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Assay Detail

CHEMBL895651

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

Functional
Antagonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
Grundt P, Prevatt KM, Cao J, Taylor M, Floresca CZ, Choi JK, Jenkins BG, Luedtke RR, Newman AH.
J Med Chem (2007) 50 : 4135 -4146
PubMed 17672446 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.72 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL244774 1 7.64
CHEMBL244562 1 7.39
CHEMBL180010 1 7.09
CHEMBL390253 1 7.05
CHEMBL241973 1 6.97
CHEMBL394541 1 6.76
CHEMBL244989 1 6.75
CHEMBL110365 1 6.65
CHEMBL244773 1 6.43
CHEMBL231156 1 6.17
CHEMBL300780 1 5.89
CHEMBL398175 1 5.89
CHEMBL304605 1 -
CHEMBL396024 1 -
CHEMBL242644 1 -
CHEMBL242434 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL244774 IC50 = 22.9 nM 7.64
CHEMBL244562 IC50 = 41.0 nM 7.39
CHEMBL180010 IC50 = 80.9 nM 7.09
CHEMBL390253 IC50 = 88.3 nM 7.05
CHEMBL241973 IC50 = 107.0 nM 6.97
CHEMBL394541 IC50 = 175.0 nM 6.76
CHEMBL244989 IC50 = 179.0 nM 6.75
CHEMBL110365 IC50 = 224.0 nM 6.65
CHEMBL244773 IC50 = 368.0 nM 6.43
CHEMBL231156 IC50 = 672.0 nM 6.17
CHEMBL300780 IC50 = 1280.0 nM 5.89
CHEMBL398175 IC50 = 1300.0 nM 5.89
CHEMBL304605 IC50 - -
CHEMBL396024 IC50 - -
CHEMBL242644 IC50 - -
CHEMBL242434 IC50 - -