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Assay Detail

CHEMBL684119

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Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL ↗
47
Total Activities
47
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 (CHEMBL1985) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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 47 7.06 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL347663 — — 1 8.52
CHEMBL160287 — — 1 8.40
CHEMBL155686 — — 1 8.22
CHEMBL351772 — — 1 8.15
CHEMBL156458 — — 1 8.10
CHEMBL158676 — — 1 8.00
CHEMBL158535 — — 1 7.77
CHEMBL348555 — — 1 7.70
CHEMBL436022 — — 1 7.58
CHEMBL160561 — — 1 7.52
CHEMBL346698 — — 1 7.40
CHEMBL347462 — — 1 7.40
CHEMBL160638 — — 1 7.40
CHEMBL345834 — — 1 7.40
CHEMBL160281 — — 1 7.40
CHEMBL160550 — — 1 7.22
CHEMBL351104 — — 1 7.22
CHEMBL158477 — — 1 7.22
CHEMBL160380 — — 1 7.16
CHEMBL328126 — — 1 7.10
CHEMBL157529 — — 1 7.05
CHEMBL348401 — — 1 7.05
CHEMBL345863 — — 1 7.05
CHEMBL160735 — — 1 7.00
CHEMBL155694 — — 1 7.00
CHEMBL160372 — — 1 6.85
CHEMBL158989 — — 1 6.85
CHEMBL159198 — — 1 6.85
CHEMBL350255 — — 1 6.82
CHEMBL160490 — — 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL347663 — IC50 = 3.0 nM 8.52
CHEMBL160287 — IC50 = 4.0 nM 8.40
CHEMBL155686 — IC50 = 6.0 nM 8.22
CHEMBL351772 — IC50 = 7.0 nM 8.15
CHEMBL156458 — IC50 = 8.0 nM 8.10
CHEMBL158676 — IC50 = 10.0 nM 8.00
CHEMBL158535 — IC50 = 17.0 nM 7.77
CHEMBL348555 — IC50 = 20.0 nM 7.70
CHEMBL436022 — IC50 = 26.0 nM 7.58
CHEMBL160561 — IC50 = 30.0 nM 7.52
CHEMBL345834 — IC50 = 40.0 nM 7.40
CHEMBL160281 — IC50 = 40.0 nM 7.40
CHEMBL160638 — IC50 = 40.0 nM 7.40
CHEMBL347462 — IC50 = 40.0 nM 7.40
CHEMBL346698 — IC50 = 40.0 nM 7.40
CHEMBL160550 — IC50 = 60.0 nM 7.22
CHEMBL158477 — IC50 = 60.0 nM 7.22
CHEMBL351104 — IC50 = 60.0 nM 7.22
CHEMBL160380 — IC50 = 70.0 nM 7.16
CHEMBL328126 — IC50 = 80.0 nM 7.10
CHEMBL157529 — IC50 = 90.0 nM 7.05
CHEMBL348401 — IC50 = 90.0 nM 7.05
CHEMBL345863 — IC50 = 90.0 nM 7.05
CHEMBL160735 — IC50 = 100.0 nM 7.00
CHEMBL155694 — IC50 = 100.0 nM 7.00
CHEMBL160372 — IC50 = 140.0 nM 6.85
CHEMBL158989 — IC50 = 140.0 nM 6.85
CHEMBL159198 — IC50 = 140.0 nM 6.85
CHEMBL350255 — IC50 = 150.0 nM 6.82
CHEMBL160490 — IC50 = 190.0 nM 6.72
CHEMBL160289 — IC50 = 250.0 nM 6.60
CHEMBL156207 — IC50 = 290.0 nM 6.54
CHEMBL160525 — IC50 = 360.0 nM 6.44
CHEMBL160238 — IC50 = 370.0 nM 6.43
CHEMBL158671 — IC50 = 390.0 nM 6.41
CHEMBL17370 — IC50 = 490.0 nM 6.31
CHEMBL160401 — IC50 = 590.0 nM 6.23
CHEMBL160690 — IC50 = 850.0 nM 6.07
CHEMBL350237 — IC50 = 850.0 nM 6.07
CHEMBL155687 — IC50 = 1100.0 nM 5.96
CHEMBL159163 — IC50 = 1400.0 nM 5.85
CHEMBL158548 — IC50 = 3032.0 nM 5.52
CHEMBL423781 — IC50 > 3000.0 nM -
CHEMBL156566 — IC50 > 3000.0 nM -
CHEMBL156961 — IC50 > 3000.0 nM -
CHEMBL160627 — IC50 > 3000.0 nM -
CHEMBL160314 — IC50 > 3000.0 nM -