RPL18A

Summary

RPL18A (ribosomal protein L18a, HGNC:10311) is a protein-coding gene on chromosome 19p13.11, encoding Large ribosomal subunit protein eL20 (Q02543). Component of the large 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 member of the L18AE family of ribosomal proteins that is a component of the 60S subunit. The encoded protein may play a role in viral replication by interacting with the hepatitis C virus internal ribosome entry site (IRES). This gene is co-transcribed with the U68 snoRNA, located within the third intron. As is typical for genes encoding ribosomal proteins, there are multiple processed pseudogenes of this gene dispersed throughout the genome.

Source: NCBI Gene 6142 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 33 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_000980

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:10311
Approved symbol	RPL18A
Name	ribosomal protein L18a
Location	19p13.11
Locus type	gene with protein product
Status	Approved
Aliases	L18A, eL20
Ensembl gene	ENSG00000105640
Ensembl biotype	protein_coding
OMIM	604178
Entrez	6142

Gene structure

Transcript identifiers

Ensembl transcripts: 17 — 15 protein_coding, 2 retained_intron

ENST00000222247, ENST00000597648, ENST00000599870, ENST00000599898, ENST00000600147, ENST00000600238, ENST00000602216, ENST00000878958, ENST00000916998, ENST00000916999, ENST00000917000, ENST00000917001, ENST00000917002, ENST00000917003, ENST00000917004, ENST00000917005, ENST00000917006

RefSeq mRNA: 1 — MANE Select: NM_000980 NM_000980

CCDS: CCDS12367

Canonical transcript exons

ENST00000222247 — 5 exons

Exon	Start	End
ENSE00000689839	17862094	17862223
ENSE00000689842	17862918	17863027
ENSE00002986563	17863171	17863319
ENSE00002995368	17859910	17859974
ENSE00003575361	17861293	17861472

Expression profiles

Bgee: expression breadth ubiquitous, 158 present calls, max score 99.90.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 22.7064 / max 212.1675, expressed in 1784 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
174555	21.3083	1783
174554	1.3981	752

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
skin of leg	UBERON:0001511	99.90	gold quality
zone of skin	UBERON:0000014	99.89	gold quality
skin of abdomen	UBERON:0001416	99.89	gold quality
left ovary	UBERON:0002119	99.88	gold quality
granulocyte	CL:0000094	99.87	gold quality
right ovary	UBERON:0002118	99.87	gold quality
endocervix	UBERON:0000458	99.86	gold quality
ovary	UBERON:0000992	99.86	gold quality
lymph node	UBERON:0000029	99.85	gold quality
body of stomach	UBERON:0001161	99.85	gold quality
right uterine tube	UBERON:0001302	99.85	gold quality
left uterine tube	UBERON:0001303	99.85	gold quality
spleen	UBERON:0002106	99.85	gold quality
body of uterus	UBERON:0009853	99.85	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	99.84	gold quality
vagina	UBERON:0000996	99.84	gold quality
saliva-secreting gland	UBERON:0001044	99.84	gold quality
right lobe of thyroid gland	UBERON:0001119	99.84	gold quality
fundus of stomach	UBERON:0001160	99.84	gold quality
minor salivary gland	UBERON:0001830	99.84	gold quality
subcutaneous adipose tissue	UBERON:0002190	99.84	gold quality
fallopian tube	UBERON:0003889	99.84	gold quality
mucosa of transverse colon	UBERON:0004991	99.84	gold quality
cortical plate	UBERON:0005343	99.84	gold quality
ectocervix	UBERON:0012249	99.84	gold quality
muscle layer of sigmoid colon	UBERON:0035805	99.84	gold quality
adipose tissue	UBERON:0001013	99.83	gold quality
left lobe of thyroid gland	UBERON:0001120	99.83	gold quality
body of pancreas	UBERON:0001150	99.83	gold quality
transverse colon	UBERON:0001157	99.83	gold quality

Single-cell (SCXA)

Detected in 35 experiment(s), a significant marker in 18.

Experiment	Marker?	Max mean expression
E-MTAB-9067	yes	17183.04
E-CURD-97	yes	16093.73
E-CURD-46	yes	8603.93
E-CURD-88	yes	8006.51
E-HCAD-9	yes	6333.83
E-MTAB-7008	yes	5160.04
E-MTAB-7381	yes	2837.55
E-CURD-122	yes	97.00
E-MTAB-9221	yes	52.37
E-CURD-112	yes	38.42
E-HCAD-31	yes	23.59
E-GEOD-135922	yes	21.72
E-MTAB-10042	yes	17.46
E-GEOD-130148	yes	11.44
E-HCAD-35	yes	9.29

Regulation

Is transcription factor: no

Functional genomics

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

Literature-anchored findings (GeneRIF, showing 1)

• L18a might influence the HCV IRES mediated translation. (PMID:16195786)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
danio_rerio	rpl18a	ENSDARG00000025073
mus_musculus	Rpl18a	ENSMUSG00000045128
rattus_norvegicus	Rpl18a	ENSRNOG00000018795
rattus_norvegicus	AABR07001902.1	ENSRNOG00000042547
drosophila_melanogaster	RpL18A	FBGN0010409
caenorhabditis_elegans		WBGENE00004432

Protein

Protein identifiers

Large ribosomal subunit protein eL20 — Q02543 (reviewed: Q02543)

Alternative names: 60S ribosomal protein L18a

All UniProt accessions (5): Q02543, M0R0P7, M0R117, M0R1A7, M0R3D6

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. Binds IPO9 with high affinity.

Subcellular location. Cytoplasm.

Similarity. Belongs to the eukaryotic ribosomal protein eL20 family.

RefSeq proteins (1): NP_000971* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR021138	Ribosomal_eL20_euk	Family
IPR023573	Ribosomal_eL20_dom	Domain
IPR028877	Ribosomal_eL20	Family

Pfam: PF01775

UniProt features (10 total): modified residue 4, cross-link 3, sequence conflict 2, chain 1

Structure

Experimental structures (PDB)

194 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
8A3D	ELECTRON MICROSCOPY	1.67
8GLP	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
8G5Y	ELECTRON MICROSCOPY	2.29
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
8FKV	ELECTRON MICROSCOPY	2.47
9QLO	ELECTRON MICROSCOPY	2.47
8FLE	ELECTRON MICROSCOPY	2.48
9P8B	ELECTRON MICROSCOPY	2.48

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q02543-F1	96.34	0.97

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 (7): 63, 71, 76, 123, 11, 128, 170

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: 180 (showing top): GOBP_CYTOPLASMIC_TRANSLATION, MODULE_151, ENK_UV_RESPONSE_KERATINOCYTE_UP, MORF_UBE2I, GOBP_STRIATED_MUSCLE_CELL_DIFFERENTIATION, HSIAO_HOUSEKEEPING_GENES, GOBP_MALE_GAMETE_GENERATION, GGCNKCCATNK_UNKNOWN, GOBP_NEGATIVE_REGULATION_OF_CELLULAR_COMPONENT_ORGANIZATION, GOBP_TRANSLATION, GOBP_MUSCLE_STRUCTURE_DEVELOPMENT, GOBP_MUSCLE_CONTRACTION, GOBP_REGULATION_OF_SYNCYTIUM_FORMATION_BY_PLASMA_MEMBRANE_FUSION, GOMF_STRUCTURAL_CONSTITUENT_OF_RIBOSOME, LUI_TARGETS_OF_PAX8_PPARG_FUSION

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): cytoplasm (GO:0005737), cytosol (GO:0005829), postsynaptic density (GO:0014069), membrane (GO:0016020), cytosolic large ribosomal subunit (GO:0022625), cytosolic ribosome (GO:0022626), ribosome (GO:0005840), 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
cellular anatomical structure	3
ribosome	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
intracellular anatomical structure	1
cytoplasm	1
asymmetric synapse	1
postsynaptic specialization	1
large ribosomal subunit	1
cytosolic ribosome	1
cytosol	1
intracellular membraneless organelle	1
protein-containing complex	1

Protein interactions and networks

STRING

3113 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
RPL18A	RPS24	P16632	779
RPL18A	RPL21	P46778	768
RPL18A	RPS2	P15880	748
RPL18A	RPL14	P50914	733
RPL18A	RPS8	P09058	726
RPL18A	RPL7	P18124	723
RPL18A	RPLP2	P05387	710
RPL18A	RPS16	P17008	689
RPL18A	RPL27	P08526	686
RPL18A	RPL7A	P11518	674
RPL18A	RPS3A	P33443	665
RPL18A	RPS15A	P39027	664
RPL18A	RPL35	P42766	658
RPL18A	RPL26L1	Q9UNX3	650
RPL18A	RPS25	P25111	646

IntAct

215 interactions, top by confidence:

A	B	Type	Score
MAP3K14	CHUK	psi-mi:“MI:0914”(association)	0.950
XPC	CETN3	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
RPL4	RPL18A	psi-mi:“MI:0915”(physical association)	0.670
RPL10A	RRP8	psi-mi:“MI:0914”(association)	0.640
DHX8	AHCYL1	psi-mi:“MI:0914”(association)	0.640
RACK1	RPS17	psi-mi:“MI:0915”(physical association)	0.610
MAPT	KIF2A	psi-mi:“MI:0914”(association)	0.530
NSA2	TYW5	psi-mi:“MI:0914”(association)	0.530
MAGEB10	GTPBP10	psi-mi:“MI:0914”(association)	0.530
RPL37A	MPHOSPH10	psi-mi:“MI:0914”(association)	0.530
RPL18	NOP56	psi-mi:“MI:0914”(association)	0.530
PRR11	NVL	psi-mi:“MI:0914”(association)	0.530
ZNF71	NVL	psi-mi:“MI:0914”(association)	0.530
RPL8	RRP8	psi-mi:“MI:0914”(association)	0.530
RPL18A	RRP8	psi-mi:“MI:0914”(association)	0.530
MAGEB2	POLRMT	psi-mi:“MI:0914”(association)	0.530
DDX31	MAGEB2	psi-mi:“MI:0914”(association)	0.530
RRP8	MAGEB2	psi-mi:“MI:0914”(association)	0.530
TAF1C	DNAJA2	psi-mi:“MI:0914”(association)	0.530
CFTR	PLEKHG3	psi-mi:“MI:0914”(association)	0.480

BioGRID (777): RPL18A (Affinity Capture-MS), RPL18A (Affinity Capture-MS), RPL18A (Affinity Capture-MS), BRIX1 (Co-fractionation), DDX27 (Co-fractionation), DDX56 (Co-fractionation), EEF1A1 (Co-fractionation), EIF6 (Co-fractionation), NIFK (Co-fractionation), NOC2L (Co-fractionation), NOP2 (Co-fractionation), PES1 (Co-fractionation), RPL10 (Co-fractionation), RPL10A (Co-fractionation), RPL10L (Co-fractionation)

ESM2 similar proteins: A0A1D8PLC9, A0RHY8, A5IRX7, A6U0Q8, A7GS04, A8Z1M9, A9VUD8, B3WE10, B7JKV0, C1EPZ0, C3LI42, C3P6Y3, G1TTY7, O44480, O57561, P0CT68, P0CT69, P0CX23, P0CX24, P0DJ18, P41093, P51418, P62717, P62718, Q02543, Q039P0, Q042S0, Q2FHZ0, Q2FZG8, Q2YX59, Q3T003, Q54MK8, Q5HGZ4, Q5HQ79, Q5WFA1, Q635V2, Q6GAC4, Q6GHZ5, Q6HEI9, Q74JW3

Diamond homologs: A0A1D8PLC9, G1TTY7, O44480, O57561, P0CT68, P0CT69, P0CX23, P0CX24, P0DJ18, P41093, P51418, P62717, P62718, Q02543, Q3T003, Q54MK8, Q7ZWJ4, Q8L7K0, Q8WQI7, Q90YU9, Q943F3, Q9ATF5, Q9LUD4

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
RPL18A	“form complex”	“60S cytosolic large ribosomal subunit”	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 216 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
Peptide chain elongation	19	17.2×	1e-16
Viral mRNA Translation	19	17.2×	1e-16
PELO:HBS1L and ABCE1 dissociate a ribosome on a non-stop mRNA	19	17.0×	1e-16
Selenocysteine synthesis	19	16.3×	2e-16
Eukaryotic Translation Termination	19	16.3×	2e-16
Formation of a pool of free 40S subunits	20	16.0×	1e-16
Nonsense Mediated Decay (NMD) independent of the Exon Junction Complex (EJC)	19	16.0×	3e-16
ZNF598 and the Ribosome-associated Quality Trigger (RQT) complex dissociate a ribosome stalled on a no-go mRNA	19	16.0×	3e-16

GO biological processes:

GO term	Partners	Fold	FDR
positive regulation of transcription by RNA polymerase III	5	25.3×	2e-04
ribosomal large subunit biogenesis	9	21.6×	7e-08
cytoplasmic translation	21	21.0×	3e-19
positive regulation of transcription by RNA polymerase I	6	21.0×	7e-05
negative regulation of mRNA splicing, via spliceosome	5	20.7×	5e-04
rRNA processing	16	12.2×	9e-11
translation	22	12.2×	4e-15
mRNA stabilization	6	11.9×	1e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	25
Likely benign	0
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

748 predictions. Top by Δscore:

Variant	Effect	Δscore
19:17859970:GCACG:G	donor_gain	1.0000
19:17859975:G:GG	donor_gain	1.0000
19:17859976:T:A	donor_loss	1.0000
19:17862088:T:TA	acceptor_gain	1.0000
19:17862091:CA:C	acceptor_loss	1.0000
19:17862092:A:AG	acceptor_gain	1.0000
19:17862092:AG:A	acceptor_gain	1.0000
19:17862092:AGGT:A	acceptor_gain	1.0000
19:17862093:G:GA	acceptor_gain	1.0000
19:17862093:GG:G	acceptor_gain	1.0000
19:17862093:GGT:G	acceptor_gain	1.0000
19:17862093:GGTG:G	acceptor_gain	1.0000
19:17862093:GGTGT:G	acceptor_gain	1.0000
19:17862219:GTGCT:G	donor_gain	1.0000
19:17862220:TGCT:T	donor_gain	1.0000
19:17862221:GCT:G	donor_gain	1.0000
19:17862221:GCTG:G	donor_gain	1.0000
19:17862222:CTGT:C	donor_loss	1.0000
19:17862224:G:GG	donor_gain	1.0000
19:17862225:T:A	donor_loss	1.0000
19:17862915:C:G	acceptor_gain	1.0000
19:17862915:CA:C	acceptor_loss	1.0000
19:17862916:A:AG	acceptor_gain	1.0000
19:17862916:A:C	acceptor_loss	1.0000
19:17862916:AGACC:A	acceptor_gain	1.0000
19:17862917:G:GC	acceptor_gain	1.0000
19:17862917:GA:G	acceptor_gain	1.0000
19:17862917:GAC:G	acceptor_gain	1.0000
19:17862917:GACC:G	acceptor_gain	1.0000
19:17862917:GACCG:G	acceptor_gain	1.0000

AlphaMissense

1139 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
19:17861371:T:C	F33L	1.000
19:17861373:T:A	F33L	1.000
19:17861373:T:G	F33L	1.000
19:17861393:C:A	A40D	1.000
19:17861404:T:C	F44L	1.000
19:17861406:C:A	F44L	1.000
19:17861406:C:G	F44L	1.000
19:17861407:T:A	W45R	1.000
19:17861407:T:C	W45R	1.000
19:17861450:G:A	G59E	1.000
19:17862126:C:A	N77K	1.000
19:17862126:C:G	N77K	1.000
19:17862131:G:A	G79E	1.000
19:17862136:T:A	W81R	1.000
19:17862136:T:C	W81R	1.000
19:17862140:T:C	L82P	1.000
19:17862145:T:C	Y84H	1.000
19:17862151:T:C	S86P	1.000
19:17862152:C:T	S86F	1.000
19:17862154:C:T	R87W	1.000
19:17862166:C:G	H91D	1.000
19:17862171:C:A	N92K	1.000
19:17862171:C:G	N92K	1.000
19:17862179:G:C	R95P	1.000
19:17862188:G:C	R98P	1.000
19:17862212:T:A	V106D	1.000
19:17862220:T:C	C109R	1.000
19:17862221:G:A	C109Y	1.000
19:17862222:C:G	C109W	1.000
19:17862921:G:C	R111P	1.000

dbSNP variants (sampled 300 via entrez): RS1000078583 (19:17858334 C>G), RS1000262 (19:17859818 C>A,G,T), RS1000338719 (19:17861301 G>C), RS1000665306 (19:17860344 G>A), RS1000718570 (19:17860554 C>G,T), RS1001422649 (19:17862035 T>C), RS1001875539 (19:17862334 G>A), RS1001941410 (19:17860832 G>A), RS1002676545 (19:17858401 G>A,C,T), RS1003499292 (19:17861101 C>A,T), RS1003841554 (19:17860862 C>G,T), RS1003883741 (19:17860378 C>G,T), RS1004419666 (19:17860632 G>C,T), RS1005599323 (19:17860054 G>A), RS1005974181 (19:17858920 C>T)

Disease associations

OMIM: gene MIM:604178 | disease phenotypes: MIM:600802

GenCC curated gene-disease

Mondo (1): T-B+ severe combined immunodeficiency due to JAK3 deficiency (MONDO:0010938)

Orphanet (1): T-B+ severe combined immunodeficiency due to JAK3 deficiency (Orphanet:35078)

HPO phenotypes

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

GWAS associations

0 associations (top):

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
C563440	Severe Combined Immunodeficiency, Autosomal Recessive, T Cell-Negative, B Cell-Positive, NK Cell-Negative (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL3987582 (PROTEIN NUCLEIC-ACID COMPLEX), CHEMBL6067541 (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
7.01	Kd	98.14	nM	CHEMBL3752910
7.01	ED50	98.14	nM	CHEMBL3752910
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
5.50	Kd	3154	nM	CHEMBL5653589
5.50	ED50	3154	nM	CHEMBL5653589
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-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149249: Binding affinity to human RPL18A incubated for 45 mins by Kinobead based pull down assay	kd	0.0981	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
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
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149249: Binding affinity to human RPL18A incubated for 45 mins by Kinobead based pull down assay	kd	3.1541	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

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

Chemical	Actions (top 5)	PubMed papers
bisphenol A	decreases expression	2
sodium arsenite	decreases expression, affects cotreatment, increases abundance, increases expression	2
Valproic Acid	affects cotreatment, increases expression, increases methylation	2
Particulate Matter	decreases expression, increases abundance, increases expression	2
aristolochic acid I	decreases expression	1
FR900359	increases phosphorylation	1
bisphenol F	increases expression	1
TAK-243	increases sumoylation	1
triphenyl phosphate	affects expression	1
deoxynivalenol	increases expression	1
pyrogallol 1,3-dimethyl ether	affects cotreatment, affects localization, increases expression	1
beta-lapachone	increases expression	1
arsenite	affects binding, increases reaction	1
manganese chloride	affects cotreatment, increases abundance, increases expression	1
potassium chromate(VI)	affects cotreatment, increases expression	1
coumarin	increases phosphorylation	1
epigallocatechin gallate	affects cotreatment, increases expression	1
chloropicrin	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
3-(4’-hydroxy-3’-adamantylbiphenyl-4-yl)acrylic acid	decreases expression	1
bisphenol B	increases expression	1
bisphenol S	affects expression	1
LDN 193189	decreases expression, affects cotreatment	1
bisphenol AF	increases expression	1
Arsenic Trioxide	decreases expression	1
Air Pollutants	decreases expression, increases abundance	1
Arsenic	affects cotreatment, increases abundance, increases expression	1
Vehicle Emissions	increases abundance, increases expression	1
Cadmium	increases expression	1
Cuprizone	affects cotreatment, increases expression, decreases 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.