ikarugamyin

An antiprotozoal antibiotic found to inhibit cholesteryl ester accumulation in macrophage. Shown to be efficient inhibitor of clathrin-dependent endocytosis.

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Source SMILES: standardizedunstandardized
Compound:
Screen ID SGTC_463
Screen concentration 104.0 μM
Source ICCB bioactive library
PubChem CID 54714554
SMILES CCC1C(CC2C1C=CC3C2CC4C3CC=CC(=O)NCCCC5C(=O)C(=C(C=C4)O)C(=O)N5)C
Standardized SMILES CCC1C(C)CC2C3CC4C=CC(=C5C(=O)NC(CCCNC(=O)C=CCC4C3C=CC12)C5=O)O
Molecular weight 478.623
ALogP 3.67
H-bond donor count 3
H-bond acceptor count 4
Response signature

Pool Growth Kinetics
% growth inhibition (Het. pool) 3.68
% growth inhibition (Hom. pool) 1.53


HIP profile

Heterozygous deletion strains
Scale: fixedexpanded
Heterozygous profile for 54714554
Download HIP data (tab-delimited text)  (excel)

HOP profile

Homozygous deletion strains
Scale: fixedexpanded
Homozygous profile for 54714554
Download HOP data (tab-delimited text)  (excel)
Gene:ATC1(YDR184C)|FD-Score:3.97|P-value:3.60E-5||SGD DESC:Nuclear protein; possibly involved in regulation of cation stress responses and/or in the establishment of bipolar budding pattern; relative distribution to the nucleus decreases upon DNA replication stress Gene:CSF1(YLR087C)|FD-Score:-3.46|P-value:2.74E-4||SGD DESC:Protein required for fermentation at low temperature; the authentic, non-tagged protein is detected in highly purified mitochondria in high-throughput studies Gene:EDS1(YBR033W_p)|FD-Score:3.23|P-value:6.22E-4||SGD DESC:Putative zinc cluster protein, predicted to be a transcription factor; not an essential gene; EDS1 has a paralog, RGT1, that arose from the whole genome duplication Gene:LCB3(YJL134W)|FD-Score:3.12|P-value:8.98E-4||SGD DESC:Long-chain base-1-phosphate phosphatase; specific for dihydrosphingosine-1-phosphate, regulates ceramide and long-chain base phosphates levels, involved in incorporation of exogenous long chain bases in sphingolipids; LCB3 has a paralog, YSR3, that arose from the whole genome duplication Gene:NYV1(YLR093C)|FD-Score:3.13|P-value:8.79E-4||SGD DESC:v-SNARE component of the vacuolar SNARE complex involved in vesicle fusion; inhibits ATP-dependent Ca(2+) transport activity of Pmc1p in the vacuolar membrane Gene:PIB1(YDR313C)|FD-Score:3.4|P-value:3.41E-4||SGD DESC:RING-type ubiquitin ligase of the endosomal and vacuolar membranes, binds phosphatidylinositol(3)-phosphate; contains a FYVE finger domain Gene:RFU1(YLR073C)|FD-Score:3.54|P-value:1.96E-4||SGD DESC:Protein that inhibits Doa4p deubiquitinating activity; contributes to ubiquitin homeostasis by regulating the conversion of free ubiquitin chains to ubiquitin monomers by Doa4p; GFP-fusion protein localizes to endosomes Gene:SUR2(YDR297W)|FD-Score:29.4|P-value:5.93E-190||SGD DESC:Sphinganine C4-hydroxylase, catalyses the conversion of sphinganine to phytosphingosine in sphingolipid biosyntheis Gene:YGR168C(YGR168C_p)|FD-Score:3.27|P-value:5.46E-4||SGD DESC:Putative protein of unknown function; YGR168C is not an essential gene Gene:ATC1(YDR184C)|FD-Score:3.97|P-value:3.60E-5||SGD DESC:Nuclear protein; possibly involved in regulation of cation stress responses and/or in the establishment of bipolar budding pattern; relative distribution to the nucleus decreases upon DNA replication stress Gene:CSF1(YLR087C)|FD-Score:-3.46|P-value:2.74E-4||SGD DESC:Protein required for fermentation at low temperature; the authentic, non-tagged protein is detected in highly purified mitochondria in high-throughput studies Gene:EDS1(YBR033W_p)|FD-Score:3.23|P-value:6.22E-4||SGD DESC:Putative zinc cluster protein, predicted to be a transcription factor; not an essential gene; EDS1 has a paralog, RGT1, that arose from the whole genome duplication Gene:LCB3(YJL134W)|FD-Score:3.12|P-value:8.98E-4||SGD DESC:Long-chain base-1-phosphate phosphatase; specific for dihydrosphingosine-1-phosphate, regulates ceramide and long-chain base phosphates levels, involved in incorporation of exogenous long chain bases in sphingolipids; LCB3 has a paralog, YSR3, that arose from the whole genome duplication Gene:NYV1(YLR093C)|FD-Score:3.13|P-value:8.79E-4||SGD DESC:v-SNARE component of the vacuolar SNARE complex involved in vesicle fusion; inhibits ATP-dependent Ca(2+) transport activity of Pmc1p in the vacuolar membrane Gene:PIB1(YDR313C)|FD-Score:3.4|P-value:3.41E-4||SGD DESC:RING-type ubiquitin ligase of the endosomal and vacuolar membranes, binds phosphatidylinositol(3)-phosphate; contains a FYVE finger domain Gene:RFU1(YLR073C)|FD-Score:3.54|P-value:1.96E-4||SGD DESC:Protein that inhibits Doa4p deubiquitinating activity; contributes to ubiquitin homeostasis by regulating the conversion of free ubiquitin chains to ubiquitin monomers by Doa4p; GFP-fusion protein localizes to endosomes Gene:SUR2(YDR297W)|FD-Score:29.4|P-value:5.93E-190||SGD DESC:Sphinganine C4-hydroxylase, catalyses the conversion of sphinganine to phytosphingosine in sphingolipid biosyntheis Gene:YGR168C(YGR168C_p)|FD-Score:3.27|P-value:5.46E-4||SGD DESC:Putative protein of unknown function; YGR168C is not an essential gene

Click on Significant Values for Strain Details

Top 15 HET fitness defect scores (HIP)

Download all HIP Data (tab-delimited text)  (excel)
Deletion Strain FD score P-value Clearance Gene Gene Description
YOL144W2.700.003440.21NOP8Nucleolar protein required for 60S ribosomal subunit biogenesis
YDL153C2.570.005140.21SAS10Essential subunit of U3-containing Small Subunit (SSU) processome complex involved in production of 18S rRNA and assembly of small ribosomal subunit; disrupts silencing when overproduced; mutant has increased aneuploidy tolerance
YJL086C_d2.360.009160.02YJL086C_dDubious open reading frame unlikely to encode a protein, based on available experimental and comparative sequence data; partially overlaps the verified genes YJL085W/EXO70 and YJL087C/TRL1
YDL195W2.340.009600.15SEC31Component of the Sec13p-Sec31p complex of the COPII vesicle coat, required for vesicle formation in ER to Golgi transport; mutant has increased aneuploidy tolerance
YDL008W2.190.014100.07APC11Catalytic core subunit of the Anaphase-Promoting Complex/Cyclosome (APC/C), which is a ubiquitin-protein ligase required for degradation of anaphase inhibitors, including mitotic cyclins, during the metaphase/anaphase transition; contains a RING-H2 domain that is required for activity
YLR140W_d2.120.017000.01YLR140W_dDubious open reading frame unlikely to encode a functional protein; overlaps essential RRN5 gene which encodes a member of the UAF transcription factor involved in transcription of rDNA by RNA polymerase I
YGR120C2.110.017400.04COG2Essential component of the conserved oligomeric Golgi complex (Cog1p through Cog8p), a cytosolic tethering complex that functions in protein trafficking to mediate fusion of transport vesicles to Golgi compartments
YEL034W2.070.019400.01HYP2Translation elongation factor eIF-5A; may function in translation initiation; structural homolog of bacterial EF-P; undergoes an essential hypusination modification; HYP2 has a paralog, ANB1, that arose from the whole genome duplication
YGR094W2.060.019900.02VAS1Mitochondrial and cytoplasmic valyl-tRNA synthetase
YGL171W2.040.020700.01ROK1RNA-dependent ATPase; involved in pre-rRNA processing at sites A0, A1, and A2, and in control of cell cycle progression; contains two upstream open reading frames (uORFs) in 5' untranslated region which regulate translation
YLR141W2.030.021300.03RRN5Protein involved in transcription of rDNA by RNA polymerase I; transcription factor, member of UAF (upstream activation factor) family along with Rrn9p and Rrn10p
YGL123W2.000.023000.05RPS2Protein component of the small (40S) subunit; essential for control of translational accuracy; phosphorylation by C-terminal domain kinase I (CTDK-I) enhances translational accuracy; methylated on one or more arginine residues by Hmt1p; homologous to mammalian ribosomal protein S2 and bacterial S5
YLR459W1.950.025700.01GAB1GPI transamidase subunit, involved in attachment of glycosylphosphatidylinositol (GPI) anchors to proteins; may have a role in recognition of the attachment signal or of the lipid portion of GPI
YGL092W1.940.026200.04NUP145Essential protein with distinct roles in two nuclear pore subcomplexes; catalyzes its own proteolytic cleavage in vivo to generate a C-terminal fragment that is a structural component of the Nup84p subcomplex (with roles in NPC biogenesis and localization of genes to the nuclear periphery), and an N-terminal fragment that is one of several FG-nucleoporins within the NPC central core directly responsible for nucleocytoplasmic transport; homologous to human NUP98
YGR048W1.900.028500.01UFD1Substrate-recruiting cofactor of the Cdc48p-Npl4p-Ufd1p segregase; polyubiquitin binding protein that assists in the dislocation of misfolded, ERAD substrates that are subsequently delivered to the proteasome for degradation; involved in regulated destruction of ER membrane proteins such as HMG-CoA reductase (Hmg1/2p) and cytoplasmic proteins (Fbp1p); involved in mobilizing membrane bound transaction factors by regulated Ub/proteasome-dependent processing (RUP)

Top 15 HOM fitness defect scores (HOP)

Download all HOP Data (tab-delimited text)  (excel)
Deletion Strain FD score P-value Gene Gene Description
YDR297W29.405.93E-190SUR2Sphinganine C4-hydroxylase, catalyses the conversion of sphinganine to phytosphingosine in sphingolipid biosyntheis
YDR184C3.973.60E-5ATC1Nuclear protein; possibly involved in regulation of cation stress responses and/or in the establishment of bipolar budding pattern; relative distribution to the nucleus decreases upon DNA replication stress
YLR073C3.541.96E-4RFU1Protein that inhibits Doa4p deubiquitinating activity; contributes to ubiquitin homeostasis by regulating the conversion of free ubiquitin chains to ubiquitin monomers by Doa4p; GFP-fusion protein localizes to endosomes
YDR313C3.403.41E-4PIB1RING-type ubiquitin ligase of the endosomal and vacuolar membranes, binds phosphatidylinositol(3)-phosphate; contains a FYVE finger domain
YGR168C_p3.275.46E-4YGR168C_pPutative protein of unknown function; YGR168C is not an essential gene
YBR033W_p3.236.22E-4EDS1_pPutative zinc cluster protein, predicted to be a transcription factor; not an essential gene; EDS1 has a paralog, RGT1, that arose from the whole genome duplication
YLR093C3.138.79E-4NYV1v-SNARE component of the vacuolar SNARE complex involved in vesicle fusion; inhibits ATP-dependent Ca(2+) transport activity of Pmc1p in the vacuolar membrane
YJL134W3.128.98E-4LCB3Long-chain base-1-phosphate phosphatase; specific for dihydrosphingosine-1-phosphate, regulates ceramide and long-chain base phosphates levels, involved in incorporation of exogenous long chain bases in sphingolipids; LCB3 has a paralog, YSR3, that arose from the whole genome duplication
YGL202W3.080.00104ARO8Aromatic aminotransferase I, expression is regulated by general control of amino acid biosynthesis
YGL168W3.080.00105HUR1Protein of unknown function; reported null mutant phenotype of hydroxyurea sensitivity may be due to effects on overlapping PMR1 gene
YGL222C3.070.00106EDC1RNA-binding protein that activates mRNA decapping directly; binds to the mRNA substrate and enhances the activity of the decapping proteins Dcp1p and Dcp2p; has a role in translation during heat stress; protein becomes more abundant and forms cytoplasmic foci in response to DNA replication stress
YEL050C3.050.00116RML2Mitochondrial ribosomal protein of the large subunit, has similarity to E. coli L2 ribosomal protein; fat21 mutant allele causes inability to utilize oleate and may interfere with activity of the Adr1p transcription factor
YGL108C_p3.010.00130YGL108C_pProtein of unknown function, predicted to be palmitoylated; green fluorescent protein (GFP)-fusion protein localizes to the cell periphery; protein abundance increases in response to DNA replication stress
YER183C2.980.00145FAU15,10-methenyltetrahydrofolate synthetase, involved in folic acid biosynthesis
YER161C2.960.00155SPT2Protein involved in negative regulation of transcription; required for RNA polyadenylation; exhibits regulated interactions with both histones and SWI-SNF components, has similarity to mammalian HMG1 proteins

GO enrichment analysis for SGTC_463
No biological processes are significantly enriched (FDR < 0.1).

No protein complexes are significantly enriched (FDR < 0.1).

Coinhibitory screens
Download Coinhibition data (tab-delimited text)  (excel)

Correlation pval Screen ID Condition Source PubChem
CID
Tanimoto
Score
Response
Signature
0.3862.15E-209SGTC_2618avocadyne 43.4 μMMicrosource (Natural product library)3015189NA
0.2094.46E-59SGTC_2524avocatin b 10.6 μMMicrosource (Natural product library)6710748NA
0.1739.64E-41SGTC_27937325131 81.8 μMChembridge (Drug-like library)4176441NA
0.1577.08E-34SGTC_1687st020778 55.4 μMTimTec (Natural product derivative library)4259299NA
0.1461.10E-29SGTC_457grayanotoxin iii 135.0 μMICCB bioactive library46864190NA
0.1223.38E-21SGTC_30039075612 71.4 μMChembridge (Drug-like library)6501993NA
0.1219.11E-21SGTC_31309127414 49.5 μMChembridge (Drug-like library)1494646NA
0.1171.69E-19SGTC_2521angolensin 13.4 μMMicrosource (Natural product library)821428NA
0.1102.34E-17SGTC_13381486-1223 76.0 μMChemDiv (Drug-like library)3444526NA
0.1041.16E-15SGTC_2683piperine 63.0 μMTimTec (Pure natural product library)638024NA
0.1024.78E-15SGTC_20735212005 126.0 μMChembridge (Fragment library)691789NA
0.0952.64E-13SGTC_13591582-0056 520.0 nMChemDiv (Drug-like library)3661189NA
0.0944.25E-13SGTC_30009075062 71.4 μMChembridge (Drug-like library)17057871NA
0.0904.95E-12SGTC_2502avocadyne acetate 18.6 μMMicrosource (Natural product library)3952079NA
0.0881.04E-11SGTC_2581avocatin a 64.0 μMMicrosource (Natural product library)6710728NAsphingolipid biosynthesis & PDR1

Screens with compounds having similar structures
Screen ID Chemical Concentration Tanimoto Score PubChem ID Source Molecular Weight AlogP H-bond
donor
count
H-bond
acceptor
count
Response
Signature