PSMG1

Summary

PSMG1 (proteasome assembly chaperone 1, HGNC:3043) is a protein-coding gene on chromosome 21q22.2, encoding Proteasome assembly chaperone 1 (O95456). Chaperone protein which promotes assembly of the 20S proteasome as part of a heterodimer with PSMG2. It is a selective cancer dependency (DepMap: 54.1% of cell lines).

Enables molecular adaptor activity. Involved in chaperone-mediated protein complex assembly. Located in several cellular components, including Golgi apparatus; endoplasmic reticulum; and nucleoplasm. Part of protein folding chaperone complex.

Source: NCBI Gene 8624 — RefSeq curated summary.

At a glance

• GWAS associations: 23
• Clinical variants (ClinVar): 51 total
• Druggable target: yes
• Cancer dependency (DepMap): dependent in 54.1% of screened cell lines
• MANE Select transcript: NM_003720

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:3043
Approved symbol	PSMG1
Name	proteasome assembly chaperone 1
Location	21q22.2
Locus type	gene with protein product
Status	Approved
Aliases	c21-LRP, LRPC21, PAC1
Ensembl gene	ENSG00000183527
Ensembl biotype	protein_coding
OMIM	605296
Entrez	8624

Gene structure

Transcript identifiers

Ensembl transcripts: 13 — 10 protein_coding, 2 nonsense_mediated_decay, 1 retained_intron

ENST00000331573, ENST00000380900, ENST00000411828, ENST00000431628, ENST00000481921, ENST00000889165, ENST00000889166, ENST00000889167, ENST00000924000, ENST00000924001, ENST00000924002, ENST00000924003, ENST00000971315

RefSeq mRNA: 4 — MANE Select: NM_003720 NM_001261824, NM_001320795, NM_003720, NM_203433

CCDS: CCDS13660, CCDS13661

Canonical transcript exons

ENST00000331573 — 7 exons

Exon	Start	End
ENSE00001486754	39174769	39175664
ENSE00001921756	39183252	39183451
ENSE00003473157	39178449	39178647
ENSE00003574701	39180285	39180436
ENSE00003605373	39179924	39179986
ENSE00003675559	39181772	39181878
ENSE00003689596	39177435	39177571

Expression profiles

Bgee: expression breadth ubiquitous, 134 present calls, max score 98.64.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 47.8782 / max 1103.7730, expressed in 1823 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
190478	41.2685	1819
190479	6.1699	1638
209319	0.4398	179

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
left testis	UBERON:0004533	98.64	gold quality
right testis	UBERON:0004534	98.52	gold quality
testis	UBERON:0000473	97.86	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	95.89	gold quality
rectum	UBERON:0001052	95.47	gold quality
endometrium	UBERON:0001295	94.51	gold quality
mucosa of transverse colon	UBERON:0004991	94.25	gold quality
body of pancreas	UBERON:0001150	94.24	gold quality
esophagus mucosa	UBERON:0002469	93.61	gold quality
right adrenal gland	UBERON:0001233	93.49	gold quality
right adrenal gland cortex	UBERON:0035827	93.45	gold quality
pancreas	UBERON:0001264	93.44	gold quality
islet of Langerhans	UBERON:0000006	93.38	gold quality
left adrenal gland	UBERON:0001234	93.30	gold quality
left adrenal gland cortex	UBERON:0035825	93.22	gold quality
adenohypophysis	UBERON:0002196	93.14	gold quality
adrenal gland	UBERON:0002369	92.80	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	92.73	gold quality
stromal cell of endometrium	CL:0002255	92.68	gold quality
tibial artery	UBERON:0007610	92.66	gold quality
popliteal artery	UBERON:0002250	92.63	gold quality
pituitary gland	UBERON:0000007	92.55	gold quality
right lobe of liver	UBERON:0001114	92.53	gold quality
gastrocnemius	UBERON:0001388	92.46	gold quality
metanephros cortex	UBERON:0010533	92.46	gold quality
left lobe of thyroid gland	UBERON:0001120	92.38	gold quality
endocervix	UBERON:0000458	92.37	gold quality
thoracic aorta	UBERON:0001515	92.27	gold quality
ascending aorta	UBERON:0001496	92.26	gold quality
ectocervix	UBERON:0012249	92.21	gold quality

Single-cell (SCXA)

Detected in 6 experiment(s), a significant marker in 4.

Experiment	Marker?	Max mean expression
E-GEOD-134144	yes	28.29
E-MTAB-10042	yes	14.23
E-CURD-112	yes	8.70
E-ANND-3	yes	8.52
E-MTAB-6379	no	927.38
E-MTAB-9689	no	605.97

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): MYC

miRNA regulators (miRDB)

9 targeting PSMG1, 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-371B-5P	99.99	75.34	4759
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-4789-5P	99.98	70.76	2721
HSA-MIR-1283	99.69	72.42	3009
HSA-MIR-513C-5P	99.50	68.42	1730
HSA-MIR-514B-5P	99.50	68.19	1766
HSA-MIR-1468-5P	94.18	69.04	176

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 54.1% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 9)

• The DSCR2 protein is associated with the endoplasmic reticulum; it is not an integral membrane protein and it is maintained on the cytoplasmic side of the ER by indirect interaction with the ER membrane or with another protein. (PMID:15590417)
• Further, the results of intracellular localization studies and membrane fractionation assays indicate that DSCR2 is targeted to a cytoplasmic compartment as a soluble form. (PMID:15670775)
• two chaperones, designated proteasome assembling chaperone-1 (PAC1) and PAC2, form a heterodimer and are involved in the maturation of mammalian 20S proteasomes (PMID:16251969)
• DSCR2 was found to interact with PPARbeta and to inhibit it. (PMID:18793612)
• Data show that an additive gene-gene interaction involving TLR4, PSMG1, TNFRSF6B and IRGM was identified with CD. (PMID:21079743)
• PSMG1 gene expression is increased in classic variant of papillary thyroid carcinoma. (PMID:21509594)
• PSMG1 mutation is associated with Crohn’s disease. (PMID:22593026)
• RNA-seq evidence of biallelic expression of PSMG1 and 10 neighboring genes in at least one primary human tissue tested indicates that the expression of PSMG1 is uncoupled from the control of the maternally inherited 5mCpG imprints at the WRB differentially methylated region (DMR) in disomic controls or trisomy (Down syndrome) individuals. (PMID:27100087)
• miR-484 is associated with disease recurrence and promotes migration in prostate cancer. (PMID:32338277)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	psmg1	ENSDARG00000040620
mus_musculus	Psmg1	ENSMUSG00000022913
rattus_norvegicus	Psmg1	ENSRNOG00000001643

Protein

Protein identifiers

Proteasome assembly chaperone 1 — O95456 (reviewed: O95456)

Alternative names: Chromosome 21 leucine-rich protein, Down syndrome critical region protein 2, Proteasome chaperone homolog 1

All UniProt accessions (3): F8WBH7, H7C3B4, O95456

UniProt curated annotations — full annotation on UniProt →

Function. Chaperone protein which promotes assembly of the 20S proteasome as part of a heterodimer with PSMG2. The PSMG1-PSMG2 heterodimer binds to the PSMA5 and PSMA7 proteasome subunits, promotes assembly of the proteasome alpha subunits into the heteroheptameric alpha ring and prevents alpha ring dimerization.

Subunit / interactions. Forms a heterodimer with PSMG2. The PSMG1-PSMG2 heterodimer interacts directly with the PSMA5 and PSMA7 proteasome alpha subunits.

Subcellular location. Cytoplasm. Endoplasmic reticulum.

Tissue specificity. In the adult, detected in brain, colon, leukocytes, breast and testis. Widely expressed in the fetus. Also expressed in a variety of proliferating cell lines.

Post-translational modifications. Degraded by the proteasome upon completion of 20S proteasome maturation.

Similarity. Belongs to the PSMG1 family.

Isoforms (2)

UniProt ID	Names	Canonical?
O95456-1	1	yes
O95456-2	2

RefSeq proteins (4): NP_001248753, NP_001307724, NP_003711, NP_982257 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR016565	Proteasome_assmbl_chp_1	Family

Pfam: PF16094

UniProt features (43 total): strand 15, helix 11, turn 5, modified residue 5, initiator methionine 1, chain 1, sequence variant 1, sequence conflict 1, region of interest 1, compositionally biased region 1, splice variant 1

Structure

Experimental structures (PDB)

13 structures.

PDB	Method	Resolution (Å)
8QYL	ELECTRON MICROSCOPY	2.67
8QYJ	ELECTRON MICROSCOPY	2.73
8QYM	ELECTRON MICROSCOPY	2.73
8TM6	ELECTRON MICROSCOPY	2.8
8QYN	ELECTRON MICROSCOPY	2.88
8YIX	ELECTRON MICROSCOPY	2.91
8QZ9	ELECTRON MICROSCOPY	2.95
8TM3	ELECTRON MICROSCOPY	3
8TM4	ELECTRON MICROSCOPY	3
8TM5	ELECTRON MICROSCOPY	3
8YIY	ELECTRON MICROSCOPY	3.41
8YIZ	ELECTRON MICROSCOPY	3.79
8QYS	ELECTRON MICROSCOPY	3.89

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O95456-F1	81.90	0.40

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 (5): 2, 18, 54, 180, 264

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

ID	Pathway
R-HSA-9907900	Proteasome assembly

MSigDB gene sets: 186 (showing top): GOBP_HINDBRAIN_DEVELOPMENT, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_UP, CHIANG_LIVER_CANCER_SUBCLASS_UNANNOTATED_DN, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_DN, GOBP_PROTEASOME_ASSEMBLY, GOBP_CHAPERONE_MEDIATED_PROTEIN_COMPLEX_ASSEMBLY, MODULE_16, GOBP_NEURAL_PRECURSOR_CELL_PROLIFERATION, WEI_MYCN_TARGETS_WITH_E_BOX, RUTELLA_RESPONSE_TO_CSF2RB_AND_IL4_UP, BROWNE_HCMV_INFECTION_14HR_DN, GOBP_HEAD_DEVELOPMENT, DODD_NASOPHARYNGEAL_CARCINOMA_UP, MASSARWEH_RESPONSE_TO_ESTRADIOL

GO Biological Process (4): cerebellar granule cell precursor proliferation (GO:0021930), chaperone-mediated protein complex assembly (GO:0051131), proteasome core complex assembly (GO:0080129), proteasome assembly (GO:0043248)

GO Molecular Function (3): molecular adaptor activity (GO:0060090), proteasome binding (GO:0070628), protein binding (GO:0005515)

GO Cellular Component (7): nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), endoplasmic reticulum (GO:0005783), Golgi apparatus (GO:0005794), cytosol (GO:0005829), protein folding chaperone complex (GO:0101031)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
Post-translational protein modification	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
intracellular membrane-bounded organelle	3
cellular anatomical structure	3
cytoplasm	3
protein-containing complex assembly	2
binding	2
endomembrane system	2
cell proliferation in external granule layer	1
proteasome assembly	1
molecular_function	1
protein-containing complex binding	1
nuclear lumen	1
intracellular anatomical structure	1
intracellular protein-containing complex	1

Protein interactions and networks

STRING

3080 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PSMG1	PSMG2	Q969U7	976
PSMG1	POMP	Q9Y244	849
PSMG1	VPS26C	O14972	763
PSMG1	LCA5L	O95447	698
PSMG1	MX1	P20591	687
PSMG1	PSMA3	P25788	628
PSMG1	SH3BGR	P55822	624
PSMG1	BRWD1	Q9NSI6	603
PSMG1	TNFRSF6B	O95407	593
PSMG1	PSMA4	P25789	591
PSMG1	PSMB1	P20618	590
PSMG1	CRELD1	Q96HD1	589
PSMG1	PSMA5	P28066	587
PSMG1	RCAN1	P53805	585
PSMG1	PSMA7	O14818	579

IntAct

97 interactions, top by confidence:

A	B	Type	Score
PSMA1	PSMA7	psi-mi:“MI:0914”(association)	0.950
PSMA1	PSMA7	psi-mi:“MI:2364”(proximity)	0.950
PSMG1	PSMG2	psi-mi:“MI:0915”(physical association)	0.850
PSMA2	PSMA7	psi-mi:“MI:0914”(association)	0.850
PSMG2	PSMG1	psi-mi:“MI:0914”(association)	0.850
PSMA5	PSMA7	psi-mi:“MI:0914”(association)	0.800
PSMB7	PSMA7	psi-mi:“MI:0914”(association)	0.790
PSMB2	PSMA7	psi-mi:“MI:0914”(association)	0.790
PSMB3	PSMA7	psi-mi:“MI:0914”(association)	0.770
PSMB2	PSMD11	psi-mi:“MI:0914”(association)	0.730
PSMB4	PSMA7	psi-mi:“MI:0914”(association)	0.730
POMP	PSMA7	psi-mi:“MI:0915”(physical association)	0.720
PSMB3	PSMD11	psi-mi:“MI:0914”(association)	0.640
PSMB1	PSMA7	psi-mi:“MI:0914”(association)	0.640
CA10	WDHD1	psi-mi:“MI:0914”(association)	0.640
PSMB7	PSMD11	psi-mi:“MI:0914”(association)	0.640
PSMG1	PRKAR1B	psi-mi:“MI:0915”(physical association)	0.560
PSMB9	PSMD11	psi-mi:“MI:0914”(association)	0.530
SOST	KPNA4	psi-mi:“MI:0914”(association)	0.530
PSMG2	PSMA7	psi-mi:“MI:0914”(association)	0.530

BioGRID (178): PSMG1 (Affinity Capture-MS), PSMG1 (Affinity Capture-MS), PSMG1 (Affinity Capture-MS), PSMG1 (Affinity Capture-MS), PSMG1 (Affinity Capture-MS), PSMG1 (Co-fractionation), PSMG1 (Co-fractionation), PSMG1 (Co-fractionation), PSMG1 (Co-fractionation), PSMG1 (Co-fractionation), PSMG1 (Co-fractionation), PSMG1 (Co-fractionation), PSMG1 (Co-fractionation), PSMG1 (Co-fractionation), PSMG1 (Proximity Label-MS)

ESM2 similar proteins: A2RT67, A2RUS2, A4IHY1, B0CM32, B0KW86, E1B8U2, E7F240, F1MDL2, O08983, O94955, O95456, P48553, Q05AX3, Q0P5F2, Q1JQA1, Q1RMZ1, Q2HJ90, Q3T0J1, Q3TLI0, Q3ZBK8, Q4KM95, Q5FVM6, Q5R4T7, Q5R989, Q5RAQ5, Q5RFG8, Q60GF7, Q6DG91, Q6VNB8, Q7Z7H3, Q80TA6, Q8BXK4, Q8CHQ0, Q8IZQ1, Q8K2I9, Q8NFZ0, Q91W96, Q92902, Q96QE5, Q99LV7

Diamond homologs: A4IHY1, B0CM32, B0KW86, O95456, Q05AX3, Q0P5F2, Q6DG91, Q9JK23, A7RV13

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 75 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
Antigen processing: Ub, ATP-independent proteasomal degradation	14	137.8×	1e-27
Regulation of activated PAK-2p34 by proteasome mediated degradation	17	81.6×	3e-28
Proteasome assembly	23	80.9×	1e-37
Regulation of ornithine decarboxylase (ODC)	17	79.7×	5e-28
Cross-presentation of soluble exogenous antigens (endosomes)	18	78.8×	8e-29
Vpu mediated degradation of CD4	17	77.8×	6e-28
Autodegradation of the E3 ubiquitin ligase COP1	17	77.8×	6e-28
Ubiquitin-dependent degradation of Cyclin D	17	77.8×	6e-28

GO biological processes:

GO term	Partners	Fold	FDR
proteasome-mediated ubiquitin-dependent protein catabolic process	22	16.6×	1e-18

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	37
Likely benign	2
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

1278 predictions. Top by Δscore:

Variant	Effect	Δscore
21:39177567:TAGAA:T	acceptor_gain	1.0000
21:39177568:AGAA:A	acceptor_gain	1.0000
21:39177569:GAA:G	acceptor_gain	1.0000
21:39177569:GAAC:G	acceptor_loss	1.0000
21:39177572:C:CC	acceptor_gain	1.0000
21:39177574:A:AC	acceptor_gain	1.0000
21:39177574:A:C	acceptor_gain	1.0000
21:39180319:AAAG:A	donor_gain	1.0000
21:39181766:ACTT:A	donor_loss	1.0000
21:39181767:CTTA:C	donor_loss	1.0000
21:39181768:TTA:T	donor_loss	1.0000
21:39181771:C:CT	donor_loss	1.0000
21:39181771:CCTA:C	donor_gain	1.0000
21:39181874:CTTCC:C	acceptor_gain	1.0000
21:39181876:TCCCT:T	acceptor_loss	1.0000
21:39181877:CC:C	acceptor_gain	1.0000
21:39181878:CC:C	acceptor_gain	1.0000
21:39181879:C:CC	acceptor_gain	1.0000
21:39181879:CTA:C	acceptor_loss	1.0000
21:39177569:GAACT:G	acceptor_gain	0.9900
21:39177570:AA:A	acceptor_gain	0.9900
21:39177570:AACTA:A	acceptor_gain	0.9900
21:39177571:ACTAT:A	acceptor_gain	0.9900
21:39177572:CTATG:C	acceptor_gain	0.9900
21:39177578:A:AC	acceptor_gain	0.9900
21:39177581:C:CT	acceptor_gain	0.9900
21:39180435:TG:T	acceptor_gain	0.9900
21:39180437:C:CC	acceptor_gain	0.9900
21:39181765:CACT:C	donor_loss	0.9900
21:39181774:A:AC	donor_gain	0.9900

AlphaMissense

1874 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
21:39179935:A:G	W149R	0.998
21:39179935:A:T	W149R	0.998
21:39177571:A:T	V219D	0.994
21:39178452:C:G	A218P	0.993
21:39177564:G:C	S221R	0.992
21:39177564:G:T	S221R	0.992
21:39177566:T:G	S221R	0.992
21:39177568:A:G	L220P	0.992
21:39183371:G:C	F5L	0.991
21:39183371:G:T	F5L	0.991
21:39183373:A:G	F5L	0.991
21:39178529:A:G	L192P	0.990
21:39179958:A:T	V141D	0.990
21:39179977:A:G	C135R	0.990
21:39178604:A:G	L167P	0.989
21:39180401:A:G	W93R	0.989
21:39180401:A:T	W93R	0.989
21:39183366:C:T	G7E	0.989
21:39178454:G:T	A217E	0.988
21:39183368:G:C	F6L	0.988
21:39183368:G:T	F6L	0.988
21:39183370:A:G	F6L	0.988
21:39183378:G:T	A3D	0.988
21:39181792:G:T	A74D	0.986
21:39177532:A:G	L232P	0.985
21:39178474:A:C	N210K	0.985
21:39178474:A:T	N210K	0.985
21:39183367:C:G	G7R	0.985
21:39183367:C:T	G7R	0.985
21:39179946:T:G	Q145P	0.984

dbSNP variants (sampled 300 via entrez): RS1000476375 (21:39180168 A>G), RS1000554284 (21:39177034 T>A,C), RS1000882905 (21:39184093 G>A), RS1000899160 (21:39183542 C>G,T), RS1000950919 (21:39183668 T>C), RS1000977260 (21:39184296 G>A), RS1001001968 (21:39183833 T>A), RS1001169064 (21:39183149 A>G), RS1001494233 (21:39178973 G>A,C), RS1002226504 (21:39183921 C>A,G), RS1002337863 (21:39178981 T>A), RS1002411258 (21:39183730 A>C,G), RS1002579415 (21:39178223 G>A), RS1002828090 (21:39183906 T>C), RS1003179519 (21:39184742 A>C)

Disease associations

OMIM: gene MIM:605296 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

23 associations (top):

Study	Trait	p-value
GCST000225_5	Inflammatory bowel disease	4.000000e-12
GCST000563_3	Ankylosing spondylitis	8.000000e-20
GCST000624_4	Ulcerative colitis	1.000000e-08
GCST000965_5	C-reactive protein levels	2.000000e-07
GCST002147_19	Fibrinogen	2.000000e-11
GCST003097_34	Pediatric autoimmune diseases	5.000000e-08
GCST003194_17	Fibrinogen levels	3.000000e-20
GCST003518_70	Daytime sleep phenotypes	3.000000e-06
GCST004030_11	Primary sclerosing cholangitis	4.000000e-13
GCST004121_18	Fibrinogen levels	5.000000e-16
GCST004122_35	Fibrinogen levels	2.000000e-14
GCST006105_10	Eye morphology	2.000000e-06
GCST006670_3	Primary sclerosing cholangitis	3.000000e-17
GCST006863_5	Takayasu arteritis	4.000000e-07
GCST007614_6	C-reactive protein levels	8.000000e-26
GCST008839_114	Height	1.000000e-10
GCST009391_692	Metabolite levels	9.000000e-06
GCST010244_378	Triglyceride levels	1.000000e-10
GCST011494_104	Daytime nap	9.000000e-09
GCST90010717_4	Finger osteoarthritis severity (hand Klsum)	6.000000e-07
GCST90011770_83	Glaucoma (primary open-angle)	8.000000e-07
GCST90011898_165	Alanine aminotransferase levels	6.000000e-11
GCST90011900_15	Serum alkaline phosphatase levels	1.000000e-08

EFO canonical traits (5, from GWAS)

EFO ID	Trait name
EFO:0004458	C-reactive protein measurement
EFO:0007828	daytime rest measurement
EFO:0008529	kynurenine measurement
EFO:0004530	triglyceride measurement
EFO:0004533	alkaline phosphatase measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3885624 (PROTEIN COMPLEX)

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

ChEMBL bioactivities

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

pChembl	Type	Value	Unit	Molecule
5.22	IC50	6000	nM	CHEMBL1097925

PubChem BioAssay actives

1 with measured affinity, of 49 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
(2S)-2-[[(2S,4E)-4-[[(1R,2R,4aS,8aR)-2-methyl-1,2,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]-hydroxymethylidene]-1-methyl-3,5-dioxopyrrolidin-2-yl]methyl]-2-hydroxy-3-methylbutanoic acid	477402: Inhibition of PAC1/PAC2 interaction by protein fragment complementation assay	ic50	6.0000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, increases expression, affects expression	5
cobaltous chloride	decreases expression	2
TAK-243	increases sumoylation	1
uranyl acetate	affects expression	1
bisphenol A	decreases expression	1
trichostatin A	increases expression	1
sodium arsenite	decreases expression	1
CGP 52608	affects binding, increases reaction	1
K 7174	decreases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression	1
ICG 001	decreases expression	1
dorsomorphin	affects cotreatment, increases expression	1
bisphenol AF	increases expression	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
Acetaminophen	decreases expression	1
Air Pollutants	decreases expression, increases abundance	1
Caffeine	decreases phosphorylation	1
Enzyme Inhibitors	increases O-linked glycosylation, decreases activity	1
Formaldehyde	decreases expression	1
Hydrogen Peroxide	affects expression	1
Isoniazid	decreases expression	1
Ivermectin	decreases expression	1
Manganese	decreases expression	1
Plant Extracts	decreases expression	1
Quercetin	decreases expression	1
Rotenone	decreases expression	1
Smoke	decreases expression	1
Thiram	decreases expression	1
Tretinoin	decreases expression	1
Uranium	affects expression	1

ChEMBL screening assays

5 unique, capped per target: 5 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1111853	Binding	Inhibition of PAC1/PAC2 interaction by protein fragment complementation assay	JBIR-22, an inhibitor for protein-protein interaction of the homodimer of proteasome assembly factor 3. — J Nat Prod

Clinical trials (associated diseases)

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