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Assay Detail

CHEMBL2330982

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

Binding
Inhibition of TNKS2 (unknown origin) by NAD+-dependent autopoly(ADP ribosyl)lation assay
10
Total Activities
10
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

Poly [ADP-ribose] polymerase tankyrase-2 (CHEMBL6154)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structural basis and SAR for G007-LK, a lead stage 1,2,4-triazole based specific tankyrase 1/2 inhibitor.
Voronkov A, Holsworth DD, Waaler J, Wilson SR, Ekblad B, Perdreau-Dahl H, Dinh H, Drewes G, Hopf C, Morth JP, Krauss S.
J Med Chem (2013) 56 : 3012 -3023
PubMed 23473363 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.63 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2325503 1 7.60
CHEMBL2325500 1 7.37
CHEMBL2325497 1 7.29
CHEMBL2325502 1 7.27
CHEMBL2325499 1 6.54
CHEMBL1552719 1 6.34
CHEMBL2325498 1 5.75
CHEMBL2325501 1 4.91
CHEMBL2325496 1 -
CHEMBL2325495 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2325503 IC50 = 25.0 nM 7.60
CHEMBL2325500 IC50 = 43.0 nM 7.37
CHEMBL2325497 IC50 = 51.0 nM 7.29
CHEMBL2325502 IC50 = 54.0 nM 7.27
CHEMBL2325499 IC50 = 290.0 nM 6.54
CHEMBL1552719 IC50 = 460.0 nM 6.34
CHEMBL2325498 IC50 = 1800.0 nM 5.75
CHEMBL2325501 IC50 = 12300.0 nM 4.91
CHEMBL2325496 IC50 > 10000.0 nM -
CHEMBL2325495 IC50 > 10000.0 nM -