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Assay Detail

CHEMBL676060

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

Binding
In vitro inhibition of [3H]spiperone binding to Dopamine D2 receptor in rat striatum.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

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
IC50 17 6.36 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL335545 CI-1007 1 7.28
CHEMBL118219 1 7.12
CHEMBL119273 1 7.00
CHEMBL117527 1 6.95
CHEMBL2111778 1 6.95
CHEMBL116205 1 6.85
CHEMBL451189 1 6.77
CHEMBL324085 1 6.48
CHEMBL119191 1 6.45
CHEMBL119339 1 6.38
CHEMBL327070 1 6.37
CHEMBL116261 1 6.20
CHEMBL333053 1 6.00
CHEMBL119575 1 5.59
CHEMBL120197 1 5.41
CHEMBL118721 1 5.33
CHEMBL118461 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL335545 CI-1007 IC50 = 53.0 nM 7.28
CHEMBL118219 IC50 = 76.0 nM 7.12
CHEMBL119273 IC50 = 100.0 nM 7.00
CHEMBL117527 IC50 = 112.0 nM 6.95
CHEMBL2111778 IC50 = 113.0 nM 6.95
CHEMBL116205 IC50 = 141.0 nM 6.85
CHEMBL451189 IC50 = 170.0 nM 6.77
CHEMBL324085 IC50 = 328.0 nM 6.48
CHEMBL119191 IC50 = 354.0 nM 6.45
CHEMBL119339 IC50 = 420.0 nM 6.38
CHEMBL327070 IC50 = 424.0 nM 6.37
CHEMBL116261 IC50 = 635.0 nM 6.20
CHEMBL333053 IC50 = 1000.0 nM 6.00
CHEMBL119575 IC50 = 2554.0 nM 5.59
CHEMBL120197 IC50 = 3936.0 nM 5.41
CHEMBL118721 IC50 = 4634.0 nM 5.33
CHEMBL118461 IC50 = 9207.0 nM 5.04