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Assay Detail

CHEMBL676133

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

Binding
Inhibition of [3H]raclopride binding to rat striatal dopamine receptor D2
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct 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
Ki 9 9.75 10.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289330 1 10.74
CHEMBL176458 1 10.62
CHEMBL76402 1 10.19
CHEMBL171921 1 9.82
CHEMBL435670 1 9.72
CHEMBL175082 1 9.37
CHEMBL283099 1 9.26
CHEMBL2096749 1 9.10
CHEMBL8809 RACLOPRIDE 2.0 1 8.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289330 Ki = 0.018 nM 10.74
CHEMBL176458 Ki = 0.024 nM 10.62
CHEMBL76402 Ki = 0.064 nM 10.19
CHEMBL171921 Ki = 0.15 nM 9.82
CHEMBL435670 Ki = 0.19 nM 9.72
CHEMBL175082 Ki = 0.43 nM 9.37
CHEMBL283099 Ki = 0.55 nM 9.26
CHEMBL2096749 Ki = 0.8 nM 9.10
CHEMBL8809 RACLOPRIDE Ki = 1.3 nM 8.89