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Assay Detail

CHEMBL2184153

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

Binding
Inhibition of rat intestinal sucrase using sucrose as substrate
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sucrase-isomaltase, intestinal (CHEMBL3114)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

α-1-C-butyl-1,4-dideoxy-1,4-imino-l-arabinitol as a second-generation iminosugar-based oral α-glucosidase inhibitor for improving postprandial hyperglycemia.
Kato A, Hayashi E, Miyauchi S, Adachi I, Imahori T, Natori Y, Yoshimura Y, Nash RJ, Shimaoka H, Nakagome I, Koseki J, Hirono S, Takahata H.
J Med Chem (2012) 55 : 10347 -10362
PubMed 23106358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.97 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1641739 1 7.50
CHEMBL1641742 1 6.96
CHEMBL1641741 1 6.72
CHEMBL307429 DUVOGLUSTAT 2.0 1 6.68
CHEMBL2177691 1 6.62
CHEMBL1641743 1 6.62
CHEMBL1645621 1 6.58
CHEMBL2177690 1 6.51
CHEMBL476960 VOGLIBOSE 4.0 1 6.43
CHEMBL1641744 1 6.35
CHEMBL405957 1 6.21
CHEMBL2177689 1 6.18
CHEMBL1645620 1 6.17
CHEMBL2177692 1 6.17
CHEMBL1561 MIGLITOL 4.0 1 6.00
CHEMBL406973 1 6.00
CHEMBL1641746 1 5.85
CHEMBL2177695 1 5.82
CHEMBL1641747 1 5.77
CHEMBL1090539 1 5.62
CHEMBL404271 ACARBOSE 4.0 1 5.54
CHEMBL1088892 1 5.42
CHEMBL2177693 1 5.24
CHEMBL1641749 1 5.06
CHEMBL1641748 1 4.89
CHEMBL1029 MIGLUSTAT 4.0 1 4.24
CHEMBL2177696 1 4.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1641739 IC50 = 32.0 nM 7.50
CHEMBL1641742 IC50 = 110.0 nM 6.96
CHEMBL1641741 IC50 = 190.0 nM 6.72
CHEMBL307429 DUVOGLUSTAT IC50 = 210.0 nM 6.68
CHEMBL2177691 IC50 = 240.0 nM 6.62
CHEMBL1641743 IC50 = 240.0 nM 6.62
CHEMBL1645621 IC50 = 260.0 nM 6.58
CHEMBL2177690 IC50 = 310.0 nM 6.51
CHEMBL476960 VOGLIBOSE IC50 = 370.0 nM 6.43
CHEMBL1641744 IC50 = 450.0 nM 6.35
CHEMBL405957 IC50 = 620.0 nM 6.21
CHEMBL2177689 IC50 = 660.0 nM 6.18
CHEMBL1645620 IC50 = 680.0 nM 6.17
CHEMBL2177692 IC50 = 680.0 nM 6.17
CHEMBL1561 MIGLITOL IC50 = 1000.0 nM 6.00
CHEMBL406973 IC50 = 1000.0 nM 6.00
CHEMBL1641746 IC50 = 1400.0 nM 5.85
CHEMBL2177695 IC50 = 1500.0 nM 5.82
CHEMBL1641747 IC50 = 1700.0 nM 5.77
CHEMBL1090539 IC50 = 2400.0 nM 5.62
CHEMBL404271 ACARBOSE IC50 = 2900.0 nM 5.54
CHEMBL1088892 IC50 = 3800.0 nM 5.42
CHEMBL2177693 IC50 = 5700.0 nM 5.24
CHEMBL1641749 IC50 = 8800.0 nM 5.06
CHEMBL1641748 IC50 = 13000.0 nM 4.89
CHEMBL1029 MIGLUSTAT IC50 = 58000.0 nM 4.24
CHEMBL2177696 IC50 = 73000.0 nM 4.14