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Assay Detail

CHEMBL3627445

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

Binding
Inhibition of Syk in anti-igM stimulated human Ramos B cells assessed as phospho-BLNK level preincubated for 30 mins followed by anti-IgM stimulation measured after 15 mins by flow cytometric analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase SYK (CHEMBL2599)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.
Thoma G, Veenstra S, Strang R, Blanz J, Vangrevelinghe E, Berghausen J, Lee CC, Zerwes HG.
Bioorg Med Chem Lett (2015) 25 : 4642 -4647
PubMed 26320624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.68 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3622204 1 7.05
CHEMBL3416026 1 7.00
CHEMBL3622698 1 6.97
CHEMBL3622208 1 6.88
CHEMBL3622206 1 6.79
CHEMBL3622209 1 6.78
CHEMBL2177736 1 6.75
CHEMBL3622207 1 6.61
CHEMBL3622203 1 6.55
CHEMBL3622205 1 6.55
CHEMBL3622697 1 6.48
CHEMBL3622210 1 6.47
CHEMBL30678 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3622204 IC50 = 89.0 nM 7.05
CHEMBL3416026 IC50 = 99.0 nM 7.00
CHEMBL3622698 IC50 = 107.0 nM 6.97
CHEMBL3622208 IC50 = 132.0 nM 6.88
CHEMBL3622206 IC50 = 161.0 nM 6.79
CHEMBL3622209 IC50 = 166.0 nM 6.78
CHEMBL2177736 IC50 = 178.0 nM 6.75
CHEMBL3622207 IC50 = 247.0 nM 6.61
CHEMBL3622203 IC50 = 284.0 nM 6.55
CHEMBL3622205 IC50 = 284.0 nM 6.55
CHEMBL3622697 IC50 = 328.0 nM 6.48
CHEMBL3622210 IC50 = 340.0 nM 6.47
CHEMBL30678 IC50 = 951.0 nM 6.02