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Assay Detail

CHEMBL3405830

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

Binding
Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Loratadine analogues as MAGL inhibitors.
Patel JZ, Ahenkorah S, Vaara M, Staszewski M, Adams Y, Laitinen T, Navia-Paldanius D, Parkkari T, Savinainen JR, Walczyński K, Laitinen JT, Nevalainen TJ.
Bioorg Med Chem Lett (2015) 25 : 1436 -1442
PubMed 25752982 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 7.32 8.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL511 PYRILAMINE 4.0 1 8.84
CHEMBL998 LORATADINE 4.0 1 7.14
CHEMBL3401455 1 6.81
CHEMBL3402827 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL511 PYRILAMINE Kd = 1.445 nM 8.84
CHEMBL998 LORATADINE Kd = 72.44 nM 7.14
CHEMBL3401455 Kd = 154.88 nM 6.81
CHEMBL3402827 Kd = 316.23 nM 6.50