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Assay Detail

CHEMBL3418948

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

ADMET
Cytotoxicity against C57BL/6 mouse bone marrow cells assessed as growth inhibition preincubated for 4 days followed by [3H]-thymidine addition measured after 5 hrs by betaplate counting analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Mus musculus
Cell Type Bone marrow cell
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

ADMET (CHEMBL612558)
Type ADMET

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 5.63 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3262355 1 6.60
CHEMBL3265032 ENTOSPLETINIB 3.0 1 6.24
CHEMBL3416025 1 6.09
CHEMBL3416023 1 5.68
CHEMBL3416021 1 5.58
CHEMBL3262356 1 5.47
CHEMBL3262624 1 5.45
CHEMBL3416027 1 5.28
CHEMBL3416024 1 5.28
CHEMBL2177736 1 5.23
CHEMBL3416026 1 5.04
CHEMBL3416028 1 -
CHEMBL3416022 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3262355 IC50 = 249.0 nM 6.60
CHEMBL3265032 ENTOSPLETINIB IC50 = 582.0 nM 6.24
CHEMBL3416025 IC50 = 811.0 nM 6.09
CHEMBL3416023 IC50 = 2110.0 nM 5.68
CHEMBL3416021 IC50 = 2601.0 nM 5.58
CHEMBL3262356 IC50 = 3411.0 nM 5.47
CHEMBL3262624 IC50 = 3515.0 nM 5.45
CHEMBL3416027 IC50 = 5270.0 nM 5.28
CHEMBL3416024 IC50 = 5267.0 nM 5.28
CHEMBL2177736 IC50 = 5853.0 nM 5.23
CHEMBL3416026 IC50 = 9020.0 nM 5.04
CHEMBL3416028 IC50 > 10000.0 nM -
CHEMBL3416022 IC50 > 10000.0 nM -