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Assay Detail

CHEMBL4422591

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

Binding
Inhibition of StrepTag-tagged human SARM1 TIR (561 to 724 residues) expressed in NRK1-HEK293T cells assessed as reduction in NADase activity by measuring maximal ADPR conversion pre-incubated up to 120 mins before NAD+ addition and further incubated for 60 mins by HPLC analysis
4
Total Activities
4
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

NAD(+) hydrolase SARM1 (CHEMBL4523350)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

INHIBITORS OF SARM1 NADase ACTIVITY AND USES THEREOF
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.15 5.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1219 RABEPRAZOLE 4.0 1 5.50
CHEMBL1201863 DEXLANSOPRAZOLE 4.0 1 5.48
CHEMBL1475252 TENATOPRAZOLE 2.0 1 5.06
CHEMBL4458111 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1219 RABEPRAZOLE IC50 = 3200.0 nM 5.50
CHEMBL1201863 DEXLANSOPRAZOLE IC50 = 3300.0 nM 5.48
CHEMBL1475252 TENATOPRAZOLE IC50 = 8700.0 nM 5.06
CHEMBL4458111 IC50 = 28300.0 nM 4.55