CDK17
gene geneOn this page
Also known as PCTAIRE2
Summary
CDK17 (cyclin dependent kinase 17, HGNC:8750) is a protein-coding gene on chromosome 12q23.1, encoding Cyclin-dependent kinase 17 (Q00537). May play a role in terminally differentiated neurons.
The protein encoded by this gene belongs to the cdc2/cdkx subfamily of the ser/thr family of protein kinases. It has similarity to a rat protein that is thought to play a role in terminally differentiated neurons. Alternatively spliced transcript variants encoding different isoforms have been found.
Source: NCBI Gene 5128 — RefSeq curated summary.
At a glance
- GWAS associations: 3
- Clinical variants (ClinVar): 68 total
- Druggable target: yes — 33 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_002595
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:8750 |
| Approved symbol | CDK17 |
| Name | cyclin dependent kinase 17 |
| Location | 12q23.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | PCTAIRE2 |
| Ensembl gene | ENSG00000059758 |
| Ensembl biotype | protein_coding |
| OMIM | 603440 |
| Entrez | 5128 |
Gene structure
Transcript identifiers
Ensembl transcripts: 25 — 20 protein_coding, 3 retained_intron, 2 protein_coding_CDS_not_defined
ENST00000261211, ENST00000542666, ENST00000543119, ENST00000548422, ENST00000548734, ENST00000549899, ENST00000550971, ENST00000551484, ENST00000551816, ENST00000552262, ENST00000552496, ENST00000553042, ENST00000859518, ENST00000859519, ENST00000859520, ENST00000859521, ENST00000859522, ENST00000964177, ENST00000964178, ENST00000964179, ENST00000964180, ENST00000964181, ENST00000964182, ENST00000964183, ENST00000964184
RefSeq mRNA: 2 — MANE Select: NM_002595
NM_001170464, NM_002595
CCDS: CCDS53819, CCDS9061
Canonical transcript exons
ENST00000261211 — 17 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000817991 | 96311052 | 96311177 |
| ENSE00000994210 | 96313321 | 96313454 |
| ENSE00001275553 | 96280808 | 96280885 |
| ENSE00001275561 | 96282509 | 96282599 |
| ENSE00001275567 | 96283603 | 96283645 |
| ENSE00001276071 | 96278261 | 96280279 |
| ENSE00001345590 | 96399986 | 96400439 |
| ENSE00003496344 | 96298869 | 96298983 |
| ENSE00003497295 | 96300304 | 96300360 |
| ENSE00003505363 | 96294999 | 96295122 |
| ENSE00003526008 | 96286664 | 96286761 |
| ENSE00003549841 | 96286043 | 96286148 |
| ENSE00003605664 | 96297627 | 96297721 |
| ENSE00003637695 | 96323948 | 96324112 |
| ENSE00003682723 | 96297270 | 96297332 |
| ENSE00003688747 | 96334719 | 96334865 |
| ENSE00003693586 | 96289167 | 96289287 |
Expression profiles
Bgee: expression breadth ubiquitous, 295 present calls, max score 97.41.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 31.7529 / max 440.6746, expressed in 1819 samples.
FANTOM5 promoters (12 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 132798 | 22.9953 | 1816 |
| 132800 | 2.9035 | 1547 |
| 132797 | 1.6686 | 514 |
| 132799 | 1.5621 | 951 |
| 132796 | 0.8344 | 310 |
| 132780 | 0.5431 | 215 |
| 132791 | 0.4174 | 212 |
| 132793 | 0.2545 | 104 |
| 132794 | 0.2165 | 92 |
| 132792 | 0.2077 | 89 |
Top tissues by expression
300 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| corpus callosum | UBERON:0002336 | 97.41 | gold quality |
| CA1 field of hippocampus | UBERON:0003881 | 97.34 | gold quality |
| Brodmann (1909) area 23 | UBERON:0013554 | 97.28 | gold quality |
| lateral globus pallidus | UBERON:0002476 | 96.77 | gold quality |
| calcaneal tendon | UBERON:0003701 | 96.32 | gold quality |
| visceral pleura | UBERON:0002401 | 96.00 | gold quality |
| postcentral gyrus | UBERON:0002581 | 95.73 | gold quality |
| vena cava | UBERON:0004087 | 95.73 | gold quality |
| superior frontal gyrus | UBERON:0002661 | 95.71 | gold quality |
| middle temporal gyrus | UBERON:0002771 | 95.64 | gold quality |
| entorhinal cortex | UBERON:0002728 | 95.57 | gold quality |
| parietal lobe | UBERON:0001872 | 95.47 | gold quality |
| orbitofrontal cortex | UBERON:0004167 | 95.32 | gold quality |
| substantia nigra pars reticulata | UBERON:0001966 | 95.24 | gold quality |
| germinal epithelium of ovary | UBERON:0001304 | 95.01 | gold quality |
| subthalamic nucleus | UBERON:0001906 | 94.93 | gold quality |
| globus pallidus | UBERON:0001875 | 94.89 | gold quality |
| tibia | UBERON:0000979 | 94.73 | gold quality |
| substantia nigra pars compacta | UBERON:0001965 | 94.50 | gold quality |
| colonic epithelium | UBERON:0000397 | 94.47 | gold quality |
| medial globus pallidus | UBERON:0002477 | 94.40 | gold quality |
| occipital lobe | UBERON:0002021 | 94.38 | gold quality |
| choroid plexus epithelium | UBERON:0003911 | 94.37 | gold quality |
| nucleus accumbens | UBERON:0001882 | 94.28 | gold quality |
| pleura | UBERON:0000977 | 94.27 | gold quality |
| primary visual cortex | UBERON:0002436 | 94.26 | gold quality |
| inferior olivary complex | UBERON:0002127 | 94.08 | gold quality |
| Brodmann (1909) area 46 | UBERON:0006483 | 94.08 | gold quality |
| pericardium | UBERON:0002407 | 94.07 | gold quality |
| secondary oocyte | CL:0000655 | 93.97 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 8.94 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
207 targeting CDK17, 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-5692A | 100.00 | 74.40 | 6850 |
| HSA-MIR-200B-3P | 100.00 | 73.31 | 2693 |
| HSA-MIR-200C-3P | 100.00 | 73.35 | 2685 |
| HSA-MIR-429 | 100.00 | 73.44 | 2698 |
| HSA-MIR-4262 | 100.00 | 73.26 | 3931 |
| HSA-MIR-3646 | 100.00 | 73.56 | 5283 |
| HSA-LET-7A-3P | 100.00 | 74.03 | 3932 |
| HSA-LET-7B-3P | 100.00 | 74.08 | 3913 |
| HSA-LET-7F-1-3P | 100.00 | 74.02 | 3928 |
| HSA-MIR-98-3P | 100.00 | 74.08 | 3907 |
| HSA-MIR-3163 | 100.00 | 77.23 | 8605 |
| HSA-MIR-3613-3P | 100.00 | 76.36 | 7965 |
| HSA-MIR-4682 | 100.00 | 68.89 | 1258 |
| HSA-MIR-1252-5P | 100.00 | 69.80 | 2774 |
| HSA-MIR-340-5P | 100.00 | 72.50 | 4437 |
| HSA-MIR-3064-3P | 100.00 | 70.09 | 1254 |
| HSA-MIR-196A-1-3P | 99.99 | 72.15 | 2772 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-4789-3P | 99.99 | 70.75 | 2484 |
| HSA-MIR-223-3P | 99.99 | 70.14 | 1140 |
| HSA-MIR-3662 | 99.99 | 73.82 | 5684 |
| HSA-MIR-181A-5P | 99.99 | 72.96 | 2995 |
| HSA-MIR-181B-5P | 99.99 | 72.97 | 2996 |
| HSA-MIR-181C-5P | 99.99 | 72.95 | 2996 |
| HSA-MIR-181D-5P | 99.99 | 73.04 | 2997 |
| HSA-MIR-513B-5P | 99.99 | 69.96 | 2150 |
| HSA-MIR-433-3P | 99.98 | 69.37 | 1203 |
| HSA-MIR-4775 | 99.98 | 75.00 | 6394 |
| HSA-MIR-103A-3P | 99.98 | 69.14 | 1595 |
| HSA-MIR-107 | 99.98 | 69.14 | 1595 |
Literature-anchored findings (GeneRIF, showing 3)
- Increased levels of PCTAIRE2 is associated with Alzheimer’s disease. (PMID:26885753)
- CircCDK17 knockdown inhibits tumor progression and cell glycolysis by downregulaing YWHAZ expression through sponging miR-1294 in cervical cancer. (PMID:35168653)
- CircCDK17 promotes the proliferation and metastasis of ovarian cancer cells by sponging miR-22-3p to regulate CD147 expression. (PMID:37952105)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | cdk17 | ENSDARG00000079470 |
| mus_musculus | Cdk17 | ENSMUSG00000020015 |
| rattus_norvegicus | Cdk17 | ENSRNOG00000004148 |
Paralogs (26): CDKL3 (ENSG00000006837), CDKL5 (ENSG00000008086), CDK11A (ENSG00000008128), CDK14 (ENSG00000058091), CDK13 (ENSG00000065883), CDKL1 (ENSG00000100490), CDK16 (ENSG00000102225), CDK6 (ENSG00000105810), PRP4K (ENSG00000112739), CDK18 (ENSG00000117266), CDK2 (ENSG00000123374), CDK8 (ENSG00000132964), CDK7 (ENSG00000134058), CDK4 (ENSG00000135446), CDK9 (ENSG00000136807), CDK15 (ENSG00000138395), CDKL2 (ENSG00000138769), CDK19 (ENSG00000155111), CDK20 (ENSG00000156345), CDK5 (ENSG00000164885), CDK12 (ENSG00000167258), CDK1 (ENSG00000170312), CDK10 (ENSG00000185324), CDKL4 (ENSG00000205111), CDK11B (ENSG00000248333), CDK3 (ENSG00000250506)
Protein
Protein identifiers
Cyclin-dependent kinase 17 — Q00537 (reviewed: Q00537)
Alternative names: Cell division protein kinase 17, PCTAIRE-motif protein kinase 2, Serine/threonine-protein kinase PCTAIRE-2
All UniProt accessions (6): Q00537, F5H6Z0, F8VQZ9, F8VUX2, F8VZY6, F8W1S5
UniProt curated annotations — full annotation on UniProt →
Function. May play a role in terminally differentiated neurons. Has a Ser/Thr-phosphorylating activity for histone H1.
Subunit / interactions. Found in a complex containing CABLES1, CDK16 and TDRD7. Interacts with TDRD7.
Similarity. Belongs to the protein kinase superfamily. CMGC Ser/Thr protein kinase family. CDC2/CDKX subfamily.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q00537-1 | 1 | yes |
| Q00537-2 | 2 |
RefSeq proteins (2): NP_001163935, NP_002586* (*=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)
Substrate kinetics (BRENDA)
4 substrates with measured Km, best-characterized 4. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| ADAQHATPPKKKRKVEDPKDF | 0.046–0.521 | 2 |
| ATP | 0.0052–0.017 | 2 |
| FIN1 | 0.003 | 1 |
| PKTPKKAKKL | 0.0029 | 1 |
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 (23 total): modified residue 8, region of interest 3, sequence conflict 3, compositionally biased region 2, binding site 2, chain 1, domain 1, splice variant 1, sequence variant 1, active site 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q00537-F1 | 70.51 | 0.43 |
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): 313 (proton acceptor)
Ligand- & substrate-binding residues (2): 198–206; 221
Post-translational modifications (8): 9, 80, 92, 105, 137, 146, 165, 180
Function
Pathways and Gene Ontology
Reactome pathways
0 pathways
MSigDB gene sets: 302 (showing top):
MYAATNNNNNNNGGC_UNKNOWN, TGCTGCT_MIR15A_MIR16_MIR15B_MIR195_MIR424_MIR497, GOBP_CELL_CYCLE_PHASE_TRANSITION, ACTGCAG_MIR173P, GGGTGGRR_PAX4_03, XU_HGF_SIGNALING_NOT_VIA_AKT1_48HR_UP, ONKEN_UVEAL_MELANOMA_UP, GOBP_REGULATION_OF_CELL_CYCLE, DACOSTA_UV_RESPONSE_VIA_ERCC3_COMMON_DN, DEBIASI_APOPTOSIS_BY_REOVIRUS_INFECTION_UP, AACTTT_UNKNOWN, BENPORATH_NOS_TARGETS, ATCATGA_MIR433, P300_01, ACTTTAT_MIR1425P
GO Biological Process (2): protein phosphorylation (GO:0006468), regulation of cell cycle phase transition (GO:1901987)
GO Molecular Function (9): protein kinase activity (GO:0004672), cyclin-dependent protein serine/threonine kinase activity (GO:0004693), ATP binding (GO:0005524), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein serine/threonine kinase activity (GO:0004674), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)
GO Cellular Component (2): nucleus (GO:0005634), cytoplasm (GO:0005737)
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| protein kinase activity | 2 |
| phosphorylation | 1 |
| protein modification process | 1 |
| regulation of cell cycle process | 1 |
| cell cycle phase transition | 1 |
| kinase activity | 1 |
| phosphotransferase activity, alcohol group as acceptor | 1 |
| catalytic activity, acting on a protein | 1 |
| protein serine/threonine kinase activity | 1 |
| cyclin-dependent protein kinase activity | 1 |
| adenyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| nucleoside phosphate binding | 1 |
| heterocyclic compound binding | 1 |
| binding | 1 |
| transferase activity, transferring phosphorus-containing groups | 1 |
| catalytic activity | 1 |
| intracellular membrane-bounded organelle | 1 |
| intracellular anatomical structure | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
3217 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CDK17 | TDRD7 | Q8NHU6 | 910 |
| CDK17 | CABLES1 | Q8TDN4 | 882 |
| CDK17 | CCDC180 | Q9P1Z9 | 829 |
| CDK17 | CCNA2 | P20248 | 565 |
| CDK17 | CCNY | Q8ND76 | 549 |
| CDK17 | CCNA1 | P78396 | 543 |
| CDK17 | CCNL2 | Q96S94 | 521 |
| CDK17 | CCNC | P24863 | 517 |
| CDK17 | SCGN | O76038 | 460 |
| CDK17 | CCND3 | P30281 | 455 |
| CDK17 | SUSD4 | Q5VX71 | 429 |
| CDK17 | CCNE2 | O96020 | 416 |
| CDK17 | MGAT4C | Q9UBM8 | 389 |
| CDK17 | SIK3 | Q9Y2K2 | 386 |
| CDK17 | CDK10 | Q15131 | 385 |
IntAct
91 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| S100B | S100A4 | psi-mi:“MI:0914”(association) | 0.870 |
| CDK2 | CCNB2 | psi-mi:“MI:0914”(association) | 0.860 |
| YWHAG | CDK17 | psi-mi:“MI:0915”(physical association) | 0.860 |
| CDK1 | CCNB2 | psi-mi:“MI:0914”(association) | 0.840 |
| YWHAB | PIK3C2A | psi-mi:“MI:0914”(association) | 0.800 |
| CDK17 | YWHAZ | psi-mi:“MI:0914”(association) | 0.800 |
| CDK17 | YWHAZ | psi-mi:“MI:0915”(physical association) | 0.800 |
| CDK14 | CDKN1A | psi-mi:“MI:0914”(association) | 0.770 |
| CCNB2 | CDKN1B | psi-mi:“MI:0914”(association) | 0.670 |
| YWHAG | BLTP3B | psi-mi:“MI:0914”(association) | 0.640 |
| PPP2R3A | WTIP | psi-mi:“MI:0914”(association) | 0.640 |
| CDK17 | YWHAE | psi-mi:“MI:0915”(physical association) | 0.620 |
| CDK17 | CDK16 | psi-mi:“MI:0915”(physical association) | 0.620 |
| CDK16 | CDK17 | psi-mi:“MI:0914”(association) | 0.620 |
| YWHAH | PLEKHG3 | psi-mi:“MI:0914”(association) | 0.610 |
| YWHAB | BLTP3B | psi-mi:“MI:0914”(association) | 0.610 |
| TDRD7 | TACC1 | psi-mi:“MI:0914”(association) | 0.580 |
| YWHAE | PIK3C2A | psi-mi:“MI:0914”(association) | 0.570 |
| YWHAH | BLTP3B | psi-mi:“MI:0914”(association) | 0.570 |
| YWHAZ | PIK3C2A | psi-mi:“MI:0914”(association) | 0.570 |
| CDK17 | DPY30 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CDKN2B | CDK17 | psi-mi:“MI:0915”(physical association) | 0.560 |
| BICDL2 | CDK17 | psi-mi:“MI:0915”(physical association) | 0.560 |
| YWHAG | SHTN1 | psi-mi:“MI:0914”(association) | 0.560 |
| MANSC1 | KLRG2 | psi-mi:“MI:0914”(association) | 0.530 |
| CDK16 | CSNK2A2 | psi-mi:“MI:0914”(association) | 0.530 |
| YWHAQ | IGLC7 | psi-mi:“MI:0914”(association) | 0.530 |
BioGRID (105): CDK17 (Affinity Capture-MS), CDK17 (Affinity Capture-MS), CDK17 (Affinity Capture-MS), PPP2R3A (Affinity Capture-MS), TDRD7 (Affinity Capture-MS), SUGP1 (Affinity Capture-MS), DHPS (Affinity Capture-MS), PPP2R5E (Affinity Capture-MS), C12orf43 (Affinity Capture-MS), FEM1A (Affinity Capture-MS), CDK17 (Reconstituted Complex), CDK17 (Affinity Capture-MS), CDK17 (Affinity Capture-MS), CDK17 (Affinity Capture-MS), PPP2R3A (Affinity Capture-MS)
ESM2 similar proteins: A1CL96, A1D624, A2QU77, A2X0M1, A2Y4B6, A3LUB9, A4IIW7, A4QXX4, B0VXE8, B0VXL7, B6A7Q3, C0RW22, O13958, O35495, O35831, O35832, O44514, O94921, P0CS76, P0CS77, P29620, Q00536, Q00537, Q04735, Q04899, Q07002, Q0CQK1, Q0E459, Q0TWJ7, Q11179, Q1EBK0, Q1RLU9, Q2GYV9, Q2UC58, Q336M2, Q39010, Q4FCZ5, Q4WYR6, Q5BAE1, Q5RD01
Diamond homologs: A4IIW7, A8XA58, B0VXE8, B0VXL7, B6A7Q3, C0RW22, G5ECH7, O35495, O35831, O35832, O55076, O61847, O74456, O94921, O96821, P00546, P04551, P06493, P11440, P13863, P17157, P23111, P23437, P23572, P23573, P24033, P24100, P24923, P24941, P25859, P29618, P29619, P34112, P34117, P35567, P38973, P39951, P43063, P43450, P48609
SIGNOR signaling
0 interactions.
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 85 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.
Reactome pathways:
| Pathway | Partners | Fold | FDR |
|---|---|---|---|
| Chk1/Chk2(Cds1) mediated inactivation of Cyclin B:Cdk1 complex | 8 | 89.6× | 3e-12 |
| Activation of BAD and translocation to mitochondria | 7 | 88.8× | 7e-11 |
| SARS-CoV-1 targets host intracellular signalling and regulatory pathways | 7 | 78.4× | 2e-10 |
| Activation of BH3-only proteins | 7 | 57.9× | 1e-09 |
| TP53 Regulates Transcription of Cell Cycle Genes | 5 | 45.3× | 2e-06 |
| FOXO-mediated transcription | 7 | 39.2× | 2e-08 |
| RHO GTPases activate PKNs | 7 | 37.0× | 3e-08 |
| Intrinsic Pathway for Apoptosis | 7 | 34.2× | 5e-08 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| protein targeting | 5 | 23.8× | 1e-03 |
| cellular senescence | 5 | 19.2× | 1e-03 |
| G1/S transition of mitotic cell cycle | 5 | 13.0× | 4e-03 |
| intracellular protein localization | 7 | 9.5× | 1e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
68 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 48 |
| Likely benign | 0 |
| Benign | 1 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
2803 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 12:96280883:CAC:C | acceptor_gain | 1.0000 |
| 12:96280885:CCT:C | acceptor_loss | 1.0000 |
| 12:96280886:CT:C | acceptor_loss | 1.0000 |
| 12:96280887:T:A | acceptor_loss | 1.0000 |
| 12:96282503:TCTTA:T | donor_loss | 1.0000 |
| 12:96282505:TTA:T | donor_loss | 1.0000 |
| 12:96282506:TA:T | donor_loss | 1.0000 |
| 12:96282507:A:AC | donor_gain | 1.0000 |
| 12:96282508:C:CA | donor_gain | 1.0000 |
| 12:96282508:CT:C | donor_gain | 1.0000 |
| 12:96282508:CTTT:C | donor_gain | 1.0000 |
| 12:96282511:T:A | donor_gain | 1.0000 |
| 12:96282595:TCATA:T | acceptor_gain | 1.0000 |
| 12:96282596:CATA:C | acceptor_gain | 1.0000 |
| 12:96282596:CATAC:C | acceptor_gain | 1.0000 |
| 12:96282597:ATA:A | acceptor_gain | 1.0000 |
| 12:96282598:TA:T | acceptor_gain | 1.0000 |
| 12:96282598:TACT:T | acceptor_loss | 1.0000 |
| 12:96282600:C:CA | acceptor_loss | 1.0000 |
| 12:96282600:C:CC | acceptor_gain | 1.0000 |
| 12:96282601:T:G | acceptor_loss | 1.0000 |
| 12:96282602:G:C | acceptor_gain | 1.0000 |
| 12:96282602:G:GC | acceptor_gain | 1.0000 |
| 12:96283598:CTTA:C | donor_loss | 1.0000 |
| 12:96283599:TTA:T | donor_loss | 1.0000 |
| 12:96283600:TA:T | donor_loss | 1.0000 |
| 12:96283641:CTAAC:C | acceptor_gain | 1.0000 |
| 12:96283642:TAAC:T | acceptor_gain | 1.0000 |
| 12:96283646:C:CC | acceptor_gain | 1.0000 |
| 12:96283646:CTA:C | acceptor_loss | 1.0000 |
AlphaMissense
3413 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 12:96282582:C:A | R461S | 1.000 |
| 12:96282582:C:G | R461S | 1.000 |
| 12:96286687:A:G | L398P | 1.000 |
| 12:96286708:C:T | G391E | 1.000 |
| 12:96286709:C:G | G391R | 1.000 |
| 12:96286709:C:T | G391R | 1.000 |
| 12:96286735:A:C | M382R | 1.000 |
| 12:96286737:T:A | E381D | 1.000 |
| 12:96286737:T:G | E381D | 1.000 |
| 12:96286738:T:A | E381V | 1.000 |
| 12:96286739:C:T | E381K | 1.000 |
| 12:96286749:G:C | C377W | 1.000 |
| 12:96286750:C:T | C377Y | 1.000 |
| 12:96286751:A:G | C377R | 1.000 |
| 12:96286753:C:T | G376D | 1.000 |
| 12:96286754:C:G | G376R | 1.000 |
| 12:96286760:C:G | G374R | 1.000 |
| 12:96289168:A:G | W373R | 1.000 |
| 12:96289168:A:T | W373R | 1.000 |
| 12:96289173:T:A | D371V | 1.000 |
| 12:96289173:T:C | D371G | 1.000 |
| 12:96289173:T:G | D371A | 1.000 |
| 12:96289174:C:A | D371Y | 1.000 |
| 12:96289174:C:G | D371H | 1.000 |
| 12:96289188:T:C | Y366C | 1.000 |
| 12:96289189:A:G | Y366H | 1.000 |
| 12:96289206:A:G | L360P | 1.000 |
| 12:96289206:A:T | L360H | 1.000 |
| 12:96289215:G:T | P357H | 1.000 |
| 12:96289218:G:T | P356Q | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000033130 (12:96305081 C>A,G,T), RS1000049339 (12:96347182 G>C), RS1000051447 (12:96328351 G>A), RS1000081841 (12:96328673 C>G), RS1000121856 (12:96369146 T>C), RS1000122384 (12:96345766 A>G), RS1000153846 (12:96351136 C>G), RS1000185986 (12:96304291 C>T), RS1000216718 (12:96391500 A>G), RS1000256340 (12:96298577 AGTTT>A), RS1000317595 (12:96377081 T>C), RS1000343945 (12:96310247 C>A,G), RS1000346470 (12:96310855 T>C), RS1000382644 (12:96322161 G>A), RS1000410734 (12:96397175 T>C)
Disease associations
OMIM: gene MIM:603440 | disease phenotypes:
GenCC curated gene-disease
Mondo (1): breast ductal adenocarcinoma (MONDO:0005590)
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
3 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST001414_1 | Phospholipid levels (plasma) | 3.000000e-08 |
| GCST002932_5 | Manganese levels | 6.000000e-06 |
| GCST006630_36 | Diastolic blood pressure | 4.000000e-11 |
EFO canonical traits (1, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0006336 | diastolic blood pressure |
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D018270 | Carcinoma, Ductal, Breast | C04.557.470.200.025.232.500; C04.557.470.615.132.500; C04.588.180.390; C17.800.090.500.390 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (4): CHEMBL3559691 (PROTEIN FAMILY), CHEMBL4523636 (PROTEIN COMPLEX), CHEMBL4523637 (PROTEIN COMPLEX), CHEMBL5790 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
33 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 273,526 (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 |
|---|---|---|---|
| CHEMBL1078178 | MOMELOTINIB | 4 | 3,481 |
| CHEMBL1171837 | PONATINIB | 4 | 8,955 |
| CHEMBL1287853 | FEDRATINIB | 4 | 3,554 |
| CHEMBL1336 | SORAFENIB | 4 | 86,060 |
| CHEMBL189963 | PALBOCICLIB | 4 | 13,102 |
| CHEMBL1946170 | REGORAFENIB | 4 | 12,678 |
| CHEMBL2028663 | DABRAFENIB | 4 | 12,430 |
| CHEMBL502835 | NINTEDANIB | 4 | 8,545 |
| CHEMBL535 | SUNITINIB | 4 | 79,020 |
| CHEMBL576982 | QUIZARTINIB | 4 | 4,432 |
| CHEMBL2103840 | DINACICLIB | 3 | 2,257 |
| CHEMBL428690 | ALVOCIDIB | 3 | 27,781 |
| CHEMBL522892 | DOVITINIB | 3 | 4,944 |
| CHEMBL603469 | LESTAURTINIB | 3 | |
| CHEMBL1276127 | INDIRUBIN | 2 | 181 |
| CHEMBL5199065 | ISTISOCICLIB | 2 | 21 |
| CHEMBL1230609 | FORETINIB | 2 | 3,096 |
| CHEMBL1738757 | REBASTINIB | 2 | 1,478 |
| CHEMBL3039513 | DECERNOTINIB | 2 | 1,418 |
| CHEMBL384304 | RG-547 | 2 | 93 |
| CHEMBL3991932 | PEXMETINIB | 2 | |
| CHEMBL445813 | AT-7519 | 2 | |
| CHEMBL475251 | R-406 | 2 | |
| CHEMBL495727 | AT-9283 | 2 | |
| CHEMBL564829 | MILCICLIB | 2 | |
| CHEMBL572878 | TOZASERTIB | 2 | |
| CHEMBL1084546 | PF-00562271 | 1 | |
| CHEMBL1908397 | KW-2449 | 1 | |
| CHEMBL296468 | BMS-387032 | 1 | |
| CHEMBL3128043 | PF-03758309 | 1 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — TAIRE subfamily
Binding affinities (BindingDB)
8 measured of 8 human assays (8 total across all organisms); most potent 8 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| Staurosporine | KD | 1.7 nM |
| 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide | KD | 370 nM |
| (3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyril | KD | 520 nM |
| 1-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea | KD | 1400 nM |
| BMS-387072 | KD | 1800 nM |
| 1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b | KD | 3100 nM |
| N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | KD | 3500 nM |
| 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S)-3-hydroxy-1-methyl-4-piperidinyl]-1-benzopyran-4-one | KD | 5300 nM |
ChEMBL bioactivities
62 potent at pChembl≥5 of 66 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.07 | Kd | 0.86 | nM | RG-547 |
| 9.02 | Kd | 0.95 | nM | AT-7519 |
| 8.70 | Kd | 2 | nM | BMS-387032 |
| 8.30 | Kd | 5 | nM | XL-228 |
| 8.22 | Kd | 6 | nM | ALVOCIDIB |
| 8.15 | Kd | 7 | nM | CYC-116 |
| 8.15 | Kd | 7 | nM | AT-7519 |
| 8.15 | Kd | 7 | nM | REBASTINIB |
| 7.97 | IC50 | 10.7 | nM | STAUROSPORINE |
| 7.89 | Kd | 13 | nM | BMS-387032 |
| 7.86 | IC50 | 13.8 | nM | STAUROSPORINE |
| 7.85 | Kd | 14 | nM | PF-03758309 |
| 7.82 | Kd | 15 | nM | AST-487 |
| 7.79 | IC50 | 16.3 | nM | STAUROSPORINE |
| 7.44 | Kd | 36 | nM | DABRAFENIB |
| 7.16 | Kd | 69 | nM | CHEMBL1082152 |
| 7.05 | Kd | 89 | nM | PF-00562271 |
| 7.03 | Kd | 93 | nM | NINTEDANIB |
| 7.02 | Kd | 96 | nM | STAUROSPORINE |
| 6.92 | Kd | 120.5 | nM | CHEMBL5653589 |
| 6.92 | ED50 | 120.5 | nM | CHEMBL5653589 |
| 6.86 | Kd | 139 | nM | DECERNOTINIB |
| 6.77 | Kd | 170 | nM | FORETINIB |
| 6.54 | Kd | 290 | nM | JNJ-7706621 |
| 6.48 | Kd | 330 | nM | R-406 |
| 6.47 | Kd | 335 | nM | PONATINIB |
| 6.46 | Kd | 350 | nM | FEDRATINIB |
| 6.40 | Kd | 402 | nM | PEXMETINIB |
| 6.32 | Kd | 480 | nM | ALVOCIDIB |
| 6.14 | Kd | 719 | nM | REGORAFENIB |
| 6.14 | Kd | 720 | nM | LESTAURTINIB |
| 6.11 | Kd | 778 | nM | DINACICLIB |
| 6.09 | Kd | 810 | nM | TAE-684 |
| 6.06 | Kd | 880 | nM | PHA-665752 |
| 6.00 | IC50 | 1000 | nM | TP-030-1 |
| 6.00 | IC50 | 1000 | nM | TP-030-2 |
| 6.00 | IC50 | 1000 | nM | TP-030n |
| 5.94 | Kd | 1148 | nM | AT-9283 |
| 5.93 | Kd | 1177 | nM | MILCICLIB |
| 5.92 | Kd | 1200 | nM | SUNITINIB |
| 5.90 | Kd | 1272 | nM | PALBOCICLIB |
| 5.86 | Kd | 1382 | nM | MOMELOTINIB |
| 5.82 | IC50 | 1500 | nM | CHEMBL3656841 |
| 5.80 | Kd | 1600 | nM | SORAFENIB |
| 5.75 | Kd | 1780 | nM | CHEMBL4084193 |
| 5.72 | Kd | 1900 | nM | KW-2449 |
| 5.72 | Kd | 1900 | nM | CHEMBL379218 |
| 5.66 | IC50 | 2200 | nM | INDIRUBIN |
| 5.54 | Kd | 2880 | nM | SUNITINIB |
| 5.52 | Kd | 3000 | nM | DOVITINIB |
PubChem BioAssay actives
56 with measured affinity, of 546 total; 39 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 4-[(2,6-dichlorobenzoyl)amino]-N-piperidin-4-yl-1H-pyrazole-5-carboxamide | 624776: Binding constant for PCTK2 kinase domain | kd | 0.0009 | uM |
| [4-amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl]-(2,3-difluoro-6-methoxyphenyl)methanone | 624776: Binding constant for PCTK2 kinase domain | kd | 0.0009 | uM |
| N-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-4-carboxamide | 1424942: 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 | 0.0020 | uM |
| 4-N-(5-cyclopropyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-N-[(3-propan-2-yl-1,2-oxazol-5-yl)methyl]pyrimidine-2,4-diamine | 1424942: 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 | 0.0050 | uM |
| 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one | 1424942: 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 | 0.0060 | uM |
| 4-[4-[(3-tert-butyl-1-quinolin-6-ylpyrazol-5-yl)carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide | 1424942: 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 | 0.0070 | uM |
| 4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine | 1424942: 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 | 0.0070 | 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 | 1715415: Inhibition of human CDK17/cyclin-Y using MBP protein as substrate by [gamma-33P]-ATP assay | ic50 | 0.0107 | uM |
| N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-1,4-dihydropyrrolo[3,4-d]pyrazole-5-carboxamide | 1424942: 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 | 0.0140 | uM |
| 1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea | 435688: Binding constant for full-length PCTK2 | kd | 0.0150 | uM |
| Dabrafenib | 1424942: 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 | 0.0360 | uM |
| 3-[3-(2,3-dihydroxypropylamino)phenyl]-4-(5-fluoro-1-methylindol-3-yl)pyrrole-2,5-dione | 465268: Inhibition of PCTK2 | kd | 0.0690 | uM |
| N-methyl-N-[3-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]methanesulfonamide | 1424942: 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 | 0.0890 | uM |
| methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate | 624776: Binding constant for PCTK2 kinase domain | kd | 0.0930 | uM |
| 4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | 2148046: Binding affinity to human CDK17 incubated for 45 mins by Kinobead based pull down assay | kd | 0.1205 | uM |
| (2R)-2-methyl-2-[[2-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl]amino]-N-(2,2,2-trifluoroethyl)butanamide | 1424942: 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 | 0.1390 | uM |
| 1-N’-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | 624776: Binding constant for PCTK2 kinase domain | kd | 0.1700 | uM |
| 4-[[5-amino-1-(2,6-difluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide | 435688: Binding constant for full-length PCTK2 | kd | 0.2900 | uM |
| 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 | 624776: Binding constant for PCTK2 kinase domain | kd | 0.3300 | uM |
| Ponatinib | 1424942: 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 | 0.3350 | uM |
| Fedratinib | 624776: Binding constant for PCTK2 kinase domain | kd | 0.3500 | uM |
| 1-[3-tert-butyl-1-(4-methylphenyl)pyrazol-5-yl]-3-[[5-fluoro-2-[1-(2-hydroxyethyl)indazol-5-yl]oxyphenyl]methyl]urea | 1424942: 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 | 0.4020 | uM |
| regorafenib anhydrous | 1424942: 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 | 0.7190 | 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 | 507663: Binding affinity to PCTK2 | kd | 0.7200 | 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 | 1424942: 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 | 0.7780 | uM |
| 5-chloro-2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine | 624776: Binding constant for PCTK2 kinase domain | kd | 0.8100 | uM |
| (3Z)-5-[(2,6-dichlorophenyl)methylsulfonyl]-3-[[3,5-dimethyl-4-[(2R)-2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl]-1H-pyrrol-2-yl]methylidene]-1H-indol-2-one | 624776: Binding constant for PCTK2 kinase domain | kd | 0.8800 | uM |
| 1-cyclopropyl-3-[5-[6-(morpholin-4-ylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]urea | 1424942: 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 | 1.1480 | uM |
| N,1,4,4-tetramethyl-8-[4-(4-methylpiperazin-1-yl)anilino]-5H-pyrazolo[4,5-h]quinazoline-3-carboxamide | 1424942: 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 | 1.1770 | uM |
| Sunitinib | 435688: Binding constant for full-length PCTK2 | kd | 1.2000 | uM |
| Palbociclib | 1424942: 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 | 1.2720 | uM |
| Momelotinib | 1424942: 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 | 1.3820 | uM |
| 4-[[[6-[5-chloro-2-[[4-[[(2R)-1-methoxypropan-2-yl]amino]cyclohexyl]amino]-4-pyridinyl]-2-pyridinyl]amino]methyl]oxane-4-carbonitrile | 1921485: Inhibition of CDK17 (unknown origin) by Kinomescan method | ic50 | 1.5000 | uM |
| Sorafenib | 435688: Binding constant for full-length PCTK2 | kd | 1.6000 | uM |
| (2S)-1-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]-3-phenylpropan-2-amine | 624776: Binding constant for PCTK2 kinase domain | kd | 1.9000 | uM |
| [4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone | 624776: Binding constant for PCTK2 kinase domain | kd | 1.9000 | uM |
| 2-(2-hydroxy-1H-indol-3-yl)indol-3-one | 1378312: Inhibition of recombinant human CDK expressed in baculovirus infected sf9 cells after 10 mins by SDS-PAGE based autoradiography | ic50 | 2.2000 | uM |
| 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one | 435688: Binding constant for full-length PCTK2 | kd | 3.0000 | uM |
| N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide | 624776: Binding constant for PCTK2 kinase domain | kd | 5.6000 | uM |
CTD chemical–gene interactions
32 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| cobaltous chloride | decreases expression, increases expression | 2 |
| Tetrachlorodibenzodioxin | decreases expression | 2 |
| Sodium Selenite | decreases expression, increases expression | 2 |
| aristolochic acid I | decreases expression | 1 |
| FR900359 | decreases phosphorylation | 1 |
| arsenite | affects binding, decreases reaction | 1 |
| sodium arsenite | increases expression | 1 |
| potassium chromate(VI) | affects cotreatment, decreases expression | 1 |
| 2,3-bis(3’-hydroxybenzyl)butyrolactone | affects cotreatment, decreases expression | 1 |
| aflatoxin B2 | decreases methylation | 1 |
| 1-nitropyrene | increases expression | 1 |
| epigallocatechin gallate | affects cotreatment, decreases expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| chromium hexavalent ion | decreases expression | 1 |
| abrine | increases expression | 1 |
| jinfukang | decreases expression | 1 |
| Leflunomide | increases expression | 1 |
| Amiodarone | increases expression | 1 |
| Benzo(a)pyrene | affects methylation | 1 |
| Caffeine | decreases phosphorylation | 1 |
| Coumestrol | affects cotreatment, decreases expression | 1 |
| Potassium Dichromate | decreases expression | 1 |
| Rotenone | decreases expression | 1 |
| Tobacco Smoke Pollution | increases expression | 1 |
| Urethane | increases expression | 1 |
| Valproic Acid | affects expression | 1 |
| Vanadium | decreases expression | 1 |
| 7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide | decreases expression | 1 |
| Cadmium Chloride | increases expression | 1 |
| Copper Sulfate | increases expression | 1 |
ChEMBL screening assays
182 unique, capped per target: 182 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1064257 | Binding | Inhibition of CDK in human A2780 cells assessed as reduction of RNAP2 phosphorylation at Ser2 site at 5 uM after 6 hrs by Western bloting | Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5-dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors. — J Med Chem |
Cellosaurus cell lines
3 cell lines: 3 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B1N0 | Abcam HeLa CDK17 KO | Cancer cell line | Female |
| CVCL_SI26 | HAP1 CDK17 (-) 1 | Cancer cell line | Male |
| CVCL_SI27 | HAP1 CDK17 (-) 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
11 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT03414970 | PHASE3 | ACTIVE_NOT_RECRUITING | Hypofractionated Radiation Therapy After Mastectomy in Preventing Recurrence in Patients With Stage IIa-IIIa Breast Cancer |
| NCT00461344 | PHASE2 | TERMINATED | Docetaxel + Doxorubicin as Neoadjuvant Chemotherapy in Patients With Breast Cancer |
| NCT07499999 | PHASE2 | NOT_YET_RECRUITING | Randomized Double-Blind Phase II Trial of Baby Exemestane Versus Baby Tamoxifen in Post-Menopausal Women at High Risk for Breast Cancer |
| NCT00637364 | PHASE1/PHASE2 | SUSPENDED | High Intensity Focused Ultrasound Tumor Treatment for Pancreatic Cancer Pain |
| NCT02779855 | PHASE1/PHASE2 | COMPLETED | Talimogene Laherparepvec in Combination With Neoadjuvant Chemotherapy in Triple Negative Breast Cancer |
| NCT01753908 | EARLY_PHASE1 | COMPLETED | Broccoli Sprout Extract in Treating Patients With Breast Cancer |
| NCT01796041 | EARLY_PHASE1 | COMPLETED | Intraoperative Imaging of Breast Cancer With Indocyanine Green |
| NCT01208974 | Not specified | ACTIVE_NOT_RECRUITING | Nipple-Areola Complex (NAC) Irradiation After Nipple-Sparing Mastectomy and Reconstruction |
| NCT01875198 | Not specified | TERMINATED | Oncologic Impact of Splenectomy-omitting Radical Pancreatectomy in Well-selected Left-sided Pancreatic Cancer |
| NCT03543397 | Not specified | UNKNOWN | MRI in Ductal Carcinoma in Situ (DCIS) |
| NCT03834532 | Not specified | COMPLETED | Living Well After Breast Surgery |
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.