LLY-283 2.6μM R06 exp290

Inhibits protein arginine methyltransferase PRMT5, inactive control is LLY-284

PubChem Name: (2R,3R,4S,5R)-2-(4-Aminopyrrolo[2,3-d]pyrimidin-7-yl)-5-[(R)-hydroxy(phenyl)methyl]oxolane-3,4-diol
Synonyms: N/A
CAS #: 2040291-27-6
PubChem CID: 122669401
IUPAC: (2R,3R,4S,5R)-2-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-5-[(R)-hydroxy(phenyl)methyl]oxolane-3,4-diol
INCHI Name: InChI=1S/C17H18N4O4/c18-15-10-6-7-21(16(10)20-8-19-15)17-13(24)12(23)14(25-17)11(22)9-4-2-1-3-5-9/h1-8,11-14,17,22-24H,(H2,18,19,20)/t11-,12+,13-,14-,17-/m1/s1
INCHI Key: WWOOWAHTEXIWBO-QFRSUPTLSA-N
Molecular Weight: 342.35
Canonical SMILES: C1=CC=C(C=C1)C(C2C(C(C(O2)N3C=CC4=C(N=CN=C43)N)O)O)O
Isomeric SMILES: C1=CC=C(C=C1)[C@H]([C@@H]2[C@H]([C@H]([C@@H](O2)N3C=CC4=C(N=CN=C43)N)O)O)O
Molecular Formula: C17H18N4O4

Sensitive/Resistant hits (FDR<0.05)	CRANKS	Score Plot	Top 30 Genes	Screen Similarity	Top 30 Sensitive GO terms	Top 30 Resistant GO terms
16/5	Scores	View	View	View	View	View

Screen	Correlation	Plot
Thimerosal 0.85μM R08 exp529	0.096	View
iCRT14 30μM R08 exp492	0.074	View
UM0125461 0.74μM R02 exp84	0.065	View
UM131593 0.2μM R03 exp106	0.064	View
QNZ 0.01μM R08 exp439	0.063	View
Oligomycin-A 2μM R00 exp25	0.06	View
PU-H71 1μM R08 exp515	0.058	View
Quercetin 20μM R08 exp517	0.051	View
UMK57 1μM R01 exp59	0.051	View
Phenformin 20μM R05 exp212	0.051	View
GSK591 2.6μM R03 exp128	0.089	View
CB-5083 0.4μM R08 exp468	0.068	View
Aphidicolin 0.4μM R08 exp440	0.062	View
Hydroxyurea 100μM R07 exp329	0.061	View
2-Methoxyestradiol 0.55 to 1μM on day4 R07 exp312	0.058	View
BML-284 0.09μM R08 exp460	0.057	View
Doxorubicin 0.02μM R08 exp478	0.055	View
GSK-J4 1.5μM R08 exp441	0.053	View
BI-D1870 3.15μM R02 exp66	0.052	View
Arsenate 40μM R06 exp264	0.051	View

GO Term	Fold Change	Genes
spliceosomal complex	17.77	SNRPB2,API5,PRPF38B,TXNL4A,AKAP17A,PRPF4B
nuclear speck	14.08	ZC3H14,SNRPB2,DDX39A,KMT2E,YLPM1,API5,BRD1,ACIN1,AKAP17A,PRPF4B
RNA splicing	11.14	SNRPB2,DDX39A,PRPF38B,TXNL4A,ACIN1,AKAP17A,PRPF4B
mRNA metabolic process	8.76	SNRPB2,DDX39A,PRPF38B,PCBP2,TXNL4A,ACIN1,CNOT2,AKAP17A,PRPF4B
nuclear body	7.76	ZC3H14,SNRPB2,DDX39A,KMT2E,YLPM1,API5,BRD1,ACIN1,GFI1,AKAP17A,PRPF4B
ribonucleoprotein complex	6.63	ZC3H14,SNRPB2,API5,PRPF38B,PCBP2,TXNL4A,AKAP17A,PRPF4B

GO Term	Fold Change	Genes
tRNA aminoacylation for mitochondrial protein translation	236.74	YARS2,DARS2,EARS2
ligase activity, forming carbon-oxygen bonds	59.72	RARS2,YARS2,DARS2,EARS2
aminoacyl-tRNA ligase activity	59.72	RARS2,YARS2,DARS2,EARS2
tRNA aminoacylation for protein translation	59.72	RARS2,YARS2,DARS2,EARS2
tRNA aminoacylation	55.24	RARS2,YARS2,DARS2,EARS2
amino acid activation	53.89	RARS2,YARS2,DARS2,EARS2
mitochondrial translation	36.14	RARS2,MRPS6,YARS2,DARS2,MRPL57,EARS2,GFM1
mitochondrial gene expression	27.82	RARS2,MRPS6,YARS2,DARS2,MRPL57,EARS2,GFM1
catalytic activity, acting on a tRNA	22.27	RARS2,YARS2,TRMT61A,DARS2,EARS2
ligase activity	20.98	RARS2,YARS2,DPH6,DARS2,ATP5F1A,EARS2
translation	15.47	RPS8,RARS2,MRPS6,YARS2,RPL36A,DARS2,RPL11,MRPL57,EARS2,GFM1
peptide biosynthetic process	14.46	RPS8,RARS2,MRPS6,YARS2,RPL36A,DARS2,RPL11,MRPL57,EARS2,GFM1
peptide metabolic process	11.65	RPS8,RARS2,MRPS6,YARS2,RPL36A,DARS2,RPL11,MRPL57,EARS2,GFM1
amide biosynthetic process	10.98	RPS8,RARS2,MRPS6,YARS2,RPL36A,DARS2,RPL11,MRPL57,EARS2,GFM1
mitochondrial matrix	10.51	TP53,RARS2,MRPS6,YARS2,DARS2,ATP5F1A,MRPL57,EARS2,GFM1
ncRNA metabolic process	8.79	RPS8,TP53,RARS2,YARS2,TRMT61A,DARS2,RPL11,EARS2
mitochondrial envelope	7.36	PTPMT1,MRPS6,GNPAT,SLC11A2,COX17,BCS1L,ATP5F1A,MRPL57,OMA1,CRLS1
amide metabolic process	7.30	RPS8,RARS2,MRPS6,YARS2,RPL36A,DARS2,RPL11,MRPL57,EARS2,GFM1
mitochondrial membrane	7.05	PTPMT1,MRPS6,GNPAT,SLC11A2,BCS1L,ATP5F1A,MRPL57,OMA1,CRLS1