FURIN

Summary

FURIN (furin, paired basic amino acid cleaving enzyme, HGNC:8568) is a protein-coding gene on chromosome 15q26.1, encoding Furin (P09958). Ubiquitous endoprotease within constitutive secretory pathways capable of cleavage at the RX(K/R)R consensus motif. It is a selective cancer dependency (DepMap: 16.1% of cell lines).

This gene encodes a member of the subtilisin-like proprotein convertase family, which includes proteases that process protein and peptide precursors trafficking through regulated or constitutive branches of the secretory pathway. It encodes a type 1 membrane bound protease that is expressed in many tissues, including neuroendocrine, liver, gut, and brain. The encoded protein undergoes an initial autocatalytic processing event in the ER and then sorts to the trans-Golgi network through endosomes where a second autocatalytic event takes place and the catalytic activity is acquired. Like other members of this convertase family, the product of this gene specifically cleaves substrates at single or paired basic residues. Some of its substrates include proparathyroid hormone, transforming growth factor beta 1 precursor, proalbumin, pro-beta-secretase, membrane type-1 matrix metalloproteinase, beta subunit of pro-nerve growth factor and von Willebrand factor. It is thought to be one of the proteases responsible for the activation of HIV envelope glycoproteins gp160 and gp140, and may play a role in tumor progression. Unlike SARS-CoV and other coronaviruses, the spike protein of SARS-CoV-2 is thought to be uniquely cleaved by this protease. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 5045 — RefSeq curated summary.

At a glance

• GWAS associations: 54
• Clinical variants (ClinVar): 128 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 16.1% of screened cell lines
• MANE Select transcript: NM_002569

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:8568
Approved symbol	FURIN
Name	furin, paired basic amino acid cleaving enzyme
Location	15q26.1
Locus type	gene with protein product
Status	Approved
Aliases	SPC1
Ensembl gene	ENSG00000140564
Ensembl biotype	protein_coding
OMIM	136950
Entrez	5045

Gene structure

Transcript identifiers

Ensembl transcripts: 25 — 20 protein_coding, 3 nonsense_mediated_decay, 1 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000268171, ENST00000558794, ENST00000560018, ENST00000610579, ENST00000618099, ENST00000680053, ENST00000680086, ENST00000680687, ENST00000681804, ENST00000681865, ENST00000853380, ENST00000853381, ENST00000853382, ENST00000853383, ENST00000853384, ENST00000853385, ENST00000853386, ENST00000916022, ENST00000916023, ENST00000916024, ENST00000916025, ENST00000916026, ENST00000916027, ENST00000916028, ENST00000916029

RefSeq mRNA: 7 — MANE Select: NM_002569 NM_001289823, NM_001289824, NM_001382619, NM_001382620, NM_001382621, NM_001382622, NM_002569

CCDS: CCDS10364

Canonical transcript exons

ENST00000268171 — 16 exons

Exon	Start	End
ENSE00000943885	90876255	90876353
ENSE00000943886	90876462	90876557
ENSE00000943887	90876896	90877024
ENSE00000943888	90877135	90877211
ENSE00000943889	90877527	90877615
ENSE00000943890	90878132	90878304
ENSE00000943891	90878764	90878976
ENSE00000943892	90879444	90879544
ENSE00000943893	90879671	90879774
ENSE00000943894	90879867	90879984
ENSE00000943895	90880094	90880273
ENSE00000943896	90880691	90880815
ENSE00000943897	90880930	90881040
ENSE00001309513	90875582	90875917
ENSE00001340347	90868588	90868711
ENSE00003847972	90881286	90883457

Expression profiles

Bgee: expression breadth ubiquitous, 278 present calls, max score 98.19.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 6.4977 / max 725.1967, expressed in 1239 samples.

FANTOM5 promoters (9 alternative TSS)

Promoter ID	TPM avg	Samples expressed
148484	4.3618	532
148494	0.5645	264
148489	0.4164	212
148485	0.2300	94
148488	0.2236	84
148492	0.2195	99
148487	0.2186	99
148490	0.1544	54
148491	0.1090	39

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right lobe of liver	UBERON:0001114	98.19	gold quality
body of pancreas	UBERON:0001150	96.39	gold quality
right lung	UBERON:0002167	95.86	gold quality
liver	UBERON:0002107	95.15	gold quality
right lobe of thyroid gland	UBERON:0001119	94.68	gold quality
left lobe of thyroid gland	UBERON:0001120	94.55	gold quality
apex of heart	UBERON:0002098	94.54	gold quality
skin of leg	UBERON:0001511	94.46	gold quality
upper lobe of left lung	UBERON:0008952	94.43	gold quality
saliva-secreting gland	UBERON:0001044	94.26	gold quality
pancreas	UBERON:0001264	94.08	gold quality
metanephros cortex	UBERON:0010533	93.92	gold quality
adenohypophysis	UBERON:0002196	93.85	gold quality
minor salivary gland	UBERON:0001830	93.84	gold quality
monocyte	CL:0000576	93.73	gold quality
thyroid gland	UBERON:0002046	93.70	gold quality
upper lobe of lung	UBERON:0008948	93.33	gold quality
granulocyte	CL:0000094	93.32	gold quality
leukocyte	CL:0000738	93.32	gold quality
blood	UBERON:0000178	93.25	gold quality
mononuclear cell	CL:0000842	93.24	gold quality
skin of abdomen	UBERON:0001416	93.23	gold quality
omental fat pad	UBERON:0010414	93.23	gold quality
peritoneum	UBERON:0002358	93.21	gold quality
type B pancreatic cell	CL:0000169	93.17	silver quality
olfactory bulb	UBERON:0002264	93.00	silver quality
mucosa of stomach	UBERON:0001199	92.87	gold quality
gastrocnemius	UBERON:0001388	92.72	gold quality
right atrium auricular region	UBERON:0006631	92.72	gold quality
parotid gland	UBERON:0001831	92.63	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 3.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	15.22
E-ENAD-27	yes	4.83
E-MTAB-6678	yes	4.61

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CDX2, CEBPB, GATA1, HIF1A, LITAF, PPARA, RAI1, SMAD2, SOX9, SP1, TP53

miRNA regulators (miRDB)

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

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-4283	100.00	66.42	2097
HSA-MIR-4455	100.00	65.48	1587
HSA-MIR-9-5P	100.00	72.28	2361
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-3667-3P	99.99	67.17	1636
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-6778-3P	99.96	67.29	2693
HSA-MIR-548AA	99.96	70.64	3753
HSA-MIR-548AP-3P	99.96	70.64	3753
HSA-MIR-548T-3P	99.96	70.64	3753
HSA-MIR-3912-5P	99.95	66.11	925
HSA-MIR-6755-5P	99.95	65.59	464
HSA-MIR-128-3P	99.95	71.17	2484
HSA-MIR-216A-3P	99.95	71.19	2505
HSA-MIR-3143	99.93	71.96	3104
HSA-MIR-6721-5P	99.93	68.92	2981
HSA-MIR-22-3P	99.93	68.13	917
HSA-MIR-515-5P	99.92	69.82	2343
HSA-MIR-519E-5P	99.92	69.62	2358
HSA-MIR-219A-5P	99.91	73.36	735
HSA-MIR-106A-5P	99.90	73.94	2683
HSA-MIR-17-5P	99.89	73.83	2665
HSA-MIR-4731-5P	99.89	67.23	2537
HSA-MIR-124-3P	99.89	73.74	3043
HSA-MIR-506-3P	99.89	73.55	3057
HSA-MIR-106B-5P	99.88	74.72	2795
HSA-MIR-20A-5P	99.88	74.76	2769
HSA-MIR-20B-5P	99.88	74.01	2621
HSA-MIR-4782-3P	99.88	73.31	735
HSA-MIR-519D-3P	99.88	73.97	2607

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 16.1% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 40)

• we investigated the specificity and potency of complete prodomains and short C-terminal prodomain peptides of each SPC on highly purified, soluble enzyme preparations of human SPC1, SPC6, and SPC7. (PMID:11723118)
• Furin proteolytically processes the heparin-binding region of extracellular superoxide dismutase (PMID:11861638)
• results show that shedding of furin occurs rapidly and further suggest that specific cysteine residues may impart a conformation to the enzyme, thereby affecting its susceptibility to proteolysis (PMID:12220680)
• involvement of the proximal GATA recognition motif in the P1 promoter and impact on the maturation of furin substrates of Furin gene regulation in differentiating megakaryoblastic cells. (PMID:12411321)
• Increased activity of this enzyme enhances the malignant phenotype of human head and neck cancer cells. (PMID:12547702)
• role in Semliki Forest virus p62 processing (PMID:12584323)
• furin has a role in processing human pro-CNP (PMID:12736257)
• Data suggest that mutations that diminish domain 2 Ca(2+) binding allow furin access to an otherwise protected cleavage site, initiating the proteolytic cascade that leads to gelsolin amyloidogenesis and familial amyloidosis of Finnish type. (PMID:14596804)
• findings established the existence of a novel alternative/complementary pathway by which furin increases tumor cell invasion through an amplification/activation loop between MMP-2 and TGFbeta (PMID:14644155)
• furin is a novel chemokine-modifying enzyme in vitro and most probably also in vivo, generating a C-terminally truncated CXCL10, which fully retains its (inverse) agonistic properties. (PMID:14739277)
• modelling of furin’s pro-region revealed that Ile-60 and His-66 might be crucial in forming the binding interface with the catalytic domain, while residues Trp-34 and Phe-67 might be involved in maintaining a hydrophobic core within the pro-region itself (PMID:14741044)
• furin is responsible for VEGF-C processing in human oral tongue squamous cell carcinoma progression (PMID:15240540)
• Results report the identification of Spn4A, a previously uncharacterized secretory pathway serine protease inhibitor (serpin) from Drosophila melanogaster that contains a consensus furin cleavage site. (PMID:15247425)
• HIV-1 gp160 processing by furin is inhibited by polyarginine (PMID:15371436)
• releases Feline foamy virus (FFV) Env leader protein (Elp)from ENV precursor protein. (PMID:15564468)
• HGF and BCL-2 family proteins use a furin-dependent pathway to promote invasion via TGF-beta and MMP in human malignant glioma cells and the pro-invasive properties of TGF-beta require furin- dependent MMP activity. (PMID:15584904)
• From a brain cDNA library of possible interacting proteins, furin efficiently processes both the beta-secretase beta-amyloid protein converting enzyme pro-BACE1 and its novel interacting partner brain-specific type II membrane protein pro-BRI3. (PMID:15606899)
• Analysis of furin promoters revealed the presence of putative binding sites for HIF-1; hypoxic/HIF-1 regulation of furin correlated with increased proteolytic activation of substrates MMP1 and TFGbeta1. (PMID:15611046)
• furin can directly cleave the RXXR amino acid sequence in the propeptide domain of proMMP-2 leading to inactivation of the enzyme. (PMID:15637056)
• serpin/furin complex stability depends on pH and regulation at the deacylation step (PMID:15659365)
• furin and PC5 play a role in a MT-MMP-MMP-2 proteolytic cascade, involving provision of macrophage MT1-MMP for the activation of pro-MMP-2; furin and PC5 are expressed in monocytes and colocalize with MT1-MMP in macrophages in the atherosclerotic plaque (PMID:15911696)
• an amino acid substitution in the PC1/3 propeptide can induce significant modifications of its inhibitory profile toward furin (PMID:16407210)
• pro-ADAMTS9 is processed at the cell surface by furin (PMID:16537537)
• IL-12 caused Furin to be preferentially expressed in differentiated Th1 cells in a Stat4-dependent manner (PMID:16627761)
• Furin mediates cleavage of a receptor tyrosine phosphatase and regulation of beta catenin’s transcriptional activity. (PMID:16648485)
• PCSK9 levels are finely regulated by the basic amino acid convertases furin and PC5/6A (PMID:16912035)
• furin enhances alpha-secretase activity via the cleavage of ADAM10 and TACE, and attenuated furin activity is connected to the production of Abeta (PMID:16942750)
• These findings highlight a pivotal role for furin, MT1-MMP, and MMP2 in TNF-alpha-induced sphingolipid signaling, and they identify this system as a possible target to inhibit SMC proliferation in vascular diseases. (PMID:17283058)
• Furin P1A promoter undergoes transactivation via Sox9 binding during chondrogenesis. (PMID:17360815)
• This study provides valuable insights into the structural properties of the furin prodomain in relation to its role in the folding of the furin zymogen and its inhibitory action toward furin. (PMID:17477394)
• Furin may constitute a marker for ovarian tumor progression and could contribute to predict the outcome of this disease. (PMID:17641413)
• HEPC MISSENSE MUTATION CAUSING INEFFICIENT CLEAVAGE INDICATES THAT THE FURIN BINDING SITE BE MORE THAN 4 RESIDUES (PMID:17905608)
• the hepatic prohormone convertase furin mediates the posttranslational processing of hepcidin. The proteolytic cleavage of prohepcidin to hepcidin is not regulated by iron-transferrin or the HIF pathway (PMID:17905609)
• ppFurin expression in breast cancer cells decreased MMP-9 activity, but had no significant effect on TIMP-1 secretion. (PMID:17909005)
• s-HJV originates from a furin cleavage at position 332-335 (PMID:17938254)
• Data suggest that furin levels in cystic fibrosis respiratory epithelial cells contributes to bacterial toxin-induced cell death, fibrosis, and local immunosuppression. (PMID:17948127)
• These data support the hypothesis of a direct binding of heparin with site1 and site2, allowing selective exposure/accessibility of the REKR sequence, which is only then optimally cleaved by furin. (PMID:18037384)
• PC furin is a major IGF-1 receptor convertase. (PMID:18064302)
• The Ca2+-binding capacity of epidermal furin is disrupted by H2O2-mediated oxidation in vitiligo. (PMID:18174282)
• fibrates simultaneously decreased PCSK9 expression while increasing PC5/6A and furin expression, indicating a broad action of PPARalpha activation in proprotein convertase-mediated lipid homeostasis. (PMID:18245819)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	furina	ENSDARG00000062909
danio_rerio	furinb	ENSDARG00000070971
mus_musculus	Furin	ENSMUSG00000030530
rattus_norvegicus	Furin	ENSRNOG00000011352

Paralogs (9): PCSK5 (ENSG00000099139), PCSK4 (ENSG00000115257), PCSK2 (ENSG00000125851), TPP2 (ENSG00000134900), PCSK6 (ENSG00000140479), MBTPS1 (ENSG00000140943), PCSK7 (ENSG00000160613), PCSK9 (ENSG00000169174), PCSK1 (ENSG00000175426)

Protein

Protein identifiers

Furin — P09958 (reviewed: P09958)

Alternative names: Dibasic-processing enzyme, Paired basic amino acid residue-cleaving enzyme

All UniProt accessions (5): A0A7P0T8P1, A0A7P0T8U2, A0A7P0T9X7, P09958, H0YNB5

UniProt curated annotations — full annotation on UniProt →

Function. Ubiquitous endoprotease within constitutive secretory pathways capable of cleavage at the RX(K/R)R consensus motif. Mediates processing of TGFB1, an essential step in TGF-beta-1 activation. Converts through proteolytic cleavage the non-functional Brain natriuretic factor prohormone into its active hormone BNP(1-32). By mediating processing of accessory subunit ATP6AP1/Ac45 of the V-ATPase, regulates the acidification of dense-core secretory granules in islets of Langerhans cells. (Microbial infection) Cleaves and activates diphtheria toxin DT. (Microbial infection) Cleaves and activates anthrax toxin protective antigen (PA). (Microbial infection) Cleaves and activates HIV-1 virus Envelope glycoprotein gp160. (Microbial infection) Required for H7N1 and H5N1 influenza virus infection probably by cleaving hemagglutinin. (Microbial infection) Able to cleave S.pneumoniae serine-rich repeat protein PsrP. (Microbial infection) Facilitates human coronaviruses EMC and SARS-CoV-2 infections by proteolytically cleaving the spike protein at the monobasic S1/S2 cleavage site. This cleavage is essential for spike protein-mediated cell-cell fusion and entry into human lung cells. (Microbial infection) Facilitates mumps virus infection by proteolytically cleaving the viral fusion protein F.

Subunit / interactions. Interacts with FLNA. Binds to PACS1 which mediates TGN localization and connection to clathrin adapters. Interacts with LAMP1, LAMP2 and LAMP3.

Subcellular location. Golgi apparatus. trans-Golgi network membrane. Cell membrane. Secreted. Endosome membrane.

Tissue specificity. Seems to be expressed ubiquitously.

Post-translational modifications. The inhibition peptide, which plays the role of an intramolecular chaperone, is autocatalytically removed in the endoplasmic reticulum (ER) and remains non-covalently bound to furin as a potent autoinhibitor. Following transport to the trans Golgi, a second cleavage within the inhibition propeptide results in propeptide dissociation and furin activation. Phosphorylation is required for TGN localization of the endoprotease. In vivo, exists as di-, mono- and non-phosphorylated forms.

Activity regulation. Inhibited by the not secondly cleaved propeptide. Inhibited by m-guanidinomethyl-phenylacetyl-Arg-Val-Arg-(amidomethyl)-benzamidine (m-guanidinomethyl-Phac-RVR-Amb) and 4-guanidinomethyl-phenylacetyl-Arg-Tle-Arg-4-amidinobenzylamide (MI-1148). Inhibited by Decanoyl-Arg-Val-Lys-Arg-chloromethylketone (decanoyl-RVKR-CMK). Inhibited by heparin/heparan sulfate-binding.

Cofactor. Binds 3 calcium ions per subunit.

Domain organisation. Contains a cytoplasmic domain responsible for its TGN localization and recycling from the cell surface.

Similarity. Belongs to the peptidase S8 family. Furin subfamily.

RefSeq proteins (7): NP_001276752, NP_001276753, NP_001369548, NP_001369549, NP_001369550, NP_001369551, NP_002560* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000209	Peptidase_S8/S53_dom	Domain
IPR002884	P_dom	Domain
IPR006212	Furin_repeat	Repeat
IPR008979	Galactose-bd-like_sf	Homologous_superfamily
IPR009030	Growth_fac_rcpt_cys_sf	Homologous_superfamily
IPR015500	Peptidase_S8_subtilisin-rel	Family
IPR022398	Peptidase_S8_His-AS	Active_site
IPR023827	Peptidase_S8_Asp-AS	Active_site
IPR023828	Peptidase_S8_Ser-AS	Active_site
IPR032815	S8_pro-domain	Domain
IPR034182	Kexin/furin	Domain
IPR036852	Peptidase_S8/S53_dom_sf	Homologous_superfamily
IPR038466	S8_pro-domain_sf	Homologous_superfamily

Pfam: PF00082, PF01483, PF16470

Enzyme classification (BRENDA):

• EC 3.4.21.75 — Furin (BRENDA: 22 organisms, 324 substrates, 368 inhibitors, 122 Km, 111 kcat entries)

Substrate kinetics (BRENDA)

98 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ABZ-GIRRKRSVSHQ-N-(2,4-DINITROPHENYL)ETHYLENEDIA	0.0004	2
ABZ-GRRTRREAIVQ-N-(2,4-DINITROPHENYL)ETHYLENEDIA	0.0002–0.0012	2
ABZ-HHRQRRSVSIQ-N-(2,4-DINITROPHENYL)ETHYLENEDIA	0.0003–0.0032	2
ABZ-HKREKRQAKHQ-N-(2,4-DINITROPHENYL)ETHYLENEDIA	0.0004–0.0027	2
ABZ-HRREKRSVALQ-N-(2,4-DINITROPHENYL)ETHYLENEDIA	0.0002	2
ABZ-HRRQKRSVALQ-N-(2,4-DINITROPHENYL)ETHYLENEDIA	0.0003–0.0004	2
ABZ-KIRRRRDVVDQ-N-(2,4-DINITROPHENYL)ETHYLENEDIA	0.0001	2
ABZ-LKRRRRDTQQQ-N-(2,4-DINITROPHENYL)ETHYLENEDIA	0.0003–0.0052	2
ABZ-NLRRRRDLVDQ-N-(2,4-DINITROPHENYL)ETHYLENEDIA	0.0003–0.0014	2
ABZ-RERRRKKRGLFGQ-N-(2,4-DINITROPHENYL)ETHYLENED	0.0001	2
ABZ-RKRSRRQVNTQ-N-(2,4-DINITROPHENYL)ETHYLENEDIA	0.0002–0.0065	2
ABZ-RRRAKRSPKHQ-N-(2,4-DINITROPHENYL)ETHYLENEDIA	0.0012–0.0122	2
ABZ-RRRDKRSVALQ-N-(2,4-DINITROPHENYL)ETHYLENEDIA	0.0004	2
ABZ-RRRKKRGLFGQ-N-(2,4-DINITROPHENYL)ETHYLENEDIA	0.0155	2
ABZ-RRRKKRGLSGQ-N-(2,4-DINITROPHENYL)ETHYLENEDIA	0.0002	2

UniProt features (116 total): strand 23, binding site 21, helix 20, turn 10, mutagenesis site 6, sequence variant 5, region of interest 4, active site 3, glycosylation site 3, disulfide bond 3, short sequence motif 2, compositionally biased region 2, topological domain 2, site 2, modified residue 2, domain 2, repeat 2, signal peptide 1, propeptide 1, chain 1, transmembrane region 1

Structure

Experimental structures (PDB)

48 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
7LCU	X-RAY DIFFRACTION	1.24
7QY1	X-RAY DIFFRACTION	1.45
7QXY	X-RAY DIFFRACTION	1.48
9QWC	X-RAY DIFFRACTION	1.5
7QY0	X-RAY DIFFRACTION	1.54
7QY2	X-RAY DIFFRACTION	1.55
8B4V	X-RAY DIFFRACTION	1.6
8B4W	X-RAY DIFFRACTION	1.6
8B4X	X-RAY DIFFRACTION	1.6
9QWB	X-RAY DIFFRACTION	1.6
9QWD	X-RAY DIFFRACTION	1.6
9QWE	X-RAY DIFFRACTION	1.6
9QWG	X-RAY DIFFRACTION	1.6
9QWF	X-RAY DIFFRACTION	1.65
6YD4	X-RAY DIFFRACTION	1.7
7O1U	X-RAY DIFFRACTION	1.7
7O1Y	X-RAY DIFFRACTION	1.7
5JXG	X-RAY DIFFRACTION	1.8
6YD2	X-RAY DIFFRACTION	1.8
6YD7	X-RAY DIFFRACTION	1.8
7O1W	X-RAY DIFFRACTION	1.8
7O20	X-RAY DIFFRACTION	1.8
7O22	X-RAY DIFFRACTION	1.8
7QXZ	X-RAY DIFFRACTION	1.8
8OYH	X-RAY DIFFRACTION	1.8
4Z2A	X-RAY DIFFRACTION	1.89
6EQV	X-RAY DIFFRACTION	1.9
5MIM	X-RAY DIFFRACTION	1.9
6HZA	X-RAY DIFFRACTION	1.9
6HZB	X-RAY DIFFRACTION	1.9

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P09958-F1	84.71	0.66

Antibody-complex structures (SAbDab): 1 — 5JMO

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 (5): 153 (charge relay system); 194 (charge relay system); 368 (charge relay system); 75–76 (cleavage, second; by autolysis); 107–108 (cleavage, first; by autolysis)

Ligand- & substrate-binding residues (21): 115; 154; 162; 174; 179; 181; 191–192; 205; 208; 210; 212; 236 …

Post-translational modifications (2): 773, 775

Disulfide bonds (3): 211–360, 303–333, 450–474

Glycosylation sites (3): 387, 440, 553

Mutagenesis-validated functional residues (6):

Position	Phenotype
72	loss of catalytic activity and propeptide second cleavage and removal. abnormal accumulation in the early secretory path
75	loss of catalytic activity and, propeptide second cleavage and removal. normal trafficking to the golgi.
153	loss of catalytic activity and propeptide first cleavage. abnormal accumulation in the early secretory pathway.
773–775	phosphomimetic mutant. localization in early endosome is increased.
773	slight reduction in phosphorylation. loss of phosphorylation and abnormal accumulation in the early secretory pathway; w
775	slight reduction in phosphorylation. loss of phosphorylation and abnormal accumulation in the early secretory pathway; w

Function

Pathways and Gene Ontology

Reactome pathways

25 pathways

ID	Pathway
R-HSA-1181150	Signaling by NODAL
R-HSA-1442490	Collagen degradation
R-HSA-1566948	Elastic fibre formation
R-HSA-1592389	Activation of Matrix Metalloproteinases
R-HSA-159782	Removal of aminoterminal propeptides from gamma-carboxylated proteins
R-HSA-167060	NGF processing
R-HSA-171286	Synthesis and processing of ENV and VPU
R-HSA-186797	Signaling by PDGF
R-HSA-1912420	Pre-NOTCH Processing in Golgi
R-HSA-2173789	TGF-beta receptor signaling activates SMADs
R-HSA-2173796	SMAD2/SMAD3:SMAD4 heterotrimer regulates transcription
R-HSA-5210891	Uptake and function of anthrax toxins
R-HSA-6809371	Formation of the cornified envelope
R-HSA-8963889	Assembly of active LPL and LIPC lipase complexes
R-HSA-9662834	CD163 mediating an anti-inflammatory response
R-HSA-9679191	Potential therapeutics for SARS
R-HSA-9694614	Attachment and Entry
R-HSA-9733458	Induction of Cell-Cell Fusion
R-HSA-9768727	Regulation of CDH1 posttranslational processing and trafficking to plasma membrane
R-HSA-977225	Amyloid fiber formation
R-HSA-9820960	Respiratory syncytial virus (RSV) attachment and entry
R-HSA-9828806	Maturation of hRSV A proteins
R-HSA-9918476	Assembly and Release of Dengue Virus Virions
R-HSA-9918485	Dengue Virus Attachment and Entry
R-HSA-9953170	GBP-mediated host defense

MSigDB gene sets: 0 (showing top):

GO Biological Process (32): blastocyst formation (GO:0001825), negative regulation of inflammatory response to antigenic stimulus (GO:0002862), obsolete signal peptide processing (GO:0006465), transforming growth factor beta receptor signaling pathway (GO:0007179), regulation of signal transduction (GO:0009966), protein processing (GO:0016485), peptide hormone processing (GO:0016486), viral life cycle (GO:0019058), viral protein processing (GO:0019082), extracellular matrix disassembly (GO:0022617), extracellular matrix organization (GO:0030198), collagen catabolic process (GO:0030574), zymogen activation (GO:0031638), regulation of cholesterol transport (GO:0032374), negative regulation of low-density lipoprotein particle receptor catabolic process (GO:0032804), nerve growth factor production (GO:0032902), negative regulation of transforming growth factor beta1 production (GO:0032911), secretion by cell (GO:0032940), plasma lipoprotein particle remodeling (GO:0034369), regulation of protein catabolic process (GO:0042176), cholesterol homeostasis (GO:0042632), peptide biosynthetic process (GO:0043043), positive regulation of viral entry into host cell (GO:0046598), positive regulation of membrane protein ectodomain proteolysis (GO:0051044), protein maturation (GO:0051604), dibasic protein processing (GO:0090472), cytokine precursor processing (GO:0140447), amyloid fibril formation (GO:1990000), proteolysis (GO:0006508), viral translation (GO:0019081), symbiont entry into host cell (GO:0046718), symbiont-mediated induction of syncytium formation (GO:0060141)

GO Molecular Function (15): protease binding (GO:0002020), endopeptidase activity (GO:0004175), serine-type endopeptidase activity (GO:0004252), endopeptidase inhibitor activity (GO:0004866), serine-type endopeptidase inhibitor activity (GO:0004867), heparin binding (GO:0008201), peptidase activity (GO:0008233), serine-type peptidase activity (GO:0008236), peptide binding (GO:0042277), metal ion binding (GO:0046872), nerve growth factor binding (GO:0048406), endopeptidase activator activity (GO:0061133), heparan sulfate binding (GO:1904399), protein binding (GO:0005515), hydrolase activity (GO:0016787)

GO Cellular Component (16): Golgi membrane (GO:0000139), extracellular region (GO:0005576), endoplasmic reticulum (GO:0005783), Golgi lumen (GO:0005796), trans-Golgi network (GO:0005802), plasma membrane (GO:0005886), cell surface (GO:0009986), endosome membrane (GO:0010008), membrane (GO:0016020), trans-Golgi network transport vesicle (GO:0030140), membrane raft (GO:0045121), extracellular exosome (GO:0070062), endosome (GO:0005768), Golgi apparatus (GO:0005794), organelle membrane (GO:0031090), Golgi apparatus subcompartment (GO:0098791)

Reactome top-level categories

Rollup of top-19 pathways:

Category	Pathways
Degradation of the extracellular matrix	2
Developmental Biology	1
Extracellular matrix organization	1
Gamma-carboxylation, transport, and amino-terminal cleavage of proteins	1
Expression and Processing of Neurotrophins	1
Assembly Of The HIV Virion	1
Signaling by Receptor Tyrosine Kinases	1
Pre-NOTCH Expression and Processing	1
Signaling by TGF-beta Receptor Complex	1
Transcriptional activity of SMAD2/SMAD3:SMAD4 heterotrimer	1
Uptake and actions of bacterial toxins	1
Keratinization	1
Plasma lipoprotein remodeling	1
Anti-inflammatory response favouring Leishmania parasite infection	1
SARS-CoV Infections	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
endopeptidase activity	3
Golgi apparatus	3
cellular anatomical structure	3
endomembrane system	3
viral process	2
peptidase activity	2
endopeptidase regulator activity	2
glycosaminoglycan binding	2
sulfur compound binding	2
binding	2
bounding membrane of organelle	2
cytoplasm	2
intracellular membrane-bounded organelle	2
membrane	2
blastocyst development	1
anatomical structure formation involved in morphogenesis	1
inflammatory response to antigenic stimulus	1
regulation of inflammatory response to antigenic stimulus	1
negative regulation of inflammatory response	1
negative regulation of immune response	1
cellular response to transforming growth factor beta stimulus	1
transforming growth factor beta receptor superfamily signaling pathway	1
signal transduction	1
regulation of cell communication	1
regulation of signaling	1
regulation of response to stimulus	1
proteolysis	1
protein maturation	1
hormone metabolic process	1
signaling receptor ligand precursor processing	1
viral gene expression	1
cellular component disassembly	1
extracellular matrix organization	1
extracellular structure organization	1
external encapsulating structure organization	1
catabolic process	1
collagen metabolic process	1
protein processing	1
cholesterol transport	1
regulation of sterol transport	1

Protein interactions and networks

STRING

4322 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
FURIN	PACS1	Q6VY07	947
FURIN	ACE2	Q9BYF1	904
FURIN	TMPRSS2	O15393	898
FURIN	NRP1	O14786	808
FURIN	RSPO4	Q2I0M5	803
FURIN	ACE	P12821	803
FURIN	CTSL	P07711	794
FURIN	ADAMTS1	Q9UHI8	774
FURIN	ADAM17	P78536	767
FURIN	ADAMTS3	O15072	765
FURIN	ADAMTS4	O75173	756
FURIN	TGOLN2	O43493	755
FURIN	ERVW-1	Q9UQF0	754
FURIN	HPX	P02790	746
FURIN	CD4	P01730	745
FURIN	MMP28	Q9H239	745

IntAct

68 interactions, top by confidence:

A	B	Type	Score
FURIN	S	psi-mi:“MI:0570”(protein cleavage)	0.850
FURIN	S	psi-mi:“MI:0194”(cleavage reaction)	0.850
S	FURIN	psi-mi:“MI:0570”(protein cleavage)	0.850
FURIN	MSTN	psi-mi:“MI:0194”(cleavage reaction)	0.620
FURIN	S	psi-mi:“MI:0570”(protein cleavage)	0.620
FURIN	S	psi-mi:“MI:0194”(cleavage reaction)	0.620
MMP28	FURIN	psi-mi:“MI:0915”(physical association)	0.560
MMP14	FURIN	psi-mi:“MI:0915”(physical association)	0.560
MMP28	FURIN	psi-mi:“MI:0403”(colocalization)	0.560
APP	FURIN	psi-mi:“MI:0915”(physical association)	0.560
FURIN	MMP14	psi-mi:“MI:0914”(association)	0.560
FCGRT	GOLIM4	psi-mi:“MI:0914”(association)	0.530
SERPINA5	ZZEF1	psi-mi:“MI:0914”(association)	0.530
PRAMEF5	PRAMEF4	psi-mi:“MI:0914”(association)	0.530
PXYLP1	ADCY9	psi-mi:“MI:0914”(association)	0.500
Gdf11	FURIN	psi-mi:“MI:0407”(direct interaction)	0.440
FURIN	s	psi-mi:“MI:0194”(cleavage reaction)	0.440
	FURIN	psi-mi:“MI:0570”(protein cleavage)	0.440
FURIN	MST1R	psi-mi:“MI:0194”(cleavage reaction)	0.440

BioGRID (319): FURIN (Affinity Capture-MS), FURIN (Affinity Capture-MS), FURIN (Affinity Capture-MS), FURIN (Affinity Capture-MS), FURIN (Affinity Capture-MS), FURIN (Affinity Capture-MS), FURIN (Affinity Capture-MS), FURIN (Affinity Capture-MS), MMP14 (Biochemical Activity), MMP14 (Reconstituted Complex), S (Biochemical Activity), S (Biochemical Activity), S (Biochemical Activity), Flna (Two-hybrid), Flna (Reconstituted Complex)

ESM2 similar proteins: A0A044RE18, B4F6N6, B5DF27, E1C3U7, F1QQC3, G5ECN9, O17798, O35548, O64481, P09231, P09958, P13134, P16519, P21661, P23188, P23377, P28840, P28841, P29119, P29120, P29122, P29145, P29146, P30432, P41413, P51512, P51559, P58022, P63239, P63240, P91863, Q03333, Q04592, Q08B63, Q09175, Q28193, Q5REC2, Q63415, Q8QGP3, Q8SQJ3

Diamond homologs: A0A044RE18, G5ECN9, O13359, O17798, P09231, P09958, P13134, P16519, P21661, P23188, P23377, P26016, P28840, P28841, P29119, P29120, P29121, P29122, P29141, P29145, P29146, P30430, P30432, P41413, P42781, P51559, P63239, P63240, P91863, Q03333, Q04592, Q09175, Q16549, Q28193, Q5REC2, Q61139, Q62849, Q63415, Q6UW60, Q78EH2

SIGNOR signaling

5 interactions.

A	Effect	B	Mechanism
FURIN	up-regulates	NOTCH1	binding
FURIN	“up-regulates activity”	INSR	cleavage
FURIN	“up-regulates activity”	S	cleavage
FURIN	“up-regulates activity”	VWF	cleavage

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 66 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.

GO biological processes:

GO term	Partners	Fold	FDR
transport across blood-brain barrier	5	16.3×	8e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	101
Likely benign	6
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

2853 predictions. Top by Δscore:

Variant	Effect	Δscore
15:90875915:CAGG:C	donor_loss	1.0000
15:90875916:AGGTA:A	donor_loss	1.0000
15:90875918:GT:G	donor_loss	1.0000
15:90876250:TGCAG:T	acceptor_loss	1.0000
15:90876252:CA:C	acceptor_loss	1.0000
15:90876253:A:AG	acceptor_gain	1.0000
15:90876253:A:AT	acceptor_loss	1.0000
15:90876254:G:GT	acceptor_gain	1.0000
15:90876254:GAT:G	acceptor_gain	1.0000
15:90876254:GATC:G	acceptor_gain	1.0000
15:90876344:G:GT	donor_gain	1.0000
15:90876349:CTCAA:C	donor_gain	1.0000
15:90876350:TCAA:T	donor_gain	1.0000
15:90876351:CAA:C	donor_gain	1.0000
15:90876352:AA:A	donor_gain	1.0000
15:90876354:G:C	donor_loss	1.0000
15:90876354:GTGA:G	donor_gain	1.0000
15:90876355:T:A	donor_loss	1.0000
15:90876458:ACAG:A	acceptor_gain	1.0000
15:90876459:C:G	acceptor_gain	1.0000
15:90876460:A:AG	acceptor_gain	1.0000
15:90876460:A:G	acceptor_loss	1.0000
15:90876460:AG:A	acceptor_gain	1.0000
15:90876461:G:GA	acceptor_gain	1.0000
15:90876461:GG:G	acceptor_gain	1.0000
15:90876461:GGT:G	acceptor_gain	1.0000
15:90876461:GGTA:G	acceptor_gain	1.0000
15:90876461:GGTAC:G	acceptor_gain	1.0000
15:90876558:G:GG	donor_gain	1.0000
15:90876559:T:G	donor_loss	1.0000

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000186268 (15:90880498 C>T), RS1000289443 (15:90869987 A>C), RS1000441776 (15:90874538 T>A), RS1000677492 (15:90881233 G>A), RS1000682930 (15:90874673 A>G), RS1000794808 (15:90879352 C>T), RS1000934944 (15:90879141 A>C,G), RS1000985048 (15:90874862 A>C), RS1001438647 (15:90871218 C>A,T), RS1001527817 (15:90877842 G>A), RS1001549606 (15:90883464 T>C), RS1001580580 (15:90883253 C>T), RS1001684392 (15:90875157 C>G), RS1001715458 (15:90875396 C>G,T), RS1001718813 (15:90873604 C>A,T)

Disease associations

OMIM: gene MIM:136950 | disease phenotypes: MIM:613657

GenCC curated gene-disease

Mondo (1): d-2-hydroxyglutaric aciduria 2 (MONDO:0013345)

Orphanet (1): D-2-hydroxyglutaric aciduria (Orphanet:79315)

HPO phenotypes

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

GWAS associations

54 associations (top):

Study	Trait	p-value
GCST001227_15	Systolic blood pressure	5.000000e-19
GCST001228_12	Diastolic blood pressure	2.000000e-15
GCST001238_9	Hypertension	7.000000e-07
GCST002539_79	Schizophrenia	8.000000e-14
GCST003116_43	Coronary artery disease	3.000000e-07
GCST003117_19	Myocardial infarction	2.000000e-07
GCST003272_4	Systolic blood pressure	6.000000e-08
GCST003518_37	Daytime sleep phenotypes	9.000000e-06
GCST004279_42	Systolic blood pressure	1.000000e-09
GCST004521_101	Autism spectrum disorder or schizophrenia	2.000000e-08
GCST004521_95	Autism spectrum disorder or schizophrenia	1.000000e-10
GCST004776_67	Systolic blood pressure	1.000000e-12
GCST004777_54	Diastolic blood pressure	1.000000e-13
GCST004787_62	Coronary artery disease (myocardial infarction, percutaneous transluminal coronary angioplasty, coronary artery bypass grafting, angina or chromic ischemic heart disease)	7.000000e-13
GCST005194_13	Coronary artery disease	2.000000e-25
GCST005195_37	Coronary artery disease	1.000000e-26
GCST005196_14	Coronary artery disease	8.000000e-27
GCST005979_22	Systolic blood pressure	3.000000e-08
GCST006166_89	Diastolic blood pressure x alcohol consumption interaction (2df test)	6.000000e-37
GCST006167_48	Mean arterial pressure x alcohol consumption interaction (2df test)	1.000000e-24
GCST006169_24	Diastolic blood pressure x alcohol consumption (light vs heavy) interaction (2df test)	1.000000e-17
GCST006170_12	Systolic blood pressure x alcohol consumption (light vs heavy) interaction (2df test)	5.000000e-22
GCST006187_42	Diastolic blood pressure (cigarette smoking interaction)	3.000000e-40
GCST006188_46	Systolic blood pressure (cigarette smoking interaction)	6.000000e-45
GCST006231_1	Mean arterial pressure	2.000000e-10
GCST006258_53	Diastolic blood pressure	2.000000e-17
GCST006259_12	Systolic blood pressure	3.000000e-20
GCST006434_68	Systolic blood pressure x alcohol consumption interaction (2df test)	1.000000e-40
GCST006697_20	Parental longevity (combined parental attained age, Martingale residuals)	7.000000e-10
GCST006701_11	Parental longevity (father’s attained age)	1.000000e-07

EFO canonical traits (19, from GWAS)

EFO ID	Trait name
EFO:0006335	systolic blood pressure
EFO:0006336	diastolic blood pressure
EFO:0007828	daytime rest measurement
EFO:0004329	alcohol drinking
EFO:0006340	mean arterial pressure
EFO:0006527	smoking status measurement
EFO:0007796	parental longevity
EFO:0008579	risk-taking behaviour
EFO:0009749	age at first sexual intercourse measurement
EFO:0004344	birth weight
EFO:0005939	parental genotype effect measurement
EFO:0004337	intelligence
EFO:0004784	self reported educational attainment
EFO:0004614	apolipoprotein A 1 measurement
EFO:0004346	neuroimaging measurement
EFO:0009762	healthspan
EFO:0004833	neutrophil count
EFO:0009902	handedness
EFO:0007797	language measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2611 (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: 1,993 (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
CHEMBL35241	DIMINAZENE	2	1,993

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — S8: Subtilisin

Most potent curated ligand interactions (4 total), top 4:

Ligand	Action	Affinity	Parameter
MI-1148	Inhibition	11.26	pKi
phenylacetyl-Arg-Val-Arg-4-amidinobenzylamide	Inhibition	9.1	pKi
peptide 18 [PMID: 24350995]	Inhibition	8.37	pKi
furin inhibitor peptide	Inhibition	7.64	pKi

Binding affinities (BindingDB)

6 measured of 13 human assays (14 total across all organisms); most potent 6 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(2S)-2-acetamido-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoyl-3-fluorophenyl)methylamino]-3-[4-(diaminomethylideneamino)phenyl]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-5-(diaminomethylideneamino)pentanamide	IC50	3.7 nM	US-9266828: Inhibitors of Furin and other pro-protein convertases
(2S)-2-acetamido-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-3-[4-(diaminomethylideneamino)phenyl]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-5-(diaminomethylideneamino)pentanamide	IC50	7 nM	US-9266828: Inhibitors of Furin and other pro-protein convertases
(2S)-2-acetamido-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoyl-2-fluorophenyl)methylamino]-3-[4-(diaminomethylideneamino)phenyl]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-5-(diaminomethylideneamino)pentanamide	IC50	9 nM	US-9266828: Inhibitors of Furin and other pro-protein convertases
(2S)-N-[(4-carbamimidoylphenyl)methyl]-2-[[(2S)-2-[(4-carbamimidoylphenyl)methylsulfonylamino]-3-methylbutanoyl]amino]-5-(diaminomethylideneamino)pentanamide	IC50	300 nM	US-9266828: Inhibitors of Furin and other pro-protein convertases
(2S)-2-acetamido-5-(diaminomethylideneamino)-N-[(2S)-1-[[(2S)-3-[4-(diaminomethylideneamino)phenyl]-1-[[4-[(Z)-N’-hydroxycarbamimidoyl]phenyl]methylamino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]pentanamide	IC50	1200 nM	US-9266828: Inhibitors of Furin and other pro-protein convertases
3-ethyl-2-[(E,3E)-3-(3-ethylthiazolidin-2-ylidene)prop-1-enyl]-2-thiazolin-3-ium;iodide	IC50	31500 nM

ChEMBL bioactivities

544 potent at pChembl≥5 of 560 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	Ki	0.0101	nM	CHEMBL4790628
11.00	Ki	0.0101	nM	CHEMBL5188244
10.88	Ki	0.0131	nM	CHEMBL4794635
10.88	Ki	0.0131	nM	CHEMBL5193701
10.86	Ki	0.0138	nM	CHEMBL5205365
10.80	Ki	0.016	nM	CHEMBL5175269
10.65	Ki	0.0224	nM	CHEMBL5207872
10.65	Ki	0.0223	nM	CHEMBL5202322
10.55	Ki	0.0283	nM	CHEMBL5203853
10.47	Ki	0.0342	nM	CHEMBL4750900
10.47	Ki	0.0337	nM	CHEMBL5176040
10.44	Ki	0.0363	nM	CHEMBL4742184
10.27	Ki	0.0538	nM	CHEMBL5207759
10.11	Ki	0.0768	nM	CHEMBL4779067
9.96	Ki	0.11	nM	CHEMBL5207183
9.94	Ki	0.114	nM	CHEMBL4747919
9.80	IC50	0.1585	nM	CHEMBL5203869
9.80	IC50	0.1585	nM	CHEMBL5197625
9.80	IC50	0.16	nM	CHEMBL5203869
9.77	Ki	0.17	nM	CHEMBL5179893
9.71	Ki	0.196	nM	CHEMBL5191544
9.68	Ki	0.21	nM	CHEMBL5271690
9.60	IC50	0.2512	nM	CHEMBL5175553
9.60	Ki	0.25	nM	CHEMBL5275267
9.60	IC50	0.25	nM	CHEMBL5175553
9.57	Ki	0.27	nM	CHEMBL5276332
9.42	Ki	0.38	nM	CHEMBL5285236
9.40	Ki	0.4	nM	CHEMBL4065072
9.31	Ki	0.491	nM	CHEMBL5202985
9.31	Ki	0.49	nM	CHEMBL5277422
9.30	Ki	0.5	nM	CHEMBL4070237
9.30	Ki	0.5	nM	CHEMBL4091099
9.30	Ki	0.504	nM	CHEMBL5175238
9.30	IC50	0.5012	nM	CHEMBL5190891
9.30	IC50	0.5	nM	CHEMBL5190891
9.25	IC50	0.56	nM	CHEMBL5202322
9.25	IC50	0.56	nM	CHEMBL5184039
9.22	Ki	0.6	nM	CHEMBL4100996
9.21	Ki	0.618	nM	CHEMBL5174341
9.20	IC50	0.631	nM	CHEMBL5175809
9.18	Ki	0.66	nM	CHEMBL566340
9.17	Ki	0.68	nM	CHEMBL5179100
9.15	Ki	0.7	nM	CHEMBL4089819
9.10	Ki	0.8	nM	CHEMBL5199257
9.10	IC50	0.7943	nM	CHEMBL5171461
9.10	IC50	0.7943	nM	CHEMBL5182363
9.10	IC50	0.7943	nM	CHEMBL5208861
9.10	IC50	0.7943	nM	CHEMBL5206910
9.09	Ki	0.81	nM	CHEMBL2049152
9.09	Ki	0.81	nM	CHEMBL566340

PubChem BioAssay actives

545 with measured affinity, of 929 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.

Compound	Assay	Type	Value	Unit
(2S)-2-[[(2S)-2-[[2-[4-(aminomethyl)phenyl]acetyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-3,3-dimethylbutanamide	1895605: Inhibition of furin (unknown origin)	ki	<0.0001	uM
(2S)-2-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-5-(diaminomethylideneamino)pentanamide	1895607: Inhibition of recombinant human furin using Phac-Arg-Val-Arg-Arg-AMC as substrate incubated for 30 mins and measured by microplate reader method	ki	<0.0001	uM
(2S)-6-amino-N-[(4-carbamimidoylphenyl)methyl]-2-[[(2S)-2-[[(2S)-2-[[2-[4-[(diaminomethylideneamino)methyl]phenyl]acetyl]amino]-4-(diaminomethylideneamino)oxybutanoyl]amino]-3,3-dimethylbutanoyl]amino]hexanamide	1694461: Inhibition of recombinant soluble human furin using Phac-Arg-Val-Arg-Arg-AMC fluorogenic substrate	ki	<0.0001	uM
(2S)-2-[[(2S)-2-[[2-[4-(aminomethyl)phenyl]acetyl]amino]-4-(diaminomethylideneamino)oxybutanoyl]amino]-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-4-(diaminomethylideneamino)oxy-1-oxobutan-2-yl]-3,3-dimethylbutanamide	1694461: Inhibition of recombinant soluble human furin using Phac-Arg-Val-Arg-Arg-AMC fluorogenic substrate	ki	<0.0001	uM
(2S)-6-amino-N-[(4-carbamimidoylphenyl)methyl]-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-[4-[(diaminomethylideneamino)methyl]phenyl]acetyl]amino]pentanoyl]amino]-3,3-dimethylbutanoyl]amino]hexanamide	1694461: Inhibition of recombinant soluble human furin using Phac-Arg-Val-Arg-Arg-AMC fluorogenic substrate	ki	<0.0001	uM
(2S)-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-4-(diaminomethylideneamino)oxy-1-oxobutan-2-yl]-2-[[(2S)-2-[[2-[4-[(diaminomethylideneamino)methyl]phenyl]acetyl]amino]-4-(diaminomethylideneamino)oxybutanoyl]amino]-3,3-dimethylbutanamide	1694461: Inhibition of recombinant soluble human furin using Phac-Arg-Val-Arg-Arg-AMC fluorogenic substrate	ki	<0.0001	uM
(2S)-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-4-(diaminomethylideneamino)oxy-1-oxobutan-2-yl]-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-[4-[(diaminomethylideneamino)methyl]phenyl]acetyl]amino]pentanoyl]amino]-3,3-dimethylbutanamide	1694461: Inhibition of recombinant soluble human furin using Phac-Arg-Val-Arg-Arg-AMC fluorogenic substrate	ki	<0.0001	uM
(2S)-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)oxy-1-oxopentan-2-yl]-2-[[(2S)-2-[[2-[4-[(diaminomethylideneamino)methyl]phenyl]acetyl]amino]-5-(diaminomethylideneamino)oxypentanoyl]amino]-3,3-dimethylbutanamide	1895607: Inhibition of recombinant human furin using Phac-Arg-Val-Arg-Arg-AMC as substrate incubated for 30 mins and measured by microplate reader method	ki	<0.0001	uM
(2S)-2-[[(2S)-2-[[(2S)-2,5-bis(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-5-(diaminomethylideneamino)pentanamide	1895607: Inhibition of recombinant human furin using Phac-Arg-Val-Arg-Arg-AMC as substrate incubated for 30 mins and measured by microplate reader method	ki	<0.0001	uM
(2S)-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)oxy-1-oxopentan-2-yl]-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-[4-[(diaminomethylideneamino)methyl]phenyl]acetyl]amino]pentanoyl]amino]-3,3-dimethylbutanamide	1895607: Inhibition of recombinant human furin using Phac-Arg-Val-Arg-Arg-AMC as substrate incubated for 30 mins and measured by microplate reader method	ki	<0.0001	uM
(2S)-N-[(2S)-1-[(4-carbamimidoyl-3-fluorophenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-[4-[(diaminomethylideneamino)methyl]phenyl]acetyl]amino]pentanoyl]amino]-3,3-dimethylbutanamide	1895605: Inhibition of furin (unknown origin)	ki	<0.0001	uM
(2S)-N-[(2S)-5-amino-1-[(4-carbamimidoylphenyl)methylamino]-1-oxopentan-2-yl]-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-[4-[(diaminomethylideneamino)methyl]phenyl]acetyl]amino]pentanoyl]amino]-3,3-dimethylbutanamide	1895605: Inhibition of furin (unknown origin)	ki	<0.0001	uM
(2R)-2-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-5-(diaminomethylideneamino)pentanamide	1895607: Inhibition of recombinant human furin using Phac-Arg-Val-Arg-Arg-AMC as substrate incubated for 30 mins and measured by microplate reader method	ki	<0.0001	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide	1895607: Inhibition of recombinant human furin using Phac-Arg-Val-Arg-Arg-AMC as substrate incubated for 30 mins and measured by microplate reader method	ki	<0.0001	uM
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-5-(diaminomethylideneamino)-2-[[2-[4-[(diaminomethylideneamino)methyl]phenyl]acetyl]amino]pentanamide	1895604: Inhibition of human furin expressed in HEK293 cells using pGlu-Arg-Thr-LysArg-AMC as substrate and measured by fluorescence based assay	ki	<0.0001	uM
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-5-(diaminomethylideneamino)-2-[[2-[3-[(diaminomethylideneamino)methyl]phenyl]acetyl]amino]pentanamide	1895604: Inhibition of human furin expressed in HEK293 cells using pGlu-Arg-Thr-LysArg-AMC as substrate and measured by fluorescence based assay	ki	<0.0001	uM
(2S)-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-[4-[(diaminomethylideneamino)methyl]phenyl]acetyl]amino]pentanoyl]amino]-3,3-dimethylbutanamide	1694461: Inhibition of recombinant soluble human furin using Phac-Arg-Val-Arg-Arg-AMC fluorogenic substrate	ki	<0.0001	uM
(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[2-[4-(aminomethyl)phenyl]acetyl]amino]-4-(diaminomethylideneamino)oxybutanoyl]amino]-3,3-dimethylbutanoyl]amino]-N-[(4-carbamimidoylphenyl)methyl]hexanamide	1694461: Inhibition of recombinant soluble human furin using Phac-Arg-Val-Arg-Arg-AMC fluorogenic substrate	ki	0.0001	uM
(2S)-2-[[(2S)-2-[[2-[4-(aminomethyl)phenyl]acetyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-4-(diaminomethylideneamino)oxy-1-oxobutan-2-yl]-3,3-dimethylbutanamide	1694461: Inhibition of recombinant soluble human furin using Phac-Arg-Val-Arg-Arg-AMC fluorogenic substrate	ki	0.0001	uM
(3S,6S,9S,12S,15S,18S,29S)-18-benzyl-N-[(2S)-5-carbamimidamido-1-[(4-carbamimidoylphenyl)methylamino]-1-oxopentan-2-yl]-3,6,9,12-tetrakis(3-carbamimidamidopropyl)-15-(naphthalen-2-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,24-octazacyclononacosane-29-carboxamide	1895605: Inhibition of furin (unknown origin)	ki	0.0001	uM
(2S)-2-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-5-(diaminomethylideneamino)pentanamide	1895605: Inhibition of furin (unknown origin)	ki	0.0001	uM
3-[4-[5-[[4-[[4-(acetamidomethyl)piperidin-1-yl]methyl]-6-(3,5-dichlorophenyl)-2-pyridinyl]oxy]pyrimidin-2-yl]piperazin-1-yl]propanoic acid	1895622: Inhibition of Tev-FLAG-His-tagged furin (108 to 574 residues) (unknown origin) using FAM-QRVRRAVGIDK-TAMRA as substrate and measured after 2 hrs	ic50	0.0002	uM
3-[4-[5-[[6-(3,5-dichlorophenyl)-4-[[4-[(methoxycarbonylamino)methyl]piperidin-1-yl]methyl]-2-pyridinyl]oxy]pyrimidin-2-yl]piperazin-1-yl]propanoic acid	1895622: Inhibition of Tev-FLAG-His-tagged furin (108 to 574 residues) (unknown origin) using FAM-QRVRRAVGIDK-TAMRA as substrate and measured after 2 hrs	ic50	0.0002	uM
(2S)-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanoyl]amino]-3,3-dimethylbutanamide	1895604: Inhibition of human furin expressed in HEK293 cells using pGlu-Arg-Thr-LysArg-AMC as substrate and measured by fluorescence based assay	ki	0.0002	uM
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-5-(diaminomethylideneamino)-2-[[2-[2-[(diaminomethylideneamino)methyl]phenyl]acetyl]amino]pentanamide	1895604: Inhibition of human furin expressed in HEK293 cells using pGlu-Arg-Thr-LysArg-AMC as substrate and measured by fluorescence based assay	ki	0.0002	uM
2-[3-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,37S,40S,43S)-25,28,40-tris(4-aminobutyl)-43-benzyl-4,19-bis[(2S)-butan-2-yl]-34-[3-(diaminomethylideneamino)propyl]-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,36,39,42,45-tridecaoxo-47,48-dithia-2,5,11,17,20,23,26,29,32,35,38,41,44-tridecazatetracyclo[29.14.4.07,11.013,17]nonatetracontan-37-yl]propyl]guanidine	1952707: Inhibition of recombinant human furin assessed as inhibition constant using Pyr-Arg-Thr-Lys-Arg-AMC as substrate preincubated for 30 mins followed by substrate addition and measured for 40 mins by Cheng-Prusoff equation analysis	ki	0.0002	uM
3-[4-[5-[[4-[[4-(acetamidomethyl)piperidin-1-yl]methyl]-6-(3,5-dichlorophenyl)-2-pyridinyl]oxy]-2-pyridinyl]piperazin-1-yl]propanoic acid	1895622: Inhibition of Tev-FLAG-His-tagged furin (108 to 574 residues) (unknown origin) using FAM-QRVRRAVGIDK-TAMRA as substrate and measured after 2 hrs	ic50	0.0003	uM
(3S,9S,12S,15S,18S,21R,26R,29S,32S)-15,18-bis(4-aminobutyl)-21-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-9,29-bis[(2S)-butan-2-yl]-12-(hydroxymethyl)-2,8,11,14,17,20,28,31-octaoxo-23,24-dithia-1,7,10,13,16,19,27,30-octazatricyclo[30.3.0.03,7]pentatriacontane-26-carboxamide	1952707: Inhibition of recombinant human furin assessed as inhibition constant using Pyr-Arg-Thr-Lys-Arg-AMC as substrate preincubated for 30 mins followed by substrate addition and measured for 40 mins by Cheng-Prusoff equation analysis	ki	0.0003	uM
2-[3-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,37S,40S,43S)-25,28-bis(4-aminobutyl)-43-benzyl-4,19-bis[(2S)-butan-2-yl]-34,37-bis[3-(diaminomethylideneamino)propyl]-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,36,39,42,45-tridecaoxo-47,48-dithia-2,5,11,17,20,23,26,29,32,35,38,41,44-tridecazatetracyclo[29.14.4.07,11.013,17]nonatetracontan-40-yl]propyl]guanidine	1952707: Inhibition of recombinant human furin assessed as inhibition constant using Pyr-Arg-Thr-Lys-Arg-AMC as substrate preincubated for 30 mins followed by substrate addition and measured for 40 mins by Cheng-Prusoff equation analysis	ki	0.0003	uM
(2S)-2-acetamido-6-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[(4-carbamimidoylphenyl)methylamino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]hexanamide	1481482: Inhibition of recombinant human furin expressed in drosophila S2 cells using pyrGlu-Arg-Thr-Lys-Arg-7-amido-4-methylcoumarin as substrate after 60 mins by spectrofluorometry method	ki	0.0004	uM
(3S,9S,12S,15S,18S,21R,26R,29S,32S)-15,18-bis(4-aminobutyl)-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-9,29-bis[(2S)-butan-2-yl]-21-[[(2S)-2-[[(2S)-2,6-diaminohexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-12-(hydroxymethyl)-2,8,11,14,17,20,28,31-octaoxo-23,24-dithia-1,7,10,13,16,19,27,30-octazatricyclo[30.3.0.03,7]pentatriacontane-26-carboxamide	1952707: Inhibition of recombinant human furin assessed as inhibition constant using Pyr-Arg-Thr-Lys-Arg-AMC as substrate preincubated for 30 mins followed by substrate addition and measured for 40 mins by Cheng-Prusoff equation analysis	ki	0.0004	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylbutanoyl]amino]-6-amino-N-[(4-carbamimidoylphenyl)methyl]hexanamide	1481482: Inhibition of recombinant human furin expressed in drosophila S2 cells using pyrGlu-Arg-Thr-Lys-Arg-7-amido-4-methylcoumarin as substrate after 60 mins by spectrofluorometry method	ki	0.0005	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylbutanoyl]amino]-6-amino-N-[(4-carbamimidoylphenyl)methyl]hexanamide	1481482: Inhibition of recombinant human furin expressed in drosophila S2 cells using pyrGlu-Arg-Thr-Lys-Arg-7-amido-4-methylcoumarin as substrate after 60 mins by spectrofluorometry method	ki	0.0005	uM
4-[4-[5-[[4-[[4-(acetamidomethyl)piperidin-1-yl]methyl]-6-(3,5-dichlorophenyl)-2-pyridinyl]oxy]pyrimidin-2-yl]piperazin-1-yl]-2-methylbutanoic acid	1895622: Inhibition of Tev-FLAG-His-tagged furin (108 to 574 residues) (unknown origin) using FAM-QRVRRAVGIDK-TAMRA as substrate and measured after 2 hrs	ic50	0.0005	uM
(2S,5S,8S)-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2,5-bis[3-(diaminomethylideneamino)propyl]-3,6,14,18-tetraoxo-1,4,7,13-tetrazacyclooctadecane-8-carboxamide	1895605: Inhibition of furin (unknown origin)	ki	0.0005	uM
(10S,13S,16S,19S,22S)-22-amino-13-tert-butyl-N-[(4-carbamimidoylphenyl)methyl]-16-[3-(diaminomethylamino)propyl]-19-[3-(diaminomethylideneamino)propyl]-4,12,15,18,21,28-hexaoxo-1,5,11,14,17,20,27,31-octazabicyclo[29.2.2]pentatriacontane-10-carboxamide	1895605: Inhibition of furin (unknown origin)	ki	0.0005	uM
(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,43S,46S,52S)-39-amino-25-(4-aminobutyl)-52-benzyl-4,19-bis[(2S)-butan-2-yl]-34-carbamoyl-28-[(1S)-1-hydroxyethyl]-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,41,45,51,54-tridecaoxo-56,57-dithia-2,5,11,17,20,23,26,29,32,38,40,44,50,53-tetradecazapentacyclo[29.23.4.07,11.013,17.046,50]octapentacont-38-ene-43-carboxylic acid	1952707: Inhibition of recombinant human furin assessed as inhibition constant using Pyr-Arg-Thr-Lys-Arg-AMC as substrate preincubated for 30 mins followed by substrate addition and measured for 40 mins by Cheng-Prusoff equation analysis	ki	0.0005	uM
(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-6-amino-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[(4-carbamimidoylphenyl)methylamino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]hexanamide	1481482: Inhibition of recombinant human furin expressed in drosophila S2 cells using pyrGlu-Arg-Thr-Lys-Arg-7-amido-4-methylcoumarin as substrate after 60 mins by spectrofluorometry method	ki	0.0006	uM
2-[1-[[2-(3,5-dichlorophenyl)-6-[2-[4-[(2R)-2-hydroxypropyl]piperazin-1-yl]pyrimidin-5-yl]oxy-4-pyridinyl]methyl]piperidin-4-yl]acetic acid	1895622: Inhibition of Tev-FLAG-His-tagged furin (108 to 574 residues) (unknown origin) using FAM-QRVRRAVGIDK-TAMRA as substrate and measured after 2 hrs	ic50	0.0006	uM
(3S,6S,9S,12S,15S,26S)-N-[(2S)-6-amino-1-[(4-carbamimidoylphenyl)methylamino]-1-oxohexan-2-yl]-15-benzyl-3,6,9-tris[3-(diaminomethylideneamino)propyl]-12-(naphthalen-2-ylmethyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,21-heptazacyclohexacosane-26-carboxamide	1895605: Inhibition of furin (unknown origin)	ki	0.0006	uM
(2S)-N-[(2S)-1-(benzylamino)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-[4-[(diaminomethylideneamino)methyl]phenyl]acetyl]amino]pentanoyl]amino]-3,3-dimethylbutanamide	1895605: Inhibition of furin (unknown origin)	ic50	0.0006	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylbutanoyl]amino]-6-amino-N-[(4-carbamimidoylphenyl)methyl]hexanamide	1481482: Inhibition of recombinant human furin expressed in drosophila S2 cells using pyrGlu-Arg-Thr-Lys-Arg-7-amido-4-methylcoumarin as substrate after 60 mins by spectrofluorometry method	ki	0.0007	uM
(2S,5S,8S,11S)-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2,5,8-tris[3-(diaminomethylideneamino)propyl]-3,6,9,17,21-pentaoxo-1,4,7,10,16-pentazacyclohenicosane-11-carboxamide	1895605: Inhibition of furin (unknown origin)	ki	0.0007	uM
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide	1895604: Inhibition of human furin expressed in HEK293 cells using pGlu-Arg-Thr-LysArg-AMC as substrate and measured by fluorescence based assay	ki	0.0007	uM
3-[1-[[2-(3,5-dichlorophenyl)-6-[2-(4-methylpiperazin-1-yl)pyrimidin-5-yl]oxy-4-pyridinyl]methyl]piperidin-4-yl]-2-methylpropanoic acid	1895622: Inhibition of Tev-FLAG-His-tagged furin (108 to 574 residues) (unknown origin) using FAM-QRVRRAVGIDK-TAMRA as substrate and measured after 2 hrs	ic50	0.0008	uM
3-[4-[5-[[6-(3,5-dichlorophenyl)-4-[[4-[(methylcarbamoylamino)methyl]piperidin-1-yl]methyl]-2-pyridinyl]oxy]-2-pyridinyl]piperazin-1-yl]propanoic acid	1895622: Inhibition of Tev-FLAG-His-tagged furin (108 to 574 residues) (unknown origin) using FAM-QRVRRAVGIDK-TAMRA as substrate and measured after 2 hrs	ic50	0.0008	uM
N-[[1-[[2-(3,5-dichlorophenyl)-6-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-3-pyridinyl]oxy]-4-pyridinyl]methyl]piperidin-4-yl]methyl]acetamide	1895622: Inhibition of Tev-FLAG-His-tagged furin (108 to 574 residues) (unknown origin) using FAM-QRVRRAVGIDK-TAMRA as substrate and measured after 2 hrs	ic50	0.0008	uM
2-[1-[[2-(3,5-dichlorophenyl)-6-[2-(4-methylpiperazin-1-yl)pyrimidin-5-yl]oxy-4-pyridinyl]methyl]piperidin-4-yl]acetic acid	1895622: Inhibition of Tev-FLAG-His-tagged furin (108 to 574 residues) (unknown origin) using FAM-QRVRRAVGIDK-TAMRA as substrate and measured after 2 hrs	ic50	0.0008	uM
(2S)-N-[(2S)-1-[(6-amino-3-pyridinyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-[4-[(diaminomethylideneamino)methyl]phenyl]acetyl]amino]pentanoyl]amino]-3,3-dimethylbutanamide	1895605: Inhibition of furin (unknown origin)	ki	0.0008	uM
(2S,3S)-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanoyl]amino]-3-methylpentanamide	609914: Inhibition of recombinant human furin expressed in CHO cells using pyroGlu- Arg-Thr-Lys-Arg-AMC as the substrate after 30 mins	ki	0.0008	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	increases expression	3
Air Pollutants	increases abundance, increases expression	2
Arsenic	affects methylation, decreases expression, increases abundance	2
Benzo(a)pyrene	affects methylation, decreases expression	2
Cyclosporine	decreases expression, increases expression	2
Particulate Matter	increases abundance, increases expression	2
FR900359	increases phosphorylation	1
moringin	increases expression	1
dicrotophos	increases expression	1
diminazene aceturate	decreases expression	1
triphenyl phosphate	affects expression	1
2,2’-methylenebis(4-methyl-6-tert-butylphenol)	affects expression, affects response to substance	1
tris(1,3-dichloro-2-propyl)phosphate	increases expression	1
cobaltous chloride	decreases expression	1
butyraldehyde	decreases expression	1
nickel chloride	decreases expression	1
rutecarpine	decreases expression	1
cupric chloride	increases expression	1
benazol P	affects expression	1
testosterone-3-carboxymethyloxime-bovine serum albumin conjugate	affects expression	1
arsenic trichloride	increases abundance, decreases expression	1
9-chloro-2-(2-furyl)-(1,2,4)triazolo(1,5-c)quinazolin-5-imine	decreases expression	1
cordycepin	decreases expression	1
2,3-dimethoxy-1,4-naphthoquinone	decreases expression	1
batimastat	decreases activity	1
kenpaullone	decreases expression	1
ICG 001	decreases expression	1
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acid	decreases expression	1
Acetaminophen	increases expression	1
Apomorphine	decreases expression	1

ChEMBL screening assays

62 unique, capped per target: 62 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1008221	Binding	Inhibition of human recombinant furin assessed as fluorescent Pyr-RTKR-AMC substrate cleavage	Targeting host cell furin proprotein convertases as a therapeutic strategy against bacterial toxins and viral pathogens. — J Biol Chem

Cellosaurus cell lines

9 cell lines: 5 transformed cell line, 3 cancer cell line, 1 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_C7NL	Vero-furin	Spontaneously immortalized cell line	Female
CVCL_D4C5	HEK293 FRT FURIN KO	Transformed cell line	Female
CVCL_E0DE	Ubigene HeLa FURIN KO	Cancer cell line	Female
CVCL_E3KX	CHOEBNALT85-furin	Transformed cell line	Female
CVCL_E4IG	EMC-G5 G5P.7A 3C9	Transformed cell line	Female
CVCL_E4JT	CHO FIX.1F	Transformed cell line	Female
CVCL_F1PD	HyCyte HEK293-FT KO-hFURIN	Transformed cell line	Female
CVCL_SP02	HAP1 FURIN (-) 1	Cancer cell line	Male
CVCL_SP03	HAP1 FURIN (-) 2	Cancer cell line	Male

Clinical trials (associated diseases)

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