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Assay Detail

CHEMBL647725

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

Binding
Inhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptor
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Alpha-2A adrenergic receptor (CHEMBL1867)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.
Belliotti TR, Wustrow DJ, Brink WA, Zoski KT, Shih YH, Whetzel SZ, Georgic LM, Corbin AE, Akunne HC, Heffner TG, Pugsley TA, Wise LD.
J Med Chem (1999) 42 : 5181 -5187
PubMed 10602703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.45 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL15245 YOHIMBINE 3.0 1 8.51
CHEMBL346389 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL15245 YOHIMBINE Ki = 3.1 nM 8.51
CHEMBL346389 Ki = 411.0 nM 6.39