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NAPRT

gene
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Also known as PP3856

Summary

NAPRT (nicotinate phosphoribosyltransferase, HGNC:30450) is a protein-coding gene on chromosome 8q24.3, encoding Nicotinate phosphoribosyltransferase (Q6XQN6). Catalyzes the first step in the biosynthesis of NAD from nicotinic acid, the ATP-dependent synthesis of beta-nicotinate D-ribonucleotide from nicotinate and 5-phospho-D-ribose 1-phosphate. In precision oncology, NAPRT Promoter Hypermethylation confers sensitivity to GNE-617 in Cancer (CIViC Level D).

Nicotinic acid (NA; niacin) is converted by nicotinic acid phosphoribosyltransferase (NAPRT; EC 2.4.2.11) to NA mononucleotide (NaMN), which is then converted to NA adenine dinucleotide (NaAD), and finally to nicotinamide adenine dinucleotide (NAD), which serves as a coenzyme in cellular redox reactions and is an essential component of a variety of processes in cellular metabolism including response to stress (Hara et al., 2007).

Source: NCBI Gene 93100 — RefSeq curated summary.

At a glance

  • GWAS associations: 3
  • Clinical variants (ClinVar): 150 total
  • Druggable target: yes — 11 molecules with ChEMBL bioactivity
  • Precision-oncology evidence (CIViC): 1 curated variant–drug association
  • MANE Select transcript: NM_145201

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:30450
Approved symbolNAPRT
Namenicotinate phosphoribosyltransferase
Location8q24.3
Locus typegene with protein product
StatusApproved
AliasesPP3856
Ensembl geneENSG00000147813
Ensembl biotypeprotein_coding
OMIM611552
Entrez93100

Gene structure

Transcript identifiers

Ensembl transcripts: 38 — 27 protein_coding, 7 retained_intron, 2 non_stop_decay, 2 nonsense_mediated_decay

ENST00000340490, ENST00000426292, ENST00000435154, ENST00000449291, ENST00000460623, ENST00000462059, ENST00000464332, ENST00000480946, ENST00000488096, ENST00000491904, ENST00000498076, ENST00000525583, ENST00000529179, ENST00000532645, ENST00000896704, ENST00000896705, ENST00000896706, ENST00000896707, ENST00000896708, ENST00000896709, ENST00000896710, ENST00000896711, ENST00000896712, ENST00000896713, ENST00000896714, ENST00000896715, ENST00000896716, ENST00000896717, ENST00000896718, ENST00000933603, ENST00000933604, ENST00000933605, ENST00000955117, ENST00000955118, ENST00000955119, ENST00000955120, ENST00000955121, ENST00000955122

RefSeq mRNA: 4 — MANE Select: NM_145201 NM_001286829, NM_001363145, NM_001363146, NM_145201

CCDS: CCDS6403, CCDS69555

Canonical transcript exons

ENST00000449291 — 13 exons

ExonStartEnd
ENSE00002146374143578093143578330
ENSE00003482025143575622143575702
ENSE00003510338143576646143576842
ENSE00003542919143575423143575525
ENSE00003553156143576432143576572
ENSE00003556511143577657143577739
ENSE00003559413143577062143577177
ENSE00003618724143576078143576162
ENSE00003645013143575191143575345
ENSE00003655258143577816143577943
ENSE00003675092143577269143577399
ENSE00003678711143574986143575093
ENSE00003683696143574785143574900

Expression profiles

Bgee: expression breadth ubiquitous, 134 present calls, max score 98.01.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 16.7570 / max 1026.3619, expressed in 1633 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter IDTPM avgSamples expressed
9549315.66321617
954940.7570392
954950.3149154
954920.01354
954910.00843

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
mucosa of transverse colonUBERON:000499198.01gold quality
right lobe of liverUBERON:000111497.95gold quality
lower esophagus mucosaUBERON:003583497.73gold quality
duodenumUBERON:000211497.62gold quality
esophagus mucosaUBERON:000246996.59gold quality
liverUBERON:000210796.53gold quality
small intestine Peyer’s patchUBERON:000345496.22gold quality
skin of legUBERON:000151196.05gold quality
small intestineUBERON:000210896.04gold quality
transverse colonUBERON:000115795.97gold quality
zone of skinUBERON:000001495.93gold quality
skin of abdomenUBERON:000141695.91gold quality
apex of heartUBERON:000209895.85gold quality
metanephros cortexUBERON:001053395.63gold quality
bloodUBERON:000017895.45gold quality
body of stomachUBERON:000116195.34gold quality
spleenUBERON:000210695.27gold quality
fundus of stomachUBERON:000116095.15gold quality
minor salivary glandUBERON:000183094.96gold quality
saliva-secreting glandUBERON:000104494.94gold quality
monocyteCL:000057694.78gold quality
olfactory segment of nasal mucosaUBERON:000538694.63gold quality
right adrenal gland cortexUBERON:003582794.62gold quality
vaginaUBERON:000099694.53gold quality
right lungUBERON:000216794.49gold quality
leukocyteCL:000073894.45gold quality
ectocervixUBERON:001224994.45gold quality
adult mammalian kidneyUBERON:000008294.35gold quality
mucosa of stomachUBERON:000119994.21gold quality
esophagusUBERON:000104394.11gold quality

Single-cell (SCXA)

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

ExperimentMarker?Max mean expression
E-ANND-3no0.00

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 12)

  • NA elevates cellular NAD levels through NAPRT function and, thus, protects the cells against stress, partly due to lack of feedback inhibition of NAPRT but not NamPRT by NAD (PMID:17604275)
  • NAPRT expression was varied in lymphomas with 30-50% low expression except for Hodgkin’s lymphoma where 85% displayed low expression (PMID:21492230)
  • Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) activity by small molecule GMX1778 regulates reactive oxygen species (ROS)-mediated cytotoxicity in a p53- and nicotinic acid phosphoribosyltransferase1 (NAPRT1)-dependent manner (PMID:22570471)
  • Tumor-specific promoter hypermethylation of NAPRT1 inactivates one of two NAD salvage pathways, resulting in synthetic lethality with the coadministration of a NAMPT inhibitor. (PMID:24097869)
  • High NAPRTase expression is associated with neoplasms. (PMID:26675378)
  • Synthesis and Degradation of Adenosine 5’-Tetraphosphate by Nicotinamide and Nicotinate Phosphoribosyltransferases (PMID:28416276)
  • No correlation between IDH1/2 mutation status and sensitivity for NAMPT inhibitors was observed. Strikingly, higher methylation of the NAPRT promoter was observed in high-grade versus low-grade chondrosarcomas. In conclusion, this study identified NAMPT as a potential target for treatment of chondrosarcoma (PMID:28860121)
  • Association of Schizophrenia Risk With Disordered Niacin Metabolism in an Indian Genome-wide Association Study. (PMID:31268507)
  • Study demonstrated that PPM1D mutant astrocytes and patient-derived PPM1D mutant diffuse intrinsic pontine glioma lines are particularly sensitive to treatment with NAMPT inhibitors. Mutant PPM1D-induced NAMPT inhibitor sensitivity is driven by hypermethylation of CpG islands throughout the genome and the epigenetic silencing of NAPRT, a key gene involved in NAD biosynthesis. (PMID:31439867)
  • these data identify NAPRT as a endogenous ligand for TLR4 and a mediator of inflammation. (PMID:31511522)
  • NAPRT Expression Regulation Mechanisms: Novel Functions Predicted by a Bioinformatics Approach. (PMID:34946971)
  • NAPRT, but Not NAMPT, Provides Additional Support for NAD Synthesis in Esophageal Precancerous Lesions. (PMID:36432602)

Cross-species orthologs

5 orthologs

OrganismSymbolGene ID
danio_rerionaprtENSDARG00000027930
mus_musculusNaprtENSMUSG00000022574
rattus_norvegicusNaprtENSRNOG00000007939
drosophila_melanogasterNaprtFBGN0031589
caenorhabditis_elegansWBGENE00021882

Paralogs (1): NAMPT (ENSG00000105835)

Protein

Protein identifiers

Nicotinate phosphoribosyltransferase — Q6XQN6 (reviewed: Q6XQN6)

Alternative names: FHA-HIT-interacting protein, Nicotinate phosphoribosyltransferase domain-containing protein 1

All UniProt accessions (6): Q6XQN6, A0A087WUT5, C9J8U2, G5E977, H0YDA6, H0YF31

UniProt curated annotations — full annotation on UniProt →

Function. Catalyzes the first step in the biosynthesis of NAD from nicotinic acid, the ATP-dependent synthesis of beta-nicotinate D-ribonucleotide from nicotinate and 5-phospho-D-ribose 1-phosphate. Helps prevent cellular oxidative stress via its role in NAD biosynthesis.

Subunit / interactions. Homodimer.

Subcellular location. Cytoplasm. Cytosol.

Post-translational modifications. Transiently phosphorylated on a His residue during the reaction cycle. Phosphorylation strongly increases the affinity for substrates and increases the rate of nicotinate D-ribonucleotide production. Dephosphorylation regenerates the low-affinity form of the enzyme, leading to product release.

Cofactor. Activity is highest with Mn(2+).

Pathway. Cofactor biosynthesis; NAD(+) biosynthesis; nicotinate D-ribonucleotide from nicotinate: step 1/1.

Similarity. Belongs to the NAPRTase family.

Isoforms (3)

UniProt IDNamesCanonical?
Q6XQN6-11yes
Q6XQN6-22
Q6XQN6-33

RefSeq proteins (4): NP_001273758, NP_001350074, NP_001350075, NP_660202* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR006405Nic_PRibTrfase_pncBFamily
IPR007229Nic_PRibTrfase-FamFamily
IPR013785Aldolase_TIMHomologous_superfamily
IPR036068Nicotinate_pribotase-like_CHomologous_superfamily
IPR040727NAPRTase_NDomain
IPR041619NAPRTase_CDomain

Pfam: PF17767, PF17956

Enzyme classification (BRENDA):

  • EC 6.3.4.21 — nicotinate phosphoribosyltransferase (BRENDA: 15 organisms, 35 substrates, 62 inhibitors, 38 Km, 5 kcat entries)

Substrate kinetics (BRENDA)

6 substrates with measured Km, best-characterized 6. Km ranges are aggregated across organisms/conditions.

SubstrateKm (mM)Measurements
5-PHOSPHO-ALPHA-D-RIBOSE 1-DIPHOSPHATE0.0002–4.513
NICOTINATE0.0005–0.312
ATP0.07–0.45
NICOTINIC ACID0.0127–0.01552
GTP0.341
ITP1.161

Catalyzed reactions (Rhea), 1 shown:

  • 5-phospho-alpha-D-ribose 1-diphosphate + nicotinate + ATP + H2O = nicotinate beta-D-ribonucleotide + ADP + phosphate + diphosphate (RHEA:36163)

UniProt features (68 total): helix 21, strand 20, mutagenesis site 11, binding site 4, sequence conflict 4, turn 2, modified residue 2, splice variant 2, chain 1, sequence variant 1

Structure

Experimental structures (PDB)

1 structures.

PDBMethodResolution (Å)
4YUBX-RAY DIFFRACTION2.9

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q6XQN6-F194.940.92

Functional residue map

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

Ligand- & substrate-binding residues (4): 21; 210; 318; 380

Post-translational modifications (2): 213, 537

Mutagenesis-validated functional residues (11):

PositionPhenotype
19complete loss of activity.
21partial loss of activity in the presence of atp, complete loss in the absence of atp.
169partial loss of activity.
209partial loss of activity.
213partial loss of activity.
288partial loss of activity.
318partial loss of activity in the presence of atp, almost complete loss in the absence of atp.
357small loss of activity.
379complete loss of activity.
380partial loss of activity.
381partial loss of activity.

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

IDPathway
R-HSA-196807Nicotinate metabolism
R-HSA-6798695Neutrophil degranulation

MSigDB gene sets: 95 (showing top): GSE18804_BRAIN_VS_COLON_TUMORAL_MACROPHAGE_DN, GSE45365_CTRL_VS_MCMV_INFECTION_NK_CELL_DN, REACTOME_INNATE_IMMUNE_SYSTEM, GOCC_SECRETORY_GRANULE, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_NUCLEOSIDE_PHOSPHATE_BIOSYNTHETIC_PROCESS, GOBP_ORGANOPHOSPHATE_BIOSYNTHETIC_PROCESS, GOBP_PURINE_CONTAINING_COMPOUND_SALVAGE, GOBP_NADPLUS_METABOLIC_PROCESS, GOBP_NUCLEOBASE_CONTAINING_SMALL_MOLECULE_METABOLIC_PROCESS, SCHAEFFER_PROSTATE_DEVELOPMENT_48HR_DN, GOMF_LIGASE_ACTIVITY_FORMING_CARBON_NITROGEN_BONDS, GOBP_PURINE_CONTAINING_COMPOUND_METABOLIC_PROCESS, GOBP_NUCLEOTIDE_SALVAGE, GOBP_METABOLIC_COMPOUND_SALVAGE

GO Biological Process (4): response to oxidative stress (GO:0006979), NAD+ biosynthetic process via the salvage pathway (GO:0034355), NAD+ biosynthetic process (GO:0009435), pyridine nucleotide biosynthetic process (GO:0019363)

GO Molecular Function (6): nicotinate phosphoribosyltransferase activity (GO:0004516), transferase activity (GO:0016740), metal ion binding (GO:0046872), protein binding (GO:0005515), glycosyltransferase activity (GO:0016757), ligase activity (GO:0016874)

GO Cellular Component (5): extracellular region (GO:0005576), cytosol (GO:0005829), azurophil granule lumen (GO:0035578), extracellular exosome (GO:0070062), cytoplasm (GO:0005737)

Reactome top-level categories

Rollup of top-2 pathways:

CategoryPathways
Metabolism of water-soluble vitamins and cofactors1
Innate Immune System1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure3
catalytic activity2
response to stress1
NAD+ biosynthetic process1
pyridine nucleotide salvage1
purine nucleotide salvage1
purine nucleotide biosynthetic process1
nicotinamide nucleotide biosynthetic process1
NAD+ metabolic process1
nucleotide biosynthetic process1
pyridine-containing compound biosynthetic process1
ligase activity, forming carbon-nitrogen bonds1
cation binding1
binding1
transferase activity1
cytoplasm1
vacuolar lumen1
secretory granule lumen1
azurophil granule1
extracellular vesicle1
intracellular anatomical structure1

Protein interactions and networks

STRING

1106 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
NAPRTNAMPTP43490949
NAPRTQPRTQ15274844
NAPRTNMNAT1Q9HAN9820
NAPRTNMRK1Q9NWW6772
NAPRTA0A2R8YFG2A0A2R8YFG2769
NAPRTNMNAT2Q9BZQ4767
NAPRTNADSYN1Q6IA69709
NAPRTTLR4O00206666
NAPRTNMRK2Q9NPI5646
NAPRTNADKO95544617
NAPRTHAAOP46952610
NAPRTTDO2P48775588
NAPRTKMOO15229581
NAPRTBST1Q10588549
NAPRTACMSDQ8TDX5513

IntAct

15 interactions, top by confidence:

ABTypeScore
IGBP1PPP6Cpsi-mi:“MI:0914”(association)0.940
RBPMSNAPRTpsi-mi:“MI:0915”(physical association)0.560
NAPRTGRAMD2Bpsi-mi:“MI:0915”(physical association)0.560
MAP2K3SUPT5Hpsi-mi:“MI:0914”(association)0.350
OR2A4A2ML1psi-mi:“MI:0914”(association)0.350
PPP2R2BA2ML1psi-mi:“MI:0914”(association)0.350
CDK15A2ML1psi-mi:“MI:0914”(association)0.350
ST7A2ML1psi-mi:“MI:0914”(association)0.350
SMPD2A2ML1psi-mi:“MI:0914”(association)0.350
PIDD1IPO5psi-mi:“MI:0914”(association)0.350

BioGRID (50): NAPRT (Two-hybrid), NAPRT (Two-hybrid), NAPRT (Two-hybrid), KRT40 (Two-hybrid), CCDC57 (Two-hybrid), C6orf211 (Co-fractionation), EEF1A1 (Co-fractionation), NAPRT (Co-fractionation), NAPRT (Co-fractionation), NAPRT (Co-fractionation), NAPRT (Co-fractionation), NAPRT (Co-fractionation), NAPRT (Co-fractionation), NAPRT (Co-fractionation), NAPRT (Co-fractionation)

ESM2 similar proteins: A4FV98, A5D7B1, A5PK51, A6QLN9, A8MUP2, D3ZVU9, O15527, O35595, O75078, O95848, P57775, Q05B60, Q06643, Q14728, Q14CX5, Q1LZB9, Q27HK4, Q2T9T5, Q2TBS1, Q3UGX3, Q4R3I0, Q4V892, Q58CT4, Q5E9H2, Q5RCI5, Q5SUV1, Q5TM22, Q642A6, Q6IA17, Q6PCB0, Q6XQN6, Q862Z7, Q8N8L6, Q8R2R5, Q8R2Z5, Q8R366, Q8WUG5, Q95JH0, Q95JH2, Q969P0

Diamond homologs: A5PK51, O32090, P9WJI6, P9WJI7, P9WJI8, P9WJI9, Q55G10, Q6P3H4, Q6XQN1, Q6XQN6, Q84WV8, Q8CC86, Q8RWM2, Q95XX1, Q9VQX4, Q9HJ28, Q12Z05

SIGNOR signaling

0 interactions.

Disease & clinical

Cancer significance

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance104
Likely benign6
Benign2

Top pathogenic / likely-pathogenic (0)

SpliceAI

2016 predictions. Top by Δscore:

VariantEffectΔscore
8:143575417:CCTCA:Cdonor_loss1.0000
8:143575418:CTCA:Cdonor_loss1.0000
8:143575419:TCAC:Tdonor_loss1.0000
8:143575420:CACCG:Cdonor_loss1.0000
8:143575421:A:ACdonor_gain1.0000
8:143575421:A:ATdonor_loss1.0000
8:143575422:C:CCdonor_gain1.0000
8:143575422:C:CTdonor_loss1.0000
8:143575422:CCGT:Cdonor_gain1.0000
8:143575521:ACCAG:Aacceptor_gain1.0000
8:143575522:CCAG:Cacceptor_gain1.0000
8:143575522:CCAGC:Cacceptor_gain1.0000
8:143575523:CAG:Cacceptor_gain1.0000
8:143575523:CAGC:Cacceptor_gain1.0000
8:143575524:AG:Aacceptor_gain1.0000
8:143575525:GCT:Gacceptor_loss1.0000
8:143575526:C:CCacceptor_gain1.0000
8:143575526:CTG:Cacceptor_loss1.0000
8:143575530:A:Tacceptor_gain1.0000
8:143576079:T:TAdonor_gain1.0000
8:143576428:TCA:Tdonor_loss1.0000
8:143576430:A:ACdonor_gain1.0000
8:143576431:C:CCdonor_gain1.0000
8:143576431:CT:Cdonor_gain1.0000
8:143576431:CTG:Cdonor_gain1.0000
8:143576431:CTGG:Cdonor_gain1.0000
8:143576431:CTGGG:Cdonor_gain1.0000
8:143576568:CACTC:Cacceptor_gain1.0000
8:143576570:CTC:Cacceptor_gain1.0000
8:143576571:TC:Tacceptor_gain1.0000

AlphaMissense

3395 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
8:143577690:T:AE135V0.996
8:143577399:G:CS146R0.994
8:143577399:G:TS146R0.994
8:143577658:T:GS146R0.994
8:143578196:G:CF41L0.994
8:143578196:G:TF41L0.994
8:143578198:A:GF41L0.994
8:143575622:C:AK396N0.993
8:143575622:C:GK396N0.993
8:143575451:C:AK421N0.992
8:143575451:C:GK421N0.992
8:143575627:A:CY395D0.991
8:143577164:G:CS194R0.990
8:143577164:G:TS194R0.990
8:143577166:T:GS194R0.990
8:143577279:G:CS186R0.988
8:143577279:G:TS186R0.988
8:143577281:T:GS186R0.988
8:143577158:G:CN196K0.987
8:143577158:G:TN196K0.987
8:143577161:G:CS195R0.987
8:143577161:G:TS195R0.987
8:143577163:T:GS195R0.987
8:143577689:C:AE135D0.987
8:143577689:C:GE135D0.987
8:143577717:C:TG126E0.986
8:143576120:G:CS355R0.984
8:143576120:G:TS355R0.984
8:143576122:T:GS355R0.984
8:143577292:G:TA182D0.981

dbSNP variants (sampled 300 via entrez): RS1000142130 (8:143572882 G>A,T), RS1000384538 (8:143577451 C>A,T), RS1000423832 (8:143577638 C>A,G), RS1001393860 (8:143578453 T>A,C,G), RS1002724586 (8:143574504 C>T), RS1002946427 (8:143576411 C>A,T), RS1003388135 (8:143576547 C>A,G,T), RS1003477098 (8:143578752 G>A,C), RS1003985841 (8:143577380 C>G,T), RS1004162223 (8:143573175 G>A,T), RS1005360878 (8:143576186 T>C), RS1006299431 (8:143578275 G>A,C,T), RS1006463034 (8:143573952 C>T), RS1006475819 (8:143575587 C>A), RS1006760811 (8:143573719 G>A,C)

Disease associations

OMIM: gene MIM:611552 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

3 associations (top):

StudyTraitp-value
GCST000281_16Attention deficit hyperactivity disorder9.000000e-06
GCST008459_52Schizophrenia4.000000e-08
GCST008459_53Schizophrenia1.000000e-09

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4523354 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

11 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,827,993 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL101PHENYLBUTAZONE459,455
CHEMBL1228OXYPHENBUTAZONE ANHYDROUS424,044
CHEMBL25ASPIRIN4694,602
CHEMBL269644ACETANILIDE423,640
CHEMBL288470AMINOPYRINE48,254
CHEMBL424SALICYLIC ACID4669,423
CHEMBL6INDOMETHACIN4156,366
CHEMBL686MEFENAMIC ACID461,835
CHEMBL832SULFINPYRAZONE413,780
CHEMBL277474ANTIPYRINE381,797
CHEMBL23588FLUFENAMIC ACID234,797

Clinical evidence (CIViC)

Drug × variant × indication: 1 predictive associations from 1 curated evidence items.

VariantTherapyIndicationEffectLevelCIViC
NAPRT Promoter HypermethylationGNE-617CancerSensitivity/ResponseCIViC DEID897

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

ChEMBL bioactivities

24 potent at pChembl≥5 of 24 total, top 24 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
11.00Ki0.01nMFLUFENAMIC ACID
10.30Ki0.05nMMEFENAMIC ACID
10.12Ki0.075nMPYRAZINOIC ACID
10.00Ki0.1nMPHENYLBUTAZONE
9.82Ki0.15nMINDOMETHACIN
9.80Ki0.16nMSALICYLIC ACID
9.64Ki0.23nMCHEMBL53297
9.55Ki0.28nMCHEMBL394308
9.52Ki0.3nMOXYPHENBUTAZONE ANHYDROUS
9.30Ki0.5nMSULFINPYRAZONE
9.30Ki0.5nMASPIRIN
9.30Kd0.495nMCHEMBL5653589
9.30ED500.495nMCHEMBL5653589
9.25Ki0.56nM6-CHLORONICOTINIC ACID
9.12Ki0.75nMCHEMBL4438353
9.12Ki0.75nMISONICOTINIC ACID
9.11Ki0.78nMPYRIDINE
9.09Ki0.82nMCHEMBL3322868
9.00Ki1nMANTIPYRINE
9.00Ki1nMAMINOPYRINE
9.00Ki1nMACETANILIDE
8.94Ki1.16nM2-PICOLINIC ACID
8.89Ki1.28nMCHEMBL1741437
8.72Ki1.9nMBENZOIC ACID

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.

CompoundAssayTypeValueUnit
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide2148823: Binding affinity to human NAPRT incubated for 45 mins by Kinobead based pull down assaykd0.0005uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
Valproic Acidaffects expression, decreases expression, increases methylation3
N-(4-(1-benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamidedecreases activity2
Air Pollutantsincreases abundance, increases expression, decreases expression2
Benzo(a)pyrenedecreases expression, decreases methylation2
Smokedecreases expression, increases abundance, increases expression2
Cyclosporinedecreases expression2
FR900359decreases phosphorylation1
triphenyl phosphateaffects expression1
bisphenol Aincreases expression1
lead acetatedecreases expression1
beta-lapachonedecreases expression1
sodium arsenitedecreases expression1
benzo(e)pyrenedecreases methylation1
puag-haadincreases expression1
ICG 001increases expression1
hexabrominated diphenyl ether 153decreases expression1
3-(2-hydroxy-4-(2-methylnonan-2-yl)phenyl)cyclohexan-1-olincreases expression1
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acidincreases expression1
Sunitinibdecreases expression1
Dinitrochlorobenzeneaffects binding1
Doxorubicindecreases expression1
Estradiolaffects cotreatment, decreases expression1
Ivermectindecreases expression1
Methapyrilenedecreases methylation1
Pesticidesaffects methylation1
Thimerosaldecreases expression1
Thiramdecreases expression1
Aflatoxin B1affects expression1
Acrylamidedecreases expression1
Particulate Matterdecreases expression, increases abundance1

ChEMBL screening assays

16 unique, capped per target: 16 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL4418184BindingInhibition of NAPRT (unknown origin)Sensitization of cancer cells to nampt inhibitors by nicotinic acid phosphoribosyltransferase neutralization

Cellosaurus cell lines

3 cell lines: 3 cancer cell line

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

CellosaurusNameCategorySex
CVCL_D1NXAbcam K-562 NAPRT KOCancer cell lineFemale
CVCL_D2KHAbcam Raji NAPRT KOCancer cell lineMale
CVCL_UQ99Abcam Jurkat NAPRT KOCancer cell lineMale

Clinical trials (associated diseases)

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

  • Associated diseases: cancer
  • Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): cancer

About this page

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

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 79

This page pulls from 79 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot