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Assay Detail

CHEMBL670973

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

Binding
Binding affinity at native Dopamine receptor D2 in rat striatum by [3H]spiperone displacement.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 6.22 7.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13647 BMY-7378 1 7.32
CHEMBL341665 1 5.71
CHEMBL27013 1 5.63
CHEMBL2 PRAZOSIN 4.0 1 -
CHEMBL29591 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13647 BMY-7378 Ki = 47.86 nM 7.32
CHEMBL341665 Ki = 1949.84 nM 5.71
CHEMBL27013 Ki = 2344.23 nM 5.63
CHEMBL2 PRAZOSIN Ki < 10000.0 nM -
CHEMBL29591 Ki < 10000.0 nM -