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Assay Detail

CHEMBL5043470

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

Binding
Inhibition of recombinant full length H-RNAase L (1 to 741 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition rate in presence of 2-5A and ATP/MgCl2 by STD-NMR spectroscopy
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

2-5A-dependent ribonuclease (CHEMBL3575)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Small Molecule Inhibitors of RNase L by Fragment-Based Drug Discovery.
Tang J, Dong B, Liu M, Liu S, Niu X, Gaughan C, Asthana A, Zhou H, Xu Z, Zhang G, Silverman RH, Huang H.
J Med Chem (2022) 65 : 1445 -1457
PubMed 34841869 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.00 5.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL251254 HYPEROSIDE 1 5.79
CHEMBL164 MYRICETIN 1 3.58
CHEMBL459008 BUTYLPARABEN -1.0 1 2.62
CHEMBL487417 VITEXIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL251254 HYPEROSIDE IC50 = 1630.0 nM 5.79
CHEMBL164 MYRICETIN IC50 = 264000.0 nM 3.58
CHEMBL459008 BUTYLPARABEN IC50 = 2400000.0 nM 2.62
CHEMBL487417 VITEXIN IC50 = 190000.0 nM -