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Assay Detail

CHEMBL895631

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

Binding
Displacement of [3H]RX 821002 from adrenergic alpha-2 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-2 (CHEMBL2093864)
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 7 6.83 8.10
Activity 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 8.10
CHEMBL42 CLOZAPINE 4.0 1 7.10
CHEMBL243712 AMISULPRIDE 4.0 1 6.90
CHEMBL131495 1 6.60
CHEMBL715 OLANZAPINE 4.0 1 6.50
CHEMBL708 ZIPRASIDONE 4.0 1 6.30
CHEMBL71 CHLORPROMAZINE 4.0 1 6.30
CHEMBL221692 ADOPRAZINE 2.0 1 -
CHEMBL1112 ARIPIPRAZOLE 4.0 1 -
CHEMBL716 QUETIAPINE 4.0 1 -
CHEMBL54 HALOPERIDOL 4.0 1 -
CHEMBL196514 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 7.943 nM 8.10
CHEMBL42 CLOZAPINE Ki = 79.43 nM 7.10
CHEMBL243712 AMISULPRIDE Ki = 125.89 nM 6.90
CHEMBL131495 Ki = 251.19 nM 6.60
CHEMBL715 OLANZAPINE Ki = 316.23 nM 6.50
CHEMBL708 ZIPRASIDONE Ki = 501.19 nM 6.30
CHEMBL71 CHLORPROMAZINE Ki = 501.19 nM 6.30
CHEMBL221692 ADOPRAZINE Activity - -
CHEMBL1112 ARIPIPRAZOLE Activity - -
CHEMBL716 QUETIAPINE Activity - -
CHEMBL54 HALOPERIDOL Activity - -
CHEMBL196514 Activity - -