Childhood-onset schizophrenia

disease
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Summary

Childhood-onset schizophrenia (MONDO:0957430) is a disease with 20 cohort genes.

At a glance

  • Prevalence: Unknown (Europe) [Orphanet-validated]
  • Cohort genes: 20
  • ClinVar variants: 21

Clinical features

Epidemiology

Prevalence records

1 prevalence record(s), Orphanet:

TypeClassValueGeographyValidation
Annual incidence1-5 / 10 000EuropeValidated

Identifiers

Disease identifiers

FieldValue
Canonical namechildhood-onset schizophrenia
Mondo IDMONDO:0957430
Orphanet641496
UMLSC0036346
MedGen48576
GARD0004766
Is cancer (heuristic)no

Data availability: 21 ClinVar variants.

Disease family

Classification path: disease › human disease › disease by developmental or physiological process › psychiatric disordercognitive disorderpsychotic disorderschizophreniachildhood-onset schizophrenia

Related subtypes (17): paranoid schizophrenia, treatment-refractory schizophrenia, schizophrenia 1, schizophrenia 3, schizophrenia 5, schizophrenia 7, schizophrenia 8, schizophrenia 2, schizophrenia 10, schizophrenia 11, schizophrenia 12, schizophrenia 15, schizophrenia 16, chromosome 2p16.3 deletion syndrome, early-onset schizophrenia, schizophrenia 19, schizophrenia 17

Genetics & variants

GWAS landscape

No GWAS associations recorded — common-variant (GWAS) studies don’t cover this disease (typical for Mendelian / rare diseases). See the curated gene cohort and Mendelian overlap below.

Variant details and genetic-evidence tiers

ClinVar germline variants

21 retrieved; paginated sample, class counts are floors:

16 likely pathogenic, 3 benign, 2 conflicting classifications of pathogenicity

ClinVarVariant (HGVS)GeneClassificationReview
208393NM_001040025.3(ARL16):c.-41G>TARL16Likely pathogeniccriteria provided, single submitter
208399NM_138706.5(B3GNT6):c.552C>G (p.Asp184Glu)B3GNT6Likely pathogeniccriteria provided, single submitter
208382NM_207361.6(FREM2):c.8351G>A (p.Arg2784Lys)FREM2Likely pathogeniccriteria provided, single submitter
208386NM_003774.5(GALNT4):c.1194C>T (p.Asn398=)GALNT4Likely pathogeniccriteria provided, single submitter
208391NM_207370.4(GPR153):c.217C>T (p.Arg73Cys)GPR153Likely pathogeniccriteria provided, single submitter
208388NM_005685.4(GTF2IRD1):c.973C>T (p.Arg325Cys)GTF2IRD1Likely pathogeniccriteria provided, single submitter
208387NM_000210.4(ITGA6):c.*91AGA[1]ITGA6Likely pathogeniccriteria provided, single submitter
208394NM_002402.4(MEST):c.559C>T (p.Pro187Ser)MESTLikely pathogeniccriteria provided, single submitter
208395NM_015009.3(PDZRN3):c.820G>A (p.Asp274Asn)PDZRN3Likely pathogeniccriteria provided, single submitter
208402NM_000961.4(PTGIS):c.824G>A (p.Arg275Gln)PTGISLikely pathogeniccriteria provided, single submitter
208401NM_021975.4(RELA):c.329T>C (p.Ile110Thr)RELALikely pathogeniccriteria provided, single submitter
208396NM_001035.3(RYR2):c.2236C>T (p.Gln746Ter)RYR2Likely pathogeniccriteria provided, single submitter
208397NM_001035.3(RYR2):c.2238A>C (p.Gln746His)RYR2Likely pathogeniccriteria provided, single submitter
208383NM_178860.5(SEZ6):c.678_686del (p.Thr227_Thr229del)SEZ6Likely pathogeniccriteria provided, single submitter
208390NM_198993.5(STAC2):c.257G>A (p.Arg86Lys)STAC2Likely pathogeniccriteria provided, single submitter
208398NM_032538.3(TTBK1):c.773G>A (p.Arg258Gln)TTBK1Likely pathogeniccriteria provided, single submitter
208389NM_005529.7(HSPG2):c.4233C>T (p.Tyr1411=)HSPG2Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
208384NM_144687.4(NLRP12):c.858C>G (p.Pro286=)NLRP12Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
208404NM_001326411.2(PISD):c.322-3886G>ALOC110121499Benigncriteria provided, single submitter
208405NM_017514.5(PLXNA3):c.1847G>A (p.Arg616Gln)PLXNA3Benigncriteria provided, single submitter
208406NM_015316.3(PPP1R13B):c.215G>A (p.Arg72Gln)PPP1R13BBenigncriteria provided, single submitter

Genes & proteins

Mendelian disease overlap and somatic drivers

GenCC: 0 · Orphanet: 16 · OMIM-shared: 0 · Dual-evidence (GWAS+Mendelian): 0

Orphanet rare-disease linkage (cohort genes)

GeneOrphanet IDRare disease
RYR2Orphanet:293888Inherited isolated arrhythmogenic cardiomyopathy, dominant-left variant
RYR2Orphanet:293899Inherited isolated arrhythmogenic ventricular dysplasia, biventricular variant
RYR2Orphanet:293910Inherited isolated arrhythmogenic cardiomyopathy, dominant-right variant
RYR2Orphanet:3286Catecholaminergic polymorphic ventricular tachycardia
B4GAT1Orphanet:899Walker-Warburg syndrome
NLRP12Orphanet:247868NLRP12-associated hereditary periodic fever syndrome
FREM2Orphanet:2052Fraser syndrome
FREM2Orphanet:93100Renal agenesis, unilateral
FREM2Orphanet:98949Complete cryptophthalmia
GTF2IRD1Orphanet:904Williams syndrome
HSPG2Orphanet:16061p36 deletion syndrome
HSPG2Orphanet:1865Dyssegmental dysplasia, Silverman-Handmaker type
HSPG2Orphanet:800Schwartz-Jampel syndrome
ITGA6Orphanet:79403Junctional epidermolysis bullosa with pyloric atresia
RELAOrphanet:530792RELA fusion-positive ependymoma
RELAOrphanet:596759Combined immunodeficiency due to RELA haploinsufficiency

Cohort genes → proteins

20 cohort genes, 20 distinct canonical proteins.

Evidence partition

SubsetGenes
multi_evidence20

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
RYR2HGNC:10484ENSG00000198626Q92736Ryanodine receptor 2clinvar
PPP1R13BHGNC:14950ENSG00000088808Q96KQ4Apoptosis-stimulating of p53 protein 1clinvar
B4GAT1HGNC:15685ENSG00000174684O43505Beta-1,4-glucuronyltransferase 1clinvar
SEZ6HGNC:15955ENSG00000063015Q53EL9Seizure protein 6 homologclinvar
PDZRN3HGNC:17704ENSG00000121440Q9UPQ7E3 ubiquitin-protein ligase PDZRN3clinvar
TTBK1HGNC:19140ENSG00000146216Q5TCY1Tau-tubulin kinase 1clinvar
NLRP12HGNC:22938ENSG00000142405P59046NACHT, LRR and PYD domains-containing protein 12clinvar
GPR153HGNC:23618ENSG00000158292Q6NV75Probable G-protein coupled receptor 153clinvar
STAC2HGNC:23990ENSG00000141750Q6ZMT1SH3 and cysteine-rich domain-containing protein 2clinvar
B3GNT6HGNC:24141ENSG00000198488Q6ZMB0Acetylgalactosaminyl-O-glycosyl-glycoprotein beta-1,3-N-acetylglucosaminyltransferaseclinvar
FREM2HGNC:25396ENSG00000150893Q5SZK8FRAS1-related extracellular matrix protein 2clinvar
ARL16HGNC:27902ENSG00000214087Q0P5N6ADP-ribosylation factor-like protein 16clinvar
GALNT4HGNC:4126ENSG00000257594Q8N4A0Polypeptide N-acetylgalactosaminyltransferase 4clinvar
GTF2IRD1HGNC:4661ENSG00000006704Q9UHL9General transcription factor II-I repeat domain-containing protein 1clinvar
HSPG2HGNC:5273ENSG00000142798P98160Basement membrane-specific heparan sulfate proteoglycan core proteinclinvar
ITGA6HGNC:6142ENSG00000091409P23229Integrin alpha-6clinvar
MESTHGNC:7028ENSG00000106484Q5EB52Mesoderm-specific transcript homolog proteinclinvar
PLXNA3HGNC:9101ENSG00000130827P51805Plexin-A3clinvar
PTGISHGNC:9603ENSG00000124212Q16647Prostacyclin synthaseclinvar
RELAHGNC:9955ENSG00000173039Q04206Transcription factor p65clinvar

Cohort function summary

Lead sentence per gene, UniProt-curated.

SymbolProtein nameFunction (lead sentence)
RYR2Ryanodine receptor 2Cytosolic calcium-activated calcium channel that mediates the release of Ca(2+) from the sarcoplasmic reticulum into the cytosol and thereby plays a key role in triggering cardiac muscle contraction.
PPP1R13BApoptosis-stimulating of p53 protein 1Regulator that plays a central role in regulation of apoptosis via its interaction with p53/TP53.
B4GAT1Beta-1,4-glucuronyltransferase 1Beta-1,4-glucuronyltransferase involved in O-mannosylation of alpha-dystroglycan (DAG1).
SEZ6Seizure protein 6 homologMay play a role in cell-cell recognition and in neuronal membrane signaling.
PDZRN3E3 ubiquitin-protein ligase PDZRN3E3 ubiquitin-protein ligase.
TTBK1Tau-tubulin kinase 1Serine/threonine kinase which is able to phosphorylate TAU on serine, threonine and tyrosine residues.
NLRP12NACHT, LRR and PYD domains-containing protein 12Plays an essential role as an potent mitigator of inflammation.
GPR153Probable G-protein coupled receptor 153Orphan receptor.
STAC2SH3 and cysteine-rich domain-containing protein 2Plays a redundant role in promoting the expression of calcium channel CACNA1S at the cell membrane, and thereby contributes to increased channel activity.
B3GNT6Acetylgalactosaminyl-O-glycosyl-glycoprotein beta-1,3-N-acetylglucosaminyltransferaseBeta-1,3-N-acetylglucosaminyltransferase that synthesizes the core 3 structure of the O-glycan, an important precursor in the biosynthesis of mucin-type glycoproteins.
FREM2FRAS1-related extracellular matrix protein 2Extracellular matrix protein required for maintenance of the integrity of the skin epithelium and for maintenance of renal epithelia.
ARL16ADP-ribosylation factor-like protein 16Required for the trafficking of ciliary proteins IFT140 and INPP5E from the Golgi to the cilia, thus playing a role in ciliogenesis.
GALNT4Polypeptide N-acetylgalactosaminyltransferase 4Catalyzes the initial reaction in O-linked oligosaccharide biosynthesis, the transfer of an N-acetyl-D-galactosamine residue to a serine or threonine residue on the protein receptor.
GTF2IRD1General transcription factor II-I repeat domain-containing protein 1May be a transcription regulator involved in cell-cycle progression and skeletal muscle differentiation.
HSPG2Basement membrane-specific heparan sulfate proteoglycan core proteinIntegral component of basement membranes.
ITGA6Integrin alpha-6Integrin alpha-6/beta-1 (ITGA6:ITGB1) is a receptor for laminin on platelets.
MESTMesoderm-specific transcript homolog proteinPlays an important role in enabling neurons to transition from bipolar to multipolar shapes, a process essential for their correct migration toward the cortical plate during brain development.
PLXNA3Plexin-A3Coreceptor for SEMA3A and SEMA3F.
PTGISProstacyclin synthaseCatalyzes the biosynthesis and metabolism of eicosanoids.
RELATranscription factor p65NF-kappa-B is a pleiotropic transcription factor present in almost all cell types and is the endpoint of a series of signal transduction events that are initiated by a vast array of stimuli related to many biological processes such as infl…

Protein-family classification

Druggable: 11 · Difficult: 5 · Unknown: 4 · Druggable fraction: 0.55

Family distribution

Cohort families vs a genome-wide background (hypergeometric, BH-FDR; fold = observed/expected). Counts kept; sorted by enrichment, so the catch-all Other/Unknown bucket no longer leads.

FamilyGenesFoldFDR
Complement113.4×0.239
Antibody/Immunoglobulin34.4×0.239
Enzyme (other)42.4×0.239
Ion channel15.6×0.371
Scaffold/PPI21.7×0.582
Kinase11.4×0.646
Transcription factor31.2×0.646
GPCR11.2×0.646
Other/Unknown40.4×1.000

Per-gene assignment

SymbolFamilyDruggable?ECInterPro (top 3)
RYR2Ion channelyesRIH_dom, B30.2/SPRY, EF_hand_dom
PPP1R13BScaffold/PPInoSH3_domain, Ankyrin_rpt, ASPP1_RA
B4GAT1Enzyme (other)yes2.4.1.149B4GAT1
SEZ6ComplementyesSushi_SCR_CCP_dom, CUB_dom, Sperma_CUB_dom_sf
PDZRN3Transcription factornoZnf_TRAF, PDZ, Znf_RING
TTBK1Kinaseyes2.7.11.26Prot_kinase_dom, Kinase-like_dom_sf, Protein_kinase_ATP_BS
NLRP12Other/UnknownnoLeu-rich_rpt, DAPIN, NACHT_NTPase
GPR153GPCRyesGPCR_Rhodpsn, GPCR_Rhodpsn_7TM, GPR153
STAC2Scaffold/PPInoSH3_domain, PKC_DAG/PE, Stac2_SH3
B3GNT6Enzyme (other)yes2.4.1.147Glyco_trans_31
FREM2Other/UnknownnoCalx_beta, CalX-like_sf, CSPG_rpt
ARL16Other/UnknownnoSmall_GTPase_ARF/SAR, P-loop_NTPase
GALNT4Enzyme (other)yes2.4.1.41Ricin_B_lectin, Glyco_trans_2-like, Nucleotide-diphossugar_trans
GTF2IRD1Transcription factornoGTF2I, TF_II-I, GTF2I-like_rpt_sf
HSPG2Antibody/ImmunoglobulinyesLaminin_IV, SEA_dom, EGF
ITGA6Antibody/ImmunoglobulinyesIntegrin_alpha, FG-GAP, Int_alpha_beta-p
MESTOther/UnknownnoAB_hydrolase_1, Epox_hydrolase-like, AB_hydrolase_fold
PLXNA3Antibody/ImmunoglobulinyesSemap_dom, Plexin_repeat, IPT_dom
PTGISEnzyme (other)yes5.3.99.4Cyt_P450, Cyt_P450_E_grp-IV, Cyt_P450_CYP7A1-type
RELATranscription factornoNFkB/Dor, IPT_dom, p53-like_TF_DNA-bd_sf

Expression context

Cohort genes with no expression data: 0.

16 cohort genes are a single-cell marker in ≥1 SCXA experiment.

Breadth distribution (Bgee present_calls)

BucketGenes
narrow (1-5 tissues)0
moderate (6-20)0
broad (>20)20
unknown0

Top tissues across cohort

TissueCohort genes
popliteal artery3
tibial artery3
right hemisphere of cerebellum2
blood vessel layer2
mucosa of stomach2
lateral nuclear group of thalamus2
prefrontal cortex2
rectum2
heart right ventricle1
left ventricle myocardium1
myocardium1
left lobe of thyroid gland1
right lobe of thyroid gland1
thyroid gland1
endothelial cell1
middle temporal gyrus1
pons1
cortical plate1
ganglionic eminence1
hair follicle1

Per-gene tissue summary (top 30)

SymbolBgee breadthFANTOM5 breadthSCXATop tissues
RYR2210broadmarkerheart right ventricle, left ventricle myocardium, myocardium
PPP1R13B277ubiquitousmarkerright lobe of thyroid gland, left lobe of thyroid gland, thyroid gland
B4GAT1285ubiquitousmarkerendothelial cell, middle temporal gyrus, pons
SEZ6167broadmarkercortical plate, ganglionic eminence, right hemisphere of cerebellum
PDZRN3282broadmarkerblood vessel layer, hair follicle, mucosa of stomach
TTBK1126broadyeslateral nuclear group of thalamus, prefrontal cortex, postcentral gyrus
NLRP12117tissue_specificmarkerblood, monocyte, leukocyte
GPR153265ubiquitousyesileal mucosa, lateral nuclear group of thalamus, triceps brachii
STAC2164broadmarkerpopliteal artery, tibial artery, right frontal lobe
B3GNT676tissue_specificyesrectum, mucosa of sigmoid colon, mucosa of transverse colon
FREM2160broadmarkeradrenal tissue, kidney epithelium, renal medulla
ARL16134ubiquitousmarkermetanephros cortex, prefrontal cortex, right uterine tube
GALNT4132ubiquitousyesendometrium, rectum, duodenum
GTF2IRD1270ubiquitousmarkerlower esophagus mucosa, hindlimb stylopod muscle, tibialis anterior
HSPG2271ubiquitousmarkersaphenous vein, popliteal artery, tibial artery
ITGA6297ubiquitousmarkertibial nerve, sural nerve, dorsal root ganglion
MEST287ubiquitousmarkercartilage tissue, placenta, secondary oocyte
PLXNA3204ubiquitousmarkeradenohypophysis, stromal cell of endometrium, right hemisphere of cerebellum
PTGIS232broadmarkerparietal pleura, right coronary artery, blood vessel layer
RELA295ubiquitousmarkermucosa of stomach, popliteal artery, tibial artery

Protein interactions among cohort

Intra-cohort edges: 1.

Hub genes (top 10 by interactor count)

SymbolInteractor count
RELA8,449
ITGA63,130
RYR22,653
HSPG22,463
GPR1532,092
PTGIS2,053
SEZ62,025
MEST1,862
STAC21,811
TTBK11,784

Intra-cohort edges

ABSources
PPP1R13BRELAstring_interaction

Structural data

PDB: 12 · AlphaFold-only: 8 · No structure: 0

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
RELAQ0420688
RYR2Q9273626
TTBK1Q5TCY116
GTF2IRD1Q9UHL94
NLRP12P590463
STAC2Q6ZMT13
PDZRN3Q9UPQ72
GALNT4Q8N4A02
HSPG2P981602
ITGA6P232292
PTGISQ166472
PPP1R13BQ96KQ41

AlphaFold-only cohort genes (top 30 by pLDDT)

SymbolUniProtpLDDT
MESTQ5EB5291.88
B4GAT1O4350588.46
B3GNT6Q6ZMB087.19
ARL16Q0P5N686.91
PLXNA3P5180584.77
SEZ6Q53EL970.43
GPR153Q6NV7565.60
FREM2Q5SZK8

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 172. Enrichment computed across 20 evidence-associated genes (11 with Reactome annotation).

Pathways by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 11 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

PathwayCohort genesFoldFDRSample cohort genes
Laminin interactions269.2×0.062HSPG2, ITGA6
Defective LARGE causes MDDGA6 and MDDGB61346.1×0.070B4GAT1
p75NTR signals via NF-kB1173.0×0.070RELA
CLEC7A/inflammasome pathway1173.0×0.070RELA
DEx/H-box helicases activate type I IFN and inflammatory cytokines production1148.3×0.070RELA
IkBA variant leads to EDA-ID1148.3×0.070RELA
Regulation of NFE2L2 gene expression1129.8×0.070RELA
Interleukin-1 processing1115.3×0.070RELA
Activation of PUMA and translocation to mitochondria1103.8×0.070PPP1R13B
Inflammasomes1103.8×0.070RELA
Cell recruitment (pro-inflammatory response)1103.8×0.070RELA
ZBP1(DAI) mediated induction of type I IFNs194.4×0.070RELA
Regulated proteolysis of p75NTR194.4×0.070RELA
Type I hemidesmosome assembly194.4×0.070ITGA6
Eicosanoids186.5×0.070PTGIS
SUMOylation of immune response proteins186.5×0.070RELA
TP53 Regulates Transcription of Death Receptors and Ligands186.5×0.070PPP1R13B
NF-kB is activated and signals survival179.9×0.070RELA
Diseases of Immune System179.9×0.070RELA
Diseases associated with the TLR signaling cascade179.9×0.070RELA
Downstream signaling events of B Cell Receptor (BCR)174.2×0.070RELA
Defective EXT2 causes exostoses 2174.2×0.070HSPG2
Defective EXT1 causes exostoses 1, TRPS2 and CHDS174.2×0.070HSPG2
Regulation of TP53 Activity through Association with Co-factors174.2×0.070PPP1R13B
Matriglycan biosynthesis on DAG1174.2×0.070B4GAT1
Synthesis of Prostaglandins (PG) and Thromboxanes (TX)169.2×0.070PTGIS
SEMA3A-Plexin repulsion signaling by inhibiting Integrin adhesion169.2×0.070PLXNA3
TP53 regulates transcription of several additional cell death genes whose specific roles in p53-dependent apoptosis remain uncertain169.2×0.070PPP1R13B
Developmental Lineage of Mammary Stem Cells169.2×0.070ITGA6
RIP-mediated NFkB activation via ZBP1161.1×0.070RELA

GO biological processes by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 18 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

GO termCohort genesFoldFDRSample cohort genes
transition between slow and fast fiber1936.2×0.026GTF2IRD1
regulation of interleukin-18 production1936.2×0.026NLRP12
positive regulation of astrocyte activation1936.2×0.026TTBK1
establishment of protein localization to endoplasmic reticulum1936.2×0.026RYR2
cellular response to interleukin-62110.1×0.026PTGIS, RELA
response to muscle stretch285.1×0.026RYR2, RELA
negative regulation of non-canonical NF-kappaB signal transduction256.7×0.026NLRP12, RELA
protein O-linked glycosylation via N-acetylgalactosamine248.0×0.026B3GNT6, GALNT4
negative regulation of extrinsic apoptotic signaling pathway246.8×0.026ITGA6, RELA
embryo implantation239.0×0.026HSPG2, PTGIS
olfactory nerve formation1468.1×0.030PLXNA3
prolactin signaling pathway1468.1×0.030RELA
negative regulation of Toll signaling pathway1468.1×0.030NLRP12
Purkinje myocyte to ventricular cardiac muscle cell signaling1468.1×0.030RYR2
cellular response to interleukin-1231.2×0.030PTGIS, RELA
positive regulation of interleukin-1 beta production228.8×0.030NLRP12, RELA
negative regulation of synaptic transmission, cholinergic1312.1×0.031HSPG2
type B pancreatic cell apoptotic process1312.1×0.031RYR2
regulation of AV node cell action potential1312.1×0.031RYR2
regulation of atrial cardiac muscle cell action potential1312.1×0.031RYR2
positive regulation of voltage-gated calcium channel activity1312.1×0.031STAC2
positive regulation of miRNA metabolic process1312.1×0.031RELA
protein O-linked glycosylation225.0×0.031B3GNT6, GALNT4
left ventricular cardiac muscle tissue morphogenesis1234.1×0.032RYR2
negative regulation of glycoprotein biosynthetic process1234.1×0.032MEST
ectodermal cell differentiation1234.1×0.032ITGA6
toll-like receptor TLR6:TLR2 signaling pathway1234.1×0.032RELA
obsolete positive regulation of sequestering of calcium ion1234.1×0.032RYR2
neuron projection guidance1234.1×0.032PLXNA3
radial glia-guided pyramidal neuron migration1234.1×0.032MEST

Therapeutics

Drug target analysis

Approved (phase 4): 1 · Phase ≥3: 1 · Phased (≥1): 3 · Undrugged: 17

Druggability breadth: 9 of 20 evidence-associated genes (45%) have a ChEMBL target (buckets above are over the deeply-mined display cohort).

Genes with an approved drug

The molecule shown is one approved compound that hits the gene — not necessarily a drug of choice or one indicated for this disease.

SymbolExample approved molecule
RELAINDOPROFEN

Top cohort targets by molecule count

SymbolMoleculesMax phase
RELA174
RYR212
PTGIS12
PPP1R13B00
B4GAT100
SEZ600
PDZRN300
TTBK100
NLRP1200
GPR15300

Drugs targeting cohort genes (top 30)

MoleculeMax phaseTargets in cohort
INDOPROFEN4RELA
VAMOROLONE4RELA
BORTEZOMIB4RELA
DEXAMETHASONE4RELA
SULFASALAZINE4RELA
GEFITINIB4RELA
CURCUMIN3RELA
RESVERATROL3RELA
IXAZOMIB3RELA
WITHANOLIDE D3RELA
TRIPTOLIDE3RELA
ALADORIAN2RYR2
PIRMAGREL2PTGIS
FRENTIZOLE2RELA
LAPACHONE2RELA
SANGUINARIUM2RELA
URSOLIC ACID2RELA
AS-6028681RELA
WITHAFERIN A1RELA

Bioactivity and enzyme data

Enzyme cohort genes (≥1 EC): 5.

Cohort genes with ChEMBL bioactivity (full, sorted by assay count)

SymbolAssaysType breakdown
RELA422Binding:417, Functional:4, ADMET:1
TTBK174Binding:74
MEST20Binding:20
RYR215Binding:15
PTGIS12Binding:12
ITGA63Binding:3
GPR1532Binding:2
HSPG22Binding:2
B3GNT61Binding:1

Cohort enzymes (BRENDA EC)

SymbolEC numbersNames
B4GAT12.4.1.149N-acetyllactosaminide beta-1,3-N-acetylglucosaminyltransferase
TTBK12.7.11.26tau-protein kinase
B3GNT62.4.1.147acetylgalactosaminyl-O-glycosyl-glycoprotein beta-1,3-N-acetylglucosaminyltransferase
GALNT42.4.1.41polypeptide N-acetylgalactosaminyltransferase
PTGIS5.3.99.4prostaglandin-I synthase

Cohort genes with high screening signal

≥100 ChEMBL assays — a studied-ness signal; see Therapeutics for approved-drug status.

SymbolChEMBL assays
RELA422

Pharmacogenomics

Cohort genes with a PharmGKB record: 20; with CPIC/DPWG dosing guidelines: 0.

No cohort gene has a CPIC/DPWG genotype-guided dosing guideline (PharmGKB).

Chemical tractability of cohort targets

19 approved/phased compounds have measured bioactivity against a cohort gene (and aren’t yet in disease-level trials). This is a research / tractability signal, NOT a therapeutic recommendation — a bioactivity row often reflects off-target or screening binding (e.g. promiscuous kinase inhibitors against a cohort kinase), implying no disease mechanism.

CompoundMax phaseCohort target (bioactivity)
INDOPROFEN4RELA
VAMOROLONE4RELA
BORTEZOMIB4RELA
DEXAMETHASONE4RELA
SULFASALAZINE4RELA
GEFITINIB4RELA
CURCUMIN3RELA
RESVERATROL3RELA
IXAZOMIB3RELA
WITHANOLIDE D3RELA
TRIPTOLIDE3RELA
ALADORIAN2RYR2
PIRMAGREL2PTGIS
FRENTIZOLE2RELA
LAPACHONE2RELA
SANGUINARIUM2RELA
URSOLIC ACID2RELA
AS-6028681RELA
WITHAFERIN A1RELA

Druggability pyramid

Cohort genes binned by druggability tier (high → low):

TierDefinitionGenesSymbols
AApproved (phase 4 drug)1RELA
BPhased (≥1) drug, not yet approved2RYR2, PTGIS
CDruggable family + PDB, no drug4TTBK1, GALNT4, HSPG2, ITGA6
DDruggable family + AlphaFold only, no drug5B4GAT1, SEZ6, GPR153, B3GNT6, PLXNA3
EDifficult family or no structure, no drug8PPP1R13B, PDZRN3, NLRP12, STAC2, FREM2, ARL16, GTF2IRD1, MEST

Undrugged target profiles

17 cohort genes are undrugged. Ranked by ‘starting-point quality’ (assay depth + drugged-partner adjacency).

SymbolChEMBL assaysDrugged partners (top 3)
PPP1R13B0RELA
B4GAT10
SEZ60
PDZRN30
TTBK174
NLRP120
GPR1532
STAC20
B3GNT61
FREM20
ARL160
GALNT40
GTF2IRD10
HSPG22
ITGA63
MEST20
PLXNA30

Clinical trials & evidence

Clinical trials

Clinical trials: 0.