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Assay Detail

CHEMBL5318195

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Binding
Inhibition of N-terminal 6 His-MBP tagged human PARP6 expressed in Sf21 cells incubated for 18 hrs in presence of NAD+
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein mono-ADP-ribosyltransferase PARP6 (CHEMBL2380187)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

[1,2,4]Triazolo[3,4-<i>b</i>]benzothiazole Scaffold as Versatile Nicotinamide Mimic Allowing Nanomolar Inhibition of Different PARP Enzymes.
Murthy S, Nizi MG, Maksimainen MM, Massari S, Alaviuhkola J, Lippok BE, Vagaggini C, Sowa ST, Galera-Prat A, Ashok Y, Venkannagari H, Prunskaite-Hyyryläinen R, Dreassi E, Lüscher B, Korn P, Tabarrini O, Lehtiö L.
J Med Chem (2023) 66 : 1301 -1320
PubMed 36598465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.11 5.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5404785 1 5.11
CHEMBL5406267 1 -
CHEMBL5431108 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5404785 IC50 = 7700.0 nM 5.11
CHEMBL5406267 IC50 - -
CHEMBL5431108 IC50 > 10000.0 nM -