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Assay Detail

CHEMBL675884

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Binding
In vitro affinity for rat striatal Dopamine receptor D2 labeled with [3H]spiperone
26
Total Activities
26
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

Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.
Yevich JP, New JS, Smith DW, Lobeck WG, Catt JD, Minielli JL, Eison MS, Taylor DP, Riblet LA, Temple DL.
J Med Chem (1986) 29 : 359 -369
PubMed 2869146 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.18 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL123338 1 8.70
CHEMBL1204189 TIOSPIRONE HYDROCHLORIDE -1.0 1 8.10
CHEMBL124291 1 8.00
CHEMBL332147 1 7.64
CHEMBL123653 1 7.60
CHEMBL331227 1 7.52
CHEMBL1203226 1 7.38
CHEMBL1203225 1 7.31
CHEMBL1203220 1 7.28
CHEMBL1203224 1 7.26
CHEMBL121774 1 7.23
CHEMBL331221 1 7.19
CHEMBL420164 1 7.16
CHEMBL121065 1 7.11
CHEMBL123133 1 6.84
CHEMBL122100 1 6.84
CHEMBL123121 1 6.69
CHEMBL123048 1 6.63
CHEMBL332241 1 6.62
CHEMBL333257 1 6.44
CHEMBL124119 1 6.36
CHEMBL124047 1 6.06
CHEMBL1204336 1 -
CHEMBL123834 1 -
CHEMBL1203222 1 -
CHEMBL1203223 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL123338 IC50 = 2.0 nM 8.70
CHEMBL1204189 TIOSPIRONE HYDROCHLORIDE IC50 = 8.0 nM 8.10
CHEMBL124291 IC50 = 10.0 nM 8.00
CHEMBL332147 IC50 = 23.0 nM 7.64
CHEMBL123653 IC50 = 25.0 nM 7.60
CHEMBL331227 IC50 = 30.0 nM 7.52
CHEMBL1203226 IC50 = 42.0 nM 7.38
CHEMBL1203225 IC50 = 49.0 nM 7.31
CHEMBL1203220 IC50 = 53.0 nM 7.28
CHEMBL1203224 IC50 = 55.0 nM 7.26
CHEMBL121774 IC50 = 59.0 nM 7.23
CHEMBL331221 IC50 = 64.0 nM 7.19
CHEMBL420164 IC50 = 69.0 nM 7.16
CHEMBL121065 IC50 = 78.0 nM 7.11
CHEMBL123133 IC50 = 145.0 nM 6.84
CHEMBL122100 IC50 = 145.0 nM 6.84
CHEMBL123121 IC50 = 203.0 nM 6.69
CHEMBL123048 IC50 = 235.0 nM 6.63
CHEMBL332241 IC50 = 240.0 nM 6.62
CHEMBL333257 IC50 = 360.0 nM 6.44
CHEMBL124119 IC50 = 440.0 nM 6.36
CHEMBL124047 IC50 = 870.0 nM 6.06
CHEMBL1204336 IC50 > 1000.0 nM -
CHEMBL123834 IC50 > 1000.0 nM -
CHEMBL1203222 IC50 > 1000.0 nM -
CHEMBL1203223 IC50 > 1000.0 nM -