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Assay Detail

CHEMBL995932

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

Binding
Binding affinity to glucagon receptor in rat liver membrane by membrane filter assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glucagon receptor (CHEMBL4720)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Human glucagon receptor antagonists with thiazole cores. A novel series with superior pharmacokinetic properties.
Madsen P, Kodra JT, Behrens C, Nishimura E, Jeppesen CB, Pridal L, Andersen B, Knudsen LB, Valcarce-Aspegren C, Guldbrandt M, Christensen IT, Jørgensen AS, Ynddal L, Brand CL, Bagger MA, Lau J.
J Med Chem (2009) 52 : 2989 -3000
PubMed 19385613 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.63 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL471580 1 5.85
CHEMBL492813 1 5.80
CHEMBL519776 1 5.77
CHEMBL455323 1 5.75
CHEMBL501628 1 5.70
CHEMBL470729 1 5.57
CHEMBL446821 1 5.36
CHEMBL492605 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL471580 IC50 = 1400.0 nM 5.85
CHEMBL492813 IC50 = 1600.0 nM 5.80
CHEMBL519776 IC50 = 1700.0 nM 5.77
CHEMBL455323 IC50 = 1800.0 nM 5.75
CHEMBL501628 IC50 = 2000.0 nM 5.70
CHEMBL470729 IC50 = 2700.0 nM 5.57
CHEMBL446821 IC50 = 4400.0 nM 5.36
CHEMBL492605 IC50 = 5400.0 nM 5.27