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Assay Detail

CHEMBL616132

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

Binding
Inhibition of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor serotonergic receptor in human HeLa cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New potential uroselective NO-donor alpha1-antagonists.
Boschi D, Tron GC, Di Stilo A, Fruttero R, Gasco A, Poggesi E, Motta G, Leonardi A.
J Med Chem (2003) 46 : 3762 -3765
PubMed 12904082 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.55 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL125365 1 8.92
CHEMBL338608 1 8.80
CHEMBL125989 1 8.66
CHEMBL278865 UPIDOSIN 2.0 1 8.23
CHEMBL338029 1 8.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL125365 Ki = 1.2 nM 8.92
CHEMBL338608 Ki = 1.6 nM 8.80
CHEMBL125989 Ki = 2.2 nM 8.66
CHEMBL278865 UPIDOSIN Ki = 5.9 nM 8.23
CHEMBL338029 Ki = 7.2 nM 8.14