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Assay Detail

CHEMBL895653

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

Functional
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay
10
Total Activities
5
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(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
EC50 5 7.05 7.80
Activity 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL244990 2 7.80
CHEMBL69451 2 7.04
CHEMBL241973 2 6.94
CHEMBL231156 2 6.82
CHEMBL244774 2 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL244990 EC50 = 15.8 nM 7.80
CHEMBL69451 EC50 = 92.0 nM 7.04
CHEMBL241973 EC50 = 114.0 nM 6.94
CHEMBL231156 EC50 = 150.0 nM 6.82
CHEMBL244774 EC50 = 231.0 nM 6.64
CHEMBL69451 Activity = 20.0 % -
CHEMBL241973 Activity = 17.0 % -
CHEMBL231156 Activity = 17.0 % -
CHEMBL244990 Activity = 26.0 % -
CHEMBL244774 Activity = 31.0 % -