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Assay Detail

CHEMBL823939

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
Kd 16 6.76 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL511 PYRILAMINE 4.0 1 9.00
CHEMBL1202934 1 8.70
CHEMBL1202938 1 8.30
CHEMBL1202942 1 7.70
CHEMBL1202936 1 7.40
CHEMBL1202937 1 7.40
CHEMBL1202939 1 7.10
CHEMBL1202932 1 6.40
CHEMBL1202933 1 6.40
CHEMBL1202941 1 6.40
CHEMBL319829 1 6.20
CHEMBL1202935 1 6.00
CHEMBL100486 1 5.60
CHEMBL1202940 1 5.40
CHEMBL1202943 1 5.20
CHEMBL1202929 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL511 PYRILAMINE Kd = 1.0 nM 9.00
CHEMBL1202934 Kd = 1.995 nM 8.70
CHEMBL1202938 Kd = 5.012 nM 8.30
CHEMBL1202942 Kd = 19.95 nM 7.70
CHEMBL1202936 Kd = 39.81 nM 7.40
CHEMBL1202937 Kd = 39.81 nM 7.40
CHEMBL1202939 Kd = 79.43 nM 7.10
CHEMBL1202932 Kd = 398.11 nM 6.40
CHEMBL1202933 Kd = 398.11 nM 6.40
CHEMBL1202941 Kd = 398.11 nM 6.40
CHEMBL319829 Kd = 630.96 nM 6.20
CHEMBL1202935 Kd = 1000.0 nM 6.00
CHEMBL100486 Kd = 2511.89 nM 5.60
CHEMBL1202940 Kd = 3981.07 nM 5.40
CHEMBL1202943 Kd = 6309.57 nM 5.20
CHEMBL1202929 Kd = 10000.0 nM 5.00