Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3614290

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

Binding
Displacement of [3H]spiperone from human dopamine D2L receptor expressed in CHO cell membranes by radioligand competition binding assay
35
Total Activities
35
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(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: Quantitative structure-selectivity investigations, docking, synthesis and biological evaluation.
Möller D, Salama I, Kling RC, Hübner H, Gmeiner P.
Bioorg Med Chem (2015) 23 : 6195 -6209
PubMed 26299826 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 7.68 9.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1112 ARIPIPRAZOLE 4.0 1 9.32
CHEMBL217981 1 9.24
CHEMBL221129 1 9.04
CHEMBL221866 1 8.82
CHEMBL221587 1 8.60
CHEMBL220754 1 8.57
CHEMBL386986 1 8.52
CHEMBL425285 1 8.19
CHEMBL218607 1 8.19
CHEMBL3613874 1 8.17
CHEMBL139600 1 8.15
CHEMBL218351 1 8.15
CHEMBL3613876 1 7.96
CHEMBL437525 1 7.89
CHEMBL373873 1 7.85
CHEMBL385289 1 7.77
CHEMBL3613877 1 7.75
CHEMBL3613878 1 7.66
CHEMBL3613880 1 7.64
CHEMBL424294 1 7.60
CHEMBL344677 1 7.47
CHEMBL140968 1 7.46
CHEMBL221843 1 7.46
CHEMBL342060 1 7.24
CHEMBL139926 1 7.09
CHEMBL141845 1 7.07
CHEMBL142020 1 7.00
CHEMBL3613875 1 6.96
CHEMBL3613879 1 6.89
CHEMBL3613873 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1112 ARIPIPRAZOLE Ki = 0.48 nM 9.32
CHEMBL217981 Ki = 0.58 nM 9.24
CHEMBL221129 Ki = 0.91 nM 9.04
CHEMBL221866 Ki = 1.5 nM 8.82
CHEMBL221587 Ki = 2.5 nM 8.60
CHEMBL220754 Ki = 2.7 nM 8.57
CHEMBL386986 Ki = 3.0 nM 8.52
CHEMBL425285 Ki = 6.4 nM 8.19
CHEMBL218607 Ki = 6.4 nM 8.19
CHEMBL3613874 Ki = 6.7 nM 8.17
CHEMBL139600 Ki = 7.1 nM 8.15
CHEMBL218351 Ki = 7.1 nM 8.15
CHEMBL3613876 Ki = 11.0 nM 7.96
CHEMBL437525 Ki = 13.0 nM 7.89
CHEMBL373873 Ki = 14.0 nM 7.85
CHEMBL385289 Ki = 17.0 nM 7.77
CHEMBL3613877 Ki = 18.0 nM 7.75
CHEMBL3613878 Ki = 22.0 nM 7.66
CHEMBL3613880 Ki = 23.0 nM 7.64
CHEMBL424294 Ki = 25.0 nM 7.60
CHEMBL344677 Ki = 34.0 nM 7.47
CHEMBL140968 Ki = 35.0 nM 7.46
CHEMBL221843 Ki = 35.0 nM 7.46
CHEMBL342060 Ki = 58.0 nM 7.24
CHEMBL139926 Ki = 82.0 nM 7.09
CHEMBL141845 Ki = 85.0 nM 7.07
CHEMBL142020 Ki = 99.0 nM 7.00
CHEMBL3613875 Ki = 110.0 nM 6.96
CHEMBL3613879 Ki = 130.0 nM 6.89
CHEMBL3613873 Ki = 140.0 nM 6.85
CHEMBL357684 Ki = 150.0 nM 6.82
CHEMBL124444 Ki = 170.0 nM 6.77
CHEMBL143352 Ki = 290.0 nM 6.54
CHEMBL346692 Ki = 760.0 nM 6.12
CHEMBL59725 Ki = 1000.0 nM 6.00