MKNK1

Summary

MKNK1 (MAPK interacting serine/threonine kinase 1, HGNC:7110) is a protein-coding gene on chromosome 1p33, encoding MAP kinase-interacting serine/threonine-protein kinase 1 (Q9BUB5). May play a role in the response to environmental stress and cytokines.

This gene encodes a Ser/Thr protein kinase that interacts with, and is activated by ERK1 and p38 mitogen-activated protein kinases, and thus may play a role in the response to environmental stress and cytokines. This kinase may also regulate transcription by phosphorylating eIF4E via interaction with the C-terminal region of eIF4G. Alternatively spliced transcript variants have been noted for this gene.

Source: NCBI Gene 8569 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 74 total
• Druggable target: yes — 25 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001135553

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:7110
Approved symbol	MKNK1
Name	MAPK interacting serine/threonine kinase 1
Location	1p33
Locus type	gene with protein product
Status	Approved
Aliases	MNK1
Ensembl gene	ENSG00000079277
Ensembl biotype	protein_coding
OMIM	606724
Entrez	8569

Gene structure

Transcript identifiers

Ensembl transcripts: 75 — 58 protein_coding, 8 retained_intron, 6 protein_coding_CDS_not_defined, 3 nonsense_mediated_decay

ENST00000341183, ENST00000342571, ENST00000371945, ENST00000371946, ENST00000428112, ENST00000460098, ENST00000465783, ENST00000468852, ENST00000470237, ENST00000474868, ENST00000477883, ENST00000480531, ENST00000484301, ENST00000486716, ENST00000496619, ENST00000524417, ENST00000524749, ENST00000525888, ENST00000526513, ENST00000528077, ENST00000528237, ENST00000529170, ENST00000530528, ENST00000531355, ENST00000531769, ENST00000532110, ENST00000532783, ENST00000532897, ENST00000649800, ENST00000650026, ENST00000650508, ENST00000898407, ENST00000898408, ENST00000898409, ENST00000898410, ENST00000898411, ENST00000898412, ENST00000898413, ENST00000898414, ENST00000898415, ENST00000898416, ENST00000898417, ENST00000898418, ENST00000898419, ENST00000898420, ENST00000898421, ENST00000898422, ENST00000898423, ENST00000898424, ENST00000898425, ENST00000898426, ENST00000898427, ENST00000898428, ENST00000940352, ENST00000940353, ENST00000940354, ENST00000940355, ENST00000967056, ENST00000967057, ENST00000967058, ENST00000967059, ENST00000967060, ENST00000967061, ENST00000967062, ENST00000967063, ENST00000967064, ENST00000967065, ENST00000967066, ENST00000967067, ENST00000967068, ENST00000967069, ENST00000967070, ENST00000967071, ENST00000967072, ENST00000967073

RefSeq mRNA: 11 — MANE Select: NM_001135553 NM_001135553, NM_001377337, NM_001377338, NM_001377341, NM_001377342, NM_001377343, NM_001377373, NM_001377374, NM_001377375, NM_003684, NM_198973

CCDS: CCDS30705, CCDS44134, CCDS538

Canonical transcript exons

ENST00000371945 — 13 exons

Exon	Start	End
ENSE00002173866	46604185	46604268
ENSE00003471601	46574947	46575020
ENSE00003476480	46594113	46594280
ENSE00003501932	46561478	46561642
ENSE00003517498	46580530	46580627
ENSE00003580019	46560234	46560277
ENSE00003580253	46576575	46576654
ENSE00003581084	46562649	46562843
ENSE00003583480	46565041	46565136
ENSE00003657056	46572063	46572167
ENSE00003676067	46557407	46558800
ENSE00003784111	46568443	46568498
ENSE00003834184	46583228	46583329

Expression profiles

Bgee: expression breadth ubiquitous, 289 present calls, max score 99.12.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 21.4987 / max 282.1950, expressed in 1815 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
12184	15.4049	1807
12186	2.7879	911
12187	2.7165	1319
12185	0.5895	340

Top tissues by expression

294 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
body of pancreas	UBERON:0001150	99.12	gold quality
spleen	UBERON:0002106	96.32	gold quality
descending thoracic aorta	UBERON:0002345	96.26	gold quality
blood	UBERON:0000178	96.15	gold quality
mucosa of stomach	UBERON:0001199	95.79	gold quality
secondary oocyte	CL:0000655	95.66	gold quality
muscle layer of sigmoid colon	UBERON:0035805	95.60	gold quality
right coronary artery	UBERON:0001625	95.54	gold quality
monocyte	CL:0000576	95.35	gold quality
upper lobe of left lung	UBERON:0008952	95.35	gold quality
tibial nerve	UBERON:0001323	95.25	gold quality
granulocyte	CL:0000094	95.23	gold quality
mononuclear cell	CL:0000842	95.23	gold quality
thoracic aorta	UBERON:0001515	95.19	gold quality
apex of heart	UBERON:0002098	95.18	gold quality
ascending aorta	UBERON:0001496	95.15	gold quality
right lung	UBERON:0002167	95.10	gold quality
small intestine Peyer’s patch	UBERON:0003454	95.00	gold quality
omental fat pad	UBERON:0010414	94.92	gold quality
leukocyte	CL:0000738	94.87	gold quality
peritoneum	UBERON:0002358	94.87	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	94.83	gold quality
upper lobe of lung	UBERON:0008948	94.78	gold quality
sural nerve	UBERON:0015488	94.78	gold quality
transverse colon	UBERON:0001157	94.71	gold quality
right atrium auricular region	UBERON:0006631	94.58	gold quality
adipose tissue of abdominal region	UBERON:0007808	94.58	gold quality
pancreas	UBERON:0001264	94.57	gold quality
right uterine tube	UBERON:0001302	94.50	gold quality
body of stomach	UBERON:0001161	94.45	gold quality

Single-cell (SCXA)

Detected in 6 experiment(s), a significant marker in 4.

Experiment	Marker?	Max mean expression
E-MTAB-6701	yes	42.92
E-ANND-3	yes	16.74
E-HCAD-25	yes	16.33
E-MTAB-6678	yes	10.96
E-MTAB-6386	no	170.66
E-GEOD-100618	no	134.42

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

55 targeting MKNK1, 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-568	99.98	69.86	2084
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-497-5P	99.92	71.83	2674
HSA-MIR-498-3P	99.91	71.27	1114
HSA-MIR-15A-5P	99.90	72.80	2787
HSA-MIR-15B-5P	99.90	72.78	2798
HSA-MIR-16-5P	99.90	72.80	2780
HSA-MIR-195-5P	99.90	72.81	2805
HSA-MIR-345-3P	99.89	70.23	1421
HSA-MIR-424-5P	99.89	71.90	2641
HSA-MIR-6838-5P	99.89	71.94	2690
HSA-MIR-30A-3P	99.87	69.74	2928
HSA-MIR-30D-3P	99.87	69.92	2917
HSA-MIR-30E-3P	99.87	69.68	2942
HSA-MIR-4319	99.76	69.83	2586
HSA-MIR-1200	99.71	70.42	1838
HSA-MIR-518A-5P	99.70	69.01	2209
HSA-MIR-527	99.70	69.01	2209
HSA-MIR-379-3P	99.69	69.60	1524
HSA-MIR-411-3P	99.69	69.63	1524
HSA-MIR-670-5P	99.67	69.94	1565
HSA-MIR-10394-5P	99.65	66.83	1852
HSA-MIR-1205	99.65	66.76	1826
HSA-MIR-378A-5P	99.65	66.33	1311
HSA-MIR-4499	99.62	67.29	1470
HSA-MIR-4328	99.57	71.06	4094
HSA-MIR-4524A-5P	99.57	71.73	1193
HSA-MIR-4524B-5P	99.57	71.68	1195
HSA-MIR-5584-5P	99.49	68.22	2814
HSA-MIR-3140-5P	99.39	69.04	1136

Literature-anchored findings (GeneRIF, showing 40)

• Adenovirus 100K protein blocks cellular protein synthesis by coopting eIF4G and cap-initiation complexes and displacing or blocking binding by Mnk1, which occurs only on preassembled complexes, resulting in dephosphorylation of eIF4E. (PMID:15220445)
• Mnk1 phosphorylation by caspase-activated Pak2/gamma-PAK inhibits phosphorylation and interaction of eIF4G with Mnk (PMID:15234964)
• role for MNK1 in the AML fusion protein-associated differentiation block (PMID:15516979)
• Interleukins 2 and 15 regulate Ets1 expression via ERK1/2 and MNK1 in human natural killer cells (PMID:15563472)
• Data show that Mnk1 suppression decreases eukaryotic initiation factor 4F phosphorylation without causing any change in global protein synthesis rate and cell proliferation. (PMID:15581611)
• Mnk1-mediated serine phosphorylation of Spry2 constitutes a regulatory mechanism to extend the temporal range of Spry2 activity. (PMID:16479008)
• Data show that inorganic phosphate controls cell growth by activating ERK1/2 cascades and by facilitating the translocation of Mnk1 from cytosol into nucleus through an Akt-mediated MEK pathway. (PMID:16763222)
• The activity of MKNK1 was characterized. (PMID:17590453)
• mTOR inhibition increases eIF4E phosphorylation through a PI3K-dependent and Mnk-mediated mechanism. (PMID:17724079)
• A conserved phenylalanine residue in an Mnk-specific insert is playing a key role in governing the ease with which Mnk1a can be phosphorylated. (PMID:19650764)
• Data suggest that a proportion of breast cancers could be sensitive to inhibiting MNK kinase activity, and that the presence of phosphorylated eIF4E could provide a biomarker for the identification of responsive tumours. (PMID:20686366)
• siRNA-mediated Mnk1/2 knockdown results in partial reversal of the suppressive effects of IFNgamma on human CD34+-derived myeloid (CFU-GM) and erythroid (BFU-E) progenitors. (PMID:21149447)
• Findings offer insights into how MNK1 pathways control translation of cancer-related mRNAs including SMAD2, a key component of the TGF-beta signaling pathway. (PMID:21406405)
• Data show that PKCalpha activation elicits a cascade of orchestrated phosphorylation events that may modulate eIF4G1 structure and control interaction with the eIF4E kinase, Mnk1. (PMID:21576361)
• These data suggest that MNK1 regulates the phosphorylation and the subcellular distribution of hnRNP A1 and that MNK1 may play a role in the induction of senescence (PMID:22227431)
• Resistance to trastuzumab was observed in tumor cells with elevated MNK1 expression, furthermore, inhibition of RSK1 restored sensitivity to resistant cells. (PMID:22249268)
• MNK1 kinase activity is required for abscission. (PMID:22454512)
• TGFbeta induces signaling involving PI3kinase-dependent Mnk-1-mediated phosphorylation of eIF4E at Ser-209 to facilitate mesangial cell hypertrophy. A role for dissociation of 4EBP-1-eIF4E complex for Mnk-1-mediated phosphorylation of eIF4E. (PMID:23359369)
• Chemical inhibition or siRNA knockdown of MKNK1 significantly impaired entry of genotype 1a hepatitis C virus in Huh-7 cells but had only minimal impact on viral RNA replication or cell proliferation and viability. (PMID:23365451)
• MNK1, which participates in translational control in several cell types, is activated in response to physiological neutrophil agonists (LPS, TNF-alpha) in the cytoplasmic and nuclear compartments. (PMID:23401599)
• Our findings identify the MNK-eIF4E axis as a specific and critical regulator of blast crisis self-renewal, and suggest that pharmacologic inhibition of the MNK kinases may be therapeutically useful in BC chronic myeloid leukemia. (PMID:23737503)
• These findings provide evidence for key and essential roles of the Mnk kinase pathway in the generation of the antineoplastic effects of type I IFNs in Jak2V617F-dependent myeloproliferative neoplasms. (PMID:23814052)
• rapalog-activated MNK1 signaling promotes glioma growth through regulation of 4EBP1; there is a molecular cross-talk between the mTORC1 and MNK1 pathways (PMID:24401275)
• High expression of p-Mnk1 and p-eIF4E might be novel valuable biomarkers to predict poor prognosis of nasopharyngeal carcinoma. (PMID:24551240)
• Authors show that MNK regulates SRPK via mTOR and AKT. (PMID:25187540)
• ERK1/2 signal induced MNK catalytic activity enabled enterovirus type 1 internal ribosomal entry site-mediated translation/host cell cytotoxicity through negative regulation of the Ser/Arg (SR)-rich protein kinase (SRPK). (PMID:25187541)
• MNK1 and MNK2 inhibition ablates eIF4E1 phosphorylation and concurrently enhances eIF4E3 expression in diffuse large B-cell lymphoma. (PMID:25403230)
• Data suggest that a combined pharmacologic inhibition of mTORC1 and Mnk1/2 kinases offers a therapeutic opportunity in blast crisis-chronic myeloid leukemia (BC-CML). (PMID:25527453)
• Simultaneous targeting of androgen receptor and MNK1 by novel retinamides inhibits growth of human prostate cancer cell lines. (PMID:25605250)
• Data show that interferon-gamma regulated the metabolism and mRNA translation of macrophages by targeting the kinases mTORC1 and MNK1/2, both of which converge on the selective regulator of translation initiation eukaryotic initiation factor-4E (eIF4E). (PMID:26147685)
• Data suggest MNK1/MNK2 stimulate mRNA translation but only of mRNA containing both 5-prime-terminal cap and hairpin duplex; this stimulation involves up-regulation of phosphorylation/mRNA un-winding activity of eIF4E (via decreased binding to eIF4G). (PMID:26668315)
• MNK1 encodes a Ser/Thr protein kinase that interacts with extracellular signal-regulated kinase 1 and p38 mitogen-activated protein kinase, a pathway that is involved in Blood Pressure regulation through norepinephrine and angiotensin II. (PMID:27271309)
• data suggest a physiological role for MNK1a-Ser(353) phosphorylation in regulation of the MNK1a kinase, which correlates with increased eIF4E phosphorylation in vitro and in vivo. (PMID:27413184)
• MNK-1 controls chemokine secretion and proliferation in human airway smooth muscle cells. (PMID:27418099)
• Data show that galeterone (gal) and VNPT55 inhibit migration and invasion of prostate cancer cells, possibly by down-regulating protein expression via antagonizing the Mnk1/2-eIF4E axis. (PMID:27618366)
• Elevated levels of p-Mnk1, p-eIF4E and p-p70S6K proteins are associated with tumor recurrence and poor prognosis in astrocytomas. Overexpression of p-eIF4E and co-expression of p-Mnk1, p-eIF4E and p-p70S6K proteins could be used as novel independent poor prognostic biomarkers for patients with astrocytomas. (PMID:27900644)
• High MNK1 expression in epithelial ovarian cancer tissues indicates poor clinical outcomes (PMID:28332091)
• these data show that NDRG1 is regulated by the oncogenic MAP kinase-interacting kinase pathway, a target for cancer therapy (PMID:28545025)
• In GBM cells, ATO-activated translation initiation cellular events via the MNK1-eIF4E signaling axis. (PMID:29042487)
• MKNK1 polymorphism was associated with treatment response in metastatic colorectal cancer. (PMID:29045529)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	si:ch73-60h1.1	ENSDARG00000078504
mus_musculus	Mknk1	ENSMUSG00000028708
caenorhabditis_elegans		WBGENE00007007

Paralogs (6): DCX (ENSG00000077279), MAPKAPK5 (ENSG00000089022), MKNK2 (ENSG00000099875), MAPKAPK3 (ENSG00000114738), CAMK4 (ENSG00000152495), MAPKAPK2 (ENSG00000162889)

Protein

Protein identifiers

MAP kinase-interacting serine/threonine-protein kinase 1 — Q9BUB5 (reviewed: Q9BUB5)

Alternative names: MAP kinase signal-integrating kinase 1

All UniProt accessions (14): Q9BUB5, A0A499FIS5, A0A499FJN1, A0A499FJS1, E9PIA0, E9PII5, E9PLE7, E9PMM8, E9PN34, E9PQ26, E9PSC9, E9PSE0, H0YE67, Q7Z319

UniProt curated annotations — full annotation on UniProt →

Function. May play a role in the response to environmental stress and cytokines. Appears to regulate translation by phosphorylating EIF4E, thus increasing the affinity of this protein for the 7-methylguanosine-containing mRNA cap.

Subunit / interactions. Interacts with the C-terminal regions of EIF4G1 and EIF4G2. Also binds to dephosphorylated ERK1 and ERK2, and to the p38 kinases.

Subcellular location. Cytoplasm Cytoplasm. Nucleus.

Tissue specificity. Ubiquitous.

Post-translational modifications. Dual phosphorylation of Thr-250 and Thr-255 activates the kinase. Phosphorylation of Thr-385 activates the kinase. MAPK3/ERK1 is one of the kinases which activate MKNK1/MNK1. Phosphorylation by PAK2 leads to a reduced phosphorylation of EIF4G1.

Activity regulation. Phosphorylated and activated by the p38 kinases and kinases in the Erk pathway.

Similarity. Belongs to the protein kinase superfamily. CAMK Ser/Thr protein kinase family.

Isoforms (3)

UniProt ID	Names	Canonical?
Q9BUB5-1	1	yes
Q9BUB5-2	2, MNK1a
Q9BUB5-3	3, MNK1b

RefSeq proteins (11): NP_001129025, NP_001364266, NP_001364267, NP_001364270, NP_001364271, NP_001364272, NP_001364302, NP_001364303, NP_001364304, NP_003675, NP_945324 (=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
IPR050205	CDPK_Ser/Thr_kinases	Family

Pfam: PF00069

Catalyzed reactions (Rhea), 2 shown:

• L-seryl-[protein] + ATP = O-phospho-L-seryl-[protein] + ADP + H(+) (RHEA:17989)
• L-threonyl-[protein] + ATP = O-phospho-L-threonyl-[protein] + ADP + H(+) (RHEA:46608)

UniProt features (52 total): helix 11, strand 9, modified residue 7, mutagenesis site 5, sequence variant 4, region of interest 3, turn 3, compositionally biased region 3, binding site 2, splice variant 2, chain 1, domain 1, active site 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
2Y9Q	X-RAY DIFFRACTION	1.55
2HW6	X-RAY DIFFRACTION	2.5
5WVD	X-RAY DIFFRACTION	3

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9BUB5-F1	71.14	0.42

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): 211 (proton acceptor)

Ligand- & substrate-binding residues (2): 78; 55–63

Post-translational modifications (7): 39, 221, 226, 250, 255, 385, 460

Mutagenesis-validated functional residues (5):

Position	Phenotype
78	loss of kinase activity; when associated with d-232.
232	loss of kinase activity; when associated with k-78.
250	loss of kinase activity; when associated with t-255.
255	loss of kinase activity; when associated with t-250.
385	constitutively active.

Function

Pathways and Gene Ontology

Reactome pathways

12 pathways

ID	Pathway
R-HSA-1295596	Spry regulation of FGF signaling
R-HSA-162582	Signal Transduction
R-HSA-190236	Signaling by FGFR
R-HSA-5654726	Negative regulation of FGFR1 signaling
R-HSA-5654727	Negative regulation of FGFR2 signaling
R-HSA-5654732	Negative regulation of FGFR3 signaling
R-HSA-5654733	Negative regulation of FGFR4 signaling
R-HSA-5654736	Signaling by FGFR1
R-HSA-5654738	Signaling by FGFR2
R-HSA-5654741	Signaling by FGFR3
R-HSA-5654743	Signaling by FGFR4
R-HSA-9006934	Signaling by Receptor Tyrosine Kinases

MSigDB gene sets: 213 (showing top): GRUETZMANN_PANCREATIC_CANCER_DN, KEGG_MAPK_SIGNALING_PATHWAY, MODULE_45, REACTOME_SIGNALING_BY_FGFR, AAGCCAT_MIR135A_MIR135B, GRAESSMANN_RESPONSE_TO_MC_AND_SERUM_DEPRIVATION_DN, GOBP_TRANSLATION, GOBP_POST_TRANSCRIPTIONAL_REGULATION_OF_GENE_EXPRESSION, RICKMAN_TUMOR_DIFFERENTIATED_WELL_VS_POORLY_DN, LIAO_METASTASIS, BIOCARTA_MAPK_PATHWAY, TATA_C, NUMATA_CSF3_SIGNALING_VIA_STAT3, LASTOWSKA_NEUROBLASTOMA_COPY_NUMBER_DN, ZHAN_EARLY_DIFFERENTIATION_GENES_DN

GO Biological Process (3): regulation of translation (GO:0006417), protein phosphorylation (GO:0006468), intracellular signal transduction (GO:0035556)

GO Molecular Function (12): protein serine/threonine kinase activity (GO:0004674), calcium/calmodulin-dependent protein kinase activity (GO:0004683), calmodulin binding (GO:0005516), ATP binding (GO:0005524), calcium-dependent protein serine/threonine kinase activity (GO:0009931), metal ion binding (GO:0046872), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (4): nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytosol (GO:0005829)

Reactome top-level categories

Rollup of top-11 pathways:

Category	Pathways
Signaling by FGFR	4
Negative regulation of FGFR1 signaling	1
Negative regulation of FGFR2 signaling	1
Negative regulation of FGFR3 signaling	1
Negative regulation of FGFR4 signaling	1
Signaling by Receptor Tyrosine Kinases	1
Signaling by FGFR1	1
Signaling by FGFR2	1
Signaling by FGFR3	1
Signaling by FGFR4	1
Signal Transduction	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
intracellular anatomical structure	2
protein kinase activity	2
protein serine/threonine kinase activity	2
translation	1
post-transcriptional regulation of gene expression	1
regulation of protein metabolic process	1
phosphorylation	1
protein modification process	1
signal transduction	1
protein binding	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
cation 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
binding	1
transferase activity, transferring phosphorus-containing groups	1
catalytic activity	1
intracellular membrane-bounded organelle	1
nuclear lumen	1
cytoplasm	1

Protein interactions and networks

STRING

1112 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
MKNK1	EIF4G1	Q04637	984
MKNK1	EIF4E	P06730	948
MKNK1	EIF4A2	Q14240	929
MKNK1	EIF4A1	P04765	928
MKNK1	EIF4G2	P78344	877
MKNK1	ATP7A	Q04656	841
MKNK1	KNCN	A6PVL3	805
MKNK1	EIF4G3	O43432	768
MKNK1	PABPC1	P11940	721
MKNK1	ATOX1	O00244	591
MKNK1	EIF4EBP2	Q13542	576
MKNK1	MAPK1	P28482	558
MKNK1	EIF3E	P60228	534
MKNK1	MAP2K1	Q02750	526
MKNK1	IPO7	O95373	515

IntAct

203 interactions, top by confidence:

A	B	Type	Score
MAPK1	MKNK1	psi-mi:“MI:0915”(physical association)	0.820
MAPK14	MAP2K3	psi-mi:“MI:0914”(association)	0.800
MAPK14	OBSL1	psi-mi:“MI:0914”(association)	0.790
CREM	MKNK1	psi-mi:“MI:0915”(physical association)	0.560
MKNK1		psi-mi:“MI:0915”(physical association)	0.560
OPTN	MKNK1	psi-mi:“MI:0915”(physical association)	0.560
HTT	MKNK1	psi-mi:“MI:0915”(physical association)	0.560
ATXN1	MKNK1	psi-mi:“MI:0915”(physical association)	0.560

BioGRID (98): MKNK1 (Affinity Capture-RNA), MKNK1 (Affinity Capture-MS), MKNK1 (Affinity Capture-MS), MKNK1 (Affinity Capture-MS), MKNK1 (Affinity Capture-MS), MKNK1 (Affinity Capture-MS), MKNK1 (Affinity Capture-MS), MKNK1 (Affinity Capture-MS), MKNK1 (Affinity Capture-MS), MKNK1 (Affinity Capture-MS), MKNK1 (Affinity Capture-MS), MKNK1 (Affinity Capture-MS), MKNK1 (Affinity Capture-MS), MKNK1 (Affinity Capture-MS), MKNK1 (Affinity Capture-MS)

ESM2 similar proteins: A2YBX5, B1WAR9, B5X564, F4I114, F4I4F2, F4ICB6, F4J394, O13839, P15792, P25341, P83101, Q05999, Q09831, Q0DCT8, Q0PKV7, Q17QV9, Q1PFB9, Q39183, Q4R7T5, Q5R667, Q5U2N4, Q5XIT0, Q63553, Q64FQ2, Q66I46, Q6DBX4, Q6NTJ3, Q6P431, Q6UDG0, Q7T0B0, Q7TNL3, Q7TSJ6, Q8CDB0, Q8N2I9, Q8VDU5, Q8W490, Q922Y0, Q924X7, Q9BUB5, Q9BYT3

Diamond homologs: A0A509AFG4, A0A509AQE6, A0A5K1K8H0, A2ZVI7, D2I3C6, O08605, O15075, O15865, O54992, O75582, O75676, O77708, P08413, P10665, P11275, P11798, P11801, P15791, P18652, P18653, P18654, P25323, P28582, P28652, P49137, P49138, P49139, P51812, P53683, P62345, Q06850, Q0V7M1, Q13554, Q13557, Q15349, Q15418, Q16644, Q18846, Q2HJF7, Q38868

SIGNOR signaling

23 interactions.

A	Effect	B	Mechanism
MKNK1	up-regulates	EIF4E	phosphorylation
PPP2CA	down-regulates	MKNK1	dephosphorylation
MKNK1	down-regulates	SPRY2	phosphorylation
MKNK1	“up-regulates activity”	PLA2G4A	phosphorylation
PAK2	“down-regulates activity”	MKNK1	phosphorylation
ERK1/2	“up-regulates activity”	MKNK1	phosphorylation
Tomivosertib	“down-regulates activity”	MKNK1	“chemical inhibition”
Gbeta	up-regulates	MKNK1	phosphorylation
MAPK1	up-regulates	MKNK1	phosphorylation
MAPK14	“up-regulates activity”	MKNK1	phosphorylation
MAPK14	up-regulates	MKNK1	phosphorylation
MAPK3	up-regulates	MKNK1	phosphorylation
MAPK3	“up-regulates activity”	MKNK1	phosphorylation
MKNK1	“up-regulates activity”	PNPLA8	phosphorylation
SGK1	“down-regulates activity”	MKNK1	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 119 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.

Reactome pathways:

Pathway	Partners	Fold	FDR
Ras activation upon Ca2+ influx through NMDA receptor	5	34.4×	3e-05
Unblocking of NMDA receptors, glutamate binding and activation	5	32.8×	3e-05
Negative regulation of NMDA receptor-mediated neuronal transmission	5	32.8×	3e-05
Assembly and cell surface presentation of NMDA receptors	10	30.6×	2e-10
Dopamine Neurotransmitter Release Cycle	5	29.9×	5e-05
Long-term potentiation	5	28.7×	5e-05
Neurexins and neuroligins	11	26.1×	2e-10
Protein-protein interactions at synapses	7	22.4×	4e-06

GO biological processes:

GO term	Partners	Fold	FDR
establishment or maintenance of epithelial cell apical/basal polarity	10	51.0×	2e-12
protein localization to synapse	6	40.3×	1e-06
receptor clustering	7	38.3×	2e-07
regulation of postsynaptic membrane neurotransmitter receptor levels	7	30.4×	7e-07
bicellular tight junction assembly	5	14.5×	1e-03
Golgi organization	8	9.4×	2e-04
protein-containing complex assembly	9	9.0×	6e-05
cell-cell adhesion	10	8.9×	2e-05

Disease & clinical

Clinical variants and AI predictions

ClinVar

74 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	50
Likely benign	4
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

3238 predictions. Top by Δscore:

Variant	Effect	Δscore
1:46558796:TGTTC:T	acceptor_gain	1.0000
1:46558798:TTC:T	acceptor_gain	1.0000
1:46558799:TC:T	acceptor_gain	1.0000
1:46558799:TCC:T	acceptor_loss	1.0000
1:46558800:CC:C	acceptor_gain	1.0000
1:46558801:C:CA	acceptor_loss	1.0000
1:46558801:C:CC	acceptor_gain	1.0000
1:46558802:T:G	acceptor_loss	1.0000
1:46558810:C:CT	acceptor_gain	1.0000
1:46558811:A:T	acceptor_gain	1.0000
1:46562844:C:CC	acceptor_gain	1.0000
1:46565036:CGTA:C	donor_gain	1.0000
1:46565037:GTA:G	donor_loss	1.0000
1:46565038:TACTG:T	donor_loss	1.0000
1:46565039:A:AC	donor_gain	1.0000
1:46565039:ACT:A	donor_loss	1.0000
1:46565040:C:CC	donor_gain	1.0000
1:46565040:CT:C	donor_gain	1.0000
1:46565040:CTGG:C	donor_gain	1.0000
1:46565134:CAC:C	acceptor_gain	1.0000
1:46565136:CCT:C	acceptor_loss	1.0000
1:46565137:C:CA	acceptor_loss	1.0000
1:46565137:C:CC	acceptor_gain	1.0000
1:46580528:A:AC	donor_gain	1.0000
1:46580529:C:CC	donor_gain	1.0000
1:46583238:T:A	donor_gain	1.0000
1:46594280:CCT:C	acceptor_gain	1.0000
1:46594281:C:CC	acceptor_gain	1.0000
1:46594282:T:C	acceptor_gain	1.0000
1:46594282:T:TC	acceptor_gain	1.0000

AlphaMissense

2711 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
1:46562818:G:T	P265H	1.000
1:46565113:G:C	D232E	1.000
1:46565113:G:T	D232E	1.000
1:46565114:T:A	D232V	1.000
1:46580534:A:T	V77D	1.000
1:46561489:A:G	W373R	0.999
1:46561489:A:T	W373R	0.999
1:46561520:T:A	R362S	0.999
1:46561520:T:G	R362S	0.999
1:46561521:C:G	R362T	0.999
1:46561545:A:G	L354P	0.999
1:46561557:A:G	L350P	0.999
1:46562663:A:G	C317R	0.999
1:46562709:G:C	F301L	0.999
1:46562709:G:T	F301L	0.999
1:46562711:A:G	F301L	0.999
1:46562722:C:A	G297V	0.999
1:46562722:C:T	G297D	0.999
1:46562749:C:T	G288D	0.999
1:46562750:C:G	G288R	0.999
1:46562754:G:C	S286R	0.999
1:46562754:G:T	S286R	0.999
1:46562756:T:G	S286R	0.999
1:46562757:C:A	W285C	0.999
1:46562757:C:G	W285C	0.999
1:46562759:A:G	W285R	0.999
1:46562759:A:T	W285R	0.999
1:46562764:T:A	D283V	0.999
1:46562799:G:C	F271L	0.999
1:46562799:G:T	F271L	0.999

dbSNP variants (sampled 300 via entrez): RS1000001941 (1:46591819 G>A), RS1000097993 (1:46575779 C>T), RS1000178619 (1:46584974 G>A), RS1000252703 (1:46578324 G>A,T), RS1000349808 (1:46603460 C>T), RS1000362072 (1:46584335 T>C), RS1000507172 (1:46564292 G>C), RS1000530246 (1:46575897 G>A,T), RS1000588784 (1:46577485 T>A), RS1000659346 (1:46565384 T>G), RS1000697590 (1:46582663 C>T), RS1000771131 (1:46578598 T>TG), RS1000781505 (1:46597272 A>G), RS1000791951 (1:46583128 C>T), RS1000862996 (1:46596254 T>A)

Disease associations

OMIM: gene MIM:606724 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST003050_19	Schizophrenia	2.000000e-06
GCST008150_1	Triglyceride levels	7.000000e-06

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0004530	triglyceride measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (3): CHEMBL3883293 (PROTEIN FAMILY), CHEMBL4718 (SINGLE PROTEIN), CHEMBL6195540 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

25 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 501,385 (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
CHEMBL1173655	AFATINIB	4	15,144
CHEMBL1287853	FEDRATINIB	4	3,554
CHEMBL1336	SORAFENIB	4	86,060
CHEMBL24828	VANDETANIB	4	42,230
CHEMBL3545311	BRIGATINIB	4	5,634
CHEMBL535	SUNITINIB	4	79,020
CHEMBL553	ERLOTINIB	4	108,300
CHEMBL939	GEFITINIB	4	117,814
CHEMBL223360	LINIFANIB	3	3,925
CHEMBL31965	CANERTINIB	3	8,083
CHEMBL603469	LESTAURTINIB	3
CHEMBL91829	RUBOXISTAURIN	3	77
CHEMBL4073443	TOMIVOSERTIB	2	473
CHEMBL4211649	TINODASERTIB	2	53
CHEMBL103667	DORAMAPIMOD	2	1,681
CHEMBL1230609	FORETINIB	2	3,096
CHEMBL151	LUTEOLIN	2	23,523
CHEMBL1721885	SU-014813	2	363
CHEMBL230011	TG100-115	2	1,504
CHEMBL3545307	MERESTINIB	2	851
CHEMBL475251	R-406	2
CHEMBL5089410	PILAVAPADIN	2
CHEMBL296468	BMS-387032	1
CHEMBL4298140	TOMIVOSERTIB HYDROCHLORIDE	1
CHEMBL574738	AST-487	1

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — MKN subfamily

Most potent curated ligand interactions (5 total), top 5:

Ligand	Action	Affinity	Parameter
tomivosertib	Inhibition	8.62	pIC50
compound 20j [PMID: 38564512]	Inhibition	8.36	pIC50
dorsomorphin	Inhibition	7.96	pIC50
tinodasertib	Inhibition	7.19	pIC50
MNK1 inhibitor	Inhibition	6.06	pIC50

Binding affinities (BindingDB)

541 measured of 786 human assays (786 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
N-benzyl-N-[2-(dimethylamino)ethyl]-4-[(5-methoxy-2-oxo-3H-1,3-benzothiazol-6-yl)amino]-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidine-7-carboxamide	IC50	0.6 nM	US-9296757: Substituted benzothienopyrimidines
N,N-bis(2-methoxyethyl)-4-[(5-methoxy-2-oxo-3H-1,3-benzothiazol-6-yl)amino]-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidine-7-carboxamide	IC50	0.7 nM	US-9296757: Substituted benzothienopyrimidines
N-butyl-N-(cyanomethyl)-4-[(5-methoxy-2-oxo-3H-1,3-benzothiazol-6-yl)amino]-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidine-7-carboxamide	IC50	1 nM	US-9296757: Substituted benzothienopyrimidines
N-ethyl-N-(2-methoxyethyl)-4-[(5-methoxy-2-oxo-3H-1,3-benzothiazol-6-yl)amino]-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidine-7-carboxamide	IC50	1 nM	US-9296757: Substituted benzothienopyrimidines
3-bromo-n-(6-methoxy-1h-indazol-5-yl)-1h-pyrazolo[3,4-d]pyrimidin-4-amine	IC50	1 nM	US-9556181: Substituted pyrazolopyrimidinylamino-indazoles
3-bromo-n-(6-isopropoxy-1h-indazol-5-yl)-1h-pyrazolo[3,4-d]pyrimidin-4-amine	IC50	1 nM	US-9556181: Substituted pyrazolopyrimidinylamino-indazoles
3-[3-(4-fluoro-1-benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]oxycyclobutan-1-amine	IC50	1 nM	US-9499547: Amino-substituted imidazopyridazines
2-{3-(Furo[2,3-c]pyridin-2-yl)imidazo[1,2-b]pyridazin-6-ylamino}-1-phenylethanol	IC50	1 nM	US-9730929: Substituted aminoimidazopyridazines
2-{3-(Furo[3,2-c]pyridin-2-yl)imidazo[1,2-b]pyridazin-6-ylamino}-1-phenylethanol	IC50	1 nM	US-9730929: Substituted aminoimidazopyridazines
3-(1-Benzofuran-2-yl)-N-[(2S)-1-hydroxy-3-methylbutan-2-yl]imidazo[1,2-b]-pyridazine-6-carboxamide	IC50	1.3 nM	US-10214545
N-[3-(dimethylamino)propyl]-3-[4-(morpholin-4-yl)furo[3,2-c]pyridin-2-yl]-imidazo[1,2-b]pyridazine-6-carboxamide	IC50	1.5 nM	US-10214545
Staurosporine	KD	1.7 nM
3-(1-Benzofuran-2-yl)-N-[2-(dimethylamino)ethyl]imidazo[1,2-b]pyridazine-6-carboxamide	IC50	1.7 nM	US-10214545
N-butyl-4-[(5-methoxy-2-oxo-3H-1,3-benzothiazol-6-yl)amino]-N-methyl-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidine-7-carboxamide	IC50	1.9 nM	US-9296757: Substituted benzothienopyrimidines
N-(2-methoxyethyl)-4-[(5-methoxy-2-oxo-3H-1,3-benzothiazol-6-yl)amino]-N-propyl-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidine-7-carboxamide	IC50	2 nM	US-9296757: Substituted benzothienopyrimidines
3-(4-methoxy-1-benzofuran-2-yl)-6-(3-methylsulfinylpropoxy)imidazo[1,2-b]pyridazine	IC50	2 nM	US-9320737: Substituted imidazopyridazines
3-(4-methoxy-1-benzofuran-2-yl)-6-(3-methylsulfonylpropoxy)imidazo[1,2-b]pyridazine	IC50	2 nM	US-9320737: Substituted imidazopyridazines
imino-[3-[3-(4-methoxy-1-benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]oxypropyl]-methyl-oxo-lambda6-sulfane	IC50	2 nM	US-9320737: Substituted imidazopyridazines
3-(4-fluorophenyl)-n-(6-methoxy-1h-indazol-5-yl)-1h-pyrazolo[3,4-d]pyrimidin-4-amine	IC50	2 nM	US-9556181: Substituted pyrazolopyrimidinylamino-indazoles
3-[(1R)-1-{[3-(1- Benzofuran-2- yl)imidazo[1,2-b]pyridazin- 6-yl]oxy}-2- (methylamino)ethyl]phenol	IC50	2 nM	US-9730929: Substituted aminoimidazopyridazines
2-{3-(1-Benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-ylamino}-1-(pyridin-3-yl)ethanol	IC50	2 nM	US-9730929: Substituted aminoimidazopyridazines
N-(2-methoxyethyl)-N-methyl-3-[4-(morpholin-4-yl)furo[3,2-c]pyridin-2-yl]imidazo[1,2-b]pyridazine-6-carboxamide	IC50	2.6 nM	US-10214545
N-[(2R)-1-hydroxypropan-2-yl]-3-[4-(morpholin-4-yl)furo[3,2-c]pyridin-2-yl]-imidazo[1,2-b]pyridazine-6-carboxamide	IC50	2.8 nM	US-10214545
N-ethyl-4-[(5-methoxy-2-oxo-3H-1,3-benzothiazol-6-yl)amino]-N-propan-2-yl-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidine-7-carboxamide	IC50	3 nM	US-9296757: Substituted benzothienopyrimidines
4-[3-(4-methoxy-1-benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]oxybutan-1-amine	IC50	3 nM	US-9499547: Amino-substituted imidazopyridazines
3-[3-(5-methoxy-1-benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]oxycyclobutan-1-amine	IC50	3 nM	US-9499547: Amino-substituted imidazopyridazines
3-[3-(5-fluoro-1-benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]oxycyclobutan-1-amine	IC50	3 nM	US-9499547: Amino-substituted imidazopyridazines
2-{3-(4-Methoxyfuro[3,2-c]pyridin-2-yl)imidazo[1,2-b]pyridazin-6-ylamino}-1-phenylethanol	IC50	3 nM	US-9730929: Substituted aminoimidazopyridazines
N-[3-(1-Benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]-2-hydroxy-2-(pyridin-3-yl)acetamide	IC50	3 nM	US-9745304: Amidoimidazopyridazines as MKNK-1 kinase inhibitors
N-[3-(1-Benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]-3-(pyridin-3-yl)propanamide	IC50	3 nM	US-9745304: Amidoimidazopyridazines as MKNK-1 kinase inhibitors
(5S)-1-[3-(1-Benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]-5-(hydroxymethyl)-pyrrolidin-2-one	IC50	3 nM	US-9745304: Amidoimidazopyridazines as MKNK-1 kinase inhibitors
(2R)-2-hydroxy-N-[3-(4-methoxyfuro[3,2-c]pyridin-2-yl)imidazo[1,2-b]-pyridazin-6-yl]propanamide	IC50	3 nM	US-9745304: Amidoimidazopyridazines as MKNK-1 kinase inhibitors
(7S) N-(1H-Indol-5-yl)-4-[(6-methoxypyrazolo[1,5-a]pyridin-5-yl)amino]-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidine-7-carboxamide	IC50	3 nM	US-10487092
3-(1-Benzofuran-2-yl)-N-[3-(dimethylamino)propyl]imidazo[1,2-b]pyridazine-6-carboxamide	IC50	3.3 nM	US-10214545
N-(3-methoxypropyl)-3-[4-(morpholin-4-yl)furo[3,2-c]pyridin-2-yl]imidazo[1,2-b]pyridazine-6-carboxamide	IC50	3.8 nM	US-10214545
4-[(5-methoxy-2-oxo-3H-1,3-benzothiazol-6-yl)amino]-N-propan-2-yl-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidine-7-carboxamide	IC50	4 nM	US-9296757: Substituted benzothienopyrimidines
4-[(5-methoxy-2-oxo-3H-1,3-benzothiazol-6-yl)amino]-N,N-dimethyl-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidine-7-carboxamide	IC50	4 nM	US-9296757: Substituted benzothienopyrimidines
3-(1-benzofuran-2-yl)-6-(3-methylsulfinylpropoxy)imidazo[1,2-b]pyridazine	IC50	4 nM	US-9320737: Substituted imidazopyridazines
3-[3-(1-benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]oxypropyl-imino-methyl-oxo-lambda6-sulfane	IC50	4 nM	US-9320737: Substituted imidazopyridazines
[3-[3-(1-benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]oxycyclobutyl]methanamine	IC50	4 nM	US-9499547: Amino-substituted imidazopyridazines
3-[3-(5-chloro-1-benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]oxycyclobutan-1-amine	IC50	4 nM	US-9499547: Amino-substituted imidazopyridazines
3-[(1R)-1-Hydroxy-2- {3-(4-methoxy-1- benzofuran-2- yl)imidazo[1,2-b]pyridazin- 6-ylamino}eth- yl]phenol	IC50	4 nM	US-9730929: Substituted aminoimidazopyridazines
2-{3-(1-Benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-ylamino}-1-phenylethanol	IC50	4 nM	US-9730929: Substituted aminoimidazopyridazines
(−)-2-{3-(1-Benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-ylamino}-1-phenylethanol	IC50	4 nM	US-9730929: Substituted aminoimidazopyridazines
N-[3-(1-Benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]-2-hydroxy-2-(tetrahydro-2H-pyran-4-yl)acetamide	IC50	4 nM	US-9745304: Amidoimidazopyridazines as MKNK-1 kinase inhibitors
(2R)¿N-[3-(1-Benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]-2-hydroxypropanamide	IC50	4 nM	US-9745304: Amidoimidazopyridazines as MKNK-1 kinase inhibitors
N-[3-(1-Benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]-3-methylbutanamide	IC50	4 nM	US-9745304: Amidoimidazopyridazines as MKNK-1 kinase inhibitors
3-(1-Benzofuran-2-yl)-6-[2-(morpholin-2-yl)ethoxy]imidazo[1,2-b]pyridazine	IC50	4 nM	US-9777004: Amino-substituted imidazopyridazines
3-(1-Benzofuran-2-yl)-N-[(2R)-1-hydroxypropan-2-yl]imidazo[1,2-b]pyridazine-6-carboxamide	IC50	4.1 nM	US-10214545
N-benzyl-3-[4-(morpholin-4-yl)furo[3,2-c]pyridin-2-yl]imidazo[1,2-b]pyridazine-6-carboxamide	IC50	4.4 nM	US-10214545

ChEMBL bioactivities

1716 potent at pChembl≥5 of 1771 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.08	IC50	0.084	nM	CHEMBL4086747
10.00	IC50	0.1	nM	CHEMBL5855544
9.82	IC50	0.15	nM	CHEMBL4879010
9.52	IC50	0.3	nM	CHEMBL5984153
9.52	IC50	0.3	nM	CHEMBL6052925
9.51	IC50	0.31	nM	CHEMBL4073743
9.40	IC50	0.4	nM	CHEMBL5844466
9.30	IC50	0.5	nM	CHEMBL6002798
9.29	IC50	0.51	nM	CHEMBL4073743
9.22	EC50	0.6	nM	CHEMBL3800585
9.22	IC50	0.6	nM	CHEMBL5771700
9.21	IC50	0.62	nM	CHEMBL4094975
9.19	IC50	0.65	nM	CHEMBL4076439
9.15	IC50	0.7	nM	CHEMBL5885279
9.15	IC50	0.7	nM	CHEMBL6000872
9.15	IC50	0.7	nM	CHEMBL6016313
9.10	IC50	0.79	nM	CHEMBL4076439
9.10	IC50	0.8	nM	CHEMBL5558538
9.06	IC50	0.88	nM	CHEMBL4094975
9.00	IC50	1	nM	CHEMBL3355000
9.00	IC50	1	nM	CHEMBL3355002
9.00	IC50	1	nM	CHEMBL4859971
9.00	IC50	1	nM	CHEMBL4869634
9.00	IC50	1	nM	CHEMBL5201681
9.00	IC50	1	nM	CHEMBL5174006
9.00	IC50	1	nM	CHEMBL5747076
9.00	IC50	1	nM	CHEMBL5798886
9.00	IC50	1	nM	CHEMBL6060117
9.00	IC50	1	nM	CHEMBL5751972
9.00	IC50	1	nM	CHEMBL5974613
9.00	IC50	1	nM	CHEMBL5811626
9.00	IC50	1	nM	CHEMBL5906096
9.00	IC50	1	nM	CHEMBL6045874
9.00	IC50	1	nM	CHEMBL5959489
9.00	IC50	1	nM	CHEMBL6042962
9.00	IC50	1	nM	CHEMBL5862530
9.00	IC50	1	nM	CHEMBL5965088
9.00	IC50	1	nM	CHEMBL6023477
9.00	IC50	1	nM	CHEMBL5985857
9.00	IC50	1	nM	CHEMBL6053557
9.00	IC50	1	nM	CHEMBL5797070
9.00	IC50	1	nM	CHEMBL5760229
9.00	IC50	1	nM	CHEMBL5967573
9.00	IC50	1	nM	CHEMBL5981918
9.00	IC50	1	nM	CHEMBL5764452
9.00	IC50	1	nM	CHEMBL5979012
9.00	IC50	1	nM	CHEMBL5922419
8.96	IC50	1.1	nM	CHEMBL4876307
8.96	IC50	1.1	nM	CHEMBL5561655
8.96	IC50	1.1	nM	CHEMBL6000872

PubChem BioAssay actives

657 with measured affinity, of 1538 total; 50 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
6-[(6-amino-5-chloropyrimidin-4-yl)amino]-8-chlorospiro[2H-imidazo[1,5-a]pyridine-3,1’-cyclohexane]-1,5-dione	1479626: Inhibition of MNK1/2 in human HCT116 cells assessed as decrease in eIF4E phosphorylation at Ser209 after 2 hrs by HTRF assay	ic50	0.0001	uM
4-[[6-[4-(piperazine-1-carbonyl)phenyl]pyrido[3,2-d]pyrimidin-4-yl]amino]benzonitrile	1769037: Inhibition of MKN1 (unknown origin) in presence of ATP by HTRF assay	ic50	0.0001	uM
N-[6-[(8-chloro-1,5-dioxospiro[2H-imidazo[1,5-a]pyridine-3,1’-cyclohexane]-6-yl)amino]pyrimidin-4-yl]cyclopropanecarboxamide	1479626: Inhibition of MNK1/2 in human HCT116 cells assessed as decrease in eIF4E phosphorylation at Ser209 after 2 hrs by HTRF assay	ic50	0.0003	uM
6-[(6-aminopyrimidin-4-yl)amino]-8-chlorospiro[2H-imidazo[1,5-a]pyridine-3,1’-cyclohexane]-1,5-dione	1479624: Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins followed by ATP addition measured after 40 mins by ADP-Glo assay	ic50	0.0006	uM
6-[(6-aminopyrimidin-4-yl)amino]-8-chlorospiro[2H-imidazo[1,5-a]pyridine-3,1’-cyclopentane]-1,5-dione	1479626: Inhibition of MNK1/2 in human HCT116 cells assessed as decrease in eIF4E phosphorylation at Ser209 after 2 hrs by HTRF assay	ic50	0.0006	uM
2-[5-amino-6-[1-methyl-7-[(3S)-3-methylpiperazin-1-yl]benzimidazol-2-yl]pyrazin-2-yl]-N,N-dimethylpyridine-4-carboxamide	1296847: Inhibition of MNK1/2 in human KMS11-luc cells assessed as inhibition of EIF4E phosphorylation at S209 after 3 hrs by quantitative electrochemiluminescence assay	ec50	0.0006	uM
[3-[4-(2,3-dihydroindol-1-yl)pyrido[3,2-d]pyrimidin-6-yl]phenyl]-piperazin-1-ylmethanone	2064721: Inhibition of Mnk1 (unknown origin) incubated for 60 mins in presence of ATP/substrateby HTRF assay	ic50	0.0008	uM
[4-[4-(4-fluoro-2-propan-2-yloxyanilino)pyrido[3,2-d]pyrimidin-6-yl]phenyl]-piperazin-1-ylmethanone	1769037: Inhibition of MKN1 (unknown origin) in presence of ATP by HTRF assay	ic50	0.0010	uM
[4-[4-(4-fluoro-3-methoxyanilino)pyrido[3,2-d]pyrimidin-6-yl]phenyl]-piperazin-1-ylmethanone	1769037: Inhibition of MKN1 (unknown origin) in presence of ATP by HTRF assay	ic50	0.0010	uM
N-(6-methoxy-1H-indazol-5-yl)-2-(4-methylphenyl)sulfonyl-1H-pyrrolo[2,3-b]pyridin-4-amine	1846623: Inhibition of MNK1 (unknown origin)	ic50	0.0010	uM
N-(3-methylsulfonylpropyl)-4-[(6-propan-2-yloxy-1H-indazol-5-yl)amino]-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b]indole-6-carboxamide	1177106: Inhibition of human full-length MKNK1 using biotin-Ahx-IKKRKLTRRKSLKG substrate by TR-FRET-based high ATP assay	ic50	0.0010	uM
N-benzyl-4-[(6-methoxy-1H-indazol-5-yl)amino]-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b]indole-6-carboxamide	1177106: Inhibition of human full-length MKNK1 using biotin-Ahx-IKKRKLTRRKSLKG substrate by TR-FRET-based high ATP assay	ic50	0.0010	uM
6-[(5-fluoro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-5-methoxy-3H-1,3-benzothiazol-2-one	1846623: Inhibition of MNK1 (unknown origin)	ic50	0.0010	uM
[4-[3-(1-benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]phenyl]-piperazin-1-ylmethanone	2083030: Inhibition of recombinant MNK1 (unknown origin) using TATKSGSTTKNR as substrate preincubated for 15 mins followed by ATP addition and measured after 1 hr by ADP-glo kinase assay	ic50	0.0011	uM
[4-[4-(4-fluoroanilino)pyrido[3,2-d]pyrimidin-6-yl]phenyl]-piperazin-1-ylmethanone	1769037: Inhibition of MKN1 (unknown origin) in presence of ATP by HTRF assay	ic50	0.0011	uM
[4-[4-(4-fluoro-2-methoxyanilino)pyrido[3,2-d]pyrimidin-6-yl]phenyl]-piperazin-1-ylmethanone	1769037: Inhibition of MKN1 (unknown origin) in presence of ATP by HTRF assay	ic50	0.0012	uM
6-[(6-aminopyrimidin-4-yl)amino]-4’,4’-difluoro-8-methylspiro[2H-imidazo[1,5-a]pyridine-3,1’-cyclohexane]-1,5-dione	1479624: Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins followed by ATP addition measured after 40 mins by ADP-Glo assay	ic50	0.0014	uM
3-[5-amino-6-[1-methyl-7-[(3S)-3-methylpiperazin-1-yl]benzimidazol-2-yl]pyrazin-2-yl]-N,N-dimethylbenzamide	1296841: Inhibition of ERK2-activated full length wild type MNK1a (unknown origin) using biotin-SGSGKRREILSRRPSYR-NH2 as substrate after 2 hrs by HTRF assay	ic50	0.0015	uM
3-(3-isoquinolin-6-ylimidazo[1,2-b]pyridazin-6-yl)oxycyclobutan-1-amine	1479624: Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins followed by ATP addition measured after 40 mins by ADP-Glo assay	ic50	0.0015	uM
N-[6-[[8-chloro-3-(3-chlorophenyl)-3-methyl-1,5-dioxo-2H-imidazo[1,5-a]pyridin-6-yl]amino]pyrimidin-4-yl]cyclopropanecarboxamide	1479624: Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins followed by ATP addition measured after 40 mins by ADP-Glo assay	ic50	0.0016	uM
[3-[4-(5-fluoro-2,3-dihydroindol-1-yl)pyrido[3,2-d]pyrimidin-6-yl]phenyl]-piperazin-1-ylmethanone	2064721: Inhibition of Mnk1 (unknown origin) incubated for 60 mins in presence of ATP/substrateby HTRF assay	ic50	0.0018	uM
[(3R)-3-aminopiperidin-1-yl]-[4-[3-(1-benzofuran-2-yl)imidazo[1,2-a]pyridin-6-yl]phenyl]methanone	2083030: Inhibition of recombinant MNK1 (unknown origin) using TATKSGSTTKNR as substrate preincubated for 15 mins followed by ATP addition and measured after 1 hr by ADP-glo kinase assay	ic50	0.0018	uM
6-[(6-aminopyrimidin-4-yl)amino]-8-methylspiro[2H-imidazo[1,5-a]pyridine-3,1’-cyclohexane]-1,5-dione	2083030: Inhibition of recombinant MNK1 (unknown origin) using TATKSGSTTKNR as substrate preincubated for 15 mins followed by ATP addition and measured after 1 hr by ADP-glo kinase assay	ic50	0.0019	uM
N-[6-[(1-oxo-2,3-dihydroisoindol-5-yl)amino]pyrimidin-4-yl]cyclopropanecarboxamide	1479624: Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins followed by ATP addition measured after 40 mins by ADP-Glo assay	ic50	0.0019	uM
8-chloro-6-(pyrimidin-4-ylamino)spiro[2H-imidazo[1,5-a]pyridine-3,1’-cyclohexane]-1,5-dione	1552871: Inhibition of recombinant GST-tagged MNK1 (unknown origin) using eIF4E-derived peptide as substrate in presence of ATP at km concentration by ADP-Glo assay	ki	0.0020	uM
6-[(6-aminopyrimidin-4-yl)amino]-8-methylspiro[2H-imidazo[1,5-a]pyridine-3,1’-cyclohexane]-1,5-dione;hydrochloride	1534877: Inhibition of MNK1 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis	ic50	0.0020	uM
3-[5-amino-6-(1-methyl-7-piperazin-1-ylbenzimidazol-2-yl)pyrazin-2-yl]-N,N-dimethylbenzamide	1296841: Inhibition of ERK2-activated full length wild type MNK1a (unknown origin) using biotin-SGSGKRREILSRRPSYR-NH2 as substrate after 2 hrs by HTRF assay	ic50	0.0020	uM
[4-[4-(2,3-dihydroindol-1-yl)pyrido[3,2-d]pyrimidin-6-yl]phenyl]-piperazin-1-ylmethanone	2064721: Inhibition of Mnk1 (unknown origin) incubated for 60 mins in presence of ATP/substrateby HTRF assay	ic50	0.0020	uM
[4-[3-(1-benzofuran-2-yl)imidazo[1,2-a]pyridin-6-yl]phenyl]-(4-piperidin-1-ylpiperidin-1-yl)methanone	2083030: Inhibition of recombinant MNK1 (unknown origin) using TATKSGSTTKNR as substrate preincubated for 15 mins followed by ATP addition and measured after 1 hr by ADP-glo kinase assay	ic50	0.0021	uM
6-[(6-aminopyrimidin-4-yl)amino]-8-chloro-3,3-dimethyl-2H-imidazo[1,5-a]pyridine-1,5-dione	1479624: Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins followed by ATP addition measured after 40 mins by ADP-Glo assay	ic50	0.0022	uM
[(3S)-3-aminopiperidin-1-yl]-[4-(3-isoquinolin-6-ylimidazo[1,2-b]pyridazin-6-yl)phenyl]methanone	1763880: Inhibition of N-terminal GST-fused human full length recombinant MNK1 (1 to 424 residues) expressed in baculovirus-infected Sf21 cells using TATKSGSTTKNR as substrate preincubated with enzyme and substrate for 10 mins followed by ATP addition and measured after 40 mins by ADP-glo luminescence assay	ic50	0.0023	uM
[4-(3-isoquinolin-6-ylimidazo[1,2-a]pyridin-6-yl)phenyl]-(4-piperidin-1-ylpiperidin-1-yl)methanone	1763880: Inhibition of N-terminal GST-fused human full length recombinant MNK1 (1 to 424 residues) expressed in baculovirus-infected Sf21 cells using TATKSGSTTKNR as substrate preincubated with enzyme and substrate for 10 mins followed by ATP addition and measured after 40 mins by ADP-glo luminescence assay	ic50	0.0024	uM
1-[4-[4-[4-(2,3-dihydroindol-1-yl)pyrido[3,2-d]pyrimidin-6-yl]benzoyl]piperazin-1-yl]ethanone	2064721: Inhibition of Mnk1 (unknown origin) incubated for 60 mins in presence of ATP/substrateby HTRF assay	ic50	0.0024	uM
N-[3-(dimethylamino)propyl]-7-(5-fluoro-2,3-dihydroindol-1-yl)-[1,3]thiazolo[5,4-d]pyrimidine-2-carboxamide	1881764: Inhibition of Mnk1 (unknown origin)	ic50	0.0025	uM
[(3S)-3-aminopiperidin-1-yl]-[4-(3-isoquinolin-6-ylimidazo[1,2-a]pyridin-6-yl)phenyl]methanone	1763880: Inhibition of N-terminal GST-fused human full length recombinant MNK1 (1 to 424 residues) expressed in baculovirus-infected Sf21 cells using TATKSGSTTKNR as substrate preincubated with enzyme and substrate for 10 mins followed by ATP addition and measured after 40 mins by ADP-glo luminescence assay	ic50	0.0025	uM
N-[6-[(3,3-dimethyl-1,5-dioxo-2H-imidazo[1,5-a]pyridin-6-yl)amino]pyrimidin-4-yl]cyclopropanecarboxamide	1479624: Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins followed by ATP addition measured after 40 mins by ADP-Glo assay	ic50	0.0027	uM
[4-[3-(1-benzofuran-2-yl)imidazo[1,2-a]pyridin-6-yl]phenyl]-(4-methylpiperazin-1-yl)methanone	2083030: Inhibition of recombinant MNK1 (unknown origin) using TATKSGSTTKNR as substrate preincubated for 15 mins followed by ATP addition and measured after 1 hr by ADP-glo kinase assay	ic50	0.0028	uM
[4-[3-(1-benzofuran-2-yl)imidazo[1,2-a]pyridin-6-yl]phenyl]-piperidin-1-ylmethanone	2083030: Inhibition of recombinant MNK1 (unknown origin) using TATKSGSTTKNR as substrate preincubated for 15 mins followed by ATP addition and measured after 1 hr by ADP-glo kinase assay	ic50	0.0028	uM
[(3S)-3-aminopiperidin-1-yl]-[4-[3-(1-benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]phenyl]methanone	2083030: Inhibition of recombinant MNK1 (unknown origin) using TATKSGSTTKNR as substrate preincubated for 15 mins followed by ATP addition and measured after 1 hr by ADP-glo kinase assay	ic50	0.0029	uM
[(3R)-3-aminopiperidin-1-yl]-[4-[3-(1-benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]phenyl]methanone	2083030: Inhibition of recombinant MNK1 (unknown origin) using TATKSGSTTKNR as substrate preincubated for 15 mins followed by ATP addition and measured after 1 hr by ADP-glo kinase assay	ic50	0.0031	uM
7-(5-chloro-2,3-dihydroindol-1-yl)-N-(piperidin-4-ylmethyl)-[1,3]thiazolo[5,4-d]pyrimidine-2-carboxamide	1881764: Inhibition of Mnk1 (unknown origin)	ic50	0.0032	uM
7-(3,3-dimethyl-2H-indol-1-yl)-N-(piperidin-4-ylmethyl)-[1,3]thiazolo[5,4-d]pyrimidine-2-carboxamide	1881764: Inhibition of Mnk1 (unknown origin)	ic50	0.0032	uM
(4-aminopiperidin-1-yl)-[4-[3-(1-benzofuran-2-yl)imidazo[1,2-a]pyridin-6-yl]phenyl]methanone	2083030: Inhibition of recombinant MNK1 (unknown origin) using TATKSGSTTKNR as substrate preincubated for 15 mins followed by ATP addition and measured after 1 hr by ADP-glo kinase assay	ic50	0.0032	uM
8-chloro-3,3-dimethyl-6-(pyrimidin-4-ylamino)-2H-imidazo[1,5-a]pyridine-1,5-dione	1479624: Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins followed by ATP addition measured after 40 mins by ADP-Glo assay	ic50	0.0033	uM
(4-aminopiperidin-1-yl)-[4-[3-(1-benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]phenyl]methanone	2083030: Inhibition of recombinant MNK1 (unknown origin) using TATKSGSTTKNR as substrate preincubated for 15 mins followed by ATP addition and measured after 1 hr by ADP-glo kinase assay	ic50	0.0036	uM
[4-[3-(1-benzofuran-2-yl)imidazo[1,2-a]pyridin-6-yl]phenyl]-piperazin-1-ylmethanone	2083030: Inhibition of recombinant MNK1 (unknown origin) using TATKSGSTTKNR as substrate preincubated for 15 mins followed by ATP addition and measured after 1 hr by ADP-glo kinase assay	ic50	0.0038	uM
[4-[3-(1-benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl]phenyl]-[4-(dimethylamino)piperidin-1-yl]methanone	2083030: Inhibition of recombinant MNK1 (unknown origin) using TATKSGSTTKNR as substrate preincubated for 15 mins followed by ATP addition and measured after 1 hr by ADP-glo kinase assay	ic50	0.0039	uM
3-[6-amino-5-(4-piperazin-1-yl-1H-benzimidazol-2-yl)-3-pyridinyl]-N,N-dimethylbenzamide	1296841: Inhibition of ERK2-activated full length wild type MNK1a (unknown origin) using biotin-SGSGKRREILSRRPSYR-NH2 as substrate after 2 hrs by HTRF assay	ic50	0.0040	uM
5-[3-amino-4-(oxan-4-ylmethylamino)-1H-indazol-6-yl]-1-[(3-chlorophenyl)methyl]pyridin-2-one	1881764: Inhibition of Mnk1 (unknown origin)	ic50	0.0040	uM
[4-(3-isoquinolin-6-ylimidazo[1,2-a]pyridin-6-yl)phenyl]-(4-morpholin-4-ylpiperidin-1-yl)methanone	1763880: Inhibition of N-terminal GST-fused human full length recombinant MNK1 (1 to 424 residues) expressed in baculovirus-infected Sf21 cells using TATKSGSTTKNR as substrate preincubated with enzyme and substrate for 10 mins followed by ATP addition and measured after 40 mins by ADP-glo luminescence assay	ic50	0.0040	uM

CTD chemical–gene interactions

41 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects expression, increases expression, increases methylation	5
Arsenic Trioxide	increases expression, decreases reaction, increases reaction, affects reaction, increases activity (+4 more)	4
arsenite	increases activity, increases phosphorylation, decreases reaction	2
SB 203580	affects cotreatment, decreases reaction, increases phosphorylation, increases activity, increases reaction	2
2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one	affects cotreatment, decreases reaction, increases phosphorylation, increases activity, increases reaction	2
Cisplatin	affects expression, affects cotreatment, decreases expression	2
Estradiol	affects cotreatment, increases expression, decreases expression	2
Tetradecanoylphorbol Acetate	affects cotreatment, decreases reaction, increases phosphorylation, increases activity, increases reaction	2
aristolochic acid I	increases expression	1
triphenyl phosphate	affects expression	1
beta-lapachone	decreases expression	1
manganese chloride	decreases expression, increases abundance	1
M-VAC protocol	decreases response to substance	1
CGP 52608	affects binding, increases reaction	1
U 0126	decreases reaction, increases phosphorylation	1
CGP 57380	decreases reaction, increases activity, increases phosphorylation, decreases activity	1
abrine	decreases expression	1
Sorafenib	decreases reaction, increases phosphorylation	1
Decitabine	affects expression	1
Sunitinib	increases expression	1
Vorinostat	increases expression	1
Norethindrone Acetate	increases expression, affects cotreatment	1
Acetaminophen	increases expression	1
Anisomycin	increases activity, decreases reaction	1
Vehicle Emissions	increases abundance, increases expression	1
Benzo(a)pyrene	affects methylation	1
Doxorubicin	decreases expression	1
Hydrogen Peroxide	increases activity	1
Manganese	decreases expression, increases abundance	1
Methyl Methanesulfonate	increases expression	1

ChEMBL screening assays

453 unique, capped per target: 453 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3803169	Binding	Inhibition of MNK1/2 in human KMS11-luc cells assessed as inhibition of EIF4E phosphorylation at S209 after 3 hrs by quantitative electrochemiluminescence assay	Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design. — J Med Chem

Cellosaurus cell lines

8 cell lines: 7 cancer cell line, 1 transformed cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_B1X6	Abcam HeLa MKNK1 KO	Cancer cell line	Female
CVCL_D7V3	Ubigene A-549 MKNK1 KO	Cancer cell line	Male
CVCL_D8QM	Ubigene HCT 116 MKNK1 KO	Cancer cell line	Male
CVCL_D9KC	Ubigene HEK293 MKNK1 KO	Transformed cell line	Female
CVCL_E0I4	Ubigene HeLa MKNK1 KO	Cancer cell line	Female
CVCL_SY47	HAP1 MKNK1 (-) 1	Cancer cell line	Male
CVCL_SY48	HAP1 MKNK1 (-) 2	Cancer cell line	Male
CVCL_SY49	HAP1 MKNK1 (-) 3	Cancer cell line	Male

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.