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Assay Detail

CHEMBL672308

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Binding
Binding affinity for dopamine receptor D2 determined using [3H]spiperone
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
Feenstra RW, de Moes J, Hofma JJ, Kling H, Kuipers W, Long SK, Tulp MT, van der Heyden JA, Kruse CG.
Bioorg Med Chem Lett (2001) 11 : 2345 -2349
PubMed 11527728 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 8.47 9.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL80230 1 9.39
CHEMBL292187 ELOPIPRAZOLE 2.0 1 9.38
CHEMBL308345 1 9.33
CHEMBL310048 1 9.03
CHEMBL305920 1 9.00
CHEMBL310045 1 8.89
CHEMBL54 HALOPERIDOL 4.0 1 8.85
CHEMBL77472 1 8.77
CHEMBL76990 1 8.74
CHEMBL420016 1 8.70
CHEMBL218166 BIFEPRUNOX 3.0 1 8.66
CHEMBL75621 1 8.66
CHEMBL74805 1 8.54
CHEMBL419275 1 8.52
CHEMBL85 RISPERIDONE 4.0 1 8.51
CHEMBL308476 1 8.40
CHEMBL78058 1 8.34
CHEMBL58377 1 8.30
CHEMBL80156 1 8.22
CHEMBL308875 1 8.09
CHEMBL306830 1 8.09
CHEMBL305834 1 8.03
CHEMBL306634 1 8.00
CHEMBL78241 1 8.00
CHEMBL309215 1 8.00
CHEMBL77334 1 7.92
CHEMBL77934 1 7.75
CHEMBL42 CLOZAPINE 4.0 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL80230 Ki = 0.41 nM 9.39
CHEMBL292187 ELOPIPRAZOLE Ki = 0.42 nM 9.38
CHEMBL308345 Ki = 0.47 nM 9.33
CHEMBL310048 Ki = 0.93 nM 9.03
CHEMBL305920 Ki = 1.0 nM 9.00
CHEMBL310045 Ki = 1.3 nM 8.89
CHEMBL54 HALOPERIDOL Ki = 1.4 nM 8.85
CHEMBL77472 Ki = 1.7 nM 8.77
CHEMBL76990 Ki = 1.8 nM 8.74
CHEMBL420016 Ki = 2.0 nM 8.70
CHEMBL218166 BIFEPRUNOX Ki = 2.2 nM 8.66
CHEMBL75621 Ki = 2.2 nM 8.66
CHEMBL74805 Ki = 2.9 nM 8.54
CHEMBL419275 Ki = 3.0 nM 8.52
CHEMBL85 RISPERIDONE Ki = 3.1 nM 8.51
CHEMBL308476 Ki = 4.0 nM 8.40
CHEMBL78058 Ki = 4.6 nM 8.34
CHEMBL58377 Ki = 5.0 nM 8.30
CHEMBL80156 Ki = 6.0 nM 8.22
CHEMBL308875 Ki = 8.1 nM 8.09
CHEMBL306830 Ki = 8.1 nM 8.09
CHEMBL305834 Ki = 9.3 nM 8.03
CHEMBL306634 Ki = 10.0 nM 8.00
CHEMBL78241 Ki = 10.0 nM 8.00
CHEMBL309215 Ki = 10.0 nM 8.00
CHEMBL77334 Ki = 12.0 nM 7.92
CHEMBL77934 Ki = 18.0 nM 7.75
CHEMBL42 CLOZAPINE Ki = 69.0 nM 7.16