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Assay Detail

CHEMBL2019769

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

Functional
Inhibition of IgE-mediated human LAD2 cell degranulation assessed as beta-hexosaminidase release using p-nitrophenyl-N-acetyl-D-glucosamide as substrate preincubated for 30 mins measured 90 mins after substrate addition by spectrophotometric analysis
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type LAD2
Confidence 1 — Organism
Curated By Autocuration

Target

LAD2 (CHEMBL4483253)
Type CELL-LINE
Organism Homo sapiens

Publication

Pyrazine-based Syk kinase inhibitors.
Forns P, Esteve C, Taboada L, Alonso JA, Orellana A, Maldonado M, Carreño C, Ramis I, López M, Miralpeix M, Vidal B.
Bioorg Med Chem Lett (2012) 22 : 2784 -2788
PubMed 22425453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.62 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2018022 1 7.05
CHEMBL2018020 1 7.00
CHEMBL2018025 1 6.96
CHEMBL2018145 1 6.92
CHEMBL2018029 1 6.92
CHEMBL2018018 1 6.92
CHEMBL2018147 1 6.85
CHEMBL2018026 1 6.85
CHEMBL2018024 1 6.85
CHEMBL2018023 1 6.82
CHEMBL2018032 1 6.80
CHEMBL2018027 1 6.77
CHEMBL2018019 1 6.75
CHEMBL2018143 1 6.75
CHEMBL2018146 1 6.75
CHEMBL2018028 1 6.66
CHEMBL2018144 1 6.40
CHEMBL2018016 1 6.26
CHEMBL2018015 1 6.25
CHEMBL2018012 1 6.07
CHEMBL2018030 1 6.00
CHEMBL2018010 1 5.96
CHEMBL2018009 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2018022 IC50 = 90.0 nM 7.05
CHEMBL2018020 IC50 = 100.0 nM 7.00
CHEMBL2018025 IC50 = 110.0 nM 6.96
CHEMBL2018145 IC50 = 120.0 nM 6.92
CHEMBL2018029 IC50 = 120.0 nM 6.92
CHEMBL2018018 IC50 = 120.0 nM 6.92
CHEMBL2018147 IC50 = 140.0 nM 6.85
CHEMBL2018026 IC50 = 140.0 nM 6.85
CHEMBL2018024 IC50 = 140.0 nM 6.85
CHEMBL2018023 IC50 = 150.0 nM 6.82
CHEMBL2018032 IC50 = 160.0 nM 6.80
CHEMBL2018027 IC50 = 170.0 nM 6.77
CHEMBL2018019 IC50 = 180.0 nM 6.75
CHEMBL2018143 IC50 = 180.0 nM 6.75
CHEMBL2018146 IC50 = 180.0 nM 6.75
CHEMBL2018028 IC50 = 220.0 nM 6.66
CHEMBL2018144 IC50 = 400.0 nM 6.40
CHEMBL2018016 IC50 = 550.0 nM 6.26
CHEMBL2018015 IC50 = 560.0 nM 6.25
CHEMBL2018012 IC50 = 860.0 nM 6.07
CHEMBL2018030 IC50 = 1000.0 nM 6.00
CHEMBL2018010 IC50 = 1100.0 nM 5.96
CHEMBL2018009 IC50 = 1960.0 nM 5.71