9137475

6-(4-methylphenyl)-2-methylsulfanyl-6,7-dihydro-5H-[1,2,4]triazolo[5,1-b]quinazolin-8-one

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Source SMILES: standardizedunstandardized
Compound:
Screen ID SGTC_3261
Screen concentration 49.5 μM
Source Chembridge (Drug-like library)
PubChem CID 17027690
SMILES CC1=CC=C(C=C1)C2CC3=NC4=NC(=NN4C=C3C(=O)C2)SC
Standardized SMILES CSc1nc2nc3CC(CC(=O)c3cn2n1)c4ccc(C)cc4
Molecular weight 324.4001
ALogP 3.6
H-bond donor count 0
H-bond acceptor count 5
Response signature RPP1 & pyrimidine depletion

Pool Growth Kinetics
% growth inhibition (Het. pool) 6.29
% growth inhibition (Hom. pool) 1.31


HIP profile

Heterozygous deletion strains
Scale: fixedexpanded
Heterozygous profile for 17027690
Download HIP data (tab-delimited text)  (excel)
Gene:CCT6(YDR188W)|FD-Score:-3.52|P-value:2.13E-4|Clearance:0||SGD DESC:Subunit of the cytosolic chaperonin Cct ring complex, related to Tcp1p, essential protein that is required for the assembly of actin and tubulins in vivo; contains an ATP-binding motif Gene:NOP15(YNL110C)|FD-Score:-4.36|P-value:6.63E-6|Clearance:0||SGD DESC:Constituent of 66S pre-ribosomal particles, involved in 60S ribosomal subunit biogenesis; localizes to both nucleolus and cytoplasm Gene:RPP1(YHR062C)|FD-Score:7.79|P-value:3.39E-15|Clearance:4.81||SGD DESC:Subunit of both RNase MRP and nuclear RNase P; RNase MRP cleaves pre-rRNA, while nuclear RNase P cleaves tRNA precursors to generate mature 5' ends and facilitates turnover of nuclear RNAs Gene:CCT6(YDR188W)|FD-Score:-3.52|P-value:2.13E-4|Clearance:0||SGD DESC:Subunit of the cytosolic chaperonin Cct ring complex, related to Tcp1p, essential protein that is required for the assembly of actin and tubulins in vivo; contains an ATP-binding motif Gene:NOP15(YNL110C)|FD-Score:-4.36|P-value:6.63E-6|Clearance:0||SGD DESC:Constituent of 66S pre-ribosomal particles, involved in 60S ribosomal subunit biogenesis; localizes to both nucleolus and cytoplasm Gene:RPP1(YHR062C)|FD-Score:7.79|P-value:3.39E-15|Clearance:4.81||SGD DESC:Subunit of both RNase MRP and nuclear RNase P; RNase MRP cleaves pre-rRNA, while nuclear RNase P cleaves tRNA precursors to generate mature 5' ends and facilitates turnover of nuclear RNAs

HOP profile

Homozygous deletion strains
Scale: fixedexpanded
Homozygous profile for 17027690
Download HOP data (tab-delimited text)  (excel)
Gene:DUG2(YBR281C)|FD-Score:3.42|P-value:3.18E-4||SGD DESC:Component of glutamine amidotransferase (GATase II); forms a complex with Dug3p to degrade glutathione (GSH) and other peptides containing a gamma-glu-X bond in an alternative pathway to GSH degradation by gamma-glutamyl transpeptidase (Ecm38p) Gene:FRE7(YOL152W)|FD-Score:-3.16|P-value:7.90E-4||SGD DESC:Putative ferric reductase with similarity to Fre2p; expression induced by low copper levels Gene:GCV2(YMR189W)|FD-Score:3.1|P-value:9.79E-4||SGD DESC:P subunit of the mitochondrial glycine decarboxylase complex, required for the catabolism of glycine to 5,10-methylene-THF; expression is regulated by levels of 5,10-methylene-THF in the cytoplasm Gene:GOS1(YHL031C)|FD-Score:3.34|P-value:4.26E-4||SGD DESC:v-SNARE protein involved in Golgi transport, homolog of the mammalian protein GOS-28/GS28 Gene:GPT2(YKR067W)|FD-Score:-3.58|P-value:1.71E-4||SGD DESC:Glycerol-3-phosphate/dihydroxyacetone phosphate dual substrate-specific sn-1 acyltransferase located in lipid particles and the ER; involved in the stepwise acylation of glycerol-3-phosphate and dihydroxyacetone in lipid biosynthesis; the most conserved motifs and functionally relevant residues are oriented towards the ER lumen Gene:MRPL35(YDR322W)|FD-Score:-3.53|P-value:2.07E-4||SGD DESC:Mitochondrial ribosomal protein of the large subunit Gene:MRS3(YJL133W)|FD-Score:3.44|P-value:2.88E-4||SGD DESC:Iron transporter, mediates Fe2+ transport across inner mito membrane; mitochondrial carrier family member; active under low-iron conditions; may transport other cations; MRS3 has a paralog, MRS4, that arose from the whole genome duplication Gene:SCP160(YJL080C)|FD-Score:3.38|P-value:3.65E-4||SGD DESC:Essential RNA-binding G protein effector of mating response pathway, mainly associated with nuclear envelope and ER, interacts in mRNA-dependent manner with translating ribosomes via multiple KH domains, similar to vertebrate vigilins Gene:SLM2(YNL047C)|FD-Score:-3.31|P-value:4.67E-4||SGD DESC:Phosphoinositide PI4,5P(2) binding protein, forms a complex with Slm1p; acts downstream of Mss4p in a pathway regulating actin cytoskeleton organization in response to stress; phosphorylated by the TORC2 complex; SLM2 has a paralog, SLM1, that arose from the whole genome duplication Gene:SSU1(YPL092W)|FD-Score:-3.22|P-value:6.46E-4||SGD DESC:Plasma membrane sulfite pump involved in sulfite metabolism and required for efficient sulfite efflux; major facilitator superfamily protein Gene:SUR4(YLR372W)|FD-Score:4.17|P-value:1.52E-5||SGD DESC:Elongase, involved in fatty acid and sphingolipid biosynthesis; synthesizes very long chain 20-26-carbon fatty acids from C18-CoA primers; involved in regulation of sphingolipid biosynthesis Gene:TUF1(YOR187W)|FD-Score:-3.38|P-value:3.61E-4||SGD DESC:Mitochondrial translation elongation factor Tu; comprises both GTPase and guanine nucleotide exchange factor activities, while these activities are found in separate proteins in S. pombe and humans Gene:VMA5(YKL080W)|FD-Score:-3.48|P-value:2.47E-4||SGD DESC:Subunit C of the eight-subunit V1 peripheral membrane domain of vacuolar H+-ATPase (V-ATPase), an electrogenic proton pump found throughout the endomembrane system; required for the V1 domain to assemble onto the vacuolar membrane Gene:YHI9(YHR029C)|FD-Score:-3.7|P-value:1.06E-4||SGD DESC:Protein of unknown function; null mutant is defective in unfolded protein response; possibly involved in a membrane regulation metabolic pathway; member of the PhzF superfamily, though most likely not involved in phenazine production Gene:DUG2(YBR281C)|FD-Score:3.42|P-value:3.18E-4||SGD DESC:Component of glutamine amidotransferase (GATase II); forms a complex with Dug3p to degrade glutathione (GSH) and other peptides containing a gamma-glu-X bond in an alternative pathway to GSH degradation by gamma-glutamyl transpeptidase (Ecm38p) Gene:FRE7(YOL152W)|FD-Score:-3.16|P-value:7.90E-4||SGD DESC:Putative ferric reductase with similarity to Fre2p; expression induced by low copper levels Gene:GCV2(YMR189W)|FD-Score:3.1|P-value:9.79E-4||SGD DESC:P subunit of the mitochondrial glycine decarboxylase complex, required for the catabolism of glycine to 5,10-methylene-THF; expression is regulated by levels of 5,10-methylene-THF in the cytoplasm Gene:GOS1(YHL031C)|FD-Score:3.34|P-value:4.26E-4||SGD DESC:v-SNARE protein involved in Golgi transport, homolog of the mammalian protein GOS-28/GS28 Gene:GPT2(YKR067W)|FD-Score:-3.58|P-value:1.71E-4||SGD DESC:Glycerol-3-phosphate/dihydroxyacetone phosphate dual substrate-specific sn-1 acyltransferase located in lipid particles and the ER; involved in the stepwise acylation of glycerol-3-phosphate and dihydroxyacetone in lipid biosynthesis; the most conserved motifs and functionally relevant residues are oriented towards the ER lumen Gene:MRPL35(YDR322W)|FD-Score:-3.53|P-value:2.07E-4||SGD DESC:Mitochondrial ribosomal protein of the large subunit Gene:MRS3(YJL133W)|FD-Score:3.44|P-value:2.88E-4||SGD DESC:Iron transporter, mediates Fe2+ transport across inner mito membrane; mitochondrial carrier family member; active under low-iron conditions; may transport other cations; MRS3 has a paralog, MRS4, that arose from the whole genome duplication Gene:SCP160(YJL080C)|FD-Score:3.38|P-value:3.65E-4||SGD DESC:Essential RNA-binding G protein effector of mating response pathway, mainly associated with nuclear envelope and ER, interacts in mRNA-dependent manner with translating ribosomes via multiple KH domains, similar to vertebrate vigilins Gene:SLM2(YNL047C)|FD-Score:-3.31|P-value:4.67E-4||SGD DESC:Phosphoinositide PI4,5P(2) binding protein, forms a complex with Slm1p; acts downstream of Mss4p in a pathway regulating actin cytoskeleton organization in response to stress; phosphorylated by the TORC2 complex; SLM2 has a paralog, SLM1, that arose from the whole genome duplication Gene:SSU1(YPL092W)|FD-Score:-3.22|P-value:6.46E-4||SGD DESC:Plasma membrane sulfite pump involved in sulfite metabolism and required for efficient sulfite efflux; major facilitator superfamily protein Gene:SUR4(YLR372W)|FD-Score:4.17|P-value:1.52E-5||SGD DESC:Elongase, involved in fatty acid and sphingolipid biosynthesis; synthesizes very long chain 20-26-carbon fatty acids from C18-CoA primers; involved in regulation of sphingolipid biosynthesis Gene:TUF1(YOR187W)|FD-Score:-3.38|P-value:3.61E-4||SGD DESC:Mitochondrial translation elongation factor Tu; comprises both GTPase and guanine nucleotide exchange factor activities, while these activities are found in separate proteins in S. pombe and humans Gene:VMA5(YKL080W)|FD-Score:-3.48|P-value:2.47E-4||SGD DESC:Subunit C of the eight-subunit V1 peripheral membrane domain of vacuolar H+-ATPase (V-ATPase), an electrogenic proton pump found throughout the endomembrane system; required for the V1 domain to assemble onto the vacuolar membrane Gene:YHI9(YHR029C)|FD-Score:-3.7|P-value:1.06E-4||SGD DESC:Protein of unknown function; null mutant is defective in unfolded protein response; possibly involved in a membrane regulation metabolic pathway; member of the PhzF superfamily, though most likely not involved in phenazine production

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
YHR062C7.793.39E-154.81RPP1Subunit of both RNase MRP and nuclear RNase P; RNase MRP cleaves pre-rRNA, while nuclear RNase P cleaves tRNA precursors to generate mature 5' ends and facilitates turnover of nuclear RNAs
YPL007C2.980.001460.29TFC8One of six subunits of RNA polymerase III transcription initiation factor complex (TFIIIC); part of TFIIIC TauB domain that binds BoxB promoter sites of tRNA and other genes; linker between TauB and TauA domains; human homolog is TFIIIC-90
YFR050C2.690.003610.19PRE4Beta 7 subunit of the 20S proteasome
YML105C2.500.006260.02SEC65Subunit of the signal recognition particle (SRP), involved in protein targeting to the ER; interacts with Srp54p; homolog of mammalian SRP19
YER133W2.480.006660.04GLC7Type 1 serine/threonine protein phosphatase catalytic subunit; involved in various processes including glycogen metabolism, sporulation, mitosis; accumulates at mating projections by interaction with Afr1p; interacts with many regulatory subunits; involved in regulation of the nucleocytoplasmic shuttling of Hxk2p; import into nucleus is inhibited during spindle assembly checkpoint arrest
YNL310C2.430.007460.05ZIM17Heat shock protein with a zinc finger motif; essential for protein import into mitochondria; may act with Pam18p to facilitate recognition and folding of imported proteins by Ssc1p (mtHSP70) in the mitochondrial matrix
YNR035C2.380.008650.01ARC35Subunit of the ARP2/3 complex, which is required for the motility and integrity of cortical actin patches; required for cortical localization of calmodulin
YNL290W2.370.008800.04RFC3Subunit of heteropentameric Replication factor C (RF-C), which is a DNA binding protein and ATPase that acts as a clamp loader of the proliferating cell nuclear antigen (PCNA) processivity factor for DNA polymerases delta and epsilon
YGL099W2.330.009910.02LSG1Putative GTPase involved in 60S ribosomal subunit biogenesis; required for the release of Nmd3p from 60S subunits in the cytoplasm
YLR033W2.310.010500.01RSC58Component of the RSC chromatin remodeling complex; RSC functions in transcriptional regulation and elongation, chromosome stability, and establishing sister chromatid cohesion; involved in telomere maintenance
YFL029C2.290.010900.08CAK1Cyclin-dependent kinase-activating kinase required for passage through the cell cycle, phosphorylates and activates Cdc28p; nucleotide-binding pocket differs significantly from those of most other protein kinases
YDL147W2.210.013600.04RPN5Subunit of the COP9 signalosome (CSN) and non-ATPase regulatory subunit of the 26S proteasome lid, similar to mammalian p55 subunit and to another S. cerevisiae regulatory subunit, Rpn7p; Rpn5p is an essential protein
YLR208W2.170.015000.09SEC13Structural component of 3 distinct complexes; subunit of Nup84 nuclear pore sub-complex (NPC), COPII vesicle coat, and Seh1-associated (SEA) complex; COPII vesicle coat is required for ER to Golgi transport; the Nup84 subcomplex contributes to nucleocytoplasmic transport, NPC biogenesis and processes that may require localization of chromosomes at the nuclear periphery, including transcription; homologous to human SEC13; abundance increases under DNA replication stress
YBR049C2.090.018500.06REB1RNA polymerase I enhancer binding protein; DNA binding protein that binds to genes transcribed by both RNA polymerase I and RNA polymerase II; required for termination of RNA polymerase I transcription; REB1 has a paralog, NSI1, that arose from the whole genome duplication
YHR007C2.020.021700.00ERG11Lanosterol 14-alpha-demethylase; catalyzes the C-14 demethylation of lanosterol to form 4,4''-dimethyl cholesta-8,14,24-triene-3-beta-ol in the ergosterol biosynthesis pathway; member of the cytochrome P450 family; associated and coordinately regulated with the P450 reductase Ncp1p

Top 15 HOM fitness defect scores (HOP)

Download all HOP Data (tab-delimited text)  (excel)
Deletion Strain FD score P-value Gene Gene Description
YLR372W4.171.52E-5SUR4Elongase, involved in fatty acid and sphingolipid biosynthesis; synthesizes very long chain 20-26-carbon fatty acids from C18-CoA primers; involved in regulation of sphingolipid biosynthesis
YJL133W3.442.88E-4MRS3Iron transporter, mediates Fe2+ transport across inner mito membrane; mitochondrial carrier family member; active under low-iron conditions; may transport other cations; MRS3 has a paralog, MRS4, that arose from the whole genome duplication
YBR281C3.423.18E-4DUG2Component of glutamine amidotransferase (GATase II); forms a complex with Dug3p to degrade glutathione (GSH) and other peptides containing a gamma-glu-X bond in an alternative pathway to GSH degradation by gamma-glutamyl transpeptidase (Ecm38p)
YJL080C3.383.65E-4SCP160Essential RNA-binding G protein effector of mating response pathway, mainly associated with nuclear envelope and ER, interacts in mRNA-dependent manner with translating ribosomes via multiple KH domains, similar to vertebrate vigilins
YHL031C3.344.26E-4GOS1v-SNARE protein involved in Golgi transport, homolog of the mammalian protein GOS-28/GS28
YMR189W3.109.79E-4GCV2P subunit of the mitochondrial glycine decarboxylase complex, required for the catabolism of glycine to 5,10-methylene-THF; expression is regulated by levels of 5,10-methylene-THF in the cytoplasm
YOR356W2.960.00156CIR2Putative ortholog of human electron transfer flavoprotein dehydrogenase (ETF-dH); found in a large supramolecular complex with other mitochondrial dehydrogenases; may have a role in oxidative stress response
YEL007W2.950.00158MIT1Transcriptional regulator of pseudohyphal growth; protein with sequence similarity to S. pombe gti1+ (gluconate transport inducer 1) and C. albicans Wor1
YJR038C_d2.890.00194YJR038C_dDubious open reading frame unlikely to encode a functional protein, based on available experimental and comparative sequence data
YLL056C_p2.880.00201YLL056C_pPutative protein of unknown function, transcription is activated by paralogous transcription factors Yrm1p and Yrr1p and genes involved in pleiotropic drug resistance (PDR); expression is induced in cells treated with the mycotoxin patulin
YAL054C2.790.00268ACS1Acetyl-coA synthetase isoform which, along with Acs2p, is the nuclear source of acetyl-coA for histone acetylation; expressed during growth on nonfermentable carbon sources and under aerobic conditions
YEL009C2.780.00271GCN4Basic leucine zipper (bZIP) transcriptional activator of amino acid biosynthetic genes in response to amino acid starvation; expression is tightly regulated at both the transcriptional and translational levels
YJR025C2.740.00307BNA13-hydroxyanthranilic acid dioxygenase, required for the de novo biosynthesis of NAD from tryptophan via kynurenine; expression regulated by Hst1p
YDR344C_d2.720.00330YDR344C_dDubious open reading frame unlikely to encode a functional protein, based on available experimental and comparative sequence data
YDR011W2.710.00334SNQ2Plasma membrane ATP-binding cassette (ABC) transporter, multidrug transporter involved in multidrug resistance and resistance to singlet oxygen species

GO enrichment analysis for SGTC_3261
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
0.2281.44E-70SGTC_265mycophenolic acid 32.9 μMMiscellaneous4465410.0689655RPP1 & pyrimidine depletion
0.1924.03E-50SGTC_2685mycophenolic acid 18.9 μMMiscellaneous4465410.0689655RNA pol III & RNase P/MRP
0.1775.54E-43SGTC_24984'-Methoxychalcone 54.6 μMMicrosource (Natural product library)6418180.0714286RPP1 & pyrimidine depletion
0.1736.98E-41SGTC_15346-azauridine 81.6 μMTimTec (Pure natural product library)2335020.08RNA pol III & RNase P/MRP
0.1624.63E-36SGTC_1661st013063 9.7 μMTimTec (Natural product derivative library)7213950.0769231
0.1611.67E-35SGTC_13993562-5772 25.0 μMChemDiv (Drug-like library)238474900.0833333RPP1 & pyrimidine depletion
0.1561.62E-33SGTC_466geldanamycin 89.2 μMICCB bioactive library52883820.0841122RPP1 & pyrimidine depletion
0.1541.40E-32SGTC_31699102970 49.5 μMChembridge (Drug-like library)170278390.08RPP1 & pyrimidine depletion
0.1533.22E-32SGTC_14853909-9022 254.0 μMChemDiv (Drug-like library)7145160.0759494RPP1 & pyrimidine depletion
0.1533.31E-32SGTC_2686alizarin 95.4 μMMiscellaneous62930.0952381RPP1 & pyrimidine depletion
0.1506.16E-31SGTC_6790422-0091 41.4 μMChemDiv (Drug-like library)6273840.0597015Golgi
0.1462.07E-29SGTC_28609025725 39.0 μMChembridge (Drug-like library)405462480.0470588RPP1 & pyrimidine depletion
0.1432.73E-28SGTC_1115galangin 695.7 nMTimTec (Natural product library)52816160.0684932RPP1 & pyrimidine depletion
0.1433.82E-28SGTC_10164226-1401 38.0 μMChemDiv (Drug-like library)29016130.0666667RNA pol III & RNase P/MRP
0.1419.12E-28SGTC_389tpck 16.7 μMMiscellaneous4396470.12

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
SGTC_21866124449200 μM0.2727273834182Chembridge (Fragment library)245.300241.3815RSC complex & mRNA processing
SGTC_21725754775163.92 μM0.2419352263357Chembridge (Fragment library)257.327561.72113
SGTC_2474532157043.32 μM0.2121212841384Miscellaneous297.37153.55303
SGTC_5891227-007034.1 μM0.2121212841384ChemDiv (Drug-like library)297.37153.55303
SGTC_1970st07012235.8 μM0.212121102928TimTec (Natural product derivative library)254.280563.08303TSC3-RPN4
SGTC_16014'-hydroxyflavanone55.5 μM0.203125165506TimTec (Pure natural product library)240.253982.85713RPP1 & pyrimidine depletion
SGTC_1695st02691434.5 μM0.2025323289191TimTec (Natural product derivative library)380.43855.26814
SGTC_13151237-00193.69 μM0.190476825140ChemDiv (Drug-like library)246.26343.7303
SGTC_2469565501990.81 μM0.1891892788239Miscellaneous341.3813.18315
SGTC_2707st07855666.6 μM0.18918917250899TimTec (Natural product derivative library)300.378742.89813