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Assay Detail

CHEMBL4723819

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human JAK1 (866 to end residues) using GEEPLYWSFPAKKK as substrate after 40 mins by [gamma-33ATP] radiometric assay
8
Total Activities
8
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

Target

Tyrosine-protein kinase JAK1 (CHEMBL2835)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms.
Yang T,Hu M,Chen Y,Xiang M,Tang M,Qi W,Shi M,He J,Yuan X,Zhang C,Liu K,Li J,Yang Z,Chen L
J Med Chem (2020) 63 : 14921 -14936
PubMed 33256400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.38 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4789273 1 7.62
CHEMBL4754856 1 7.58
CHEMBL4741075 1 7.52
CHEMBL4753549 1 7.38
CHEMBL4798378 1 7.37
CHEMBL4748354 1 7.33
CHEMBL4759953 1 7.22
CHEMBL4756422 1 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4789273 IC50 = 24.0 nM 7.62
CHEMBL4754856 IC50 = 26.0 nM 7.58
CHEMBL4741075 IC50 = 30.0 nM 7.52
CHEMBL4753549 IC50 = 42.0 nM 7.38
CHEMBL4798378 IC50 = 43.0 nM 7.37
CHEMBL4748354 IC50 = 47.0 nM 7.33
CHEMBL4759953 IC50 = 60.0 nM 7.22
CHEMBL4756422 IC50 = 91.0 nM 7.04