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Assay Detail

CHEMBL807574

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Binding
Inhibitory activity against spleen tyrosine kinase (SYK)
ChEMBL ↗
57
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Spleen
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Discovery and SAR of novel Naphthyridines as potent inhibitors of spleen tyrosine kinase (SYK).
Cywin CL, Zhao BP, McNeil DW, Hrapchak M, Prokopowicz AS, Goldberg DR, Morwick TM, Gao A, Jakes S, Kashem M, Magolda RL, Soll RM, Player MR, Bobko MA, Rinker J, DesJarlais RL, Winters MP.
Bioorg Med Chem Lett (2003) 13 : 1415 -1418
PubMed 12668002 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 6.35 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287478 — — 1 8.10
CHEMBL282342 — — 1 7.72
CHEMBL30381 — — 1 7.70
CHEMBL30678 — — 1 7.47
CHEMBL284590 — — 1 7.47
CHEMBL30708 — — 1 7.37
CHEMBL33466 — — 1 7.20
CHEMBL285889 — — 1 7.15
CHEMBL30548 — — 1 7.14
CHEMBL30824 — — 1 7.11
CHEMBL30873 — — 1 7.05
CHEMBL33626 — — 1 6.92
CHEMBL281696 — — 1 6.85
CHEMBL284675 — — 1 6.85
CHEMBL31141 — — 1 6.80
CHEMBL30826 — — 1 6.72
CHEMBL30514 — — 1 6.70
CHEMBL30355 — — 1 6.70
CHEMBL281108 — — 1 6.68
CHEMBL30566 — — 1 6.64
CHEMBL285346 — — 1 6.58
CHEMBL285916 — — 1 6.58
CHEMBL30633 — — 1 6.51
CHEMBL30123 — — 1 6.48
CHEMBL33009 — — 1 6.38
CHEMBL30706 — — 1 6.38
CHEMBL30588 — — 1 6.36
CHEMBL30774 — — 1 6.31
CHEMBL34104 — — 1 6.30
CHEMBL30949 — — 2 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287478 — IC50 = 8.0 nM 8.10
CHEMBL282342 — IC50 = 19.0 nM 7.72
CHEMBL30381 — IC50 = 20.0 nM 7.70
CHEMBL284590 — IC50 = 34.0 nM 7.47
CHEMBL30678 — IC50 = 34.0 nM 7.47
CHEMBL30708 — IC50 = 43.0 nM 7.37
CHEMBL33466 — IC50 = 63.0 nM 7.20
CHEMBL285889 — IC50 = 71.0 nM 7.15
CHEMBL30548 — IC50 = 72.0 nM 7.14
CHEMBL30824 — IC50 = 78.0 nM 7.11
CHEMBL30873 — IC50 = 90.0 nM 7.05
CHEMBL33626 — IC50 = 120.0 nM 6.92
CHEMBL281696 — IC50 = 140.0 nM 6.85
CHEMBL284675 — IC50 = 140.0 nM 6.85
CHEMBL31141 — IC50 = 160.0 nM 6.80
CHEMBL30826 — IC50 = 190.0 nM 6.72
CHEMBL30355 — IC50 = 200.0 nM 6.70
CHEMBL30514 — IC50 = 200.0 nM 6.70
CHEMBL281108 — IC50 = 210.0 nM 6.68
CHEMBL30566 — IC50 = 230.0 nM 6.64
CHEMBL285916 — IC50 = 260.0 nM 6.58
CHEMBL285346 — IC50 = 260.0 nM 6.58
CHEMBL30633 — IC50 = 310.0 nM 6.51
CHEMBL30123 — IC50 = 330.0 nM 6.48
CHEMBL30706 — IC50 = 420.0 nM 6.38
CHEMBL33009 — IC50 = 420.0 nM 6.38
CHEMBL30588 — IC50 = 440.0 nM 6.36
CHEMBL30774 — IC50 = 490.0 nM 6.31
CHEMBL34104 — IC50 = 500.0 nM 6.30
CHEMBL30949 — IC50 = 500.0 nM 6.30
CHEMBL33069 — IC50 = 830.0 nM 6.08
CHEMBL30885 — IC50 = 850.0 nM 6.07
CHEMBL30640 — IC50 = 850.0 nM 6.07
CHEMBL30642 — IC50 = 890.0 nM 6.05
CHEMBL30823 — IC50 = 900.0 nM 6.05
CHEMBL30661 — IC50 = 1100.0 nM 5.96
CHEMBL30240 — IC50 = 1200.0 nM 5.92
CHEMBL30949 — IC50 = 1300.0 nM 5.89
CHEMBL30388 — IC50 = 1500.0 nM 5.82
CHEMBL31668 — IC50 = 1500.0 nM 5.82
CHEMBL440797 — IC50 = 1600.0 nM 5.80
CHEMBL281078 — IC50 = 1700.0 nM 5.77
CHEMBL281965 — IC50 = 3600.0 nM 5.44
CHEMBL30716 — IC50 = 3800.0 nM 5.42
CHEMBL30723 — IC50 = 5900.0 nM 5.23
CHEMBL281015 — IC50 = 8600.0 nM 5.07
CHEMBL283181 — IC50 = 13000.0 nM 4.89
CHEMBL34211 — IC50 = 17000.0 nM 4.77
CHEMBL33175 — IC50 = 25000.0 nM 4.60
CHEMBL33373 — IC50 = 40000.0 nM 4.40