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Assay Detail

CHEMBL4005714

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

Binding
Inhibition of JAK3 in human whole blood assessed as inhibition of IL-15 induced STAT5 phosphorylation preincubated for 45 mins followed by IL-15 addition and measured after 15 mins by Alexa Fluor 647 staining based flow cytometric analysis
8
Total Activities
8
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

Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.
Thorarensen A, Dowty ME, Banker ME, Juba B, Jussif J, Lin T, Vincent F, Czerwinski RM, Casimiro-Garcia A, Unwalla R, Trujillo JI, Liang S, Balbo P, Che Y, Gilbert AM, Brown MF, Hayward M, Montgomery J, Leung L, Yang X, Soucy S, Hegen M, Coe J, Langille J, Vajdos F, Chrencik J, Telliez JB.
J Med Chem (2017) 60 : 1971 -1993
PubMed 28139931 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.25 6.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4085457 RITLECITINIB 4.0 1 6.71
CHEMBL4064018 1 6.40
CHEMBL4062946 1 6.24
CHEMBL4085582 1 5.64
CHEMBL4083094 1 -
CHEMBL4090883 1 -
CHEMBL4075230 1 -
CHEMBL4095629 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4085457 RITLECITINIB IC50 = 197.0 nM 6.71
CHEMBL4064018 IC50 = 399.0 nM 6.40
CHEMBL4062946 IC50 = 580.0 nM 6.24
CHEMBL4085582 IC50 = 2280.0 nM 5.64
CHEMBL4083094 IC50 - -
CHEMBL4090883 IC50 - -
CHEMBL4075230 IC50 - -
CHEMBL4095629 IC50 - -