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Assay Detail

CHEMBL1006239

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

Binding
Inhibition of ITK in chicken DT40 B cells assessed as calcium flux inhibition assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Gallus gallus
Cell Type B
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

5-Aminomethyl-1H-benzimidazoles as orally active inhibitors of inducible T-cell kinase (Itk).
Winters MP, Robinson DJ, Khine HH, Pullen SS, Woska JR, Raymond EL, Sellati R, Cywin CL, Snow RJ, Kashem MA, Wolak JP, King J, Kaplita PV, Liu LH, Farrell TM, DesJarlais R, Roth GP, Takahashi H, Moriarty KJ.
Bioorg Med Chem Lett (2008) 18 : 5541 -5544
PubMed 18823779 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.44 7.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL528989 1 7.12
CHEMBL460824 1 6.47
CHEMBL486757 1 6.39
CHEMBL488398 1 6.27
CHEMBL488187 1 6.22
CHEMBL487982 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL528989 IC50 = 75.0 nM 7.12
CHEMBL460824 IC50 = 340.0 nM 6.47
CHEMBL486757 IC50 = 410.0 nM 6.39
CHEMBL488398 IC50 = 540.0 nM 6.27
CHEMBL488187 IC50 = 600.0 nM 6.22
CHEMBL487982 IC50 = 650.0 nM 6.19