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Assay Detail

CHEMBL4122797

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Binding
Inhibition of full length recombinant His6-tagged human PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay
ChEMBL ↗
42
Total Activities
21
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

Design, synthesis and evaluation of potent and selective inhibitors of mono-(ADP-ribosyl)transferases PARP10 and PARP14.
Holechek J, Lease R, Thorsell AG, Karlberg T, McCadden C, Grant R, Keen A, Callahan E, Schüler H, Ferraris D.
Bioorg Med Chem Lett (2018) 28 : 2050 -2054
PubMed 29748053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 6.07 6.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4128574 — — 2 6.61
CHEMBL4125748 — — 2 6.41
CHEMBL4129789 — — 2 6.40
CHEMBL4130035 — — 2 6.34
CHEMBL4127497 — — 2 6.34
CHEMBL4129923 — — 2 6.33
CHEMBL4126054 — — 2 6.29
CHEMBL4127327 — — 2 6.24
CHEMBL4128256 — — 2 6.22
CHEMBL1438938 — — 2 6.19
CHEMBL4129542 — — 2 6.11
CHEMBL4126241 — — 2 5.97
CHEMBL4129939 — — 2 5.97
CHEMBL4127476 — — 2 5.96
CHEMBL4126046 — — 2 5.91
CHEMBL4129001 — — 2 5.87
CHEMBL4127063 — — 2 5.82
CHEMBL4129367 — — 2 5.78
CHEMBL4129782 — — 2 5.60
CHEMBL4126166 — — 2 5.55
CHEMBL4126260 — — 2 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4128574 — IC50 = 245.47 nM 6.61
CHEMBL4128574 — IC50 = 250.0 nM 6.60
CHEMBL4125748 — IC50 = 387.26 nM 6.41
CHEMBL4125748 — IC50 = 390.0 nM 6.41
CHEMBL4129789 — IC50 = 400.0 nM 6.40
CHEMBL4129789 — IC50 = 398.11 nM 6.40
CHEMBL4130035 — IC50 = 460.0 nM 6.34
CHEMBL4127497 — IC50 = 460.0 nM 6.34
CHEMBL4127497 — IC50 = 457.09 nM 6.34
CHEMBL4129923 — IC50 = 470.0 nM 6.33
CHEMBL4129923 — IC50 = 467.74 nM 6.33
CHEMBL4130035 — IC50 = 467.74 nM 6.33
CHEMBL4126054 — IC50 = 512.86 nM 6.29
CHEMBL4126054 — IC50 = 510.0 nM 6.29
CHEMBL4127327 — IC50 = 580.0 nM 6.24
CHEMBL4127327 — IC50 = 575.44 nM 6.24
CHEMBL4128256 — IC50 = 600.0 nM 6.22
CHEMBL4128256 — IC50 = 602.56 nM 6.22
CHEMBL1438938 — IC50 = 640.0 nM 6.19
CHEMBL1438938 — IC50 = 645.65 nM 6.19
CHEMBL4129542 — IC50 = 780.0 nM 6.11
CHEMBL4129542 — IC50 = 776.25 nM 6.11
CHEMBL4126241 — IC50 = 1071.52 nM 5.97
CHEMBL4129939 — IC50 = 1060.0 nM 5.97
CHEMBL4129939 — IC50 = 1071.52 nM 5.97
CHEMBL4126241 — IC50 = 1100.0 nM 5.96
CHEMBL4127476 — IC50 = 1096.48 nM 5.96
CHEMBL4127476 — IC50 = 1100.0 nM 5.96
CHEMBL4126046 — IC50 = 1220.0 nM 5.91
CHEMBL4126046 — IC50 = 1230.27 nM 5.91
CHEMBL4129001 — IC50 = 1348.96 nM 5.87
CHEMBL4129001 — IC50 = 1400.0 nM 5.85
CHEMBL4127063 — IC50 = 1500.0 nM 5.82
CHEMBL4127063 — IC50 = 1520.55 nM 5.82
CHEMBL4129367 — IC50 = 1659.59 nM 5.78
CHEMBL4129367 — IC50 = 1650.0 nM 5.78
CHEMBL4129782 — IC50 = 2500.0 nM 5.60
CHEMBL4129782 — IC50 = 2511.89 nM 5.60
CHEMBL4126260 — IC50 = 2818.38 nM 5.55
CHEMBL4126166 — IC50 = 2800.0 nM 5.55
CHEMBL4126166 — IC50 = 2818.38 nM 5.55
CHEMBL4126260 — IC50 = 2810.0 nM 5.55