CDK11A
gene geneOn this page
Also known as PITSLRECDK11-p110CDK11-p58CDK11-p46p58GTA
Summary
CDK11A (cyclin dependent kinase 11A, HGNC:1730) is a protein-coding gene on chromosome 1p36.33, encoding Cyclin-dependent kinase 11A (Q9UQ88). Cyclin-dependent protein kinase that acts as a regulator of transcription and pre-mRNA splicing. It is a selective cancer dependency (DepMap: 20.0% of cell lines).
This gene encodes a member of the serine/threonine protein kinase family. Members of this kinase family are known to be essential for eukaryotic cell cycle control. Due to a segmental duplication, this gene shares very high sequence identity with a neighboring gene. These two genes are frequently deleted or altered in neuroblastoma. The protein kinase encoded by this gene can be cleaved by caspases and may play a role in cell apoptosis. Alternative splicing results in multiple transcript variants.
Source: NCBI Gene 728642 — RefSeq curated summary.
At a glance
- GWAS associations: 1
- Clinical variants (ClinVar): 138 total
- Druggable target: yes — 10 molecules with ChEMBL bioactivity
- Cancer dependency (DepMap): dependent in 20.0% of screened cell lines
- MANE Select transcript:
NM_024011
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:1730 |
| Approved symbol | CDK11A |
| Name | cyclin dependent kinase 11A |
| Location | 1p36.33 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | PITSLRE, CDK11-p110, CDK11-p58, CDK11-p46, p58GTA |
| Ensembl gene | ENSG00000008128 |
| Ensembl biotype | protein_coding |
| OMIM | 116951 |
| Entrez | 728642 |
Gene structure
Transcript identifiers
Ensembl transcripts: 29 — 14 protein_coding, 12 retained_intron, 2 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined
ENST00000356200, ENST00000356937, ENST00000357760, ENST00000358779, ENST00000378633, ENST00000378638, ENST00000401096, ENST00000404249, ENST00000460465, ENST00000463652, ENST00000464748, ENST00000468397, ENST00000468800, ENST00000474916, ENST00000478901, ENST00000479362, ENST00000487462, ENST00000489300, ENST00000491311, ENST00000492390, ENST00000495016, ENST00000498810, ENST00000509982, ENST00000893735, ENST00000893736, ENST00000893737, ENST00000893738, ENST00000893739, ENST00000937803
RefSeq mRNA: 4 — MANE Select: NM_024011
NM_001313896, NM_001313982, NM_024011, NM_033529
CCDS: CCDS44042, CCDS44043, CCDS81253, CCDS81254
Canonical transcript exons
ENST00000404249 — 20 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001714517 | 1719328 | 1719455 |
| ENSE00003466910 | 1712264 | 1712400 |
| ENSE00003476013 | 1704039 | 1704146 |
| ENSE00003484918 | 1705642 | 1705732 |
| ENSE00003490604 | 1708180 | 1708245 |
| ENSE00003493098 | 1709038 | 1709133 |
| ENSE00003507378 | 1703824 | 1703940 |
| ENSE00003525046 | 1721596 | 1721711 |
| ENSE00003532668 | 1709518 | 1709640 |
| ENSE00003538477 | 1704223 | 1704344 |
| ENSE00003540484 | 1708794 | 1708952 |
| ENSE00003563203 | 1722708 | 1722831 |
| ENSE00003573320 | 1707409 | 1707584 |
| ENSE00003629837 | 1704550 | 1704655 |
| ENSE00003646560 | 1703080 | 1703269 |
| ENSE00003647264 | 1716346 | 1716478 |
| ENSE00003652156 | 1703476 | 1703624 |
| ENSE00003673770 | 1704904 | 1705025 |
| ENSE00003845610 | 1702379 | 1702999 |
| ENSE00003850628 | 1724258 | 1724357 |
Expression profiles
Bgee: expression breadth ubiquitous, 134 present calls, max score 98.32.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 23.8482 / max 370.1381, expressed in 1809 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 9817 | 22.3811 | 1806 |
| 9818 | 1.4671 | 879 |
Top tissues by expression
134 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| sural nerve | UBERON:0015488 | 98.32 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 97.59 | gold quality |
| granulocyte | CL:0000094 | 97.44 | gold quality |
| spleen | UBERON:0002106 | 97.15 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 96.95 | gold quality |
| small intestine | UBERON:0002108 | 96.44 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 96.21 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 96.06 | gold quality |
| pituitary gland | UBERON:0000007 | 96.01 | gold quality |
| transverse colon | UBERON:0001157 | 95.97 | gold quality |
| fundus of stomach | UBERON:0001160 | 95.93 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 95.91 | gold quality |
| cerebellum | UBERON:0002037 | 95.83 | gold quality |
| cerebellar cortex | UBERON:0002129 | 95.83 | gold quality |
| right lung | UBERON:0002167 | 95.80 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 95.49 | gold quality |
| right testis | UBERON:0004534 | 95.46 | gold quality |
| body of stomach | UBERON:0001161 | 95.38 | gold quality |
| left testis | UBERON:0004533 | 95.37 | gold quality |
| mucosa of stomach | UBERON:0001199 | 95.31 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 95.31 | gold quality |
| bone marrow | UBERON:0002371 | 95.27 | gold quality |
| left ovary | UBERON:0002119 | 95.15 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 95.15 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 95.12 | gold quality |
| blood | UBERON:0000178 | 95.11 | gold quality |
| apex of heart | UBERON:0002098 | 95.09 | gold quality |
| metanephros cortex | UBERON:0010533 | 95.09 | gold quality |
| body of uterus | UBERON:0009853 | 94.95 | gold quality |
| intestine | UBERON:0000160 | 94.93 | gold quality |
Single-cell (SCXA)
Detected in 4 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 6.09 |
| E-MTAB-8271 | no | 203.49 |
| E-MTAB-8559 | no | 188.83 |
| E-CURD-112 | no | 2.51 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): CREB1, ETS1
miRNA regulators (miRDB)
20 targeting CDK11A, 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-4481 | 100.00 | 66.42 | 1669 |
| HSA-MIR-4745-5P | 99.98 | 65.95 | 1028 |
| HSA-MIR-568 | 99.98 | 69.86 | 2084 |
| HSA-MIR-4267 | 99.96 | 66.53 | 2368 |
| HSA-MIR-651-3P | 99.94 | 73.48 | 5177 |
| HSA-MIR-4731-5P | 99.89 | 67.23 | 2537 |
| HSA-MIR-4492 | 99.87 | 68.25 | 3611 |
| HSA-MIR-6715A-3P | 99.83 | 68.05 | 1473 |
| HSA-MIR-374C-5P | 99.80 | 72.06 | 2910 |
| HSA-MIR-655-3P | 99.80 | 72.19 | 2909 |
| HSA-MIR-1283 | 99.69 | 72.42 | 3009 |
| HSA-MIR-6081 | 99.48 | 66.07 | 1446 |
| HSA-MIR-766-3P | 99.47 | 65.24 | 1811 |
| HSA-MIR-3911 | 99.38 | 66.95 | 1087 |
| HSA-MIR-6731-5P | 99.28 | 67.42 | 2375 |
| HSA-MIR-8085 | 99.28 | 67.56 | 2362 |
| HSA-MIR-3973 | 99.20 | 69.19 | 1990 |
| HSA-MIR-6830-5P | 99.01 | 68.73 | 1884 |
| HSA-MIR-4671-5P | 97.10 | 65.70 | 93 |
| HSA-MIR-7847-3P | 96.63 | 64.58 | 952 |
Functional genomics
DepMap (CRISPR cell-line fitness): dependent in 20.0% of screened cell lines.
Literature-anchored findings (GeneRIF, showing 15)
- demonstrates that CDK11(p46) directly interacts with RanBPM in vitro and in human cells (PMID:14511641)
- the PITSLRE IRES interacts with the Unr protein, which is more prominently expressed at the G2/M stage of the cell cycle (PMID:15330758)
- CDK11 kinases could be regulated by interaction with 14-3-3 proteins during cell cycle and apoptosis (PMID:15883043)
- CDK11(p58) is a new interacting protein and a novel regulator of histone acetyltransferase (HAT) HBO1. (PMID:15963510)
- CDK11p60 can contribute to apoptosis by direct signalling at the mitochondria, thereby amplifying Fas-induced apoptosis in melanoma cells. (PMID:16004605)
- These findings suggest that CDK11 may contribute to apoptosis by regulating the activity of NOT2 independent of its kinase activity. (PMID:16039607)
- mitotic CDK11(p58) isoform, but not the CDK11(p110) isoform, associates with mitotic centrosomes (PMID:16462731)
- CDC2L2 gene may contribute to the susceptibility of type 2 diabetes in the northern Han Chinese population. (PMID:17177267)
- findings show that, in addition to playing a role in spindle formation and structure, CDK11(p58) is also required for sister chromatid cohesion and the completion of mitosis (PMID:17606997)
- These data identified a new negative regulatory protein of ERalpha and provided a new pathway by which CDK11(p58) negatively regulated cells. (PMID:19122208)
- Phosphorylation of the eukaryotic initiation factor 3f by cyclin-dependent kinase 11 during apoptosis. (PMID:19245811)
- study identified p21 activated kinase 1 (PAK1) as a new CDK11(p58) substrate; mapped a new phosphorylation site of Ser174 on PAK1; results indicated PAK1 may serve as a downstream effector of CDK11(p58) during mitosis progression (PMID:19520772)
- CDK11 has a role in human cancers [review] (PMID:27049727)
- These results provided evidence that CDK11(p110) play a critical role in the tumorigenicity of esophageal squamous cell carcinoma cells, which suggests that CDK11(p110) may be a promising therapeutic target in esophageal squamous cell carcinoma. (PMID:30722725)
- Galactosyltransferase B4GALT1 confers chemoresistance in pancreatic ductal adenocarcinomas by upregulating N-linked glycosylation of CDK11(p110). (PMID:33309857)
Cross-species orthologs
5 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | cdk11b | ENSDARG00000102546 |
| mus_musculus | Cdk11b | ENSMUSG00000029062 |
| rattus_norvegicus | AABR07040938.1 | ENSRNOG00000005402 |
| rattus_norvegicus | Cdk11b | ENSRNOG00000017213 |
| drosophila_melanogaster | Pitslre | FBGN0016696 |
Paralogs (26): CDKL3 (ENSG00000006837), CDKL5 (ENSG00000008086), CDK14 (ENSG00000058091), CDK17 (ENSG00000059758), CDK13 (ENSG00000065883), CDKL1 (ENSG00000100490), CDK16 (ENSG00000102225), CDK6 (ENSG00000105810), PRP4K (ENSG00000112739), CDK18 (ENSG00000117266), CDK2 (ENSG00000123374), CDK8 (ENSG00000132964), CDK7 (ENSG00000134058), CDK4 (ENSG00000135446), CDK9 (ENSG00000136807), CDK15 (ENSG00000138395), CDKL2 (ENSG00000138769), CDK19 (ENSG00000155111), CDK20 (ENSG00000156345), CDK5 (ENSG00000164885), CDK12 (ENSG00000167258), CDK1 (ENSG00000170312), CDK10 (ENSG00000185324), CDKL4 (ENSG00000205111), CDK11B (ENSG00000248333), CDK3 (ENSG00000250506)
Protein
Protein identifiers
Cyclin-dependent kinase 11A — Q9UQ88 (reviewed: Q9UQ88)
Alternative names: Cell division cycle 2-like protein kinase 2, Cell division protein kinase 11A, Galactosyltransferase-associated protein kinase p58/GTA, PITSLRE serine/threonine-protein kinase CDC2L2
All UniProt accessions (7): Q9UQ88, E7ESP2, E9PFJ2, J3KS35, Q5QPQ9, Q5QPR3, Q5QPR4
UniProt curated annotations — full annotation on UniProt →
Function. Cyclin-dependent protein kinase that acts as a regulator of transcription and pre-mRNA splicing. Acts as a key regulator of pre-mRNA splicing by mediating phosphorylation of SF3B1, enabling the association between SF3B1 and U5 and U6 snRNAs in the activated spliceosome, thereby promoting spliceosome assembly. Also acts as a regulator of transcription by phosphorylating ‘Ser-2’ of the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAP II) POLR2A. Involved in replication-dependent transcription of histone genes: binds to histone genes and phosphorylates POLR2A at ‘Ser-2’ of the CTD to specifically control transcriptional elongation of histones and recruitment of 3’-end processing factors. Part of a transcription checkpoint upstream of CDK9, which regulates promoter-proximal pausing by RNA polymerase II, a transcription halt following transcription initiation, but prior to elongation. Probably regulates promoter-proximal pausing by mediating phosphorylation of POLR2A at ‘Ser-2’ of the CTD. Isoform expressed in a non-cell cycle-dependent manner. Isoform specifically expressed during the G2-M phases of the cell cycle. Phosphorylates ‘Ser-2’ of the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAP II) POLR2A. Promotes centromeric transcription to maintain centromeric cohesion during mitosis.
Subunit / interactions. Associates with cyclin-L1 (CCNL1) or cyclin-L2 (CCNL2) to form an active cyclin-L-CDK11 cyclin-dependent protein kinase complex. Interacts with SAP30BP; promoting assenbly of the cyclin-L-CDK11 cyclin-dependent protein kinase complex. Interacts with CASP8AP2/FLASH; promoting 3’ end cleavage of histone pre-mRNAs. Associates with cyclin-L1 (CCNL1) or cyclin-L2 (CCNL2) to form an active cyclin-L-CDK11 cyclin-dependent protein kinase complex. Interacts with SFRS7. The cleaved p110 isoform, p110C, binds to the serine/threonine kinase PAK1. Associates with cyclin-D3 (CCND3) to form an active cyclin-dependent protein kinase complex.
Subcellular location. Nucleus. Chromosome. Cytoplasm Nucleus Nucleus. Centromere.
Tissue specificity. Expressed ubiquitously.
Post-translational modifications. During apoptosis, induced by Fas or tumor necrosis factor, specific CKD11 p110 isoforms are cleaved by caspases to produce a protein (p110C) that contains the C-terminal kinase domain of the CDK11 proteins.
Activity regulation. Phosphorylation at Thr-436 or Tyr-437 inactivates the enzyme, while phosphorylation at Thr-583 activates it. CDK11 (CDK11A and/or CDK11B) is specifically inhibited by the anticancer agent OTS964.
Induction. Specifically induced in G2/M phase of the cell cycle.
Miscellaneous. Duplicated gene. CDK11A and CDK11B encode almost identical protein kinases of 110 kDa that contain at their C-termini the open reading frame of a smaller 58 kDa isoform which is expressed following IRES-mediated alternative initiation of translation. Many references talk about ‘p110 isoforms’ but it is not yet known if this refers to CDK11A and/or CDK11B or one/some of the isoforms of each. Produced by alternative initiation at Met-345 of isoform SV6.
Similarity. Belongs to the protein kinase superfamily. CMGC Ser/Thr protein kinase family. CDC2/CDKX subfamily.
Isoforms (8)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q9UQ88-1 | SV6, p110 | yes |
| Q9UQ88-2 | SV1, Pbeta21, Beta 2-1 | |
| Q9UQ88-3 | SV2, Pbeta22 | |
| Q9UQ88-4 | SV3 | |
| Q9UQ88-5 | SV7, SV8 | |
| Q9UQ88-8 | SV12 | |
| Q9UQ88-9 | SV13 | |
| Q9UQ88-10 | 4, Beta 1, p58 |
RefSeq proteins (4): NP_001300825, NP_001300911, NP_076916, NP_277071 (=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 |
| IPR045267 | CDK11/PITSLRE_STKc | Domain |
| IPR050108 | CDK | Family |
Pfam: PF00069
Catalyzed reactions (Rhea), 3 shown:
- [DNA-directed RNA polymerase] + ATP = phospho-[DNA-directed RNA polymerase] + ADP + H(+) (RHEA:10216)
- 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 (53 total): modified residue 12, splice variant 11, sequence conflict 10, compositionally biased region 8, sequence variant 5, binding site 2, region of interest 2, chain 1, domain 1, active site 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9UQ88-F1 | 66.94 | 0.23 |
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): 550 (proton acceptor)
Ligand- & substrate-binding residues (2): 432–440; 455
Post-translational modifications (12): 47, 72, 271, 436, 437, 470, 476, 577, 582, 583, 739, 740
Function
Pathways and Gene Ontology
Reactome pathways
6 pathways
| ID | Pathway |
|---|---|
| R-HSA-380270 | Recruitment of mitotic centrosome proteins and complexes |
| R-HSA-1640170 | Cell Cycle |
| R-HSA-380287 | Centrosome maturation |
| R-HSA-453274 | Mitotic G2-G2/M phases |
| R-HSA-69275 | G2/M Transition |
| R-HSA-69278 | Cell Cycle, Mitotic |
MSigDB gene sets: 152 (showing top):
MORF_DNMT1, GOBP_REGULATION_OF_MICROTUBULE_BASED_PROCESS, MODULE_255, GOBP_GROWTH, MODULE_317, MORF_HDAC2, NKX61_01, GOBP_REGULATION_OF_CELL_CYCLE, GOBP_REGULATION_OF_CENTROSOME_CYCLE, MORF_RFC4, GOBP_RNA_SPLICING, HP1SITEFACTOR_Q6, MORF_PRKDC, GOBP_MITOTIC_CELL_CYCLE, BIOCARTA_HIVNEF_PATHWAY
GO Biological Process (10): mitotic cell cycle (GO:0000278), regulation of cell growth (GO:0001558), regulation of DNA-templated transcription (GO:0006355), protein phosphorylation (GO:0006468), apoptotic process (GO:0006915), regulation of apoptotic process (GO:0042981), regulation of RNA splicing (GO:0043484), regulation of centrosome cycle (GO:0046605), regulation of mRNA processing (GO:0050684), regulation of cell cycle (GO:0051726)
GO Molecular Function (9): protein kinase activity (GO:0004672), protein serine/threonine kinase activity (GO:0004674), cyclin-dependent protein serine/threonine kinase activity (GO:0004693), ATP binding (GO:0005524), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)
GO Cellular Component (3): cyclin-dependent protein kinase holoenzyme complex (GO:0000307), nucleus (GO:0005634), cytoplasm (GO:0005737)
Reactome top-level categories
Rollup of top-5 pathways:
| Category | Pathways |
|---|---|
| Centrosome maturation | 1 |
| G2/M Transition | 1 |
| Cell Cycle, Mitotic | 1 |
| Mitotic G2-G2/M phases | 1 |
| Cell Cycle | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cell cycle | 2 |
| regulation of cellular component organization | 2 |
| regulation of gene expression | 2 |
| protein kinase activity | 2 |
| mitotic nuclear division | 1 |
| cell growth | 1 |
| regulation of growth | 1 |
| DNA-templated transcription | 1 |
| regulation of RNA biosynthetic process | 1 |
| phosphorylation | 1 |
| protein modification process | 1 |
| programmed cell death | 1 |
| apoptotic signaling pathway | 1 |
| execution phase of apoptosis | 1 |
| apoptotic process | 1 |
| regulation of programmed cell death | 1 |
| RNA splicing | 1 |
| regulation of primary metabolic process | 1 |
| centrosome cycle | 1 |
| regulation of cell cycle process | 1 |
| regulation of microtubule-based process | 1 |
| mRNA processing | 1 |
| regulation of mRNA metabolic process | 1 |
| regulation of cellular process | 1 |
| kinase activity | 1 |
| phosphotransferase activity, alcohol group as acceptor | 1 |
| catalytic activity, acting on a protein | 1 |
| protein serine/threonine kinase activity | 1 |
| cyclin-dependent protein kinase activity | 1 |
| adenyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| nucleoside phosphate binding | 1 |
| heterocyclic compound binding | 1 |
| binding | 1 |
| transferase activity, transferring phosphorus-containing groups | 1 |
| catalytic activity | 1 |
| serine/threonine protein kinase complex | 1 |
| intracellular membrane-bounded organelle | 1 |
| intracellular anatomical structure | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
2229 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CDK11A | CCNL1 | Q9UK58 | 901 |
| CDK11A | MMP23B | O75900 | 861 |
| CDK11A | RNPS1 | Q15287 | 782 |
| CDK11A | MMP21 | Q8N119 | 767 |
| CDK11A | CCNL2 | Q96S94 | 766 |
| CDK11A | SRSF7 | Q16629 | 605 |
| CDK11A | SRSF2 | Q01130 | 586 |
| CDK11A | SFN | P31947 | 515 |
| CDK11A | CSDE1 | O75534 | 495 |
| CDK11A | CKAP5 | Q14008 | 485 |
| CDK11A | EIF4B | P23588 | 467 |
| CDK11A | H1-0 | P07305 | 451 |
| CDK11A | TRIM25 | Q14258 | 428 |
| CDK11A | RAD17 | O75943 | 417 |
| CDK11A | AACS | Q86V21 | 410 |
IntAct
64 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| MED4 | MED19 | psi-mi:“MI:0914”(association) | 0.900 |
| COMMD4 | VPS26C | psi-mi:“MI:0914”(association) | 0.730 |
| HSP90AA1 | CHUK | psi-mi:“MI:0914”(association) | 0.670 |
| FKBP5 | IKBKB | psi-mi:“MI:0914”(association) | 0.640 |
| YWHAE | RGS12 | psi-mi:“MI:0914”(association) | 0.610 |
| CHEK2 | PPM1G | psi-mi:“MI:0914”(association) | 0.560 |
| YWHAE | SRSF10 | psi-mi:“MI:0914”(association) | 0.560 |
| HSP90AB1 | CDK11A | psi-mi:“MI:0915”(physical association) | 0.560 |
| CDK11A | HSP90AA1 | psi-mi:“MI:0914”(association) | 0.530 |
| CCNL1 | CDK11B | psi-mi:“MI:0914”(association) | 0.530 |
| HSPB8 | VWA8 | psi-mi:“MI:0914”(association) | 0.530 |
| Dlg4 | CDK11A | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| GADD45A | CDK11A | psi-mi:“MI:0915”(physical association) | 0.370 |
| CSNK2A1 | MYO1B | psi-mi:“MI:0914”(association) | 0.350 |
| JUN | TPM3 | psi-mi:“MI:0914”(association) | 0.350 |
| BCAR1 | CEP290 | psi-mi:“MI:0914”(association) | 0.350 |
| PDHA1 | psi-mi:“MI:0914”(association) | 0.350 | |
| ESR1 | ESYT2 | psi-mi:“MI:0914”(association) | 0.350 |
| M | psi-mi:“MI:0914”(association) | 0.350 | |
| HTRA4 | PSMD12 | psi-mi:“MI:0914”(association) | 0.350 |
| SOX2 | CBX4 | psi-mi:“MI:0914”(association) | 0.350 |
| CSNK2A1 | EIF3F | psi-mi:“MI:0914”(association) | 0.350 |
| CDK11A | APOA1 | psi-mi:“MI:0914”(association) | 0.350 |
| HSP90AA1 | URI1 | psi-mi:“MI:0914”(association) | 0.350 |
| HLA-C | psi-mi:“MI:0914”(association) | 0.350 | |
| CSNK2A2 | VWA8 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (245): CDK11A (Affinity Capture-MS), WDR47 (Affinity Capture-MS), DDB2 (Affinity Capture-MS), CDK11B (Affinity Capture-MS), ZG16B (Affinity Capture-MS), C12orf43 (Affinity Capture-MS), SPRR3 (Affinity Capture-MS), CRNN (Affinity Capture-MS), AP3B1 (Co-fractionation), CTR9 (Co-fractionation), DPF2 (Co-fractionation), LEO1 (Co-fractionation), NOLC1 (Co-fractionation), PELP1 (Co-fractionation), SAP30BP (Co-fractionation)
ESM2 similar proteins: A2X6X1, A2XUW1, A9RVK2, B9FMJ3, F4HRJ4, F4I114, F4ICB6, O08678, O08679, O45818, P21127, P24788, P27448, P78362, Q03141, Q05512, Q08DZ2, Q09437, Q13523, Q23357, Q39008, Q40541, Q5R814, Q5RKH1, Q5Z9J0, Q5ZCI1, Q61136, Q6K5F8, Q6L5D4, Q6L5F7, Q6Z829, Q7KZI7, Q7XUF4, Q8H0U8, Q8RX66, Q8VHF0, Q8VHJ5, Q96VK3, Q9C9U4, Q9C9U5
Diamond homologs: A1CL96, A1D624, A2QU77, A2X6X1, A2XUW1, A3LUB9, A4QXX4, A8XA58, O13958, O55076, O61847, O96821, P00546, P06493, P0C661, P0CS76, P0CS77, P11440, P21127, P23111, P23437, P23572, P24033, P24100, P24788, P24923, P24941, P29618, P29619, P34112, P34117, P34556, P35567, P39073, P39951, P43063, P43450, P46892, P48734, P48963
SIGNOR signaling
9 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| CDK11A | up-regulates | CDK11B | phosphorylation |
| CDK11A | “down-regulates quantity by destabilization” | SPDEF | phosphorylation |
| GADD45A | “down-regulates activity” | CDK11A | binding |
| GADD45B | “down-regulates activity” | CDK11A | binding |
| GADD45G | “down-regulates activity” | CDK11A | binding |
| CDK11A | “up-regulates activity” | PAK1 | phosphorylation |
| CDK11A | “form complex” | CyclinD3/CDK11A | binding |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 84 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 |
|---|---|---|---|
| Orc1 removal from chromatin | 5 | 13.9× | 2e-03 |
| G2/M Checkpoints | 6 | 12.6× | 1e-03 |
| Assembly of the pre-replicative complex | 5 | 10.9× | 2e-03 |
| ESR-mediated signaling | 5 | 10.0× | 2e-03 |
| SARS-CoV-2 activates/modulates innate and adaptive immune responses | 5 | 7.0× | 7e-03 |
| Cell Cycle Checkpoints | 5 | 6.9× | 7e-03 |
| Cell Cycle, Mitotic | 8 | 6.0× | 2e-03 |
| Cellular responses to stress | 8 | 4.6× | 4e-03 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| negative regulation of proteasomal ubiquitin-dependent protein catabolic process | 5 | 25.7× | 3e-04 |
| protein stabilization | 8 | 6.9× | 2e-03 |
| regulation of cell cycle | 7 | 6.7× | 6e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
138 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 120 |
| Likely benign | 9 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
3169 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 1:1703474:A:AC | donor_gain | 1.0000 |
| 1:1703475:C:CC | donor_gain | 1.0000 |
| 1:1703622:CTC:C | acceptor_gain | 1.0000 |
| 1:1703623:TCCTG:T | acceptor_loss | 1.0000 |
| 1:1703624:CCT:C | acceptor_loss | 1.0000 |
| 1:1703625:C:CC | acceptor_gain | 1.0000 |
| 1:1703626:T:A | acceptor_loss | 1.0000 |
| 1:1703819:CCCA:C | donor_loss | 1.0000 |
| 1:1703820:CCACC:C | donor_loss | 1.0000 |
| 1:1703938:TTCCT:T | acceptor_loss | 1.0000 |
| 1:1703939:TCCT:T | acceptor_loss | 1.0000 |
| 1:1703940:CCTA:C | acceptor_loss | 1.0000 |
| 1:1703941:C:CC | acceptor_gain | 1.0000 |
| 1:1703941:CTAAG:C | acceptor_loss | 1.0000 |
| 1:1703942:T:G | acceptor_loss | 1.0000 |
| 1:1704034:CTCA:C | donor_loss | 1.0000 |
| 1:1704035:TCA:T | donor_loss | 1.0000 |
| 1:1704036:CA:C | donor_loss | 1.0000 |
| 1:1704037:A:AC | donor_gain | 1.0000 |
| 1:1704038:C:CC | donor_gain | 1.0000 |
| 1:1704038:C:CT | donor_loss | 1.0000 |
| 1:1704142:CCCAC:C | acceptor_gain | 1.0000 |
| 1:1704143:CCAC:C | acceptor_gain | 1.0000 |
| 1:1704143:CCACC:C | acceptor_gain | 1.0000 |
| 1:1704144:CAC:C | acceptor_gain | 1.0000 |
| 1:1704144:CACC:C | acceptor_gain | 1.0000 |
| 1:1704145:AC:A | acceptor_gain | 1.0000 |
| 1:1704145:ACCTG:A | acceptor_loss | 1.0000 |
| 1:1704146:CC:C | acceptor_gain | 1.0000 |
| 1:1704147:C:CA | acceptor_loss | 1.0000 |
AlphaMissense
5167 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 1:1702917:A:T | L781H | 1.000 |
| 1:1702922:G:C | F779L | 1.000 |
| 1:1702922:G:T | F779L | 1.000 |
| 1:1702923:A:G | F779S | 1.000 |
| 1:1702924:A:G | F779L | 1.000 |
| 1:1704272:C:G | R549P | 1.000 |
| 1:1704296:A:G | L541P | 1.000 |
| 1:1704624:A:C | I500S | 1.000 |
| 1:1704624:A:T | I500N | 1.000 |
| 1:1704642:C:A | G494V | 1.000 |
| 1:1704642:C:T | G494D | 1.000 |
| 1:1704643:C:A | G494C | 1.000 |
| 1:1704643:C:G | G494R | 1.000 |
| 1:1704645:A:T | V493E | 1.000 |
| 1:1704648:A:T | V492E | 1.000 |
| 1:1704959:A:G | L471P | 1.000 |
| 1:1704973:G:C | F466L | 1.000 |
| 1:1704973:G:T | F466L | 1.000 |
| 1:1704974:A:C | F466C | 1.000 |
| 1:1704974:A:G | F466S | 1.000 |
| 1:1704975:A:G | F466L | 1.000 |
| 1:1704978:C:G | G465R | 1.000 |
| 1:1705001:A:G | L457P | 1.000 |
| 1:1705001:A:T | L457Q | 1.000 |
| 1:1705006:C:A | K455N | 1.000 |
| 1:1705006:C:G | K455N | 1.000 |
| 1:1705010:A:G | L454P | 1.000 |
| 1:1705010:A:T | L454Q | 1.000 |
| 1:1705709:G:C | F426L | 1.000 |
| 1:1705709:G:T | F426L | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000740395 (1:1714741 A>T), RS1001223299 (1:1702242 C>G,T), RS1001388900 (1:1720260 A>G), RS1001407908 (1:1710294 C>G,T), RS1001418649 (1:1720034 G>C), RS1001692248 (1:1710691 G>A), RS1001797386 (1:1703360 T>C), RS1001951364 (1:1725963 T>C), RS1002295137 (1:1707992 C>T), RS1002382689 (1:1725218 G>A), RS1002849032 (1:1719013 T>C), RS1002949405 (1:1724307 G>A,C), RS1002982109 (1:1724042 T>C), RS1003251104 (1:1706625 C>T), RS1003367300 (1:1706429 G>A)
Disease associations
OMIM: gene MIM:116951 | 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 |
|---|---|---|
| GCST005951_34 | Body mass index | 3.000000e-08 |
EFO canonical traits (1, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004340 | body mass index |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (3): CHEMBL5416 (SINGLE PROTEIN), CHEMBL5483187 (PROTEIN COMPLEX), CHEMBL6066064 (PROTEIN FAMILY)
Molecules with ChEMBL bioactivity
10 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 45,567 (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 |
|---|---|---|---|
| CHEMBL477772 | PAZOPANIB | 4 | 15,540 |
| CHEMBL601719 | CRIZOTINIB | 4 | 14,403 |
| CHEMBL223360 | LINIFANIB | 3 | 3,925 |
| CHEMBL1230609 | FORETINIB | 2 | 3,096 |
| CHEMBL215152 | DEFOSBARASERTIB | 2 | 372 |
| CHEMBL384304 | RG-547 | 2 | 93 |
| CHEMBL445813 | AT-7519 | 2 | 2,614 |
| CHEMBL572878 | TOZASERTIB | 2 | 2,998 |
| CHEMBL296468 | BMS-387032 | 1 | 2,075 |
| CHEMBL574738 | AST-487 | 1 | 451 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — PITSLRE subfamily
Binding affinities (BindingDB)
7 measured of 7 human assays (7 total across all organisms); most potent 7 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| 1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methyl-phenyl)urea | KD | 450 nM |
| N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide | KD | 1100 nM |
| 1-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea | KD | 1400 nM |
| BMS-387072 | KD | 1800 nM |
| 2-{3-[(7-{3-[ethyl(2-hydroxyethyl)amino]propoxy}quinazolin-4-yl)amino]-1H-pyrazol-5-yl}-N-(3-fluorophenyl)acetamide | KD | 1900 nM |
| 5-({4-[(2,3-dimethyl-2H-indazol-6-yl)(methyl)amino]pyrimidin-2-yl}amino)-2-methylbenzene-1-sulfonamide | KD | 2900 nM |
| 1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b | KD | 3100 nM |
ChEMBL bioactivities
75 potent at pChembl≥5 of 75 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.77 | IC50 | 1.7 | nM | CHEMBL4455382 |
| 8.28 | Kd | 5.2 | nM | AT-7519 |
| 7.48 | Kd | 33 | nM | CHEMBL1989043 |
| 7.42 | Kd | 38 | nM | CHEMBL5185990 |
| 7.41 | Kd | 39 | nM | CHEMBL5175800 |
| 7.37 | Kd | 43 | nM | CHEMBL5185655 |
| 7.32 | Kd | 48 | nM | BMS-387032 |
| 7.31 | Kd | 49 | nM | CHEMBL5200963 |
| 7.16 | Kd | 69 | nM | CHEMBL5180190 |
| 7.00 | Kd | 99 | nM | CHEMBL5184522 |
| 6.96 | Kd | 110 | nM | JNJ-7706621 |
| 6.89 | Kd | 130 | nM | CHEMBL5206282 |
| 6.85 | Kd | 140 | nM | CHEMBL5170651 |
| 6.82 | Kd | 150 | nM | CHEMBL5182610 |
| 6.77 | Kd | 170 | nM | CHEMBL5171843 |
| 6.77 | IC50 | 170 | nM | CHEMBL1989043 |
| 6.72 | IC50 | 190 | nM | CHEMBL5175800 |
| 6.64 | IC50 | 230 | nM | CHEMBL5185990 |
| 6.64 | IC50 | 230 | nM | CHEMBL5180190 |
| 6.58 | IC50 | 260 | nM | CHEMBL5185655 |
| 6.58 | Kd | 260 | nM | TOZASERTIB |
| 6.54 | Kd | 290 | nM | CHEMBL5208491 |
| 6.48 | Kd | 330 | nM | CHEMBL5200790 |
| 6.48 | IC50 | 330 | nM | CHEMBL5206282 |
| 6.43 | Kd | 370 | nM | CHEMBL4553037 |
| 6.41 | Kd | 390 | nM | BMS-345541 |
| 6.40 | Kd | 399 | nM | CHEMBL4799297 |
| 6.39 | Kd | 410 | nM | CHEMBL5180851 |
| 6.38 | Kd | 420 | nM | CRIZOTINIB |
| 6.33 | IC50 | 470 | nM | CHEMBL5200790 |
| 6.32 | Kd | 480 | nM | FORETINIB |
| 6.24 | Kd | 570 | nM | CHEMBL5207135 |
| 6.24 | IC50 | 580 | nM | CHEMBL5208491 |
| 6.21 | IC50 | 620 | nM | CHEMBL5173236 |
| 6.16 | Kd | 690 | nM | CHEMBL5199067 |
| 6.16 | IC50 | 700 | nM | CHEMBL5200963 |
| 6.15 | IC50 | 710 | nM | CHEMBL5184522 |
| 6.10 | IC50 | 800 | nM | CHEMBL5182610 |
| 6.05 | IC50 | 900 | nM | CHEMBL5171843 |
| 6.02 | Kd | 960 | nM | CHEMBL5180130 |
| 6.00 | IC50 | 1000 | nM | TP-030-1 |
| 6.00 | IC50 | 1000 | nM | TP-030-2 |
| 6.00 | IC50 | 1000 | nM | TP-030n |
| 6.00 | Kd | 1000 | nM | CHEMBL5180577 |
| 6.00 | IC50 | 1000 | nM | CHEMBL5194816 |
| 6.00 | Kd | 1000 | nM | DEFOSBARASERTIB |
| 5.96 | Kd | 1100 | nM | CHEMBL5169674 |
| 5.96 | Kd | 1100 | nM | AST-487 |
| 5.92 | IC50 | 1200 | nM | CHEMBL5180130 |
| 5.92 | IC50 | 1200 | nM | CHEMBL5203750 |
PubChem BioAssay actives
66 with measured affinity, of 219 total; 42 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 4-[(2,6-dichlorobenzoyl)amino]-N-piperidin-4-yl-1H-pyrazole-5-carboxamide | 625133: Binding constant for CDC2L2 kinase domain | kd | 0.0052 | uM |
| [4-amino-2-[4-(4-methylpiperazin-1-yl)anilino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.0330 | uM |
| [4-amino-2-[[6-(4-methylpiperazin-1-yl)-3-pyridinyl]amino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.0380 | uM |
| [4-amino-2-[4-[(4-methylpiperazin-1-yl)methyl]anilino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.0390 | uM |
| [4-amino-2-[4-(4-methylpiperazin-1-yl)anilino]-1,3-thiazol-5-yl]-(2,6-difluorophenyl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.0430 | uM |
| N-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-4-carboxamide | 435649: Binding constant for CDC2L2 kinase domain | kd | 0.0480 | uM |
| [4-amino-2-[[5-(4-methylpiperazin-1-yl)-2-pyridinyl]amino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.0490 | uM |
| [4-amino-2-[[2-methyl-6-(4-methylpiperazin-1-yl)-3-pyridinyl]amino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.0690 | uM |
| [4-amino-2-[3-methoxy-4-(4-methylpiperazin-1-yl)anilino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.0990 | uM |
| 4-[[5-amino-1-(2,6-difluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide | 435649: Binding constant for CDC2L2 kinase domain | kd | 0.1100 | uM |
| [4-amino-2-[4-(4-methylpiperazin-1-yl)anilino]-1,3-thiazol-5-yl]-(2-chlorophenyl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.1300 | uM |
| [4-[[4-amino-5-(2,6-dichlorobenzoyl)-1,3-thiazol-2-yl]amino]phenyl]-(4-methylpiperazin-1-yl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.1400 | uM |
| [4-amino-2-[2-methyl-4-(4-methylpiperazin-1-yl)anilino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.1500 | uM |
| [4-amino-2-[4-(4-methylpiperazin-1-yl)anilino]-1,3-thiazol-5-yl]-[2-fluoro-6-(trifluoromethyl)phenyl]methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.1700 | uM |
| N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide | 435649: Binding constant for CDC2L2 kinase domain | kd | 0.2600 | uM |
| [4-amino-2-[[4-methyl-2-(4-methylpiperazin-1-yl)pyrimidin-5-yl]amino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.2900 | uM |
| [4-amino-2-[[3-methyl-5-(4-methylpiperazin-1-yl)-2-pyridinyl]amino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.3300 | uM |
| N’-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine | 625133: Binding constant for CDC2L2 kinase domain | kd | 0.3900 | uM |
| [4-amino-2-[3-(4-methylpiperazin-1-yl)anilino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.4100 | uM |
| Crizotinib | 625133: Binding constant for CDC2L2 kinase domain | kd | 0.4200 | uM |
| 1-N’-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | 625133: Binding constant for CDC2L2 kinase domain | kd | 0.4800 | uM |
| [4-amino-2-[4-(4-methylpiperazin-1-yl)anilino]-1,3-thiazol-5-yl]-[(2S,6R)-2,6-dimethylpiperidin-1-yl]methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.5700 | uM |
| [4-amino-2-[[6-(2,4-dimethylpiperazin-1-yl)-2-methyl-3-pyridinyl]amino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860789: Inhibition of N-terminus or C-terminus NLuc fused CDK11A (unknown origin) transfected in HEK293 cells by NanoBRET assay | ic50 | 0.6200 | uM |
| [4-amino-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.6900 | uM |
| [4-amino-2-[4-(4-methylpiperazin-1-yl)sulfonylanilino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 0.9600 | uM |
| 2-[3-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]quinazolin-4-yl]amino]-1H-pyrazol-5-yl]-N-(3-fluorophenyl)acetamide | 435649: Binding constant for CDC2L2 kinase domain | kd | 1.0000 | uM |
| N-[5-(2,6-dichlorobenzoyl)-2-[4-(4-methylpiperazin-1-yl)anilino]-1,3-thiazol-4-yl]acetamide | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 1.0000 | uM |
| [4-amino-2-[[2-methyl-6-(9-methyl-3,9-diazaspiro[5.5]undecan-3-yl)-3-pyridinyl]amino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860789: Inhibition of N-terminus or C-terminus NLuc fused CDK11A (unknown origin) transfected in HEK293 cells by NanoBRET assay | ic50 | 1.0000 | uM |
| 1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea | 435649: Binding constant for CDC2L2 kinase domain | kd | 1.1000 | uM |
| [4-amino-2-[4-(4-methylpiperazin-1-yl)anilino]-1,3-thiazol-5-yl]-(3-chloro-2-pyridinyl)methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 1.1000 | uM |
| 1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea | 435649: Binding constant for CDC2L2 kinase domain | kd | 1.2000 | uM |
| [4-amino-2-[(2-methyl-6-piperazin-1-yl-3-pyridinyl)amino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860789: Inhibition of N-terminus or C-terminus NLuc fused CDK11A (unknown origin) transfected in HEK293 cells by NanoBRET assay | ic50 | 1.2000 | uM |
| Pazopanib | 435649: Binding constant for CDC2L2 kinase domain | kd | 1.3000 | uM |
| [4-amino-2-[[2-methyl-6-(4-methyl-3-propan-2-ylpiperazin-1-yl)-3-pyridinyl]amino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860789: Inhibition of N-terminus or C-terminus NLuc fused CDK11A (unknown origin) transfected in HEK293 cells by NanoBRET assay | ic50 | 1.5000 | uM |
| [4-amino-2-[[6-(4-hydroxypiperidin-1-yl)-2-methyl-3-pyridinyl]amino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860789: Inhibition of N-terminus or C-terminus NLuc fused CDK11A (unknown origin) transfected in HEK293 cells by NanoBRET assay | ic50 | 2.2000 | uM |
| (4-hydroxypiperidin-1-yl)-[4-[[4-[4-(3-methylsulfonylpropoxy)indol-1-yl]pyrimidin-2-yl]amino]cyclohexyl]methanone | 769528: Binding affinity to CDC2L2 (unknown origin) | kd | 2.4000 | uM |
| [4-amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl]-(2,3-difluoro-6-methoxyphenyl)methanone | 625133: Binding constant for CDC2L2 kinase domain | kd | 2.9000 | uM |
| [4-amino-2-[(2-methyl-6-morpholin-4-yl-3-pyridinyl)amino]-1,3-thiazol-5-yl]-(2,6-dichlorophenyl)methanone | 1860789: Inhibition of N-terminus or C-terminus NLuc fused CDK11A (unknown origin) transfected in HEK293 cells by NanoBRET assay | ic50 | 3.4000 | uM |
| [4-amino-2-[4-(4-methylpiperazin-1-yl)anilino]-1,3-thiazol-5-yl]-phenylmethanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 4.2000 | uM |
| (2,6-dichlorophenyl)-[4-(methylamino)-2-[4-(4-methylpiperazin-1-yl)anilino]-1,3-thiazol-5-yl]methanone | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 4.8000 | uM |
| 4-amino-N-(2,6-dichlorophenyl)-2-[4-(4-methylpiperazin-1-yl)anilino]-1,3-thiazole-5-carboxamide | 1860788: Binding affinity to wild type human partial length CDK11A (D391 to K730 residues) expressed in bacterial expression system assessed as dissociation constant by KdELECT assay | kd | 4.8000 | uM |
| [4-amino-2-[4-(4-methylpiperazin-1-yl)anilino]-1,3-thiazol-5-yl]-(2,4,6-trimethylphenyl)methanone | 1860789: Inhibition of N-terminus or C-terminus NLuc fused CDK11A (unknown origin) transfected in HEK293 cells by NanoBRET assay | ic50 | 6.1000 | uM |
CTD chemical–gene interactions
22 total (human), top 22 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Tretinoin | increases expression, affects cotreatment, decreases expression | 2 |
| GSK-J4 | increases expression | 1 |
| FR900359 | increases phosphorylation | 1 |
| triphenyl phosphate | affects expression | 1 |
| sodium arsenite | affects cotreatment, decreases expression | 1 |
| cobaltous chloride | increases expression | 1 |
| coumarin | increases phosphorylation | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| 2,3,5-(triglutathion-S-yl)hydroquinone | increases ADP-ribosylation | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| abrine | increases expression | 1 |
| licochalcone B | increases expression | 1 |
| Ascorbic Acid | affects cotreatment, increases expression | 1 |
| Formaldehyde | increases expression | 1 |
| Silicon Dioxide | decreases expression | 1 |
| Valproic Acid | increases methylation | 1 |
| Cyclosporine | decreases expression | 1 |
| Aflatoxin B1 | increases methylation | 1 |
| Cadmium Chloride | increases expression | 1 |
| Acrylamide | increases expression | 1 |
| Chlorodiphenyl (54% Chlorine) | increases expression | 1 |
| Particulate Matter | increases expression | 1 |
ChEMBL screening assays
111 unique, capped per target: 111 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1032228 | Binding | Inhibition of CDC2L2 at 3 uM | Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. — J Med Chem |
Cellosaurus cell lines
2 cell lines: 1 transformed cell line, 1 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B2U0 | Abcam HEK293T CDK11A KO | Transformed cell line | Female |
| CVCL_SI20 | HAP1 CDK11A (-) | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.