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Assay Detail

CHEMBL890992

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

Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part II: Influence of the substitution on the benzyl moiety on the affinity for D2L, D4.2, and 5-HT2A receptors.
Carato P, Graulich A, Jensen N, Roth BL, Liégeois JF.
Bioorg Med Chem Lett (2007) 17 : 1570 -1574
PubMed 17251022 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 7.16 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL228972 1 7.96
CHEMBL234825 1 7.96
CHEMBL234645 1 7.80
CHEMBL234826 1 7.68
CHEMBL234647 1 7.58
CHEMBL234646 1 7.51
CHEMBL234472 1 7.47
CHEMBL395867 1 7.44
CHEMBL233581 1 7.43
CHEMBL234641 1 7.37
CHEMBL234643 1 7.36
CHEMBL233580 1 7.27
CHEMBL395631 1 7.18
CHEMBL233578 1 7.16
CHEMBL233404 1 7.11
CHEMBL430167 1 7.08
CHEMBL234824 1 7.02
CHEMBL234473 1 6.99
CHEMBL234640 1 6.94
CHEMBL398990 1 6.92
CHEMBL395632 1 6.81
CHEMBL229019 1 6.79
CHEMBL434583 1 6.78
CHEMBL234644 1 6.74
CHEMBL233403 1 6.65
CHEMBL234827 1 6.52
CHEMBL394042 1 6.49
CHEMBL233214 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL228972 Ki = 11.0 nM 7.96
CHEMBL234825 Ki = 11.0 nM 7.96
CHEMBL234645 Ki = 16.0 nM 7.80
CHEMBL234826 Ki = 21.0 nM 7.68
CHEMBL234647 Ki = 26.0 nM 7.58
CHEMBL234646 Ki = 31.0 nM 7.51
CHEMBL234472 Ki = 34.0 nM 7.47
CHEMBL395867 Ki = 36.0 nM 7.44
CHEMBL233581 Ki = 37.0 nM 7.43
CHEMBL234641 Ki = 43.0 nM 7.37
CHEMBL234643 Ki = 44.0 nM 7.36
CHEMBL233580 Ki = 54.0 nM 7.27
CHEMBL395631 Ki = 66.0 nM 7.18
CHEMBL233578 Ki = 69.0 nM 7.16
CHEMBL233404 Ki = 77.0 nM 7.11
CHEMBL430167 Ki = 84.0 nM 7.08
CHEMBL234824 Ki = 96.0 nM 7.02
CHEMBL234473 Ki = 103.0 nM 6.99
CHEMBL234640 Ki = 116.0 nM 6.94
CHEMBL398990 Ki = 119.0 nM 6.92
CHEMBL395632 Ki = 155.0 nM 6.81
CHEMBL229019 Ki = 162.0 nM 6.79
CHEMBL434583 Ki = 168.0 nM 6.78
CHEMBL234644 Ki = 181.0 nM 6.74
CHEMBL233403 Ki = 223.0 nM 6.65
CHEMBL234827 Ki = 299.0 nM 6.52
CHEMBL394042 Ki = 326.0 nM 6.49
CHEMBL233214 Ki = 329.0 nM 6.48