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Assay Detail

CHEMBL3705548

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

5-hydroxytryptamine receptor 2A (CHEMBL224)
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 8.17 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL708 ZIPRASIDONE 4.0 1 9.55
CHEMBL85 RISPERIDONE 4.0 1 9.30
CHEMBL715 OLANZAPINE 4.0 1 8.60
CHEMBL1112 ARIPIPRAZOLE 4.0 1 8.05
CHEMBL42 CLOZAPINE 4.0 1 8.02
CHEMBL54 HALOPERIDOL 4.0 1 7.00
CHEMBL716 QUETIAPINE 4.0 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL708 ZIPRASIDONE Ki = 0.28 nM 9.55
CHEMBL85 RISPERIDONE Ki = 0.5 nM 9.30
CHEMBL715 OLANZAPINE Ki = 2.5 nM 8.60
CHEMBL1112 ARIPIPRAZOLE Ki = 9.0 nM 8.05
CHEMBL42 CLOZAPINE Ki = 9.6 nM 8.02
CHEMBL54 HALOPERIDOL Ki = 100.0 nM 7.00
CHEMBL716 QUETIAPINE Ki = 202.0 nM 6.70