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Assay Detail

CHEMBL4671907

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Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
11
Total Activities
11
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

Automated Design of Macrocycles for Therapeutic Applications: From Small Molecules to Peptides and Proteins.
Sindhikara D,Wagner M,Gkeka P,Güssregen S,Tiwari G,Hessler G,Yapici E,Li Z,Evers A
J Med Chem (2020) 63 : 12100 -12115
PubMed 33017535 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 9.83 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4761047 1 10.89
CHEMBL4098061 1 10.54
CHEMBL4755815 1 10.27
CHEMBL4751319 1 10.22
CHEMBL4745985 1 9.92
CHEMBL4745235 1 9.91
CHEMBL4757675 1 9.43
CHEMBL4762061 1 9.24
CHEMBL4756489 1 8.07
CHEMBL4758415 1 -
CHEMBL4741348 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4761047 EC50 = 0.0129 nM 10.89
CHEMBL4098061 EC50 = 0.0286 nM 10.54
CHEMBL4755815 EC50 = 0.0542 nM 10.27
CHEMBL4751319 EC50 = 0.0596 nM 10.22
CHEMBL4745985 EC50 = 0.119 nM 9.92
CHEMBL4745235 EC50 = 0.122 nM 9.91
CHEMBL4757675 EC50 = 0.369 nM 9.43
CHEMBL4762061 EC50 = 0.578 nM 9.24
CHEMBL4756489 EC50 = 8.43 nM 8.07
CHEMBL4758415 EC50 = 0.0078 nM -
CHEMBL4741348 EC50 = 0.0023 nM -