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BioAssay: AID 482279

Binding affinity to human recombinant TNSK1 expressed in Escherichia coli by isothermal titration calorimetry

We report two crystal structures of the PARP domain of human tankyrase-2 (TNKS2). Tankyrases are involved in fundamental cellular processes such as telomere homeostasis and Wnt signaling. The complex of TNKS2 with the potent inhibitor XAV939 provides insights into the molecular basis of the strong interaction and suggests routes for further development of tankyrase inhibitors. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Active(1)
 
 
AID: 482279
Data Source: ChEMBL (633154)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-09-27
Modify Date: 2014-05-25

Data Table ( Complete ):           Active    All
Target
Sequence: RecName: Full=Tankyrase-1; Short=TANK1; AltName: Full=ADP-ribosyltransferase diphtheria toxin-like 5; Short=ARTD5; AltName: Full=Poly [ADP-ribose] polymerase 5A; AltName: Full=TNKS-1; AltName: Full=TRF1-interacting ankyrin-related ADP-ribose polymerase; AltName: Full=Tankyrase I
Description ..   
Protein Family: tankyrase_like
Comment ..   

Gene:TNKS     Related Protein 3D Structures     More BioActivity Data..
BioActive Compound: 1
Description:
Title: Structural basis for the interaction between tankyrase-2 and a potent Wnt-signaling inhibitor.

Abstract: We report two crystal structures of the PARP domain of human tankyrase-2 (TNKS2). Tankyrases are involved in fundamental cellular processes such as telomere homeostasis and Wnt signaling. The complex of TNKS2 with the potent inhibitor XAV939 provides insights into the molecular basis of the strong interaction and suggests routes for further development of tankyrase inhibitors.
(PMID: 20565110)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

Target Type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Kd*Kd PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6Kd activity commentKd activity commentString
7Kd standard flagKd standard flagInteger
8Kd qualifierKd qualifierString
9Kd published valueKd published valueFloatnM
10Kd standard valueKd standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
Classification
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