RPL37A

Summary

RPL37A (ribosomal protein L37a, HGNC:10348) is a protein-coding gene on chromosome 2q35, encoding Large ribosomal subunit protein eL43 (P61513). 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 L37AE family of ribosomal proteins. It is located in the cytoplasm. The protein contains a C4-type zinc finger-like domain. As is typical for genes encoding ribosomal proteins, there are multiple processed pseudogenes of this gene dispersed through the genome.

Source: NCBI Gene 6168 — RefSeq curated summary.

At a glance

• GWAS associations: 8
• 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_000998

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:10348
Approved symbol	RPL37A
Name	ribosomal protein L37a
Location	2q35
Locus type	gene with protein product
Status	Approved
Aliases	L37A, eL43
Ensembl gene	ENSG00000197756
Ensembl biotype	protein_coding
OMIM	613314
Entrez	6168

Gene structure

Transcript identifiers

Ensembl transcripts: 18 — 12 protein_coding, 4 retained_intron, 1 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000359681, ENST00000420712, ENST00000427280, ENST00000441179, ENST00000446558, ENST00000456586, ENST00000478153, ENST00000487233, ENST00000490649, ENST00000491306, ENST00000598925, ENST00000600880, ENST00000624436, ENST00000939366, ENST00000939367, ENST00000939368, ENST00000939369, ENST00000948942

RefSeq mRNA: 1 — MANE Select: NM_000998 NM_000998

CCDS: CCDS2404

Canonical transcript exons

ENST00000491306 — 4 exons

Exon	Start	End
ENSE00001818144	216498844	216498877
ENSE00001829854	216501341	216504086
ENSE00003507040	216499949	216500031
ENSE00003574352	216499270	216499398

Expression profiles

Bgee: expression breadth ubiquitous, 295 present calls, max score 100.00.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 1379.2794 / max 14291.4950, expressed in 1827 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
25215	1379.1288	1827
25216	0.1409	18
25217	0.0098	4

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
endothelial cell	CL:0000115	100.00	gold quality
superficial temporal artery	UBERON:0001614	100.00	gold quality
mammary duct	UBERON:0001765	100.00	gold quality
nipple	UBERON:0002030	100.00	gold quality
parietal pleura	UBERON:0002400	100.00	gold quality
pericardium	UBERON:0002407	100.00	gold quality
epithelium of mammary gland	UBERON:0003244	100.00	gold quality
upper leg skin	UBERON:0004262	100.00	gold quality
caput epididymis	UBERON:0004358	100.00	gold quality
cerebellar vermis	UBERON:0004720	100.00	gold quality
pancreatic ductal cell	CL:0002079	99.99	gold quality
urethra	UBERON:0000057	99.99	gold quality
colonic mucosa	UBERON:0000317	99.99	gold quality
embryo	UBERON:0000922	99.99	gold quality
cranial nerve II	UBERON:0000941	99.99	gold quality
pleura	UBERON:0000977	99.99	gold quality
penis	UBERON:0000989	99.99	gold quality
mammalian vulva	UBERON:0000997	99.99	gold quality
mucosa of urinary bladder	UBERON:0001259	99.99	gold quality
germinal epithelium of ovary	UBERON:0001304	99.99	gold quality
skin of hip	UBERON:0001554	99.99	gold quality
pigmented layer of retina	UBERON:0001782	99.99	gold quality
palpebral conjunctiva	UBERON:0001812	99.99	gold quality
globus pallidus	UBERON:0001875	99.99	gold quality
gingival epithelium	UBERON:0001949	99.99	gold quality
heart right ventricle	UBERON:0002080	99.99	gold quality
inferior olivary complex	UBERON:0002127	99.99	gold quality
synovial joint	UBERON:0002217	99.99	gold quality
thymus	UBERON:0002370	99.99	gold quality
visceral pleura	UBERON:0002401	99.99	gold quality

Single-cell (SCXA)

Detected in 37 experiment(s), a significant marker in 12.

Experiment	Marker?	Max mean expression
E-CURD-98	yes	6552.12
E-MTAB-9067	yes	6355.72
E-GEOD-137537	yes	3228.38
E-MTAB-6819	yes	2055.95
E-ENAD-17	yes	707.04
E-CURD-122	yes	85.53
E-CURD-88	yes	61.97
E-MTAB-9221	yes	56.01
E-MTAB-10042	yes	14.78
E-HCAD-35	yes	9.04
E-MTAB-9801	yes	6.24
E-MTAB-10432	no	11714.90
E-MTAB-10885	no	8282.97
E-GEOD-139324	no	7497.03
E-MTAB-10596	no	7298.81

Regulation

Is transcription factor: no

Functional genomics

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

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	RPL37A	ENSDARG00000115271
mus_musculus	Rpl37a	ENSMUSG00000046330
rattus_norvegicus	Rpl37al2	ENSRNOG00000003227

Protein

Protein identifiers

Large ribosomal subunit protein eL43 — P61513 (reviewed: P61513)

Alternative names: 60S ribosomal protein L37a

All UniProt accessions (7): C9J4Z3, E9PEL3, G5E9R3, M0R0A1, M0R2L6, P61513, Q6P4E4

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 eL43 family.

RefSeq proteins (1): NP_000989* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002674	Ribosomal_eL43	Family
IPR011331	Ribosomal_eL37/eL43	Homologous_superfamily
IPR011332	Ribosomal_zn-bd	Homologous_superfamily

Pfam: PF01780

UniProt features (6 total): binding site 4, chain 1, zinc finger region 1

Structure

Experimental structures (PDB)

182 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-P61513-F1	96.31	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.

Ligand- & substrate-binding residues (4): 39; 42; 57; 60

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: 0 (showing top):

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

GO Molecular Function (5): RNA binding (GO:0003723), structural constituent of ribosome (GO:0003735), zinc ion binding (GO:0008270), protein binding (GO:0005515), metal ion binding (GO:0046872)

GO Cellular Component (10): nucleus (GO:0005634), cytoplasm (GO:0005737), cytosol (GO:0005829), focal adhesion (GO:0005925), cytosolic large ribosomal subunit (GO:0022625), cytosolic ribosome (GO:0022626), synapse (GO:0045202), extracellular exosome (GO:0070062), 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
ribosome	2
cellular anatomical structure	2
translation	1
peptidyltransferase activity	1
translational initiation	1
translational elongation	1
translational termination	1
macromolecule biosynthetic process	1
protein metabolic process	1
protein biosynthetic process	1
nucleic acid binding	1
structural molecule activity	1
transition metal ion binding	1
binding	1
cation binding	1
intracellular membrane-bounded organelle	1
intracellular anatomical structure	1
cytoplasm	1
cell-substrate junction	1
large ribosomal subunit	1
cytosolic ribosome	1
cytosol	1
cell junction	1
extracellular vesicle	1
intracellular membraneless organelle	1
protein-containing complex	1

Protein interactions and networks

STRING

0 interactions, top by confidence (×1000):

IntAct

190 interactions, top by confidence:

A	B	Type	Score
MAP3K14	CHUK	psi-mi:“MI:0914”(association)	0.950
RPL37A	MAGEA6	psi-mi:“MI:0915”(physical association)	0.720
MAGEA6	RPL37A	psi-mi:“MI:0915”(physical association)	0.720
SART1	PRPF3	psi-mi:“MI:0914”(association)	0.720
CFTR	ESYT2	psi-mi:“MI:0914”(association)	0.710
WDR5	MEN1	psi-mi:“MI:0914”(association)	0.710
RRP8	RPL37A	psi-mi:“MI:0915”(physical association)	0.670
LIN28A	IGF2BP3	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
RPL37A	SERPINH1	psi-mi:“MI:0915”(physical association)	0.560
RPL37A	PECAM1	psi-mi:“MI:0915”(physical association)	0.560
RPL37A	PRKACA	psi-mi:“MI:0915”(physical association)	0.560
RPL37A	TGFBR2	psi-mi:“MI:0915”(physical association)	0.560
TGFBR2	RPL37A	psi-mi:“MI:0915”(physical association)	0.560
CDK18	UBL4A	psi-mi:“MI:0914”(association)	0.530

BioGRID (642): RPL37A (Two-hybrid), RPL37A (Affinity Capture-MS), RPL37A (Affinity Capture-MS), RPL37A (Affinity Capture-MS), EIF6 (Co-fractionation), RPL10A (Co-fractionation), RPL12 (Co-fractionation), RPL37A (Co-fractionation), RPL37A (Co-fractionation), RPL37A (Co-fractionation), RPL37A (Co-fractionation), RPL37A (Co-fractionation), RPL37A (Co-fractionation), RPL37A (Co-fractionation), RPL37A (Co-fractionation)

ESM2 similar proteins: A0A1D8PP14, A4S6Z4, A5UNQ7, B6YTZ8, C6A452, G1SY53, O17307, O61462, O61598, O94686, O96184, P05733, P0CX25, P0CX26, P0DKK1, P0DKK2, P32046, P43209, P61513, P61514, P61515, P61927, P61928, P79244, Q00VK4, Q23G98, Q2NEX3, Q3MIC0, Q54MG6, Q54UG4, Q5JDM6, Q5RBF9, Q6BPF6, Q6FRG6, Q6LY46, Q751L1, Q7SZB4, Q8RXU5, Q8TZI4, Q90YT0

Diamond homologs: A0A1D8PP14, A1RSS8, A4FZT8, A4S6Z4, A5UNQ7, A6NKH3, A6URN7, A6UTE9, A6VIN8, A9A848, B0R2Y1, B1Y976, B6YTZ8, B8D6B7, C5A4Z4, C6A452, G1SY53, O17307, O26777, O30179, O61462, O61598, O74106, O94686, O96184, P0CX25, P0CX26, P0DKK1, P0DKK2, P32046, P43209, P54051, P60619, P61513, P61514, P61515, Q00VK4, Q23G98, Q3MIC0, Q54UG4

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
RPL37A	“form complex”	“60S cytosolic large ribosomal subunit”	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 212 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
Eukaryotic Translation Initiation	7	15.3×	1e-05
Cap-dependent Translation Initiation	7	15.3×	1e-05
SARS-CoV-1 modulates host translation machinery	7	15.3×	1e-05
Nuclear events stimulated by ALK signaling in cancer	6	13.9×	1e-04
Eukaryotic Translation Elongation	7	13.8×	2e-05
Activation of the mRNA upon binding of the cap-binding complex and eIFs, and subsequent binding to 43S	7	13.5×	3e-05
SRP-dependent cotranslational protein targeting to membrane	17	12.1×	3e-11
Peptide chain elongation	13	11.7×	1e-08

GO biological processes:

GO term	Partners	Fold	FDR
negative regulation of DNA recombination	5	29.6×	1e-04
chromosome condensation	5	22.2×	4e-04
negative regulation of mRNA splicing, via spliceosome	5	20.2×	6e-04
ribosomal large subunit biogenesis	8	18.7×	3e-06
cytoplasmic translation	16	15.6×	6e-12
rRNA processing	15	11.2×	3e-09
ribosomal small subunit biogenesis	9	10.8×	4e-05
translation	16	8.7×	2e-08

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	8
Likely benign	0
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

366 predictions. Top by Δscore:

Variant	Effect	Δscore
2:216499394:GCAAA:G	donor_gain	1.0000
2:216499397:AA:A	donor_gain	1.0000
2:216499399:G:A	donor_loss	1.0000
2:216499399:G:GG	donor_gain	1.0000
2:216499400:T:G	donor_loss	1.0000
2:216499403:G:GG	donor_gain	1.0000
2:216499944:TATA:T	acceptor_loss	1.0000
2:216499946:T:G	acceptor_gain	1.0000
2:216499947:A:AG	acceptor_gain	1.0000
2:216499947:A:G	acceptor_loss	1.0000
2:216499948:G:GG	acceptor_gain	1.0000
2:216499948:GA:G	acceptor_gain	1.0000
2:216499948:GAC:G	acceptor_gain	1.0000
2:216499948:GACCA:G	acceptor_gain	1.0000
2:216500023:G:GT	donor_gain	1.0000
2:216500027:TAC:T	donor_gain	1.0000
2:216500028:ACA:A	donor_gain	1.0000
2:216500031:AG:A	donor_loss	1.0000
2:216500032:G:A	donor_loss	1.0000
2:216500032:G:GG	donor_gain	1.0000
2:216500033:T:G	donor_loss	1.0000
2:216499264:A:AG	acceptor_gain	0.9900
2:216499266:ACAGG:A	acceptor_loss	0.9900
2:216499267:CAGG:C	acceptor_loss	0.9900
2:216499268:A:AC	acceptor_loss	0.9900
2:216499269:G:T	acceptor_loss	0.9900
2:216499269:GGCC:G	acceptor_gain	0.9900
2:216499269:GGCCA:G	acceptor_gain	0.9900
2:216499343:TG:T	donor_gain	0.9900
2:216499392:TGGCA:T	donor_gain	0.9900

AlphaMissense

593 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
2:216499322:G:A	G19E	1.000
2:216499381:T:C	C39R	1.000
2:216499974:G:A	G53E	1.000
2:216499321:G:A	G19R	0.999
2:216499321:G:C	G19R	0.999
2:216499321:G:T	G19W	0.999
2:216499322:G:T	G19V	0.999
2:216499962:G:C	R49T	0.999
2:216499963:A:C	R49S	0.999
2:216499963:A:T	R49S	0.999
2:216499973:G:A	G53R	0.999
2:216499973:G:C	G53R	0.999
2:216499973:G:T	G53W	0.999
2:216499974:G:T	G53V	0.999
2:216499979:T:A	W55R	0.999
2:216499979:T:C	W55R	0.999
2:216499985:T:C	C57R	0.999
2:216500010:C:A	A65D	0.999
2:216500021:T:A	W69R	0.999
2:216500021:T:C	W69R	0.999
2:216499301:G:A	G12D	0.998
2:216499301:G:T	G12V	0.998
2:216499318:T:C	Y18H	0.998
2:216499382:G:A	C39Y	0.998
2:216499383:C:G	C39W	0.998
2:216499387:T:C	F41L	0.998
2:216499389:C:A	F41L	0.998
2:216499389:C:G	F41L	0.998
2:216499390:T:C	C42R	0.998
2:216499391:G:A	C42Y	0.998

dbSNP variants (sampled 300 via entrez): RS1000054678 (2:216503219 C>T), RS1000212798 (2:216497076 C>T), RS1000379461 (2:216498813 C>G,T), RS1001396366 (2:216499595 C>G,T), RS1001763872 (2:216503857 T>C,G), RS1001934509 (2:216500784 C>G,T), RS1002851355 (2:216502156 G>A), RS1002857126 (2:216503065 T>A), RS1002939540 (2:216501942 C>A), RS1003188831 (2:216502208 TC>T), RS1003860985 (2:216503125 G>A), RS1003954182 (2:216502890 G>A), RS1004565070 (2:216503402 C>G), RS1005165474 (2:216497665 T>G), RS1005202643 (2:216499039 C>T)

Disease associations

OMIM: gene MIM:613314 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

8 associations (top):

Study	Trait	p-value
GCST007044_9	Extremely high intelligence	3.000000e-08
GCST010102_3	White matter integrity (fractional anisotropy)	1.000000e-08
GCST010698_88	Subcortical volume (min-P)	1.000000e-18
GCST010699_97	Brain morphology (min-P)	5.000000e-12
GCST010700_52	Cortical thickness (MOSTest)	4.000000e-10
GCST010701_122	Cortical surface area (MOSTest)	7.000000e-11
GCST010702_157	Subcortical volume (MOSTest)	4.000000e-24
GCST010703_234	Brain morphology (MOSTest)	2.000000e-12

EFO canonical traits (4, from GWAS)

EFO ID	Trait name
EFO:0004337	intelligence
EFO:0004641	white matter integrity
EFO:0004346	neuroimaging measurement
EFO:0004840	cortical thickness

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL3987582 (PROTEIN NUCLEIC-ACID COMPLEX), CHEMBL6067566 (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

48 potent at pChembl≥5 of 52 total, top 47 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.31	Kd	48.98	nM	CHEMBL5653589
7.31	ED50	48.98	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
5.03	IC50	9320	nM	CHEMBL4127016
5.03	IC50	9240	nM	CHEMBL4128560

PubChem BioAssay actives

47 with measured affinity, of 207 total; 27 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	2149268: Binding affinity to human RPL37A incubated for 45 mins by Kinobead based pull down assay	kd	0.0490	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

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
bisphenol A	affects expression, decreases expression, decreases methylation	5
Valproic Acid	decreases expression, decreases methylation, affects cotreatment, increases expression	4
methylparaben	decreases expression, increases expression	2
Formaldehyde	decreases expression, increases expression	2
7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide	decreases expression, increases expression	2
aristolochic acid I	decreases expression	1
beauvericin	affects cotreatment, increases expression	1
methylmercuric chloride	increases expression	1
triphenyl phosphate	affects expression	1
arsenite	affects binding, increases reaction	1
cobaltous chloride	increases expression	1
beryllium sulfate	increases expression	1
potassium chromate(VI)	affects cotreatment, increases expression	1
phenanthrene	decreases expression	1
perfluorodecanoic acid	decreases expression	1
N-benzyloxycarbonylprolylprolinal	increases expression	1
epigallocatechin gallate	decreases expression, affects cotreatment, increases expression	1
4-hydroxy-equilenin	increases expression	1
enniatins	affects cotreatment, increases expression	1
perfluoro-n-nonanoic acid	decreases expression	1
bisphenol B	increases expression	1
abrine	decreases expression	1
jinfukang	increases expression	1
Sunitinib	increases expression	1
Coumestrol	decreases expression	1
Demecolcine	decreases expression	1
Diethylhexyl Phthalate	decreases expression	1
Succimer	affects expression, affects cotreatment	1
Enzyme Inhibitors	decreases activity, increases O-linked glycosylation	1
Estradiol	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.