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Assay Detail

CHEMBL814834

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

Binding
Inhibitory activity against human Syk protein tyrosine kinase expressed in yeast Klyveromyces lactis
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Potent small molecule inhibitors of spleen tyrosine kinase (Syk).
Lai JY, Cox PJ, Patel R, Sadiq S, Aldous DJ, Thurairatnam S, Smith K, Wheeler D, Jagpal S, Parveen S, Fenton G, Harrison TK, McCarthy C, Bamborough P.
Bioorg Med Chem Lett (2003) 13 : 3111 -3114
PubMed 12941345 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.93 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL104333 1 8.30
CHEMBL105438 1 7.96
CHEMBL431645 1 7.92
CHEMBL104279 1 7.85
CHEMBL319613 1 7.85
CHEMBL104519 1 7.70
CHEMBL106095 1 7.57
CHEMBL106226 1 7.55
CHEMBL107061 1 7.50
CHEMBL105427 1 7.22
CHEMBL108258 1 7.01
CHEMBL322368 1 7.00
CHEMBL321955 1 6.89
CHEMBL322152 1 6.88
CHEMBL318079 1 6.84
CHEMBL105061 1 6.69
CHEMBL104813 1 6.56
CHEMBL321976 1 6.33
CHEMBL316756 1 6.21
CHEMBL104691 1 6.18
CHEMBL104651 1 6.17
CHEMBL1788130 1 6.07
CHEMBL105740 1 6.03
CHEMBL104583 1 6.00
CHEMBL105421 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL104333 IC50 = 5.0 nM 8.30
CHEMBL105438 IC50 = 11.0 nM 7.96
CHEMBL431645 IC50 = 12.0 nM 7.92
CHEMBL104279 IC50 = 14.0 nM 7.85
CHEMBL319613 IC50 = 14.0 nM 7.85
CHEMBL104519 IC50 = 20.0 nM 7.70
CHEMBL106095 IC50 = 27.0 nM 7.57
CHEMBL106226 IC50 = 28.0 nM 7.55
CHEMBL107061 IC50 = 32.0 nM 7.50
CHEMBL105427 IC50 = 60.0 nM 7.22
CHEMBL108258 IC50 = 98.0 nM 7.01
CHEMBL322368 IC50 = 100.0 nM 7.00
CHEMBL321955 IC50 = 128.0 nM 6.89
CHEMBL322152 IC50 = 133.0 nM 6.88
CHEMBL318079 IC50 = 145.0 nM 6.84
CHEMBL105061 IC50 = 204.0 nM 6.69
CHEMBL104813 IC50 = 273.0 nM 6.56
CHEMBL321976 IC50 = 465.0 nM 6.33
CHEMBL316756 IC50 = 616.0 nM 6.21
CHEMBL104691 IC50 = 658.0 nM 6.18
CHEMBL104651 IC50 = 678.0 nM 6.17
CHEMBL1788130 IC50 = 850.0 nM 6.07
CHEMBL105740 IC50 = 937.0 nM 6.03
CHEMBL104583 IC50 = 1000.0 nM 6.00
CHEMBL105421 IC50 = 8100.0 nM 5.09