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Assay Detail

CHEMBL673248

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

Binding
Tested for binding affinity towards human D2L receptor using [3H]spiperone as radioligand
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery and structure-activity relationships of 1,2,3,6-tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine autoreceptor agonists and potential antipsychotic agents.
Wright JL, Caprathe BW, Downing DM, Glase SA, Heffner TG, Jaen JC, Johnson SJ, Kesten SR, MacKenzie RG, Meltzer LT.
J Med Chem (1994) 37 : 3523 -3533
PubMed 7932581 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.15 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.30
CHEMBL335545 CI-1007 1 7.59
CHEMBL53 APOMORPHINE 4.0 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 0.5 nM 9.30
CHEMBL335545 CI-1007 Ki = 25.5 nM 7.59
CHEMBL53 APOMORPHINE Ki = 28.0 nM 7.55