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Assay Detail

CHEMBL770866

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

Binding
Potency to displace the specific in vitro binding of [3H]DP-5,6-ADTN to rat striatal membrane
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and pharmacology of trans-4-n-propyl-3,4,4a,10b-tetrahydro-2H,5H-1-benzopyrano[4,3-b ]-1,4-oxazin-7- and -9-ols: the significance of nitrogen pKa values for central dopamine receptor activation.
Dijkstra D, Mulder TB, Rollema H, Tepper PG, Van der Weide J, Horn AS.
J Med Chem (1988) 31 : 2178 -2182
PubMed 2903247 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.05 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69271 NAXAGOLIDE 2.0 1 8.52
CHEMBL38428 1 8.40
CHEMBL285755 1 7.52
CHEMBL607437 1 7.12
CHEMBL69414 1 6.75
CHEMBL607438 1 5.53
CHEMBL70565 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69271 NAXAGOLIDE IC50 = 3.0 nM 8.52
CHEMBL38428 IC50 = 4.0 nM 8.40
CHEMBL285755 IC50 = 30.0 nM 7.52
CHEMBL607437 IC50 = 75.0 nM 7.12
CHEMBL69414 IC50 = 180.0 nM 6.75
CHEMBL607438 IC50 = 2923.0 nM 5.53
CHEMBL70565 IC50 = 3070.0 nM 5.51