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Assay Detail

CHEMBL4145427

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

Functional
Antagonist activity at human SSTR3 expressed in HEK293 cells assessed as [Tyr1]-somatostatin 14-induced beta-arrestin recruitment pre-incubated for 30 mins before [Tyr1]-somatostatin 14 stimulation for 90 or 180 mins by chemiluminescence method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Somatostatin receptor type 3 (CHEMBL2028)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery, Synthesis, Pharmacological Profiling, and Biological Characterization of Brintonamides A-E, Novel Dual Protease and GPCR Modulators from a Marine Cyanobacterium.
Al-Awadhi FH, Gao B, Rezaei MA, Kwan JC, Li C, Ye T, Paul VJ, Luesch H.
J Med Chem (2018) 61 : 6364 -6378
PubMed 30015488 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.36 5.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4168948 1 5.51
CHEMBL4163618 1 5.21
CHEMBL4173913 1 -
CHEMBL4174297 1 -
CHEMBL4161021 1 -
CHEMBL4165525 1 -
CHEMBL4176134 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4168948 IC50 = 3120.0 nM 5.51
CHEMBL4163618 IC50 = 6110.0 nM 5.21
CHEMBL4173913 IC50 > 20000.0 nM -
CHEMBL4174297 IC50 > 20000.0 nM -
CHEMBL4161021 IC50 > 20000.0 nM -
CHEMBL4165525 IC50 > 20000.0 nM -
CHEMBL4176134 IC50 > 20000.0 nM -