RPS18

Summary

RPS18 (ribosomal protein S18, HGNC:10401) is a protein-coding gene on chromosome 6p21.32, encoding Small ribosomal subunit protein uS13 (P62269). Component of the small ribosomal subunit. It is a common-essential gene (DepMap: required in 100.0% of cancer cell lines).

Ribosomes, the 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 40S subunit. The protein belongs to the S13P family of ribosomal proteins. It is located in the cytoplasm. The gene product of the E. coli ortholog (ribosomal protein S13) is involved in the binding of fMet-tRNA, and thus, in the initiation of translation. This gene is an ortholog of mouse Ke3. As is typical for genes encoding ribosomal proteins, there are multiple processed pseudogenes of this gene dispersed through the genome.

Source: NCBI Gene 6222 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 9 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 100.0% of screened cell lines (common-essential)
• MANE Select transcript: NM_022551

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:10401
Approved symbol	RPS18
Name	ribosomal protein S18
Location	6p21.32
Locus type	gene with protein product
Status	Approved
Aliases	KE3, KE-3, HKE3, S18, uS13
Ensembl gene	ENSG00000231500
Ensembl biotype	protein_coding
OMIM	180473
Entrez	6222

Gene structure

Transcript identifiers

Ensembl transcripts: 13 — 7 protein_coding, 5 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000439602, ENST00000472218, ENST00000474626, ENST00000474973, ENST00000476222, ENST00000479802, ENST00000490191, ENST00000496813, ENST00000893314, ENST00000940273, ENST00000940274, ENST00000940275, ENST00000940276

RefSeq mRNA: 1 — MANE Select: NM_022551 NM_022551

CCDS: CCDS4771

Canonical transcript exons

ENST00000211372 — 0 exons

Expression profiles

Bgee: expression breadth ubiquitous, 134 present calls, max score 99.97.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 387.1501 / max 3216.3779, expressed in 1823 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
67262	387.1501	1823

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
ovary	UBERON:0000992	99.97	gold quality
skin of leg	UBERON:0001511	99.97	gold quality
right ovary	UBERON:0002118	99.97	gold quality
left ovary	UBERON:0002119	99.97	gold quality
zone of skin	UBERON:0000014	99.96	gold quality
lymph node	UBERON:0000029	99.96	gold quality
endocervix	UBERON:0000458	99.96	gold quality
skin of abdomen	UBERON:0001416	99.96	gold quality
ectocervix	UBERON:0012249	99.96	gold quality
vagina	UBERON:0000996	99.95	gold quality
right uterine tube	UBERON:0001302	99.95	gold quality
left uterine tube	UBERON:0001303	99.95	gold quality
fallopian tube	UBERON:0003889	99.95	gold quality
thoracic mammary gland	UBERON:0005200	99.95	gold quality
cortical plate	UBERON:0005343	99.95	gold quality
body of uterus	UBERON:0009853	99.95	gold quality
granulocyte	CL:0000094	99.94	gold quality
stromal cell of endometrium	CL:0002255	99.94	gold quality
uterine cervix	UBERON:0000002	99.94	gold quality
adipose tissue	UBERON:0001013	99.94	gold quality
myometrium	UBERON:0001296	99.94	gold quality
subcutaneous adipose tissue	UBERON:0002190	99.94	gold quality
prostate gland	UBERON:0002367	99.94	gold quality
esophagus mucosa	UBERON:0002469	99.94	gold quality
mucosa of transverse colon	UBERON:0004991	99.94	gold quality
omental fat pad	UBERON:0010414	99.94	gold quality
islet of Langerhans	UBERON:0000006	99.93	gold quality
rectum	UBERON:0001052	99.93	gold quality
right lobe of thyroid gland	UBERON:0001119	99.93	gold quality
left lobe of thyroid gland	UBERON:0001120	99.93	gold quality

Single-cell (SCXA)

Detected in 39 experiment(s), a significant marker in 14.

Experiment	Marker?	Max mean expression
E-MTAB-9067	yes	11397.88
E-MTAB-11268	yes	7718.33
E-CURD-112	yes	4128.35
E-CURD-122	yes	3366.97
E-GEOD-84465	yes	2785.63
E-MTAB-6678	yes	2783.58
E-MTAB-10042	yes	1878.51
E-MTAB-8142	yes	132.06
E-MTAB-9221	yes	55.12
E-HCAD-31	yes	23.38
E-MTAB-9543	yes	11.91
E-HCAD-35	yes	10.99
E-GEOD-137537	yes	6.77
E-MTAB-9801	yes	6.68
E-MTAB-10287	no	14320.59

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): MYC

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 100.0% of screened cell lines, common-essential.

Literature-anchored findings (GeneRIF, showing 2)

• cofilin interacts with S18 protein at the actin-binding site (PMID:15532723)
• Ribosomal protein S18e seems to act as a molecular staple fixing the 18S rRNA 3’-major domain core. (PMID:21256985)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	rps18	ENSDARG00000100392
mus_musculus	Rps18	ENSMUSG00000008668
rattus_norvegicus	Rps18l1	ENSRNOG00000033152
drosophila_melanogaster	RpS18	FBGN0010411
caenorhabditis_elegans		WBGENE00004487

Protein

Protein identifiers

Small ribosomal subunit protein uS13 — P62269 (reviewed: P62269)

Alternative names: 40S ribosomal protein S18, Ke-3

All UniProt accessions (2): P62269, J3JS69

UniProt curated annotations — full annotation on UniProt →

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

Subunit / interactions. Component of the small ribosomal subunit.

Subcellular location. Cytoplasm.

Similarity. Belongs to the universal ribosomal protein uS13 family.

RefSeq proteins (1): NP_072045* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001892	Ribosomal_uS13	Family
IPR010979	Ribosomal_uS13-like_H2TH	Homologous_superfamily
IPR018269	Ribosomal_uS13_CS	Conserved_site
IPR027437	Rbsml_uS13_C	Homologous_superfamily

Pfam: PF00416

UniProt features (29 total): helix 10, strand 8, modified residue 3, cross-link 3, turn 2, initiator methionine 1, chain 1, sequence conflict 1

Structure

Experimental structures (PDB)

211 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
8GLP	ELECTRON MICROSCOPY	1.67
8QOI	ELECTRON MICROSCOPY	1.9
9O3W	ELECTRON MICROSCOPY	1.9
8YOO	ELECTRON MICROSCOPY	2
9C3H	ELECTRON MICROSCOPY	2
7R4X	ELECTRON MICROSCOPY	2.15
9I2D	ELECTRON MICROSCOPY	2.19
9PBE	ELECTRON MICROSCOPY	2.19
8YOP	ELECTRON MICROSCOPY	2.2
9O3V	ELECTRON MICROSCOPY	2.2
9O3Y	ELECTRON MICROSCOPY	2.2
8JDK	ELECTRON MICROSCOPY	2.26
8G5Y	ELECTRON MICROSCOPY	2.29
9S3D	ELECTRON MICROSCOPY	2.32
9RPV	ELECTRON MICROSCOPY	2.35
9S3B	ELECTRON MICROSCOPY	2.38
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
9P8B	ELECTRON MICROSCOPY	2.48
7XNY	ELECTRON MICROSCOPY	2.5
8JDJ	ELECTRON MICROSCOPY	2.5
9RUC	ELECTRON MICROSCOPY	2.5
8G60	ELECTRON MICROSCOPY	2.54
8IFE	ELECTRON MICROSCOPY	2.57
9P7D	ELECTRON MICROSCOPY	2.57

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P62269-F1	88.95	0.71

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 (6): 2, 94, 106, 91, 94, 106

Function

Pathways and Gene Ontology

Reactome pathways

50 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-72649	Translation initiation complex formation
R-HSA-72689	Formation of a pool of free 40S subunits
R-HSA-72695	Formation of the ternary complex, and subsequently, the 43S complex
R-HSA-72702	Ribosomal scanning and start codon recognition
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-9735869	SARS-CoV-1 modulates host translation machinery
R-HSA-9754678	SARS-CoV-2 modulates host translation machinery
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-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
R-HSA-1266738	Developmental Biology
R-HSA-1430728	Metabolism
R-HSA-156842	Eukaryotic Translation Elongation
R-HSA-1643685	Disease
R-HSA-168255	Influenza Infection
R-HSA-168273	Influenza Viral RNA Transcription and Replication
R-HSA-2262752	Cellular responses to stress
R-HSA-2408522	Selenoamino acid metabolism
R-HSA-376176	Signaling by ROBO receptors
R-HSA-392499	Metabolism of proteins

MSigDB gene sets: 246 (showing top): GOBP_CYTOPLASMIC_TRANSLATION, FREAC2_01, YAGI_AML_WITH_INV_16_TRANSLOCATION, GNF2_TPT1, GCANCTGNY_MYOD_Q6, GCM_NPM1, GRAESSMANN_APOPTOSIS_BY_SERUM_DEPRIVATION_UP, HSIAO_HOUSEKEEPING_GENES, GOBP_TRANSLATION, MARTINEZ_RB1_TARGETS_DN, GOMF_STRUCTURAL_CONSTITUENT_OF_RIBOSOME, BENPORATH_NOS_TARGETS, NRF2_01, MARTORIATI_MDM4_TARGETS_FETAL_LIVER_UP, MODULE_29

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

GO Molecular Function (5): RNA binding (GO:0003723), structural constituent of ribosome (GO:0003735), rRNA binding (GO:0019843), nucleic acid binding (GO:0003676), protein binding (GO:0005515)

GO Cellular Component (15): nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytosol (GO:0005829), ribosome (GO:0005840), focal adhesion (GO:0005925), postsynaptic density (GO:0014069), small ribosomal subunit (GO:0015935), membrane (GO:0016020), cytosolic ribosome (GO:0022626), cytosolic small ribosomal subunit (GO:0022627), extracellular exosome (GO:0070062), collagen trimer (GO:0005581), synapse (GO:0045202), ribonucleoprotein complex (GO:1990904)

Reactome top-level categories

Rollup of top-14 pathways:

Category	Pathways
Cap-dependent Translation Initiation	4
Translation	2
Nonsense-Mediated Decay (NMD)	2
Ribosome-associated quality control	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
Activation of the mRNA upon binding of the cap-binding complex and eIFs, and subsequent binding to 43S	1
Signaling by ROBO receptors	1
Cellular response to starvation	1
SARS-CoV-1-host interactions	1
SARS-CoV-2-host interactions	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	4
ribosome	2
binding	2
protein-containing complex	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
RNA binding	1
intracellular membrane-bounded organelle	1
nuclear lumen	1
intracellular anatomical structure	1
cytoplasm	1
intracellular membraneless organelle	1
cell-substrate junction	1
asymmetric synapse	1
postsynaptic specialization	1
ribosomal subunit	1
cytosol	1
small ribosomal subunit	1
cytosolic ribosome	1
extracellular vesicle	1
cell junction	1

Protein interactions and networks

STRING

0 interactions, top by confidence (×1000):

IntAct

296 interactions, top by confidence:

A	B	Type	Score
MAP3K14	CHUK	psi-mi:“MI:0914”(association)	0.950
FBL	NOP56	psi-mi:“MI:0914”(association)	0.800
H2AX	PPM1G	psi-mi:“MI:0914”(association)	0.730
CFTR	ESYT2	psi-mi:“MI:0914”(association)	0.710
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
NCBP2	KPNA3	psi-mi:“MI:0914”(association)	0.640
ESR1	TRIM24	psi-mi:“MI:0914”(association)	0.640
DDX6	RPLP0	psi-mi:“MI:0915”(physical association)	0.620
RACK1	RPS17	psi-mi:“MI:0915”(physical association)	0.610
RPS18	CSNK2A1	psi-mi:“MI:0217”(phosphorylation reaction)	0.590
MAPT	KIF2A	psi-mi:“MI:0914”(association)	0.530
SYNGAP1	IGF2BP3	psi-mi:“MI:0914”(association)	0.530
RPS18	RPS2	psi-mi:“MI:0914”(association)	0.530
RPS3	ZNF316	psi-mi:“MI:0914”(association)	0.530
DDX6	MCRIP1	psi-mi:“MI:0914”(association)	0.510
CFTR	PLEKHG3	psi-mi:“MI:0914”(association)	0.480
ESR1		psi-mi:“MI:0914”(association)	0.460
ESR2	FBLL1	psi-mi:“MI:0914”(association)	0.460
RBM45	HNRNPDL	psi-mi:“MI:0914”(association)	0.460
FUS	DDX3X	psi-mi:“MI:0914”(association)	0.430
RPS15	RPS18	psi-mi:“MI:0915”(physical association)	0.400

BioGRID (550): RPS18 (Affinity Capture-MS), RPS18 (Affinity Capture-MS), RPS18 (Affinity Capture-MS), RPS18 (Affinity Capture-MS), RPS18 (Affinity Capture-MS), RPS18 (Affinity Capture-MS), RPS18 (Affinity Capture-MS), MRPL24 (Co-fractionation), MRPS10 (Co-fractionation), RPL10A (Co-fractionation), RPL26 (Co-fractionation), RPL26L1 (Co-fractionation), RPL3 (Co-fractionation), RPL31 (Co-fractionation), RPL35 (Co-fractionation)

ESM2 similar proteins: A0A1D8PQQ5, A0B9L1, A1RT04, A3MUT0, A4WM28, A5IMA8, A5JST6, A8F4T6, B1LBL5, B9K8B1, G1TPG3, O26141, O27999, O74021, P0CT66, P0CT67, P0CX55, P0CX56, P34788, P39470, P41094, P48151, P49202, P54019, P62269, P62270, P62271, P62272, Q12ZR6, Q2FT96, Q3T0R1, Q46GC7, Q5JJF1, Q5TJE9, Q6KZP8, Q74M95, Q869U7, Q8ISP0, Q8IT98, Q8JGS9

Diamond homologs: A0A1D8PQQ5, A0B9L1, A0RY01, A1QZT6, A1RT04, A1RWT9, A2BK76, A2SSW0, A3CWH6, A3DMQ3, A3MUT0, A4WM28, A5IMA8, A5IYW1, A5JST6, A5UN52, A6LLN8, A7HM27, A8MLG6, B0B883, B0BCE8, B1AIP4, B1LBL5, B1ZNC6, B2S0K3, B3CN47, B3DVZ3, B3PMM3, B5RM58, B5RPK4, B5YG25, B5ZB64, B7IHX0, B9K8B1, G1TPG3, O26141, O27999, O66486, O74021, P0CE04

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
RPS18	“form complex”	“40S cytosolic small ribosomal subunit”	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 191 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
SARS-CoV-1 modulates host translation machinery	11	24.6×	1e-11
Eukaryotic Translation Initiation	10	22.4×	4e-10
Cap-dependent Translation Initiation	10	22.4×	4e-10
Formation of the ternary complex, and subsequently, the 43S complex	14	21.9×	6e-14
Ribosomal scanning and start codon recognition	15	20.7×	1e-14
Nonsense-Mediated Decay (NMD)	12	20.3×	1e-11
Eukaryotic Translation Elongation	10	20.2×	1e-09
Activation of the mRNA upon binding of the cap-binding complex and eIFs, and subsequent binding to 43S	10	19.7×	1e-09

GO biological processes:

GO term	Partners	Fold	FDR
formation of cytoplasmic translation initiation complex	5	34.2×	3e-05
cytoplasmic translation	21	23.7×	2e-20
stress granule assembly	5	18.4×	7e-04
translational initiation	8	17.5×	4e-06
mRNA stabilization	7	15.6×	4e-05
ribosomal small subunit biogenesis	11	15.3×	5e-08
regulation of translational initiation	5	14.3×	2e-03
ribosomal large subunit biogenesis	5	13.5×	2e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

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

Top pathogenic / likely-pathogenic (0)

SpliceAI

676 predictions. Top by Δscore:

Variant	Effect	Δscore
6:33272174:A:T	donor_gain	1.0000
6:33272256:A:T	donor_gain	1.0000
6:33272261:G:T	donor_gain	1.0000
6:33272285:A:T	donor_gain	1.0000
6:33272299:G:GT	donor_gain	1.0000
6:33272300:A:T	donor_gain	1.0000
6:33272626:A:AG	acceptor_gain	1.0000
6:33272627:G:GG	acceptor_gain	1.0000
6:33272722:TTAAG:T	donor_gain	1.0000
6:33272725:AG:A	donor_gain	1.0000
6:33272726:GG:G	donor_gain	1.0000
6:33272727:G:GG	donor_gain	1.0000
6:33275791:A:AG	acceptor_gain	1.0000
6:33275792:TTCA:T	acceptor_loss	1.0000
6:33275795:A:AG	acceptor_gain	1.0000
6:33275795:AG:A	acceptor_gain	1.0000
6:33275795:AGGGT:A	acceptor_gain	1.0000
6:33275796:G:GT	acceptor_gain	1.0000
6:33275796:GG:G	acceptor_gain	1.0000
6:33275796:GGGT:G	acceptor_gain	1.0000
6:33275796:GGGTG:G	acceptor_gain	1.0000
6:33275878:GA:G	donor_gain	1.0000
6:33275881:GAG:G	donor_gain	1.0000
6:33275881:GAGGT:G	donor_loss	1.0000
6:33275882:AGG:A	donor_loss	1.0000
6:33275883:GGTGA:G	donor_loss	1.0000
6:33275884:G:GA	donor_loss	1.0000
6:33275884:G:GG	donor_gain	1.0000
6:33275885:T:A	donor_loss	1.0000
6:33275959:T:A	acceptor_gain	1.0000

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000382741 (6:33275295 T>A), RS1000874094 (6:33273980 CAG>C), RS1000984609 (6:33276833 C>G,T), RS1001167353 (6:33274701 G>A), RS1001682491 (6:33274401 T>G), RS1002076048 (6:33270403 T>G), RS1002115850 (6:33274978 C>G,T), RS1002696843 (6:33273466 GTCT>G,GTCTTCT), RS1002807468 (6:33273686 C>T), RS1002953315 (6:33273216 T>C), RS1003249161 (6:33273430 C>T), RS1004002807 (6:33275630 T>C), RS1004113816 (6:33275637 G>A), RS1004386991 (6:33270374 G>A), RS1004980258 (6:33274668 C>T)

Disease associations

OMIM: gene MIM:180473 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST004521_287	Autism spectrum disorder or schizophrenia	5.000000e-08
GCST005951_153	Body mass index	5.000000e-09

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0004340	body mass index

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL3987582 (PROTEIN NUCLEIC-ACID COMPLEX), CHEMBL6067556 (SINGLE PROTEIN)

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

50 potent at pChembl≥5 of 54 total, top 49 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.16	Kd	6.909	nM	CHEMBL5653589
8.16	ED50	6.909	nM	CHEMBL5653589
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
5.55	Kd	2790	nM	CHEMBL3752910
5.55	ED50	2790	nM	CHEMBL3752910
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

48 with measured affinity, of 209 total; 28 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
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149291: Binding affinity to human RPS18 incubated for 45 mins by Kinobead based pull down assay	kd	0.0069	uM
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
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149291: Binding affinity to human RPS18 incubated for 45 mins by Kinobead based pull down assay	kd	2.7901	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

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

Chemical	Actions (top 5)	PubMed papers
bisphenol A	affects expression, decreases expression, affects cotreatment	5
sodium arsenite	decreases expression, increases activity	3
bisphenol F	decreases expression, increases expression, affects cotreatment	2
bisphenol S	increases expression, affects cotreatment, decreases expression	2
Arsenic	decreases expression, increases abundance, decreases ubiquitination	2
Particulate Matter	decreases expression, increases expression	2
triphenyl phosphate	affects expression	1
pyrogallol 1,3-dimethyl ether	increases expression, affects cotreatment, affects localization	1
tris(2-butoxyethyl) phosphate	increases expression	1
beta-lapachone	increases expression	1
arsenite	increases reaction, affects binding	1
methylparaben	decreases expression	1
artenimol	affects binding	1
arsenic trichloride	decreases expression, increases abundance	1
perfluorooctane sulfonic acid	increases expression	1
azoxystrobin	increases expression	1
chloropicrin	affects expression	1
deguelin	increases expression	1
fenpyroximate	increases expression	1
4-chloro-N-((4-(1,1-dimethylethyl)phenyl)methyl)-3-ethyl-1-methyl-1H-pyrazole-5-carboxamide	increases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
pyrimidifen	increases expression	1
nutlin 3	affects cotreatment, increases secretion	1
bisphenol B	increases expression	1
pyrachlostrobin	increases expression	1
jinfukang	increases expression	1
LDN 193189	affects cotreatment, decreases expression	1
picoxystrobin	increases expression	1
Temozolomide	increases expression	1
Sunitinib	increases expression	1

ChEMBL screening assays

90 unique, capped per target: 90 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

Clinical trials (associated diseases)

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