Bethlem myopathy 1A

disease
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Also known as Bethlem myopathy 1BTHLM1

Summary

Bethlem myopathy 1A (MONDO:0024530) is a disease caused by variants in COL6A1, COL6A3, and COL6A2, with 10 cohort genes and 1 clinical trial. The dominant Reactome pathway is Collagen chain trimerization (4 cohort genes).

At a glance

  • Causal genes: COL6A1 (GenCC Definitive), COL6A3 (GenCC Definitive), COL6A2 (GenCC Strong)
  • Cohort genes: 10
  • ClinVar variants: 6,616
  • Clinical trials: 1

Clinical features

No curated clinical features (Orphanet) for this disease.

Identifiers

Disease identifiers

FieldValue
Canonical nameBethlem myopathy 1A
Mondo IDMONDO:0024530
OMIM158810
DOIDDOID:0061198
GARD0025413
Is cancer (heuristic)no

Also known as: Bethlem myopathy 1 · BTHLM1

Data availability: 6,616 ClinVar variants · 8 GenCC gene-disease records · 17 cell lines.

Disease family

Classification path: disease › human disease › disease by body system or component › musculoskeletal system disordermuscle tissue disorderskeletal muscle disordermyopathymuscular dystrophyprogressive muscular dystrophyBethlem myopathyBethlem myopathy 1A

Related subtypes (3): Bethlem myopathy 2, Bethlem myopathy 1B, Bethlem myopathy 1C

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:

237 likely benign, 219 uncertain significance, 77 conflicting classifications of pathogenicity, 36 pathogenic, 14 benign, 7 likely pathogenic, 6 benign/likely benign, 4 pathogenic/likely pathogenic

ClinVarVariant (HGVS)GeneClassificationReview
1013195NM_001848.3(COL6A1):c.887G>A (p.Gly296Glu)COL6A1Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
1072275NM_001848.3(COL6A1):c.823G>A (p.Gly275Arg)COL6A1Pathogeniccriteria provided, single submitter
1073810NM_001848.3(COL6A1):c.1738del (p.Gln580fs)COL6A1Pathogeniccriteria provided, single submitter
1073927NM_001848.3(COL6A1):c.1318G>T (p.Gly440Ter)COL6A1Pathogeniccriteria provided, single submitter
1076562NM_001848.3(COL6A1):c.877G>C (p.Gly293Arg)COL6A1Pathogeniccriteria provided, single submitter
1322138NM_001848.3(COL6A1):c.1056+1G>CCOL6A1Pathogeniccriteria provided, multiple submitters, no conflicts
1322139NM_001848.3(COL6A1):c.2197_2200del (p.Asp733fs)COL6A1Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
1322141NM_001848.3(COL6A1):c.1612-1G>ACOL6A1Pathogeniccriteria provided, multiple submitters, no conflicts
1328167NM_001848.3(COL6A1):c.824G>A (p.Gly275Glu)COL6A1Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
1374571NM_001848.3(COL6A1):c.931G>T (p.Gly311Cys)COL6A1Pathogeniccriteria provided, single submitter
1375454NM_001848.3(COL6A1):c.244C>T (p.Arg82Ter)COL6A1Pathogeniccriteria provided, single submitter
1389428NM_001848.3(COL6A1):c.1867_1868del (p.Ser623fs)COL6A1Pathogeniccriteria provided, single submitter
1060752NM_001849.4(COL6A2):c.2097_2098delinsTA (p.Gly700Ser)COL6A2Pathogeniccriteria provided, single submitter
1061166NM_001849.4(COL6A2):c.2832_2927del (p.Phe944_Ala975del)COL6A2Pathogeniccriteria provided, single submitter
1068195NM_001849.4(COL6A2):c.1817-2A>GCOL6A2Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
1068296NM_001849.4(COL6A2):c.1053+2T>GCOL6A2Pathogeniccriteria provided, single submitter
1070014NC_000021.8:g.(?_47529674)_47540994delCOL6A2Pathogeniccriteria provided, single submitter
1070015NC_000021.8:g.(?_47533070)_47584395delCOL6A2Pathogeniccriteria provided, single submitter
1070123NM_001849.4(COL6A2):c.2023C>T (p.Gln675Ter)COL6A2Pathogeniccriteria provided, single submitter
1070535NM_001849.4(COL6A2):c.999+9_1053+32delinsGCTGAAGGAGGGGTGCAAACGGCCCTTACCCGGTTTCCAGGGTCTCCCTTGCAGCCTTCACOL6A2Pathogeniccriteria provided, single submitter
1071804NM_001849.4(COL6A2):c.955-1G>CCOL6A2Pathogeniccriteria provided, single submitter
1072953NM_001849.4(COL6A2):c.1053+2T>ACOL6A2Pathogeniccriteria provided, single submitter
1073260NM_001849.4(COL6A2):c.998del (p.Lys333fs)COL6A2Pathogeniccriteria provided, single submitter
1073867NM_001849.4(COL6A2):c.954G>C (p.Lys318Asn)COL6A2Pathogeniccriteria provided, single submitter
1073909NM_001849.4(COL6A2):c.2560_2569dup (p.Glu857fs)COL6A2Pathogeniccriteria provided, single submitter
1074374NM_001849.4(COL6A2):c.1075dup (p.Glu359fs)COL6A2Pathogeniccriteria provided, single submitter
1075831NM_001849.4(COL6A2):c.2500_2501del (p.Ile834fs)COL6A2Pathogeniccriteria provided, single submitter
1184919NM_001849.4(COL6A2):c.439C>T (p.Gln147Ter)COL6A2Pathogeniccriteria provided, single submitter
1348005NM_001849.4(COL6A2):c.821G>A (p.Gly274Asp)COL6A2Pathogeniccriteria provided, single submitter
1351958NM_001849.4(COL6A2):c.874G>A (p.Gly292Ser)COL6A2Pathogeniccriteria provided, multiple submitters, no conflicts

Genes & proteins

Mendelian disease overlap and somatic drivers

GenCC: 35 · Orphanet: 42 · 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
COL6A1DefinitiveAutosomal dominantBethlem myopathy 1A9
COL6A3DefinitiveSemidominantBethlem myopathy 1A15
COL6A2StrongAutosomal dominantBethlem myopathy 1A11

Orphanet rare-disease linkage (cohort genes)

GeneOrphanet IDRare disease
COL6A1Orphanet:610Bethlem muscular dystrophy
COL6A1Orphanet:646113Intermediate collagen VI-related muscular dystrophy
COL6A1Orphanet:75840Ullrich congenital muscular dystrophy
COL6A2Orphanet:289380Myosclerosis
COL6A2Orphanet:610Bethlem muscular dystrophy
COL6A2Orphanet:646113Intermediate collagen VI-related muscular dystrophy
COL6A2Orphanet:75840Ullrich congenital muscular dystrophy
COL6A3Orphanet:464440Primary dystonia, DYT27 type
COL6A3Orphanet:610Bethlem muscular dystrophy
COL6A3Orphanet:646113Intermediate collagen VI-related muscular dystrophy
COL6A3Orphanet:75840Ullrich congenital muscular dystrophy
SLC7A9Orphanet:93613Cystinuria type B
CLCN5Orphanet:93622Dent disease type 1
COL12A1Orphanet:536516Myopathic Ehlers-Danlos syndrome
COL12A1Orphanet:610Bethlem muscular dystrophy
COL12A1Orphanet:75840Ullrich congenital muscular dystrophy
DMPKOrphanet:589821Congenital-onset Steinert myotonic dystrophy
DMPKOrphanet:589824Childhood-onset Steinert myotonic dystrophy
DMPKOrphanet:589827Juvenile-onset Steinert myotonic dystrophy
DMPKOrphanet:589830Adult-onset Steinert myotonic dystrophy
DMPKOrphanet:589833Late-onset Steinert myotonic dystrophy
LMNAOrphanet:154Familial isolated dilated cardiomyopathy
LMNAOrphanet:157973Congenital muscular dystrophy due to LMNA mutation
LMNAOrphanet:1662Restrictive dermopathy
LMNAOrphanet:168796Heart-hand syndrome, Slovenian type
LMNAOrphanet:2229Dilated cardiomyopathy-hypergonadotropic hypogonadism syndrome
LMNAOrphanet:2348Familial partial lipodystrophy, Dunnigan type
LMNAOrphanet:280365Autosomal semi-dominant severe lipodystrophic laminopathy
LMNAOrphanet:293888Inherited isolated arrhythmogenic cardiomyopathy, dominant-left variant
LMNAOrphanet:293899Inherited isolated arrhythmogenic ventricular dysplasia, biventricular variant
LMNAOrphanet:293910Inherited isolated arrhythmogenic cardiomyopathy, dominant-right variant
LMNAOrphanet:300751Familial dilated cardiomyopathy with conduction defect due to LMNA mutation
LMNAOrphanet:363618LMNA-related cardiocutaneous progeria syndrome
LMNAOrphanet:54260Left ventricular noncompaction
LMNAOrphanet:675396Epithelioid hemangioma
LMNAOrphanet:740Hutchinson-Gilford progeria syndrome
LMNAOrphanet:79084Familial partial lipodystrophy, Köbberling type
LMNAOrphanet:79474Atypical Werner syndrome
LMNAOrphanet:90153Mandibuloacral dysplasia with type A lipodystrophy
LMNAOrphanet:98853Autosomal dominant Emery-Dreifuss muscular dystrophy
LMNAOrphanet:98855Autosomal recessive Emery-Dreifuss muscular dystrophy
LMNAOrphanet:98856Charcot-Marie-Tooth disease type 2B1

Cohort genes → proteins

10 cohort genes, 10 distinct canonical proteins.

Evidence partition

SubsetGenes
multi_evidence10

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
COL6A1HGNC:2211ENSG00000142156P12109Collagen alpha-1(VI) chaingencc,clinvar
COL6A2HGNC:2212ENSG00000142173P12110Collagen alpha-2(VI) chaingencc,clinvar
COL6A3HGNC:2213ENSG00000163359P12111Collagen alpha-3(VI) chaingencc,clinvar
SLC7A9HGNC:11067ENSG00000021488P82251b(0,+)-type amino acid transporter 1clinvar
CLCN5HGNC:2023ENSG00000171365P51795H(+)/Cl(-) exchange transporter 5clinvar
ANKMY1HGNC:20987ENSG00000144504Q9P2S6Ankyrin repeat and MYND domain-containing protein 1clinvar
COL12A1HGNC:2188ENSG00000111799Q99715Collagen alpha-1(XII) chainclinvar
ACKR3HGNC:23692ENSG00000144476P25106Atypical chemokine receptor 3clinvar
DMPKHGNC:2933ENSG00000104936Q09013Myotonin-protein kinaseclinvar
LMNAHGNC:6636ENSG00000160789P02545Prelamin-A/Cclinvar

Cohort function summary

Lead sentence per gene, UniProt-curated.

SymbolProtein nameFunction (lead sentence)
COL6A1Collagen alpha-1(VI) chainCollagen VI acts as a cell-binding protein.
COL6A2Collagen alpha-2(VI) chainCollagen VI acts as a cell-binding protein.
COL6A3Collagen alpha-3(VI) chainCollagen VI acts as a cell-binding protein.
SLC7A9b(0,+)-type amino acid transporter 1Associates with SLC3A1 to form a functional transporter complex that mediates the electrogenic exchange between cationic amino acids and neutral amino acids, with a stoichiometry of 1:1.
CLCN5H(+)/Cl(-) exchange transporter 5Proton-coupled chloride transporter.
COL12A1Collagen alpha-1(XII) chainType XII collagen interacts with type I collagen-containing fibrils, the COL1 domain could be associated with the surface of the fibrils, and the COL2 and NC3 domains may be localized in the perifibrillar matrix.
ACKR3Atypical chemokine receptor 3Atypical chemokine receptor that controls chemokine levels and localization via high-affinity chemokine binding that is uncoupled from classic ligand-driven signal transduction cascades, resulting instead in chemokine sequestration, degrad…
DMPKMyotonin-protein kinaseNon-receptor serine/threonine protein kinase which is necessary for the maintenance of skeletal muscle structure and function.
LMNAPrelamin-A/CLamins are intermediate filament proteins that assemble into a filamentous meshwork, and which constitute the major components of the nuclear lamina, a fibrous layer on the nucleoplasmic side of the inner nuclear membrane.

Protein-family classification

Druggable: 5 · Difficult: 1 · Unknown: 4 · Druggable fraction: 0.5

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
Antibody/Immunoglobulin25.8×0.264
Transporter17.8×0.364
Kinase12.8×0.521
GPCR12.4×0.521
Transcription factor10.8×0.870
Other/Unknown40.7×0.907

Per-gene assignment

SymbolFamilyDruggable?ECInterPro (top 3)
COL6A1Other/UnknownnoVWF_A, Collagen, vWFA_dom_sf
COL6A2Other/UnknownnoVWF_A, Collagen, vWFA_dom_sf
COL6A3Antibody/ImmunoglobulinyesVWF_A, Kunitz_BPTI, FN3_dom
SLC7A9TransporteryesAA/rel_permease1, AminoAcid_Transporter
CLCN5Other/UnknownnoCBS_dom, ClC, Cl_channel-5
ANKMY1Transcription factornoAnkyrin_rpt, Znf_MYND, MORN
COL12A1Antibody/ImmunoglobulinyesVWF_A, FN3_dom, Collagen
ACKR3GPCRyesGPCR_Rhodpsn, ACKR3, GPCR_Rhodpsn_7TM
DMPKKinaseyes2.7.11.1Prot_kinase_dom, AGC-kinase_C, Ser/Thr_kinase_AS
LMNAOther/UnknownnoLamin_tail_dom, IF_conserved, Lamin_tail_dom_sf

Expression context

Cohort genes with no expression data: 0.

10 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)10
unknown0

Top tissues across cohort

TissueCohort genes
stromal cell of endometrium3
tendon of biceps brachii2
right coronary artery2
secondary oocyte2
mucosa of stomach2
lower esophagus muscularis layer1
descending thoracic aorta1
skin of hip1
visceral pleura1
ileal mucosa1
jejunal mucosa1
corpus epididymis1
renal medulla1
left testis1
right testis1
right uterine tube1
calcaneal tendon1
cartilage tissue1
tibia1
synovial joint1

Per-gene tissue summary (top 30)

SymbolBgee breadthFANTOM5 breadthSCXATop tissues
COL6A1291ubiquitousmarkerstromal cell of endometrium, tendon of biceps brachii, lower esophagus muscularis layer
COL6A2263ubiquitousmarkerstromal cell of endometrium, right coronary artery, descending thoracic aorta
COL6A3264broadmarkerstromal cell of endometrium, visceral pleura, skin of hip
SLC7A9173tissue_specificmarkerileal mucosa, secondary oocyte, jejunal mucosa
CLCN5218ubiquitousmarkerrenal medulla, secondary oocyte, corpus epididymis
ANKMY1191ubiquitousmarkerright uterine tube, right testis, left testis
COL12A1240ubiquitousmarkertibia, calcaneal tendon, cartilage tissue
ACKR3278ubiquitousmarkersynovial joint, vena cava, tendon of biceps brachii
DMPK246broadmarkerapex of heart, right coronary artery, mucosa of stomach
LMNA295ubiquitousmarkernipple, mucosa of stomach, skin of abdomen

Protein interactions among cohort

Intra-cohort edges: 5.

Hub genes (top 10 by interactor count)

SymbolInteractor count
LMNA7,173
COL6A13,049
COL6A22,786
DMPK2,467
COL6A32,267
COL12A12,219
CLCN51,345
ACKR31,142
SLC7A91,106
ANKMY1495

Intra-cohort edges

ABSources
COL12A1COL6A1string_interaction
COL12A1COL6A3string_interaction
COL6A1COL6A2string_interaction
COL6A1COL6A3string_interaction
COL6A2COL6A3string_interaction

Structural data

PDB: 9 · AlphaFold-only: 1 · No structure: 0

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
LMNAP0254528
ACKR3P2510614
COL6A3P121116
SLC7A9P822514
CLCN5P517952
DMPKQ090132
COL6A1P121091
COL6A2P121101
COL12A1Q997151

AlphaFold-only cohort genes (top 30 by pLDDT)

SymbolUniProtpLDDT
ANKMY1Q9P2S678.09

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 44. Enrichment computed across 10 evidence-associated genes (9 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 9 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

PathwayCohort genesFoldFDRSample cohort genes
Collagen chain trimerization4115.3×1e-06COL6A1, COL6A2, COL6A3, COL12A1
Assembly of collagen fibrils and other multimeric structures489.0×1e-06COL6A1, COL6A2, COL6A3, COL12A1
Collagen degradation478.1×1e-06COL6A1, COL6A2, COL6A3, COL12A1
Collagen biosynthesis and modifying enzymes475.8×1e-06COL6A1, COL6A2, COL6A3, COL12A1
Signaling by PDGF384.6×4e-05COL6A1, COL6A2, COL6A3
NCAM1 interactions382.8×4e-05COL6A1, COL6A2, COL6A3
ECM proteoglycans350.1×1e-04COL6A1, COL6A2, COL6A3
Integrin cell surface interactions344.8×2e-04COL6A1, COL6A2, COL6A3
Defective SLC3A1 causes cystinuria (CSNU)1634.4×0.007SLC7A9
Defective amino acid transport by SLC7A9 causes cystinuria (CSNU)1634.4×0.007SLC7A9
Breakdown of the nuclear lamina1423.0×0.009LMNA
Depolymerization of the Nuclear Lamina184.6×0.043LMNA
Initiation of Nuclear Envelope (NE) Reformation166.8×0.050LMNA
IRE1alpha activates chaperones157.7×0.050LMNA
Deregulated CDK5 triggers multiple neurodegenerative pathways in Alzheimer’s disease models157.7×0.050LMNA
Nuclear Envelope Breakdown150.8×0.053LMNA
Basigin interactions148.8×0.053SLC7A9
Unfolded Protein Response (UPR)139.6×0.061LMNA
Amino acid transport across the plasma membrane133.4×0.068SLC7A9
Oncogenic MAPK signaling127.6×0.079LMNA
XBP1(S) activates chaperone genes123.9×0.083LMNA
Ion homeostasis122.7×0.083DMPK
SLC transporter disorders122.7×0.083SLC7A9
Chemokine receptors bind chemokines120.8×0.086ACKR3
Signaling by BRAF and RAF1 fusions118.9×0.091LMNA
Meiotic synapsis115.7×0.101LMNA
Disorders of transmembrane transporters115.5×0.101SLC7A9
Stimuli-sensing channels115.1×0.101CLCN5
R-HSA-425393114.4×0.102SLC7A9
Cell surface interactions at the vascular wall110.6×0.133SLC7A9

GO biological processes by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 9 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

GO termCohort genesFoldFDRSample cohort genes
muscle cell apoptotic process21872.4×3e-05COL6A1, DMPK
response to UV3122.1×7e-05COL6A1, COL6A2, COL6A3
cell adhesion520.8×7e-05COL6A1, COL6A2, COL6A3, COL12A1, ACKR3
phosphatidylinositol 3-kinase/protein kinase B signal transduction370.2×3e-04COL6A1, COL6A2, COL6A3
neuron apoptotic process361.7×3e-04COL6A1, COL6A2, COL6A3
nuclear envelope organization2220.3×7e-04DMPK, LMNA
endodermal cell differentiation2110.1×0.003COL6A1, COL12A1
regulation of excitatory postsynaptic membrane potential involved in skeletal muscle contraction11872.4×0.007DMPK
response to polyamine macromolecule11872.4×0.007COL6A1
response to glucose256.7×0.007COL6A2, COL6A3
collagen fibril organization249.9×0.008COL6A1, COL12A1
regulation of skeletal muscle contraction by calcium ion signaling1936.2×0.010DMPK
oculomotor nerve development1936.2×0.010ACKR3
response to decreased oxygen levels1936.2×0.010COL6A1
limb joint morphogenesis1624.1×0.010COL6A1
fat cell proliferation1624.1×0.010COL6A1
multicellular organismal locomotion1624.1×0.010COL6A1
regulation of collagen fibril organization1624.1×0.010COL6A1
DNA double-strand break attachment to nuclear envelope1624.1×0.010LMNA
muscle organ development237.1×0.010COL6A3, LMNA
muscle system process1468.1×0.011COL6A1
establishment or maintenance of microtubule cytoskeleton polarity1468.1×0.011LMNA
sensory perception of mechanical stimulus1468.1×0.011COL6A1
regulation of synapse structural plasticity1468.1×0.011DMPK
positive regulation of mesenchymal stem cell migration1468.1×0.011ACKR3
regulation of myotube differentiation1374.5×0.012DMPK
nuclear pore localization1374.5×0.012LMNA
response to bleomycin1374.5×0.012COL6A1
L-cystine transport1312.1×0.013SLC7A9
apoptotic nuclear changes1312.1×0.013COL6A1

Therapeutics

Drug target analysis

Approved (phase 4): 2 · Phase ≥3: 2 · Phased (≥1): 2 · Undrugged: 8

Druggability breadth: 6 of 10 evidence-associated genes (60%) 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
DMPKFEDRATINIB
LMNABEPRIDIL

Top cohort targets by molecule count

SymbolMoleculesMax phase
LMNA8234
DMPK204
COL6A100
COL6A200
COL6A300
SLC7A900
CLCN500
ANKMY100
COL12A100
ACKR300

Drugs targeting cohort genes (top 30)

MoleculeMax phaseTargets in cohort
FEDRATINIB4DMPK
RUXOLITINIB4DMPK
TOFACITINIB CITRATE4DMPK
TOFACITINIB4DMPK
BOSUTINIB4DMPK
DASATINIB4DMPK
ERLOTINIB4DMPK, LMNA
CRIZOTINIB4DMPK
MIDOSTAURIN4DMPK
GEFITINIB4DMPK
BEPRIDIL4LMNA
PHENYLBUTAZONE4LMNA
CEFOTAXIME SODIUM4LMNA
DIENESTROL4LMNA
IFOSFAMIDE4LMNA
PROGESTERONE4LMNA
CLOTRIMAZOLE4LMNA
DAPSONE4LMNA
AMINOCAPROIC ACID4LMNA
FLUCONAZOLE4LMNA
COLCHICINE4LMNA
NABUMETONE4LMNA
OXAPROZIN4LMNA
BUMETANIDE4LMNA
GLIPIZIDE4LMNA
BROMFENAC4LMNA
ROPIVACAINE4LMNA
TIZANIDINE4LMNA
METAXALONE4LMNA
CARBAMAZEPINE4LMNA

Bioactivity and enzyme data

Enzyme cohort genes (≥1 EC): 1.

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

SymbolAssaysType breakdown
DMPK210Binding:210
ACKR3102Binding:77, Functional:24, ADMET:1
LMNA12Binding:9, Functional:3

Cohort enzymes (BRENDA EC)

SymbolEC numbersNames
DMPK2.7.11.1non-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
ACKR3102
DMPK210

Pharmacogenomics

Cohort genes with a PharmGKB record: 10; 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)
FEDRATINIB4DMPK
RUXOLITINIB4DMPK
TOFACITINIB CITRATE4DMPK
TOFACITINIB4DMPK
BOSUTINIB4DMPK
DASATINIB4DMPK
ERLOTINIB4DMPK, LMNA
CRIZOTINIB4DMPK
MIDOSTAURIN4DMPK
GEFITINIB4DMPK
BEPRIDIL4LMNA
PHENYLBUTAZONE4LMNA
CEFOTAXIME SODIUM4LMNA
DIENESTROL4LMNA
IFOSFAMIDE4LMNA
PROGESTERONE4LMNA
CLOTRIMAZOLE4LMNA
DAPSONE4LMNA
AMINOCAPROIC ACID4LMNA
FLUCONAZOLE4LMNA
COLCHICINE4LMNA
NABUMETONE4LMNA
OXAPROZIN4LMNA
BUMETANIDE4LMNA
GLIPIZIDE4LMNA
BROMFENAC4LMNA
ROPIVACAINE4LMNA
TIZANIDINE4LMNA
METAXALONE4LMNA
CARBAMAZEPINE4LMNA

Druggability pyramid

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

TierDefinitionGenesSymbols
AApproved (phase 4 drug)2DMPK, LMNA
BPhased (≥1) drug, not yet approved0
CDruggable family + PDB, no drug4COL6A3, SLC7A9, COL12A1, ACKR3
DDruggable family + AlphaFold only, no drug0
EDifficult family or no structure, no drug4COL6A1, COL6A2, CLCN5, ANKMY1

Undrugged target profiles

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

SymbolChEMBL assaysDrugged partners (top 3)
ACKR3102
COL6A10
COL6A20
COL6A30
SLC7A90
CLCN50
ANKMY10
COL12A10

Clinical trials & evidence

Clinical trials

Clinical trials: 1.

Phase distribution (across all retrieved trials)

PhaseTrials
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04020159Not specifiedUNKNOWNGlobal Registry for COL6-related Dystrophies