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Assay Detail

CHEMBL761611

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

Binding
Inhibitory concentration against purified recombinant human Poly (ADP-ribose) polymerase 1
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis of substituted 5[H]phenanthridin-6-ones as potent poly(ADP-ribose)polymerase-1 (PARP1) inhibitors.
Li JH, Serdyuk L, Ferraris DV, Xiao G, Tays KL, Kletzly PW, Li W, Lautar S, Zhang J, Kalish VJ.
Bioorg Med Chem Lett (2001) 11 : 1687 -1690
PubMed 11425538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.71 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL46137 1 8.00
CHEMBL47508 1 7.85
CHEMBL298053 1 7.68
CHEMBL540525 1 7.52
CHEMBL47283 1 7.48
CHEMBL296032 1 7.46
CHEMBL417002 1 7.44
CHEMBL46196 1 7.43
CHEMBL48138 1 7.24
CHEMBL296750 1 7.04
CHEMBL47371 1 6.87
CHEMBL289834 1 6.82
CHEMBL48391 1 6.81
CHEMBL225725 1 6.75
CHEMBL45764 1 6.75
CHEMBL294995 1 6.74
CHEMBL297175 1 6.71
CHEMBL298450 1 6.62
CHEMBL298064 1 6.51
CHEMBL45245 1 6.28
CHEMBL45072 1 5.70
CHEMBL47840 1 5.49
CHEMBL45904 1 5.21
CHEMBL297200 1 4.85
CHEMBL47846 1 4.46
CHEMBL44692 1 -
CHEMBL46267 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL46137 IC50 = 10.0 nM 8.00
CHEMBL47508 IC50 = 14.0 nM 7.85
CHEMBL298053 IC50 = 21.0 nM 7.68
CHEMBL540525 IC50 = 30.0 nM 7.52
CHEMBL47283 IC50 = 33.0 nM 7.48
CHEMBL296032 IC50 = 35.0 nM 7.46
CHEMBL417002 IC50 = 36.0 nM 7.44
CHEMBL46196 IC50 = 37.0 nM 7.43
CHEMBL48138 IC50 = 57.0 nM 7.24
CHEMBL296750 IC50 = 92.0 nM 7.04
CHEMBL47371 IC50 = 136.0 nM 6.87
CHEMBL289834 IC50 = 150.0 nM 6.82
CHEMBL48391 IC50 = 156.0 nM 6.81
CHEMBL225725 IC50 = 180.0 nM 6.75
CHEMBL45764 IC50 = 180.0 nM 6.75
CHEMBL294995 IC50 = 184.0 nM 6.74
CHEMBL297175 IC50 = 195.0 nM 6.71
CHEMBL298450 IC50 = 240.0 nM 6.62
CHEMBL298064 IC50 = 312.0 nM 6.51
CHEMBL45245 IC50 = 520.0 nM 6.28
CHEMBL45072 IC50 = 2010.0 nM 5.70
CHEMBL47840 IC50 = 3260.0 nM 5.49
CHEMBL45904 IC50 = 6100.0 nM 5.21
CHEMBL297200 IC50 = 14000.0 nM 4.85
CHEMBL47846 IC50 = 35000.0 nM 4.46
CHEMBL44692 IC50 > 60000.0 nM -
CHEMBL46267 IC50 > 100000.0 nM -