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Assay Detail

CHEMBL672934

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

Binding
In vitro binding affinity towards dopamine receptor was determined in bovine anterior pituitary membrane using [3H]dihydroergocriptine as the radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dopamine receptor (CHEMBL2096970)
Type PROTEIN FAMILY
Organism Bos taurus

Publication

Synthesis and central dopaminergic activities of (+/-)-hexahydro-7H-indolo[3,4-gh][1,4]benzoxazine derivatives [(+/-)-9-oxaergolines].
Nedelec L, Pierdet A, Fauveau P, Euvrard C, Proulx-Ferland L, Dumont C, Labrie F, Boissier JR.
J Med Chem (1983) 26 : 522 -527
PubMed 6834383 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.14 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333795 1 7.40
CHEMBL1275 PERGOLIDE MESYLATE 4.0 1 7.30
CHEMBL148600 1 6.52
CHEMBL347326 1 6.30
CHEMBL330997 1 5.60
CHEMBL147244 1 5.52
CHEMBL359414 1 5.32
CHEMBL121653 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333795 IC50 = 40.0 nM 7.40
CHEMBL1275 PERGOLIDE MESYLATE IC50 = 50.0 nM 7.30
CHEMBL148600 IC50 = 300.0 nM 6.52
CHEMBL347326 IC50 = 500.0 nM 6.30
CHEMBL330997 IC50 = 2500.0 nM 5.60
CHEMBL147244 IC50 = 3000.0 nM 5.52
CHEMBL359414 IC50 = 4800.0 nM 5.32
CHEMBL121653 IC50 = 7000.0 nM 5.16