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Assay Detail

CHEMBL3796252

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Binding
Inhibition of recombinant human TDP2 using 18-mer single stranded oligonucleotide DNA as substrate incubated for 15 mins by PAGE assay
ChEMBL ↗
64
Total Activities
64
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosyl-DNA phosphodiesterase 2 (CHEMBL2169736) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Isoquinoline-1,3-diones as Selective Inhibitors of Tyrosyl DNA Phosphodiesterase II (TDP2).
Kankanala J, Marchand C, Abdelmalak M, Aihara H, Pommier Y, Wang Z.
J Med Chem (2016) 59 : 2734 -2746
PubMed 26910725 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 64 5.01 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3792690 — — 1 5.77
CHEMBL3792834 — — 1 5.72
CHEMBL3792475 — — 1 5.52
CHEMBL3792608 — — 1 5.52
CHEMBL3792448 — — 1 5.50
CHEMBL3793616 — — 1 5.39
CHEMBL3793925 — — 1 5.35
CHEMBL3792897 — — 1 5.35
CHEMBL3793413 — — 1 5.29
CHEMBL3794248 — — 1 5.27
CHEMBL3792520 — — 1 5.26
CHEMBL3793043 — — 1 5.25
CHEMBL3793872 — — 1 5.19
CHEMBL3793011 — — 1 5.16
CHEMBL3792592 — — 1 5.15
CHEMBL3793467 — — 1 5.12
CHEMBL3792519 — — 1 5.12
CHEMBL3794044 — — 1 5.10
CHEMBL3793669 — — 1 5.03
CHEMBL3794340 — — 1 5.01
CHEMBL3792752 — — 1 5.00
CHEMBL3792917 — — 1 5.00
CHEMBL3793839 — — 1 5.00
CHEMBL3794550 — — 1 4.96
CHEMBL3794036 — — 1 4.96
CHEMBL3792890 — — 1 4.96
CHEMBL3793210 — — 1 4.96
CHEMBL3793509 — — 1 4.89
CHEMBL3794329 — — 1 4.89
CHEMBL3793974 — — 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3792690 — IC50 = 1700.0 nM 5.77
CHEMBL3792834 — IC50 = 1900.0 nM 5.72
CHEMBL3792608 — IC50 = 3000.0 nM 5.52
CHEMBL3792475 — IC50 = 3000.0 nM 5.52
CHEMBL3792448 — IC50 = 3200.0 nM 5.50
CHEMBL3793616 — IC50 = 4100.0 nM 5.39
CHEMBL3793925 — IC50 = 4500.0 nM 5.35
CHEMBL3792897 — IC50 = 4500.0 nM 5.35
CHEMBL3793413 — IC50 = 5100.0 nM 5.29
CHEMBL3794248 — IC50 = 5400.0 nM 5.27
CHEMBL3792520 — IC50 = 5500.0 nM 5.26
CHEMBL3793043 — IC50 = 5600.0 nM 5.25
CHEMBL3793872 — IC50 = 6400.0 nM 5.19
CHEMBL3793011 — IC50 = 7000.0 nM 5.16
CHEMBL3792592 — IC50 = 7100.0 nM 5.15
CHEMBL3793467 — IC50 = 7600.0 nM 5.12
CHEMBL3792519 — IC50 = 7500.0 nM 5.12
CHEMBL3794044 — IC50 = 8000.0 nM 5.10
CHEMBL3793669 — IC50 = 9300.0 nM 5.03
CHEMBL3794340 — IC50 = 9800.0 nM 5.01
CHEMBL3792752 — IC50 = 10000.0 nM 5.00
CHEMBL3792917 — IC50 = 10000.0 nM 5.00
CHEMBL3793839 — IC50 = 10000.0 nM 5.00
CHEMBL3793210 — IC50 = 11000.0 nM 4.96
CHEMBL3792890 — IC50 = 11000.0 nM 4.96
CHEMBL3794550 — IC50 = 11000.0 nM 4.96
CHEMBL3794036 — IC50 = 11000.0 nM 4.96
CHEMBL3793509 — IC50 = 13000.0 nM 4.89
CHEMBL3794329 — IC50 = 13000.0 nM 4.89
CHEMBL3793974 — IC50 = 14000.0 nM 4.85
CHEMBL3792741 — IC50 = 14000.0 nM 4.85
CHEMBL3794188 — IC50 = 15000.0 nM 4.82
CHEMBL3792845 — IC50 = 16000.0 nM 4.80
CHEMBL3794489 — IC50 = 16000.0 nM 4.80
CHEMBL3793459 — IC50 = 16000.0 nM 4.80
CHEMBL3793606 — IC50 = 18000.0 nM 4.75
CHEMBL3793979 — IC50 = 19000.0 nM 4.72
CHEMBL3793030 — IC50 = 19000.0 nM 4.72
CHEMBL3794268 — IC50 = 20000.0 nM 4.70
CHEMBL3793425 — IC50 = 21000.0 nM 4.68
CHEMBL3793861 — IC50 = 23000.0 nM 4.64
CHEMBL1210769 — IC50 = 25000.0 nM 4.60
CHEMBL3793108 — IC50 = 26000.0 nM 4.58
CHEMBL3793154 — IC50 = 30000.0 nM 4.52
CHEMBL3794008 — IC50 = 36000.0 nM 4.44
CHEMBL3792554 — IC50 = 42000.0 nM 4.38
CHEMBL3793508 — IC50 > 111000.0 nM -
CHEMBL3792469 — IC50 > 111000.0 nM -
CHEMBL3793399 — IC50 > 37000.0 nM -
CHEMBL3793523 — IC50 > 111000.0 nM -