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Assay Detail

CHEMBL5658249

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

Binding
Inhibition of JAK3 (unknown origin) in presence of ATP by radiometric assay
13
Total Activities
13
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 JAK3 (CHEMBL2148)
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 13 8.69 9.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4564280 1 9.90
CHEMBL5188882 1 9.81
CHEMBL221959 TOFACITINIB 4.0 1 9.54
CHEMBL2325895 1 9.52
CHEMBL5661829 1 9.05
CHEMBL1650951 1 8.82
CHEMBL5661904 1 8.52
CHEMBL3601223 1 8.32
CHEMBL5661931 1 8.15
CHEMBL5661858 1 7.70
CHEMBL4128410 1 7.66
CHEMBL4204801 1 7.31
CHEMBL3601115 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4564280 IC50 = 0.127 nM 9.90
CHEMBL5188882 IC50 = 0.154 nM 9.81
CHEMBL221959 TOFACITINIB IC50 = 0.292 nM 9.54
CHEMBL2325895 IC50 = 0.3 nM 9.52
CHEMBL5661829 IC50 = 0.9 nM 9.05
CHEMBL1650951 IC50 = 1.5 nM 8.82
CHEMBL5661904 IC50 = 3.0 nM 8.52
CHEMBL3601223 IC50 = 4.8 nM 8.32
CHEMBL5661931 IC50 = 7.0 nM 8.15
CHEMBL5661858 IC50 = 20.0 nM 7.70
CHEMBL4128410 IC50 = 22.0 nM 7.66
CHEMBL4204801 IC50 = 49.0 nM 7.31
CHEMBL3601115 IC50 < 0.5 nM -