FN3K

Summary

FN3K (fructosamine 3 kinase, HGNC:24822) is a protein-coding gene on chromosome 17q25.3, encoding Fructosamine-3-kinase (Q9H479). Fructosamine-3-kinase involved in protein deglycation by mediating phosphorylation of fructoselysine residues on glycated proteins, to generate fructoselysine-3 phosphate.

A high concentration of glucose can result in non-enzymatic oxidation of proteins by reaction of glucose and lysine residues (glycation). Proteins modified in this way, fructosamines, are less active or functional. This gene encodes an enzyme which catalyzes the phosphorylation of fructosamines which may result in deglycation.

Source: NCBI Gene 64122 — RefSeq curated summary.

At a glance

• GWAS associations: 11
• Clinical variants (ClinVar): 70 total
• Druggable target: yes
• MANE Select transcript: NM_022158

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:24822
Approved symbol	FN3K
Name	fructosamine 3 kinase
Location	17q25.3
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000167363
Ensembl biotype	protein_coding
OMIM	608425
Entrez	64122

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 4 protein_coding, 3 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000300784, ENST00000570734, ENST00000572813, ENST00000573841, ENST00000574496, ENST00000910353, ENST00000910354, ENST00000910355

RefSeq mRNA: 1 — MANE Select: NM_022158 NM_022158

CCDS: CCDS11818

Canonical transcript exons

ENST00000300784 — 6 exons

Exon	Start	End
ENSE00001112260	82748855	82748977
ENSE00001154990	82735615	82735777
ENSE00001302268	82750417	82751196
ENSE00003516759	82740763	82740854
ENSE00003632419	82741311	82741393
ENSE00003642444	82738489	82738640

Expression profiles

Bgee: expression breadth ubiquitous, 167 present calls, max score 97.92.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 26.4941 / max 493.4396, expressed in 1608 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
163536	24.8392	1589
163535	0.9215	440
163534	0.5692	324
208470	0.1642	67

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
sural nerve	UBERON:0015488	97.92	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	95.89	gold quality
left adrenal gland cortex	UBERON:0035825	95.42	gold quality
right adrenal gland cortex	UBERON:0035827	95.41	gold quality
right adrenal gland	UBERON:0001233	95.00	gold quality
left adrenal gland	UBERON:0001234	94.96	gold quality
anterior cingulate cortex	UBERON:0009835	94.63	gold quality
cingulate cortex	UBERON:0003027	94.45	gold quality
right hemisphere of cerebellum	UBERON:0014890	94.43	gold quality
right frontal lobe	UBERON:0002810	94.30	gold quality
apex of heart	UBERON:0002098	94.21	gold quality
cerebellar hemisphere	UBERON:0002245	94.06	gold quality
cerebellar cortex	UBERON:0002129	93.93	gold quality
prefrontal cortex	UBERON:0000451	93.68	gold quality
right atrium auricular region	UBERON:0006631	93.62	gold quality
right lobe of liver	UBERON:0001114	93.26	gold quality
adenohypophysis	UBERON:0002196	92.69	gold quality
hindlimb stylopod muscle	UBERON:0004252	92.63	gold quality
Brodmann (1909) area 9	UBERON:0013540	92.13	gold quality
adrenal gland	UBERON:0002369	91.91	gold quality
left ovary	UBERON:0002119	91.72	gold quality
adrenal cortex	UBERON:0001235	91.60	gold quality
metanephros cortex	UBERON:0010533	91.42	gold quality
cortical plate	UBERON:0005343	91.05	gold quality
mucosa of transverse colon	UBERON:0004991	90.99	gold quality
right ovary	UBERON:0002118	90.97	gold quality
heart left ventricle	UBERON:0002084	90.55	gold quality
body of stomach	UBERON:0001161	90.34	gold quality
spinal cord	UBERON:0002240	90.33	gold quality
nucleus accumbens	UBERON:0001882	90.20	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 2.

Experiment	Marker?	Max mean expression
E-CURD-122	yes	19.63
E-ANND-3	yes	4.09
E-MTAB-7249	no	4.04

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

15 targeting FN3K, 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-6798-5P	100.00	65.77	699
HSA-MIR-4534	99.99	66.58	1907
HSA-MIR-8082	99.95	67.27	1170
HSA-MIR-6794-5P	99.76	66.38	1048
HSA-MIR-149-3P	99.72	68.22	3963
HSA-MIR-4716-3P	99.69	66.73	1022
HSA-MIR-3191-3P	99.45	63.94	356
HSA-MIR-92B-5P	99.36	63.29	110
HSA-MIR-6887-5P	98.56	68.49	1295
HSA-MIR-6795-5P	98.52	68.51	1277
HSA-MIR-211-3P	98.14	66.77	1052
HSA-MIR-139-3P	95.24	63.10	316
HSA-MIR-483-5P	93.53	65.81	111
HSA-MIR-6889-5P	90.26	64.13	291
HSA-MIR-6777-5P	88.76	62.64	222

Literature-anchored findings (GeneRIF, showing 17)

• involved in the removal of fructosamine residues from hemoglobin in erythrocytes. (PMID:11975663)
• The aim of this work was to identify the fructosamine residues on hemoglobin that are removed as a result of the action of FN3K in intact erythrocytes. (PMID:15102834)
• These data suggest that FN3K and FN3KRP act as protein repair enzymes and are expressed constitutively in human cells independently of some of the variables altered in the diabetic state. (PMID:15381090)
• Enzyme is a constitutive “housekeeping” gene and that ig plays an important role in cell metabolism, possibly as a deglycating enzyme. (PMID:16037310)
• No significant correlation between FN3K activity and the levels of HbA1c, total glycated haemoglobin (GHb) and haemoglobin fructoselysine residues, either in the normoglycaemic or diabetic group. (PMID:16523184)
• In this paper we propose a resolution of both these quandaries by proposing that fructosamine-6-phosphates are deglycated by phosphorylation to fructosamine-3,6-bisphosphates catalyzed by FN3KRP and/or possibly FN3K. (PMID:16920277)
• G900C polymorphism associates with the level of HbA (1c) and the onset of type 2 diabetes mellitus, but not with either of the diabetic microvascular complications. (PMID:19834870)
• These findings suggest that deglycating enzymes Glyoxalase I and fructosamine-3-kinase may be involved in the malignant transformation of colon mucosa. (PMID:21253391)
• two new mutations and additional variants within the FN3K gene in diabetic patients (PMID:21288167)
• The marginal association of rs1056534 of FN3K is located in exon 6 with diabetic nephropathy progression. (PMID:23492569)
• Report association of rs1056534 and rs3848403 of fructosamine 3-kinase gene with sRAGE in patients with diabetes. (PMID:24908234)
• FN3K could act in concert with other molecular mechanisms and may impact on gene expression and activity of other enzymes involved in deglycation process (PMID:26352355)
• In a multiple regression analysis, FN3K rs1056534, TF polymorphism and presence of diabetes mellitus were predictors for HHV-8 infection. (PMID:27461879)
• FN3K is a targetable modulator of NRF2 activity in cancer. (PMID:31398338)
• A redox-active switch in fructosamine-3-kinases expands the regulatory repertoire of the protein kinase superfamily. (PMID:32636308)
• FN3K expression in COPD: a potential comorbidity factor for cardiovascular disease. (PMID:33208304)
• Structural basis for FN3K-mediated protein deglycation. (PMID:39173621)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
mus_musculus	Fn3k	ENSMUSG00000025175
rattus_norvegicus	Fn3k	ENSRNOG00000036659
caenorhabditis_elegans		WBGENE00013802

Paralogs (1): FN3KRP (ENSG00000141560)

Protein

Protein identifiers

Fructosamine-3-kinase — Q9H479 (reviewed: Q9H479)

Alternative names: Protein-psicosamine 3-kinase FN3K, Protein-ribulosamine 3-kinase FN3K

All UniProt accessions (1): Q9H479

UniProt curated annotations — full annotation on UniProt →

Function. Fructosamine-3-kinase involved in protein deglycation by mediating phosphorylation of fructoselysine residues on glycated proteins, to generate fructoselysine-3 phosphate. Fructoselysine-3 phosphate adducts are unstable and decompose under physiological conditions. Involved in intracellular deglycation in erythrocytes. Involved in the response to oxidative stress by mediating deglycation of NFE2L2/NRF2, glycation impairing NFE2L2/NRF2 function. Also able to phosphorylate psicosamines and ribulosamines.

Subunit / interactions. Monomer.

Tissue specificity. Widely expressed. Expressed in erythrocytes.

Similarity. Belongs to the fructosamine kinase family.

RefSeq proteins (1): NP_071441* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR016477	Fructo-/Ketosamine-3-kinase	Family

Pfam: PF03881

Enzyme classification (BRENDA):

• EC 2.7.1.171 — protein-fructosamine 3-kinase (BRENDA: 6 organisms, 38 substrates, 9 inhibitors, 23 Km, 0 kcat entries)

Substrate kinetics (BRENDA)

14 substrates with measured Km, best-characterized 14. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
1-DEOXY-1-MORPHOLIN-4-YL-D-FRUCTOSE	0.001–0.1	5
N2-(1-DEOXY-D-FRUCTOSYL)-GLYCINE	0.001–0.0022	3
N6-(1-DEOXY-D-FRUCTOSYL)-LYSINE	0.0072–0.0132	3
(R)-1-(5-(3-AMINO-4-HYDROXY-3-METHYLBUTYL)-1-MET	0.922	1
1-DEOXY-1-MORPHOLIN-4-YL-D-PSICOSE	0.16	1
1-DEOXY-1-MORPHOLIN-4-YL-D-RIBULOSE	0.0026	1
D-FRUCTOSE	50	1
N2-(1-DEOXY-D-FRUCTOSYL)-GLYCYLGLYCINE	1.5	1
N2-(1-DEOXY-D-FRUCTOSYL)-L-VALINE	0.8	1
N5-D-FRUCTOSYL-L-ORNITHINE	0.5	1
N6-(1-DEOXY-D-FRUCTOSYL)-L-LYSINE	0.0072	1
N6-D-FRUCTOSYL-L-LYSINE	0.75	1
N6-D-PSICOSYL-L-LYSINE	0.14	1
[PROTEIN]-N6-D-FRUCTOSYL-L-LYSINE	0.01	1

Catalyzed reactions (Rhea), 3 shown:

• N(6)-D-ribulosyl-L-lysyl-[protein] + ATP = N(6)-(3-O-phospho-D-ribulosyl)-L-lysyl-[protein] + ADP + H(+) (RHEA:48432)
• N(6)-(D-fructosyl)-L-lysyl-[protein] + ATP = N(6)-(3-O-phospho-D-fructosyl)-L-lysyl-[protein] + ADP + H(+) (RHEA:59832)
• N(6)-(D-psicosyl)-L-lysyl-[protein] + ATP = N(6)-(3-O-phospho-D-psicosyl)-L-lysyl-[protein] + ADP + H(+) (RHEA:61392)

UniProt features (35 total): strand 15, helix 14, turn 2, chain 1, active site 1, binding site 1, modified residue 1

Structure

Experimental structures (PDB)

7 structures.

PDB	Method	Resolution (Å)
9CX8	X-RAY DIFFRACTION	1.67
9CXM	X-RAY DIFFRACTION	1.76
9CXV	X-RAY DIFFRACTION	1.8
9CXW	X-RAY DIFFRACTION	1.8
9CXN	X-RAY DIFFRACTION	1.9
9CXO	X-RAY DIFFRACTION	2.32
8UE1	X-RAY DIFFRACTION	2.85

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9H479-F1	94.76	0.91

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 (1): 217 (proton acceptor)

Ligand- & substrate-binding residues (1): 89–91

Post-translational modifications (1): 1

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

ID	Pathway
R-HSA-163841	Gamma carboxylation, hypusinylation, hydroxylation, and arylsulfatase activation

MSigDB gene sets: 64 (showing top): GOBP_EPITHELIUM_DEVELOPMENT, STARK_PREFRONTAL_CORTEX_22Q11_DELETION_DN, IVANOVA_HEMATOPOIESIS_MATURE_CELL, GOBP_CARBOHYDRATE_DERIVATIVE_METABOLIC_PROCESS, GOBP_POST_TRANSLATIONAL_PROTEIN_MODIFICATION, GOBP_AMINO_SUGAR_METABOLIC_PROCESS, GOBP_ORGANIC_ACID_METABOLIC_PROCESS, AFFAR_YY1_TARGETS_DN, NIKOLSKY_BREAST_CANCER_17Q21_Q25_AMPLICON, GOMF_KINASE_ACTIVITY, GOMF_ADENYL_NUCLEOTIDE_BINDING, CHEN_METABOLIC_SYNDROM_NETWORK, GOMF_TRANSFERASE_ACTIVITY_TRANSFERRING_PHOSPHORUS_CONTAINING_GROUPS, REACTOME_POST_TRANSLATIONAL_PROTEIN_MODIFICATION, MIKKELSEN_ES_ICP_WITH_H3K4ME3

GO Biological Process (5): fructosamine metabolic process (GO:0030389), fructoselysine metabolic process (GO:0030393), epithelial cell differentiation (GO:0030855), protein deglycation (GO:0036525), post-translational protein modification (GO:0043687)

GO Molecular Function (6): ATP binding (GO:0005524), kinase activity (GO:0016301), protein-ribulosamine 3-kinase activity (GO:0102193), protein-fructosamine 3-kinase activity (GO:0102194), nucleotide binding (GO:0000166), transferase activity (GO:0016740)

GO Cellular Component (2): mitochondrion (GO:0005739), cytosol (GO:0005829)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
Post-translational protein modification	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
protein modification process	2
catalytic activity, acting on a protein	2
cytoplasm	2
amino sugar metabolic process	1
carboxylic acid metabolic process	1
fructosamine metabolic process	1
cell differentiation	1
epithelium development	1
protein repair	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
transferase activity, transferring phosphorus-containing groups	1
phosphotransferase activity, alcohol group as acceptor	1
kinase activity	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
catalytic activity	1
intracellular membrane-bounded organelle	1
cellular anatomical structure	1

Protein interactions and networks

STRING

458 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
FN3K	TBC1D21	Q8IYX1	495
FN3K	CIZ1	Q9ULV3	426
FN3K	TUBGCP3	Q96CW5	417
FN3K	GPSM2	P81274	410
FN3K	GLO1	P78375	402
FN3K	TMPRSS6	Q8IU80	396
FN3K	MDP1	Q86V88	395
FN3K	TBCD	Q9BTW9	391
FN3K	STRN4	Q9NRL3	386
FN3K	HSPB6	O14558	378
FN3K	MTNR1B	P49286	370
FN3K	TMEM79	Q9BSE2	366
FN3K	COMT	P21964	366
FN3K	ATP11A	P98196	357
FN3K	HDAC11	Q96DB2	353

IntAct

17 interactions, top by confidence:

A	B	Type	Score
Eea1	WWP2	psi-mi:“MI:0914”(association)	0.350
PLEKHA7	PLEKHG3	psi-mi:“MI:0914”(association)	0.350
P		psi-mi:“MI:0914”(association)	0.350
M		psi-mi:“MI:0914”(association)	0.350
MAPT	SHTN1	psi-mi:“MI:0914”(association)	0.350
ITM2B	ILVBL	psi-mi:“MI:0914”(association)	0.350
DOK2	PALM	psi-mi:“MI:0914”(association)	0.350
GMFG	CLSTN1	psi-mi:“MI:0914”(association)	0.350
VCP	SHTN1	psi-mi:“MI:0914”(association)	0.350
VCP	FAM171A2	psi-mi:“MI:0914”(association)	0.350
	PIK3R2	psi-mi:“MI:0914”(association)	0.350
RBM11	FN3K	psi-mi:“MI:0915”(physical association)	0.000
DSCR9	FN3K	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (16): FN3K (Affinity Capture-MS), FN3K (Negative Genetic), FN3K (Negative Genetic), NPR1 (Negative Genetic), PRKCA (Negative Genetic), MAP2K5 (Negative Genetic), FN3K (Affinity Capture-MS), FN3K (Affinity Capture-MS), FN3K (Affinity Capture-RNA), FN3K (Affinity Capture-MS), FN3K (Affinity Capture-MS), FN3K (Affinity Capture-MS), FN3K (Affinity Capture-MS), FN3K (Two-hybrid), FN3K (Two-hybrid)

ESM2 similar proteins: A3KG59, A4IFH5, B9N1F9, D3ZVR9, O04059, O35331, O35621, O46560, P11172, P24298, P37111, Q03154, Q04609, Q15124, Q17QK3, Q2R483, Q501L1, Q5E9T8, Q5I0K3, Q5NAY4, Q5R514, Q5R5C9, Q5RDE7, Q5RDN7, Q5RFB0, Q5RFI8, Q6AY30, Q6AYS7, Q6K2E8, Q6PTT0, Q6Q0N1, Q6ZV70, Q7TSV4, Q7X7L3, Q8BZF8, Q8CG45, Q8CG76, Q8IYS1, Q8K183, Q8N0X4

Diamond homologs: A2XBT1, F9UPU7, P46381, P46382, P58065, P74594, P77739, Q10SM2, Q3XZZ9, Q87PM1, Q8D9N5, Q8K274, Q9CN56, Q9ER35, Q9H479, Q9HA64, Q9KRU5, Q9LEW8, P41370, Q2FV31, Q5SJ35

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	60
Likely benign	1
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

1100 predictions. Top by Δscore:

Variant	Effect	Δscore
17:82735771:G:GT	donor_gain	1.0000
17:82735773:CGCAG:C	donor_loss	1.0000
17:82735775:CAG:C	donor_loss	1.0000
17:82735776:AGGTG:A	donor_loss	1.0000
17:82735777:GGTGC:G	donor_loss	1.0000
17:82735778:G:A	donor_loss	1.0000
17:82735779:T:G	donor_loss	1.0000
17:82738484:TGCA:T	acceptor_loss	1.0000
17:82738485:GCA:G	acceptor_loss	1.0000
17:82738486:CAG:C	acceptor_loss	1.0000
17:82738487:A:AG	acceptor_gain	1.0000
17:82738487:AGGCC:A	acceptor_loss	1.0000
17:82738488:G:GG	acceptor_gain	1.0000
17:82738488:GGCCC:G	acceptor_gain	1.0000
17:82738637:GCAG:G	donor_gain	1.0000
17:82738639:AGGT:A	donor_loss	1.0000
17:82738641:G:A	donor_loss	1.0000
17:82738642:T:A	donor_loss	1.0000
17:82740761:A:AG	acceptor_gain	1.0000
17:82740762:G:GG	acceptor_gain	1.0000
17:82740762:GT:G	acceptor_gain	1.0000
17:82740762:GTC:G	acceptor_gain	1.0000
17:82740762:GTCA:G	acceptor_gain	1.0000
17:82740762:GTCAA:G	acceptor_gain	1.0000
17:82740839:G:GT	donor_gain	1.0000
17:82740850:AGTGG:A	donor_loss	1.0000
17:82740851:G:GG	donor_gain	1.0000
17:82740851:GTGG:G	donor_loss	1.0000
17:82740852:TGG:T	donor_gain	1.0000
17:82740853:GG:G	donor_gain	1.0000

AlphaMissense

2021 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
17:82738519:A:C	S58R	0.993
17:82738521:C:A	S58R	0.993
17:82738521:C:G	S58R	0.993
17:82735755:T:A	V40D	0.991
17:82735759:A:C	K41N	0.991
17:82735759:A:T	K41N	0.991
17:82741358:T:C	F145L	0.991
17:82741360:C:A	F145L	0.991
17:82741360:C:G	F145L	0.991
17:82748876:T:A	W164R	0.990
17:82748876:T:C	W164R	0.990
17:82750475:A:T	D217V	0.988
17:82741352:T:C	F143L	0.987
17:82741354:C:A	F143L	0.987
17:82741354:C:G	F143L	0.987
17:82750475:A:C	D217A	0.987
17:82750699:T:C	F292L	0.987
17:82750701:C:A	F292L	0.987
17:82750701:C:G	F292L	0.987
17:82735751:T:C	F39L	0.986
17:82735753:C:A	F39L	0.986
17:82735753:C:G	F39L	0.986
17:82750472:G:T	G216V	0.986
17:82750527:C:A	D234E	0.986
17:82750527:C:G	D234E	0.986
17:82750472:G:A	G216E	0.985
17:82750475:A:G	D217G	0.985
17:82750476:T:A	D217E	0.985
17:82750476:T:G	D217E	0.985
17:82750480:T:A	W219R	0.985

dbSNP variants (sampled 300 via entrez): RS1000058679 (17:82747267 T>G), RS1000187657 (17:82744654 C>T), RS1000244645 (17:82739603 G>A), RS1000298493 (17:82738947 T>A), RS1000435410 (17:82739352 A>G), RS1000727079 (17:82734773 C>A,T), RS1000744406 (17:82750237 TAA>T), RS1000804008 (17:82739331 C>T), RS1000833908 (17:82735583 G>A,C), RS1001489797 (17:82747734 T>C), RS1001586224 (17:82735082 G>A), RS1001883864 (17:82749231 C>G), RS1001966713 (17:82737884 G>A), RS1001998794 (17:82743736 G>C), RS1002040793 (17:82733883 G>A)

Disease associations

OMIM: gene MIM:608425 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

11 associations (top):

Study	Trait	p-value
GCST000803_6	Glycated hemoglobin levels	2.000000e-26
GCST002270_3	Glycated hemoglobin levels	2.000000e-07
GCST002390_8	Glycated hemoglobin levels	4.000000e-17
GCST005145_4	Glycated hemoglobin levels	6.000000e-17
GCST005145_7	Glycated hemoglobin levels	2.000000e-16
GCST006001_16	Hemoglobin A1c levels	1.000000e-16
GCST008034_19	Hemoglobin A1c levels	4.000000e-08
GCST008034_4	Hemoglobin A1c levels	4.000000e-08
GCST008398_5	Glycated hemoglobin levels	2.000000e-11
GCST90002401_559	Platelet distribution width	1.000000e-26
GCST90002404_188	Red cell distribution width	2.000000e-13

EFO canonical traits (3, from GWAS)

EFO ID	Trait name
EFO:0004541	HbA1c measurement
EFO:0007984	platelet component distribution width
EFO:0009188	Red cell distribution width

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5724680 (SINGLE PROTEIN)

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

ChEMBL bioactivities

4 potent at pChembl≥5 of 4 total, top 4 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
6.54	Kd	286.7	nM	CHEMBL5653589
6.54	ED50	291.3	nM	CHEMBL5653589
5.14	Kd	7199	nM	CHEMBL3752910
5.14	ED50	7315	nM	CHEMBL3752910

PubChem BioAssay actives

2 with measured affinity, of 8 total; 2 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
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148397: Binding affinity to human FN3K incubated for 45 mins by Kinobead based pull down assay	kd	0.2867	uM
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148397: Binding affinity to human FN3K incubated for 45 mins by Kinobead based pull down assay	kd	7.1987	uM

CTD chemical–gene interactions

28 total (human), top 28 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	decreases expression, increases methylation	2
aristolochic acid I	increases expression	1
2,4,6-tribromophenol	decreases expression	1
propionaldehyde	decreases expression	1
bisphenol A	decreases expression	1
deoxynivalenol	decreases expression	1
glycidyl methacrylate	decreases expression	1
decabromobiphenyl ether	increases expression	1
tetrabromobisphenol A	decreases expression	1
S-(1,2-dichlorovinyl)cysteine	affects response to substance, increases expression	1
abrine	decreases expression	1
2,2’,4,4’-tetrabromodiphenyl ether	decreases expression	1
Sunitinib	increases expression	1
Acetaminophen	decreases expression	1
Air Pollutants	increases expression, increases abundance	1
Cadmium	increases expression	1
Cisplatin	decreases expression	1
Estradiol	affects cotreatment, decreases expression	1
Lipopolysaccharides	decreases expression, affects response to substance, increases expression	1
N-Nitrosopyrrolidine	decreases expression	1
Phthalic Acids	increases methylation	1
Smoke	decreases expression	1
Tobacco Smoke Pollution	decreases expression	1
Valproic Acid	increases methylation	1
Aflatoxin B1	decreases expression	1
Okadaic Acid	decreases expression	1
beta-Naphthoflavone	decreases expression	1
Particulate Matter	increases abundance, increases expression	1

ChEMBL screening assays

5 unique, capped per target: 5 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL5651439	Binding	Binding affinity to human FN3K incubated for 45 mins by Kinobead based pull down assay	NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family. — ChemMedChem

Clinical trials (associated diseases)

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