MYLK3
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Also known as caMLCKMLCK
Summary
MYLK3 (myosin light chain kinase 3, HGNC:29826) is a protein-coding gene on chromosome 16q11.2, encoding Myosin light chain kinase 3 (Q32MK0). Kinase that phosphorylates MYL2 in vitro.
Phosphorylation of cardiac myosin heavy chains (see MYH7B, MIM 609928) and light chains (see MYL2, MIM 160781) by a kinase, such as MYLK3, potentiates the force and rate of cross-bridge recruitment in cardiac myocytes (Chan et al., 2008 [PubMed 18202317]).
Source: NCBI Gene 91807 — RefSeq curated summary.
At a glance
- Gene–disease (curated): dilated cardiomyopathy (Moderate, ClinGen)
- Clinical variants (ClinVar): 1,054 total — 1 likely-pathogenic
- Phenotypes (HPO): 1
- Druggable target: yes — 24 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_182493
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:29826 |
| Approved symbol | MYLK3 |
| Name | myosin light chain kinase 3 |
| Location | 16q11.2 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | caMLCK, MLCK |
| Ensembl gene | ENSG00000140795 |
| Ensembl biotype | protein_coding |
| OMIM | 612147 |
| Entrez | 91807 |
Gene structure
Transcript identifiers
Ensembl transcripts: 10 — 5 protein_coding, 3 retained_intron, 2 protein_coding_CDS_not_defined
ENST00000394809, ENST00000536476, ENST00000562104, ENST00000564731, ENST00000565182, ENST00000569810, ENST00000569844, ENST00000874186, ENST00000874187, ENST00000971334
RefSeq mRNA: 2 — MANE Select: NM_182493
NM_001308301, NM_182493
CCDS: CCDS10723, CCDS76861
Canonical transcript exons
ENST00000394809 — 13 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000945062 | 46747717 | 46748344 |
| ENSE00000945064 | 46737711 | 46738143 |
| ENSE00000945070 | 46721123 | 46721193 |
| ENSE00000945071 | 46712648 | 46712776 |
| ENSE00000945076 | 46727236 | 46727377 |
| ENSE00002603072 | 46702282 | 46707763 |
| ENSE00003542772 | 46740057 | 46740147 |
| ENSE00003574018 | 46709539 | 46709671 |
| ENSE00003606376 | 46730593 | 46730698 |
| ENSE00003606473 | 46732208 | 46732668 |
| ENSE00003619656 | 46710637 | 46710789 |
| ENSE00003630562 | 46729024 | 46729133 |
| ENSE00003672514 | 46729594 | 46729687 |
Expression profiles
Bgee: expression breadth ubiquitous, 194 present calls, max score 98.13.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 1.3151 / max 334.2785, expressed in 114 samples.
FANTOM5 promoters (8 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 157220 | 0.5650 | 65 |
| 157210 | 0.5597 | 44 |
| 157218 | 0.0627 | 25 |
| 157217 | 0.0383 | 17 |
| 207864 | 0.0342 | 13 |
| 157219 | 0.0332 | 21 |
| 157209 | 0.0114 | 3 |
| 157216 | 0.0106 | 9 |
Top tissues by expression
268 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| cardiac muscle of right atrium | UBERON:0003379 | 98.13 | gold quality |
| myocardium | UBERON:0002349 | 97.63 | gold quality |
| heart right ventricle | UBERON:0002080 | 97.45 | gold quality |
| left ventricle myocardium | UBERON:0006566 | 97.07 | gold quality |
| cardiac atrium | UBERON:0002081 | 95.61 | gold quality |
| right atrium auricular region | UBERON:0006631 | 95.22 | gold quality |
| cardiac ventricle | UBERON:0002082 | 94.18 | gold quality |
| heart left ventricle | UBERON:0002084 | 94.08 | gold quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 93.96 | gold quality |
| body of tongue | UBERON:0011876 | 93.42 | gold quality |
| apex of heart | UBERON:0002098 | 92.99 | gold quality |
| biceps brachii | UBERON:0001507 | 92.25 | gold quality |
| diaphragm | UBERON:0001103 | 91.94 | gold quality |
| skeletal muscle tissue of rectus abdominis | UBERON:0004511 | 91.30 | gold quality |
| triceps brachii | UBERON:0001509 | 90.41 | gold quality |
| heart | UBERON:0000948 | 90.00 | gold quality |
| vena cava | UBERON:0004087 | 89.87 | gold quality |
| vastus lateralis | UBERON:0001379 | 89.44 | gold quality |
| skeletal muscle tissue | UBERON:0001134 | 88.42 | gold quality |
| buccal mucosa cell | CL:0002336 | 88.40 | gold quality |
| quadriceps femoris | UBERON:0001377 | 88.36 | gold quality |
| muscle tissue | UBERON:0002385 | 87.30 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 85.11 | gold quality |
| deltoid | UBERON:0001476 | 84.99 | silver quality |
| renal glomerulus | UBERON:0000074 | 84.75 | gold quality |
| gluteal muscle | UBERON:0002000 | 83.52 | silver quality |
| muscle organ | UBERON:0001630 | 83.44 | gold quality |
| metanephric glomerulus | UBERON:0004736 | 83.17 | gold quality |
| tibialis anterior | UBERON:0001385 | 82.62 | silver quality |
| muscle of leg | UBERON:0001383 | 81.23 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 5.65 |
| E-HCAD-5 | no | 226.97 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): NKX2-5
miRNA regulators (miRDB)
167 targeting MYLK3, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-6867-5P | 100.00 | 82.21 | 3464 |
| HSA-MIR-3613-3P | 100.00 | 76.36 | 7965 |
| HSA-MIR-4668-3P | 100.00 | 68.74 | 2635 |
| HSA-MIR-6851-5P | 100.00 | 65.63 | 1294 |
| HSA-MIR-3689D | 100.00 | 66.14 | 1181 |
| HSA-MIR-3646 | 100.00 | 73.56 | 5283 |
| HSA-MIR-3163 | 100.00 | 77.23 | 8605 |
| HSA-MIR-8485 | 100.00 | 77.57 | 4731 |
| HSA-MIR-6833-3P | 100.00 | 70.63 | 3197 |
| HSA-MIR-4768-5P | 100.00 | 69.49 | 2861 |
| HSA-MIR-7110-3P | 100.00 | 73.18 | 2486 |
| HSA-MIR-4481 | 100.00 | 66.42 | 1669 |
| HSA-MIR-6873-3P | 100.00 | 71.42 | 2626 |
| HSA-MIR-371B-5P | 99.99 | 75.34 | 4759 |
| HSA-MIR-548C-3P | 99.99 | 74.01 | 7587 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-150-5P | 99.99 | 66.69 | 1976 |
| HSA-MIR-373-5P | 99.98 | 75.36 | 4753 |
| HSA-MIR-616-5P | 99.98 | 75.58 | 4775 |
| HSA-MIR-8068 | 99.98 | 73.85 | 2376 |
| HSA-MIR-12136 | 99.98 | 72.81 | 5713 |
| HSA-MIR-4775 | 99.98 | 75.00 | 6394 |
| HSA-MIR-5696 | 99.98 | 72.36 | 4487 |
| HSA-MIR-6891-5P | 99.98 | 66.53 | 1372 |
| HSA-MIR-607 | 99.97 | 73.62 | 5593 |
| HSA-MIR-3148 | 99.97 | 75.06 | 6478 |
| HSA-MIR-590-3P | 99.96 | 74.34 | 6478 |
| HSA-MIR-3658 | 99.96 | 73.87 | 4379 |
| HSA-MIR-6778-3P | 99.96 | 67.29 | 2693 |
| HSA-MIR-548AA | 99.96 | 70.64 | 3753 |
Literature-anchored findings (GeneRIF, showing 6)
- Integrated cDNA expression analysis of failing human myocardia uncovered a novel protein kinase, cardiac-specific myosin light chain kinase (cardiac-MLCK), which acts on MLC2v. (PMID:17885681)
- data indicate that the IL-1beta-induced increase in MLCK protein expression and Caco-2 TJ permeability was mediated by an increase in MLCK expression and activity and by an NF-kappaB-dependent increase in MLCK gene transcription (PMID:18390750)
- These findings suggest that hepatitis B virus X protein disrupts stress fiber formation and triggers apoptosis via an MLCK and a PTEN-dependent pathway. (PMID:23591626)
- Biochemical and physiological regulation of cardiac myocyte contraction by cardiac-specific myosin light chain kinase. (PMID:23863751)
- This study demonstrates that cyclic stretch disrupts tight junctions and adherens junctions by a JNK2, c-Src, and MLCK-dependent mechanism. (PMID:24722904)
- Study identified MYLK3 mutations associated with familial dilated cardiomyopathy. In vitro experiments and immunohistochemistry suggested that the MYLK3 mutations identified in this study result in markedly reduced levels of protein expression and myosin light chain 2 phosphorylation. (PMID:29235529)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | mylk3 | ENSDARG00000076348 |
| mus_musculus | Mylk3 | ENSMUSG00000031698 |
| rattus_norvegicus | Mylk3 | ENSRNOG00000017546 |
Paralogs (22): CAMKK1 (ENSG00000004660), CAMK1G (ENSG00000008118), CAMK2B (ENSG00000058404), CAMK2A (ENSG00000070808), MYLK2 (ENSG00000101306), CAMKK2 (ENSG00000110931), STK11 (ENSG00000118046), STK33 (ENSG00000130413), PNCK (ENSG00000130822), DCLK1 (ENSG00000133083), CAMK1 (ENSG00000134072), CAMK2D (ENSG00000145349), MYLK4 (ENSG00000145949), PSKH2 (ENSG00000147613), CAMK2G (ENSG00000148660), PHKG2 (ENSG00000156873), PSKH1 (ENSG00000159792), DCLK3 (ENSG00000163673), CAMKV (ENSG00000164076), PHKG1 (ENSG00000164776), DCLK2 (ENSG00000170390), CAMK1D (ENSG00000183049)
Protein
Protein identifiers
Myosin light chain kinase 3 — Q32MK0 (reviewed: Q32MK0)
Alternative names: Cardiac-MyBP-C-associated Ca/CaM kinase
All UniProt accessions (1): Q32MK0
UniProt curated annotations — full annotation on UniProt →
Function. Kinase that phosphorylates MYL2 in vitro. Promotes sarcomere formation in cardiomyocytes and increases cardiomyocyte contractility.
Subcellular location. Cytoplasm.
Tissue specificity. Restricted to heart.
Post-translational modifications. Phosphorylated on serine residues.
Similarity. Belongs to the protein kinase superfamily. CAMK Ser/Thr protein kinase family.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q32MK0-3 | 1 | yes |
| Q32MK0-4 | 2 |
RefSeq proteins (2): NP_001295230, NP_872299* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000719 | Prot_kinase_dom | Domain |
| IPR008271 | Ser/Thr_kinase_AS | Active_site |
| IPR011009 | Kinase-like_dom_sf | Homologous_superfamily |
| IPR017441 | Protein_kinase_ATP_BS | Binding_site |
Pfam: PF00069
Catalyzed reactions (Rhea), 2 shown:
- L-seryl-[myosin light chain] + ATP = O-phospho-L-seryl-[myosin light chain] + ADP + H(+) (RHEA:22004)
- L-threonyl-[myosin light chain] + ATP = O-phospho-L-threonyl-[myosin light chain] + ADP + H(+) (RHEA:53900)
UniProt features (21 total): modified residue 4, sequence variant 3, region of interest 3, compositionally biased region 3, binding site 2, sequence conflict 2, chain 1, domain 1, splice variant 1, active site 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q32MK0-F1 | 63.26 | 0.29 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Catalytic / active sites (1): 636 (proton acceptor)
Ligand- & substrate-binding residues (2): 544; 521–529
Post-translational modifications (4): 152, 355, 401, 408
Function
Pathways and Gene Ontology
Reactome pathways
0 pathways
MSigDB gene sets: 132 (showing top):
GOBP_MUSCLE_TISSUE_DEVELOPMENT, GOBP_RESPONSE_TO_PEPTIDE, GOBP_POSITIVE_REGULATION_OF_MUSCLE_CELL_DIFFERENTIATION, GOBP_STRIATED_MUSCLE_CELL_DIFFERENTIATION, GOBP_REGULATION_OF_STRIATED_MUSCLE_CELL_DIFFERENTIATION, GOBP_CARDIAC_MYOFIBRIL_ASSEMBLY, GOBP_POSITIVE_REGULATION_OF_ORGANELLE_ORGANIZATION, GOBP_SARCOMERE_ORGANIZATION, GOBP_REGULATION_OF_ACTIN_FILAMENT_BASED_PROCESS, GOBP_CELL_JUNCTION_ORGANIZATION, GOBP_CELLULAR_COMPONENT_ASSEMBLY_INVOLVED_IN_MORPHOGENESIS, GOBP_MUSCLE_STRUCTURE_DEVELOPMENT, GOBP_POSITIVE_REGULATION_OF_CELL_DIFFERENTIATION, GOBP_REGULATION_OF_MUSCLE_CELL_DIFFERENTIATION, TGCTGAY_UNKNOWN
GO Biological Process (9): signal transduction (GO:0007165), sarcomere organization (GO:0045214), sarcomerogenesis (GO:0048769), cardiac myofibril assembly (GO:0055003), positive regulation of sarcomere organization (GO:0060298), cellular response to interleukin-1 (GO:0071347), positive regulation of tight junction disassembly (GO:1905075), positive regulation of membrane permeability (GO:1905710), protein phosphorylation (GO:0006468)
GO Molecular Function (9): calcium/calmodulin-dependent protein kinase activity (GO:0004683), myosin light chain kinase activity (GO:0004687), ATP binding (GO:0005524), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein serine/threonine kinase activity (GO:0004674), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)
GO Cellular Component (3): cytoplasm (GO:0005737), cytosol (GO:0005829), actin cytoskeleton (GO:0015629)
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| myofibril assembly | 3 |
| actomyosin structure organization | 2 |
| protein serine/threonine kinase activity | 2 |
| cellular anatomical structure | 2 |
| cell communication | 1 |
| cellular process | 1 |
| signaling | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| cardiac muscle cell development | 1 |
| sarcomere organization | 1 |
| positive regulation of striated muscle cell differentiation | 1 |
| positive regulation of cytoskeleton organization | 1 |
| regulation of sarcomere organization | 1 |
| positive regulation of supramolecular fiber organization | 1 |
| response to interleukin-1 | 1 |
| cellular response to cytokine stimulus | 1 |
| positive regulation of cellular component organization | 1 |
| tight junction disassembly | 1 |
| regulation of tight junction disassembly | 1 |
| regulation of membrane permeability | 1 |
| phosphorylation | 1 |
| protein modification process | 1 |
| adenyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| nucleoside phosphate binding | 1 |
| heterocyclic compound binding | 1 |
| kinase activity | 1 |
| phosphotransferase activity, alcohol group as acceptor | 1 |
| catalytic activity, acting on a protein | 1 |
| protein kinase activity | 1 |
| binding | 1 |
| transferase activity, transferring phosphorus-containing groups | 1 |
| catalytic activity | 1 |
| intracellular anatomical structure | 1 |
| cytoplasm | 1 |
| cytoskeleton | 1 |
Protein interactions and networks
STRING
1533 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| MYLK3 | CALML3 | P27482 | 964 |
| MYLK3 | CALML5 | Q9NZT1 | 964 |
| MYLK3 | CALML6 | Q8TD86 | 962 |
| MYLK3 | CALML4 | Q96GE6 | 962 |
| MYLK3 | CALM1 | P02593 | 928 |
| MYLK3 | MYL7 | Q01449 | 825 |
| MYLK3 | MYL2 | P10916 | 791 |
| MYLK3 | MYH7B | A7E2Y1 | 760 |
| MYLK3 | PPP1R12A | O14974 | 727 |
| MYLK3 | MYL12B | O14950 | 657 |
| MYLK3 | RHOA | P06749 | 640 |
| MYLK3 | PPP1R14A | Q96A00 | 609 |
| MYLK3 | ACTC1 | P04270 | 599 |
| MYLK3 | MYL9 | P24844 | 586 |
| MYLK3 | PAK1 | Q13153 | 456 |
IntAct
14 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| MAPK14 | RPS6KA5 | psi-mi:“MI:0914”(association) | 0.660 |
| MAPK12 | MAPK13 | psi-mi:“MI:0914”(association) | 0.640 |
| MYLK3 | YWHAE | psi-mi:“MI:0915”(physical association) | 0.400 |
| SFN | MYLK3 | psi-mi:“MI:0915”(physical association) | 0.400 |
| HSP90AB1 | MYLK3 | psi-mi:“MI:0915”(physical association) | 0.400 |
| ALB | CNOT1 | psi-mi:“MI:0914”(association) | 0.350 |
| MAPK14 | PRKY | psi-mi:“MI:0914”(association) | 0.350 |
| MYLK3 | psi-mi:“MI:0914”(association) | 0.350 | |
| MYLK3 | OBSL1 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (17): MYLK3 (Affinity Capture-MS), MYLK3 (Affinity Capture-MS), MYLK3 (Affinity Capture-MS), MYLK3 (Affinity Capture-MS), CALM3 (Affinity Capture-MS), OBSL1 (Affinity Capture-MS), PCDHB11 (Affinity Capture-MS), PCDHB5 (Affinity Capture-MS), OBSL1 (Affinity Capture-MS), MYLK3 (Affinity Capture-MS), CALM3 (Affinity Capture-MS), MYLK3 (Affinity Capture-MS), RBM17 (Cross-Linking-MS (XL-MS)), MYLK3 (Affinity Capture-RNA), MYLK3 (Dosage Lethality)
ESM2 similar proteins: A4IFM7, A8C984, B6D5P1, B6D5P6, E9PT87, O08815, O54988, O55092, O70551, O88831, P00519, P00520, P00521, P07313, P0C865, P13234, P20689, P42684, P46087, Q13164, Q14028, Q16566, Q2KI23, Q32MK0, Q3SYS4, Q3UH66, Q3UIZ8, Q3ULB5, Q4JIM5, Q4KMM3, Q4V8B0, Q5R8Z4, Q5RDG7, Q5TGJ6, Q63553, Q6AYH9, Q6PDI6, Q80XI3, Q8BHL3, Q8BWQ5
Diamond homologs: A0A509AFG4, A0A5K1K8H0, A2AAJ9, A2ZVI7, A4IFM7, A8C984, A8WXF6, B9FKW9, C0HKC8, C0HKC9, E9PT87, O02827, O43293, O44997, O54784, O62305, O70150, O75147, O80673, O88764, O94768, P07313, P08414, P11801, P13234, P15735, P18653, P20689, P29294, P31325, P34101, P43292, P53355, P53681, Q00168, Q00771, Q0KHT7, Q0V7M1, Q10KY3, Q14012
SIGNOR signaling
1 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| MYLK3 | “up-regulates activity” | MEF2C | phosphorylation |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 11 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.
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| intracellular signal transduction | 5 | 19.1× | 5e-04 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
1054 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 1 |
| Uncertain significance | 657 |
| Likely benign | 341 |
| Benign | 21 |
Top pathogenic / likely-pathogenic (1)
| Variant ID | HGVS | Classification |
|---|---|---|
| 2419098 | NM_182493.3(MYLK3):c.1915-1G>T | Likely pathogenic |
SpliceAI
2278 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 16:46712644:TCACA:T | donor_loss | 1.0000 |
| 16:46712645:CA:C | donor_loss | 1.0000 |
| 16:46712646:A:AC | donor_gain | 1.0000 |
| 16:46712647:C:CC | donor_gain | 1.0000 |
| 16:46712647:CAG:C | donor_gain | 1.0000 |
| 16:46712647:CAGCA:C | donor_gain | 1.0000 |
| 16:46727231:CCCA:C | donor_loss | 1.0000 |
| 16:46727232:CCA:C | donor_loss | 1.0000 |
| 16:46727233:CA:C | donor_loss | 1.0000 |
| 16:46727234:ACC:A | donor_loss | 1.0000 |
| 16:46727235:C:A | donor_loss | 1.0000 |
| 16:46729020:TCACT:T | donor_loss | 1.0000 |
| 16:46729021:CA:C | donor_loss | 1.0000 |
| 16:46729022:A:AC | donor_gain | 1.0000 |
| 16:46729022:ACT:A | donor_loss | 1.0000 |
| 16:46729023:C:CA | donor_gain | 1.0000 |
| 16:46729023:C:CT | donor_loss | 1.0000 |
| 16:46729023:CT:C | donor_gain | 1.0000 |
| 16:46729023:CTA:C | donor_gain | 1.0000 |
| 16:46729023:CTACT:C | donor_gain | 1.0000 |
| 16:46729028:C:CA | donor_gain | 1.0000 |
| 16:46729145:C:CT | acceptor_gain | 1.0000 |
| 16:46729145:C:T | acceptor_gain | 1.0000 |
| 16:46729146:A:T | acceptor_gain | 1.0000 |
| 16:46740145:ATTC:A | acceptor_loss | 1.0000 |
| 16:46740146:TT:T | acceptor_gain | 1.0000 |
| 16:46740148:C:CC | acceptor_gain | 1.0000 |
| 16:46740148:CTA:C | acceptor_loss | 1.0000 |
| 16:46709541:T:TA | donor_gain | 0.9900 |
| 16:46711401:C:CT | acceptor_gain | 0.9900 |
AlphaMissense
5352 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 16:46712676:A:G | W696R | 1.000 |
| 16:46712676:A:T | W696R | 1.000 |
| 16:46712728:G:C | F678L | 1.000 |
| 16:46712728:G:T | F678L | 1.000 |
| 16:46712730:A:G | F678L | 1.000 |
| 16:46721141:T:A | D656V | 1.000 |
| 16:46727246:A:G | L635P | 1.000 |
| 16:46709634:A:G | W769R | 0.999 |
| 16:46709634:A:T | W769R | 0.999 |
| 16:46709665:T:A | R758S | 0.999 |
| 16:46709665:T:G | R758S | 0.999 |
| 16:46709666:C:G | R758T | 0.999 |
| 16:46712667:C:G | G699R | 0.999 |
| 16:46712667:C:T | G699R | 0.999 |
| 16:46712671:A:C | S697R | 0.999 |
| 16:46712671:A:T | S697R | 0.999 |
| 16:46712673:T:G | S697R | 0.999 |
| 16:46712674:C:A | W696C | 0.999 |
| 16:46712674:C:G | W696C | 0.999 |
| 16:46712682:C:A | D694Y | 0.999 |
| 16:46712682:C:G | D694H | 0.999 |
| 16:46712696:A:T | V689D | 0.999 |
| 16:46712711:A:T | V684D | 0.999 |
| 16:46712729:A:G | F678S | 0.999 |
| 16:46712741:C:T | G674D | 0.999 |
| 16:46721129:G:T | A660D | 0.999 |
| 16:46721140:G:C | D656E | 0.999 |
| 16:46721140:G:T | D656E | 0.999 |
| 16:46721141:T:C | D656G | 0.999 |
| 16:46721141:T:G | D656A | 0.999 |
dbSNP variants (sampled 300 via entrez): RS1000020905 (16:46754710 C>A,T), RS1000041279 (16:46720036 C>A,G,T), RS1000071844 (16:46702168 T>C), RS1000072529 (16:46720449 C>T), RS1000077140 (16:46762495 G>A), RS1000147805 (16:46739550 C>T), RS1000184620 (16:46752682 T>C), RS1000221747 (16:46737417 C>A,T), RS1000234971 (16:46719824 C>T), RS1000248810 (16:46764587 A>C,T), RS1000259215 (16:46743790 G>A,T), RS1000280371 (16:46743310 A>G), RS1000309875 (16:46726948 C>T), RS1000339893 (16:46713724 C>T), RS1000448378 (16:46752095 G>A)
Disease associations
OMIM: gene MIM:612147 | disease phenotypes: MIM:614203, MIM:115200
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| dilated cardiomyopathy | Moderate | Autosomal recessive |
ClinGen Gene-Disease Validity (1)
Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.
| Disease | Classification | Inheritance |
|---|---|---|
| dilated cardiomyopathy | Moderate | AD |
Mondo (3): Parkinson disease 17 (MONDO:0013625), dilated cardiomyopathy (MONDO:0005021), familial dilated cardiomyopathy (MONDO:0016333)
Orphanet (3): Hereditary late-onset Parkinson disease (Orphanet:411602), Dilated cardiomyopathy (Orphanet:217604), Familial dilated cardiomyopathy (Orphanet:217607)
HPO phenotypes
1 total (1 of 1 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0001644 | Dilated cardiomyopathy |
GWAS associations
0 associations (top):
MeSH disease descriptors (2)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D002311 | Cardiomyopathy, Dilated | C14.280.195.160; C14.280.238.070; C16.320.488.750 |
| C536231 | familial dilated cardiomyopathy (supp.) |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL4627 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
24 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 224,246 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL1287853 | FEDRATINIB | 4 | 3,554 |
| CHEMBL1289926 | AXITINIB | 4 | 15,732 |
| CHEMBL1336 | SORAFENIB | 4 | 86,060 |
| CHEMBL502835 | NINTEDANIB | 4 | 8,545 |
| CHEMBL535 | SUNITINIB | 4 | 79,020 |
| CHEMBL576982 | QUIZARTINIB | 4 | 4,432 |
| CHEMBL608533 | MIDOSTAURIN | 4 | 7,259 |
| CHEMBL522892 | DOVITINIB | 3 | 4,944 |
| CHEMBL603469 | LESTAURTINIB | 3 | |
| CHEMBL1230609 | FORETINIB | 2 | 3,096 |
| CHEMBL1614713 | CC-401 | 2 | 389 |
| CHEMBL1721885 | SU-014813 | 2 | 363 |
| CHEMBL2386889 | SCH-900776 | 2 | 740 |
| CHEMBL3218578 | BGT-226 FREE BASE | 2 | 2,878 |
| CHEMBL495727 | AT-9283 | 2 | 1,376 |
| CHEMBL564829 | MILCICLIB | 2 | 821 |
| CHEMBL572878 | TOZASERTIB | 2 | 2,998 |
| CHEMBL1090479 | GSK-1070916 | 1 | 177 |
| CHEMBL1908397 | KW-2449 | 1 | 622 |
| CHEMBL2041933 | AZD-7762 | 1 | 1,240 |
| CHEMBL296468 | BMS-387032 | 1 | |
| CHEMBL3128043 | PF-03758309 | 1 | |
| CHEMBL3545328 | XL-019 | 1 | |
| CHEMBL4289017 | PF-03814735 | 1 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — Myosin Light Chain Kinase (MLCK) family
Binding affinities (BindingDB)
6 measured of 8 human assays (8 total across all organisms); most potent 6 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| Staurosporine | KD | 1.7 nM |
| (3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyril | KD | 520 nM |
| N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide | KD | 1100 nM |
| BMS-387072 | KD | 1800 nM |
| 5-[(Z)-(5-fluoranyl-2-oxidanylidene-1H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[(2S)-3-morpholin-4-yl-2-oxidanyl-propyl]-1H-pyrrole-3-carboxamide | KD | 2600 nM |
| N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | KD | 3500 nM |
ChEMBL bioactivities
46 potent at pChembl≥5 of 47 total, top 45 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.70 | Kd | 2 | nM | DOVITINIB |
| 8.37 | Kd | 4.3 | nM | KW-2449 |
| 7.92 | Kd | 12 | nM | LESTAURTINIB |
| 7.82 | Kd | 15 | nM | TOZASERTIB |
| 7.70 | Kd | 20 | nM | SU-014813 |
| 7.64 | Kd | 23 | nM | SUNITINIB |
| 7.51 | Kd | 31 | nM | CHEMBL3990456 |
| 7.38 | Kd | 42 | nM | SU-014813 |
| 7.38 | Kd | 42 | nM | CHEMBL1908395 |
| 7.02 | Kd | 95 | nM | LESTAURTINIB |
| 7.01 | Kd | 98 | nM | K-252A |
| 7.01 | Kd | 98 | nM | XL-019 |
| 6.98 | Kd | 104 | nM | GSK-1070916 |
| 6.96 | Kd | 109 | nM | PF-03814735 |
| 6.96 | Kd | 110 | nM | NINTEDANIB |
| 6.93 | IC50 | 118 | nM | STAUROSPORINE |
| 6.89 | Kd | 129 | nM | AT-9283 |
| 6.89 | IC50 | 129 | nM | STAUROSPORINE |
| 6.85 | Kd | 140 | nM | CHEMBL386051 |
| 6.85 | Kd | 140 | nM | STAUROSPORINE |
| 6.84 | Kd | 146 | nM | CHEMBL4465866 |
| 6.73 | IC50 | 188 | nM | STAUROSPORINE |
| 6.72 | Kd | 189 | nM | SCH-900776 |
| 6.54 | Kd | 284.9 | nM | CHEMBL5653589 |
| 6.49 | ED50 | 327.4 | nM | CHEMBL5653589 |
| 6.46 | Kd | 349 | nM | PF-03758309 |
| 6.46 | Kd | 350 | nM | MILCICLIB |
| 6.44 | Kd | 360 | nM | CHEMBL1241674 |
| 6.40 | Kd | 400 | nM | CHEMBL379218 |
| 6.39 | Kd | 410 | nM | QUIZARTINIB |
| 6.32 | Kd | 483 | nM | CC-401 |
| 6.00 | IC50 | 1000 | nM | TP-030-1 |
| 6.00 | IC50 | 1000 | nM | TP-030-2 |
| 6.00 | IC50 | 1000 | nM | TP-030n |
| 5.96 | Kd | 1105 | nM | BGT-226 FREE BASE |
| 5.77 | Kd | 1700 | nM | BMS-387032 |
| 5.77 | Kd | 1700 | nM | AXITINIB |
| 5.64 | Kd | 2300 | nM | MIDOSTAURIN |
| 5.53 | Kd | 2939 | nM | NMS-1286937 |
| 5.52 | Kd | 3000 | nM | FORETINIB |
| 5.44 | Kd | 3647 | nM | AZD-7762 |
| 5.41 | Kd | 3904 | nM | AXITINIB |
| 5.25 | Kd | 5600 | nM | QUIZARTINIB |
| 5.02 | Kd | 9600 | nM | SORAFENIB |
| 5.01 | Kd | 9700 | nM | FEDRATINIB |
PubChem BioAssay actives
42 with measured affinity, of 392 total; 34 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one | 624738: Binding constant for MLCK kinase domain | kd | 0.0020 | uM |
| [4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone | 624738: Binding constant for MLCK kinase domain | kd | 0.0043 | uM |
| (15S,16S,18R)-16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one | 624738: Binding constant for MLCK kinase domain | kd | 0.0120 | uM |
| N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide | 1425082: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0150 | uM |
| 5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | 1425082: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0200 | uM |
| Sunitinib | 624738: Binding constant for MLCK kinase domain | kd | 0.0230 | uM |
| 2-amino-2-cyclohexyl-N-[2-(1-methylpyrazol-4-yl)-9-oxo-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl]acetamide | 1425082: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0310 | uM |
| 5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-[2-(dimethylamino)acetyl]piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide;hydrochloride | 624738: Binding constant for MLCK kinase domain | kd | 0.0420 | uM |
| methyl (15S,16R,18R)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylate | 1425082: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0980 | uM |
| N-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]pyrrolidine-2-carboxamide | 1425082: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0980 | uM |
| 3-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethylpyrazol-3-yl]phenyl]-1,1-dimethylurea | 1425082: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.1040 | uM |
| N-[2-[4-[[4-(cyclobutylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-11-azatricyclo[6.2.1.02,7]undeca-2(7),3,5-trien-11-yl]-2-oxoethyl]acetamide | 1425082: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.1090 | uM |
| methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate | 624738: Binding constant for MLCK kinase domain | kd | 0.1100 | uM |
| (2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one | 2198335: Inhibition of human MYLK3 using KKRPQRRYSNVF as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by radiometric Hot-SpotSM Kinase assay | ic50 | 0.1180 | uM |
| 1-cyclopropyl-3-[5-[6-(morpholin-4-ylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]urea | 1425082: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.1290 | uM |
| 6-(2,6-dichlorophenyl)-8-methyl-2-(3-methylsulfanylanilino)pyrido[2,3-d]pyrimidin-7-one | 624738: Binding constant for MLCK kinase domain | kd | 0.1400 | uM |
| 3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]amino]ethoxy]ethoxy]ethoxy]ethyl]propanamide | 1526132: Binding affinity to recombinant full-length N-terminal His-FLAG-GST-tagged MYLK3 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay | kd | 0.1460 | uM |
| 6-bromo-3-(1-methylpyrazol-4-yl)-5-[(3R)-piperidin-3-yl]pyrazolo[1,5-a]pyrimidin-7-amine | 1425082: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.1890 | uM |
| 4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | 2148811: Binding affinity to human MYLK3 incubated for 45 mins by Kinobead based pull down assay | kd | 0.2849 | uM |
| N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-1,4-dihydropyrrolo[3,4-d]pyrazole-5-carboxamide | 1425082: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.3490 | uM |
| N,1,4,4-tetramethyl-8-[4-(4-methylpiperazin-1-yl)anilino]-5H-pyrazolo[4,5-h]quinazoline-3-carboxamide | 1425082: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.3500 | uM |
| 2-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol | 624738: Binding constant for MLCK kinase domain | kd | 0.3600 | uM |
| (2S)-1-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]-3-phenylpropan-2-amine | 624738: Binding constant for MLCK kinase domain | kd | 0.4000 | uM |
| Quizartinib | 624738: Binding constant for MLCK kinase domain | kd | 0.4100 | uM |
| 3-[3-(2-piperidin-1-ylethoxy)phenyl]-5-(1H-1,2,4-triazol-5-yl)-1H-indazole | 1425082: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.4830 | uM |
| 8-(6-methoxy-3-pyridinyl)-3-methyl-1-[4-piperazin-1-yl-3-(trifluoromethyl)phenyl]imidazo[4,5-c]quinolin-2-one | 1425082: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 1.1050 | uM |
| N-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-4-carboxamide | 624738: Binding constant for MLCK kinase domain | kd | 1.7000 | uM |
| Axitinib | 624738: Binding constant for MLCK kinase domain | kd | 1.7000 | uM |
| Midostaurin | 624738: Binding constant for MLCK kinase domain | kd | 2.3000 | uM |
| 8-[2-methoxy-5-(4-methylpiperazin-1-yl)anilino]-1-methyl-4,5-dihydropyrazolo[4,5-h]quinazoline-3-carboxamide | 1425082: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 2.9390 | uM |
| 1-N’-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | 624738: Binding constant for MLCK kinase domain | kd | 3.0000 | uM |
| 3-(carbamoylamino)-5-(3-fluorophenyl)-N-[(3S)-piperidin-3-yl]thiophene-2-carboxamide | 1425082: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 3.6470 | uM |
| Sorafenib | 624738: Binding constant for MLCK kinase domain | kd | 9.6000 | uM |
| Fedratinib | 624738: Binding constant for MLCK kinase domain | kd | 9.7000 | uM |
CTD chemical–gene interactions
28 total (human), top 28 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Benzo(a)pyrene | affects methylation, decreases expression, decreases methylation, increases mutagenesis | 4 |
| bisphenol A | decreases methylation, increases expression | 3 |
| Phenylmercuric Acetate | affects cotreatment, increases expression | 2 |
| Valproic Acid | affects expression, increases expression | 2 |
| Aflatoxin B1 | increases methylation, decreases expression | 2 |
| aristolochic acid I | increases expression | 1 |
| Asian ginseng | decreases expression, decreases reaction | 1 |
| hydroxyhydroquinone | decreases expression | 1 |
| sulforaphane | decreases expression | 1 |
| sodium arsenite | affects expression | 1 |
| benzo(e)pyrene | increases methylation | 1 |
| aflatoxin B2 | increases methylation | 1 |
| cyanoginosin LR | increases expression, decreases methylation | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | affects cotreatment, increases expression | 1 |
| abrine | increases expression | 1 |
| dorsomorphin | affects cotreatment, increases expression | 1 |
| theaflavin-3,3’-digallate | affects expression | 1 |
| Resveratrol | affects cotreatment, decreases expression | 1 |
| Copper | affects cotreatment, decreases expression | 1 |
| Diazinon | increases methylation | 1 |
| Diethylhexyl Phthalate | decreases expression, decreases reaction | 1 |
| Estradiol | increases expression, affects binding | 1 |
| Methapyrilene | increases methylation | 1 |
| Triclosan | decreases expression | 1 |
| Asbestos, Serpentine | decreases methylation | 1 |
| Asbestos, Crocidolite | decreases methylation | 1 |
| Asbestos, Amosite | decreases methylation | 1 |
| Nanotubes, Carbon | decreases expression | 1 |
ChEMBL screening assays
95 unique, capped per target: 95 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1908435 | Binding | Binding constant for MLCK kinase domain | Comprehensive analysis of kinase inhibitor selectivity. — Nat Biotechnol |
Cellosaurus cell lines
5 cell lines: 5 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_E0IP | Ubigene HeLa MYLK3 KO | Cancer cell line | Female |
| CVCL_SZ62 | HAP1 MYLK3 (-) 1 | Cancer cell line | Male |
| CVCL_SZ63 | HAP1 MYLK3 (-) 2 | Cancer cell line | Male |
| CVCL_SZ64 | HAP1 MYLK3 (-) 3 | Cancer cell line | Male |
| CVCL_SZ65 | HAP1 MYLK3 (-) 4 | Cancer cell line | Male |
Clinical trials (associated diseases)
158 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00374465 | PHASE4 | UNKNOWN | Therapy With Verapamil or Carvedilol in Chronic Heart Failure |
| NCT01293903 | PHASE4 | COMPLETED | Study of Qiliqiangxin Capsule to Treat Dilated Cardiomyopathy |
| NCT01557140 | PHASE4 | COMPLETED | A Randomized Trial of Carvedilol in Chronic Chagas Cardiomyopathy |
| NCT01917149 | PHASE4 | COMPLETED | Supramaximal Titrated Inhibition of RAAS in Dilated Cardiomyopathy |
| NCT02115581 | PHASE4 | COMPLETED | Coenzyme Q10 Supplementation in Children With Idiopathic Dilated Cardiomyopathy |
| NCT06236022 | PHASE4 | RECRUITING | The Effects of Sirolimus in Patients With Dilated Cardiomyopathy Infected With Kaposi Sarcoma-associated Virus |
| NCT00333827 | PHASE3 | COMPLETED | Cell Therapy In Dilated Cardiomyopathy |
| NCT00505154 | PHASE3 | COMPLETED | Effect of Rosuvastatin on Left Ventricular Remodeling |
| NCT01223703 | PHASE3 | COMPLETED | PUFAs and Left Ventricular Function in Heart Failure |
| NCT01583114 | PHASE3 | TERMINATED | PREclinical Mutation CARriers From Families With DIlated Cardiomyopathy and ACE Inhibitors |
| NCT01914081 | PHASE3 | UNKNOWN | Resveratrol: A Potential Anti- Remodeling Agent in Heart Failure, From Bench to Bedside |
| NCT02989181 | PHASE3 | UNKNOWN | Continues Positive Airway Pressure Treatment for Patients With Dilated Cardiomyopathy and Obstructive Sleep Apnea |
| NCT03439514 | PHASE3 | TERMINATED | A Study of ARRY-371797 (PF-07265803) in Patients With Symptomatic Dilated Cardiomyopathy Due to a Lamin A/C Gene Mutation |
| NCT05237323 | PHASE3 | COMPLETED | Micophenolate Mofetil Versus Azathioprine in Myocarditis |
| NCT05849766 | PHASE3 | COMPLETED | Effect of Dapagliflozin on Cardiac Structure, Function and Secondary Mitral Regurgitation in Patients with Left Ventricle Dysfunction |
| NCT06250257 | PHASE3 | RECRUITING | Bromocriptine in Dilated Cardiomyopathy Among Women of Reproductive Age |
| NCT00629018 | PHASE2 | COMPLETED | Safety and Efficacy Study of Stem Cell Transplantation to Treat Dilated Cardiomyopathy |
| NCT00629096 | PHASE2 | COMPLETED | Intracoronary Infusion of Autologous Bone Marrow Cells for Treatment of Idiopathic Dilated Cardiomyopathy |
| NCT00765518 | PHASE2 | COMPLETED | Use of Ixmyelocel-T (Formerly Cardiac Repair Cell [CRC] Treatment) in Patients With Heart Failure Due to Dilated Cardiomyopathy (IMPACT-DCM) |
| NCT00847964 | PHASE2 | COMPLETED | Safety and Feasibility of Algisyl-LVR™ as a Method of Left Ventricular Restoration in Patients With DCM Undergoing Open-heart Surgery |
| NCT01020968 | PHASE2 | COMPLETED | Use of Ixmyelocel-T (Formerly Catheter-based Cardiac Repair Cell [CRC]) Treatment in Patients With Heart Failure Due to Dilated Cardiomyopathy |
| NCT01302171 | PHASE2 | COMPLETED | Bone Marrow Derived Adult Stem Cells for Dilated Cardiomyopathy |
| NCT01350310 | PHASE2 | COMPLETED | Safety and Efficacy Study of Intramyocardial Stem Cell Therapy in Patients With Dilated Cardiomyopathy |
| NCT02133911 | PHASE2 | COMPLETED | A Pilot Trial of Ranolazine to Treat Patients With Dilated Cardiomyopathy |
| NCT03071653 | PHASE2 | SUSPENDED | Left Cardiac Sympathetic Denervation for Cardiomyopathy Feasibility Pilot Study |
| NCT03572660 | PHASE2 | ACTIVE_NOT_RECRUITING | Use of Bone Marrow Derived Stem Cell and G-CSF With Circulatory Assistance in the Treatment of DCM |
| NCT03775070 | PHASE2 | COMPLETED | Simvastatin Therapy in Patients With Dilated Cardiomyopathy. |
| NCT04405804 | PHASE2 | UNKNOWN | Early Administration of Ivabradine in Children With Heart Failure |
| NCT05410873 | PHASE2 | COMPLETED | Examining the Effects of Mitochondrial Oxidative Stress in DCM |
| NCT06632834 | PHASE2 | RECRUITING | Outcome-targeted Therapy: Principle and Outcome Evaluation: Clinical Study and Phenotype-genotype Correlation |
| NCT00585546 | PHASE1 | TERMINATED | Harefield Recovery Protocol Study for Patients With Refractory Chronic Heart Failure |
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Related Atlas pages
- Associated diseases: dilated cardiomyopathy
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): dilated cardiomyopathy, familial dilated cardiomyopathy, Parkinson disease 17