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Assay Detail

CHEMBL5168516

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

Binding
Displacement of [3H]PF-06883365 from FAP-tagged human GLP-1R expressed in CHO cells assessed as inhibition constant by radioligand binding assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor.
Griffith DA, Edmonds DJ, Fortin JP, Kalgutkar AS, Kuzmiski JB, Loria PM, Saxena AR, Bagley SW, Buckeridge C, Curto JM, Derksen DR, Dias JM, Griffor MC, Han S, Jackson VM, Landis MS, Lettiere D, Limberakis C, Liu Y, Mathiowetz AM, Patel JC, Piotrowski DW, Price DA, Ruggeri RB, Tess DA.
J Med Chem (2022) 65 : 8208 -8226
PubMed 35647711 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.22 10.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL414357 EXENATIDE 4.0 1 10.28
CHEMBL4084119 LIRAGLUTIDE 4.0 1 8.20
CHEMBL5191519 1 7.29
CHEMBL4518483 DANUGLIPRON 2.0 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL414357 EXENATIDE Ki = 0.053 nM 10.28
CHEMBL4084119 LIRAGLUTIDE Ki = 6.3 nM 8.20
CHEMBL5191519 Ki = 51.0 nM 7.29
CHEMBL4518483 DANUGLIPRON Ki = 80.0 nM 7.10