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Assay Detail

CHEMBL5041858

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

Binding
Inhibition of human GAA using 4-methylumbelliferyl-alpha-D-glucopyranoside as substrate preincubated for 45 min followed by substrate addition and measured after 30 min by fluorescence spectrophotometer analysis
17
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Lysosomal alpha-glucosidase (CHEMBL2608)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-<i>C</i>-Branched Deoxynojirimycin: Strategy for Designing a 1-Deoxynojirimycin-Based Pharmacological Chaperone with a Nanomolar Affinity for Pompe Disease.
Kato A, Nakagome I, Kanekiyo U, Lu TT, Li YX, Yoshimura K, Kishida M, Shinzawa K, Yoshida T, Tanaka N, Jia YM, Nash RJ, Fleet GWJ, Yu CY.
J Med Chem (2022) 65 : 2329 -2341
PubMed 35072486 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.82 8.33
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5028005 1 8.33
CHEMBL5028265 1 8.21
CHEMBL5029066 1 7.72
CHEMBL5027974 1 7.43
CHEMBL307429 DUVOGLUSTAT 2.0 1 7.23
CHEMBL5028138 1 7.23
CHEMBL75971 1 7.23
CHEMBL1651551 1 7.02
CHEMBL1651550 1 6.89
CHEMBL1029 MIGLUSTAT 4.0 1 6.70
CHEMBL5080975 1 6.68
CHEMBL1651549 1 6.68
CHEMBL5080744 1 6.44
CHEMBL5028105 1 5.60
CHEMBL5028084 1 5.22
CHEMBL5028072 1 4.43
CHEMBL175901 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5028005 Ki = 4.7 nM 8.33
CHEMBL5028265 Ki = 6.1 nM 8.21
CHEMBL5029066 Ki = 19.0 nM 7.72
CHEMBL5027974 Ki = 37.0 nM 7.43
CHEMBL307429 DUVOGLUSTAT Ki = 59.0 nM 7.23
CHEMBL5028138 Ki = 59.0 nM 7.23
CHEMBL75971 Ki = 59.0 nM 7.23
CHEMBL1651551 Ki = 95.0 nM 7.02
CHEMBL1651550 Ki = 130.0 nM 6.89
CHEMBL1029 MIGLUSTAT Ki = 200.0 nM 6.70
CHEMBL5080975 Ki = 210.0 nM 6.68
CHEMBL1651549 Ki = 210.0 nM 6.68
CHEMBL5080744 Ki = 360.0 nM 6.44
CHEMBL5028105 Ki = 2500.0 nM 5.60
CHEMBL5028084 Ki = 6000.0 nM 5.22
CHEMBL5028072 Ki = 37000.0 nM 4.43
CHEMBL175901 Inhibition - % -