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Assay Detail

CHEMBL670974

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

Binding
Binding affinity against Dopamine receptor D2 in rat striatal membranes using [3H]spiperone
9
Total Activities
9
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 Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N,N-6-bis-[2-(3,4-dihydroxybenzyl)pyrrolidinyl]hexane, a potent, selective, orally active dopamine analog with hypotensive and diuretic activity
Fisher LE, Rosenkranz RP, Clark RD, Muchowski JM, McClelland DL, Michel A, Caroon JM, Galeazzi E, Eglen R, Whiting RL
Bioorg Med Chem Lett (1995) 5 : 2371 -2376
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.87 8.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL80369 1 8.50
CHEMBL308295 1 8.49
CHEMBL310997 1 8.21
CHEMBL80974 1 8.05
CHEMBL588 FENOLDOPAM 4.0 1 7.88
CHEMBL80686 1 7.83
CHEMBL15564 1 7.65
CHEMBL240773 QUINPIROLE 2.0 1 7.20
CHEMBL59 DOPAMINE 4.0 1 6.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL80369 Ki = 3.162 nM 8.50
CHEMBL308295 Ki = 3.236 nM 8.49
CHEMBL310997 Ki = 6.166 nM 8.21
CHEMBL80974 Ki = 8.913 nM 8.05
CHEMBL588 FENOLDOPAM Ki = 13.18 nM 7.88
CHEMBL80686 Ki = 14.79 nM 7.83
CHEMBL15564 Ki = 22.39 nM 7.65
CHEMBL240773 QUINPIROLE Ki = 63.1 nM 7.20
CHEMBL59 DOPAMINE Ki = 104.71 nM 6.98