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Assay Detail

CHEMBL692705

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

Binding
Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Brain membranes
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
Liao Y, DeBoer P, Meier E, Wikström H.
J Med Chem (1997) 40 : 4146 -4153
PubMed 9406603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.04 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 7.64
CHEMBL72292 1 7.33
CHEMBL310712 1 6.14
CHEMBL54 HALOPERIDOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE IC50 = 23.0 nM 7.64
CHEMBL72292 IC50 = 47.0 nM 7.33
CHEMBL310712 IC50 = 720.0 nM 6.14
CHEMBL54 HALOPERIDOL IC50 > 1000.0 nM -