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Assay Detail

CHEMBL4311836

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Binding
Inhibition of human PARP10 catalytic domain assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay
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

Rational Design of Cell-Active Inhibitors of PARP10.
Morgan RK, Kirby IT, Vermehren-Schmaedick A, Rodriguez K, Cohen MS.
ACS Med Chem Lett (2019) 10 : 74 -79
PubMed 30655950 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 5.49 6.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4462418 — — 2 6.15
CHEMBL4455412 — — 2 5.96
CHEMBL4450751 — — 2 5.96
CHEMBL1438938 — — 2 5.89
CHEMBL4559852 — — 2 5.85
CHEMBL4572268 — — 2 5.85
CHEMBL4577063 — — 2 5.81
CHEMBL4544104 — — 2 5.80
CHEMBL4524394 — — 2 5.76
CHEMBL4545565 — — 2 5.75
CHEMBL4585230 — — 2 5.75
CHEMBL4589699 — — 2 5.72
CHEMBL4573527 — — 2 5.68
CHEMBL4475063 — — 2 5.66
CHEMBL4452747 — — 2 5.65
CHEMBL4565850 — — 2 5.61
CHEMBL4513504 — — 2 5.60
CHEMBL4447011 — — 2 5.57
CHEMBL125200 — — 2 5.07
CHEMBL4470303 — — 2 5.00
CHEMBL4565268 — — 2 4.77
CHEMBL4473649 — — 2 4.48
CHEMBL4580007 — — 2 4.46
CHEMBL1688212 — — 2 4.15
CHEMBL4515501 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4462418 — IC50 = 710.0 nM 6.15
CHEMBL4462418 — IC50 = 707.95 nM 6.15
CHEMBL4455412 — IC50 = 1096.48 nM 5.96
CHEMBL4450751 — IC50 = 1100.0 nM 5.96
CHEMBL4455412 — IC50 = 1100.0 nM 5.96
CHEMBL4450751 — IC50 = 1122.02 nM 5.95
CHEMBL1438938 — IC50 = 1300.0 nM 5.89
CHEMBL1438938 — IC50 = 1318.26 nM 5.88
CHEMBL4559852 — IC50 = 1400.0 nM 5.85
CHEMBL4572268 — IC50 = 1412.54 nM 5.85
CHEMBL4572268 — IC50 = 1400.0 nM 5.85
CHEMBL4559852 — IC50 = 1445.44 nM 5.84
CHEMBL4577063 — IC50 = 1548.82 nM 5.81
CHEMBL4544104 — IC50 = 1584.89 nM 5.80
CHEMBL4544104 — IC50 = 1600.0 nM 5.80
CHEMBL4577063 — IC50 = 1600.0 nM 5.80
CHEMBL4524394 — IC50 = 1737.8 nM 5.76
CHEMBL4585230 — IC50 = 1800.0 nM 5.75
CHEMBL4524394 — IC50 = 1800.0 nM 5.75
CHEMBL4545565 — IC50 = 1800.0 nM 5.75
CHEMBL4585230 — IC50 = 1778.28 nM 5.75
CHEMBL4545565 — IC50 = 1819.7 nM 5.74
CHEMBL4589699 — IC50 = 1900.0 nM 5.72
CHEMBL4589699 — IC50 = 1949.84 nM 5.71
CHEMBL4573527 — IC50 = 2100.0 nM 5.68
CHEMBL4573527 — IC50 = 2137.96 nM 5.67
CHEMBL4475063 — IC50 = 2187.76 nM 5.66
CHEMBL4475063 — IC50 = 2200.0 nM 5.66
CHEMBL4452747 — IC50 = 2238.72 nM 5.65
CHEMBL4452747 — IC50 = 2300.0 nM 5.64
CHEMBL4565850 — IC50 = 2454.71 nM 5.61
CHEMBL4565850 — IC50 = 2500.0 nM 5.60
CHEMBL4513504 — IC50 = 2511.89 nM 5.60
CHEMBL4513504 — IC50 = 2500.0 nM 5.60
CHEMBL4447011 — IC50 = 2691.53 nM 5.57
CHEMBL4447011 — IC50 = 2700.0 nM 5.57
CHEMBL125200 — IC50 = 8600.0 nM 5.07
CHEMBL125200 — IC50 = 9772.37 nM 5.01
CHEMBL4470303 — IC50 = 10100.0 nM 5.00
CHEMBL4470303 — IC50 = 10232.93 nM 4.99
CHEMBL4565268 — IC50 = 16982.44 nM 4.77
CHEMBL4565268 — IC50 = 17100.0 nM 4.77
CHEMBL4473649 — IC50 = 33113.11 nM 4.48
CHEMBL4473649 — IC50 = 33100.0 nM 4.48
CHEMBL4580007 — IC50 = 34673.69 nM 4.46
CHEMBL4580007 — IC50 = 35000.0 nM 4.46
CHEMBL1688212 — IC50 = 70794.58 nM 4.15
CHEMBL1688212 — IC50 = 70300.0 nM 4.15
CHEMBL4515501 — IC50 > 50000.0 nM -