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Assay Detail

CHEMBL5116007

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Functional
Agonist activity at human SST3
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of 4-(3-aminopyrrolidinyl)-3-aryl-5-(benzimidazol-2-yl)-pyridines as potent and selective SST5 agonists for the treatment of congenital hyperinsulinism.
Zhao J, Wang S, Hee Kim S, Han S, Rico-Bautista E, Sturchler E, Nguyen J, Tan H, Staley C, Karin Kusnetzow A, Betz SF, Johns M, Goulet L, Luo R, Fowler M, Athanacio J, Markison S, Scott Struthers R, Zhu Y.
Bioorg Med Chem Lett (2022) 71 : 128807 -128807
PubMed 35605837 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.70 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5174433 1 8.00
CHEMBL5195355 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5174433 EC50 = 10.0 nM 8.00
CHEMBL5195355 EC50 = 39.81 nM 7.40