====== Dorsomorphin 5μM R07 exp357 ====== ==== Mechanism of Action ==== Putative inhibitor of AMPK and BMP signalling * **Class / Subclass 1:** Signal Transduction / Kinase Inhibitor ==== Technical Notes ==== * **PubChem Name:** %%Dorsomorphin%% * **Synonyms:** BML-275; Compound C * **CAS #:** 866405-64-3 * **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/11524144|11524144]] * **IUPAC:** %%6-[4-(2-piperidin-1-ylethoxy)phenyl]-3-pyridin-4-ylpyrazolo[1,5-a]pyrimidine%% * **INCHI Name:** InChI=1S/C24H25N5O/c1-2-12-28(13-3-1)14-15-30-22-6-4-19(5-7-22)21-16-26-24-23(17-27-29(24)18-21)20-8-10-25-11-9-20/h4-11,16-18H,1-3,12-15H2 * **INCHI Key:** XHBVYDAKJHETMP-UHFFFAOYSA-N * **Molecular Weight:** 399.5 * **Canonical SMILES:** C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3 * **Isomeric SMILES:** N/A * **Molecular Formula:** C24H25N5O {{:chemogenomics:structures:chem-0212.svg?nolink}} * **Supplier Name:** Ark Pharm Inc. * **Catalog #:** AK-88052 * **Lot #:** YF0257195-170620001 * **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C24H25N5O 400.21319; found 400.21387 * **Platform ID:** Dorsomorphin * **Min:** 1.3456; **Max:** 94.1274 {{:chemogenomics:dose_response:dr_427.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |N/A | | IC20 |1.5365 | | IC30 |2.2301 | | IC40 |3.0231 | | IC50 |4.0073 | | IC60 |N/A | | IC70 |N/A | | IC80 |N/A | | IC90 |N/A | \\ ==== Screen Summary ==== * **Round**: 07 * **Dose**: 5µM * **Days of incubation**: 8 * **Doublings**: 1.0 * **Numbers of reads**: 16049330 ==== 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^ |21/17|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Dorsomorphin_5uM_Round-7_exp357.txt|Scores]]|||||| {{:chemogenomics:cranks_plots:exp357.png?nolink}} ^Gene^CRANKS Score^FDR^ |[[:human_genes:P:PRAMEF25|PRAMEF25]]|-4.24|0.03| |[[:human_genes:P:PRAMEF26|PRAMEF26]]|-4.20|0.03| |[[:human_genes:B:BCL2|BCL2]]|-3.99|<0.01| |[[:human_genes:R:RANBP1|RANBP1]]|-3.54|<0.01| |[[:human_genes:C:CLK3|CLK3]]|-3.28|<0.01| |[[:human_genes:P:PDS5B|PDS5B]]|-3.15|<0.01| |[[:human_genes:K:KIF20A|KIF20A]]|-3.05|<0.01| |[[:human_genes:Z:ZNF451|ZNF451]]|-2.96|<0.01| |[[:human_genes:A:ARL1|ARL1]]|-2.93|<0.01| |[[:human_genes:N:NRAS|NRAS]]|-2.86|0.01| |[[:human_genes:A:ATP6V0A2|ATP6V0A2]]|-2.77|0.02| |[[:human_genes:L:LIG4|LIG4]]|-2.73|0.02| |[[:human_genes:S:SCAF1|SCAF1]]|-2.72|0.22| |[[:human_genes:D:DCLRE1C|DCLRE1C]]|-2.67|0.01| |[[:human_genes:T:TCF4|TCF4]]|-2.65|0.01| |[[:human_genes:P:PUS7|PUS7]]|-2.58|0.03| |[[:human_genes:M:MAD2L2|MAD2L2]]|-2.57|0.02| |[[:human_genes:P:PSME3|PSME3]]|-2.56|0.02| |[[:human_genes:R:RRM2B|RRM2B]]|-2.46|0.03| |[[:human_genes:C:C1orf68|C1orf68]]|-2.42|0.03| |[[:human_genes:E:EDF1|EDF1]]|-2.42|0.03| |[[:human_genes:S:SMG1|SMG1]]|-2.39|0.04| |[[:human_genes:O:OTUB1|OTUB1]]|-2.36|0.07| |[[:human_genes:H:HIST1H1B|HIST1H1B]]|-2.32|0.05| |[[:human_genes:N:NELFA|NELFA]]|-2.32|0.07| |[[:human_genes:K:KCNJ2|KCNJ2]]|-2.29|0.06| |[[:human_genes:I:INCENP|INCENP]]|-2.29|0.21| |[[:human_genes:I:IGLL1|IGLL1]]|-2.28|0.06| |[[:human_genes:M:MAD2L1|MAD2L1]]|-2.28|0.06| |[[:human_genes:Y:YPEL5|YPEL5]]|-2.25|0.06| |[[:human_genes:B:BRWD1|BRWD1]]|2.20|0.09| |[[:human_genes:K:KCTD5|KCTD5]]|2.21|0.09| |[[:human_genes:S:SLC7A1|SLC7A1]]|2.22|0.12| |[[:human_genes:C:C15orf41|C15orf41]]|2.25|0.07| |[[:human_genes:C:CYCS|CYCS]]|2.28|0.06| |[[:human_genes:M:MRPL23|MRPL23]]|2.29|0.06| |[[:human_genes:S:SART1|SART1]]|2.31|0.35| |[[:human_genes:L:LARP1|LARP1]]|2.33|0.09| |[[:human_genes:T:TFAP4|TFAP4]]|2.34|0.05| |[[:human_genes:L:LOC100505679|LOC100505679]]|2.35|0.44| |[[:human_genes:D:DGKD|DGKD]]|2.41|0.04| |[[:human_genes:E:EIF4A1|EIF4A1]]|2.42|0.06| |[[:human_genes:O:OAZ1|OAZ1]]|2.43|0.04| |[[:human_genes:S:SMEK1|SMEK1]]|2.44|0.04| |[[:human_genes:P:PPA1|PPA1]]|2.57|0.07| |[[:human_genes:K:KLF16|KLF16]]|2.64|0.06| |[[:human_genes:E:EBF1|EBF1]]|2.70|0.02| |[[:human_genes:S:SERF2|SERF2]]|2.71|<0.01| |[[:human_genes:S:SETDB1|SETDB1]]|2.74|0.04| |[[:human_genes:C:CRLS1|CRLS1]]|2.90|<0.01| |[[:human_genes:U:UBQLN1|UBQLN1]]|3.17|0.00| |[[:human_genes:L:LCMT1|LCMT1]]|3.32|0.00| |[[:human_genes:M:MARCH5|MARCH5]]|3.39|0.00| |[[:human_genes:A:APAF1|APAF1]]|3.47|0.00| |[[:human_genes:V:VDAC2|VDAC2]]|3.48|0.00| |[[:human_genes:P:PLAA|PLAA]]|3.75|0.00| |[[:human_genes:T:TAZ|TAZ]]|4.36|0.00| |[[:human_genes:M:MLST8|MLST8]]|4.92|0.00| |[[:human_genes:B:BAK1|BAK1]]|5.23|0.00| |[[:human_genes:T:TOP2B|TOP2B]]|7.21|0.00| ^Screen^Correlation^Plot^ |[[:results:exp80|RO-3307 4.7μM R02 exp80]]|0.09|| |[[:results:exp485|GSK626616 14μM R08 exp485]]|0.089|| |[[:results:exp502|Milciclib 2μM R08 exp502]]|0.088|| |[[:results:exp478|Doxorubicin 0.02μM R08 exp478]]|0.084|| |[[:results:exp488|Hippuristanol 0.12μM R08 exp488]]|0.084|| |[[:results:exp503|Mitomycin-C 0.06μM R08 exp503]]|0.083|| |[[:results:exp240|Pyridostatin 4μM R05 exp240]]|0.083|| |[[:results:exp524|Staurosporine 0.02μM R08 exp524]]|0.079|| |[[:results:exp85|UM0129480 7μM R02 exp85]]|0.079|| |[[:results:exp489|Hippuristanol 0.12μM R08 exp489 no dilution day6]]|0.077|| |[[:results:exp435|JQ1 0.8μM R08 exp435]]|0.075|| |[[:results:exp199|Etoposide 0.3μM R05 exp199]]|0.072|| |[[:results:exp517|Quercetin 20μM R08 exp517]]|0.071|| |[[:results:exp28|Pimelic-diphenylamide-106 5μM R00 exp28]]|0.071|| |[[:results:exp512|Olaparib 4μM R08 exp512]]|0.069|| |[[:results:exp135|MS023 7μM R03 exp135]]|0.069|| |[[:results:exp492|iCRT14 30μM R08 exp492]]|0.06|| |[[:results:exp329|Hydroxyurea 100μM R07 exp329]]|0.06|| |[[:results:exp443|SNS-032 15μM R08 exp443]]|0.058|| |[[:results:exp515|PU-H71 1μM R08 exp515]]|0.056|| |[[:results:exp38|Wortmannin 5μM R00 exp38]]|0.056|| |[[:results:exp360|Genistein 15μM R07 exp360]]|0.056|| |[[:results:exp407|Thapsigargin 0.005μM R07 exp407]]|0.055|| |[[:results:exp34|Rotenone 20μM R00 exp34]]|0.055|| |[[:results:exp527|Tanespimycin 14μM R08 exp527]]|0.053|| |[[:results:exp531|THZ1 0.06μM R08 exp531]]|0.052|| |[[:results:exp529|Thimerosal 0.85μM R08 exp529]]|0.051|| |[[:results:exp440|Aphidicolin 0.4μM R08 exp440]]|0.085|| |[[:results:exp456|Benzoate 20000μM R08 exp456]]|0.085|| |[[:results:exp3|Actinomycin-D 0.001μM R00 exp3]]|0.078|| |[[:results:exp259|6-Thio-2-deoxyguanosine 2μM R06 exp259]]|0.076|| |[[:results:exp474|CR131-b 0.005μM R08 exp474]]|0.075|| |[[:results:exp459|Bleomycin 5μM R08 exp459]]|0.07|| |[[:results:exp67|BVD-523 15μM R02 exp67]]|0.07|| |[[:results:exp343|Centrinone 0.5μM R07 exp343]]|0.065|| |[[:results:exp445|∆-9-Tetrahydrocannabinol 30μM R08 exp445]]|0.062|| |[[:results:exp116|AICAR 240μM R03 exp116]]|0.059|| |[[:results:exp355|Dinaciclib 0.007μM R07 exp355]]|0.056|| |[[:results:exp460|BML-284 0.09μM R08 exp460]]|0.055|| |[[:results:exp2|5-Fluorouracil 20μM R00 exp2]]|0.054|| |[[:results:exp468|CB-5083 0.4μM R08 exp468]]|0.053|| |[[:results:exp330|5-Azacytidine 2μM R07 exp330]]|0.053|| |[[:results:exp466|Cannabidiol 20μM R08 exp466]]|0.052|| |[[:results:exp7|Bortezomib 0.05μM R00 exp7]]|0.051|| {{:chemogenomics:comparison_plots:exp357_vs_exp80.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp485.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp502.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp478.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp488.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp503.png?nolink |}} {{:chemogenomics:comparison_plots:exp240_vs_exp357.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp85.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp489.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp435.png?nolink |}} {{:chemogenomics:comparison_plots:exp199_vs_exp357.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp517.png?nolink |}} {{:chemogenomics:comparison_plots:exp28_vs_exp357.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp512.png?nolink |}} {{:chemogenomics:comparison_plots:exp135_vs_exp357.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp492.png?nolink |}} {{:chemogenomics:comparison_plots:exp329_vs_exp357.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp443.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp515.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp38.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp360.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp407.png?nolink |}} {{:chemogenomics:comparison_plots:exp34_vs_exp357.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp527.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp531.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp529.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp440.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp456.png?nolink |}} {{:chemogenomics:comparison_plots:exp3_vs_exp357.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp357.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp474.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp459.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp67.png?nolink |}} {{:chemogenomics:comparison_plots:exp343_vs_exp357.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp445.png?nolink |}} {{:chemogenomics:comparison_plots:exp116_vs_exp357.png?nolink |}} {{:chemogenomics:comparison_plots:exp355_vs_exp357.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp460.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp357.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp468.png?nolink |}} {{:chemogenomics:comparison_plots:exp330_vs_exp357.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp466.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp7.png?nolink |}} ^GO Term^Fold Change^Genes^ |regulation of mitotic cell cycle phase transition|11.48|BCL2,MAD2L2,PSME3,RRM2B,INCENP,MAD2L1| |DNA damage response|6.88|BCL2,PDS5B,LIG4,DCLRE1C,MAD2L2,RRM2B,SMG1,OTUB1| ^GO Term^Fold Change^Genes^ |mitochondrial membrane|7.04|BAK1,VDAC2,MARCHF5,CRLS1,MRPL23,CYCS,ROMO1,MTG2,PMAIP1| |mitochondrial envelope|6.61|BAK1,VDAC2,MARCHF5,CRLS1,MRPL23,CYCS,ROMO1,MTG2,PMAIP1|