◎ Sugi Atlas

Atlas / Gene / KIFC1

KIFC1

gene
On this page

Also known as HSET

Summary

KIFC1 (kinesin family member C1, HGNC:6389) is a protein-coding gene on chromosome 6p21.32, encoding Kinesin-like protein KIFC1 (Q9BW19). Minus end-directed microtubule-dependent motor required for bipolar spindle formation.

Predicted to enable ATP hydrolysis activity; microtubule binding activity; and minus-end-directed microtubule motor activity. Involved in mitotic metaphase chromosome alignment and mitotic spindle assembly. Located in membrane.

Source: NCBI Gene 3833 — RefSeq curated summary.

At a glance

  • GWAS associations: 7
  • Clinical variants (ClinVar): 119 total — 1 likely-pathogenic
  • Druggable target: yes — 1 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_002263

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:6389
Approved symbolKIFC1
Namekinesin family member C1
Location6p21.32
Locus typegene with protein product
StatusApproved
AliasesHSET
Ensembl geneENSG00000237649
Ensembl biotypeprotein_coding
OMIM603763
Entrez3833

Gene structure

Transcript identifiers

Ensembl transcripts: 12 — 11 protein_coding, 1 retained_intron

ENST00000428849, ENST00000450504, ENST00000486695, ENST00000494554, ENST00000895636, ENST00000895637, ENST00000927217, ENST00000927218, ENST00000927219, ENST00000927220, ENST00000927221, ENST00000927222

RefSeq mRNA: 1 — MANE Select: NM_002263 NM_002263

CCDS: CCDS34430

Canonical transcript exons

ENST00000374523 — 0 exons

Expression profiles

Bgee: expression breadth ubiquitous, 133 present calls, max score 97.53.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 26.5573 / max 325.2660, expressed in 1482 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter IDTPM avgSamples expressed
6728226.55731482

Top tissues by expression

134 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
ventricular zoneUBERON:000305397.53gold quality
ganglionic eminenceUBERON:000402394.95gold quality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099186.80gold quality
bone marrowUBERON:000237186.54gold quality
mucosa of transverse colonUBERON:000499184.88gold quality
lymph nodeUBERON:000002983.96gold quality
vermiform appendixUBERON:000115483.30gold quality
stromal cell of endometriumCL:000225582.86gold quality
bone marrow cellCL:000209282.24gold quality
right testisUBERON:000453481.94gold quality
esophagus mucosaUBERON:000246981.33gold quality
lower esophagus mucosaUBERON:003583481.32gold quality
left testisUBERON:000453381.18gold quality
testisUBERON:000047380.95gold quality
duodenumUBERON:000211480.13gold quality
placentaUBERON:000198779.93gold quality
rectumUBERON:000105279.79gold quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047378.26gold quality
tonsilUBERON:000237273.37gold quality
smooth muscle tissueUBERON:000113573.14gold quality
skin of abdomenUBERON:000141672.38gold quality
adrenal tissueUBERON:001830372.25gold quality
spleenUBERON:000210672.13gold quality
transverse colonUBERON:000115772.04gold quality
zone of skinUBERON:000001471.88gold quality
skin of legUBERON:000151171.34gold quality
endometriumUBERON:000129571.09gold quality
small intestineUBERON:000210870.94gold quality
small intestine Peyer’s patchUBERON:000345470.70gold quality
vaginaUBERON:000099667.94gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

ExperimentMarker?Max mean expression
E-ANND-3no1.96

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

10 targeting KIFC1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-8485100.0077.574731
HSA-MIR-548AA99.9670.643753
HSA-MIR-548AP-3P99.9670.643753
HSA-MIR-548T-3P99.9670.643753
HSA-MIR-26A-1-3P99.6466.81788
HSA-MIR-26A-2-3P99.6466.82786
HSA-MIR-429098.5165.17907
HSA-MIR-376C-3P97.6368.881263
HSA-MIR-63596.0065.54687
HSA-MIR-6774-5P95.9465.18722

Literature-anchored findings (GeneRIF, showing 40)

  • An analysis was made of the weak interactions of ADP-Unc104 and ADP-kinesin with microtubules and their inhibition by MAP2. (PMID:17326138)
  • HSET has a role in controlling spindle length by cross-linking and sliding microtubules. (PMID:19116309)
  • High KIFC1 expression is associated with metastatic spread to the brain in primary non-small cell lung cancer. (PMID:19190132)
  • Chromosome congression in HSET + hNuf2 co-depleted cells required the plus-end directed motor CENP-E , which has been implicated in the gliding of mono-oriented kinetochores alongside adjacent K-fibres. (PMID:19525938)
  • The intense placental expression of KIFC1 in syncytiotrophoblast and KIF17 in vascular endothelium suggests that both proteins might be important in a cargo-transport system. KIFC1 and KIF17 expression are increased of both in preeclamptia and diabetes. (PMID:19679349)
  • A case-control analysis was carried out by comparing the genotype distribution of six KIFC1 single-nucleotide polymorphisms between 93 aspirin exacerbated respiratory disease cases and 96 aspirin-tolerant asthma controls in a Korean population (PMID:22201025)
  • Acentrosomal spindle assembly mechanisms are hyperactive in cancer cells and promote HSET. (PMID:22946058)
  • we suggest that KIFC1 plays an essential role for bipolar MTOC formation and maintaining chromosomal stability in the mitosis . (PMID:23318213)
  • Study demonstrates microtubule tip-tracking of human kinesin-14 HSET and show that EB1 is sufficient to induce this dynamic microtubule end localization. (PMID:24039245)
  • We show that some are new substrates of the anaphase-promoting complex/cyclosome and validate KIFC1 and RacGAP1/Cyk4 as two such targets involved respectively in timely mitotic spindle disassembly and cell spreading (PMID:24857844)
  • Our data underscore KIFC1 as a putative biomarker that predicts worse prognosis, poor overall survival and may serve as a potential marker of onset of metastatic dissemination in ovarian cancer patients. (PMID:25028599)
  • Data provides the first evidence of centrosome clustering-independent activities of HSET that fuel tumor progression. (PMID:25788277)
  • KIFC1 silencing significantly reduces breast cancer cell viability. (PMID:26177331)
  • stabilization of the centrosome-spindle pole interface by the CEP215-HSET complex could promote survival of cancer cells containing supernumerary centrosomes. (PMID:26987684)
  • Association of KIFC1 gene expression and centrosome amplification with high-grade serous ovarian carcinoma. (PMID:26992853)
  • KIFC1 is overexpressed in GC. (PMID:27176706)
  • Taken together, these results suggest that up-regulation of KIFC1 may induce docetaxel resistance. (PMID:27665358)
  • Low post translational modifications of KIFC1 protein is associated with neoplasms. (PMID:28209915)
  • nuclear KIFC1 (nKIFC1) correlated significantly with Ki67 in White triple-negative breast cancer (TNBCs) but not in African American (AA) TNBCs, suggesting that nKIFC1 is not merely a surrogate for proliferation in AA TNBCs. (PMID:28218233)
  • These findings reveal a new stationary binding model that kinesin-14 KIFC1 proteins function as crosslinkers between the Golgi apparatus and the microtubules and contribute to the central positioning and structural maintenance of the Golgi apparatus. (PMID:28430595)
  • Results identified Stathmin as a direct target of KIFC1. (PMID:28885720)
  • Circulating pri-miRNA-944 and 3662 can improve non-invasive potential non-small cell lung cancer detection of operable stages of SCC and AC (PMID:28964573)
  • The antiproliferative effect of KIFC1 silencing was also observed in xenografted tumors in vivo. miR-338-3p could directly bind to the 3’-untranslated region (3’-UTR) of KIFC1, and ectopic miR-338-3p expression mimicked the inhibitory functions of KIFC1 silencing on RCC cells through inactivation of the PI3K/AKT signaling pathway (PMID:29562961)
  • The overexpression of KIFC1 was correlated closely with the progression of hepatocellular carcinoma (HCC) and poor prognosis, and suggested that the expression levels of KIFC1 are a potential prognostic biomarker for HCC. (PMID:29620256)
  • Data show that kinesin-related protein HSET (HSET) is incapable of forming asters from preformed, nongrowing microtubule (non-MT) MTs, but rapidly forms MT asters in the presence of soluble (non-MT) tubulin. (PMID:29985404)
  • KIFC1 interacts with F508del-CFTR. (PMID:30066085)
  • Kifc1 deletion leads to defects in metaphase mitotic spindle assembly, and then results in chromosome structural abnormality. The kifc1(-/-) cells finally form micronuclei in daughter cells, and results in aneuploidy and chromosome loss in cell cycle. (PMID:31127080)
  • KIFC1 was significantly upregulated in bladder cancer (BC) specimens at both the mRNA and protein levels and associated with both shorter cancer-specific survival and recurrence-free survival time. Overexpression of KIFC1 in vitro phosphorylated GSK3beta and promoted Snail through activating AKT to induce proliferation and epithelial-mesenchymal transition and, therefore, substantially promoted BC migration and metasta… (PMID:31278883)
  • Our findings suggest that KIFC1, activated by TCF-4 (TCF7L2), functions as an oncogene and promotes hepatocellular carcinoma (HCC) pathogenesis through regulating HMGA1 transcriptional activity and that KIFC1 is a potential therapeutic target to enhance the paclitaxel sensitivity of HCC (PMID:31340839)
  • miR-635 targets KIFC1 to inhibit the progression of gastric cancer. (PMID:32753405)
  • Kinesin Family Member C1 (KIFC1) Accelerates Proliferation and Invasion of Endometrial Cancer Cells Through Modulating the PI3K/AKT Signaling Pathway. (PMID:33034273)
  • Kinesin Family Member C1 (KIFC1) Regulated by Centrosome Protein E (CENPE) Promotes Proliferation, Migration, and Epithelial-Mesenchymal Transition of Ovarian Cancer. (PMID:33361741)
  • The ATM and ATR kinases regulate centrosome clustering and tumor recurrence by targeting KIFC1 phosphorylation. (PMID:33397932)
  • High KIFC1 expression is associated with poor prognosis in prostate cancer. (PMID:33760984)
  • Increased expression levels of AURKA and KIFC1 are promising predictors of progression and poor survival associated with gastric cancer. (PMID:34148003)
  • Mechanism of spindle pole organization and instability in human oocytes. (PMID:35143306)
  • Kinesin Family Member C1 Overexpression Exerts Tumor-Promoting Properties in Head and Neck Squamous Cell Carcinoma via the Rac1/Wnt/beta-catenin Pathway. (PMID:36990154)
  • DNA methylation of KIFC1 gene in determination of histological diagnosis, prognosis and metastasis of lung cancer. (PMID:37666088)
  • Kinesin Family Member C1 (KIFC1/HSET) Underlies Aggressive Disease in Androgen Receptor-Low and Basal-Like Triple-Negative Breast Cancers. (PMID:38003261)
  • A comprehensive analysis of the prognostic and immunotherapeutic characteristics of KIFC1 in pan-cancer and its role in the malignant phenotype of pancreatic cancer. (PMID:38112634)

Cross-species orthologs

4 orthologs

OrganismSymbolGene ID
danio_reriokifc1ENSDARG00000001558
mus_musculusKifc5bENSMUSG00000024301
mus_musculusKifc1ENSMUSG00000079553
rattus_norvegicusKifc1ENSRNOG00000000479

Paralogs (41): KIF1B (ENSG00000054523), KIF26A (ENSG00000066735), KIF2A (ENSG00000068796), KIF22 (ENSG00000079616), KIF3C (ENSG00000084731), KIF9 (ENSG00000088727), KIF16B (ENSG00000089177), KIF4A (ENSG00000090889), KIF3B (ENSG00000101350), KIF20A (ENSG00000112984), KIF21B (ENSG00000116852), KIF17 (ENSG00000117245), KIF14 (ENSG00000118193), KIF18A (ENSG00000121621), KIF25 (ENSG00000125337), KIF1C (ENSG00000129250), KIF1A (ENSG00000130294), KIF3A (ENSG00000131437), KIF12 (ENSG00000136883), KIF13A (ENSG00000137177), KIF23 (ENSG00000137807), KIF11 (ENSG00000138160), CENPE (ENSG00000138778), KIF21A (ENSG00000139116), KIFC3 (ENSG00000140859), KIF2B (ENSG00000141200), KIF2C (ENSG00000142945), KIF5A (ENSG00000155980), KIF26B (ENSG00000162849), KIF15 (ENSG00000163808), KIF6 (ENSG00000164627), KIF27 (ENSG00000165115), KIF7 (ENSG00000166813), KIFC2 (ENSG00000167702), KIF5C (ENSG00000168280), KIF5B (ENSG00000170759), KIF18B (ENSG00000186185), KIF24 (ENSG00000186638), KIF19 (ENSG00000196169), KIF13B (ENSG00000197892)

Protein

Protein identifiers

Kinesin-like protein KIFC1 — Q9BW19 (reviewed: Q9BW19)

Alternative names: Kinesin-like protein 2, Kinesin-related protein HSET

All UniProt accessions (4): A0A024RCS7, A0A087X1W5, A2AB20, Q9BW19

UniProt curated annotations — full annotation on UniProt →

Function. Minus end-directed microtubule-dependent motor required for bipolar spindle formation. May contribute to movement of early endocytic vesicles. Regulates cilium formation and structure.

Subunit / interactions. Binds NUBP1 and NUBP2. Interacts with PPP1R42.

Subcellular location. Nucleus. Cytoplasm. Cytoskeleton. Microtubule organizing center. Centrosome. Spindle. Early endosome.

Miscellaneous. HeLa cells lacking KIFC1 show multipolar mitotic spindles and a defect in chromosome congression and chromosome alignment during mitosis.

Similarity. Belongs to the TRAFAC class myosin-kinesin ATPase superfamily. Kinesin family. NCD subfamily.

RefSeq proteins (1): NP_002254* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR001752Kinesin_motor_domDomain
IPR019821Kinesin_motor_CSConserved_site
IPR027417P-loop_NTPaseHomologous_superfamily
IPR027640Kinesin-like_famFamily
IPR036961Kinesin_motor_dom_sfHomologous_superfamily

Pfam: PF00225

UniProt features (43 total): helix 14, strand 13, modified residue 5, region of interest 3, chain 1, domain 1, sequence variant 1, sequence conflict 1, turn 1, coiled-coil region 1, compositionally biased region 1, binding site 1

Structure

Experimental structures (PDB)

1 structures.

PDBMethodResolution (Å)
5WDHX-RAY DIFFRACTION2.25

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q9BW19-F178.160.53

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Ligand- & substrate-binding residues (1): 410–417

Post-translational modifications (5): 31, 33, 359, 6, 26

Function

Pathways and Gene Ontology

Reactome pathways

8 pathways

IDPathway
R-HSA-6811434COPI-dependent Golgi-to-ER retrograde traffic
R-HSA-983189Kinesins
R-HSA-109582Hemostasis
R-HSA-199991Membrane Trafficking
R-HSA-5653656Vesicle-mediated transport
R-HSA-6811442Intra-Golgi and retrograde Golgi-to-ER traffic
R-HSA-8856688Golgi-to-ER retrograde transport
R-HSA-983231Factors involved in megakaryocyte development and platelet production

MSigDB gene sets: 259 (showing top): BROWNE_HCMV_INFECTION_30MIN_DN, GOBP_CHROMOSOME_ORGANIZATION, MODULE_52, BUYTAERT_PHOTODYNAMIC_THERAPY_STRESS_DN, MORF_ESPL1, GNF2_CENPF, YAGI_AML_WITH_INV_16_TRANSLOCATION, GOBP_CHROMOSOME_LOCALIZATION, GOCC_KINESIN_COMPLEX, RIZKI_TUMOR_INVASIVENESS_3D_DN, GOBP_MALE_GAMETE_GENERATION, REACTOME_MEMBRANE_TRAFFICKING, GOCC_MICROTUBULE_ORGANIZING_CENTER, GOLDRATH_ANTIGEN_RESPONSE, PUJANA_CHEK2_PCC_NETWORK

GO Biological Process (6): mitotic sister chromatid segregation (GO:0000070), microtubule-based movement (GO:0007018), mitotic metaphase chromosome alignment (GO:0007080), spermatogenesis (GO:0007283), cell division (GO:0051301), mitotic spindle assembly (GO:0090307)

GO Molecular Function (6): microtubule motor activity (GO:0003777), ATP binding (GO:0005524), microtubule binding (GO:0008017), ATP hydrolysis activity (GO:0016887), nucleotide binding (GO:0000166), cytoskeletal motor activity (GO:0003774)

GO Cellular Component (12): nucleus (GO:0005634), cytoplasm (GO:0005737), early endosome (GO:0005769), centrosome (GO:0005813), microtubule organizing center (GO:0005815), kinesin complex (GO:0005871), microtubule (GO:0005874), membrane (GO:0016020), mitotic spindle (GO:0072686), endosome (GO:0005768), spindle (GO:0005819), cytoskeleton (GO:0005856)

Reactome top-level categories

Rollup of top-6 pathways:

CategoryPathways
Golgi-to-ER retrograde transport1
Factors involved in megakaryocyte development and platelet production1
Vesicle-mediated transport1
Membrane Trafficking1
Intra-Golgi and retrograde Golgi-to-ER traffic1
Hemostasis1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure3
microtubule cytoskeleton3
mitotic nuclear division2
mitotic cell cycle process2
mitotic sister chromatid segregation2
ATP-dependent activity2
intracellular membraneless organelle2
sister chromatid segregation1
microtubule-based process1
mitotic cell cycle1
metaphase chromosome alignment1
developmental process involved in reproduction1
male gamete generation1
cellular process1
mitotic spindle organization1
spindle assembly1
cytoskeletal motor activity1
polypeptide conformation or assembly isomerase activity1
adenyl ribonucleotide binding1
purine ribonucleoside triphosphate binding1
tubulin binding1
ribonucleoside triphosphate phosphatase activity1
nucleoside phosphate binding1
heterocyclic compound binding1
molecular_function1
intracellular membrane-bounded organelle1
intracellular anatomical structure1
endosome1
centriole1
microtubule organizing center1
microtubule associated complex1
polymeric cytoskeletal fiber1
spindle1
endomembrane system1
cytoplasmic vesicle1

Protein interactions and networks

STRING

2414 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
KIFC1RGL2O15211861
KIFC1SLC39A7Q92504855
KIFC1CDK5RAP2Q96SN8851
KIFC1RPS18P25232836
KIFC1HSD17B8Q92506817
KIFC1PFDN6O15212812
KIFC1COL11A2P13942795
KIFC1TAPBPO15533751
KIFC1RXRBP28702745
KIFC1NUMA1Q14980720
KIFC1RING1Q06587707
KIFC1CKAP5Q14008694
KIFC1DLGAP5Q15398679
KIFC1BUB1O43683649
KIFC1NCAPGQ9BPX3633

IntAct

96 interactions, top by confidence:

ABTypeScore
NUP50KPNA4psi-mi:“MI:0914”(association)0.830
NUP50KPNA3psi-mi:“MI:0914”(association)0.780
RALBP1JUNpsi-mi:“MI:0914”(association)0.640
KPNA1TCERG1psi-mi:“MI:0914”(association)0.640
KPNB1POM121Cpsi-mi:“MI:0914”(association)0.530
MINDY3UBBpsi-mi:“MI:0914”(association)0.530
EPS15L1NDC80psi-mi:“MI:0914”(association)0.530
GRB2SH3PXD2Bpsi-mi:“MI:0914”(association)0.530
LIN28BELAVL2psi-mi:“MI:0914”(association)0.530
PNMA2CCDC85Cpsi-mi:“MI:0914”(association)0.530
H3C1SMCHD1psi-mi:“MI:2364”(proximity)0.410
KIFC1PLECpsi-mi:“MI:0915”(physical association)0.400
Ranbp2psi-mi:“MI:0915”(physical association)0.400
Ndc80RRBP1psi-mi:“MI:0915”(physical association)0.400
Kifc1TPRpsi-mi:“MI:0915”(physical association)0.400
SDC1ILVBLpsi-mi:“MI:0915”(physical association)0.400
PARD6BPARD3psi-mi:“MI:0914”(association)0.350
Nek2WDR46psi-mi:“MI:0914”(association)0.350
NUP153POM121Cpsi-mi:“MI:0914”(association)0.350
Pdlim5HECTD4psi-mi:“MI:0914”(association)0.350
JUNTPM3psi-mi:“MI:0914”(association)0.350
ASPMKIF2Apsi-mi:“MI:0914”(association)0.350
MAPTMEX3Apsi-mi:“MI:0914”(association)0.350
ESR1ESYT2psi-mi:“MI:0914”(association)0.350

BioGRID (133): KIFC1 (Affinity Capture-MS), KIFC1 (Affinity Capture-MS), KIFC1 (Affinity Capture-MS), KIFC1 (Co-fractionation), KIFC1 (Co-fractionation), KIFC1 (Co-fractionation), KIFC1 (Proximity Label-MS), KIFC1 (Proximity Label-MS), KIFC1 (Affinity Capture-MS), KIFC1 (Affinity Capture-MS), KIFC1 (Affinity Capture-MS), KIFC1 (Affinity Capture-MS), KIFC1 (Affinity Capture-MS), KIFC1 (Affinity Capture-MS), KIFC1 (Affinity Capture-MS)

ESM2 similar proteins: A0A8I3NFE2, A2AP18, A6QP29, A6QPL4, A8WFU8, B1AVH7, B5DFA1, D2H0G5, D7PF45, O15357, O43304, O75038, O75808, Q0GNC1, Q0QWG9, Q14807, Q27J81, Q3V300, Q4R918, Q5I0E8, Q5REP4, Q5VV41, Q5XI63, Q60443, Q60806, Q61152, Q61846, Q69ZT1, Q6DT37, Q6L512, Q6P3R1, Q6P549, Q6ZMV9, Q7ZYL5, Q80UW5, Q8BL80, Q8C7W7, Q99952, Q9BVG8, Q9BW19

Diamond homologs: A2ZRG4, A3BFT0, A8BB91, A8BKD1, B2GU58, B3H6Z8, B7EJ91, B9EUM5, B9F7C8, B9FAF3, B9FL70, B9FTR1, B9G2X9, B9G8P1, F1QN54, F4HZF0, F4I1T9, F4IAR2, F4IBQ9, F4IIS5, F4IJK6, F4IL57, F4J2M6, F4JGP4, F4JX00, F4K4C5, O08672, O15066, O23826, O35231, O43093, O81635, O95239, P17119, P20480, P23678, P28025, P28739, P28741, P33174

SIGNOR signaling

9 interactions.

AEffectBMechanism
KIFC1up-regulatesProliferation
KIFC1up-regulatesCell_migration
KIFC1“up-regulates activity”CENPEbinding
KIFC1up-regulatesEpithelial-mesenchymal_transition
ATM“up-regulates quantity by stabilization”KIFC1phosphorylation
ATR“up-regulates quantity by stabilization”KIFC1phosphorylation
APC-c“down-regulates quantity by destabilization”KIFC1ubiquitination
CyclinB/CDK1“up-regulates quantity by stabilization”KIFC1phosphorylation
CDK1“up-regulates quantity by stabilization”KIFC1phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 128 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:

PathwayPartnersFoldFDR
NS1 Mediated Effects on Host Pathways1033.2×2e-10
Nuclear import of Rev protein831.2×3e-08
Transport of Ribonucleoproteins into the Host Nucleus729.1×7e-07
NEP/NS2 Interacts with the Cellular Export Machinery624.1×2e-05
Vpr-mediated nuclear import of PICs623.4×2e-05
Rev-mediated nuclear export of HIV RNA622.1×3e-05
IPs transport between nucleus and cytosol522.1×1e-04
IP3 and IP4 transport between cytosol and nucleus522.1×1e-04

GO biological processes:

GO termPartnersFoldFDR
NLS-bearing protein import into nucleus748.0×3e-08
RNA export from nucleus540.0×3e-05
ribosomal large subunit biogenesis518.9×1e-03
protein import into nucleus1518.5×2e-12
nucleocytoplasmic transport516.8×2e-03
mRNA transport511.2×8e-03
mRNA splicing, via spliceosome86.3×6e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

119 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic1
Uncertain significance81
Likely benign17
Benign1

Top pathogenic / likely-pathogenic (1)

Variant IDHGVSClassification
814807GRCh37/hg19 6p21.33-21.31(chr6:31036397-34088832)x3Likely pathogenic

SpliceAI

2080 predictions. Top by Δscore:

VariantEffectΔscore
6:33398023:CAACA:Cacceptor_loss1.0000
6:33398025:ACAGA:Aacceptor_loss1.0000
6:33398026:CAGA:Cacceptor_loss1.0000
6:33398027:A:AGacceptor_gain1.0000
6:33398027:A:ATacceptor_loss1.0000
6:33398028:G:GGacceptor_gain1.0000
6:33398028:GA:Gacceptor_gain1.0000
6:33398028:GAGGT:Gacceptor_gain1.0000
6:33398164:AAGG:Adonor_loss1.0000
6:33398165:AGG:Adonor_loss1.0000
6:33398166:GGTG:Gdonor_loss1.0000
6:33398167:G:Adonor_loss1.0000
6:33398168:T:Gdonor_loss1.0000
6:33403301:A:AGacceptor_gain1.0000
6:33403302:T:Gacceptor_gain1.0000
6:33403307:T:TAacceptor_gain1.0000
6:33403308:G:Aacceptor_gain1.0000
6:33403483:AG:Aacceptor_gain1.0000
6:33403484:GG:Gacceptor_gain1.0000
6:33403536:G:GGdonor_gain1.0000
6:33403728:GCAT:Gacceptor_gain1.0000
6:33404088:G:GTdonor_gain1.0000
6:33404126:GGAG:Gdonor_gain1.0000
6:33404127:GAGG:Gdonor_gain1.0000
6:33404128:AGG:Adonor_loss1.0000
6:33404131:T:Gdonor_loss1.0000
6:33404845:T:TAacceptor_gain1.0000
6:33404846:G:Aacceptor_gain1.0000
6:33405011:G:GTdonor_gain1.0000
6:33405629:G:GTdonor_gain1.0000

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000079989 (6:33391730 G>A), RS1000229944 (6:33401248 C>A,T), RS1000420976 (6:33408691 A>T), RS1000449187 (6:33395466 G>T), RS1000453515 (6:33408184 T>C), RS1000601597 (6:33401716 T>C,G), RS1000643844 (6:33394476 C>A), RS1000725043 (6:33402765 A>G), RS1000806306 (6:33410217 C>T), RS1000911328 (6:33395020 A>T), RS1001571744 (6:33407361 A>G), RS1001732836 (6:33402684 C>T), RS1001847307 (6:33402198 G>A), RS1001976407 (6:33401127 ATTTTTGT>A,ATTTTTGTTTTTTGT), RS1002007686 (6:33400909 C>T)

Disease associations

OMIM: gene MIM:603763 | 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

7 associations (top):

StudyTraitp-value
GCST004521_251Autism spectrum disorder or schizophrenia6.000000e-12
GCST004521_287Autism spectrum disorder or schizophrenia5.000000e-08
GCST004521_75Autism spectrum disorder or schizophrenia8.000000e-10
GCST004748_120Lung cancer2.000000e-06
GCST004749_13Lung cancer in ever smokers8.000000e-06
GCST005951_153Body mass index5.000000e-09
GCST007656_5Chronic obstructive pulmonary disease or resting heart rate (pleiotropy)3.000000e-15

EFO canonical traits (1, from GWAS)

EFO IDTrait name
EFO:0004340body mass index

MeSH disease descriptors (1)

DescriptorNameTree numbers
D018270Carcinoma, Ductal, BreastC04.557.470.200.025.232.500; 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 (1): CHEMBL3351200 (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: 287,353 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL14249ADENOSINE TRIPHOSPHATE2287,353

PharmGKB: 1 entry (VIP=true, CPIC=false)

ChEMBL bioactivities

60 potent at pChembl≥5 of 71 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
7.96IC5011nMCHEMBL5399029
7.92IC5012nMCHEMBL5432943
7.89IC5013nMCHEMBL5410651
7.72IC5019nMCHEMBL5402640
7.57IC5027nMCHEMBL5424226
7.41IC5039nMCHEMBL5413808
7.29IC5051nMCHEMBL5432943
7.21IC5061nMCHEMBL5437239
7.20IC5063nMCHEMBL5408867
7.18IC5066nMCHEMBL5402640
7.07IC5086nMCHEMBL5424226
7.05IC5089nMCHEMBL5402097
7.05IC5090nMCHEMBL5399029
7.03IC5093nMCHEMBL5401191
7.00IC50101nMCHEMBL5397143
6.97IC50107nMCHEMBL5414939
6.96IC50109nMCHEMBL5408867
6.85IC50140nMCHEMBL3358263
6.82IC50150nMCHEMBL3358276
6.80IC50157nMCHEMBL5398604
6.77IC50171nMCHEMBL3358270
6.75IC50180nMCHEMBL3358261
6.72IC50190nMCHEMBL3358280
6.66IC50217nMCHEMBL5413274
6.60IC50250nMCHEMBL3358264
6.59IC50257nMCHEMBL5395577
6.58IC50260nMCHEMBL5431102
6.58IC50260nMCHEMBL5417430
6.54IC50288nMCHEMBL5405412
6.51IC50310nMCHEMBL3358270
6.50IC50320nMCHEMBL3358262
6.50Kd315nMCHEMBL5395577
6.48IC50332nMCHEMBL5401191
6.48Kd332nMCHEMBL5395577
6.43Kd371nMCHEMBL5395577
6.40Kd400nMADENOSINE DIPHOSPHATE
6.39IC50405nMCHEMBL5423487
6.36Kd436nMADENOSINE TRIPHOSPHATE
6.30IC50500nMCHEMBL3358271
6.28IC50520nMCHEMBL3358281
6.16IC50700nMCHEMBL3358272
6.08IC50825nMCHEMBL3358270
6.02IC50960nMCHEMBL3358265
5.89IC501300nMCHEMBL3358258
5.77IC501700nMCHEMBL3358278
5.72IC501900nMCHEMBL3358257
5.70IC502000nMCHEMBL3358275
5.70IC502000nMCHEMBL3358273
5.68IC502100nMCHEMBL3358259
5.68IC502100nMCHEMBL5402598

PubChem BioAssay actives

60 with measured affinity, of 112 total; 49 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
propyl 2-[[(3S)-6-(dimethylamino)-3-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]hexanoyl]amino]-4-methyl-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.0110uM
propyl 4-methyl-2-[3-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]propanoylamino]-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.0120uM
propyl 2-[[(3S)-6-amino-3-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]hexanoyl]amino]-4-methyl-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.0130uM
propyl 4-methyl-2-[[(3S)-6-(methylamino)-3-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]hexanoyl]amino]-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.0190uM
ethyl 4-methyl-2-[3-[[3-(2-methyltetrazol-5-yl)benzoyl]amino]propanoylamino]-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.0270uM
propyl 2-[[(3S)-6-[4-[[(1S,4E)-cyclooct-4-en-1-yl]oxycarbonylamino]but-2-ynyl-methylamino]-3-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]hexanoyl]amino]-4-methyl-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.0390uM
ethyl 4-methyl-2-[[(3S)-3-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]butanoyl]amino]-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.0610uM
ethyl 4-methyl-2-[3-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]propanoylamino]-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.0630uM
ethyl 4-methyl-2-[methyl-[3-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]propanoyl]amino]-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.0890uM
ethyl 3-methyl-5-[3-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]propanoylamino]thiophene-2-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.0930uM
ethyl 4-methyl-2-[3-[[3-(3-methyl-1,2,4-oxadiazol-5-yl)benzoyl]amino]propanoylamino]-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.1010uM
propyl 2-[[(3S)-6-[2-[2-[2-[[(1S,4E)-cyclooct-4-en-1-yl]oxycarbonylamino]ethoxy]ethoxy]ethyl-methylamino]-3-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]hexanoyl]amino]-4-methyl-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.1070uM
N-[1-[2-(dimethylamino)ethylamino]-1-oxo-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propan-2-yl]-4-methyl-3-[(E)-prop-1-enyl]benzamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic500.1400uM
N-[(2R)-1-[2-(dimethylamino)ethylamino]-1-oxo-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propan-2-yl]-5-methyl-4-propylthiophene-2-carboxamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic500.1500uM
propyl 1-methyl-3-[3-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]propanoylamino]pyrazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.1570uM
5-methyl-N-[(2R)-1-oxo-1-[[(3R)-pyrrolidin-3-yl]amino]-3-[6-[3-(trifluoromethoxy)phenyl]-3-pyridinyl]propan-2-yl]-4-propylthiophene-2-carboxamide2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.1710uM
N-[1-[2-(dimethylamino)ethylamino]-1-oxo-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propan-2-yl]-5-methyl-4-propylthiophene-2-carboxamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic500.1800uM
4-methyl-N-[(2R)-1-oxo-1-[[(3R)-pyrrolidin-3-yl]amino]-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propan-2-yl]-3-[(E)-prop-1-enyl]benzamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic500.1900uM
propyl 2-[[(3S)-6-[[(1S,4E)-cyclooct-4-en-1-yl]oxycarbonyl-methylamino]-3-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]hexanoyl]amino]-4-methyl-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.2170uM
N-[1-[2-(dimethylamino)ethylamino]-1-oxo-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propan-2-yl]-4-methyl-3-propylbenzamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic500.2500uM
(2E)-3,3-dimethyl-1-[6-[[(4S)-4-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]-6-[(4-methyl-5-propoxycarbonyl-1,3-thiazol-2-yl)amino]-6-oxohexyl]amino]-6-oxohexyl]-2-[(2E,4E)-5-(1,3,3-trimethyl-5-sulfoindol-1-ium-2-yl)penta-2,4-dienylidene]indole-5-sulfonic acid2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.2570uM
propyl 4-methyl-2-[[(3R)-6-(methylamino)-3-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]hexanoyl]amino]-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.2600uM
ethyl 4-methyl-2-[3-[[3-(5-methyl-1,3,4-oxadiazol-2-yl)benzoyl]amino]propanoylamino]-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.2600uM
ethyl 4-methyl-2-[[(3R)-3-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]butanoyl]amino]-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.2880uM
2-cyclopropyl-N-[1-[2-(dimethylamino)ethylamino]-1-oxo-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propan-2-yl]-5-methylfuran-3-carboxamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic500.3200uM
[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphono hydrogen phosphate2028235: Displacement of FP-Probe from N-terminal His-tagged full length recombinant human HSET incubated for 2 hrs by fluorescence polarization based competitive binding assaykd0.4000uM
ethyl 4-methyl-2-[2-[[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]ethylcarbamoyl]-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic500.4050uM
[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate2028235: Displacement of FP-Probe from N-terminal His-tagged full length recombinant human HSET incubated for 2 hrs by fluorescence polarization based competitive binding assaykd0.4360uM
N-[(2R)-1-[2-(dimethylamino)ethylamino]-1-oxo-3-[6-[3-(trifluoromethoxy)phenyl]-3-pyridinyl]propan-2-yl]-5-methyl-4-propylthiophene-2-carboxamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic500.5000uM
4-methyl-N-[(2S)-1-oxo-1-[[(3R)-pyrrolidin-3-yl]amino]-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propan-2-yl]-3-[(E)-prop-1-enyl]benzamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic500.5200uM
N-[(2R)-1-[2-(dimethylamino)ethylamino]-1-oxo-3-[6-[3-(trifluoromethyl)phenyl]-3-pyridinyl]propan-2-yl]-5-methyl-4-propylthiophene-2-carboxamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic500.7000uM
N-[1-[2-(dimethylamino)ethylamino]-1-oxo-3-[4-[3-(trifluoromethoxy)phenyl]phenyl]propan-2-yl]-4-methoxy-3-(methoxymethyl)benzamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic500.9600uM
N-[1-[2-(dimethylamino)ethylamino]-1-oxo-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propan-2-yl]-3-ethoxy-4-methoxybenzamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic501.3000uM
(2R)-2-[(5-methyl-4-propylthiophene-2-carbonyl)amino]-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propanoic acid1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic501.7000uM
N-[1-[2-(dimethylamino)ethylamino]-1-oxo-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propan-2-yl]-4-methoxy-3-(methoxymethyl)benzamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic501.9000uM
3-ethoxy-4-methyl-N-[(2R)-1-oxo-1-[[(3R)-pyrrolidin-3-yl]amino]-3-[6-[3-(trifluoromethoxy)phenyl]-3-pyridinyl]propan-2-yl]benzamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic502.0000uM
N-[(2S)-1-[2-(dimethylamino)ethylamino]-1-oxo-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propan-2-yl]-4-methoxy-3-(methoxymethyl)benzamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic502.0000uM
N-[1-[2-(dimethylamino)ethylamino]-1-oxo-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propan-2-yl]-3,5-diethoxybenzamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic502.1000uM
ethyl 2-[3-[[3-(5-ethyl-1,2,4-oxadiazol-3-yl)benzoyl]amino]propanoylamino]-4-methyl-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic502.1000uM
ethyl 2-[3-[(3-ethylbenzoyl)amino]propanoylamino]-4-methyl-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic502.3200uM
ethyl 4-methyl-2-[3-[(3-phenylbenzoyl)amino]propanoylamino]-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic502.4400uM
N-[(2R)-1-[2-(dimethylamino)ethylamino]-1-oxo-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propan-2-yl]-4-methoxy-3-(methoxymethyl)benzamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic502.6000uM
ethyl 4-methyl-2-[3-[(3-methylbenzoyl)amino]propanoylamino]-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic502.7300uM
N-[1-[2-(dimethylamino)ethylamino]-1-oxo-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propan-2-yl]-3-ethoxybenzamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic503.2000uM
ethyl 2-[3-[(3-methoxybenzoyl)amino]propanoylamino]-4-methyl-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic503.5400uM
N-[(2S)-1-[2-(dimethylamino)ethylamino]-1-oxo-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propan-2-yl]-5-methyl-4-propylthiophene-2-carboxamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic504.5000uM
ethyl 4-methyl-2-[3-[(4-methylbenzoyl)amino]propanoylamino]-1,3-thiazole-5-carboxylate2028224: Inhibition of N-terminal His-tagged full length recombinant human HSET assessed as inhibition of microtubule-stimulated ATPase activity incubated for 10 mins in presence of 3 uM of ultra-ATP by ADP-Glo kinase assayic504.7300uM
(2R)-2-[[4-methyl-3-[(E)-prop-1-enyl]benzoyl]amino]-3-[4-[3-(trifluoromethyl)phenyl]phenyl]propanoic acid1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic504.8000uM
N-[1-[2-(dimethylamino)ethylamino]-3-[4-(3-ethylphenyl)phenyl]-1-oxopropan-2-yl]-4-methoxy-3-(methoxymethyl)benzamide1174089: Inhibition of recombinant N-terminal His6-tagged KIFC1 (Q305-K673 aa) (unknown origin) expressed in Escherichia coli BL21 (DE3) by malachite green assayic506.0000uM

CTD chemical–gene interactions

79 total (human), top 30 by PubMed support.

ChemicalActions (top 5)PubMed papers
sodium arseniteincreases expression, affects expression, decreases expression, affects cotreatment, increases abundance5
bisphenol Aincreases reaction, decreases expression, affects expression, affects cotreatment, decreases methylation (+1 more)4
N-(oxo-5,6-dihydrophenanthridin-2-yl)-N,N-dimethylacetamide hydrochlorideaffects binding, decreases reaction, decreases expression, increases metabolic processing2
Acetaminophenincreases expression, decreases expression2
Arsenicdecreases expression, increases abundance, affects methylation, affects cotreatment2
Benzo(a)pyreneaffects methylation, decreases expression2
Valproic Aciddecreases expression, increases methylation2
7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxidedecreases expression2
Cyclosporinedecreases expression2
Cadmium Chloridedecreases expression, increases expression2
FR900359affects phosphorylation1
propionaldehydedecreases expression1
beta-lapachonedecreases expression1
arseniteaffects binding, increases reaction1
tris(1,3-dichloro-2-propyl)phosphatedecreases expression1
perfluorooctanoic aciddecreases expression1
zinc chromatedecreases expression, increases abundance1
manganese chloridedecreases expression, increases abundance, affects cotreatment1
2,3-bis(3’-hydroxybenzyl)butyrolactoneaffects cotreatment, increases expression1
cupric oxidedecreases expression1
2-amino-3,8-dimethylimidazo(4,5-f)quinoxalinedecreases expression1
phenanthridoneincreases metabolic processing1
diallyl trisulfidedecreases expression1
chromium hexavalent iondecreases expression, increases abundance1
2-palmitoylglycerolincreases expression1
K 7174decreases expression1
erucylphospho-N,N,N-trimethylpropylammoniumdecreases expression1
thieno(2,3-c)isoquinolin-5-oneincreases metabolic processing1
ICG 001decreases expression1
palbociclibdecreases expression1

ChEMBL screening assays

27 unique, capped per target: 27 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1226594BindingInhibition of HSET at 10 uM by puruvate kinsase-lactate dehydrogenase detection systemATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism. — Nat Chem Biol

Cellosaurus cell lines

3 cell lines: 3 cancer cell line

First 10 cell lines (id-ordered, not curated):

CellosaurusNameCategorySex
CVCL_E0G4Ubigene HeLa KIFC1 KOCancer cell lineFemale
CVCL_SU88HAP1 KIFC1 (-) 1Cancer cell lineMale
CVCL_SU89HAP1 KIFC1 (-) 2Cancer cell lineMale

Clinical trials (associated diseases)

11 trials via MONDO — disease-level, not drug-specific.

TrialPhaseStatusTitle
NCT03414970PHASE3ACTIVE_NOT_RECRUITINGHypofractionated Radiation Therapy After Mastectomy in Preventing Recurrence in Patients With Stage IIa-IIIa Breast Cancer
NCT00461344PHASE2TERMINATEDDocetaxel + Doxorubicin as Neoadjuvant Chemotherapy in Patients With Breast Cancer
NCT07499999PHASE2NOT_YET_RECRUITINGRandomized Double-Blind Phase II Trial of Baby Exemestane Versus Baby Tamoxifen in Post-Menopausal Women at High Risk for Breast Cancer
NCT00637364PHASE1/PHASE2SUSPENDEDHigh Intensity Focused Ultrasound Tumor Treatment for Pancreatic Cancer Pain
NCT02779855PHASE1/PHASE2COMPLETEDTalimogene Laherparepvec in Combination With Neoadjuvant Chemotherapy in Triple Negative Breast Cancer
NCT01753908EARLY_PHASE1COMPLETEDBroccoli Sprout Extract in Treating Patients With Breast Cancer
NCT01796041EARLY_PHASE1COMPLETEDIntraoperative Imaging of Breast Cancer With Indocyanine Green
NCT01208974Not specifiedACTIVE_NOT_RECRUITINGNipple-Areola Complex (NAC) Irradiation After Nipple-Sparing Mastectomy and Reconstruction
NCT01875198Not specifiedTERMINATEDOncologic Impact of Splenectomy-omitting Radical Pancreatectomy in Well-selected Left-sided Pancreatic Cancer
NCT03543397Not specifiedUNKNOWNMRI in Ductal Carcinoma in Situ (DCIS)
NCT03834532Not specifiedCOMPLETEDLiving Well After Breast Surgery

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.4
BioBTree
v2.0.2

Sources 79

This page pulls from 79 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot