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Assay Detail

CHEMBL675834

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

Binding
In vitro affinity for dopamine receptor by displacement of [3H]- apomorphine in rat striatal membranes
11
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Dopamine receptor (CHEMBL2093868)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis of (7R)-7H-indolo[3,4-gh][1,4]benzoxazines, a new class of D-heteroergolines with dopamine agonist activity.
Anderson PS, Baldwin JJ, McClure DE, Lundell GF, Jones JH, Randall WC, Martin GE, Williams M, Hirshfield JM, Clineschmidt BV, Lumma PK, Remy DC.
J Med Chem (1983) 26 : 363 -367
PubMed 6298427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.65 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333794 4 8.70
CHEMBL333795 1 8.66
CHEMBL531 PERGOLIDE 4.0 1 8.51
CHEMBL332546 1 7.64
CHEMBL493 BROMOCRIPTINE 4.0 1 7.55
CHEMBL330997 1 7.54
CHEMBL332337 1 7.48
CHEMBL121653 1 7.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333794 IC50 = 2.0 nM 8.70
CHEMBL333795 IC50 = 2.2 nM 8.66
CHEMBL531 PERGOLIDE IC50 = 3.1 nM 8.51
CHEMBL333794 IC50 = 4.65 nM 8.33
CHEMBL332546 IC50 = 23.0 nM 7.64
CHEMBL493 BROMOCRIPTINE IC50 = 27.9 nM 7.55
CHEMBL330997 IC50 = 28.9 nM 7.54
CHEMBL332337 IC50 = 33.0 nM 7.48
CHEMBL121653 IC50 = 59.6 nM 7.22
CHEMBL333794 IC50 = 219.0 nM 6.66
CHEMBL333794 IC50 = 1240.0 nM 5.91