PKMYT1

Summary

PKMYT1 (protein kinase, membrane associated tyrosine/threonine 1, HGNC:29650) is a protein-coding gene on chromosome 16p13.3, encoding Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (Q99640). Acts as a negative regulator of entry into mitosis (G2 to M transition) by phosphorylation of the CDK1 kinase specifically when CDK1 is complexed to cyclins. It is a common-essential gene (DepMap: required in 94.2% of cancer cell lines).

This gene encodes a member of the serine/threonine protein kinase family. The encoded protein is a membrane-associated kinase that negatively regulates the G2/M transition of the cell cycle by phosphorylating and inactivating cyclin-dependent kinase 1. The activity of the encoded protein is regulated by polo-like kinase 1. Alternatively spliced transcript variants encoding multiple isoforms have been observed for this gene.

Source: NCBI Gene 9088 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 108 total
• Druggable target: yes — 14 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 94.2% of screened cell lines (common-essential)
• MANE Select transcript: NM_004203

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:29650
Approved symbol	PKMYT1
Name	protein kinase, membrane associated tyrosine/threonine 1
Location	16p13.3
Locus type	gene with protein product
Status	Approved
Aliases	MYT1, PPP1R126
Ensembl gene	ENSG00000127564
Ensembl biotype	protein_coding
OMIM	602474
Entrez	9088

Gene structure

Transcript identifiers

Ensembl transcripts: 28 — 20 protein_coding, 4 retained_intron, 3 protein_coding_CDS_not_defined, 1 nonsense_mediated_decay

ENST00000262300, ENST00000382240, ENST00000431515, ENST00000440027, ENST00000570649, ENST00000571102, ENST00000572059, ENST00000572619, ENST00000572658, ENST00000572832, ENST00000573944, ENST00000574333, ENST00000574385, ENST00000574415, ENST00000574680, ENST00000574730, ENST00000575040, ENST00000575632, ENST00000575981, ENST00000576268, ENST00000896660, ENST00000896661, ENST00000896662, ENST00000934454, ENST00000934455, ENST00000934456, ENST00000934457, ENST00000934458

RefSeq mRNA: 4 — MANE Select: NM_004203 NM_001258450, NM_001258451, NM_004203, NM_182687

CCDS: CCDS10486, CCDS45391, CCDS58414, CCDS58415

Canonical transcript exons

ENST00000262300 — 9 exons

Exon	Start	End
ENSE00001062467	2979648	2979912
ENSE00001118919	2974550	2974656
ENSE00001118922	2975319	2975812
ENSE00002663830	2980286	2980446
ENSE00003499132	2974000	2974157
ENSE00003504472	2972808	2973064
ENSE00003518642	2973138	2973215
ENSE00003645903	2976664	2977031
ENSE00003655503	2974245	2974417

Expression profiles

Bgee: expression breadth ubiquitous, 179 present calls, max score 97.28.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 30.1276 / max 425.0634, expressed in 1498 samples.

FANTOM5 promoters (7 alternative TSS)

Promoter ID	TPM avg	Samples expressed
155970	26.9557	1374
155969	1.9982	753
155967	0.8262	433
155964	0.1912	110
155965	0.0789	32
155968	0.0577	19
155966	0.0198	5

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right testis	UBERON:0004534	97.28	gold quality
left testis	UBERON:0004533	96.86	gold quality
endometrium epithelium	UBERON:0004811	94.77	gold quality
testis	UBERON:0000473	93.47	gold quality
ventricular zone	UBERON:0003053	92.15	gold quality
ganglionic eminence	UBERON:0004023	91.38	gold quality
mucosa of transverse colon	UBERON:0004991	91.28	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	88.75	gold quality
Brodmann (1909) area 10	UBERON:0013541	88.52	silver quality
oocyte	CL:0000023	87.74	gold quality
lower esophagus mucosa	UBERON:0035834	87.55	gold quality
secondary oocyte	CL:0000655	87.32	gold quality
middle frontal gyrus	UBERON:0002702	83.86	silver quality
paraflocculus	UBERON:0005351	83.73	gold quality
esophagus mucosa	UBERON:0002469	83.57	gold quality
embryo	UBERON:0000922	82.85	gold quality
prefrontal cortex	UBERON:0000451	82.52	gold quality
right hemisphere of cerebellum	UBERON:0014890	81.23	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	81.03	gold quality
cerebellar hemisphere	UBERON:0002245	80.83	gold quality
cerebellar cortex	UBERON:0002129	80.79	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	80.76	gold quality
stromal cell of endometrium	CL:0002255	80.48	gold quality
cerebellum	UBERON:0002037	79.40	gold quality
right frontal lobe	UBERON:0002810	79.20	gold quality
spinal cord	UBERON:0002240	78.50	gold quality
anterior cingulate cortex	UBERON:0009835	78.29	gold quality
bone marrow	UBERON:0002371	78.26	gold quality
cingulate cortex	UBERON:0003027	78.22	gold quality
frontal cortex	UBERON:0001870	77.88	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	4.11

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

13 targeting PKMYT1, 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-6768-5P	99.92	67.36	1942
HSA-MIR-106A-5P	99.90	73.94	2683
HSA-MIR-3671	99.90	73.04	3897
HSA-MIR-17-5P	99.89	73.83	2665
HSA-MIR-106B-5P	99.88	74.72	2795
HSA-MIR-20A-5P	99.88	74.76	2769
HSA-MIR-20B-5P	99.88	74.01	2621
HSA-MIR-519D-3P	99.88	73.97	2607
HSA-MIR-526B-3P	99.88	74.06	2587
HSA-MIR-93-5P	99.88	73.98	2606
HSA-MIR-6814-5P	99.03	66.68	1273
HSA-MIR-12135	98.99	70.26	1814
HSA-MIR-4755-3P	98.77	65.59	1915

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 94.2% of screened cell lines, common-essential.

Literature-anchored findings (GeneRIF, showing 24)

• MYT1 binds to TSAP6 in tumor cells and has a role in cell cycle regulation (PMID:12606722)
• Myt1 is phosphorylated by polo-like kinase 1 (PMID:12738781)
• the induction of Cdc2 phosphorylation due to the increase of Wee1 and Myt1 as well as the reduction of Cdc2 and cyclin B1 are involved in 1,25[OH]2VD3-induced G2/M arrest of keratinocytes. (PMID:15175024)
• overexpressed during the S phase of the cell cycle compared with the G0/1 phase (PMID:16476973)
• The results show that Myt1-mediated suppression of Cdc2 activity is not indispensable for the regulation of a broad range of mitotic events but is specifically required for the control of intracellular membrane dynamics during mitosis in Hela cells. (PMID:18378775)
• Myt1 is inactivated by MEK1 mediated phosphorylation to fragment the Golgi complex in G2 and for the entry of cells into mitosis. (PMID:23241949)
• PKMYT1 positively regulated the growth, migration, colony formation, metastasis and epithelia mesenchymal transition of hepatocellular carcinoma cells (PMID:28648520)
• Study found that PKMYT1 was essential for the proliferation and mobility of CRC cells in vitro. Also, results demonstrated that patients expressing high level of PKMYT1 displayed a worse overall survival rate than those with a low level of PKMYT1. These data indicated that PKMYT1 was a biomarker for the prediction of the prognosis of the disease. (PMID:29658598)
• Overexpression of PKMYT1 indicates the poor prognosis and enhances proliferation and tumorigenesis in non-small cell lung cancer via activation of Notch signal pathway. (PMID:31173292)
• Cancer cells with intrinsic or acquired adavosertib resistance had higher levels of Myt1 compared with sensitive cancer cells. Downregulating Myt1 enhanced ectopic Cdk1 activity and restored sensitivity to adavosertib. Myt1 expression was associated with both a worse disease-free and overall survival in breast cancer patients. (PMID:31594837)
• Overexpression of PKMYT1 is always found in breast cancer. (PMID:31837068)
• PKMYT1 promoted the growth of prostate cancer cells through targeting CCNB1 and CCNE1 expression. (PMID:32234541)
• PKMYT1 aggravates the progression of ovarian cancer by targeting SIRT3. (PMID:32495859)
• Overexpression of PKMYT1 Facilitates Tumor Development and Is Correlated with Poor Prognosis in Clear Cell Renal Cell Carcinoma. (PMID:33024069)
• LncRNA PKMYT1AR promotes cancer stem cell maintenance in non-small cell lung cancer via activating Wnt signaling pathway. (PMID:34856993)
• PKMYT1, exacerbating the progression of clear cell renal cell carcinoma, is implied as a biomarker for the diagnosis and prognosis. (PMID:34959223)
• Demethylase ALKBH5 suppresses invasion of gastric cancer via PKMYT1 m6A modification. (PMID:35114989)
• CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition. (PMID:35444283)
• KDM2B mediates the Wnt/beta-catenin pathway through transcriptional activation of PKMYT1 via microRNA-let-7b-5p/EZH2 to affect the development of non-small cell lung cancer. (PMID:35580699)
• PKMYT1 inhibits lung adenocarcinoma progression by abrogating AKT1 activity. (PMID:36350496)
• Knockdown of PKMYT1 is associated with autophagy inhibition and apoptosis induction and suppresses tumor progression in hepatocellular carcinoma. (PMID:36512849)
• ELF3 promotes gemcitabine resistance through PKMYT1/CDK1 signaling pathway in gallbladder cancer. (PMID:36988891)
• PKMYT1: A Potential Target for CCNE1 Amplificated Colorectal Tumors. (PMID:37572218)
• PKMYT1 Promotes Epithelial-Mesenchymal Transition Process in Triple-Negative Breast Cancer by Activating Notch Signaling. (PMID:38442372)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
danio_rerio	pkmyt1	ENSDARG00000074730
mus_musculus	Pkmyt1	ENSMUSG00000023908
rattus_norvegicus	Pkmyt1	ENSRNOG00000003657
drosophila_melanogaster	Myt1	FBGN0040298
caenorhabditis_elegans		WBGENE00006938
caenorhabditis_elegans		WBGENE00006940

Paralogs (8): EIF2AK2 (ENSG00000055332), EIF2AK1 (ENSG00000086232), STK35 (ENSG00000125834), EIF2AK4 (ENSG00000128829), WEE1 (ENSG00000166483), EIF2AK3 (ENSG00000172071), PDIK1L (ENSG00000175087), WEE2 (ENSG00000214102)

Protein

Protein identifiers

Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase — Q99640 (reviewed: Q99640)

Alternative names: Myt1 kinase

All UniProt accessions (9): Q99640, A6NHV6, B4DZM6, I3L136, I3L1H7, I3L2S4, I3L3P0, I3L4K3, I3L4Y0

UniProt curated annotations — full annotation on UniProt →

Function. Acts as a negative regulator of entry into mitosis (G2 to M transition) by phosphorylation of the CDK1 kinase specifically when CDK1 is complexed to cyclins. Mediates phosphorylation of CDK1 predominantly on ‘Thr-14’. Also involved in Golgi fragmentation. May be involved in phosphorylation of CDK1 on ‘Tyr-15’ to a lesser degree, however tyrosine kinase activity is unclear and may be indirect.

Subunit / interactions. Interacts with CDC2-CCNB1 complex. Can also interact with PIN1 when phosphorylated by CDC2-CCNB1.

Subcellular location. Endoplasmic reticulum membrane. Golgi apparatus membrane.

Post-translational modifications. Autophosphorylated. Phosphorylated by CDC2-CCNB1 complexes on undefined serine and threonine residues. The phosphorylation by CDC2-CCNB1 complexes may inhibit the catalytic activity.

Activity regulation. Negatively regulated by hyperphosphorylation during mitosis. The hyperphosphorylated form does not associate with CCNB1-CDC2 complexes. The PLK1 protein kinase may be required for mitotic phosphorylation.

Domain organisation. The membrane-association motif is essential for the localization to membrane of Golgi stack. According to some authors, it is a transmembrane domain; the existence of a transmembrane region is however unproven.

Similarity. Belongs to the protein kinase superfamily. Ser/Thr protein kinase family. WEE1 subfamily.

Isoforms (4)

UniProt ID	Names	Canonical?
Q99640-1	1	yes
Q99640-2	2
Q99640-3	3
Q99640-4	4

RefSeq proteins (4): NP_001245379, NP_001245380, NP_004194, NP_872629 (=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
IPR016235	Tyr/Thr_kinase_Cdc2_inhib	Family
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR050339	CC_SR_Kinase	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 (72 total): helix 14, modified residue 12, strand 11, sequence variant 6, binding site 5, region of interest 5, sequence conflict 4, turn 4, splice variant 3, mutagenesis site 3, chain 1, domain 1, short sequence motif 1, compositionally biased region 1, active site 1

Structure

Experimental structures (PDB)

25 structures.

PDB	Method	Resolution (Å)
5VCZ	X-RAY DIFFRACTION	1.5
8ZUD	X-RAY DIFFRACTION	1.51
5VCY	X-RAY DIFFRACTION	1.56
23FW	X-RAY DIFFRACTION	1.59
3P1A	X-RAY DIFFRACTION	1.7
5VD1	X-RAY DIFFRACTION	1.7
8ZTX	X-RAY DIFFRACTION	1.7
23ES	X-RAY DIFFRACTION	1.74
8ZU2	X-RAY DIFFRACTION	1.8
5VD3	X-RAY DIFFRACTION	1.8
8ZUL	X-RAY DIFFRACTION	1.8
8WJY	X-RAY DIFFRACTION	1.88
5VCV	X-RAY DIFFRACTION	1.92
9LGN	X-RAY DIFFRACTION	2.03
9LGV	X-RAY DIFFRACTION	2.04
9LID	X-RAY DIFFRACTION	2.06
5VD0	X-RAY DIFFRACTION	2.13
8D6E	X-RAY DIFFRACTION	2.15
9LGL	X-RAY DIFFRACTION	2.17
8D6C	X-RAY DIFFRACTION	2.2
5VCW	X-RAY DIFFRACTION	2.25
8D6D	X-RAY DIFFRACTION	2.35
9M6P	X-RAY DIFFRACTION	2.38
8D6F	X-RAY DIFFRACTION	2.49
5VCX	X-RAY DIFFRACTION	2.7

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q99640-F1	76.24	0.56

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): 233 (proton acceptor)

Ligand- & substrate-binding residues (5): 116–124; 139; 238; 251; 253

Post-translational modifications (12): 1, 17, 40, 94, 120, 143, 160, 426, 469, 473, 482, 495

Mutagenesis-validated functional residues (3):

Position	Phenotype
238	loss of kinase activity.
251	loss of kinase activity.
486–488	loss of cdc2-ccnb1 interaction.

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-156711	Polo-like kinase mediated events
R-HSA-69273	Cyclin A/B1/B2 associated events during G2/M transition
R-HSA-69478	G2/M DNA replication checkpoint

MSigDB gene sets: 473 (showing top): GSE18804_BRAIN_VS_COLON_TUMORAL_MACROPHAGE_UP, E2F_Q4, MODULE_52, E2F_Q4_01, GOBP_NEGATIVE_REGULATION_OF_REPRODUCTIVE_PROCESS, TAATAAT_MIR126, GGTGTGT_MIR329, TGCGCANK_UNKNOWN, E2F4DP1_01, GOBP_REGULATION_OF_PHOSPHORYLATION, GOBP_REGULATION_OF_NUCLEAR_DIVISION, TGCACTT_MIR519C_MIR519B_MIR519A, GCANCTGNY_MYOD_Q6, GOBP_CELL_CYCLE_PHASE_TRANSITION, DACOSTA_UV_RESPONSE_VIA_ERCC3_UP

GO Biological Process (8): regulation of cyclin-dependent protein serine/threonine kinase activity (GO:0000079), G2/M transition of mitotic cell cycle (GO:0000086), mitotic cell cycle (GO:0000278), regulation of mitotic nuclear division (GO:0007088), negative regulation of G2/M transition of mitotic cell cycle (GO:0010972), meiotic cell cycle (GO:0051321), negative regulation of G2/MI transition of meiotic cell cycle (GO:0110031), protein phosphorylation (GO:0006468)

GO Molecular Function (9): protein kinase activity (GO:0004672), protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), kinase activity (GO:0016301), metal ion binding (GO:0046872), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein binding (GO:0005515), transferase activity (GO:0016740)

GO Cellular Component (10): Golgi membrane (GO:0000139), nucleus (GO:0005634), nucleoplasm (GO:0005654), nucleolus (GO:0005730), cytoplasm (GO:0005737), endoplasmic reticulum (GO:0005783), endoplasmic reticulum membrane (GO:0005789), Golgi apparatus (GO:0005794), cytosol (GO:0005829), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
G2/M Transition	2
G2/M Checkpoints	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	4
intracellular membrane-bounded organelle	3
cytoplasm	3
cell cycle	2
mitotic nuclear division	2
negative regulation of cell cycle G2/M phase transition	2
protein kinase activity	2
nuclear lumen	2
endomembrane system	2
cyclin-dependent protein serine/threonine kinase activity	1
regulation of protein serine/threonine kinase activity	1
mitotic cell cycle	1
mitotic cell cycle phase transition	1
cell cycle G2/M phase transition	1
regulation of mitotic cell cycle	1
regulation of cell cycle process	1
regulation of nuclear division	1
G2/M transition of mitotic cell cycle	1
regulation of G2/M transition of mitotic cell cycle	1
negative regulation of mitotic cell cycle phase transition	1
sexual reproduction	1
reproductive process	1
meiotic nuclear division	1
G2/MI transition of meiotic cell cycle	1
regulation of G2/MI transition of meiotic cell cycle	1
negative regulation of meiotic cell cycle phase transition	1
phosphorylation	1
protein modification process	1
kinase activity	1
phosphotransferase activity, alcohol group as acceptor	1
catalytic activity, acting on a protein	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
transferase activity, transferring phosphorus-containing groups	1
cation binding	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
binding	1
catalytic activity	1
Golgi apparatus	1

Protein interactions and networks

STRING

2052 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PKMYT1	STEAP3	Q658P3	908
PKMYT1	BNIP3L	O60238	823
PKMYT1	MYT1	Q01538	803
PKMYT1	TPT1	P13693	796
PKMYT1	CDC25A	P30304	717
PKMYT1	CDC20	Q12834	690
PKMYT1	BUB1	O43683	675
PKMYT1	BNIP3	Q12983	666
PKMYT1	PTTG1	O95997	618
PKMYT1	ORC6	Q9Y5N6	602
PKMYT1	CDC25C	P30307	567
PKMYT1	PLK1	P53350	557
PKMYT1	NCAPH	Q15003	539
PKMYT1	CDC25B	P30305	530
PKMYT1	CCNB1	P14635	517

IntAct

78 interactions, top by confidence:

A	B	Type	Score
BCL2	BCL2L11	psi-mi:“MI:0914”(association)	0.930
CDK1	PKMYT1	psi-mi:“MI:0217”(phosphorylation reaction)	0.890
PKMYT1	CDK1	psi-mi:“MI:0217”(phosphorylation reaction)	0.890
PKMYT1	CCNB1	psi-mi:“MI:0915”(physical association)	0.870
CCNB1	PKMYT1	psi-mi:“MI:0915”(physical association)	0.870
PKMYT1	CCNB1	psi-mi:“MI:2364”(proximity)	0.870
CCNB1	PKMYT1	psi-mi:“MI:2364”(proximity)	0.870
CDK1	CCNB2	psi-mi:“MI:0914”(association)	0.840
PKMYT1	CCNB2	psi-mi:“MI:0914”(association)	0.730
CCNB2	CDKN1B	psi-mi:“MI:0914”(association)	0.670
CCNA2	GMNN	psi-mi:“MI:0914”(association)	0.640
SPINT2	UPK3BL1	psi-mi:“MI:0914”(association)	0.530
CKS2	GMNN	psi-mi:“MI:0914”(association)	0.530
CKS1B	GMNN	psi-mi:“MI:0914”(association)	0.530
IL4R	RHOBTB3	psi-mi:“MI:0914”(association)	0.530
TMEM9	ESYT2	psi-mi:“MI:0914”(association)	0.530
FAM20C	PKMYT1	psi-mi:“MI:0217”(phosphorylation reaction)	0.440
PKMYT1	PPP1CA	psi-mi:“MI:0407”(direct interaction)	0.440
Cdk1		psi-mi:“MI:0915”(physical association)	0.400
Tubg1	BDP1	psi-mi:“MI:0914”(association)	0.350
Cdk1	CHEK1	psi-mi:“MI:0914”(association)	0.350
Cdk1	IFT88	psi-mi:“MI:0914”(association)	0.350
CCNA2	ZC3H18	psi-mi:“MI:0914”(association)	0.350

BioGRID (215): PKMYT1 (Affinity Capture-MS), PKMYT1 (Affinity Capture-MS), PKMYT1 (Affinity Capture-MS), PKMYT1 (Affinity Capture-MS), PKMYT1 (Affinity Capture-MS), PKMYT1 (Synthetic Growth Defect), PKMYT1 (Proximity Label-MS), PKMYT1 (Affinity Capture-MS), PKMYT1 (Affinity Capture-MS), PKMYT1 (Affinity Capture-MS), PKMYT1 (Affinity Capture-MS), PKMYT1 (Affinity Capture-MS), PKMYT1 (Affinity Capture-MS), PKMYT1 (Affinity Capture-MS), PKMYT1 (Affinity Capture-MS)

ESM2 similar proteins: A6NGC4, A6NKX4, A6NM10, F1NZP5, O96011, P0C242, P27544, P27545, Q0VCY6, Q2TBI8, Q3SYU3, Q4V8E5, Q5F2F2, Q5JZQ7, Q5RFI0, Q5U2T1, Q5U419, Q6AYM9, Q6GQT6, Q6PIS1, Q6TCG5, Q6UXD7, Q6UXT9, Q71RH2, Q7TNV1, Q7Z403, Q80ZE4, Q863Y8, Q86WI3, Q8BMT9, Q8CHK3, Q8IU68, Q8IXF9, Q8N9H8, Q8TBR7, Q8VC26, Q8WUG5, Q96N66, Q99640, Q99JT6

Diamond homologs: A4K2Q5, A4K2S1, A4PES0, A4QNA8, A5D791, D2HHP1, E1BTE1, E2RSS3, F4I1N8, O02827, O13148, O13889, O18209, O22042, O57473, O80397, P07527, P0C1S8, P11799, P15442, P27636, P29294, P30291, P32581, P33279, P47810, P47817, P54350, P54737, Q15746, Q1LX51, Q28824, Q4R8E0, Q54E34, Q54F40, Q54JQ1, Q54RP7, Q54ZN3, Q558U1, Q55F45

SIGNOR signaling

8 interactions.

A	Effect	B	Mechanism
MAPK8	up-regulates	PKMYT1	phosphorylation
PLK1	unknown	PKMYT1	phosphorylation
CDK1	“down-regulates activity”	PKMYT1	phosphorylation
PKMYT1	down-regulates	CDK1	phosphorylation
PLK1	“down-regulates activity”	PKMYT1	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 90 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
TP53 Regulates Transcription of Cell Cycle Genes	5	47.7×	1e-05
Cyclin A/B1/B2 associated events during G2/M transition	5	27.1×	1e-04
The role of GTSE1 in G2/M progression after G2 checkpoint	5	14.1×	1e-03
Regulation of PLK1 Activity at G2/M Transition	5	11.1×	3e-03
Mitotic G2-G2/M phases	5	11.1×	3e-03
G2/M Transition	5	11.1×	3e-03
Cell Cycle Checkpoints	5	7.8×	7e-03
Transcriptional Regulation by TP53	6	6.5×	5e-03

GO biological processes:

GO term	Partners	Fold	FDR
G2/M transition of mitotic cell cycle	6	22.8×	2e-04
G1/S transition of mitotic cell cycle	6	14.7×	1e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	92
Likely benign	2
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

7142 predictions. Top by Δscore:

Variant	Effect	Δscore
16:2969836:GCACG:G	donor_gain	1.0000
16:2969837:CACGG:C	donor_loss	1.0000
16:2969839:CGG:C	donor_loss	1.0000
16:2969840:GGT:G	donor_loss	1.0000
16:2971513:AGG:A	acceptor_gain	1.0000
16:2971514:GGG:G	acceptor_gain	1.0000
16:2973998:AC:A	donor_gain	1.0000
16:2973999:CC:C	donor_gain	1.0000
16:2974239:GCTTA:G	donor_loss	1.0000
16:2974240:CTTAC:C	donor_loss	1.0000
16:2974241:TTA:T	donor_loss	1.0000
16:2974242:TA:T	donor_loss	1.0000
16:2974244:C:CG	donor_loss	1.0000
16:2974383:C:CT	acceptor_gain	1.0000
16:2974546:TCA:T	donor_loss	1.0000
16:2974549:CCGG:C	donor_gain	1.0000
16:2974652:CCAGA:C	acceptor_gain	1.0000
16:2974653:CAGA:C	acceptor_gain	1.0000
16:2974653:CAGAC:C	acceptor_gain	1.0000
16:2974654:AGA:A	acceptor_gain	1.0000
16:2974655:GA:G	acceptor_gain	1.0000
16:2974656:ACTGG:A	acceptor_loss	1.0000
16:2974657:C:A	acceptor_loss	1.0000
16:2974657:C:CC	acceptor_gain	1.0000
16:2974661:C:CT	acceptor_gain	1.0000
16:2974667:CGGGA:C	acceptor_gain	1.0000
16:2974668:G:T	acceptor_gain	1.0000
16:2974671:A:AC	acceptor_gain	1.0000
16:2974671:A:C	acceptor_gain	1.0000
16:2976660:TCA:T	donor_loss	1.0000

AlphaMissense

3175 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
16:2975774:C:A	K139N	0.997
16:2975774:C:G	K139N	0.997
16:2975321:G:C	F290L	0.995
16:2975321:G:T	F290L	0.995
16:2975323:A:G	F290L	0.995
16:2975486:C:A	K235N	0.993
16:2975486:C:G	K235N	0.993
16:2975438:G:C	D251E	0.992
16:2975438:G:T	D251E	0.992
16:2974656:A:C	S291R	0.990
16:2974656:A:T	S291R	0.990
16:2975320:T:G	S291R	0.990
16:2975439:T:A	D251V	0.990
16:2975490:A:T	V234D	0.989
16:2975660:C:A	W177C	0.989
16:2975660:C:G	W177C	0.989
16:2975488:T:C	K235E	0.987
16:2975781:G:T	A137E	0.987
16:2975776:T:C	K139E	0.986
16:2975439:T:G	D251A	0.985
16:2975492:A:C	D233E	0.985
16:2975492:A:T	D233E	0.985
16:2975493:T:A	D233V	0.984
16:2974583:G:T	R316S	0.982
16:2975477:G:C	N238K	0.982
16:2975477:G:T	N238K	0.982
16:2976712:G:C	F110L	0.982
16:2976712:G:T	F110L	0.982
16:2976714:A:G	F110L	0.982
16:2975439:T:C	D251G	0.981

dbSNP variants (sampled 300 via entrez): RS1000174286 (16:2973725 C>A,G), RS1000390064 (16:2978148 G>A), RS1000442249 (16:2978315 G>A), RS1000961499 (16:2978952 G>A,C), RS1001288145 (16:2973325 G>A,C), RS1001328420 (16:2978661 T>A,C), RS1001735033 (16:2982224 C>T), RS1002145024 (16:2979461 C>T), RS1002300473 (16:2974302 C>A), RS1002476845 (16:2980555 G>C), RS1002601005 (16:2975146 G>T), RS1003856887 (16:2973628 C>T), RS1004133165 (16:2978633 A>G), RS1004638537 (16:2976416 G>C), RS1004767565 (16:2980569 G>A)

Disease associations

OMIM: gene MIM:602474 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST000753_6	Metabolic syndrome	6.000000e-06

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0000195	metabolic syndrome
EFO:0004343	waist-hip ratio

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3984 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

14 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 173,089 (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
CHEMBL1421	DASATINIB ANHYDROUS	4	55,003
CHEMBL288441	BOSUTINIB	4	12,255
CHEMBL5416410	DASATINIB	4	655
CHEMBL217092	SARACATINIB	3	3,982
CHEMBL297453	EPIGALOCATECHIN GALLATE	3	22,804
CHEMBL498485	ICARITIN	3	700
CHEMBL151	LUTEOLIN	2	23,523
CHEMBL1976040	ADAVOSERTIB	2	1,738
CHEMBL3545396	BMS-690514	2	567
CHEMBL44	GENISTEIN	2	44,212
CHEMBL5199076	LUNRESERTIB	2	34
CHEMBL564829	MILCICLIB	2	821
CHEMBL607707	PELITINIB	2	6,340
CHEMBL49120	PD-0166285	1	455

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — WEE family

Most potent curated ligand interactions (2 total), top 2:

Ligand	Action	Affinity	Parameter
(S)-RP-6306	Inhibition	8.7	pIC50
PD166285	Inhibition	8.15	pIC50

Binding affinities (BindingDB)

93 measured of 293 human assays (293 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
US20250197405, Compound 7	IC50	1.5 nM	US-20250197405: HETEROAROMATIC COMPOUNDS AS PKMYT1 INHIBITORS AND USE THEREOF
US20250197405, Compound 12-P2	IC50	1.5 nM	US-20250197405: HETEROAROMATIC COMPOUNDS AS PKMYT1 INHIBITORS AND USE THEREOF
6-amino-7-(3-fluoro-5-hydroxy-2,6-dimethylphenyl)-2-methylpyrrolo[2,3-d]pyrimidine-5-carboxamide	IC50	1.8 nM	US-20250197405: HETEROAROMATIC COMPOUNDS AS PKMYT1 INHIBITORS AND USE THEREOF
6-amino-7-(3-hydroxy-2,6-dimethylphenyl)-2-methylpyrrolo[2,3-d]pyrimidine-5-carboxamide	IC50	2.1 nM	US-20250197405: HETEROAROMATIC COMPOUNDS AS PKMYT1 INHIBITORS AND USE THEREOF
US20250197405, Compound 11	IC50	2.3 nM	US-20250197405: HETEROAROMATIC COMPOUNDS AS PKMYT1 INHIBITORS AND USE THEREOF
US20250197405, Compound 9	IC50	2.8 nM	US-20250197405: HETEROAROMATIC COMPOUNDS AS PKMYT1 INHIBITORS AND USE THEREOF
6-amino-7-(3-hydroxy-2,6-dimethylphenyl)-2-methylpyrrolo[2,3-d]pyrimidine-5-carboxamide	IC50	3 nM	US-20250197405: HETEROAROMATIC COMPOUNDS AS PKMYT1 INHIBITORS AND USE THEREOF
US20250197405, Compound 10	IC50	3.4 nM	US-20250197405: HETEROAROMATIC COMPOUNDS AS PKMYT1 INHIBITORS AND USE THEREOF
US20250197405, Compound 5-P1	IC50	3.9 nM	US-20250197405: HETEROAROMATIC COMPOUNDS AS PKMYT1 INHIBITORS AND USE THEREOF
6-amino-7-(2-chloro-3-hydroxy-6-methylphenyl)-2-methylpyrrolo[2,3-d]pyrimidine-5-carboxamide	IC50	4.1 nM	US-20250197405: HETEROAROMATIC COMPOUNDS AS PKMYT1 INHIBITORS AND USE THEREOF
6-amino-7-(3-hydroxy-2,6-dimethylphenyl)-2-(trifluoromethyl)pyrrolo[2,3-d]pyrimidine-5-carboxamide	IC50	8.9 nM	US-20250197405: HETEROAROMATIC COMPOUNDS AS PKMYT1 INHIBITORS AND USE THEREOF
2-amino-1-(3-hydroxy-2,6-dimethylphenyl)-5,6-dimethyl-4-oxopyrrolo[3,2-c]pyridine-3-carboxamide	IC50	11.9 nM	US-20250197405: HETEROAROMATIC COMPOUNDS AS PKMYT1 INHIBITORS AND USE THEREOF
US20250197405, Compound 8	IC50	13 nM	US-20250197405: HETEROAROMATIC COMPOUNDS AS PKMYT1 INHIBITORS AND USE THEREOF
BMS-354825	KD	27 nM
2,4-dimethyl-3-[2-(6-methyl-3-pyridinyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]phenol	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
2,4-dimethyl-3-[2-(2-methylpyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridin-5-yl]phenol	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
3-[2-(5-methoxy-3-pyridinyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]-2,4-dimethylphenol	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
4-[5-(3-hydroxy-2,6-dimethylphenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl]-1-methylpyridin-2-one	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
3-[7-fluoro-6-(2-methylpyrimidin-5-yl)-5H-pyrrolo[2,3-b]pyrazin-2-yl]-2,4-dimethylphenol	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
2,4-dimethyl-3-[7-methyl-6-(2-methylpyrimidin-5-yl)-5H-pyrrolo[2,3-b]pyrazin-2-yl]phenol	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
2,4-dimethyl-3-[6-(2-methylpyrimidin-5-yl)-5H-pyrrolo[2,3-b]pyrazin-2-yl]phenol	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
2,4-dimethyl-3-[6-(2-methyl-1,3-thiazol-5-yl)-5H-pyrrolo[2,3-b]pyrazin-2-yl]phenol	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
5-(3-hydroxy-2,6-dimethylphenyl)-2-(2-methylpyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
2-(3,6-dihydro-2H-pyran-5-yl)-5-(3-hydroxy-2,6-dimethylphenyl)-1H-pyrrolo[2,3-b]pyridine-4-carbonitrile	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
3-chloro-5-(3-hydroxy-2,6-dimethylphenyl)-2-(5-methyl-6-oxo-1H-pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine-4-carbonitrile	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
2-(2,4-dimethylpyrimidin-5-yl)-5-(3-hydroxy-2,6-dimethylphenyl)-1H-pyrrolo[2,3-b]pyridine-4-carbonitrile	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
3-[7-chloro-6-(2-methylpyrimidin-5-yl)-5H-pyrrolo[2,3-b]pyrazin-2-yl]-2,4-dimethylphenol	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
3-[2-[2-(2-hydroxypropan-2-yl)pyrimidin-5-yl]-1H-pyrrolo[2,3-b]pyridin-5-yl]-2,4-dimethylphenol	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
5-(2-ethyl-3-hydroxy-6-methylphenyl)-2-(2-methylpyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-4-carbonitrile	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
5-(3-hydroxy-2,6-dimethylphenyl)-2-[2-[methyl(oxetan-3-yl)amino]pyrimidin-5-yl]-1H-pyrrolo[2,3-b]pyridine-4-carbonitrile	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
3-cyclopropyl-5-(3-hydroxy-2,6-dimethylphenyl)-2-(2-methylpyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-4-carbonitrile	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
5-(3-hydroxy-2,6-dimethylphenyl)-2-(2-methylpyrimidin-5-yl)-3-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridine-4-carbonitrile	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
5-(3-hydroxy-2,6-dimethylphenyl)-2-(2H-triazol-4-yl)-1H-pyrrolo[2,3-b]pyridine-4-carbonitrile	IC50	30 nM	US-20250136596: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
[6-amino-5-(3-hydroxy-2,6-dimethylphenyl)-2,3-dimethylpyrrolo[2,3-b]pyrazin-7-yl]-[2-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[1,5-a]pyrazin-7-yl]methanone	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
[6-amino-5-(3-hydroxy-2,6-dimethylphenyl)-2,3-dimethylpyrrolo[2,3-b]pyrazin-7-yl]-(6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-5-yl)methanone	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
[6-amino-5-(3-hydroxy-2,6-dimethylphenyl)-2,3-dimethylpyrrolo[2,3-b]pyrazin-7-yl]-(2-methyl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl)methanone	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
[2-amino-5-chloro-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]pyridin-3-yl]-(6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-5-yl)methanone	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
[2-amino-5-chloro-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]pyridin-3-yl]-(6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-5-yl)methanone	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
[2-amino-5-chloro-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]pyridin-3-yl]-(2-methyl-6,8-dihydro-5H-[1,2,4]triazolo[1,5-a]pyrazin-7-yl)methanone	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
[2-amino-5-chloro-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]pyridin-3-yl]-(2-methyl-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-5-yl)methanone	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
[2-amino-5-chloro-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]pyridin-3-yl]-[2-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[1,5-a]pyrazin-7-yl]methanone	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
2-[6-amino-5-(3-hydroxy-2,6-dimethylphenyl)-2,3-dimethylpyrrolo[2,3-b]pyrazine-7-carbonyl]-3,4-dihydro-1H-pyrido[1,2-a]pyrazin-6-one	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
[6-amino-5-(3-hydroxy-2,6-dimethylphenyl)-2,3-dimethylpyrrolo[2,3-b]pyrazin-7-yl]-[3-(2-hydroxypropan-2-yl)-6,8-dihydro-5H-imidazo[1,5-a]pyrazin-7-yl]methanone	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
[6-amino-5-(3-hydroxy-2,6-dimethylphenyl)-2,3-dimethylpyrrolo[2,3-b]pyrazin-7-yl]-(7,8-dihydro-5H-pyrido[3,4-b]pyrazin-6-yl)methanone	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
[6-amino-5-(4-fluoro-3-hydroxy-2,6-dimethylphenyl)-2,3-dimethylpyrrolo[2,3-b]pyrazin-7-yl]-(6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-5-yl)methanone	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
[6-amino-2-ethenyl-5-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]pyrazin-7-yl]-(6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-5-yl)methanone	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
[6-amino-5-(3-hydroxy-2,6-dimethylphenyl)-2-methyl-3-(1-methylpiperidin-4-yl)pyrrolo[2,3-b]pyrazin-7-yl]-(6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-5-yl)methanone	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
[6-amino-5-(3-hydroxy-2,6-dimethylphenyl)-3-[(3R)-3-hydroxypiperidin-1-yl]-2-methylpyrrolo[2,3-b]pyrazin-7-yl]-(6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-5-yl)methanone	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
[6-amino-5-(3-hydroxy-2,6-dimethylphenyl)-3-methyl-2-prop-1-ynylpyrrolo[2,3-b]pyrazin-7-yl]-(6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-5-yl)methanone	IC50	30 nM	US-20250163077: MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF
6-amino-7-(3-hydroxy-2,6-dimethylphenyl)-2-methylpyrrolo[2,3-d]pyrimidine-5-carboxamide	IC50	46.1 nM	US-20250197405: HETEROAROMATIC COMPOUNDS AS PKMYT1 INHIBITORS AND USE THEREOF

ChEMBL bioactivities

408 potent at pChembl≥5 of 445 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.00	Ki	0.1	nM	CHEMBL6133305
10.00	Ki	0.1	nM	CHEMBL6164722
10.00	Ki	0.1	nM	CHEMBL6146271
9.77	Ki	0.17	nM	CHEMBL6168984
9.74	Ki	0.18	nM	CHEMBL6172486
9.72	Ki	0.19	nM	CHEMBL6165232
9.68	Ki	0.21	nM	LUNRESERTIB
9.64	Ki	0.23	nM	CHEMBL6143148
9.64	Ki	0.23	nM	CHEMBL6147496
9.62	Ki	0.24	nM	CHEMBL6143248
9.39	Ki	0.41	nM	CHEMBL6174118
9.36	Ki	0.44	nM	CHEMBL6143411
9.31	Ki	0.49	nM	CHEMBL6151763
9.30	Ki	0.5	nM	DASATINIB
9.30	Ki	0.5	nM	CHEMBL4583196
9.25	Ki	0.56	nM	CHEMBL6165924
9.19	Ki	0.64	nM	CHEMBL6145586
9.10	Ki	0.8	nM	PD-0166285
9.10	Ki	0.8	nM	CHEMBL6141720
9.00	IC50	1	nM	CHEMBL5201803
9.00	IC50	1	nM	CHEMBL5174684
9.00	IC50	1	nM	CHEMBL5196713
9.00	IC50	1	nM	LUNRESERTIB
9.00	IC50	1	nM	CHEMBL6160250
8.97	Ki	1.06	nM	CHEMBL6152793
8.86	Ki	1.38	nM	CHEMBL6163921
8.84	Ki	1.45	nM	CHEMBL6160115
8.83	Ki	1.48	nM	CHEMBL6144020
8.82	IC50	1.5	nM	CHEMBL6148600
8.80	IC50	1.6	nM	LUNRESERTIB
8.80	IC50	1.6	nM	CHEMBL6166891
8.74	IC50	1.8	nM	CHEMBL6141923
8.72	IC50	1.9	nM	CHEMBL6142087
8.72	IC50	1.9	nM	CHEMBL6146271
8.70	Ki	2	nM	PD-0166285
8.70	Ki	1.995	nM	PD-0166285
8.70	IC50	2	nM	LUNRESERTIB
8.68	IC50	2.1	nM	CHEMBL6134190
8.68	IC50	2.1	nM	LUNRESERTIB
8.68	IC50	2.1	nM	CHEMBL6142344
8.66	IC50	2.2	nM	CHEMBL6164722
8.66	IC50	2.2	nM	CHEMBL6143148
8.64	Ki	2.3	nM	CHEMBL106772
8.64	IC50	2.3	nM	CHEMBL6142455
8.62	IC50	2.4	nM	CHEMBL6160348
8.60	Ki	2.5	nM	CHEMBL6145221
8.60	IC50	2.5	nM	CHEMBL6143248
8.60	IC50	2.5	nM	CHEMBL6147496
8.59	IC50	2.6	nM	CHEMBL5566629
8.54	IC50	2.9	nM	CHEMBL5200005

PubChem BioAssay actives

253 with measured affinity, of 902 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
N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide;hydrate	1396666: Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay	ki	0.0005	uM
N-(2-chlorophenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide	1532002: Displacement of (6-FAM)KI(pY)VV from full length PKMYT1 (unknown origin) by fluorescence polarization immuno assay	ki	0.0005	uM
6-(2,6-dichlorophenyl)-2-[4-[2-(diethylamino)ethoxy]anilino]-8-methylpyrido[2,3-d]pyrimidin-7-one	1396666: Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay	ki	0.0008	uM
6-amino-2-cyclopropyl-5-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]pyrazine-7-carboxamide	1885733: Inhibition of full length Nano-luc fused PKMYT1 in human HEK-293T cells incubated for 2 hrs by cell based NanoBRET target engagement assay	ic50	0.0010	uM
2-amino-5-chloro-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]pyridine-3-carboxamide	1885733: Inhibition of full length Nano-luc fused PKMYT1 in human HEK-293T cells incubated for 2 hrs by cell based NanoBRET target engagement assay	ic50	0.0010	uM
2-amino-1-(3-hydroxy-2,6-dimethylphenyl)-5-methylpyrrolo[2,3-b]pyridine-3-carboxamide	1885733: Inhibition of full length Nano-luc fused PKMYT1 in human HEK-293T cells incubated for 2 hrs by cell based NanoBRET target engagement assay	ic50	0.0010	uM
2-amino-1-(3-hydroxy-2,6-dimethylphenyl)-5,6-dimethylpyrrolo[2,3-b]pyridine-3-carboxamide	1885733: Inhibition of full length Nano-luc fused PKMYT1 in human HEK-293T cells incubated for 2 hrs by cell based NanoBRET target engagement assay	ic50	0.0020	uM
6-(2,6-dichlorophenyl)-8-methyl-2-(4-morpholin-4-ylanilino)pyrido[2,3-d]pyrimidin-7-one	1396666: Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay	ki	0.0023	uM
2-amino-5-cyclopropyl-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]pyridine-3-carboxamide	1885733: Inhibition of full length Nano-luc fused PKMYT1 in human HEK-293T cells incubated for 2 hrs by cell based NanoBRET target engagement assay	ic50	0.0030	uM
2-amino-6-bromo-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0030	uM
2-amino-5-bromo-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0030	uM
2-amino-1-(3-hydroxy-2,6-dimethylphenyl)-8-(2-methylpyrazol-3-yl)pyrrolo[3,2-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0030	uM
2-amino-8-(cyclopenten-1-yl)-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[3,2-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0030	uM
2-amino-8-bromo-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[3,2-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0030	uM
2-amino-1-(3-hydroxy-2,6-dimethylphenyl)-6-(2-methylpyrazol-3-yl)pyrrolo[2,3-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0040	uM
2-amino-8-cyano-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[3,2-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0040	uM
6-amino-5-(3-hydroxy-2,6-dimethylphenyl)-2,3-dimethylpyrrolo[2,3-b]pyrazine-7-carboxamide	1885733: Inhibition of full length Nano-luc fused PKMYT1 in human HEK-293T cells incubated for 2 hrs by cell based NanoBRET target engagement assay	ic50	0.0050	uM
2-amino-6-cyano-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0050	uM
2-amino-6-(cyclopenten-1-yl)-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0050	uM
2-amino-1-(2-chloro-3-hydroxy-6-methylphenyl)pyrrolo[3,2-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0050	uM
2-amino-7-bromo-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[3,2-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0050	uM
2-amino-5-cyano-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0050	uM
2-amino-1-(3-hydroxy-2,6-dimethylphenyl)-5-(2-methylpyrazol-3-yl)pyrrolo[2,3-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0060	uM
2-amino-5-chloro-1-(3-hydroxy-2,6-dimethylphenyl)-6-methylpyrrolo[2,3-b]pyridine-3-carboxamide	1885732: Inhibition of N-terminal recombinant PKMYT1 (76 to 362 residues) in CCNE1 amplified human FU-OV-1 cells assessed as phosphorylation of CDK1 at Thr14 incubated for 2 hrs by AlphaLisa assay	ic50	0.0070	uM
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149017: Binding affinity to human PKMYT1 incubated for 45 mins by Kinobead based pull down assay	kd	0.0073	uM
2-amino-5-(cyclopenten-1-yl)-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0080	uM
2-amino-1-(2,6-dichloro-3-hydroxyphenyl)pyrrolo[3,2-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0080	uM
2-amino-1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[3,2-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0080	uM
2-amino-1-(3-hydroxy-2-methylphenyl)pyrrolo[3,2-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0100	uM
2-amino-1-(6-chloro-3-hydroxy-2-methylphenyl)pyrrolo[3,2-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0100	uM
6-(2,6-dichlorophenyl)-2-(4-fluoro-3-methylanilino)-8-methylpyrido[2,3-d]pyrimidin-7-one	1396666: Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay	ki	0.0104	uM
N-methyl-2-[[5-methyl-2-[3-(methylsulfonylmethyl)anilino]pyrimidin-4-yl]amino]benzamide	1396666: Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay	ki	0.0109	uM
1-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[3,2-b]quinoxaline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0110	uM
6-amino-5-(3-hydroxy-2,6-dimethylphenyl)pyrrolo[2,3-b]pyrazine-7-carboxamide	1885733: Inhibition of full length Nano-luc fused PKMYT1 in human HEK-293T cells incubated for 2 hrs by cell based NanoBRET target engagement assay	ic50	0.0120	uM
2-amino-1-(5-hydroxy-2-methylphenyl)pyrrolo[2,3-b]quinoline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0120	uM
Bosutinib	1396666: Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay	ki	0.0127	uM
2-amino-5-[2-[(3R)-3-aminopyrrolidin-1-yl]-6-fluoro-4-pyridinyl]-3-(3-hydroxy-2,6-dimethylphenyl)benzamide	2122447: Inhibition of recombinant human GST-tagged PKMYT1 (75 to 362 residues) expressed in insect cells using GTDEGIYDVPLLG as substrate preincubated for 15 mins followed by substrate and ATP addition and measured after 1 hr by ADP-Glo kinase assay	ic50	0.0165	uM
4-methyl-3-[(6-methylsulfonylquinolin-4-yl)amino]phenol	1396666: Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay	ki	0.0169	uM
(4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(1R)-1-carboxy-2-sulfanylethyl]amino]-1-oxohexan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-1-oxo-3-(4-phosphonooxyphenyl)propan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[2-[[(2S,3S)-2-[[(2S)-6-amino-2-[[(2S)-2,5-diamino-5-oxopentanoyl]amino]hexanoyl]amino]-3-methylpentanoyl]amino]acetyl]amino]-5-oxopentanoic acid	643482: Activity at full length human Myt1 expressed in human HEK293 cells at 10 uM after 30 mins by fluorescence polarization immunoassay	ec50	0.0180	uM
6-amino-5-(3-hydroxy-2,6-dimethylphenyl)-2-(2-hydroxypropan-2-yl)pyrrolo[2,3-b]pyrazine-7-carboxamide	1885733: Inhibition of full length Nano-luc fused PKMYT1 in human HEK-293T cells incubated for 2 hrs by cell based NanoBRET target engagement assay	ic50	0.0230	uM
6-amino-5-(3-hydroxy-2,6-dimethylphenyl)-2-morpholin-4-ylpyrrolo[2,3-b]pyrazine-7-carboxamide	1885732: Inhibition of N-terminal recombinant PKMYT1 (76 to 362 residues) in CCNE1 amplified human FU-OV-1 cells assessed as phosphorylation of CDK1 at Thr14 incubated for 2 hrs by AlphaLisa assay	ic50	0.0250	uM
2-[[5-chloro-2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]amino]-N-methylbenzamide	1396666: Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay	ki	0.0257	uM
2-amino-1-(5-hydroxy-2-methylphenyl)pyrrolo[3,2-b]quinoline-3-carboxamide	1885725: Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay	ic50	0.0290	uM
2-[[5-cyano-2-[3-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzamide	1396666: Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay	ki	0.0324	uM
2-[[5-cyano-2-[4-methoxy-3-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzamide	1532002: Displacement of (6-FAM)KI(pY)VV from full length PKMYT1 (unknown origin) by fluorescence polarization immuno assay	ki	0.0324	uM
6-amino-5-(3-hydroxy-2,6-dimethylphenyl)-2-(1,3-thiazol-2-yl)pyrrolo[2,3-b]pyrazine-7-carboxamide	1885732: Inhibition of N-terminal recombinant PKMYT1 (76 to 362 residues) in CCNE1 amplified human FU-OV-1 cells assessed as phosphorylation of CDK1 at Thr14 incubated for 2 hrs by AlphaLisa assay	ic50	0.0340	uM
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(oxan-4-yloxy)quinazolin-4-amine	1396666: Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay	ki	0.0398	uM
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-6-(oxan-4-yloxy)quinazolin-4-amine	1532002: Displacement of (6-FAM)KI(pY)VV from full length PKMYT1 (unknown origin) by fluorescence polarization immuno assay	ki	0.0398	uM
6-(2,6-dichlorophenyl)-8-methyl-2-(3-methylsulfanylanilino)pyrido[2,3-d]pyrimidin-7-one	1532000: Displacement of (6-FAM)KI(pY)VV from PKMYT1 kinase domain (unknown origin) by fluorescence polarization binding assay	ki	0.0437	uM
3-[[4-(2,3-dihydro-1H-indazol-7-ylamino)pyrimidin-2-yl]amino]benzamide	1532002: Displacement of (6-FAM)KI(pY)VV from full length PKMYT1 (unknown origin) by fluorescence polarization immuno assay	ki	0.0485	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, decreases expression, increases expression	4
sodium arsenite	increases expression, decreases expression	3
Arsenic Trioxide	decreases expression, increases expression	2
Cisplatin	affects cotreatment, increases expression	2
Tobacco Smoke Pollution	affects expression, decreases methylation	2
aristolochic acid I	increases expression	1
afuresertib	decreases expression	1
FR900359	affects phosphorylation	1
echimidine	affects expression, increases metabolic processing	1
bufotalin	increases expression	1
bisphenol A	decreases expression	1
geraniol	decreases expression	1
lead acetate	increases expression	1
riddelliine	decreases expression, increases metabolic processing	1
methylparaben	increases expression	1
cypermethrin	decreases expression	1
perfluorooctanoic acid	decreases expression	1
zinc chromate	increases abundance, decreases expression	1
2,3-bis(3’-hydroxybenzyl)butyrolactone	increases expression, affects cotreatment	1
cupric chloride	increases expression	1
di-n-butylphosphoric acid	affects expression	1
chromium hexavalent ion	decreases expression, increases abundance	1
cylindrospermopsin	decreases expression	1
PD 0166285	decreases activity	1
erucylphospho-N,N,N-trimethylpropylammonium	decreases expression	1
ICG 001	decreases expression	1
8-(2,6-dichlorophenyl)-10-methyl-3-((4-morpholin-4-ylphenyl)amino)-2,4,10-triazabicyclo(4.4.0)deca-1,3,5,7-tetraen-9-one	decreases activity	1
saracatinib	decreases activity	1
jinfukang	affects cotreatment, increases expression	1
(+)-JQ1 compound	decreases expression	1

ChEMBL screening assays

148 unique, capped per target: 146 binding, 2 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1057598	Binding	Inhibition of PKMYT1 assessed as enzyme activity at 1 uM relative to untreated control	Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline. — J Med Chem
CHEMBL6113842	Functional	In vivo inhibition of PKMYT1 in female NOD-SCID mouse xenografted with human HCC1569 cells assessed as reduction in CDK1 phosphorylation at T14 level in tumor at 15 mg/kg, po administered twice daily for 21 days and measured after 8 hrs pos	Discovery of Naphthyridinone Derivatives as Selective and Potent PKMYT1 Inhibitors with Antitumor Efficacy. — J Med Chem

Clinical trials (associated diseases)

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