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Assay Detail

CHEMBL3384690

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

Binding
Inhibition of GBA1 (unknown origin) using beta-D-[1-14C]glucocerebroside assessed as 4-methylumbelliferrone by fluorimetry
ChEMBL ↗
77
Total Activities
77
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Lysosomal acid glucosylceramidase (CHEMBL2179) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification and development of biphenyl substituted iminosugars as improved dual glucosylceramide synthase/neutral glucosylceramidase inhibitors.
Ghisaidoobe AT, van den Berg RJ, Butt SS, Strijland A, Donker-Koopman WE, Scheij S, van den Nieuwendijk AM, Koomen GJ, van Loevezijn A, Leemhuis M, Wennekes T, van der Stelt M, van der Marel GA, van Boeckel CA, Aerts JM, Overkleeft HS.
J Med Chem (2014) 57 : 9096 -9104
PubMed 25250725 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 77 5.82 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3354017 — — 1 7.22
CHEMBL3354041 — — 1 7.16
CHEMBL574645 — — 1 7.00
CHEMBL3354627 — — 1 7.00
CHEMBL3354620 — — 1 6.90
CHEMBL3354016 — — 1 6.70
CHEMBL3354625 — — 1 6.70
CHEMBL3354626 — — 1 6.70
CHEMBL1088158 — — 1 6.70
CHEMBL3354049 — — 1 6.60
CHEMBL3354624 — — 1 6.60
CHEMBL3354040 — — 1 6.60
CHEMBL3354039 — — 1 6.60
CHEMBL3354055 — — 1 6.60
CHEMBL3354623 — — 1 6.52
CHEMBL3354063 — — 1 6.52
CHEMBL3354621 — — 1 6.52
CHEMBL3354021 — — 1 6.52
CHEMBL3354045 — — 1 6.46
CHEMBL3354019 — — 1 6.40
CHEMBL3354048 — — 1 6.40
CHEMBL3354025 — — 1 6.40
CHEMBL3354051 — — 1 6.30
CHEMBL3354015 — — 1 6.30
CHEMBL3354054 — — 1 6.30
CHEMBL3354024 — — 1 6.30
CHEMBL2170199 — — 1 6.30
CHEMBL3354018 — — 1 6.30
CHEMBL3354044 — — 1 6.22
CHEMBL3354047 — — 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3354017 — IC50 = 60.0 nM 7.22
CHEMBL3354041 — IC50 = 70.0 nM 7.16
CHEMBL3354627 — IC50 = 100.0 nM 7.00
CHEMBL574645 — IC50 = 100.0 nM 7.00
CHEMBL3354620 — IC50 = 125.0 nM 6.90
CHEMBL3354016 — IC50 = 200.0 nM 6.70
CHEMBL3354625 — IC50 = 200.0 nM 6.70
CHEMBL3354626 — IC50 = 200.0 nM 6.70
CHEMBL1088158 — IC50 = 200.0 nM 6.70
CHEMBL3354055 — IC50 = 250.0 nM 6.60
CHEMBL3354039 — IC50 = 250.0 nM 6.60
CHEMBL3354040 — IC50 = 250.0 nM 6.60
CHEMBL3354624 — IC50 = 250.0 nM 6.60
CHEMBL3354049 — IC50 = 250.0 nM 6.60
CHEMBL3354021 — IC50 = 300.0 nM 6.52
CHEMBL3354623 — IC50 = 300.0 nM 6.52
CHEMBL3354621 — IC50 = 300.0 nM 6.52
CHEMBL3354063 — IC50 = 300.0 nM 6.52
CHEMBL3354045 — IC50 = 350.0 nM 6.46
CHEMBL3354019 — IC50 = 400.0 nM 6.40
CHEMBL3354048 — IC50 = 400.0 nM 6.40
CHEMBL3354025 — IC50 = 400.0 nM 6.40
CHEMBL3354018 — IC50 = 500.0 nM 6.30
CHEMBL2170199 — IC50 = 500.0 nM 6.30
CHEMBL3354024 — IC50 = 500.0 nM 6.30
CHEMBL3354015 — IC50 = 500.0 nM 6.30
CHEMBL3354051 — IC50 = 500.0 nM 6.30
CHEMBL3354054 — IC50 = 500.0 nM 6.30
CHEMBL3354044 — IC50 = 600.0 nM 6.22
CHEMBL3354047 — IC50 = 600.0 nM 6.22
CHEMBL3354050 — IC50 = 600.0 nM 6.22
CHEMBL3354046 — IC50 = 700.0 nM 6.16
CHEMBL3354053 — IC50 = 800.0 nM 6.10
CHEMBL3354052 — IC50 = 800.0 nM 6.10
CHEMBL3354022 — IC50 = 1000.0 nM 6.00
CHEMBL3354062 — IC50 = 1250.0 nM 5.90
CHEMBL3354014 — IC50 = 1500.0 nM 5.82
CHEMBL3354064 — IC50 = 1500.0 nM 5.82
CHEMBL3354057 — IC50 = 2000.0 nM 5.70
CHEMBL3354060 — IC50 = 2000.0 nM 5.70
CHEMBL1086996 — IC50 = 2000.0 nM 5.70
CHEMBL3354042 — IC50 = 2500.0 nM 5.60
CHEMBL3354043 — IC50 = 2500.0 nM 5.60
CHEMBL3354020 — IC50 = 2500.0 nM 5.60
CHEMBL3354056 — IC50 = 3000.0 nM 5.52
CHEMBL3354058 — IC50 = 3000.0 nM 5.52
CHEMBL3354061 — IC50 = 3000.0 nM 5.52
CHEMBL3354634 — IC50 = 5000.0 nM 5.30
CHEMBL3354029 — IC50 = 5000.0 nM 5.30
CHEMBL3354637 NIZUBAGLUSTAT IC50 = 6000.0 nM 5.22