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Assay Detail

CHEMBL5534280

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Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as cAMP level measured after 60 mins by HTRF based assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glucagon receptor (CHEMBL1985)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Novel Glucagon-like Peptide-1 (GLP-1) Analogue from Bullfrog and Investigation of Its Potential for Designing GLP-1-Based Multiagonists.
Jiang N, Su D, Chen, Huang S, Tang C, Jing L, Yang C, Zhou Z, Yan Z, Han J.
J Med Chem (2024) 67 : 180 -198
PubMed 38117235 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 9.24 10.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5573719 1 10.57
CHEMBL5573706 1 10.28
CHEMBL5314341 GLUCAGON 4.0 1 10.04
CHEMBL5575146 1 9.89
CHEMBL5584018 1 9.82
CHEMBL4297630 COTADUTIDE 2.0 1 9.77
CHEMBL5584095 1 9.74
CHEMBL5572101 1 9.72
CHEMBL5590721 1 9.64
CHEMBL5575497 1 9.29
CHEMBL5579680 1 9.28
CHEMBL5573864 1 9.28
CHEMBL5570478 1 9.21
CHEMBL5563008 1 9.21
CHEMBL5574566 1 9.18
CHEMBL5593907 1 9.10
CHEMBL5571917 1 9.07
CHEMBL5572113 1 9.04
CHEMBL5590909 1 8.92
CHEMBL5594986 1 8.85
CHEMBL5569213 1 8.74
CHEMBL5575699 1 8.74
CHEMBL5570630 1 8.74
CHEMBL5570738 1 8.59
CHEMBL5571645 1 8.59
CHEMBL5575723 1 8.51
CHEMBL5565062 1 8.51
CHEMBL5570925 1 8.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5573719 EC50 = 0.027 nM 10.57
CHEMBL5573706 EC50 = 0.052 nM 10.28
CHEMBL5314341 GLUCAGON EC50 = 0.092 nM 10.04
CHEMBL5575146 EC50 = 0.13 nM 9.89
CHEMBL5584018 EC50 = 0.15 nM 9.82
CHEMBL4297630 COTADUTIDE EC50 = 0.17 nM 9.77
CHEMBL5584095 EC50 = 0.18 nM 9.74
CHEMBL5572101 EC50 = 0.19 nM 9.72
CHEMBL5590721 EC50 = 0.23 nM 9.64
CHEMBL5575497 EC50 = 0.51 nM 9.29
CHEMBL5579680 EC50 = 0.53 nM 9.28
CHEMBL5573864 EC50 = 0.53 nM 9.28
CHEMBL5570478 EC50 = 0.62 nM 9.21
CHEMBL5563008 EC50 = 0.61 nM 9.21
CHEMBL5574566 EC50 = 0.66 nM 9.18
CHEMBL5593907 EC50 = 0.8 nM 9.10
CHEMBL5571917 EC50 = 0.85 nM 9.07
CHEMBL5572113 EC50 = 0.91 nM 9.04
CHEMBL5590909 EC50 = 1.2 nM 8.92
CHEMBL5594986 EC50 = 1.4 nM 8.85
CHEMBL5569213 EC50 = 1.8 nM 8.74
CHEMBL5575699 EC50 = 1.8 nM 8.74
CHEMBL5570630 EC50 = 1.8 nM 8.74
CHEMBL5570738 EC50 = 2.6 nM 8.59
CHEMBL5571645 EC50 = 2.6 nM 8.59
CHEMBL5575723 EC50 = 3.1 nM 8.51
CHEMBL5565062 EC50 = 3.1 nM 8.51
CHEMBL5570925 EC50 = 3.5 nM 8.46