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Assay Detail

CHEMBL873485

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

Binding
Binding affinity at Alpha-1 adrenergic receptor sites on rat cerebral cortical membranes by [3H]prazosin displacement.
17
Total Activities
17
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

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 17 7.74 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL414196 1 9.29
CHEMBL263077 1 8.47
CHEMBL6208 1 8.27
CHEMBL415285 1 7.94
CHEMBL266081 1 7.93
CHEMBL6366 1 7.90
CHEMBL6351 1 7.90
CHEMBL6313 1 7.70
CHEMBL6348 1 7.68
CHEMBL6218 1 7.56
CHEMBL112998 1 7.47
CHEMBL6323 1 7.31
CHEMBL447227 1 7.29
CHEMBL6290 1 7.10
CHEMBL6321 1 7.06
CHEMBL6302 1 7.01
CHEMBL264721 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL414196 IC50 = 0.5129 nM 9.29
CHEMBL263077 IC50 = 3.388 nM 8.47
CHEMBL6208 IC50 = 5.37 nM 8.27
CHEMBL415285 IC50 = 11.48 nM 7.94
CHEMBL266081 IC50 = 11.75 nM 7.93
CHEMBL6366 IC50 = 12.59 nM 7.90
CHEMBL6351 IC50 = 12.59 nM 7.90
CHEMBL6313 IC50 = 19.95 nM 7.70
CHEMBL6348 IC50 = 20.89 nM 7.68
CHEMBL6218 IC50 = 27.54 nM 7.56
CHEMBL112998 IC50 = 33.88 nM 7.47
CHEMBL6323 IC50 = 48.98 nM 7.31
CHEMBL447227 IC50 = 51.29 nM 7.29
CHEMBL6290 IC50 = 79.43 nM 7.10
CHEMBL6321 IC50 = 87.1 nM 7.06
CHEMBL6302 IC50 = 97.72 nM 7.01
CHEMBL264721 IC50 = 0.006918 nM -