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Assay Detail

CHEMBL673464

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

Binding
Displacement of [3H]spiperone from Dopamine receptor D2 of rat corpora striata synaptic membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1-(2-METHOXYPHENYL)-4-ALKYLPIPERAZINES: EFFECT OF THE N-4 SUBSTITUENT ON THE AFFINITY AND SELECTIVITY FOR DOPAMINE D4 RECEPTOR
Perrone R, Berardi F, Colabufo NA, Leopoldo M, Tortorella V
Bioorg Med Chem Lett (1997) 7 : 1327 -1330
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.55 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.77
CHEMBL26677 1 8.52
CHEMBL28209 1 8.30
CHEMBL26929 1 8.15
CHEMBL26758 1 7.50
CHEMBL283211 1 7.40
CHEMBL26135 1 7.25
CHEMBL42 CLOZAPINE 4.0 1 6.93
CHEMBL286725 1 6.85
CHEMBL26426 1 6.82
CHEMBL28063 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 1.7 nM 8.77
CHEMBL26677 Ki = 3.0 nM 8.52
CHEMBL28209 Ki = 5.0 nM 8.30
CHEMBL26929 Ki = 7.0 nM 8.15
CHEMBL26758 Ki = 32.0 nM 7.50
CHEMBL283211 Ki = 40.0 nM 7.40
CHEMBL26135 Ki = 56.0 nM 7.25
CHEMBL42 CLOZAPINE Ki = 117.0 nM 6.93
CHEMBL286725 Ki = 141.0 nM 6.85
CHEMBL26426 Ki = 150.0 nM 6.82
CHEMBL28063 Ki = 253.0 nM 6.60