Assay Detail
Binding
CHEMBL4033004
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged recombinant human JAK3 catalytic domain expressed in baculovirus expression system using LCB-EQEDEPEGDYFEWLW-NH2 as substrate preincubated for 30 mins followed by ATP addition measured after 120 mins by HTRF assay
23
Total Activities
23
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
The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.57 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 9.47 |
| CHEMBL4078799 | — | — | 1 | 7.04 |
| CHEMBL4089118 | — | — | 1 | 7.00 |
| CHEMBL4096821 | — | — | 1 | 6.94 |
| CHEMBL4102140 | — | — | 1 | 6.71 |
| CHEMBL4061128 | — | — | 1 | 6.64 |
| CHEMBL4089234 | — | — | 1 | 6.59 |
| CHEMBL4077886 | — | — | 1 | 6.55 |
| CHEMBL4104623 | — | — | 1 | 6.52 |
| CHEMBL4066906 | — | — | 1 | 6.50 |
| CHEMBL4100288 | — | — | 1 | 6.44 |
| CHEMBL4072848 | — | — | 1 | 6.41 |
| CHEMBL4071005 | — | — | 1 | 6.40 |
| CHEMBL4067915 | — | — | 1 | 6.29 |
| CHEMBL4085737 | — | — | 1 | 6.25 |
| CHEMBL4064171 | — | — | 1 | 6.18 |
| CHEMBL4092626 | — | — | 1 | 6.15 |
| CHEMBL4079092 | — | — | 1 | 6.11 |
| CHEMBL4076473 | — | — | 1 | 6.00 |
| CHEMBL4066193 | ATINVICITINIB | 2.0 | 1 | 5.95 |
| CHEMBL3703085 | — | — | 1 | 5.91 |
| CHEMBL4098999 | — | — | 1 | - |
| CHEMBL4088262 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL4078799 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4089118 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4096821 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL4102140 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL4061128 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4089234 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL4077886 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4104623 | — | IC50 | = | 304.0 | nM | 6.52 |
| CHEMBL4066906 | — | IC50 | = | 315.0 | nM | 6.50 |
| CHEMBL4100288 | — | IC50 | = | 361.0 | nM | 6.44 |
| CHEMBL4072848 | — | IC50 | = | 391.0 | nM | 6.41 |
| CHEMBL4071005 | — | IC50 | = | 397.0 | nM | 6.40 |
| CHEMBL4067915 | — | IC50 | = | 511.0 | nM | 6.29 |
| CHEMBL4085737 | — | IC50 | = | 556.0 | nM | 6.25 |
| CHEMBL4064171 | — | IC50 | = | 656.0 | nM | 6.18 |
| CHEMBL4092626 | — | IC50 | = | 701.0 | nM | 6.15 |
| CHEMBL4079092 | — | IC50 | = | 783.0 | nM | 6.11 |
| CHEMBL4076473 | — | IC50 | = | 1012.0 | nM | 6.00 |
| CHEMBL4066193 | ATINVICITINIB | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL3703085 | — | IC50 | = | 1226.0 | nM | 5.91 |
| CHEMBL4098999 | — | IC50 | > | 1496.0 | nM | - |
| CHEMBL4088262 | — | IC50 | > | 1496.0 | nM | - |