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Assay Detail

CHEMBL643760

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

Binding
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-1A adrenergic receptor (CHEMBL229)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological activity of prazosin-related antagonists. Role of the piperazine and furan units of prazosin on the selectivity for alpha1-adrenoreceptor subtypes.
Bolognesi ML, Budriesi R, Chiarini A, Poggesi E, Leonardi A, Melchiorre C.
J Med Chem (1998) 41 : 4844 -4853
PubMed 9822553 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.85 9.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27013 1 9.78
CHEMBL341665 1 9.49
CHEMBL29591 1 9.38
CHEMBL2 PRAZOSIN 4.0 1 9.23
CHEMBL13647 BMY-7378 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27013 Ki = 0.166 nM 9.78
CHEMBL341665 Ki = 0.3236 nM 9.49
CHEMBL29591 Ki = 0.4169 nM 9.38
CHEMBL2 PRAZOSIN Ki = 0.5888 nM 9.23
CHEMBL13647 BMY-7378 Ki = 436.52 nM 6.36