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Assay Detail

CHEMBL3369124

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

Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D(2)-like receptors.
Salama I, Löber S, Hübner H, Gmeiner P.
Bioorg Med Chem Lett (2014) 24 : 3753 -3756
PubMed 25047579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 7.01 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3318824 1 8.60
CHEMBL1200986 HALOPERIDOL DECANOATE 4.0 1 8.24
CHEMBL54 HALOPERIDOL 4.0 1 8.23
CHEMBL3318848 1 8.06
CHEMBL3318845 1 8.03
CHEMBL3318849 1 7.72
CHEMBL3318831 1 7.62
CHEMBL3318847 1 7.54
CHEMBL3318832 1 7.48
CHEMBL3318846 1 7.48
CHEMBL3317465 1 7.39
CHEMBL3318833 1 7.39
CHEMBL3318851 1 7.34
CHEMBL3318850 1 7.05
CHEMBL3318844 1 6.89
CHEMBL3318842 1 6.80
CHEMBL3318835 1 6.52
CHEMBL3318834 1 6.44
CHEMBL3318839 1 6.31
CHEMBL3318837 1 6.31
CHEMBL3318836 1 6.28
CHEMBL3318841 1 6.24
CHEMBL3318843 1 6.07
CHEMBL3318840 1 5.85
CHEMBL3318838 1 5.66
CHEMBL3318852 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3318824 Ki = 2.5 nM 8.60
CHEMBL1200986 HALOPERIDOL DECANOATE Ki = 5.8 nM 8.24
CHEMBL54 HALOPERIDOL Ki = 5.9 nM 8.23
CHEMBL3318848 Ki = 8.7 nM 8.06
CHEMBL3318845 Ki = 9.3 nM 8.03
CHEMBL3318849 Ki = 19.0 nM 7.72
CHEMBL3318831 Ki = 24.0 nM 7.62
CHEMBL3318847 Ki = 29.0 nM 7.54
CHEMBL3318832 Ki = 33.0 nM 7.48
CHEMBL3318846 Ki = 33.0 nM 7.48
CHEMBL3317465 Ki = 41.0 nM 7.39
CHEMBL3318833 Ki = 41.0 nM 7.39
CHEMBL3318851 Ki = 46.0 nM 7.34
CHEMBL3318850 Ki = 89.0 nM 7.05
CHEMBL3318844 Ki = 130.0 nM 6.89
CHEMBL3318842 Ki = 160.0 nM 6.80
CHEMBL3318835 Ki = 300.0 nM 6.52
CHEMBL3318834 Ki = 360.0 nM 6.44
CHEMBL3318839 Ki = 490.0 nM 6.31
CHEMBL3318837 Ki = 490.0 nM 6.31
CHEMBL3318836 Ki = 520.0 nM 6.28
CHEMBL3318841 Ki = 570.0 nM 6.24
CHEMBL3318843 Ki = 850.0 nM 6.07
CHEMBL3318840 Ki = 1400.0 nM 5.85
CHEMBL3318838 Ki = 2200.0 nM 5.66
CHEMBL3318852 Ki = 18000.0 nM 4.75