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Assay Detail

CHEMBL647125

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

Binding
Displacement of [3H]prazosin binding to Alpha-1 adrenergic receptor sites on rat cerebral cortical membranes at 100 nM concentration
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Alkylating prazosin analogue: irreversible label for alpha 1-adrenoceptors.
Pitha J, Szabo L, Szurmai Z, Buchowiecki W, Kusiak JW.
J Med Chem (1989) 32 : 96 -100
PubMed 2535878 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.09 9.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2 PRAZOSIN 4.0 1 9.79
CHEMBL268768 1 9.16
CHEMBL6347 1 8.47
CHEMBL6340 1 8.36
CHEMBL266223 1 8.35
CHEMBL6358 1 7.64
CHEMBL6219 1 7.53
CHEMBL6342 1 7.40
CHEMBL6343 1 7.17
CHEMBL6314 1 6.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2 PRAZOSIN IC50 = 0.1622 nM 9.79
CHEMBL268768 IC50 = 0.6918 nM 9.16
CHEMBL6347 IC50 = 3.388 nM 8.47
CHEMBL6340 IC50 = 4.365 nM 8.36
CHEMBL266223 IC50 = 4.467 nM 8.35
CHEMBL6358 IC50 = 22.91 nM 7.64
CHEMBL6219 IC50 = 29.51 nM 7.53
CHEMBL6342 IC50 = 39.81 nM 7.40
CHEMBL6343 IC50 = 67.61 nM 7.17
CHEMBL6314 IC50 = 102.33 nM 6.99