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Assay Detail

CHEMBL5343829

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Functional
Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type HEK
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bombesin receptor subtype-3 (CHEMBL1075140)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of Dimethyl Shikonin Oxime 5a, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Type 2 Diabetes Mellitus.
Wu L, Cui J, Zhao C, Wang Z, Lu J, Li S, Jia J, Xiao H, Zhang Y.
J Med Chem (2023) 66 : 8011 -8029
PubMed 37272653 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.27 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1672354 1 8.52
CHEMBL5406411 1 7.17
CHEMBL5430646 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1672354 EC50 = 2.992 nM 8.52
CHEMBL5406411 EC50 = 66.99 nM 7.17
CHEMBL5430646 EC50 = 779.83 nM 6.11