====== iCRT14 30μM R08 exp492 ======
==== Mechanism of Action ====
Inhibits β-catenin-dependent transcription, may alter interaction of β-catenin with TCF4
* **Class / Subclass 1:** Gene Regulation / Transcription Inhibitor
==== Technical Notes ====
* **PubChem Name:** %%CID 5967294%%
* **Synonyms:** N/A
* **CAS #:** 677331-12-3
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/5967294|5967294]]
* **IUPAC:** %%(5Z)-5-[(2,5-dimethyl-1-pyridin-3-ylpyrrol-3-yl)methylidene]-3-phenyl-1,3-thiazolidine-2,4-dione%%
* **INCHI Name:** InChI=1S/C21H17N3O2S/c1-14-11-16(15(2)23(14)18-9-6-10-22-13-18)12-19-20(25)24(21(26)27-19)17-7-4-3-5-8-17/h3-13H,1-2H3/b19-12-
* **INCHI Key:** NCSHZXNGQYSKLR-UNOMPAQXSA-N
* **Molecular Weight:** 375.4
* **Canonical SMILES:** CC1=CC(=C(N1C2=CN=CC=C2)C)C=C3C(=O)N(C(=O)S3)C4=CC=CC=C4
* **Isomeric SMILES:** CC1=CC(=C(N1C2=CN=CC=C2)C)/C=C\\3/C(=O)N(C(=O)S3)C4=CC=CC=C4
* **Molecular Formula:** C21H17N3O2S
{{:chemogenomics:structures:chem-0300.svg?nolink}}
* **Supplier Name:** Med Chem Express
* **Catalog #:** HY-16665
* **Lot #:** 23429
* **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C21H17N3O2S 376.11142; found 376.11235
* **Platform ID:** iCRT14
* **Min:** -11.0010; **Max:** 69.6272
{{:chemogenomics:dose_response:dr_547.png?nolink&500 |}}
\\
\\
\\
\\
|< 300px 100px 200px >|
^ IC ^ Concentration (µM) ^
| IC10 |4.0980 |
| IC20 |8.5500 |
| IC30 |13.9400 |
| IC40 |20.8100 |
| IC50 |30.0600 |
| IC60 |43.4100 |
| IC70 |64.8100 |
| IC80 |N/A |
| IC90 |N/A |
\\
==== Screen Summary ====
* **Round**: 08
* **Dose**: 30µM
* **Days of incubation**: 8
* **Doublings**: 1.2
* **Numbers of reads**: 17101968
==== Screen Results ====
^Sensitive/Resistant hits (FDR<0.05)^CRANKS^Score Plot^Top 30 Genes^Screen Similarity^Top 30 Sensitive GO terms^Top 30 Resistant GO terms^
|12/56|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/iCRT14_30uM_Round-8_exp492.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp492.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:G:GOT1|GOT1]]|-3.77|<0.01|
|[[:human_genes:P:PRKAG1|PRKAG1]]|-3.72|<0.01|
|[[:human_genes:D:DERL2|DERL2]]|-3.50|<0.01|
|[[:human_genes:F:FAM3A|FAM3A]]|-3.30|<0.01|
|[[:human_genes:R:RPS17L|RPS17L]]|-3.28|0.04|
|[[:human_genes:S:SNX27|SNX27]]|-3.10|<0.01|
|[[:human_genes:S:SLC5A3|SLC5A3]]|-2.98|<0.01|
|[[:human_genes:M:MGA|MGA]]|-2.82|<0.01|
|[[:human_genes:U:URB1|URB1]]|-2.81|0.08|
|[[:human_genes:C:CDK2|CDK2]]|-2.78|<0.01|
|[[:human_genes:T:TCF4|TCF4]]|-2.77|<0.01|
|[[:human_genes:C:CMC2|CMC2]]|-2.66|0.16|
|[[:human_genes:P:PLK1|PLK1]]|-2.60|0.31|
|[[:human_genes:P:PLD3|PLD3]]|-2.59|0.02|
|[[:human_genes:Z:ZBTB1|ZBTB1]]|-2.56|0.05|
|[[:human_genes:U:UXS1|UXS1]]|-2.54|0.03|
|[[:human_genes:M:MNT|MNT]]|-2.51|0.06|
|[[:human_genes:C:CDC20|CDC20]]|-2.45|0.16|
|[[:human_genes:P:POLA1|POLA1]]|-2.38|0.30|
|[[:human_genes:O:OGT|OGT]]|-2.36|0.31|
|[[:human_genes:Z:ZFAND2B|ZFAND2B]]|-2.32|0.12|
|[[:human_genes:T:THOC2|THOC2]]|-2.32|0.15|
|[[:human_genes:S:SLC16A10|SLC16A10]]|-2.27|0.08|
|[[:human_genes:D:DOT1L|DOT1L]]|-2.27|0.08|
|[[:human_genes:R:RAB7A|RAB7A]]|-2.27|0.08|
|[[:human_genes:H:HMGCS1|HMGCS1]]|-2.24|0.15|
|[[:human_genes:Y:YPEL5|YPEL5]]|-2.21|0.11|
|[[:human_genes:K:KEAP1|KEAP1]]|-2.20|0.15|
|[[:human_genes:A:ATP6V0A2|ATP6V0A2]]|-2.19|0.15|
|[[:human_genes:O:OR13G1|OR13G1]]|-2.19|0.12|
|[[:human_genes:Z:ZBTB18|ZBTB18]]|2.55|0.01|
|[[:human_genes:A:ALG13|ALG13]]|2.57|0.02|
|[[:human_genes:P:PMAIP1|PMAIP1]]|2.59|<0.01|
|[[:human_genes:Z:ZCRB1|ZCRB1]]|2.61|0.02|
|[[:human_genes:P:P4HB|P4HB]]|2.63|<0.01|
|[[:human_genes:H:HSD17B10|HSD17B10]]|2.70|0.01|
|[[:human_genes:S:SEC62|SEC62]]|2.76|<0.01|
|[[:human_genes:A:ALAS1|ALAS1]]|2.76|0.03|
|[[:human_genes:P:PET117|PET117]]|2.77|<0.01|
|[[:human_genes:P:PGM3|PGM3]]|2.77|<0.01|
|[[:human_genes:S:SLC25A51|SLC25A51]]|2.79|<0.01|
|[[:human_genes:R:RALGAPB|RALGAPB]]|2.82|<0.01|
|[[:human_genes:D:DPH1|DPH1]]|2.84|<0.01|
|[[:human_genes:A:ARRDC4|ARRDC4]]|2.86|<0.01|
|[[:human_genes:K:KCTD5|KCTD5]]|2.86|<0.01|
|[[:human_genes:K:KIAA0922|KIAA0922]]|2.89|<0.01|
|[[:human_genes:W:WBSCR16|WBSCR16]]|2.93|0.08|
|[[:human_genes:O:OMA1|OMA1]]|2.95|<0.01|
|[[:human_genes:M:MLEC|MLEC]]|2.97|<0.01|
|[[:human_genes:N:NDUFA2|NDUFA2]]|2.97|<0.01|
|[[:human_genes:B:BAK1|BAK1]]|2.99|<0.01|
|[[:human_genes:N:NANS|NANS]]|3.04|<0.01|
|[[:human_genes:S:SYNCRIP|SYNCRIP]]|3.36|<0.01|
|[[:human_genes:S:STARD7|STARD7]]|3.38|<0.01|
|[[:human_genes:S:SPI1|SPI1]]|3.63|<0.01|
|[[:human_genes:M:MLX|MLX]]|3.65|<0.01|
|[[:human_genes:T:TMEM39A|TMEM39A]]|3.68|<0.01|
|[[:human_genes:C:CXorf56|CXorf56]]|3.72|<0.01|
|[[:human_genes:D:DDX3X|DDX3X]]|3.97|<0.01|
|[[:human_genes:P:PPP6C|PPP6C]]|3.97|<0.01|
^Screen^Correlation^Plot^
|[[:results:exp25|Oligomycin-A 2μM R00 exp25]]|0.095||
|[[:results:exp400|Senexin-A 25μM R07 exp400]]|0.091||
|[[:results:exp85|UM0129480 7μM R02 exp85]]|0.09||
|[[:results:exp529|Thimerosal 0.85μM R08 exp529]]|0.088||
|[[:results:exp488|Hippuristanol 0.12μM R08 exp488]]|0.077||
|[[:results:exp466|Cannabidiol 20μM R08 exp466]]|0.074||
|[[:results:exp290|LLY-283 2.6μM R06 exp290]]|0.074||
|[[:results:exp535|Trimetrexate 0.03μM R08 exp535]]|0.073||
|[[:results:exp431|Rotenone 0.07μM R08 exp431]]|0.071||
|[[:results:exp342|Calcium Ionophore 0.4μM R07 exp342]]|0.069||
|[[:results:exp116|AICAR 240μM R03 exp116]]|0.069||
|[[:results:exp497|Lead acetate 2000μM R08 exp497]]|0.067||
|[[:results:exp498|Lead acetate 2000μM R08 exp498 no dilution day6]]|0.066||
|[[:results:exp447|Amiloride 100μM R08 exp447]]|0.066||
|[[:results:exp65|Mubritinib 0.2μM R02 exp65]]|0.064||
|[[:results:exp359|FK-506 30μM R07 exp359]]|0.063||
|[[:results:exp440|Aphidicolin 0.4μM R08 exp440]]|0.063||
|[[:results:exp212|Phenformin 20μM R05 exp212]]|0.06||
|[[:results:exp513|ONC212 0.15μM R08 exp513]]|0.06||
|[[:results:exp357|Dorsomorphin 5μM R07 exp357]]|0.06||
|[[:results:exp234|Ethanol 0.01 R05 exp234]]|0.058||
|[[:results:exp445|∆-9-Tetrahydrocannabinol 30μM R08 exp445]]|0.057||
|[[:results:exp241|QNZ 0.01μM R05 exp241]]|0.057||
|[[:results:exp470|Chloroquine 32μM R08 exp470]]|0.057||
|[[:results:exp329|Hydroxyurea 100μM R07 exp329]]|0.057||
|[[:results:exp439|QNZ 0.01μM R08 exp439]]|0.057||
|[[:results:exp84|UM0125461 0.74μM R02 exp84]]|0.056||
|[[:results:exp474|CR131-b 0.005μM R08 exp474]]|0.055||
|[[:results:exp435|JQ1 0.8μM R08 exp435]]|0.055||
|[[:results:exp82|Torin1 0.08μM R02 exp82]]|0.054||
|[[:results:exp502|Milciclib 2μM R08 exp502]]|0.053||
|[[:results:exp407|Thapsigargin 0.005μM R07 exp407]]|0.053||
|[[:results:exp489|Hippuristanol 0.12μM R08 exp489 no dilution day6]]|0.052||
|[[:results:exp441|GSK-J4 1.5μM R08 exp441]]|0.052||
{{:chemogenomics:comparison_plots:exp25_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp400_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp492_vs_exp85.png?nolink |}}
{{:chemogenomics:comparison_plots:exp492_vs_exp529.png?nolink |}}
{{:chemogenomics:comparison_plots:exp488_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp466_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp290_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp492_vs_exp535.png?nolink |}}
{{:chemogenomics:comparison_plots:exp431_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp342_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp116_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp492_vs_exp497.png?nolink |}}
{{:chemogenomics:comparison_plots:exp492_vs_exp498.png?nolink |}}
{{:chemogenomics:comparison_plots:exp447_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp492_vs_exp65.png?nolink |}}
{{:chemogenomics:comparison_plots:exp359_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp440_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp212_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp492_vs_exp513.png?nolink |}}
{{:chemogenomics:comparison_plots:exp357_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp234_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp445_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp241_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp470_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp329_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp439_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp492_vs_exp84.png?nolink |}}
{{:chemogenomics:comparison_plots:exp474_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp435_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp492_vs_exp82.png?nolink |}}
{{:chemogenomics:comparison_plots:exp492_vs_exp502.png?nolink |}}
{{:chemogenomics:comparison_plots:exp407_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp489_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp441_vs_exp492.png?nolink |}}
^GO Term^Fold Change^Genes^
|regulation of anaphase-promoting complex-dependent catabolic process|443.81|CDK2,PLK1,CDC20|
|regulation of proteasomal ubiquitin-dependent protein catabolic process|21.29|CDK2,PLK1,CDC20,OGT,KEAP1|
|regulation of ubiquitin-dependent protein catabolic process|16.91|CDK2,PLK1,CDC20,OGT,KEAP1|
|regulation of proteasomal protein catabolic process|15.65|CDK2,PLK1,CDC20,OGT,KEAP1|
|transferase complex|6.44|PRKAG1,DERL2,MGA,CDK2,CDC20,POLA1,OGT,YPEL5,KEAP1|
No GO term hits below threshold. (FDR <0.05)