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Assay Detail

CHEMBL5658247

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Binding
Inhibition of JAK1 (unknown origin) in presence of ATP by radiometric assay
4
Total Activities
4
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

Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket.
Forster M, Chaikuad A, Bauer SM, Holstein J, Robers MB, Corona CR, Gehringer M, Pfaffenrot E, Ghoreschi K, Knapp S, Laufer SA.
Cell Chem Biol (2016) 23 : 1335 -1340
PubMed 27840070 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.87 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL221959 TOFACITINIB 4.0 1 9.30
CHEMBL4128410 1 7.72
CHEMBL4564280 1 7.28
CHEMBL5188882 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL221959 TOFACITINIB IC50 = 0.496 nM 9.30
CHEMBL4128410 IC50 = 19.0 nM 7.72
CHEMBL4564280 IC50 = 52.0 nM 7.28
CHEMBL5188882 IC50 = 64.0 nM 7.19