NEK5
gene geneOn this page
Summary
NEK5 (NIMA related kinase 5, HGNC:7748) is a protein-coding gene on chromosome 13q14.3, encoding Serine/threonine-protein kinase Nek5 (Q6P3R8).
Predicted to enable protein kinase activity. Predicted to be involved in chromatin remodeling. Predicted to act upstream of or within positive regulation of striated muscle cell differentiation. Located in sperm flagellum.
Source: NCBI Gene 341676 — RefSeq curated summary.
At a glance
- Clinical variants (ClinVar): 116 total
- Druggable target: yes — 10 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_001365552
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:7748 |
| Approved symbol | NEK5 |
| Name | NIMA related kinase 5 |
| Location | 13q14.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000197168 |
| Ensembl biotype | protein_coding |
| OMIM | 616731 |
| Entrez | 341676 |
Gene structure
Transcript identifiers
Ensembl transcripts: 10 — 7 protein_coding, 1 nonsense_mediated_decay, 1 retained_intron, 1 protein_coding_CDS_not_defined
ENST00000355568, ENST00000465811, ENST00000529080, ENST00000617045, ENST00000647945, ENST00000652119, ENST00000652502, ENST00000684899, ENST00000966557, ENST00000966558
RefSeq mRNA: 2 — MANE Select: NM_001365552
NM_001365552, NM_199289
CCDS: CCDS31979, CCDS91811
Canonical transcript exons
ENST00000684899 — 24 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001400891 | 52083260 | 52083352 |
| ENSE00001401739 | 52102092 | 52102292 |
| ENSE00001402890 | 52101933 | 52102014 |
| ENSE00001403501 | 52099743 | 52099876 |
| ENSE00001421462 | 52104498 | 52104552 |
| ENSE00001423499 | 52110340 | 52110410 |
| ENSE00001424715 | 52108318 | 52108404 |
| ENSE00001426138 | 52112268 | 52112365 |
| ENSE00001426763 | 52110494 | 52110577 |
| ENSE00001429426 | 52119319 | 52119415 |
| ENSE00001430316 | 52076063 | 52076143 |
| ENSE00001432414 | 52093054 | 52093235 |
| ENSE00001476350 | 52127595 | 52127662 |
| ENSE00002188414 | 52127366 | 52127504 |
| ENSE00003493010 | 52087338 | 52087454 |
| ENSE00003579546 | 52075758 | 52075826 |
| ENSE00003586656 | 52071944 | 52072070 |
| ENSE00003606744 | 52089247 | 52089313 |
| ENSE00003617327 | 52086277 | 52086363 |
| ENSE00003832466 | 52061819 | 52061953 |
| ENSE00003833287 | 52050104 | 52050221 |
| ENSE00003833810 | 52065484 | 52065609 |
| ENSE00003838129 | 52033611 | 52037218 |
| ENSE00003932067 | 52129029 | 52129073 |
Expression profiles
Bgee: expression breadth ubiquitous, 185 present calls, max score 98.32.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.2954 / max 24.8304, expressed in 141 samples.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 137410 | 0.2954 | 141 |
Top tissues by expression
251 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| bronchial epithelial cell | CL:0002328 | 98.32 | gold quality |
| bronchus | UBERON:0002185 | 97.09 | gold quality |
| right uterine tube | UBERON:0001302 | 95.22 | gold quality |
| oviduct epithelium | UBERON:0004804 | 95.11 | gold quality |
| buccal mucosa cell | CL:0002336 | 95.05 | gold quality |
| mucosa of paranasal sinus | UBERON:0005030 | 95.05 | gold quality |
| endothelial cell | CL:0000115 | 90.31 | gold quality |
| fallopian tube | UBERON:0003889 | 84.52 | gold quality |
| olfactory segment of nasal mucosa | UBERON:0005386 | 84.22 | gold quality |
| sperm | CL:0000019 | 82.99 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 82.94 | gold quality |
| epithelium of nasopharynx | UBERON:0001951 | 81.80 | gold quality |
| nasal cavity epithelium | UBERON:0005384 | 81.66 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 79.47 | gold quality |
| caput epididymis | UBERON:0004358 | 76.89 | gold quality |
| right testis | UBERON:0004534 | 76.71 | gold quality |
| left testis | UBERON:0004533 | 76.70 | gold quality |
| germinal epithelium of ovary | UBERON:0001304 | 76.42 | gold quality |
| testis | UBERON:0000473 | 76.32 | gold quality |
| nasal cavity mucosa | UBERON:0001826 | 71.56 | gold quality |
| ventricular zone | UBERON:0003053 | 70.58 | gold quality |
| calcaneal tendon | UBERON:0003701 | 70.07 | gold quality |
| right lung | UBERON:0002167 | 69.33 | gold quality |
| tendon | UBERON:0000043 | 68.47 | gold quality |
| parietal pleura | UBERON:0002400 | 67.59 | gold quality |
| corpus callosum | UBERON:0002336 | 67.21 | gold quality |
| hypothalamus | UBERON:0001898 | 66.38 | gold quality |
| left uterine tube | UBERON:0001303 | 65.69 | gold quality |
| tendon of biceps brachii | UBERON:0008188 | 65.33 | silver quality |
| endometrium | UBERON:0001295 | 64.48 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 2.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-CURD-114 | yes | 60.85 |
| E-ANND-3 | yes | 9.68 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
25 targeting NEK5, 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-4713-3P | 100.00 | 65.92 | 505 |
| HSA-MIR-4533 | 100.00 | 69.48 | 2758 |
| HSA-MIR-196A-1-3P | 99.99 | 72.15 | 2772 |
| HSA-MIR-4487 | 99.96 | 64.58 | 1252 |
| HSA-MIR-6772-5P | 99.94 | 67.01 | 577 |
| HSA-MIR-95-5P | 99.89 | 72.17 | 3973 |
| HSA-MIR-6764-5P | 99.75 | 67.89 | 2304 |
| HSA-MIR-494-3P | 99.70 | 71.45 | 2795 |
| HSA-MIR-3202 | 99.66 | 67.70 | 2737 |
| HSA-MIR-4690-5P | 99.65 | 66.24 | 813 |
| HSA-MIR-1915-3P | 99.58 | 66.79 | 1988 |
| HSA-MIR-143-3P | 99.49 | 69.05 | 1457 |
| HSA-MIR-4770 | 99.49 | 69.09 | 1451 |
| HSA-MIR-6088 | 99.29 | 68.45 | 1284 |
| HSA-MIR-146A-3P | 99.13 | 68.99 | 1881 |
| HSA-MIR-5001-3P | 98.91 | 67.28 | 1394 |
| HSA-MIR-6760-5P | 98.87 | 66.73 | 1515 |
| HSA-MIR-198 | 98.70 | 67.32 | 920 |
| HSA-MIR-3921 | 97.81 | 67.45 | 1431 |
| HSA-MIR-144-5P | 97.66 | 69.90 | 531 |
| HSA-MIR-4653-5P | 97.22 | 67.72 | 1429 |
| HSA-MIR-921 | 97.09 | 66.45 | 562 |
| HSA-MIR-3184-3P | 96.96 | 66.91 | 845 |
| HSA-MIR-3156-5P | 96.93 | 67.36 | 800 |
| HSA-MIR-3162-5P | 95.67 | 67.53 | 794 |
Literature-anchored findings (GeneRIF, showing 10)
- The hNek5 is mitochondrial localization and its role on cell death and cell respiration defects through COX11, MTX2 and BCLAF1. (PMID:25725288)
- Nek5 is required for the loss of centrosome linker proteins and enhanced microtubule nucleation that lead to timely centrosome separation and bipolar spindle formation in mitosis (PMID:25963817)
- Data show that up-regulated NEK5 was significantly associated with breast tumor progression and poor overall prognosis; and that silencing of NEK5 can significantly suppress the proliferation both in vivo and in vitro, inhibiting migration, and invasion. NEK5 can up-regulate Cyclin A2 by direct interaction. (PMID:30675923)
- NEK5 interacts with topoisomerase IIbeta and is involved in the DNA damage response induced by etoposide. (PMID:31090963)
- the NEK protein kinases emerge as important proteins in thyroid cancer development and may help to identify malignancy and aggressiveness features during diagnosis. (PMID:31906878)
- Knockdown of lncRNA XIST inhibits hypoxia-induced glycolysis, migration and invasion through regulating miR-381-3p/NEK5 axis in nasopharyngeal carcinoma. (PMID:32196601)
- NEK5 interacts with LonP1 and its kinase activity is essential for the regulation of mitochondrial functions and mtDNA maintenance. (PMID:33547867)
- Targeting Never-In-Mitosis-A Related Kinase 5 in Cancer: A Review. (PMID:33749548)
- NEK5 activity regulates the mesenchymal and migratory phenotype in breast cancer cells. (PMID:34196902)
- Identification of biological pathways and processes regulated by NEK5 in breast epithelial cells via an integrated proteomic approach. (PMID:36550548)
Cross-species orthologs
2 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Nek5 | ENSMUSG00000037738 |
| rattus_norvegicus | Nek5 | ENSRNOG00000048769 |
Paralogs (8): NEK11 (ENSG00000114670), NEK2 (ENSG00000117650), NEK6 (ENSG00000119408), NEK9 (ENSG00000119638), NEK3 (ENSG00000136098), NEK7 (ENSG00000151414), NEK8 (ENSG00000160602), NEK10 (ENSG00000163491)
Protein
Protein identifiers
Serine/threonine-protein kinase Nek5 — Q6P3R8 (reviewed: Q6P3R8)
Alternative names: Never in mitosis A-related kinase 5
All UniProt accessions (5): A0A3B3ITQ6, A0A494C168, A0A8I5KQI9, E9PIX7, Q6P3R8
UniProt curated annotations — full annotation on UniProt →
Subcellular location. Cell projection. Cilium. Flagellum.
Similarity. Belongs to the protein kinase superfamily. NEK Ser/Thr protein kinase family. NIMA subfamily.
RefSeq proteins (2): NP_001352481, NP_954983 (=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 |
| IPR051131 | NEK_Ser/Thr_kinase_NIMA | Family |
Pfam: PF00069
Catalyzed reactions (Rhea), 2 shown:
- L-seryl-[protein] + ATP = O-phospho-L-seryl-[protein] + ADP + H(+) (RHEA:17989)
- L-threonyl-[protein] + ATP = O-phospho-L-threonyl-[protein] + ADP + H(+) (RHEA:46608)
UniProt features (11 total): sequence variant 3, region of interest 2, binding site 2, chain 1, domain 1, compositionally biased region 1, active site 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q6P3R8-F1 | 59.66 | 0.26 |
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): 128 (proton acceptor)
Ligand- & substrate-binding residues (2): 10–18; 33
Function
Pathways and Gene Ontology
Reactome pathways
0 pathways
MSigDB gene sets: 43 (showing top):
SENGUPTA_NASOPHARYNGEAL_CARCINOMA_DN, chr13q14, GOCC_MOTILE_CILIUM, GOCC_CILIUM, GOMF_PROTEIN_KINASE_ACTIVITY, GOMF_KINASE_ACTIVITY, GOMF_PROTEIN_SERINE_THREONINE_KINASE_ACTIVITY, DODD_NASOPHARYNGEAL_CARCINOMA_DN, GOMF_ADENYL_NUCLEOTIDE_BINDING, GOMF_TRANSFERASE_ACTIVITY_TRANSFERRING_PHOSPHORUS_CONTAINING_GROUPS, GOCC_9PLUS2_MOTILE_CILIUM, CHARAFE_BREAST_CANCER_LUMINAL_VS_BASAL_UP, GSE5503_MLN_DC_VS_PLN_DC_ACTIVATED_ALLOGENIC_TCELL_DN, GSE13522_WT_VS_IFNG_KO_SKIN_UP, ZNF7_TARGET_GENES
GO Biological Process (2): protein phosphorylation (GO:0006468), positive regulation of striated muscle cell differentiation (GO:0051155)
GO Molecular Function (8): protein kinase activity (GO:0004672), protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), metal ion binding (GO:0046872), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), kinase activity (GO:0016301), transferase activity (GO:0016740)
GO Cellular Component (4): cilium (GO:0005929), sperm flagellum (GO:0036126), motile cilium (GO:0031514), cell projection (GO:0042995)
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| protein kinase activity | 2 |
| phosphorylation | 1 |
| protein modification process | 1 |
| striated muscle cell differentiation | 1 |
| positive regulation of muscle cell differentiation | 1 |
| regulation of striated muscle cell differentiation | 1 |
| kinase activity | 1 |
| phosphotransferase activity, alcohol group as acceptor | 1 |
| catalytic activity, acting on a protein | 1 |
| adenyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| cation binding | 1 |
| nucleoside phosphate binding | 1 |
| heterocyclic compound binding | 1 |
| transferase activity, transferring phosphorus-containing groups | 1 |
| catalytic activity | 1 |
| intraciliary transport particle | 1 |
| membrane-bounded organelle | 1 |
| plasma membrane bounded cell projection | 1 |
| 9+2 motile cilium | 1 |
| cilium | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
632 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| NEK5 | COX11 | Q9Y6N1 | 507 |
| NEK5 | BCLAF1 | Q9NYF8 | 490 |
| NEK5 | TMEM69 | Q5SWH9 | 394 |
| NEK5 | CLPP | Q16740 | 375 |
| NEK5 | CCDC137 | Q6PK04 | 339 |
| NEK5 | LRRC45 | Q96CN5 | 333 |
| NEK5 | ADGRG2 | Q8IZP9 | 333 |
| NEK5 | CROCC | Q5TZA2 | 332 |
| NEK5 | HIPK4 | Q8NE63 | 325 |
| NEK5 | CSRNP2 | Q9H175 | 319 |
| NEK5 | ANKRD34B | A5PLL1 | 317 |
| NEK5 | NAGK | Q9UJ70 | 315 |
| NEK5 | C1QTNF7 | Q9BXJ2 | 311 |
| NEK5 | MRGPRX3 | Q96LB0 | 309 |
| NEK5 | FN3K | Q9H479 | 306 |
IntAct
6 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| NEK1 | CFAP410 | psi-mi:“MI:0914”(association) | 0.510 |
| P | psi-mi:“MI:0914”(association) | 0.350 | |
| M | psi-mi:“MI:0914”(association) | 0.350 | |
| FTL | SH3PXD2B | psi-mi:“MI:0914”(association) | 0.350 |
| NEK5 | NEK1 | psi-mi:“MI:0915”(physical association) | 0.000 |
BioGRID (10): NEK1 (Affinity Capture-MS), NEK5 (Synthetic Lethality), NEK5 (Affinity Capture-MS), NEK5 (Affinity Capture-MS), NEK5 (Affinity Capture-MS), NEK5 (Positive Genetic), HMGB1 (Cross-Linking-MS (XL-MS)), ATP5B (Cross-Linking-MS (XL-MS)), NEK5 (Cross-Linking-MS (XL-MS)), RPL26 (Cross-Linking-MS (XL-MS))
ESM2 similar proteins: A0AUV4, A0JM98, A1A5Q6, A2KF29, B1WAS2, C0HKC8, C0HKC9, O60285, O70551, O88866, P51957, P57058, P57059, Q2T9U5, Q4R9F7, Q5R7G9, Q5RD27, Q5REX1, Q5XHI9, Q60670, Q641K5, Q66HE5, Q68UT7, Q6IFT4, Q6P3R8, Q6REY9, Q6VZ17, Q80VH0, Q8BI55, Q8BLD6, Q8BZN4, Q8C0N0, Q8C0V7, Q8C0X8, Q8CFH6, Q8NE63, Q8TF76, Q96SB4, Q9H093, Q9H0K1
Diamond homologs: A0A078CGE6, A2BD05, A2QHV0, A2ZMH2, A7SNN5, D3ZBE5, D3ZGQ5, E9Q3S4, G5EFM9, H2L099, O01775, O13839, O14047, O22040, O22042, O35942, O61122, P11837, P22209, P41892, P48479, P48963, P51954, P51955, P51956, P51957, P59895, P84199, Q03428, Q08942, Q0CL79, Q0KHQ5, Q0WPH8, Q10GB1, Q2QAV0, Q2QMH1, Q3SWY6, Q3UGM2, Q40541, Q4FZD7
SIGNOR signaling
1 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| NEK5 | “up-regulates activity” | CCNA2 | binding |
Disease & clinical
Clinical variants and AI predictions
ClinVar
116 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 95 |
| Likely benign | 9 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
3691 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 13:52072113:T:TC | acceptor_gain | 1.0000 |
| 13:52076057:TCTTA:T | donor_loss | 1.0000 |
| 13:52076058:CTTAC:C | donor_loss | 1.0000 |
| 13:52076059:TTA:T | donor_loss | 1.0000 |
| 13:52076060:TA:T | donor_loss | 1.0000 |
| 13:52076061:ACC:A | donor_loss | 1.0000 |
| 13:52076062:C:CA | donor_loss | 1.0000 |
| 13:52076140:TGTC:T | acceptor_gain | 1.0000 |
| 13:52086270:AATTT:A | donor_loss | 1.0000 |
| 13:52086271:ATTT:A | donor_loss | 1.0000 |
| 13:52086272:TTTAC:T | donor_loss | 1.0000 |
| 13:52086273:TTA:T | donor_loss | 1.0000 |
| 13:52086274:TACC:T | donor_loss | 1.0000 |
| 13:52086275:ACCTC:A | donor_loss | 1.0000 |
| 13:52086276:C:CT | donor_loss | 1.0000 |
| 13:52086276:CCT:C | donor_gain | 1.0000 |
| 13:52087342:T:TA | donor_gain | 1.0000 |
| 13:52089315:T:C | acceptor_gain | 1.0000 |
| 13:52089315:T:TC | acceptor_gain | 1.0000 |
| 13:52127359:A:C | donor_gain | 1.0000 |
| 13:52127360:CTTTA:C | donor_loss | 1.0000 |
| 13:52127361:TTTA:T | donor_loss | 1.0000 |
| 13:52127362:TTAC:T | donor_loss | 1.0000 |
| 13:52127363:TACC:T | donor_loss | 1.0000 |
| 13:52127364:ACCT:A | donor_loss | 1.0000 |
| 13:52127501:TTTC:T | acceptor_gain | 1.0000 |
| 13:52127503:TC:T | acceptor_gain | 1.0000 |
| 13:52127504:CC:C | acceptor_gain | 1.0000 |
| 13:52127505:C:CC | acceptor_gain | 1.0000 |
| 13:52127506:T:C | acceptor_loss | 1.0000 |
AlphaMissense
5572 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 13:52110507:T:A | D128V | 0.998 |
| 13:52110507:T:G | D128A | 0.998 |
| 13:52127384:T:A | K33N | 0.998 |
| 13:52127384:T:G | K33N | 0.998 |
| 13:52104545:A:G | W188R | 0.997 |
| 13:52104545:A:T | W188R | 0.997 |
| 13:52110500:T:A | K130N | 0.996 |
| 13:52110500:T:G | K130N | 0.996 |
| 13:52110501:T:A | K130I | 0.996 |
| 13:52110543:A:G | L116P | 0.996 |
| 13:52104517:A:G | L197P | 0.995 |
| 13:52110366:G:C | D147E | 0.995 |
| 13:52110366:G:T | D147E | 0.995 |
| 13:52110367:T:A | D147V | 0.995 |
| 13:52110506:G:C | D128E | 0.995 |
| 13:52110506:G:T | D128E | 0.995 |
| 13:52110507:T:C | D128G | 0.995 |
| 13:52104551:C:G | D186H | 0.994 |
| 13:52110367:T:G | D147A | 0.994 |
| 13:52110568:A:G | W108R | 0.994 |
| 13:52110568:A:T | W108R | 0.994 |
| 13:52112331:A:C | C83W | 0.994 |
| 13:52102290:A:C | F204L | 0.993 |
| 13:52102290:A:T | F204L | 0.993 |
| 13:52102292:A:G | F204L | 0.993 |
| 13:52104543:C:A | W188C | 0.993 |
| 13:52104543:C:G | W188C | 0.993 |
| 13:52110367:T:C | D147G | 0.993 |
| 13:52110368:C:G | D147H | 0.993 |
| 13:52127385:T:A | K33I | 0.993 |
dbSNP variants (sampled 300 via entrez): RS1000018567 (13:52129714 A>T), RS1000034579 (13:52041379 G>A), RS1000059191 (13:52082247 G>A,C,T), RS1000076538 (13:52129617 A>C), RS1000104736 (13:52094611 G>A), RS1000132909 (13:52034831 GCCA>G), RS1000186218 (13:52073474 C>T), RS1000187552 (13:52056025 C>A), RS1000229644 (13:52068041 G>A), RS1000237926 (13:52067850 C>A,T), RS1000248660 (13:52063327 G>A), RS1000267439 (13:52109099 C>T), RS1000274331 (13:52116495 T>C), RS1000312272 (13:52095599 G>C), RS1000315772 (13:52050172 C>T)
Disease associations
OMIM: gene MIM:616731 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
0 associations (top):
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL4524130 (PROTEIN FAMILY), CHEMBL5044 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
10 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 32,685 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL1287853 | FEDRATINIB | 4 | 3,554 |
| CHEMBL477772 | PAZOPANIB | 4 | 15,540 |
| CHEMBL522892 | DOVITINIB | 3 | 4,944 |
| CHEMBL603469 | LESTAURTINIB | 3 | |
| CHEMBL475251 | R-406 | 2 | 762 |
| CHEMBL558752 | RAF-265 | 2 | 2,721 |
| CHEMBL572878 | TOZASERTIB | 2 | 2,998 |
| CHEMBL1908394 | GSK-461364 | 1 | 1,093 |
| CHEMBL1908397 | KW-2449 | 1 | 622 |
| 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 — NIMA (never in mitosis gene a)- related kinase (NEK) family
Binding affinities (BindingDB)
5 measured of 5 human assays (5 total across all organisms); most potent 5 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| Staurosporine | KD | 1.7 nM |
| (3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyril | KD | 520 nM |
| N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide | KD | 1100 nM |
| 1-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea | KD | 1400 nM |
| 1-methyl-5-[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl]oxy-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine | KD | 4500 nM |
ChEMBL bioactivities
32 potent at pChembl≥5 of 32 total, top 22 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 7.89 | Kd | 13 | nM | R-406 |
| 7.12 | IC50 | 76.3 | nM | STAUROSPORINE |
| 7.11 | IC50 | 77.4 | nM | STAUROSPORINE |
| 7.01 | IC50 | 96.5 | nM | STAUROSPORINE |
| 6.88 | IC50 | 132 | nM | CHEMBL5575113 |
| 6.24 | Kd | 570 | nM | FEDRATINIB |
| 6.14 | Kd | 730 | nM | CHEMBL537757 |
| 6.09 | Kd | 810 | nM | STAUROSPORINE |
| 6.05 | Kd | 890 | nM | CHEMBL386051 |
| 6.00 | IC50 | 1000 | nM | TP-030-1 |
| 6.00 | IC50 | 1000 | nM | TP-030-2 |
| 6.00 | IC50 | 1000 | nM | TP-030n |
| 5.96 | Kd | 1100 | nM | AST-487 |
| 5.96 | Kd | 1100 | nM | GSK-461364 |
| 5.85 | Kd | 1400 | nM | CHEMBL2425628 |
| 5.64 | Kd | 2300 | nM | KW-2449 |
| 5.64 | Kd | 2300 | nM | DOVITINIB |
| 5.50 | Kd | 3200 | nM | RAF-265 |
| 5.38 | Kd | 4200 | nM | TOZASERTIB |
| 5.36 | IC50 | 4420 | nM | CHEMBL3745885 |
| 5.25 | Kd | 5600 | nM | LESTAURTINIB |
| 5.14 | Kd | 7300 | nM | PAZOPANIB |
PubChem BioAssay actives
29 with measured affinity, of 252 total; 16 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | 1948826: Inhibition of NEK5 (unknown origin) assessed as dissociation constant | kd | 0.0130 | 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 | 1715241: Inhibition of human NEK5 using MBP as substrate by [gamma-33P]-ATP assay | ic50 | 0.0763 | uM |
| N-propan-2-yl-4-[[4-(2-pyrrolidin-1-ylquinazolin-6-yl)pyrimidin-2-yl]amino]benzamide | 2095013: Inhibition of NEK5 (unknown origin) in presence of ATP | ic50 | 0.1320 | uM |
| Fedratinib | 1948826: Inhibition of NEK5 (unknown origin) assessed as dissociation constant | kd | 0.5700 | uM |
| 7-(1H-indol-2-yl)-5-methyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine | 1948826: Inhibition of NEK5 (unknown origin) assessed as dissociation constant | kd | 0.7300 | uM |
| 6-(2,6-dichlorophenyl)-8-methyl-2-(3-methylsulfanylanilino)pyrido[2,3-d]pyrimidin-7-one | 1948826: Inhibition of NEK5 (unknown origin) assessed as dissociation constant | kd | 0.8900 | uM |
| 1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea | 1948826: Inhibition of NEK5 (unknown origin) assessed as dissociation constant | kd | 1.1000 | uM |
| 5-[6-[(4-methylpiperazin-1-yl)methyl]benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide | 624742: Binding constant for NEK5 kinase domain | kd | 1.1000 | uM |
| (4-hydroxypiperidin-1-yl)-[4-[[4-[4-(3-methylsulfonylpropoxy)indol-1-yl]pyrimidin-2-yl]amino]cyclohexyl]methanone | 769501: Binding affinity to NEK5 (unknown origin) | kd | 1.4000 | uM |
| [4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone | 1948826: Inhibition of NEK5 (unknown origin) assessed as dissociation constant | kd | 2.3000 | uM |
| 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one | 435534: Binding constant for NEK5 kinase domain | kd | 2.3000 | uM |
| 1-methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine | 435534: Binding constant for NEK5 kinase domain | kd | 3.2000 | uM |
| N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide | 435534: Binding constant for NEK5 kinase domain | kd | 4.2000 | uM |
| 6-(2,4-difluorophenyl)sulfonyl-2-(1H-indol-5-ylamino)-8-methylpyrido[2,3-d]pyrimidin-7-one | 1269895: Inhibition of human NEK5 using MBP as substrate | ic50 | 4.4200 | uM |
| (15S,16S,18R)-16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one | 624742: Binding constant for NEK5 kinase domain | kd | 5.6000 | uM |
| Pazopanib | 624742: Binding constant for NEK5 kinase domain | kd | 7.3000 | uM |
CTD chemical–gene interactions
12 total (human), top 12 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| benzo(e)pyrene | increases methylation | 1 |
| aflatoxin B2 | increases methylation | 1 |
| Sunitinib | increases expression | 1 |
| Fulvestrant | increases methylation | 1 |
| Air Pollutants | increases abundance, increases expression | 1 |
| Benzo(a)pyrene | decreases methylation, increases methylation | 1 |
| Methapyrilene | increases methylation | 1 |
| Smoke | increases expression, increases abundance | 1 |
| Tobacco Smoke Pollution | decreases expression | 1 |
| Tretinoin | decreases expression | 1 |
| Triclosan | increases expression | 1 |
| Aflatoxin B1 | increases methylation | 1 |
ChEMBL screening assays
96 unique, capped per target: 96 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL4887137 | Binding | NEK Invitrogen kinase activity assay | Data for DCP probe PF-04554878 |
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.