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Assay Detail

CHEMBL940856

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

Binding
Displacement of [3H]mepyramine from H1R in rat brain
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H1 receptor (CHEMBL4701)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase.
Kim SF, Huang AS, Snowman AM, Teuscher C, Snyder SH.
Proc Natl Acad Sci U S A (2007) 104 : 3456 -3459
PubMed 17360666 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.45 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 8.05
CHEMBL715 OLANZAPINE 4.0 1 7.89
CHEMBL716 QUETIAPINE 4.0 1 7.40
CHEMBL85 RISPERIDONE 4.0 1 7.10
CHEMBL708 ZIPRASIDONE 4.0 1 6.82
CHEMBL1112 ARIPIPRAZOLE 4.0 1 -
CHEMBL54 HALOPERIDOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE IC50 = 9.0 nM 8.05
CHEMBL715 OLANZAPINE IC50 = 13.0 nM 7.89
CHEMBL716 QUETIAPINE IC50 = 40.0 nM 7.40
CHEMBL85 RISPERIDONE IC50 = 80.0 nM 7.10
CHEMBL708 ZIPRASIDONE IC50 = 150.0 nM 6.82
CHEMBL1112 ARIPIPRAZOLE IC50 > 3000.0 nM -
CHEMBL54 HALOPERIDOL IC50 > 2000.0 nM -