====== Geldanamycin 0.015 to 0.05μM on day4 R07 exp317 ======
==== Mechanism of Action ====
HSP90 inhibitor
* **Class / Subclass 1:** Proteostasis / Chaperone Inhibitor
==== Technical Notes ====
* **PubChem Name:** %%Geldanamycin%%
* **Synonyms:** N/A
* **CAS #:** 30562-34-6
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/5288382|5288382]]
* **IUPAC:** %%[(4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13-hydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl] carbamate%%
* **INCHI Name:** InChI=1S/C29H40N2O9/c1-15-11-19-25(34)20(14-21(32)27(19)39-7)31-28(35)16(2)9-8-10-22(37-5)26(40-29(30)36)18(4)13-17(3)24(33)23(12-15)38-6/h8-10,13-15,17,22-24,26,33H,11-12H2,1-7H3,(H2,30,36)(H,31,35)/b10-8-,16-9+,18-13+/t15-,17+,22+,23+,24-,26+/m1/s1
* **INCHI Key:** QTQAWLPCGQOSGP-KSRBKZBZSA-N
* **Molecular Weight:** 560.6
* **Canonical SMILES:** CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)OC)C)OC)OC(=O)N)C)C)O)OC
* **Isomeric SMILES:** C[C@H]1C[C@@H]([C@@H]([C@H](/C=C(/[C@@H]([C@H](/C=C\\C=C(\\C(=O)NC2=CC(=O)C(=C(C1)C2=O)OC)/C)OC)OC(=O)N)\\C)C)O)OC
* **Molecular Formula:** C29H40N2O9
{{:chemogenomics:structures:chem-0140.svg?nolink}}
* **Supplier Name:** Ark Pharm Inc.
* **Catalog #:** AK130527
* **Lot #:** WG0131921-180318001
* **HRMS (ESI-TOF) m/z:** (M+Na)+ Calcd for C29 H40 N2 O9 583.2626; found 583.26208
* **Platform ID:** Geldanamycin
* **Min:** 5.0711; **Max:** 99.6467
{{:chemogenomics:dose_response:dr_428.png?nolink&500 |}}
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^ IC ^ Concentration (µM) ^
| IC10 |N/A |
| IC20 |N/A |
| IC30 |0.0079 |
| IC40 |0.0197 |
| IC50 |0.0440 |
| IC60 |N/A |
| IC70 |N/A |
| IC80 |N/A |
| IC90 |N/A |
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==== Screen Summary ====
* **Round**: 07
* **Dose**: 0.015-0.05µM
* **Days of incubation**: 8
* **Doublings**: 5.4
* **Numbers of reads**: 13571170
==== 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^
|4/10|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Geldanamycin_0.015-0.05day4uM_Round-7_exp317.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp317.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:H:HSP90AA1|HSP90AA1]]|-3.46|<0.01|
|[[:human_genes:S:SEPHS1|SEPHS1]]|-3.19|<0.01|
|[[:human_genes:N:NPIPA2|NPIPA2]]|-3.12|0.19|
|[[:human_genes:N:NPIPA3|NPIPA3]]|-2.77|0.31|
|[[:human_genes:R:RHOA|RHOA]]|-2.67|0.04|
|[[:human_genes:P:PRKAA1|PRKAA1]]|-2.63|0.04|
|[[:human_genes:D:DCAF15|DCAF15]]|-2.62|0.07|
|[[:human_genes:T:TBCD|TBCD]]|-2.55|0.08|
|[[:human_genes:G:GPR75-ASB3|GPR75-ASB3]]|-2.51|0.08|
|[[:human_genes:H:HSP90AB1|HSP90AB1]]|-2.51|0.14|
|[[:human_genes:U:UXS1|UXS1]]|-2.50|0.07|
|[[:human_genes:U:UBE2D3|UBE2D3]]|-2.46|0.07|
|[[:human_genes:T:TCF4|TCF4]]|-2.42|0.08|
|[[:human_genes:P:PTEN|PTEN]]|-2.36|0.08|
|[[:human_genes:C:CRTC3|CRTC3]]|-2.27|0.12|
|[[:human_genes:M:MAPK14|MAPK14]]|-2.24|0.14|
|[[:human_genes:S:SCAF8|SCAF8]]|-2.21|0.14|
|[[:human_genes:C:COX15|COX15]]|-2.19|0.23|
|[[:human_genes:A:ASXL2|ASXL2]]|-2.15|0.24|
|[[:human_genes:C:C7orf55-LUC7L2|C7orf55-LUC7L2]]|-2.14|0.19|
|[[:human_genes:V:VRK2|VRK2]]|-2.14|0.24|
|[[:human_genes:U:USP54|USP54]]|-2.13|0.19|
|[[:human_genes:Z:ZC3H11A|ZC3H11A]]|-2.10|0.21|
|[[:human_genes:R:RSRC2|RSRC2]]|-2.10|0.64|
|[[:human_genes:P:PROSER1|PROSER1]]|-2.07|0.29|
|[[:human_genes:E:ERG|ERG]]|-2.06|0.29|
|[[:human_genes:M:MESDC2|MESDC2]]|-2.06|0.23|
|[[:human_genes:S:SCN8A|SCN8A]]|-2.06|0.29|
|[[:human_genes:T:TNFSF11|TNFSF11]]|-2.05|0.23|
|[[:human_genes:Z:ZNF410|ZNF410]]|-2.05|0.23|
|[[:human_genes:L:LYAR|LYAR]]|2.08|0.25|
|[[:human_genes:A:ACRC|ACRC]]|2.10|0.19|
|[[:human_genes:P:PIH1D1|PIH1D1]]|2.11|0.18|
|[[:human_genes:G:GLYR1|GLYR1]]|2.15|0.16|
|[[:human_genes:P:PSMD7|PSMD7]]|2.16|0.50|
|[[:human_genes:S:SAMD4B|SAMD4B]]|2.18|0.28|
|[[:human_genes:O:OR1L1|OR1L1]]|2.19|0.19|
|[[:human_genes:P:POLE|POLE]]|2.19|0.40|
|[[:human_genes:W:WDR75|WDR75]]|2.19|0.40|
|[[:human_genes:P:PPP3CA|PPP3CA]]|2.25|0.12|
|[[:human_genes:K:KIAA1033|KIAA1033]]|2.30|0.09|
|[[:human_genes:H:HNRNPF|HNRNPF]]|2.31|0.09|
|[[:human_genes:B:BMS1|BMS1]]|2.32|0.19|
|[[:human_genes:M:MLNR|MLNR]]|2.34|0.19|
|[[:human_genes:W:WISP2|WISP2]]|2.35|0.12|
|[[:human_genes:M:MGST1|MGST1]]|2.36|0.12|
|[[:human_genes:S:SMNDC1|SMNDC1]]|2.41|0.17|
|[[:human_genes:R:RPS4X|RPS4X]]|2.46|0.15|
|[[:human_genes:E:EIF3G|EIF3G]]|2.49|0.08|
|[[:human_genes:C:CTNS|CTNS]]|2.50|0.08|
|[[:human_genes:I:IKZF2|IKZF2]]|2.59|0.03|
|[[:human_genes:I:IREB2|IREB2]]|2.93|<0.01|
|[[:human_genes:P:PKD2|PKD2]]|2.93|0.01|
|[[:human_genes:P:PCGF1|PCGF1]]|2.94|<0.01|
|[[:human_genes:C:CBLB|CBLB]]|3.00|0.02|
|[[:human_genes:E:ELF1|ELF1]]|3.09|<0.01|
|[[:human_genes:S:SF3A1|SF3A1]]|3.09|0.03|
|[[:human_genes:C:CYB561A3|CYB561A3]]|3.09|<0.01|
|[[:human_genes:P:PDS5B|PDS5B]]|3.33|<0.01|
|[[:human_genes:C:CISD1|CISD1]]|3.65|<0.01|
^Screen^Correlation^Plot^
|[[:results:exp242|Radicicol 0.16μM R05 exp242]]|0.071||
|[[:results:exp30|Rapamycin 10μM R00 exp30]]|0.054||
|[[:results:exp316|Geldanamycin 0.015 to 0.025μM on day4 R07 exp316]]|0.168||
{{:chemogenomics:comparison_plots:exp242_vs_exp317.png?nolink |}}
{{:chemogenomics:comparison_plots:exp30_vs_exp317.png?nolink |}}
{{:chemogenomics:comparison_plots:exp316_vs_exp317.png?nolink |}}
No GO term hits below threshold. (FDR <0.05)
No GO term hits below threshold. (FDR <0.05)