Cornelia de Lange syndrome 1

disease
On this page

Also known as CDLS1Cornelia de Lange syndrome caused by mutation in NIPBLCornelia De Lange syndrome type 1NIPBL Cornelia de Lange syndrome

Summary

Cornelia de Lange syndrome 1 (MONDO:0007387) is a disease caused by NIPBL (GenCC Definitive), with 11 cohort genes. The dominant Reactome pathway is Cohesin Loading onto Chromatin (4 cohort genes).

At a glance

  • Causal gene: NIPBL (GenCC Definitive)
  • Cohort genes: 11
  • ClinVar variants: 1,698

Clinical features

No curated clinical features (Orphanet) for this disease.

Identifiers

Disease identifiers

FieldValue
Canonical nameCornelia de Lange syndrome 1
Mondo IDMONDO:0007387
OMIM122470
DOIDDOID:0080505
SNOMED CT40354009
UMLSC4551851
MedGen1645760
GARD0024555
Is cancer (heuristic)no

Also known as: CDLS1 · Cornelia de Lange syndrome 1 · Cornelia de Lange syndrome caused by mutation in NIPBL · Cornelia De Lange syndrome type 1 · NIPBL Cornelia de Lange syndrome

Data availability: 1,698 ClinVar variants · 3 GenCC gene-disease records.

Disease family

Classification path: disease › human disease › disease by body system or component › syndromic diseaseCornelia de Lange syndromeCornelia de Lange syndrome 1

Related subtypes (5): Cornelia de Lange syndrome 2, Cornelia de Lange syndrome 5, Cornelia de Lange syndrome 3, Cornelia de Lange syndrome 4, Cornelia de Lange syndrome 6

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

600 retrieved; paginated sample, class counts are floors:

208 pathogenic, 134 uncertain significance, 85 likely benign, 67 conflicting classifications of pathogenicity, 63 likely pathogenic, 15 pathogenic/likely pathogenic, 14 benign/likely benign, 14 benign

ClinVarVariant (HGVS)GeneClassificationReview
1459695NC_000005.9:g.(?36970958)(37371079_?)delCPLANE1Pathogeniccriteria provided, single submitter
180201NM_001197104.2(KMT2A):c.2233C>T (p.Arg745Ter)KMT2APathogeniccriteria provided, multiple submitters, no conflicts
1000617NM_133433.4(NIPBL):c.7199G>C (p.Arg2400Pro)NIPBLPathogeniccriteria provided, single submitter
1066128NM_133433.4(NIPBL):c.5808+2T>CNIPBLPathogeniccriteria provided, single submitter
1070037NM_133433.4(NIPBL):c.7854del (p.Tyr2618_Leu2619insTer)NIPBLPathogeniccriteria provided, single submitter
1071194NM_133433.4(NIPBL):c.5269del (p.Val1757fs)NIPBLPathogeniccriteria provided, single submitter
1072674NM_133433.4(NIPBL):c.4675_4750dup (p.Leu1584delinsGlnThrThrValTer)NIPBLPathogeniccriteria provided, single submitter
1074354NM_133433.4(NIPBL):c.4643+1G>ANIPBLPathogeniccriteria provided, single submitter
1075044NM_133433.4(NIPBL):c.2837dup (p.Leu946fs)NIPBLPathogeniccriteria provided, single submitter
1075076NC_000005.9:g.(?36953799)(37064994_?)delNIPBLPathogeniccriteria provided, single submitter
1075092NM_133433.4(NIPBL):c.7013del (p.Ala2338fs)NIPBLPathogeniccriteria provided, single submitter
1075290NM_133433.4(NIPBL):c.1942del (p.Thr648fs)NIPBLPathogeniccriteria provided, single submitter
1076020NM_133433.4(NIPBL):c.4335T>G (p.Tyr1445Ter)NIPBLPathogeniccriteria provided, single submitter
1076024NM_133433.4(NIPBL):c.8326del (p.Ile2776fs)NIPBLPathogeniccriteria provided, single submitter
1076298NM_133433.4(NIPBL):c.2207del (p.Pro736fs)NIPBLPathogeniccriteria provided, multiple submitters, no conflicts
1195876NM_133433.4(NIPBL):c.-467C>TNIPBLPathogenic/Likely pathogenicno assertion criteria provided
1319902NM_133433.4(NIPBL):c.5808+5G>ANIPBLPathogenic/Likely pathogenicno assertion criteria provided
1320125NM_133433.4(NIPBL):c.10dup (p.Asp4fs)NIPBLPathogeniccriteria provided, single submitter
1328515NM_133433.4(NIPBL):c.7948dup (p.Ile2650fs)NIPBLPathogeniccriteria provided, single submitter
1351385NM_133433.4(NIPBL):c.3178del (p.Glu1060fs)NIPBLPathogeniccriteria provided, single submitter
1359106NM_133433.4(NIPBL):c.6359T>G (p.Leu2120Ter)NIPBLPathogeniccriteria provided, single submitter
1366117NM_133433.4(NIPBL):c.4455_4456dup (p.Tyr1486fs)NIPBLPathogeniccriteria provided, single submitter
1379181NM_133433.4(NIPBL):c.1786_1790del (p.Asn595_His596insTer)NIPBLPathogeniccriteria provided, single submitter
1382932NM_133433.4(NIPBL):c.3040del (p.Gln1014fs)NIPBLPathogeniccriteria provided, single submitter
1383143NM_133433.4(NIPBL):c.3100A>T (p.Lys1034Ter)NIPBLPathogeniccriteria provided, single submitter
1390979NM_133433.4(NIPBL):c.4502_4503dup (p.Val1502fs)NIPBLPathogeniccriteria provided, single submitter
1395044NM_133433.4(NIPBL):c.373C>T (p.Gln125Ter)NIPBLPathogeniccriteria provided, single submitter
1399376NM_133433.4(NIPBL):c.6080_6083dup (p.Gln2028fs)NIPBLPathogeniccriteria provided, single submitter
1402649NM_133433.4(NIPBL):c.8326dup (p.Ile2776fs)NIPBLPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
1406195NM_133433.4(NIPBL):c.5725dup (p.Thr1909fs)NIPBLPathogeniccriteria provided, single submitter

Genes & proteins

Mendelian disease overlap and somatic drivers

GenCC: 4 · Orphanet: 27 · OMIM-shared: 0 · Dual-evidence (GWAS+Mendelian): 0

GenCC gene–disease validity (cohort genes)

the Disease column is the GenCC-asserted condition — a cohort gene’s strongest validity may be for a related predisposition syndrome.

GeneClassificationInheritanceDiseaseRecords
NIPBLDefinitiveAutosomal dominantCornelia de Lange syndrome 14

Orphanet rare-disease linkage (cohort genes)

GeneOrphanet IDRare disease
NIPBLOrphanet:199Cornelia de Lange syndrome
NIPBLOrphanet:3298025p13 microduplication syndrome
SMC1AOrphanet:199Cornelia de Lange syndrome
SMC1AOrphanet:220386Semilobar holoprosencephaly
SMC1AOrphanet:3095Atypical Rett syndrome
SMC1AOrphanet:708203Intellectual disability-small hands and feet-drug-resistant epilepsy syndrome
TAF6Orphanet:694946Alazami-Yuan syndrome
HDAC8Orphanet:199Cornelia de Lange syndrome
HDAC8Orphanet:3459Wilson-Turner syndrome
BRD4Orphanet:199Cornelia de Lange syndrome
BRD4Orphanet:443167NUT midline carcinoma
ANTXR1Orphanet:2067GAPO syndrome
SMC3Orphanet:199Cornelia de Lange syndrome
CPLANE1Orphanet:2754Orofaciodigital syndrome type 6
CPLANE1Orphanet:475Isolated Joubert syndrome
CPLANE1Orphanet:65684Monomelic amyotrophy
KMT2AOrphanet:319182Wiedemann-Steiner syndrome
KMT2AOrphanet:402017Acute myeloid leukemia with t(9;11)(p22;q23)
KMT2AOrphanet:585918B-lymphoblastic leukemia/lymphoma with t(v;11q23.3)
KMT2AOrphanet:589534Mixed phenotype acute leukemia with t(9;22)(q34.1;q11.2)
KMT2AOrphanet:589595Mixed phenotype acute leukemia with t(v;11q23.3)
KMT2AOrphanet:98831Acute myeloid leukemia with 11q23 abnormalities
KMT2AOrphanet:98835Acute undifferentiated leukemia
ATROrphanet:313846Familial cutaneous telangiectasia and oropharyngeal cancer predisposition syndrome
ATROrphanet:808Seckel syndrome
RAD21Orphanet:199Cornelia de Lange syndrome
RAD21Orphanet:502Trichorhinophalangeal syndrome type 2

Cohort genes → proteins

11 cohort genes, 11 distinct canonical proteins.

Evidence partition

SubsetGenes
multi_evidence11

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
NIPBLHGNC:28862ENSG00000164190Q6KC79Nipped-B-like proteingencc,clinvar
SMC1AHGNC:11111ENSG00000072501Q14683Structural maintenance of chromosomes protein 1Aclinvar
TAF6HGNC:11540ENSG00000106290P49848Transcription initiation factor TFIID subunit 6clinvar
HDAC8HGNC:13315ENSG00000147099Q9BY41Histone deacetylase 8clinvar
BRD4HGNC:13575ENSG00000141867O60885Bromodomain-containing protein 4clinvar
ANTXR1HGNC:21014ENSG00000169604Q9H6X2Anthrax toxin receptor 1clinvar
SMC3HGNC:2468ENSG00000108055Q9UQE7Structural maintenance of chromosomes protein 3clinvar
CPLANE1HGNC:25801ENSG00000197603Q9H799Ciliogenesis and planar polarity effector 1clinvar
KMT2AHGNC:7132ENSG00000118058Q03164Histone-lysine N-methyltransferase 2Aclinvar
ATRHGNC:882ENSG00000175054Q13535Serine/threonine-protein kinase ATRclinvar
RAD21HGNC:9811ENSG00000164754O60216Double-strand-break repair protein rad21 homologclinvar

Cohort function summary

Lead sentence per gene, UniProt-curated.

SymbolProtein nameFunction (lead sentence)
NIPBLNipped-B-like proteinPlays an important role in the loading of the cohesin complex on to DNA.
SMC1AStructural maintenance of chromosomes protein 1AInvolved in chromosome cohesion during cell cycle and in DNA repair.
TAF6Transcription initiation factor TFIID subunit 6The TFIID basal transcription factor complex plays a major role in the initiation of RNA polymerase II (Pol II)-dependent transcription.
HDAC8Histone deacetylase 8Histone deacetylase that catalyzes the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4).
BRD4Bromodomain-containing protein 4Chromatin reader protein that recognizes and binds acetylated histones and plays a key role in transmission of epigenetic memory across cell divisions and transcription regulation.
ANTXR1Anthrax toxin receptor 1Plays a role in cell attachment and migration.
SMC3Structural maintenance of chromosomes protein 3Central component of cohesin, a complex required for chromosome cohesion during the cell cycle.
CPLANE1Ciliogenesis and planar polarity effector 1Involved in ciliogenesis.
KMT2AHistone-lysine N-methyltransferase 2AHistone methyltransferase that plays an essential role in early development and hematopoiesis.
ATRSerine/threonine-protein kinase ATRSerine/threonine protein kinase which activates checkpoint signaling upon genotoxic stresses such as ionizing radiation (IR), ultraviolet light (UV), or DNA replication stalling, thereby acting as a DNA damage sensor.
RAD21Double-strand-break repair protein rad21 homologAs a member of the cohesin complex, involved in sister chromatid cohesion from the time of DNA replication in S phase to their segregation in mitosis, a function that is essential for proper chromosome segregation, post-replicative DNA rep…

Protein-family classification

Druggable: 2 · Difficult: 2 · Unknown: 7 · Druggable fraction: 0.18

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
Kinase12.5×0.758
Scaffold/PPI11.6×0.758
Other/Unknown71.1×0.758
Enzyme (other)11.1×0.758
Transcription factor10.8×0.758

Per-gene assignment

SymbolFamilyDruggable?ECInterPro (top 3)
NIPBLOther/UnknownnoARM-like, ARM-type_fold, Nipped-B_C
SMC1AOther/UnknownnoRecF/RecN/SMC_N, SMC_hinge, SMC
TAF6Other/UnknownnoTAF_TATA-bd_Histone-like_dom, Histone-fold, TAF6_C
HDAC8Enzyme (other)yes3.5.1.98HDACs, HDAC_I/II, Ureohydrolase_dom_sf
BRD4Other/UnknownnoBromodomain, Bromodomain_CS, NET_dom
ANTXR1Other/UnknownnoVWF_A, Anthrax_toxin_rcpt_C, Anthrax_toxin_rcpt_extracel
SMC3Other/UnknownnoRecF/RecN/SMC_N, SMC_hinge, SMC
CPLANE1Scaffold/PPInoCPLANE1, WD40_repeat_dom_sf
KMT2ATranscription factornoSET_dom, Bromodomain, Znf_PHD
ATRKinaseyes2.7.11.1PI3/4_kinase_cat_dom, PIK-rel_kinase_FAT, FATC_dom
RAD21Other/UnknownnoRad21/Rec8_C_eu, Rad21_Rec8_N, ScpA-like_C

Expression context

Cohort genes with no expression data: 0.

11 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)11
unknown0

Top tissues across cohort

TissueCohort genes
sural nerve4
colonic epithelium3
ventricular zone3
calcaneal tendon2
male germ line stem cell (sensu Vertebrata) in testis2
stromal cell of endometrium2
adrenal tissue2
tendon of biceps brachii2
embryo1
trabecular bone tissue1
right frontal lobe1
right hemisphere of cerebellum1
left adrenal gland1
buccal mucosa cell1
decidua1
palpebral conjunctiva1
oocyte1
Brodmann (1909) area 231
epithelium of nasopharynx1
ganglionic eminence1

Per-gene tissue summary (top 30)

SymbolBgee breadthFANTOM5 breadthSCXATop tissues
NIPBL288ubiquitousmarkermale germ line stem cell (sensu Vertebrata) in testis, calcaneal tendon, colonic epithelium
SMC1A289ubiquitousmarkersural nerve, trabecular bone tissue, embryo
TAF6290ubiquitousmarkerstromal cell of endometrium, right hemisphere of cerebellum, right frontal lobe
HDAC8244ubiquitousmarkercolonic epithelium, adrenal tissue, left adrenal gland
BRD4300ubiquitousmarkerbuccal mucosa cell, sural nerve, tendon of biceps brachii
ANTXR1270ubiquitousmarkerstromal cell of endometrium, decidua, palpebral conjunctiva
SMC3276ubiquitousmarkertendon of biceps brachii, ventricular zone, oocyte
CPLANE1195ubiquitousmarkersural nerve, calcaneal tendon, male germ line stem cell (sensu Vertebrata) in testis
KMT2A285ubiquitousmarkerventricular zone, colonic epithelium, sural nerve
ATR289ubiquitousmarkerBrodmann (1909) area 23, epithelium of nasopharynx, adrenal tissue
RAD21301ubiquitousmarkerventricular zone, ganglionic eminence, superficial temporal artery

Protein interactions among cohort

Intra-cohort edges: 12.

Hub genes (top 10 by interactor count)

SymbolInteractor count
BRD47,883
SMC1A5,246
SMC35,056
RAD215,042
KMT2A4,314
ATR3,541
NIPBL3,278
HDAC83,087
TAF62,598
ANTXR12,039

Intra-cohort edges

ABSources
BRD4NIPBLstring_interaction
CPLANE1NIPBLstring_interaction
HDAC8NIPBLstring_interaction
HDAC8SMC1Astring_interaction
HDAC8SMC3string_interaction
KMT2ATAF6biogrid_interaction
NIPBLRAD21intact, string_interaction
NIPBLSMC1Aintact, string_interaction
NIPBLSMC3string_interaction
RAD21SMC1Abiogrid_interaction, intact, string_interaction
RAD21SMC3biogrid_interaction, intact, string_interaction
SMC1ASMC3biogrid_interaction, intact, string_interaction

Structural data

PDB: 10 · AlphaFold-only: 1 · No structure: 0

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
BRD4O60885619
KMT2AQ0316460
HDAC8Q9BY4153
RAD21O6021636
TAF6P4984832
SMC1AQ1468318
SMC3Q9UQE712
ATRQ1353510
ANTXR1Q9H6X25
NIPBLQ6KC793

AlphaFold-only cohort genes (top 30 by pLDDT)

SymbolUniProtpLDDT
CPLANE1Q9H799

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 92. Enrichment computed across 11 evidence-associated genes (10 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 10 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

PathwayCohort genesFoldFDRSample cohort genes
Cohesin Loading onto Chromatin4456.8×6e-09NIPBL, SMC1A, SMC3, RAD21
Establishment of Sister Chromatid Cohesion3311.4×4e-06SMC1A, SMC3, RAD21
Meiotic synapsis456.4×1e-05SMC1A, SMC3, ATR, RAD21
Resolution of Sister Chromatid Cohesion434.6×8e-05SMC1A, HDAC8, SMC3, RAD21
Meiosis385.7×9e-05SMC1A, SMC3, ATR
Reproduction357.1×2e-04SMC1A, SMC3, ATR
Separation of Sister Chromatids424.3×2e-04SMC1A, HDAC8, SMC3, RAD21
Mitotic Telophase/Cytokinesis2285.5×2e-04SMC1A, SMC3
SUMOylation of DNA damage response and repair proteins343.9×4e-04SMC1A, SMC3, RAD21
Estrogen-dependent gene expression322.7×0.002SMC1A, SMC3, RAD21
S Phase236.2×0.010SMC1A, SMC3
SUMO E3 ligases SUMOylate target proteins235.7×0.010SMC1A, SMC3
SUMOylation232.6×0.011SMC1A, SMC3
Differentiation of naive CD4+ T cells to T helper 2 cells (Th2 cells)229.3×0.013HDAC8, KMT2A
Cell Cycle310.8×0.013SMC1A, SMC3, ATR
Regulation of TP53 Activity226.6×0.014TAF6, ATR
ESR-mediated signaling225.7×0.014SMC1A, SMC3
Regulation of TP53 Activity through Phosphorylation223.6×0.016TAF6, ATR
Regulation of PD-L1(CD274) transcription221.8×0.017BRD4, KMT2A
Signaling by Nuclear Receptors220.4×0.019SMC1A, SMC3
Mitotic Metaphase and Anaphase219.4×0.019SMC1A, SMC3
Mitotic Anaphase219.4×0.019SMC1A, SMC3
RNA Polymerase II Transcription36.8×0.033TAF6, KMT2A, ATR
Mitotic Prometaphase213.8×0.033SMC1A, SMC3
M Phase213.2×0.035SMC1A, SMC3
Uptake and function of anthrax toxins195.2×0.036ANTXR1
Transcriptional Regulation by TP53212.4×0.036TAF6, ATR
Phosphorylation of CLOCK, acetylation of BMAL1 (ARNTL) at target gene promoters187.8×0.037KMT2A
Diseases of DNA Double-Strand Break Repair181.6×0.037ATR
Defective homologous recombination repair (HRR) due to BRCA2 loss of function181.6×0.037ATR

GO biological processes 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.

GO termCohort genesFoldFDRSample cohort genes
establishment of mitotic sister chromatid cohesion4875.4×5e-10NIPBL, SMC1A, SMC3, RAD21
mitotic sister chromatid cohesion4408.5×9e-09NIPBL, SMC1A, HDAC8, SMC3
establishment of meiotic sister chromatid cohesion31149.0×4e-08SMC1A, SMC3, RAD21
sister chromatid cohesion3208.9×1e-05SMC1A, SMC3, RAD21
replication-born double-strand break repair via sister chromatid exchange2510.7×2e-04NIPBL, RAD21
chromatin looping2218.9×8e-04NIPBL, RAD21
mitotic sister chromatid segregation287.5×0.005NIPBL, SMC1A
mitotic spindle assembly262.5×0.008SMC1A, SMC3
external genitalia morphogenesis11532.0×0.009NIPBL
regulation of developmental growth1766.0×0.009NIPBL
gallbladder development1766.0×0.009NIPBL
response to DNA damage checkpoint signaling1766.0×0.009SMC1A
negative regulation of DNA methylation-dependent heterochromatin formation1766.0×0.009KMT2A
establishment of RNA localization to telomere1766.0×0.009ATR
establishment of protein-containing complex localization to telomere1766.0×0.009ATR
positive regulation of telomerase catalytic core complex assembly1766.0×0.009ATR
somatic stem cell population maintenance245.1×0.009NIPBL, SMC1A
meiotic cell cycle244.4×0.009SMC1A, SMC3
double-strand break repair236.9×0.009ATR, RAD21
DNA repair317.4×0.009SMC1A, SMC3, ATR
DNA damage response314.6×0.009NIPBL, BRD4, ATR
cell division312.6×0.009SMC1A, SMC3, RAD21
nuclear membrane disassembly1510.7×0.011ATR
negative regulation of DNA damage checkpoint1510.7×0.011BRD4
maintenance of mitotic sister chromatid cohesion1383.0×0.013NIPBL
ear morphogenesis1383.0×0.013NIPBL
negative regulation of mitotic metaphase/anaphase transition1383.0×0.013RAD21
eye morphogenesis1383.0×0.013NIPBL
negative regulation of extracellular matrix assembly1383.0×0.013ANTXR1
positive regulation of sister chromatid cohesion1306.4×0.015RAD21

Therapeutics

Drug target analysis

Approved (phase 4): 4 · Phase ≥3: 5 · Phased (≥1): 6 · Undrugged: 5

Druggability breadth: 7 of 11 evidence-associated genes (64%) 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
SMC1ASELUMETINIB
HDAC8CELECOXIB
BRD4ACETAMINOPHEN
KMT2AFLUORESCEIN

Top cohort targets by molecule count

SymbolMoleculesMax phase
KMT2A5354
HDAC8374
BRD4314
ATR83
SMC1A24
SMC312
NIPBL00
TAF600
ANTXR100
CPLANE100

Drugs targeting cohort genes (top 30)

MoleculeMax phaseTargets in cohort
SELUMETINIB4SMC1A
CELECOXIB4HDAC8
PHENYLBUTANOIC ACID4HDAC8
SODIUM PHENYLBUTYRATE4HDAC8
ROMIDEPSIN4BRD4, HDAC8
BELINOSTAT4BRD4, HDAC8
PANOBINOSTAT4BRD4, HDAC8
VORINOSTAT4BRD4, HDAC8
GIVINOSTAT4HDAC8
DAUNORUBICIN4HDAC8, KMT2A
BORTEZOMIB4HDAC8
BENDAMUSTINE4HDAC8
ACETAMINOPHEN4BRD4, KMT2A
FEDRATINIB4BRD4
NITROXOLINE4BRD4
ALPRAZOLAM4BRD4
LENALIDOMIDE4BRD4
NORFLOXACIN4BRD4
FLUORESCEIN4KMT2A
METHYSERGIDE4KMT2A
OXCARBAZEPINE4KMT2A
TRYPAN BLUE FREE ACID4KMT2A
RALOXIFENE HYDROCHLORIDE4KMT2A
IDARUBICIN4KMT2A
DULOXETINE4KMT2A
PYRITHIONE ZINC4KMT2A
HYDROCORTISONE VALERATE4KMT2A
PROMETHAZINE HYDROCHLORIDE4KMT2A
THIORIDAZINE HYDROCHLORIDE4KMT2A
METHYSERGIDE MALEATE4KMT2A

Bioactivity and enzyme data

Enzyme cohort genes (≥1 EC): 2.

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

SymbolAssaysType breakdown
BRD44,603Binding:4569, Functional:30, ADMET:4
HDAC82,631Binding:2599, ADMET:25, Functional:6, Toxicity:1
ATR231Binding:226, Functional:5
KMT2A188Binding:180, Functional:8
SMC1A10Binding:10
SMC37Binding:7
TAF61Binding:1

Cohort enzymes (BRENDA EC)

SymbolEC numbersNames
HDAC83.5.1.98histone deacetylase
ATR2.7.11.1non-specific serine/threonine protein kinase

Cohort genes with high screening signal

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

SymbolChEMBL assays
HDAC82,631
BRD44,603
KMT2A188
ATR231

Pharmacogenomics

Cohort genes with a PharmGKB record: 11; with CPIC/DPWG dosing guidelines: 0.

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

Chemical tractability of cohort targets

30 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)
SELUMETINIB4SMC1A
CELECOXIB4HDAC8
PHENYLBUTANOIC ACID4HDAC8
SODIUM PHENYLBUTYRATE4HDAC8
ROMIDEPSIN4BRD4, HDAC8
BELINOSTAT4BRD4, HDAC8
PANOBINOSTAT4BRD4, HDAC8
VORINOSTAT4BRD4, HDAC8
GIVINOSTAT4HDAC8
DAUNORUBICIN4HDAC8, KMT2A
BORTEZOMIB4HDAC8
BENDAMUSTINE4HDAC8
ACETAMINOPHEN4BRD4, KMT2A
FEDRATINIB4BRD4
NITROXOLINE4BRD4
ALPRAZOLAM4BRD4
LENALIDOMIDE4BRD4
NORFLOXACIN4BRD4
FLUORESCEIN4KMT2A
METHYSERGIDE4KMT2A
OXCARBAZEPINE4KMT2A
TRYPAN BLUE FREE ACID4KMT2A
RALOXIFENE HYDROCHLORIDE4KMT2A
IDARUBICIN4KMT2A
DULOXETINE4KMT2A
PYRITHIONE ZINC4KMT2A
HYDROCORTISONE VALERATE4KMT2A
PROMETHAZINE HYDROCHLORIDE4KMT2A
THIORIDAZINE HYDROCHLORIDE4KMT2A
METHYSERGIDE MALEATE4KMT2A

Druggability pyramid

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

TierDefinitionGenesSymbols
AApproved (phase 4 drug)4SMC1A, HDAC8, BRD4, KMT2A
BPhased (≥1) drug, not yet approved2SMC3, ATR
CDruggable family + PDB, no drug0
DDruggable family + AlphaFold only, no drug0
EDifficult family or no structure, no drug5NIPBL, TAF6, ANTXR1, CPLANE1, RAD21

Undrugged target profiles

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

SymbolChEMBL assaysDrugged partners (top 3)
NIPBL0SMC1A, SMC3
RAD210SMC1A, SMC3
TAF61
ANTXR10
CPLANE10

Clinical trials & evidence

Clinical trials

Clinical trials: 0.