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Assay Detail

CHEMBL680807

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 [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
27
Total Activities
27
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 27 6.63 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL156458 1 7.52
CHEMBL351772 1 7.43
CHEMBL160287 1 7.31
CHEMBL155686 1 7.30
CHEMBL160735 1 7.22
CHEMBL158548 1 7.22
CHEMBL158676 1 7.10
CHEMBL347663 1 6.82
CHEMBL328126 1 6.70
CHEMBL160490 1 6.66
CHEMBL158989 1 6.64
CHEMBL155694 1 6.62
CHEMBL158535 1 6.57
CHEMBL346698 1 6.47
CHEMBL345834 1 6.47
CHEMBL160638 1 6.47
CHEMBL160380 1 6.40
CHEMBL157529 1 6.37
CHEMBL348555 1 6.36
CHEMBL160281 1 6.34
CHEMBL345863 1 6.30
CHEMBL347462 1 6.17
CHEMBL160561 1 6.16
CHEMBL160372 1 6.16
CHEMBL351104 1 6.10
CHEMBL158671 1 5.57
CHEMBL348401 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL156458 IC50 = 30.0 nM 7.52
CHEMBL351772 IC50 = 37.0 nM 7.43
CHEMBL160287 IC50 = 49.0 nM 7.31
CHEMBL155686 IC50 = 50.0 nM 7.30
CHEMBL160735 IC50 = 60.0 nM 7.22
CHEMBL158548 IC50 = 60.0 nM 7.22
CHEMBL158676 IC50 = 80.0 nM 7.10
CHEMBL347663 IC50 = 150.0 nM 6.82
CHEMBL328126 IC50 = 200.0 nM 6.70
CHEMBL160490 IC50 = 220.0 nM 6.66
CHEMBL158989 IC50 = 230.0 nM 6.64
CHEMBL155694 IC50 = 240.0 nM 6.62
CHEMBL158535 IC50 = 270.0 nM 6.57
CHEMBL346698 IC50 = 340.0 nM 6.47
CHEMBL345834 IC50 = 340.0 nM 6.47
CHEMBL160638 IC50 = 340.0 nM 6.47
CHEMBL160380 IC50 = 400.0 nM 6.40
CHEMBL157529 IC50 = 430.0 nM 6.37
CHEMBL348555 IC50 = 440.0 nM 6.36
CHEMBL160281 IC50 = 460.0 nM 6.34
CHEMBL345863 IC50 = 500.0 nM 6.30
CHEMBL347462 IC50 = 670.0 nM 6.17
CHEMBL160561 IC50 = 700.0 nM 6.16
CHEMBL160372 IC50 = 700.0 nM 6.16
CHEMBL351104 IC50 = 800.0 nM 6.10
CHEMBL158671 IC50 = 2700.0 nM 5.57
CHEMBL348401 IC50 > 1000.0 nM -