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Assay Detail

CHEMBL643678

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

Binding
Binding affinity towards alpha-2 adrenergic receptors in rat brain synaptosomal preparations
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
Reitz AB, Bennett DJ, Blum PS, Codd EE, Maryanoff CA, Ortegon ME, Renzi MJ, Scott MK, Shank RP, Vaught JL.
J Med Chem (1994) 37 : 1060 -1062
PubMed 7909336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.20 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10327 1 7.80
CHEMBL10085 MAZAPERTINE 2.0 1 7.77
CHEMBL42 CLOZAPINE 4.0 1 7.24
CHEMBL275045 1 6.00
CHEMBL54 HALOPERIDOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10327 Ki = 16.0 nM 7.80
CHEMBL10085 MAZAPERTINE Ki = 17.0 nM 7.77
CHEMBL42 CLOZAPINE Ki = 58.0 nM 7.24
CHEMBL275045 Ki = 1000.0 nM 6.00
CHEMBL54 HALOPERIDOL Ki > 1000.0 nM -