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Assay Detail

CHEMBL671401

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

Binding
Inhibition of [3H]spiperone binding to rat striatal dopamine receptor D2 was determined in vitro
31
Total Activities
30
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

Potential antipsychotic agents. 9. Synthesis and stereoselective dopamine D-2 receptor blockade of a potent class of substituted (R)-N-[(1-benzyl-2-pyrrolidinyl)methyl]benzamides. Relations to other side chain congeners.
Högberg T, Ström P, de Paulis T, Stensland B, Csöregh I, Lundin K, Hall H, Ogren SO.
J Med Chem (1991) 34 : 948 -955
PubMed 1672158 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.57 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL172536 1 9.44
CHEMBL177762 1 9.19
CHEMBL8946 ETICLOPRIDE 2.0 1 9.04
CHEMBL289330 1 8.92
CHEMBL435670 1 8.89
CHEMBL176458 1 8.85
CHEMBL76402 1 8.85
CHEMBL176804 1 8.62
CHEMBL75842 1 8.30
CHEMBL366766 1 8.27
CHEMBL123282 1 8.20
CHEMBL173536 1 8.03
CHEMBL283099 1 7.92
CHEMBL2096749 2 7.75
CHEMBL173717 1 7.68
CHEMBL176373 1 7.68
CHEMBL175082 1 7.55
CHEMBL172092 1 7.54
CHEMBL8809 RACLOPRIDE 2.0 1 7.50
CHEMBL177436 1 7.44
CHEMBL174472 1 7.39
CHEMBL295621 1 7.28
CHEMBL174606 1 6.91
CHEMBL1204286 1 6.90
CHEMBL171894 1 5.73
CHEMBL367751 1 5.66
CHEMBL262403 1 5.62
CHEMBL172865 1 5.46
CHEMBL367065 1 4.79
CHEMBL171921 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL172536 IC50 = 0.36 nM 9.44
CHEMBL177762 IC50 = 0.65 nM 9.19
CHEMBL8946 ETICLOPRIDE IC50 = 0.92 nM 9.04
CHEMBL289330 IC50 = 1.2 nM 8.92
CHEMBL435670 IC50 = 1.3 nM 8.89
CHEMBL176458 IC50 = 1.4 nM 8.85
CHEMBL76402 IC50 = 1.4 nM 8.85
CHEMBL176804 IC50 = 2.4 nM 8.62
CHEMBL75842 IC50 = 5.0 nM 8.30
CHEMBL366766 IC50 = 5.4 nM 8.27
CHEMBL123282 IC50 = 6.3 nM 8.20
CHEMBL173536 IC50 = 9.4 nM 8.03
CHEMBL283099 IC50 = 12.0 nM 7.92
CHEMBL2096749 IC50 = 18.0 nM 7.75
CHEMBL173717 IC50 = 21.0 nM 7.68
CHEMBL176373 IC50 = 21.0 nM 7.68
CHEMBL175082 IC50 = 28.0 nM 7.55
CHEMBL172092 IC50 = 29.0 nM 7.54
CHEMBL8809 RACLOPRIDE IC50 = 32.0 nM 7.50
CHEMBL177436 IC50 = 36.0 nM 7.44
CHEMBL174472 IC50 = 41.0 nM 7.39
CHEMBL295621 IC50 = 52.0 nM 7.28
CHEMBL174606 IC50 = 124.0 nM 6.91
CHEMBL1204286 IC50 = 126.0 nM 6.90
CHEMBL171894 IC50 = 1860.0 nM 5.73
CHEMBL367751 IC50 = 2210.0 nM 5.66
CHEMBL262403 IC50 = 2380.0 nM 5.62
CHEMBL2096749 IC50 = 2680.0 nM 5.57
CHEMBL172865 IC50 = 3450.0 nM 5.46
CHEMBL367065 IC50 = 16300.0 nM 4.79
CHEMBL171921 IC50 > 10000.0 nM -