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Assay Detail

CHEMBL1781414

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

Binding
Displacement of [3H]N-methylspiperone from human D2 receptor expressed in HEK cells
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (σ) receptor ligands modulates off-target activity and subtype selectivity.
Banister SD, Moussa IA, Jorgensen WT, Chua SW, Kassiou M.
Bioorg Med Chem Lett (2011) 21 : 3622 -3626
PubMed 21555222 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.77 9.00
IC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.00
CHEMBL1779058 1 5.76
CHEMBL64260 1 5.54
CHEMBL1779059 1 -
CHEMBL1779060 1 -
CHEMBL521582 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 1.0 nM 9.00
CHEMBL1779058 Ki = 1724.0 nM 5.76
CHEMBL64260 Ki = 2850.0 nM 5.54
CHEMBL1779059 Ki > 10000.0 nM -
CHEMBL1779060 Ki > 10000.0 nM -
CHEMBL521582 IC50 > 10000.0 nM -