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Assay Detail

CHEMBL828832

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Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand.
Matulenko MA, Surber B, Fan L, Kolasa T, Nakane M, Terranova MA, Uchic ME, Miller LN, Chang R, Donnelly-Roberts DL, Namovic MT, Moreland RB, Brioni JD, Stewart AO.
Bioorg Med Chem Lett (2004) 14 : 5095 -5098
PubMed 15380206 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.48 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.85
CHEMBL362542 1 8.57
CHEMBL42 CLOZAPINE 4.0 1 7.55
CHEMBL182432 1 7.34
CHEMBL184853 1 7.27
CHEMBL185263 1 7.21
CHEMBL184772 1 7.00
CHEMBL183466 1 6.03
CHEMBL364865 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 1.4 nM 8.85
CHEMBL362542 Ki = 2.7 nM 8.57
CHEMBL42 CLOZAPINE Ki = 28.4 nM 7.55
CHEMBL182432 Ki = 46.0 nM 7.34
CHEMBL184853 Ki = 54.2 nM 7.27
CHEMBL185263 Ki = 61.9 nM 7.21
CHEMBL184772 Ki = 101.0 nM 7.00
CHEMBL183466 Ki = 936.0 nM 6.03
CHEMBL364865 Ki > 10000.0 nM -