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Assay Detail

CHEMBL3268713

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

Binding
Inhibition of Syk in anti IgM-stimulated human Ramos cells assessed as BLNK phosphorylation by cellular assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Syk inhibitors with high potency in presence of blood.
Thoma G, Blanz J, Bühlmayer P, Drückes P, Kittelmann M, Smith AB, van Eis M, Vangrevelinghe E, Zerwes HG, Che JJ, He X, Jin Y, Lee CC, Michellys PY, Uno T, Liu H.
Bioorg Med Chem Lett (2014) 24 : 2278 -2282
PubMed 24726806 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.77 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3262616 1 7.46
CHEMBL3262620 1 7.43
CHEMBL3262357 1 7.33
CHEMBL3262624 1 7.26
CHEMBL3262617 1 7.22
CHEMBL3262622 1 7.11
CHEMBL3262356 1 7.05
CHEMBL3262625 1 7.02
CHEMBL2177736 1 6.75
CHEMBL3262618 1 6.68
CHEMBL3262623 1 6.55
CHEMBL3262358 1 6.50
CHEMBL3262619 1 6.42
CHEMBL475251 R-406 2.0 1 6.34
CHEMBL3262355 1 6.11
CHEMBL3262359 1 5.03
CHEMBL3262621 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3262616 IC50 = 35.0 nM 7.46
CHEMBL3262620 IC50 = 37.0 nM 7.43
CHEMBL3262357 IC50 = 47.0 nM 7.33
CHEMBL3262624 IC50 = 55.0 nM 7.26
CHEMBL3262617 IC50 = 60.0 nM 7.22
CHEMBL3262622 IC50 = 78.0 nM 7.11
CHEMBL3262356 IC50 = 90.0 nM 7.05
CHEMBL3262625 IC50 = 95.0 nM 7.02
CHEMBL2177736 IC50 = 178.0 nM 6.75
CHEMBL3262618 IC50 = 209.0 nM 6.68
CHEMBL3262623 IC50 = 283.0 nM 6.55
CHEMBL3262358 IC50 = 320.0 nM 6.50
CHEMBL3262619 IC50 = 378.0 nM 6.42
CHEMBL475251 R-406 IC50 = 457.0 nM 6.34
CHEMBL3262355 IC50 = 778.0 nM 6.11
CHEMBL3262359 IC50 = 9274.0 nM 5.03
CHEMBL3262621 IC50 - -