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Assay Detail

CHEMBL648792

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

Binding
Compound was tested for its binding affinity towards CHO cells expressing human Alpha-1a adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)
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 Autocuration

Target

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

Publication

Marine sponge bis(indole) alkaloids that displace ligand binding to 1 adrenergic receptors
Phife DW, Ramos RA, Feng M, King I, Gunasekera SP, Wright A, Patel M, Pachter JA, Coval SJ
Bioorg Med Chem Lett (1996) 6 : 2103 -2106
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 5.96 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL302882 1 6.85
CHEMBL63208 NORTOPSENTIN C 1 6.26
CHEMBL292801 NORTOPSENTIN B 1 6.11
CHEMBL302637 NORTOPSENTIN A 1 5.67
CHEMBL436760 BROMOTOPSENTIN 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL302882 Ki = 140.0 nM 6.85
CHEMBL63208 NORTOPSENTIN C Ki = 550.0 nM 6.26
CHEMBL292801 NORTOPSENTIN B Ki = 770.0 nM 6.11
CHEMBL302637 NORTOPSENTIN A Ki = 2140.0 nM 5.67
CHEMBL436760 BROMOTOPSENTIN Ki = 12590.0 nM 4.90