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Assay Detail

CHEMBL2173408

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

Binding
Inhibition of SYK
44
Total Activities
44
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery and development of spleen tyrosine kinase (SYK) inhibitors.
Singh R, Masuda ES, Payan DG.
J Med Chem (2012) 55 : 3614 -3643
PubMed 22257213 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 6.46 8.40
Ki 7 7.36 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2170582 R-343 2.0 1 8.74
CHEMBL1235110 1 8.40
CHEMBL1190711 1 8.12
CHEMBL287478 1 8.10
CHEMBL2170585 1 8.00
CHEMBL431645 1 7.92
CHEMBL104279 1 7.85
CHEMBL282342 1 7.72
CHEMBL104519 1 7.70
CHEMBL475251 R-406 2.0 1 7.52
CHEMBL107061 1 7.50
CHEMBL30678 1 7.47
CHEMBL30548 1 7.14
CHEMBL30824 1 7.11
CHEMBL30873 1 7.05
CHEMBL515271 R-112 2.0 1 7.02
CHEMBL284675 1 6.85
CHEMBL318079 1 6.84
CHEMBL31141 1 6.80
CHEMBL56904 1 6.80
CHEMBL30826 1 6.72
CHEMBL30355 1 6.70
CHEMBL285346 1 6.58
CHEMBL285916 1 6.58
CHEMBL104813 1 6.56
CHEMBL33009 1 6.38
CHEMBL30774 1 6.31
CHEMBL30885 1 6.07
CHEMBL30661 1 5.96
CHEMBL30240 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2170582 R-343 Ki = 1.8 nM 8.74
CHEMBL1235110 IC50 = 4.0 nM 8.40
CHEMBL1190711 Ki = 7.5 nM 8.12
CHEMBL287478 IC50 = 8.0 nM 8.10
CHEMBL2170585 Ki = 10.0 nM 8.00
CHEMBL431645 IC50 = 12.0 nM 7.92
CHEMBL104279 IC50 = 14.0 nM 7.85
CHEMBL282342 IC50 = 19.0 nM 7.72
CHEMBL104519 IC50 = 20.0 nM 7.70
CHEMBL475251 R-406 Ki = 30.0 nM 7.52
CHEMBL107061 IC50 = 32.0 nM 7.50
CHEMBL30678 IC50 = 34.0 nM 7.47
CHEMBL30548 IC50 = 72.0 nM 7.14
CHEMBL30824 IC50 = 78.0 nM 7.11
CHEMBL30873 IC50 = 90.0 nM 7.05
CHEMBL515271 R-112 Ki = 96.0 nM 7.02
CHEMBL284675 IC50 = 140.0 nM 6.85
CHEMBL318079 IC50 = 145.0 nM 6.84
CHEMBL31141 IC50 = 160.0 nM 6.80
CHEMBL56904 Ki = 160.0 nM 6.80
CHEMBL30826 IC50 = 190.0 nM 6.72
CHEMBL30355 IC50 = 200.0 nM 6.70
CHEMBL285346 IC50 = 260.0 nM 6.58
CHEMBL285916 IC50 = 260.0 nM 6.58
CHEMBL104813 IC50 = 273.0 nM 6.56
CHEMBL33009 IC50 = 420.0 nM 6.38
CHEMBL30774 IC50 = 490.0 nM 6.31
CHEMBL30885 IC50 = 850.0 nM 6.07
CHEMBL30661 IC50 = 1100.0 nM 5.96
CHEMBL30240 IC50 = 1200.0 nM 5.92
CHEMBL31668 IC50 = 1500.0 nM 5.82
CHEMBL28 APIGENIN IC50 = 4200.0 nM 5.38
CHEMBL941 IMATINIB Ki = 5000.0 nM 5.30
CHEMBL164 MYRICETIN IC50 = 6400.0 nM 5.19
CHEMBL105421 IC50 = 8100.0 nM 5.09
CHEMBL151 LUTEOLIN IC50 = 12000.0 nM 4.92
CHEMBL31574 FISETIN IC50 = 15000.0 nM 4.82
CHEMBL50 QUERCETIN IC50 = 20000.0 nM 4.70
CHEMBL28626 MORIN IC50 = 28000.0 nM 4.55
CHEMBL33373 IC50 = 40000.0 nM 4.40
CHEMBL33984 IC50 > 30.0 ug.mL-1 -
CHEMBL434202 IC50 > 30.0 ug.mL-1 -
CHEMBL417315 IC50 > 30.0 ug.mL-1 -
CHEMBL30271 IC50 > 30.0 ug.mL-1 -