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Assay Detail

CHEMBL648797

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

Binding
Compound was tested for its binding affinity towards Rat-1 cells stably expressing hamster Alpha-1b adrenergic receptor by displacing [125I]HEAT (2-beta-(4-hydroxyphenyl)-ethylaminomethyltetralone)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cricetulus griseus
Cell Type Rat-1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Alpha-1B adrenergic receptor (CHEMBL232)
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 6 6.52 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL302882 1 7.10
CHEMBL292801 NORTOPSENTIN B 1 6.89
CHEMBL63208 NORTOPSENTIN C 1 6.77
CHEMBL302637 NORTOPSENTIN A 1 6.28
CHEMBL436760 BROMOTOPSENTIN 1 6.13
CHEMBL303282 TOPSENTIN 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL302882 Ki = 80.0 nM 7.10
CHEMBL292801 NORTOPSENTIN B Ki = 130.0 nM 6.89
CHEMBL63208 NORTOPSENTIN C Ki = 170.0 nM 6.77
CHEMBL302637 NORTOPSENTIN A Ki = 520.0 nM 6.28
CHEMBL436760 BROMOTOPSENTIN Ki = 740.0 nM 6.13
CHEMBL303282 TOPSENTIN Ki = 1150.0 nM 5.94