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Assay Detail

CHEMBL684418

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Binding
Glucagon receptor binding measured as 50% inhibitory concentration
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glucagon receptor (CHEMBL4720)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

A new approach to search for the bioactive conformation of glucagon: positional cyclization scanning.
Ahn JM, Gitu PM, Medeiros M, Swift JR, Trivedi D, Hruby VJ.
J Med Chem (2001) 44 : 3109 -3116
PubMed 11543679 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.90 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL428460 1 9.70
CHEMBL412488 1 9.62
CHEMBL5314341 GLUCAGON 4.0 1 8.82
CHEMBL439885 1 8.77
CHEMBL267189 1 8.44
CHEMBL263603 1 8.25
CHEMBL437648 1 8.22
CHEMBL414077 1 8.19
CHEMBL442135 1 7.87
CHEMBL409654 1 7.86
CHEMBL414490 1 7.07
CHEMBL441011 1 7.00
CHEMBL437465 1 6.25
CHEMBL410553 1 6.25
CHEMBL269490 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL428460 IC50 = 0.2 nM 9.70
CHEMBL412488 IC50 = 0.24 nM 9.62
CHEMBL5314341 GLUCAGON IC50 = 1.5 nM 8.82
CHEMBL439885 IC50 = 1.7 nM 8.77
CHEMBL267189 IC50 = 3.6 nM 8.44
CHEMBL263603 IC50 = 5.6 nM 8.25
CHEMBL437648 IC50 = 6.0 nM 8.22
CHEMBL414077 IC50 = 6.4 nM 8.19
CHEMBL442135 IC50 = 13.6 nM 7.87
CHEMBL409654 IC50 = 13.7 nM 7.86
CHEMBL414490 IC50 = 84.5 nM 7.07
CHEMBL441011 IC50 = 101.0 nM 7.00
CHEMBL437465 IC50 = 558.0 nM 6.25
CHEMBL410553 IC50 = 562.0 nM 6.25
CHEMBL269490 IC50 = 652.0 nM 6.19