KIF5B
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Also known as KNSuKHC
Summary
KIF5B (kinesin family member 5B, HGNC:6324) is a protein-coding gene on chromosome 10p11.22, encoding Kinesin-1 heavy chain (P33176). Microtubule-dependent motor required for normal distribution of mitochondria and lysosomes.
Enables identical protein binding activity; microtubule binding activity; and microtubule motor activity. Involved in several processes, including natural killer cell mediated cytotoxicity; positive regulation of protein localization to plasma membrane; and vesicle transport along microtubule. Located in several cellular components, including centriolar satellite; cytosol; and nuclear membrane.
Source: NCBI Gene 3799 — RefSeq curated summary.
At a glance
- Gene–disease (curated): skeletal dysplasia (Strong, GenCC) — +1 more curated relationship
- GWAS associations: 9
- Clinical variants (ClinVar): 135 total — 2 pathogenic, 3 likely-pathogenic
- Phenotypes (HPO): 2
- Druggable target: yes — 3 molecules with ChEMBL bioactivity
- Cancer driver (intOGen): activating (oncogene-like) across 1 cancer types
- MANE Select transcript:
NM_004521
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:6324 |
| Approved symbol | KIF5B |
| Name | kinesin family member 5B |
| Location | 10p11.22 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | KNS, uKHC |
| Ensembl gene | ENSG00000170759 |
| Ensembl biotype | protein_coding |
| OMIM | 602809 |
| Entrez | 3799 |
Gene structure
Transcript identifiers
Ensembl transcripts: 6 — 5 protein_coding, 1 protein_coding_CDS_not_defined
ENST00000302418, ENST00000493889, ENST00000861448, ENST00000861449, ENST00000948543, ENST00000948544
RefSeq mRNA: 1 — MANE Select: NM_004521
NM_004521
CCDS: CCDS7171
Canonical transcript exons
ENST00000302418 — 26 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001135810 | 32015509 | 32015659 |
| ENSE00001163712 | 32017143 | 32017359 |
| ENSE00001163722 | 32018316 | 32018387 |
| ENSE00001163747 | 32022140 | 32022257 |
| ENSE00001163755 | 32022848 | 32023036 |
| ENSE00001163760 | 32028428 | 32028571 |
| ENSE00001163763 | 32031073 | 32031279 |
| ENSE00001163772 | 32033845 | 32034038 |
| ENSE00001163777 | 32034690 | 32034838 |
| ENSE00001163782 | 32035522 | 32035667 |
| ENSE00001163795 | 32037254 | 32037378 |
| ENSE00001163802 | 32037520 | 32037607 |
| ENSE00001163809 | 32038163 | 32038218 |
| ENSE00001163815 | 32038778 | 32038826 |
| ENSE00001163819 | 32039327 | 32039431 |
| ENSE00001163823 | 32040384 | 32040457 |
| ENSE00001163825 | 32048464 | 32048551 |
| ENSE00001376582 | 32021226 | 32021287 |
| ENSE00001387593 | 32021022 | 32021131 |
| ENSE00001551533 | 32055848 | 32056425 |
| ENSE00001799163 | 32035890 | 32035994 |
| ENSE00001872441 | 32009015 | 32011516 |
| ENSE00002512595 | 32032706 | 32032774 |
| ENSE00003508460 | 32018052 | 32018156 |
| ENSE00003543329 | 32018502 | 32018562 |
| ENSE00003621273 | 32019858 | 32019959 |
Expression profiles
Bgee: expression breadth ubiquitous, 303 present calls, max score 99.63.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 79.0836 / max 832.9894, expressed in 1823 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 108992 | 78.4676 | 1823 |
| 108991 | 0.6161 | 225 |
Top tissues by expression
303 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| cauda epididymis | UBERON:0004360 | 99.63 | gold quality |
| caput epididymis | UBERON:0004358 | 99.49 | gold quality |
| cranial nerve II | UBERON:0000941 | 99.44 | gold quality |
| corpus epididymis | UBERON:0004359 | 99.41 | gold quality |
| mucosa of paranasal sinus | UBERON:0005030 | 99.40 | gold quality |
| inferior vagus X ganglion | UBERON:0005363 | 99.37 | gold quality |
| visceral pleura | UBERON:0002401 | 99.30 | gold quality |
| lower lobe of lung | UBERON:0008949 | 99.29 | gold quality |
| medial globus pallidus | UBERON:0002477 | 99.23 | gold quality |
| globus pallidus | UBERON:0001875 | 99.19 | gold quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 99.13 | gold quality |
| mucosa of sigmoid colon | UBERON:0004993 | 99.06 | gold quality |
| superficial temporal artery | UBERON:0001614 | 99.04 | gold quality |
| subthalamic nucleus | UBERON:0001906 | 99.04 | gold quality |
| medulla oblongata | UBERON:0001896 | 98.94 | gold quality |
| dorsal motor nucleus of vagus nerve | UBERON:0002870 | 98.87 | gold quality |
| bronchial epithelial cell | CL:0002328 | 98.86 | gold quality |
| heart right ventricle | UBERON:0002080 | 98.85 | gold quality |
| superior vestibular nucleus | UBERON:0007227 | 98.84 | gold quality |
| saphenous vein | UBERON:0007318 | 98.84 | gold quality |
| biceps brachii | UBERON:0001507 | 98.83 | gold quality |
| lateral globus pallidus | UBERON:0002476 | 98.79 | gold quality |
| choroid plexus epithelium | UBERON:0003911 | 98.79 | gold quality |
| pylorus | UBERON:0001166 | 98.75 | gold quality |
| parietal pleura | UBERON:0002400 | 98.73 | gold quality |
| colonic mucosa | UBERON:0000317 | 98.70 | gold quality |
| jejunal mucosa | UBERON:0000399 | 98.70 | gold quality |
| gluteal muscle | UBERON:0002000 | 98.68 | gold quality |
| germinal epithelium of ovary | UBERON:0001304 | 98.67 | gold quality |
| pons | UBERON:0000988 | 98.66 | gold quality |
Single-cell (SCXA)
Detected in 3 experiment(s), a significant marker in 2.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-CURD-114 | yes | 7.02 |
| E-MTAB-6379 | no | 2683.11 |
| E-ANND-3 | no | 0.00 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): NEUROD6
miRNA regulators (miRDB)
227 targeting KIF5B, 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-3613-3P | 100.00 | 76.36 | 7965 |
| HSA-MIR-1277-5P | 100.00 | 73.95 | 5056 |
| HSA-MIR-340-5P | 100.00 | 72.50 | 4437 |
| 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-6833-3P | 100.00 | 70.63 | 3197 |
| HSA-MIR-4425 | 100.00 | 67.59 | 1049 |
| HSA-MIR-4768-5P | 100.00 | 69.49 | 2861 |
| HSA-MIR-3163 | 100.00 | 77.23 | 8605 |
| HSA-MIR-29A-3P | 100.00 | 73.11 | 1835 |
| HSA-MIR-29B-3P | 100.00 | 73.18 | 1833 |
| HSA-MIR-29C-3P | 100.00 | 73.15 | 1833 |
| HSA-MIR-126-5P | 100.00 | 72.71 | 3180 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-548AW | 99.99 | 72.57 | 3559 |
| HSA-MIR-5696 | 99.98 | 72.36 | 4487 |
| HSA-MIR-548P | 99.98 | 72.25 | 3784 |
| HSA-MIR-4789-5P | 99.98 | 70.76 | 2721 |
| HSA-MIR-12136 | 99.98 | 72.81 | 5713 |
| HSA-MIR-25-3P | 99.98 | 74.60 | 1817 |
| HSA-MIR-32-5P | 99.98 | 75.21 | 1964 |
| HSA-MIR-363-3P | 99.98 | 74.72 | 1821 |
| HSA-MIR-367-3P | 99.98 | 74.83 | 1819 |
| HSA-MIR-92A-3P | 99.98 | 75.21 | 1960 |
| HSA-MIR-92B-3P | 99.98 | 75.25 | 1955 |
| HSA-LET-7F-2-3P | 99.98 | 70.98 | 2588 |
| HSA-MIR-1185-1-3P | 99.98 | 71.04 | 2593 |
Literature-anchored findings (GeneRIF, showing 40)
- links neurofibromin and merlin in a common cellular pathway of neurofibromatosis (PMID:12191989)
- With residues 814-963 of human ubiquitous kinesin heavy chain (uKHC) used as bait, a synaptosome-associated protein of 25 kDa (SNAP25) has been identified as a kinesin-binding protein in a human brain cDNA library. (PMID:12475239)
- Results identify the ribosome receptor, p180, as a binding partner of the kinesin heavy chain isoform KIF5B. (PMID:15184079)
- CRMP-2 transports the Sra-1/WAVE1 complex to axons in a kinesin-1-dependent manner and thereby regulates axon outgrowth and formation (PMID:16260607)
- Demonstrates the utility of screening for PDGFRA kinase domain overexpression in patients with IHES and has identified KIF5B as a third PDGFRA fusion partner in chronic myeloproliferative disorders. (PMID:16498388)
- kinesin-1, but not kinesin-2, contributes to the specific cytoplasmic distribution of three of the four steps of VV morphogenesis tested. (PMID:17394562)
- binding of the kinesin-binding domain of RanBP2 to KIF5B and KIF5C determines mitochondria localization and function (PMID:17887960)
- We demonstrate that KIF5B mediates post-Golgi transport of an apical protein in epithelial cells, but only after polarity has developed. (PMID:17925227)
- Data suggest that the promotion of lamellipodia formation by HGF in MDA-MB-231 cells is Rac1-dependent and requires KIF5B-mediated transport of WAVE2 and IQGAP1 to the cell periphery along microtubules. (PMID:18514191)
- The interaction of the Switch I region of the kinesin-1 head with the tail is strikingly similar to the interactions of small GTPases with their regulators, indicating that other kinesin motors may share similar regulatory mechanisms. (PMID:18579780)
- data implicate kinesin-1 in the spatial organization of the ER/Golgi interface as well as in traffic outside the ER (PMID:18817524)
- training-induced changes in submaximal exercise stroke volume may be due to mitochondrial function and variation in KIF5B expression as determined by functional SNPs in its promoter. (PMID:18984674)
- KIF5B is a cancer relevant lysosomal motor protein with additional functions in autophagosome formation (PMID:19242560)
- RANBP2 is the first native and positive allosteric activator known to jump-start and boost directly the activity of KIF5B. (PMID:19305391)
- the interaction between the kinesin-1 head and its regulatory tail domain (PMID:19348763)
- role of the kinesin I isoform Kif5b in the trafficking of a cardiac voltage-gated potassium channel, Kv1.5 in Kv1.5-expressing HEK293 cells and H9c2 cardiomyoblasts (PMID:19675065)
- Na,K-ATPase traffic toward the plasma membrane in alveolar epithelial cells is driven by kinesin-1, where KLC2 is the isoform regulating this process. (PMID:19773350)
- This indicates that kinesin-1 facilitates the transport of SNAP-25 containing vesicles as a prerequisite to SNAP-25 driven membrane fusion events. (PMID:19913510)
- a kinesin-1 tail fragment associates with microtubules with submicromolar affinity and binding is largely electrostatic (PMID:20071331)
- The discovery of the novel KIF5B-ALK variant further consolidated the role of aberrant anaplastic lymphoma kinase signaling in lung carcinogenesis. (PMID:21656749)
- The conventional kinesin-microtubule binding free energy is dominated by van der Waals interactions and electrostatic interactions. (PMID:21910419)
- findings show a bipartite tryptophan-based motif in vaccinia virus A36 is required for kinesin-1-dependent transport of the virus; bioinformatic analysis reveals that related bipartite tryptophan-based motifs are present in over 450 human proteins (PMID:21915095)
- Kinesin-1-mediated capsid disassembly and disruption of the nuclear pore complex promote virus infection. (PMID:21925109)
- Arl8 and SKIP are required for lysosomes to distribute away from the microtubule-organizing center. We identify two kinesin light chain binding motifs in SKIP that are required for lysosomes to accumulate kinesin-1 and redistribute to the cell periphery. (PMID:22172677)
- Data indicate that mutant KIF5B kinesin-1 binds ATP similarly in the presence of either metal ion, but its ATP hydrolysis activity is greatly diminished in the presence of Mg(2+). (PMID:22198464)
- Expression of exogenous KIF5B-RET, induced morphological transformation and anchorage-independent growth of NIH3T3 fibroblasts (PMID:22327624)
- Nesca directly binds KIF5B, kinesin light-chain and syntaxin-1 (PMID:22404429)
- Study found the secretion of calu-1/2-EGFP required microtubule integrity, and that calu-1/2-EGFP-containing vesicles were transported by the motor proteins Kif5b and cytoplasmic dynein. (PMID:22514732)
- Patients without KIF5B-RET fusions had a better prognosis than those with KIF5B-RET fusions (median survival, 52.6 months vs 21.0 months). (PMID:23378251)
- Anti-oncogenic miR-203 had a pivotal role in melanoma through reducing melanosome transport and promoting melanogenesis by targeting kif5b and through negative regulation of the CREB1/MITF/Rab27a pathway. (PMID:23884313)
- when cargo is transported by both dynein and phosphorylated kinesin, a common occurrence in the cell, there may be a bias that favors motion toward the minus-end of microtubules. (PMID:24072715)
- Kinesin-1 transports c-MYC for proteasomal degradation in the cytoplasm. (PMID:24821626)
- Our data suggest that KIF5B-RET promotes the cell growth and tumorigenicity of non-small cell lung cancers through multilevel activation of STAT3 signaling, providing possible strategies for the treatment of KIF5B-RET positive lung cancers. (PMID:25047660)
- Authors find that pharmacological or small interfering RNA (siRNA)-mediated inhibition of cytoplasmic dynein or the kinesin 1 heavy chain KIF5B delays HIV-1 uncoating. (PMID:25231297)
- Kinesin-14 blocks microtubule nucleation in yeast and reveal that this inhibition is countered by the kinesin-5 protein, Cut7.[Cut7, Pkl1] (PMID:25348260)
- A novel role of KIF5B was shown in the spatial regulation of Cdo-BNIP-2-p38MAPK signaling and discloses a previously unappreciated linkage between the intracellular transporting system and myogenesis regulation. (PMID:25378581)
- compared to those of brain, on MCF7 microtubules, kinesin-1’s processivity is significantly reduced although its velocity is only slightly altered (PMID:25450690)
- nesprin-dependent recruitment of kinesin-1 to the nuclear envelope through the interaction of a conserved LEWD motif with kinesin light chain might be a general mechanism for cell-type-specific nuclear positioning during development. (PMID:25516977)
- This study has provided a comprehensive structural and dynamic picture of kinesin’s major ATPase states. (PMID:25537000)
- Myo1c significantly increases the frequency of kinesin-1-driven microtubule-based runs that begin at actin/microtubule intersections. The actin-binding protein tropomyosin 2 abolishes Myo1c-specific effects on both run initiation and run termination. (PMID:25660542)
Cross-species orthologs
5 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | kif5ba | ENSDARG00000074131 |
| danio_rerio | KIF5B | ENSDARG00000103394 |
| mus_musculus | Kif5b | ENSMUSG00000006740 |
| rattus_norvegicus | Kif5b | ENSRNOG00000017466 |
| drosophila_melanogaster | Khc | FBGN0001308 |
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), KIF18B (ENSG00000186185), KIF24 (ENSG00000186638), KIF19 (ENSG00000196169), KIF13B (ENSG00000197892), KIF4B (ENSG00000226650)
Protein
Protein identifiers
Kinesin-1 heavy chain — P33176 (reviewed: P33176)
Alternative names: Conventional kinesin heavy chain, Ubiquitous kinesin heavy chain
All UniProt accessions (2): P33176, V9HW29
UniProt curated annotations — full annotation on UniProt →
Function. Microtubule-dependent motor required for normal distribution of mitochondria and lysosomes. Can induce formation of neurite-like membrane protrusions in non-neuronal cells in a ZFYVE27-dependent manner. Regulates centrosome and nuclear positioning during mitotic entry. During the G2 phase of the cell cycle in a BICD2-dependent manner, antagonizes dynein function and drives the separation of nuclei and centrosomes. Required for anterograde axonal transportation of MAPK8IP3/JIP3 which is essential for MAPK8IP3/JIP3 function in axon elongation. Through binding with PLEKHM2 and ARL8B, directs lysosome movement toward microtubule plus ends. Involved in NK cell-mediated cytotoxicity. Drives the polarization of cytolytic granules and microtubule-organizing centers (MTOCs) toward the immune synapse between effector NK lymphocytes and target cells.
Subunit / interactions. Oligomer composed of two heavy chains and two light chains. Interacts with GRIP1 and PPP1R42. Interacts with SYBU. Interacts with JAKMIP1. Interacts with PLEKHM2. Interacts with ECPAS. Interacts with ZFYVE27. Found in a complex with OGT, RHOT1, RHOT2 and TRAK1. Interacts with APP (via cytoplasmic domain).
Subcellular location. Cytoplasm. Cytoskeleton. Cytolytic granule membrane. Lysosome membrane.
Domain organisation. Composed of three structural domains: a large globular N-terminal domain which is responsible for the motor activity of kinesin (it hydrolyzes ATP and binds microtubule), a central alpha-helical coiled coil domain that mediates the heavy chain dimerization; and a small globular C-terminal domain which interacts with other proteins (such as the kinesin light chains), vesicles and membranous organelles.
Similarity. Belongs to the TRAFAC class myosin-kinesin ATPase superfamily. Kinesin family. Kinesin subfamily.
RefSeq proteins (1): NP_004512* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR001752 | Kinesin_motor_dom | Domain |
| IPR019821 | Kinesin_motor_CS | Conserved_site |
| IPR027417 | P-loop_NTPase | Homologous_superfamily |
| IPR027640 | Kinesin-like_fam | Family |
| IPR036961 | Kinesin_motor_dom_sf | Homologous_superfamily |
| IPR059182 | Khc_C | Domain |
Pfam: PF00225
Enzyme classification (BRENDA):
- EC 5.6.1.3 — plus-end-directed kinesin ATPase (BRENDA: 34 organisms, 94 substrates, 257 inhibitors, 53 Km, 52 kcat entries)
Substrate kinetics (BRENDA)
5 substrates with measured Km, best-characterized 5. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| ATP | — | 45 |
| ALEXA FLUOR 647 ATP | 0.032 | 1 |
| METHYLANTHRANILOYL-ATP | 0.0004 | 1 |
| ADP | — | 0 |
| PHOSPHATE | — | 0 |
UniProt features (50 total): strand 17, helix 16, turn 6, modified residue 3, region of interest 2, initiator methionine 1, chain 1, cross-link 1, domain 1, coiled-coil region 1, binding site 1
Structure
Experimental structures (PDB)
31 structures, top 30 by resolution.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 1BG2 | X-RAY DIFFRACTION | 1.8 |
| 5LT1 | X-RAY DIFFRACTION | 1.95 |
| 5LT0 | X-RAY DIFFRACTION | 2 |
| 4LNU | X-RAY DIFFRACTION | 2.19 |
| 9L7E | X-RAY DIFFRACTION | 2.4 |
| 5LT3 | X-RAY DIFFRACTION | 2.59 |
| 5LT2 | X-RAY DIFFRACTION | 2.6 |
| 1MKJ | X-RAY DIFFRACTION | 2.7 |
| 9L6K | X-RAY DIFFRACTION | 2.8 |
| 9L78 | X-RAY DIFFRACTION | 2.82 |
| 5LT4 | X-RAY DIFFRACTION | 2.88 |
| 9GNQ | ELECTRON MICROSCOPY | 2.9 |
| 7TR2 | ELECTRON MICROSCOPY | 3 |
| 8RHB | ELECTRON MICROSCOPY | 3 |
| 8RHH | ELECTRON MICROSCOPY | 3 |
| 7TR1 | ELECTRON MICROSCOPY | 3.1 |
| 4HNA | X-RAY DIFFRACTION | 3.19 |
| 9L7M | ELECTRON MICROSCOPY | 3.48 |
| 8RIK | ELECTRON MICROSCOPY | 3.6 |
| 8RIZ | ELECTRON MICROSCOPY | 3.6 |
| 6OJQ | ELECTRON MICROSCOPY | 3.67 |
| 8IXA | ELECTRON MICROSCOPY | 4.2 |
| 8IXB | ELECTRON MICROSCOPY | 4.2 |
| 8IXD | ELECTRON MICROSCOPY | 4.4 |
| 8IXE | ELECTRON MICROSCOPY | 4.4 |
| 8IXF | ELECTRON MICROSCOPY | 4.4 |
| 8IXG | ELECTRON MICROSCOPY | 4.4 |
| 3J8X | ELECTRON MICROSCOPY | 5 |
| 3J8Y | ELECTRON MICROSCOPY | 5 |
| 2P4N | ELECTRON MICROSCOPY | 9 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P33176-F1 | 79.17 | 0.30 |
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): 85–92
Post-translational modifications (4): 213, 2, 933, 956
Function
Pathways and Gene Ontology
Reactome pathways
23 pathways
| ID | Pathway |
|---|---|
| R-HSA-2132295 | MHC class II antigen presentation |
| R-HSA-264876 | Insulin processing |
| R-HSA-5625970 | RHO GTPases activate KTN1 |
| R-HSA-6811434 | COPI-dependent Golgi-to-ER retrograde traffic |
| R-HSA-9725370 | Signaling by ALK fusions and activated point mutants |
| R-HSA-983189 | Kinesins |
| R-HSA-109582 | Hemostasis |
| R-HSA-1280218 | Adaptive Immune System |
| R-HSA-162582 | Signal Transduction |
| R-HSA-1643685 | Disease |
| R-HSA-168256 | Immune System |
| R-HSA-194315 | Signaling by Rho GTPases |
| R-HSA-195258 | RHO GTPase Effectors |
| R-HSA-199991 | Membrane Trafficking |
| R-HSA-2980736 | Peptide hormone metabolism |
| R-HSA-392499 | Metabolism of proteins |
| R-HSA-5653656 | Vesicle-mediated transport |
| R-HSA-5663202 | Diseases of signal transduction by growth factor receptors and second messengers |
| R-HSA-6811442 | Intra-Golgi and retrograde Golgi-to-ER traffic |
| R-HSA-8856688 | Golgi-to-ER retrograde transport |
| R-HSA-9700206 | Signaling by ALK in cancer |
| R-HSA-9716542 | Signaling by Rho GTPases, Miro GTPases and RHOBTB3 |
| R-HSA-983231 | Factors involved in megakaryocyte development and platelet production |
MSigDB gene sets: 384 (showing top):
GOBP_POTASSIUM_ION_TRANSPORT, GOBP_SYNAPTIC_VESICLE_LOCALIZATION, BORCZUK_MALIGNANT_MESOTHELIOMA_UP, RODRIGUES_THYROID_CARCINOMA_ANAPLASTIC_UP, GOBP_AXO_DENDRITIC_TRANSPORT, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_UP, GOBP_VESICLE_LOCALIZATION, REACTOME_ADAPTIVE_IMMUNE_SYSTEM, GOBP_INTRACELLULAR_PROTEIN_TRANSPORT, TGCTGCT_MIR15A_MIR16_MIR15B_MIR195_MIR424_MIR497, GOBP_RESPONSE_TO_PEPTIDE, GOCC_VACUOLAR_MEMBRANE, GOCC_KINESIN_COMPLEX, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GOBP_POSITIVE_REGULATION_OF_PROTEIN_LOCALIZATION
GO Biological Process (22): microtubule-based movement (GO:0007018), cytoplasm organization (GO:0007028), axon guidance (GO:0007411), positive regulation of synaptic transmission, GABAergic (GO:0032230), lysosome localization (GO:0032418), stress granule disassembly (GO:0035617), natural killer cell mediated cytotoxicity (GO:0042267), regulation of membrane potential (GO:0042391), positive regulation of potassium ion transport (GO:0043268), vesicle transport along microtubule (GO:0047496), mitochondrion transport along microtubule (GO:0047497), synaptic vesicle transport (GO:0048489), centrosome localization (GO:0051642), cellular response to type II interferon (GO:0071346), plus-end-directed vesicle transport along microtubule (GO:0072383), anterograde dendritic transport of neurotransmitter receptor complex (GO:0098971), regulation of modification of synapse structure, modulating synaptic transmission (GO:0098987), anterograde axonal protein transport (GO:0099641), mitocytosis (GO:0160040), positive regulation of protein localization to plasma membrane (GO:1903078), anterograde neuronal dense core vesicle transport (GO:1990048), retrograde neuronal dense core vesicle transport (GO:1990049)
GO Molecular Function (11): microtubule motor activity (GO:0003777), ATP binding (GO:0005524), microtubule binding (GO:0008017), plus-end-directed microtubule motor activity (GO:0008574), ATP hydrolysis activity (GO:0016887), identical protein binding (GO:0042802), protein-containing complex binding (GO:0044877), cadherin binding (GO:0045296), nucleotide binding (GO:0000166), cytoskeletal motor activity (GO:0003774), protein binding (GO:0005515)
GO Cellular Component (22): cytoplasm (GO:0005737), mitochondrion (GO:0005739), cytosol (GO:0005829), kinesin complex (GO:0005871), microtubule (GO:0005874), membrane (GO:0016020), nuclear membrane (GO:0031965), vesicle (GO:0031982), dendrite cytoplasm (GO:0032839), centriolar satellite (GO:0034451), ciliary rootlet (GO:0035253), phagocytic vesicle (GO:0045335), perinuclear region of cytoplasm (GO:0048471), sperm end piece (GO:0097229), postsynaptic cytosol (GO:0099524), cytolytic granule membrane (GO:0101004), axon cytoplasm (GO:1904115), lysosome (GO:0005764), lysosomal membrane (GO:0005765), cytoskeleton (GO:0005856), endocytic vesicle (GO:0030139), neuron projection (GO:0043005)
Reactome top-level categories
Rollup of top-14 pathways:
| Category | Pathways |
|---|---|
| Adaptive Immune System | 1 |
| Peptide hormone metabolism | 1 |
| RHO GTPase Effectors | 1 |
| Golgi-to-ER retrograde transport | 1 |
| Signaling by ALK in cancer | 1 |
| Factors involved in megakaryocyte development and platelet production | 1 |
| Immune System | 1 |
| Signaling by Rho GTPases, Miro GTPases and RHOBTB3 | 1 |
| Signaling by Rho GTPases | 1 |
| Vesicle-mediated transport | 1 |
| Metabolism of proteins | 1 |
| Disease | 1 |
| Membrane Trafficking | 1 |
| Intra-Golgi and retrograde Golgi-to-ER traffic | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular anatomical structure | 7 |
| cytoplasm | 3 |
| organelle transport along microtubule | 2 |
| ATP-dependent activity | 2 |
| binding | 2 |
| neuron projection cytoplasm | 2 |
| microtubule-based process | 1 |
| cellular component organization | 1 |
| axonogenesis | 1 |
| neuron projection guidance | 1 |
| regulation of synaptic transmission, GABAergic | 1 |
| positive regulation of synaptic transmission | 1 |
| synaptic transmission, GABAergic | 1 |
| vacuolar localization | 1 |
| protein-RNA complex disassembly | 1 |
| organelle disassembly | 1 |
| leukocyte mediated cytotoxicity | 1 |
| natural killer cell mediated immunity | 1 |
| monoatomic ion transmembrane transport | 1 |
| regulation of biological quality | 1 |
| potassium ion transport | 1 |
| regulation of potassium ion transport | 1 |
| positive regulation of monoatomic ion transport | 1 |
| vesicle cytoskeletal trafficking | 1 |
| establishment of mitochondrion localization, microtubule-mediated | 1 |
| transport | 1 |
| cellular process | 1 |
| establishment of vesicle localization | 1 |
| synaptic vesicle localization | 1 |
| microtubule organizing center localization | 1 |
| response to type II interferon | 1 |
| cellular response to cytokine stimulus | 1 |
| vesicle transport along microtubule | 1 |
| plus-end-directed organelle transport along microtubule | 1 |
| receptor localization to synapse | 1 |
| anterograde dendritic transport | 1 |
| chemical synaptic transmission | 1 |
| modulation of chemical synaptic transmission | 1 |
| regulation of modification of synaptic structure | 1 |
| anterograde axonal transport | 1 |
Protein interactions and networks
STRING
2802 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| KIF5B | KLC1 | Q07866 | 990 |
| KIF5B | KLC2 | Q9H0B6 | 982 |
| KIF5B | KLC3 | Q6P597 | 976 |
| KIF5B | RANBP2 | P49792 | 969 |
| KIF5B | SYBU | Q9NX95 | 964 |
| KIF5B | KLC4 | Q9NSK0 | 907 |
| KIF5B | SYNE4 | Q8N205 | 894 |
| KIF5B | PLEKHM2 | Q8IWE5 | 854 |
| KIF5B | RET | P07949 | 822 |
| KIF5B | ALK | Q9UM73 | 822 |
| KIF5B | ARL8B | Q9NVJ2 | 820 |
| KIF5B | EML4 | Q9HC35 | 807 |
| KIF5B | TRAK1 | Q9UPV9 | 798 |
| KIF5B | RET | P07949 | 773 |
| KIF5B | BSN | Q9UPA5 | 772 |
IntAct
299 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| MED4 | MED19 | psi-mi:“MI:2364”(proximity) | 0.900 |
| YWHAQ | WDR62 | psi-mi:“MI:0914”(association) | 0.830 |
| YWHAH | ABLIM1 | psi-mi:“MI:0914”(association) | 0.800 |
| HOMER1 | TRAF5 | psi-mi:“MI:0914”(association) | 0.740 |
| KLC1 | KIF5B | psi-mi:“MI:0914”(association) | 0.730 |
| KIF5B | KLC1 | psi-mi:“MI:0914”(association) | 0.730 |
| CFTR | ESYT2 | psi-mi:“MI:0914”(association) | 0.710 |
| CFTR | ESYT2 | psi-mi:“MI:2364”(proximity) | 0.710 |
| KIF5B | KIF5B | psi-mi:“MI:0407”(direct interaction) | 0.680 |
| KIF5B | KIF5B | psi-mi:“MI:0915”(physical association) | 0.680 |
| FYCO1 | KIF5B | psi-mi:“MI:0915”(physical association) | 0.640 |
| YWHAG | BLTP3B | psi-mi:“MI:2364”(proximity) | 0.640 |
| YWHAH | PLEKHG3 | psi-mi:“MI:0914”(association) | 0.610 |
| YWHAH | BLTP3B | psi-mi:“MI:2364”(proximity) | 0.570 |
| HSF2BP | KIF5B | psi-mi:“MI:0915”(physical association) | 0.560 |
| KIF5B | CDR2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KIF5B | psi-mi:“MI:0915”(physical association) | 0.560 | |
| KIF5B | ZBTB8A | psi-mi:“MI:0915”(physical association) | 0.560 |
| KIF5B | MEOX2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KIF5B | POU6F2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KIF5B | FHL2 | psi-mi:“MI:0915”(physical association) | 0.560 |
BioGRID (505): KIF5B (Affinity Capture-MS), PRKAR2B (Two-hybrid), VPS52 (Two-hybrid), TAX1BP1 (Two-hybrid), ZBTB8A (Two-hybrid), KIF5B (Affinity Capture-MS), KIF5B (Affinity Capture-MS), KIF5B (Affinity Capture-MS), KIF5B (Affinity Capture-MS), KIF5B (Affinity Capture-MS), KIF5B (Affinity Capture-MS), KIF5B (Affinity Capture-MS), KIF5B (Affinity Capture-MS), KIF5B (Affinity Capture-MS), KIF5B (Affinity Capture-MS)
ESM2 similar proteins: A0JN40, A8BB91, A8BKD1, B1AVY7, B9F2Y7, F1M4A4, F1M5N7, F1QN54, F4K0J3, G5EGS3, O14782, O15066, O35066, O55165, O60333, O75037, O88658, P28741, P33173, P33176, P34540, P35978, P46867, P46871, P46872, P46873, Q10E64, Q12756, Q29DY1, Q2PQA9, Q4R628, Q5JKW1, Q5R4H3, Q5R706, Q60575, Q61768, Q61771, Q6YUL8, Q7Z4S6, Q86Z98
Diamond homologs: A0A068FIK2, A0JN40, A1ZAJ2, A8BB91, A8BKD1, B1AVY7, B7EJ91, B7ZNG0, B9F2Y7, B9GE13, F1M4A4, F1M5N7, F1QN54, F4IIS5, F4J1U4, F4K0J3, G5EGS3, O14343, O14782, O15066, O23826, O35066, O35071, O35787, O43896, O45935, O55165, O60282, O60333, O75037, O88658, O95239, P17210, P21613, P23678, P28738, P28741, P33173, P33174, P33175
SIGNOR signaling
7 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| KTN1 | up-regulates | KIF5B | binding |
| DISC1 | “up-regulates activity” | KIF5B | binding |
| KIF5B | up-regulates | Organelle_transport | |
| KIF5B | “up-regulates activity” | SYBU | relocalization |
| KIF5B | up-regulates | “Plus-end directed sliding movement” | |
| KIF5B | “up-regulates activity” | JAKMIP1 | relocalization |
| KIF5B | “up-regulates activity” | GABBR1 | relocalization |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 165 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 |
|---|---|---|---|
| Activation of BAD and translocation to mitochondria | 7 | 49.4× | 1e-08 |
| Chk1/Chk2(Cds1) mediated inactivation of Cyclin B:Cdk1 complex | 7 | 43.5× | 2e-08 |
| SARS-CoV-1 targets host intracellular signalling and regulatory pathways | 7 | 43.5× | 2e-08 |
| Activation of BH3-only proteins | 7 | 32.2× | 1e-07 |
| RHO GTPases activate PKNs | 7 | 20.6× | 2e-06 |
| Intrinsic Pathway for Apoptosis | 7 | 19.0× | 3e-06 |
| FOXO-mediated transcription | 6 | 18.7× | 2e-05 |
| Apoptosis | 10 | 15.6× | 7e-08 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| protein targeting | 7 | 17.9× | 1e-04 |
| negative regulation of innate immune response | 5 | 17.9× | 4e-03 |
| intracellular protein localization | 9 | 6.6× | 4e-03 |
Disease & clinical
Cancer significance
From intOGen — cancer-driver classification: activating (oncogene-like) across 1 cancer types — HNSC.
Clinical variants and AI predictions
ClinVar
135 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 2 |
| Likely pathogenic | 3 |
| Uncertain significance | 98 |
| Likely benign | 4 |
| Benign | 2 |
Top pathogenic / likely-pathogenic (5)
| Variant ID | HGVS | Classification |
|---|---|---|
| 1691098 | NM_004521.3(KIF5B):c.1493T>C (p.Leu498Pro) | Pathogenic |
| 563765 | GRCh37/hg19 10p11.22(chr10:31425682-32599180)x1 | Pathogenic |
| 242891 | NM_004521.3(KIF5B):c.2252A>G (p.His751Arg) | Likely pathogenic |
| 3370124 | NM_004521.3(KIF5B):c.833G>A (p.Arg278Gln) | Likely pathogenic |
| 4820584 | NM_004521.3(KIF5B):c.584C>A (p.Thr195Lys) | Likely pathogenic |
SpliceAI
2519 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 10:32015506:AAC:A | donor_loss | 1.0000 |
| 10:32015507:ACC:A | donor_loss | 1.0000 |
| 10:32015508:C:CA | donor_loss | 1.0000 |
| 10:32015532:CA:C | donor_gain | 1.0000 |
| 10:32015544:T:TA | donor_gain | 1.0000 |
| 10:32015655:TTTAG:T | acceptor_gain | 1.0000 |
| 10:32015656:TTAG:T | acceptor_gain | 1.0000 |
| 10:32015657:TAG:T | acceptor_gain | 1.0000 |
| 10:32015658:AG:A | acceptor_gain | 1.0000 |
| 10:32015658:AGC:A | acceptor_loss | 1.0000 |
| 10:32015659:GC:G | acceptor_loss | 1.0000 |
| 10:32015660:C:CC | acceptor_gain | 1.0000 |
| 10:32015663:A:AC | acceptor_gain | 1.0000 |
| 10:32015665:A:AC | acceptor_gain | 1.0000 |
| 10:32015665:A:C | acceptor_gain | 1.0000 |
| 10:32017139:TAAC:T | donor_loss | 1.0000 |
| 10:32017141:A:AC | donor_gain | 1.0000 |
| 10:32017141:ACCA:A | donor_loss | 1.0000 |
| 10:32017142:C:CC | donor_gain | 1.0000 |
| 10:32017142:CCAAT:C | donor_gain | 1.0000 |
| 10:32017146:T:C | donor_gain | 1.0000 |
| 10:32017193:T:TA | donor_gain | 1.0000 |
| 10:32017211:T:TA | donor_gain | 1.0000 |
| 10:32017355:ACCAA:A | acceptor_gain | 1.0000 |
| 10:32017356:CCAA:C | acceptor_gain | 1.0000 |
| 10:32017356:CCAAC:C | acceptor_gain | 1.0000 |
| 10:32017357:CAAC:C | acceptor_gain | 1.0000 |
| 10:32017358:AA:A | acceptor_gain | 1.0000 |
| 10:32017360:C:CC | acceptor_gain | 1.0000 |
| 10:32017365:C:CT | acceptor_gain | 1.0000 |
AlphaMissense
6419 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 10:32017199:A:G | I902T | 1.000 |
| 10:32017199:A:T | I902K | 1.000 |
| 10:32017202:C:G | R901P | 1.000 |
| 10:32017254:C:G | A884P | 1.000 |
| 10:32017262:A:G | L881P | 1.000 |
| 10:32017266:C:G | A880P | 1.000 |
| 10:32017293:C:G | A871P | 1.000 |
| 10:32017304:A:G | L867P | 1.000 |
| 10:32017325:A:G | L860P | 1.000 |
| 10:32017335:G:T | R857S | 1.000 |
| 10:32017337:A:G | L856P | 1.000 |
| 10:32017337:A:T | L856H | 1.000 |
| 10:32017344:C:G | A854P | 1.000 |
| 10:32017345:A:C | N853K | 1.000 |
| 10:32017345:A:T | N853K | 1.000 |
| 10:32017347:T:C | N853D | 1.000 |
| 10:32017349:T:A | D852V | 1.000 |
| 10:32017350:C:G | D852H | 1.000 |
| 10:32017352:C:G | R851P | 1.000 |
| 10:32017357:C:A | L849F | 1.000 |
| 10:32017357:C:G | L849F | 1.000 |
| 10:32017358:A:C | L849W | 1.000 |
| 10:32017358:A:G | L849S | 1.000 |
| 10:32018055:T:A | K847N | 1.000 |
| 10:32018055:T:G | K847N | 1.000 |
| 10:32018057:T:C | K847E | 1.000 |
| 10:32018060:G:C | H846D | 1.000 |
| 10:32018068:G:A | T843I | 1.000 |
| 10:32018071:A:C | L842R | 1.000 |
| 10:32018071:A:G | L842P | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000078993 (10:32027467 G>C), RS1000188233 (10:32050870 C>T), RS1000246887 (10:32018900 T>G), RS1000256272 (10:32056682 T>C), RS1000288354 (10:32012987 C>T), RS1000328453 (10:32034203 A>AG), RS1000361603 (10:32041991 C>A), RS1000439489 (10:32019162 C>T), RS1000470413 (10:32049171 T>A,C), RS1000501651 (10:32015337 T>C), RS1000515008 (10:32032778 G>C), RS1000532382 (10:32052607 A>G), RS1000569136 (10:32048755 T>C), RS1000677310 (10:32055235 G>C,T), RS1000751318 (10:32056505 T>C,G)
Disease associations
OMIM: gene MIM:602809 | disease phenotypes:
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| skeletal dysplasia | Strong | Autosomal dominant |
| osteogenesis imperfecta | Strong | Autosomal dominant |
Mondo (8): intellectual disability (MONDO:0001071), attention deficit-hyperactivity disorder (MONDO:0007743), skeletal dysplasia (MONDO:0018230), ophthalmoplegia (MONDO:0003425), dilated cardiomyopathy (MONDO:0005021), hypertrophic cardiomyopathy (MONDO:0005045), skeletal muscle disorder (MONDO:0020120), osteogenesis imperfecta (MONDO:0019019)
Orphanet (5): Primary bone dysplasia (Orphanet:364526), Rare hypertrophic cardiomyopathy (Orphanet:217569), Dilated cardiomyopathy (Orphanet:217604), Skeletal muscle disease (Orphanet:98472), NON RARE IN EUROPE: Unexplained intellectual disability (Orphanet:319658)
HPO phenotypes
2 total (2 of 2 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0001644 | Dilated cardiomyopathy |
| HP:0001639 | Hypertrophic cardiomyopathy |
GWAS associations
9 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST001715_12 | Bipolar disorder with mood-incongruent psychosis | 5.000000e-06 |
| GCST005025_2 | Anti-saccade response | 9.000000e-06 |
| GCST005956_37 | Waist-to-hip ratio adjusted for BMI | 2.000000e-08 |
| GCST005962_50 | Waist-to-hip ratio adjusted for BMI x sex x age interaction (4df test) | 2.000000e-06 |
| GCST007096_63 | Pulse pressure | 3.000000e-09 |
| GCST007099_45 | Systolic blood pressure | 7.000000e-06 |
| GCST007638_41 | Glycine levels | 9.000000e-09 |
| GCST010796_1269 | Electrocardiogram morphology (amplitude at temporal datapoints) | 5.000000e-09 |
| GCST010796_1270 | Electrocardiogram morphology (amplitude at temporal datapoints) | 4.000000e-08 |
EFO canonical traits (8, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0006874 | antisaccade response measurement |
| EFO:0007788 | BMI-adjusted waist-hip ratio |
| EFO:0008007 | age at assessment |
| EFO:0008343 | sex interaction measurement |
| EFO:0005763 | pulse pressure measurement |
| EFO:0006335 | systolic blood pressure |
| EFO:0009767 | glycine measurement |
| EFO:0004327 | electrocardiography |
MeSH disease descriptors (5)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D002311 | Cardiomyopathy, Dilated | C14.280.195.160; C14.280.238.070; C16.320.488.750 |
| D002312 | Cardiomyopathy, Hypertrophic | C14.280.238.100; C14.280.484.048.750.070.160 |
| D008607 | Intellectual Disability | C10.597.606.360; C23.888.592.604.646; F01.700.687; F03.625.539 |
| D009886 | Ophthalmoplegia | C10.292.562.750; C10.597.622.447; C11.590.472; C23.888.592.636.447 |
| D010013 | Osteogenesis Imperfecta | C05.116.099.708.685; C16.320.737; C17.300.200.540 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (4): CHEMBL3430888 (CHIMERIC PROTEIN), CHEMBL5465390 (CHIMERIC PROTEIN), CHEMBL5864 (SINGLE PROTEIN), CHEMBL6195572 (PROTEIN-PROTEIN INTERACTION)
Molecules with ChEMBL bioactivity
3 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 62,191 (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 |
|---|---|---|---|
| CHEMBL1289601 | LENVATINIB | 4 | 8,784 |
| CHEMBL2105717 | CABOZANTINIB | 4 | 11,177 |
| CHEMBL24828 | VANDETANIB | 4 | 42,230 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
ChEMBL bioactivities
90 potent at pChembl≥5 of 92 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.92 | IC50 | 1.2 | nM | CHEMBL5618101 |
| 8.82 | IC50 | 1.51 | nM | STAUROSPORINE |
| 8.77 | IC50 | 1.7 | nM | CHEMBL4644274 |
| 8.48 | IC50 | 3.3 | nM | CHEMBL4643578 |
| 8.41 | IC50 | 3.89 | nM | CHEMBL5572034 |
| 8.30 | IC50 | 5 | nM | CHEMBL5171764 |
| 8.27 | IC50 | 5.4 | nM | CHEMBL4636056 |
| 8.22 | IC50 | 6 | nM | CHEMBL4634073 |
| 8.20 | IC50 | 6.3 | nM | CHEMBL4639022 |
| 8.15 | IC50 | 7 | nM | CHEMBL169390 |
| 8.05 | IC50 | 8.86 | nM | CHEMBL4790634 |
| 8.00 | IC50 | 10 | nM | LENVATINIB |
| 7.96 | IC50 | 11 | nM | CHEMBL4858720 |
| 7.82 | IC50 | 15 | nM | CHEMBL4874648 |
| 7.72 | IC50 | 19 | nM | CHEMBL4634073 |
| 7.70 | IC50 | 20 | nM | CHEMBL4857808 |
| 7.66 | IC50 | 22 | nM | CHEMBL4859681 |
| 7.51 | IC50 | 31 | nM | CHEMBL4638840 |
| 7.43 | IC50 | 37 | nM | CHEMBL4640601 |
| 7.39 | IC50 | 41 | nM | CHEMBL440727 |
| 7.36 | IC50 | 44 | nM | CHEMBL4877264 |
| 7.36 | IC50 | 43.7 | nM | CHEMBL5620262 |
| 7.28 | IC50 | 53 | nM | CHEMBL3774904 |
| 7.28 | IC50 | 53 | nM | CHEMBL3775169 |
| 7.25 | IC50 | 56 | nM | CHEMBL4636800 |
| 7.16 | IC50 | 70 | nM | CHEMBL4642409 |
| 7.10 | IC50 | 79 | nM | CHEMBL4640989 |
| 7.10 | IC50 | 80.2 | nM | CHEMBL5799517 |
| 7.07 | IC50 | 85 | nM | CHEMBL3774489 |
| 7.05 | IC50 | 90 | nM | CHEMBL4853155 |
| 6.92 | IC50 | 120 | nM | CHEMBL3775557 |
| 6.92 | IC50 | 120 | nM | CHEMBL4636995 |
| 6.89 | IC50 | 129 | nM | CHEMBL5619046 |
| 6.72 | IC50 | 190 | nM | CABOZANTINIB |
| 6.70 | IC50 | 200 | nM | CHEMBL3775934 |
| 6.62 | IC50 | 240 | nM | CHEMBL4854822 |
| 6.58 | IC50 | 260 | nM | CHEMBL3774953 |
| 6.57 | IC50 | 270 | nM | CHEMBL3775511 |
| 6.42 | IC50 | 380 | nM | CHEMBL127907 |
| 6.40 | IC50 | 400 | nM | VANDETANIB |
| 6.34 | IC50 | 460 | nM | CHEMBL3774951 |
| 6.34 | IC50 | 460 | nM | CHEMBL3775560 |
| 6.31 | IC50 | 490 | nM | CHEMBL3775879 |
| 6.30 | IC50 | 500 | nM | CHEMBL478442 |
| 6.24 | IC50 | 570 | nM | CHEMBL3775903 |
| 6.22 | IC50 | 600 | nM | CHEMBL3798883 |
| 6.21 | IC50 | 620 | nM | CHEMBL3775672 |
| 6.21 | IC50 | 610 | nM | CHEMBL4636995 |
| 6.11 | IC50 | 770 | nM | CHEMBL4848347 |
| 6.03 | IC50 | 940 | nM | CHEMBL235851 |
PubChem BioAssay actives
88 with measured affinity, of 198 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-[6-[2-(propan-2-ylamino)ethoxy]imidazo[1,2-b]pyridazin-3-yl]ethynyl]benzamide | 2130928: Inhibition of human KI5B-RET kinase in presence of [gamma33P]-ATP and 10 uM ATP by radiometric HotSpot assay | ic50 | 0.0012 | 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 | 1704869: Inhibition of KIF5B-RET fusion protein (unknown origin) by radiometric assay | ic50 | 0.0015 | uM |
| 3-(3,4-dimethoxyphenyl)-5-N-(1,2,2,6,6-pentamethylpiperidin-4-yl)-6-phenylpyrazolo[1,5-a]pyrimidine-5,7-diamine | 1648939: Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay | ic50 | 0.0017 | uM |
| methyl 4-[4-[7-amino-5-[(1,2,2,6,6-pentamethylpiperidin-4-yl)amino]-6-phenylpyrazolo[1,5-a]pyrimidin-3-yl]benzoyl]piperazine-1-carboxylate | 1648939: Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay | ic50 | 0.0033 | uM |
| N-[(1S)-1-[6-(4-fluoropyrazol-1-yl)-3-pyridinyl]ethyl]-1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxamide | 1895764: Inhibition of KIF5B-RET (unknown origin) assessed as inhibition of RET autophosphorylation expressed in mouse BaF3 cells | ic50 | 0.0050 | uM |
| [4-[7-amino-5-[(1,2,2,6,6-pentamethylpiperidin-4-yl)amino]-6-phenylpyrazolo[1,5-a]pyrimidin-3-yl]phenyl]-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]methanone | 1648939: Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay | ic50 | 0.0054 | uM |
| methyl N-[4-[7-amino-3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxypyrazolo[1,5-a]pyrimidin-6-yl]phenyl]carbamate | 1648939: Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay | ic50 | 0.0060 | uM |
| [4-[7-amino-5-[(1,2,2,6,6-pentamethylpiperidin-4-yl)amino]-6-phenylpyrazolo[1,5-a]pyrimidin-3-yl]phenyl]-(4-methylsulfonylpiperazin-1-yl)methanone | 1648939: Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay | ic50 | 0.0063 | uM |
| 3-(4-amino-7-cyclopentylpyrrolo[2,3-d]pyrimidin-5-yl)phenol | 1774878: Inhibition of KIF5B-RET fusion protein (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 48 hrs by cell proliferation assay | ic50 | 0.0070 | uM |
| 4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[(6-pyridin-3-yl-1H-pyrazolo[5,4-d]pyrimidin-4-yl)oxy]benzamide | 1704869: Inhibition of KIF5B-RET fusion protein (unknown origin) by radiometric assay | ic50 | 0.0089 | uM |
| Lenvatinib | 1204918: Inhibition of KIF5B/RET (unknown origin) autophoshorylation | ic50 | 0.0100 | uM |
| 3-[4-amino-7-[3-(hydroxymethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-5-yl]phenol | 1774878: Inhibition of KIF5B-RET fusion protein (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 48 hrs by cell proliferation assay | ic50 | 0.0110 | uM |
| methyl N-[4-[4-amino-5-(3-amino-4-chlorophenyl)pyrrolo[2,3-d]pyrimidin-7-yl]cyclohexyl]carbamate | 1774878: Inhibition of KIF5B-RET fusion protein (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 48 hrs by cell proliferation assay | ic50 | 0.0150 | uM |
| methyl N-[4-[4-amino-5-(3-amino-4-chlorophenyl)pyrrolo[2,3-d]pyrimidin-7-yl]-1-bicyclo[2.2.2]octanyl]carbamate | 1774878: Inhibition of KIF5B-RET fusion protein (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 48 hrs by cell proliferation assay | ic50 | 0.0200 | uM |
| methyl N-[4-[4-amino-5-(5-amino-4-chloro-2-fluorophenyl)pyrrolo[2,3-d]pyrimidin-7-yl]-1-bicyclo[2.2.2]octanyl]carbamate | 1774878: Inhibition of KIF5B-RET fusion protein (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 48 hrs by cell proliferation assay | ic50 | 0.0220 | uM |
| 3-(3,4-dimethoxyphenyl)-5-N-(1-methylpiperidin-4-yl)-6-phenylpyrazolo[1,5-a]pyrimidine-5,7-diamine | 1648939: Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay | ic50 | 0.0310 | uM |
| 3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-phenylpyrazolo[1,5-a]pyrimidin-7-amine | 1648939: Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay | ic50 | 0.0370 | uM |
| 5-[(6,7-dimethoxyquinazolin-4-yl)amino]-4-fluoro-2-methylphenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.0410 | uM |
| N-[3-(2-cyanopropan-2-yl)-5-(4-methylimidazol-1-yl)phenyl]-2-fluoro-4-methyl-5-[2-[6-(2-morpholin-4-ylethoxy)imidazo[1,2-b]pyridazin-3-yl]ethynyl]benzamide | 2130928: Inhibition of human KI5B-RET kinase in presence of [gamma33P]-ATP and 10 uM ATP by radiometric HotSpot assay | ic50 | 0.0437 | uM |
| 1-[4-[3-[4-amino-5-(3-amino-4-chlorophenyl)pyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]piperazin-1-yl]ethanone | 1774878: Inhibition of KIF5B-RET fusion protein (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 48 hrs by cell proliferation assay | ic50 | 0.0440 | uM |
| 5-[(6,7-dimethoxyquinazolin-4-yl)amino]-2,4-difluorophenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.0530 | uM |
| 3-[(6,7-dimethoxyquinazolin-4-yl)amino]-4-fluorophenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.0530 | uM |
| 3-(3,4-dimethoxyphenyl)-5-N-[3-(dimethylamino)propyl]-6-phenylpyrazolo[1,5-a]pyrimidine-5,7-diamine | 1648939: Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay | ic50 | 0.0560 | uM |
| 3-(3,4-dimethoxyphenyl)-5-[3-(dimethylamino)propoxy]-6-phenylpyrazolo[1,5-a]pyrimidin-7-amine | 1648939: Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay | ic50 | 0.0700 | uM |
| 3-(3,4-dimethoxyphenyl)-6-phenyl-5-piperidin-4-yloxypyrazolo[1,5-a]pyrimidin-7-amine | 1648939: Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay | ic50 | 0.0790 | uM |
| 4-chloro-3-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.0850 | uM |
| 1-[4-[3-[4-amino-5-(4-chloro-3-hydroxyphenyl)pyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]piperazin-1-yl]ethanone | 1774878: Inhibition of KIF5B-RET fusion protein (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 48 hrs by cell proliferation assay | ic50 | 0.0900 | uM |
| 3-[(6,7-dimethoxyquinazolin-4-yl)amino]-2,4-difluorophenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.1200 | uM |
| 3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-(1,3-thiazol-2-yl)pyrazolo[1,5-a]pyrimidin-7-amine | 1648939: Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay | ic50 | 0.1200 | uM |
| 4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-[6-(2-morpholin-4-ylethoxy)imidazo[1,2-b]pyridazin-3-yl]ethynyl]benzamide | 2130928: Inhibition of human KI5B-RET kinase in presence of [gamma33P]-ATP and 10 uM ATP by radiometric HotSpot assay | ic50 | 0.1290 | uM |
| Cabozantinib | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.1900 | uM |
| 3-[(6,7-dimethoxyquinazolin-4-yl)amino]-5-fluorophenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.2000 | uM |
| 1-[4-[3-[4-amino-5-(2-fluoro-5-hydroxyphenyl)pyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]piperazin-1-yl]ethanone | 1774878: Inhibition of KIF5B-RET fusion protein (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 48 hrs by cell proliferation assay | ic50 | 0.2400 | uM |
| 2-chloro-3-[(6,7-dimethoxyquinazolin-4-yl)amino]-4-fluorophenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.2600 | uM |
| 4-chloro-3-[(6,7-dimethoxyquinazolin-4-yl)amino]-2-fluorophenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.2700 | uM |
| 3-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.3800 | uM |
| Vandetanib | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.4000 | uM |
| 2-chloro-3-[(6,7-dimethoxyquinazolin-4-yl)amino]-6-methylphenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.4600 | uM |
| 3-[(6,7-dimethoxyquinazolin-4-yl)amino]-4-methylphenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.4600 | uM |
| 5-[(6,7-dimethoxyquinazolin-4-yl)amino]-2-fluorophenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.4900 | uM |
| 5-[(6,7-dimethoxyquinazolin-4-yl)amino]-2-methylphenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.5000 | uM |
| 3-[(6,7-dimethoxyquinazolin-4-yl)amino]-2-fluorophenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.5700 | uM |
| 4-fluoro-3-[[6-methoxy-7-[3-[2-(trifluoromethyl)pyrrolidin-1-yl]propoxy]quinazolin-4-yl]amino]-2-methylphenol | 1298124: Inhibition of recombinant KIF5B/RET (unknown origin) expressed in IL3 deficient BAF3 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo assay | ic50 | 0.6000 | uM |
| 3-(6,7-dimethoxyquinazolin-4-yl)oxyphenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.6200 | uM |
| 1-[4-[3-[4-amino-5-(3-hydroxyphenyl)pyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]piperazin-1-yl]ethanone | 1774878: Inhibition of KIF5B-RET fusion protein (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 48 hrs by cell proliferation assay | ic50 | 0.7700 | uM |
| 2-chloro-5-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 0.9400 | uM |
| 4-fluoro-3-[[6-methoxy-7-(pyridin-3-ylmethoxy)quinazolin-4-yl]amino]-2-methylphenol | 1298124: Inhibition of recombinant KIF5B/RET (unknown origin) expressed in IL3 deficient BAF3 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo assay | ic50 | 1.1000 | uM |
| 3-[(6,7-dimethoxyquinazolin-4-yl)amino]benzene-1,2-diol | 1283959: Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay | ic50 | 1.1000 | uM |
| 4-fluoro-3-[[6-methoxy-7-(2-methoxyethoxy)quinazolin-4-yl]amino]-2-methylphenol | 1298124: Inhibition of recombinant KIF5B/RET (unknown origin) expressed in IL3 deficient BAF3 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo assay | ic50 | 1.2000 | uM |
| 4-fluoro-3-[[7-[2-(3-fluoropyrrolidin-1-yl)ethoxy]-6-methoxyquinazolin-4-yl]amino]-2-methylphenol | 1298124: Inhibition of recombinant KIF5B/RET (unknown origin) expressed in IL3 deficient BAF3 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo assay | ic50 | 1.3000 | uM |
CTD chemical–gene interactions
36 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | affects expression, decreases expression | 3 |
| bisphenol A | increases expression, affects cotreatment | 2 |
| perfluorooctane sulfonic acid | decreases expression | 2 |
| Nickel | increases expression | 2 |
| Smoke | decreases expression | 2 |
| Tobacco Smoke Pollution | affects expression, increases expression | 2 |
| Cyclosporine | increases expression, increases methylation | 2 |
| FR900359 | decreases phosphorylation | 1 |
| TAK-243 | decreases sumoylation | 1 |
| dicrotophos | decreases expression | 1 |
| pyrogallol 1,3-dimethyl ether | affects cotreatment, decreases expression | 1 |
| sodium arsenite | increases expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | increases expression, affects cotreatment | 1 |
| bisphenol S | affects expression | 1 |
| jinfukang | decreases expression | 1 |
| LDN 193189 | increases expression, affects cotreatment | 1 |
| 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acid | decreases expression | 1 |
| Resveratrol | increases expression, affects cotreatment | 1 |
| Air Pollutants | decreases expression, increases abundance | 1 |
| Benzo(a)pyrene | increases methylation | 1 |
| Furaldehyde | decreases expression, affects cotreatment | 1 |
| Ivermectin | decreases expression | 1 |
| Phenobarbital | affects expression | 1 |
| Phenolsulfonphthalein | affects cotreatment, increases expression | 1 |
| Plant Extracts | affects cotreatment, increases expression | 1 |
| Plant Oils | increases expression | 1 |
| Ribonucleotides | affects binding | 1 |
| Sodium Chloride | affects cotreatment, decreases expression | 1 |
| Tamoxifen | affects expression | 1 |
ChEMBL screening assays
43 unique, capped per target: 37 binding, 6 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL3428796 | Binding | Inhibition of KIF5B/RET (unknown origin) autophoshorylation | Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer. — J Med Chem |
| CHEMBL6091206 | Functional | In vivo PROTAC activity at CRBN/KIF5B-RET-G810C mutant in male BALB/c mouse model implanted with mouse BaF3 cells stably expressing KIF5B-RET-G810C mutant assessed as induction of RET degradation in tumor at 10 mg/kg, ip measured after 3 da | Discovery of an Efficacious RET PROTAC Degrader with Enhanced Antiproliferative Activity against Resistant Cancer Cells Harboring RET Solvent-Front Mutations. — J Med Chem |
Cellosaurus cell lines
11 cell lines: 6 cancer cell line, 5 factor-dependent cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_C5VR | CUTO-22 | Cancer cell line | Female |
| CVCL_C5VS | CUTO-32 | Cancer cell line | Male |
| CVCL_SU83 | HAP1 KIF5B (-) 1 | Cancer cell line | Male |
| CVCL_SU84 | HAP1 KIF5B (-) 2 | Cancer cell line | Male |
| CVCL_UE86 | Ba/F3 KIF5B-RET | Factor-dependent cell line | |
| CVCL_XZ23 | Ba/F3 KIF5B-RET-F744I/G810A | Factor-dependent cell line | |
| CVCL_XZ24 | Ba/F3 KIF5B-RET-V804E | Factor-dependent cell line | |
| CVCL_XZ25 | Ba/F3 KIF5B-RET-V804L | Factor-dependent cell line | |
| CVCL_XZ26 | Ba/F3 KIF5B-RET-V804M | Factor-dependent cell line | |
| CVCL_YD30 | SNU-2612A | Cancer cell line | Male |
Clinical trials (associated diseases)
280 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00131469 | PHASE4 | COMPLETED | Study of Teriparatide (FORTEO) to Treat Adults With Osteogenesis Imperfecta |
| NCT00159419 | PHASE4 | COMPLETED | Bisphosphonate Therapy for Osteogenesis Imperfecta |
| NCT01713231 | PHASE4 | COMPLETED | Effect of High-Dose Vitamin D on Bone Density in Osteogenesis Imperfecta |
| NCT02303873 | PHASE4 | COMPLETED | Efficacy and Safety of Alendronate in Chinese Children or Adolescents With Osteogenesis Imperfecta |
| NCT03735537 | PHASE4 | COMPLETED | Treatment of Osteogenesis Imperfecta With Parathyroid Hormone and Zoledronic Acid |
| NCT04152551 | PHASE4 | RECRUITING | Effects of Bisphosphonates on OI-Related Hearing Loss |
| NCT05657860 | PHASE4 | COMPLETED | Guanfacine Extended Release for the Reduction of Aggression and Self-injurious Behavior Associated With Prader-Willi Syndrome |
| NCT05744479 | PHASE4 | RECRUITING | Metformin for Antipsychotic-induced Weight Gain in Adults With Intellectual Disability |
| NCT06107829 | PHASE4 | WITHDRAWN | Valbenazine Treatment of Tardive Dyskinesia in Adults With Intellectual/Developmental Disabilities |
| NCT06997198 | PHASE4 | NOT_YET_RECRUITING | Deutetrabenazine Treatment for Tardive Dyskinesia in Intellectual/Developmental Disabilities |
| NCT00001305 | PHASE3 | COMPLETED | Growth Hormone Therapy in Osteogenesis Imperfecta |
| NCT00005901 | PHASE3 | COMPLETED | Pamidronate to Treat Osteogenesis Imperfecta in Children |
| NCT00106028 | PHASE3 | COMPLETED | Safety and Efficacy of Risedronate in the Treatment of Osteogenesis Imperfecta in Children |
| NCT00982124 | PHASE3 | COMPLETED | An Efficacy and Safety Trial of Intravenous Zoledronic Acid in Infants Less Than One Year of Age, With Severe Osteogenesis Imperfecta |
| NCT02352753 | PHASE3 | TERMINATED | Multicenter,Single-arm Study to Evaluate Efficacy, Safety, & Pharmacokinetics of Denosumab in Children w/ OI |
| NCT03638128 | PHASE3 | TERMINATED | Open-label Extension of Study 20130173 of Denosumab in Children and Young Adults With Osteogenesis Imperfecta |
| NCT05768854 | PHASE3 | ACTIVE_NOT_RECRUITING | Setrusumab vs Bisphosphonates in Pediatric Subjects With Osteogenesis Imperfecta |
| NCT05972551 | PHASE3 | ACTIVE_NOT_RECRUITING | Study to Evaluate Efficacy and Safety of Romosozumab Compared With Bisphosphonates in Children and Adolescents With Osteogenesis Imperfecta |
| NCT06636071 | PHASE3 | ACTIVE_NOT_RECRUITING | Setrusumab in Pediatric Japanese Subjects With Osteogenesis Imperfecta |
| NCT07366086 | PHASE3 | RECRUITING | Pediatric Safety Follow-up Study of Prior Treatment With Romosozumab for Osteogenesis Imperfecta |
| NCT02270736 | PHASE3 | COMPLETED | Clinical Study to Investigate the Efficacy and Safety of NT 201 Compared to Placebo in the Treatment of Chronic Troublesome Drooling Associated With Neurological Disorders and/or Intellectual Disability |
| NCT00063479 | PHASE2 | COMPLETED | Bisphosphonate Treatment of Osteogenesis Imperfecta |
| NCT00131118 | PHASE2 | COMPLETED | Zoledronic Acid in Children (1 -17 Years) With Severe Osteogenesis Imperfecta |
| NCT01417091 | PHASE2 | COMPLETED | Safety, Pharmacokinetics and Pharmacodynamics of BPS804 in Osteogenesis Imperfecta |
| NCT01679080 | PHASE2 | TERMINATED | The Effect of Treatment With Teriparatide and Zoledronic Acid in Patients With Osteogenesis Imperfecta |
| NCT01799798 | PHASE2 | COMPLETED | Translational Therapy in Patients With Osteogenesis Imperfecta - A Pilot Trial on Treatment With the Rankl-Antibody Denosumab |
| NCT03208582 | PHASE2 | COMPLETED | Do Bisphosphonates Alter the Skeletal Response to Mechanical Stimulation in Children With Osteogenesis Imperfecta? |
| NCT03216486 | PHASE2 | WITHDRAWN | An Exploratory Study of BPS804 Treatment in Adult Patients With Type I, III or IV Osteogenesis Imperfecta |
| NCT05312697 | PHASE2 | TERMINATED | Long-term Extension Study of Setrusumab in Adults With Type I, III, or IV Osteogenesis Imperfecta |
| NCT07062588 | PHASE2 | RECRUITING | Osteogenesis Imperfecta Trial of AGA2115 for ADUlts With COL1A1 and/or COL1A2 GeNetic Variations (IDUN) |
| NCT07557446 | PHASE2 | NOT_YET_RECRUITING | A Dose REgimen-Finding Study of AGA2115 in Chinese Patients With Osteogenesis ImpeRfecta (EIR) |
| NCT02304302 | PHASE2 | COMPLETED | Down Syndrome Memantine Follow-up Study |
| NCT03862950 | PHASE2 | COMPLETED | A Trial of Metformin in Individuals With Fragile X Syndrome (Met) |
| NCT04529226 | PHASE2 | UNKNOWN | Study to Compare Clozapine vs Treatment as Usual in People With Intellectual Disability & Treatment-resistant Psychosis |
| NCT04821856 | PHASE2 | COMPLETED | Evaluation of the Effectiveness of Cannabidiol in Treating Severe Behavioural Problems in Children and Adolescents With Intellectual Disability |
| NCT00705120 | PHASE1 | COMPLETED | Treatment of Severe Osteogenesis Imperfecta by Allogeneic Bone Marrow Transplantation |
| NCT02172885 | PHASE1 | COMPLETED | Mesenchymal Stem Cell Based Therapy for the Treatment of Osteogenesis Imperfecta |
| NCT03064074 | PHASE1 | COMPLETED | Safety of Fresolimumab in the Treatment of Osteogenesis Imperfecta |
| NCT04545554 | PHASE1 | COMPLETED | Study to Evaluate Romosozumab in Children and Adolescents With Osteogenesis Imperfecta |
| NCT05231668 | PHASE1 | TERMINATED | Single Ascending Dose Study of SAR439459 in Adults With Osteogenesis Imperfecta (OI) |
Related Atlas pages
- Associated diseases: skeletal dysplasia, osteogenesis imperfecta
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): ophthalmoplegia, osteogenesis imperfecta, skeletal dysplasia, skeletal muscle disorder