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Assay Detail

CHEMBL616236

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

Binding
Binding affinity at human cloned 5-hydroxytryptamine 1A receptor expressed in HeLa cells by [3H]8-hydroxy-2-(di-n-propylamino)tetraline displacement.
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
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 2 7.45 8.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13647 BMY-7378 1 8.76
CHEMBL341665 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13647 BMY-7378 Ki = 1.738 nM 8.76
CHEMBL341665 Ki = 741.31 nM 6.13