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Assay Detail

CHEMBL3707498

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

Binding
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H1 receptor (CHEMBL231)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Methods and compositions for sleep disorders and other disorders
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.86 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 9.00
CHEMBL715 OLANZAPINE 4.0 1 8.70
CHEMBL716 QUETIAPINE 4.0 1 8.00
CHEMBL85 RISPERIDONE 4.0 1 7.85
CHEMBL708 ZIPRASIDONE 4.0 1 7.82
CHEMBL1112 ARIPIPRAZOLE 4.0 1 7.55
CHEMBL54 HALOPERIDOL 4.0 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE Ki = 1.0 nM 9.00
CHEMBL715 OLANZAPINE Ki = 2.0 nM 8.70
CHEMBL716 QUETIAPINE Ki = 10.0 nM 8.00
CHEMBL85 RISPERIDONE Ki = 14.0 nM 7.85
CHEMBL708 ZIPRASIDONE Ki = 15.0 nM 7.82
CHEMBL1112 ARIPIPRAZOLE Ki = 28.0 nM 7.55
CHEMBL54 HALOPERIDOL Ki = 780.0 nM 6.11