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RPL12

gene
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Also known as L12uL11

Summary

RPL12 (ribosomal protein L12, HGNC:10302) is a protein-coding gene on chromosome 9q33.3, encoding Large ribosomal subunit protein uL11 (P30050). Component of the large ribosomal subunit. It is a common-essential gene (DepMap: required in 99.9% 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 L11P family of ribosomal proteins. It is located in the cytoplasm. The protein binds directly to the 26S rRNA. This gene is co-transcribed with the U65 snoRNA, which is located in its fourth intron. As is typical for genes encoding ribosomal proteins, there are multiple processed pseudogenes of this gene dispersed through the genome.

Source: NCBI Gene 6136 — RefSeq curated summary.

At a glance

  • Clinical variants (ClinVar): 30 total
  • Druggable target: yes — 1 molecules with ChEMBL bioactivity
  • Cancer dependency (DepMap): dependent in 99.9% of screened cell lines (common-essential)
  • MANE Select transcript: NM_000976

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:10302
Approved symbolRPL12
Nameribosomal protein L12
Location9q33.3
Locus typegene with protein product
StatusApproved
AliasesL12, uL11
Ensembl geneENSG00000197958
Ensembl biotypeprotein_coding
OMIM180475
Entrez6136

Gene structure

Transcript identifiers

Ensembl transcripts: 19 — 16 protein_coding, 3 protein_coding_CDS_not_defined

ENST00000361436, ENST00000483598, ENST00000497322, ENST00000497825, ENST00000536368, ENST00000886311, ENST00000886312, ENST00000938714, ENST00000938715, ENST00000938716, ENST00000938717, ENST00000938718, ENST00000938719, ENST00000938720, ENST00000938721, ENST00000938722, ENST00000938723, ENST00000938724, ENST00000938725

RefSeq mRNA: 1 — MANE Select: NM_000976 NM_000976

CCDS: CCDS6872

Canonical transcript exons

ENST00000361436 — 7 exons

ExonStartEnd
ENSE00001431863127451281127451406
ENSE00003463552127449281127449362
ENSE00003485743127448337127448423
ENSE00003486959127447674127447726
ENSE00003519033127447877127447989
ENSE00003583792127450731127450804
ENSE00003673562127449610127449708

Expression profiles

Bgee: expression breadth ubiquitous, 136 present calls, max score 99.90.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 25.9483 / max 138.4414, expressed in 1816 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter IDTPM avgSamples expressed
10253623.00071802
1025371.6521935
1025351.2954761

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
calcaneal tendonUBERON:000370199.90gold quality
olfactory segment of nasal mucosaUBERON:000538699.88gold quality
fallopian tubeUBERON:000388999.86gold quality
endocervixUBERON:000045899.85gold quality
ovaryUBERON:000099299.85gold quality
left ovaryUBERON:000211999.85gold quality
zone of skinUBERON:000001499.84gold quality
skin of abdomenUBERON:000141699.84gold quality
skin of legUBERON:000151199.84gold quality
right ovaryUBERON:000211899.84gold quality
lymph nodeUBERON:000002999.83gold quality
smooth muscle tissueUBERON:000113599.83gold quality
gall bladderUBERON:000211099.83gold quality
thoracic mammary glandUBERON:000520099.83gold quality
uterine cervixUBERON:000000299.82gold quality
ectocervixUBERON:001224999.82gold quality
granulocyteCL:000009499.81gold quality
rectumUBERON:000105299.81gold quality
left lobe of thyroid glandUBERON:000112099.81gold quality
right coronary arteryUBERON:000162599.81gold quality
left coronary arteryUBERON:000162699.81gold quality
thyroid glandUBERON:000204699.81gold quality
body of uterusUBERON:000985399.81gold quality
muscle layer of sigmoid colonUBERON:003580599.81gold quality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099199.80gold quality
vaginaUBERON:000099699.80gold quality
right lobe of thyroid glandUBERON:000111999.80gold quality
fundus of stomachUBERON:000116099.80gold quality
myometriumUBERON:000129699.80gold quality
right uterine tubeUBERON:000130299.80gold quality

Single-cell (SCXA)

Detected in 36 experiment(s), a significant marker in 10.

ExperimentMarker?Max mean expression
E-CURD-112yes7328.92
E-CURD-122yes94.01
E-CURD-88yes57.28
E-MTAB-9221yes53.48
E-MTAB-9067yes28.36
E-MTAB-7316yes16.48
E-MTAB-10042yes16.02
E-MTAB-9801yes5.89
E-GEOD-137537yes5.78
E-MTAB-10885no10225.12
E-HCAD-15no8463.53
E-MTAB-6701no8373.53
E-MTAB-8410no7944.55
E-CURD-120no7939.14
E-MTAB-10855no6880.53

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): MYC

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 99.9% of screened cell lines, common-essential.

Literature-anchored findings (GeneRIF, showing 3)

  • propose that, when not associated with ribosomes, MRPL12 has a second function in transcription, perhaps acting to facilitate the transition from initiation to elongation (PMID:22003127)
  • RPL12 role in CFTR protein folding and stability (PMID:27168400)
  • Phosphoproteomics on the fractions reveals that phosphorylation of serine 38 in RPL12/uL11, a known mitotic CDK1 substrate, is strongly depleted in polysomes. (PMID:30220558)

Cross-species orthologs

4 orthologs

OrganismSymbolGene ID
danio_reriorpl12ENSDARG00000006691
mus_musculusRpl12ENSMUSG00000038900
drosophila_melanogasterRpL12FBGN0034968
caenorhabditis_elegansWBGENE00004424

Paralogs (1): MRPL11 (ENSG00000174547)

Protein

Protein identifiers

Large ribosomal subunit protein uL11 — P30050 (reviewed: P30050)

Alternative names: 60S ribosomal protein L12

All UniProt accessions (1): P30050

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. Binds directly to 26S ribosomal RNA.

Subunit / interactions. Component of the large ribosomal subunit. Mature ribosomes consist of a small (40S) and a large (60S) subunit. The 40S subunit contains about 33 different proteins and 1 molecule of RNA (18S). The 60S subunit contains about 49 different proteins and 3 molecules of RNA (28S, 5.8S and 5S).

Subcellular location. Cytoplasm.

Post-translational modifications. Ubiquitinated at Lys-48 and Lys-83 by RNF14 and RNF25 in response to ribosome collisions (ribosome stalling).

Similarity. Belongs to the universal ribosomal protein uL11 family.

Isoforms (2)

UniProt IDNamesCanonical?
P30050-11yes
P30050-22

RefSeq proteins (1): NP_000967* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000911Ribosomal_uL11Family
IPR020783Ribosomal_uL11_CDomain
IPR020784Ribosomal_uL11_NDomain
IPR020785Ribosomal_uL11_CSConserved_site
IPR036769Ribosomal_uL11_C_sfHomologous_superfamily
IPR036796Ribosomal_uL11_N_sfHomologous_superfamily

Pfam: PF00298, PF03946

UniProt features (18 total): helix 5, modified residue 3, strand 3, cross-link 3, turn 2, chain 1, splice variant 1

Structure

Experimental structures (PDB)

111 structures, top 30 by resolution.

PDBMethodResolution (Å)
8YOOELECTRON MICROSCOPY2
9I2DELECTRON MICROSCOPY2.19
9PBEELECTRON MICROSCOPY2.19
8YOPELECTRON MICROSCOPY2.2
9S3DELECTRON MICROSCOPY2.32
9S3BELECTRON MICROSCOPY2.38
8K2CELECTRON MICROSCOPY2.4
8XSXELECTRON MICROSCOPY2.4
9S3CELECTRON MICROSCOPY2.42
8FKVELECTRON MICROSCOPY2.47
9QLOELECTRON MICROSCOPY2.47
9P8BELECTRON MICROSCOPY2.48
8FKWELECTRON MICROSCOPY2.5
8FL3ELECTRON MICROSCOPY2.53
8G60ELECTRON MICROSCOPY2.54
8FL7ELECTRON MICROSCOPY2.55
8FLBELECTRON MICROSCOPY2.55
9P7DELECTRON MICROSCOPY2.57
9QLQELECTRON MICROSCOPY2.57
8FKXELECTRON MICROSCOPY2.59
9P7EELECTRON MICROSCOPY2.59
6ZMIELECTRON MICROSCOPY2.6
8FL6ELECTRON MICROSCOPY2.62
8FLAELECTRON MICROSCOPY2.63
8G5ZELECTRON MICROSCOPY2.64
9P7OELECTRON MICROSCOPY2.65
9P73ELECTRON MICROSCOPY2.66
8FKYELECTRON MICROSCOPY2.67
8FL2ELECTRON MICROSCOPY2.67
9PA7ELECTRON MICROSCOPY2.67

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P30050-F170.900.00

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Post-translational modifications (6): 38, 54, 165, 40, 48, 83

Function

Pathways and Gene Ontology

Reactome pathways

16 pathways

IDPathway
R-HSA-156827L13a-mediated translational silencing of Ceruloplasmin expression
R-HSA-156902Peptide chain elongation
R-HSA-1799339SRP-dependent cotranslational protein targeting to membrane
R-HSA-192823Viral mRNA Translation
R-HSA-2408557Selenocysteine synthesis
R-HSA-6791226Major pathway of rRNA processing in the nucleolus and cytosol
R-HSA-72689Formation of a pool of free 40S subunits
R-HSA-72706GTP hydrolysis and joining of the 60S ribosomal subunit
R-HSA-72764Eukaryotic Translation Termination
R-HSA-9010553Regulation of expression of SLITs and ROBOs
R-HSA-9633012Response of EIF2AK4 (GCN2) to amino acid deficiency
R-HSA-975956Nonsense Mediated Decay (NMD) independent of the Exon Junction Complex (EJC)
R-HSA-975957Nonsense Mediated Decay (NMD) enhanced by the Exon Junction Complex (EJC)
R-HSA-9954709Ribosome Quality Control (RQC) complex extracts and degrades nascent peptide
R-HSA-9954714PELO:HBS1L and ABCE1 dissociate a ribosome on a non-stop mRNA
R-HSA-9954716ZNF598 and the Ribosome-associated Quality Trigger (RQT) complex dissociate a ribosome stalled on a no-go mRNA

MSigDB gene sets: 271 (showing top): GOBP_CYTOPLASMIC_TRANSLATION, MODULE_151, GNF2_TPT1, ENK_UV_RESPONSE_KERATINOCYTE_UP, BHATI_G2M_ARREST_BY_2METHOXYESTRADIOL_DN, GOBP_STRIATED_MUSCLE_CELL_DIFFERENTIATION, ACEVEDO_NORMAL_TISSUE_ADJACENT_TO_LIVER_TUMOR_DN, HSIAO_HOUSEKEEPING_GENES, GOBP_MALE_GAMETE_GENERATION, KONG_E2F3_TARGETS, GOBP_NEGATIVE_REGULATION_OF_CELLULAR_COMPONENT_ORGANIZATION, GOBP_TRANSLATION, GOBP_MUSCLE_STRUCTURE_DEVELOPMENT, GOBP_MUSCLE_CONTRACTION, SHETH_LIVER_CANCER_VS_TXNIP_LOSS_PAM1

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

GO Molecular Function (4): RNA binding (GO:0003723), structural constituent of ribosome (GO:0003735), large ribosomal subunit rRNA binding (GO:0070180), protein binding (GO:0005515)

GO Cellular Component (10): 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), ribonucleoprotein complex (GO:1990904)

Reactome top-level categories

Rollup of top-11 pathways:

CategoryPathways
Ribosome-associated quality control3
Translation2
Cap-dependent Translation Initiation2
Nonsense-Mediated Decay (NMD)2
Eukaryotic Translation Initiation1
Eukaryotic Translation Elongation1
Influenza Viral RNA Transcription and Replication1
Selenoamino acid metabolism1
rRNA processing in the nucleus and cytosol1
Signaling by ROBO receptors1
Cellular response to starvation1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure3
ribosome2
translation1
peptidyltransferase activity1
translational initiation1
translational elongation1
translational termination1
macromolecule biosynthetic process1
protein metabolic process1
protein biosynthetic process1
nucleic acid binding1
structural molecule activity1
rRNA binding1
binding1
intracellular anatomical structure1
cytoplasm1
cell-substrate junction1
asymmetric synapse1
postsynaptic specialization1
large ribosomal subunit1
cytosolic ribosome1
cytosol1
extracellular vesicle1
intracellular membraneless organelle1
protein-containing complex1

Protein interactions and networks

STRING

4194 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
RPL12RPL23AP29316889
RPL12RPL3P39023855
RPL12IPO11Q9UI26831
RPL12RPLP0P05388824
RPL12RPL7P18124823
RPL12RPL11P25121816
RPL12RPL4P36578808
RPL12RPL6Q02878784
RPL12RPL14P50914781
RPL12RPL18Q07020778
RPL12RPS2P15880775
RPL12LRRC70Q7Z2Q7762
RPL12RPS11P04643758
RPL12RPS24P16632756
RPL12RPL32P02433752

IntAct

242 interactions, top by confidence:

ABTypeScore
CNOT2CNOT1psi-mi:“MI:0914”(association)0.740
NCK1NCK2psi-mi:“MI:0914”(association)0.730
CFTRESYT2psi-mi:“MI:0914”(association)0.710
CFTRESYT2psi-mi:“MI:2364”(proximity)0.710
NCBP1KPNA3psi-mi:“MI:0914”(association)0.640
NOM1RPLP0psi-mi:“MI:0914”(association)0.530
DLDPDHBpsi-mi:“MI:0914”(association)0.530
MECP2GTPBP10psi-mi:“MI:0914”(association)0.530
RPL30RRP8psi-mi:“MI:0914”(association)0.530
PUM3RRP8psi-mi:“MI:0914”(association)0.530
SYNGAP1IGF2BP3psi-mi:“MI:0914”(association)0.530
MAGEB10GTPBP10psi-mi:“MI:0914”(association)0.530
ZC3HAV1KHNYNpsi-mi:“MI:0914”(association)0.530
MAGEB2GTPBP10psi-mi:“MI:0914”(association)0.530
DDX6MCRIP1psi-mi:“MI:0914”(association)0.510
CFTRPLEKHG3psi-mi:“MI:0914”(association)0.480
ESR1psi-mi:“MI:0914”(association)0.460
PRDX2RPL12psi-mi:“MI:0915”(physical association)0.400
C1DRPL12psi-mi:“MI:0915”(physical association)0.400
FER1L5psi-mi:“MI:0915”(physical association)0.400
GNAT3psi-mi:“MI:0915”(physical association)0.400

BioGRID (636): RPL12 (Affinity Capture-MS), RPL12 (Affinity Capture-MS), RPL12 (Affinity Capture-MS), RPL12 (Affinity Capture-MS), RPL12 (Affinity Capture-MS), RPL12 (Affinity Capture-MS), GNB2L1 (Co-fractionation), RPL10A (Co-fractionation), RPL12 (Co-fractionation), RPL12 (Co-fractionation), RPL12 (Co-fractionation), RPL12 (Co-fractionation), RPL12 (Co-fractionation), RPL12 (Co-fractionation), RPL12 (Co-fractionation)

ESM2 similar proteins: A0B923, B1AJI2, B5ZC49, C3MR83, C3MXH2, C3MZB8, C3N7D9, C3NG95, C4KIJ7, E2RR58, G1SMR7, O50003, P0CT83, P0CT84, P0CX53, P0CX54, P23358, P30050, P34264, P35025, P35979, P50883, P50884, P53875, P61284, P61865, P61866, P62444, P62446, P96037, Q0W049, Q46EU7, Q4A5E0, Q54J50, Q5AJF7, Q5XIE3, Q6KIF0, Q6L1Y0, Q6QMZ7, Q7RX40

Diamond homologs: A2BN63, A3CSJ5, A4FW91, A4YH87, A6UQ78, A6UVR5, A6VH19, A7IAK5, A9A9N0, B1L6L2, B6YSX7, B8D5P9, B8FEU5, B8GIY2, C5A426, E2RR58, G1SMR7, O29712, O50003, O57779, P0CT83, P0CT84, P0CX53, P0CX54, P23358, P30050, P35025, P35979, P50883, P50884, P54030, P61284, P61865, P61866, P62445, Q0W049, Q2FQ31, Q54J50, Q5AJF7, Q5JH34

SIGNOR signaling

2 interactions.

AEffectBMechanism
CDK2unknownRPL12phosphorylation
RPL12“form complex”“60S cytosolic large ribosomal subunit”binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 217 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:

PathwayPartnersFoldFDR
Nuclear events stimulated by ALK signaling in cancer510.5×4e-03
SRP-dependent cotranslational protein targeting to membrane1610.3×2e-09
Formation of a pool of free 40S subunits1410.1×3e-08
Nonsense Mediated Decay (NMD) independent of the Exon Junction Complex (EJC)139.8×6e-08
Peptide chain elongation129.8×2e-07
Viral mRNA Translation129.8×2e-07
PELO:HBS1L and ABCE1 dissociate a ribosome on a non-stop mRNA129.7×3e-07
Selenocysteine synthesis129.2×4e-07

GO biological processes:

GO termPartnersFoldFDR
stress granule assembly618.9×2e-04
cytoplasmic translation1514.5×1e-10
translational initiation611.3×2e-03
negative regulation of translation99.2×2e-04
translation158.1×4e-07
rRNA processing107.4×2e-04
mRNA splicing, via spliceosome104.8×5e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance16
Likely benign0
Benign0

Top pathogenic / likely-pathogenic (0)

SpliceAI

850 predictions. Top by Δscore:

VariantEffectΔscore
9:127447725:CT:Cacceptor_gain1.0000
9:127447727:C:CCacceptor_gain1.0000
9:127447870:CACT:Cdonor_loss1.0000
9:127447871:ACTTA:Adonor_loss1.0000
9:127447872:CTT:Cdonor_loss1.0000
9:127447873:TTACG:Tdonor_loss1.0000
9:127447874:T:TGdonor_loss1.0000
9:127447875:A:ACdonor_gain1.0000
9:127447875:ACGG:Adonor_gain1.0000
9:127447876:C:CAdonor_gain1.0000
9:127447876:CG:Cdonor_gain1.0000
9:127447876:CGG:Cdonor_gain1.0000
9:127447876:CGGC:Cdonor_gain1.0000
9:127447876:CGGCT:Cdonor_gain1.0000
9:127447990:C:CCacceptor_gain1.0000
9:127448332:CTTA:Cdonor_loss1.0000
9:127448334:T:TGdonor_loss1.0000
9:127448335:A:ACdonor_gain1.0000
9:127448335:A:ATdonor_loss1.0000
9:127448336:C:CCdonor_gain1.0000
9:127448419:TTTAA:Tacceptor_gain1.0000
9:127448420:TTAA:Tacceptor_gain1.0000
9:127448421:TAA:Tacceptor_gain1.0000
9:127448421:TAAC:Tacceptor_loss1.0000
9:127448422:AA:Aacceptor_gain1.0000
9:127448422:AAC:Aacceptor_loss1.0000
9:127448423:ACT:Aacceptor_loss1.0000
9:127448424:C:Aacceptor_loss1.0000
9:127448424:C:CCacceptor_gain1.0000
9:127448427:C:CTacceptor_gain1.0000

AlphaMissense

1073 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
9:127447946:A:CC141W1.000
9:127447947:C:TC141Y1.000
9:127447968:C:AG134V1.000
9:127447968:C:TG134E1.000
9:127447969:C:AG134W1.000
9:127447969:C:GG134R1.000
9:127447969:C:TG134R1.000
9:127448378:G:TA113D1.000
9:127449294:C:AK93N1.000
9:127449294:C:GK93N1.000
9:127449297:T:AR92S1.000
9:127449297:T:GR92S1.000
9:127449298:C:GR92T1.000
9:127449337:G:TA79D1.000
9:127449343:G:TA77D1.000
9:127449614:G:TA69D1.000
9:127449619:T:AR67S1.000
9:127449619:T:GR67S1.000
9:127449620:C:AR67I1.000
9:127449620:C:GR67T1.000
9:127449629:A:TI64N1.000
9:127449635:A:GL62P1.000
9:127449635:A:TL62Q1.000
9:127449641:A:TV60E1.000
9:127449650:C:AR57M1.000
9:127449653:A:GL56P1.000
9:127449657:C:GG55R1.000
9:127449663:A:GW53R1.000
9:127449663:A:TW53R1.000
9:127449680:G:TA47D1.000

dbSNP variants (sampled 300 via entrez): RS1000228584 (9:127450305 C>G), RS1000731982 (9:127452584 A>G), RS1000738412 (9:127452838 G>A), RS1000811215 (9:127448746 G>A), RS1001056287 (9:127447816 CTG>C), RS1001119093 (9:127448517 T>C), RS1001745572 (9:127451463 C>A,T), RS1001780194 (9:127452552 A>G), RS1002052027 (9:127447456 C>G), RS1002733704 (9:127451164 C>A,G,T), RS1002742128 (9:127450494 C>T), RS1003987576 (9:127451133 A>G), RS1004297230 (9:127450936 C>G), RS1005688280 (9:127452106 C>T), RS1006311328 (9:127451023 G>A,T)

Disease associations

OMIM: gene MIM:180475 | 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), CHEMBL6066923 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds).

MoleculeNamePhasePatents
CHEMBL6067484GENTAMICIN SULFATE4

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).

pChemblTypeValueUnitMolecule
7.29Kd51.34nMCHEMBL5653589
7.29ED5051.34nMCHEMBL5653589
6.52IC50300nMCHEMBL4109308
6.42IC50380nMCHEMBL4109308
6.42IC50380nMCHEMBL4574496
6.41IC50390nMCHEMBL4126894
6.39IC50410nMCHEMBL4114159
6.35IC50450nMCHEMBL4126496
6.30IC50500nMCHEMBL4574496
6.30IC50500nMCHEMBL4560206
6.16IC50690nMCHEMBL4130157
6.15IC50710nMCHEMBL4108338
6.11IC50780nMCHEMBL4114159
6.09IC50820nMCHEMBL4109308
6.07IC50850nMCHEMBL4107559
6.07IC50850nMCHEMBL4533299
6.05IC50900nMCHEMBL4126894
6.05IC50900nMCHEMBL4126496
6.04IC50920nMCHEMBL4554909
5.97IC501060nMCHEMBL4128388
5.89IC501290nMCHEMBL4130157
5.86IC501370nMCHEMBL4107559
5.84IC501440nMCHEMBL4108338
5.81IC501540nMCHEMBL4534859
5.76IC501730nMCHEMBL4534859
5.69IC502050nMCHEMBL4566239
5.68IC502080nMCHEMBL4446635
5.66IC502210nMCHEMBL4446635
5.66EC502200nMCHEMBL4464929
5.64IC502270nMCHEMBL4533299
5.63IC502330nMCHEMBL4566239
5.62IC502380nMCHEMBL4128388
5.58IC502630nMCHEMBL4128250
5.55IC502820nMCHEMBL4127458
5.53IC502970nMCHEMBL4127311
5.51IC503080nMCHEMBL4126072
5.46IC503500nMCHEMBL4525277
5.44IC503630nMCHEMBL4469712
5.44Kd3628nMCHEMBL3752910
5.44ED503628nMCHEMBL3752910
5.39IC504100nMCHEMBL4128560
5.37IC504300nMCHEMBL4127016
5.36IC504380nMCHEMBL4527910
5.16IC507000nMCHEMBL4109308
5.13IC507400nMCHLORAMPHENICOL SULFATE SALT
5.09IC508040nMCHEMBL4128250
5.08IC508370nMCHEMBL4128250
5.03IC509320nMCHEMBL4127016
5.03IC509240nMCHEMBL4128560

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.

CompoundAssayTypeValueUnit
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide2149242: Binding affinity to human RPL12 incubated for 45 mins by Kinobead based pull down assaykd0.0513uM
N-(3-chloro-2-pyridinyl)-N-[(3R)-piperidin-3-yl]-4-(triazolo[4,5-b]pyridin-3-yl)benzamide1585498: 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 methodic500.3000uM
N-(3-chloro-2-pyridinyl)-N-[(3R)-piperidin-3-yl]-3-[4-(triazolo[4,5-b]pyridin-3-yl)phenyl]propanamide1532845: 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 assayic500.3800uM
N-isoquinolin-1-yl-N-[(3R)-piperidin-3-yl]-4-(triazolo[4,5-b]pyridin-3-yl)benzamide1497947: 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 assayic500.3900uM
N-(3-chloro-2-pyridinyl)-4-(6-methyltriazolo[4,5-b]pyridin-3-yl)-N-[(3R)-piperidin-3-yl]benzamide1497947: 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 assayic500.4100uM
N-(3-chloro-2-pyridinyl)-4-(5-methyltriazolo[4,5-b]pyridin-3-yl)-N-[(3R)-piperidin-3-yl]benzamide1497947: 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 assayic500.4500uM
N-(1-methylpyrrolo[2,3-c]pyridin-7-yl)-4-phenyl-N-[(3R)-piperidin-3-yl]piperidine-1-carboxamide1532846: 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 assayic500.5000uM
N-isoquinolin-1-yl-N-[(3R)-piperidin-3-yl]-4-pyrazolo[1,5-a]pyrimidin-3-ylbenzamide1497947: 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 assayic500.6900uM
N-(3-chloro-2-pyridinyl)-N-[(3R)-piperidin-3-yl]-5-(triazolo[4,5-b]pyridin-3-yl)pyridine-2-carboxamide1497947: 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 assayic500.7100uM
N-(3-chloro-2-pyridinyl)-3-[5-(6-methyltriazolo[4,5-b]pyridin-3-yl)-2-pyridinyl]-N-[(3R)-piperidin-3-yl]propanamide1532845: 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 assayic500.8500uM
N-(3-chloro-2-pyridinyl)-5-(6-methyltriazolo[4,5-b]pyridin-3-yl)-N-[(3R)-piperidin-3-yl]pyridine-2-carboxamide1497947: 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 assayic500.8500uM
N-(3-methyl-2-pyridinyl)-N-[(3R)-piperidin-3-yl]-4-pyrazolo[1,5-a]pyrimidin-3-ylpiperidine-1-carboxamide1532846: 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 assayic500.9200uM
N-isoquinolin-1-yl-4-(1-methylpyrazol-4-yl)-N-[(3R)-piperidin-3-yl]benzamide1497947: 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 assayic501.0600uM
N-isoquinolin-1-yl-4-phenyl-N-[(3R)-piperidin-3-yl]piperidine-1-carboxamide1532846: 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 assayic501.5400uM
N-(3-methyl-2-pyridinyl)-4-phenyl-N-[(3R)-piperidin-3-yl]piperidine-1-carboxamide1532845: 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 assayic502.0500uM
N-(3-chloro-2-pyridinyl)-4-phenyl-N-[(3R)-piperidin-3-yl]piperidine-1-carboxamide1532846: 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 assayic502.0800uM
N-(5,8-dihydroisoquinolin-1-yl)-3-(4-methoxyphenyl)-N-[(3R)-piperidin-3-yl]propanamide1584424: Inhibition of human 80S ribosome-mediated PCSK9 translation expressed in CHO-K1 cells assessed as reduction in PCSK9 secretionec502.2000uM
N-isoquinolin-1-yl-3-(4-methoxyphenyl)-N-[(3R)-piperidin-3-yl]propanamide1497947: 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 assayic502.6300uM
N-(3-chloro-2-pyridinyl)-4-(6-methylpyrazin-2-yl)-N-[(3R)-piperidin-3-yl]benzamide1497963: Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISAic502.8200uM
N-(3-chloro-2-pyridinyl)-4-[6-(dimethylamino)pyrazin-2-yl]-N-[(3R)-piperidin-3-yl]benzamide1497963: Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISAic502.9700uM
N-(3-chloro-2-pyridinyl)-4-[6-(methylamino)pyrazin-2-yl]-N-[(3R)-piperidin-3-yl]benzamide1497963: Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISAic503.0800uM
N-isoquinolin-1-yl-4-(6-methyl-1,2-benzoxazol-3-yl)-N-[(3R)-piperidin-3-yl]piperazine-1-carboxamide1532845: 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 assayic503.5000uM
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide2149242: Binding affinity to human RPL12 incubated for 45 mins by Kinobead based pull down assaykd3.6277uM
N-(3-methylpyrazin-2-yl)-4-phenyl-N-[(3R)-piperidin-3-yl]piperidine-1-carboxamide1532846: 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 assayic503.6300uM
N-(3-chloro-2-pyridinyl)-N-[(3R)-piperidin-3-yl]-6-(triazolo[4,5-b]pyridin-3-yl)pyridine-3-carboxamide1497947: 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 assayic504.1000uM
N-isoquinolin-1-yl-N-[(3R)-piperidin-3-yl]-4-pyrazin-2-ylbenzamide1497947: 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 assayic504.3000uM
4-(2-fluorophenyl)-N-(3-methyl-2-pyridinyl)-N-[(3R)-piperidin-3-yl]piperidine-1-carboxamide1532846: 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 assayic504.3800uM
2,2-dichloro-N-[(1R,2R)-1,3-dihydroxy-1-(4-nitrophenyl)propan-2-yl]acetamide;sulfuric acid717551: Inhibition of mitochondrial ribosome-mediated protein synthesis in human HeLa cells assessed as {35S]methionine incorporation by autoradiographyic507.4000uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
bisphenol Aaffects expression, decreases expression3
Cadmium Chlorideincreases abundance, increases expression2
Particulate Matterincreases expression, decreases expression2
FR900359affects phosphorylation1
bisphenol Fincreases expression1
triphenyl phosphateaffects expression1
deoxynivalenolincreases expression1
sodium arsenatedecreases expression1
beta-lapachoneincreases expression1
arseniteaffects binding, increases reaction1
sodium arsenitedecreases expression1
perfluorooctane sulfonic acidincreases expression1
CGP 52608increases reaction, affects binding1
chloropicrindecreases expression1
2-palmitoylglycerolincreases expression1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamideaffects cotreatment, decreases expression1
bisphenol Bincreases expression1
abrinedecreases expression1
jinfukangaffects cotreatment, increases expression1
LDN 193189affects cotreatment, decreases expression1
(+)-JQ1 compoundincreases expression1
bisphenol AFincreases expression1
Temozolomideincreases expression1
Sunitinibincreases expression1
Vorinostatdecreases expression1
Acetaminophendecreases expression1
Cadmiumincreases abundance, increases expression1
Cisplatinaffects cotreatment, increases expression1
Diazinonincreases methylation1
Diethylstilbestrolincreases expression1

ChEMBL screening assays

90 unique, capped per target: 90 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1920845BindingInduction of ribosome to readthrough in human A-T lymphoblastoid cells assessed as ATM ser1981 autophosphorylation at 30 uM after 4 days by PTT-ELISA assaySynthesis 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.

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.4
BioBTree
v2.0.2

Sources 79

This page pulls from 79 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot