NCF1

Summary

NCF1 (neutrophil cytosolic factor 1, HGNC:7660) is a protein-coding gene on chromosome 7q11.23, encoding Neutrophil cytosol factor 1 (P14598). Subunit of the phagocyte NADPH oxidase complex that mediates the transfer of electrons from cytosolic NADPH to O2 to produce the superoxide anion (O2(-)).

The protein encoded by this gene is a 47 kDa cytosolic subunit of neutrophil NADPH oxidase. This oxidase is a multicomponent enzyme that is activated to produce superoxide anion. Mutations in this gene have been associated with chronic granulomatous disease.

Source: NCBI Gene 653361 — RefSeq curated summary.

At a glance

• Gene–disease (curated): granulomatous disease, chronic, autosomal recessive, cytochrome b-positive, type 1 (Strong, GenCC) — +1 more curated relationship
• GWAS associations: 2
• Clinical variants (ClinVar): 13 total — 9 pathogenic, 1 likely-pathogenic
• Phenotypes (HPO): 226
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Dosage sensitivity (ClinGen): haploinsufficiency autosomal recessive, triplosensitivity no evidence
• MANE Select transcript: NM_000265

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:7660
Approved symbol	NCF1
Name	neutrophil cytosolic factor 1
Location	7q11.23
Locus type	gene with protein product
Status	Approved
Aliases	p47phox, NOXO2, NCF1A, SH3PXD1A
Ensembl gene	ENSG00000158517
Ensembl biotype	protein_coding
OMIM	608512
Entrez	653361

Gene structure

Transcript identifiers

Ensembl transcripts: 15 — 7 protein_coding, 5 retained_intron, 2 protein_coding_CDS_not_defined, 1 nonsense_mediated_decay

ENST00000289473, ENST00000398421, ENST00000433458, ENST00000438106, ENST00000442021, ENST00000443956, ENST00000449343, ENST00000455062, ENST00000464878, ENST00000486097, ENST00000488197, ENST00000969820, ENST00000969821, ENST00000969822, ENST00000969823

RefSeq mRNA: 1 — MANE Select: NM_000265 NM_000265

CCDS: CCDS34657

Canonical transcript exons

ENST00000289473 — 11 exons

Exon	Start	End
ENSE00001128348	74774011	74774103
ENSE00001666032	74789039	74789315
ENSE00003481780	74779082	74779157
ENSE00003501248	74782939	74783061
ENSE00003510291	74785182	74785299
ENSE00003522469	74780780	74780835
ENSE00003588641	74777267	74777347
ENSE00003616013	74788559	74788704
ENSE00003624448	74787984	74788088
ENSE00003693249	74783525	74783632
ENSE00003693356	74779257	74779422

Expression profiles

Bgee: expression breadth ubiquitous, 136 present calls, max score 99.29.

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
granulocyte	CL:0000094	99.29	gold quality
blood	UBERON:0000178	99.28	gold quality
monocyte	CL:0000576	99.16	gold quality
leukocyte	CL:0000738	99.13	gold quality
bone marrow cell	CL:0002092	98.67	gold quality
bone marrow	UBERON:0002371	98.46	gold quality
bone element	UBERON:0001474	98.45	gold quality
spleen	UBERON:0002106	97.79	gold quality
vermiform appendix	UBERON:0001154	96.86	gold quality
lymph node	UBERON:0000029	96.48	gold quality
small intestine Peyer’s patch	UBERON:0003454	85.83	gold quality
small intestine	UBERON:0002108	84.90	gold quality
upper lobe of left lung	UBERON:0008952	84.85	gold quality
right lung	UBERON:0002167	84.23	gold quality
mucosa of transverse colon	UBERON:0004991	83.56	gold quality
placenta	UBERON:0001987	82.98	gold quality
gall bladder	UBERON:0002110	82.34	gold quality
duodenum	UBERON:0002114	82.06	gold quality
tonsil	UBERON:0002372	81.23	gold quality
colonic epithelium	UBERON:0000397	80.91	gold quality
lung	UBERON:0002048	80.70	gold quality
omental fat pad	UBERON:0010414	79.26	gold quality
right coronary artery	UBERON:0001625	78.68	gold quality
hindlimb stylopod muscle	UBERON:0004252	78.14	gold quality
rectum	UBERON:0001052	77.94	gold quality
transverse colon	UBERON:0001157	77.80	gold quality
intestine	UBERON:0000160	77.40	gold quality
smooth muscle tissue	UBERON:0001135	76.92	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	76.73	gold quality
adipose tissue	UBERON:0001013	75.90	gold quality

Single-cell (SCXA)

Detected in 11 experiment(s), a significant marker in 8.

Experiment	Marker?	Max mean expression
E-MTAB-9801	yes	2355.80
E-HCAD-4	yes	102.17
E-CURD-122	yes	60.24
E-CURD-98	yes	53.12
E-MTAB-6678	yes	25.19
E-ANND-3	yes	22.67
E-MTAB-9067	yes	15.02
E-MTAB-8498	yes	11.64
E-MTAB-6379	no	301.11
E-MTAB-7303	no	29.98
E-MTAB-5061	no	3.72

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AHR, HBP1, HR, SPI1

miRNA regulators (miRDB)

7 targeting NCF1, 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-LET-7F-2-3P	99.98	70.98	2588
HSA-MIR-1185-1-3P	99.98	71.04	2593
HSA-MIR-1185-2-3P	99.98	71.04	2593
HSA-MIR-4729	99.69	72.18	4233
HSA-MIR-7151-3P	99.04	69.72	2370
HSA-MIR-3196	98.96	63.91	326
HSA-MIR-6732-3P	98.17	67.52	802

Functional genomics

ClinGen dosage: haploinsufficiency 30 (autosomal recessive), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map

Literature-anchored findings (GeneRIF, showing 40)

• the C-terminal alpha-helical region of the p22phox peptide increases the binding affinity for the tandem SH3 domains of p47phox more than 10-fold (PMID:16326715)
• Data show that GM-CSF and TNF-alpha induce phosphorylation of Ser345 on p47phox, a cytosolic component of NADPH oxidase, in human neutrophils. (PMID:16778989)
• The phox homology (PX) domain of p47phox localizes to the plasma membrane in human neutrophils, but is not translocated to the membrane of mature phagosomes. (PMID:17150107)
• Thr133, Ser288 and Thr356, targets for IRAK-4 phosphorylation in vitro, are also phosphorylated in endogenous p47phox after LPS stimulation and regulates NADPH oxidase activation. (PMID:17217339)
• These results indicate that a functional NADPH oxidase and the generation of oxidants in the neutrophil phagosome prevent the activation of the cytoplasmic caspase cascade. (PMID:17438039)
• Increased expression of NAD(P)H oxidase-p47phox and nuclear factor-kappaB p65 may contribute to endothelial oxidative stress with aging in humans. (PMID:17478731)
• Homocysteine increased intracellular reactive oxygen species by NAD(P)H oxidase activation, as shown by the membrane translocation of its p47(phox) subunit. (PMID:17586618)
• There is an increased expression of NADPH oxidase p47(-PHOX) and p67(-PHOX) factor in idiopathic pulmonary fibrosis patients. (PMID:17651608)
• the cytosolic regulatory subunit p47phox modulates the conformation of Cyt b (in addition to serving as an adapter protein) during oxidase activation. (PMID:18004884)
• these results indicate that activation of the ASK1/p38 MAPK/p47phox cascade plays a central role in PPD/TLR2-induced ROS generation and suggests the existence of a ‘ROS/ASK1’ inflammatory amplification feedback loop in monocytes/macrophages. (PMID:18028450)
• CD95L-induced endosomal acidification, ceramide formation, and downstream events, such as p47(phox) phosphorylation, ROS formation, CD95 activation, and apoptosis. (PMID:18045865)
• Phosphatidylinositol 3-kinase-dependent membrane recruitment of Rac-1 and p47phox is critical for alpha-platelet-derived growth factor receptor-induced production of reactive oxygen species. (PMID:18070887)
• nox1, nox2, and p47 have distinct roles in NADPH oxidase activity in human veins. (PMID:18287880)
• The kinetics of p47phox activation was investigated by comparing neutrophils from diabetic and healthy subjects, and the mechanism of hyperglycemia-induced changes was studied by using neutrophil-like HL-60 cells as a model. (PMID:18390927)
• As(2)O(3) induced phosphorylation and membrane translocation of the NADPH oxidase subunit p47(phox) and it also increased translocation of Rac1 and p67(phox). (PMID:18424721)
• NF-kappaB is necessary for CYBB and NCF1 gene expression and activation of the phagocyte NADPH oxidase normal and anhidrotic ectodermal dysplasia leukocytes. (PMID:18523147)
• mutations in CYBB, NCF1, CYBA or NCF2 may play a role in chronic granulomatous disease (PMID:18546332)
• Ile67 of the cPLA2-C2 domain is identified as a critical, centrally positioned residue in a hydrophobic interaction in the p47phox-PX domain (PMID:18765662)
• The direct interaction of PI3Kgamma with PKCalpha forms a discrete regulatory module of N-formylmethionyl-leucyl-phenylalanine-dependent reactive oxygen species production in neutrophils. (PMID:18983267)
• NCF1DeltaGT/GTGT ratios were correlated with clinical parameters and ROI (reactive oxygen intermediates) production during Plasmodium falciparum malaria and with susceptibility to the autoimmune disease multiple sclerosis (MS) (PMID:19077231)
• Nef regulates the NADPH oxidase p47(phox)activity through the activation of the Src kinases and PI3K (PMID:19130504)
• Conformational changes in p47(phox) upon activation highlighted by mass spectrometry coupled to hydrogen/deuterium exchange and limited proteolysis are reported. (PMID:19192478)
• Mutation in NCF1 in Chronic granulomatous disease patient is associated with liver abscess. (PMID:19329991)
• These results demonstrate a role of PLD in hyperoxia-mediated IQGAP1 activation through Rac1 in tyrosine phosphorylation of Src and cortactin, as well as in p47(phox) translocation and reactive oxygen species formation in human lung endothelial cells. (PMID:19366706)
• NADPH oxidase and lipid raft-associated redox signaling are required for PCB153-induced upregulation of cell adhesion molecules in human brain endothelial cells. (PMID:19632255)
• Conclude that acute exercise increases intracellular NO in endothelial progenitor cells through an NADPH oxidase-inhibition mechanism in sedentary men. (PMID:19717732)
• These results suggest that hyperoxia induces caveolin-1-dependent, c-Abl-mediated dynamin 2 phosphorylation required for recruitment of p47(phox) to caveolin-enriched microdomains and subsequent ROS production in lung endothelium. (PMID:19833721)
• Expression of the p47phox subunit and NOX activity was evaluated in affected (superior and middle temporal gyri) and unaffected (cerebellum) brain regions from a longitudinally followed group of patients with varying degrees of cognitive impairment. (PMID:19929442)
• All mutations and some polymorphisms identified in the NCF1 gene in the autosomal forms of chronic granulomatous disease are listed. Review. (PMID:20167518)
• granulomatous disease in Iran is predominantly due to mutations in p47-phox, while the number of mutations in p22-phox is roughly equal to that in gp91-phox, indicating that the genetics of CGD are ethnically variable (PMID:20407811)
• Loss of p47phox is associated with inflammasome activation resulting in chronic granulomatous disease. (PMID:20495074)
• p47phox molecular activation for assembly of the neutrophil NADPH oxidase complex. (PMID:20592030)
• a differential and agonist-dependent role of the p47(phox) PX domain for neutrophil NADPH oxidase activation. (PMID:20817944)
• Direct contact of solid tumor cells and ECs activates endothelial NAD(P)H oxidase-mediated superoxide production. The oxidative stress contributes to EC apoptosis which in turn facilitates tumor cell extravasation. (PMID:21506107)
• Results demonstrate that PBEF can prime for PMN respiratory burst activity by promoting p40 and p47 translocation to the membrane. (PMID:21518975)
• There is no correlation between C923T(Ala308Val)polymorphism and cerebral hemorrhage in Han people in Hunan province. (PMID:21566280)
• an increased copy number of NCF1 can be protective against developing RA and add support to previous findings of a role of NCF1 and the phagocyte NADPH oxidase complex in RA pathogenesis. (PMID:21728841)
• autosomal recessive mutational defects are the predominant subtype in Iranian patients with chronic granulomatous disease (PMID:21789723)
• tein disulfide isomerase redox-dependent association with p47(phox): evidence for an organizer role in leukocyte NADPH oxidase activation. (PMID:21791598)
• Resveratrol decreases hyperglycemic induced superoxide production via up-regulation of SIRT1, induction of FOXO3a and inhibition of p47phox in monocytes. (PMID:21813271)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	ncf1	ENSDARG00000033735
mus_musculus	Ncf1	ENSMUSG00000015950
rattus_norvegicus	Ncf1	ENSRNOG00000001480

Paralogs (3): SH3PXD2A (ENSG00000107957), SH3PXD2B (ENSG00000174705), NOXO1 (ENSG00000196408)

Protein

Protein identifiers

Neutrophil cytosol factor 1 — P14598 (reviewed: P14598)

Alternative names: 47 kDa autosomal chronic granulomatous disease protein, 47 kDa neutrophil oxidase factor, NCF-47K, Neutrophil NADPH oxidase factor 1, Nox organizer 2, Nox-organizing protein 2, SH3 and PX domain-containing protein 1A, p47-phox

All UniProt accessions (4): A0A087X1W0, C9J155, P14598, H7C1S1

UniProt curated annotations — full annotation on UniProt →

Function. Subunit of the phagocyte NADPH oxidase complex that mediates the transfer of electrons from cytosolic NADPH to O2 to produce the superoxide anion (O2(-)). In the activated complex, electrons are first transferred from NADPH to flavin adenine dinucleotide (FAD) and subsequently transferred via two heme molecules to molecular oxygen, producing superoxide through an outer-sphere reaction. Activation of the NADPH oxidase complex is initiated by the assembly of cytosolic subunits of the NADPH oxidase complex with the core NADPH oxidase complex to form a complex at the plasma membrane or phagosomal membrane. This activation process is initiated by phosphorylation dependent binding of the cytosolic NCF1/p47-phox subunit to the C-terminus of CYBA/p22-phox.

Subunit / interactions. Component of the phagocyte NADPH oxidase complex composed of an obligatory core heterodimer formed by the membrane proteins CYBA and CYBB and the cytosolic regulatory subunits NCF1/p47-phox, NCF2/p67-phox, NCF4/p40-phox and the small GTPase RAC1 or RAC2. Part of a cytosolic complex composed at least by NCF1, NCF2 and NCF4. Interacts (via C-terminus) with NCF2 (via the C-terminal SH3 domain). Interacts with NCF4. Interacts with CYBB. Interacts (via the second SH3 domain) with CYBA; interaction is phosphorylation-dependent. Interacts with NOXA1. Interacts with ADAM15. Interacts with TRAF4. Interacts with FASLG. Interacts with PARK7 (via C-terminus); the interaction is enhanced by LPS and modulates NCF1 phosphorylation and membrane translocation.

Subcellular location. Cytoplasm. Cytosol. Membrane.

Tissue specificity. Detected in peripheral blood monocytes and neutrophils (at protein level).

Post-translational modifications. Phosphorylated by PRKCD; phosphorylation induces activation of NCF1, leading to assembly and activation of the NADPH oxidase complex.

Disease relevance. Granulomatous disease, chronic, autosomal recessive, 1 (CGD1) [MIM:233700] A form of chronic granulomatous disease, a primary immunodeficiency characterized by severe recurrent bacterial and fungal infections, along with manifestations of chronic granulomatous inflammation. It results from an impaired ability of phagocytes to mount a burst of reactive oxygen species in response to pathogens. The disease is caused by variants affecting the gene represented in this entry.

Domain organisation. The PX domain mediates interaction with phosphatidylinositol 3,4-bisphosphate and other anionic phospholipids. In the autoinhibited, unphosphorylated state an intramolecular interaction with the C-terminal SH3 domain precludes phospholipid binding and interaction with CYBA. Phosphorylation disrupts the autoinhibited state.

Miscellaneous. Due to intron retention.

Isoforms (2)

UniProt ID	Names	Canonical?
P14598-1	1	yes
P14598-2	2

RefSeq proteins (1): NP_000256* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001452	SH3_domain	Domain
IPR001655	P47PHOX	Family
IPR001683	PX_dom	Domain
IPR015039	NCF1_C	Domain
IPR032136	NCF1_PBR/AIR	Domain
IPR034909	PX_p47phox	Domain
IPR035756	NCF1_SH3_1	Domain
IPR035757	NCF1_SH3_2	Domain
IPR036028	SH3-like_dom_sf	Homologous_superfamily
IPR036871	PX_dom_sf	Homologous_superfamily
IPR051228	NADPH_Oxidase/PX-Domain	Family

Pfam: PF00018, PF00787, PF08944, PF16621

UniProt features (64 total): strand 18, helix 14, sequence variant 8, mutagenesis site 8, modified residue 6, domain 3, splice variant 2, chain 1, sequence conflict 1, turn 1, region of interest 1, compositionally biased region 1

Structure

Experimental structures (PDB)

11 structures.

PDB	Method	Resolution (Å)
1KQ6	X-RAY DIFFRACTION	1.18
1W70	X-RAY DIFFRACTION	1.46
1NG2	X-RAY DIFFRACTION	1.7
1OV3	X-RAY DIFFRACTION	1.8
1UEC	X-RAY DIFFRACTION	1.82
1O7K	X-RAY DIFFRACTION	2
7YXW	X-RAY DIFFRACTION	2.5
8WEJ	ELECTRON MICROSCOPY	2.79
1GD5	SOLUTION NMR
1K4U	SOLUTION NMR
1WLP	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P14598-F1	83.16	0.52

Antibody-complex structures (SAbDab): 1 — 8WEJ

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 (6): 345, 348, 303, 304, 320, 328

Mutagenesis-validated functional residues (8):

Position	Phenotype
43	reduces affinity for membranes enriched in phosphatidylinositol 3,4-bisphosphate.
90	reduces affinity for membranes enriched in phosphatidylinositol 3,4-bisphosphate.
263	abolishes autoinhibition and promotes phospholipid binding.
303	abolishes autoinhibition and promotes phospholipid binding; when associated with e-304; e-328; e-359 and e-370.
304	abolishes autoinhibition and promotes phospholipid binding; when associated with e-303; e-328; e-359 and e-370.
328	abolishes autoinhibition and promotes phospholipid binding; when associated with e-303; e-304; e-359 and e-370.
359	abolishes autoinhibition and promotes phospholipid binding; when associated with e-303; e-304; e-328 and e-370.
370	abolishes autoinhibition and promotes phospholipid binding; when associated with e-303; e-304; e-328 and e-359.

Function

Pathways and Gene Ontology

Reactome pathways

23 pathways

ID	Pathway
R-HSA-1222556	ROS and RNS production in phagocytes
R-HSA-1236973	Cross-presentation of particulate exogenous antigens (phagosomes)
R-HSA-3299685	Detoxification of Reactive Oxygen Species
R-HSA-4420097	VEGFA-VEGFR2 Pathway
R-HSA-5668599	RHO GTPases Activate NADPH Oxidases
R-HSA-9013149	RAC1 GTPase cycle
R-HSA-9013404	RAC2 GTPase cycle
R-HSA-9013423	RAC3 GTPase cycle
R-HSA-1236975	Antigen processing-Cross presentation
R-HSA-1280218	Adaptive Immune System
R-HSA-162582	Signal Transduction
R-HSA-168249	Innate Immune System
R-HSA-168256	Immune System
R-HSA-194138	Signaling by VEGF
R-HSA-194315	Signaling by Rho GTPases
R-HSA-195258	RHO GTPase Effectors
R-HSA-2262752	Cellular responses to stress
R-HSA-8953897	Cellular responses to stimuli
R-HSA-9006934	Signaling by Receptor Tyrosine Kinases
R-HSA-9012999	RHO GTPase cycle
R-HSA-9711123	Cellular response to chemical stress
R-HSA-9716542	Signaling by Rho GTPases, Miro GTPases and RHOBTB3
R-HSA-983169	Class I MHC mediated antigen processing & presentation

MSigDB gene sets: 809 (showing top): GOBP_REGULATION_OF_RESPIRATORY_BURST, BIOCARTA_FMLP_PATHWAY, REACTOME_INNATE_IMMUNE_SYSTEM, REACTOME_ADAPTIVE_IMMUNE_SYSTEM, GOBP_INFLAMMATORY_RESPONSE, GOBP_CELLULAR_RESPONSE_TO_LIPID, REACTOME_CLASS_I_MHC_MEDIATED_ANTIGEN_PROCESSING_PRESENTATION, GOBP_CELLULAR_RESPONSE_TO_CARBOHYDRATE_STIMULUS, GOBP_PROTEIN_TARGETING, GOBP_LEUKOCYTE_MEDIATED_CYTOTOXICITY, GOBP_SUPEROXIDE_METABOLIC_PROCESS, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOBP_LEUKOCYTE_MEDIATED_IMMUNITY, BOYLAN_MULTIPLE_MYELOMA_D_DN, PARK_TRETINOIN_RESPONSE_AND_RARA_PLZF_FUSION

GO Biological Process (24): response to yeast (GO:0001878), respiratory burst involved in defense response (GO:0002679), protein targeting to membrane (GO:0006612), leukotriene metabolic process (GO:0006691), superoxide metabolic process (GO:0006801), inflammatory response (GO:0006954), cellular defense response (GO:0006968), superoxide anion generation (GO:0042554), innate immune response (GO:0045087), respiratory burst (GO:0045730), hydrogen peroxide biosynthetic process (GO:0050665), epithelial cell proliferation (GO:0050673), regulation of respiratory burst involved in inflammatory response (GO:0060264), neutrophil-mediated killing of gram-positive bacterium (GO:0070946), neutrophil-mediated killing of fungus (GO:0070947), cellular response to glucose stimulus (GO:0071333), cellular response to testosterone stimulus (GO:0071394), leukocyte mediated cytotoxicity (GO:0001909), response to bacterium (GO:0009617), defense response to bacterium (GO:0042742), defense response to Gram-positive bacterium (GO:0050830), defense response to fungus (GO:0050832), reactive oxygen species metabolic process (GO:0072593), reactive oxygen species biosynthetic process (GO:1903409)

GO Molecular Function (8): electron transfer activity (GO:0009055), superoxide-generating NAD(P)H oxidase activity (GO:0016175), superoxide-generating NADPH oxidase activator activity (GO:0016176), SH3 domain binding (GO:0017124), phosphatidylinositol binding (GO:0035091), phosphatidylinositol-3,4-bisphosphate binding (GO:0043325), protein binding (GO:0005515), lipid binding (GO:0008289)

GO Cellular Component (9): cytoplasm (GO:0005737), cytosol (GO:0005829), plasma membrane (GO:0005886), cytoplasmic side of plasma membrane (GO:0009898), membrane (GO:0016020), dendrite (GO:0030425), phagolysosome (GO:0032010), NADPH oxidase complex (GO:0043020), neuronal cell body (GO:0043025)

Reactome top-level categories

Rollup of top-13 pathways:

Category	Pathways
RHO GTPase cycle	3
Immune System	2
Signaling by Rho GTPases	2
Innate Immune System	1
Antigen processing-Cross presentation	1
Cellular response to chemical stress	1
Signaling by VEGF	1
RHO GTPase Effectors	1
Class I MHC mediated antigen processing & presentation	1
Signaling by Receptor Tyrosine Kinases	1
Signaling by Rho GTPases, Miro GTPases and RHOBTB3	1
Cellular responses to stimuli	1
Signal Transduction	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
defense response	4
cellular anatomical structure	3
binding	2
response to fungus	1
immune effector process	1
respiratory burst	1
protein targeting	1
establishment of protein localization to membrane	1
icosanoid metabolic process	1
reactive oxygen species metabolic process	1
superoxide metabolic process	1
immune response	1
defense response to symbiont	1
metabolic process	1
hydrogen peroxide metabolic process	1
reactive oxygen species biosynthetic process	1
cell population proliferation	1
respiratory burst involved in inflammatory response	1
regulation of immune effector process	1
regulation of innate immune response	1
regulation of inflammatory response	1
regulation of multicellular organismal process	1
regulation of respiratory burst	1
defense response to Gram-positive bacterium	1
neutrophil-mediated killing of bacterium	1
defense response to fungus	1
neutrophil-mediated killing of symbiont cell	1
intracellular glucose homeostasis	1
response to glucose	1
cellular response to hexose stimulus	1
response to testosterone	1
cellular response to lipid	1
cellular response to ketone	1
cell killing	1
leukocyte mediated immunity	1
response to other organism	1
response to bacterium	1
molecular_function	1
oxidoreductase activity, acting on NAD(P)H, oxygen as acceptor	1
enzyme activator activity	1

Protein interactions and networks

STRING

3068 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
NCF1	CYBA	P13498	999
NCF1	CYBB	P04839	999
NCF1	NCF2	P19878	999
NCF1	NOXA1	Q86UR1	999
NCF1	NOX1	Q9Y5S8	999
NCF1	RAC2	P15153	997
NCF1	NOX4	Q9NPH5	997
NCF1	AKT1	P31749	993
NCF1	NCF4	Q15080	990
NCF1	NOXO1	Q8NFA2	988
NCF1	DUOX1	Q9NRD9	968
NCF1	NOX3	Q9HBY0	956
NCF1	MT-CYB	P00156	950
NCF1	NOX5	Q96PH1	946
NCF1	RAC1	P15154	939

IntAct

213 interactions, top by confidence:

A	B	Type	Score
NCF1	NCF2	psi-mi:“MI:0915”(physical association)	0.930
NCF2	NCF1	psi-mi:“MI:0407”(direct interaction)	0.930
NCF1	NCF2	psi-mi:“MI:0407”(direct interaction)	0.930
NCF2	NCF1	psi-mi:“MI:0915”(physical association)	0.930
NCF1	CYBA	psi-mi:“MI:0407”(direct interaction)	0.740
NCF1	TRAF4	psi-mi:“MI:0915”(physical association)	0.680
RELA	NCF1	psi-mi:“MI:0915”(physical association)	0.680
ABI1	NCF1	psi-mi:“MI:0915”(physical association)	0.580
NCF1	ABI1	psi-mi:“MI:0915”(physical association)	0.580
NCF2	GNAI2	psi-mi:“MI:0914”(association)	0.580
PRKCZ	NCF1	psi-mi:“MI:0915”(physical association)	0.560
NCF1	PRKCZ	psi-mi:“MI:0403”(colocalization)	0.560
ADAM8	NCF1	psi-mi:“MI:0407”(direct interaction)	0.560
	NCF1	psi-mi:“MI:0915”(physical association)	0.560
NCF1	CHAT	psi-mi:“MI:0915”(physical association)	0.560

BioGRID (122): NCF1 (Reconstituted Complex), NCF1 (Affinity Capture-Western), PLA2G4A (Reconstituted Complex), PLA2G4A (FRET), NCF1 (Affinity Capture-Western), TRIM9 (Two-hybrid), SH3GL3 (Affinity Capture-MS), NFE2L2 (Affinity Capture-Western), RELA (Reconstituted Complex), RELA (Affinity Capture-Western), NCF1 (Reconstituted Complex), NCF1 (Far Western), ARCN1 (Affinity Capture-MS), COPA (Affinity Capture-MS), COPB1 (Affinity Capture-MS)

ESM2 similar proteins: A1ZAY1, A2RT67, A6NI72, A7MBL8, A8MVU1, F1LXF1, F1M707, O08874, O15034, O75563, O77774, O88382, P11274, P14598, P15056, P15498, P27870, P28028, P54100, Q04982, Q08DN7, Q09014, Q16513, Q32LP7, Q3UND0, Q3ZBA3, Q5BKC9, Q5RDS2, Q5RDX5, Q5RED8, Q5VUG0, Q66H62, Q69ZK0, Q6PAJ1, Q70Z35, Q80TQ2, Q80U40, Q86UL8, Q8BWW9, Q8CHT1

Diamond homologs: A1X283, A1ZAY1, A2AAY5, A4RE77, A6NI72, A6SED8, A7EK16, A8MVU1, A8N2Y6, A8PWF6, B0CRJ3, F1M707, O00443, O43586, O77774, O89032, P0CP00, P0CP01, P10569, P14598, P29366, P62484, P97814, Q09014, Q1LYG0, Q2HDI2, Q2KJB5, Q54FG5, Q5I0D6, Q5RAY1, Q5TCX8, Q5TCZ1, Q61194, Q6WKZ7, Q7Z8J6, Q8IVI9, Q8VDG6, Q9NYB9, Q9QX73, Q9Y7Z8

SIGNOR signaling

52 interactions.

A	Effect	B	Mechanism
MAPK1	up-regulates	NCF1	phosphorylation
MAPK3	up-regulates	NCF1	phosphorylation
IRAK4	up-regulates	NCF1	phosphorylation
AKT1	up-regulates	NCF1	phosphorylation
HBP1	“down-regulates quantity by repression”	NCF1	“transcriptional regulation”
Gbeta	up-regulates	NCF1	phosphorylation
ERK1/2	up-regulates	NCF1	phosphorylation
NCF1	“up-regulates activity”	NOX3	binding
NCF1	“up-regulates activity”	CYBA	binding
NCF1	“form complex”	“Phagocyte NADPH oxidase complex”	binding
AKT	up-regulates	NCF1	phosphorylation
PRKCA	up-regulates	NCF1	phosphorylation
PRKCB	up-regulates	NCF1	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 113 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
Trafficking of GluR2-containing AMPA receptors	5	42.5×	5e-06
RHO GTPases Activate NADPH Oxidases	7	40.5×	4e-08
Ras activation upon Ca2+ influx through NMDA receptor	5	36.1×	1e-05
Unblocking of NMDA receptors, glutamate binding and activation	5	34.4×	1e-05
Negative regulation of NMDA receptor-mediated neuronal transmission	5	34.4×	1e-05
Assembly and cell surface presentation of NMDA receptors	10	32.1×	1e-10
Dopamine Neurotransmitter Release Cycle	5	31.4×	2e-05
Long-term potentiation	5	30.1×	2e-05

GO biological processes:

GO term	Partners	Fold	FDR
establishment or maintenance of epithelial cell apical/basal polarity	12	64.6×	1e-16
protein localization to synapse	6	42.6×	8e-07
receptor clustering	7	40.5×	9e-08
regulation of postsynaptic membrane neurotransmitter receptor levels	7	32.1×	4e-07
protein-containing complex assembly	10	10.5×	5e-06
cell-cell adhesion	11	10.3×	1e-06
Golgi organization	6	7.4×	5e-03
protein phosphorylation	9	5.7×	2e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	9
Likely pathogenic	1
Uncertain significance	1
Likely benign	1
Benign	0

Top pathogenic / likely-pathogenic (10)

Variant ID	HGVS	Classification
1176255	GRCh37/hg19 7q11.23(chr7:74191613-74191693)x1	Pathogenic
2250	NM_000265.7(NCF1):c.502del (p.Glu168fs)	Pathogenic
2251	NM_000265.7(NCF1):c.125G>A (p.Arg42Gln)	Pathogenic
2252	NM_000265.7(NCF1):c.811del (p.Val271fs)	Pathogenic
2253	NM_000265.7(NCF1):c.271C>T (p.Gln91Ter)	Pathogenic
2254	NM_000265.7(NCF1):c.333T>A (p.Cys111Ter)	Pathogenic
4682096	GRCh37/hg19 7q11.23(chr7:74191613-74199645)x1	Pathogenic
870704	GRCh37/hg19 7q11.23(chr7:74191613-74191693)x3	Pathogenic
872359	GRCh37/hg19 7q11.23(chr7:74191613-74191693)x0	Pathogenic
2501061	NC_000007.13:g.(74188451_74191612)_(74193769_74195125)dup	Likely pathogenic

SpliceAI

1635 predictions. Top by Δscore:

Variant	Effect	Δscore
7:74774099:ACTAT:A	donor_gain	1.0000
7:74774100:CTAT:C	donor_gain	1.0000
7:74774101:TAT:T	donor_gain	1.0000
7:74774101:TATG:T	donor_loss	1.0000
7:74774102:AT:A	donor_gain	1.0000
7:74774102:ATGT:A	donor_loss	1.0000
7:74774104:G:GG	donor_gain	1.0000
7:74774104:GTG:G	donor_loss	1.0000
7:74774108:G:GG	donor_gain	1.0000
7:74777263:CCA:C	acceptor_loss	1.0000
7:74777264:CAG:C	acceptor_loss	1.0000
7:74777265:A:AG	acceptor_gain	1.0000
7:74777265:A:T	acceptor_loss	1.0000
7:74777266:G:GG	acceptor_gain	1.0000
7:74777266:G:GT	acceptor_loss	1.0000
7:74777266:GGT:G	acceptor_gain	1.0000
7:74777343:TCCAT:T	donor_gain	1.0000
7:74777346:AT:A	donor_gain	1.0000
7:74777346:ATG:A	donor_loss	1.0000
7:74777347:TG:T	donor_loss	1.0000
7:74777348:G:GA	donor_loss	1.0000
7:74777348:G:GG	donor_gain	1.0000
7:74777349:T:A	donor_loss	1.0000
7:74777350:G:GT	donor_loss	1.0000
7:74779080:A:AG	acceptor_gain	1.0000
7:74779081:G:GG	acceptor_gain	1.0000
7:74779248:T:TA	acceptor_gain	1.0000
7:74779255:A:AG	acceptor_gain	1.0000
7:74779256:G:GG	acceptor_gain	1.0000
7:74779419:ACCA:A	donor_gain	1.0000

AlphaMissense

2562 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
7:74783530:T:A	W194R	0.999
7:74783530:T:C	W194R	0.999
7:74785286:T:A	W263R	0.999
7:74785286:T:C	W263R	0.999
7:74785289:T:A	W264R	0.999
7:74785289:T:C	W264R	0.999
7:74777319:G:C	R42P	0.998
7:74783579:T:A	L210H	0.998
7:74783579:T:C	L210P	0.998
7:74785284:G:T	G262V	0.998
7:74785288:G:C	W263C	0.998
7:74785288:G:T	W263C	0.998
7:74788010:C:A	P276Q	0.998
7:74788022:T:C	L280P	0.998
7:74783538:T:G	C196W	0.997
7:74785263:T:A	V255D	0.997
7:74785284:G:A	G262D	0.997
7:74789108:T:C	I374T	0.997
7:74783536:T:C	C196R	0.996
7:74785283:G:C	G262R	0.996
7:74779100:T:C	F58L	0.995
7:74779102:C:A	F58L	0.995
7:74779102:C:G	F58L	0.995
7:74779112:G:C	A62P	0.995
7:74782968:T:G	Y161D	0.995
7:74782972:G:C	R162P	0.995
7:74783041:T:A	V185D	0.995
7:74783525:G:A	G192D	0.995
7:74783527:T:A	W193R	0.995
7:74783527:T:C	W193R	0.995

dbSNP variants (sampled 300 via entrez): RS1057519503 (7:74789339 G>A), RS10614 (7:74779322 A>C,G,T), RS111979289 (7:74772242 G>A), RS112000369 (7:74783077 T>C), RS112894340 (7:74777495 T>G), RS113297930 (7:74775965 G>A,T), RS113623758 (7:74787032 C>T), RS1156272463 (7:74773300 TAAA>T,TAA,TAAAA), RS1156364926 (7:74776159 C>T), RS1156436114 (7:74772402 G>C), RS1156657755 (7:74778735 C>T), RS1156867339 (7:74777503 C>T), RS1156940409 (7:74781952 A>G), RS1157422966 (7:74785261 G>A), RS1157428702 (7:74781550 A>G)

Disease associations

OMIM: gene MIM:608512 | disease phenotypes: MIM:233700, MIM:306400

GenCC curated gene-disease

Disease	Classification	Inheritance
granulomatous disease, chronic, autosomal recessive, cytochrome b-positive, type 1	Strong	Autosomal recessive
chronic granulomatous disease	Supportive	Autosomal recessive

Mondo (2): granulomatous disease, chronic, autosomal recessive, cytochrome b-positive, type 1 (MONDO:0009309), chronic granulomatous disease (MONDO:0018305)

Orphanet (1): Chronic granulomatous disease (Orphanet:379)

HPO phenotypes

226 total (30 of 226 shown, HPO-id order):

HPO	Term
HP:0000007	Autosomal recessive inheritance
HP:0000010	Recurrent urinary tract infections
HP:0000014	Abnormality of the bladder
HP:0000015	Bladder diverticulum
HP:0000023	Inguinal hernia
HP:0000025	Functional abnormality of male internal genitalia
HP:0000028	Cryptorchidism
HP:0000044	Hypogonadotropic hypogonadism
HP:0000075	Renal duplication
HP:0000076	Vesicoureteral reflux
HP:0000083	Renal insufficiency
HP:0000089	Renal hypoplasia
HP:0000093	Proteinuria
HP:0000121	Nephrocalcinosis
HP:0000125	Pelvic kidney
HP:0000147	Polycystic ovaries
HP:0000154	Wide mouth
HP:0000158	Macroglossia
HP:0000179	Thick lower lip vermilion
HP:0000212	Gingival overgrowth
HP:0000230	Gingivitis
HP:0000232	Everted lower lip vermilion
HP:0000246	Sinusitis
HP:0000252	Microcephaly
HP:0000275	Narrow face
HP:0000280	Coarse facial features
HP:0000286	Epicanthus
HP:0000307	Pointed chin
HP:0000337	Broad forehead
HP:0000343	Long philtrum

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST011491_2	Systemic lupus erythematosus	3.000000e-81
GCST90014238_1	Systemic lupus erythematosus	2.000000e-26

MeSH disease descriptors (2)

Descriptor	Name	Tree numbers
D006105	Granulomatous Disease, Chronic	C15.378.553.774.535; C16.320.322.233; C20.673.774.535; C23.550.291.500.423
C565532	Granulomatous Disease, Chronic, Autosomal Recessive, Cytochrome B-Positive, Type I (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1613743 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 13,237 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL51085	EBSELEN	3	13,237

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

Binding affinities (BindingDB)

880 measured of 928 human assays (1015 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
5-phenyl-[1,2,4]triazolo[4,3-c]quinazoline	EC50	0.00172 nM
2-[[3-(4-ethylphenyl)-1-phenyl-pyrazol-4-yl]methyl]isothiourea;hydrochloride	EC50	39.9 nM
(E)-3-amino-2-[2-[[5-(1,3-benzodioxol-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]acetyl]but-2-enenitrile	EC50	59 nM
MLS000111651	IC50	124 nM
2-chloranyl-3-[[4-(diethylamino)phenyl]amino]naphthalene-1,4-dione	EC50	170 nM
MLS000052401	IC50	264 nM	US-9247759: Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
MLS000911514	EC50	340 nM
(E)-2-cyano-3-[(3E)-3-[[4-(diethylamino)phenyl]methylidene]-2-(4-morpholinyl)-1-cyclopentenyl]-N-(2-fluorophenyl)-2-propenamide	IC50	390 nM
3-[2-[[5-(4-nitrophenyl)-2-furanyl]methylidene]hydrazinyl]-2-indolone	IC50	400 nM
3-acetamido-4-methylbenzoic acid (2-oxo-1,2-diphenylethyl) ester	EC50	402 nM
2-amino-4-[4-(4-chlorobenzyl)oxy-3-methoxy-phenyl]-6-phenyl-1,4-dihydropyrimidine-5-carboxylic acid ethyl ester	EC50	580 nM
(NZ)-N-[3-(4-hydroxyanilino)-4-keto-1-naphthylidene]thiophene-2-sulfonamide	IC50	656 nM
5-Bromo-6-oxo-6H-pyran-3-carboxylic acid (4-isopropyl-3-methyl-phenyl)-amide	IC50	685 nM
3-(ethylthio)-6-(4-methylphenyl)pyridazine	EC50	690 nM
cid_6161440	IC50	730 nM
2-Cyano-N-[2-(1H-indol-3-yl)-ethyl]-3-(5-piperidin-1-yl-furan-2-yl)-acrylamide	EC50	753 nM
(5Z)-5-{[4-(dimethylamino)phenyl]imino}-1-(3-hydroxypropyl)-4-methyl-2,6-dioxo-1,2,5,6-tetrahydropyridine-3-carbonitrile	EC50	760 nM
(5Z)-4-methyl-5-[(3-methylphenyl)hydrazinylidene]-2,6-bis(oxidanylidene)pyridine-3-carbonitrile	EC50	775 nM
MLS000591719	EC50	950 nM
SMR000391146	EC50	1010 nM
5-hydroxy-4-[[4-(2-hydroxyethyl)-1-piperazinyl]methyl]-2-methyl-3-benzo[g]benzofurancarboxylic acid ethyl ester	IC50	1130 nM
2-{3-[(2-Hydroxy-benzoyl)-hydrazono]-2-oxo-2,3-dihydro-indol-1-yl}-N-o-tolyl-acetamide	IC50	1230 nM
4-[4-[[2-(3-methyl-4-oxo-1-phthalazinyl)-1-oxoethyl]amino]phenyl]-1-piperazinecarboxylic acid tert-butyl ester	IC50	1250 nM
cid_6701	IC50	1310 nM
3-(2-furanyl)-5-[(E)-2-(4-nitrophenyl)ethenyl]-2-phenyl-3,4-dihydropyrazole	EC50	1340 nM
4-chloranyl-N-(1-thiophen-2-ylethylideneamino)benzamide	EC50	1400 nM
4-[2-[1-(1,3-benzodioxol-5-yl)ethylidene]hydrazinyl]-3-nitro-benzenesulfonamide	EC50	1400 nM
2-((2E)-2-{[5-(4-chloro-2-nitrophenyl)-2-furyl]methylene}hydrazino)-4-(methoxymethyl)-6-methylnicotinonitrile	IC50	1420 nM
(5S)-4-[2-(3,4-dichlorophenyl)ethyl]-1-[(1R)-5-[methyl(p-anisyl)amino]-1-[(p-anisylamino)methyl]pentyl]-5-phenyl-piperazine-2,3-quinone	EC50	1480 nM
MLS000392355	IC50	1490 nM
2,5-bis(diethylaminomethyl)benzene-1,4-diol	IC50	1580 nM
5-[4-(dimethylamino)phenyl]imino-1-(2-hydroxyethyl)-2,6-diketo-4-methyl-nicotinonitrile	EC50	1630 nM
SMR000391068	EC50	1750 nM
MLS001007244	EC50	1840 nM
4-[5-[(Z)-[3-(1,1-diketothiolan-3-yl)-4-keto-2-thioxo-thiazolidin-5-ylidene]methyl]-2-furyl]benzenesulfonamide	IC50	1850 nM
2-[[4-(2,4-dichlorobenzyl)oxybenzylidene]amino]guanidine	EC50	1910 nM
3-(3-chloro-4-methoxybenzyl)-6,7-dimethoxy-2-[(4-methylbenzyl)sulfanyl]-4(3H)-quinazolinimine	EC50	1970 nM
MLS000548432	IC50	1990 nM
3-(4-methylphenyl)-5-(4-morpholinyl)-2-phenyl-1,2,4-thiadiazol-2-ium	EC50	2040 nM
MLS000041935	IC50	2090 nM
MLS000548244	IC50	2100 nM
5-methyl-N-[[(3E)-6-oxidanylidene-3-(phenylhydrazinylidene)cyclohexa-1,4-dien-1-yl]methylideneamino]-1H-pyrazole-3-carboxamide	IC50	2220 nM
2-amino-4-[4-(4-carbomethoxybenzyl)oxyphenyl]-6-phenyl-1,4-dihydropyrimidine-5-carboxylic acid ethyl ester	EC50	2380 nM
5-chloranyl-7-[(4-ethylpiperazin-1-yl)-pyridin-3-yl-methyl]quinolin-8-ol	IC50	2390 nM
cid_1548953	IC50	2410 nM
MLS000110474	EC50	2430 nM
13-chloro-10-(4-methylpiperazin-1-yl)-2-oxa-9-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,9,12,14-heptaene	KI	2460 nM
2-nitro-4-[(6-nitro-4-quinolinyl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide	IC50	2460 nM
MLS000562851	IC50	2550 nM
2-{3-[(3-Hydroxy-naphthalene-2-carbonyl)-hydrazono]-2-oxo-2,3-dihydro-indol-1-yl}-N-p-tolyl-acetamide	IC50	2570 nM

ChEMBL bioactivities

69 potent at pChembl≥5 of 161 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.37	Kd	43	nM	CHEMBL5197024
6.67	Kd	214	nM	CHEMBL5205264
6.66	Ki	220	nM	CHEMBL5411448
6.62	Ki	240	nM	CHEMBL5410142
6.62	Ki	240	nM	CHEMBL5419067
6.51	Kd	312	nM	CHEMBL5177721
6.51	Ki	310	nM	CHEMBL5427803
6.38	Ki	420	nM	CHEMBL5427803
6.38	Ki	420	nM	CHEMBL5410678
6.38	Ki	420	nM	CHEMBL5410142
6.36	Ki	440	nM	CHEMBL5411448
6.36	Ki	440	nM	CHEMBL5410142
6.33	Ki	470	nM	CHEMBL5406295
6.30	Ki	500	nM	CHEMBL5412642
6.28	Kd	530	nM	CHEMBL5410142
6.25	Ki	560	nM	CHEMBL5437628
6.22	Ki	600	nM	CHEMBL5419067
6.22	Ki	600	nM	CHEMBL5410142
6.20	Kd	630	nM	CHEMBL5410142
6.19	Ki	640	nM	CHEMBL5410678
6.17	Ki	680	nM	CHEMBL5413540
6.17	Ki	680	nM	CHEMBL5412642
6.15	Kd	710	nM	CHEMBL5419067
6.10	Kd	790	nM	CHEMBL5419067
6.09	Kd	810	nM	CHEMBL5410142
6.01	Ki	980	nM	CHEMBL5437628
5.91	Ki	1220	nM	CHEMBL5398246
5.91	Ki	1230	nM	CHEMBL5411421
5.89	Ki	1290	nM	CHEMBL5439674
5.88	Ki	1320	nM	CHEMBL5438922
5.87	Ki	1360	nM	CHEMBL5439369
5.82	Ki	1500	nM	CHEMBL5419067
5.80	Ki	1580	nM	CHEMBL5426199
5.80	Ki	1600	nM	CHEMBL5419067
5.79	Ki	1640	nM	CHEMBL5433544
5.75	Ki	1770	nM	CHEMBL5429601
5.74	Ki	1820	nM	CHEMBL5422476
5.73	Ki	1880	nM	CHEMBL5399098
5.71	Ki	1930	nM	CHEMBL5406852
5.70	Kd	2000	nM	CHEMBL5419067
5.66	Ki	2170	nM	CHEMBL5425286
5.59	Ki	2580	nM	CHEMBL5414953
5.55	Ki	2840	nM	CHEMBL5437289
5.53	Ki	2940	nM	CHEMBL5436213
5.50	Ki	3180	nM	CHEMBL5432879
5.47	Ki	3370	nM	CHEMBL5421420
5.44	Ki	3620	nM	CHEMBL5438924
5.44	Ki	3630	nM	CHEMBL5425482
5.44	Ki	3600	nM	CHEMBL5419067
5.43	Ki	3740	nM	CHEMBL5404103

PubChem BioAssay actives

67 with measured affinity, of 348 total; 48 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)-N-[(2S)-1-(2-cyclopropylethylamino)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-1-[(2S)-1-[(2S)-1-[4-[3-(3,4-dichlorophenyl)anilino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxamide	1880670: Binding affinity to human N-terminal TEV cleavable 6His tagged p47phox (151-285 residues) assessed as dissociation rate constant by Surface plasmon resonance assay	kd	0.0430	uM
(2S)-2-[[(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-1-[(2S)-1-[(2S)-1-[(2S)-4-amino-2-[[(2S)-3-hydroxy-2-[[(2S)-1-[(2S)-pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]propanoic acid	1880670: Binding affinity to human N-terminal TEV cleavable 6His tagged p47phox (151-285 residues) assessed as dissociation rate constant by Surface plasmon resonance assay	kd	0.2140	uM
5-[2-[2-(2-aminoquinolin-5-yl)oxyethoxy]ethoxy]-4-methylquinolin-2-amine	2020335: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tag cleaved human p47phox (151 to 386 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins in presence of 0.005% Tween20 and 2% DMSO by fluorescence polarization assay	ki	0.2200	uM
6-[2-[2-[4-[(2-aminoquinolin-6-yl)oxymethyl]triazol-1-yl]ethoxy]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	0.2400	uM
5-[2-[2-(2-aminoquinolin-5-yl)oxyethoxy]ethoxy]quinolin-2-amine	2020335: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tag cleaved human p47phox (151 to 386 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins in presence of 0.005% Tween20 and 2% DMSO by fluorescence polarization assay	ki	0.2400	uM
5-[2-[2-(2-aminoquinolin-5-yl)oxyethylamino]ethoxy]quinolin-2-amine	2020335: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tag cleaved human p47phox (151 to 386 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins in presence of 0.005% Tween20 and 2% DMSO by fluorescence polarization assay	ki	0.3100	uM
trans-(1R,2R)-N-[(2S)-1-(2-cyclopropylethylamino)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[(R)-[(2S)-1-[(2S)-1-[4-[3-(3,4-dichlorophenyl)anilino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]pyrrolidin-2-yl]-hydroxymethyl]cyclopentane-1-carboxamide	1880670: Binding affinity to human N-terminal TEV cleavable 6His tagged p47phox (151-285 residues) assessed as dissociation rate constant by Surface plasmon resonance assay	kd	0.3120	uM
5-[2-[2-(2-aminoquinolin-5-yl)oxyethyl-methylamino]ethoxy]quinolin-2-amine	2020335: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tag cleaved human p47phox (151 to 386 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins in presence of 0.005% Tween20 and 2% DMSO by fluorescence polarization assay	ki	0.4200	uM
5-[2-[2-(2-amino-4-methylquinolin-5-yl)oxyethoxy]ethoxy]-4-methylquinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	0.4700	uM
6-[4-[4-[(2-aminoquinolin-6-yl)oxymethyl]triazol-1-yl]butoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	0.5000	uM
5-[2-[2-(2-aminoquinolin-5-yl)oxyethoxy]ethoxy]-7-methylquinolin-2-amine	2020335: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tag cleaved human p47phox (151 to 386 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins in presence of 0.005% Tween20 and 2% DMSO by fluorescence polarization assay	ki	0.5600	uM
5-[5-(2-aminoquinolin-5-yl)oxypentoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	0.6800	uM
5-[2-[2-(2-aminoquinolin-5-yl)oxyethoxy]ethoxy]-3-methylquinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	1.2200	uM
6-[[1-[2-[2-(2-aminoquinolin-6-yl)oxyethoxy]ethyl]triazol-4-yl]methoxy]-4-chloroquinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	1.2300	uM
5-[[1-[2-[2-(2-aminoquinolin-6-yl)oxyethoxy]ethyl]triazol-4-yl]methoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	1.2900	uM
5-[2-[2-[2-(methylamino)quinolin-5-yl]oxyethoxy]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	1.3200	uM
6-[2-[2-[4-[(2-aminoquinolin-6-yl)oxymethyl]triazol-1-yl]ethoxy]ethoxy]-4-(azepan-1-yl)quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	1.3600	uM
5-[2-[2-(2-aminoquinolin-5-yl)oxyethoxy]ethoxy]-7-phenylquinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	1.5800	uM
5-[2-[2-(2-amino-3-methylquinolin-5-yl)oxyethoxy]ethoxy]-3-methylquinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	1.6400	uM
5-[2-[2-(2-aminoquinolin-5-yl)oxyethoxy]ethoxy]-8-methylquinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	1.7700	uM
6-[[1-[2-[2-[4-[(2-aminoquinolin-6-yl)oxymethyl]triazol-1-yl]ethoxy]ethyl]triazol-4-yl]methoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	1.8200	uM
6-[[1-[2-[2-(2-aminoquinolin-6-yl)oxyethoxy]ethyl]triazol-4-yl]methoxy]-4-(azepan-1-yl)quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	1.8800	uM
5-[2-[2-[2-(ethylamino)quinolin-5-yl]oxyethoxy]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	1.9300	uM
6-[2-[2-[2-[4-[(2-aminoquinolin-6-yl)oxymethyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	2.1700	uM
6-[2-[2-[4-[[2-amino-4-(azepan-1-yl)quinolin-6-yl]oxymethyl]triazol-1-yl]ethoxy]ethoxy]-4-(azepan-1-yl)quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	2.5800	uM
5-[2-[N-[2-(2-aminoquinolin-5-yl)oxyethyl]anilino]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	2.8400	uM
6-[2-[2-[4-[(2-amino-3-methylquinolin-6-yl)oxymethyl]triazol-1-yl]ethoxy]ethoxy]-3-methylquinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	2.9400	uM
5-[2-[2-[2-(2-aminoquinolin-5-yl)oxyethoxy]ethoxy]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	3.1800	uM
4-[[1-[2-[2-(2-aminoquinolin-6-yl)oxyethoxy]ethyl]triazol-4-yl]methoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	3.3700	uM
6-[2-[4-[(2-aminoquinolin-6-yl)oxymethyl]triazol-1-yl]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	3.6200	uM
2-(2-aminoquinolin-6-yl)oxy-N-[2-[2-(2-aminoquinolin-6-yl)oxyethoxy]ethyl]acetamide	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	3.6300	uM
5-[2-[2-[4-[(2-aminoquinolin-5-yl)oxymethyl]triazol-1-yl]ethoxy]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	3.7400	uM
N,N-bis[2-(2-aminoquinolin-5-yl)oxyethyl]-4-methylbenzenesulfonamide	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	4.2500	uM
6-[2-[2-[4-[(2-aminoquinolin-6-yl)oxymethyl]triazol-1-yl]ethoxy]ethoxy]-4-chloroquinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	4.9000	uM
4-[(2S)-2-[(2S)-2-[(2S)-2-[4-[(diaminomethylideneamino)methyl]piperidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-N-[3-(1,3-oxazol-5-yl)phenyl]-4-oxobutanamide	1880670: Binding affinity to human N-terminal TEV cleavable 6His tagged p47phox (151-285 residues) assessed as dissociation rate constant by Surface plasmon resonance assay	kd	5.1700	uM
7-[2-[4-[(2-aminoquinolin-7-yl)oxymethyl]triazol-1-yl]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	5.5000	uM
7-[2-[2-[2-[2-(2-aminoquinolin-7-yl)oxyethoxy]ethoxy]ethoxy]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	5.7200	uM
4-[2-[2-[4-[(2-aminoquinolin-4-yl)oxymethyl]triazol-1-yl]ethoxy]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	5.9200	uM
5-[2-[2-[2-(tert-butylamino)quinolin-5-yl]oxyethoxy]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	6.3100	uM
7-[2-[2-(2-aminoquinolin-7-yl)oxyethoxy]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	6.3400	uM
7-[2-[2-[4-[(2-aminoquinolin-7-yl)oxymethyl]triazol-1-yl]ethoxy]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	6.3900	uM
7-[2-[2-[4-[(2-aminoquinolin-6-yl)oxymethyl]triazol-1-yl]ethoxy]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	6.7800	uM
5-[2-[2-[4-[(2-aminoquinolin-6-yl)oxymethyl]triazol-1-yl]ethoxy]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	6.8500	uM
7-[2-[2-[2-[2-[2-[2-(2-aminoquinolin-7-yl)oxyethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	7.5800	uM
7-[[1-[2-[2-(2-aminoquinolin-6-yl)oxyethoxy]ethyl]triazol-4-yl]methoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	8.4000	uM
6-[2-[2-(2-aminoquinolin-6-yl)oxyethoxy]ethoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	9.4400	uM
5-[2-[2-(2-aminoquinolin-5-yl)oxyethoxy]ethoxy]-8-fluoroquinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	9.5300	uM
6-[3-[4-[(2-aminoquinolin-6-yl)oxymethyl]triazol-1-yl]propoxy]quinolin-2-amine	2020331: Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay	ki	9.9000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
acetovanillone	increases expression, decreases reaction, increases phosphorylation, affects localization, increases activity	7
Quercetin	affects cotreatment, affects localization, decreases reaction, increases expression, decreases expression	5
Tetradecanoylphorbol Acetate	affects localization, decreases reaction, increases expression, increases phosphorylation	5
Arsenic Trioxide	increases expression, increases reaction, affects localization, increases phosphorylation, decreases reaction	4
Benzo(a)pyrene	affects binding, increases reaction, decreases reaction, increases expression, affects localization (+1 more)	4
Catechin	decreases reaction, increases expression, decreases expression, affects cotreatment, affects localization	4
Glucose	decreases reaction, increases activity, increases expression, affects localization, increases phosphorylation (+1 more)	4
Tobacco Smoke Pollution	affects metabolic processing, affects localization, increases activity, increases expression	4
Tretinoin	decreases reaction, increases expression, increases reaction	4
2,4,5,2’,4’,5’-hexachlorobiphenyl	affects localization, affects binding, increases reaction, increases expression, increases localization (+2 more)	3
3,4,5,3’,4’-pentachlorobiphenyl	increases localization, increases phosphorylation, decreases reaction, affects binding, increases reaction (+1 more)	3
2,3’,4,4’,5-pentachlorobiphenyl	affects reaction, affects binding, increases reaction, increases expression, increases localization (+2 more)	3
chromium hexavalent ion	increases phosphorylation, increases abundance, decreases reaction, increases activity, affects reaction (+3 more)	3
Resveratrol	affects cotreatment, decreases reaction, increases expression, increases phosphorylation	3
diphenyleneiodonium	affects localization, decreases reaction, increases phosphorylation	2
bisindolylmaleimide I	affects localization, decreases reaction	2
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo(3,4-d)pyrimidine	affects localization, decreases reaction, affects binding, increases reaction, increases localization (+1 more)	2
Dichlorodiphenyl Dichloroethylene	decreases reaction, increases expression	2
Endosulfan	decreases reaction, increases expression	2
Folic Acid	decreases reaction, increases phosphorylation, affects cotreatment, increases abundance, increases expression	2
Homocysteine	increases phosphorylation, affects localization, increases abundance, increases reaction, increases activity (+2 more)	2
Lipopolysaccharides	increases phosphorylation, increases expression, increases reaction, affects localization, decreases reaction	2
Valproic Acid	affects cotreatment, increases expression, increases methylation	2
Arachidonic Acid	decreases reaction, increases localization, affects localization, affects reaction	2
Reactive Oxygen Species	increases abundance, increases reaction, affects reaction	2
Cadmium Chloride	increases expression, increases phosphorylation	2
Particulate Matter	increases abundance, increases expression, affects reaction, increases phosphorylation, affects cotreatment (+1 more)	2
Polyphenols	affects cotreatment, decreases reaction, increases expression, decreases expression	2
aristolochic acid I	increases expression	1
1-(3,4-dihydroxyphenyl)-3-(2-methoxyphenyl)prop-2-en-1-one	decreases reaction, affects localization	1

ChEMBL screening assays

49 unique, capped per target: 49 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4381025	Binding	Covalent inhibition of recombinant human His-tagged p47phox SH3A-B domain (151 to 285 residues) expressed in Escherichia coli BL21 (DE3) cells interaction with Cy5-p22phox149-162 incubated for 10 mins by fluorescence polarization competitio	Developing Inhibitors of the p47phox-p22phox Protein-Protein Interaction by Fragment-Based Drug Discovery. — J Med Chem

Cellosaurus cell lines

6 cell lines: 2 cancer cell line, 2 induced pluripotent stem cell, 2 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_C8HI	PLB-985 NCF1 DeltaGT	Cancer cell line	Female
CVCL_E1N4	HyCyte THP-1 KO-hNCF1	Cancer cell line	Male
CVCL_V181	iPSC-CGD1.1	Induced pluripotent stem cell	Male
CVCL_V182	iPSC-CGD1.2	Induced pluripotent stem cell	Male
CVCL_V329	CHO-91-22-47-67	Spontaneously immortalized cell line	Female
CVCL_V330	CHO-91-47-67	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00001317	PHASE4	COMPLETED	A Phase IV Study of Recombinant Human Gamma Interferon in Patients With Chronic Granulomatous Diseases of Childhood
NCT00023192	PHASE3	COMPLETED	Treatment of Chronic Granulomatous Disease With Allogeneic Stem Cell Transplantation Versus Standard of Care
NCT00033982	PHASE3	COMPLETED	Posaconazole to Treat Invasive Fungal Infections
NCT00006417	PHASE2	COMPLETED	Modified Stem Cell Transplantation Procedure for Treating Chronic Granulomatous Disease
NCT00578643	PHASE2	COMPLETED	Matched Unrelated or Non-Genotype Identical Related Donor Transplantation For Chronic Granulomatous Disease
NCT00799071	PHASE2	COMPLETED	Pharmacokinetics of Posaconazole in Children With Chronic Granulomatous Disease (CGD)
NCT01821781	PHASE2	ACTIVE_NOT_RECRUITING	Immune Disorder HSCT Protocol
NCT01998633	PHASE2	COMPLETED	Reduced Intensity Conditioning for Hemophagocytic Syndromes or Selected Primary Immune Deficiencies (BMT CTN 1204)
NCT02512679	PHASE2	TERMINATED	Related Hematopoietic Stem Cell Transplantation (HSCT) for Genetic Diseases of Blood Cells
NCT03333486	PHASE2	TERMINATED	Fludarabine Phosphate, Cyclophosphamide, Total Body Irradiation, and Donor Stem Cell Transplant in Treating Patients With Blood Cancer
NCT03547830	PHASE2	UNKNOWN	Plerixafor/G-CSF as Additional Agents for Conditioning Before HSCT in CGD Patients
NCT03983837	PHASE2	COMPLETED	Elemental Diet for Treatment of Inflammatory Bowel Disease in Patients With Chronic Granulomatous Disease
NCT07284641	PHASE2	RECRUITING	Hematopoietic Stem Cell Transplantation (HSCT) for Common Variable Immunodeficiency (CVID) and Other Autoimmune Manifestations of Primary Immune Regulatory Disorders (PIRD)
NCT00001476	PHASE1	COMPLETED	Gene Therapy for Chronic Granulomatous Diseases - Long-term Follow-up
NCT00001515	PHASE1	COMPLETED	Diagnostic Effectiveness of Virtual Bronchoscopy
NCT00001765	PHASE1	COMPLETED	Stem Cell Transplant Following Low-Intensity Chemotherapy to Treat Chronic Granulomatous Disease
NCT01917708	PHASE1	COMPLETED	Bone Marrow Transplant With Abatacept for Non-Malignant Diseases
NCT02609932	PHASE1	COMPLETED	Effect of IFN-γ on Innate Immune Cells
NCT05189925	PHASE1	RECRUITING	NADPH Oxidase Correction in mRNA-transfected Granulocyte-enriched Cells in Chronic Granulomatous Disease (CGD)
NCT03984890	PHASE2/PHASE3	COMPLETED	Vitamin D3 For CGD Patients With BCGosis/Itis
NCT00325078	PHASE1/PHASE2	TERMINATED	Infliximab to Treat Crohn’S-like Inflammatory Bowel Disease in Chronic Granulomatous Disease
NCT00564759	PHASE1/PHASE2	UNKNOWN	Gene Therapy for Chronic Granulomatous Disease
NCT00778882	PHASE1/PHASE2	WITHDRAWN	Gene Therapy for Chronic Granulomatous Disease in Korea
NCT00927134	PHASE1/PHASE2	COMPLETED	Gene Therapy for X-linked Chronic Granulomatous Disease (CGD) in Children
NCT01338675	PHASE1/PHASE2	UNKNOWN	Targeted Busulfan, Fludarabine Conditioning Regimen for Hematopoietic Stem Cell Transplantation in Chronic Granulomatous Disease(CGD)
NCT01852370	PHASE1/PHASE2	ENROLLING_BY_INVITATION	Sequential Cadaveric Lung and Bone Marrow Transplant for Immune Deficiency Diseases
NCT02282904	PHASE1/PHASE2	TERMINATED	Haploidentical Transplant for People With Chronic Granulomatous Disease Using Post Transplant Cyclophosphamide
NCT03080480	PHASE1/PHASE2	TERMINATED	Pioglitazone Therapy for Chronic Granulomatous Disease
NCT03513328	PHASE1/PHASE2	COMPLETED	Conditioning Regimen for Allogeneic Hematopoietic Stem-Cell Transplantation
NCT05104723	PHASE1/PHASE2	COMPLETED	Safety and Efficacy of Tofacitinib for Chronic Granulomatous Disease With Inflammatory Complications
NCT05463133	PHASE1/PHASE2	RECRUITING	Allogeneic Hematopoietic Stem Cell Transplantation for Chronic Granulomatous Disease (CGD) With an Alemtuzumab, Busulfan and TBI-based Conditioning Regimen Combined With Cytokine (IL-6, +/- IFN-gamma) Antagonists
NCT06253507	PHASE1/PHASE2	ENROLLING_BY_INVITATION	pCCLCHIM-p47 (Lentiviral Vector Transduced CD34 Plus Cells) in Patients With p47 Autosomal Recessive Chronic Granulomatous Disease (AR-CGD)
NCT06325709	PHASE1/PHASE2	RECRUITING	Base Editing for Mutation Repair in Hematopoietic Stem & Progenitor Cells for X-Linked Chronic Granulomatous Disease
NCT06559176	PHASE1/PHASE2	ENROLLING_BY_INVITATION	A Study of the Safety and Efficacy of Prime Editing (PM359) in Participants With p47phox Autosomal Recessive Chronic Granulomatous Disease (CGD )
NCT07113743	PHASE1/PHASE2	ENROLLING_BY_INVITATION	Part B- G1X-CGD (Lentiviral Vector Transduced CD34+ Cells) in Patients With X-Linked Chronic Granulomatous Disease
NCT00394316	EARLY_PHASE1	TERMINATED	Gene Therapy for Chronic Granulomatous Disease
NCT03910452	EARLY_PHASE1	ACTIVE_NOT_RECRUITING	Haploidentical Transplant for People With Chronic Granulomatous Disease (CGD) Using Alemtuzumab, Busulfan and TBI With Post-Transplant Cyclophosphamide
NCT03921515	EARLY_PHASE1	WITHDRAWN	Skin Immunity Sample Collection Involving Blisters and Biopsies
NCT04136028	EARLY_PHASE1	COMPLETED	IL-1 Receptor Inhibitor for Granulomatous Complications in Patients With Chronic Granulomatous Disease
NCT05600907	EARLY_PHASE1	ACTIVE_NOT_RECRUITING	Study to Assess the Use of JSP191 in Matched Unrelated Donor Transplantation for Chronic Granulomatous Disease (CGD)