Page last updated: 2024-12-09
iwr-1 exo
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Description
IWR-1-exo : A dicarboximide having an exo bridged phthalimide structure, substituted at nitrogen by a 4-(quinolin-8-ylcarbamoyl)benzoyl group. It is a weak axin stabilizer, an analogue of IWR-1-endo. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 1163034 |
| CHEBI ID | 62883 |
| SCHEMBL ID | 17369116 |
| MeSH ID | M0590294 |
Synonyms (18)
| Synonym |
|---|
| chebi:62883 , |
| exo-iwr-1 |
| iwr-1-exo |
| 4-[(3ar,4r,7s,7as)-1,3-dioxo-1,3,3a,4,7,7a-hexahydro-2h-4,7-methanoisoindol-2-yl]-n-(quinolin-8-yl)benzamide |
| 1127442-87-8 |
| SCHEMBL17369116 |
| AKOS024457891 |
| 4-[(3ar,4r,7s,7as-rel)-1,3,3a,4,7,7a-hexahydro-1,3-dioxo-4,7-methano-2h-isoindol-2-yl]-n-8-quinolinylbenzamide |
| exo-iwr 1 |
| iwr 1-exo |
| J-002832 |
| DTXSID50360787 |
| 4-[(1r,2r,6s,7s)-3,5-dioxo-4-azatricyclo[5.2.1.02,6]dec-8-en-4-yl]-n-quinolin-8-ylbenzamide |
| Q27132253 |
| F81704 |
| rel-4-((3ar,4r,7s,7as)-1,3-dioxo-1,3,3a,4,7,7a-hexahydro-2h-4,7-methanoisoindol-2-yl)-n-(quinolin-8-yl)benzamide |
| HY-108437 |
| CS-0028662 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Roles (1)
| Role | Description |
|---|---|
| axin stabilizer | null |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
Drug Classes (2)
| Class | Description |
|---|---|
| dicarboximide | An imide in which the two acyl substituents on nitrogen are carboacyl groups. |
| bridged compound | A polycyclic compound in which two rings have two or more atoms in common. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
Protein Targets (3)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Poly [ADP-ribose] polymerase tankyrase-1 | Homo sapiens (human) | IC50 (µMol) | 0.6515 | 0.0019 | 0.6293 | 5.0000 | AID1655633; AID748264 |
| Poly [ADP-ribose] polymerase tankyrase-2 | Homo sapiens (human) | IC50 (µMol) | 0.0292 | 0.0021 | 0.6750 | 5.1300 | AID1655635 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Proto-oncogene Wnt-3 | Homo sapiens (human) | EC50 (µMol) | 5.0000 | 0.6500 | 2.8250 | 5.0000 | AID425205 |
| Poly [ADP-ribose] polymerase tankyrase-2 | Homo sapiens (human) | EC50 (µMol) | 5.0000 | 0.2000 | 2.5667 | 5.0000 | AID661307 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (48)
Molecular Functions (12)
Ceullar Components (23)
Bioassays (12)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID525194 | Induction of Axin2 in mouse L cell expressing Wnt and STF assessed as decreased beta-casein level by Western blot method | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID1655635 | Inhibition of full length human N-terminal GST-tagged TNKS2 ADP-ART catalytic domain (1001 to 1327 residues) using histone H2A as substrate incubated for 20 mins followed by [32P[-NAD+ addition and further incubated for 1 hr by liquid scintillation counte | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | From PARP1 to TNKS2 Inhibition: A Structure-Based Approach. |
| AID1655632 | Inhibition of full length human N-terminal His-tagged PARP2 expressed in baculovirus infected Sf9 cells at 200 uM using histone H3.3 as substrate incubated for 20 mins followed by [32P[-NAD+ addition and further incubated for 1 hr by liquid scintillation | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | From PARP1 to TNKS2 Inhibition: A Structure-Based Approach. |
| AID748264 | Inhibition of 6XHis-tagged tankyrase1 (1091 to 1325) (unknown origin) after 60 mins in presence of NAD | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. |
| AID525450 | Inhibition of caudal fin regeneration after mechanical resection in zebrafish at 10 uM after 7 days | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID525197 | Induction of Axin2 stabilization in human DLD1 cells assessed as inhibition of Wnt/beta-casein pathway | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID1655630 | Inhibition of full length human C-terminal His-tagged PARP1 expressed in baculovirus infected Sf9 cells at 200 uM using chicken core histone as substrate incubated for 20 mins followed by [32P[-NAD+ addition and further incubated for 1 hr by liquid scinti | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | From PARP1 to TNKS2 Inhibition: A Structure-Based Approach. |
| AID1655633 | Inhibition of full length human N-terminal GST-tagged TNKS1 ADP-ART catalytic domain (1001 to 1327 residues) using histone H2A as substrate incubated for 20 mins followed by [32P[-NAD+ addition and further incubated for 1 hr by liquid scintillation counte | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | From PARP1 to TNKS2 Inhibition: A Structure-Based Approach. |
| AID661307 | Activity of N-terminus hexaHis-tagged human TNSK2 expressed in Escherichia coli BL21 (DE3) cells using biotinylated NAD+ as substrate after 90 mins by Western blot analysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | Structural basis of selective inhibition of human tankyrases. |
| AID525451 | Inhibition of Wnt3A mediated fgf20a expression in Zebrafish resected tail fins after 24 hrs post amputation | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. |
| AID1655641 | Inhibition of colony formation in human DLD1 cells at 1 uM incubated for 12 days by crystal violet staining based assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | From PARP1 to TNKS2 Inhibition: A Structure-Based Approach. |
| AID425205 | Inhibition of Wnt3 expressed in mouse L-cells assessed as inhibition of Wnt/catanin signaling pathway by luciferase reporter gene assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14 | Structure-activity relationship studies of small-molecule inhibitors of Wnt response. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (5)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (40.00) | 29.6817 |
| 2010's | 2 (40.00) | 24.3611 |
| 2020's | 1 (20.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||