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Assay Detail

CHEMBL895620

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

Binding
Displacement of [3H]8-OH-DPAT from human 5HT1A 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 1A (CHEMBL214)
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 7.95 9.10
Activity 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL221692 ADOPRAZINE 2.0 1 9.10
CHEMBL708 ZIPRASIDONE 4.0 1 8.80
CHEMBL131495 1 8.60
CHEMBL196514 1 8.30
CHEMBL1112 ARIPIPRAZOLE 4.0 1 8.10
CHEMBL716 QUETIAPINE 4.0 1 7.10
CHEMBL42 CLOZAPINE 4.0 1 7.00
CHEMBL85 RISPERIDONE 4.0 1 6.60
CHEMBL71 CHLORPROMAZINE 4.0 1 -
CHEMBL243712 AMISULPRIDE 4.0 1 -
CHEMBL715 OLANZAPINE 4.0 1 -
CHEMBL54 HALOPERIDOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL221692 ADOPRAZINE Ki = 0.7943 nM 9.10
CHEMBL708 ZIPRASIDONE Ki = 1.585 nM 8.80
CHEMBL131495 Ki = 2.512 nM 8.60
CHEMBL196514 Ki = 5.012 nM 8.30
CHEMBL1112 ARIPIPRAZOLE Ki = 7.943 nM 8.10
CHEMBL716 QUETIAPINE Ki = 79.43 nM 7.10
CHEMBL42 CLOZAPINE Ki = 100.0 nM 7.00
CHEMBL85 RISPERIDONE Ki = 251.19 nM 6.60
CHEMBL71 CHLORPROMAZINE Activity - -
CHEMBL243712 AMISULPRIDE Activity - -
CHEMBL715 OLANZAPINE Activity - -
CHEMBL54 HALOPERIDOL Activity - -