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Assay Detail

CHEMBL671408

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

Binding
In vitro agonist binding affinity was determined by displacing the [3H]N-propylnorapomorphine ([3H]NPA) in rat striatal Dopamine receptor D2
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and pharmacological evaluation of the enantiomers of the dopamine autoreceptor agonist PD 135385
Jaen JC, Caprathe BW, Wise LD, Meltzer LT, Pugsley TA, Huffner TG
Bioorg Med Chem Lett (1993) 3 : 639 -644
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.36 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53 APOMORPHINE 4.0 1 8.77
CHEMBL348547 1 7.19
CHEMBL418937 1 7.09
CHEMBL160672 1 7.06
CHEMBL350920 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53 APOMORPHINE IC50 = 1.7 nM 8.77
CHEMBL348547 IC50 = 64.0 nM 7.19
CHEMBL418937 IC50 = 82.0 nM 7.09
CHEMBL160672 IC50 = 88.0 nM 7.06
CHEMBL350920 IC50 = 202.0 nM 6.70