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Assay Detail

CHEMBL697534

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

Binding
Ability to displace [3H]Nalpha-methylhistamine from histamine H3 receptors in homogenates of rat cerebral cortex
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Histamine H3 receptor (CHEMBL4124)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE.
De Esch IJ, Mills JE, Perkins TD, Romeo G, Hoffmann M, Wieland K, Leurs R, Menge WM, Nederkoorn PH, Dean PM, Timmerman H.
J Med Chem (2001) 44 : 1666 -1674
PubMed 11356102 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.82 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL43934 1 9.30
CHEMBL45028 1 8.50
CHEMBL46458 1 8.10
CHEMBL44842 1 7.90
CHEMBL47036 1 5.30
CHEMBL46488 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL43934 Ki = 0.5012 nM 9.30
CHEMBL45028 Ki = 3.162 nM 8.50
CHEMBL46458 Ki = 7.943 nM 8.10
CHEMBL44842 Ki = 12.59 nM 7.90
CHEMBL47036 Ki = 5011.87 nM 5.30
CHEMBL46488 Ki < 100000.0 nM -