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Assay Detail

CHEMBL769865

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

Functional
Effect on IgE/Fcepsilon RI triggered rat basophil cell (RBL-2H3) degranulation assessed by measuring the amount of 5-HT release
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Low affinity immunoglobulin epsilon Fc receptor (CHEMBL2940)
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
EC50 17 5.78 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL318079 1 7.00
CHEMBL104519 1 6.96
CHEMBL104279 1 6.50
CHEMBL104333 1 5.85
CHEMBL104691 1 5.71
CHEMBL104813 1 5.46
CHEMBL322152 1 5.25
CHEMBL321976 1 5.20
CHEMBL104651 1 5.16
CHEMBL105438 1 4.68
CHEMBL431645 1 -
CHEMBL316756 1 -
CHEMBL108258 1 -
CHEMBL107061 1 -
CHEMBL106226 1 -
CHEMBL322153 1 -
CHEMBL105427 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL318079 EC50 = 100.0 nM 7.00
CHEMBL104519 EC50 = 110.0 nM 6.96
CHEMBL104279 EC50 = 313.0 nM 6.50
CHEMBL104333 EC50 = 1400.0 nM 5.85
CHEMBL104691 EC50 = 1940.0 nM 5.71
CHEMBL104813 EC50 = 3500.0 nM 5.46
CHEMBL322152 EC50 = 5600.0 nM 5.25
CHEMBL321976 EC50 = 6300.0 nM 5.20
CHEMBL104651 EC50 = 6960.0 nM 5.16
CHEMBL105438 EC50 = 20700.0 nM 4.68
CHEMBL431645 EC50 > 10000.0 nM -
CHEMBL316756 EC50 > 30000.0 nM -
CHEMBL108258 EC50 > 10000.0 nM -
CHEMBL107061 EC50 > 10000.0 nM -
CHEMBL106226 EC50 > 10000.0 nM -
CHEMBL322153 EC50 > 10000.0 nM -
CHEMBL105427 EC50 > 10000.0 nM -