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Assay Detail

CHEMBL3418947

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

Binding
Inhibition of Syk (unknown origin) using 5-Fluo-Ahx-GAPDYENLQELNKK-Amide as substrate after 60 mins by microfluidic mobility shift assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery and profiling of a selective and efficacious Syk inhibitor.
Thoma G, Smith AB, van Eis MJ, Vangrevelinghe E, Blanz J, Aichholz R, Littlewood-Evans A, Lee CC, Liu H, Zerwes HG.
J Med Chem (2015) 58 : 1950 -1963
PubMed 25633741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.87 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3416027 1 9.00
CHEMBL3416023 1 9.00
CHEMBL3262356 1 8.40
CHEMBL3416025 1 8.30
CHEMBL3416024 1 8.30
CHEMBL3262355 1 8.30
CHEMBL2177736 1 7.89
CHEMBL3416021 1 7.72
CHEMBL3262624 1 7.66
CHEMBL3416026 1 7.46
CHEMBL3416028 1 7.03
CHEMBL3416022 1 6.78
CHEMBL3265032 ENTOSPLETINIB 3.0 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3416027 IC50 = 1.0 nM 9.00
CHEMBL3416023 IC50 = 1.0 nM 9.00
CHEMBL3262356 IC50 = 4.0 nM 8.40
CHEMBL3416025 IC50 = 5.0 nM 8.30
CHEMBL3416024 IC50 = 5.0 nM 8.30
CHEMBL3262355 IC50 = 5.0 nM 8.30
CHEMBL2177736 IC50 = 13.0 nM 7.89
CHEMBL3416021 IC50 = 19.0 nM 7.72
CHEMBL3262624 IC50 = 22.0 nM 7.66
CHEMBL3416026 IC50 = 35.0 nM 7.46
CHEMBL3416028 IC50 = 94.0 nM 7.03
CHEMBL3416022 IC50 = 165.0 nM 6.78
CHEMBL3265032 ENTOSPLETINIB IC50 = 377.0 nM 6.42