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Assay Detail

CHEMBL3595275

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

Binding
Inhibition of human TNKS2 (956 to 1161 and 873 to 1161) using 500 nM NAD substrate after 20 mins incubation by fluorescence assay
ChEMBL ↗
59
Total Activities
33
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

Discovery of potent and selective nonplanar tankyrase inhibiting nicotinamide mimics.
Nkizinkiko Y, Suneel Kumar BV, Jeankumar VU, Haikarainen T, Koivunen J, Madhuri C, Yogeeswari P, Venkannagari H, Obaji E, Pihlajaniemi T, Sriram D, Lehtiö L.
Bioorg Med Chem (2015) 23 : 4139 -4149
PubMed 26183543 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 59 5.55 7.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3593715 — — 2 7.15
CHEMBL3594137 — — 2 6.82
CHEMBL3594136 — — 2 6.64
CHEMBL3593716 — — 2 6.52
CHEMBL268379 — — 2 6.45
CHEMBL1448672 — — 2 6.39
CHEMBL3594132 — — 2 6.24
CHEMBL2144572 — — 2 6.14
CHEMBL3594127 — — 2 6.12
CHEMBL138007 — — 2 6.00
CHEMBL3594126 — — 2 5.72
CHEMBL3594129 — — 2 5.68
CHEMBL3593717 — — 2 5.64
CHEMBL3594133 — — 2 5.57
CHEMBL3594134 — — 2 5.57
CHEMBL3594124 — — 2 5.35
CHEMBL3594128 — — 2 5.27
CHEMBL129312 — — 2 5.26
CHEMBL3593718 — — 2 5.21
CHEMBL3593719 — — 2 5.18
CHEMBL1900376 — — 2 5.14
CHEMBL3593720 — — 2 5.00
CHEMBL7443 — — 2 4.94
CHEMBL3594131 — — 2 4.82
CHEMBL1580791 — — 1 4.51
CHEMBL3594135 — — 2 4.28
CHEMBL1892778 — — 2 4.20
CHEMBL3594123 — — 1 4.20
CHEMBL3594130 — — 1 4.04
CHEMBL3594122 — — 1 4.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3593715 — IC50 = 71.0 nM 7.15
CHEMBL3593715 — IC50 = 70.79 nM 7.15
CHEMBL3594137 — IC50 = 150.0 nM 6.82
CHEMBL3594137 — IC50 = 154.88 nM 6.81
CHEMBL3594136 — IC50 = 230.0 nM 6.64
CHEMBL3594136 — IC50 = 234.42 nM 6.63
CHEMBL3593716 — IC50 = 302.0 nM 6.52
CHEMBL3593716 — IC50 = 300.0 nM 6.52
CHEMBL268379 — IC50 = 354.81 nM 6.45
CHEMBL268379 — IC50 = 360.0 nM 6.44
CHEMBL1448672 — IC50 = 410.0 nM 6.39
CHEMBL1448672 — IC50 = 416.87 nM 6.38
CHEMBL3594132 — IC50 = 580.0 nM 6.24
CHEMBL3594132 — IC50 = 575.44 nM 6.24
CHEMBL2144572 — IC50 = 724.44 nM 6.14
CHEMBL2144572 — IC50 = 720.0 nM 6.14
CHEMBL3594127 — IC50 = 758.58 nM 6.12
CHEMBL3594127 — IC50 = 760.0 nM 6.12
CHEMBL138007 — IC50 = 990.0 nM 6.00
CHEMBL138007 — IC50 = 1000.0 nM 6.00
CHEMBL3594126 — IC50 = 1900.0 nM 5.72
CHEMBL3594126 — IC50 = 1949.84 nM 5.71
CHEMBL3594129 — IC50 = 2100.0 nM 5.68
CHEMBL3594129 — IC50 = 2137.96 nM 5.67
CHEMBL3593717 — IC50 = 2300.0 nM 5.64
CHEMBL3593717 — IC50 = 2344.23 nM 5.63
CHEMBL3594134 — IC50 = 2700.0 nM 5.57
CHEMBL3594133 — IC50 = 2691.53 nM 5.57
CHEMBL3594134 — IC50 = 2691.53 nM 5.57
CHEMBL3594133 — IC50 = 2700.0 nM 5.57
CHEMBL3594124 — IC50 = 4500.0 nM 5.35
CHEMBL3594124 — IC50 = 4466.84 nM 5.35
CHEMBL3594128 — IC50 = 5400.0 nM 5.27
CHEMBL3594128 — IC50 = 5370.32 nM 5.27
CHEMBL129312 — IC50 = 5495.41 nM 5.26
CHEMBL129312 — IC50 = 5500.0 nM 5.26
CHEMBL3593718 — IC50 = 6200.0 nM 5.21
CHEMBL3593718 — IC50 = 6309.57 nM 5.20
CHEMBL3593719 — IC50 = 6600.0 nM 5.18
CHEMBL1900376 — IC50 = 7300.0 nM 5.14
CHEMBL1900376 — IC50 = 7244.36 nM 5.14
CHEMBL3593720 — IC50 = 10000.0 nM 5.00
CHEMBL3593719 — IC50 = 10000.0 nM 5.00
CHEMBL3593720 — IC50 = 11000.0 nM 4.96
CHEMBL7443 — IC50 = 11481.54 nM 4.94
CHEMBL7443 — IC50 = 12000.0 nM 4.92
CHEMBL3594131 — IC50 = 15000.0 nM 4.82
CHEMBL3594131 — IC50 = 15135.61 nM 4.82
CHEMBL1580791 — IC50 = 31200.0 nM 4.51
CHEMBL3594135 — IC50 = 53000.0 nM 4.28