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Assay Detail

CHEMBL684416

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

Binding
Inhibition of [125I]glucagon binding towards Glucagon receptor
11
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glucagon receptor (CHEMBL4720)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Topographical amino acid substitution in position 10 of glucagon leads to antagonists/partial agonists with greater binding differences.
Azizeh BY, Shenderovich MD, Trivedi D, Li G, Sturm NS, Hruby VJ.
J Med Chem (1996) 39 : 2449 -2455
PubMed 8691441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.42 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429362 1 8.82
CHEMBL413666 1 8.64
CHEMBL2115191 1 8.39
CHEMBL3037804 1 8.00
CHEMBL2114176 1 7.46
CHEMBL2369127 1 7.13
CHEMBL328942 3 6.92
CHEMBL2114177 1 6.40
CHEMBL2115192 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429362 IC50 = 1.5 nM 8.82
CHEMBL413666 IC50 = 2.3 nM 8.64
CHEMBL2115191 IC50 = 4.1 nM 8.39
CHEMBL3037804 IC50 = 10.0 nM 8.00
CHEMBL2114176 IC50 = 34.5 nM 7.46
CHEMBL2369127 IC50 = 74.0 nM 7.13
CHEMBL328942 IC50 = 120.0 nM 6.92
CHEMBL328942 IC50 = 170.0 nM 6.77
CHEMBL328942 IC50 = 180.0 nM 6.75
CHEMBL2114177 IC50 = 395.0 nM 6.40
CHEMBL2115192 IC50 = 510.0 nM 6.29