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Assay Detail

CHEMBL3390067

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Binding
Inhibition of PLC gamma-1 phosphorylation in human Jurkat T cells after 30 mins
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Design, synthesis and structure-activity relationships of a novel class of sulfonylpyridine inhibitors of Interleukin-2 inducible T-cell kinase (ITK).
Trani G, Barker JJ, Bromidge SM, Brookfield FA, Burch JD, Chen Y, Eigenbrot C, Heifetz A, Ismaili MH, Johnson A, Krülle TM, MacKinnon CH, Maghames R, McEwan PA, Montalbetti CA, Ortwine DF, Pérez-Fuertes Y, Vaidya DG, Wang X, Zarrin AA, Pei Z.
Bioorg Med Chem Lett (2014) 24 : 5818 -5823
PubMed 25455497 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.20 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3355737 1 6.75
CHEMBL3355726 1 6.27
CHEMBL3355311 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3355737 IC50 = 180.0 nM 6.75
CHEMBL3355726 IC50 = 540.0 nM 6.27
CHEMBL3355311 IC50 = 2600.0 nM 5.58