====== Senexin-A 25μM R07 exp400 ======
==== Mechanism of Action ====
Inhibits CDK8, suppresses induction of gene expression
* **Class / Subclass 1:** Signal Transduction / Kinase Inhibitor
* **Class / Subclass 2:** Gene Regulation / Transcription Inhibitor
==== Technical Notes ====
* **PubChem Name:** %%4-(2-Phenylethylamino)quinazoline-6-carbonitrile;hydrochloride%%
* **Synonyms:** N/A
* **CAS #:** 1780390-76-2
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/90488980|90488980]]
* **IUPAC:** %%4-(2-phenylethylamino)quinazoline-6-carbonitrile;hydrochloride%%
* **INCHI Name:** InChI=1S/C17H14N4.ClH/c18-11-14-6-7-16-15(10-14)17(21-12-20-16)19-9-8-13-4-2-1-3-5-13;/h1-7,10,12H,8-9H2,(H,19,20,21);1H
* **INCHI Key:** POENYXHGUHRXFR-UHFFFAOYSA-N
* **Molecular Weight:** 310.8
* **Canonical SMILES:** C1=CC=C(C=C1)CCNC2=NC=NC3=C2C=C(C=C3)C#N.Cl
* **Isomeric SMILES:** N/A
* **Molecular Formula:** C17H15ClN4
{{:chemogenomics:structures:chem-0238.svg?nolink}}
* **Supplier Name:** Tocris Bioscience
* **Catalog #:** 4875
* **Lot #:** N/A
* **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C17H14N4 275.12912; found 275.12926
* **Platform ID:** Senexin_A
* **Min:** -11.6276; **Max:** 42.3607
{{:chemogenomics:dose_response:dr_401.png?nolink&500 |}}
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^ IC ^ Concentration (µM) ^
| IC10 |N/A |
| IC20 |16.7423 |
| IC30 |N/A |
| IC40 |N/A |
| IC50 |N/A |
| IC60 |N/A |
| IC70 |N/A |
| IC80 |N/A |
| IC90 |N/A |
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==== Screen Summary ====
* **Round**: 07
* **Dose**: 25µM
* **Days of incubation**: 8
* **Doublings**: 3.2
* **Numbers of reads**: 22291136
==== 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^
|13/4|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Senexin_A_25uM_Round-7_exp400.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp400.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:S:SNX27|SNX27]]|-4.81|<0.01|
|[[:human_genes:P:PRKAA1|PRKAA1]]|-3.83|<0.01|
|[[:human_genes:G:GOT1|GOT1]]|-3.70|<0.01|
|[[:human_genes:R:RAB10|RAB10]]|-3.30|<0.01|
|[[:human_genes:D:DENND4A|DENND4A]]|-3.15|<0.01|
|[[:human_genes:L:LMAN1L|LMAN1L]]|-2.83|0.03|
|[[:human_genes:B:BCL2|BCL2]]|-2.76|0.01|
|[[:human_genes:C:CCDC22|CCDC22]]|-2.74|0.01|
|[[:human_genes:L:L3MBTL2|L3MBTL2]]|-2.71|0.02|
|[[:human_genes:M:MYSM1|MYSM1]]|-2.69|0.01|
|[[:human_genes:C:CMTM6|CMTM6]]|-2.65|0.02|
|[[:human_genes:M:MGA|MGA]]|-2.58|0.02|
|[[:human_genes:C:COMMD5|COMMD5]]|-2.55|0.02|
|[[:human_genes:Q:QRICH1|QRICH1]]|-2.52|0.11|
|[[:human_genes:S:SLC2A1|SLC2A1]]|-2.40|0.10|
|[[:human_genes:R:RAB7A|RAB7A]]|-2.35|0.07|
|[[:human_genes:A:ARPC4|ARPC4]]|-2.26|0.10|
|[[:human_genes:N:NKX2-5|NKX2-5]]|-2.21|0.19|
|[[:human_genes:P:PBRM1|PBRM1]]|-2.21|0.12|
|[[:human_genes:V:VPS29|VPS29]]|-2.17|0.23|
|[[:human_genes:T:TSC22D1|TSC22D1]]|-2.16|0.15|
|[[:human_genes:C:CDC25A|CDC25A]]|-2.14|0.25|
|[[:human_genes:T:TAZ|TAZ]]|-2.13|0.34|
|[[:human_genes:P:PSTPIP2|PSTPIP2]]|-2.12|0.17|
|[[:human_genes:P:PRKAG1|PRKAG1]]|-2.11|0.18|
|[[:human_genes:I:INTS3|INTS3]]|-2.10|0.37|
|[[:human_genes:K:KIF13A|KIF13A]]|-2.09|0.28|
|[[:human_genes:G:GPAA1|GPAA1]]|-2.08|0.19|
|[[:human_genes:A:ARID1A|ARID1A]]|-2.04|0.34|
|[[:human_genes:P:PRKAR2B|PRKAR2B]]|-2.01|0.26|
|[[:human_genes:S:SLC25A32|SLC25A32]]|2.15|0.22|
|[[:human_genes:S:SHMT2|SHMT2]]|2.17|0.22|
|[[:human_genes:B:BTAF1|BTAF1]]|2.17|0.22|
|[[:human_genes:G:GANAB|GANAB]]|2.17|0.23|
|[[:human_genes:C:CDC45|CDC45]]|2.18|0.37|
|[[:human_genes:S:SSR3|SSR3]]|2.19|0.15|
|[[:human_genes:M:MSI2|MSI2]]|2.20|0.22|
|[[:human_genes:M:MLEC|MLEC]]|2.20|0.22|
|[[:human_genes:A:ATP5B|ATP5B]]|2.21|0.14|
|[[:human_genes:F:FH|FH]]|2.23|0.22|
|[[:human_genes:M:MBD1|MBD1]]|2.24|0.22|
|[[:human_genes:P:PPP6C|PPP6C]]|2.27|0.18|
|[[:human_genes:S:SRD5A3|SRD5A3]]|2.29|0.11|
|[[:human_genes:T:TMEM206|TMEM206]]|2.30|0.11|
|[[:human_genes:I:ISY1|ISY1]]|2.32|0.32|
|[[:human_genes:A:ALG5|ALG5]]|2.33|0.11|
|[[:human_genes:H:HIST1H2AJ|HIST1H2AJ]]|2.36|0.14|
|[[:human_genes:N:NDUFB6|NDUFB6]]|2.36|0.14|
|[[:human_genes:S:SIRT1|SIRT1]]|2.38|0.10|
|[[:human_genes:U:UGP2|UGP2]]|2.38|0.10|
|[[:human_genes:P:PMVK|PMVK]]|2.39|0.10|
|[[:human_genes:G:GPR33|GPR33]]|2.43|0.11|
|[[:human_genes:A:ARGLU1|ARGLU1]]|2.44|0.18|
|[[:human_genes:I:ISY1-RAB43|ISY1-RAB43]]|2.52|0.23|
|[[:human_genes:D:DDX3X|DDX3X]]|2.55|0.06|
|[[:human_genes:E:ECD|ECD]]|2.77|0.24|
|[[:human_genes:A:AP1S1|AP1S1]]|3.02|0.01|
|[[:human_genes:V:VHL|VHL]]|3.06|<0.01|
|[[:human_genes:S:SPI1|SPI1]]|4.05|<0.01|
|[[:human_genes:T:TXNIP|TXNIP]]|4.53|<0.01|
^Screen^Correlation^Plot^
|[[:results:exp492|iCRT14 30μM R08 exp492]]|0.091||
{{:chemogenomics:comparison_plots:exp400_vs_exp492.png?nolink |}}
^GO Term^Fold Change^Genes^
|endocytic recycling|42.64|SNX27,CCDC22,CMTM6,RAB7A,VPS29|
|vesicle-mediated transport to the plasma membrane|34.95|SNX27,RAB10,CCDC22,CMTM6,RAB7A,VPS29,KIF13A|
|endosomal transport|15.88|SNX27,RAB10,CCDC22,CMTM6,RAB7A,VPS29|
No GO term hits below threshold. (FDR <0.05)