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Assay Detail

CHEMBL645520

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

Binding
Binding affinity against Alpha-2 adrenergic receptor in rat brain membrane using [3H]yohimbine as radioligand
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
Type PROTEIN FAMILY
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 26 6.36 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26929 1 7.77
CHEMBL15245 YOHIMBINE 3.0 1 7.52
CHEMBL444590 1 7.32
CHEMBL108245 1 7.02
CHEMBL326017 1 6.95
CHEMBL108942 1 6.84
CHEMBL321184 1 6.74
CHEMBL111760 1 6.73
CHEMBL325565 1 6.60
CHEMBL322275 1 6.58
CHEMBL108241 1 6.55
CHEMBL325092 1 6.51
CHEMBL107486 1 6.34
CHEMBL110968 1 6.25
CHEMBL324637 1 6.13
CHEMBL325079 1 6.10
CHEMBL56 8-OH-DPAT 1 6.09
CHEMBL28063 1 5.90
CHEMBL323242 1 5.88
CHEMBL26426 1 5.86
CHEMBL107921 1 5.85
CHEMBL320587 1 5.73
CHEMBL108858 1 5.57
CHEMBL107503 1 5.14
CHEMBL49 BUSPIRONE 4.0 1 5.00
CHEMBL109263 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26929 IC50 = 17.0 nM 7.77
CHEMBL15245 YOHIMBINE IC50 = 30.0 nM 7.52
CHEMBL444590 IC50 = 48.0 nM 7.32
CHEMBL108245 IC50 = 95.0 nM 7.02
CHEMBL326017 IC50 = 112.0 nM 6.95
CHEMBL108942 IC50 = 144.0 nM 6.84
CHEMBL321184 IC50 = 183.0 nM 6.74
CHEMBL111760 IC50 = 186.0 nM 6.73
CHEMBL325565 IC50 = 250.0 nM 6.60
CHEMBL322275 IC50 = 260.0 nM 6.58
CHEMBL108241 IC50 = 280.0 nM 6.55
CHEMBL325092 IC50 = 310.0 nM 6.51
CHEMBL107486 IC50 = 458.0 nM 6.34
CHEMBL110968 IC50 = 564.0 nM 6.25
CHEMBL324637 IC50 = 746.0 nM 6.13
CHEMBL325079 IC50 = 788.0 nM 6.10
CHEMBL56 8-OH-DPAT IC50 = 810.0 nM 6.09
CHEMBL28063 IC50 = 1250.0 nM 5.90
CHEMBL323242 IC50 = 1330.0 nM 5.88
CHEMBL26426 IC50 = 1380.0 nM 5.86
CHEMBL107921 IC50 = 1420.0 nM 5.85
CHEMBL320587 IC50 = 1850.0 nM 5.73
CHEMBL108858 IC50 = 2680.0 nM 5.57
CHEMBL107503 IC50 = 7220.0 nM 5.14
CHEMBL49 BUSPIRONE IC50 = 10000.0 nM 5.00
CHEMBL109263 IC50 > 10000.0 nM -