POLR1E

Summary

POLR1E (RNA polymerase I subunit E, HGNC:17631) is a protein-coding gene on chromosome 9p13.2, encoding DNA-directed RNA polymerase I subunit RPA49 (Q9GZS1). Component of RNA polymerase I (Pol I), a DNA-dependent RNA polymerase which synthesizes ribosomal RNA precursors using the four ribonucleoside triphosphates as substrates. It is a selective cancer dependency (DepMap: 79.4% of cell lines).

Predicted to enable DNA binding activity and RNA polymerase I general transcription initiation factor binding activity. Involved in nucleolar large rRNA transcription by RNA polymerase I and transcription initiation at RNA polymerase I promoter. Located in fibrillar center and nucleoplasm. Part of RNA polymerase I complex.

Source: NCBI Gene 64425 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 68 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 79.4% of screened cell lines
• MANE Select transcript: NM_022490

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:17631
Approved symbol	POLR1E
Name	RNA polymerase I subunit E
Location	9p13.2
Locus type	gene with protein product
Status	Approved
Aliases	FLJ13390, PAF53, FLJ13970, RPA49
Ensembl gene	ENSG00000137054
Ensembl biotype	protein_coding
OMIM	621031
Entrez	64425

Gene structure

Transcript identifiers

Ensembl transcripts: 6 — 5 protein_coding, 1 nonsense_mediated_decay

ENST00000377792, ENST00000377798, ENST00000442009, ENST00000875219, ENST00000916168, ENST00000916169

RefSeq mRNA: 2 — MANE Select: NM_022490 NM_001282766, NM_022490

CCDS: CCDS6611

Canonical transcript exons

ENST00000377798 — 12 exons

Exon	Start	End
ENSE00000700578	37492657	37492715
ENSE00000700581	37493559	37493703
ENSE00000700582	37495169	37495276
ENSE00000700583	37495890	37495986
ENSE00000700585	37498091	37498224
ENSE00000700586	37500840	37500921
ENSE00000700588	37501713	37501844
ENSE00001850835	37503043	37503697
ENSE00002252404	37485948	37486123
ENSE00003459279	37486703	37486806
ENSE00003507591	37487863	37487939
ENSE00003526455	37489315	37489400

Expression profiles

Bgee: expression breadth ubiquitous, 222 present calls, max score 89.78.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 24.2162 / max 296.9287, expressed in 1795 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
96735	16.6827	1771
96736	7.5336	1505

Top tissues by expression

266 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
body of pancreas	UBERON:0001150	89.78	gold quality
left ovary	UBERON:0002119	89.65	gold quality
cortical plate	UBERON:0005343	89.34	gold quality
adrenal tissue	UBERON:0018303	89.07	gold quality
calcaneal tendon	UBERON:0003701	88.98	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	88.87	gold quality
body of uterus	UBERON:0009853	88.20	gold quality
ovary	UBERON:0000992	87.73	gold quality
pancreas	UBERON:0001264	87.49	gold quality
right ovary	UBERON:0002118	87.47	gold quality
secondary oocyte	CL:0000655	87.43	gold quality
ganglionic eminence	UBERON:0004023	86.99	gold quality
ectocervix	UBERON:0012249	86.82	gold quality
left uterine tube	UBERON:0001303	86.77	gold quality
popliteal artery	UBERON:0002250	86.72	gold quality
tibial artery	UBERON:0007610	86.72	gold quality
ventricular zone	UBERON:0003053	86.69	gold quality
endocervix	UBERON:0000458	86.52	gold quality
omental fat pad	UBERON:0010414	86.35	gold quality
tendon	UBERON:0000043	86.32	gold quality
peritoneum	UBERON:0002358	86.30	gold quality
gastrocnemius	UBERON:0001388	86.21	gold quality
cervix squamous epithelium	UBERON:0006922	86.16	gold quality
muscle of leg	UBERON:0001383	86.14	gold quality
aorta	UBERON:0000947	86.08	gold quality
adipose tissue of abdominal region	UBERON:0007808	85.94	gold quality
islet of Langerhans	UBERON:0000006	85.81	gold quality
embryo	UBERON:0000922	85.69	gold quality
smooth muscle tissue	UBERON:0001135	85.66	gold quality
muscle layer of sigmoid colon	UBERON:0035805	85.52	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ENAD-17	no	299.72
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): UBTF

miRNA regulators (miRDB)

17 targeting POLR1E, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-3688-3P	99.97	72.02	2834
HSA-MIR-6778-3P	99.96	67.29	2693
HSA-MIR-627-3P	99.90	71.42	3316
HSA-MIR-544A	99.84	68.66	1965
HSA-MIR-4694-3P	99.79	69.53	2640
HSA-MIR-4679	99.76	69.19	1229
HSA-MIR-5093	99.67	69.26	2291
HSA-MIR-5580-5P	99.38	66.96	1139
HSA-MIR-7974	99.24	65.48	1137
HSA-MIR-6815-3P	99.13	68.98	1530
HSA-MIR-198	98.70	67.32	920
HSA-MIR-619-5P	98.57	64.97	1988
HSA-MIR-3670	97.88	64.39	763
HSA-MIR-1914-5P	97.83	66.21	807
HSA-MIR-6747-3P	97.73	64.84	1596
HSA-MIR-4790-5P	96.67	67.45	167
HSA-MIR-7973	96.48	65.54	502

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 79.4% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 2)

• Nucleolar detention requires binding of SIRT7 to nascent pre-rRNA, linking the spatial distribution of SIRT7 and deacetylation of PAF53 to ongoing transcription. (PMID:24207024)
• PAF49: An RNA Polymerase I subunit essential for rDNA transcription and stabilization of PAF53. (PMID:37356716)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	polr1e	ENSDARG00000006434
mus_musculus	Polr1e	ENSMUSG00000028318
rattus_norvegicus	Polr1e	ENSRNOG00000012664
drosophila_melanogaster	Polr1E	FBGN0038601
caenorhabditis_elegans		WBGENE00017749

Protein

Protein identifiers

DNA-directed RNA polymerase I subunit RPA49 — Q9GZS1 (reviewed: Q9GZS1)

Alternative names: DNA-directed RNA polymerase I subunit E, RNA polymerase I-associated factor 1, RNA polymerase I-associated factor 53

All UniProt accessions (2): E7EX70, Q9GZS1

UniProt curated annotations — full annotation on UniProt →

Function. Component of RNA polymerase I (Pol I), a DNA-dependent RNA polymerase which synthesizes ribosomal RNA precursors using the four ribonucleoside triphosphates as substrates. Appears to be involved in the formation of the initiation complex at the promoter by mediating the interaction between Pol I and UBTF/UBF.

Subunit / interactions. Component of the RNA polymerase I (Pol I) complex consisting of 13 subunits: a ten-subunit catalytic core composed of POLR1A/RPA1, POLR1B/RPA2, POLR1C/RPAC1, POLR1D/RPAC2, POLR1H/RPA12, POLR2E/RPABC1, POLR2F/RPABC2, POLR2H/RPABC3, POLR2K/RPABC4 and POLR2L/RPABC5; a mobile stalk subunit POLR1F/RPA43 protruding from the core and additional subunits homologous to general transcription factors POLR1E/RPA49 and POLR1G/RPA34. Forms a heterodimer with POLR1G/RPA34. Interacts with POLR1G. Also binds UBTF/UBF. Interacts with PWP1.

Subcellular location. Nucleus. Nucleolus.

Post-translational modifications. Acetylated at Lys-373 by CREBBP/CBP, leading to decreased RNA polymerase I transcription. In normal conditions, deacetylated by SIRT7, promoting the association of RNA polymerase I with the rDNA promoter region and coding region. In response to stress, SIRT7 is released from nucleoli leading to hyperacetylation of POLR1E/PAF53 and decreased association of RNA polymerase I with the rDNA promoter region.

Miscellaneous. Dubious isoform produced through intron retention.

Similarity. Belongs to the eukaryotic RPA49/POLR1E RNA polymerase subunit family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q9GZS1-2	2	yes
Q9GZS1-1	1

RefSeq proteins (2): NP_001269695, NP_071935* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR009668	RNA_pol-assoc_fac_A49-like	Family

Pfam: PF06870

UniProt features (49 total): strand 16, helix 14, turn 8, modified residue 3, sequence variant 3, chain 1, region of interest 1, sequence conflict 1, splice variant 1, mutagenesis site 1

Structure

Experimental structures (PDB)

7 structures.

PDB	Method	Resolution (Å)
7OB9	ELECTRON MICROSCOPY	2.7
7VBB	ELECTRON MICROSCOPY	2.81
7VBA	ELECTRON MICROSCOPY	2.89
7VBC	ELECTRON MICROSCOPY	3.01
7OBA	ELECTRON MICROSCOPY	3.1
7OBB	ELECTRON MICROSCOPY	3.3
8A43	ELECTRON MICROSCOPY	4.09

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9GZS1-F1	83.10	0.44

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Post-translational modifications (3): 35, 163, 373

Mutagenesis-validated functional residues (1):

Position	Phenotype
373	decreased acetylation.

Function

Pathways and Gene Ontology

Reactome pathways

11 pathways

ID	Pathway
R-HSA-427413	NoRC negatively regulates rRNA expression
R-HSA-5250924	B-WICH complex positively regulates rRNA expression
R-HSA-73762	RNA Polymerase I Transcription Initiation
R-HSA-73772	RNA Polymerase I Promoter Escape
R-HSA-73863	RNA Polymerase I Transcription Termination
R-HSA-212165	Epigenetic regulation of gene expression
R-HSA-5250913	Positive epigenetic regulation of rRNA expression
R-HSA-5250941	Negative epigenetic regulation of rRNA expression
R-HSA-73854	RNA Polymerase I Promoter Clearance
R-HSA-73864	RNA Polymerase I Transcription
R-HSA-74160	Gene expression (Transcription)

MSigDB gene sets: 142 (showing top): GSE45365_CD8A_DC_VS_CD11B_DC_IFNAR_KO_DN, GOBP_DNA_TEMPLATED_TRANSCRIPTION_TERMINATION, SHEPARD_CRASH_AND_BURN_MUTANT_UP, REACTOME_RNA_POLYMERASE_I_TRANSCRIPTION_INITIATION, GOBP_RRNA_TRANSCRIPTION, chr9p13, GOBP_DNA_TEMPLATED_TRANSCRIPTION_INITIATION, BENPORATH_ES_CORE_NINE_CORRELATED, KEGG_PURINE_METABOLISM, NADLER_HYPERGLYCEMIA_AT_OBESITY, KIM_GASTRIC_CANCER_CHEMOSENSITIVITY, GOCC_RNA_POLYMERASE_COMPLEX, FISCHER_DREAM_TARGETS, GOBP_PROTEIN_DNA_COMPLEX_ORGANIZATION, BERENJENO_TRANSFORMED_BY_RHOA_UP

GO Biological Process (5): RNA polymerase I preinitiation complex assembly (GO:0001188), transcription initiation at RNA polymerase I promoter (GO:0006361), transcription elongation by RNA polymerase I (GO:0006362), nucleolar large rRNA transcription by RNA polymerase I (GO:0042790), DNA-templated transcription (GO:0006351)

GO Molecular Function (3): RNA polymerase I general transcription initiation factor binding (GO:0001179), DNA binding (GO:0003677), protein binding (GO:0005515)

GO Cellular Component (6): fibrillar center (GO:0001650), nucleoplasm (GO:0005654), nucleolus (GO:0005730), RNA polymerase I complex (GO:0005736), DNA-directed RNA polymerase complex (GO:0000428), nucleus (GO:0005634)

Reactome top-level categories

Rollup of top-6 pathways:

Category	Pathways
RNA Polymerase I Promoter Clearance	2
RNA Polymerase I Transcription	2
Gene expression (Transcription)	2
Epigenetic regulation of gene expression	2
Negative epigenetic regulation of rRNA expression	1
Positive epigenetic regulation of rRNA expression	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
transcription by RNA polymerase I	3
nucleolus	2
cellular anatomical structure	2
nuclear lumen	2
transcription initiation at RNA polymerase I promoter	1
transcription preinitiation complex assembly	1
DNA-templated transcription initiation	1
DNA-templated transcription elongation	1
rRNA transcription	1
gene expression	1
RNA biosynthetic process	1
general transcription initiation factor binding	1
nucleic acid binding	1
binding	1
intracellular membraneless organelle	1
DNA-directed RNA polymerase complex	1
nuclear protein-containing complex	1
RNA polymerase complex	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

2148 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
POLR1E	POLR1G	O15446	979
POLR1E	TAF1A	Q15573	944
POLR1E	UBTF	P17480	895
POLR1E	POLI	Q9UNA4	817
POLR1E	POLR1A	O95602	808
POLR1E	RRN3	Q9NYV6	795
POLR1E	POLR1F	Q3B726	710
POLR1E	POLR1H	Q9P1U0	675
POLR1E	POLR1B	Q9H9Y6	667
POLR1E	TAF1C	Q15572	642
POLR1E	SIRT7	Q9NRC8	602
POLR1E	POLR1D	P0DPB6	599
POLR1E	RRP9	O43818	593
POLR1E	POLR1C	O15160	587
POLR1E	POLR2L	P52436	479

IntAct

96 interactions, top by confidence:

A	B	Type	Score
POLR2E	POLR3A	psi-mi:“MI:0914”(association)	0.870
NFKBIB	NFKB1	psi-mi:“MI:0914”(association)	0.820
POLR2E	MED19	psi-mi:“MI:0914”(association)	0.730
KBTBD7	METTL15	psi-mi:“MI:0914”(association)	0.730
POLR1A	POLR1C	psi-mi:“MI:0914”(association)	0.730
POLR1E	POLR1C	psi-mi:“MI:0914”(association)	0.670
POLR2L	RCCD1	psi-mi:“MI:0914”(association)	0.640
KPNA1	TCERG1	psi-mi:“MI:0914”(association)	0.640
POLR2F	POLR3A	psi-mi:“MI:0914”(association)	0.640
POLR2L	POLR3A	psi-mi:“MI:0914”(association)	0.640
POLR1E	KLK6	psi-mi:“MI:0915”(physical association)	0.560
POLR1B	POLR1C	psi-mi:“MI:0914”(association)	0.530
GPN3	POLR3A	psi-mi:“MI:0914”(association)	0.530
POLR1C	POLR3A	psi-mi:“MI:0914”(association)	0.530
KRR1	MPHOSPH10	psi-mi:“MI:0914”(association)	0.530
POLR1D	POLR3A	psi-mi:“MI:0914”(association)	0.530
RRN3	POLR1A	psi-mi:“MI:0914”(association)	0.530
ESR2	FBLL1	psi-mi:“MI:0914”(association)	0.460
POLR1E	SUPT16H	psi-mi:“MI:0915”(physical association)	0.400
MYO1C	POLR1E	psi-mi:“MI:0403”(colocalization)	0.370
ARRB1		psi-mi:“MI:0914”(association)	0.350

BioGRID (426): POLR1E (Affinity Capture-MS), POLR1E (Affinity Capture-MS), POLR1E (Affinity Capture-MS), POLR1E (Affinity Capture-MS), POLR1E (Co-fractionation), POLR1E (Co-fractionation), POLR1E (Co-fractionation), POLR1E (Co-fractionation), POLR1E (Affinity Capture-MS), POLR1E (Affinity Capture-MS), POLR1E (Affinity Capture-MS), POLR1E (Affinity Capture-MS), POLR1E (Affinity Capture-MS), POLR1E (Affinity Capture-MS), POLR1E (Affinity Capture-MS)

ESM2 similar proteins: A4IH75, B0S6R1, F4K265, O14417, O75165, O94915, P28660, P60670, P97878, Q10LJ0, Q2HJE0, Q2TBN7, Q3B736, Q3B8G8, Q3TPX4, Q499N2, Q4R6Q7, Q4R708, Q556Y9, Q5E9X5, Q5R6U8, Q5R8B7, Q5RBT3, Q5VZE5, Q5XHA1, Q5ZHV2, Q642Q3, Q6AY69, Q6DE58, Q6DKG0, Q6GLR7, Q6NPF4, Q6P2C8, Q6PFL0, Q6PHQ8, Q6Q7J5, Q7T322, Q8BJ63, Q8TAT6, Q8VDP2

Diamond homologs: Q6GLI9, Q8K202, Q9GZS1

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
POLR1E	“form complex”	“RNA Polymerase I”	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 100 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
RNA Polymerase III Chain Elongation	8	73.6×	2e-12
Positive epigenetic regulation of rRNA expression	13	65.2×	3e-19
RNA Polymerase I Transcription Termination	13	61.5×	6e-19
RNA Polymerase I Promoter Clearance	14	59.4×	9e-20
RNA Polymerase I Transcription	14	57.9×	9e-20
RNA Polymerase III Transcription Termination	8	57.6×	1e-11
RNA Polymerase III Transcription Initiation From Type 2 Promoter	9	55.2×	1e-12
FGFR2 mutant receptor activation	5	55.2×	4e-07

GO biological processes:

GO term	Partners	Fold	FDR
ribosomal small subunit biogenesis	6	14.8×	5e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

68 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	51
Likely benign	1
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1659 predictions. Top by Δscore:

Variant	Effect	Δscore
9:37486802:TCCTG:T	donor_gain	1.0000
9:37486805:TG:T	donor_gain	1.0000
9:37486805:TGGTA:T	donor_loss	1.0000
9:37486806:GG:G	donor_gain	1.0000
9:37486806:GGTA:G	donor_loss	1.0000
9:37486807:G:GG	donor_gain	1.0000
9:37486807:GTA:G	donor_loss	1.0000
9:37486808:T:A	donor_loss	1.0000
9:37487862:GGCA:G	acceptor_gain	1.0000
9:37489309:A:AG	acceptor_gain	1.0000
9:37489310:T:G	acceptor_gain	1.0000
9:37489310:TTCA:T	acceptor_loss	1.0000
9:37489311:TCAGG:T	acceptor_loss	1.0000
9:37489312:CAGGC:C	acceptor_loss	1.0000
9:37489313:A:AG	acceptor_gain	1.0000
9:37489313:AG:A	acceptor_gain	1.0000
9:37489314:G:A	acceptor_loss	1.0000
9:37489314:G:GT	acceptor_gain	1.0000
9:37489314:GG:G	acceptor_gain	1.0000
9:37489314:GGC:G	acceptor_gain	1.0000
9:37489314:GGCA:G	acceptor_gain	1.0000
9:37489314:GGCAC:G	acceptor_gain	1.0000
9:37489355:G:GT	donor_gain	1.0000
9:37489397:TCAGG:T	donor_loss	1.0000
9:37489398:CAGG:C	donor_loss	1.0000
9:37489400:GGT:G	donor_loss	1.0000
9:37489401:GTAG:G	donor_loss	1.0000
9:37489402:T:A	donor_loss	1.0000
9:37492642:T:TA	acceptor_gain	1.0000
9:37492644:T:TA	acceptor_gain	1.0000

AlphaMissense

2765 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
9:37493580:T:C	F142L	0.998
9:37493582:T:A	F142L	0.998
9:37493582:T:G	F142L	0.998
9:37486708:T:C	F28L	0.996
9:37486710:C:A	F28L	0.996
9:37486710:C:G	F28L	0.996
9:37487866:G:C	A62P	0.996
9:37489326:G:A	G90E	0.996
9:37493584:G:A	G143D	0.995
9:37487887:T:G	Y69D	0.993
9:37487894:G:A	G71E	0.993
9:37489325:G:A	G90R	0.993
9:37489325:G:C	G90R	0.993
9:37489367:G:C	A104P	0.993
9:37493577:G:C	A141P	0.993
9:37493602:G:C	R149P	0.993
9:37503072:T:C	L377P	0.993
9:37486709:T:C	F28S	0.992
9:37487867:C:A	A62D	0.992
9:37487893:G:A	G71R	0.992
9:37487893:G:C	G71R	0.992
9:37489368:C:A	A104D	0.992
9:37493608:T:C	L151P	0.992
9:37487902:T:C	F74L	0.991
9:37487904:T:A	F74L	0.991
9:37487904:T:G	F74L	0.991
9:37489323:T:A	V89E	0.991
9:37493670:G:C	A172P	0.991
9:37486078:T:A	W11R	0.990
9:37486078:T:C	W11R	0.990

dbSNP variants (sampled 300 via entrez): RS1000123363 (9:37485963 G>A,C,T), RS1000237209 (9:37485806 G>A,C), RS1000290046 (9:37497819 C>G,T), RS1000393787 (9:37497490 T>C), RS1000446680 (9:37503558 A>C), RS1000460619 (9:37494449 T>C), RS1000497835 (9:37487420 G>A), RS1000655114 (9:37487046 A>G), RS1000678972 (9:37493375 T>C), RS1000748289 (9:37494676 C>G,T), RS1000910751 (9:37498376 C>T), RS1001181007 (9:37493080 T>C), RS1001347226 (9:37498958 C>T), RS1001535218 (9:37487056 A>C,G,T), RS1001604181 (9:37493761 T>C)

Disease associations

OMIM: gene MIM:621031 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5725143 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,538 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1232461	MOLIBRESIB	2	1,538

PharmGKB: 1 entry (VIP=true, CPIC=false)

ChEMBL bioactivities

1 potent at pChembl≥5 of 1 total, top 1 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
5.42	IC50	3780	nM	MOLIBRESIB

PubChem BioAssay actives

1 with measured affinity, of 6 total; 1 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide	2178692: Inhibition of POLR1E (unknown origin) incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysis	ic50	3.7800	uM

CTD chemical–gene interactions

25 total (human), top 25 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression, increases abundance, increases expression	3
aristolochic acid I	increases expression	1
triphenyl phosphate	affects expression	1
bisphenol A	decreases expression	1
deoxynivalenol	increases expression	1
mono-(2-ethylhexyl)phthalate	increases expression	1
di-n-butylphosphoric acid	affects expression	1
ICG 001	decreases expression	1
Rosiglitazone	increases expression	1
Resveratrol	affects cotreatment, increases expression	1
Temozolomide	increases expression	1
Arsenic	increases abundance, increases expression	1
Dichlorodiphenyl Dichloroethylene	increases expression	1
Dimethyl Sulfoxide	increases expression	1
Doxorubicin	decreases expression	1
Enzyme Inhibitors	decreases activity, increases O-linked glycosylation	1
Formaldehyde	decreases expression	1
Plant Extracts	increases expression, affects cotreatment	1
Tobacco Smoke Pollution	increases expression	1
Tretinoin	decreases expression	1
Valproic Acid	increases expression	1
Cyclosporine	increases expression	1
Aflatoxin B1	increases expression	1
Cadmium Chloride	decreases expression	1
Lactic Acid	decreases expression	1

ChEMBL screening assays

6 unique, capped per target: 6 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL5697422	Binding	Inhibition of POLR1E (unknown origin) assessed as fold change at 10 uM incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysis	Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. — Nature

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.