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Assay Detail

CHEMBL684123

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

Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
31
Total Activities
31
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 (CHEMBL1985)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted imidazoles as glucagon receptor antagonists.
Chang LL, Sidler KL, Cascieri MA, de Laszlo S, Koch G, Li B, MacCoss M, Mantlo N, O'Keefe S, Pang M, Rolando A, Hagmann WK.
Bioorg Med Chem Lett (2001) 11 : 2549 -2553
PubMed 11549467 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.45 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86086 1 8.19
CHEMBL314701 1 8.19
CHEMBL315828 1 8.07
CHEMBL85807 1 7.89
CHEMBL316361 1 7.89
CHEMBL315613 1 7.57
CHEMBL87611 1 7.21
CHEMBL84840 1 7.13
CHEMBL315311 1 6.89
CHEMBL315800 1 6.89
CHEMBL85102 1 6.85
CHEMBL85009 1 6.72
CHEMBL87588 1 6.57
CHEMBL314238 1 6.40
CHEMBL17370 1 6.31
CHEMBL314181 1 6.29
CHEMBL86250 1 6.16
CHEMBL312928 1 6.11
CHEMBL84759 1 5.96
CHEMBL420232 1 5.89
CHEMBL85534 1 5.85
CHEMBL314652 1 5.82
CHEMBL17736 1 5.70
CHEMBL316264 1 5.70
CHEMBL84917 1 5.66
CHEMBL312825 1 5.55
CHEMBL17396 1 5.10
CHEMBL17722 1 5.06
CHEMBL85741 1 5.00
CHEMBL276063 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86086 IC50 = 6.5 nM 8.19
CHEMBL314701 IC50 = 6.5 nM 8.19
CHEMBL315828 IC50 = 8.5 nM 8.07
CHEMBL85807 IC50 = 13.0 nM 7.89
CHEMBL316361 IC50 = 13.0 nM 7.89
CHEMBL315613 IC50 = 27.0 nM 7.57
CHEMBL87611 IC50 = 61.0 nM 7.21
CHEMBL84840 IC50 = 74.0 nM 7.13
CHEMBL315311 IC50 = 130.0 nM 6.89
CHEMBL315800 IC50 = 130.0 nM 6.89
CHEMBL85102 IC50 = 140.0 nM 6.85
CHEMBL85009 IC50 = 190.0 nM 6.72
CHEMBL87588 IC50 = 270.0 nM 6.57
CHEMBL314238 IC50 = 400.0 nM 6.40
CHEMBL17370 IC50 = 490.0 nM 6.31
CHEMBL314181 IC50 = 510.0 nM 6.29
CHEMBL86250 IC50 = 700.0 nM 6.16
CHEMBL312928 IC50 = 782.0 nM 6.11
CHEMBL84759 IC50 = 1100.0 nM 5.96
CHEMBL420232 IC50 = 1300.0 nM 5.89
CHEMBL85534 IC50 = 1400.0 nM 5.85
CHEMBL314652 IC50 = 1500.0 nM 5.82
CHEMBL17736 IC50 = 2000.0 nM 5.70
CHEMBL316264 IC50 = 2000.0 nM 5.70
CHEMBL84917 IC50 = 2200.0 nM 5.66
CHEMBL312825 IC50 = 2800.0 nM 5.55
CHEMBL17396 IC50 = 8000.0 nM 5.10
CHEMBL17722 IC50 = 8700.0 nM 5.06
CHEMBL85741 IC50 = 10000.0 nM 5.00
CHEMBL276063 IC50 = 13000.0 nM 4.89
CHEMBL416169 IC50 > 20000.0 nM -