Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL647614

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

Binding
Binding affinity against Alpha-1 adrenergic receptor in rat brain membrane using [3H]prazosin as radioligand
27
Total Activities
27
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-1 (CHEMBL1907610)
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 27 6.67 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2 PRAZOSIN 4.0 1 8.85
CHEMBL26929 1 8.19
CHEMBL111760 1 7.72
CHEMBL322275 1 7.37
CHEMBL444590 1 7.18
CHEMBL28209 1 7.11
CHEMBL110968 1 7.08
CHEMBL28063 1 6.82
CHEMBL108942 1 6.80
CHEMBL26426 1 6.78
CHEMBL108241 1 6.66
CHEMBL321184 1 6.53
CHEMBL108858 1 6.50
CHEMBL324637 1 6.49
CHEMBL320587 1 6.37
CHEMBL325565 1 6.29
CHEMBL323242 1 6.27
CHEMBL325079 1 6.20
CHEMBL108245 1 6.14
CHEMBL325092 1 6.10
CHEMBL107503 1 6.08
CHEMBL107486 1 6.05
CHEMBL326017 1 6.05
CHEMBL107921 1 5.94
CHEMBL109263 1 5.22
CHEMBL56 8-OH-DPAT 1 -
CHEMBL49 BUSPIRONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2 PRAZOSIN IC50 = 1.4 nM 8.85
CHEMBL26929 IC50 = 6.5 nM 8.19
CHEMBL111760 IC50 = 19.0 nM 7.72
CHEMBL322275 IC50 = 43.0 nM 7.37
CHEMBL444590 IC50 = 66.0 nM 7.18
CHEMBL28209 IC50 = 78.3 nM 7.11
CHEMBL110968 IC50 = 84.0 nM 7.08
CHEMBL28063 IC50 = 153.0 nM 6.82
CHEMBL108942 IC50 = 159.0 nM 6.80
CHEMBL26426 IC50 = 166.0 nM 6.78
CHEMBL108241 IC50 = 220.0 nM 6.66
CHEMBL321184 IC50 = 297.0 nM 6.53
CHEMBL108858 IC50 = 313.0 nM 6.50
CHEMBL324637 IC50 = 327.0 nM 6.49
CHEMBL320587 IC50 = 427.0 nM 6.37
CHEMBL325565 IC50 = 510.0 nM 6.29
CHEMBL323242 IC50 = 534.0 nM 6.27
CHEMBL325079 IC50 = 626.0 nM 6.20
CHEMBL108245 IC50 = 725.0 nM 6.14
CHEMBL325092 IC50 = 790.0 nM 6.10
CHEMBL107503 IC50 = 838.0 nM 6.08
CHEMBL107486 IC50 = 881.0 nM 6.05
CHEMBL326017 IC50 = 887.0 nM 6.05
CHEMBL107921 IC50 = 1150.0 nM 5.94
CHEMBL109263 IC50 = 5980.0 nM 5.22
CHEMBL56 8-OH-DPAT IC50 > 10000.0 nM -
CHEMBL49 BUSPIRONE IC50 > 10000.0 nM -