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Assay Detail

CHEMBL645692

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

Binding
Binding affinity towards alpha-1 adrenergic receptors in rat brain synaptosomal preparations
9
Total Activities
9
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-1 (CHEMBL1907610)
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 9 8.34 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275045 1 9.15
CHEMBL54 HALOPERIDOL 4.0 1 9.00
CHEMBL10085 MAZAPERTINE 2.0 1 8.89
CHEMBL42 CLOZAPINE 4.0 1 8.85
CHEMBL10417 1 8.52
CHEMBL416703 1 8.40
CHEMBL428175 RWJ-25730 1 8.09
CHEMBL10105 1 7.50
CHEMBL10327 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275045 Ki = 0.7 nM 9.15
CHEMBL54 HALOPERIDOL Ki = 1.0 nM 9.00
CHEMBL10085 MAZAPERTINE Ki = 1.3 nM 8.89
CHEMBL42 CLOZAPINE Ki = 1.4 nM 8.85
CHEMBL10417 Ki = 3.0 nM 8.52
CHEMBL416703 Ki = 4.0 nM 8.40
CHEMBL428175 RWJ-25730 Ki = 8.2 nM 8.09
CHEMBL10105 Ki = 32.0 nM 7.50
CHEMBL10327 Ki = 220.0 nM 6.66