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Assay Detail

CHEMBL5149848

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Functional
Agonist activity at human GLP1R expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
6
Total Activities
6
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

Glucagon-like peptide 1 receptor (CHEMBL1784)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Insulin/GLP-1/Glucagon Triagonists for the Treatment of Diabetes and Obesity.
Huang C, Palani A, Yang Z, Deng Q, Reddy V, Nargund RP, Lin S, Altezza S, Bianchi E, Orvieto F, Carrington P.
ACS Med Chem Lett (2022) 13 : 1255 -1261
PubMed 35978702 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 10.00 10.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5186705 1 10.55
CHEMBL5183317 1 10.48
CHEMBL5196728 1 10.32
CHEMBL5188299 1 10.22
CHEMBL5182822 1 9.47
CHEMBL5197522 1 8.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5186705 EC50 = 0.028 nM 10.55
CHEMBL5183317 EC50 = 0.033 nM 10.48
CHEMBL5196728 EC50 = 0.048 nM 10.32
CHEMBL5188299 EC50 = 0.06 nM 10.22
CHEMBL5182822 EC50 = 0.34 nM 9.47
CHEMBL5197522 EC50 = 1.04 nM 8.98