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Assay Detail

CHEMBL895616

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

Binding
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells
12
Total Activities
12
Compounds Tested
1
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 2A (CHEMBL224)
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 12 7.75 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL708 ZIPRASIDONE 4.0 1 9.20
CHEMBL85 RISPERIDONE 4.0 1 9.00
CHEMBL715 OLANZAPINE 4.0 1 8.80
CHEMBL42 CLOZAPINE 4.0 1 8.30
CHEMBL71 CHLORPROMAZINE 4.0 1 8.20
CHEMBL1112 ARIPIPRAZOLE 4.0 1 7.80
CHEMBL196514 1 7.70
CHEMBL716 QUETIAPINE 4.0 1 7.20
CHEMBL131495 1 7.00
CHEMBL54 HALOPERIDOL 4.0 1 7.00
CHEMBL221692 ADOPRAZINE 2.0 1 6.60
CHEMBL243712 AMISULPRIDE 4.0 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL708 ZIPRASIDONE Ki = 0.631 nM 9.20
CHEMBL85 RISPERIDONE Ki = 1.0 nM 9.00
CHEMBL715 OLANZAPINE Ki = 1.585 nM 8.80
CHEMBL42 CLOZAPINE Ki = 5.012 nM 8.30
CHEMBL71 CHLORPROMAZINE Ki = 6.31 nM 8.20
CHEMBL1112 ARIPIPRAZOLE Ki = 15.85 nM 7.80
CHEMBL196514 Ki = 19.95 nM 7.70
CHEMBL716 QUETIAPINE Ki = 63.1 nM 7.20
CHEMBL131495 Ki = 100.0 nM 7.00
CHEMBL54 HALOPERIDOL Ki = 100.0 nM 7.00
CHEMBL221692 ADOPRAZINE Ki = 251.19 nM 6.60
CHEMBL243712 AMISULPRIDE Ki = 630.96 nM 6.20