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Assay Detail

CHEMBL5346703

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

Binding
Inhibition of N-terminal hexa-histidine tagged recombinant SARS-CoV-2 nsp14 RNA cap N7-methyltransferase activity expressed in Escherichia coli C2566 using GpppAC4 synthetic RNA and [3H]-SAM as substrate incubated for 30 mins by filter binding assay based liquid scintillation counter analysis
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Severe acute respiratory syndrome coronavirus 2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Replicase polyprotein 1ab (CHEMBL4523582)
Type SINGLE PROTEIN
Organism Severe acute respiratory syndrome coronavirus 2

Publication

<i>N</i>-Arylsulfonamide-based adenosine analogues to target RNA cap <i>N</i>7-methyltransferase nsp14 of SARS-CoV-2.
Ahmed-Belkacem R, Troussier J, Delpal A, Canard B, Vasseur JJ, Decroly E, Debart F.
RSC Med Chem (2024) 15 : 839 -847
PubMed 38516599 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 5.20 6.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1214186 SINEFUNGIN 2.0 1 6.56
CHEMBL5411147 1 6.05
CHEMBL5421616 1 6.05
CHEMBL5418419 1 5.69
CHEMBL5406405 1 5.66
CHEMBL5437799 1 5.34
CHEMBL5423053 1 5.33
CHEMBL5403276 1 5.14
CHEMBL5409052 1 4.81
CHEMBL5420170 1 4.63
CHEMBL5439086 1 4.56
CHEMBL5438646 1 4.42
CHEMBL5410336 1 4.31
CHEMBL5394078 1 4.28
CHEMBL5429136 1 -
CHEMBL5412699 1 -
CHEMBL5439737 1 -
CHEMBL5437349 1 -
CHEMBL5396255 1 -
CHEMBL5397749 1 -
CHEMBL5419451 1 -
CHEMBL5422414 1 -
CHEMBL5429277 1 -
CHEMBL5434990 1 -
CHEMBL5426066 1 -
CHEMBL5430883 1 -
CHEMBL5402533 1 -
CHEMBL5432305 1 -
CHEMBL5412863 1 -
CHEMBL5428845 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1214186 SINEFUNGIN IC50 = 278.0 nM 6.56
CHEMBL5411147 IC50 = 900.0 nM 6.05
CHEMBL5421616 IC50 = 900.0 nM 6.05
CHEMBL5418419 IC50 = 2040.0 nM 5.69
CHEMBL5406405 IC50 = 2200.0 nM 5.66
CHEMBL5437799 IC50 = 4600.0 nM 5.34
CHEMBL5423053 IC50 = 4700.0 nM 5.33
CHEMBL5403276 IC50 = 7300.0 nM 5.14
CHEMBL5409052 IC50 = 15600.0 nM 4.81
CHEMBL5420170 IC50 = 23300.0 nM 4.63
CHEMBL5439086 IC50 = 27400.0 nM 4.56
CHEMBL5438646 IC50 = 38400.0 nM 4.42
CHEMBL5410336 IC50 = 49000.0 nM 4.31
CHEMBL5394078 IC50 = 52400.0 nM 4.28
CHEMBL5400552 IC50 - -
CHEMBL5401955 IC50 - -
CHEMBL5429136 IC50 - -
CHEMBL5412699 IC50 - -
CHEMBL5439737 IC50 - -
CHEMBL5437349 IC50 - -
CHEMBL5396255 IC50 - -
CHEMBL5397749 IC50 - -
CHEMBL5419451 IC50 - -
CHEMBL5422414 IC50 - -
CHEMBL5429277 IC50 - -
CHEMBL5434990 IC50 - -
CHEMBL5426066 IC50 - -
CHEMBL5430883 IC50 - -
CHEMBL5402533 IC50 - -
CHEMBL5432305 IC50 - -
CHEMBL5412863 IC50 - -
CHEMBL5428845 IC50 - -