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Assay Detail

CHEMBL761609

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

Binding
Inhibition of human recombinant Poly (ADP-ribose) polymerase 1
25
Total Activities
25
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

Design and synthesis of poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors. Part 3: In vitro evaluation of 1,3,4,5-tetrahydro-benzo[c][1,6]- and [c][1,7]-naphthyridin-6-ones.
Ferraris D, Ficco RP, Pahutski T, Lautar S, Huang S, Zhang J, Kalish V.
Bioorg Med Chem Lett (2003) 13 : 2513 -2518
PubMed 12852955 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.88 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL444846 1 7.70
CHEMBL84096 1 7.60
CHEMBL83224 1 7.52
CHEMBL310320 1 7.51
CHEMBL84371 1 7.50
CHEMBL84979 1 7.46
CHEMBL84741 1 7.38
CHEMBL84192 1 7.23
CHEMBL310120 1 7.05
CHEMBL82336 1 7.00
CHEMBL312316 1 6.94
CHEMBL82342 1 6.89
CHEMBL84886 1 6.79
CHEMBL83760 1 6.78
CHEMBL311091 1 6.77
CHEMBL85733 1 6.73
CHEMBL84265 1 6.68
CHEMBL309636 1 6.62
CHEMBL420964 1 6.61
CHEMBL45245 1 6.46
CHEMBL83432 1 6.46
CHEMBL82940 1 6.45
CHEMBL313782 1 6.42
CHEMBL312183 1 6.34
CHEMBL84044 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL444846 IC50 = 20.0 nM 7.70
CHEMBL84096 IC50 = 25.0 nM 7.60
CHEMBL83224 IC50 = 30.0 nM 7.52
CHEMBL310320 IC50 = 31.0 nM 7.51
CHEMBL84371 IC50 = 32.0 nM 7.50
CHEMBL84979 IC50 = 35.0 nM 7.46
CHEMBL84741 IC50 = 42.0 nM 7.38
CHEMBL84192 IC50 = 59.0 nM 7.23
CHEMBL310120 IC50 = 89.0 nM 7.05
CHEMBL82336 IC50 = 99.0 nM 7.00
CHEMBL312316 IC50 = 116.0 nM 6.94
CHEMBL82342 IC50 = 128.0 nM 6.89
CHEMBL84886 IC50 = 162.0 nM 6.79
CHEMBL83760 IC50 = 167.0 nM 6.78
CHEMBL311091 IC50 = 169.0 nM 6.77
CHEMBL85733 IC50 = 185.0 nM 6.73
CHEMBL84265 IC50 = 210.0 nM 6.68
CHEMBL309636 IC50 = 240.0 nM 6.62
CHEMBL420964 IC50 = 243.0 nM 6.61
CHEMBL45245 IC50 = 350.0 nM 6.46
CHEMBL83432 IC50 = 349.0 nM 6.46
CHEMBL82940 IC50 = 357.0 nM 6.45
CHEMBL313782 IC50 = 376.0 nM 6.42
CHEMBL312183 IC50 = 457.0 nM 6.34
CHEMBL84044 IC50 = 7500.0 nM 5.12