RPL10A

Summary

RPL10A (ribosomal protein L10a, HGNC:10299) is a protein-coding gene on chromosome 6p21.31, encoding Large ribosomal subunit protein uL1 (P62906). 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 ribosomal protein that is a component of the 60S subunit. The protein belongs to the L1P family of ribosomal proteins. It is located in the cytoplasm. The expression of this gene is downregulated in the thymus by cyclosporin-A (CsA), an immunosuppressive drug. Studies in mice have shown that the expression of the ribosomal protein L10a gene is downregulated in neural precursor cells during development. This gene previously was referred to as NEDD6 (neural precursor cell expressed, developmentally downregulated 6), but it has been renamed RPL10A (ribosomal protein 10a). As is typical for genes encoding ribosomal proteins, there are multiple processed pseudogenes of this gene dispersed through the genome.

Source: NCBI Gene 4736 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 20 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_007104

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:10299
Approved symbol	RPL10A
Name	ribosomal protein L10a
Location	6p21.31
Locus type	gene with protein product
Status	Approved
Aliases	Csa-19, L10A, uL1
Ensembl gene	ENSG00000198755
Ensembl biotype	protein_coding
OMIM	615660
Entrez	4736

Gene structure

Transcript identifiers

Ensembl transcripts: 16 — 12 protein_coding, 4 protein_coding_CDS_not_defined

ENST00000322203, ENST00000464112, ENST00000467020, ENST00000478340, ENST00000490335, ENST00000864372, ENST00000864373, ENST00000864374, ENST00000918617, ENST00000918618, ENST00000918619, ENST00000918620, ENST00000918621, ENST00000918622, ENST00000918623, ENST00000961684

RefSeq mRNA: 1 — MANE Select: NM_007104 NM_007104

CCDS: CCDS4806

Canonical transcript exons

ENST00000322203 — 6 exons

Exon	Start	End
ENSE00003475534	35470179	35470351
ENSE00003531003	35468401	35468439
ENSE00003563281	35469381	35469529
ENSE00003578374	35468947	35469027
ENSE00003601153	35468799	35468873
ENSE00003680458	35470580	35470780

Expression profiles

Bgee: expression breadth ubiquitous, 153 present calls, max score 99.87.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 78.5766 / max 798.4792, expressed in 1822 samples.

FANTOM5 promoters (7 alternative TSS)

Promoter ID	TPM avg	Samples expressed
67443	66.7780	1822
67444	4.1153	1512
67442	4.0696	1525
67447	3.0579	1144
67445	0.3703	101
67446	0.1673	52
67448	0.0182	8

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right uterine tube	UBERON:0001302	99.87	gold quality
left ovary	UBERON:0002119	99.86	gold quality
ovary	UBERON:0000992	99.85	gold quality
fallopian tube	UBERON:0003889	99.85	gold quality
right ovary	UBERON:0002118	99.84	gold quality
endocervix	UBERON:0000458	99.83	gold quality
smooth muscle tissue	UBERON:0001135	99.82	gold quality
cortical plate	UBERON:0005343	99.82	gold quality
body of uterus	UBERON:0009853	99.82	gold quality
zone of skin	UBERON:0000014	99.81	gold quality
left uterine tube	UBERON:0001303	99.81	gold quality
skin of abdomen	UBERON:0001416	99.81	gold quality
skin of leg	UBERON:0001511	99.80	gold quality
ganglionic eminence	UBERON:0004023	99.80	gold quality
ectocervix	UBERON:0012249	99.80	gold quality
sigmoid colon	UBERON:0001159	99.79	gold quality
muscle layer of sigmoid colon	UBERON:0035805	99.79	gold quality
vagina	UBERON:0000996	99.78	gold quality
mucosa of stomach	UBERON:0001199	99.78	gold quality
myometrium	UBERON:0001296	99.78	gold quality
prostate gland	UBERON:0002367	99.78	gold quality
ventricular zone	UBERON:0003053	99.78	gold quality
lymph node	UBERON:0000029	99.77	gold quality
rectum	UBERON:0001052	99.77	gold quality
right lobe of thyroid gland	UBERON:0001119	99.77	gold quality
thyroid gland	UBERON:0002046	99.77	gold quality
thoracic mammary gland	UBERON:0005200	99.77	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	99.77	gold quality
uterine cervix	UBERON:0000002	99.76	gold quality
left lobe of thyroid gland	UBERON:0001120	99.76	gold quality

Single-cell (SCXA)

Detected in 32 experiment(s), a significant marker in 16.

Experiment	Marker?	Max mean expression
E-CURD-112	yes	5101.16
E-GEOD-130148	yes	3149.94
E-CURD-122	yes	91.46
E-CURD-46	yes	66.30
E-CURD-88	yes	59.55
E-MTAB-9221	yes	56.17
E-HCAD-11	yes	54.32
E-MTAB-6678	yes	38.92
E-MTAB-9067	yes	28.82
E-HCAD-9	yes	27.55
E-HCAD-31	yes	20.29
E-GEOD-135922	yes	19.68
E-MTAB-10042	yes	16.80
E-MTAB-9801	yes	6.50
E-GEOD-137537	yes	5.42

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)

• two genes coding for ribosomal proteins (S2 and L10a) encoded tumor antigens recognized by HLA-A26-restricted CTLs (PMID:12694581)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	rpl10a	ENSDARG00000042905
mus_musculus	Rpl10a	ENSMUSG00000037805
rattus_norvegicus	Rpl10a	ENSRNOG00000000505
drosophila_melanogaster	RpL10Ab	FBGN0036213

Paralogs (3): NHP2 (ENSG00000145912), RPL7A (ENSG00000148303), RSL1D1 (ENSG00000171490)

Protein

Protein identifiers

Large ribosomal subunit protein uL1 — P62906 (reviewed: P62906)

Alternative names: 60S ribosomal protein L10a, CSA-19, Neural precursor cell expressed developmentally down-regulated protein 6

All UniProt accessions (1): P62906

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 universal ribosomal protein uL1 family.

RefSeq proteins (1): NP_009035* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002143	Ribosomal_uL1	Family
IPR016095	Ribosomal_uL1_3-a/b-sand	Homologous_superfamily
IPR023673	Ribosomal_uL1_CS	Conserved_site
IPR023674	Ribosomal_uL1-like	Homologous_superfamily
IPR028364	Ribosomal_uL1/biogenesis	Family
IPR050257	eL8/uL1-like	Family

Pfam: PF00687

UniProt features (34 total): strand 10, helix 8, modified residue 5, turn 3, cross-link 3, sequence conflict 2, initiator methionine 1, chain 1, sequence variant 1

Structure

Experimental structures (PDB)

70 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
8YOP	ELECTRON MICROSCOPY	2.2
8G5Y	ELECTRON MICROSCOPY	2.29
9RPV	ELECTRON MICROSCOPY	2.35
8K2C	ELECTRON MICROSCOPY	2.4
8XSX	ELECTRON MICROSCOPY	2.4
8FKV	ELECTRON MICROSCOPY	2.47
8FKW	ELECTRON MICROSCOPY	2.5
8FL3	ELECTRON MICROSCOPY	2.53
8G60	ELECTRON MICROSCOPY	2.54
8IFE	ELECTRON MICROSCOPY	2.57
8FKX	ELECTRON MICROSCOPY	2.59
8IFD	ELECTRON MICROSCOPY	2.59
6ZMI	ELECTRON MICROSCOPY	2.6
8FKY	ELECTRON MICROSCOPY	2.67
8FL2	ELECTRON MICROSCOPY	2.67
6ZM7	ELECTRON MICROSCOPY	2.7
6Y6X	ELECTRON MICROSCOPY	2.8
8G6J	ELECTRON MICROSCOPY	2.8
8FKT	ELECTRON MICROSCOPY	2.81
8FKU	ELECTRON MICROSCOPY	2.82
9B0P	ELECTRON MICROSCOPY	2.82
8FL4	ELECTRON MICROSCOPY	2.89
6QZP	ELECTRON MICROSCOPY	2.9
6Z6N	ELECTRON MICROSCOPY	2.9
8OJ5	ELECTRON MICROSCOPY	2.9
8G61	ELECTRON MICROSCOPY	2.94
9I2E	ELECTRON MICROSCOPY	2.95
6Z6L	ELECTRON MICROSCOPY	3
6ZME	ELECTRON MICROSCOPY	3
8IDY	ELECTRON MICROSCOPY	3

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P62906-F1	79.23	0.02

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 (8): 2, 11, 91, 106, 118, 118, 118, 161

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: 233 (showing top): GOBP_CYTOPLASMIC_TRANSLATION, GOBP_RESPONSE_TO_ETHANOL, MODULE_151, ENK_UV_RESPONSE_KERATINOCYTE_UP, BHATI_G2M_ARREST_BY_2METHOXYESTRADIOL_DN, GCM_NPM1, WANG_RECURRENT_LIVER_CANCER_UP, MORF_UBE2I, GOBP_STRIATED_MUSCLE_CELL_DIFFERENTIATION, HSIAO_HOUSEKEEPING_GENES, GOBP_MALE_GAMETE_GENERATION, GGGTGGRR_PAX4_03, GOBP_NEGATIVE_REGULATION_OF_CELLULAR_COMPONENT_ORGANIZATION, GOBP_TRANSLATION, GCM_PSME1

GO Biological Process (3): cytoplasmic translation (GO:0002181), translation (GO:0006412), response to ethanol (GO:0045471)

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

GO Cellular Component (12): nucleus (GO:0005634), cytoplasm (GO:0005737), cytosol (GO:0005829), focal adhesion (GO:0005925), postsynaptic density (GO:0014069), membrane (GO:0016020), cytosolic large ribosomal subunit (GO:0022625), cytosolic ribosome (GO:0022626), extracellular exosome (GO:0070062), ribosome (GO:0005840), large ribosomal subunit (GO:0015934), 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
response to alcohol	1
nucleic acid binding	1
structural molecule activity	1
binding	1
intracellular membrane-bounded organelle	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
extracellular vesicle	1
intracellular membraneless organelle	1
ribosomal subunit	1
protein-containing complex	1

Protein interactions and networks

STRING

0 interactions, top by confidence (×1000):

IntAct

285 interactions, top by confidence:

A	B	Type	Score
MAP3K14	CHUK	psi-mi:“MI:0914”(association)	0.950
NCK1	NCK2	psi-mi:“MI:0914”(association)	0.730
XPC	CETN3	psi-mi:“MI:0914”(association)	0.730
RPL10A	RGS17	psi-mi:“MI:0915”(physical association)	0.720
RGS17	RPL10A	psi-mi:“MI:0915”(physical 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
RPL10A	RPL11	psi-mi:“MI:0915”(physical association)	0.670
FAM90A1	KPNA3	psi-mi:“MI:0914”(association)	0.670
RPL10A	RRP8	psi-mi:“MI:0914”(association)	0.640
RACK1	RPS17	psi-mi:“MI:0915”(physical association)	0.610
CFTR	HAX1	psi-mi:“MI:0914”(association)	0.610
RPS3A	RPL10A	psi-mi:“MI:0915”(physical association)	0.560
MECP2	GTPBP10	psi-mi:“MI:0914”(association)	0.530
MAGEB10	GTPBP10	psi-mi:“MI:0914”(association)	0.530
ZNF707	ZNF316	psi-mi:“MI:0914”(association)	0.530
H1-6	ZNF724	psi-mi:“MI:0914”(association)	0.530
RPL37A	MPHOSPH10	psi-mi:“MI:0914”(association)	0.530

BioGRID (761): RPL10A (Affinity Capture-MS), RGS17 (Two-hybrid), RPL10A (Affinity Capture-MS), RPL10A (Affinity Capture-MS), RPL10A (Affinity Capture-MS), RPL10A (Affinity Capture-MS), RPL10A (Affinity Capture-MS), DDX27 (Affinity Capture-MS), HIST2H2BF (Affinity Capture-MS), RPL26L1 (Affinity Capture-MS), URB1 (Affinity Capture-MS), NOL8 (Affinity Capture-MS), NPM1 (Affinity Capture-MS), GTPBP4 (Affinity Capture-MS), WDR89 (Affinity Capture-MS)

ESM2 similar proteins: A6H769, A6MZM2, C9WPN6, F1QGW6, G1SVB0, O14602, O48650, O60739, P02362, P20461, P35268, P41091, P41567, P41568, P47813, P47814, P48024, P51971, P53026, P56330, P61220, P62081, P62082, P62083, P62084, P62906, P62907, P81795, Q0D5W6, Q2KHU8, Q2VIR3, Q4R4X9, Q4R5P3, Q5E938, Q5E9E6, Q5R797, Q5RA42, Q5RFF4, Q5RT64, Q5ZMS3

Diamond homologs: A0B922, A0RX07, A1RRR1, A1RWQ3, A2BN64, A2STT9, A3CSJ6, A3DIZ1, A3DNI1, A3MX83, A4FZS7, A4WL88, A4XLK1, A4YH88, A5ELP1, A5UKU9, A5VR18, A6LKQ6, A6UTF9, A6VIQ0, A7HCI0, A7HWQ1, A7IAK4, A7IKP7, A8HTX8, A9A837, A9KD42, A9M5R3, A9NAL1, B0K5G5, B0R4W2, B1L6L3, B1L938, B1YAC8, B1ZFX0, B2S690, B2V7M3, B3QC04, B6J274, B6J5B9

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
RPL10A	“form complex”	“60S cytosolic large ribosomal subunit”	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 220 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	8	11.2×	2e-05
Ribosomal scanning and start codon recognition	9	11.1×	4e-06
GTP hydrolysis and joining of the 60S ribosomal subunit	17	11.1×	1e-10
Eukaryotic Translation Termination	14	10.9×	3e-09
Response of EIF2AK4 (GCN2) to amino acid deficiency	15	10.8×	1e-09
Peptide chain elongation	13	10.7×	1e-08
Viral mRNA Translation	13	10.7×	1e-08
Nonsense Mediated Decay (NMD) independent of the Exon Junction Complex (EJC)	14	10.7×	4e-09

GO biological processes:

GO term	Partners	Fold	FDR
negative regulation of mRNA splicing, via spliceosome	5	20.1×	1e-03
stress granule assembly	5	15.8×	2e-03
cytoplasmic translation	16	15.5×	6e-12
translational initiation	7	13.1×	4e-04
ribosomal small subunit biogenesis	8	9.5×	6e-04
translation	17	9.2×	3e-09
negative regulation of translation	8	8.2×	1e-03
rRNA processing	8	5.9×	8e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	9
Likely benign	0
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

807 predictions. Top by Δscore:

Variant	Effect	Δscore
6:35468870:GCAA:G	donor_gain	1.0000
6:35468873:AGT:A	donor_loss	1.0000
6:35468874:G:GG	donor_gain	1.0000
6:35468874:GTG:G	donor_loss	1.0000
6:35468942:CGAA:C	acceptor_loss	1.0000
6:35468946:G:GC	acceptor_loss	1.0000
6:35469024:TCAGG:T	donor_loss	1.0000
6:35469025:CAG:C	donor_loss	1.0000
6:35469026:AGG:A	donor_loss	1.0000
6:35469027:GGTT:G	donor_loss	1.0000
6:35469028:GTT:G	donor_loss	1.0000
6:35469029:T:A	donor_loss	1.0000
6:35469404:A:G	acceptor_gain	1.0000
6:35469422:T:TA	acceptor_gain	1.0000
6:35469423:G:A	acceptor_gain	1.0000
6:35469518:TC:T	donor_gain	1.0000
6:35469525:GCTGG:G	donor_gain	1.0000
6:35469528:GG:G	donor_gain	1.0000
6:35469529:GG:G	donor_gain	1.0000
6:35469530:GT:G	donor_loss	1.0000
6:35469531:T:G	donor_loss	1.0000
6:35470175:TCAGC:T	acceptor_loss	1.0000
6:35470176:CAGCC:C	acceptor_loss	1.0000
6:35470177:A:AG	acceptor_gain	1.0000
6:35470177:AGCCA:A	acceptor_loss	1.0000
6:35470178:G:GA	acceptor_gain	1.0000
6:35470178:GC:G	acceptor_gain	1.0000
6:35470178:GCCAA:G	acceptor_gain	1.0000
6:35470348:GAAG:G	donor_gain	1.0000
6:35470349:AAGGT:A	donor_loss	1.0000

AlphaMissense

1428 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
6:35468979:T:C	L38S	1.000
6:35469002:G:C	D46H	1.000
6:35469008:C:A	R48S	1.000
6:35469011:T:C	F49L	1.000
6:35469012:T:C	F49S	1.000
6:35469013:C:A	F49L	1.000
6:35469013:C:G	F49L	1.000
6:35469017:G:C	G51R	1.000
6:35469018:G:A	G51D	1.000
6:35469024:T:A	V53D	1.000
6:35469419:T:A	V67D	1.000
6:35469424:G:A	G69R	1.000
6:35469424:G:C	G69R	1.000
6:35469424:G:T	G69W	1.000
6:35469425:G:A	G69E	1.000
6:35469488:T:C	L90P	1.000
6:35469518:T:A	V100D	1.000
6:35470197:T:C	F110S	1.000
6:35470203:C:A	A112D	1.000
6:35470241:G:C	G125R	1.000
6:35470242:G:A	G125D	1.000
6:35470251:T:C	L128S	1.000
6:35470263:G:A	G132E	1.000
6:35470268:T:C	F134L	1.000
6:35470269:T:C	F134S	1.000
6:35470269:T:G	F134C	1.000
6:35470270:C:A	F134L	1.000
6:35470270:C:G	F134L	1.000
6:35470272:C:A	P135H	1.000
6:35470338:T:C	F157S	1.000

dbSNP variants (sampled 300 via entrez): RS1000742892 (6:35469064 C>T), RS1000818583 (6:35469256 G>A), RS1000891606 (6:35468394 A>C,G), RS1001890787 (6:35468561 A>C,G), RS1001927737 (6:35467547 A>C,G), RS1002032372 (6:35468000 G>A), RS1002633664 (6:35466972 T>A), RS1003010849 (6:35466628 G>A), RS1003234313 (6:35466617 T>A,C), RS1003828855 (6:35467942 C>G), RS1003951962 (6:35468529 C>A,T), RS1004325449 (6:35468729 C>G,T), RS1004662687 (6:35469954 G>T), RS1005322260 (6:35467725 G>C), RS1005862314 (6:35469667 G>A,C)

Disease associations

OMIM: gene MIM:615660 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL3987582 (PROTEIN NUCLEIC-ACID COMPLEX), CHEMBL6067548 (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
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
6.24	Kd	577.3	nM	CHEMBL3752910
6.24	ED50	577.3	nM	CHEMBL3752910
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
5.05	Kd	8922	nM	CHEMBL5653589
5.05	ED50	8922	nM	CHEMBL5653589
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
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
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149240: Binding affinity to human RPL10A incubated for 45 mins by Kinobead based pull down assay	kd	0.5773	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-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149240: Binding affinity to human RPL10A incubated for 45 mins by Kinobead based pull down assay	kd	8.9218	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
bisphenol A	affects expression, decreases expression, increases expression, affects cotreatment	5
sodium arsenite	decreases expression, increases activity, affects cotreatment, increases abundance, increases expression	3
Benzo(a)pyrene	decreases expression, increases methylation	2
Particulate Matter	affects cotreatment, increases abundance, increases expression	2
bisphenol F	affects cotreatment, decreases expression	1
2,4,6-tribromophenol	decreases expression	1
triphenyl phosphate	affects expression	1
alpha-pinene	affects cotreatment, increases expression, increases abundance	1
deoxynivalenol	increases expression	1
sodium arsenate	decreases expression	1
pyrogallol 1,3-dimethyl ether	affects cotreatment, affects localization, increases expression	1
decabromobiphenyl ether	decreases expression	1
beta-lapachone	increases expression	1
arsenite	affects binding, increases reaction	1
tetrabromobisphenol A	decreases expression	1
ochratoxin A	increases expression	1
methacrylaldehyde	affects cotreatment, increases expression, increases abundance	1
isobutyl alcohol	increases abundance, increases expression, affects cotreatment	1
epigallocatechin gallate	decreases expression	1
perfluorooctane sulfonic acid	increases expression	1
CGP 52608	increases reaction, affects binding	1
chloropicrin	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
ICG 001	decreases expression	1
bisphenol B	increases expression	1
abrine	decreases expression	1
pentabrominated diphenyl ether 100	decreases expression	1
hexabrominated diphenyl ether 153	decreases expression	1
bisphenol S	increases expression	1
jinfukang	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.