CDK13
gene geneOn this page
Also known as CHEDCDC2LKIAA1791
Summary
CDK13 (cyclin dependent kinase 13, HGNC:1733) is a protein-coding gene on chromosome 7p14.1, encoding Cyclin-dependent kinase 13 (Q14004). Cyclin-dependent kinase which displays CTD kinase activity and is required for RNA splicing. It is haploinsufficient (ClinGen: sufficient evidence).
The protein encoded by this gene is a member of the cyclin-dependent serine/threonine protein kinase family. Members of this family are well known for their essential roles as master switches in cell cycle control. The exact function of this protein has not yet been determined, but it may play a role in mRNA processing and may be involved in regulation of hematopoiesis. Alternatively spliced transcript variants have been described.
Source: NCBI Gene 8621 — RefSeq curated summary.
At a glance
- Gene–disease (curated): syndromic intellectual disability (Definitive, ClinGen) — +1 more curated relationship
- GWAS associations: 5
- Clinical variants (ClinVar): 1,264 total — 40 pathogenic, 42 likely-pathogenic (top 2% of genes corpus-wide)
- Regional missense constraint (gnomAD): 2 of 5 regions constrained (≈20% of expected missense variation)
- GTEx eGene: eQTL in 12 tissues, sQTL in 2 (q < 0.05)
- Phenotypes (HPO): 67
- ChEMBL bioactivity: 20 clinical-phase molecules tested; no curated mechanism-of-action drug
- Dosage sensitivity (ClinGen): haploinsufficiency sufficient evidence, triplosensitivity no evidence
- Constraint (gnomAD): pLI 1.00 (loss-of-function intolerant), LOEUF 0.43 (moderately constrained)
- MANE Select transcript:
NM_003718
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:1733 |
| Approved symbol | CDK13 |
| Name | cyclin dependent kinase 13 |
| Location | 7p14.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | CHED, CDC2L, KIAA1791 |
| Ensembl gene | ENSG00000065883 |
| Ensembl biotype | protein_coding |
| OMIM | 603309 |
| Entrez | 8621 |
Gene structure
Transcript identifiers
Ensembl transcripts: 25 — 13 protein_coding, 6 retained_intron, 6 protein_coding_CDS_not_defined
MANE Select: ENST00000181839
Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 4, TSL 4: 1
ENST00000181839, ENST00000340829, ENST00000465643, ENST00000478563, ENST00000484589, ENST00000642213, ENST00000642592, ENST00000642626, ENST00000642660, ENST00000643859, ENST00000643868, ENST00000643915, ENST00000644221, ENST00000644561, ENST00000645470, ENST00000645826, ENST00000646039, ENST00000646437, ENST00000647453, ENST00000647518, ENST00000700485, ENST00000700486, ENST00000700487, ENST00000966764, ENST00001139842
RefSeq mRNA: 2 — MANE Select: NM_003718
NM_003718, NM_031267
CCDS: CCDS5461, CCDS5462
Canonical transcript exons
ENST00000181839 — 14 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000521990 | 40078720 | 40078851 |
| ENSE00000832466 | 40078005 | 40078121 |
| ENSE00000832468 | 40092785 | 40093237 |
| ENSE00001709712 | 39987599 | 39988258 |
| ENSE00001886832 | 39950256 | 39951852 |
| ENSE00003494733 | 40045836 | 40046025 |
| ENSE00003525244 | 39997494 | 39997664 |
| ENSE00003581011 | 40062826 | 40062927 |
| ENSE00003586066 | 40001861 | 40002031 |
| ENSE00003592719 | 40063023 | 40063100 |
| ENSE00003629850 | 40047821 | 40047877 |
| ENSE00003674806 | 39999361 | 39999500 |
| ENSE00003687550 | 40088126 | 40088331 |
| ENSE00004795686 | 40094130 | 40099580 |
Expression profiles
Bgee: expression breadth ubiquitous, 297 present calls, max score 99.82.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 23.1769 / max 371.8702, expressed in 1813 samples.
Highest expression (Bgee): buccal mucosa cell, renal medulla, visceral pleura, pylorus, nipple.
Genetic regulation across tissues (GTEx eQTL / sQTL)
CDK13 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 12 tissues and its splicing (sQTL) in 2 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.
14 significant tissue × QTL associations:
| Tissue | QTL | q-value | Slope | Lead variant |
|---|---|---|---|---|
| Cells EBV-transformed lymphocytes | eqtl | 6.3e-08 | +0.27 | 7:39945120:C:T |
| Nerve Tibial | eqtl | 1.6e-05 | -0.13 | 7:40055042:A:G |
| Cells Cultured fibroblasts | eqtl | 2.6e-03 | -0.10 | 7:39875962:A:C |
| Brain Cerebellar Hemisphere | eqtl | 1.0e-02 | +0.60 | 7:40455411:G:T |
| Brain Putamen basal ganglia | eqtl | 1.4e-02 | -0.82 | 7:39049161:G:A |
| Testis | eqtl | 1.7e-02 | -0.09 | 7:39875962:A:C |
| Esophagus Muscularis | eqtl | 2.2e-02 | -0.12 | 7:40046166:C:T |
| Brain Anterior cingulate cortex BA24 | eqtl | 2.3e-02 | -0.81 | 7:40872908:AGAACTGAGGTG:A |
| Whole Blood | eqtl | 2.9e-02 | +0.07 | 7:39809989:T:C |
| Cells Cultured fibroblasts | sqtl | 3.4e-02 | -1.11 | 7:39766413:A:G |
| Heart Atrial Appendage | eqtl | 3.7e-02 | -0.26 | 7:40124831:C:T |
| Brain Cerebellum | eqtl | 3.8e-02 | +0.93 | 7:39828382:C:T |
| Artery Tibial | eqtl | 4.2e-02 | +0.36 | 7:40321424:C:T |
| Cells EBV-transformed lymphocytes | sqtl | 4.3e-02 | +1.33 | 7:39897537:T:A |
FANTOM5 promoters
8 alternative TSS:
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 78276 | 7.6433 | 1635 |
| 78274 | 7.3987 | 1774 |
| 78275 | 4.2767 | 1693 |
| 78273 | 1.8750 | 934 |
| 78279 | 1.0764 | 569 |
| 78277 | 0.4641 | 185 |
| 78278 | 0.3132 | 130 |
| 78280 | 0.1295 | 41 |
Top tissues by expression
showing 100 of 300 tissues by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| buccal mucosa cell | CL:0002336 | 99.82 | gold quality |
| renal medulla | UBERON:0000362 | 99.69 | gold quality |
| visceral pleura | UBERON:0002401 | 99.67 | gold quality |
| pylorus | UBERON:0001166 | 99.55 | gold quality |
| nipple | UBERON:0002030 | 99.51 | gold quality |
| endothelial cell | CL:0000115 | 99.47 | gold quality |
| cardia of stomach | UBERON:0001162 | 99.47 | gold quality |
| ventral tegmental area | UBERON:0002691 | 99.46 | gold quality |
| inferior vagus X ganglion | UBERON:0005363 | 99.43 | gold quality |
| parietal pleura | UBERON:0002400 | 99.42 | gold quality |
| lateral globus pallidus | UBERON:0002476 | 99.40 | gold quality |
| superior surface of tongue | UBERON:0007371 | 99.39 | gold quality |
| trigeminal ganglion | UBERON:0001675 | 99.38 | gold quality |
| subthalamic nucleus | UBERON:0001906 | 99.37 | gold quality |
| superior vestibular nucleus | UBERON:0007227 | 99.37 | gold quality |
| tibia | UBERON:0000979 | 99.34 | gold quality |
| substantia nigra pars reticulata | UBERON:0001966 | 99.30 | gold quality |
| substantia nigra pars compacta | UBERON:0001965 | 99.26 | gold quality |
| pericardium | UBERON:0002407 | 99.06 | gold quality |
| urethra | UBERON:0000057 | 98.99 | gold quality |
| penis | UBERON:0000989 | 98.91 | gold quality |
| superficial temporal artery | UBERON:0001614 | 98.85 | gold quality |
| tendon of biceps brachii | UBERON:0008188 | 98.85 | gold quality |
| synovial joint | UBERON:0002217 | 98.83 | gold quality |
| lateral nuclear group of thalamus | UBERON:0002736 | 98.80 | gold quality |
| adult organism | UBERON:0007023 | 98.80 | gold quality |
| saphenous vein | UBERON:0007318 | 98.79 | gold quality |
| pharyngeal mucosa | UBERON:0000355 | 98.78 | gold quality |
| pleura | UBERON:0000977 | 98.76 | gold quality |
| caput epididymis | UBERON:0004358 | 98.60 | gold quality |
| body of tongue | UBERON:0011876 | 98.55 | gold quality |
| mucosa of paranasal sinus | UBERON:0005030 | 98.51 | gold quality |
| pons | UBERON:0000988 | 98.45 | gold quality |
| mammalian vulva | UBERON:0000997 | 98.45 | gold quality |
| oral cavity | UBERON:0000167 | 98.43 | gold quality |
| tongue | UBERON:0001723 | 98.43 | gold quality |
| seminal vesicle | UBERON:0000998 | 98.34 | gold quality |
| bronchial epithelial cell | CL:0002328 | 98.30 | gold quality |
| globus pallidus | UBERON:0001875 | 98.30 | gold quality |
| sperm | CL:0000019 | 98.29 | gold quality |
| cauda epididymis | UBERON:0004360 | 98.29 | gold quality |
| jejunal mucosa | UBERON:0000399 | 98.25 | gold quality |
| germinal epithelium of ovary | UBERON:0001304 | 98.22 | gold quality |
| skin of hip | UBERON:0001554 | 98.19 | gold quality |
| jejunum | UBERON:0002115 | 98.16 | gold quality |
| trabecular bone tissue | UBERON:0002483 | 98.13 | gold quality |
| vena cava | UBERON:0004087 | 98.12 | gold quality |
| corpus epididymis | UBERON:0004359 | 98.08 | gold quality |
| medial globus pallidus | UBERON:0002477 | 98.01 | gold quality |
| upper leg skin | UBERON:0004262 | 97.47 | gold quality |
| epithelium of nasopharynx | UBERON:0001951 | 97.41 | gold quality |
| dorsal root ganglion | UBERON:0000044 | 97.40 | gold quality |
| nasopharynx | UBERON:0001728 | 97.39 | gold quality |
| tendon | UBERON:0000043 | 97.23 | gold quality |
| pigmented layer of retina | UBERON:0001782 | 97.21 | gold quality |
| retina | UBERON:0000966 | 97.18 | gold quality |
| calcaneal tendon | UBERON:0003701 | 96.79 | gold quality |
| corpus callosum | UBERON:0002336 | 96.70 | gold quality |
| lower lobe of lung | UBERON:0008949 | 96.46 | gold quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 96.39 | gold quality |
| pancreatic ductal cell | CL:0002079 | 96.25 | gold quality |
| parietal lobe | UBERON:0001872 | 96.09 | gold quality |
| mammary duct | UBERON:0001765 | 95.96 | gold quality |
| tonsil | UBERON:0002372 | 95.94 | gold quality |
| dorsal plus ventral thalamus | UBERON:0001897 | 95.89 | gold quality |
| male germ cell | CL:0000015 | 95.79 | gold quality |
| medulla oblongata | UBERON:0001896 | 95.64 | gold quality |
| postcentral gyrus | UBERON:0002581 | 95.44 | gold quality |
| gingival epithelium | UBERON:0001949 | 95.41 | gold quality |
| entorhinal cortex | UBERON:0002728 | 95.04 | gold quality |
| biceps brachii | UBERON:0001507 | 94.92 | gold quality |
| cartilage tissue | UBERON:0002418 | 94.92 | gold quality |
| adrenal tissue | UBERON:0018303 | 94.83 | gold quality |
| endometrium | UBERON:0001295 | 94.75 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 94.53 | gold quality |
| epithelium of mammary gland | UBERON:0003244 | 94.48 | gold quality |
| skeletal muscle tissue of rectus abdominis | UBERON:0004511 | 94.38 | gold quality |
| bronchus | UBERON:0002185 | 94.13 | gold quality |
| mammary gland | UBERON:0001911 | 94.11 | gold quality |
| gingiva | UBERON:0001828 | 94.10 | gold quality |
| Brodmann (1909) area 23 | UBERON:0013554 | 94.05 | gold quality |
| colonic epithelium | UBERON:0000397 | 94.04 | gold quality |
| cervix squamous epithelium | UBERON:0006922 | 94.04 | gold quality |
| thoracic mammary gland | UBERON:0005200 | 94.02 | gold quality |
| bone element | UBERON:0001474 | 94.01 | gold quality |
| mucosa of sigmoid colon | UBERON:0004993 | 94.01 | gold quality |
| epithelium of bronchus | UBERON:0002031 | 93.94 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 93.81 | gold quality |
| colonic mucosa | UBERON:0000317 | 93.73 | gold quality |
| occipital lobe | UBERON:0002021 | 93.72 | gold quality |
| amniotic fluid | UBERON:0000173 | 93.70 | gold quality |
| squamous epithelium | UBERON:0006914 | 93.64 | gold quality |
| superior frontal gyrus | UBERON:0002661 | 93.58 | gold quality |
| eye | UBERON:0000970 | 93.56 | gold quality |
| right uterine tube | UBERON:0001302 | 93.51 | gold quality |
| uterus | UBERON:0000995 | 93.41 | gold quality |
| oviduct epithelium | UBERON:0004804 | 93.39 | gold quality |
| sural nerve | UBERON:0015488 | 93.30 | gold quality |
| ovary | UBERON:0000992 | 93.24 | gold quality |
| tongue squamous epithelium | UBERON:0006919 | 93.09 | gold quality |
Single-cell (SCXA)
Detected in 3 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-GEOD-75140 | no | 614.20 |
| E-MTAB-2983 | no | 279.94 |
| E-ANND-3 | no | 0.00 |
HPA expression
RNA tissue specificity: Low tissue specificity
showing 60 of 78 HPA tissues / cells by nTPM:
| Tissue / cell | Axis | nTPM | Protein (IHC) |
|---|---|---|---|
| Cerebellum | tissue | 109.0 | not detected |
| Putamen | tissue | 69.7 | |
| Hypothalamus | tissue | 65.8 | |
| Pons | tissue | 64.6 | |
| Septum | tissue | 62.7 | |
| Basal ganglia | tissue | 62.3 | not detected |
| Nucleus accumbens | tissue | 61.4 | |
| Ventral forebrain | tissue | 59.3 | |
| Periaqueductal gray | tissue | 56.9 | |
| Thalamus | tissue | 55.8 | |
| Superior colliculi | tissue | 55.6 | |
| Cerebral cortex | tissue | 55.5 | not detected |
| Occipital cortex | tissue | 55.5 | |
| Substantia nigra | tissue | 55.4 | |
| Choroid plexus | tissue | 55.0 | |
| Prefrontal cortex | tissue | 54.6 | |
| Motor cortex | tissue | 54.6 | |
| Midbrain | tissue | 54.3 | |
| Amygdala | tissue | 53.3 | |
| Hippocampus | tissue | 52.9 | not detected |
| Hippocampal formation | tissue | 52.4 | |
| Entorhinal cortex | tissue | 52.4 | |
| Locus coeruleus | tissue | 51.4 | |
| Olfactory bulb | tissue | 51.1 | |
| Medulla oblongata | tissue | 50.8 | |
| Postcentral gyrus | tissue | 49.6 | |
| Somatosensory cortex | tissue | 49.3 | |
| Insular cortex | tissue | 49.1 | |
| Temporal cortex | tissue | 48.9 | |
| Spinal cord | tissue | 48.4 | |
| Retrosplenial and cingulate cortex | tissue | 47.9 | |
| Retrosplenial cortex | tissue | 47.7 | |
| Corpus callosum | tissue | 45.2 | |
| Bone marrow | tissue | 26.1 | not detected |
| Lymph node | tissue | 18.6 | not detected |
| Thyroid gland | tissue | 18.0 | not detected |
| Retina | tissue | 17.5 | |
| Tonsil | tissue | 17.3 | low |
| Caudate putamen | tissue | 17.0 | |
| Testis | tissue | 16.5 | high |
| Thymus | tissue | 16.1 | |
| Frontal cortex | tissue | 15.7 | |
| Spleen | tissue | 15.0 | not detected |
| Parathyroid gland | tissue | 14.7 | |
| Liver | tissue | 14.2 | not detected |
| Ovary | tissue | 13.3 | not detected |
| Fallopian tube | tissue | 13.1 | medium |
| Epididymis | tissue | 13.0 | not detected |
| Appendix | tissue | 12.9 | low |
| Placenta | tissue | 12.4 | low |
| Vagina | tissue | 12.3 | medium |
| Esophagus | tissue | 12.2 | low |
| Tongue | tissue | 12.2 | |
| Endometrium 1 | tissue | 11.9 | not detected |
| Rectum | tissue | 11.8 | medium |
| Stomach 1 | tissue | 11.3 | medium |
| Pancreas | tissue | 11.3 | not detected |
| Kidney | tissue | 11.3 | high |
| Salivary gland | tissue | 11.2 | not detected |
| Gallbladder | tissue | 11.1 | not detected |
Brain sub-regions (HPA Brain Atlas): detected in 190; highest nTPM — Flocculonodular lobe (79.2), Vermis (77.7), Cerebellar cortex (77.5), Parieto-temporal junction (white matter) (68.4), Temporal white matter (68.2).
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
Targeting CDK13 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).
showing 30 of 185 miRNAs:
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-3163 | 100.00 | 77.23 | 8605 |
| HSA-MIR-3613-3P | 100.00 | 76.36 | 7965 |
| HSA-MIR-4795-3P | 100.00 | 74.62 | 4024 |
| HSA-MIR-4692 | 100.00 | 67.32 | 2066 |
| HSA-MIR-126-5P | 100.00 | 72.71 | 3180 |
| HSA-MIR-6867-5P | 100.00 | 82.21 | 3464 |
| HSA-MIR-4533 | 100.00 | 69.48 | 2758 |
| HSA-MIR-188-3P | 100.00 | 68.76 | 1240 |
| HSA-MIR-190A-3P | 100.00 | 80.35 | 5520 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-3662 | 99.99 | 73.82 | 5684 |
| HSA-MIR-4514 | 99.99 | 67.10 | 1870 |
| HSA-MIR-548C-3P | 99.99 | 74.01 | 7587 |
| HSA-MIR-150-5P | 99.99 | 66.69 | 1976 |
| HSA-MIR-4775 | 99.98 | 75.00 | 6394 |
| HSA-MIR-8068 | 99.98 | 73.85 | 2376 |
| HSA-MIR-5696 | 99.98 | 72.36 | 4487 |
| HSA-MIR-548N | 99.98 | 71.94 | 4170 |
| HSA-MIR-607 | 99.97 | 73.62 | 5593 |
| HSA-MIR-9-3P | 99.96 | 70.88 | 2068 |
| HSA-MIR-3658 | 99.96 | 73.87 | 4379 |
| HSA-MIR-590-3P | 99.96 | 74.34 | 6478 |
| HSA-LET-7C-3P | 99.95 | 73.42 | 2862 |
| HSA-MIR-3910 | 99.95 | 71.13 | 2227 |
| HSA-MIR-141-3P | 99.94 | 72.79 | 2421 |
| HSA-MIR-200A-3P | 99.94 | 72.68 | 2420 |
| HSA-MIR-335-3P | 99.93 | 73.36 | 4958 |
| HSA-MIR-6835-3P | 99.93 | 70.49 | 2904 |
| HSA-MIR-22-3P | 99.93 | 68.13 | 917 |
| HSA-MIR-205-3P | 99.92 | 69.92 | 3165 |
Functional genomics
gnomAD constraint: pLI 1, LOEUF 0.434, missense Z -1.11 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD
Regional missense constraint (gnomAD)
ENST00000181839 splits into 5 regions with different missense tolerance; 2 are missense-constrained (≈20% of the expected missense variation). Missense variants in a constrained region (low observed/expected) are more likely to be pathogenic. gnomAD
| Region (GRCh38) | Missense obs / exp | o/e | Constrained |
|---|---|---|---|
| 7:39,950,642–39,997,634 | 1051 / 931.0 | 1.13 | no |
| 7:39,997,635–40,078,720 | 130 / 362.4 | 0.36 | yes (p 2.9e-34) |
| 7:40,078,721–40,078,850 | 45 / 57.0 | 0.79 | no |
| 7:40,078,851–40,088,185 | 3 / 22.1 | 0.14 | yes (p 4.8e-05) |
| 7:40,088,186–40,094,977 | 475 / 579.3 | 0.82 | no |
ClinGen dosage: haploinsufficiency 3 (sufficient evidence), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map |
Literature-anchored findings (GeneRIF, showing 24)
- Data demonstrate that CDC2L5 is located in the nucleoplasm, where it directly interacts with the ASF/SF2-associated protein p32, a protein involved in splicing regulation. (PMID:16721827)
- CDK13 interacts with cyclin K, and is required for self-renewal in ES cells. (PMID:22547058)
- Coincidently amplified CDK13, GMNN, and CENPF genes can play a role as common cancer-driver genes in human cancers. (PMID:22912832)
- High CDK13 expression is associated with pancreatic cancer. (PMID:25216700)
- CDK12 and CDK13 losses in HCT116 cells preferentially affect expression of DNA damage response. (PMID:25561469)
- CDK13 gene is amplified in different types of cancer indicate that this kinase can contribute to cancer development in human. (PMID:26886422)
- Mutation in CHK13 gene is associated with congenital heart defects. (PMID:27479907)
- Detailed phenotypic and molecular characterisation of 9 individuals with pathogenic variants in CDK13 is provided. Two individuals had novel CDK13 variants (p.Asn842Asp, p.Lys734Glu), while the remaining seven unrelated individuals had a recurrent, previously published p.Asn842Ser variant. (PMID:28807008)
- heterozygous, likely dominant negative mutations affecting the protein kinase domain of the CDK13 gene result in a recognisable, syndromic form of intellectual disability, with or without congenital heart disease. (PMID:29021403)
- Heterozygous constitutional CDK13 mutations in 3 patients cause intellectual disability without cardiac defects. (PMID:29222009)
- We demonstrate the synthesis of two aberrant CDK13 transcripts in lymphoblastoid cells from an individual with a splice-site variant. Clinical characteristics of the individuals include mild to severe intellectual disability (ID), developmental delay, behavioural problems, (neonatal) hypotonia and a variety of facial dysmorphism. (PMID:29393965)
- CDK13 RNA over-editing sites mediated by ADAR1 may serve as novel cancer driver events in HCC progression. (PMID:29996118)
- CDK13 is important for proper expression of a number of genes, but it also probably plays yet-to-be-discovered roles in other processes. (PMID:30319007)
- Insight into the molecular mechanism of LINC00152/miR-215/CDK13 axis in hepatocellular carcinoma progression. (PMID:31297882)
- Expression of CDK13 Was Associated with Prognosis and Expression of HIF-1alpha and beclin1 in Breast Cancer Patients. (PMID:33292020)
- CDK13 upregulation-induced formation of the positive feedback loop among circCDK13, miR-212-5p/miR-449a and E2F5 contributes to prostate carcinogenesis. (PMID:33390186)
- Wolfram-like syndrome with bicuspid aortic valve due to a homozygous missense variant in CDK13. (PMID:33879837)
- HIV-1 Nef interacts with the cyclin K/CDK13 complex to antagonize SERINC5 for optimal viral infectivity. (PMID:34380030)
- An ADAR1-dependent RNA editing event in the cyclin-dependent kinase CDK13 promotes thyroid cancer hallmarks. (PMID:34496885)
- CDK13-related disorder: Report of a series of 18 previously unpublished individuals and description of an epigenetic signature. (PMID:35063350)
- CDK13-related disorder: a deep characterization of speech and language abilities and addition of 33 novel cases. (PMID:36599938)
- CDK12/13 promote splicing of proximal introns by enhancing the interaction between RNA polymerase II and the splicing factor SF3B1. (PMID:37026485)
- Oncogenic CDK13 mutations impede nuclear RNA surveillance. (PMID:37079685)
- CDK13 promotes lipid deposition and prostate cancer progression by stimulating NSUN5-mediated m5C modification of ACC1 mRNA. (PMID:37845385)
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | cdk13 | ENSDARG00000076791 |
| mus_musculus | Cdk13 | ENSMUSG00000041297 |
| rattus_norvegicus | Cdk13 | ENSRNOG00000013620 |
| drosophila_melanogaster | Cdk12 | FBGN0037093 |
Paralogs (26): CDKL3 (ENSG00000006837), CDKL5 (ENSG00000008086), CDK11A (ENSG00000008128), CDK14 (ENSG00000058091), CDK17 (ENSG00000059758), 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)
Mouse-model phenotypes
Observed phenotypes of the mouse ortholog (MGI:1916812) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 33 distinct phenotype terms.
| Mouse phenotype (MP) | Records |
|---|---|
| midline facial cleft | 1 |
| abnormal blood flow velocity | 1 |
| abnormal heart morphology | 1 |
| thin ventricular wall | 1 |
| abnormal kidney development | 1 |
| delayed kidney development | 1 |
| abnormal liver development | 1 |
| small liver | 1 |
| decreased brain size | 1 |
| increased startle reflex | 1 |
| irregular heartbeat | 1 |
| decreased embryo size | 1 |
| delayed brain development | 1 |
| small heart | 1 |
| thin myocardium | 1 |
| small kidney | 1 |
| small lung | 1 |
| abnormal capillary morphology | 1 |
| abnormal facial morphology | 1 |
| embryonic growth retardation | 1 |
| abnormal heart ventricle morphology | 1 |
| pericardial effusion | 1 |
| abnormal myocardium layer morphology | 1 |
| abnormal palate development | 1 |
| abnormal secondary palate development | 1 |
+8 more (showing top 25).
Additional cross-species homologs
Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.
| Organism | UniProt | Identity | Method |
|---|---|---|---|
| Oryza sativa Indica Group | A2XUW1 | 100.0% | Diamond |
| Oryza sativa Japonica Group | Q7XUF4 | 100.0% | Diamond |
| Bos taurus | Q5EAB2 | 99.5% | Diamond |
| Macaca mulatta | Q5EDC3 | 99.4% | Diamond |
| Pongo abelii | Q5R754 | 98.4% | Diamond |
| Xenopus laevis | Q4V862 | 97.9% | Diamond |
| Xenopus tropicalis | Q6GLD8 | 97.9% | Diamond |
| Gallus gallus | Q5ZKN1 | 94.9% | Diamond |
| Ailuropoda melanoleuca | D2H526 | 92.5% | Diamond |
| Lathyrus oleraceus | P28567 | 90.8% | Diamond |
| Oryctolagus cuniculus | Q9TTK0 | 90.5% | Diamond |
| Arabidopsis thaliana | Q8W4P1 | 89.4% | Diamond |
| Macaca fascicularis | Q4R7T5 | 89.3% | Diamond |
| Aspergillus fumigatus Af293 | Q4WTN5 | 87.2% | Diamond |
| Aspergillus nidulans FGSC A4 | Q96VK3 | 87.2% | Diamond |
| Saccharomyces cerevisiae S288C | P23293 | 72.2% | Diamond |
| Nakaseomyces glabratus CBS 138 | Q6FQ83 | 72.2% | Diamond |
| Eremothecium gossypii ATCC 10895 | Q75D46 | 70.0% | Diamond |
| Kluyveromyces lactis NRRL Y-1140 | Q6CRA9 | 68.6% | Diamond |
| Debaryomyces hansenii CBS767 | Q6BV06 | 68.2% | Diamond |
| Candida albicans SC5314 | Q9Y7W4 | 68.2% | Diamond |
| Neurospora crassa OR74A | Q871M9 | 67.7% | Diamond |
| Fusarium graminearum PH-1 | Q4I5U9 | 67.6% | Diamond |
| Dictyostelium discoideum | Q75JN1 | 59.6% | Diamond |
| Caenorhabditis elegans | Q23357 | 58.2% | Diamond |
| Schizosaccharomyces pombe 972h- | Q96WV9 | 56.9% | Diamond |
| Yarrowia lipolytica CLIB122 | Q6C842 | 52.0% | Diamond |
| Encephalitozoon cuniculi GB-M1 | Q8SR90 | 43.4% | Diamond |
| Invertebrate iridescent virus 6 | Q91FD5 | 53.7% | Diamond |
| Fowlpox virus strain NVSL | Q9J523 | 48.9% | Diamond |
| Acanthamoeba polyphaga mimivirus | Q5UNT1 | 37.9% | Diamond |
Genomic neighbors (locus context)
Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).
| Symbol | Type | Entrez |
|---|---|---|
| CDK13-DT | ncRNA | 112267983 |
| MPLKIP | protein-coding | 136647 |
| SUGCT | protein-coding | 79783 |
| LINC00265 | ncRNA | 349114 |
Protein
Protein identifiers
Cyclin-dependent kinase 13 — Q14004 (reviewed: Q14004)
Alternative names: CDC2-related protein kinase 5, Cell division cycle 2-like protein kinase 5, Cell division protein kinase 13, Cholinesterase-related cell division controller
All UniProt accessions (10): A0A2R8Y4Z0, A0A2R8Y644, A0A2R8Y7W5, A0A2R8Y7Y0, A0A2R8YCQ1, A0A2R8YD28, A0A2R8YEB7, A0A2R8YF61, A0A2R8YFE7, Q14004
UniProt curated annotations — full annotation on UniProt →
Function. Cyclin-dependent kinase which displays CTD kinase activity and is required for RNA splicing. Has CTD kinase activity by hyperphosphorylating the C-terminal heptapeptide repeat domain (CTD) of the largest RNA polymerase II subunit RPB1, thereby acting as a key regulator of transcription elongation. Required for RNA splicing, probably by phosphorylating SRSF1/SF2. Required during hematopoiesis. In case of infection by HIV-1 virus, interacts with HIV-1 Tat protein acetylated at ‘Lys-50’ and ‘Lys-51’, thereby increasing HIV-1 mRNA splicing and promoting the production of the doubly spliced HIV-1 protein Nef.
Subunit / interactions. (Microbial infection) Interacts with human herpes virus 1 (HHV-1) transcriptional regulator ICP22. Interacts with CCNL1 and CCNL2. Interacts with CCNK. Interacts with C1QBP. (Microbial infection) Interacts with HIV-1 Tat.
Subcellular location. Nucleus speckle.
Tissue specificity. Expressed in fetal brain, liver, muscle and in adult brain. Also expressed in neuroblastoma and glioblastoma tumors.
Disease relevance. Congenital heart defects, dysmorphic facial features, and intellectual developmental disorder (CHDFIDD) [MIM:617360] An autosomal dominant syndrome characterized by atrial and/or ventricular septal congenital heart defects, facial dysmorphism with hypertelorism, upslanted palpebral fissures, epicanthal folds, ptosis, strabismus, posteriorly rotated ears, thin upper lip, and small mouth. Patients manifest global developmental delay, delayed walking and speech acquisition, and intellectual disability. Some patients have mild microcephaly, a small cerebral cortex, and agenesis of corpus callosum. More variable features include clinodactyly and/or camptodactyly of the fingers, hypotonia, and joint hypermobility. The disease is caused by variants affecting the gene represented in this entry.
Similarity. Belongs to the protein kinase superfamily. CMGC Ser/Thr protein kinase family. CDC2/CDKX subfamily.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q14004-1 | 1 | yes |
| Q14004-2 | 2 |
RefSeq proteins (2): NP_003709, NP_112557 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000719 | Prot_kinase_dom | Domain |
| IPR008271 | Ser/Thr_kinase_AS | Active_site |
| IPR011009 | Kinase-like_dom_sf | Homologous_superfamily |
| IPR017441 | Protein_kinase_ATP_BS | Binding_site |
| IPR050108 | CDK | Family |
Pfam: PF00069
Enzyme classification (BRENDA)
- EC 2.7.11.22 — cyclin-dependent kinase (BRENDA: 49 organisms, 441 substrates, 555 inhibitors, 8 Km, 4 kcat entries)
- EC 2.7.11.23 — [RNA-polymerase]-subunit kinase (BRENDA: 12 organisms, 155 substrates, 47 inhibitors, 15 Km, 0 kcat entries)
Substrate kinetics (BRENDA)
11 substrates with measured Km, best-characterized 11. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| ATP | 0.01–0.06 | 6 |
| ADAQHATPPKKKRKVEDPKDF | 0.046–0.521 | 2 |
| ATP | 0.0052–0.017 | 2 |
| HEPTA-SIX PEPTIDE | 0.189–0.2 | 2 |
| L-ARG-HEPTA PEPTIDE | 0.212–0.243 | 2 |
| FIN1 | 0.003 | 1 |
| PKTPKKAKKL | 0.0029 | 1 |
| CTD-CONTAINING FUSION PROTEIN | 0.0002 | 1 |
| GTP | 0.18 | 1 |
| SYNTHETIC PEPTIDE | 0.15 | 1 |
| [DNA-DIRECTED RNA POLYMERASE] | 0.0001 | 1 |
Catalyzed reactions (Rhea)
- [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 (121 total): compositionally biased region 21, modified residue 20, helix 19, sequence variant 18, region of interest 11, strand 11, turn 7, sequence conflict 6, binding site 2, cross-link 2, chain 1, domain 1, active site 1, splice variant 1
Structure
Experimental structures (PDB)
2 structures by resolution:
| PDB | Title | Method | Resolution (Å) |
|---|---|---|---|
| 5EFQ | Crystal structure of human Cdk13/Cyclin K in complex with ADP-aluminum fluoride | X-RAY DIFFRACTION | 2 |
| 7NXJ | Crystal structure of human Cdk13/Cyclin K in complex with the inhibitor THZ531 | X-RAY DIFFRACTION | 2.36 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q14004-F1 | 50.59 | 0.19 |
Human Protein Atlas
Protein class: Enzymes, ENZYME proteins, Transferases, Kinases, CMGC Ser/Thr protein kinases, Predicted intracellular proteins, Disease related genes, Potential drug targets, Human disease related genes, Congenital malformations, Congenital malformations of the circulatory system
Protein evidence: Evidence at protein level
Subcellular location (HPA, imaging): nuclear speckles; cytosol; golgi apparatus
Antibody reliability (HPA): IH uncertain · IF supported
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)
| Position | Role |
|---|---|
| 837 | proton acceptor |
Ligand- & substrate-binding residues (2)
| Position | Role |
|---|---|
| 711–719 | ATP |
| 734 | ATP |
Post-translational modifications (22)
| Type | Positions |
|---|---|
| Phosphoserine | 315, 317, 325, 340, 342, 358, 360, 383, 395, 397, 400, 437, 439, 525, 1048 |
| N6-acetyllysine | 556 |
| Phosphothreonine | 588, 871, 1058, 1246 |
| Glycyl lysine isopeptide (lys-gly) (interchain with g-cter in sumo2) | 519, 547 |
Function
Pathways and Gene Ontology
Reactome pathways
2 curated (TAS) of 8; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).
8 pathways:
| ID | Pathway | Evidence |
|---|---|---|
| R-HSA-6798695 | Neutrophil degranulation | curated |
| R-HSA-6796648 | TP53 Regulates Transcription of DNA Repair Genes | curated |
| R-HSA-74160 | Gene expression (Transcription) | — |
| R-HSA-212436 | Generic Transcription Pathway | — |
| R-HSA-168256 | Immune System | — |
| R-HSA-168249 | Innate Immune System | — |
| R-HSA-73857 | RNA Polymerase II Transcription | — |
| R-HSA-3700989 | Transcriptional Regulation by TP53 | — |
MSigDB gene sets: 410 (showing top):
REACTOME_INNATE_IMMUNE_SYSTEM, SCHWAB_TARGETS_OF_BMYB_POLYMORPHIC_VARIANTS_DN, GOCC_SECRETORY_GRANULE, GOBP_NEGATIVE_REGULATION_OF_STEM_CELL_DIFFERENTIATION, GOBP_ALTERNATIVE_MRNA_SPLICING_VIA_SPLICEOSOME, MORF_ATRX, THEILGAARD_NEUTROPHIL_AT_SKIN_WOUND_DN, TGACCTY_ERR1_Q2, MORF_ESR1, CTATGCA_MIR153, RODRIGUES_NTN1_TARGETS_DN, MODULE_239, MORF_PPP5C, BLALOCK_ALZHEIMERS_DISEASE_UP, MORF_FANCG
GO Biological Process (23): alternative mRNA splicing, via spliceosome (GO:0000380), regulation of signal transduction (GO:0009966), hemopoiesis (GO:0030097), positive regulation of transcription elongation by RNA polymerase II (GO:0032968), positive regulation of transcription by RNA polymerase II (GO:0045944), regulation of transcription by RNA polymerase II (GO:0006357), mRNA processing (GO:0006397), protein phosphorylation (GO:0006468), epidermal growth factor receptor signaling pathway (GO:0007173), RNA splicing (GO:0008380), positive regulation of macrophage chemotaxis (GO:0010759), positive regulation of telomere maintenance (GO:0032206), regulation of stress-activated MAPK cascade (GO:0032872), cellular response to amino acid starvation (GO:0034198), stress-activated MAPK cascade (GO:0051403), regulation of cytoskeleton organization (GO:0051493), regulation of cell cycle (GO:0051726), interleukin-34-mediated signaling pathway (GO:0061514), response to epidermal growth factor (GO:0070849), caveolin-mediated endocytosis (GO:0072584), regulation of Golgi inheritance (GO:0090170), positive regulation of macrophage proliferation (GO:0120041), regulation of early endosome to late endosome transport (GO:2000641)
GO Molecular Function (15): RNA binding (GO:0003723), protein kinase activity (GO:0004672), cyclin-dependent protein serine/threonine kinase activity (GO:0004693), ATP binding (GO:0005524), RNA polymerase II CTD heptapeptide repeat kinase activity (GO:0008353), protein kinase binding (GO:0019901), cyclin binding (GO:0030332), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein serine/threonine kinase activity (GO:0004674), MAP kinase activity (GO:0004707), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740), phosphatase binding (GO:0019902)
GO Cellular Component (14): cyclin K-CDK13 complex (GO:0002945), extracellular region (GO:0005576), nucleus (GO:0005634), nucleoplasm (GO:0005654), cyclin/CDK positive transcription elongation factor complex (GO:0008024), nuclear speck (GO:0016607), nuclear cyclin-dependent protein kinase holoenzyme complex (GO:0019908), ficolin-1-rich granule lumen (GO:1904813), cyclin-dependent protein kinase holoenzyme complex (GO:0000307), early endosome (GO:0005769), late endosome (GO:0005770), Golgi apparatus (GO:0005794), caveola (GO:0005901), focal adhesion (GO:0005925)
Reactome top-level categories
6 top-level categories:
| Category | Pathways |
|---|---|
| Transcriptional Regulation by TP53 | 1 |
| Innate Immune System | 1 |
| Immune System | 1 |
| RNA Polymerase II Transcription | 1 |
| Generic Transcription Pathway | 1 |
| Gene expression (Transcription) | 1 |
GO top-level categories
showing 60 of 80 GO namespaces:
| Category | Terms |
|---|---|
| protein serine/threonine kinase activity | 3 |
| transcription by RNA polymerase II | 2 |
| RNA processing | 2 |
| MAPK cascade | 2 |
| protein kinase activity | 2 |
| cyclin-dependent protein kinase holoenzyme complex | 2 |
| cellular anatomical structure | 2 |
| intracellular membrane-bounded organelle | 2 |
| endosome | 2 |
| mRNA splicing, via spliceosome | 1 |
| signal transduction | 1 |
| regulation of cell communication | 1 |
| regulation of signaling | 1 |
| regulation of response to stimulus | 1 |
| cell development | 1 |
| transcription elongation by RNA polymerase II | 1 |
| positive regulation of DNA-templated transcription, elongation | 1 |
| regulation of transcription elongation by RNA polymerase II | 1 |
| positive regulation of transcription by RNA polymerase II | 1 |
| regulation of transcription by RNA polymerase II | 1 |
| positive regulation of DNA-templated transcription | 1 |
| regulation of DNA-templated transcription | 1 |
| mRNA metabolic process | 1 |
| phosphorylation | 1 |
| protein modification process | 1 |
| ERBB signaling pathway | 1 |
| positive regulation of leukocyte chemotaxis | 1 |
| regulation of macrophage chemotaxis | 1 |
| macrophage chemotaxis | 1 |
| regulation of granulocyte chemotaxis | 1 |
| positive regulation of macrophage migration | 1 |
| telomere maintenance | 1 |
| regulation of telomere maintenance | 1 |
| positive regulation of DNA metabolic process | 1 |
| positive regulation of chromosome organization | 1 |
| regulation of MAPK cascade | 1 |
| stress-activated MAPK cascade | 1 |
| regulation of stress-activated protein kinase signaling cascade | 1 |
| cellular response to starvation | 1 |
| response to amino acid starvation | 1 |
| stress-activated protein kinase signaling cascade | 1 |
| cytoskeleton organization | 1 |
| regulation of organelle organization | 1 |
| cell cycle | 1 |
| regulation of cellular process | 1 |
| cytokine-mediated signaling pathway | 1 |
| response to growth factor | 1 |
| endocytosis | 1 |
| vesicle-mediated transport | 1 |
| nucleic acid binding | 1 |
| kinase activity | 1 |
| phosphotransferase activity, alcohol group as acceptor | 1 |
| catalytic activity, acting on a protein | 1 |
| cyclin-dependent protein kinase activity | 1 |
| adenyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| anion binding | 1 |
| RNA polymerase II CTD heptapeptide repeat modifying activity | 1 |
| kinase binding | 1 |
| protein binding | 1 |
Experimentally-supported GO annotations
GO terms backed by direct experimental evidence (ECO experimental codes) — 9 of 53 annotations. The rest are phylogenetic / computational / electronic (IEA).
9 experimentally-supported GO terms:
| GO term | NS | Evidence |
|---|---|---|
| hemopoiesis | BP | mutant phenotype |
| positive regulation of transcription by RNA polymerase II | BP | direct assay |
| positive regulation of transcription elongation by RNA polymerase II | BP | direct assay |
| regulation of signal transduction | BP | direct assay |
| cyclin K-CDK13 complex | CC | physical interaction |
| nuclear speck | CC | direct assay |
| RNA binding | MF | high-throughput assay |
| RNA polymerase II CTD heptapeptide repeat kinase activity | MF | direct assay |
| cyclin binding | MF | physical interaction |
Protein interactions and networks
STRING
showing 15 of 1,712 interactions by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CDK13 | MMP23B | O75900 | 916 |
| CDK13 | MMP21 | Q8N119 | 849 |
| CDK13 | CCNK | O75909 | 831 |
| CDK13 | CCNH | P51946 | 638 |
| CDK13 | CCNT1 | O60563 | 632 |
| CDK13 | SUPT5H | O00267 | 583 |
| CDK13 | CCNT2 | O60583 | 556 |
| CDK13 | CCNL1 | Q9UK58 | 542 |
| CDK13 | CCNC | P24863 | 540 |
| CDK13 | POLR2A | P24928 | 540 |
| CDK13 | JAG2 | Q9Y219 | 535 |
| CDK13 | CCNL2 | Q96S94 | 519 |
| CDK13 | BCHE | P06276 | 497 |
| CDK13 | CTDP1 | Q9Y5B0 | 494 |
| CDK13 | SUPT6H | Q7KZ85 | 460 |
IntAct
Human interaction partners of CDK13 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).
11 partners by confidence:
| Partner | Interaction type | MIscore | Records |
|---|---|---|---|
| CCNK | direct interaction | 0.830 | 6 |
| CDC37 | physical association | 0.560 | 1 |
| H3-4 | physical association | 0.400 | 1 |
| CHMP4A | physical association | 0.370 | 2 |
| CHMP5 | physical association | 0.370 | 1 |
| CHMP6 | physical association | 0.370 | 1 |
| PRPF40A | physical association | 0.370 | 1 |
| AIP | association | 0.350 | 1 |
| EEF2 | association | 0.350 | 1 |
| H1-4 | association | 0.350 | 1 |
| DISC1 | physical association | 0.000 | 1 |
BioGRID (233 interactions; top human partners by supporting records): CCNK (Affinity Capture-MS; 6 records), CDK12 (Affinity Capture-MS; 6 records), FKBP5 (Affinity Capture-MS; 4 records), HSP90AA1 (Affinity Capture-MS; 4 records), HSP90AB1 (Affinity Capture-MS; 4 records), BANF1 (Cross-Linking-MS (XL-MS); 3 records), DSTYK (Affinity Capture-MS; 3 records), FBXO11 (Affinity Capture-MS; 3 records), FBXO44 (Affinity Capture-MS; 3 records), HSP90AA4P (Affinity Capture-MS; 3 records), HSP90AA5P (Affinity Capture-MS; 3 records), HSP90AB3P (Affinity Capture-MS; 3 records), HSP90AB4P (Affinity Capture-MS; 3 records), KEAP1 (Affinity Capture-MS; 3 records), NEK3 (Affinity Capture-MS; 3 records)
SIGNOR signaling
showing 6 of 30 signaling interactions:
| A | Effect | B | Mechanism |
|---|---|---|---|
| CDK13 | “form complex” | CyclinK/CDK13 | binding |
| CDK13 | “up-regulates activity” | POLR2A | phosphorylation |
| CDK13 | “up-regulates activity” | EIF4EBP1 | phosphorylation |
| CDK13 | “up-regulates activity” | EIF4B | phosphorylation |
| CDK13 | “down-regulates quantity by destabilization” | SERINC5 | phosphorylation |
| CCNO | “up-regulates activity” | CDK13 | binding |
Protein complexes (CORUM) (1)
Experimentally-characterized complexes this protein is a subunit of (★ = the complex contains a known drug target).
1 complexes by size:
| Complex | Subunits | Members |
|---|---|---|
| CCNK-CDK13 complex | 2 | CCNK, CDK13 |
Disease & clinical
Genetic variants
Variant evidence for CDK13: 1,264 ClinVar records (82 pathogenic / likely pathogenic); 5 GWAS associations. Per-variant detail is on Sugi Variant.
ClinVar
1,264 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 40 |
| Likely pathogenic | 42 |
| Uncertain significance | 612 |
| Likely benign | 365 |
| Benign | 75 |
Top pathogenic / likely-pathogenic (15)
Showing the 15 best-reviewed of 82 pathogenic / likely-pathogenic ClinVar records, ranked by ClinVar review status (expert panel → multiple submitters → single submitter), then by number of submitting labs.
| Variant ID | HGVS | Classification | Review | Submitters |
|---|---|---|---|---|
| 375737 | NM_003718.5(CDK13):c.2149G>A (p.Gly717Arg) | Pathogenic | criteria provided, multiple submitters, no conflicts | 15 |
| 449224 | NM_003718.5(CDK13):c.2141G>A (p.Gly714Asp) | Pathogenic | criteria provided, multiple submitters, no conflicts | 4 |
| 423480 | NM_003718.5(CDK13):c.2209C>T (p.Arg737Cys) | Pathogenic | criteria provided, multiple submitters, no conflicts | 2 |
| 1215514 | NM_003718.5(CDK13):c.454C>T (p.Gln152Ter) | Pathogenic | criteria provided, multiple submitters, no conflicts | 2 |
| 827814 | NM_003718.5(CDK13):c.2194G>A (p.Ala732Thr) | Likely pathogenic | criteria provided, multiple submitters, no conflicts | 2 |
| 1299065 | NM_003718.5(CDK13):c.2627C>T (p.Thr876Ile) | Likely pathogenic | criteria provided, multiple submitters, no conflicts | 2 |
| 1339033 | NM_003718.5(CDK13):c.2563G>A (p.Asp855Asn) | Likely pathogenic | criteria provided, multiple submitters, no conflicts | 2 |
| 1691565 | NM_003718.5(CDK13):c.2609A>G (p.Tyr870Cys) | Likely pathogenic | criteria provided, multiple submitters, no conflicts | 2 |
| 4293604 | NM_003718.5(CDK13):c.2119ATC[1] (p.Ile708del) | Likely pathogenic | criteria provided, multiple submitters, no conflicts | 2 |
| 375738 | NM_003718.5(CDK13):c.2140G>C (p.Gly714Arg) | Pathogenic | criteria provided, single submitter | 2 |
| 422362 | NM_003718.5(CDK13):c.2200A>G (p.Lys734Glu) | Pathogenic | criteria provided, single submitter | 2 |
| 973023 | NM_003718.5(CDK13):c.2511T>G (p.Asp837Glu) | Pathogenic | criteria provided, single submitter | 2 |
| 987083 | NM_003718.5(CDK13):c.1187del (p.Arg396fs) | Pathogenic | criteria provided, single submitter | 1 |
| 1695188 | NM_003718.5(CDK13):c.2227G>T (p.Glu743Ter) | Pathogenic | criteria provided, single submitter | 1 |
| 2034771 | NM_003718.5(CDK13):c.352_353insCGGGCGGA (p.Arg118fs) | Pathogenic | criteria provided, single submitter | 1 |
Per-variant reference — Sugi Variant
Explore CDK13’s pathogenic and likely-pathogenic variants individually — each with its ClinVar classification and conditions, applied ACMG criteria (ClinGen expert panel, where curated), the calibrated in-silico predictors (AlphaMissense, REVEL, SaProt, conservation), gnomAD frequency, and the predictor-disagreement QC signal — on Sugi Variant.
SpliceAI
Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 24 predictions of 1,536):
| Position(s) | Effect | Δscore | Sites |
|---|---|---|---|
| 7:39997622 | donor_gain | 1.0000 | |
| 7:39997642 | donor_gain | 1.0000 | |
| 7:39997661 | donor_gain | 1.0000 | |
| 7:40001857 | acceptor_gain | 1.0000 | |
| 7:40001859–40001860 | acceptor_loss | 1.0000 | 5 |
| 7:40002032–40002033 | donor_loss | 1.0000 | 3 |
| 7:40047811 | acceptor_gain | 1.0000 | |
| 7:40047820 | acceptor_gain | 1.0000 | |
| 7:40047878–40047879 | donor_loss | 1.0000 | 5 |
| 7:40062824–40062825 | acceptor_loss | 1.0000 | 5 |
AlphaMissense
3,481 missense substitutions predicted likely pathogenic (of 9,791 scored), across 778 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:
| Residue | Likely-pathogenic substitutions | Mean am_pathogenicity | Max am_pathogenicity |
|---|---|---|---|
| M799 | 9 | 0.988 | 1.000 |
| M794 | 9 | 0.948 | 0.999 |
| M767 | 9 | 0.937 | 0.999 |
| M818 | 9 | 0.856 | 0.997 |
| F745 | 8 | 1.000 | 1.000 |
| H796 | 8 | 1.000 | 1.000 |
| D797 | 8 | 1.000 | 1.000 |
| D837 | 8 | 1.000 | 1.000 |
| N842 | 8 | 1.000 | 1.000 |
| D855 | 8 | 1.000 | 1.000 |
| D896 | 8 | 1.000 | 1.000 |
| H1018 | 8 | 1.000 | 1.000 |
| D773 | 8 | 0.999 | 1.000 |
| F791 | 8 | 0.999 | 1.000 |
| H829 | 8 | 0.999 | 1.000 |
| H835 | 8 | 0.999 | 1.000 |
| F856 | 8 | 0.999 | 1.000 |
| D1016 | 8 | 0.999 | 1.000 |
| F780 | 8 | 0.998 | 1.000 |
| F787 | 8 | 0.998 | 1.000 |
HPA cancer prognostics
RNA cancer specificity: Low cancer specificity
Disease associations
OMIM: gene MIM:603309 | disease phenotypes: MIM:617360
GenCC curated gene-disease
1 curated gene-disease records:
| Disease | Classification | Inheritance | Records |
|---|---|---|---|
| congenital heart defects, dysmorphic facial features, and intellectual developmental disorder | Definitive | Autosomal dominant | 3 |
ClinGen Gene-Disease Validity
Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.
1 validity classifications:
| Disease | Classification | Inheritance |
|---|---|---|
| syndromic intellectual disability | Definitive | AD |
Genomics England panels (PanelApp)
Clinical diagnostic gene panels including this gene (9 panels, 9 green/diagnostic-grade). Confidence: green = diagnostic, amber = moderate.
9 panels:
| Panel | Rating |
|---|---|
| Cerebral malformation | green |
| DDG2P | green |
| Fetal anomalies | green |
| Hypotonic infant | green |
| Intellectual disability | green |
| Leukodystrophy, childhood onset | green |
| Malformations of cortical development | green |
| Paediatric disorders | green |
| Rare syndromic craniosynostosis or isolated multisuture synostosis | green |
Mondo (4): congenital heart defects, dysmorphic facial features, and intellectual developmental disorder (MONDO:0044302), syndromic intellectual disability (MONDO:0000508), neurodevelopmental disorder (MONDO:0700092), autism spectrum disorder (MONDO:0005258)
Orphanet (3): CDK13-related developmental delay-intellectual disability-facial dysmorphism-congenital heart defects syndrome (Orphanet:646278), Rare genetic syndromic intellectual disability (Orphanet:183763), NON RARE IN EUROPE: Autism (Orphanet:106)
HPO phenotypes
showing 60 of 67 phenotypes (HPO-id order):
| HPO | Term |
|---|---|
| HP:0000006 | Autosomal dominant inheritance |
| HP:0000160 | Narrow mouth |
| HP:0000200 | Short lingual frenulum |
| HP:0000215 | Thick upper lip vermilion |
| HP:0000219 | Thin upper lip vermilion |
| HP:0000233 | Thin vermilion border |
| HP:0000252 | Microcephaly |
| HP:0000269 | Prominent occiput |
| HP:0000286 | Epicanthus |
| HP:0000316 | Hypertelorism |
| HP:0000319 | Smooth philtrum |
| HP:0000322 | Short philtrum |
| HP:0000324 | Facial asymmetry |
| HP:0000356 | Abnormality of the outer ear |
| HP:0000358 | Posteriorly rotated ears |
| HP:0000369 | Low-set ears |
| HP:0000396 | Overfolded helix |
| HP:0000414 | Bulbous nose |
| HP:0000426 | Prominent nasal bridge |
| HP:0000431 | Wide nasal bridge |
| HP:0000486 | Strabismus |
| HP:0000506 | Telecanthus |
| HP:0000508 | Ptosis |
| HP:0000574 | Thick eyebrow |
| HP:0000581 | Blepharophimosis |
| HP:0000582 | Upslanted palpebral fissure |
| HP:0000691 | Microdontia |
| HP:0000717 | Autism |
| HP:0000750 | Delayed speech and language development |
| HP:0001249 | Intellectual disability |
| HP:0001250 | Seizure |
| HP:0001252 | Hypotonia |
| HP:0001263 | Global developmental delay |
| HP:0001270 | Motor delay |
| HP:0001274 | Agenesis of corpus callosum |
| HP:0001357 | Plagiocephaly |
| HP:0001382 | Joint hypermobility |
| HP:0001511 | Intrauterine growth retardation |
| HP:0001561 | Polyhydramnios |
| HP:0001629 | Ventricular septal defect |
| HP:0001631 | Atrial septal defect |
| HP:0002019 | Constipation |
| HP:0002020 | Gastroesophageal reflux |
| HP:0002079 | Hypoplasia of the corpus callosum |
| HP:0002121 | Generalized non-motor (absence) seizure |
| HP:0002162 | Low posterior hairline |
| HP:0002212 | Curly hair |
| HP:0002472 | Small cerebral cortex |
| HP:0002553 | Highly arched eyebrow |
| HP:0002572 | Episodic vomiting |
| HP:0002650 | Scoliosis |
| HP:0002714 | Downturned corners of mouth |
| HP:0003298 | Spina bifida occulta |
| HP:0003577 | Congenital onset |
| HP:0004322 | Short stature |
| HP:0005989 | Redundant neck skin |
| HP:0006610 | Wide intermamillary distance |
| HP:0006970 | Periventricular leukomalacia |
| HP:0007413 | Nevus flammeus of the forehead |
| HP:0010536 | Central sleep apnea |
GWAS associations
5 associations:
| Study | Trait | p-value |
|---|---|---|
| GCST90002388_425 | Lymphocyte count | 2e-18 |
| GCST90002400_193 | Plateletcrit | 3e-10 |
| GCST90002389_248 | Lymphocyte percentage of white cells | 1e-9 |
| GCST90002399_38 | Neutrophil percentage of white cells | 3e-9 |
| GCST004751_14 | Serum uric acid levels in response to allopurinol in gout | 3e-6 |
EFO canonical traits (from GWAS)
5 canonical traits:
| EFO ID | Trait name |
|---|---|
| EFO:0004761 | uric acid measurement |
| EFO:0004587 | lymphocyte count |
| EFO:0007993 | lymphocyte percentage of leukocytes |
| EFO:0007990 | neutrophil percentage of leukocytes |
| EFO:0007985 | platelet crit |
MeSH disease descriptors
1 disease descriptors:
| Descriptor | Name | Tree numbers |
|---|---|---|
| D065886 | Neurodevelopmental Disorders | F03.625 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (5): CHEMBL1795192 (SINGLE PROTEIN), CHEMBL3559691 (PROTEIN FAMILY), CHEMBL4296067 (PROTEIN COMPLEX), CHEMBL4630753 (PROTEIN FAMILY), CHEMBL5169085 (PROTEIN-PROTEIN INTERACTION)
Molecules with ChEMBL bioactivity
Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 62,398 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
20 molecules by phase:
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL428690 | ALVOCIDIB | 3 | 28,145 |
| CHEMBL3137331 | DEFACTINIB | 3 | 1,286 |
| CHEMBL2103840 | DINACICLIB | 3 | 2,395 |
| CHEMBL38380 | FASUDIL | 3 | 12,137 |
| CHEMBL603469 | LESTAURTINIB | 3 | |
| CHEMBL223360 | LINIFANIB | 3 | 4,094 |
| CHEMBL445813 | AT-7519 | 2 | 2,733 |
| CHEMBL215152 | DEFOSBARASERTIB | 2 | 381 |
| CHEMBL103667 | DORAMAPIMOD | 2 | 1,746 |
| CHEMBL1230609 | FORETINIB | 2 | 3,230 |
| CHEMBL1276127 | INDIRUBIN | 2 | 183 |
| CHEMBL5199065 | ISTISOCICLIB | 2 | 22 |
| CHEMBL3544964 | RAVOXERTINIB | 2 | 1,317 |
| CHEMBL384304 | RG-547 | 2 | 93 |
| CHEMBL2140408 | AMG-900 | 1 | 708 |
| CHEMBL574738 | AST-487 | 1 | 468 |
| CHEMBL296468 | BMS-387032 | 1 | 2,127 |
| CHEMBL1084546 | PF-00562271 | 1 | 424 |
| CHEMBL1230607 | PHA-793887 | 1 | 316 |
| CHEMBL3545083 | RGB-286638 | 1 | 593 |
PharmGKB: 1 entry (CPIC guideline: no)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — CRK7 subfamily
Most potent curated ligand interactions (2 total), top 2:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| CDK12 inhibitor 2 | Inhibition | 8.0 | pIC50 |
| YJZ5118 | Inhibition | 7.58 | pIC50 |
Binding affinities (BindingDB)
141 measured of 212 human assays (214 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| 1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea | KD | 0.37 nM | |
| CHEMBL4077071 | IC50 | 2 nM | |
| CEP-701 | KD | 3.4 nM | |
| Staurosporine, 8 | IC50 | 6.5 nM | |
| N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-(1’-propioloyl-1’,2’,3’,6’-tetrahydro-[2,4’- bipyridin]-5-yl)propanamide | IC50 | 7 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| 2-(6-(1-acryloyl-2,5-dihydro-1H-pyrrol-3-yl)pyridin-3-yl)-N-(5-cyclopropyl-1H- pyrazol-3-yl)acetamide | IC50 | 10 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| N-[3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]phenyl]-4-[[(E)-4-(dimethylamino)but-2-enoyl]amino]benzamide | EC50 | 10 nM | US-10787436: Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| CHEMBL5182767 | IC50 | 11 nM | |
| CHEMBL5169449 | IC50 | 12 nM | |
| 2-(4-(1-acryloyl-1,2,5,6-tetrahydropyridin-3-yl)-3-fluorophenyl)-N-(5- cyclopropyl-1H-pyrazol-3-yl)propanamide | IC50 | 14 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| N-[4-[[(2-hydroxy-1H-indol-3-yl)-phenylmethylidene]amino]phenyl]-N-methyl-2-(4-methylpiperazin-1-yl)acetamide | KI | 15 nM | US-10981896: Indolinone derivatives as inhibitors of maternal embryonic leucine zipper kinase |
| 2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluoro-benzamide | IC50 | 17 nM | |
| CHEMBL5194202 | IC50 | 20 nM | |
| 2-(1’-acryloyl-1’,2’,5’,6’-tetrahydro-[2,3’-bipyridin]-5-yl)-N-(5-cyclopropyl-1H- pyrazol-3-yl)acetamide | IC50 | 23 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| CHEMBL5187378 | IC50 | 23 nM | |
| CHEMBL5203891 | KD | 27 nM | |
| N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-[6-(1-prop-2-enoyl-3,6-dihydro-2H-pyridin-5-yl)-3-pyridinyl]propanamide | IC50 | 29 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| 2-(1’-acryloyl-1’,2’,5’,6’-tetrahydro-[2,3’-bipyridin]-5-yl)-N-(5-cyclopropyl-1H- pyrazol-3-yl)propanamide | IC50 | 30 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-[6-(1-prop-2-enoyl-2,5-dihydropyrrol-3-yl)-3-pyridinyl]propanamide | IC50 | 32 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| N-(5-(3-benzyl-1-((1r,4r)-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)ureido)-2-(4-(dimethylamino)piperidin-1-yl)phenyl)acrylamide | IC50 | 32.5 nM | US-20250100994: CDK12/13 COVALENT INHIBITORS OR PHARMACEUTICAL COMPOSITION THEREOF, AND USES THEREOF |
| N-(5-(3-benzyl-1-(((1r,4r)-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)ureido)-2-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenyl)acrylamide | IC50 | 32.5 nM | US-20250100994: CDK12/13 COVALENT INHIBITORS OR PHARMACEUTICAL COMPOSITION THEREOF, AND USES THEREOF |
| N-(5-(3-benzyl-1-((1r,4r)-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)ureido)-2-bromophenyl)acrylamide | IC50 | 32.5 nM | US-20250100994: CDK12/13 COVALENT INHIBITORS OR PHARMACEUTICAL COMPOSITION THEREOF, AND USES THEREOF |
| N-(5-(3-benzyl-1-(((1r,4S)-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)ureido)-2-((S)-3-methylpiperazin-1-yl)phenyl)acrylamide | IC50 | 32.5 nM | US-20250100994: CDK12/13 COVALENT INHIBITORS OR PHARMACEUTICAL COMPOSITION THEREOF, AND USES THEREOF |
| N-(2-(4-acetylpiperazin-1-yl)-5-(3-benzyl-1-((1r,4r)-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)ureido)phenyl)acrylamide | IC50 | 32.5 nM | US-20250100994: CDK12/13 COVALENT INHIBITORS OR PHARMACEUTICAL COMPOSITION THEREOF, AND USES THEREOF |
| N-(5-(3-benzyl-1-((1r,4R)-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)ureido)-2-((1R,4R)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl)phenyl)acrylamide | IC50 | 32.5 nM | US-20250100994: CDK12/13 COVALENT INHIBITORS OR PHARMACEUTICAL COMPOSITION THEREOF, AND USES THEREOF |
| N-(5-(3-benzyl-1-((1r,4S)-4-((5-chloropyridin-2-yl)amino)cyclohexyl)ureido)-2-((S)-3,4-dimethylpiperazin-1-yl)phenyl)acrylamide | IC50 | 32.5 nM | US-20250100994: CDK12/13 COVALENT INHIBITORS OR PHARMACEUTICAL COMPOSITION THEREOF, AND USES THEREOF |
| N-(5-(3-benzyl-1-((1r,4S)-4-((5-(trifluoromethyl)pyridin-2-yl)amino)cyclohexyl)ureido)-2-((S)-3,4-dimethylpiperazin-1-yl)phenyl)acrylamide | IC50 | 32.5 nM | US-20250100994: CDK12/13 COVALENT INHIBITORS OR PHARMACEUTICAL COMPOSITION THEREOF, AND USES THEREOF |
| N-(5-(1-((1r,4S)-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-3-((S)-1-phenylethyl)ureido)-2-((S)-3,4-dimethylpiperazin-1-yl)phenyl)acrylamide | IC50 | 32.5 nM | US-20250100994: CDK12/13 COVALENT INHIBITORS OR PHARMACEUTICAL COMPOSITION THEREOF, AND USES THEREOF |
| N-(5-(1-((1r,4S)-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-3-(2-fluorobenzyl)ureido)-2-((S)-3,4-dimethylpiperazin-1-yl)phenyl)acrylamide | IC50 | 32.5 nM | US-20250100994: CDK12/13 COVALENT INHIBITORS OR PHARMACEUTICAL COMPOSITION THEREOF, AND USES THEREOF |
| N-(5-(1-((1r,4S)-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-3-(3-fluorobenzyl)ureido)-2-((S)-3,4-dimethylpiperazin-1-yl)phenyl)acrylamide | IC50 | 32.5 nM | US-20250100994: CDK12/13 COVALENT INHIBITORS OR PHARMACEUTICAL COMPOSITION THEREOF, AND USES THEREOF |
| N-(5-(1-((1r,4S)-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-3-(4-fluorobenzyl)ureido)-2-((S)-3,4-dimethylpiperazin-1-yl)phenyl)acrylamide | IC50 | 32.5 nM | US-20250100994: CDK12/13 COVALENT INHIBITORS OR PHARMACEUTICAL COMPOSITION THEREOF, AND USES THEREOF |
| 2-(6-(1-acryloyl-2,5-dihydro-1H-pyrrol-3-yl)pyridin-3-yl)-N-(5-cyclopropyl-1H- pyrazol-3-yl)propanamide | IC50 | 34 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| 2-(1’-(but-2-ynoyl)-1’,2’,5’,6’-tetrahydro-[2,3’-bipyridin]-5-yl)-N-(5-cyclopropyl- 1H-pyrazol-3-yl)acetamide | IC50 | 37 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| CHEMBL5194833 | IC50 | 38 nM | |
| 2-(1’-acryloyl-1’,2’,3’,6’-tetrahydro-[2,4’-bipyridin]-5-yl)-N-(5-cyclopropyl-1H- pyrazol-3-yl)acetamide | IC50 | 40 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| CHEMBL6147235 | EC50 | 40 nM | |
| 2-(1’-acryloyl-1’,2’,5’,6’-tetrahydro-[2,3’-bipyridin]-5-yl)-N-(5-cyclopropyl-1H- pyrazol-3-yl)butanamide | IC50 | 41 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-(1’-propioloyl-1’,2’,5’,6’-tetrahydro-[2,3’- bipyridin]-5-yl)acetamide | IC50 | 49 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| CHEMBL4861833 | IC50 | 49 nM | |
| CHEMBL5193291 | IC50 | 52 nM | |
| CHEMBL4632717 | IC50 | 53 nM | |
| 2-(6-(1-acryloylpyrrolidin-3-yl)pyridin-3-yl)-N-(5-cyclopropyl-1H-pyrazol-3- yl)propanamide | IC50 | 55 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| CHEMBL6144395 | IC50 | 55 nM | |
| 2-(6-(1-acryloylpiperidin-4-yl)pyridin-3-yl)-N-(5-cyclopropyl-1H-pyrazol-3- yl)propanamide | IC50 | 58 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| (S)-2-(4-(1-acryloyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl)-N-(5-cyclopropyl- 1H-pyrazol-3-yl)propanamide | IC50 | 60 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| CHEMBL5191136 | IC50 | 62 nM | |
| 2-(1’-acryloyl-1’,2’,3’,6’-tetrahydro-[2,4’-bipyridin]-5-yl)-N-(5-cyclopropyl-1H- pyrazol-3-yl)propanamide | IC50 | 72 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| 2-(4-(1-acryloyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl)-N-(5-cyclopropyl-1H- pyrazol-3-yl)propanamide | IC50 | 84 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| (E)-2-(1’-(but-2-enoyl)-1’,2’,5’,6’-tetrahydro-[2,3’-bipyridin]-5-yl)-N-(5- cyclopropyl-1H-pyrazol-3-yl)acetamide | IC50 | 94 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| 2-(6-(4-acryloylpiperazin-1-yl)pyridin-3-yl)-N-(5-cyclopropyl-1H-pyrazol-3- yl)propanamide | IC50 | 99 nM | US-10894786: Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
ChEMBL bioactivities
264 potent at pChembl≥5 of 266 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
126 with measured affinity, of 721 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 |
|---|---|---|---|---|
| 1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea | 624761: Binding constant for CDC2L5 kinase domain | kd | 0.0009 | uM |
| 3-benzyl-1-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]-1-[4-[4-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]amino]acetyl]piperazin-1-yl]phenyl]urea | 1870807: Protac activity at CRBN/CDK13 in human MDA-MB-231 cells assessed as induction of CDK13 degradation incubated for 15 hrs by immunoblotting analysis | ec50 | 0.0021 | uM |
| 4-[(2,6-dichlorobenzoyl)amino]-N-piperidin-4-yl-1H-pyrazole-5-carboxamide | 624761: Binding constant for CDC2L5 kinase domain | kd | 0.0032 | uM |
| 4-[4-[benzylcarbamoyl-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]amino]phenyl]-N-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]piperazine-1-carboxamide | 1870807: Protac activity at CRBN/CDK13 in human MDA-MB-231 cells assessed as induction of CDK13 degradation incubated for 15 hrs by immunoblotting analysis | ec50 | 0.0045 | uM |
| N-[(5,6-dichloro-1H-benzimidazol-2-yl)methyl]-9-(1-methylpyrazol-4-yl)-2-morpholin-4-ylpurin-6-amine | 1890148: Binding affinity to CDK13 (unknown origin) assessed as dissociation constant | kd | 0.0049 | uM |
| 3-benzyl-1-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]-1-[4-[4-[2-[[2-(2,6-dioxopiperidin-3-yl)-3-oxo-1H-isoindol-5-yl]amino]acetyl]piperazin-1-yl]phenyl]urea | 1870807: Protac activity at CRBN/CDK13 in human MDA-MB-231 cells assessed as induction of CDK13 degradation incubated for 15 hrs by immunoblotting analysis | ec50 | 0.0062 | uM |
| 2-[4-[4-[benzylcarbamoyl-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]amino]phenyl]piperazin-1-yl]-N-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]acetamide | 1870807: Protac activity at CRBN/CDK13 in human MDA-MB-231 cells assessed as induction of CDK13 degradation incubated for 15 hrs by immunoblotting analysis | ec50 | 0.0071 | uM |
| 3-benzyl-1-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]-1-[4-[4-[2-[[2-(2,6-dioxopiperidin-3-yl)-1-oxo-3H-isoindol-5-yl]amino]acetyl]piperazin-1-yl]phenyl]urea | 1870807: Protac activity at CRBN/CDK13 in human MDA-MB-231 cells assessed as induction of CDK13 degradation incubated for 15 hrs by immunoblotting analysis | ec50 | 0.0085 | uM |
| 3-benzyl-1-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]-1-[4-(1-methyl-6-oxo-3-pyridinyl)phenyl]urea | 1870804: Binding affinity to human CDK13 (694 to 1039 residues)/CyclinK (1 to 267 residues) expressed in baculovirus infected in Sf9 cells by Biolayer interferometry | kd | 0.0086 | uM |
| N-[4-[(3R)-3-[(5-chloro-4-methoxypyrimidin-2-yl)amino]pyrrolidine-1-carbonyl]phenyl]prop-2-enamide | 2269957: Inhibition of CDK13/Cyclin K (unknown origin) using pS7-CTD peptide and ATP as substrate incubated for 120 mins by ADP-Glo reagent based luminescence analysis | ic50 | 0.0092 | uM |
| 5-(2-aminoethylsulfanyl)-3-cyclobutyl-N-[(4-pyridin-2-ylphenyl)methyl]-2H-pyrazolo[4,3-d]pyrimidin-7-amine | 1880980: Inhibition of GST-tagged human CDK13/Cyclin K expressed in Sf9 cells using RBER-IRStide peptide as substrate in presence of ATP and [gamma33-P] ATP by radioisotope filter binding assay | ic50 | 0.0120 | uM |
| N-[4-[2-[2-[(5-cyclobutyl-1H-pyrazol-3-yl)amino]-2-oxoethyl]imidazo[1,2-b]pyridazin-6-yl]-2-fluorophenyl]prop-2-enamide | 2244260: Inhibition of CDK13 (unknown origin) using GSRTPMY-NH2 as substrate in presence of ATP by ADP-glo assay | ic50 | 0.0122 | uM |
| 3-[4-[4-[benzylcarbamoyl-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]amino]phenyl]piperazin-1-yl]-N-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]propanamide | 1870807: Protac activity at CRBN/CDK13 in human MDA-MB-231 cells assessed as induction of CDK13 degradation incubated for 15 hrs by immunoblotting analysis | ec50 | 0.0125 | uM |
| N-[1-benzyl-3-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]-6-morpholin-4-yl-2-oxo-7,8,9,9a-tetrahydroperimidin-5-yl]prop-2-enamide | 2246319: Inhibition of CDK13/cyclin K (unknown origin) by ADP-Glo kinase assay | ic50 | 0.0128 | uM |
| N-[5-[benzylcarbamoyl-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]amino]-2-(1-methyl-6-oxo-3-pyridinyl)phenyl]prop-2-enamide | 2246319: Inhibition of CDK13/cyclin K (unknown origin) by ADP-Glo kinase assay | ic50 | 0.0149 | uM |
| 3-benzyl-1-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]-1-(4-piperazin-1-ylphenyl)urea | 1870804: Binding affinity to human CDK13 (694 to 1039 residues)/CyclinK (1 to 267 residues) expressed in baculovirus infected in Sf9 cells by Biolayer interferometry | kd | 0.0170 | uM |
| 3-benzyl-1-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]-1-[4-[4-[(E)-3-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]prop-2-enoyl]piperazin-1-yl]phenyl]urea | 1870807: Protac activity at CRBN/CDK13 in human MDA-MB-231 cells assessed as induction of CDK13 degradation incubated for 15 hrs by immunoblotting analysis | ec50 | 0.0207 | uM |
| 2-[(2S)-1-[3-ethyl-7-[(1-oxidopyridin-1-ium-3-yl)methylamino]pyrazolo[1,5-a]pyrimidin-5-yl]piperidin-2-yl]ethanol | 1424940: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0210 | uM |
| 4-N-[4-[5-(cyclopropylmethyl)-1-methylpyrazol-4-yl]-5-fluoropyrimidin-2-yl]cyclohexane-1,4-diamine | 1983417: Inhibition of CDK13/Cyclin K (unknown origin) preincubated for 10 mins followed by substrate and ATP addition measured after 200 mins by ADP-Glo luminescence assay | ic50 | 0.0215 | uM |
| N-[5-[benzylcarbamoyl-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]amino]-2-[(1R,4R)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]phenyl]prop-2-enamide | 2246319: Inhibition of CDK13/cyclin K (unknown origin) by ADP-Glo kinase assay | ic50 | 0.0217 | uM |
| 5-(2-aminoethylsulfanyl)-3-cyclobutyl-N-[(4-pyrazol-1-ylphenyl)methyl]-2H-pyrazolo[4,3-d]pyrimidin-7-amine | 1880980: Inhibition of GST-tagged human CDK13/Cyclin K expressed in Sf9 cells using RBER-IRStide peptide as substrate in presence of ATP and [gamma33-P] ATP by radioisotope filter binding assay | ic50 | 0.0220 | uM |
| 5-(2-aminoethylsulfanyl)-3-propan-2-yl-N-[(4-pyrazin-2-ylphenyl)methyl]-2H-pyrazolo[4,3-d]pyrimidin-7-amine | 1880980: Inhibition of GST-tagged human CDK13/Cyclin K expressed in Sf9 cells using RBER-IRStide peptide as substrate in presence of ATP and [gamma33-P] ATP by radioisotope filter binding assay | ic50 | 0.0220 | uM |
| N-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-4-carboxamide | 624761: Binding constant for CDC2L5 kinase domain | kd | 0.0230 | uM |
| N-[3-[[3-ethyl-5-[(2S)-2-(2-hydroxyethyl)piperidin-1-yl]pyrazolo[1,5-a]pyrimidin-7-yl]amino]phenyl]prop-2-enamide | 1983417: Inhibition of CDK13/Cyclin K (unknown origin) preincubated for 10 mins followed by substrate and ATP addition measured after 200 mins by ADP-Glo luminescence assay | ic50 | 0.0293 | uM |
| 3-benzyl-1-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]-1-[4-[4-[2-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]oxyacetyl]piperazin-1-yl]phenyl]urea | 1870807: Protac activity at CRBN/CDK13 in human MDA-MB-231 cells assessed as induction of CDK13 degradation incubated for 15 hrs by immunoblotting analysis | ec50 | 0.0360 | uM |
| 1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea | 624761: Binding constant for CDC2L5 kinase domain | kd | 0.0380 | uM |
| (E)-N-[4-[(3R)-3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]piperidine-1-carbonyl]phenyl]-4-(dimethylamino)but-2-enamide | 1983417: Inhibition of CDK13/Cyclin K (unknown origin) preincubated for 10 mins followed by substrate and ATP addition measured after 200 mins by ADP-Glo luminescence assay | ic50 | 0.0400 | uM |
| N-[4-[(3R)-3-[[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]amino]piperidine-1-carbonyl]phenyl]prop-2-enamide | 1652531: Inhibition of human CDK13/cyclin K using Pol2-CTD as substrate by [gamma-33P]ATP-based radioisotope filter binding assay | ic50 | 0.0490 | uM |
| (E)-N-[4-[(3R)-3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]pyrrolidine-1-carbonyl]phenyl]-4-(dimethylamino)but-2-enamide | 1769507: Inhibition of human recombinant CDK13/CyclinK assessed as reduction in substrate phosphorylation using His-c-Myc as substrate preincubated with enzyme for 5 mins followed by substrate addition for 15 mins in presence of [gamma 32P-ATP] by radioactive kinase assay | ic50 | 0.0502 | uM |
| (2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one | 1356600: Inhibition of N-terminal FLAG-tagged human full-length CDK13 (1 to 1512 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pre-incubated for 60 mins by LANCE Ultra assay | ic50 | 0.0570 | uM |
| N-[5-[benzylcarbamoyl-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]amino]-2-(4-methylpiperazin-1-yl)phenyl]prop-2-enamide | 2246319: Inhibition of CDK13/cyclin K (unknown origin) by ADP-Glo kinase assay | ic50 | 0.0668 | uM |
| 5-(2-aminoethylsulfanyl)-N-[(4-imidazol-1-ylphenyl)methyl]-3-propan-2-yl-2H-pyrazolo[4,3-d]pyrimidin-7-amine | 1880980: Inhibition of GST-tagged human CDK13/Cyclin K expressed in Sf9 cells using RBER-IRStide peptide as substrate in presence of ATP and [gamma33-P] ATP by radioisotope filter binding assay | ic50 | 0.0670 | uM |
| (E)-N-[4-[(3S)-3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]piperidine-1-carbonyl]phenyl]-4-(dimethylamino)but-2-enamide | 1653046: Inhibition of CDK13 (unknown origin) | ic50 | 0.0690 | uM |
| N-[5-[benzylcarbamoyl-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]amino]-2-[3-(dimethylamino)azetidin-1-yl]phenyl]prop-2-enamide | 2246319: Inhibition of CDK13/cyclin K (unknown origin) by ADP-Glo kinase assay | ic50 | 0.0737 | uM |
| 1-[4-[(3R)-3-[(5-chloro-4-methoxypyrimidin-2-yl)amino]pyrrolidin-1-yl]-2-methyl-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]prop-2-en-1-one | 2269957: Inhibition of CDK13/Cyclin K (unknown origin) using pS7-CTD peptide and ATP as substrate incubated for 120 mins by ADP-Glo reagent based luminescence analysis | ic50 | 0.0748 | uM |
| 1-[4-[(3R)-3-[(5-chloro-4-methoxypyrimidin-2-yl)amino]pyrrolidin-1-yl]-1,3-dihydropyrrolo[3,4-c]pyridin-2-yl]prop-2-en-1-one | 2269957: Inhibition of CDK13/Cyclin K (unknown origin) using pS7-CTD peptide and ATP as substrate incubated for 120 mins by ADP-Glo reagent based luminescence analysis | ic50 | 0.0761 | uM |
| N-[5-[benzylcarbamoyl-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]amino]-2-[2-(dimethylamino)ethyl-methylamino]phenyl]prop-2-enamide | 2246319: Inhibition of CDK13/cyclin K (unknown origin) by ADP-Glo kinase assay | ic50 | 0.0793 | uM |
| 1-[4-[(3R)-3-[(5-chloro-4-methoxypyrimidin-2-yl)amino]pyrrolidin-1-yl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]prop-2-en-1-one | 2269957: Inhibition of CDK13/Cyclin K (unknown origin) using pS7-CTD peptide and ATP as substrate incubated for 120 mins by ADP-Glo reagent based luminescence analysis | ic50 | 0.0794 | uM |
| N-[5-[benzylcarbamoyl-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]amino]-2-[(3S)-3,4-dimethylpiperazin-1-yl]phenyl]prop-2-enamide | 2246319: Inhibition of CDK13/cyclin K (unknown origin) by ADP-Glo kinase assay | ic50 | 0.0839 | uM |
| 1-[4-[(3R)-3-[(5-chloro-4-methoxypyrimidin-2-yl)amino]pyrrolidin-1-yl]-2-methoxy-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]prop-2-en-1-one | 2269957: Inhibition of CDK13/Cyclin K (unknown origin) using pS7-CTD peptide and ATP as substrate incubated for 120 mins by ADP-Glo reagent based luminescence analysis | ic50 | 0.0954 | uM |
| N-[3-[benzylcarbamoyl-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]amino]phenyl]prop-2-enamide | 2246319: Inhibition of CDK13/cyclin K (unknown origin) by ADP-Glo kinase assay | ic50 | 0.0990 | uM |
| 1-[5-[(3R)-3-[(5-chloro-4-methoxypyrimidin-2-yl)amino]pyrrolidin-1-yl]-3,4-dihydro-1H-2,6-naphthyridin-2-yl]prop-2-en-1-one | 2269957: Inhibition of CDK13/Cyclin K (unknown origin) using pS7-CTD peptide and ATP as substrate incubated for 120 mins by ADP-Glo reagent based luminescence analysis | ic50 | 0.1069 | uM |
| [4-amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl]-(2,3-difluoro-6-methoxyphenyl)methanone | 624761: Binding constant for CDC2L5 kinase domain | kd | 0.1100 | uM |
| (E)-N-[6-[(3R)-3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]piperidin-1-yl]-3-pyridinyl]but-2-enamide | 1769507: Inhibition of human recombinant CDK13/CyclinK assessed as reduction in substrate phosphorylation using His-c-Myc as substrate preincubated with enzyme for 5 mins followed by substrate addition for 15 mins in presence of [gamma 32P-ATP] by radioactive kinase assay | ic50 | 0.1200 | uM |
| 1-[[3-propan-2-yl-7-[(4-pyrazol-1-ylphenyl)methylamino]-2H-pyrazolo[4,3-d]pyrimidin-5-yl]sulfanyl]propan-2-ol | 1880980: Inhibition of GST-tagged human CDK13/Cyclin K expressed in Sf9 cells using RBER-IRStide peptide as substrate in presence of ATP and [gamma33-P] ATP by radioisotope filter binding assay | ic50 | 0.1220 | uM |
| (E)-N-[4-[(3R)-3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]piperidin-1-yl]phenyl]but-2-enamide | 1769507: Inhibition of human recombinant CDK13/CyclinK assessed as reduction in substrate phosphorylation using His-c-Myc as substrate preincubated with enzyme for 5 mins followed by substrate addition for 15 mins in presence of [gamma 32P-ATP] by radioactive kinase assay | ic50 | 0.1230 | uM |
| (E)-N-[4-[(3R)-3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]piperidin-1-yl]-3-fluorophenyl]but-2-enamide | 1769507: Inhibition of human recombinant CDK13/CyclinK assessed as reduction in substrate phosphorylation using His-c-Myc as substrate preincubated with enzyme for 5 mins followed by substrate addition for 15 mins in presence of [gamma 32P-ATP] by radioactive kinase assay | ic50 | 0.1266 | uM |
| 2-N-[4-(3-aminopropylamino)phenyl]-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine | 1983417: Inhibition of CDK13/Cyclin K (unknown origin) preincubated for 10 mins followed by substrate and ATP addition measured after 200 mins by ADP-Glo luminescence assay | ic50 | 0.1545 | uM |
| N-[2-(4-acetylpiperazin-1-yl)-5-[benzylcarbamoyl-[4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]amino]phenyl]prop-2-enamide | 2246319: Inhibition of CDK13/cyclin K (unknown origin) by ADP-Glo kinase assay | ic50 | 0.1640 | uM |
| 1-[4-[(3R)-3-[(5-chloro-4-methoxypyrimidin-2-yl)amino]pyrrolidin-1-yl]-2-morpholin-4-yl-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]prop-2-en-1-one | 2269957: Inhibition of CDK13/Cyclin K (unknown origin) using pS7-CTD peptide and ATP as substrate incubated for 120 mins by ADP-Glo reagent based luminescence analysis | ic50 | 0.1648 | uM |
CTD chemical–gene interactions
41 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Cadmium | affects reaction, decreases expression, increases abundance | 2 |
| Formaldehyde | increases expression, decreases expression | 2 |
| Valproic Acid | decreases expression, increases methylation | 2 |
| 7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide | decreases expression | 2 |
| FR900359 | affects phosphorylation | 1 |
| ginger extract | increases abundance, decreases expression | 1 |
| geldanamycin | increases expression | 1 |
| bisphenol A | decreases expression | 1 |
| lead acetate | increases expression, affects cotreatment | 1 |
| cypermethrin | decreases expression | 1 |
| zinc protoporphyrin | affects cotreatment, increases expression | 1 |
| sodium arsenite | increases expression | 1 |
| coumarin | decreases phosphorylation | 1 |
| 2-amino-3,8-dimethylimidazo(4,5-f)quinoxaline | increases expression | 1 |
| 2-amino-1-methyl-6-phenylimidazo(4,5-b)pyridine | increases expression | 1 |
| polyhexamethyleneguanidine | increases expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| ICG 001 | decreases expression | 1 |
| Irinotecan | decreases expression | 1 |
| Leflunomide | decreases expression | 1 |
| Air Pollutants | affects expression, increases abundance | 1 |
| Caffeine | affects phosphorylation | 1 |
| Coumestrol | decreases expression | 1 |
| Doxorubicin | decreases expression | 1 |
| Emodin | decreases expression | 1 |
| Estradiol | affects expression | 1 |
| Hydrogen Peroxide | affects cotreatment, increases expression | 1 |
| Menthol | increases expression | 1 |
| Nicotine | increases expression | 1 |
| Oils, Volatile | decreases expression, increases abundance | 1 |
ChEMBL screening assays
257 unique, capped per target: 250 binding, 7 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1174102 | Binding | Inhibition of CDC2L5 at 10 uM | Broad spectrum alkynyl inhibitors of T315I Bcr-Abl. — *Bioorg Med Chem Lett* |
| CHEMBL5445783 | Functional | Affinity Phenotypic Cellular interaction: (In-Cell western blot (using MDA-MB-231 cells)) EUB0001632a CDK13 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
Cellosaurus cell lines
3 cell lines: 3 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_SI21 | HAP1 CDK13 (-) 1 | Cancer cell line | Male |
| CVCL_SI22 | HAP1 CDK13 (-) 2 | Cancer cell line | Male |
| CVCL_SI23 | HAP1 CDK13 (-) 3 | Cancer cell line | Male |
Clinical trials (associated diseases)
Via MONDO — disease-level, not drug-specific.
showing 60 of 300 trials:
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT04586348 | Phase 4 | UNKNOWN | Prenatal Iodine Supplementation and Early Childhood Neurodevelopment |
| NCT04873115 | Phase 4 | UNKNOWN | Double-blind, Placebo-controlled, Randomized Clinical Trial Comparing the Efficacy and Safety of Sialanar Plus orAl rehabiLitation Against Placebo Plus Oral Rehabilitation for chIldren and Adolescents With seVere Sialorrhoea and Neurodisabilties, |
| NCT00391261 | Phase 4 | COMPLETED | An Open-label Trial of Metformin for Weight Control of Pediatric Patients on Antipsychotic Medications. |
| NCT01028820 | Phase 4 | COMPLETED | FMRI Brain Activation of Aripiprazole Treatment in Autism Spectrum Disorders |
| NCT01333865 | Phase 4 | COMPLETED | A Study of Memantine Hydrochloride (Namenda®) for Cognitive and Behavioral Impairment in Adults With Autism Spectrum Disorders |
| NCT01337700 | Phase 4 | COMPLETED | Milnacipran in Autism and the Functional Locus Coeruleus and Noradrenergic Model of Autism |
| NCT01695200 | Phase 4 | COMPLETED | Omega-3 Fatty Acids in Autism Spectrum Disorders |
| NCT02096952 | Phase 4 | COMPLETED | Methylphenidate ER Liquid Formulation in Adults With ASD and ADHD |
| NCT02235467 | Phase 4 | COMPLETED | Multisite Study: Parental Training Using Video Modelling to Develop Social Skills in Children With Autism |
| NCT02940574 | Phase 4 | COMPLETED | Neural and Behavioral Effects of Oxytocin in Autism Spectrum Disorders |
| NCT03333629 | Phase 4 | COMPLETED | Promoting Positive Outcomes for Individuals With ASD: Linking Early Detection, Treatment, and Long-term Outcomes |
| NCT03337646 | Phase 4 | COMPLETED | Evaluation of the Effect and Safety of Lisdexamfetamine in Children Aged 6-12 With ADHD and Autism |
| NCT03538431 | Phase 4 | COMPLETED | Improving Driving in Young People With Autism Spectrum Disorders |
| NCT03757585 | Phase 4 | COMPLETED | Natural Treatments for the Management of Emotional Dysregulation in Youth With Non-verbal Learning Disability (NVLD) and/or Autism Spectrum Disorders (ASD) |
| NCT04903353 | Phase 4 | COMPLETED | Pragmatic Trial Comparing Weight Gain in Children With Autism Taking Risperidone Versus Aripiprazole |
| NCT05063656 | Phase 4 | COMPLETED | Biomarker-Driven Pharmacological Treatment of Adolescents With Autism Spectrum Disorder With Gabapentin |
| NCT05146245 | Phase 4 | UNKNOWN | Safety and Pharmacokinetics of Antipsychotics in Children 2: Studying TDM in an RCT |
| NCT05916339 | Phase 4 | RECRUITING | AWARE: Management of ADHD in Autism Spectrum Disorder |
| NCT05954052 | Phase 4 | TERMINATED | A Study of Glutathione in Children With Autism Spectrum Disorder |
| NCT06853665 | Phase 4 | RECRUITING | The TEAM Study - Treatment Efficacy for Autism/Attention Using Mixed Amphetamine |
| NCT07054697 | Phase 4 | COMPLETED | Pilot-RCT With Individualized Homeopathic Treatment in the Children With Autism Spectrum Disorder |
| NCT07161804 | Phase 4 | COMPLETED | Pilot RCT Using Homeopathic Medicines in ASD |
| NCT07439042 | Phase 4 | RECRUITING | Buspirone for Anxiety in Autistic Youth |
| NCT07770152 | Phase 4 | NOT_YET_RECRUITING | Semaglutide in Youth With Autism Spectrum Disorder |
| NCT02559102 | Phase 3 | COMPLETED | Dexmedetomidine Sedation Versus General Anaesthesia for Inguinal Hernia Surgery in Infants |
| NCT02757079 | Phase 3 | COMPLETED | Study of the Efficacy and Safety of NPC-15 for Sleep Disorders of Children With Neurodevelopmental Disorders |
| NCT06915480 | Phase 3 | RECRUITING | Reducing Missed Appointments |
| NCT07377032 | Phase 3 | RECRUITING | TAP-GRIN: Interventional Study on Patients With GRIN-related Neurodevelopmental Disorders |
| NCT01302964 | Phase 3 | COMPLETED | Mirtazapine Treatment of Anxiety in Children and Adolescents With Pervasive Developmental Disorders |
| NCT01706523 | Phase 3 | TERMINATED | Open Label Extension Study of STX209 (Arbaclofen) in Autism Spectrum Disorders |
| NCT01825798 | Phase 3 | COMPLETED | Treatment of Overweight Induced by Antipsychotic Medication in Young People With Autism Spectrum Disorders (ASD) |
| NCT01972074 | Phase 3 | COMPLETED | Behavioral and Neural Response to Memantine in Adolescents With Autism Spectrum Disorder |
| NCT02985749 | Phase 3 | COMPLETED | A Study of Oxytocin for the Treatment of Social Impairment in Individuals With High Functioning Autism Spectrum Disorder |
| NCT03197922 | Phase 3 | COMPLETED | Treatment of Encopresis in Children With Autism Spectrum Disorders |
| NCT03504917 | Phase 3 | TERMINATED | A Study of Balovaptan in Adults With Autism Spectrum Disorder With a 2-Year Open-Label Extension |
| NCT03553875 | Phase 3 | TERMINATED | Memantine for the Treatment of Social Deficits in Youth With Disorders of Impaired Social Interactions |
| NCT03640156 | Phase 3 | COMPLETED | Modulating Socially Adaptive Mirror System Functioning in Autism by Oxytocin |
| NCT03715153 | Phase 3 | TERMINATED | Efficacy and Safety of Bumetanide Oral Liquid Formulation in Children Aged From 2 to Less Than 7 Years Old With Autism Spectrum Disorder. |
| NCT03715166 | Phase 3 | TERMINATED | Efficacy and Safety of Bumetanide Oral Liquid Formulation in Children and Adolescents Aged From 7 to Less Than 18 Years Old With Autism Spectrum Disorder |
| NCT04233502 | Phase 3 | WITHDRAWN | Efficacy and Safety of Slenyto for Insomnia in Children With ASD |
| NCT04578756 | Phase 3 | COMPLETED | Open-Label, Flexible-dose Study to Evaluate the Long-Term Safety and Tolerability of Cariprazine in the Treatment of Pediatric Participants With Schizophrenia, Bipolar I Disorder, or Autism Spectrum Disorder |
| NCT04623398 | Phase 3 | COMPLETED | Effect of Lithium in Patients With Autism Spectrum Disorder and Phelan-McDermid Syndrome (SHANK3 Haploinsufficiency) |
| NCT04725383 | Phase 3 | TERMINATED | Amitriptyline for Repetitive Behaviors in Autism Spectrum Disorders |
| NCT05212493 | Phase 3 | COMPLETED | The Effects of Medical Cannabis in Children With Autistic Spectrum Disorder |
| NCT05361707 | Phase 3 | UNKNOWN | Evaluating the Effects of Tasimelteon in Individuals With Autism Spectrum Disorder (ASD) and Sleep Disturbances |
| NCT05439616 | Phase 3 | COMPLETED | Study of Cariprazine Oral Capsules or Solution to Assess Adverse Events and Change in Irritability Due to Autism Spectrum Disorder (ASD) in Participants Aged 5-17 Years With ASD |
| NCT06229210 | Phase 3 | RECRUITING | Safety and Tolerability Trial of Lumateperone in Pediatric Patients With Schizophrenia, Bipolar Disorder or Autism Spectrum Disorder |
| NCT06333964 | Phase 3 | COMPLETED | A Study to Evaluate the Efficacy and Safety of AST-001 in ASD Children |
| NCT07257939 | Phase 3 | NOT_YET_RECRUITING | NTI164 in Autism Spectrum Disorder |
| NCT07655115 | Phase 3 | RECRUITING | Single Dose Double-blind, Placebo-controlled Cross-over (SDDBPCCO) Shiftability Study, Will be Followed by a 10-week Open-label Study With Arbaclofen (4 Weeks of Titration and Then 6 Weeks of Active/Stable Treatment). The Effects of Arbaclofen on Target EEG and ERG Metrics Will be Associated With th |
| NCT02909959 | Phase 2 | COMPLETED | Sulforaphane for the Treatment of Young Men With Autism Spectrum Disorder |
| NCT06081348 | Phase 2 | RECRUITING | Sertraline vs. Placebo in the Treatment of Anxiety in Children and AdoLescents With NeurodevelopMental Disorders |
| NCT06352372 | Phase 2 | COMPLETED | Safety and Efficacy of tPBM for Epileptiform Activity in Autism |
| NCT00251303 | Phase 2 | COMPLETED | Riluzole to Treat Child and Adolescent Obsessive-Compulsive Disorder With or Without Autism Spectrum Disorders |
| NCT00614198 | Phase 2 | COMPLETED | ScanBrit Dietary Intervention in Autism |
| NCT00619190 | Phase 2 | COMPLETED | Study of Aripiprazole to Treat Children and Adolescents With Autism |
| NCT00709202 | Phase 2 | COMPLETED | Efficacy and Tolerability Study of Betahistine to Ameliorate Antipsychotic Associated Weight Gain |
| NCT00846547 | Phase 2 | COMPLETED | Open-Label Study of the Safety and Tolerability of STX209 in Subjects With Autism Spectrum Disorders |
| NCT01064973 | Phase 2 | TERMINATED | An Open Label Extension Study of STX209 in Subjects With Autism Spectrum Disorders |
| NCT01170325 | Phase 2 | WITHDRAWN | A Study of Divalproex Sodium in Children With ASD and Epileptiform EEG |
Predicted chemistry — Sugi Predict
The predicted patent-compound landscape for CDK13 across ~30M SureChEMBL compounds — explore on Sugi Predict.
Related Atlas pages
- Associated diseases: congenital heart defects, dysmorphic facial features, and intellectual developmental disorder, syndromic intellectual disability
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): cardiomyopathy, congenital heart defects, dysmorphic facial features, and intellectual developmental disorder, primary amenorrhea, syndromic intellectual disability