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Assay Detail

CHEMBL675124

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

Binding
Affinity constant of compound was evaluated in rat striatum tissue preparation.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Dopamine D-2 receptor imaging radiopharmaceuticals: synthesis, radiolabeling, and in vitro binding of (R)-(+)- and (S)-(-)-3-iodo-2-hydroxy-6-methoxy-N- [(1-ethyl-2-pyrrolidinyl)methyl]benzamide.
Kung HF, Kasliwal R, Pan SG, Kung MP, Mach RH, Guo YZ.
J Med Chem (1988) 31 : 1039 -1043
PubMed 2966245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 8.89 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8946 ETICLOPRIDE 2.0 1 9.77
CHEMBL8475 1 9.37
CHEMBL8809 RACLOPRIDE 2.0 1 8.96
CHEMBL26 SULPIRIDE 3.0 1 8.82
CHEMBL8945 1 7.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8946 ETICLOPRIDE Kd = 0.17 nM 9.77
CHEMBL8475 Kd = 0.43 nM 9.37
CHEMBL8809 RACLOPRIDE Kd = 1.1 nM 8.96
CHEMBL26 SULPIRIDE Kd = 1.5 nM 8.82
CHEMBL8945 Kd = 31.1 nM 7.51