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Assay Detail

CHEMBL859320

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

Binding
Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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)-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H(1)-receptor agonists.
Menghin S, Pertz HH, Kramer K, Seifert R, Schunack W, Elz S.
J Med Chem (2003) 46 : 5458 -5470
PubMed 14640554 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.29 8.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL264491 1 8.01
CHEMBL347796 1 7.85
CHEMBL275035 1 7.40
CHEMBL153067 1 7.09
CHEMBL356449 1 7.08
CHEMBL275507 1 6.80
CHEMBL90 HISTAMINE 4.0 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL264491 EC50 = 9.772 nM 8.01
CHEMBL347796 EC50 = 14.13 nM 7.85
CHEMBL275035 EC50 = 39.81 nM 7.40
CHEMBL153067 EC50 = 81.28 nM 7.09
CHEMBL356449 EC50 = 83.18 nM 7.08
CHEMBL275507 EC50 = 158.49 nM 6.80
CHEMBL90 HISTAMINE EC50 = 162.18 nM 6.79