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Assay Detail

CHEMBL663103

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]N-0437 to calf striatal membrane
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Tissue Striatum
Subcellular Membrane
Confidence 3 — Cell-line / Tissue
Curated By Intermediate

Target

Nucleic Acid (CHEMBL345)
Type NUCLEIC-ACID

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 6.79 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38428 1 8.10
CHEMBL69271 NAXAGOLIDE 2.0 1 7.89
CHEMBL607437 1 7.62
CHEMBL285755 1 7.20
CHEMBL69414 1 5.85
CHEMBL70565 1 5.80
CHEMBL607438 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38428 IC50 = 8.0 nM 8.10
CHEMBL69271 NAXAGOLIDE IC50 = 13.0 nM 7.89
CHEMBL607437 IC50 = 24.0 nM 7.62
CHEMBL285755 IC50 = 63.0 nM 7.20
CHEMBL69414 IC50 = 1400.0 nM 5.85
CHEMBL70565 IC50 = 1600.0 nM 5.80
CHEMBL607438 IC50 = 8900.0 nM 5.05