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Assay Detail

CHEMBL4311837

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Binding
Inhibition of full length human His-SUMO-tagged PARP11 expressed in Escherichia coli BL21 assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay
ChEMBL ↗
50
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 PARP11 (CHEMBL2380189) ↗
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 50 4.94 5.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4580007 — — 2 5.93
CHEMBL125200 — — 2 5.68
CHEMBL1438938 — — 2 5.68
CHEMBL4470303 — — 2 5.54
CHEMBL4455412 — — 2 5.38
CHEMBL4573527 — — 2 5.34
CHEMBL4577063 — — 2 5.31
CHEMBL4450751 — — 2 5.24
CHEMBL4572268 — — 2 5.22
CHEMBL1688212 — — 2 5.10
CHEMBL4565850 — — 2 5.06
CHEMBL4462418 — — 2 4.92
CHEMBL4565268 — — 2 4.87
CHEMBL4585230 — — 2 4.86
CHEMBL4515501 — — 2 4.78
CHEMBL4452747 — — 2 4.76
CHEMBL4559852 — — 2 4.67
CHEMBL4544104 — — 2 4.58
CHEMBL4524394 — — 2 4.57
CHEMBL4513504 — — 2 4.52
CHEMBL4473649 — — 2 4.47
CHEMBL4589699 — — 2 4.35
CHEMBL4545565 — — 2 4.29
CHEMBL4475063 — — 2 4.26
CHEMBL4447011 — — 2 4.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4580007 — IC50 = 1174.9 nM 5.93
CHEMBL4580007 — IC50 = 1200.0 nM 5.92
CHEMBL125200 — IC50 = 2100.0 nM 5.68
CHEMBL1438938 — IC50 = 2100.0 nM 5.68
CHEMBL1438938 — IC50 = 2089.3 nM 5.68
CHEMBL125200 — IC50 = 2137.96 nM 5.67
CHEMBL4470303 — IC50 = 2900.0 nM 5.54
CHEMBL4470303 — IC50 = 2884.03 nM 5.54
CHEMBL4455412 — IC50 = 4168.69 nM 5.38
CHEMBL4455412 — IC50 = 4200.0 nM 5.38
CHEMBL4573527 — IC50 = 4600.0 nM 5.34
CHEMBL4573527 — IC50 = 4570.88 nM 5.34
CHEMBL4577063 — IC50 = 4897.79 nM 5.31
CHEMBL4577063 — IC50 = 4900.0 nM 5.31
CHEMBL4450751 — IC50 = 5800.0 nM 5.24
CHEMBL4450751 — IC50 = 5754.4 nM 5.24
CHEMBL4572268 — IC50 = 6025.6 nM 5.22
CHEMBL4572268 — IC50 = 6100.0 nM 5.21
CHEMBL1688212 — IC50 = 8000.0 nM 5.10
CHEMBL1688212 — IC50 = 7943.28 nM 5.10
CHEMBL4565850 — IC50 = 8709.64 nM 5.06
CHEMBL4565850 — IC50 = 8700.0 nM 5.06
CHEMBL4462418 — IC50 = 12000.0 nM 4.92
CHEMBL4462418 — IC50 = 12022.64 nM 4.92
CHEMBL4565268 — IC50 = 13500.0 nM 4.87
CHEMBL4565268 — IC50 = 13489.63 nM 4.87
CHEMBL4585230 — IC50 = 13803.84 nM 4.86
CHEMBL4585230 — IC50 = 14000.0 nM 4.85
CHEMBL4515501 — IC50 = 16595.87 nM 4.78
CHEMBL4515501 — IC50 = 16700.0 nM 4.78
CHEMBL4452747 — IC50 = 17378.01 nM 4.76
CHEMBL4452747 — IC50 = 17400.0 nM 4.76
CHEMBL4559852 — IC50 = 21200.0 nM 4.67
CHEMBL4559852 — IC50 = 21379.62 nM 4.67
CHEMBL4544104 — IC50 = 26302.68 nM 4.58
CHEMBL4544104 — IC50 = 26400.0 nM 4.58
CHEMBL4524394 — IC50 = 27000.0 nM 4.57
CHEMBL4524394 — IC50 = 26915.35 nM 4.57
CHEMBL4513504 — IC50 = 30400.0 nM 4.52
CHEMBL4513504 — IC50 = 30199.52 nM 4.52
CHEMBL4473649 — IC50 = 34100.0 nM 4.47
CHEMBL4473649 — IC50 = 33884.42 nM 4.47
CHEMBL4589699 — IC50 = 44668.36 nM 4.35
CHEMBL4589699 — IC50 = 44700.0 nM 4.35
CHEMBL4545565 — IC50 = 51700.0 nM 4.29
CHEMBL4545565 — IC50 = 51286.14 nM 4.29
CHEMBL4475063 — IC50 = 54700.0 nM 4.26
CHEMBL4475063 — IC50 = 58884.37 nM 4.23
CHEMBL4447011 — IC50 = 92100.0 nM 4.04
CHEMBL4447011 — IC50 = 91201.08 nM 4.04