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Assay Detail

CHEMBL902500

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

Functional
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR.
Grundt P, Husband SL, Luedtke RR, Taylor M, Newman AH.
Bioorg Med Chem Lett (2007) 17 : 745 -749
PubMed 17095222 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 37 6.88 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL246439 1 7.70
CHEMBL246637 1 7.38
CHEMBL445102 1 7.04
CHEMBL400827 1 7.01
CHEMBL397770 1 6.63
CHEMBL246438 1 6.61
CHEMBL246020 1 6.46
CHEMBL246855 1 6.18
CHEMBL246642 1 -
CHEMBL400826 1 -
CHEMBL396092 1 -
CHEMBL247058 1 -
CHEMBL401031 1 -
CHEMBL246856 1 -
CHEMBL246854 1 -
CHEMBL246644 1 -
CHEMBL246643 1 -
CHEMBL394066 1 -
CHEMBL246021 1 -
CHEMBL246848 1 -
CHEMBL246849 1 -
CHEMBL392823 1 -
CHEMBL245614 1 -
CHEMBL398368 1 -
CHEMBL245615 1 -
CHEMBL393027 1 -
CHEMBL245815 1 -
CHEMBL245816 1 -
CHEMBL394065 1 -
CHEMBL430198 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL246439 EC50 = 20.2 nM 7.70
CHEMBL246637 EC50 = 41.5 nM 7.38
CHEMBL445102 EC50 = 90.4 nM 7.04
CHEMBL400827 EC50 = 98.6 nM 7.01
CHEMBL397770 EC50 = 232.0 nM 6.63
CHEMBL246438 EC50 = 248.0 nM 6.61
CHEMBL246020 EC50 = 347.0 nM 6.46
CHEMBL246855 EC50 = 661.0 nM 6.18
CHEMBL246856 EC50 - -
CHEMBL392822 EC50 - -
CHEMBL246854 EC50 - -
CHEMBL246644 EC50 - -
CHEMBL246643 EC50 - -
CHEMBL394066 EC50 - -
CHEMBL246021 EC50 - -
CHEMBL400826 EC50 - -
CHEMBL246437 EC50 - -
CHEMBL399601 EC50 - -
CHEMBL246232 EC50 - -
CHEMBL399396 EC50 - -
CHEMBL246231 EC50 - -
CHEMBL246230 EC50 - -
CHEMBL401031 EC50 - -
CHEMBL247058 EC50 - -
CHEMBL396092 EC50 - -
CHEMBL246642 EC50 - -
CHEMBL246848 EC50 - -
CHEMBL246849 EC50 - -
CHEMBL392823 EC50 - -
CHEMBL245614 EC50 - -
CHEMBL398368 EC50 - -
CHEMBL245615 EC50 - -
CHEMBL393027 EC50 - -
CHEMBL245815 EC50 - -
CHEMBL245816 EC50 - -
CHEMBL394065 EC50 - -
CHEMBL430198 EC50 - -