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Assay Detail

CHEMBL4003454

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

Binding
Inhibition of GST tagged human recombinant JAK1 catalytic domain expressed in baculovirus using peptide substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by microfluidic assay
19
Total Activities
19
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

Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
Jones P, Storer RI, Sabnis YA, Wakenhut FM, Whitlock GA, England KS, Mukaiyama T, Dehnhardt CM, Coe JW, Kortum SW, Chrencik JE, Brown DG, Jones RM, Murphy JR, Yeoh T, Morgan P, Kilty I.
J Med Chem (2017) 60 : 767 -786
PubMed 27983835 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.25 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3928932 1 9.40
CHEMBL4093813 1 9.30
CHEMBL4103980 1 9.10
CHEMBL4086057 1 9.05
CHEMBL4069951 1 8.89
CHEMBL4096219 1 8.77
CHEMBL4097152 1 8.74
CHEMBL4066236 1 8.68
CHEMBL3644620 1 8.66
CHEMBL4089515 1 8.64
CHEMBL3914503 1 8.21
CHEMBL4078165 1 8.12
CHEMBL4104931 1 8.01
CHEMBL4087076 1 7.57
CHEMBL4068357 1 7.43
CHEMBL4101534 1 7.22
CHEMBL3929865 1 7.16
CHEMBL4074855 1 5.56
CHEMBL3644618 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3928932 IC50 = 0.4 nM 9.40
CHEMBL4093813 IC50 = 0.5 nM 9.30
CHEMBL4103980 IC50 = 0.8 nM 9.10
CHEMBL4086057 IC50 = 0.9 nM 9.05
CHEMBL4069951 IC50 = 1.3 nM 8.89
CHEMBL4096219 IC50 = 1.7 nM 8.77
CHEMBL4097152 IC50 = 1.8 nM 8.74
CHEMBL4066236 IC50 = 2.1 nM 8.68
CHEMBL3644620 IC50 = 2.2 nM 8.66
CHEMBL4089515 IC50 = 2.3 nM 8.64
CHEMBL3914503 IC50 = 6.1 nM 8.21
CHEMBL4078165 IC50 = 7.5 nM 8.12
CHEMBL4104931 IC50 = 9.7 nM 8.01
CHEMBL4087076 IC50 = 26.8 nM 7.57
CHEMBL4068357 IC50 = 37.5 nM 7.43
CHEMBL4101534 IC50 = 60.0 nM 7.22
CHEMBL3929865 IC50 = 68.6 nM 7.16
CHEMBL4074855 IC50 = 2756.5 nM 5.56
CHEMBL3644618 IC50 < 0.1 nM -