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Assay Detail

CHEMBL4701487

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Binding
Inhibition of SYK (unknown origin)
25
Total Activities
25
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

Novel potent and selective pyrazolylpyrimidine-based SYK inhibitors.
Barlaam B,Boiko S,Boyd S,Dry H,Gingipalli L,Ikeda T,Johnson T,Kawatkar S,Lorthioir O,Pike A,Pollard H,Read J,Su Q,Wang H,Wang H,Wang L,Wang P,Edmondson SD
Bioorg Med Chem Lett (2020) 30 : 127523 -127523
PubMed 32877741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 9.12 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4758052 1 9.72
CHEMBL4740533 1 9.70
CHEMBL4740065 1 9.68
CHEMBL4797815 1 9.66
CHEMBL4785413 1 9.64
CHEMBL4800498 1 9.62
CHEMBL4776734 1 9.52
CHEMBL4751083 1 9.51
CHEMBL4786007 1 9.48
CHEMBL4742918 1 9.47
CHEMBL4748041 1 9.47
CHEMBL4763433 1 9.44
CHEMBL4795975 1 9.40
CHEMBL4782062 1 9.29
CHEMBL4753097 1 9.22
CHEMBL4760325 1 9.14
CHEMBL4796370 1 9.08
CHEMBL4741509 1 9.06
CHEMBL4758301 1 8.89
CHEMBL4743842 1 8.82
CHEMBL4760470 1 8.54
CHEMBL4741959 1 8.49
CHEMBL4787606 1 8.10
CHEMBL4781915 1 7.96
CHEMBL4786769 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4758052 IC50 = 0.19 nM 9.72
CHEMBL4740533 IC50 = 0.2 nM 9.70
CHEMBL4740065 IC50 = 0.21 nM 9.68
CHEMBL4797815 IC50 = 0.22 nM 9.66
CHEMBL4785413 IC50 = 0.23 nM 9.64
CHEMBL4800498 IC50 = 0.24 nM 9.62
CHEMBL4776734 IC50 = 0.3 nM 9.52
CHEMBL4751083 IC50 = 0.31 nM 9.51
CHEMBL4786007 IC50 = 0.33 nM 9.48
CHEMBL4742918 IC50 = 0.34 nM 9.47
CHEMBL4748041 IC50 = 0.34 nM 9.47
CHEMBL4763433 IC50 = 0.36 nM 9.44
CHEMBL4795975 IC50 = 0.4 nM 9.40
CHEMBL4782062 IC50 = 0.51 nM 9.29
CHEMBL4753097 IC50 = 0.6 nM 9.22
CHEMBL4760325 IC50 = 0.73 nM 9.14
CHEMBL4796370 IC50 = 0.83 nM 9.08
CHEMBL4741509 IC50 = 0.88 nM 9.06
CHEMBL4758301 IC50 = 1.3 nM 8.89
CHEMBL4743842 IC50 = 1.5 nM 8.82
CHEMBL4760470 IC50 = 2.9 nM 8.54
CHEMBL4741959 IC50 = 3.2 nM 8.49
CHEMBL4787606 IC50 = 7.9 nM 8.10
CHEMBL4781915 IC50 = 11.0 nM 7.96
CHEMBL4786769 IC50 = 62.0 nM 7.21