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Assay Detail

CHEMBL961827

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Functional
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as stimulation of mitogenesis
2
Total Activities
2
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 Autocuration

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl)heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists.
Newman AH, Grundt P, Cyriac G, Deschamps JR, Taylor M, Kumar R, Ho D, Luedtke RR.
J Med Chem (2009) 52 : 2559 -2570
PubMed 19331412 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.36 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1627316 1 7.64
CHEMBL1627318 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1627316 EC50 = 22.8 nM 7.64
CHEMBL1627318 EC50 = 84.0 nM 7.08