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Assay Detail

CHEMBL895630

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

Binding
Displacement of [3H]prazosin from adrenergic alpha1 receptor in rat cerebral cortex
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

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 11 7.87 8.80
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 8.80
CHEMBL71 CHLORPROMAZINE 4.0 1 8.80
CHEMBL131495 1 8.50
CHEMBL708 ZIPRASIDONE 4.0 1 8.10
CHEMBL42 CLOZAPINE 4.0 1 8.00
CHEMBL716 QUETIAPINE 4.0 1 7.90
CHEMBL54 HALOPERIDOL 4.0 1 7.80
CHEMBL196514 1 7.80
CHEMBL715 OLANZAPINE 4.0 1 7.60
CHEMBL1112 ARIPIPRAZOLE 4.0 1 7.00
CHEMBL221692 ADOPRAZINE 2.0 1 6.30
CHEMBL243712 AMISULPRIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 1.585 nM 8.80
CHEMBL71 CHLORPROMAZINE Ki = 1.585 nM 8.80
CHEMBL131495 Ki = 3.162 nM 8.50
CHEMBL708 ZIPRASIDONE Ki = 7.943 nM 8.10
CHEMBL42 CLOZAPINE Ki = 10.0 nM 8.00
CHEMBL716 QUETIAPINE Ki = 12.59 nM 7.90
CHEMBL54 HALOPERIDOL Ki = 15.85 nM 7.80
CHEMBL196514 Ki = 15.85 nM 7.80
CHEMBL715 OLANZAPINE Ki = 25.12 nM 7.60
CHEMBL1112 ARIPIPRAZOLE Ki = 100.0 nM 7.00
CHEMBL221692 ADOPRAZINE Ki = 501.19 nM 6.30
CHEMBL243712 AMISULPRIDE Activity - -