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Assay Detail

CHEMBL4265579

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

Binding
Inhibition of JAK3 in human whole blood assessed as reduction in IL15-induced STAT5 phosphorylation preincubated for 75 mins followed by IL15 addition and measured after 15 mins by FACS analysis
11
Total Activities
11
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

Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.
Casimiro-Garcia A, Trujillo JI, Vajdos F, Juba B, Banker ME, Aulabaugh A, Balbo P, Bauman J, Chrencik J, Coe JW, Czerwinski R, Dowty M, Knafels JD, Kwon S, Leung L, Liang S, Robinson RP, Telliez JB, Unwalla R, Yang X, Thorarensen A.
J Med Chem (2018) 61 : 10665 -10699
PubMed 30423248 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.47 6.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4288086 1 6.02
CHEMBL4279720 1 5.26
CHEMBL4284396 1 5.14
CHEMBL4281393 1 -
CHEMBL4294868 1 -
CHEMBL4292320 1 -
CHEMBL4285555 1 -
CHEMBL4277610 1 -
CHEMBL4277193 1 -
CHEMBL4287845 1 -
CHEMBL4292341 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4288086 IC50 = 953.0 nM 6.02
CHEMBL4279720 IC50 = 5480.0 nM 5.26
CHEMBL4284396 IC50 = 7252.0 nM 5.14
CHEMBL4281393 IC50 > 10000.0 nM -
CHEMBL4294868 IC50 - -
CHEMBL4292320 IC50 - -
CHEMBL4285555 IC50 - -
CHEMBL4277610 IC50 > 10000.0 nM -
CHEMBL4277193 IC50 - -
CHEMBL4287845 IC50 > 10000.0 nM -
CHEMBL4292341 IC50 > 10000.0 nM -