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Assay Detail

CHEMBL992575

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

Binding
Inhibition of human ITK expressed in chicken DT40 cells assessed as B cell receptor-stimulated calcium influx by FLIPR assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type DT40
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk).
Moriarty KJ, Takahashi H, Pullen SS, Khine HH, Sallati RH, Raymond EL, Woska JR, Jeanfavre DD, Roth GP, Winters MP, Qiao L, Ryan D, DesJarlais R, Robinson D, Wilson M, Bobko M, Cook BN, Lo HY, Nemoto PA, Kashem MA, Wolak JP, White A, Magolda RL, Tomczuk B.
Bioorg Med Chem Lett (2008) 18 : 5545 -5549
PubMed 18819799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.28 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483403 1 6.50
CHEMBL485031 1 6.29
CHEMBL485564 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483403 IC50 = 320.0 nM 6.50
CHEMBL485031 IC50 = 510.0 nM 6.29
CHEMBL485564 IC50 = 900.0 nM 6.05