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Assay Detail

CHEMBL680103

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

Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glucagon receptor (CHEMBL4773)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Potent, orally absorbed glucagon receptor antagonists.
de Laszlo SE, Hacker C, Li B, Kim D, MacCoss M, Mantlo N, Pivnichny JV, Colwell L, Koch GE, Cascieri MA, Hagmann WK.
Bioorg Med Chem Lett (1999) 9 : 641 -646
PubMed 10201821 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.05 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL351772 1 6.60
CHEMBL156458 1 6.16
CHEMBL160287 1 6.08
CHEMBL155686 1 6.00
CHEMBL158676 1 5.92
CHEMBL158548 1 5.52
CHEMBL160735 1 -
CHEMBL160372 1 -
CHEMBL348555 1 -
CHEMBL345863 1 -
CHEMBL347462 1 -
CHEMBL348401 1 -
CHEMBL160561 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL351772 IC50 = 250.0 nM 6.60
CHEMBL156458 IC50 = 700.0 nM 6.16
CHEMBL160287 IC50 = 830.0 nM 6.08
CHEMBL155686 IC50 = 1000.0 nM 6.00
CHEMBL158676 IC50 = 1200.0 nM 5.92
CHEMBL158548 IC50 = 3000.0 nM 5.52
CHEMBL160735 IC50 > 3000.0 nM -
CHEMBL160372 IC50 > 3000.0 nM -
CHEMBL348555 IC50 > 3000.0 nM -
CHEMBL345863 IC50 > 3000.0 nM -
CHEMBL347462 IC50 > 3000.0 nM -
CHEMBL348401 IC50 > 1000.0 nM -
CHEMBL160561 IC50 > 1000.0 nM -