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Assay Detail

CHEMBL669055

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

Binding
Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
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 a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
Hrib NJ, Jurcak JG, Huger FP, Errico CL, Dunn RW.
J Med Chem (1991) 34 : 1068 -1072
PubMed 1672156 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.23 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 7.70
CHEMBL35057 TIOSPIRONE 2.0 1 7.66
CHEMBL85 RISPERIDONE 4.0 1 7.52
CHEMBL276175 1 6.85
CHEMBL269176 1 6.77
CHEMBL274334 1 6.57
CHEMBL10880 1 6.17
CHEMBL269458 1 6.14
CHEMBL276378 1 6.13
CHEMBL10366 1 6.03
CHEMBL42 CLOZAPINE 4.0 1 6.00
CHEMBL10640 1 6.00
CHEMBL274306 1 5.70
CHEMBL418526 1 5.70
CHEMBL268267 1 5.57
CHEMBL10821 1 5.55
CHEMBL10355 1 5.54
CHEMBL10875 1 5.43
CHEMBL10963 1 5.39
CHEMBL430329 1 -
CHEMBL10658 1 -
CHEMBL418340 1 -
CHEMBL10692 1 -
CHEMBL10194 1 -
CHEMBL10623 1 -
CHEMBL10546 1 -
CHEMBL273505 1 -
CHEMBL274566 1 -
CHEMBL264472 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL IC50 = 20.0 nM 7.70
CHEMBL35057 TIOSPIRONE IC50 = 22.0 nM 7.66
CHEMBL85 RISPERIDONE IC50 = 30.0 nM 7.52
CHEMBL276175 IC50 = 140.0 nM 6.85
CHEMBL269176 IC50 = 170.0 nM 6.77
CHEMBL274334 IC50 = 270.0 nM 6.57
CHEMBL10880 IC50 = 680.0 nM 6.17
CHEMBL269458 IC50 = 720.0 nM 6.14
CHEMBL276378 IC50 = 740.0 nM 6.13
CHEMBL10366 IC50 = 930.0 nM 6.03
CHEMBL42 CLOZAPINE IC50 = 1000.0 nM 6.00
CHEMBL10640 IC50 = 1000.0 nM 6.00
CHEMBL274306 IC50 = 2000.0 nM 5.70
CHEMBL418526 IC50 = 2000.0 nM 5.70
CHEMBL268267 IC50 = 2700.0 nM 5.57
CHEMBL10821 IC50 = 2800.0 nM 5.55
CHEMBL10355 IC50 = 2900.0 nM 5.54
CHEMBL10875 IC50 = 3700.0 nM 5.43
CHEMBL10963 IC50 = 4090.0 nM 5.39
CHEMBL430329 IC50 > 20000.0 nM -
CHEMBL10658 IC50 > 20000.0 nM -
CHEMBL418340 IC50 > 20000.0 nM -
CHEMBL10692 IC50 > 20000.0 nM -
CHEMBL10194 IC50 > 20000.0 nM -
CHEMBL10623 IC50 > 20000.0 nM -
CHEMBL10546 IC50 > 20000.0 nM -
CHEMBL273505 IC50 > 20000.0 nM -
CHEMBL274566 IC50 > 20000.0 nM -
CHEMBL264472 IC50 > 20000.0 nM -