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Assay Detail

CHEMBL895623

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

Binding
Displacement of [3H]mesulergine from 5HT2C receptor expressed in CHO cells
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
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
Ki 8 7.75 8.90
Activity 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL708 ZIPRASIDONE 4.0 1 8.90
CHEMBL715 OLANZAPINE 4.0 1 8.30
CHEMBL42 CLOZAPINE 4.0 1 8.10
CHEMBL85 RISPERIDONE 4.0 1 7.90
CHEMBL131495 1 7.40
CHEMBL71 CHLORPROMAZINE 4.0 1 7.40
CHEMBL1112 ARIPIPRAZOLE 4.0 1 7.30
CHEMBL196514 1 6.70
CHEMBL221692 ADOPRAZINE 2.0 1 -
CHEMBL243712 AMISULPRIDE 4.0 1 -
CHEMBL716 QUETIAPINE 4.0 1 -
CHEMBL54 HALOPERIDOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL708 ZIPRASIDONE Ki = 1.259 nM 8.90
CHEMBL715 OLANZAPINE Ki = 5.012 nM 8.30
CHEMBL42 CLOZAPINE Ki = 7.943 nM 8.10
CHEMBL85 RISPERIDONE Ki = 12.59 nM 7.90
CHEMBL131495 Ki = 39.81 nM 7.40
CHEMBL71 CHLORPROMAZINE Ki = 39.81 nM 7.40
CHEMBL1112 ARIPIPRAZOLE Ki = 50.12 nM 7.30
CHEMBL196514 Ki = 199.53 nM 6.70
CHEMBL221692 ADOPRAZINE Activity - -
CHEMBL243712 AMISULPRIDE Activity - -
CHEMBL716 QUETIAPINE Activity - -
CHEMBL54 HALOPERIDOL Activity - -