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Assay Detail

CHEMBL4410741

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

Functional
Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced mast cell degranulation preincubated with compound for 30 mins and then treated with C48/80 for 1 hr by neutral red dye based method
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type RBL-2H3
Confidence 1 — Organism
Curated By Autocuration

Target

RBL-2H3 (CHEMBL614632)
Type CELL-LINE
Organism Rattus norvegicus

Publication

Design, synthesis and biological activity of a novel ethylenediamine derivatives as H1 receptor antagonists.
Zhou S, Huang G, Chen G.
Bioorg Med Chem (2019) 27 : 115127 -115127
PubMed 31703894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.89 7.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4462043 1 7.97
CHEMBL4576383 1 7.74
CHEMBL4438743 1 7.54
CHEMBL505 CHLORPHENIRAMINE 4.0 1 7.50
CHEMBL4444270 1 7.34
CHEMBL296419 ASTEMIZOLE 4.0 1 7.27
CHEMBL4546089 1 7.26
CHEMBL511 PYRILAMINE 4.0 1 7.09
CHEMBL4545003 1 7.08
CHEMBL4437364 1 7.05
CHEMBL4529352 1 6.89
CHEMBL320650 1 6.84
CHEMBL4465483 1 6.82
CHEMBL4543689 1 6.51
CHEMBL4472820 1 5.92
CHEMBL4442571 1 5.87
CHEMBL4446125 1 5.65
CHEMBL4474062 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4462043 IC50 = 10.6 nM 7.97
CHEMBL4576383 IC50 = 18.1 nM 7.74
CHEMBL4438743 IC50 = 28.9 nM 7.54
CHEMBL505 CHLORPHENIRAMINE IC50 = 31.8 nM 7.50
CHEMBL4444270 IC50 = 45.3 nM 7.34
CHEMBL296419 ASTEMIZOLE IC50 = 53.3 nM 7.27
CHEMBL4546089 IC50 = 55.3 nM 7.26
CHEMBL511 PYRILAMINE IC50 = 81.5 nM 7.09
CHEMBL4545003 IC50 = 83.9 nM 7.08
CHEMBL4437364 IC50 = 89.2 nM 7.05
CHEMBL4529352 IC50 = 129.0 nM 6.89
CHEMBL320650 IC50 = 143.0 nM 6.84
CHEMBL4465483 IC50 = 153.0 nM 6.82
CHEMBL4543689 IC50 = 306.0 nM 6.51
CHEMBL4472820 IC50 = 1206.0 nM 5.92
CHEMBL4442571 IC50 = 1338.0 nM 5.87
CHEMBL4446125 IC50 = 2228.0 nM 5.65
CHEMBL4474062 IC50 = 2310.0 nM 5.64