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Assay Detail

CHEMBL5141276

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

Binding
Inhibition of GST tagged recombinant human JAK3 expressed in baculovirus infection system by FRET assay
22
Total Activities
22
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

Discovery of Hexahydrofuro[3,2-<i>b</i>]furans as New Kinase-Selective and Orally Bioavailable JAK3 Inhibitors for the Treatment of Leukemia Harboring a JAK3 Activating Mutant.
Li S, Si H, Song X, Lei C, He X, Wang J, Liu Y, Zhou Y, Song JG, Peng L, Tang X, Chan S, Ren X, Tu Z, Li Z, Wang Z, Zhang Z, Ding K.
J Med Chem (2022) 65 : 10674 -10690
PubMed 35860875 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 8.54 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5193702 1 8.92
CHEMBL5189603 1 8.92
CHEMBL5192736 1 8.92
CHEMBL5176661 1 8.89
CHEMBL5180117 1 8.89
CHEMBL5186937 1 8.89
CHEMBL5201705 1 8.89
CHEMBL5184187 1 8.82
CHEMBL5205480 1 8.82
CHEMBL5182065 1 8.80
CHEMBL5208026 1 8.77
CHEMBL5191734 1 8.74
CHEMBL5190599 1 8.72
CHEMBL5174210 1 8.72
CHEMBL5184019 1 8.66
CHEMBL4085457 RITLECITINIB 4.0 1 8.64
CHEMBL5185016 1 8.60
CHEMBL5207354 1 8.26
CHEMBL221959 TOFACITINIB 4.0 1 8.17
CHEMBL5185440 1 7.75
CHEMBL5182374 1 7.50
CHEMBL5203904 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5193702 IC50 = 1.2 nM 8.92
CHEMBL5189603 IC50 = 1.2 nM 8.92
CHEMBL5192736 IC50 = 1.2 nM 8.92
CHEMBL5176661 IC50 = 1.3 nM 8.89
CHEMBL5180117 IC50 = 1.3 nM 8.89
CHEMBL5186937 IC50 = 1.3 nM 8.89
CHEMBL5201705 IC50 = 1.3 nM 8.89
CHEMBL5184187 IC50 = 1.5 nM 8.82
CHEMBL5205480 IC50 = 1.5 nM 8.82
CHEMBL5182065 IC50 = 1.6 nM 8.80
CHEMBL5208026 IC50 = 1.7 nM 8.77
CHEMBL5191734 IC50 = 1.8 nM 8.74
CHEMBL5190599 IC50 = 1.9 nM 8.72
CHEMBL5174210 IC50 = 1.9 nM 8.72
CHEMBL5184019 IC50 = 2.2 nM 8.66
CHEMBL4085457 RITLECITINIB IC50 = 2.3 nM 8.64
CHEMBL5185016 IC50 = 2.5 nM 8.60
CHEMBL5207354 IC50 = 5.5 nM 8.26
CHEMBL221959 TOFACITINIB IC50 = 6.7 nM 8.17
CHEMBL5185440 IC50 = 18.0 nM 7.75
CHEMBL5182374 IC50 = 32.0 nM 7.50
CHEMBL5203904 IC50 = 268.0 nM 6.57