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Assay Detail

CHEMBL996768

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

Binding
Binding affinity to glucagon receptor in pig liver membrane by membrane filter assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Tissue Liver
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 5 5.31 5.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492813 1 5.48
CHEMBL471580 1 5.40
CHEMBL501628 1 5.28
CHEMBL519776 1 5.24
CHEMBL470729 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492813 IC50 = 3300.0 nM 5.48
CHEMBL471580 IC50 = 4000.0 nM 5.40
CHEMBL501628 IC50 = 5300.0 nM 5.28
CHEMBL519776 IC50 = 5700.0 nM 5.24
CHEMBL470729 IC50 = 7000.0 nM 5.16