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Assay Detail

CHEMBL975013

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

Binding
Displacement of [3H]spiperone from rat dopamine D2 receptor in brain striatal membrane
12
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and neuropharmacological evaluation of 2-aryl- and alkylapomorphines.
Sipos A, Kiss B, Schmidt E, Greiner I, Berényi S.
Bioorg Med Chem (2008) 16 : 3773 -3779
PubMed 18289859 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.99 8.07
Ki 6 7.29 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL458579 2 8.38
CHEMBL458397 2 7.93
CHEMBL507567 2 7.68
CHEMBL3187985 APOMORPHINE HYDROCHLORIDE 4.0 2 7.32
CHEMBL3216443 2 6.62
CHEMBL465696 2 5.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL458579 Ki = 4.14 nM 8.38
CHEMBL458579 IC50 = 8.5 nM 8.07
CHEMBL458397 Ki = 11.7 nM 7.93
CHEMBL507567 Ki = 20.7 nM 7.68
CHEMBL458397 IC50 = 23.3 nM 7.63
CHEMBL507567 IC50 = 43.0 nM 7.37
CHEMBL3187985 APOMORPHINE HYDROCHLORIDE Ki = 47.7 nM 7.32
CHEMBL3187985 APOMORPHINE HYDROCHLORIDE IC50 = 87.0 nM 7.06
CHEMBL3216443 Ki = 242.0 nM 6.62
CHEMBL3216443 IC50 = 484.0 nM 6.32
CHEMBL465696 Ki = 1627.0 nM 5.79
CHEMBL465696 IC50 = 3259.0 nM 5.49