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Assay Detail

CHEMBL692703

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

Binding
Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
Liao Y, Venhuis BJ, Rodenhuis N, Timmerman W, Wikström H, Meier E, Bartoszyk GD, Böttcher H, Seyfried CA, Sundell S.
J Med Chem (1999) 42 : 2235 -2244
PubMed 10377229 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.81 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 7.64
CHEMBL72292 1 7.33
CHEMBL430798 1 6.92
CHEMBL310712 1 6.14
CHEMBL831 LOXAPINE 4.0 1 6.00
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
CHEMBL430798 IC50 = 120.0 nM 6.92
CHEMBL310712 IC50 = 720.0 nM 6.14
CHEMBL831 LOXAPINE IC50 = 1000.0 nM 6.00
CHEMBL54 HALOPERIDOL IC50 > 1000.0 nM -