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Assay Detail

CHEMBL981176

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Binding
Inhibition of human Syk
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

Lysine--tRNA ligase (CHEMBL5575)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A novel Syk family kinase inhibitor: design, synthesis, and structure-activity relationship of 1,2,4-triazolo[4,3-c]pyrimidine and 1,2,4-triazolo[1,5-c]pyrimidine derivatives.
Hirabayashi A, Mukaiyama H, Kobayashi H, Shiohara H, Nakayama S, Ozawa M, Miyazawa K, Misawa K, Ohnota H, Isaji M.
Bioorg Med Chem (2008) 16 : 7347 -7357
PubMed 18585046 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.72 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL475575 1 8.40
CHEMBL388978 STAUROSPORINE 1 8.05
CHEMBL475609 1 8.05
CHEMBL474582 1 8.05
CHEMBL471901 1 7.39
CHEMBL472840 1 7.30
CHEMBL478642 1 7.08
CHEMBL475882 1 6.92
CHEMBL476741 1 6.82
CHEMBL476537 1 5.21
CHEMBL477165 1 5.11
CHEMBL513915 1 4.82
CHEMBL514365 1 4.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL475575 IC50 = 4.0 nM 8.40
CHEMBL388978 STAUROSPORINE IC50 = 9.0 nM 8.05
CHEMBL475609 IC50 = 9.0 nM 8.05
CHEMBL474582 IC50 = 9.0 nM 8.05
CHEMBL471901 IC50 = 41.0 nM 7.39
CHEMBL472840 IC50 = 50.0 nM 7.30
CHEMBL478642 IC50 = 83.0 nM 7.08
CHEMBL475882 IC50 = 120.0 nM 6.92
CHEMBL476741 IC50 = 150.0 nM 6.82
CHEMBL476537 IC50 = 6100.0 nM 5.21
CHEMBL477165 IC50 = 7700.0 nM 5.11
CHEMBL513915 IC50 = 15200.0 nM 4.82
CHEMBL514365 IC50 = 79100.0 nM 4.10