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Assay Detail

CHEMBL684124

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

Binding
Affinity for human glucagon receptor in presence of Mg2+
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glucagon receptor (CHEMBL1985)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted imidazoles as glucagon receptor antagonists.
Chang LL, Sidler KL, Cascieri MA, de Laszlo S, Koch G, Li B, MacCoss M, Mantlo N, O'Keefe S, Pang M, Rolando A, Hagmann WK.
Bioorg Med Chem Lett (2001) 11 : 2549 -2553
PubMed 11549467 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.31 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86086 1 7.28
CHEMBL315828 1 6.96
CHEMBL315613 1 6.96
CHEMBL316361 1 6.92
CHEMBL85807 1 6.82
CHEMBL84840 1 6.82
CHEMBL314701 1 6.54
CHEMBL315311 1 6.12
CHEMBL85009 1 5.66
CHEMBL87588 1 5.54
CHEMBL314238 1 5.50
CHEMBL315800 1 5.47
CHEMBL85102 1 5.42
CHEMBL87611 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86086 IC50 = 53.0 nM 7.28
CHEMBL315828 IC50 = 110.0 nM 6.96
CHEMBL315613 IC50 = 110.0 nM 6.96
CHEMBL316361 IC50 = 120.0 nM 6.92
CHEMBL85807 IC50 = 150.0 nM 6.82
CHEMBL84840 IC50 = 150.0 nM 6.82
CHEMBL314701 IC50 = 290.0 nM 6.54
CHEMBL315311 IC50 = 750.0 nM 6.12
CHEMBL85009 IC50 = 2200.0 nM 5.66
CHEMBL87588 IC50 = 2900.0 nM 5.54
CHEMBL314238 IC50 = 3200.0 nM 5.50
CHEMBL315800 IC50 = 3400.0 nM 5.47
CHEMBL85102 IC50 = 3800.0 nM 5.42
CHEMBL87611 IC50 > 3000.0 nM -