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Assay Detail

CHEMBL975083

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

Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Striatum
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(1A) dopamine receptor (CHEMBL265)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Halogenated boldine derivatives with enhanced monoamine receptor selectivity.
Sobarzo-Sánchez EM, Arbaoui J, Protais P, Cassels BK.
J Nat Prod (2000) 63 : 480 -484
PubMed 10785418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.18 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL256075 1 8.52
CHEMBL225853 3-BROMOBOLDINE 1 7.18
CHEMBL524439 1 7.09
CHEMBL388564 1 6.69
CHEMBL388342 BOLDINE 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL256075 IC50 = 3.0 nM 8.52
CHEMBL225853 3-BROMOBOLDINE IC50 = 66.0 nM 7.18
CHEMBL524439 IC50 = 81.0 nM 7.09
CHEMBL388564 IC50 = 206.0 nM 6.69
CHEMBL388342 BOLDINE IC50 = 400.0 nM 6.40