Fraser syndrome 3

disease
On this page

Also known as FRASRS3

Summary

Fraser syndrome 3 (MONDO:0054739) is a disease caused by GRIP1 (GenCC Strong), with 17 cohort genes.

At a glance

  • Causal gene: GRIP1 (GenCC Strong)
  • Cohort genes: 17
  • ClinVar variants: 221

Clinical features

No curated clinical features (Orphanet) for this disease.

Identifiers

Disease identifiers

FieldValue
Canonical nameFraser syndrome 3
Mondo IDMONDO:0054739
OMIM617667
DOIDDOID:0111406
UMLSC4540040
MedGen1621907
GARD0025964
Is cancer (heuristic)no

Also known as: Fraser syndrome 3 · FRASRS3

Data availability: 221 ClinVar variants · 3 GenCC gene-disease records.

Disease family

Classification path: disease › human disease › disease by body system or component › syndromic diseaseFraser syndromeFraser syndrome 3

Related subtypes (2): Fraser syndrome 1, Fraser syndrome 2

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

221 retrieved; paginated sample, class counts are floors:

155 uncertain significance, 23 conflicting classifications of pathogenicity, 12 likely benign, 10 benign, 9 benign/likely benign, 8 likely pathogenic, 3 pathogenic, 1 pathogenic/likely pathogenic

ClinVarVariant (HGVS)GeneClassificationReview
36970NM_001366722.1(GRIP1):c.2269+1G>CGRIP1Pathogenicno assertion criteria provided
36971NM_001366722.1(GRIP1):c.1337_1340del (p.Lys446fs)GRIP1Pathogenicno assertion criteria provided
620314NM_001366722.1(GRIP1):c.30T>A (p.Cys10Ter)GRIP1Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
974698NM_001366722.1(GRIP1):c.1930C>T (p.Gln644Ter)GRIP1Pathogenicno assertion criteria provided
2802784NM_001366722.1(GRIP1):c.1199-2delGRIP1Likely pathogeniccriteria provided, multiple submitters, no conflicts
3575200NM_021150.4(GRIP1):c.1618_1619insTATATCTCCATTATTACAGCACCATGRIP1Likely pathogeniccriteria provided, single submitter
3575202NM_001366722.1(GRIP1):c.1688-1G>CGRIP1Likely pathogeniccriteria provided, single submitter
3575209NM_001366722.1(GRIP1):c.1285del (p.Leu429fs)GRIP1Likely pathogeniccriteria provided, single submitter
3575210NM_001366722.1(GRIP1):c.1279C>T (p.Arg427Ter)GRIP1Likely pathogeniccriteria provided, single submitter
3575215NM_001366722.1(GRIP1):c.1199-2A>GGRIP1Likely pathogeniccriteria provided, single submitter
3575234NM_001366722.1(GRIP1):c.206C>A (p.Ser69Ter)GRIP1Likely pathogeniccriteria provided, single submitter
3575236NM_001366722.1(GRIP1):c.116_117del (p.Val39fs)GRIP1Likely pathogeniccriteria provided, single submitter
974703NM_000049.4(ASPA):c.806C>T (p.Thr269Met)ASPAConflicting classifications of pathogenicitycriteria provided, conflicting classifications
1698650NM_001366722.1(GRIP1):c.386T>C (p.Val129Ala)GRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
227419NM_001366722.1(GRIP1):c.2381T>G (p.Met794Arg)GRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
2540277NM_001366722.1(GRIP1):c.2393C>T (p.Thr798Met)GRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
265191NM_001366722.1(GRIP1):c.1756A>C (p.Ile586Leu)GRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
2794528NM_001366722.1(GRIP1):c.1710A>T (p.Gly570=)GRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
2838552NM_001366722.1(GRIP1):c.419-11C>TGRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
2978523NM_001366722.1(GRIP1):c.43C>T (p.Arg15Ter)GRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
310298NM_001366722.1(GRIP1):c.3048T>C (p.Phe1016=)GRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
310301NM_001366722.1(GRIP1):c.2793G>A (p.Ser931=)GRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
310311NM_001366722.1(GRIP1):c.872+7A>GGRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
310313NM_001366722.1(GRIP1):c.345C>T (p.Asp115=)GRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
310315NM_001366722.1(GRIP1):c.240A>G (p.Val80=)GRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
381678NM_001366722.1(GRIP1):c.1645A>G (p.Ile549Val)GRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
402210NM_001366722.1(GRIP1):c.160G>A (p.Val54Ile)GRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
754761NM_001366722.1(GRIP1):c.1428G>A (p.Thr476=)GRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
755754NM_001366722.1(GRIP1):c.1688-6T>CGRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
881655NM_001366722.1(GRIP1):c.3223G>A (p.Gly1075Arg)GRIP1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications

Genes & proteins

Mendelian disease overlap and somatic drivers

GenCC: 8 · Orphanet: 22 · 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
GRIP1StrongAutosomal recessiveFraser syndrome 34
NCOA2StrongAutosomal recessiveFraser syndrome 34

Orphanet rare-disease linkage (cohort genes)

GeneOrphanet IDRare disease
GRIP1Orphanet:2052Fraser syndrome
MYO18BOrphanet:447974Klippel-Feil anomaly-myopathy-facial dysmorphism syndrome
MPC1Orphanet:447784Mitochondrial pyruvate carrier deficiency
MED23Orphanet:88616Autosomal recessive non-syndromic intellectual disability
ODAD1Orphanet:244Primary ciliary dyskinesia
WDR81Orphanet:1766Dysequilibrium syndrome
WDR81Orphanet:269505Congenital communicating hydrocephalus
WDR81Orphanet:269510Congenital non-communicating hydrocephalus
AIPL1Orphanet:1872Cone rod dystrophy
AIPL1Orphanet:65Leber congenital amaurosis
GNB5Orphanet:542306GNB5-related intellectual disability-cardiac arrhythmia syndrome
ASPAOrphanet:314911Severe Canavan disease
ASPAOrphanet:314918Mild Canavan disease
PTCH1Orphanet:220386Semilobar holoprosencephaly
PTCH1Orphanet:2353Schilbach-Rott syndrome
PTCH1Orphanet:280195Septopreoptic holoprosencephaly
PTCH1Orphanet:280200Microform holoprosencephaly
PTCH1Orphanet:377Gorlin syndrome
PTCH1Orphanet:77301Monosomy 9q22.3 syndrome
PTCH1Orphanet:93924Lobar holoprosencephaly
PTCH1Orphanet:93925Alobar holoprosencephaly
PTCH1Orphanet:93926Midline interhemispheric variant of holoprosencephaly

Cohort genes → proteins

17 cohort genes, 17 distinct canonical proteins.

Evidence partition

SubsetGenes
multi_evidence17

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
GRIP1HGNC:18708ENSG00000155974Q9Y3R0Glutamate receptor-interacting protein 1gencc,clinvar
NCOA2HGNC:7669ENSG00000140396Q15596Nuclear receptor coactivator 2gencc,clinvar
ZXDAHGNC:13198ENSG00000198205P98168Zinc finger X-linked protein ZXDAclinvar
ADAMTS14HGNC:14899ENSG00000138316Q8WXS8A disintegrin and metalloproteinase with thrombospondin motifs 14clinvar
BCLAF1HGNC:16863ENSG00000029363Q9NYF8Bcl-2-associated transcription factor 1clinvar
LSM10HGNC:17562ENSG00000181817Q969L4U7 snRNA-associated Sm-like protein LSm10clinvar
MYO18BHGNC:18150ENSG00000133454Q8IUG5Unconventional myosin-XVIIIbclinvar
MPC1HGNC:21606ENSG00000060762Q9Y5U8Mitochondrial pyruvate carrier 1clinvar
MED23HGNC:2372ENSG00000112282Q9ULK4Mediator of RNA polymerase II transcription subunit 23clinvar
BORCS6HGNC:25939ENSG00000196544Q96GS4BLOC-1-related complex subunit 6clinvar
ODAD1HGNC:26560ENSG00000105479Q96M63Outer dynein arm-docking complex subunit 1clinvar
WDR81HGNC:26600ENSG00000167716Q562E7WD repeat-containing protein 81clinvar
TLCD3AHGNC:29646ENSG00000167695Q8TBR7TLC domain-containing protein 3Aclinvar
AIPL1HGNC:359ENSG00000129221Q9NZN9Aryl-hydrocarbon-interacting protein-like 1clinvar
GNB5HGNC:4401ENSG00000069966O14775Guanine nucleotide-binding protein subunit beta-5clinvar
ASPAHGNC:756ENSG00000108381P45381Aspartoacylaseclinvar
PTCH1HGNC:9585ENSG00000185920Q13635Protein patched homolog 1clinvar

Cohort function summary

Lead sentence per gene, UniProt-curated.

SymbolProtein nameFunction (lead sentence)
GRIP1Glutamate receptor-interacting protein 1May play a role as a localized scaffold for the assembly of a multiprotein signaling complex and as mediator of the trafficking of its binding partners at specific subcellular location in neurons.
NCOA2Nuclear receptor coactivator 2Transcriptional coactivator for steroid receptors and nuclear receptors.
ZXDAZinc finger X-linked protein ZXDACooperates with CIITA to promote transcription of MHC class I and MHC class II genes.
ADAMTS14A disintegrin and metalloproteinase with thrombospondin motifs 14Has aminoprocollagen type I processing activity in the absence of ADAMTS2.
BCLAF1Bcl-2-associated transcription factor 1Death-promoting transcriptional repressor.
LSM10U7 snRNA-associated Sm-like protein LSm10Appears to function in the U7 snRNP complex that is involved in histone 3’-end processing.
MYO18BUnconventional myosin-XVIIIbMay be involved in intracellular trafficking of the muscle cell when in the cytoplasm, whereas entering the nucleus, may be involved in the regulation of muscle specific genes.
MPC1Mitochondrial pyruvate carrier 1Mediates the uptake of pyruvate into mitochondria to maintain the balance between glycolysis and oxidative phosphorylation.
MED23Mediator of RNA polymerase II transcription subunit 23Required for transcriptional activation subsequent to the assembly of the pre-initiation complex.
BORCS6BLOC-1-related complex subunit 6As part of the BORC complex may play a role in lysosomes movement and localization at the cell periphery.
ODAD1Outer dynein arm-docking complex subunit 1Component of the outer dynein arm-docking complex (ODA-DC) that mediates outer dynein arms (ODA) binding onto the doublet microtubule.
WDR81WD repeat-containing protein 81Functions as a negative regulator of the PI3 kinase/PI3K activity associated with endosomal membranes via BECN1, a core subunit of the PI3K complex.
AIPL1Aryl-hydrocarbon-interacting protein-like 1May be important in protein trafficking and/or protein folding and stabilization.
GNB5Guanine nucleotide-binding protein subunit beta-5Enhances GTPase-activating protein (GAP) activity of regulator of G protein signaling (RGS) proteins, such as RGS7 and RGS9, hence involved in the termination of the signaling initiated by the G protein coupled receptors (GPCRs) by acceler…
ASPAAspartoacylaseCatalyzes the deacetylation of N-acetylaspartic acid (NAA) to produce acetate and L-aspartate.
PTCH1Protein patched homolog 1Acts as a receptor for sonic hedgehog (SHH), indian hedgehog (IHH) and desert hedgehog (DHH).

Protein-family classification

Druggable: 3 · Difficult: 4 · Unknown: 10 · 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
Protease12.1×0.753
Scaffold/PPI22.0×0.753
Kinase11.6×0.753
Other/Unknown101.1×0.753
Transcription factor21.0×0.753
Enzyme (other)10.7×0.773

Per-gene assignment

SymbolFamilyDruggable?ECInterPro (top 3)
GRIP1Scaffold/PPInoPDZ, PDZ_sf, PDZ_6
NCOA2Transcription factornoPAS, Nuc_rcpt_coact, NCO_DUF1518
ZXDATranscription factornoZnf_C2H2_type, Znf_C2H2_sf,
ADAMTS14Proteaseyes3.4.24.14TSP1_rpt, Peptidase_M12B, Peptidase_M12B_N
BCLAF1Other/UnknownnoTHRAP3_BCLAF1
LSM10Other/UnknownnoSm_dom_euk/arc, LSM_dom_sf, Sm
MYO18BOther/UnknownnoMyosin_head_motor_dom-like, P-loop_NTPase, MYSc_Myo18
MPC1Other/UnknownnoMPC
MED23Other/UnknownnoMediator_Med23
BORCS6Other/UnknownnoBORCS6, BORCS6_C
ODAD1Other/UnknownnoODAD1_CC, ODA-DC/CCD
WDR81KinaseyesBEACH_dom, WD40_rpt, Kinase-like_dom_sf
TLCD3AOther/UnknownnoTLC-dom, TLCD
AIPL1Other/UnknownnoTPR-like_helical_dom_sf, TPR_rpt, AIP/AIPL1/TTC9
GNB5Scaffold/PPInoWD40_G-protein_beta-like, WD40_rpt, WD40/YVTN_repeat-like_dom_sf
ASPAEnzyme (other)yes3.5.1.15Aste_AspA_hybrid_dom, Aspartoacylase, AspA/AstE_fam
PTCH1Other/UnknownnoSSD, TM_rcpt_patched, HMGCR/SNAP/NPC1-like_SSD

Expression context

Cohort genes with no expression data: 0.

13 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)17
unknown0

Top tissues across cohort

TissueCohort genes
endothelial cell3
granulocyte3
buccal mucosa cell2
calcaneal tendon2
tibia2
gastrocnemius2
hindlimb stylopod muscle2
cerebellar hemisphere2
cortical plate1
ganglionic eminence1
ventricular zone1
corpus epididymis1
secondary oocyte1
male germ line stem cell (sensu Vertebrata) in testis1
gall bladder1
mucosa of transverse colon1
vena cava1
embryo1
apex of heart1
cardiac ventricle1

Per-gene tissue summary (top 30)

SymbolBgee breadthFANTOM5 breadthSCXATop tissues
GRIP1192broadmarkercortical plate, ganglionic eminence, ventricular zone
NCOA2292ubiquitousmarkercorpus epididymis, endothelial cell, secondary oocyte
ZXDA208tissue_specificyesendothelial cell, buccal mucosa cell, male germ line stem cell (sensu Vertebrata) in testis
ADAMTS14156broadyesgall bladder, vena cava, mucosa of transverse colon
BCLAF1295ubiquitousmarkercalcaneal tendon, tibia, embryo
LSM10245ubiquitousmarkerhindlimb stylopod muscle, gastrocnemius, granulocyte
MYO18B148broadmarkerapex of heart, gastrocnemius, hindlimb stylopod muscle
MPC1288ubiquitousmarkerheart right ventricle, cardiac ventricle, heart left ventricle
MED23283ubiquitousyesright hemisphere of cerebellum, calcaneal tendon, cerebellar hemisphere
BORCS6219ubiquitousyestype B pancreatic cell, olfactory bulb, granulocyte
ODAD1174broadmarkeroviduct epithelium, right uterine tube, bronchial epithelial cell
WDR81138ubiquitousmarkergranulocyte, left ovary, right ovary
TLCD3A228ubiquitousmarkerskin of abdomen, skin of leg, zone of skin
AIPL162tissue_specificmarkerbuccal mucosa cell, pancreatic ductal cell, tendon of biceps brachii
GNB5279ubiquitousmarkermiddle temporal gyrus, endothelial cell, cerebellar hemisphere
ASPA238broadmarkercorpus callosum, nephron tubule, medial globus pallidus
PTCH1275ubiquitousmarkertibia, dorsal root ganglion, trigeminal ganglion

Protein interactions among cohort

Intra-cohort edges: 1.

Hub genes (top 10 by interactor count)

SymbolInteractor count
BCLAF14,230
GRIP13,602
PTCH13,368
GNB52,987
NCOA22,464
MED232,155
MYO18B1,775
LSM101,724
WDR811,404
ODAD11,224

Intra-cohort edges

ABSources
MED23NCOA2intact

Structural data

PDB: 11 · AlphaFold-only: 6 · No structure: 0

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
NCOA2Q15596381
GNB5O1477532
PTCH1Q1363516
MPC1Q9Y5U813
MED23Q9ULK413
ASPAP453818
AIPL1Q9NZN96
LSM10Q969L45
BCLAF1Q9NYF82
GRIP1Q9Y3R01
ODAD1Q96M631

AlphaFold-only cohort genes (top 30 by pLDDT)

SymbolUniProtpLDDT
TLCD3AQ8TBR792.98
ADAMTS14Q8WXS870.22
WDR81Q562E769.23
BORCS6Q96GS466.53
MYO18BQ8IUG560.66
ZXDAP9816855.14

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 117. Enrichment computed across 17 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
Epigenetic regulation of adipogenesis genes by MLL3 and MLL4 complexes243.1×0.049NCOA2, MED23
Epigenetic regulation of gene expression by MLL3 and MLL4 complexes239.4×0.049NCOA2, MED23
Adipogenesis231.3×0.049NCOA2, MED23
Epigenetic regulation by WDR5-containing histone modifying complexes230.9×0.049NCOA2, MED23
Regulation of lipid metabolism by PPARalpha228.2×0.049NCOA2, MED23
Transcriptional regulation of white adipocyte differentiation225.9×0.049NCOA2, MED23
GLI proteins bind promoters of Hh responsive genes to promote transcription1163.1×0.067PTCH1
Ligand-receptor interactions1142.8×0.067PTCH1
SLBP independent Processing of Histone Pre-mRNAs1114.2×0.067LSM10
Processing of Capped Intronless Pre-mRNA1103.8×0.067LSM10
SLBP Dependent Processing of Replication-Dependent Histone Pre-mRNAs1103.8×0.067LSM10
Aspartate and asparagine metabolism1103.8×0.067ASPA
Synthesis of bile acids and bile salts via 27-hydroxycholesterol176.1×0.067NCOA2
R-HSA-1368082171.4×0.067NCOA2
Cytochrome P450 - arranged by substrate type171.4×0.067NCOA2
Trafficking of GluR2-containing AMPA receptors167.2×0.067GRIP1
Activation of SMO163.4×0.067PTCH1
G beta:gamma signalling through BTK163.4×0.067GNB5
Recycling of bile acids and salts160.1×0.067NCOA2
Prostacyclin signalling through prostacyclin receptor160.1×0.067GNB5
G beta:gamma signalling through PLC beta157.1×0.067GNB5
G beta:gamma signalling through CDC42157.1×0.067GNB5
Presynaptic function of Kainate receptors154.4×0.067GNB5
Bile acid and bile salt metabolism149.6×0.067NCOA2
ADP signalling through P2Y purinoceptor 12149.6×0.067GNB5
G-protein activation147.6×0.067GNB5
Thromboxane signalling through TP receptor147.6×0.067GNB5
Collagen formation145.7×0.067ADAMTS14
Synthesis of bile acids and bile salts via 7alpha-hydroxycholesterol145.7×0.067NCOA2
ADP signalling through P2Y purinoceptor 1145.7×0.067GNB5

GO biological processes by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 17 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

GO termCohort genesFoldFDRSample cohort genes
acetate metabolic process1991.3×0.033ASPA
response to chlorate1495.6×0.033PTCH1
neural plate axis specification1495.6×0.033PTCH1
cell proliferation involved in metanephros development1495.6×0.033PTCH1
dark adaptation1495.6×0.033GNB5
positive regulation of T cell extravasation1495.6×0.033MED23
pyruvate import into mitochondria1330.4×0.033MPC1
protein farnesylation1330.4×0.033AIPL1
light adaption1330.4×0.033GNB5
cell differentiation involved in kidney development1330.4×0.033PTCH1
negative regulation of smoothened signaling pathway253.6×0.033NCOA2, PTCH1
cellular response to Thyroglobulin triiodothyronine1247.8×0.040NCOA2
epidermal cell fate specification1198.3×0.041PTCH1
mRNA 3’-end processing by stem-loop binding and cleavage1165.2×0.041LSM10
neural tube patterning1165.2×0.041PTCH1
hindlimb morphogenesis1165.2×0.041PTCH1
negative regulation of cell division1141.6×0.041PTCH1
mammary gland duct morphogenesis1141.6×0.041PTCH1
aspartate metabolic process1123.9×0.041ASPA
positive regulation of epidermal cell differentiation1123.9×0.041PTCH1
positive regulation of neuron projection arborization1123.9×0.041GRIP1
G protein-coupled dopamine receptor signaling pathway1110.1×0.041GNB5
regulation of lysosome size1110.1×0.041BORCS6
neurotransmitter receptor transport, endosome to postsynaptic membrane1110.1×0.041GRIP1
positive regulation of DNA-templated transcription initiation1110.1×0.041BCLAF1
regulation of opsin-mediated signaling pathway199.1×0.041AIPL1
aggrephagy199.1×0.041WDR81
metanephric collecting duct development199.1×0.041PTCH1
peroxisome proliferator activated receptor signaling pathway190.1×0.041NCOA2
response to alkaloid190.1×0.041PTCH1

Therapeutics

Drug target analysis

Approved (phase 4): 2 · Phase ≥3: 2 · Phased (≥1): 3 · Undrugged: 14

Druggability breadth: 5 of 17 evidence-associated genes (29%) 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
NCOA2METHYLENE BLUE ANHYDROUS
MED23PALBOCICLIB

Top cohort targets by molecule count

SymbolMoleculesMax phase
NCOA214
BCLAF112
MED2314
GRIP100
ZXDA00
ADAMTS1400
LSM1000
MYO18B00
MPC100
BORCS600

Drugs targeting cohort genes (top 30)

MoleculeMax phaseTargets in cohort
METHYLENE BLUE ANHYDROUS4NCOA2
PALBOCICLIB4MED23
MOLIBRESIB2BCLAF1

Bioactivity and enzyme data

Enzyme cohort genes (≥1 EC): 2.

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

SymbolAssaysType breakdown
MED239Binding:9
BCLAF18Binding:8
PTCH14Binding:4
NCOA23Functional:2, Binding:1
AIPL11Binding:1

Cohort enzymes (BRENDA EC)

SymbolEC numbersNames
ADAMTS143.4.24.14procollagen N-endopeptidase
ASPA3.5.1.15aspartoacylase

Pharmacogenomics

Cohort genes with a PharmGKB record: 17; with CPIC/DPWG dosing guidelines: 0.

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

Chemical tractability of cohort targets

3 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)
METHYLENE BLUE ANHYDROUS4NCOA2
PALBOCICLIB4MED23
MOLIBRESIB2BCLAF1

Druggability pyramid

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

TierDefinitionGenesSymbols
AApproved (phase 4 drug)2NCOA2, MED23
BPhased (≥1) drug, not yet approved1BCLAF1
CDruggable family + PDB, no drug1ASPA
DDruggable family + AlphaFold only, no drug2ADAMTS14, WDR81
EDifficult family or no structure, no drug11GRIP1, ZXDA, LSM10, MYO18B, MPC1, BORCS6, ODAD1, TLCD3A, AIPL1, GNB5 (+1 more)

Undrugged target profiles

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

SymbolChEMBL assaysDrugged partners (top 3)
GRIP10
ZXDA0
ADAMTS140
LSM100
MYO18B0
MPC10
BORCS60
ODAD10
WDR810
TLCD3A0
AIPL11
GNB50
ASPA0
PTCH14

Clinical trials & evidence

Clinical trials

Clinical trials: 0.