TUBA3E
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Summary
TUBA3E (tubulin alpha 3e, HGNC:20765) is a protein-coding gene on chromosome 2q21.1, encoding Tubulin alpha-3E chain (Q6PEY2). Tubulin is the major constituent of microtubules, a cylinder consisting of laterally associated linear protofilaments composed of alpha- and beta-tubulin heterodimers.
Microtubules of the eukaryotic cytoskeleton perform essential and diverse functions and are composed of a heterodimer of alpha and beta tubulin. The genes encoding these microtubule constituents are part of the tubulin superfamily, which is composed of six distinct families. Genes from the alpha, beta and gamma tubulin families are found in all eukaryotes. The alpha and beta tubulins represent the major components of microtubules, while gamma tubulin plays a critical role in the nucleation of microtubule assembly. This gene encodes an alpha tubulin that highly conserved among species. A missense mutation in this gene has been potentially linked to microlissencephaly and global developmental delay.
Source: NCBI Gene 112714 — RefSeq curated summary.
At a glance
- Gene–disease (curated): complex neurodevelopmental disorder (Limited, GenCC)
- Clinical variants (ClinVar): 8 total — 2 likely-pathogenic
- Druggable target: yes — 21 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_207312
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:20765 |
| Approved symbol | TUBA3E |
| Name | tubulin alpha 3e |
| Location | 2q21.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000152086 |
| Ensembl biotype | protein_coding |
| OMIM | 619918 |
| Entrez | 112714 |
Gene structure
Transcript identifiers
Ensembl transcripts: 1 — 1 protein_coding
ENST00000312988
RefSeq mRNA: 1 — MANE Select: NM_207312
NM_207312
CCDS: CCDS2158
Canonical transcript exons
ENST00000312988 — 5 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001401730 | 130198358 | 130198439 |
| ENSE00002434420 | 130195079 | 130195227 |
| ENSE00002481616 | 130193786 | 130194466 |
| ENSE00002519674 | 130191745 | 130192127 |
| ENSE00002531268 | 130196149 | 130196371 |
Expression profiles
Bgee: expression breadth broad, 74 present calls, max score 89.75.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.0332 / max 36.5379, expressed in 3 samples.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 30618 | 0.0332 | 3 |
Top tissues by expression
106 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| right testis | UBERON:0004534 | 89.75 | gold quality |
| left testis | UBERON:0004533 | 88.32 | gold quality |
| heart left ventricle | UBERON:0002084 | 88.13 | gold quality |
| testis | UBERON:0000473 | 87.83 | gold quality |
| apex of heart | UBERON:0002098 | 86.68 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 83.60 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 83.31 | gold quality |
| heart | UBERON:0000948 | 75.79 | gold quality |
| right atrium auricular region | UBERON:0006631 | 73.19 | gold quality |
| placenta | UBERON:0001987 | 62.71 | gold quality |
| left uterine tube | UBERON:0001303 | 54.51 | gold quality |
| body of uterus | UBERON:0009853 | 54.05 | gold quality |
| fallopian tube | UBERON:0003889 | 53.07 | gold quality |
| endocervix | UBERON:0000458 | 51.67 | gold quality |
| myometrium | UBERON:0001296 | 50.49 | gold quality |
| uterus | UBERON:0000995 | 48.61 | gold quality |
| smooth muscle tissue | UBERON:0001135 | 48.43 | gold quality |
| stromal cell of endometrium | CL:0002255 | 47.93 | gold quality |
| bone marrow cell | CL:0002092 | 46.69 | gold quality |
| uterine cervix | UBERON:0000002 | 45.08 | gold quality |
| endometrium | UBERON:0001295 | 44.65 | gold quality |
| right uterine tube | UBERON:0001302 | 43.67 | silver quality |
| hypothalamus | UBERON:0001898 | 42.12 | gold quality |
| metanephros cortex | UBERON:0010533 | 41.28 | gold quality |
| bone marrow | UBERON:0002371 | 41.22 | gold quality |
| ectocervix | UBERON:0012249 | 40.70 | gold quality |
| left ovary | UBERON:0002119 | 40.52 | gold quality |
| ganglionic eminence | UBERON:0004023 | 40.48 | gold quality |
| cortical plate | UBERON:0005343 | 40.23 | gold quality |
| liver | UBERON:0002107 | 40.22 | silver quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 2.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-GEOD-134144 | yes | 29.86 |
| E-ANND-3 | yes | 10.40 |
Regulation
Is transcription factor: no
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | tuba7l | ENSDARG00000104643 |
| rattus_norvegicus | Tuba3a | ENSRNOG00000031707 |
| drosophila_melanogaster | alphaTub84B | FBGN0003884 |
| drosophila_melanogaster | alphaTub84D | FBGN0003885 |
Paralogs (23): TUBG2 (ENSG00000037042), TUBE1 (ENSG00000074935), TUBA3D (ENSG00000075886), TUBB1 (ENSG00000101162), TUBB4A (ENSG00000104833), TUBD1 (ENSG00000108423), TUBA1B (ENSG00000123416), TUBA4A (ENSG00000127824), TUBG1 (ENSG00000131462), TUBB2A (ENSG00000137267), TUBB2B (ENSG00000137285), TUBA1A (ENSG00000167552), TUBA1C (ENSG00000167553), TUBB8B (ENSG00000173213), TUBB6 (ENSG00000176014), TUBAL3 (ENSG00000178462), TUBA8 (ENSG00000183785), TUBB4B (ENSG00000188229), TUBB (ENSG00000196230), TUBA3C (ENSG00000198033), TUBA4B (ENSG00000243910), TUBB3 (ENSG00000258947), TUBB8 (ENSG00000261456)
Protein
Protein identifiers
Tubulin alpha-3E chain — Q6PEY2 (reviewed: Q6PEY2)
Alternative names: Alpha-tubulin 3E
All UniProt accessions (1): Q6PEY2
UniProt curated annotations — full annotation on UniProt →
Function. Tubulin is the major constituent of microtubules, a cylinder consisting of laterally associated linear protofilaments composed of alpha- and beta-tubulin heterodimers. Microtubules grow by the addition of GTP-tubulin dimers to the microtubule end, where a stabilizing cap forms. Below the cap, tubulin dimers are in GDP-bound state, owing to GTPase activity of alpha-tubulin.
Subunit / interactions. Dimer of alpha and beta chains. A typical microtubule is a hollow water-filled tube with an outer diameter of 25 nm and an inner diameter of 15 nM. Alpha-beta heterodimers associate head-to-tail to form protofilaments running lengthwise along the microtubule wall with the beta-tubulin subunit facing the microtubule plus end conferring a structural polarity. Microtubules usually have 13 protofilaments but different protofilament numbers can be found in some organisms and specialized cells.
Subcellular location. Cytoplasm. Cytoskeleton.
Post-translational modifications. Some glutamate residues at the C-terminus are polyglutamylated, resulting in polyglutamate chains on the gamma-carboxyl group. Polyglutamylation plays a key role in microtubule severing by spastin (SPAST). SPAST preferentially recognizes and acts on microtubules decorated with short polyglutamate tails: severing activity by SPAST increases as the number of glutamates per tubulin rises from one to eight, but decreases beyond this glutamylation threshold. Glutamylation is also involved in cilia motility. Some glutamate residues at the C-terminus are monoglycylated but not polyglycylated due to the absence of functional TTLL10 in human. Monoglycylation is mainly limited to tubulin incorporated into cilia and flagella axonemes, which is required for their stability and maintenance. Flagella glycylation controls sperm motility. Both polyglutamylation and monoglycylation can coexist on the same protein on adjacent residues, and lowering glycylation levels increases polyglutamylation, and reciprocally. Acetylation of alpha chains at Lys-40 is located inside the microtubule lumen. This modification has been correlated with increased microtubule stability, intracellular transport and ciliary assembly. Methylation of alpha chains at Lys-40 is found in mitotic microtubules and is required for normal mitosis and cytokinesis contributing to genomic stability. Nitration of Tyr-450 is irreversible and interferes with normal dynein intracellular distribution. Undergoes a tyrosination/detyrosination cycle, the cyclic removal and re-addition of a C-terminal tyrosine residue by the enzymes tubulin tyrosine carboxypeptidase (MATCAP1/KIAA0895L, VASH1 or VASH2) and tubulin tyrosine ligase (TTL), respectively. Tyrosination promotes microtubule interaction with CAP-Gly domain-containing proteins such as CLIP1, CLIP2 and DCTN1. Tyrosination regulates the initiation of dynein-dynactin motility via interaction with DCTN1, which brings the dynein-dynactin complex into contact with microtubules. In neurons, tyrosinated tubulins mediate the initiation of retrograde vesicle transport. Detyrosination is involved in metaphase plate congression by guiding chromosomes during mitosis: detyrosination promotes interaction with CENPE, promoting pole-proximal transport of chromosomes toward the equator. Detyrosination increases microtubules-dependent mechanotransduction in dystrophic cardiac and skeletal muscle. In cardiomyocytes, detyrosinated microtubules are required to resist to contractile compression during contraction: detyrosination promotes association with desmin (DES) at force-generating sarcomeres, leading to buckled microtubules and mechanical resistance to contraction.
Domain organisation. The MREC motif may be critical for tubulin autoregulation.
Similarity. Belongs to the tubulin family.
RefSeq proteins (1): NP_997195* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000217 | Tubulin | Family |
| IPR002452 | Alpha_tubulin | Family |
| IPR003008 | Tubulin_FtsZ_GTPase | Domain |
| IPR008280 | Tub_FtsZ_C | Homologous_superfamily |
| IPR017975 | Tubulin_CS | Conserved_site |
| IPR018316 | Tubulin/FtsZ_2-layer-sand-dom | Domain |
| IPR023123 | Tubulin_C | Homologous_superfamily |
| IPR036525 | Tubulin/FtsZ_GTPase_sf | Homologous_superfamily |
| IPR037103 | Tubulin/FtsZ-like_C | Homologous_superfamily |
Pfam: PF00091, PF03953
Catalyzed reactions (Rhea), 1 shown:
- GTP + H2O = GDP + phosphate + H(+) (RHEA:19669)
UniProt features (23 total): binding site 9, sequence variant 5, modified residue 4, chain 2, site 1, short sequence motif 1, active site 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q6PEY2-F1 | 91.38 | 0.79 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Catalytic / active sites (2): 450 (involved in polymerization); 254
Ligand- & substrate-binding residues (9): 179; 206; 228; 11; 71; 71; 140; 144; 145
Post-translational modifications (4): 40, 282, 439, 450
Function
Pathways and Gene Ontology
Reactome pathways
82 pathways
| ID | Pathway |
|---|---|
| R-HSA-1445148 | Translocation of SLC2A4 (GLUT4) to the plasma membrane |
| R-HSA-190840 | Microtubule-dependent trafficking of connexons from Golgi to the plasma membrane |
| R-HSA-190861 | Gap junction assembly |
| R-HSA-2132295 | MHC class II antigen presentation |
| R-HSA-2467813 | Separation of Sister Chromatids |
| R-HSA-2500257 | Resolution of Sister Chromatid Cohesion |
| R-HSA-3371497 | HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand |
| R-HSA-380320 | Recruitment of NuMA to mitotic centrosomes |
| R-HSA-389960 | Formation of tubulin folding intermediates by CCT/TriC |
| R-HSA-389977 | Post-chaperonin tubulin folding pathway |
| R-HSA-437239 | Recycling pathway of L1 |
| R-HSA-5620920 | Cargo trafficking to the periciliary membrane |
| R-HSA-5626467 | RHO GTPases activate IQGAPs |
| R-HSA-5663220 | RHO GTPases Activate Formins |
| R-HSA-6807878 | COPI-mediated anterograde transport |
| R-HSA-6811434 | COPI-dependent Golgi-to-ER retrograde traffic |
| R-HSA-6811436 | COPI-independent Golgi-to-ER retrograde traffic |
| R-HSA-68877 | Mitotic Prometaphase |
| R-HSA-8852276 | The role of GTSE1 in G2/M progression after G2 checkpoint |
| R-HSA-8955332 | Carboxyterminal post-translational modifications of tubulin |
| R-HSA-9609690 | HCMV Early Events |
| R-HSA-9609736 | Assembly and cell surface presentation of NMDA receptors |
| R-HSA-9619483 | Activation of AMPK downstream of NMDARs |
| R-HSA-9646399 | Aggrephagy |
| R-HSA-9648025 | EML4 and NUDC in mitotic spindle formation |
| R-HSA-9668328 | Sealing of the nuclear envelope (NE) by ESCRT-III |
| R-HSA-983189 | Kinesins |
| R-HSA-9833482 | PKR-mediated signaling |
| R-HSA-5617833 | Cilium Assembly |
| R-HSA-109582 | Hemostasis |
MSigDB gene sets: 125 (showing top):
E2F_Q4_01, BORCZUK_MALIGNANT_MESOTHELIOMA_UP, REACTOME_ADAPTIVE_IMMUNE_SYSTEM, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, CMYB_01, MITSIADES_RESPONSE_TO_APLIDIN_DN, REACTOME_MEMBRANE_TRAFFICKING, GOBP_MITOTIC_CELL_CYCLE, REACTOME_GAP_JUNCTION_ASSEMBLY, KAAB_FAILED_HEART_VENTRICLE_DN, REACTOME_TRANSMISSION_ACROSS_CHEMICAL_SYNAPSES, E2F_Q6_01, MORF_PPP1CC, GOMF_STRUCTURAL_CONSTITUENT_OF_CYTOSKELETON, REACTOME_POST_CHAPERONIN_TUBULIN_FOLDING_PATHWAY
GO Biological Process (3): microtubule cytoskeleton organization (GO:0000226), mitotic cell cycle (GO:0000278), microtubule-based process (GO:0007017)
GO Molecular Function (6): structural constituent of cytoskeleton (GO:0005200), GTP binding (GO:0005525), hydrolase activity (GO:0016787), metal ion binding (GO:0046872), nucleotide binding (GO:0000166), protein binding (GO:0005515)
GO Cellular Component (6): nucleus (GO:0005634), cytoplasm (GO:0005737), microtubule (GO:0005874), cilium (GO:0005929), microtubule cytoskeleton (GO:0015630), cytoskeleton (GO:0005856)
Reactome top-level categories
Rollup of top-17 pathways:
| Category | Pathways |
|---|---|
| Mitotic Prometaphase | 2 |
| RHO GTPase Effectors | 2 |
| Golgi-to-ER retrograde transport | 2 |
| Membrane Trafficking | 1 |
| Transport of connexons to the plasma membrane | 1 |
| Gap junction trafficking | 1 |
| Adaptive Immune System | 1 |
| Mitotic Anaphase | 1 |
| Cellular responses to stress | 1 |
| Cooperation of Prefoldin and TriC/CCT in actin and tubulin folding | 1 |
| Protein folding | 1 |
| L1CAM interactions | 1 |
| Assembly of the 9+0 primary cilium | 1 |
| ER to Golgi Anterograde Transport | 1 |
| M Phase | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cytoskeleton organization | 2 |
| cytoskeleton | 2 |
| microtubule-based process | 1 |
| cell cycle | 1 |
| mitotic nuclear division | 1 |
| cellular process | 1 |
| structural molecule activity | 1 |
| guanyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| catalytic activity | 1 |
| cation binding | 1 |
| nucleoside phosphate binding | 1 |
| heterocyclic compound binding | 1 |
| binding | 1 |
| intracellular membrane-bounded organelle | 1 |
| intracellular anatomical structure | 1 |
| cellular anatomical structure | 1 |
| microtubule cytoskeleton | 1 |
| polymeric cytoskeletal fiber | 1 |
| intraciliary transport particle | 1 |
| membrane-bounded organelle | 1 |
| plasma membrane bounded cell projection | 1 |
| intracellular membraneless organelle | 1 |
Protein interactions and networks
STRING
3366 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| TUBA3E | TUBB | P05218 | 886 |
| TUBA3E | TUBB2A | Q13885 | 886 |
| TUBA3E | TUBB6 | Q9BUF5 | 811 |
| TUBA3E | TUBB4A | P04350 | 809 |
| TUBA3E | TUBB1 | Q9H4B7 | 807 |
| TUBA3E | TUBB8 | Q3ZCM7 | 807 |
| TUBA3E | TUBB2B | Q9BVA1 | 806 |
| TUBA3E | TUBB4B | P05217 | 806 |
| TUBA3E | TUBB3 | Q13509 | 804 |
| TUBA3E | ROBO3 | Q96MS0 | 769 |
| TUBA3E | HTATIP2 | Q9BUP3 | 761 |
| TUBA3E | HDAC6 | Q9UBN7 | 505 |
| TUBA3E | TUB | P50607 | 457 |
| TUBA3E | PRKN | O60260 | 455 |
| TUBA3E | EEF1A1 | P04719 | 451 |
IntAct
33 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| TUBA3E | NMI | psi-mi:“MI:0915”(physical association) | 0.720 |
| NMI | TUBA3E | psi-mi:“MI:0915”(physical association) | 0.720 |
| FHL3 | TUBA3E | psi-mi:“MI:0915”(physical association) | 0.560 |
| TUBA3E | TCP11L2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| TUBA3E | PFDN6 | psi-mi:“MI:0915”(physical association) | 0.400 |
| FER1L5 | psi-mi:“MI:0915”(physical association) | 0.400 | |
| GNAT3 | psi-mi:“MI:0915”(physical association) | 0.400 | |
| TUBA3E | psi-mi:“MI:0915”(physical association) | 0.370 | |
| KATNAL1 | CDK1 | psi-mi:“MI:0914”(association) | 0.350 |
| KATNA1 | AURKA | psi-mi:“MI:0914”(association) | 0.350 |
| KATNAL2 | CDK1 | psi-mi:“MI:0914”(association) | 0.350 |
| KATNB1 | TUBA8 | psi-mi:“MI:0914”(association) | 0.350 |
| NEK4 | E2F8 | psi-mi:“MI:0914”(association) | 0.350 |
| TUBA3E | CCT2 | psi-mi:“MI:0914”(association) | 0.350 |
| PAK1 | psi-mi:“MI:0914”(association) | 0.350 | |
| VAV1 | psi-mi:“MI:0914”(association) | 0.350 | |
| P | psi-mi:“MI:0914”(association) | 0.350 | |
| OSGIN1 | TUBA3E | psi-mi:“MI:0914”(association) | 0.350 |
| K3 | ATP6AP2 | psi-mi:“MI:0914”(association) | 0.350 |
| SNW1 | psi-mi:“MI:0914”(association) | 0.350 | |
| TUBA3E | rep | psi-mi:“MI:2364”(proximity) | 0.270 |
| TUBA3E | FHL3 | psi-mi:“MI:0915”(physical association) | 0.000 |
| TUBA3E | NMI | psi-mi:“MI:0915”(physical association) | 0.000 |
BioGRID (64): TUBA3E (Two-hybrid), CCT7 (Affinity Capture-MS), CCT3 (Affinity Capture-MS), CCT2 (Affinity Capture-MS), TCP11L2 (Affinity Capture-MS), TUBA3E (Co-fractionation), TUBA3E (Co-fractionation), TUBA3E (Affinity Capture-MS), TUBA3E (Affinity Capture-MS), TCP11L2 (Affinity Capture-MS), CCT2 (Affinity Capture-MS), TUBA3E (Affinity Capture-MS), TUBA3E (Affinity Capture-MS), TUBA3E (Affinity Capture-MS), TUBA3E (Affinity Capture-MS)
ESM2 similar proteins: A5A6J1, P02550, P02552, P05213, P05214, P06603, P06604, P06605, P08537, P09644, P0DPH7, P0DPH8, P18258, P18288, P30436, P34690, P36220, P41383, P52273, P68360, P68361, P68362, P68363, P68365, P68366, P68367, P68368, P68369, P68370, P68373, P81947, P81948, Q06331, Q28IX8, Q2HJ86, Q2XVP4, Q32KN8, Q3ZCJ7, Q4R538, Q52PV9
Diamond homologs: A5A6J1, B9DGT7, B9DHQ0, O22347, P02550, P02552, P04106, P05213, P05214, P06603, P06604, P06605, P08537, P09204, P09205, P09243, P09644, P0DPH7, P0DPH8, P10872, P10873, P11237, P11480, P11481, P14640, P14641, P14642, P18258, P18288, P28268, P28287, P29511, P30436, P33623, P33625, P33629, P34690, P36220, P41351, P41383
SIGNOR signaling
5 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| NUMA1 | up-regulates | TUBA3E | binding |
| TTL | down-regulates | TUBA3E | tyrosination |
| “Elongator complex” | “up-regulates activity” | TUBA3E | acetylation |
| TUBA3E | up-regulates | Neuron_migration | |
| ATAT1 | “up-regulates quantity by stabilization” | TUBA3E | acetylation |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 24 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.
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| cell division | 5 | 11.0× | 6e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
8 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 2 |
| Uncertain significance | 1 |
| Likely benign | 1 |
| Benign | 3 |
Top pathogenic / likely-pathogenic (2)
| Variant ID | HGVS | Classification |
|---|---|---|
| 562617 | GRCh37/hg19 2q21.1(chr2:130874475-131765997)x1 | Likely pathogenic |
| 929341 | GRCh37/hg19 2q14.3-21.2(chr2:122952356-133826358)x1 | Likely pathogenic |
SpliceAI
861 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 2:130195060:TGAA:T | donor_gain | 1.0000 |
| 2:130195075:TTAC:T | donor_loss | 1.0000 |
| 2:130195076:TACCA:T | donor_loss | 1.0000 |
| 2:130195077:A:AC | donor_gain | 1.0000 |
| 2:130195077:A:C | donor_loss | 1.0000 |
| 2:130195077:AC:A | donor_gain | 1.0000 |
| 2:130195078:C:CG | donor_loss | 1.0000 |
| 2:130195078:C:CT | donor_gain | 1.0000 |
| 2:130195078:CC:C | donor_gain | 1.0000 |
| 2:130195078:CCA:C | donor_gain | 1.0000 |
| 2:130195078:CCAG:C | donor_gain | 1.0000 |
| 2:130195078:CCAGT:C | donor_gain | 1.0000 |
| 2:130195223:TTCAT:T | acceptor_gain | 1.0000 |
| 2:130195224:TCAT:T | acceptor_gain | 1.0000 |
| 2:130195225:CAT:C | acceptor_gain | 1.0000 |
| 2:130195225:CATC:C | acceptor_gain | 1.0000 |
| 2:130195226:AT:A | acceptor_gain | 1.0000 |
| 2:130195228:C:CC | acceptor_gain | 1.0000 |
| 2:130195229:T:G | acceptor_loss | 1.0000 |
| 2:130195231:C:CT | acceptor_gain | 1.0000 |
| 2:130195232:A:T | acceptor_gain | 1.0000 |
| 2:130196143:ACCT:A | donor_loss | 1.0000 |
| 2:130196145:CTA:C | donor_loss | 1.0000 |
| 2:130196146:TA:T | donor_loss | 1.0000 |
| 2:130196147:A:AC | donor_gain | 1.0000 |
| 2:130196147:AC:A | donor_loss | 1.0000 |
| 2:130196148:C:CC | donor_gain | 1.0000 |
| 2:130196148:CCGA:C | donor_gain | 1.0000 |
| 2:130196368:CGCG:C | acceptor_gain | 1.0000 |
| 2:130196370:CG:C | acceptor_gain | 1.0000 |
AlphaMissense
2958 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 2:130192064:C:G | A374P | 1.000 |
| 2:130192096:A:T | V363D | 1.000 |
| 2:130192116:G:C | N356K | 1.000 |
| 2:130192116:G:T | N356K | 1.000 |
| 2:130193880:C:A | G321V | 1.000 |
| 2:130193880:C:T | G321E | 1.000 |
| 2:130193881:C:A | G321W | 1.000 |
| 2:130193881:C:G | G321R | 1.000 |
| 2:130193881:C:T | G321R | 1.000 |
| 2:130193882:C:A | R320S | 1.000 |
| 2:130193882:C:G | R320S | 1.000 |
| 2:130193883:C:A | R320M | 1.000 |
| 2:130193883:C:G | R320T | 1.000 |
| 2:130196300:G:C | C25W | 1.000 |
| 2:130196307:A:G | L23P | 1.000 |
| 2:130192063:G:T | A374D | 0.999 |
| 2:130192078:G:T | A369D | 0.999 |
| 2:130192105:G:C | P360R | 0.999 |
| 2:130192105:G:T | P360H | 0.999 |
| 2:130192120:A:T | I355N | 0.999 |
| 2:130193874:A:T | V323E | 0.999 |
| 2:130193887:A:C | Y319D | 0.999 |
| 2:130194021:G:T | P274Q | 0.999 |
| 2:130194110:A:C | F244L | 0.999 |
| 2:130194110:A:T | F244L | 0.999 |
| 2:130194112:A:G | F244L | 0.999 |
| 2:130194123:G:T | A240D | 0.999 |
| 2:130194135:G:A | S236F | 0.999 |
| 2:130195197:A:G | L86P | 0.999 |
| 2:130196286:A:T | I30N | 0.999 |
dbSNP variants (sampled 300 via entrez): RS1000227143 (2:130193270 A>T), RS1000510490 (2:130194562 G>C), RS1003011961 (2:130196529 C>A,T), RS1003292081 (2:130200029 G>A), RS1003846571 (2:130196622 T>G), RS1004393243 (2:130191621 TAC>T), RS1004409392 (2:130191397 A>G), RS1005519264 (2:130200310 G>A), RS1007243911 (2:130194519 C>A,T), RS1008864865 (2:130195294 G>A,C), RS1010865143 (2:130191674 G>A), RS1011175829 (2:130198609 G>A,T), RS1012994670 (2:130200294 G>C), RS1013716947 (2:130193330 T>C,G), RS1013770858 (2:130193672 C>T)
Disease associations
OMIM: gene MIM:619918 | disease phenotypes:
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| complex neurodevelopmental disorder | Limited | Autosomal recessive |
Mondo (2): breast ductal adenocarcinoma (MONDO:0005590), complex neurodevelopmental disorder (MONDO:0100038)
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
0 associations (top):
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D018270 | Carcinoma, Ductal, Breast | C04.557.470.200.025.232.500; C04.557.470.615.132.500; C04.588.180.390; C17.800.090.500.390 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (3): CHEMBL2095182 (PROTEIN COMPLEX GROUP), CHEMBL3832941 (PROTEIN FAMILY), CHEMBL6067579 (PROTEIN-PROTEIN INTERACTION)
Molecules with ChEMBL bioactivity
21 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,641,397 (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 |
|---|---|---|---|
| CHEMBL107 | COLCHICINE | 4 | 93,932 |
| CHEMBL159 | VINBLASTINE | 4 | 412,636 |
| CHEMBL33 | LEVOFLOXACIN ANHYDROUS | 4 | 43,403 |
| CHEMBL3545252 | DOCETAXEL | 4 | 1,009 |
| CHEMBL364713 | NOSCAPINE | 4 | 14,987 |
| CHEMBL378544 | VINBLASTINE SULFATE | 4 | 32,829 |
| CHEMBL428647 | PACLITAXEL | 4 | 332,542 |
| CHEMBL5315124 | LEVOFLOXACIN | 4 | 189 |
| CHEMBL553025 | VINORELBINE | 4 | 142,159 |
| CHEMBL571546 | TIRBANIBULIN | 4 | 1,192 |
| CHEMBL61 | PODOFILOX | 4 | 37,640 |
| CHEMBL90555 | VINCRISTINE | 4 | 268,031 |
| CHEMBL92 | DOCETAXEL ANHYDROUS | 4 | 196,686 |
| CHEMBL94657 | PATUPILONE | 3 | 14,934 |
| CHEMBL20684 | ABT-751 | 2 | 2,238 |
| CHEMBL292702 | MAYTANSINE | 2 | 9,300 |
| CHEMBL39541 | DOLASTATIN-10 | 2 | 1,380 |
| CHEMBL49642 | INDIBULIN | 2 | 963 |
| CHEMBL528271 | PARBENDAZOLE | 2 | 6,102 |
| CHEMBL9514 | NOCODAZOLE | 2 | 29,245 |
| CHEMBL246600 | COMBRETASTATIN | 1 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
ChEMBL bioactivities
1159 potent at pChembl≥5 of 1310 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
1088 with measured affinity, of 5775 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 |
|---|---|---|---|---|
| (Z)-1-[4-bromo-2-(4-fluorophenyl)-1-benzofuran-7-yl]-3-(4-methoxyphenyl)prop-2-en-1-one | 1882651: Inhibition of tubulin polymerization (unknown origin) measured every 3 secs for 1 hr by spectroflourimetric analysis | ic50 | 0.0001 | uM |
| (Z)-1-[4-bromo-2-(4-fluorophenyl)-1-benzofuran-7-yl]-3-[4-(trifluoromethoxy)phenyl]prop-2-en-1-one | 1882651: Inhibition of tubulin polymerization (unknown origin) measured every 3 secs for 1 hr by spectroflourimetric analysis | ic50 | 0.0002 | uM |
| Vinorelbine | 1993632: Inhibition of tubulin polymerization (unknown origin) | ic50 | 0.0003 | uM |
| (2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-N-[(3R,4S,5S)-3-methoxy-1-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide | 270819: Inhibition of tubulin polymerization | ic50 | 0.0005 | uM |
| (2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-N-[(3R,4S,5S)-3-methoxy-1-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-(2-pyridin-2-ylethylamino)propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide | 1896115: Binding affinity to tubulin (unknown origin) | ic50 | 0.0012 | uM |
| (3Z,6Z)-3-[(5-tert-butyl-1H-imidazol-4-yl)methylidene]-6-phenacylidenepiperazine-2,5-dione | 1587857: Inhibition of tubulin polymerization (unknown origin) | ic50 | 0.0014 | uM |
| (3Z,6Z)-3-[(5-tert-butyl-1H-imidazol-4-yl)methylidene]-6-[(2,5-difluorophenyl)methylidene]piperazine-2,5-dione | 1587857: Inhibition of tubulin polymerization (unknown origin) | ic50 | 0.0026 | uM |
| 3-hydroxy-2-[N-[2-(methoxymethyl)-1-benzofuran-7-yl]-C-methylcarbonimidoyl]-5-phenylcyclohex-2-en-1-one | 2034736: Displacement of fluorescent probe (R)-(+)-ethyl 5-amino2-methyl-1,2-dihydro-3-phenylpyrido[3,4-b]pyrazin-7-ylcarbamate from tubulin colchicine binding site (unknown origin) assessed as dissociation constant | kd | 0.0030 | uM |
| 2-methoxy-5-[(Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenol | 1862628: Inhibition of tubulin polymerization in human HeLa cells assessed as microtubule network polymerization after 30 mins by immunofluorescence analysis | ic50 | 0.0030 | uM |
| Colchicine | 2074087: Inhibition of microtubule polymerization in human K562 cells measured for 60 mins by fluorescence based analysis | ic50 | 0.0030 | uM |
| (1S,3S,7S,10R,11S,12S,16R)-7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-[(E)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione | 1408257: Inhibition of tubulin polymerization in human MCF7 cells assessed as induction of mitotic arrest | ic50 | 0.0035 | uM |
| tert-butyl (3R,4S,5S)-4-[[(2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-3-methylbutanoyl]-methylamino]-3-methoxy-5-methylheptanoate | 1896110: Inhibition of tubulin (unknown origin) polymerization assessed as reduction in microtubule formation measured for 20 mins by spectrophotometric analysis | ic50 | 0.0042 | uM |
| 3-methoxy-6-[4-(3,4,5-trimethoxyphenyl)-1H-pyrazol-5-yl]benzene-1,2-diol | 1929685: Inhibition of tubulin polymerization in human SH-SY5Y cells incubated for 24 hrs by SDS-PAGE based analysis | ic50 | 0.0054 | uM |
| 2-methoxy-5-[1-(3,4,5-trimethoxyphenyl)ethenyl]phenol | 1862628: Inhibition of tubulin polymerization in human HeLa cells assessed as microtubule network polymerization after 30 mins by immunofluorescence analysis | ic50 | 0.0060 | uM |
| (E)-1-[1-(4-chlorophenyl)-5-methyltriazol-4-yl]-3-(3,4-dimethoxyphenyl)prop-2-en-1-one | 1689700: Inhibition of Tubulin in human RPMI-8226 cells incubated for 2 hrs by ELISA | ic50 | 0.0098 | uM |
| N-(1,3-benzodioxol-5-yl)-5-[2-(3,5-dimethoxyphenoxy)-3-pyridinyl]-1H-1,2,4-triazol-3-amine | 256882: Displacement of [3H]colchicine from tubulin | ki | 0.0100 | uM |
| N-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-[2-(pyridin-2-ylmethylamino)phenyl]-1,3-oxazol-2-amine | 261214: Displacement of [3H]colchicine from tubulin at 65 nM | ic50 | 0.0100 | uM |
| [(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] acetate | 2126113: Displacement of fluorescent Maytansine probe from tubulin (unknown origin) assessed as dissociation constant by competitive binding based fluorescence anisotropy | kd | 0.0110 | uM |
| [(1S,2R,3S,5S,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[acetyl(methyl)amino]propanoate | 2126113: Displacement of fluorescent Maytansine probe from tubulin (unknown origin) assessed as dissociation constant by competitive binding based fluorescence anisotropy | kd | 0.0140 | uM |
| N-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-[2-(3,5-dimethoxyphenoxy)-3-pyridinyl]-1H-1,2,4-triazol-3-amine | 256882: Displacement of [3H]colchicine from tubulin | ki | 0.0200 | uM |
| methyl (13S,15S,17S)-13-[(1R,9R,10S,11R,12R,19R)-10-(1-diethoxyphosphorylhexylcarbamoyl)-12-ethyl-10,11-dihydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraen-4-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraene-13-carboxylate | 214333: The compound tested for the inhibition of tubulin polymerization. | ic50 | 0.0200 | uM |
| (E)-3-[5-[(2-cyanoquinolin-4-yl)-methylamino]-2-methoxyphenyl]-N-hydroxyprop-2-enamide | 1862628: Inhibition of tubulin polymerization in human HeLa cells assessed as microtubule network polymerization after 30 mins by immunofluorescence analysis | ic50 | 0.0200 | uM |
| [(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] hept-6-ynoate | 2126113: Displacement of fluorescent Maytansine probe from tubulin (unknown origin) assessed as dissociation constant by competitive binding based fluorescence anisotropy | kd | 0.0200 | uM |
| N-(4-methoxyphenyl)-N,5-dimethylfuro[2,3-d]pyrimidin-4-amine | 1635267: Induction of microtubule depolymerization in human A10 cells incubated for 18 hrs by indirect immunofluorescence analysis | ec50 | 0.0240 | uM |
| (2R,3R)-3-ethyl-2-[(E,2R,3S,4R,5S)-2-hydroxy-4-methoxy-3,5-dimethylnon-7-enyl]-2,3-dihydropyran-6-one | 1572465: Inhibition of tubulin alpha in human A2780 cells assessed as reduction in cell growth | ic50 | 0.0260 | uM |
| N-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-[2-(pyridin-3-ylmethylamino)-3-pyridinyl]-1,3,4-oxadiazol-2-amine | 261214: Displacement of [3H]colchicine from tubulin at 65 nM | ic50 | 0.0300 | uM |
| N-(1,3-benzodioxol-5-yl)-5-[2-(pyridin-4-ylmethylamino)-3-pyridinyl]-1,3,4-oxadiazol-2-amine | 261214: Displacement of [3H]colchicine from tubulin at 65 nM | ic50 | 0.0300 | uM |
| N-(1,3-benzodioxol-5-yl)-5-[2-(pyridin-2-ylmethylamino)-3-pyridinyl]-1,3,4-oxadiazol-2-amine | 261214: Displacement of [3H]colchicine from tubulin at 65 nM | ic50 | 0.0300 | uM |
| Paclitaxel | 260235: Effect on induction of mitotic arrest by phosphohistone H3 (pH3) assay | ec50 | 0.0310 | uM |
| 6-(3-chloro-6,11,11-trioxobenzo[b][1,4]benzothiazepin-5-yl)-N-hydroxyhexanamide | 580932: Inhibition of HDAC activity in human NB4 cells assessed as acetylated tubulin after 24 hrs by Western blot analysis | ec50 | 0.0400 | uM |
| N,5-dimethyl-N-(4-methylsulfanylphenyl)furo[2,3-d]pyrimidin-4-amine | 1635267: Induction of microtubule depolymerization in human A10 cells incubated for 18 hrs by indirect immunofluorescence analysis | ec50 | 0.0450 | uM |
| [7-(3-hydroxyprop-1-ynyl)-6-methoxy-2H-indazol-3-yl]-(3,4,5-trimethoxyphenyl)methanone | 280080: Displacement of [3H]colchicine from tubulin in MCF7 cells | ic50 | 0.0460 | uM |
| (3S,10R,13E,16S)-10-[(3-chloro-4-methoxyphenyl)methyl]-6,6-dimethyl-3-(2-methylpropyl)-16-[(1S)-1-[(2R,3S)-3-phenyloxiran-2-yl]ethyl]-1,4-dioxa-8,11-diazacyclohexadec-13-ene-2,5,9,12-tetrone | 2061859: Binding affinity to tubulin (unknown origin) assessed as dissociation constant by SPR analysis | kd | 0.0470 | uM |
| N-hydroxy-6-(3-methoxy-6,11,11-trioxobenzo[b][1,4]benzothiazepin-5-yl)hexanamide | 580932: Inhibition of HDAC activity in human NB4 cells assessed as acetylated tubulin after 24 hrs by Western blot analysis | ec50 | 0.0500 | uM |
| N-hydroxy-6-(6,11,11-trioxobenzo[b][1,4]benzothiazepin-5-yl)hexanamide | 580932: Inhibition of HDAC activity in human NB4 cells assessed as acetylated tubulin after 24 hrs by Western blot analysis | ec50 | 0.0500 | uM |
| 5-[2-(3,5-dimethoxyphenoxy)-3-pyridinyl]-N-(3-methoxyphenyl)-1H-1,2,4-triazol-3-amine | 256882: Displacement of [3H]colchicine from tubulin | ki | 0.0500 | uM |
| [(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] benzoate | 2126113: Displacement of fluorescent Maytansine probe from tubulin (unknown origin) assessed as dissociation constant by competitive binding based fluorescence anisotropy | kd | 0.0510 | uM |
| N-ethyl-N-(4-methoxyphenyl)-5-methylfuro[2,3-d]pyrimidin-4-amine | 1635267: Induction of microtubule depolymerization in human A10 cells incubated for 18 hrs by indirect immunofluorescence analysis | ec50 | 0.0530 | uM |
| 3-[3-(1,3-benzodioxol-5-ylamino)-1H-1,2,4-triazol-5-yl]-N-(3,5-dimethoxyphenyl)pyridin-2-amine | 256882: Displacement of [3H]colchicine from tubulin | ki | 0.0600 | uM |
| Vinblastine | 214333: The compound tested for the inhibition of tubulin polymerization. | ic50 | 0.0700 | uM |
| methyl (13S,15S,17S)-13-[(1R,9R,10S,11R,12R,19R)-10-[(1-diethoxyphosphoryl-2-phenylethyl)carbamoyl]-12-ethyl-10,11-dihydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraen-4-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraene-13-carboxylate | 214333: The compound tested for the inhibition of tubulin polymerization. | ic50 | 0.0700 | uM |
| N-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-[3-(pyridin-2-ylmethylamino)thiophen-2-yl]-1,3,4-oxadiazol-2-amine | 261214: Displacement of [3H]colchicine from tubulin at 65 nM | ic50 | 0.0750 | uM |
| methyl (13S,15S,17S)-13-[(1R,9R,10S,11R,12R,19R)-10-[[(1S)-1-diethoxyphosphorylethyl]carbamoyl]-12-ethyl-10,11-dihydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraen-4-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraene-13-carboxylate | 214333: The compound tested for the inhibition of tubulin polymerization. | ic50 | 0.0800 | uM |
| 4-methoxy-2-[(Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]thiophene | 1267532: Inhibition of Tubulin polymerization in human HeLa cells assessed as decrease in dynamic tyrosinated microtubules after 2 hrs by microplate reader analysis | ec50 | 0.0810 | uM |
| N-[2-[[(E)-(2,4-dihydroxyphenyl)methylideneamino]carbamoyl]phenyl]furan-2-carboxamide | 1882654: Inhibition of tubulin polymerization (unknown origin) | ic50 | 0.0876 | uM |
| N-hydroxy-6-(3-methoxy-6-oxobenzo[b][1,4]benzoxazepin-5-yl)hexanamide | 580932: Inhibition of HDAC activity in human NB4 cells assessed as acetylated tubulin after 24 hrs by Western blot analysis | ec50 | 0.0900 | uM |
| N-(3,5-dimethoxyphenyl)-3-[3-(3-methoxyanilino)-1H-1,2,4-triazol-5-yl]pyridin-2-amine | 256882: Displacement of [3H]colchicine from tubulin | ki | 0.1000 | uM |
| methyl (13S,15S,17S)-13-[(1R,9R,10S,11R,12R,19R)-10-[[(1R)-1-diethoxyphosphoryl-2-(1H-indol-3-yl)ethyl]carbamoyl]-12-ethyl-10,11-dihydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraen-4-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraene-13-carboxylate | 214333: The compound tested for the inhibition of tubulin polymerization. | ic50 | 0.1000 | uM |
| methyl (13S,15S,17S)-13-[(1R,9R,10S,11R,12R,19R)-10-(1-diethoxyphosphorylethylcarbamoyl)-12-ethyl-10,11-dihydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraen-4-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraene-13-carboxylate | 214333: The compound tested for the inhibition of tubulin polymerization. | ic50 | 0.1000 | uM |
| methyl (13S,15S,17S)-13-[(1R,9R,10S,11R,12R,19R)-10-[[(1S)-1-diethoxyphosphoryl-2-(1H-indol-3-yl)ethyl]carbamoyl]-12-ethyl-10,11-dihydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraen-4-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraene-13-carboxylate | 214333: The compound tested for the inhibition of tubulin polymerization. | ic50 | 0.1000 | uM |
CTD chemical–gene interactions
16 total (human), top 16 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Estradiol | affects binding, increases expression | 2 |
| methyleugenol | decreases expression | 1 |
| bisphenol A | increases expression | 1 |
| decabromobiphenyl ether | decreases expression | 1 |
| sodium arsenite | increases abundance, increases expression | 1 |
| tetrabromobisphenol A | decreases expression | 1 |
| manganese chloride | increases abundance, increases expression | 1 |
| abrine | increases expression | 1 |
| bromovanin | increases expression | 1 |
| Arsenic | increases abundance, increases expression | 1 |
| Manganese | increases abundance, increases expression | 1 |
| N-Nitrosopyrrolidine | decreases expression | 1 |
| Tunicamycin | decreases expression | 1 |
| Valproic Acid | increases methylation | 1 |
| Aflatoxin B1 | decreases expression | 1 |
| Okadaic Acid | affects expression | 1 |
ChEMBL screening assays
1686 unique, capped per target: 1645 binding, 35 functional, 6 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1009021 | Binding | Inhibition of tubulin polymerization in human MCF7 cells at 1 uM after 2 hrs by SDS-PAGE | A new cytotoxic epothilone from modified polyketide synthases heterologously expressed in Myxococcus xanthus. — J Nat Prod |
| CHEMBL4146506 | ADMET | Inhibition of tubulin polymerization in human HaCaT cells assessed as chromatin condensation at 1 uM after 24 hrs by Hoechst 33258 staining-based fluorescence microscopic analysis | Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents. — Eur J Med Chem |
| CHEMBL5056161 | Functional | Inhibition of tubulin polymerization (unknown origin) assessed as fluorescence intensity measured for 90 mins by DAPI based microplate reader | Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors. — Eur J Med Chem |
Clinical trials (associated diseases)
13 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT03414970 | PHASE3 | ACTIVE_NOT_RECRUITING | Hypofractionated Radiation Therapy After Mastectomy in Preventing Recurrence in Patients With Stage IIa-IIIa Breast Cancer |
| NCT00461344 | PHASE2 | TERMINATED | Docetaxel + Doxorubicin as Neoadjuvant Chemotherapy in Patients With Breast Cancer |
| NCT07499999 | PHASE2 | NOT_YET_RECRUITING | Randomized Double-Blind Phase II Trial of Baby Exemestane Versus Baby Tamoxifen in Post-Menopausal Women at High Risk for Breast Cancer |
| NCT06310681 | Not specified | COMPLETED | Pilot Testing of a Co-adapted Group Programme for Parents/Carers of Children With Complex Neurodisability |
| NCT07303049 | Not specified | NOT_YET_RECRUITING | Cognitive Benefit of Intensive Rehabilitation Using Rhythmic Music Training in Children With Complex Neurodevelopmental Disorder |
| NCT00637364 | PHASE1/PHASE2 | SUSPENDED | High Intensity Focused Ultrasound Tumor Treatment for Pancreatic Cancer Pain |
| NCT02779855 | PHASE1/PHASE2 | COMPLETED | Talimogene Laherparepvec in Combination With Neoadjuvant Chemotherapy in Triple Negative Breast Cancer |
| NCT01753908 | EARLY_PHASE1 | COMPLETED | Broccoli Sprout Extract in Treating Patients With Breast Cancer |
| NCT01796041 | EARLY_PHASE1 | COMPLETED | Intraoperative Imaging of Breast Cancer With Indocyanine Green |
| NCT01208974 | Not specified | ACTIVE_NOT_RECRUITING | Nipple-Areola Complex (NAC) Irradiation After Nipple-Sparing Mastectomy and Reconstruction |
| NCT01875198 | Not specified | TERMINATED | Oncologic Impact of Splenectomy-omitting Radical Pancreatectomy in Well-selected Left-sided Pancreatic Cancer |
| NCT03543397 | Not specified | UNKNOWN | MRI in Ductal Carcinoma in Situ (DCIS) |
| NCT03834532 | Not specified | COMPLETED | Living Well After Breast Surgery |
Related Atlas pages
- Associated diseases: complex neurodevelopmental disorder
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): complex neurodevelopmental disorder