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Assay Detail

CHEMBL761792

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

Binding
Inhibition of the DNA repair Poly (ADP-ribose) polymerase 1, in permeabilised L1210 murine leukemia cells
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type L1210
Confidence 9 — Direct single protein target
Curated By Expert

Target

Poly [ADP-ribose] polymerase 1 (CHEMBL3740)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Griffin RJ, Srinivasan S, Bowman K, Calvert AH, Curtin NJ, Newell DR, Pemberton LC, Golding BT.
J Med Chem (1998) 41 : 5247 -5256
PubMed 9857092 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 5.96 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127396 1 6.89
CHEMBL127101 1 6.72
CHEMBL125244 1 6.66
CHEMBL338088 1 6.64
CHEMBL123797 1 6.57
CHEMBL127335 1 6.54
CHEMBL151549 1 6.41
CHEMBL123904 1 6.40
CHEMBL125200 1 6.36
CHEMBL541203 1 6.36
CHEMBL126167 1 6.28
CHEMBL435871 1 6.11
CHEMBL125154 1 6.07
CHEMBL124749 1 6.06
CHEMBL341142 1 5.97
CHEMBL339631 1 5.87
CHEMBL147359 1 5.71
CHEMBL340481 1 5.70
CHEMBL126871 1 5.38
CHEMBL340620 1 5.32
CHEMBL419424 1 5.10
CHEMBL339695 1 4.80
CHEMBL81977 3-AMINOBENZAMIDE 1 4.72
CHEMBL123798 1 4.41
CHEMBL151728 1 -
CHEMBL346886 1 -
CHEMBL150423 1 -
CHEMBL266608 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127396 IC50 = 130.0 nM 6.89
CHEMBL127101 IC50 = 190.0 nM 6.72
CHEMBL125244 IC50 = 220.0 nM 6.66
CHEMBL338088 IC50 = 230.0 nM 6.64
CHEMBL123797 IC50 = 270.0 nM 6.57
CHEMBL127335 IC50 = 290.0 nM 6.54
CHEMBL151549 IC50 = 390.0 nM 6.41
CHEMBL123904 IC50 = 400.0 nM 6.40
CHEMBL125200 IC50 = 440.0 nM 6.36
CHEMBL541203 IC50 = 440.0 nM 6.36
CHEMBL126167 IC50 = 520.0 nM 6.28
CHEMBL435871 IC50 = 780.0 nM 6.11
CHEMBL125154 IC50 = 850.0 nM 6.07
CHEMBL124749 IC50 = 870.0 nM 6.06
CHEMBL341142 IC50 = 1060.0 nM 5.97
CHEMBL339631 IC50 = 1340.0 nM 5.87
CHEMBL147359 IC50 = 1930.0 nM 5.71
CHEMBL340481 IC50 = 2000.0 nM 5.70
CHEMBL126871 IC50 = 4200.0 nM 5.38
CHEMBL340620 IC50 = 4800.0 nM 5.32
CHEMBL419424 IC50 = 8000.0 nM 5.10
CHEMBL339695 IC50 = 15800.0 nM 4.80
CHEMBL81977 3-AMINOBENZAMIDE IC50 = 19100.0 nM 4.72
CHEMBL123798 IC50 = 39000.0 nM 4.41
CHEMBL151728 IC50 > 300.0 nM -
CHEMBL346886 IC50 > 10000.0 nM -
CHEMBL150423 IC50 > 100000.0 nM -
CHEMBL266608 IC50 > 100000.0 nM -