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Assay Detail

CHEMBL668874

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Binding
In vitro binding affinity to Dopamine receptor D1/Dopamine receptor D2 in rat striatal membranes using [3H]N-propylnorapomorphine
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Dopamine receptors; D1 & D2 (CHEMBL2096910)
Type SELECTIVITY GROUP
Organism Rattus norvegicus

Publication

Synthesis and dopaminergic activity of the enantiomers of 6-methyl-4,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine (PD 128483).
Jaen JC, Caprathe BW, Wise LD, Pugsley TA, Meltzer LT, Heffner TG
Bioorg Med Chem Lett (1991) 1 : 539 -544
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.08 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53 APOMORPHINE 4.0 1 8.77
CHEMBL150523 1 6.90
CHEMBL150551 1 6.86
CHEMBL150550 1 6.53
CHEMBL348012 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53 APOMORPHINE IC50 = 1.7 nM 8.77
CHEMBL150523 IC50 = 127.0 nM 6.90
CHEMBL150551 IC50 = 138.0 nM 6.86
CHEMBL150550 IC50 = 295.0 nM 6.53
CHEMBL348012 IC50 = 464.0 nM 6.33