RPL36A

Summary

RPL36A (ribosomal protein L36a, HGNC:10359) is a protein-coding gene on chromosome Xq22.1, encoding Large ribosomal subunit protein eL42 (P83881). Component of the large ribosomal subunit.

Cytoplasmic ribosomes, organelles that catalyze protein synthesis, consist of a small 40S subunit and a large 60S subunit. Together these subunits are composed of 4 RNA species and approximately 80 structurally distinct proteins. This gene encodes a ribosomal protein that is a component of the 60S subunit. The protein, which shares sequence similarity with yeast ribosomal protein L44, belongs to the L44E (L36AE) family of ribosomal proteins. Although this gene has been referred to as ribosomal protein L44 (RPL44), its official name is ribosomal protein L36a (RPL36A). This gene and the human gene officially named ribosomal protein L36a-like (RPL36AL) encode nearly identical proteins; however, they are distinct genes. As is typical for genes encoding ribosomal proteins, there are multiple processed pseudogenes of this gene dispersed through the genome. Naturally occurring read-through transcription occurs between this locus and the heterogeneous nuclear ribonucleoprotein H2 (H’) gene.

Source: NCBI Gene 6173 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 9 total — 1 pathogenic
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_021029

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:10359
Approved symbol	RPL36A
Name	ribosomal protein L36a
Location	Xq22.1
Locus type	gene with protein product
Status	Approved
Aliases	L36A, eL42
Ensembl gene	ENSG00000241343
Ensembl biotype	protein_coding
OMIM	300902
Entrez	6173

Gene structure

Transcript identifiers

Ensembl transcripts: 13 — 8 protein_coding, 4 retained_intron, 1 nonsense_mediated_decay

ENST00000372849, ENST00000392994, ENST00000427805, ENST00000465340, ENST00000465744, ENST00000471855, ENST00000489407, ENST00000491851, ENST00000553110, ENST00000614077, ENST00000903140, ENST00000933520, ENST00000933521

RefSeq mRNA: 1 — MANE Select: NM_021029 NM_021029

CCDS: CCDS14483

Canonical transcript exons

ENST00000553110 — 5 exons

Exon	Start	End
ENSE00000000228	101395728	101396155
ENSE00002340912	101391011	101391046
ENSE00003515065	101391459	101391564
ENSE00003639312	101391755	101391822
ENSE00003689198	101395335	101395457

Expression profiles

Bgee: expression breadth ubiquitous, 134 present calls, max score 99.88.

FANTOM5 (CAGE): breadth broad, TPM avg 1.3343 / max 46.8616, expressed in 628 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
196950	182.5453	1821
196952	1.0122	457
196951	0.3221	164

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
cortical plate	UBERON:0005343	99.88	gold quality
ganglionic eminence	UBERON:0004023	99.86	gold quality
colonic epithelium	UBERON:0000397	99.83	gold quality
ventricular zone	UBERON:0003053	99.79	gold quality
ovary	UBERON:0000992	99.76	gold quality
left ovary	UBERON:0002119	99.76	gold quality
right ovary	UBERON:0002118	99.74	gold quality
right uterine tube	UBERON:0001302	99.73	gold quality
skin of abdomen	UBERON:0001416	99.72	gold quality
zone of skin	UBERON:0000014	99.71	gold quality
granulocyte	CL:0000094	99.70	gold quality
skin of leg	UBERON:0001511	99.69	gold quality
thoracic mammary gland	UBERON:0005200	99.69	gold quality
uterine cervix	UBERON:0000002	99.68	gold quality
endocervix	UBERON:0000458	99.68	gold quality
cortex of kidney	UBERON:0001225	99.68	gold quality
body of pancreas	UBERON:0001150	99.67	gold quality
bone marrow cell	CL:0002092	99.66	gold quality
lymph node	UBERON:0000029	99.66	gold quality
rectum	UBERON:0001052	99.66	gold quality
tonsil	UBERON:0002372	99.66	gold quality
fallopian tube	UBERON:0003889	99.66	gold quality
bone marrow	UBERON:0002371	99.65	gold quality
body of uterus	UBERON:0009853	99.65	gold quality
ectocervix	UBERON:0012249	99.65	gold quality
prostate gland	UBERON:0002367	99.64	gold quality
vagina	UBERON:0000996	99.63	gold quality
myometrium	UBERON:0001296	99.62	gold quality
mucosa of transverse colon	UBERON:0004991	99.62	gold quality
adipose tissue	UBERON:0001013	99.61	gold quality

Single-cell (SCXA)

Detected in 38 experiment(s), a significant marker in 17.

Experiment	Marker?	Max mean expression
E-MTAB-8410	yes	6810.41
E-GEOD-125970	yes	5132.86
E-CURD-98	yes	4282.26
E-CURD-122	yes	89.96
E-CURD-88	yes	60.52
E-MTAB-9221	yes	55.24
E-CURD-112	yes	39.29
E-MTAB-9067	yes	29.63
E-HCAD-9	yes	24.34
E-MTAB-7316	yes	18.61
E-ANND-3	yes	18.07
E-MTAB-10042	yes	12.37
E-GEOD-135922	yes	10.86
E-GEOD-130148	yes	9.04
E-GEOD-137537	yes	6.60

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): MYC

miRNA regulators (miRDB)

20 targeting RPL36A, 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-545-3P	99.95	70.74	2783
HSA-MIR-7-1-3P	99.91	71.53	4384
HSA-MIR-7-2-3P	99.91	71.40	4394
HSA-MIR-8062	99.88	68.43	995
HSA-MIR-5580-3P	99.70	69.41	2052
HSA-MIR-3616-5P	99.55	67.02	989
HSA-MIR-573	99.55	67.44	955
HSA-MIR-3120-3P	99.54	70.28	2669
HSA-MIR-6740-3P	99.48	68.49	1392
HSA-MIR-5697	99.39	67.74	1249
HSA-MIR-6505-3P	99.34	67.39	1071
HSA-MIR-4667-3P	99.26	65.45	1608
HSA-MIR-4293	99.22	65.46	1263
HSA-MIR-4795-5P	99.11	66.90	876
HSA-MIR-5701	98.97	69.54	1502
HSA-MIR-219A-2-3P	98.62	68.78	797
HSA-MIR-6867-3P	98.12	66.07	1305
HSA-MIR-1470	98.11	63.53	399
HSA-MIR-6730-3P	97.03	67.54	889
HSA-MIR-624-5P	96.00	68.88	728

Literature-anchored findings (GeneRIF, showing 3)

• RPL36A plays a role in tumor cell proliferation and may be a potential target for anticancer therapy of hepatocellular carcinoma (PMID:14752831)
• miR-589-5p facilitated the growth of liver cancer cells by targeting MIG-6 and could be a prognosis biomarker for hepatocellular carcinoma (PMID:30249105)
• Coupled folding-upon-binding of human tumor suppressor MIG6 to lung cancer EGFR kinase domain and molecular trimming/stapling of MIG6-derived beta-hairpins to target the coupling event. (PMID:36547692)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
mus_musculus	Rpl36al	ENSMUSG00000049751
rattus_norvegicus	Rpl36al1	ENSRNOG00000031315
rattus_norvegicus		ENSRNOG00000072711

Paralogs (1): RPL36AL (ENSG00000165502)

Protein

Protein identifiers

Large ribosomal subunit protein eL42 — P83881 (reviewed: P83881)

Alternative names: 60S ribosomal protein L36a, 60S ribosomal protein L44, Cell growth-inhibiting gene 15 protein, Cell migration-inducing gene 6 protein

All UniProt accessions (5): H0Y5B4, H7BY91, J3KQN4, P83881, R4GN19

UniProt curated annotations — full annotation on UniProt →

Function. Component of the large ribosomal subunit. The ribosome is a large ribonucleoprotein complex responsible for the synthesis of proteins in the cell.

Subunit / interactions. Component of the large ribosomal subunit.

Subcellular location. Cytoplasm.

Similarity. Belongs to the eukaryotic ribosomal protein eL42 family.

RefSeq proteins (1): NP_066357* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000552	Ribosomal_eL44	Family
IPR011332	Ribosomal_zn-bd	Homologous_superfamily
IPR053708	Ribosomal_LSU_eL42	Homologous_superfamily

Pfam: PF00935

UniProt features (2 total): chain 1, region of interest 1

Structure

Experimental structures (PDB)

159 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
8A3D	ELECTRON MICROSCOPY	1.67
8QYX	ELECTRON MICROSCOPY	1.78
8QOI	ELECTRON MICROSCOPY	1.9
9O3W	ELECTRON MICROSCOPY	1.9
8YOO	ELECTRON MICROSCOPY	2
9C3H	ELECTRON MICROSCOPY	2
9I2D	ELECTRON MICROSCOPY	2.19
9PBE	ELECTRON MICROSCOPY	2.19
8QFD	ELECTRON MICROSCOPY	2.2
8YOP	ELECTRON MICROSCOPY	2.2
9GUL	ELECTRON MICROSCOPY	2.2
9O3V	ELECTRON MICROSCOPY	2.2
9O3Y	ELECTRON MICROSCOPY	2.2
8JDK	ELECTRON MICROSCOPY	2.26
9S3D	ELECTRON MICROSCOPY	2.32
9RPV	ELECTRON MICROSCOPY	2.35
9S3B	ELECTRON MICROSCOPY	2.38
7OW7	ELECTRON MICROSCOPY	2.4
8K2C	ELECTRON MICROSCOPY	2.4
8XSX	ELECTRON MICROSCOPY	2.4
9SPF	ELECTRON MICROSCOPY	2.4
9SPI	ELECTRON MICROSCOPY	2.4
8JDL	ELECTRON MICROSCOPY	2.42
9S3C	ELECTRON MICROSCOPY	2.42
9QLO	ELECTRON MICROSCOPY	2.47
8FLE	ELECTRON MICROSCOPY	2.48
9P8B	ELECTRON MICROSCOPY	2.48
8JDJ	ELECTRON MICROSCOPY	2.5
9RUC	ELECTRON MICROSCOPY	2.5
8FL7	ELECTRON MICROSCOPY	2.55

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P83881-F1	94.41	0.87

Function

Pathways and Gene Ontology

Reactome pathways

16 pathways

ID	Pathway
R-HSA-156827	L13a-mediated translational silencing of Ceruloplasmin expression
R-HSA-156902	Peptide chain elongation
R-HSA-1799339	SRP-dependent cotranslational protein targeting to membrane
R-HSA-192823	Viral mRNA Translation
R-HSA-2408557	Selenocysteine synthesis
R-HSA-6791226	Major pathway of rRNA processing in the nucleolus and cytosol
R-HSA-72689	Formation of a pool of free 40S subunits
R-HSA-72706	GTP hydrolysis and joining of the 60S ribosomal subunit
R-HSA-72764	Eukaryotic Translation Termination
R-HSA-9010553	Regulation of expression of SLITs and ROBOs
R-HSA-9633012	Response of EIF2AK4 (GCN2) to amino acid deficiency
R-HSA-975956	Nonsense Mediated Decay (NMD) independent of the Exon Junction Complex (EJC)
R-HSA-975957	Nonsense Mediated Decay (NMD) enhanced by the Exon Junction Complex (EJC)
R-HSA-9954709	Ribosome Quality Control (RQC) complex extracts and degrades nascent peptide
R-HSA-9954714	PELO:HBS1L and ABCE1 dissociate a ribosome on a non-stop mRNA
R-HSA-9954716	ZNF598 and the Ribosome-associated Quality Trigger (RQT) complex dissociate a ribosome stalled on a no-go mRNA

MSigDB gene sets: 209 (showing top): GOBP_CYTOPLASMIC_TRANSLATION, MODULE_151, BHATI_G2M_ARREST_BY_2METHOXYESTRADIOL_DN, GCM_NPM1, STARK_PREFRONTAL_CORTEX_22Q11_DELETION_DN, GOBP_STRIATED_MUSCLE_CELL_DIFFERENTIATION, HSIAO_HOUSEKEEPING_GENES, GOBP_NEGATIVE_REGULATION_OF_CELLULAR_COMPONENT_ORGANIZATION, GOBP_TRANSLATION, GOBP_MUSCLE_STRUCTURE_DEVELOPMENT, WATANABE_RECTAL_CANCER_RADIOTHERAPY_RESPONSIVE_UP, GOBP_MUSCLE_CONTRACTION, GOBP_REGULATION_OF_SYNCYTIUM_FORMATION_BY_PLASMA_MEMBRANE_FUSION, GOMF_STRUCTURAL_CONSTITUENT_OF_RIBOSOME, WINTER_HYPOXIA_METAGENE

GO Biological Process (2): cytoplasmic translation (GO:0002181), translation (GO:0006412)

GO Molecular Function (3): RNA binding (GO:0003723), structural constituent of ribosome (GO:0003735), protein binding (GO:0005515)

GO Cellular Component (8): endoplasmic reticulum (GO:0005783), cytosol (GO:0005829), ribosome (GO:0005840), plasma membrane (GO:0005886), cytosolic large ribosomal subunit (GO:0022625), cytosolic ribosome (GO:0022626), cytoplasm (GO:0005737), ribonucleoprotein complex (GO:1990904)

Reactome top-level categories

Rollup of top-11 pathways:

Category	Pathways
Ribosome-associated quality control	3
Translation	2
Cap-dependent Translation Initiation	2
Nonsense-Mediated Decay (NMD)	2
Eukaryotic Translation Initiation	1
Eukaryotic Translation Elongation	1
Influenza Viral RNA Transcription and Replication	1
Selenoamino acid metabolism	1
rRNA processing in the nucleus and cytosol	1
Signaling by ROBO receptors	1
Cellular response to starvation	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
ribosome	2
cytoplasm	2
cellular anatomical structure	2
translation	1
peptidyltransferase activity	1
translational initiation	1
translational elongation	1
translational termination	1
macromolecule biosynthetic process	1
protein metabolic process	1
protein biosynthetic process	1
nucleic acid binding	1
structural molecule activity	1
binding	1
endomembrane system	1
intracellular membrane-bounded organelle	1
intracellular membraneless organelle	1
membrane	1
cell periphery	1
large ribosomal subunit	1
cytosolic ribosome	1
cytosol	1
intracellular anatomical structure	1
protein-containing complex	1

Protein interactions and networks

STRING

0 interactions, top by confidence (×1000):

IntAct

86 interactions, top by confidence:

A	B	Type	Score
MAP3K14	CHUK	psi-mi:“MI:0914”(association)	0.950
RACK1	RPS17	psi-mi:“MI:0915”(physical association)	0.610
RPL36A	AIDA	psi-mi:“MI:0915”(physical association)	0.560
NAP1L1	RPL17	psi-mi:“MI:0914”(association)	0.530
L3MBTL1	DNAJB6	psi-mi:“MI:0914”(association)	0.530
ESR1		psi-mi:“MI:0914”(association)	0.460
LRRK2	RPL36A	psi-mi:“MI:0217”(phosphorylation reaction)	0.440
AIFM1	SEC16A	psi-mi:“MI:2364”(proximity)	0.420
H3C1	SMCHD1	psi-mi:“MI:2364”(proximity)	0.410
	DKC1	psi-mi:“MI:0914”(association)	0.350
Srp72		psi-mi:“MI:0914”(association)	0.350
Rrbp1	PIPSL	psi-mi:“MI:0914”(association)	0.350
HNRNPU		psi-mi:“MI:0914”(association)	0.350
JUN	TPM3	psi-mi:“MI:0914”(association)	0.350
PHACTR3	KCNK3	psi-mi:“MI:0914”(association)	0.350
RRP1B	ZNF785	psi-mi:“MI:0914”(association)	0.350
ZC3H18	SAP18	psi-mi:“MI:0914”(association)	0.350
NEK4	QSOX1	psi-mi:“MI:0914”(association)	0.350
Prdm16	ESYT2	psi-mi:“MI:0914”(association)	0.350
Mecom	ESYT2	psi-mi:“MI:0914”(association)	0.350
PRKAR1A	RBFOX3	psi-mi:“MI:0914”(association)	0.350
PRKAR1A	ADAM10	psi-mi:“MI:0914”(association)	0.350
SH3GL3	RBFOX3	psi-mi:“MI:0914”(association)	0.350
JMJD4	SPTLC1	psi-mi:“MI:0914”(association)	0.350
ESR1		psi-mi:“MI:0914”(association)	0.350
E2F1	IGF2BP3	psi-mi:“MI:0914”(association)	0.350

BioGRID (196): RPL36A (Affinity Capture-MS), RPL36A (Two-hybrid), RPL36A (Affinity Capture-MS), RPL36A (Proximity Label-MS), RPL36A (Affinity Capture-MS), RPL36A (Affinity Capture-MS), RPL36A (Affinity Capture-MS), RPL36A (Biochemical Activity), RPL36A (Proximity Label-MS), RPL36A (Affinity Capture-MS), RPL36A (Affinity Capture-MS), RPL36A (Affinity Capture-MS), RPL36A (Affinity Capture-MS), RPL36A (Negative Genetic), RPL36A (Negative Genetic)

ESM2 similar proteins: A0A1D8PEV4, A8PCG3, A9L948, D0VWQ4, G1T040, O23290, O27365, O28936, O59870, O97231, P0CQ50, P0CQ51, P0CX27, P0CX28, P17843, P27074, P27075, P27076, P31027, P31028, P31866, P36533, P48166, P49213, P52809, P54027, P61485, P61486, P61487, P83881, P83882, P83883, P83884, P90702, Q00477, Q22X38, Q3ISI8, Q3SZ59, Q4PNY0, Q55CW5

Diamond homologs: A0A1D8PEV4, A8PCG3, A9L948, B8D537, D0VWQ4, F2L1X6, G1T040, O23290, O27365, O59870, O97231, P0CQ50, P0CQ51, P0CX27, P0CX28, P17843, P27074, P27075, P27076, P31027, P31028, P31866, P48166, P49213, P52809, P61485, P61486, P61487, P83881, P83882, P83883, P83884, P90702, Q00477, Q22X38, Q3SZ59, Q4PNY0, Q55CW5, Q5R9D2, Q6BLK0

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
RPL36A	“form complex”	“60S cytosolic large ribosomal subunit”	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 77 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
Formation of a pool of free 40S subunits	7	14.8×	1e-04
Peptide chain elongation	6	14.4×	3e-04
Viral mRNA Translation	6	14.4×	3e-04
PELO:HBS1L and ABCE1 dissociate a ribosome on a non-stop mRNA	6	14.2×	3e-04
Selenocysteine synthesis	6	13.6×	3e-04
Eukaryotic Translation Termination	6	13.6×	3e-04
L13a-mediated translational silencing of Ceruloplasmin expression	7	13.3×	1e-04
Nonsense Mediated Decay (NMD) independent of the Exon Junction Complex (EJC)	6	13.3×	3e-04

GO biological processes:

GO term	Partners	Fold	FDR
cytoplasmic translation	7	19.1×	2e-05
rRNA processing	9	18.7×	7e-07
translation	7	10.6×	9e-04
positive regulation of apoptotic process	8	6.7×	4e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	0
Uncertain significance	4
Likely benign	0
Benign	1

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
2425021	NC_000023.10:g.(?99551275)(101097764_?)del	Pathogenic

SpliceAI

0 predictions. Top by Δscore:

AlphaMissense

692 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
X:101391794:G:A	G50E	1.000
X:101391794:G:T	G50V	1.000
X:101395340:A:C	K61N	1.000
X:101395340:A:T	K61N	1.000
X:101395417:G:C	R87T	1.000
X:101395417:G:T	R87I	1.000
X:101395418:A:C	R87S	1.000
X:101395418:A:T	R87S	1.000
X:101395421:C:G	C88W	1.000
X:101391466:T:A	V4D	0.999
X:101391489:T:C	C12R	0.999
X:101391523:T:A	V23E	0.999
X:101391531:T:C	Y26H	0.999
X:101391536:G:C	K27N	0.999
X:101391536:G:T	K27N	0.999
X:101391564:G:A	G37R	0.999
X:101391564:G:C	G37R	0.999
X:101391755:G:A	G37E	0.999
X:101391755:G:T	G37V	0.999
X:101391766:T:C	Y41H	0.999
X:101391777:G:C	K44N	0.999
X:101391777:G:T	K44N	0.999
X:101391784:G:C	G47R	0.999
X:101391785:G:A	G47D	0.999
X:101391785:G:T	G47V	0.999
X:101391793:G:A	G50R	0.999
X:101391793:G:C	G50R	0.999
X:101391793:G:T	G50W	0.999
X:101391798:A:C	Q51H	0.999
X:101391798:A:T	Q51H	0.999

dbSNP variants (sampled 300 via entrez): RS1000073656 (X:101389238 T>C), RS1000424934 (X:101389643 C>T), RS1003026035 (X:101396587 G>T), RS1003413854 (X:101393358 T>C), RS1003487732 (X:101395955 A>T), RS1004254248 (X:101389950 C>T), RS1006320701 (X:101395863 G>A), RS1006371623 (X:101394942 C>T), RS1007495242 (X:101394236 A>G), RS1007548961 (X:101393990 T>A), RS1007831666 (X:101392369 G>A,T), RS1009210823 (X:101396009 G>A), RS1010734880 (X:101394185 T>C,G), RS1010786947 (X:101393911 G>C), RS1012014843 (X:101393297 C>A,G)

Disease associations

OMIM: gene MIM:300902 | 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): CHEMBL3987582 (PROTEIN NUCLEIC-ACID COMPLEX)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds).

Molecule	Name	Phase	Patents
CHEMBL6067484	GENTAMICIN SULFATE	4

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

ChEMBL bioactivities

46 potent at pChembl≥5 of 50 total, top 45 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
6.52	IC50	300	nM	CHEMBL4109308
6.42	IC50	380	nM	CHEMBL4109308
6.42	IC50	380	nM	CHEMBL4574496
6.41	IC50	390	nM	CHEMBL4126894
6.39	IC50	410	nM	CHEMBL4114159
6.35	IC50	450	nM	CHEMBL4126496
6.30	IC50	500	nM	CHEMBL4574496
6.30	IC50	500	nM	CHEMBL4560206
6.16	IC50	690	nM	CHEMBL4130157
6.15	IC50	710	nM	CHEMBL4108338
6.11	IC50	780	nM	CHEMBL4114159
6.09	IC50	820	nM	CHEMBL4109308
6.07	IC50	850	nM	CHEMBL4107559
6.07	IC50	850	nM	CHEMBL4533299
6.05	IC50	900	nM	CHEMBL4126894
6.05	IC50	900	nM	CHEMBL4126496
6.04	IC50	920	nM	CHEMBL4554909
5.97	IC50	1060	nM	CHEMBL4128388
5.89	IC50	1290	nM	CHEMBL4130157
5.86	IC50	1370	nM	CHEMBL4107559
5.84	IC50	1440	nM	CHEMBL4108338
5.81	IC50	1540	nM	CHEMBL4534859
5.76	IC50	1730	nM	CHEMBL4534859
5.69	IC50	2050	nM	CHEMBL4566239
5.68	IC50	2080	nM	CHEMBL4446635
5.66	IC50	2210	nM	CHEMBL4446635
5.66	EC50	2200	nM	CHEMBL4464929
5.64	IC50	2270	nM	CHEMBL4533299
5.63	IC50	2330	nM	CHEMBL4566239
5.62	IC50	2380	nM	CHEMBL4128388
5.58	IC50	2630	nM	CHEMBL4128250
5.55	IC50	2820	nM	CHEMBL4127458
5.53	IC50	2970	nM	CHEMBL4127311
5.51	IC50	3080	nM	CHEMBL4126072
5.46	IC50	3500	nM	CHEMBL4525277
5.44	IC50	3630	nM	CHEMBL4469712
5.39	IC50	4100	nM	CHEMBL4128560
5.37	IC50	4300	nM	CHEMBL4127016
5.36	IC50	4380	nM	CHEMBL4527910
5.16	IC50	7000	nM	CHEMBL4109308
5.13	IC50	7400	nM	CHLORAMPHENICOL SULFATE SALT
5.09	IC50	8040	nM	CHEMBL4128250
5.08	IC50	8370	nM	CHEMBL4128250
5.03	IC50	9320	nM	CHEMBL4127016
5.03	IC50	9240	nM	CHEMBL4128560

PubChem BioAssay actives

46 with measured affinity, of 205 total; 26 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
N-(3-chloro-2-pyridinyl)-N-[(3R)-piperidin-3-yl]-4-(triazolo[4,5-b]pyridin-3-yl)benzamide	1585498: Binding affinity to 80S ribosome in human HuH7 cells expressing human C-terminal V5/6-His-tagged PCSK9 assessed as inhibition of PCSK9 secretion after 16 to 24 hrs by AlphaLISA method	ic50	0.3000	uM
N-(3-chloro-2-pyridinyl)-N-[(3R)-piperidin-3-yl]-3-[4-(triazolo[4,5-b]pyridin-3-yl)phenyl]propanamide	1532845: Binding affinity to 80S ribosome in human HuH7 cells harboring human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	ic50	0.3800	uM
N-isoquinolin-1-yl-N-[(3R)-piperidin-3-yl]-4-(triazolo[4,5-b]pyridin-3-yl)benzamide	1497947: Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	ic50	0.3900	uM
N-(3-chloro-2-pyridinyl)-4-(6-methyltriazolo[4,5-b]pyridin-3-yl)-N-[(3R)-piperidin-3-yl]benzamide	1497947: Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	ic50	0.4100	uM
N-(3-chloro-2-pyridinyl)-4-(5-methyltriazolo[4,5-b]pyridin-3-yl)-N-[(3R)-piperidin-3-yl]benzamide	1497947: Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	ic50	0.4500	uM
N-(1-methylpyrrolo[2,3-c]pyridin-7-yl)-4-phenyl-N-[(3R)-piperidin-3-yl]piperidine-1-carboxamide	1532846: Binding affinity to 80S ribosome in human HeLa cells lysates using human full length PCSK9 encoding mRNAs assessed as inhibition of PCSK9 mRNA translation after 45 mins by Steady-Glo luciferase reporter gene assay	ic50	0.5000	uM
N-isoquinolin-1-yl-N-[(3R)-piperidin-3-yl]-4-pyrazolo[1,5-a]pyrimidin-3-ylbenzamide	1497947: Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	ic50	0.6900	uM
N-(3-chloro-2-pyridinyl)-N-[(3R)-piperidin-3-yl]-5-(triazolo[4,5-b]pyridin-3-yl)pyridine-2-carboxamide	1497947: Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	ic50	0.7100	uM
N-(3-chloro-2-pyridinyl)-3-[5-(6-methyltriazolo[4,5-b]pyridin-3-yl)-2-pyridinyl]-N-[(3R)-piperidin-3-yl]propanamide	1532845: Binding affinity to 80S ribosome in human HuH7 cells harboring human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	ic50	0.8500	uM
N-(3-chloro-2-pyridinyl)-5-(6-methyltriazolo[4,5-b]pyridin-3-yl)-N-[(3R)-piperidin-3-yl]pyridine-2-carboxamide	1497947: Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	ic50	0.8500	uM
N-(3-methyl-2-pyridinyl)-N-[(3R)-piperidin-3-yl]-4-pyrazolo[1,5-a]pyrimidin-3-ylpiperidine-1-carboxamide	1532846: Binding affinity to 80S ribosome in human HeLa cells lysates using human full length PCSK9 encoding mRNAs assessed as inhibition of PCSK9 mRNA translation after 45 mins by Steady-Glo luciferase reporter gene assay	ic50	0.9200	uM
N-isoquinolin-1-yl-4-(1-methylpyrazol-4-yl)-N-[(3R)-piperidin-3-yl]benzamide	1497947: Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	ic50	1.0600	uM
N-isoquinolin-1-yl-4-phenyl-N-[(3R)-piperidin-3-yl]piperidine-1-carboxamide	1532846: Binding affinity to 80S ribosome in human HeLa cells lysates using human full length PCSK9 encoding mRNAs assessed as inhibition of PCSK9 mRNA translation after 45 mins by Steady-Glo luciferase reporter gene assay	ic50	1.5400	uM
N-(3-methyl-2-pyridinyl)-4-phenyl-N-[(3R)-piperidin-3-yl]piperidine-1-carboxamide	1532845: Binding affinity to 80S ribosome in human HuH7 cells harboring human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	ic50	2.0500	uM
N-(3-chloro-2-pyridinyl)-4-phenyl-N-[(3R)-piperidin-3-yl]piperidine-1-carboxamide	1532846: Binding affinity to 80S ribosome in human HeLa cells lysates using human full length PCSK9 encoding mRNAs assessed as inhibition of PCSK9 mRNA translation after 45 mins by Steady-Glo luciferase reporter gene assay	ic50	2.0800	uM
N-(5,8-dihydroisoquinolin-1-yl)-3-(4-methoxyphenyl)-N-[(3R)-piperidin-3-yl]propanamide	1584424: Inhibition of human 80S ribosome-mediated PCSK9 translation expressed in CHO-K1 cells assessed as reduction in PCSK9 secretion	ec50	2.2000	uM
N-isoquinolin-1-yl-3-(4-methoxyphenyl)-N-[(3R)-piperidin-3-yl]propanamide	1497947: Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	ic50	2.6300	uM
N-(3-chloro-2-pyridinyl)-4-(6-methylpyrazin-2-yl)-N-[(3R)-piperidin-3-yl]benzamide	1497963: Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISA	ic50	2.8200	uM
N-(3-chloro-2-pyridinyl)-4-[6-(dimethylamino)pyrazin-2-yl]-N-[(3R)-piperidin-3-yl]benzamide	1497963: Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISA	ic50	2.9700	uM
N-(3-chloro-2-pyridinyl)-4-[6-(methylamino)pyrazin-2-yl]-N-[(3R)-piperidin-3-yl]benzamide	1497963: Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISA	ic50	3.0800	uM
N-isoquinolin-1-yl-4-(6-methyl-1,2-benzoxazol-3-yl)-N-[(3R)-piperidin-3-yl]piperazine-1-carboxamide	1532845: Binding affinity to 80S ribosome in human HuH7 cells harboring human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	ic50	3.5000	uM
N-(3-methylpyrazin-2-yl)-4-phenyl-N-[(3R)-piperidin-3-yl]piperidine-1-carboxamide	1532846: Binding affinity to 80S ribosome in human HeLa cells lysates using human full length PCSK9 encoding mRNAs assessed as inhibition of PCSK9 mRNA translation after 45 mins by Steady-Glo luciferase reporter gene assay	ic50	3.6300	uM
N-(3-chloro-2-pyridinyl)-N-[(3R)-piperidin-3-yl]-6-(triazolo[4,5-b]pyridin-3-yl)pyridine-3-carboxamide	1497947: Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	ic50	4.1000	uM
N-isoquinolin-1-yl-N-[(3R)-piperidin-3-yl]-4-pyrazin-2-ylbenzamide	1497947: Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	ic50	4.3000	uM
4-(2-fluorophenyl)-N-(3-methyl-2-pyridinyl)-N-[(3R)-piperidin-3-yl]piperidine-1-carboxamide	1532846: Binding affinity to 80S ribosome in human HeLa cells lysates using human full length PCSK9 encoding mRNAs assessed as inhibition of PCSK9 mRNA translation after 45 mins by Steady-Glo luciferase reporter gene assay	ic50	4.3800	uM
2,2-dichloro-N-[(1R,2R)-1,3-dihydroxy-1-(4-nitrophenyl)propan-2-yl]acetamide;sulfuric acid	717551: Inhibition of mitochondrial ribosome-mediated protein synthesis in human HeLa cells assessed as {35S]methionine incorporation by autoradiography	ic50	7.4000	uM

CTD chemical–gene interactions

41 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression, affects binding, increases reaction	3
bisphenol F	increases expression, affects cotreatment	2
Air Pollutants	affects cotreatment, increases abundance, increases expression, decreases expression	2
aristolochic acid I	decreases expression	1
dicrotophos	decreases expression	1
triphenyl phosphate	affects expression	1
alpha-pinene	increases expression, increases abundance, affects cotreatment	1
bisphenol A	decreases expression	1
beta-lapachone	increases expression	1
arsenite	affects binding, increases reaction	1
perfluorooctanoic acid	increases expression	1
methacrylaldehyde	affects cotreatment, increases expression, increases abundance	1
epigallocatechin gallate	decreases expression	1
di-n-butylphosphoric acid	affects expression	1
CGP 52608	affects binding, increases reaction	1
CD 437	decreases expression	1
3-(4’-hydroxy-3’-adamantylbiphenyl-4-yl)acrylic acid	decreases expression	1
ICG 001	decreases expression	1
bisphenol B	increases expression	1
abrine	decreases expression	1
bisphenol S	increases expression	1
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acid	decreases expression	1
Arsenic Trioxide	increases expression	1
Acrolein	affects cotreatment, increases expression, increases abundance	1
Amiodarone	increases expression	1
Benzo(a)pyrene	affects methylation, increases methylation	1
Caffeine	decreases expression	1
Dexamethasone	increases expression, affects cotreatment	1
Enzyme Inhibitors	decreases activity, increases O-linked glycosylation	1
Estradiol	decreases expression	1

ChEMBL screening assays

89 unique, capped per target: 89 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1920845	Binding	Induction of ribosome to readthrough in human A-T lymphoblastoid cells assessed as ATM ser1981 autophosphorylation at 30 uM after 4 days by PTT-ELISA assay	Synthesis and evaluation of compounds that induce readthrough of premature termination codons. — Bioorg Med Chem Lett

Cellosaurus cell lines

1 cell lines: 1 cancer cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_B2E3	Abcam HeLa RPL36A KO	Cancer cell line	Female

Clinical trials (associated diseases)

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