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Assay Detail

CHEMBL911249

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

Binding
Displacement of [3H]spiperone from dopamine D2-like receptor in porcine striata homogenate
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist.
Cueva JP, Giorgioni G, Grubbs RA, Chemel BR, Watts VJ, Nichols DE.
J Med Chem (2006) 49 : 6848 -6857
PubMed 17154515 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.23 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71 CHLORPROMAZINE 4.0 1 8.10
CHEMBL25856 DIHYDREXIDINE 2.0 1 6.62
CHEMBL1203924 1 6.47
CHEMBL387250 1 5.60
CHEMBL217299 DOXANTHRINE 1 5.43
CHEMBL384046 1 5.17
CHEMBL59 DOPAMINE 4.0 1 -
CHEMBL62 SCH-23390 1 -
CHEMBL240773 QUINPIROLE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71 CHLORPROMAZINE Ki = 8.0 nM 8.10
CHEMBL25856 DIHYDREXIDINE Ki = 240.0 nM 6.62
CHEMBL1203924 Ki = 340.0 nM 6.47
CHEMBL387250 Ki = 2500.0 nM 5.60
CHEMBL217299 DOXANTHRINE Ki = 3700.0 nM 5.43
CHEMBL384046 Ki = 6800.0 nM 5.17
CHEMBL59 DOPAMINE Ki - -
CHEMBL62 SCH-23390 Ki - -
CHEMBL240773 QUINPIROLE Ki - -