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Assay Detail

CHEMBL895627

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

Binding
Displacement of [3H]paraxetine from human 5HT transporter expressed in HEK293 cells
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium-dependent serotonin transporter (CHEMBL228)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
Lange JH, Reinders JH, Tolboom JT, Glennon JC, Coolen HK, Kruse CG.
J Med Chem (2007) 50 : 5103 -5108
PubMed 17880057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 7 - -
Ki 5 8.10 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196514 1 9.60
CHEMBL131495 1 9.10
CHEMBL1112 ARIPIPRAZOLE 4.0 1 7.50
CHEMBL71 CHLORPROMAZINE 4.0 1 7.20
CHEMBL708 ZIPRASIDONE 4.0 1 7.10
CHEMBL221692 ADOPRAZINE 2.0 1 -
CHEMBL243712 AMISULPRIDE 4.0 1 -
CHEMBL85 RISPERIDONE 4.0 1 -
CHEMBL716 QUETIAPINE 4.0 1 -
CHEMBL715 OLANZAPINE 4.0 1 -
CHEMBL42 CLOZAPINE 4.0 1 -
CHEMBL54 HALOPERIDOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196514 Ki = 0.2512 nM 9.60
CHEMBL131495 Ki = 0.7943 nM 9.10
CHEMBL1112 ARIPIPRAZOLE Ki = 31.62 nM 7.50
CHEMBL71 CHLORPROMAZINE Ki = 63.1 nM 7.20
CHEMBL708 ZIPRASIDONE Ki = 79.43 nM 7.10
CHEMBL221692 ADOPRAZINE Activity - -
CHEMBL243712 AMISULPRIDE Activity - -
CHEMBL85 RISPERIDONE Activity - -
CHEMBL716 QUETIAPINE Activity - -
CHEMBL715 OLANZAPINE Activity - -
CHEMBL42 CLOZAPINE Activity - -
CHEMBL54 HALOPERIDOL Activity - -