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Assay Detail

CHEMBL1777182

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

Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(4) dopamine receptor (CHEMBL219)
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
Ki 16 5.67 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL180010 1 6.43
CHEMBL1774534 1 5.83
CHEMBL1774384 1 5.51
CHEMBL1774536 1 5.50
CHEMBL1774535 1 5.47
CHEMBL1774386 1 5.27
CHEMBL1774383 1 -
CHEMBL1774385 1 -
CHEMBL1774532 1 -
CHEMBL1774533 1 -
CHEMBL1774537 1 -
CHEMBL1774538 1 -
CHEMBL1774539 1 -
CHEMBL1774540 1 -
CHEMBL1774541 1 -
CHEMBL1774542 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL180010 Ki = 375.0 nM 6.43
CHEMBL1774534 Ki = 1490.0 nM 5.83
CHEMBL1774384 Ki = 3090.0 nM 5.51
CHEMBL1774536 Ki = 3180.0 nM 5.50
CHEMBL1774535 Ki = 3360.0 nM 5.47
CHEMBL1774386 Ki = 5340.0 nM 5.27
CHEMBL1774383 Ki - -
CHEMBL1774385 Ki - -
CHEMBL1774532 Ki - -
CHEMBL1774533 Ki - -
CHEMBL1774537 Ki - -
CHEMBL1774538 Ki - -
CHEMBL1774539 Ki - -
CHEMBL1774540 Ki - -
CHEMBL1774541 Ki - -
CHEMBL1774542 Ki - -