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Assay Detail

CHEMBL4010460

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

Binding
Inhibition of SYK (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 25 mins
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

Discovery of new Syk inhibitors through structure-based virtual screening.
Huang Y, Zhang Y, Fan K, Dong G, Li B, Zhang W, Li J, Sheng C.
Bioorg Med Chem Lett (2017) 27 : 1776 -1779
PubMed 28268139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.07 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4065618 1 8.70
CHEMBL2017552 1 8.40
CHEMBL512172 1 8.22
CHEMBL2017551 1 8.10
CHEMBL4103500 1 7.70
CHEMBL2347996 1 7.58
CHEMBL4077712 1 7.39
CHEMBL4104392 1 7.33
CHEMBL3125861 1 7.00
CHEMBL1458891 1 6.92
CHEMBL4104855 1 5.72
CHEMBL4079394 1 5.50
CHEMBL4103655 1 5.48
CHEMBL4067688 1 5.47
CHEMBL4077136 1 5.40
CHEMBL4089803 1 5.15
CHEMBL4090023 1 5.00
CHEMBL4062804 1 4.77
CHEMBL4100895 1 4.70
CHEMBL4075601 1 4.62
CHEMBL4082917 1 4.57
CHEMBL4104278 1 4.55
CHEMBL4070445 1 4.55
CHEMBL4099920 1 4.52
CHEMBL3192431 1 4.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4065618 IC50 = 2.0 nM 8.70
CHEMBL2017552 IC50 = 4.0 nM 8.40
CHEMBL512172 IC50 = 6.0 nM 8.22
CHEMBL2017551 IC50 = 8.0 nM 8.10
CHEMBL4103500 IC50 = 20.0 nM 7.70
CHEMBL2347996 IC50 = 26.0 nM 7.58
CHEMBL4077712 IC50 = 41.0 nM 7.39
CHEMBL4104392 IC50 = 47.0 nM 7.33
CHEMBL3125861 IC50 = 100.0 nM 7.00
CHEMBL1458891 IC50 = 120.0 nM 6.92
CHEMBL4104855 IC50 = 1900.0 nM 5.72
CHEMBL4079394 IC50 = 3200.0 nM 5.50
CHEMBL4103655 IC50 = 3300.0 nM 5.48
CHEMBL4067688 IC50 = 3400.0 nM 5.47
CHEMBL4077136 IC50 = 4000.0 nM 5.40
CHEMBL4089803 IC50 = 7100.0 nM 5.15
CHEMBL4090023 IC50 = 9900.0 nM 5.00
CHEMBL4062804 IC50 = 17000.0 nM 4.77
CHEMBL4100895 IC50 = 20000.0 nM 4.70
CHEMBL4075601 IC50 = 24000.0 nM 4.62
CHEMBL4082917 IC50 = 27000.0 nM 4.57
CHEMBL4104278 IC50 = 28400.0 nM 4.55
CHEMBL4070445 IC50 = 28000.0 nM 4.55
CHEMBL4099920 IC50 = 30000.0 nM 4.52
CHEMBL3192431 IC50 = 30900.0 nM 4.51