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Assay Detail

CHEMBL645245

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

Binding
In vitro inhibition of [3H]prazosin binding to rat alpha-1 adrenergic receptors.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

1-aryl-4-[(5-methoxy-1,2,3, 4-tetrahydronaphthalen-1-yl)alkyl]piperazines and their analogues: influence of the stereochemistry of the tetrahydronaphthalen-1-yl nucleus on 5-HT1A receptor affinity and selectivity versus alpha1 and D2 receptors. 5.
Perrone R, Berardi F, Colabufo NA, Leopoldo M, Tortorella V.
J Med Chem (1999) 42 : 490 -496
PubMed 9986719 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.82 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL144523 1 9.10
CHEMBL26929 1 8.19
CHEMBL147659 1 7.48
CHEMBL322275 1 7.37
CHEMBL147963 1 7.21
CHEMBL444590 1 7.18
CHEMBL148186 1 7.07
CHEMBL28063 1 6.82
CHEMBL108241 1 6.66
CHEMBL148234 1 6.64
CHEMBL435029 1 6.62
CHEMBL148288 1 6.24
CHEMBL147692 1 6.19
CHEMBL359245 1 6.11
CHEMBL107486 1 6.05
CHEMBL147861 1 6.02
CHEMBL147371 1 6.00
CHEMBL148397 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL144523 IC50 = 0.8 nM 9.10
CHEMBL26929 IC50 = 6.5 nM 8.19
CHEMBL147659 IC50 = 33.0 nM 7.48
CHEMBL322275 IC50 = 43.0 nM 7.37
CHEMBL147963 IC50 = 61.0 nM 7.21
CHEMBL444590 IC50 = 66.0 nM 7.18
CHEMBL148186 IC50 = 85.0 nM 7.07
CHEMBL28063 IC50 = 153.0 nM 6.82
CHEMBL108241 IC50 = 220.0 nM 6.66
CHEMBL148234 IC50 = 228.0 nM 6.64
CHEMBL435029 IC50 = 240.0 nM 6.62
CHEMBL148288 IC50 = 580.0 nM 6.24
CHEMBL147692 IC50 = 649.0 nM 6.19
CHEMBL359245 IC50 = 770.0 nM 6.11
CHEMBL107486 IC50 = 881.0 nM 6.05
CHEMBL147861 IC50 = 950.0 nM 6.02
CHEMBL147371 IC50 = 1000.0 nM 6.00
CHEMBL148397 IC50 = 1700.0 nM 5.77