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Assay Detail

CHEMBL4046975

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

Binding
Displacement of [3H]spiperone from human D3R expressed in CHO cell membranes
22
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

β-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation.
Männel B, Hübner H, Möller D, Gmeiner P.
Bioorg Med Chem (2017) 25 : 5613 -5628
PubMed 28870802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.56 9.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4063145 2 9.46
CHEMBL4079375 1 8.92
CHEMBL4103639 1 8.64
CHEMBL4068561 2 8.57
CHEMBL1112 ARIPIPRAZOLE 4.0 1 8.54
CHEMBL4065797 1 8.43
CHEMBL4087217 1 8.23
CHEMBL4095881 1 7.62
CHEMBL4085752 2 7.52
CHEMBL4084712 1 7.38
CHEMBL4102646 1 7.32
CHEMBL4066916 1 6.96
CHEMBL4093493 1 6.80
CHEMBL4094407 1 6.42
CHEMBL4092462 1 6.38
CHEMBL4072785 1 6.29
CHEMBL4064759 1 6.10
CHEMBL4064191 1 5.77
CHEMBL4094900 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4063145 Ki = 0.35 nM 9.46
CHEMBL4063145 Ki = 0.39 nM 9.41
CHEMBL4079375 Ki = 1.2 nM 8.92
CHEMBL4103639 Ki = 2.3 nM 8.64
CHEMBL4068561 Ki = 2.7 nM 8.57
CHEMBL4068561 Ki = 2.9 nM 8.54
CHEMBL1112 ARIPIPRAZOLE Ki = 2.9 nM 8.54
CHEMBL4065797 Ki = 3.7 nM 8.43
CHEMBL4087217 Ki = 5.9 nM 8.23
CHEMBL4095881 Ki = 24.0 nM 7.62
CHEMBL4085752 Ki = 30.0 nM 7.52
CHEMBL4085752 Ki = 35.0 nM 7.46
CHEMBL4084712 Ki = 42.0 nM 7.38
CHEMBL4102646 Ki = 48.0 nM 7.32
CHEMBL4066916 Ki = 110.0 nM 6.96
CHEMBL4093493 Ki = 160.0 nM 6.80
CHEMBL4094407 Ki = 380.0 nM 6.42
CHEMBL4092462 Ki = 420.0 nM 6.38
CHEMBL4072785 Ki = 510.0 nM 6.29
CHEMBL4064759 Ki = 790.0 nM 6.10
CHEMBL4064191 Ki = 1700.0 nM 5.77
CHEMBL4094900 Ki = 2800.0 nM 5.55