Assay Detail
ADMET
CHEMBL4033007
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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 | 6.53 | 7.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4078799 | — | — | 1 | 7.41 |
| CHEMBL4089118 | — | — | 1 | 7.32 |
| CHEMBL4102140 | — | — | 1 | 7.27 |
| CHEMBL4061128 | — | — | 1 | 7.05 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 6.97 |
| CHEMBL4089234 | — | — | 1 | 6.85 |
| CHEMBL4077886 | — | — | 1 | 6.70 |
| CHEMBL4100288 | — | — | 1 | 6.68 |
| CHEMBL4066906 | — | — | 1 | 6.65 |
| CHEMBL4096821 | — | — | 1 | 6.59 |
| CHEMBL4085737 | — | — | 1 | 6.58 |
| CHEMBL4071005 | — | — | 1 | 6.50 |
| CHEMBL4104623 | — | — | 1 | 6.48 |
| CHEMBL4067915 | — | — | 1 | 6.38 |
| CHEMBL4072848 | — | — | 1 | 6.37 |
| CHEMBL4092626 | — | — | 1 | 6.28 |
| CHEMBL4076473 | — | — | 1 | 6.22 |
| CHEMBL4066193 | ATINVICITINIB | 2.0 | 1 | 6.22 |
| CHEMBL3703085 | — | — | 1 | 6.16 |
| CHEMBL4098999 | — | — | 1 | 6.13 |
| CHEMBL4064171 | — | — | 1 | 5.92 |
| CHEMBL4079092 | — | — | 1 | 5.79 |
| CHEMBL4088262 | — | — | 1 | 5.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4078799 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4089118 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4102140 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4061128 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4089234 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4077886 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4100288 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL4066906 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL4096821 | — | IC50 | = | 254.0 | nM | 6.59 |
| CHEMBL4085737 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL4071005 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4104623 | — | IC50 | = | 334.0 | nM | 6.48 |
| CHEMBL4067915 | — | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL4072848 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4092626 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4076473 | — | IC50 | = | 608.0 | nM | 6.22 |
| CHEMBL4066193 | ATINVICITINIB | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3703085 | — | IC50 | = | 692.0 | nM | 6.16 |
| CHEMBL4098999 | — | IC50 | = | 744.0 | nM | 6.13 |
| CHEMBL4064171 | — | IC50 | = | 1192.0 | nM | 5.92 |
| CHEMBL4079092 | — | IC50 | = | 1635.0 | nM | 5.79 |
| CHEMBL4088262 | — | IC50 | = | 2114.0 | nM | 5.67 |