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Assay Detail

CHEMBL684125

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Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
34
Total Activities
34
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

Human glucagon receptor antagonists based on alkylidene hydrazides.
Ling A, Plewe M, Gonzalez J, Madsen P, Sams CK, Lau J, Gregor V, Murphy D, Teston K, Kuki A, Shi S, Truesdale L, Kiel D, May J, Lakis J, Anderes K, Iatsimirskaia E, Sidelmann UG, Knudsen LB, Brand CL, Polinsky A.
Bioorg Med Chem Lett (2002) 12 : 663 -666
PubMed 11844695 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 6.33 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL152765 1 7.70
CHEMBL348785 1 7.64
CHEMBL158753 1 7.51
CHEMBL161483 1 7.32
CHEMBL158330 1 7.30
CHEMBL348702 1 7.28
CHEMBL346226 1 7.24
CHEMBL153038 1 7.08
CHEMBL159071 1 6.96
CHEMBL154269 1 6.89
CHEMBL351724 1 6.85
CHEMBL161431 1 6.82
CHEMBL161505 1 6.80
CHEMBL159093 1 6.75
CHEMBL107070 1 6.70
CHEMBL160715 1 6.48
CHEMBL421833 1 6.41
CHEMBL161401 1 6.16
CHEMBL444343 1 6.16
CHEMBL435445 1 6.13
CHEMBL161827 1 6.06
CHEMBL157064 1 6.06
CHEMBL160291 1 6.03
CHEMBL160419 1 5.92
CHEMBL160138 1 5.89
CHEMBL160652 1 5.82
CHEMBL161494 1 5.72
CHEMBL158556 1 5.57
CHEMBL160135 1 5.28
CHEMBL351333 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL152765 IC50 = 20.0 nM 7.70
CHEMBL348785 IC50 = 23.0 nM 7.64
CHEMBL158753 IC50 = 31.0 nM 7.51
CHEMBL161483 IC50 = 48.0 nM 7.32
CHEMBL158330 IC50 = 50.0 nM 7.30
CHEMBL348702 IC50 = 53.0 nM 7.28
CHEMBL346226 IC50 = 58.0 nM 7.24
CHEMBL153038 IC50 = 84.0 nM 7.08
CHEMBL159071 IC50 = 110.0 nM 6.96
CHEMBL154269 IC50 = 130.0 nM 6.89
CHEMBL351724 IC50 = 140.0 nM 6.85
CHEMBL161431 IC50 = 150.0 nM 6.82
CHEMBL161505 IC50 = 160.0 nM 6.80
CHEMBL159093 IC50 = 180.0 nM 6.75
CHEMBL107070 IC50 = 200.0 nM 6.70
CHEMBL160715 IC50 = 330.0 nM 6.48
CHEMBL421833 IC50 = 390.0 nM 6.41
CHEMBL161401 IC50 = 690.0 nM 6.16
CHEMBL444343 IC50 = 690.0 nM 6.16
CHEMBL435445 IC50 = 740.0 nM 6.13
CHEMBL161827 IC50 = 880.0 nM 6.06
CHEMBL157064 IC50 = 870.0 nM 6.06
CHEMBL160291 IC50 = 940.0 nM 6.03
CHEMBL160419 IC50 = 1200.0 nM 5.92
CHEMBL160138 IC50 = 1300.0 nM 5.89
CHEMBL160652 IC50 = 1500.0 nM 5.82
CHEMBL161494 IC50 = 1900.0 nM 5.72
CHEMBL158556 IC50 = 2700.0 nM 5.57
CHEMBL160135 IC50 = 5200.0 nM 5.28
CHEMBL351333 IC50 = 6400.0 nM 5.19
CHEMBL158497 IC50 = 20000.0 nM 4.70
CHEMBL347370 IC50 = 30000.0 nM 4.52
CHEMBL158886 IC50 = 78300.0 nM 4.11
CHEMBL160521 IC50 > 100000.0 nM -