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Assay Detail

CHEMBL828154

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Binding
Inhibitory concentration against purified poly ADP-ribose polymerase-1 done in PARP inhibition assay kit
25
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Poly [ADP-ribose] polymerase 1 (CHEMBL3105)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent poly(ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone.
Jagtap PG, Baloglu E, Southan GJ, Mabley JG, Li H, Zhou J, van Duzer J, Salzman AL, Szabó C.
J Med Chem (2005) 48 : 5100 -5103
PubMed 16078828 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.63 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190434 1 9.00
CHEMBL365086 1 8.00
CHEMBL371339 1 7.10
CHEMBL194155 1 7.01
CHEMBL371819 1 7.00
CHEMBL191185 1 6.98
CHEMBL364752 1 6.97
CHEMBL371596 1 6.96
CHEMBL187834 1 6.52
CHEMBL363363 1 6.52
CHEMBL364691 1 6.41
CHEMBL192951 2 6.40
CHEMBL189695 1 6.35
CHEMBL370673 1 6.30
CHEMBL433965 1 6.30
CHEMBL370045 1 6.30
CHEMBL190895 1 6.19
CHEMBL372717 1 6.16
CHEMBL191469 1 6.10
CHEMBL426270 1 6.10
CHEMBL81977 3-AMINOBENZAMIDE 1 4.52
CHEMBL363380 1 -
CHEMBL365390 1 -
CHEMBL361500 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190434 IC50 = 1.0 nM 9.00
CHEMBL365086 IC50 = 10.0 nM 8.00
CHEMBL371339 IC50 = 80.0 nM 7.10
CHEMBL194155 IC50 = 98.0 nM 7.01
CHEMBL371819 IC50 = 100.0 nM 7.00
CHEMBL191185 IC50 = 105.0 nM 6.98
CHEMBL364752 IC50 = 107.0 nM 6.97
CHEMBL371596 IC50 = 110.0 nM 6.96
CHEMBL187834 IC50 = 300.0 nM 6.52
CHEMBL363363 IC50 = 300.0 nM 6.52
CHEMBL364691 IC50 = 394.0 nM 6.41
CHEMBL192951 IC50 = 400.0 nM 6.40
CHEMBL189695 IC50 = 450.0 nM 6.35
CHEMBL370673 IC50 = 500.0 nM 6.30
CHEMBL433965 IC50 = 500.0 nM 6.30
CHEMBL370045 IC50 = 500.0 nM 6.30
CHEMBL190895 IC50 = 650.0 nM 6.19
CHEMBL372717 IC50 = 700.0 nM 6.16
CHEMBL191469 IC50 = 800.0 nM 6.10
CHEMBL426270 IC50 = 800.0 nM 6.10
CHEMBL81977 3-AMINOBENZAMIDE IC50 = 30000.0 nM 4.52
CHEMBL363380 IC50 > 3000.0 nM -
CHEMBL192951 IC50 > 3000.0 nM -
CHEMBL365390 IC50 > 3000.0 nM -
CHEMBL361500 IC50 > 3000.0 nM -