TSSK3
gene geneOn this page
Also known as SPOGA3
Summary
TSSK3 (testis specific serine kinase 3, HGNC:15473) is a protein-coding gene on chromosome 1p35.1, encoding Testis-specific serine/threonine-protein kinase 3 (Q96PN8). Serine/threonine protein kinase required for spermatid development and male fertility.
This gene encodes a kinase expressed exclusively in the testis that is thought to play a role in either germ cell differentiation or mature sperm function.
Source: NCBI Gene 81629 — RefSeq curated summary.
At a glance
- GWAS associations: 1
- Clinical variants (ClinVar): 49 total
- Druggable target: yes — 1 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_052841
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:15473 |
| Approved symbol | TSSK3 |
| Name | testis specific serine kinase 3 |
| Location | 1p35.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | SPOGA3 |
| Ensembl gene | ENSG00000162526 |
| Ensembl biotype | protein_coding |
| OMIM | 607660 |
| Entrez | 81629 |
Gene structure
Transcript identifiers
Ensembl transcripts: 4 — 2 protein_coding, 2 protein_coding_CDS_not_defined
ENST00000373534, ENST00000421153, ENST00000574315, ENST00000574792
RefSeq mRNA: 1 — MANE Select: NM_052841
NM_052841
CCDS: CCDS362
Canonical transcript exons
ENST00000373534 — 2 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001460783 | 32363595 | 32364312 |
| ENSE00001460785 | 32362539 | 32362846 |
Expression profiles
Bgee: expression breadth ubiquitous, 159 present calls, max score 94.69.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 2.6814 / max 113.6734, expressed in 1112 samples.
FANTOM5 promoters (4 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 1984 | 1.3580 | 764 |
| 1985 | 1.2438 | 671 |
| 1987 | 0.0662 | 6 |
| 1986 | 0.0134 | 3 |
Top tissues by expression
245 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| sperm | CL:0000019 | 94.69 | gold quality |
| right testis | UBERON:0004534 | 92.39 | gold quality |
| left testis | UBERON:0004533 | 92.15 | gold quality |
| testis | UBERON:0000473 | 89.23 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 87.67 | gold quality |
| right ovary | UBERON:0002118 | 79.68 | gold quality |
| left ovary | UBERON:0002119 | 79.16 | gold quality |
| sural nerve | UBERON:0015488 | 78.87 | gold quality |
| stromal cell of endometrium | CL:0002255 | 78.52 | gold quality |
| right uterine tube | UBERON:0001302 | 78.50 | gold quality |
| vena cava | UBERON:0004087 | 78.36 | gold quality |
| body of uterus | UBERON:0009853 | 78.27 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 78.15 | gold quality |
| cerebellar cortex | UBERON:0002129 | 78.08 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 77.95 | gold quality |
| mucosa of stomach | UBERON:0001199 | 77.83 | gold quality |
| subthalamic nucleus | UBERON:0001906 | 77.58 | gold quality |
| left uterine tube | UBERON:0001303 | 77.50 | gold quality |
| endocervix | UBERON:0000458 | 77.43 | gold quality |
| cerebellum | UBERON:0002037 | 77.34 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 77.32 | gold quality |
| apex of heart | UBERON:0002098 | 76.60 | gold quality |
| right lung | UBERON:0002167 | 76.54 | gold quality |
| granulocyte | CL:0000094 | 76.47 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 76.44 | gold quality |
| epithelium of nasopharynx | UBERON:0001951 | 76.07 | gold quality |
| thyroid gland | UBERON:0002046 | 75.99 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 75.75 | gold quality |
| dorsal plus ventral thalamus | UBERON:0001897 | 75.74 | gold quality |
| gastrocnemius | UBERON:0001388 | 75.65 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 1.07 |
Regulation
Is transcription factor: no
Literature-anchored findings (GeneRIF, showing 3)
- human homolog of mouse stk22d; It was cloned and found it to be expressed exclusively in the testis. (PMID:11597141)
- PDK1-induced phosphorylation increased in vitro TSSK3 kinase activity, suggesting that TSSK3 can be regulated in the same way as AGC kinase family members. The peptide sequence RRSSSY containing Ser5 is identified as a target for TSSK3 phosphorylation (PMID:16336268)
- TSSK3, a novel target for male contraception, is required for spermiogenesis. (PMID:34623009)
Cross-species orthologs
9 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | nim1kb | ENSDARG00000079031 |
| mus_musculus | Tssk3 | ENSMUSG00000000411 |
| rattus_norvegicus | Tssk3 | ENSRNOG00000008693 |
| drosophila_melanogaster | Snrk | FBGN0033915 |
| drosophila_melanogaster | Nuak | FBGN0262617 |
| caenorhabditis_elegans | WBGENE00012638 | |
| caenorhabditis_elegans | ZK524.4 | WBGENE00013994 |
| caenorhabditis_elegans | tag-344 | WBGENE00015230 |
| caenorhabditis_elegans | WBGENE00044388 |
Paralogs (17): NUAK1 (ENSG00000074590), PRKAA1 (ENSG00000132356), TSSK4 (ENSG00000139908), HUNK (ENSG00000142149), SIK1 (ENSG00000142178), BRSK1 (ENSG00000160469), SIK3 (ENSG00000160584), PRKAA2 (ENSG00000162409), NUAK2 (ENSG00000163545), SNRK (ENSG00000163788), MELK (ENSG00000165304), SIK2 (ENSG00000170145), BRSK2 (ENSG00000174672), NIM1K (ENSG00000177453), TSSK6 (ENSG00000178093), TSSK2 (ENSG00000206203), TSSK1B (ENSG00000212122)
Protein
Protein identifiers
Testis-specific serine/threonine-protein kinase 3 — Q96PN8 (reviewed: Q96PN8)
Alternative names: Serine/threonine-protein kinase 22C
All UniProt accessions (2): Q96PN8, I3L1X4
UniProt curated annotations — full annotation on UniProt →
Function. Serine/threonine protein kinase required for spermatid development and male fertility.
Subcellular location. Cell projection. Cilium. Flagellum.
Post-translational modifications. Autophosphorylated at Ser-166. Phosphorylation at Thr-168 by PDPK1 activates the serine/threonine protein kinase activity.
Activity regulation. Activated by phosphorylation on Thr-168 by PDPK1.
Cofactor. Can use both Mg(2+) and Mn(2+) as cofactor, with a preference for Mn(2+) in vitro.
Similarity. Belongs to the protein kinase superfamily. CAMK Ser/Thr protein kinase family.
RefSeq proteins (1): NP_443073* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000719 | Prot_kinase_dom | Domain |
| IPR011009 | Kinase-like_dom_sf | Homologous_superfamily |
| IPR017441 | Protein_kinase_ATP_BS | Binding_site |
| IPR042709 | TSSK3_STKc | Domain |
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 (10 total): sequence variant 3, binding site 2, modified residue 2, chain 1, domain 1, active site 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q96PN8-F1 | 93.65 | 0.83 |
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): 134 (proton acceptor)
Ligand- & substrate-binding residues (2): 16–24; 39
Post-translational modifications (2): 166, 168
Function
Pathways and Gene Ontology
Reactome pathways
0 pathways
MSigDB gene sets: 106 (showing top):
AAGCAAT_MIR137, MAZ_Q6, TGACCTY_ERR1_Q2, GOBP_MALE_GAMETE_GENERATION, AAAYRNCTG_UNKNOWN, GATA1_01, GRE_C, GOBP_CELLULAR_PROCESS_INVOLVED_IN_REPRODUCTION_IN_MULTICELLULAR_ORGANISM, HIF1_Q3, GOBP_DEVELOPMENTAL_PROCESS_INVOLVED_IN_REPRODUCTION, CDPCR3HD_01, YY1_01, DBP_Q6, AP2_Q6_01, AP2GAMMA_01
GO Biological Process (4): protein phosphorylation (GO:0006468), spermatogenesis (GO:0007283), spermatid development (GO:0007286), cell differentiation (GO:0030154)
GO Molecular Function (11): magnesium ion binding (GO:0000287), protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), manganese ion binding (GO:0030145), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740), metal ion binding (GO:0046872)
GO Cellular Component (4): sperm flagellum (GO:0036126), cilium (GO:0005929), 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 |
| developmental process involved in reproduction | 1 |
| male gamete generation | 1 |
| germ cell development | 1 |
| spermatid differentiation | 1 |
| cellular developmental process | 1 |
| metal ion binding | 1 |
| adenyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| transition metal ion binding | 1 |
| nucleoside phosphate binding | 1 |
| heterocyclic compound binding | 1 |
| kinase activity | 1 |
| phosphotransferase activity, alcohol group as acceptor | 1 |
| catalytic activity, acting on a protein | 1 |
| binding | 1 |
| transferase activity, transferring phosphorus-containing groups | 1 |
| catalytic activity | 1 |
| cation binding | 1 |
| 9+2 motile cilium | 1 |
| intraciliary transport particle | 1 |
| membrane-bounded organelle | 1 |
| plasma membrane bounded cell projection | 1 |
| cilium | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
1581 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| TSSK3 | TSKS | Q9UJT2 | 720 |
| TSSK3 | CALY | Q9NYX4 | 594 |
| TSSK3 | KLHL10 | Q6JEL2 | 514 |
| TSSK3 | CRABP1 | P29762 | 454 |
| TSSK3 | SIGLEC1 | Q9BZZ2 | 452 |
| TSSK3 | SSMEM1 | Q8WWF3 | 417 |
| TSSK3 | TNP1 | P09430 | 401 |
| TSSK3 | IZUMO1 | Q8IYV9 | 397 |
| TSSK3 | FAM170B | A6NMN3 | 392 |
| TSSK3 | TXNDC2 | Q86VQ3 | 383 |
| TSSK3 | SPATC1 | Q76KD6 | 382 |
| TSSK3 | CCDC70 | Q6NSX1 | 380 |
| TSSK3 | PRM2 | P04554 | 364 |
| TSSK3 | SOX30 | O94993 | 354 |
| TSSK3 | TCP11 | Q8WWU5 | 351 |
IntAct
216 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| TSSK3 | LNX1 | psi-mi:“MI:0915”(physical association) | 0.780 |
| LNX1 | TSSK3 | psi-mi:“MI:0915”(physical association) | 0.780 |
| GOLGA2 | TSSK3 | psi-mi:“MI:0915”(physical association) | 0.720 |
| EFHC2 | TSSK3 | psi-mi:“MI:0915”(physical association) | 0.720 |
| TSSK3 | VPS52 | psi-mi:“MI:0915”(physical association) | 0.720 |
| TSSK3 | RBCK1 | psi-mi:“MI:0915”(physical association) | 0.720 |
| IKZF3 | TSSK3 | psi-mi:“MI:0915”(physical association) | 0.720 |
| TSSK3 | GOLGA2 | psi-mi:“MI:0915”(physical association) | 0.720 |
| TSSK3 | EFHC2 | psi-mi:“MI:0915”(physical association) | 0.720 |
| VPS52 | TSSK3 | psi-mi:“MI:0915”(physical association) | 0.720 |
| TSSK3 | IKZF3 | psi-mi:“MI:0915”(physical association) | 0.720 |
| DDIT4L | TSSK3 | psi-mi:“MI:0915”(physical association) | 0.600 |
| TCF4 | TSSK3 | psi-mi:“MI:0915”(physical association) | 0.560 |
| TSSK3 | ZBTB25 | psi-mi:“MI:0915”(physical association) | 0.560 |
| TSSK3 | REL | psi-mi:“MI:0915”(physical association) | 0.560 |
| TLE5 | TSSK3 | psi-mi:“MI:0915”(physical association) | 0.560 |
BioGRID (88): TSSK3 (Two-hybrid), TSSK3 (Two-hybrid), TSSK3 (Two-hybrid), TSSK3 (Two-hybrid), TSSK3 (Two-hybrid), TSSK3 (Two-hybrid), TSSK3 (Two-hybrid), TSSK3 (Two-hybrid), TSSK3 (Two-hybrid), TSSK3 (Two-hybrid), LNX1 (Two-hybrid), TRIM9 (Two-hybrid), TSSK3 (Two-hybrid), TSSK3 (Two-hybrid), TSSK3 (Biochemical Activity)
ESM2 similar proteins: A0A5B9GBF0, A1IVT7, A3B529, B2MVY4, O65554, O70150, O70444, P05128, P11802, P23111, P27638, P29618, P30285, P34112, P35426, P48609, P52389, P58750, P79432, P93101, Q05006, Q0U4L8, Q15759, Q1DUU8, Q2PQN9, Q2U469, Q32KY4, Q38772, Q38HL5, Q41639, Q5JLD8, Q683C9, Q69Q47, Q6ERS4, Q6P2M8, Q6SA08, Q80YP0, Q86V86, Q8C1R0, Q8TGA9
Diamond homologs: A2XFF4, A3B529, A8WYE4, B8BBT7, O08678, O08679, O22932, O22971, O54863, O60285, O65554, O94168, P06782, P27448, P54645, P57059, P92937, P92958, Q00372, Q02723, Q03141, Q05512, Q0D4B2, Q0JI49, Q10LQ2, Q12263, Q13131, Q21017, Q28GW8, Q2QY53, Q2QYM3, Q2RAX3, Q2RBF0, Q38997, Q3SZW1, Q54DF2, Q54TA3, Q54YF2, Q5EG47, Q5JLD8
SIGNOR signaling
2 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| TSSK3 | “up-regulates activity” | TSSK3 | phosphorylation |
| PDPK1 | “up-regulates activity” | TSSK3 | phosphorylation |
Disease & clinical
Clinical variants and AI predictions
ClinVar
49 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 46 |
| Likely benign | 0 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
435 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 1:32362417:GGC:G | donor_gain | 1.0000 |
| 1:32361725:CTTA:C | donor_loss | 0.9900 |
| 1:32361726:TTACC:T | donor_loss | 0.9900 |
| 1:32361727:TACC:T | donor_loss | 0.9900 |
| 1:32361728:A:T | donor_loss | 0.9900 |
| 1:32361729:C:CA | donor_loss | 0.9900 |
| 1:32362418:GC:G | donor_gain | 0.9900 |
| 1:32362419:C:G | donor_gain | 0.9900 |
| 1:32363585:A:AG | acceptor_gain | 0.9900 |
| 1:32363591:TCAG:T | acceptor_gain | 0.9900 |
| 1:32363593:A:AC | acceptor_loss | 0.9900 |
| 1:32363593:A:AG | acceptor_gain | 0.9900 |
| 1:32363594:G:GG | acceptor_gain | 0.9900 |
| 1:32363594:G:T | acceptor_loss | 0.9900 |
| 1:32363594:GA:G | acceptor_gain | 0.9900 |
| 1:32363594:GAGT:G | acceptor_gain | 0.9900 |
| 1:32361729:CCTGA:C | donor_gain | 0.9800 |
| 1:32361731:TG:T | donor_gain | 0.9800 |
| 1:32362416:GGGC:G | donor_gain | 0.9800 |
| 1:32362430:G:GA | donor_gain | 0.9800 |
| 1:32362433:G:GA | donor_gain | 0.9800 |
| 1:32362435:T:TA | donor_gain | 0.9800 |
| 1:32362436:A:AA | donor_gain | 0.9800 |
| 1:32363591:TCAGA:T | acceptor_gain | 0.9800 |
| 1:32363592:CAG:C | acceptor_gain | 0.9800 |
| 1:32363592:CAGAG:C | acceptor_gain | 0.9800 |
| 1:32363593:AGA:A | acceptor_gain | 0.9800 |
| 1:32363594:GAG:G | acceptor_gain | 0.9800 |
| 1:32363594:GAGTT:G | acceptor_gain | 0.9800 |
| 1:32361728:A:AC | donor_gain | 0.9700 |
AlphaMissense
1772 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 1:32362818:A:C | K39N | 0.999 |
| 1:32362818:A:T | K39N | 0.999 |
| 1:32363847:G:C | R133P | 0.998 |
| 1:32363850:A:C | D134A | 0.998 |
| 1:32363850:A:T | D134V | 0.998 |
| 1:32363901:A:T | D151V | 0.998 |
| 1:32363902:C:A | D151E | 0.998 |
| 1:32363902:C:G | D151E | 0.998 |
| 1:32364077:T:C | F210L | 0.998 |
| 1:32364079:T:A | F210L | 0.998 |
| 1:32364079:T:G | F210L | 0.998 |
| 1:32363850:A:G | D134G | 0.997 |
| 1:32363851:C:A | D134E | 0.997 |
| 1:32363851:C:G | D134E | 0.997 |
| 1:32363857:A:C | K136N | 0.997 |
| 1:32363857:A:T | K136N | 0.997 |
| 1:32364029:T:A | W194R | 0.997 |
| 1:32364029:T:C | W194R | 0.997 |
| 1:32363609:T:C | F54L | 0.996 |
| 1:32363611:C:A | F54L | 0.996 |
| 1:32363611:C:G | F54L | 0.996 |
| 1:32363855:A:G | K136E | 0.996 |
| 1:32363856:A:T | K136I | 0.996 |
| 1:32363901:A:C | D151A | 0.996 |
| 1:32363963:A:C | S172R | 0.996 |
| 1:32363965:T:A | S172R | 0.996 |
| 1:32363965:T:G | S172R | 0.996 |
| 1:32362811:C:A | A37E | 0.995 |
| 1:32362816:A:G | K39E | 0.995 |
| 1:32363913:C:A | A155D | 0.995 |
dbSNP variants (sampled 300 via entrez): RS1000068694 (1:32362322 A>G), RS1000652777 (1:32361200 G>A), RS1000982482 (1:32360986 C>T), RS1001722336 (1:32360696 G>A), RS1002459355 (1:32361849 G>A), RS1002472014 (1:32360794 A>G), RS1003416754 (1:32364449 CCTT>C), RS1003728868 (1:32363037 C>A,G,T), RS1004007596 (1:32364338 T>C), RS1004249861 (1:32364560 C>T), RS1004800162 (1:32361860 C>T), RS1004872163 (1:32362080 G>A,C), RS1005879120 (1:32363011 G>A,T), RS1006441808 (1:32361803 A>C), RS1006569479 (1:32362698 C>A,T)
Disease associations
OMIM: gene MIM:607660 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
1 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST008758_22 | Pre-treatment viral load in HIV-1 infection | 4.000000e-16 |
EFO canonical traits (1, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0010125 | viral load |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL3414416 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,538 (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 |
|---|---|---|---|
| CHEMBL1232461 | MOLIBRESIB | 2 | 1,538 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — Testis specific kinase (TSSK) family
ChEMBL bioactivities
10 potent at pChembl≥5 of 10 total, top 10 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.49 | IC50 | 3.21 | nM | STAUROSPORINE |
| 8.15 | IC50 | 7.01 | nM | STAUROSPORINE |
| 7.83 | IC50 | 14.9 | nM | STAUROSPORINE |
| 7.04 | IC50 | 91 | nM | CHEMBL2334586 |
| 6.48 | Kd | 330 | nM | CHEMBL4576489 |
| 6.42 | Kd | 380 | nM | CHEMBL4465866 |
| 6.38 | IC50 | 420 | nM | CHEMBL3415608 |
| 6.38 | IC50 | 420 | nM | CHEMBL3943181 |
| 6.00 | IC50 | 1000 | nM | TP-030n |
| 5.00 | IC50 | 1e+04 | nM | MOLIBRESIB |
PubChem BioAssay actives
9 with measured affinity, of 67 total; 7 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 |
|---|---|---|---|---|
| (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 | 1715136: Inhibition of human TSSK3 using KKKVSRSGLYRSPSMPENLNRPR as substrate by [gamma-33P]-ATP assay | ic50 | 0.0032 | uM |
| 4-(4-amino-3,5,12-triazatetracyclo[9.7.0.02,7.013,18]octadeca-1(11),2,4,6,13(18),14,16-heptaen-16-yl)-2-methylbut-3-yn-2-ol | 1856574: Inhibition of wild-type human full length TSSK3 (M1 to T268 residues) expressed in mammalian expression system by Kinomescan method | ic50 | 0.0910 | uM |
| 3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-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-4-yl]-methylamino]ethoxy]ethoxy]ethoxy]ethyl]propanamide | 1526261: Binding affinity to recombinant full-length N-terminal His-FLAG-GST-tagged TSSK3 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay | kd | 0.3300 | uM |
| 3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-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-4-yl]amino]ethoxy]ethoxy]ethoxy]ethyl]propanamide | 1526261: Binding affinity to recombinant full-length N-terminal His-FLAG-GST-tagged TSSK3 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay | kd | 0.3800 | uM |
| 5-[[(1R,2S)-2-aminocyclohexyl]amino]-3-(1H-benzimidazol-2-yl)pyridine-2-carboxamide | 1199576: Inhibition of TSSK3 (unknown origin) | ic50 | 0.4200 | uM |
| 5-[[(1R,2S)-2-aminocyclohexyl]amino]-3-(1H-benzimidazol-2-yl)pyrazine-2-carboxamide | 1326206: Inhibition of TSSK3 (unknown origin) | ic50 | 0.4200 | uM |
| 2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide | 2178641: Inhibition of TSSK3 (unknown origin) incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysis | ic50 | 10.0000 | uM |
CTD chemical–gene interactions
11 total (human), top 11 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| aminomethylphosphonic acid (AMPA) | decreases expression | 1 |
| tris(1,3-dichloro-2-propyl)phosphate | increases expression | 1 |
| jinfukang | increases expression, affects cotreatment | 1 |
| Air Pollutants | increases expression, increases abundance | 1 |
| Cisplatin | affects cotreatment, increases expression | 1 |
| Estradiol | decreases expression | 1 |
| Folic Acid | increases expression | 1 |
| Valproic Acid | increases methylation | 1 |
| 2,4-Dichlorophenoxyacetic Acid | decreases expression | 1 |
| Okadaic Acid | decreases expression | 1 |
| Particulate Matter | increases abundance, increases expression | 1 |
ChEMBL screening assays
83 unique, capped per target: 83 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL3418524 | Binding | Inhibition of TSSK3 (unknown origin) | Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors. — J Med Chem |
Cellosaurus cell lines
2 cell lines: 2 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B2JV | Abcam HeLa TSSK3 KO | Cancer cell line | Female |
| CVCL_TV00 | HAP1 TSSK3 (-) | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.