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Assay Detail

CHEMBL675757

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

Binding
Inhibition of 0.1 nM of [125I]- (S)-N-(1-Ethyl-pyrrolidin-2-ylmethyl)-5-iodo-2-methoxy-benzamide binding in striatal homogenates of rat brain
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

(S)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-[125I]iodo- 2-methoxybenzamide hydrochloride, a new selective radioligand for dopamine D-2 receptors.
de Paulis T, Janowsky A, Kessler RM, Clanton JA, Smith HE.
J Med Chem (1988) 31 : 2027 -2033
PubMed 3172140 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.57 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.92
CHEMBL8809 RACLOPRIDE 2.0 1 8.89
CHEMBL49897 IODOPRIDE 1 8.82
CHEMBL26 SULPIRIDE 3.0 1 7.48
CHEMBL2115023 1 6.95
CHEMBL62 SCH-23390 1 6.22
CHEMBL59 DOPAMINE 4.0 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL IC50 = 1.2 nM 8.92
CHEMBL8809 RACLOPRIDE IC50 = 1.3 nM 8.89
CHEMBL49897 IODOPRIDE IC50 = 1.5 nM 8.82
CHEMBL26 SULPIRIDE IC50 = 33.0 nM 7.48
CHEMBL2115023 IC50 = 113.0 nM 6.95
CHEMBL62 SCH-23390 IC50 = 600.0 nM 6.22
CHEMBL59 DOPAMINE IC50 = 1860.0 nM 5.73