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Assay Detail

CHEMBL4433282

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

Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions incubated for 15 mins
5
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H<sub>3</sub> receptor ligands.
Łażewska D, Kaleta M, Schwed JS, Karcz T, Mogilski S, Latacz G, Olejarz A, Siwek A, Kubacka M, Lubelska A, Honkisz E, Handzlik J, Filipek B, Stark H, Kieć-Kononowicz K.
Bioorg Med Chem (2017) 25 : 5341 -5354
PubMed 28797771 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 6.60 7.14
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1305 ANTAZOLINE 4.0 1 7.14
CHEMBL4540849 2 6.53
CHEMBL4586133 2 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1305 ANTAZOLINE Kd = 72.44 nM 7.14
CHEMBL4540849 Kd = 295.12 nM 6.53
CHEMBL4586133 Kd = 724.44 nM 6.14
CHEMBL4540849 Activity - -
CHEMBL4586133 Activity - -