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Assay Detail

CHEMBL823938

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

Functional
In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Histamine H1 receptor (CHEMBL3943)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis and antihistaminic activity of some thiazolidin-4-ones.
Diurno MV, Mazzoni O, Piscopo E, Calignano A, Giordano F, Bolognese A.
J Med Chem (1992) 35 : 2910 -2912
PubMed 1353796 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.10 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1202934 1 6.00
CHEMBL1202938 1 5.92
CHEMBL319829 1 5.66
CHEMBL1202937 1 5.64
CHEMBL1202933 1 5.51
CHEMBL1202942 1 5.30
CHEMBL1202936 1 4.70
CHEMBL100486 1 4.68
CHEMBL1202939 1 4.62
CHEMBL1202941 1 4.60
CHEMBL1202935 1 4.40
CHEMBL1202932 1 4.22
CHEMBL1202929 1 -
CHEMBL1202943 1 -
CHEMBL1202940 1 -
CHEMBL1202944 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1202934 IC50 = 1000.0 nM 6.00
CHEMBL1202938 IC50 = 1200.0 nM 5.92
CHEMBL319829 IC50 = 2200.0 nM 5.66
CHEMBL1202937 IC50 = 2300.0 nM 5.64
CHEMBL1202933 IC50 = 3100.0 nM 5.51
CHEMBL1202942 IC50 = 5000.0 nM 5.30
CHEMBL1202936 IC50 = 20000.0 nM 4.70
CHEMBL100486 IC50 = 21000.0 nM 4.68
CHEMBL1202939 IC50 = 24000.0 nM 4.62
CHEMBL1202941 IC50 = 25000.0 nM 4.60
CHEMBL1202935 IC50 = 40000.0 nM 4.40
CHEMBL1202932 IC50 = 60000.0 nM 4.22
CHEMBL1202929 IC50 > 100000.0 nM -
CHEMBL1202943 IC50 > 100000.0 nM -
CHEMBL1202940 IC50 > 100000.0 nM -
CHEMBL1202944 IC50 > 100000.0 nM -