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Assay Detail

CHEMBL2433652

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Binding
Inhibition of human TNKS1 (1030 to 1317) using NAD+ as substrate by fluorescence assay
ChEMBL ↗
53
Total Activities
32
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-1 (CHEMBL6164) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity.
Narwal M, Koivunen J, Haikarainen T, Obaji E, Legala OE, Venkannagari H, Joensuu P, Pihlajaniemi T, Lehtiö L.
J Med Chem (2013) 56 : 7880 -7889
PubMed 24116873 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 53 6.73 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2431805 — — 2 8.31
CHEMBL2431867 — — 2 8.22
CHEMBL2431803 — — 2 8.15
CHEMBL16861 — — 2 7.33
CHEMBL2431868 — — 2 7.18
CHEMBL64780 — — 2 7.18
CHEMBL16312 4'-METHOXYFLAVONE — 2 7.15
CHEMBL2431804 — — 2 6.94
CHEMBL2431801 — — 2 6.84
CHEMBL2431802 — — 2 6.84
CHEMBL2431800 — — 2 6.79
CHEMBL61745 — — 2 6.68
CHEMBL16783 — — 2 6.63
CHEMBL2431799 — — 2 6.57
CHEMBL294099 — — 2 6.50
CHEMBL275638 FLAVONE 2.0 2 6.49
CHEMBL483633 — — 2 6.44
CHEMBL293478 6-CHLOROFLAVONE — 2 6.23
CHEMBL53738 — — 2 6.16
CHEMBL327209 — — 2 6.10
CHEMBL165822 — — 2 6.07
CHEMBL16782 7-METHOXYFLAVONE — 1 5.30
CHEMBL2431798 — — 1 4.19
CHEMBL147722 — — 1 -
CHEMBL134291 6-METHYLFLAVONE — 1 -
CHEMBL137586 6-METHOXYFLAVONE — 1 -
CHEMBL2431808 — — 1 -
CHEMBL2431807 — — 1 -
CHEMBL144625 — — 1 -
CHEMBL484432 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2431805 — IC50 = 4.898 nM 8.31
CHEMBL2431867 — IC50 = 6.026 nM 8.22
CHEMBL2431867 — IC50 = 6.0 nM 8.22
CHEMBL2431803 — IC50 = 7.0 nM 8.15
CHEMBL2431803 — IC50 = 7.413 nM 8.13
CHEMBL16861 — IC50 = 47.0 nM 7.33
CHEMBL16861 — IC50 = 46.77 nM 7.33
CHEMBL64780 — IC50 = 66.0 nM 7.18
CHEMBL2431868 — IC50 = 66.07 nM 7.18
CHEMBL64780 — IC50 = 66.07 nM 7.18
CHEMBL2431868 — IC50 = 67.0 nM 7.17
CHEMBL16312 4'-METHOXYFLAVONE IC50 = 70.79 nM 7.15
CHEMBL16312 4'-METHOXYFLAVONE IC50 = 71.0 nM 7.15
CHEMBL2431804 — IC50 = 114.0 nM 6.94
CHEMBL2431804 — IC50 = 114.82 nM 6.94
CHEMBL2431801 — IC50 = 146.0 nM 6.84
CHEMBL2431802 — IC50 = 145.0 nM 6.84
CHEMBL2431802 — IC50 = 144.54 nM 6.84
CHEMBL2431801 — IC50 = 144.54 nM 6.84
CHEMBL2431800 — IC50 = 162.0 nM 6.79
CHEMBL2431800 — IC50 = 162.18 nM 6.79
CHEMBL61745 — IC50 = 208.93 nM 6.68
CHEMBL61745 — IC50 = 210.0 nM 6.68
CHEMBL16783 — IC50 = 233.0 nM 6.63
CHEMBL16783 — IC50 = 234.42 nM 6.63
CHEMBL2431799 — IC50 = 272.0 nM 6.57
CHEMBL2431799 — IC50 = 275.42 nM 6.56
CHEMBL294099 — IC50 = 313.0 nM 6.50
CHEMBL294099 — IC50 = 316.23 nM 6.50
CHEMBL275638 FLAVONE IC50 = 323.59 nM 6.49
CHEMBL275638 FLAVONE IC50 = 330.0 nM 6.48
CHEMBL483633 — IC50 = 360.0 nM 6.44
CHEMBL483633 — IC50 = 363.08 nM 6.44
CHEMBL293478 6-CHLOROFLAVONE IC50 = 588.84 nM 6.23
CHEMBL293478 6-CHLOROFLAVONE IC50 = 595.0 nM 6.22
CHEMBL53738 — IC50 = 691.83 nM 6.16
CHEMBL53738 — IC50 = 700.0 nM 6.16
CHEMBL327209 — IC50 = 788.0 nM 6.10
CHEMBL327209 — IC50 = 794.33 nM 6.10
CHEMBL165822 — IC50 = 850.0 nM 6.07
CHEMBL165822 — IC50 = 851.14 nM 6.07
CHEMBL2431805 — IC50 = 5000.0 nM 5.30
CHEMBL16782 7-METHOXYFLAVONE IC50 = 5000.0 nM 5.30
CHEMBL2431798 — IC50 = 64000.0 nM 4.19
CHEMBL147722 — IC50 > 10000.0 nM -
CHEMBL134291 6-METHYLFLAVONE IC50 > 10000.0 nM -
CHEMBL137586 6-METHOXYFLAVONE IC50 > 10000.0 nM -
CHEMBL2431808 — IC50 > 10000.0 nM -
CHEMBL2431807 — IC50 > 10000.0 nM -
CHEMBL144625 — IC50 > 10000.0 nM -