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Assay Detail

CHEMBL3865668

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

Functional
Inhibition of CysLT release from IgE/human IL3 activated basophils in human whole blood preincubated for 30 mins followed by IL-3 stimulation for 15 mins and subsequent stimulation by IgE for 20 mins by LTC4-alkaline phosphatase coupled assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 1 — Organism
Curated By Autocuration

Target

Blood (CHEMBL613416)
Type TISSUE
Organism Homo sapiens

Publication

Carboxamide Spleen Tyrosine Kinase (Syk) Inhibitors: Leveraging Ground State Interactions To Accelerate Optimization.
Ellis JM, Altman MD, Cash B, Haidle AM, Kubiak RL, Maddess ML, Yan Y, Northrup AB.
ACS Med Chem Lett (2016) 7 : 1151 -1155
PubMed 27994755 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.09 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3415583 1 7.24
CHEMBL3415610 1 7.21
CHEMBL3943181 1 7.03
CHEMBL3414584 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3415583 IC50 = 58.0 nM 7.24
CHEMBL3415610 IC50 = 62.0 nM 7.21
CHEMBL3943181 IC50 = 93.0 nM 7.03
CHEMBL3414584 IC50 = 130.0 nM 6.89