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Assay Detail

CHEMBL1777184

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

Functional
Antagonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.
Banala AK, Levy BA, Khatri SS, Furman CA, Roof RA, Mishra Y, Griffin SA, Sibley DR, Luedtke RR, Newman AH.
J Med Chem (2011) 54 : 3581 -3594
PubMed 21495689 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.72 7.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26 SULPIRIDE 3.0 1 7.99
CHEMBL1774538 1 6.38
CHEMBL1774533 1 5.80
CHEMBL1774384 1 -
CHEMBL1774385 1 -
CHEMBL1774386 1 -
CHEMBL1774532 1 -
CHEMBL1774534 1 -
CHEMBL1774535 1 -
CHEMBL1774536 1 -
CHEMBL1774383 1 -
CHEMBL1774539 1 -
CHEMBL1774540 1 -
CHEMBL1774541 1 -
CHEMBL1774542 1 -
CHEMBL1773087 1 -
CHEMBL1774537 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26 SULPIRIDE IC50 = 10.28 nM 7.99
CHEMBL1774538 IC50 = 421.0 nM 6.38
CHEMBL1774533 IC50 = 1600.0 nM 5.80
CHEMBL1774384 IC50 - -
CHEMBL1774385 IC50 - -
CHEMBL1774386 IC50 - -
CHEMBL1774532 IC50 - -
CHEMBL1774534 IC50 - -
CHEMBL1774535 IC50 - -
CHEMBL1774536 IC50 - -
CHEMBL1774383 IC50 - -
CHEMBL1774539 IC50 - -
CHEMBL1774540 IC50 - -
CHEMBL1774541 IC50 - -
CHEMBL1774542 IC50 - -
CHEMBL1773087 IC50 - -
CHEMBL1774537 IC50 - -