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Assay Detail

CHEMBL695155

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Functional
Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N alpha-alkylated derivatives of 2-phenylhistamines: synthesis and in vitro activity of potent histamine H1-receptor agonists.
Kramer K, Elz S, Pertz HH, Schunack W.
Bioorg Med Chem Lett (1998) 8 : 2583 -2588
PubMed 9873585 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 9.02 9.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL90 HISTAMINE 4.0 1 9.11
CHEMBL24665 1 9.01
CHEMBL88075 1 9.01
CHEMBL313301 1 8.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL90 HISTAMINE Kd = 0.7762 nM 9.11
CHEMBL24665 Kd = 0.9772 nM 9.01
CHEMBL88075 Kd = 0.9772 nM 9.01
CHEMBL313301 Kd = 1.148 nM 8.94