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USP1

gene
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Summary

USP1 (ubiquitin specific peptidase 1, HGNC:12607) is a protein-coding gene on chromosome 1p31.3, encoding Ubiquitin carboxyl-terminal hydrolase 1 (O94782). Negative regulator of DNA damage repair which specifically deubiquitinates monoubiquitinated FANCD2. It is a selective cancer dependency (DepMap: 18.3% of cell lines).

This gene encodes a member of the ubiquitin-specific processing (UBP) family of proteases that is a deubiquitinating enzyme (DUB) with His and Cys domains. This protein is located in the cytoplasm and cleaves the ubiquitin moiety from ubiquitin-fused precursors and ubiquitinylated proteins. The protein specifically deubiquitinates a protein in the Fanconi anemia (FA) DNA repair pathway. Alternate transcriptional splice variants have been characterized.

Source: NCBI Gene 7398 — RefSeq curated summary.

At a glance

  • Gene–disease (curated): Tourette syndrome (No Known Disease Relationship, GenCC)
  • GWAS associations: 13
  • Clinical variants (ClinVar): 93 total
  • Druggable target: yes — 4 molecules with ChEMBL bioactivity
  • Cancer dependency (DepMap): dependent in 18.3% of screened cell lines
  • MANE Select transcript: NM_003368

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:12607
Approved symbolUSP1
Nameubiquitin specific peptidase 1
Location1p31.3
Locus typegene with protein product
StatusApproved
Ensembl geneENSG00000162607
Ensembl biotypeprotein_coding
OMIM603478
Entrez7398

Gene structure

Transcript identifiers

Ensembl transcripts: 12 — 12 protein_coding

ENST00000339950, ENST00000371146, ENST00000442679, ENST00000452143, ENST00000899247, ENST00000924083, ENST00000956643, ENST00000956644, ENST00000956645, ENST00000956646, ENST00000956647, ENST00000956648

RefSeq mRNA: 3 — MANE Select: NM_003368 NM_001017415, NM_001017416, NM_003368

CCDS: CCDS621

Canonical transcript exons

ENST00000339950 — 9 exons

ExonStartEnd
ENSE000010667706244473862445429
ENSE000010667716244148862441608
ENSE000010667736244846562448666
ENSE000010667746244219562442299
ENSE000010667756244315962443319
ENSE000010667786244734162447511
ENSE000012346906243704962437400
ENSE000013761756243979962440037
ENSE000018161886245024662451804

Expression profiles

Bgee: expression breadth ubiquitous, 293 present calls, max score 98.98.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 27.4838 / max 620.6054, expressed in 1796 samples.

FANTOM5 promoters (10 alternative TSS)

Promoter IDTPM avgSamples expressed
315119.65651751
31472.56701028
31502.11541124
31450.8561467
31480.7442380
31490.6372299
31460.3765146
2015280.2612101
31520.197691
31530.072016

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
secondary oocyteCL:000065598.98gold quality
ventricular zoneUBERON:000305397.86gold quality
spermCL:000001997.55gold quality
oocyteCL:000002397.50gold quality
trabecular bone tissueUBERON:000248397.26gold quality
ganglionic eminenceUBERON:000402396.72gold quality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099196.60gold quality
endothelial cellCL:000011596.56gold quality
embryoUBERON:000092296.46gold quality
male germ cellCL:000001596.22gold quality
germinal epithelium of ovaryUBERON:000130495.83gold quality
cartilage tissueUBERON:000241895.82gold quality
tibiaUBERON:000097995.58gold quality
parietal pleuraUBERON:000240095.56gold quality
pleuraUBERON:000097795.23gold quality
upper leg skinUBERON:000426295.13gold quality
skin of hipUBERON:000155495.11gold quality
visceral pleuraUBERON:000240195.00gold quality
calcaneal tendonUBERON:000370194.96gold quality
palpebral conjunctivaUBERON:000181294.90gold quality
parotid glandUBERON:000183194.71gold quality
caput epididymisUBERON:000435894.64gold quality
corpus epididymisUBERON:000435994.46gold quality
oral cavityUBERON:000016794.26gold quality
esophagus squamous epitheliumUBERON:000692094.21gold quality
cauda epididymisUBERON:000436094.15gold quality
mucosa of sigmoid colonUBERON:000499393.99gold quality
mammary ductUBERON:000176593.87gold quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047393.85gold quality
renal glomerulusUBERON:000007493.79gold quality

Single-cell (SCXA)

Detected in 9 experiment(s), a significant marker in 6.

ExperimentMarker?Max mean expression
E-MTAB-10290yes191.19
E-CURD-112yes43.24
E-CURD-122yes22.63
E-HCAD-5yes19.08
E-ANND-3yes7.84
E-MTAB-10553yes7.05
E-GEOD-100618no393.49
E-MTAB-6386no311.94
E-MTAB-6058no267.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

89 targeting USP1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-3163100.0077.238605
HSA-MIR-4455100.0065.481587
HSA-MIR-340-5P100.0072.504437
HSA-MIR-1277-5P100.0073.955056
HSA-MIR-5011-5P100.0083.465820
HSA-MIR-190A-3P100.0080.355520
HSA-MIR-5692B100.0071.322622
HSA-MIR-5692C100.0071.322622
HSA-MIR-8485100.0077.574731
HSA-MIR-428299.9975.366408
HSA-MIR-548C-3P99.9974.017587
HSA-MIR-453199.9969.703181
HSA-MIR-4789-5P99.9870.762721
HSA-MIR-1213699.9872.815713
HSA-MIR-806899.9873.852376
HSA-LET-7F-2-3P99.9870.982588
HSA-MIR-1185-1-3P99.9871.042593
HSA-MIR-1185-2-3P99.9871.042593
HSA-MIR-60799.9773.625593
HSA-MIR-548AT-5P99.9670.832666
HSA-MIR-365899.9673.874379
HSA-MIR-381-3P99.9371.872854
HSA-MIR-314399.9371.963104
HSA-MIR-30099.9271.762856
HSA-MIR-10527-5P99.9172.283754
HSA-MIR-367199.9073.043897
HSA-MIR-124-3P99.8973.743043
HSA-MIR-506-3P99.8973.553057
HSA-MIR-548E-5P99.8972.734486
HSA-MIR-30A-3P99.8769.742928

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 18.3% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 40)

  • USP1 deubiquitinates FANCD2 protein when cells exit S phase or recommence cycling after a DNA damage insult and may play a critical role in the Fanconi anemia pathway by recycling FANCD2. (PMID:15694335)
  • USP1-regulated and damage-specific DNA-binding protein 1 (DDB1)-dependent mechanisms that are involved in the downregulation of activated CHK1 in human cells. (PMID:21389083)
  • Studies indicate that USP1 and ELG1 as regulators of PCNA ubiquitylation. (PMID:21640107)
  • USP1 levels were kept low in G1 to provide a permissive condition for inducing proliferating cell nuclear antigen (PCNA) monoubiquitination in response to ultraviolet (UV) damage before DNA replication. (PMID:21768287)
  • Study shows that the deubiquitinating enzyme USP1 promotes ID protein stability and stem cell-like characteristics in osteosarcoma. (PMID:21925315)
  • data identified a novel USP1-PHLPP1-Akt signaling axis, and decreased USP1 level in lung cancer cells may play an important role in lung cancer progress. (PMID:22426999)
  • USP1 and UAF1 form a complex in the cytoplasm that subsequently translocates to the nucleus through import mediated by USP1 nuclear localization signals. (PMID:22701671)
  • Our findings revealed an intriguing mechanism of regulating USP1 activity that combines phosphorylation of a key serine residue in USP1 and the specific interaction of USP1 with a WD40-repeat protein UAF1 (PMID:23116119)
  • Coimmunoprecipitation experiments indicated that human papillomavirus type 31 E1 assembles into a ternary complex with UAF1 and any one of these three USPs: USP1, USP12 and USP46. (PMID:24850727)
  • USP1 phosphorylation at S313 is not critical for PCNA deubiquitination, neither for binding to UAF1 in a cellular environment. (PMID:25744535)
  • USP1, p21 and Spartan are translesion DNA synthesis regulators. (Review) (PMID:26002196)
  • Ubiquitination-specific proteases 1 (USP1)-mediated protein stabilization promotes glioblastoma (GBM) stem-like cells maintenance and treatment resistance, thereby providing a rationale for USP1 inhibition as a potential therapeutic approach against GBM. (PMID:26032834)
  • No correlation was observed between the protein level of ubiquitin-specific protease 1 (USP1) and ubiquitinated PCNA in BAF180 expressing cells (PMID:26117423)
  • analysis of the function and regulation of the USP1-UAF1 complex (PMID:26758085)
  • Translational regulation of the mRNA encoding USP1 is involved in the DNA damage response as a determinant of cisplatin resistance. (PMID:26825230)
  • High USP1 expression is associated with glioma. (PMID:26951930)
  • USP1-UAF1 complex promotes homologous recombination repair via multiple mechanisms: through FANCD2 deubiquitination, as well as by interacting with RAD51AP1. (PMID:27463890)
  • The results suggest that silencing USP1 inhibits cell proliferation and invasion in U2OS cells. Therefore, USP1 may provide a novel therapeutic target for the treatment of osteosarcoma. (PMID:27840911)
  • Our preclinical studies provide the framework for clinical evaluation of USP1 inhibitors, alone or in combination, as a potential novel multiple myeloma therapy. (PMID:28270494)
  • There is evidence that USP1/WDR48 complex promotes cancer stem cell conservation and regulation of DNA damage repair. [REVIEW] (PMID:28302046)
  • These results outline a novel mechanism for the control of TBK1 activity and suggest USP1-UAF1 complex as a potential target for the prevention of viral diseases. (PMID:29138248)
  • USP1 (ubiquitin specific peptidase 1) has been identified as a key player in the modulation of ULK1 K63-linked deubiquitination. (PMID:30335599)
  • High USP1 expression is associated with Glioma Tumorigenesis. (PMID:30425057)
  • USP1 and capital ER, Cyrilliccapital EN, Cyrillic domain of Bcr-Abl oncoprotein colocalize in a model chronic myeloid leukemia cell system. (PMID:30480413)
  • Three crystal structures have been reported of a CRL2 substrate receptor, KLHDC2, in complex with the diglycine-ending C-end degrons of an early terminated selenoprotein, SelK, and the N-terminal proteolytic fragment of USP1. (PMID:30526872)
  • USP1-mediated deubiquitination and stabilization of KPNA2 are revealed as the downstream events crucial for USP1-pro-metastatic function. (PMID:30531833)
  • USP1 exhibits DNA-mediated activation at the replication fork, protects the fork, and promotes survival in BRCA1-deficient tumor cells. (PMID:30576655)
  • In this report, the authors provide evidence that the previously described interaction between the viral E1 helicase and the cellular UAF1-USP1 deubiquitinating enzyme complex is required for the completion of the bidirectional theta replication of the human papilloma virus type 11 genome and the subsequent initiation of the unidirectional replication. (PMID:30890612)
  • USP1 is phosphorylated by ATM and ATR and binds to Snail. Knockout or pharmacological inhibition of USP1 increased platinum sensitivity and decreased metastatic dissemination in a Snail-dependent manner. (PMID:31086816)
  • Inhibition of USP1, a new partner of Bcr-Abl, results in decrease of Bcr-Abl level in K562 cells. (PMID:32602291)
  • Comprehensive analysis of ubiquitin-specific protease 1 reveals its importance in hepatocellular carcinoma. (PMID:32951278)
  • Inhibition of USP1 induces apoptosis via ID1/AKT pathway in B-cell acute lymphoblastic leukemia cells. (PMID:33390793)
  • USP1-WDR48 deubiquitinase complex enhances TGF-beta induced epithelial-mesenchymal transition of TNBC cells via stabilizing TAK1. (PMID:33461373)
  • Structural basis of FANCD2 deubiquitination by USP1-UAF1. (PMID:33795880)
  • A new role of GRP75-USP1-SIX1 protein complex in driving prostate cancer progression and castration resistance. (PMID:34079090)
  • Mutation of aspartic acid 199 in USP1 disrupts its deubiquitinating activity and impairs DNA repair. (PMID:34128540)
  • USP1-dependent RPS16 protein stability drives growth and metastasis of human hepatocellular carcinoma cells. (PMID:34154657)
  • Tumor suppressor functions of miRNA-375 in nasopharyngeal carcinoma through inhibition of ubiquitin-specific protease 1 expression. (PMID:34626803)
  • USP1 Promotes GC Metastasis via Stabilizing ID2. (PMID:34873426)
  • Ubiquitin-specific protease 1 overexpression indicates poor prognosis and promotes proliferation, migration, and invasion of gastric cancer cells. (PMID:34990966)

Cross-species orthologs

3 orthologs

OrganismSymbolGene ID
danio_reriousp1ENSDARG00000056414
mus_musculusUsp1ENSMUSG00000028560
rattus_norvegicusUsp1ENSRNOG00000007890

Paralogs (71): USP2 (ENSG00000036672), USP28 (ENSG00000048028), USP36 (ENSG00000055483), USP13 (ENSG00000058056), USP33 (ENSG00000077254), USP40 (ENSG00000085982), USP48 (ENSG00000090686), USP14 (ENSG00000101557), USP11 (ENSG00000102226), USP10 (ENSG00000103194), USP31 (ENSG00000103404), USP42 (ENSG00000106346), USP5 (ENSG00000111667), USP4 (ENSG00000114316), USP9Y (ENSG00000114374), USP34 (ENSG00000115464), USP35 (ENSG00000118369), USP45 (ENSG00000123552), USP22 (ENSG00000124422), USP9X (ENSG00000124486), USP6 (ENSG00000129204), USP29 (ENSG00000131864), USP26 (ENSG00000134588), USP30 (ENSG00000135093), USP15 (ENSG00000135655), USP37 (ENSG00000135913), USP44 (ENSG00000136014), USP20 (ENSG00000136878), USP8 (ENSG00000138592), USP3 (ENSG00000140455), USP21 (ENSG00000143258), USP43 (ENSG00000154914), USP25 (ENSG00000155313), USP16 (ENSG00000156256), USP24 (ENSG00000162402), USP49 (ENSG00000164663), USP38 (ENSG00000170185), USP50 (ENSG00000170236), USP47 (ENSG00000170242), USP32 (ENSG00000170832)

Protein

Protein identifiers

Ubiquitin carboxyl-terminal hydrolase 1 — O94782 (reviewed: O94782)

Alternative names: Deubiquitinating enzyme 1, Ubiquitin thioesterase 1, Ubiquitin-specific-processing protease 1

All UniProt accessions (3): O94782, C9JC88, C9JWX4

UniProt curated annotations — full annotation on UniProt →

Function. Negative regulator of DNA damage repair which specifically deubiquitinates monoubiquitinated FANCD2. Also involved in PCNA-mediated translesion synthesis (TLS) by deubiquitinating monoubiquitinated PCNA. Has almost no deubiquitinating activity by itself and requires the interaction with WDR48 to have a high activity.

Subunit / interactions. Interacts with FANCD2 and PCNA. Interacts with WDR48. Interacts with ATAD5; the interaction regulates USP1-mediated PCNA deubiquitination.

Subcellular location. Nucleus.

Post-translational modifications. Autocatalytic cleavage of USP1 following UV irradiation inactivates it, leading to an increase in ubiquitinated PCNA, recruitment of POLH and translesion synthesis. Ubiquitinated by the CRL2(KLHDC2) complex following autocatalytic cleavage, leading to its degradation: the CRL2(KLHDC2) complex recognizes the diglycine (Gly-Gly) at the C-terminus.

Induction. Down-regulated following DNA damage.

Miscellaneous. HEK293T cells expressing reduced levels of USP1 show a higher level of ubiquitinated PCNA and an increase in point mutations upon UV irradiation.

Similarity. Belongs to the peptidase C19 family.

RefSeq proteins (3): NP_001017415, NP_001017416, NP_003359* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR001394Peptidase_C19_UCHDomain
IPR018200USP_CSConserved_site
IPR028889USPDomain
IPR033815USP1Domain
IPR038765Papain-like_cys_pep_sfHomologous_superfamily
IPR050164Peptidase_C19Family

Pfam: PF00443

UniProt features (65 total): strand 19, helix 15, turn 7, modified residue 6, compositionally biased region 4, region of interest 4, mutagenesis site 3, chain 2, active site 2, site 1, domain 1, sequence conflict 1

Structure

Experimental structures (PDB)

15 structures.

PDBMethodResolution (Å)
7ZH4ELECTRON MICROSCOPY2.49
6DO5X-RAY DIFFRACTION2.5
7ZH3ELECTRON MICROSCOPY2.5
9DI2ELECTRON MICROSCOPY2.6
9DI1ELECTRON MICROSCOPY2.7
9FCJELECTRON MICROSCOPY2.7
8A9JELECTRON MICROSCOPY2.8
8A9KELECTRON MICROSCOPY2.85
9HNWELECTRON MICROSCOPY3.04
9N9YX-RAY DIFFRACTION3.15
7AY2X-RAY DIFFRACTION3.2
9FCIELECTRON MICROSCOPY3.2
9EBSELECTRON MICROSCOPY3.3
7AY0X-RAY DIFFRACTION3.6
7AY1ELECTRON MICROSCOPY3.7

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-O94782-F160.240.29

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 (3): 90 (nucleophile); 593 (proton acceptor); 671–672 (cleavage; by autolysis)

Post-translational modifications (6): 16, 42, 67, 313, 475, 768

Mutagenesis-validated functional residues (3):

PositionPhenotype
90loss of catalytic activity including autolysis.
444strongly reduces interaction with wdr48 and activation by wdr48.
670–671loss of autolysis-mediated degradation upon uv irradiation. no effect on catalytic activity.

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

IDPathway
R-HSA-110314Recognition of DNA damage by PCNA-containing replication complex
R-HSA-6783310Fanconi Anemia Pathway

MSigDB gene sets: 312 (showing top): PID_FANCONI_PATHWAY, AHRARNT_01, MORF_DNMT1, RODRIGUES_THYROID_CARCINOMA_ANAPLASTIC_UP, GNF2_MSH2, GOBP_POSITIVE_REGULATION_OF_DNA_BIOSYNTHETIC_PROCESS, MORF_SMC1L1, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_UP, MORF_BUB1, GOBP_SKELETAL_SYSTEM_DEVELOPMENT, FISCHER_G1_S_CELL_CYCLE, STARK_PREFRONTAL_CORTEX_22Q11_DELETION_DN, GEORGES_CELL_CYCLE_MIR192_TARGETS, MORF_RRM1, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN

GO Biological Process (12): skeletal system development (GO:0001501), DNA repair (GO:0006281), regulation of DNA repair (GO:0006282), proteolysis (GO:0006508), response to UV (GO:0009411), protein deubiquitination (GO:0016579), regulation of protein stability (GO:0031647), monoubiquitinated protein deubiquitination (GO:0035520), positive regulation of receptor signaling pathway via JAK-STAT (GO:0046427), positive regulation of error-prone translesion synthesis (GO:1904333), DNA damage response (GO:0006974), cell surface receptor signaling pathway via JAK-STAT (GO:0007259)

GO Molecular Function (6): cysteine-type endopeptidase activity (GO:0004197), cysteine-type deubiquitinase activity (GO:0004843), peptidase activity (GO:0008233), protein binding (GO:0005515), cysteine-type peptidase activity (GO:0008234), hydrolase activity (GO:0016787)

GO Cellular Component (3): nucleus (GO:0005634), nucleoplasm (GO:0005654), cytosol (GO:0005829)

Reactome top-level categories

Rollup of top-2 pathways:

CategoryPathways
DNA Damage Bypass1
DNA Repair1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cysteine-type peptidase activity2
cellular anatomical structure2
system development1
DNA metabolic process1
DNA damage response1
DNA repair1
regulation of DNA metabolic process1
regulation of cellular response to stress1
protein metabolic process1
response to light stimulus1
cysteine-type deubiquitinase activity1
protein modification by small protein removal1
regulation of biological quality1
protein deubiquitination1
cell surface receptor signaling pathway via JAK-STAT1
regulation of receptor signaling pathway via JAK-STAT1
positive regulation of receptor signaling pathway via STAT1
error-prone translesion synthesis1
positive regulation of response to stimulus1
regulation of error-prone translesion synthesis1
positive regulation of DNA biosynthetic process1
cellular response to stress1
cell surface receptor signaling pathway via STAT1
endopeptidase activity1
deubiquitinase activity1
hydrolase activity1
catalytic activity, acting on a protein1
binding1
peptidase activity1
catalytic activity1
intracellular membrane-bounded organelle1
nuclear lumen1
cytoplasm1

Protein interactions and networks

STRING

2158 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
USP1WDR48Q8TAF3998
USP1VHLP40337920
USP1ZUP1Q96AP4910
USP1FANCD2Q9BXW9901
USP1USP30Q70CQ3875
USP1FANCIQ9NVI1810
USP1YOD1Q5VVQ6810
USP1JOSD1Q15040793
USP1ATAD5Q96QE3785
USP1JOSD2Q8TAC2781
USP1UCHL3P15374757
USP1RAD18Q9NS91729
USP1FANCLQ9NW38716
USP1RAD51AP1Q96B01708
USP1USP14P54578698

IntAct

56 interactions, top by confidence:

ABTypeScore
USP1WDR48psi-mi:“MI:0915”(physical association)0.820
PHLPP2NHERF1psi-mi:“MI:0914”(association)0.760
USP1PHLPP1psi-mi:“MI:0914”(association)0.740
KPNA1TCERG1psi-mi:“MI:0914”(association)0.640
PHLPP1USP12psi-mi:“MI:0914”(association)0.570
WDR48USP12psi-mi:“MI:0914”(association)0.530
KPNB1POM121Cpsi-mi:“MI:0914”(association)0.530
RAD51AP1USP12psi-mi:“MI:0914”(association)0.530
OPALINBTAF1psi-mi:“MI:0914”(association)0.530
SGO1USP12psi-mi:“MI:0914”(association)0.530
USP1UFL1psi-mi:“MI:0407”(direct interaction)0.440
USP1WDR48psi-mi:“MI:0915”(physical association)0.400
Dctn3psi-mi:“MI:0914”(association)0.350
Pip4k2cLAMA5psi-mi:“MI:0914”(association)0.350
USP43DKFZP586J0619psi-mi:“MI:0914”(association)0.350
RSRP1DMWDpsi-mi:“MI:0914”(association)0.350
KPNA1MTA3psi-mi:“MI:0914”(association)0.350
Wdr48DMWDpsi-mi:“MI:0914”(association)0.350
CERKWDR46psi-mi:“MI:0914”(association)0.350
SGTBARHGAP32psi-mi:“MI:0914”(association)0.350
SYNCRIPARHGAP32psi-mi:“MI:0914”(association)0.350
BAG6CNOT1psi-mi:“MI:0914”(association)0.350
SORT1SH3PXD2Bpsi-mi:“MI:0914”(association)0.350
TOR1AIP1USP1psi-mi:“MI:0914”(association)0.350
KATNA1KATNBL1psi-mi:“MI:0914”(association)0.350

BioGRID (290): USP1 (Affinity Capture-Western), USP1 (Affinity Capture-MS), USP1 (Affinity Capture-Western), USP1 (Affinity Capture-MS), USP1 (Affinity Capture-Western), USP1 (Affinity Capture-Western), USP1 (Affinity Capture-Western), USP1 (Affinity Capture-Western), FANCD2 (Co-fractionation), FZR1 (Affinity Capture-Western), USP1 (Biochemical Activity), USP1 (Affinity Capture-Western), USP1 (Affinity Capture-MS), USP1 (Affinity Capture-MS), WDR48 (Affinity Capture-Western)

ESM2 similar proteins: B0BLU1, B2RYR0, B8A5Y1, E1C213, E2RK09, E7F6T8, F1N5V1, F1SRY5, O94782, O96028, P14629, P52479, Q0IIM1, Q12766, Q3KR59, Q4G0A6, Q569C3, Q5BLK4, Q5RJ80, Q5VYS8, Q68FE9, Q6IE24, Q6NRE4, Q6P1H6, Q6P4F7, Q6P7W0, Q6ZPF3, Q70EL1, Q7TP65, Q7ZVU1, Q80XJ2, Q80Y19, Q86T82, Q8BFU3, Q8BJQ2, Q8BL06, Q8BMI4, Q8BVE8, Q8BW70, Q8BZ05

Diamond homologs: A1CIL1, A1CW53, A2Q9N1, A2XDG4, A3AF13, A4FUN7, A5D9H7, A5WWB0, A6QR55, B0Y4P5, B2GUZ1, B8NSV5, C0HB46, D0RB01, E2RK09, E7F6T8, E9QG68, F1M625, F1N5V1, F1SRY5, F6Z5C0, M9PD06, O22207, O24454, O74442, O75317, O94782, O94966, P0C8Z3, P34547, P35123, P38187, P39538, P39967, P40818, P43593, P51784, P55824, P62068, P62069

SIGNOR signaling

5 interactions.

AEffectBMechanism
USP1“down-regulates activity”FANCD2deubiquitination
WDR48“up-regulates activity”USP1binding
USP1“up-regulates quantity by stabilization”DGCR8deubiquitination
USP1“down-regulates activity”FANCIdeubiquitination
CDK1“up-regulates activity”USP1phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 64 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

PathwayPartnersFoldFDR
Cytokine Signaling in Immune system67.2×7e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance81
Likely benign3
Benign2

Top pathogenic / likely-pathogenic (0)

SpliceAI

1332 predictions. Top by Δscore:

VariantEffectΔscore
1:62440033:GAAAT:Gdonor_gain1.0000
1:62440038:G:GGdonor_gain1.0000
1:62441477:A:AGacceptor_gain1.0000
1:62441478:T:Gacceptor_gain1.0000
1:62441479:A:AGacceptor_gain1.0000
1:62441483:CATA:Cacceptor_loss1.0000
1:62441484:A:AGacceptor_gain1.0000
1:62441484:ATAGT:Aacceptor_gain1.0000
1:62441485:T:Gacceptor_gain1.0000
1:62441486:A:AGacceptor_gain1.0000
1:62441486:AGT:Aacceptor_gain1.0000
1:62441487:G:GGacceptor_gain1.0000
1:62441487:GT:Gacceptor_gain1.0000
1:62441487:GTG:Gacceptor_gain1.0000
1:62441487:GTGAT:Gacceptor_gain1.0000
1:62441604:TTCAG:Tdonor_loss1.0000
1:62441605:TCAG:Tdonor_loss1.0000
1:62441606:CAGG:Cdonor_loss1.0000
1:62441607:AG:Adonor_loss1.0000
1:62441608:GGTA:Gdonor_loss1.0000
1:62441609:G:Cdonor_loss1.0000
1:62441610:T:Gdonor_loss1.0000
1:62442192:TA:Tacceptor_loss1.0000
1:62442194:G:GAacceptor_loss1.0000
1:62442255:A:Gacceptor_gain1.0000
1:62442300:GTA:Gdonor_loss1.0000
1:62442301:T:Gdonor_loss1.0000
1:62443157:AG:Aacceptor_gain1.0000
1:62443158:GG:Gacceptor_gain1.0000
1:62445379:G:GTdonor_gain1.0000

AlphaMissense

5220 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
1:62441572:T:AN85K1.000
1:62441572:T:GN85K1.000
1:62441581:T:AN88K1.000
1:62441581:T:GN88K1.000
1:62441585:T:CC90R1.000
1:62441586:G:AC90Y1.000
1:62441587:C:GC90W1.000
1:62441592:T:CL92P1.000
1:62441596:T:AN93K1.000
1:62441596:T:GN93K1.000
1:62441597:A:CS94R1.000
1:62441599:T:AS94R1.000
1:62441599:T:GS94R1.000
1:62441604:T:CL96P1.000
1:62444776:A:CD199A1.000
1:62444776:A:GD199G1.000
1:62444776:A:TD199V1.000
1:62447385:G:CG432R1.000
1:62447392:T:CL434P1.000
1:62447409:T:AC440S1.000
1:62447409:T:CC440R1.000
1:62447410:G:AC440Y1.000
1:62447410:G:CC440S1.000
1:62447411:C:GC440W1.000
1:62447418:T:AC443S1.000
1:62447418:T:CC443R1.000
1:62447419:G:AC443Y1.000
1:62447419:G:CC443S1.000
1:62447420:T:GC443W1.000
1:62447448:T:CF453L1.000

dbSNP variants (sampled 300 via entrez): RS1000100118 (1:62445026 A>G), RS1000438194 (1:62451802 G>A), RS1000535672 (1:62434889 G>A), RS1000782596 (1:62439441 C>T), RS1001065479 (1:62443299 G>A,T), RS1001076883 (1:62443626 G>A), RS1001281953 (1:62442882 A>G), RS1001300706 (1:62448948 C>T), RS1001414124 (1:62449846 G>A), RS1001434485 (1:62437434 G>C,T), RS1001613484 (1:62437049 G>A,T), RS1001825402 (1:62446365 G>A), RS1001913440 (1:62440721 C>T), RS1002056171 (1:62440926 G>C), RS1002562687 (1:62435762 A>G)

Disease associations

OMIM: gene MIM:603478 | disease phenotypes:

GenCC curated gene-disease

DiseaseClassificationInheritance
Tourette syndromeNo Known Disease RelationshipUnknown

Mondo (1): Tourette syndrome (MONDO:0007661)

Orphanet (0):

HPO phenotypes

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

GWAS associations

13 associations (top):

StudyTraitp-value
GCST002321_10Lipid traits9.000000e-06
GCST002690_1Very long-chain saturated fatty acid levels (fatty acid 20:0)7.000000e-07
GCST003044_54Crohn’s disease7.000000e-08
GCST004132_95Crohn’s disease4.000000e-06
GCST006920_5Regular attendance at a gym or sports club1.000000e-08
GCST009240_439Serum metabolite levels (CMS)3.000000e-10
GCST009602_6Metabolic syndrome1.000000e-13
GCST010244_7Triglyceride levels5.000000e-304
GCST90002390_3Mean corpuscular hemoglobin6.000000e-21
GCST90002392_167Mean corpuscular volume3.000000e-21
GCST90002396_133Mean reticulocyte volume8.000000e-12
GCST90002397_632Mean spheric corpuscular volume3.000000e-27
GCST90002403_7Red blood cell count3.000000e-12

EFO canonical traits (8, from GWAS)

EFO IDTrait name
EFO:0004611low density lipoprotein cholesterol measurement
EFO:0006796very long-chain saturated fatty acid measurement
EFO:0009592social interaction measurement
EFO:0000195metabolic syndrome
EFO:0004530triglyceride measurement
EFO:0004527mean corpuscular hemoglobin
EFO:0010701mean reticulocyte volume
EFO:0004305erythrocyte count

MeSH disease descriptors (1)

DescriptorNameTree numbers
D005879Tourette SyndromeC10.228.140.079.898; C10.228.662.825.800; C10.574.500.850; C16.320.400.820; F03.625.992.850

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL1795087 (SINGLE PROTEIN), CHEMBL3430885 (PROTEIN COMPLEX)

Molecules with ChEMBL bioactivity

4 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 38,892 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL1423PIMOZIDE417,310
CHEMBL422TRIFLUOPERAZINE420,044
CHEMBL6066864FLUPENTIXOL3
CHEMBL1232461MOLIBRESIB21,538

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

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — C19: Ubiquitin-specific protease

Most potent curated ligand interactions (6 total), top 6:

LigandActionAffinityParameter
USP1 inhibitor 38-P2Inhibition8.42pIC50
KSQ-4279Inhibition7.67pIC50
TNG348Inhibition7.52pIC50
ML323Inhibition7.12pIC50
SJB2-043Inhibition6.26pIC50
compound 61 [PMID: 36221183]Inhibition5.86pIC50

Binding affinities (BindingDB)

538 measured of 959 human assays (959 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValuePatent
2-(4-Chloro-1-isopropyl-1H-pyrazol- 5-yl)-N-(4-(1-methyl-4- (trifluoromethyl)-1H-imidazol-2- yl)benzyl)furo[3,2-d]pyrimidin-4- amineIC500.45 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
5-Ethynyl-2-(2-isopropylphenyl)-N- (4-(1-methyl-4-(trifluoromethyl)-1H- imidazol-2-yl)benzyl)pyrimidin-4- amineIC500.47 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
2-(2-Cyclopropylphenyl)-5- methoxy-N-(4-(1-methyl-4- (trifluoromethyl)-1H-imidazol-2- yl)benzyl)pyrimidin-4-amineIC500.8 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
US20250368667, Compound 48IC500.92 nMUS-20250368667: USP1 INHIBITOR
US20250368667, Compound 151IC501 nMUS-20250368667: USP1 INHIBITOR
2-(2-Cyclopropylphenyl)-N-(4-(1- methyl-4-(trifluoromethyl)-1H- imidazol-2-yl)benzyl)furo[3,2- d]pyrimidin-4-amineIC501 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
4-[[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methylamino]-2-(2-propan-2-ylphenyl)pyrimidine-5-carbonitrileIC501.1 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
5-(Difluoromethoxy)-2-(2- isopropylphenyl)-N-(4-(1-methyl-4- (trifluoromethyl)-1H-imidazol-2- yl)benzyl)pyrimidin-4-amineIC501.1 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
2-(4-Chloro-1-isopropyl-1H-pyrazol- 5-yl)-5-methoxy-N-(4-(1-methyl-4- (trifluoromethyl)-1H-imidazol-2- yl)benzyl)pyrimidin-4-amineIC501.1 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
5-methoxy-N-[[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]-2-(2-propan-2-ylphenyl)pyrimidin-4-amineIC501.2 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
5-methoxy-N-[[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]cyclohexyl]methyl]-2-(2-propan-2-ylphenyl)pyrimidin-4-amineIC501.2 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
N-[[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]-2-(2-propan-2-ylphenyl)furo[3,2-d]pyrimidin-4-amineIC501.2 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
2-(4-Chloro-1-isopropyl-1H-pyrazol- 5-yl)-N-(4-(5-methyl-3- (trifluoromethyl)-1H-pyrazol-1- yl)benzyl)furo[3,2-d]pyrimidin-4- amineIC501.2 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
US20250368667, Compound 98IC501.26 nMUS-20250368667: USP1 INHIBITOR
US20250368667, Compound 43IC501.29 nMUS-20250368667: USP1 INHIBITOR
Methyl 2-(2-(2-isopropylphenyl)-4- ((4-(1-methyl-4-(trifluoromethyl)- 1H-imidazol-2- yl)benzyl)amino)pyrimidin-5- yl)acetateIC501.3 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
US20250368667, Compound 136IC501.34 nMUS-20250368667: USP1 INHIBITOR
2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-5-methoxy-N-methyl-N-[[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]pyrimidin-4-amineIC501.4 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
2-(4-Chloro-1-isopropyl-1H-pyrazol- 5-yl)-5-methoxy-N-(4-(5-methyl-3- (trifluoromethyl)-1H-pyrazol-1- yl)benzyl)pyrimidin-4-amineIC501.4 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
5-Ethynyl-2-(1-isopropyl-4-methyl- 1H-pyrazol-5-yl)-N-(4-(1-methyl-4- (trifluoromethyl)-1H-imidazol-2- yl)benzyl)pyrimidin-4-amineIC501.4 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-N-[[4-[1-cyclopropyl-4-(trifluoromethyl)imidazol-2-yl]cuban-1-yl]methyl]-5-methoxypyrimidin-4-amineIC501.4 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
4’-Cyclopropyl-N-(4-(1-isopropyl-4- (trifluoromethyl)-1H-imidazol-2- yl)benzyl)-5,6’-dimethoxy-N- methyl-[2,5’-bipyrimidin]-4-amineIC501.5 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
US20250368667, Compound 137IC501.54 nMUS-20250368667: USP1 INHIBITOR
2-(4-chloro-1-propan-2-ylpyrazol-5-yl)-5-methoxy-N-[[1-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]-2-oxabicyclo[2.2.2]octan-4-yl]methyl]pyrimidin-4-amineIC501.6 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
US20250368667, Compound 66IC501.62 nMUS-20250368667: USP1 INHIBITOR
2-(2-Isopropylphenyl)-N-(3- methoxy-4-(1-methyl-4- (trifluoromethyl)-1H-imidazol-2- yl)benzyl)furo[3,2-d]pyrimidin-4- amineIC501.7 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
2-(2-(Dimethylamino)phenyl)-5- methoxy-N-(4-(1-methyl-4- (trifluoromethyl)-1H-imidazol-2- yl)benzyl)pyrimidin-4-amineIC501.7 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
US20250368667, Compound 138IC501.8 nMUS-20250368667: USP1 INHIBITOR
US20250368667, Compound 114IC501.89 nMUS-20250368667: USP1 INHIBITOR
8-[[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]cyclohexyl]methyl]-2-(2-propan-2-ylphenyl)-6,7-dihydropyrimido[5,4-b][1,4]oxazineIC501.9 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
US20250368667, Compound 120IC501.97 nMUS-20250368667: USP1 INHIBITOR
8-[[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]-5-(2-propan-2-ylphenyl)-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaeneIC502.04 nMUS-20250368667: USP1 INHIBITOR
US20250368667, Compound 97IC502.1 nMUS-20250368667: USP1 INHIBITOR
2-(2-Isopropylphenyl)-5-methoxy-N- methyl-N-((1-(1-methyl-4- (trifluoromethyl)-1H-imidazol-2- yl)piperidin-4-yl)methyl)pyrimidin- 4-amineIC502.1 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
2-(2-Isopropylphenyl)-5-methoxy-N- ((1-(1-methyl-4-(trifluoromethyl)- 1H-imidazol-2-yl)piperidin-4- yl)methyl)pyrimidin-4-amineIC502.1 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
2-(2-Isopropylpyridin-3-yl)-5- methoxy-N-(4-(5-methyl-3- (trifluoromethyl)-1H-pyrazol-1- yl)benzyl)pyrimidin-4-amineIC502.1 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
2-(4-Chloro-1-isopropyl-1H-pyrazol- 5-yl)-N-(4-(pyridin-2- yl)benzyl)furo[3,2-d]pyrimidin-4- amineIC502.1 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
2-(2-Cyclopropylpyridin-3-yl)-5- (difluoromethoxy)-N-(4-(1-methyl- 4-(trifluoromethyl)-1H-imidazol-2- yl)benzyl)pyrimidin-4-amineIC502.2 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-5-methoxy-N-[[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]cuban-1-yl]methyl]pyrimidin-4-amineIC502.2 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
N-[[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]-2-(2-propan-2-ylphenyl)pyrido[3,2-d]pyrimidin-4-amineIC502.3 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
2-(4-Chloro-1-isopropyl-1H-pyrazol- 5-yl)-5-methoxy-N-((1-(1-methyl-4- (trifluoromethyl)-1H-imidazol-2- yl)piperidin-4-yl)methyl)pyrimidin- 4-amineIC502.3 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
2-(2-Cyclopropylphenyl)-5- methoxy-N-(2-methoxy-4-(1- methyl-4-(trifluoromethyl)-1H- imidazol-2-yl)benzyl)pyrimidin-4- amineIC502.3 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
US20250368667, Compound 93IC502.56 nMUS-20250368667: USP1 INHIBITOR
4’-Cyclopropyl-N-(4-(1-cyclopropyl- 4-(trifluoromethyl)-1H-imidazol-2- yl)benzyl)-5-fluoro-6’-methoxy-N- (methyl-d3)-[2,5’-bipyrimidin]-4- amineIC502.6 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
US20250368667, Compound 62IC502.65 nMUS-20250368667: USP1 INHIBITOR
US20250368667, Compound 63IC502.74 nMUS-20250368667: USP1 INHIBITOR
5-methoxy-N-methyl-N-[[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]-2-(2-propan-2-ylphenyl)pyrimidin-4-amineIC502.8 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
2-(2-propan-2-ylphenyl)-N-[(4-pyridin-2-ylphenyl)methyl]furo[3,2-d]pyrimidin-4-amineIC502.8 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
4-[[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methylamino]-2-(2-propan-2-ylphenyl)pyrimidine-5-carbonitrileIC502.8 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF
2-(1-Isopropyl-4-methyl-1H- pyrazol-5-yl)-5-methoxy-N-methyl- N-(4-(1-methyl-4-(trifluoromethyl)- 1H-imidazol-2-yl)benzyl)pyrimidin- 4-amineIC502.8 nMUS-20250289799: PYRIMIDINE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL USE THEREOF

ChEMBL bioactivities

935 potent at pChembl≥5 of 944 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
8.64IC502.3nMCHEMBL6167416
8.42IC503.8nMCHEMBL6169078
8.39IC504.1nMCHEMBL5558715
8.15IC507.1nMCHEMBL5593758
8.15Ki7nMCHEMBL5595820
8.06IC508.8nMCHEMBL5595820
7.96IC5011nMKSQ-4279
7.95IC5011.2nMCHEMBL5593526
7.88IC5013.1nMCHEMBL5583831
7.85IC5014.2nMCHEMBL6145929
7.79IC5016.1nMCHEMBL5592698
7.77IC5017nMCHEMBL3182437
7.73IC5018.8nMCHEMBL5594891
7.67IC5021.3nMKSQ-4279
7.64IC5022.8nMCHEMBL5595458
7.63IC5023.3nMCHEMBL5593671
7.52Kd30nMMOLIBRESIB
7.52IC5030.3nMCHEMBL6146416
7.47IC5033.9nMCHEMBL5592420
7.47IC5034nMCHEMBL5970286
7.46IC5034.4nMCHEMBL6146209
7.40IC5039.8nMCHEMBL5592802
7.37IC5043nMCHEMBL6039837
7.37IC5043nMCHEMBL3182033
7.32IC5048nMCHEMBL3181856
7.30IC5050nMCHEMBL3182033
7.26IC5055nMCHEMBL5792743
7.26IC5055nMCHEMBL5958813
7.26IC5055nMCHEMBL6012891
7.26IC5055nMCHEMBL5884913
7.26IC5055nMCHEMBL5748129
7.26IC5055nMCHEMBL5773694
7.26IC5055nMCHEMBL6036188
7.26IC5055nMCHEMBL5996439
7.26IC5055nMCHEMBL5964443
7.26IC5055nMCHEMBL5861897
7.26IC5055nMCHEMBL5898942
7.26IC5055nMCHEMBL5978315
7.26IC5055nMCHEMBL6038081
7.26IC5055nMCHEMBL5811069
7.26IC5055nMCHEMBL5969684
7.26IC5055nMCHEMBL5789237
7.26IC5055nMCHEMBL5743502
7.26IC5055nMCHEMBL5745757
7.26IC5055nMCHEMBL5868523
7.26IC5055nMCHEMBL5762400
7.26IC5055nMCHEMBL5745516
7.26IC5055nMKSQ-4279
7.26IC5055nMCHEMBL5898999
7.26IC5055nMCHEMBL5792666

PubChem BioAssay actives

116 with measured affinity, of 225 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.

CompoundAssayTypeValueUnit
9-[[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]-2-(2-propan-2-ylphenyl)-7H-purin-8-one2066585: Inhibition of human recombinant USP1 expressed in baculovirus expressed in Bac-to-Bac baculovirus expression systemic500.0041uM
2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-8-[[4-[1-propan-2-yl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]pyrido[2,3-d]pyrimidin-7-one2116480: Inhibition of USP1/UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate assessed as inhibition constant incubated for 120 mins by Lineweaver-burk plot analysiski0.0070uM
2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-8-[[4-[5-methyl-3-(trifluoromethyl)pyrazol-1-yl]phenyl]methyl]pyrido[2,3-d]pyrimidin-7-one2116468: Inhibition of USP1-UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate incubated for 2 hrs by fluorescence based analysisic500.0071uM
6-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-1-[[4-[1-propan-2-yl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]pyrazolo[3,4-d]pyrimidine2066586: Inhibition of USP1 (unknown origin)ic500.0110uM
2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-8-[[4-[1-(cyclopropylmethyl)-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]pyrido[2,3-d]pyrimidin-7-one2116468: Inhibition of USP1-UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate incubated for 2 hrs by fluorescence based analysisic500.0112uM
2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-8-[[4-[1-ethyl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]pyrido[2,3-d]pyrimidin-7-one2116468: Inhibition of USP1-UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate incubated for 2 hrs by fluorescence based analysisic500.0131uM
2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-8-[[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]pyrido[2,3-d]pyrimidin-7-one2116468: Inhibition of USP1-UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate incubated for 2 hrs by fluorescence based analysisic500.0161uM
2-(2,6-dimethoxyphenyl)-8-[[4-[1-propan-2-yl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]pyrido[2,3-d]pyrimidin-7-one2116468: Inhibition of USP1-UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate incubated for 2 hrs by fluorescence based analysisic500.0188uM
2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-8-[[3-fluoro-4-[1-propan-2-yl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]pyrido[2,3-d]pyrimidin-7-one2116468: Inhibition of USP1-UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate incubated for 2 hrs by fluorescence based analysisic500.0228uM
2-(2-fluoro-6-methoxyphenyl)-8-[[4-[1-propan-2-yl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]pyrido[2,3-d]pyrimidin-7-one2116468: Inhibition of USP1-UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate incubated for 2 hrs by fluorescence based analysisic500.0233uM
2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide2179195: Binding affinity against USP1 (unknown origin) assessed as apparent dissociation constant incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysiskd0.0300uM
2-(2-propan-2-ylphenyl)-8-[[4-[1-propan-2-yl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]pyrido[2,3-d]pyrimidin-7-one2116468: Inhibition of USP1-UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate incubated for 2 hrs by fluorescence based analysisic500.0339uM
8-[[4-[1-propan-2-yl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]-2-[2-(trifluoromethoxy)phenyl]pyrido[2,3-d]pyrimidin-7-one2116468: Inhibition of USP1-UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate incubated for 2 hrs by fluorescence based analysisic500.0398uM
5-methyl-N-[[4-(6-methyl-3-pyridinyl)phenyl]methyl]-2-(2-propan-2-ylphenyl)pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.0500uM
2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-8-[[4-[6-(trifluoromethyl)-2-pyridinyl]phenyl]methyl]pyrido[2,3-d]pyrimidin-7-one2116468: Inhibition of USP1-UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate incubated for 2 hrs by fluorescence based analysisic500.0599uM
5-methoxy-2-(2-propan-2-ylphenyl)-N-[(4-pyridin-3-ylphenyl)methyl]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.0700uM
5-methyl-2-(2-propan-2-ylphenyl)-N-[(4-pyridin-3-ylphenyl)methyl]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.0700uM
5-methyl-2-(2-propan-2-ylphenyl)-N-[[4-(triazol-1-yl)phenyl]methyl]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.0760uM
N-[[4-(6-fluoro-3-pyridinyl)phenyl]methyl]-5-methyl-2-(2-propan-2-ylphenyl)pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.0800uM
5-methyl-2-(2-propan-2-ylphenyl)-N-[(1-pyridin-3-ylpiperidin-4-yl)methyl]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.0800uM
2-(2-propan-2-ylphenyl)-N-[(4-pyridin-3-ylphenyl)methyl]furo[3,2-d]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.0800uM
2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-8-[1-[4-[1-propan-2-yl-4-(trifluoromethyl)imidazol-2-yl]phenyl]ethyl]pyrido[2,3-d]pyrimidin-7-one2116468: Inhibition of USP1-UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate incubated for 2 hrs by fluorescence based analysisic500.0839uM
5-methyl-N-[[1-(6-methyl-3-pyridinyl)piperidin-4-yl]methyl]-2-(2-propan-2-ylphenyl)pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.0900uM
2-[2-(1,1,1,2,3,3,3-heptadeuteriopropan-2-yl)phenyl]-5-methyl-N-[[4-(triazol-1-yl)phenyl]methyl]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1000uM
2-(2-propan-2-ylphenyl)-N-[(4-pyridin-3-ylphenyl)methyl]thieno[3,2-d]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1100uM
5-fluoro-2-(2-propan-2-ylphenyl)-N-[(4-pyridin-3-ylphenyl)methyl]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1100uM
5-methylsulfanyl-2-(2-propan-2-ylphenyl)-N-[(4-pyridin-3-ylphenyl)methyl]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1100uM
N-[dideuterio-[4-(triazol-1-yl)phenyl]methyl]-5-methyl-2-(2-propan-2-ylphenyl)pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1200uM
2-(2-propan-2-ylphenyl)-N-[(4-pyridin-3-ylphenyl)methyl]-7H-purin-6-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1200uM
5,6-dimethyl-2-(2-propan-2-ylphenyl)-N-[(4-pyridin-3-ylphenyl)methyl]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1200uM
5-methyl-N-[(3-methylphenyl)methyl]-2-(2-propan-2-ylphenyl)pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1300uM
2-[2-(1,1,1,3,3,3-hexadeuteriopropan-2-yl)phenyl]-5-methyl-N-[[4-(triazol-1-yl)phenyl]methyl]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1400uM
5-methyl-2-(2-propan-2-ylphenyl)-N-[(1-pyrazin-2-ylpiperidin-4-yl)methyl]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1400uM
2-(2-propan-2-ylphenyl)-N-[(4-pyridin-3-ylphenyl)methyl]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1500uM
2-(2-propan-2-ylphenyl)-N-[(4-pyridin-3-ylphenyl)methyl]-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1600uM
2-(2-cyclobutylphenyl)-5-methyl-N-[[4-(triazol-1-yl)phenyl]methyl]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1800uM
2-(2-cyclopropylphenyl)-5-methyl-N-[(4-pyridin-3-ylphenyl)methyl]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1800uM
2-(2-propan-2-ylphenyl)-N-[(4-pyridin-3-ylphenyl)methyl]quinazolin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1800uM
N-[dideuterio-[4-(triazol-1-yl)phenyl]methyl]-2-[2-(1,1,1,2,3,3,3-heptadeuteriopropan-2-yl)phenyl]-5-methylpyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1900uM
5-N,5-N-dimethyl-2-(2-propan-2-ylphenyl)-4-N-[(4-pyridin-3-ylphenyl)methyl]pyrimidine-4,5-diamine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.1900uM
8-[[4-[1-propan-2-yl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]-2-[2-(trifluoromethyl)phenyl]pyrido[2,3-d]pyrimidin-7-one2116468: Inhibition of USP1-UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate incubated for 2 hrs by fluorescence based analysisic500.1946uM
6-methyl-2-(2-propan-2-ylphenyl)-N-[(4-pyridin-3-ylphenyl)methyl]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.2100uM
2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-8-[[2,6-difluoro-4-[1-propan-2-yl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]pyrido[2,3-d]pyrimidin-7-one2116468: Inhibition of USP1-UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate incubated for 2 hrs by fluorescence based analysisic500.2457uM
2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-8-[(4-pyridin-2-ylphenyl)methyl]pyrido[2,3-d]pyrimidin-7-one2116468: Inhibition of USP1-UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate incubated for 2 hrs by fluorescence based analysisic500.2528uM
2-(2-propan-2-ylphenyl)-N-[(4-pyridin-3-ylphenyl)methyl]pyrrolo[2,1-f][1,2,4]triazin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.2600uM
5-methyl-2-(2-propan-2-ylphenyl)-N-(thiophen-2-ylmethyl)pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.2700uM
2-(2-propan-2-ylphenyl)-N-[(4-pyridin-3-ylphenyl)methyl]thieno[2,3-d]pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.2800uM
N-[(4-imidazol-1-ylphenyl)methyl]-5-methyl-2-(2-propan-2-ylphenyl)pyrimidin-4-amine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.3000uM
2-(2-propan-2-ylphenyl)-4-N-[(4-pyridin-3-ylphenyl)methyl]pyrimidine-4,5-diamine1164708: Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assayic500.3100uM
2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-8-[[2-methoxy-4-[1-propan-2-yl-4-(trifluoromethyl)imidazol-2-yl]phenyl]methyl]pyrido[2,3-d]pyrimidin-7-one2116468: Inhibition of USP1-UAF1 complex (unknown origin) using Ub-7-amido-4-methylcoumarin as substrate incubated for 2 hrs by fluorescence based analysisic500.3190uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
sodium arsenitedecreases expression, increases expression3
Benzo(a)pyrenedecreases expression, increases expression2
Tretinoindecreases expression2
Cyclosporineincreases expression2
Particulate Matterdecreases expression, increases abundance, affects expression, increases reaction2
aristolochic acid Idecreases expression1
FR900359decreases phosphorylation1
TAK-243increases sumoylation1
dicrotophosdecreases expression1
testosterone enanthateaffects expression1
triphenyl phosphateaffects expression1
bisphenol Adecreases expression1
kojic aciddecreases expression1
2,3-bis(3’-hydroxybenzyl)butyrolactoneaffects cotreatment, increases expression1
coumarinincreases phosphorylation1
beta-methylcholineaffects expression1
di-n-butylphosphoric acidaffects expression1
CGP 52608affects binding, increases reaction1
2-palmitoylglycerolincreases expression1
CPG-oligonucleotideincreases expression1
K 7174increases expression1
oxidized-L-alpha-1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphorylcholineaffects expression, increases reaction1
jinfukangdecreases expression1
(+)-JQ1 compounddecreases expression1
Resveratrolaffects cotreatment, increases expression1
Air Pollutantsdecreases expression, increases abundance1
Vehicle Emissionsaffects expression, increases reaction1
Caffeinedecreases phosphorylation1
Calcitriolaffects cotreatment, decreases expression1
Carbamazepineaffects expression1

ChEMBL screening assays

76 unique, capped per target: 71 binding, 5 functional

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1794467FunctionalPUBCHEM_BIOASSAY: Inhibitors of USP1/UAF1: Pilot qHTS. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504878]PubChem BioAssay data set
CHEMBL3412284BindingInhibition of USP1 (unknown origin) assessed as reduction in K63-linked diUb cleavage by gel electrophoresis based orthogonal diUb cleavage assayInhibiting the deubiquitinating enzymes (DUBs). — J Med Chem

Cellosaurus cell lines

5 cell lines: 5 cancer cell line

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

CellosaurusNameCategorySex
CVCL_B2KHAbcam HeLa USP1 KOCancer cell lineFemale
CVCL_TW44HAP1 USP1 (-) 1Cancer cell lineMale
CVCL_TW45HAP1 USP1 (-) 2Cancer cell lineMale
CVCL_TW46HAP1 USP1 (-) 3Cancer cell lineMale
CVCL_TW47HAP1 USP1 (-) 4Cancer cell lineMale

Clinical trials (associated diseases)

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

TrialPhaseStatusTitle
NCT00152750PHASE4UNKNOWNStudy of Clonidine on Sleep Architecture in Children With Tourette’s Syndrome (TS) and Comorbid ADHD
NCT00226824PHASE4TERMINATEDSafety Study of Galantamine in Tic Disorders
NCT00241176PHASE4COMPLETEDOpen Label Trial of Aripiprazole in Children and Adolescents With Tourette’s Disorder
NCT00370838PHASE4COMPLETEDComparison of Keppra and Clonidine in the Treatment of Tics
NCT01018056PHASE4COMPLETEDDeveloping New Treatments for Tourette Syndrome: Therapeutic Trials With Modulators of Glutamatergic Neurotransmission
NCT01547000PHASE4COMPLETEDGuanfacine in Children With Tic Disorders
NCT03239210PHASE4COMPLETEDEffects of Ondansetron in Obsessive-compulsive and Tic Disorders
NCT00004376PHASE3COMPLETEDPhase III Randomized, Double-Blind, Placebo-Controlled Study of Guanfacine for Tourette Syndrome and Attention Deficit Hyperactivity Disorder
NCT00206323PHASE3COMPLETEDA Randomized, Placebo-controlled, Tourette Syndrome Study.
NCT00206336PHASE3COMPLETEDAn Open-label Study to Determine the Efficacy and Safety of Topiramate in the Treatment of Tourette Syndrome.
NCT00478842PHASE3COMPLETEDPallidal Stimulation and Gilles de la Tourette Syndrome
NCT00681863PHASE3TERMINATEDOpen-label Extension Study of Pramipexole in the Treatment of Children and Adolescents With Tourette Syndrome
NCT01501695PHASE3COMPLETEDPhase III Study of 5LGr to Treat Tic Disorder
NCT03087201PHASE3COMPLETEDCANNAbinoids in the Treatment of TICS (CANNA-TICS)
NCT03487783PHASE3COMPLETEDAripiprazole Oral Solution in the Treatment of Children and Adolescents With Tourette’s Syndrome
NCT03567291PHASE3TERMINATEDEvaluation of Safety and Tolerability of Long-term TEV-50717 (Deutetrabenazine) for Treatment of Tourette Syndrome in Children and Adolescents
NCT03571256PHASE3COMPLETEDA Study to Test if TEV-50717 is Effective in Relieving Tics Associated With Tourette Syndrome (TS)
NCT06021522PHASE3ACTIVE_NOT_RECRUITINGA Study to Evaluate Long-term Safety of Ecopipam Tablets in Children, Adolescents and Adults With Tourette’s Disorder
NCT00004393PHASE2COMPLETEDPhase II Double Blind Placebo Controlled Trial of Risperidone in Tourette Syndrome
NCT00004652PHASE2COMPLETEDPhase II Pilot Controlled Study of Short Vs Longer Term Pimozide (Orap) Therapy in Tourette Syndrome
NCT00231985PHASE2COMPLETEDEffectiveness of Behavior Therapy and Psychosocial Therapy for the Treatment of Tourette Syndrome and Chronic Tic Disorder
NCT00311909PHASE2COMPLETEDThalamic Deep Brain Stimulation for Tourette Syndrome
NCT00529308PHASE2COMPLETEDTranscranial Magnetic Stimulation (TMS) for Individuals With Tourette’s Syndrome
NCT00558467PHASE2COMPLETEDPramipexole Pilot Phase II Study in Children and Adolescents With Tourette Disorder According to DSM-IV Criteria
NCT01043549PHASE2TERMINATEDRepetitive Transcranial Magnetic Stimulation of the Posterior Parietal Cortex in Patients Suffering From Gilles de la Tourette Syndrome
NCT01133353PHASE2WITHDRAWNA Study of the Effectiveness and Safety of Tetrabenazine MR in Pediatric Subjects With Tourette’s Syndrome
NCT01475383PHASE2WITHDRAWNStudy Evaluating The Safety And Efficacy Of PF-03654746 In Adult Subjects With Tourette’s Syndrome
NCT01647269PHASE2COMPLETEDA Trial of Bilateral Deep Brain Stimulation to the Globus Pallidus Internum in Tourette Syndrome
NCT01904773PHASE2COMPLETEDSafety, Tolerability, Pharmacokinetic, and Efficacy Study of AZD5213 in Adolescents With Tourette’s Disorder
NCT02102698PHASE2COMPLETEDEcopipam Treatment of Tourette’s Syndrome in Subjects 7-17 Years
NCT02217007PHASE2WITHDRAWNA Trial Evaluating the Efficacy, Safety, and Pharmacokinetics of SNC-102 in Subjects With Tourette Syndrome
NCT02247206PHASE2COMPLETEDVoIP Delivered Behavior Therapy for Tourette Syndrome
NCT02581865PHASE2COMPLETEDSafety and Efficacy Study of NBI-98854 in Adults With Tourette Syndrome
NCT02619084PHASE2COMPLETEDSubthalamic Stimulation in Tourette’s Syndrome
NCT02679079PHASE2COMPLETEDSafety and Efficacy Study of NBI-98854 in Children and Adolescents With Tourette Syndrome
NCT02879578PHASE2COMPLETEDSafety and Tolerability Study of NBI-98854 for the Treatment of Subjects With Tourette Syndrome
NCT03066193PHASE2COMPLETEDEfficacy of a Therapeutic Combination of Dronabinol and PEA for Tourette Syndrome
NCT03247244PHASE2TERMINATEDSafety and Efficacy of Cannabis in Tourette Syndrome
NCT03325010PHASE2COMPLETEDSafety, Tolerability, and Efficacy of NBI-98854 for the Treatment of Pediatric Subjects With Tourette Syndrome
NCT03444038PHASE2COMPLETEDOpen-Label Safety and Tolerability Study of NBI-98854 for the Treatment of Pediatric Subjects With Tourette Syndrome
  • Associated diseases: Tourette syndrome
  • Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): Tourette syndrome

About this page

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

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This page pulls from 81 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgtopdb_interactiongwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatentpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot