Perkin Elmer #AD0067), EDTA, HEPES, and Triton) was added to quench the reaction.
667
Total Activities
620
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 |
Publication
Cyanomethylpyrazole carboxamides as janus kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 667 | 8.47 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3896068 | — | — | 1 | 11.00 |
| CHEMBL3947540 | — | — | 2 | 10.70 |
| CHEMBL3929513 | — | — | 1 | 10.52 |
| CHEMBL3904265 | — | — | 3 | 10.52 |
| CHEMBL3897977 | — | — | 2 | 10.52 |
| CHEMBL3965448 | — | — | 1 | 10.52 |
| CHEMBL3940414 | — | — | 2 | 10.40 |
| CHEMBL3959005 | — | — | 1 | 10.40 |
| CHEMBL3950253 | — | — | 2 | 10.40 |
| CHEMBL3933102 | — | — | 1 | 10.40 |
| CHEMBL4106834 | — | — | 1 | 10.30 |
| CHEMBL3916947 | — | — | 2 | 10.30 |
| CHEMBL3892599 | — | — | 2 | 10.30 |
| CHEMBL3972665 | — | — | 1 | 10.30 |
| CHEMBL3984300 | — | — | 1 | 10.22 |
| CHEMBL3929641 | — | — | 1 | 10.22 |
| CHEMBL3942031 | — | — | 2 | 10.22 |
| CHEMBL3945594 | — | — | 1 | 10.22 |
| CHEMBL3895272 | — | — | 1 | 10.22 |
| CHEMBL3914149 | — | — | 1 | 10.15 |
| CHEMBL3946128 | — | — | 1 | 10.15 |
| CHEMBL3893735 | — | — | 2 | 10.15 |
| CHEMBL3973424 | — | — | 1 | 10.10 |
| CHEMBL3914311 | — | — | 2 | 10.10 |
| CHEMBL3911515 | — | — | 2 | 10.10 |
| CHEMBL3919665 | — | — | 2 | 10.10 |
| CHEMBL3943909 | — | — | 2 | 10.10 |
| CHEMBL3935178 | — | — | 1 | 10.05 |
| CHEMBL3932064 | — | — | 1 | 10.05 |
| CHEMBL3950965 | — | — | 2 | 10.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3896068 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL3947540 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL3904265 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL3929513 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL3897977 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL3965448 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL3904265 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL3933102 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL3950253 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL3940414 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL3959005 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL3972665 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL3892599 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL3916947 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL4106834 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL3945594 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3895272 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3942031 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3984300 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3929641 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3946128 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL3914149 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL3893735 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL3973424 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL3914311 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL3919665 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL3943909 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL3911515 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL3915313 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL3935178 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL3928653 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL3950965 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL3932064 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL3930900 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3932352 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3938195 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3965904 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3923034 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3931250 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3927787 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3982398 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3917002 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3949472 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3905008 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3926188 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3977608 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3914600 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3938031 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3983487 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3944488 | — | IC50 | = | 0.1 | nM | 10.00 |