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Assay Detail

CHEMBL5318189

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Binding
Inhibition of N-terminal MBP tagged/C-terminal PARP10 (unknown origin) expressed in Escherichia coli in presence of NAD+
ChEMBL ↗
42
Total Activities
31
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

Protein mono-ADP-ribosyltransferase PARP10 (CHEMBL2429708) ↗
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 42 5.77 6.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5404785 — — 2 6.93
CHEMBL5431108 — — 2 6.75
CHEMBL5421878 — — 2 6.50
CHEMBL5416085 — — 2 6.31
CHEMBL5430541 — — 1 5.96
CHEMBL5394776 — — 2 5.82
CHEMBL5402584 — — 1 5.77
CHEMBL5402663 — — 1 5.75
CHEMBL5434061 — — 2 5.72
CHEMBL4296925 — — 1 5.50
CHEMBL5427075 — — 1 5.47
CHEMBL2136900 — — 2 5.45
CHEMBL5395131 — — 2 5.31
CHEMBL5433172 — — 2 5.30
CHEMBL5427721 — — 1 5.30
CHEMBL5403002 — — 2 5.27
CHEMBL5439304 — — 2 5.26
CHEMBL5398837 — — 1 5.19
CHEMBL5398835 — — 1 5.00
CHEMBL5429120 — — 1 -
CHEMBL5406267 — — 1 -
CHEMBL5394162 — — 1 -
CHEMBL5399492 — — 1 -
CHEMBL5409536 — — 1 -
CHEMBL5416726 — — 1 -
CHEMBL5412151 — — 1 -
CHEMBL5412860 — — 1 -
CHEMBL5394260 — — 1 -
CHEMBL5400133 — — 1 -
CHEMBL5395721 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5404785 — IC50 = 117.49 nM 6.93
CHEMBL5404785 — IC50 = 120.0 nM 6.92
CHEMBL5431108 — IC50 = 180.0 nM 6.75
CHEMBL5431108 — IC50 = 186.21 nM 6.73
CHEMBL5421878 — IC50 = 320.0 nM 6.50
CHEMBL5421878 — IC50 = 316.23 nM 6.50
CHEMBL5416085 — IC50 = 490.0 nM 6.31
CHEMBL5416085 — IC50 = 489.78 nM 6.31
CHEMBL5430541 — IC50 = 1100.0 nM 5.96
CHEMBL5394776 — IC50 = 1500.0 nM 5.82
CHEMBL5394776 — IC50 = 1548.82 nM 5.81
CHEMBL5402584 — IC50 = 1700.0 nM 5.77
CHEMBL5402663 — IC50 = 1800.0 nM 5.75
CHEMBL5434061 — IC50 = 1900.0 nM 5.72
CHEMBL5434061 — IC50 = 1949.84 nM 5.71
CHEMBL4296925 — IC50 = 3200.0 nM 5.50
CHEMBL5427075 — IC50 = 3400.0 nM 5.47
CHEMBL2136900 — IC50 = 3548.13 nM 5.45
CHEMBL2136900 — IC50 = 3700.0 nM 5.43
CHEMBL5395131 — IC50 = 4900.0 nM 5.31
CHEMBL5395131 — IC50 = 4897.79 nM 5.31
CHEMBL5427721 — IC50 = 5000.0 nM 5.30
CHEMBL5433172 — IC50 = 5011.87 nM 5.30
CHEMBL5433172 — IC50 = 5100.0 nM 5.29
CHEMBL5403002 — IC50 = 5370.32 nM 5.27
CHEMBL5403002 — IC50 = 5400.0 nM 5.27
CHEMBL5439304 — IC50 = 5500.0 nM 5.26
CHEMBL5439304 — IC50 = 5495.41 nM 5.26
CHEMBL5398837 — IC50 = 6500.0 nM 5.19
CHEMBL5398835 — IC50 = 10000.0 nM 5.00
CHEMBL5400133 — IC50 > 10000.0 nM -
CHEMBL5406267 — IC50 > 10000.0 nM -
CHEMBL5394260 — IC50 > 10000.0 nM -
CHEMBL5412860 — IC50 > 10000.0 nM -
CHEMBL5412151 — IC50 - — -
CHEMBL5394162 — IC50 - — -
CHEMBL5429120 — IC50 - — -
CHEMBL5399492 — IC50 - — -
CHEMBL5409536 — IC50 - — -
CHEMBL5395721 — IC50 > 10000.0 nM -
CHEMBL5396332 — IC50 > 10000.0 nM -
CHEMBL5416726 — IC50 - — -