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Assay Detail

CHEMBL675482

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

Binding
In vitro displacement of [3H]spiperone from Dopamine receptor D2 binding site in rat striatum.
27
Total Activities
27
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 (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines.
Kuipers W, Kruse CG, van Wijngaarden I, Standaar PJ, Tulp MT, Veldman N, Spek AL, IJzerman AP.
J Med Chem (1997) 40 : 300 -312
PubMed 9022796 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.31 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58792 FLUANISONE 2.0 1 8.51
CHEMBL105345 1 8.48
CHEMBL105747 1 8.48
CHEMBL104515 ANISOPIROL 2.0 1 8.47
CHEMBL104805 1 8.39
CHEMBL58377 1 8.30
CHEMBL294633 1 8.28
CHEMBL107141 1 8.19
CHEMBL323982 1 8.00
CHEMBL106854 1 7.89
CHEMBL81728 1 7.85
CHEMBL419910 1 7.77
CHEMBL108229 1 7.64
CHEMBL278799 1 7.19
CHEMBL104204 1 7.14
CHEMBL104578 1 7.04
CHEMBL107903 1 6.89
CHEMBL1742477 FLESINOXAN 2.0 1 6.85
CHEMBL104593 1 6.64
CHEMBL107336 1 6.60
CHEMBL26447 1 6.24
CHEMBL61032 1 6.11
CHEMBL282614 ELTOPRAZINE 2.0 1 5.96
CHEMBL104591 1 5.96
CHEMBL9666 1 5.92
CHEMBL9434 PHENYLPIPERAZINE 1 5.17
CHEMBL106413 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58792 FLUANISONE Ki = 3.1 nM 8.51
CHEMBL105345 Ki = 3.3 nM 8.48
CHEMBL105747 Ki = 3.3 nM 8.48
CHEMBL104515 ANISOPIROL Ki = 3.4 nM 8.47
CHEMBL104805 Ki = 4.1 nM 8.39
CHEMBL58377 Ki = 5.0 nM 8.30
CHEMBL294633 Ki = 5.3 nM 8.28
CHEMBL107141 Ki = 6.4 nM 8.19
CHEMBL323982 Ki = 10.0 nM 8.00
CHEMBL106854 Ki = 13.0 nM 7.89
CHEMBL81728 Ki = 14.0 nM 7.85
CHEMBL419910 Ki = 17.0 nM 7.77
CHEMBL108229 Ki = 23.0 nM 7.64
CHEMBL278799 Ki = 64.0 nM 7.19
CHEMBL104204 Ki = 73.0 nM 7.14
CHEMBL104578 Ki = 92.0 nM 7.04
CHEMBL107903 Ki = 130.0 nM 6.89
CHEMBL1742477 FLESINOXAN Ki = 140.0 nM 6.85
CHEMBL104593 Ki = 230.0 nM 6.64
CHEMBL107336 Ki = 250.0 nM 6.60
CHEMBL26447 Ki = 570.0 nM 6.24
CHEMBL61032 Ki = 780.0 nM 6.11
CHEMBL282614 ELTOPRAZINE Ki = 1100.0 nM 5.96
CHEMBL104591 Ki = 1100.0 nM 5.96
CHEMBL9666 Ki = 1200.0 nM 5.92
CHEMBL9434 PHENYLPIPERAZINE Ki = 6800.0 nM 5.17
CHEMBL106413 Ki > 10000.0 nM -