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Assay Detail

CHEMBL670113

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

Binding
In vitro binding affinity at human cloned Dopamine receptor D2 by [3H]spiroperidol displacement.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: a potent and selective dopamine D4 ligand.
Perrone R, Berardi F, Colabufo NA, Leopoldo M, Tortorella V.
J Med Chem (1998) 41 : 4903 -4909
PubMed 9822559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.79 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.39
CHEMBL26677 1 7.89
CHEMBL26929 1 7.70
CHEMBL424125 1 6.82
CHEMBL42 CLOZAPINE 4.0 1 6.64
CHEMBL144811 1 6.60
CHEMBL2373210 1 6.19
CHEMBL286725 1 6.16
CHEMBL359002 1 6.12
CHEMBL356358 1 6.09
CHEMBL2373205 1 6.06
CHEMBL2373206 1 -
CHEMBL147483 1 -
CHEMBL93403 1 -
CHEMBL357448 1 -
CHEMBL2373204 1 -
CHEMBL2373207 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL IC50 = 4.1 nM 8.39
CHEMBL26677 IC50 = 13.0 nM 7.89
CHEMBL26929 IC50 = 20.0 nM 7.70
CHEMBL424125 IC50 = 150.0 nM 6.82
CHEMBL42 CLOZAPINE IC50 = 230.0 nM 6.64
CHEMBL144811 IC50 = 250.0 nM 6.60
CHEMBL2373210 IC50 = 650.0 nM 6.19
CHEMBL286725 IC50 = 700.0 nM 6.16
CHEMBL359002 IC50 = 761.0 nM 6.12
CHEMBL356358 IC50 = 810.0 nM 6.09
CHEMBL2373205 IC50 = 870.0 nM 6.06
CHEMBL2373206 IC50 > 1000.0 nM -
CHEMBL147483 IC50 > 1000.0 nM -
CHEMBL93403 IC50 > 1000.0 nM -
CHEMBL357448 IC50 > 1000.0 nM -
CHEMBL2373204 IC50 > 1000.0 nM -
CHEMBL2373207 IC50 > 1000.0 nM -