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Assay Detail

CHEMBL649628

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

Binding
Half-maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor in rat frontal cortex homogenate
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
Campiani G, Butini S, Gemma S, Nacci V, Fattorusso C, Catalanotti B, Giorgi G, Cagnotto A, Goegan M, Mennini T, Minetti P, Di Cesare MA, Mastroianni D, Scafetta N, Galletti B, Stasi MA, Castorina M, Pacifici L, Ghirardi O, Tinti O, Carminati P.
J Med Chem (2002) 45 : 344 -359
PubMed 11784139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.17 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 6.89
CHEMBL368324 1 6.68
CHEMBL54 HALOPERIDOL 4.0 1 5.57
CHEMBL715 OLANZAPINE 4.0 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE Ki = 128.0 nM 6.89
CHEMBL368324 Ki = 209.0 nM 6.68
CHEMBL54 HALOPERIDOL Ki = 2700.0 nM 5.57
CHEMBL715 OLANZAPINE Ki = 2870.0 nM 5.54