Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5115638

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

Binding
Inhibition of N-terminal His-tagged human TDP2 expressed in Escherichia coli BL21 using 4-nitrophenyl phenylphosphonate as substrate incubated for 60 mins by EDTA based chromogenic assay
38
Total Activities
35
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

Discovery, enantioselective synthesis of myrtucommulone E analogues as tyrosyl-DNA phosphodiesterase 2 inhibitors and their biological activities.
Zhang Y, Yang H, Wang FT, Peng X, Liu HY, Li QJ, An LK.
Eur J Med Chem (2022) 238 : 114445 -114445
PubMed 35580424 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 4.58 5.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2420506 1 5.58
CHEMBL5193891 1 5.27
CHEMBL5200850 1 5.00
CHEMBL5198624 1 4.96
CHEMBL5179671 1 4.92
CHEMBL5187487 1 4.77
CHEMBL5176062 1 4.72
CHEMBL5204999 1 4.70
CHEMBL5200135 1 4.70
CHEMBL5189390 1 4.70
CHEMBL5201964 1 4.68
CHEMBL5202869 1 4.66
CHEMBL5174273 1 4.60
CHEMBL5200727 1 4.60
CHEMBL5186569 1 4.58
CHEMBL5171322 1 4.58
CHEMBL5189949 1 4.55
CHEMBL5172481 2 4.54
CHEMBL5195066 1 4.51
CHEMBL5186825 1 4.50
CHEMBL5191036 1 4.50
CHEMBL5179715 2 4.48
CHEMBL5183495 1 4.47
CHEMBL5199748 1 4.44
CHEMBL5179728 1 4.41
CHEMBL5187014 2 4.39
CHEMBL5206358 1 4.39
CHEMBL5185469 1 4.38
CHEMBL5195639 1 4.28
CHEMBL5183522 1 4.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2420506 IC50 = 2600.0 nM 5.58
CHEMBL5193891 IC50 = 5400.0 nM 5.27
CHEMBL5200850 IC50 = 10000.0 nM 5.00
CHEMBL5198624 IC50 = 11000.0 nM 4.96
CHEMBL5179671 IC50 = 12000.0 nM 4.92
CHEMBL5187487 IC50 = 17000.0 nM 4.77
CHEMBL5176062 IC50 = 19000.0 nM 4.72
CHEMBL5189390 IC50 = 20000.0 nM 4.70
CHEMBL5204999 IC50 = 20000.0 nM 4.70
CHEMBL5200135 IC50 = 20000.0 nM 4.70
CHEMBL5201964 IC50 = 21000.0 nM 4.68
CHEMBL5202869 IC50 = 22000.0 nM 4.66
CHEMBL5174273 IC50 = 25000.0 nM 4.60
CHEMBL5200727 IC50 = 25000.0 nM 4.60
CHEMBL5186569 IC50 = 26000.0 nM 4.58
CHEMBL5171322 IC50 = 26000.0 nM 4.58
CHEMBL5189949 IC50 = 28000.0 nM 4.55
CHEMBL5172481 IC50 = 29000.0 nM 4.54
CHEMBL5195066 IC50 = 31000.0 nM 4.51
CHEMBL5191036 IC50 = 32000.0 nM 4.50
CHEMBL5172481 IC50 = 32000.0 nM 4.50
CHEMBL5186825 IC50 = 32000.0 nM 4.50
CHEMBL5179715 IC50 = 33000.0 nM 4.48
CHEMBL5183495 IC50 = 34000.0 nM 4.47
CHEMBL5199748 IC50 = 36000.0 nM 4.44
CHEMBL5179728 IC50 = 39000.0 nM 4.41
CHEMBL5187014 IC50 = 41000.0 nM 4.39
CHEMBL5206358 IC50 = 41000.0 nM 4.39
CHEMBL5185469 IC50 = 42000.0 nM 4.38
CHEMBL5179715 IC50 = 48000.0 nM 4.32
CHEMBL5187014 IC50 = 50000.0 nM 4.30
CHEMBL5195639 IC50 = 53000.0 nM 4.28
CHEMBL5183522 IC50 = 54000.0 nM 4.27
CHEMBL5193479 IC50 = 55000.0 nM 4.26
CHEMBL5197378 IC50 = 56000.0 nM 4.25
CHEMBL5191896 IC50 = 57000.0 nM 4.24
CHEMBL5194831 IC50 > 100000.0 nM -
CHEMBL5182411 IC50 > 100000.0 nM -