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Assay Detail

CHEMBL861673

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Functional
Inhibition of anti-CD3 antibody-induced IL2 production in human jurkat T cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Jurkat
Confidence 9 — Direct single protein target
Curated By Expert

Target

Tyrosine-protein kinase ITK/TSK (CHEMBL2959)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors.
Das J, Liu C, Moquin RV, Lin J, Furch JA, Spergel SH, Doweyko AM, McIntyre KW, Shuster DJ, O'Day KD, Penhallow B, Hung CY, Kanner SB, Lin TA, Dodd JH, Barrish JC, Wityak J.
Bioorg Med Chem Lett (2006) 16 : 2411 -2415
PubMed 16481166 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.63 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381296 1 6.16
CHEMBL382362 1 6.16
CHEMBL381367 1 5.70
CHEMBL383129 1 5.66
CHEMBL208255 1 5.62
CHEMBL204418 1 5.24
CHEMBL207329 1 4.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381296 IC50 = 700.0 nM 6.16
CHEMBL382362 IC50 = 700.0 nM 6.16
CHEMBL381367 IC50 = 2000.0 nM 5.70
CHEMBL383129 IC50 = 2200.0 nM 5.66
CHEMBL208255 IC50 = 2400.0 nM 5.62
CHEMBL204418 IC50 = 5700.0 nM 5.24
CHEMBL207329 IC50 = 13500.0 nM 4.87