RPL38

Summary

RPL38 (ribosomal protein L38, HGNC:10349) is a protein-coding gene on chromosome 17q25.1, encoding Large ribosomal subunit protein eL38 (P63173). Component of the large ribosomal subunit. It is a common-essential gene (DepMap: required in 99.1% 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 60S subunit. The protein belongs to the L38E family of ribosomal proteins. It is located in the cytoplasm. Alternative splice variants have been identified, both encoding the same protein. As is typical for genes encoding ribosomal proteins, there are multiple processed pseudogenes of this gene dispersed through the genome, including one located in the promoter region of the type 1 angiotensin II receptor gene.

Source: NCBI Gene 6169 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 14 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 99.1% of screened cell lines (common-essential)
• MANE Select transcript: NM_000999

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:10349
Approved symbol	RPL38
Name	ribosomal protein L38
Location	17q25.1
Locus type	gene with protein product
Status	Approved
Aliases	L38, eL38
Ensembl gene	ENSG00000172809
Ensembl biotype	protein_coding
OMIM	604182
Entrez	6169

Gene structure

Transcript identifiers

Ensembl transcripts: 17 — 15 protein_coding, 2 retained_intron

ENST00000311111, ENST00000439590, ENST00000528433, ENST00000529123, ENST00000530646, ENST00000533498, ENST00000534490, ENST00000584577, ENST00000910932, ENST00000910933, ENST00000928109, ENST00000928110, ENST00000928111, ENST00000928112, ENST00000928113, ENST00000928114, ENST00000928115

RefSeq mRNA: 2 — MANE Select: NM_000999 NM_000999, NM_001035258

CCDS: CCDS11696

Canonical transcript exons

ENST00000311111 — 5 exons

Exon	Start	End
ENSE00001197499	74209187	74209309
ENSE00001244827	74203678	74203745
ENSE00002174583	74209804	74210655
ENSE00003628049	74203918	74203958
ENSE00003787124	74204130	74204190

Expression profiles

Bgee: expression breadth ubiquitous, 295 present calls, max score 99.91.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 1174.3257 / max 7837.0616, expressed in 1828 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
162578	1172.9110	1828
162579	1.4147	840

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
calcaneal tendon	UBERON:0003701	99.91	gold quality
cortical plate	UBERON:0005343	99.90	gold quality
olfactory bulb	UBERON:0002264	99.89	gold quality
vena cava	UBERON:0004087	99.88	gold quality
left testis	UBERON:0004533	99.88	gold quality
right testis	UBERON:0004534	99.88	gold quality
type B pancreatic cell	CL:0000169	99.87	gold quality
mammary duct	UBERON:0001765	99.87	gold quality
nipple	UBERON:0002030	99.87	gold quality
thymus	UBERON:0002370	99.87	gold quality
medial globus pallidus	UBERON:0002477	99.87	gold quality
middle frontal gyrus	UBERON:0002702	99.87	gold quality
upper leg skin	UBERON:0004262	99.87	gold quality
tendon	UBERON:0000043	99.86	gold quality
urethra	UBERON:0000057	99.86	gold quality
pylorus	UBERON:0001166	99.86	gold quality
globus pallidus	UBERON:0001875	99.86	gold quality
epithelium of mammary gland	UBERON:0003244	99.86	gold quality
ganglionic eminence	UBERON:0004023	99.86	gold quality
penis	UBERON:0000989	99.85	gold quality
amygdala	UBERON:0001876	99.85	gold quality
pericardium	UBERON:0002407	99.85	gold quality
hindlimb stylopod muscle	UBERON:0004252	99.85	gold quality
cranial nerve II	UBERON:0000941	99.84	gold quality
ovary	UBERON:0000992	99.84	gold quality
skin of hip	UBERON:0001554	99.84	gold quality
left ovary	UBERON:0002119	99.84	gold quality
corpus callosum	UBERON:0002336	99.84	gold quality
oviduct epithelium	UBERON:0004804	99.84	gold quality
superior surface of tongue	UBERON:0007371	99.84	gold quality

Single-cell (SCXA)

Detected in 33 experiment(s), a significant marker in 13.

Experiment	Marker?	Max mean expression
E-MTAB-6701	yes	4557.64
E-MTAB-9221	yes	3372.18
E-MTAB-8142	yes	116.62
E-CURD-122	yes	91.63
E-CURD-88	yes	67.07
E-CURD-112	yes	36.28
E-MTAB-9067	yes	25.69
E-HCAD-9	yes	14.99
E-MTAB-10042	yes	12.70
E-MTAB-7316	yes	7.78
E-HCAD-35	yes	5.69
E-GEOD-137537	yes	5.48
E-MTAB-9467	no	4678.36
E-HCAD-8	no	4383.57
E-MTAB-8207	no	4228.88

Regulation

Is transcription factor: no

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 99.1% of screened cell lines, common-essential.

Literature-anchored findings (GeneRIF, showing 3)

• Knockdown of the mRNA encoding the ribosomal protein eL38 in mammalian cells causes a substantial reorganization of genomic transcription. (PMID:33675855)
• Knockdown of the Ribosomal Protein eL38 in HEK293 Cells Changes the Translational Efficiency of Specific Genes. (PMID:33926116)
• Expression and bioinformatics analysis of RPL38 protein and mRNA in gastric cancer. (PMID:38158659)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	rpl38	ENSDARG00000006413
mus_musculus	Rpl38	ENSMUSG00000057322
rattus_norvegicus		ENSRNOG00000079786
drosophila_melanogaster	RpL38	FBGN0040007
caenorhabditis_elegans		WBGENE00004452

Protein

Protein identifiers

Large ribosomal subunit protein eL38 — P63173 (reviewed: P63173)

Alternative names: 60S ribosomal protein L38

All UniProt accessions (4): P63173, J3KSP2, J3KT73, J3QL01

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 eL38 family.

RefSeq proteins (2): NP_000990, NP_001030335 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002675	Ribosomal_eL38	Family
IPR038464	Ribosomal_eL38_sf	Homologous_superfamily

Pfam: PF01781

UniProt features (5 total): modified residue 2, cross-link 2, chain 1

Structure

Experimental structures (PDB)

188 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
9QLO	ELECTRON MICROSCOPY	2.47
8FLE	ELECTRON MICROSCOPY	2.48
9P8B	ELECTRON MICROSCOPY	2.48
7XNY	ELECTRON MICROSCOPY	2.5

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P63173-F1	95.41	0.95

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 (4): 9, 67, 4, 9

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: 262 (showing top): GOBP_CYTOPLASMIC_TRANSLATION, GOBP_RIBOSOME_BIOGENESIS, HONMA_DOCETAXEL_RESISTANCE, GOBP_SKELETAL_SYSTEM_DEVELOPMENT, GOBP_SENSORY_PERCEPTION_OF_MECHANICAL_STIMULUS, MODULE_151, GNF2_TPT1, XU_HGF_TARGETS_REPRESSED_BY_AKT1_DN, CHUANG_OXIDATIVE_STRESS_RESPONSE_UP, GOBP_STRIATED_MUSCLE_CELL_DIFFERENTIATION, HSIAO_HOUSEKEEPING_GENES, GOBP_RIBOSOME_ASSEMBLY, GOBP_MALE_GAMETE_GENERATION, GOBP_NEGATIVE_REGULATION_OF_CELLULAR_COMPONENT_ORGANIZATION, GOBP_TRANSLATION

GO Biological Process (10): skeletal system development (GO:0001501), ossification (GO:0001503), cytoplasmic translation (GO:0002181), translation (GO:0006412), regulation of translation (GO:0006417), sensory perception of sound (GO:0007605), protein-RNA complex assembly (GO:0022618), 90S preribosome assembly (GO:0034463), middle ear morphogenesis (GO:0042474), axial mesoderm development (GO:0048318)

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

GO Cellular Component (10): cytoplasm (GO:0005737), cytosol (GO:0005829), focal adhesion (GO:0005925), postsynaptic density (GO:0014069), cytosolic large ribosomal subunit (GO:0022625), cytosolic ribosome (GO:0022626), eukaryotic 80S initiation complex (GO:0033291), ribosome (GO:0005840), synapse (GO:0045202), 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
translation	2
ribosome	2
cellular anatomical structure	2
system development	1
multicellular organismal process	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
post-transcriptional regulation of gene expression	1
regulation of protein metabolic process	1
sensory perception of mechanical stimulus	1
ribonucleoprotein complex biogenesis	1
protein-containing complex assembly	1
protein-RNA complex organization	1
protein-RNA complex assembly	1
cytosolic ribosome assembly	1
ear morphogenesis	1
embryonic morphogenesis	1
mesoderm development	1
nucleic acid binding	1
structural molecule activity	1
binding	1
intracellular anatomical structure	1
cytoplasm	1
cell-substrate junction	1
asymmetric synapse	1
postsynaptic specialization	1
large ribosomal subunit	1
cytosolic ribosome	1
cytosol	1
translation initiation complex	1
intracellular membraneless organelle	1
cell junction	1
protein-containing complex	1

Protein interactions and networks

STRING

0 interactions, top by confidence (×1000):

IntAct

214 interactions, top by confidence:

A	B	Type	Score
MAP3K14	CHUK	psi-mi:“MI:0914”(association)	0.950
MAPK14	RPS6KA4	psi-mi:“MI:0914”(association)	0.870
NCAPH2	SMC2	psi-mi:“MI:0914”(association)	0.720
CFTR	ESYT2	psi-mi:“MI:0914”(association)	0.710
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
DCC	NTN1	psi-mi:“MI:0914”(association)	0.700
IGF2BP1	IGF2BP3	psi-mi:“MI:0914”(association)	0.640
RACK1	RPS17	psi-mi:“MI:0915”(physical association)	0.610
	RPL38	psi-mi:“MI:0915”(physical association)	0.560
RPL38	BCCIP	psi-mi:“MI:0915”(physical association)	0.560
CHLSN	RPL14	psi-mi:“MI:0914”(association)	0.530
PA2G4	RPL35	psi-mi:“MI:0915”(physical association)	0.500
CFTR	PLEKHG3	psi-mi:“MI:0914”(association)	0.480
	FER1L5	psi-mi:“MI:0915”(physical association)	0.400
RPL38	CHMP5	psi-mi:“MI:0915”(physical association)	0.370
RPL38	AP2M1	psi-mi:“MI:0915”(physical association)	0.370
Eif3a	RPSA	psi-mi:“MI:0914”(association)	0.350
RPL10	RPS6	psi-mi:“MI:0914”(association)	0.350
Rrbp1	PIPSL	psi-mi:“MI:0914”(association)	0.350
SOX17	EEFSEC	psi-mi:“MI:0914”(association)	0.350
Prpf3	PRPF4	psi-mi:“MI:0914”(association)	0.350

BioGRID (463): RPL38 (Affinity Capture-MS), RPL38 (Affinity Capture-MS), EEF1G (Co-fractionation), PES1 (Co-fractionation), RPL10 (Co-fractionation), RPL10A (Co-fractionation), RPL13 (Co-fractionation), RPL13A (Co-fractionation), RPL15 (Co-fractionation), RPL19 (Co-fractionation), RPL22 (Co-fractionation), RPL23A (Co-fractionation), RPL26 (Co-fractionation), RPL27 (Co-fractionation), RPL27A (Co-fractionation)

ESM2 similar proteins: A2I469, A6N9N3, A7L6A2, D5LHJ0, G0SEV9, G1U001, O17570, O22860, P30057, P33095, P42678, P42798, P46291, P46297, P48149, P49205, P52865, P61221, P61222, P63173, P63174, P90707, Q00332, Q09JT4, Q1HRT4, Q23651, Q32PB9, Q39097, Q4GX86, Q4GX87, Q4PMD1, Q56FC8, Q5I0R6, Q5MGL3, Q5UAP8, Q60LW7, Q6F450, Q6XIM8, Q7KR04, Q7Q0U1

Diamond homologs: A0A1D8PG16, A2I469, A6N9N3, A7L6A2, G1U001, O17570, O22860, O61570, P46291, P49167, P63173, P63174, Q09900, Q09JT4, Q1HRT4, Q32PB9, Q4GX86, Q4GX87, Q4N921, Q4PMD1, Q4UGN5, Q55GJ7, Q56FC8, Q5MGL3, Q5UAP8, Q6F450, Q6XIM7, Q7Q0U1, Q8HXB9, Q95V84, Q962S5, Q9C2B9, Q9JJI8, Q9USR7, Q9W5N2, Q22SV3, Q9YFR9

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
RPL38	“form complex”	“60S cytosolic large ribosomal subunit”	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 181 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 the ternary complex, and subsequently, the 43S complex	9	14.5×	4e-07
Selenocysteine synthesis	16	14.3×	1e-12
Eukaryotic Translation Termination	16	14.3×	1e-12
SRP-dependent cotranslational protein targeting to membrane	19	14.2×	2e-14
GTP hydrolysis and joining of the 60S ribosomal subunit	19	14.2×	2e-14
Formation of a pool of free 40S subunits	17	14.2×	4e-13
Peptide chain elongation	15	14.2×	7e-12
Viral mRNA Translation	15	14.2×	7e-12

GO biological processes:

GO term	Partners	Fold	FDR
cytoplasmic translation	18	20.8×	5e-16
translational initiation	7	15.7×	1e-04
ribosomal large subunit biogenesis	5	13.9×	3e-03
translation	21	13.5×	3e-15
intrinsic apoptotic signaling pathway	6	13.4×	1e-03
ribosomal small subunit biogenesis	7	10.0×	1e-03
autophagosome assembly	7	9.8×	1e-03
negative regulation of translation	8	9.8×	5e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

14 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

477 predictions. Top by Δscore:

Variant	Effect	Δscore
17:74203667:G:GT	donor_gain	1.0000
17:74203667:G:T	donor_gain	1.0000
17:74203957:TG:T	donor_gain	1.0000
17:74203958:GG:G	donor_gain	1.0000
17:74203959:G:A	donor_loss	1.0000
17:74203959:G:GG	donor_gain	1.0000
17:74204126:GCA:G	acceptor_loss	1.0000
17:74204127:CA:C	acceptor_loss	1.0000
17:74204128:A:AG	acceptor_gain	1.0000
17:74204129:G:GA	acceptor_gain	1.0000
17:74204129:GC:G	acceptor_gain	1.0000
17:74204187:AAATG:A	donor_loss	1.0000
17:74204188:AATGT:A	donor_loss	1.0000
17:74204189:AT:A	donor_gain	1.0000
17:74204189:ATG:A	donor_loss	1.0000
17:74204190:TGT:T	donor_loss	1.0000
17:74204191:G:GA	donor_loss	1.0000
17:74204191:G:GG	donor_gain	1.0000
17:74204192:T:G	donor_loss	1.0000
17:74209162:A:AG	acceptor_gain	1.0000
17:74209174:T:A	acceptor_gain	1.0000
17:74209175:G:A	acceptor_gain	1.0000
17:74209181:C:CA	acceptor_gain	1.0000
17:74209183:GTA:G	acceptor_loss	1.0000
17:74209184:TAGC:T	acceptor_loss	1.0000
17:74209185:A:AG	acceptor_gain	1.0000
17:74209186:G:GG	acceptor_gain	1.0000
17:74209308:CGGT:C	donor_loss	1.0000
17:74209310:G:GG	donor_gain	1.0000
17:74209310:GTGA:G	donor_loss	1.0000

AlphaMissense

447 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
17:74204170:C:A	A15D	1.000
17:74209236:C:G	C38W	1.000
17:74204153:G:C	K9N	0.999
17:74204153:G:T	K9N	0.999
17:74204157:T:C	F11L	0.999
17:74204158:T:C	F11S	0.999
17:74204159:C:A	F11L	0.999
17:74204159:C:G	F11L	0.999
17:74204161:T:A	L12Q	0.999
17:74204161:T:C	L12P	0.999
17:74204169:G:C	A15P	0.999
17:74204181:G:C	D19H	0.999
17:74204185:C:A	A20D	0.999
17:74209190:T:A	V23D	0.999
17:74209223:T:C	F34S	0.999
17:74209227:A:C	K35N	0.999
17:74209227:A:T	K35N	0.999
17:74209229:T:A	V36D	0.999
17:74209235:G:A	C38Y	0.999
17:74209256:T:C	L45P	0.999
17:74209289:T:C	L56P	0.999
17:74209301:T:A	L60Q	0.999
17:74204152:A:T	K9M	0.998
17:74204158:T:G	F11C	0.998
17:74204164:T:C	L13P	0.998
17:74204173:G:C	R16P	0.998
17:74204176:G:C	R17P	0.998
17:74204190:T:C	S22P	0.998
17:74209222:T:C	F34L	0.998
17:74209224:T:A	F34L	0.998

dbSNP variants (sampled 300 via entrez): RS1000143463 (17:74203381 C>G), RS1000956638 (17:74208251 G>A,T), RS1001124697 (17:74203899 C>G,T), RS1001343425 (17:74208245 T>C), RS1001446004 (17:74206579 T>A), RS1001476525 (17:74206876 C>G), RS1001956542 (17:74203725 G>A), RS1002249985 (17:74203674 C>A,T), RS1002390720 (17:74203876 C>T), RS1002453229 (17:74207858 G>C,T), RS1002731920 (17:74202647 T>C), RS1003119389 (17:74205525 G>A,T), RS1003150482 (17:74205676 A>C), RS1003358684 (17:74210553 G>A,C,T), RS1003665222 (17:74202972 G>A,C,T)

Disease associations

OMIM: gene MIM:604182 | 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
GCST006052_3	Polymyositis	2.000000e-06
GCST006427_23	Depression in smokers	4.000000e-06

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL3987582 (PROTEIN NUCLEIC-ACID COMPLEX), CHEMBL6067551 (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
7.56	Kd	27.43	nM	CHEMBL5653589
7.56	ED50	27.43	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
5.53	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
5.08	Kd	8355	nM	CHEMBL3752910
5.08	ED50	8355	nM	CHEMBL3752910
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	2149269: Binding affinity to human RPL38 incubated for 45 mins by Kinobead based pull down assay	kd	0.0274	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
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
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149269: Binding affinity to human RPL38 incubated for 45 mins by Kinobead based pull down assay	kd	8.3553	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
bisphenol A	affects expression, decreases expression	2
arsenite	affects binding, increases reaction, increases methylation	2
sodium arsenite	increases abundance, increases expression, decreases expression, increases activity	2
7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide	increases expression, decreases expression	2
Particulate Matter	decreases expression, increases abundance	2
aristolochic acid I	decreases expression	1
bisphenol F	increases expression	1
TAK-243	increases sumoylation	1
methylmercuric chloride	increases expression	1
triphenyl phosphate	affects expression	1
beta-lapachone	increases expression	1
methylparaben	decreases expression	1
chloropicrin	affects expression	1
perfluoro-n-nonanoic acid	decreases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
abrine	decreases expression	1
bisphenol S	increases expression	1
10-(octyloxy)decyl-2-(trimethylammonium)ethyl phosphate	decreases expression	1
LDN 193189	affects cotreatment, decreases expression	1
bisphenol AF	increases expression	1
Sunitinib	increases expression	1
Air Pollutants	decreases expression, increases abundance	1
Arsenic	increases abundance, increases expression	1
Benzo(a)pyrene	decreases expression	1
Copper	affects binding, decreases expression	1
Disulfiram	decreases expression, affects binding	1
Diuron	decreases expression	1
Enzyme Inhibitors	decreases activity, increases O-linked glycosylation	1
Estradiol	decreases expression	1
Ivermectin	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.