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Assay Detail

CHEMBL680803

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

Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glucagon receptor (CHEMBL1985)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and structure-activity relationship of the first non-peptide competitive human glucagon receptor antagonists.
Madsen P, Knudsen LB, Wiberg FC, Carr RD.
J Med Chem (1998) 41 : 5150 -5157
PubMed 9857085 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 4.58 5.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL358886 1 5.27
CHEMBL356726 1 5.04
CHEMBL150172 1 4.92
CHEMBL265552 1 4.80
CHEMBL424134 1 4.75
CHEMBL146839 1 4.70
CHEMBL146683 1 4.39
CHEMBL359176 1 4.38
CHEMBL147331 1 4.26
CHEMBL358546 1 4.26
CHEMBL148905 1 4.14
CHEMBL149138 1 4.02
CHEMBL147173 1 -
CHEMBL149123 1 -
CHEMBL148045 1 -
CHEMBL146181 1 -
CHEMBL146374 1 -
CHEMBL146545 1 -
CHEMBL147177 1 -
CHEMBL147345 1 -
CHEMBL148750 1 -
CHEMBL358371 1 -
CHEMBL2112026 1 -
CHEMBL359177 1 -
CHEMBL342535 1 -
CHEMBL347544 1 -
CHEMBL357318 1 -
CHEMBL146399 1 -
CHEMBL147679 1 -
CHEMBL147634 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL358886 Ki = 5400.0 nM 5.27
CHEMBL356726 Ki = 9200.0 nM 5.04
CHEMBL150172 Ki = 12000.0 nM 4.92
CHEMBL265552 Ki = 16000.0 nM 4.80
CHEMBL424134 Ki = 18000.0 nM 4.75
CHEMBL146839 Ki = 20000.0 nM 4.70
CHEMBL146683 Ki = 41000.0 nM 4.39
CHEMBL359176 Ki = 42000.0 nM 4.38
CHEMBL147331 Ki = 55000.0 nM 4.26
CHEMBL358546 Ki = 55000.0 nM 4.26
CHEMBL148905 Ki = 73000.0 nM 4.14
CHEMBL149138 Ki = 95000.0 nM 4.02
CHEMBL149067 Ki > 500000.0 nM -
CHEMBL148645 Ki = 250000.0 nM -
CHEMBL147173 Ki = 380000.0 nM -
CHEMBL149123 Ki > 60000.0 nM -
CHEMBL148045 Ki = 200000.0 nM -
CHEMBL146181 Ki > 500000.0 nM -
CHEMBL146374 Ki > 500000.0 nM -
CHEMBL146545 Ki > 500000.0 nM -
CHEMBL147177 Ki > 500000.0 nM -
CHEMBL147345 Ki > 500000.0 nM -
CHEMBL148750 Ki > 500000.0 nM -
CHEMBL358371 Ki > 500000.0 nM -
CHEMBL2112026 Ki > 500000.0 nM -
CHEMBL359177 Ki = 180000.0 nM -
CHEMBL342535 Ki > 500000.0 nM -
CHEMBL347544 Ki > 500000.0 nM -
CHEMBL357318 Ki > 500000.0 nM -
CHEMBL146399 Ki > 500000.0 nM -
CHEMBL147679 Ki > 500000.0 nM -
CHEMBL147634 Ki = 160000.0 nM -