Page last updated: 2024-08-05 15:50:59

tankyrase inhibitor

Any compound that inhibits the action of tankyrase.

ChEBI ID: 62887

Members (1)

MemberDefinitionClass
xav939A thiopyranopyrimidine in which a 7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine skeleton is substituted at C-4 by a hydroxy group and at C-2 by a para-(trifluoromethyl)phenyl group.XAV939

Research

Studies (185)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (0.54)29.6817
2010's141 (76.22)24.3611
2020's43 (23.24)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews4 (2.15%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other182 (97.85%)84.16%

Protein Targets (30)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
cytochrome P450 2C9, partialHomo sapiens (human)Potency18.999111
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency21.317411
EWS/FLI fusion proteinHomo sapiens (human)Potency24.366744
GVesicular stomatitis virusPotency18.999111
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency18.999111
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency18.999112
Interferon betaHomo sapiens (human)Potency18.999111

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Chain A, Tankyrase-1Homo sapiens (human)IC500.011012
Cytochrome P450 2C9 Homo sapiens (human)IC5050.000011
Cytochrome P450 3A4Homo sapiens (human)IC5050.000011
Inosine-5'-monophosphate dehydrogenase 2Homo sapiens (human)IC5010.000011
Plasma kallikreinHomo sapiens (human)IC5030.000011
Poly [ADP-ribose] polymerase 1Homo sapiens (human)IC502.99251517
Poly [ADP-ribose] polymerase 2Homo sapiens (human)IC500.52761011
Poly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)IC5011.39622324
Poly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)IC5011.38322324
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC5030.000011
Protein mono-ADP-ribosyltransferase PARP11Homo sapiens (human)IC505.011911
Protein mono-ADP-ribosyltransferase PARP14Homo sapiens (human)IC505.600123
Protein mono-ADP-ribosyltransferase PARP15Homo sapiens (human)IC5015.000011
Protein mono-ADP-ribosyltransferase PARP16Homo sapiens (human)IC505.011911
Protein mono-ADP-ribosyltransferase PARP3Homo sapiens (human)IC503.890323
Protein mono-ADP-ribosyltransferase PARP4Homo sapiens (human)IC504.589023
Protein mono-ADP-ribosyltransferase PARP6Homo sapiens (human)IC5010.000011
Protein Wnt-3aHomo sapiens (human)IC500.078011
Protein Wnt-3aMus musculus (house mouse)IC500.078011
Vesicular acetylcholine transporterRattus norvegicus (Norway rat)IC500.015011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Axin-2Homo sapiens (human)EC500.371011
Chain A, Tankyrase-2Homo sapiens (human)Kd0.008011
Poly [ADP-ribose] polymerase 1Homo sapiens (human)Kd0.620011
Poly [ADP-ribose] polymerase tankyrase-1Homo sapiens (human)Kd0.054022
Poly [ADP-ribose] polymerase tankyrase-2Homo sapiens (human)Kd0.009433