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Assay Detail

CHEMBL1767526

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant full length mouse PARP-2 after 10 mins using [3H]NAD+ by solution-phase assay
25
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Poly [ADP-ribose] polymerase 2 (CHEMBL2794)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

5-Benzamidoisoquinolin-1-ones and 5-(ω-carboxyalkyl)isoquinolin-1-ones as isoform-selective inhibitors of poly(ADP-ribose) polymerase 2 (PARP-2).
Sunderland PT, Woon EC, Dhami A, Bergin AB, Mahon MF, Wood PJ, Jones LA, Tully SR, Lloyd MD, Thompson AS, Javaid H, Martin NM, Threadgill MD.
J Med Chem (2011) 54 : 2049 -2059
PubMed 21417348 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.56 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1767067 1 7.05
CHEMBL1767068 1 6.30
CHEMBL1767065 1 6.26
CHEMBL446240 2 6.00
CHEMBL1767053 1 5.89
CHEMBL1767054 1 5.82
CHEMBL1584950 1 5.82
CHEMBL1767056 1 5.80
CHEMBL1767066 1 5.80
CHEMBL1767064 1 5.52
CHEMBL1767057 1 5.50
CHEMBL1767048 1 5.48
CHEMBL1767050 1 5.44
CHEMBL1767051 1 5.41
CHEMBL1767063 1 5.33
CHEMBL1767055 1 5.25
CHEMBL1767061 1 5.20
CHEMBL1767049 1 5.19
CHEMBL1767058 1 5.16
CHEMBL1765110 1 4.70
CHEMBL1767059 1 4.55
CHEMBL1767060 1 4.54
CHEMBL1767062 1 -
CHEMBL1767052 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1767067 IC50 = 90.0 nM 7.05
CHEMBL1767068 IC50 = 500.0 nM 6.30
CHEMBL1767065 IC50 = 550.0 nM 6.26
CHEMBL446240 IC50 = 1000.0 nM 6.00
CHEMBL446240 IC50 = 1050.0 nM 5.98
CHEMBL1767053 IC50 = 1300.0 nM 5.89
CHEMBL1767054 IC50 = 1500.0 nM 5.82
CHEMBL1584950 IC50 = 1500.0 nM 5.82
CHEMBL1767056 IC50 = 1600.0 nM 5.80
CHEMBL1767066 IC50 = 1600.0 nM 5.80
CHEMBL1767064 IC50 = 3000.0 nM 5.52
CHEMBL1767057 IC50 = 3200.0 nM 5.50
CHEMBL1767048 IC50 = 3300.0 nM 5.48
CHEMBL1767050 IC50 = 3600.0 nM 5.44
CHEMBL1767051 IC50 = 3900.0 nM 5.41
CHEMBL1767063 IC50 = 4700.0 nM 5.33
CHEMBL1767055 IC50 = 5600.0 nM 5.25
CHEMBL1767061 IC50 = 6300.0 nM 5.20
CHEMBL1767049 IC50 = 6500.0 nM 5.19
CHEMBL1767058 IC50 = 7000.0 nM 5.16
CHEMBL1765110 IC50 = 19900.0 nM 4.70
CHEMBL1767059 IC50 = 27900.0 nM 4.55
CHEMBL1767060 IC50 = 29000.0 nM 4.54
CHEMBL1767062 IC50 > 25000.0 nM -
CHEMBL1767052 IC50 - -