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Assay Detail

CHEMBL895654

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

Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
12
Total Activities
6
Compounds Tested
2
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(3) dopamine receptor (CHEMBL234)
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
Activity 6 - -
EC50 6 8.04 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL244990 2 9.00
CHEMBL390253 2 8.47
CHEMBL242434 2 8.41
CHEMBL69451 2 8.20
CHEMBL396024 2 7.38
CHEMBL304605 2 6.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL244990 EC50 = 1.0 nM 9.00
CHEMBL390253 EC50 = 3.4 nM 8.47
CHEMBL242434 EC50 = 3.9 nM 8.41
CHEMBL69451 EC50 = 6.3 nM 8.20
CHEMBL396024 EC50 = 42.0 nM 7.38
CHEMBL304605 EC50 = 173.0 nM 6.76
CHEMBL69451 Activity = 30.0 % -
CHEMBL304605 Activity = 44.0 % -
CHEMBL244990 Activity = 48.0 % -
CHEMBL396024 Activity = 26.0 % -
CHEMBL242434 Activity = 47.0 % -
CHEMBL390253 Activity = 20.0 % -