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Assay Detail

CHEMBL828786

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

Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
13
Total Activities
13
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 13 7.59 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL184486 1 8.74
CHEMBL54 HALOPERIDOL 4.0 1 8.72
CHEMBL184853 1 7.85
CHEMBL362542 1 7.84
CHEMBL42 CLOZAPINE 4.0 1 7.52
CHEMBL182432 1 7.41
CHEMBL184772 1 7.05
CHEMBL185263 1 7.04
CHEMBL183466 1 6.95
CHEMBL363308 1 6.76
CHEMBL184263 1 -
CHEMBL183601 1 -
CHEMBL364865 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL184486 Ki = 1.8 nM 8.74
CHEMBL54 HALOPERIDOL Ki = 1.9 nM 8.72
CHEMBL184853 Ki = 14.0 nM 7.85
CHEMBL362542 Ki = 14.5 nM 7.84
CHEMBL42 CLOZAPINE Ki = 30.4 nM 7.52
CHEMBL182432 Ki = 39.1 nM 7.41
CHEMBL184772 Ki = 88.9 nM 7.05
CHEMBL185263 Ki = 90.7 nM 7.04
CHEMBL183466 Ki = 113.5 nM 6.95
CHEMBL363308 Ki = 174.5 nM 6.76
CHEMBL184263 Ki > 10000.0 nM -
CHEMBL183601 Ki > 10000.0 nM -
CHEMBL364865 Ki > 10000.0 nM -