VPS28

Summary

VPS28 (VPS28 subunit of ESCRT-I, HGNC:18178) is a protein-coding gene on chromosome 8q24.3, encoding Vacuolar protein sorting-associated protein 28 homolog (Q9UK41). Component of the ESCRT-I complex, a regulator of vesicular trafficking process. It is a common-essential gene (DepMap: required in 98.7% of cancer cell lines).

This gene encodes a protein subunit of the ESCRT-I complex (endosomal complexes required for transport), which functions in the transport and sorting of proteins into subcellular vesicles. This complex can also be hijacked to facilitate the budding of enveloped viruses from the cell membrane. Alternative splicing results in multiple transcript variants encoding different isoforms.

Source: NCBI Gene 51160 — RefSeq curated summary.

At a glance

• GWAS associations: 5
• Clinical variants (ClinVar): 60 total
• Druggable target: yes
• Cancer dependency (DepMap): dependent in 98.7% of screened cell lines (common-essential)
• MANE Select transcript: NM_016208

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:18178
Approved symbol	VPS28
Name	VPS28 subunit of ESCRT-I
Location	8q24.3
Locus type	gene with protein product
Status	Approved
Aliases	CIIA
Ensembl gene	ENSG00000160948
Ensembl biotype	protein_coding
OMIM	611952
Entrez	51160

Gene structure

Transcript identifiers

Ensembl transcripts: 49 — 40 protein_coding, 5 retained_intron, 2 protein_coding_CDS_not_defined, 2 nonsense_mediated_decay

ENST00000292510, ENST00000377348, ENST00000524521, ENST00000526054, ENST00000526204, ENST00000526734, ENST00000526977, ENST00000527797, ENST00000528142, ENST00000529182, ENST00000530790, ENST00000530836, ENST00000530983, ENST00000531032, ENST00000531924, ENST00000533806, ENST00000909910, ENST00000909911, ENST00000909912, ENST00000909913, ENST00000909914, ENST00000909915, ENST00000909916, ENST00000909917, ENST00000909918, ENST00000909919, ENST00000909920, ENST00000909921, ENST00000909922, ENST00000909923, ENST00000909924, ENST00000938153, ENST00000938154, ENST00000938155, ENST00000938156, ENST00000938157, ENST00000969314, ENST00000969315, ENST00000969316, ENST00000969317, ENST00000969318, ENST00000969319, ENST00000969320, ENST00000969321, ENST00000969322, ENST00000969323, ENST00000969324, ENST00000969325, ENST00000969326

RefSeq mRNA: 2 — MANE Select: NM_016208 NM_016208, NM_183057

CCDS: CCDS34967, CCDS6425

Canonical transcript exons

ENST00000292510 — 10 exons

Exon	Start	End
ENSE00002174785	144428489	144428548
ENSE00003484103	144424946	144425051
ENSE00003508408	144425683	144425772
ENSE00003517520	144424215	144424268
ENSE00003583602	144426026	144426063
ENSE00003626667	144424718	144424819
ENSE00003627686	144426909	144426979
ENSE00003637125	144426180	144426208
ENSE00003673772	144424041	144424132
ENSE00003888676	144423617	144423922

Expression profiles

Bgee: expression breadth ubiquitous, 145 present calls, max score 98.77.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 50.0097 / max 204.4344, expressed in 1823 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
95681	49.0291	1823
95680	0.9806	622

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right uterine tube	UBERON:0001302	98.77	gold quality
apex of heart	UBERON:0002098	98.71	gold quality
left testis	UBERON:0004533	98.71	gold quality
right lobe of thyroid gland	UBERON:0001119	98.70	gold quality
right ovary	UBERON:0002118	98.68	gold quality
left ovary	UBERON:0002119	98.67	gold quality
fundus of stomach	UBERON:0001160	98.66	gold quality
duodenum	UBERON:0002114	98.66	gold quality
right testis	UBERON:0004534	98.65	gold quality
left lobe of thyroid gland	UBERON:0001120	98.64	gold quality
embryo	UBERON:0000922	98.58	gold quality
fallopian tube	UBERON:0003889	98.58	gold quality
ganglionic eminence	UBERON:0004023	98.58	gold quality
mucosa of transverse colon	UBERON:0004991	98.58	gold quality
body of stomach	UBERON:0001161	98.57	gold quality
endocervix	UBERON:0000458	98.55	gold quality
ovary	UBERON:0000992	98.52	gold quality
small intestine Peyer’s patch	UBERON:0003454	98.51	gold quality
pituitary gland	UBERON:0000007	98.50	gold quality
thyroid gland	UBERON:0002046	98.50	gold quality
body of uterus	UBERON:0009853	98.49	gold quality
spleen	UBERON:0002106	98.46	gold quality
cortical plate	UBERON:0005343	98.46	gold quality
granulocyte	CL:0000094	98.44	gold quality
muscle layer of sigmoid colon	UBERON:0035805	98.44	gold quality
skin of leg	UBERON:0001511	98.42	gold quality
adenohypophysis	UBERON:0002196	98.42	gold quality
right hemisphere of cerebellum	UBERON:0014890	98.42	gold quality
small intestine	UBERON:0002108	98.39	gold quality
transverse colon	UBERON:0001157	98.38	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-HCAD-31	no	2.93
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

9 targeting VPS28, 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-18A-3P	99.56	65.68	1092
HSA-MIR-1324	99.46	66.57	1302
HSA-MIR-3911	99.38	66.95	1087
HSA-MIR-147A	98.33	66.40	795
HSA-MIR-3166	98.24	66.63	1223
HSA-MIR-148B-5P	97.29	66.30	992
HSA-MIR-6874-3P	97.29	66.34	975
HSA-MIR-6730-3P	97.03	67.54	889
HSA-MIR-6796-5P	95.37	66.08	1120

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 98.7% of screened cell lines, common-essential.

Literature-anchored findings (GeneRIF, showing 7)

• EIAV Gag interacts with a cellular component of the VPS machinery, VPS28, to accomplish efficient particle release (PMID:12857913)
• Overall, we see no role for the ESCRT pathway in influenza virus budding and the significance of the M1-VPS28 interaction remains to be determined. (PMID:19524996)
• Data show that gamma2-adaptin in MVB sorting specifically interacts with the ESCRT subunits Vps28 and CHMP2A. (PMID:20708039)
• CIIA functions as a negative modulator of the SOS1-Ras signaling events initiated by peptide growth factors including EGF. (PMID:24522193)
• CIIA attenuates neurotoxicity caused by OGD/R through inhibiting ASK1-dependent signaling events. (PMID:25098452)
• USP8, and the endosomal sorting protein, VPS28, are the negative regulators of NOD2-induced IL-8 secretion. (PMID:25170077)
• VPS28, an ESCRT-I protein, interacts with Gbetagamma and Eg5-TPX2. VPS28 organizes Aster Microtubules via Gbetagamma. VPS28 recruits Eg5 and TPX2 to regulate mitotic spindle bipolarity. (PMID:29548937)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	vps28	ENSDARG00000103203
mus_musculus	Vps28	ENSMUSG00000115987
rattus_norvegicus	Vps28	ENSRNOG00000014633
drosophila_melanogaster	Vps28	FBGN0021814
caenorhabditis_elegans	vps-28	WBGENE00013598

Protein

Protein identifiers

Vacuolar protein sorting-associated protein 28 homolog — Q9UK41 (reviewed: Q9UK41)

Alternative names: ESCRT-I complex subunit VPS28

All UniProt accessions (7): Q9UK41, A0A0S2Z5H5, E9PLM9, E9PM90, E9PQR7, E9PR04, Q548N1

UniProt curated annotations — full annotation on UniProt →

Function. Component of the ESCRT-I complex, a regulator of vesicular trafficking process.

Subunit / interactions. Component of the ESCRT-I complex (endosomal sorting complex required for transport I) which consists of TSG101, VPS28, a VPS37 protein (VPS37A to -D) and MVB12A or MVB12B in a 1:1:1:1 stoichiometry. Interacts with TSG101, VPS37B, VPS37C, MVB12A and MVB12B. Component of an ESCRT-I complex (endosomal sorting complex required for transport I) which consists of TSG101, VPS28, VPS37A and UBAP1 in a 1:1:1:1 stoichiometry. Interacts with VPS36; the interaction mediates the association with the ESCRT-II complex. Interacts with SNF8 and VPS25. Interacts with CEP55.

Subcellular location. Cell membrane. Late endosome membrane.

Similarity. Belongs to the VPS28 family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q9UK41-1	1	yes
Q9UK41-2	2

RefSeq proteins (2): NP_057292, NP_898880 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR007143	Vps28	Family
IPR017898	VPS28_N	Domain
IPR017899	VPS28_C	Domain
IPR037202	ESCRT_assembly_dom	Homologous_superfamily
IPR037206	VPS28_C_sf	Homologous_superfamily
IPR038358	VPS28_N_sf	Homologous_superfamily

Pfam: PF03997

UniProt features (10 total): helix 4, domain 2, chain 1, modified residue 1, splice variant 1, strand 1

Structure

Experimental structures (PDB)

1 structures.

PDB	Method	Resolution (Å)
6VME	X-RAY DIFFRACTION	2.19

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9UK41-F1	92.18	0.82

Functional residue map

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

Post-translational modifications (1): 1

Function

Pathways and Gene Ontology

Reactome pathways

5 pathways

ID	Pathway
R-HSA-162588	Budding and maturation of HIV virion
R-HSA-174490	Membrane binding and targetting of GAG proteins
R-HSA-917729	Endosomal Sorting Complex Required For Transport (ESCRT)
R-HSA-9610379	HCMV Late Events
R-HSA-9615710	Late endosomal microautophagy

MSigDB gene sets: 204 (showing top): GSE45365_CD8A_DC_VS_CD11B_DC_IFNAR_KO_DN, GSE18804_BRAIN_VS_COLON_TUMORAL_MACROPHAGE_DN, GSE18804_SPLEEN_MACROPHAGE_VS_TUMORAL_MACROPHAGE_DN, GSE45365_CTRL_VS_MCMV_INFECTION_NK_CELL_DN, REACTOME_ENDOSOMAL_SORTING_COMPLEX_REQUIRED_FOR_TRANSPORT_ESCRT, GOBP_POSITIVE_REGULATION_OF_ENDOCYTOSIS, GOBP_ENDOSOME_ORGANIZATION, GOBP_INTRACELLULAR_PROTEIN_TRANSPORT, GOBP_VESICLE_ORGANIZATION, GOBP_POSITIVE_REGULATION_OF_PROTEIN_LOCALIZATION, GOBP_POSITIVE_REGULATION_OF_PROTEIN_CATABOLIC_PROCESS, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, ACEVEDO_NORMAL_TISSUE_ADJACENT_TO_LIVER_TUMOR_DN, GOBP_VACUOLAR_TRANSPORT, GOBP_VESICLE_MEDIATED_TRANSPORT

GO Biological Process (11): macroautophagy (GO:0016236), negative regulation of protein ubiquitination (GO:0031397), multivesicular body assembly (GO:0036258), viral budding via host ESCRT complex (GO:0039702), ubiquitin-dependent protein catabolic process via the multivesicular body sorting pathway (GO:0043162), protein transport to vacuole involved in ubiquitin-dependent protein catabolic process via the multivesicular body sorting pathway (GO:0043328), positive regulation of protein catabolic process (GO:0045732), membrane fission (GO:0090148), positive regulation of ubiquitin-dependent endocytosis (GO:2000397), protein transport (GO:0015031), endosome transport via multivesicular body sorting pathway (GO:0032509)

GO Molecular Function (3): ubiquitin binding (GO:0043130), protein-containing complex binding (GO:0044877), protein binding (GO:0005515)

GO Cellular Component (10): ESCRT I complex (GO:0000813), cytoplasm (GO:0005737), endosome (GO:0005768), early endosome (GO:0005769), cytosol (GO:0005829), plasma membrane (GO:0005886), endosome membrane (GO:0010008), late endosome membrane (GO:0031902), extracellular exosome (GO:0070062), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-5 pathways:

Category	Pathways
Late Phase of HIV Life Cycle	1
Synthesis And Processing Of GAG, GAGPOL Polyproteins	1
Membrane Trafficking	1
HCMV Infection	1
Autophagy	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
multivesicular body sorting pathway	2
binding	2
endosome membrane	2
endosome	2
autophagosome assembly	1
autophagy	1
protein ubiquitination	1
regulation of protein ubiquitination	1
negative regulation of protein modification by small protein conjugation or removal	1
multivesicular body organization	1
organelle assembly	1
viral budding	1
ubiquitin-dependent protein catabolic process	1
protein catabolic process in the vacuole	1
intracellular protein transport	1
late endosome to vacuole transport via multivesicular body sorting pathway	1
ubiquitin-dependent protein catabolic process via the multivesicular body sorting pathway	1
protein localization to vacuole	1
establishment of protein localization to vacuole	1
positive regulation of catabolic process	1
protein catabolic process	1
regulation of protein catabolic process	1
positive regulation of protein metabolic process	1
membrane organization	1
positive regulation of endocytosis	1
positive regulation of protein transport	1
ubiquitin-dependent endocytosis	1
regulation of ubiquitin-dependent endocytosis	1
transport	1
intracellular protein localization	1
establishment of protein localization	1
endosomal transport	1
ubiquitin-like protein binding	1
ESCRT complex	1
membrane protein complex	1
intracellular anatomical structure	1
endomembrane system	1
cytoplasmic vesicle	1
cytoplasm	1

Protein interactions and networks

STRING

1280 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
VPS28	TSG101	Q99816	999
VPS28	VPS37A	Q8NEZ2	999
VPS28	VPS36	Q86VN1	997
VPS28	UBAP1	Q9NZ09	993
VPS28	MVB12A	Q96EY5	985
VPS28	VPS37B	Q9H9H4	984
VPS28	CHMP6	Q96FZ7	978
VPS28	VPS37C	A5D8V6	969
VPS28	VPS4A	Q9UN37	942
VPS28	MVB12B	Q9H7P6	931
VPS28	VPS25	Q9BRG1	919
VPS28	SNF8	Q96H20	869
VPS28	CHMP3	Q9Y3E7	845
VPS28	A0A140T963	A0A140T963	845
VPS28	CHMP5	Q9NZZ3	843

IntAct

174 interactions, top by confidence:

A	B	Type	Score
CEP55	TSG101	psi-mi:“MI:0914”(association)	0.970
VPS28	TSG101	psi-mi:“MI:0915”(physical association)	0.940
TSG101	VPS28	psi-mi:“MI:0915”(physical association)	0.940
VPS28	VPS37B	psi-mi:“MI:0915”(physical association)	0.890
VPS37B	VPS28	psi-mi:“MI:0915”(physical association)	0.890
TSG101	VPS37C	psi-mi:“MI:0914”(association)	0.780
GRB2	WIPF3	psi-mi:“MI:0914”(association)	0.730
VPS28	USHBP1	psi-mi:“MI:0915”(physical association)	0.720
USHBP1	VPS28	psi-mi:“MI:0915”(physical association)	0.720
VPS28	SMN1	psi-mi:“MI:0915”(physical association)	0.700
SMN1	VPS28	psi-mi:“MI:0915”(physical association)	0.700
VPS28	SKIL	psi-mi:“MI:0915”(physical association)	0.670
VPS28	VPS52	psi-mi:“MI:0915”(physical association)	0.670

BioGRID (223): VPS36 (Co-crystal Structure), VPS28 (Two-hybrid), VPS28 (Two-hybrid), VPS28 (Two-hybrid), VPS28 (Two-hybrid), VPS28 (Two-hybrid), VPS28 (Two-hybrid), VPS28 (Two-hybrid), VPS28 (Two-hybrid), VPS28 (Two-hybrid), VPS28 (Two-hybrid), MBIP (Two-hybrid), TRIM54 (Two-hybrid), CARD9 (Two-hybrid), VPS37B (Two-hybrid)

ESM2 similar proteins: A0A8I3PI99, A0M8U1, A7Y521, B5DEN9, C5HGF3, O88544, O94973, P13666, P17427, P18484, P38024, Q00765, Q0VCK5, Q0X0A5, Q13098, Q1RLU8, Q28635, Q2PG42, Q3KNM2, Q3SZA0, Q3T0N3, Q3T126, Q3T178, Q3ZC24, Q4R5E6, Q5F418, Q5I0H4, Q5M7T4, Q5R648, Q5R9B0, Q5R9M4, Q5RE33, Q5ZJ41, Q5ZJD7, Q6DGW9, Q6GM44, Q6NRT5, Q7TQ48, Q8C407, Q8R1Z9

Diamond homologs: A8XWB7, B5DEN9, O13872, O65421, Q3T178, Q54NF1, Q9D1C8, Q9NA26, Q9S9T7, Q9UK41, Q9V359, Q02767

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
VPS28	“form complex”	“ESCRT-I complex, VPS37A-UBAP1 variant”	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 116 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
Endosomal Sorting Complex Required For Transport (ESCRT)	9	40.9×	3e-10
Budding and maturation of HIV virion	7	35.2×	1e-07
Late endosomal microautophagy	8	32.2×	2e-08
RHOQ GTPase cycle	5	11.2×	5e-03
HCMV Late Events	7	8.5×	1e-03

GO biological processes:

GO term	Partners	Fold	FDR
protein transport to vacuole involved in ubiquitin-dependent protein catabolic process via the multivesicular body sorting pathway	8	86.0×	1e-11
viral budding via host ESCRT complex	6	49.1×	3e-07
multivesicular body assembly	8	43.0×	2e-09
membrane fission	10	41.9×	1e-11
ubiquitin-dependent protein catabolic process via the multivesicular body sorting pathway	6	33.3×	3e-06
protein targeting to membrane	7	21.1×	4e-06
macroautophagy	8	19.6×	1e-06
protein transport	11	4.9×	1e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	29
Likely benign	6
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1610 predictions. Top by Δscore:

Variant	Effect	Δscore
8:144424040:CCA:C	donor_gain	1.0000
8:144424269:C:CC	acceptor_gain	1.0000
8:144424685:T:A	donor_gain	1.0000
8:144424728:T:TA	donor_gain	1.0000
8:144424761:T:TA	donor_gain	1.0000
8:144424815:TCCAG:T	acceptor_gain	1.0000
8:144424816:CCAG:C	acceptor_gain	1.0000
8:144424816:CCAGC:C	acceptor_gain	1.0000
8:144424817:CAG:C	acceptor_gain	1.0000
8:144424817:CAGC:C	acceptor_gain	1.0000
8:144424817:CAGCT:C	acceptor_loss	1.0000
8:144424818:AG:A	acceptor_gain	1.0000
8:144424819:GC:G	acceptor_loss	1.0000
8:144424820:C:CC	acceptor_gain	1.0000
8:144424820:CTGTT:C	acceptor_loss	1.0000
8:144424821:T:A	acceptor_loss	1.0000
8:144424944:A:AC	donor_gain	1.0000
8:144424945:C:CC	donor_gain	1.0000
8:144424945:CG:C	donor_gain	1.0000
8:144425663:C:A	donor_gain	1.0000
8:144425680:T:TG	donor_loss	1.0000
8:144425681:A:AC	donor_gain	1.0000
8:144425682:C:CA	donor_gain	1.0000
8:144425682:CT:C	donor_gain	1.0000
8:144425682:CTCG:C	donor_gain	1.0000
8:144425701:T:TA	donor_gain	1.0000
8:144426024:A:AC	donor_gain	1.0000
8:144426025:C:CC	donor_gain	1.0000
8:144426025:CTT:C	donor_gain	1.0000
8:144426025:CTTCT:C	donor_gain	1.0000

AlphaMissense

1463 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
8:144423848:A:G	L208P	1.000
8:144423867:G:T	R202S	1.000
8:144424042:A:G	W183R	1.000
8:144424042:A:T	W183R	1.000
8:144424110:A:G	L160P	1.000
8:144424119:A:G	L157P	1.000
8:144424220:C:G	D151H	1.000
8:144424237:A:G	L145P	1.000
8:144424237:A:T	L145Q	1.000
8:144424243:A:G	L143P	1.000
8:144424248:G:C	D141E	1.000
8:144424248:G:T	D141E	1.000
8:144424249:T:A	D141V	1.000
8:144424249:T:C	D141G	1.000
8:144424249:T:G	D141A	1.000
8:144424250:C:A	D141Y	1.000
8:144424250:C:G	D141H	1.000
8:144424250:C:T	D141N	1.000
8:144424261:A:C	I137S	1.000
8:144424261:A:G	I137T	1.000
8:144424261:A:T	I137N	1.000
8:144424267:A:G	L135P	1.000
8:144424722:A:T	V133D	1.000
8:144424731:G:T	A130E	1.000
8:144424732:C:G	A130P	1.000
8:144424776:G:C	P115R	1.000
8:144424776:G:T	P115H	1.000
8:144424777:G:A	P115S	1.000
8:144424777:G:T	P115T	1.000
8:144424794:C:G	R109P	1.000

dbSNP variants (sampled 300 via entrez): RS1000448460 (8:144428995 T>C), RS1000648759 (8:144424871 G>A), RS1000801214 (8:144429246 C>G,T), RS1001644098 (8:144427156 G>A), RS1003007101 (8:144427920 G>C), RS1003209561 (8:144423714 G>A,T), RS1003240688 (8:144423540 G>A,C,T), RS1003720056 (8:144428189 G>T), RS1003874290 (8:144425602 G>C), RS1003905191 (8:144425347 C>A,T), RS1004761258 (8:144428622 G>A), RS1004914124 (8:144424443 T>A,C), RS1005545425 (8:144426635 C>T), RS1005581458 (8:144426473 G>A,T), RS1006349198 (8:144429923 C>T)

Disease associations

OMIM: gene MIM:611952 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

5 associations (top):

Study	Trait	p-value
GCST002598_30	Educational attainment	9.000000e-06
GCST006879_12	Blood metabolite levels	4.000000e-10
GCST006879_13	Blood metabolite levels	2.000000e-09
GCST006879_14	Blood metabolite levels	2.000000e-11
GCST006879_5	Blood metabolite levels	2.000000e-12

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0004784	self reported educational attainment

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL6067209 (SINGLE PROTEIN)

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

ChEMBL bioactivities

2 potent at pChembl≥5 of 2 total, top 2 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
5.10	Kd	7874	nM	CHEMBL5653589
5.10	ED50	7874	nM	CHEMBL5653589

PubChem BioAssay actives

1 with measured affinity, of 2 total; 1 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-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149771: Binding affinity to human VPS28 incubated for 45 mins by Kinobead based pull down assay	kd	7.8744	uM

CTD chemical–gene interactions

27 total (human), top 27 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	increases expression, increases methylation	3
Hydrogen Peroxide	affects expression	2
triphenyl phosphate	affects expression	1
alpha-pinene	affects cotreatment, increases expression, increases oxidation, increases abundance	1
bisphenol A	decreases methylation	1
tris(1,3-dichloro-2-propyl)phosphate	increases expression	1
sodium arsenite	decreases expression	1
cobaltous chloride	decreases expression	1
potassium chromate(VI)	decreases expression	1
methacrylaldehyde	affects cotreatment, increases expression, increases oxidation, increases abundance	1
jinfukang	increases expression	1
(+)-JQ1 compound	decreases expression	1
Acrolein	increases expression, increases oxidation, increases abundance, affects cotreatment	1
Air Pollutants	increases abundance, increases expression, increases oxidation, affects cotreatment	1
Benzo(a)pyrene	affects methylation, decreases methylation	1
Doxorubicin	decreases expression	1
Ivermectin	decreases expression	1
Ozone	affects cotreatment, increases expression, increases oxidation, increases abundance	1
Piroxicam	decreases expression	1
Selenium	increases expression	1
Smoke	decreases expression	1
Tobacco Smoke Pollution	affects expression	1
Tretinoin	increases expression	1
Cyclosporine	increases expression	1
Aflatoxin B1	increases methylation	1
Vitamin K 3	affects expression	1
Volatile Organic Compounds	affects cotreatment, increases expression, increases oxidation	1

ChEMBL screening assays

1 unique, capped per target: 1 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL5652813	Binding	Binding affinity to human VPS28 incubated for 45 mins by Kinobead based pull down assay	NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family. — ChemMedChem

Clinical trials (associated diseases)

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