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Assay Detail

CHEMBL4272739

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Binding
Inhibition of C-terminal His-tagged human ARTD10 (809 to 1017 residues) expressed in Escherichia coli Rosetta2 (DE3) using SRPK2 as substrate after 13 hrs in presence of NAD+
ChEMBL ↗
49
Total Activities
25
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

4-(Phenoxy) and 4-(benzyloxy)benzamides as potent and selective inhibitors of mono-ADP-ribosyltransferase PARP10/ARTD10.
Murthy S, Desantis J, Verheugd P, Maksimainen MM, Venkannagari H, Massari S, Ashok Y, Obaji E, Nkizinkinko Y, Lüscher B, Tabarrini O, Lehtiö L.
Eur J Med Chem (2018) 156 : 93 -102
PubMed 30006177 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 5.76 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4287262 — — 2 6.75
CHEMBL4208737 — — 2 6.64
CHEMBL1438938 — — 1 6.48
CHEMBL4287655 — — 2 6.21
CHEMBL4277717 — — 2 6.14
CHEMBL4277025 — — 2 5.96
CHEMBL4283907 — — 2 5.90
CHEMBL4285656 — — 2 5.90
CHEMBL4278641 — — 2 5.87
CHEMBL3278113 — — 2 5.87
CHEMBL4294485 — — 2 5.86
CHEMBL4289980 — — 2 5.85
CHEMBL4277166 — — 2 5.77
CHEMBL4279332 — — 2 5.76
CHEMBL4293979 — — 2 5.72
CHEMBL4293554 — — 2 5.70
CHEMBL4293771 — — 2 5.66
CHEMBL449635 — — 2 5.56
CHEMBL4203858 — — 2 5.48
CHEMBL4294759 — — 2 5.47
CHEMBL4286555 — — 2 5.42
CHEMBL4282106 — — 2 5.35
CHEMBL4283395 — — 2 5.14
CHEMBL4213137 — — 2 5.10
CHEMBL4277361 — — 2 5.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4287262 — IC50 = 180.0 nM 6.75
CHEMBL4287262 — IC50 = 186.21 nM 6.73
CHEMBL4208737 — IC50 = 230.0 nM 6.64
CHEMBL4208737 — IC50 = 234.42 nM 6.63
CHEMBL1438938 — IC50 = 330.0 nM 6.48
CHEMBL4287655 — IC50 = 616.6 nM 6.21
CHEMBL4287655 — IC50 = 710.0 nM 6.15
CHEMBL4277717 — IC50 = 724.44 nM 6.14
CHEMBL4277717 — IC50 = 720.0 nM 6.14
CHEMBL4277025 — IC50 = 1100.0 nM 5.96
CHEMBL4277025 — IC50 = 1148.15 nM 5.94
CHEMBL4283907 — IC50 = 1258.93 nM 5.90
CHEMBL4285656 — IC50 = 1258.93 nM 5.90
CHEMBL4283907 — IC50 = 1300.0 nM 5.89
CHEMBL4285656 — IC50 = 1300.0 nM 5.89
CHEMBL4278641 — IC50 = 1350.0 nM 5.87
CHEMBL4278641 — IC50 = 1348.96 nM 5.87
CHEMBL3278113 — IC50 = 1348.96 nM 5.87
CHEMBL4294485 — IC50 = 1380.38 nM 5.86
CHEMBL4289980 — IC50 = 1400.0 nM 5.85
CHEMBL4294485 — IC50 = 1400.0 nM 5.85
CHEMBL3278113 — IC50 = 1400.0 nM 5.85
CHEMBL4289980 — IC50 = 1445.44 nM 5.84
CHEMBL4277166 — IC50 = 1698.24 nM 5.77
CHEMBL4277166 — IC50 = 1700.0 nM 5.77
CHEMBL4279332 — IC50 = 1737.8 nM 5.76
CHEMBL4279332 — IC50 = 1800.0 nM 5.75
CHEMBL4293979 — IC50 = 1900.0 nM 5.72
CHEMBL4293979 — IC50 = 1949.84 nM 5.71
CHEMBL4293554 — IC50 = 2000.0 nM 5.70
CHEMBL4293771 — IC50 = 2187.76 nM 5.66
CHEMBL4293771 — IC50 = 2200.0 nM 5.66
CHEMBL4293554 — IC50 = 2290.87 nM 5.64
CHEMBL449635 — IC50 = 2754.23 nM 5.56
CHEMBL449635 — IC50 = 2800.0 nM 5.55
CHEMBL4203858 — IC50 = 3311.31 nM 5.48
CHEMBL4203858 — IC50 = 3300.0 nM 5.48
CHEMBL4294759 — IC50 = 3388.44 nM 5.47
CHEMBL4294759 — IC50 = 3500.0 nM 5.46
CHEMBL4286555 — IC50 = 3800.0 nM 5.42
CHEMBL4286555 — IC50 = 3801.89 nM 5.42
CHEMBL4282106 — IC50 = 4500.0 nM 5.35
CHEMBL4282106 — IC50 = 4570.88 nM 5.34
CHEMBL4283395 — IC50 = 7244.36 nM 5.14
CHEMBL4283395 — IC50 = 7300.0 nM 5.14
CHEMBL4213137 — IC50 = 7900.0 nM 5.10
CHEMBL4213137 — IC50 = 7943.28 nM 5.10
CHEMBL4277361 — IC50 = 9332.54 nM 5.03
CHEMBL4277361 — IC50 = 9300.0 nM 5.03