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Assay Detail

CHEMBL4729681

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Binding
Competitive inhibition of recombinant human SARM1 TIR domain (561 to 724 residues) expressed in Escherichia coli C43 (DE3) cells lysates assessed as EADPR formation using ENAD as substrate preincubated for 20 mins followed by ENAD addition and measured at 15 sec interval for 1 hr
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of the first noncompetitive SARM1 inhibitors.
Loring HS,Parelkar SS,Mondal S,Thompson PR
Bioorg Med Chem (2020) 28 : 115644 -115644
PubMed 32828421 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 4.16 4.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1201022 PHENAZOPYRIDINE HYDROCHLORIDE 4.0 1 4.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1201022 PHENAZOPYRIDINE HYDROCHLORIDE Ki = 70000.0 nM 4.16