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Assay Detail

CHEMBL667499

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

Binding
Binding affinity against Dopamine receptor D2 in rat striatal membrane using [3H]spiroperidol as radioligand
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

1-aryl-4-[(1-tetralinyl)alkyl]piperazines: alkylamido and alkylamino derivatives. Synthesis, 5-HT1A receptor affinity, and selectivity. 3.
Perrone R, Berardi F, Leopoldo M, Tortorella V, Fornaretto MG, Caccia C, McArthur RA.
J Med Chem (1996) 39 : 3195 -3202
PubMed 8759642 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.17 7.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28209 1 7.81
CHEMBL326017 1 7.14
CHEMBL110968 1 6.94
CHEMBL49 BUSPIRONE 4.0 1 6.55
CHEMBL321184 1 6.48
CHEMBL26426 1 6.35
CHEMBL108942 1 6.23
CHEMBL28063 1 6.12
CHEMBL111760 1 6.11
CHEMBL324637 1 6.09
CHEMBL325565 1 6.05
CHEMBL107486 1 5.97
CHEMBL107921 1 5.96
CHEMBL325092 1 5.92
CHEMBL108245 1 5.73
CHEMBL323242 1 5.72
CHEMBL325079 1 5.67
CHEMBL107503 1 5.61
CHEMBL108858 1 5.53
CHEMBL320587 1 5.39
CHEMBL109263 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28209 IC50 = 15.4 nM 7.81
CHEMBL326017 IC50 = 73.0 nM 7.14
CHEMBL110968 IC50 = 116.0 nM 6.94
CHEMBL49 BUSPIRONE IC50 = 280.0 nM 6.55
CHEMBL321184 IC50 = 332.0 nM 6.48
CHEMBL26426 IC50 = 448.0 nM 6.35
CHEMBL108942 IC50 = 594.0 nM 6.23
CHEMBL28063 IC50 = 761.0 nM 6.12
CHEMBL111760 IC50 = 783.0 nM 6.11
CHEMBL324637 IC50 = 819.0 nM 6.09
CHEMBL325565 IC50 = 882.0 nM 6.05
CHEMBL107486 IC50 = 1060.0 nM 5.97
CHEMBL107921 IC50 = 1100.0 nM 5.96
CHEMBL325092 IC50 = 1200.0 nM 5.92
CHEMBL108245 IC50 = 1850.0 nM 5.73
CHEMBL323242 IC50 = 1900.0 nM 5.72
CHEMBL325079 IC50 = 2160.0 nM 5.67
CHEMBL107503 IC50 = 2440.0 nM 5.61
CHEMBL108858 IC50 = 2970.0 nM 5.53
CHEMBL320587 IC50 = 4040.0 nM 5.39
CHEMBL109263 IC50 > 10000.0 nM -