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Assay Detail

CHEMBL3374188

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

Binding
Displacement of of [125I]-IABN from human D3 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
25
Total Activities
25
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(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, pharmacological evaluation and molecular modeling studies of triazole containing dopamine D3 receptor ligands.
Peng X, Wang Q, Mishra Y, Xu J, Reichert DE, Malik M, Taylor M, Luedtke RR, Mach RH.
Bioorg Med Chem Lett (2015) 25 : 519 -523
PubMed 25556097 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 8.13 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1688990 1 9.10
CHEMBL3353899 1 8.74
CHEMBL3353913 1 8.68
CHEMBL3353914 1 8.64
CHEMBL1688991 1 8.62
CHEMBL3353916 1 8.54
CHEMBL3353896 1 8.51
CHEMBL3353905 1 8.49
CHEMBL3353898 1 8.43
CHEMBL3353895 1 8.33
CHEMBL3353902 1 8.20
CHEMBL3353904 1 8.19
CHEMBL3353915 1 8.17
CHEMBL3353911 1 8.17
CHEMBL3353901 1 8.09
CHEMBL3353900 1 8.05
CHEMBL3353912 1 8.02
CHEMBL3353910 1 7.86
CHEMBL3353908 1 7.68
CHEMBL3353894 1 7.65
CHEMBL3353907 1 7.59
CHEMBL3353903 1 7.58
CHEMBL3353909 1 7.53
CHEMBL3353897 1 7.44
CHEMBL3353906 1 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1688990 Ki = 0.8 nM 9.10
CHEMBL3353899 Ki = 1.8 nM 8.74
CHEMBL3353913 Ki = 2.1 nM 8.68
CHEMBL3353914 Ki = 2.3 nM 8.64
CHEMBL1688991 Ki = 2.4 nM 8.62
CHEMBL3353916 Ki = 2.9 nM 8.54
CHEMBL3353896 Ki = 3.1 nM 8.51
CHEMBL3353905 Ki = 3.2 nM 8.49
CHEMBL3353898 Ki = 3.7 nM 8.43
CHEMBL3353895 Ki = 4.7 nM 8.33
CHEMBL3353902 Ki = 6.3 nM 8.20
CHEMBL3353904 Ki = 6.5 nM 8.19
CHEMBL3353915 Ki = 6.8 nM 8.17
CHEMBL3353911 Ki = 6.7 nM 8.17
CHEMBL3353901 Ki = 8.2 nM 8.09
CHEMBL3353900 Ki = 8.9 nM 8.05
CHEMBL3353912 Ki = 9.6 nM 8.02
CHEMBL3353910 Ki = 13.9 nM 7.86
CHEMBL3353908 Ki = 21.1 nM 7.68
CHEMBL3353894 Ki = 22.2 nM 7.65
CHEMBL3353907 Ki = 25.4 nM 7.59
CHEMBL3353903 Ki = 26.5 nM 7.58
CHEMBL3353909 Ki = 29.6 nM 7.53
CHEMBL3353897 Ki = 36.3 nM 7.44
CHEMBL3353906 Ki = 93.1 nM 7.03