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Assay Detail

CHEMBL4666925

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

Binding
Inhibition of recombinant human GST-tagged JAK1 (866 to 1154 residues) expressed in baculovirus expression system using Tyr 06 as substrate incubated for 60 mins by Z'-lyte assay
9
Total Activities
9
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

Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.
Zak M,Hanan EJ,Lupardus P,Brown DG,Robinson C,Siu M,Lyssikatos JP,Romero FA,Zhao G,Kellar T,Mendonca R,Ray NC,Goodacre SC,Crackett PH,McLean N,Hurley CA,Yuen PW,Cheng YX,Liu X,Liimatta M,Kohli PB,Nonomiya J,Salmon G,Buckley G,Lloyd J,Gibbons P,Ghilardi N,Kenny JR,Johnson A
Bioorg Med Chem Lett (2019) 29 : 1522 -1531
PubMed 30981576 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.51 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4744172 1 8.92
CHEMBL4777342 1 8.77
CHEMBL4760562 1 8.72
CHEMBL4745474 1 8.66
CHEMBL2178799 1 7.50
CHEMBL4740778 1 -
CHEMBL4742159 1 -
CHEMBL4764019 1 -
CHEMBL4746726 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4744172 IC50 = 1.2 nM 8.92
CHEMBL4777342 IC50 = 1.7 nM 8.77
CHEMBL4760562 IC50 = 1.9 nM 8.72
CHEMBL4745474 IC50 = 2.2 nM 8.66
CHEMBL2178799 IC50 = 32.0 nM 7.50
CHEMBL4740778 IC50 - -
CHEMBL4742159 IC50 - -
CHEMBL4764019 IC50 - -
CHEMBL4746726 IC50 - -