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Assay Detail

CHEMBL4308760

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

Binding
Effect on ZAP70 phosphorylation in human Jurkat cells pre-incubated for 30 mins followed by anti-CD3/CD28 stimulation measured after 10 mins
14
Total Activities
14
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

Target

Tyrosine-protein kinase ZAP-70 (CHEMBL2803)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Pyridazinone and Pyrazolo[1,5-a]pyridine Inhibitors of C-Terminal Src Kinase.
O'Malley DP, Ahuja V, Fink B, Cao C, Wang C, Swanson J, Wee S, Gavai AV, Tokarski J, Critton D, Paiva AA, Johnson BM, Szapiel N, Xie D.
ACS Med Chem Lett (2019) 10 : 1486 -1491
PubMed 31620238 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 6.40 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4582324 1 7.55
CHEMBL4445994 1 7.39
CHEMBL4577049 1 7.38
CHEMBL4443654 1 7.31
CHEMBL4537527 1 7.25
CHEMBL4545269 1 7.06
CHEMBL4437906 1 6.38
CHEMBL4483095 1 5.85
CHEMBL4591137 1 5.70
CHEMBL4588040 1 5.57
CHEMBL4518970 1 5.39
CHEMBL4555519 1 5.24
CHEMBL4559531 1 5.10
CHEMBL4469360 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4582324 EC50 = 28.0 nM 7.55
CHEMBL4445994 EC50 = 41.0 nM 7.39
CHEMBL4577049 EC50 = 42.0 nM 7.38
CHEMBL4443654 EC50 = 49.0 nM 7.31
CHEMBL4537527 EC50 = 56.0 nM 7.25
CHEMBL4545269 EC50 = 88.0 nM 7.06
CHEMBL4437906 EC50 = 420.0 nM 6.38
CHEMBL4483095 EC50 = 1400.0 nM 5.85
CHEMBL4591137 EC50 = 2000.0 nM 5.70
CHEMBL4588040 EC50 = 2700.0 nM 5.57
CHEMBL4518970 EC50 = 4050.0 nM 5.39
CHEMBL4555519 EC50 = 5700.0 nM 5.24
CHEMBL4559531 EC50 = 7900.0 nM 5.10
CHEMBL4469360 EC50 > 20000.0 nM -