FN3KRP

Summary

FN3KRP (fructosamine 3 kinase related protein, HGNC:25700) is a protein-coding gene on chromosome 17q25.3, encoding Ketosamine-3-kinase (Q9HA64). Ketosamine-3-kinase involved in protein deglycation by mediating phosphorylation of ribuloselysine and psicoselysine on glycated proteins, to generate ribuloselysine-3 phosphate and psicoselysine-3 phosphate, respectively.

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 are less active or functional. This gene encodes an enzyme which catalyzes the phosphorylation of psicosamines and ribulosamines compared to the neighboring gene which encodes a highly similar enzyme, fructosamine-3-kinase, which has different substrate specificity. The activity of both enzymes may result in deglycation of proteins to restore their function. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 79672 — RefSeq curated summary.

At a glance

• GWAS associations: 5
• Clinical variants (ClinVar): 99 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_024619

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:25700
Approved symbol	FN3KRP
Name	fructosamine 3 kinase related protein
Location	17q25.3
Locus type	gene with protein product
Status	Approved
Aliases	FLJ12171, FN3KL
Ensembl gene	ENSG00000141560
Ensembl biotype	protein_coding
OMIM	611683
Entrez	79672

Gene structure

Transcript identifiers

Ensembl transcripts: 10 — 4 protein_coding, 4 nonsense_mediated_decay, 2 retained_intron

ENST00000269373, ENST00000571482, ENST00000571594, ENST00000573158, ENST00000574206, ENST00000574356, ENST00000574832, ENST00000576363, ENST00000577128, ENST00000910132

RefSeq mRNA: 1 — MANE Select: NM_024619 NM_024619

CCDS: CCDS11817

Canonical transcript exons

ENST00000269373 — 6 exons

Exon	Start	End
ENSE00001318127	82726833	82728013
ENSE00002668747	82716706	82716896
ENSE00003470493	82726480	82726602
ENSE00003497395	82718906	82719057
ENSE00003624919	82722804	82722886
ENSE00003684854	82720272	82720363

Expression profiles

Bgee: expression breadth ubiquitous, 256 present calls, max score 94.64.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 11.1692 / max 75.8614, expressed in 1800 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
163533	11.1692	1800

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
C1 segment of cervical spinal cord	UBERON:0006469	94.64	gold quality
spinal cord	UBERON:0002240	93.95	gold quality
left ovary	UBERON:0002119	93.85	gold quality
right ovary	UBERON:0002118	93.19	gold quality
anterior cingulate cortex	UBERON:0009835	93.05	gold quality
amygdala	UBERON:0001876	93.02	gold quality
right frontal lobe	UBERON:0002810	93.01	gold quality
cingulate cortex	UBERON:0003027	92.94	gold quality
prefrontal cortex	UBERON:0000451	92.76	gold quality
Brodmann (1909) area 9	UBERON:0013540	92.63	gold quality
putamen	UBERON:0001874	92.47	gold quality
nucleus accumbens	UBERON:0001882	92.26	gold quality
caudate nucleus	UBERON:0001873	91.90	gold quality
ventricular zone	UBERON:0003053	91.90	gold quality
skin of leg	UBERON:0001511	91.87	gold quality
skin of abdomen	UBERON:0001416	91.67	gold quality
cerebellar hemisphere	UBERON:0002245	91.61	gold quality
cerebellar cortex	UBERON:0002129	91.54	gold quality
right hemisphere of cerebellum	UBERON:0014890	91.44	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	91.43	gold quality
transverse colon	UBERON:0001157	91.42	gold quality
nerve	UBERON:0001021	91.35	gold quality
tibial nerve	UBERON:0001323	91.35	gold quality
neocortex	UBERON:0001950	91.25	gold quality
tibial artery	UBERON:0007610	91.25	gold quality
popliteal artery	UBERON:0002250	91.24	gold quality
granulocyte	CL:0000094	91.21	gold quality
endocervix	UBERON:0000458	91.11	gold quality
frontal cortex	UBERON:0001870	91.10	gold quality
frontal lobe	UBERON:0016525	91.10	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	3.72

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

35 targeting FN3KRP, 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-4476	100.00	68.18	2030
HSA-MIR-6876-5P	100.00	67.68	2126
HSA-MIR-4533	100.00	69.48	2758
HSA-MIR-1252-5P	100.00	69.80	2774
HSA-MIR-19A-3P	99.98	75.33	2762
HSA-MIR-19B-3P	99.98	75.44	2754
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-629-3P	99.85	67.99	1875
HSA-MIR-1299	99.77	71.24	2389
HSA-MIR-3059-5P	99.70	69.93	2491
HSA-MIR-7154-5P	99.69	70.52	1900
HSA-MIR-2113	99.58	71.22	1521
HSA-MIR-12123	99.52	71.79	2990
HSA-MIR-4708-3P	99.51	67.99	870
HSA-MIR-409-3P	99.50	66.33	1192
HSA-MIR-520A-5P	99.35	66.72	1632
HSA-MIR-525-5P	99.35	66.85	1615
HSA-MIR-4426	99.17	66.74	1949
HSA-MIR-4758-3P	99.12	63.96	869
HSA-MIR-4695-5P	99.06	64.87	1151
HSA-MIR-670-3P	99.03	68.88	2404
HSA-MIR-3074-5P	98.82	66.56	1414
HSA-MIR-3611	98.76	68.76	1290
HSA-MIR-4709-5P	98.51	67.25	1335
HSA-MIR-4662B	98.33	66.37	1163
HSA-MIR-4647	98.30	66.41	1139
HSA-MIR-4684-3P	98.24	69.91	1075
HSA-MIR-338-3P	98.14	67.38	1137
HSA-MIR-6881-3P	98.04	68.24	1777
HSA-MIR-5189-3P	97.52	66.33	487

Literature-anchored findings (GeneRIF, showing 6)

• 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)
• 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)
• FN3KRP phosphorylates meglumine to produce meglumine-4-phosphate. (PMID:17686456)
• Studies provide evidence that Fn3KRP possesses an ATP-binding domain that is structurally related to that of both the aminoglycoside kinases and eukaryotic protein kinases. (PMID:18637789)
• Exome-Wide Association Study Identifies FN3KRP and PGP as New Candidate Longevity Genes. (PMID:33491046)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	fn3krp	ENSDARG00000098208
mus_musculus	Fn3krp	ENSMUSG00000039253
caenorhabditis_elegans		WBGENE00013802

Paralogs (1): FN3K (ENSG00000167363)

Protein

Protein identifiers

Ketosamine-3-kinase — Q9HA64 (reviewed: Q9HA64)

Alternative names: Fructosamine-3-kinase-related protein, Protein-psicosamine 3-kinase FN3KRP

All UniProt accessions (8): A0A140VK84, Q9HA64, I3L139, I3L2G3, I3L2K8, I3L378, I3L3W5, I3L407

UniProt curated annotations — full annotation on UniProt →

Function. Ketosamine-3-kinase involved in protein deglycation by mediating phosphorylation of ribuloselysine and psicoselysine on glycated proteins, to generate ribuloselysine-3 phosphate and psicoselysine-3 phosphate, respectively. Ribuloselysine-3 phosphate and psicoselysine-3 phosphate adducts are unstable and decompose under physiological conditions. Not able to phosphorylate fructoselysine.

Tissue specificity. Widely expressed; except in skeletal muscle where it is expressed at very low level. Expressed in erythrocytes.

Domain organisation. The ATP-binding domain is structurally related to aminoglycoside phosphotransferase family.

Similarity. Belongs to the fructosamine kinase family.

RefSeq proteins (1): NP_078895* (*=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)
• EC 2.7.1.172 — protein-ribulosamine 3-kinase (BRENDA: 9 organisms, 18 substrates, 8 inhibitors, 14 Km, 0 kcat entries)

Substrate kinetics (BRENDA)

23 substrates with measured Km, best-characterized 15. 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
N6-D-ERYTHRULOSYL-L-LYSINE	0.025–0.279	2
N6-D-RIBULOSYL-L-LYSINE	0.119–0.135	2
[LYSOZYME]-N6-D-ERYTHRULOSYL-L-LYSINE	0.008–0.104	2
[LYSOZYME]-N6-D-RIBULOSYL-L-LYSINE	0.274–0.659	2
(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

Catalyzed reactions (Rhea), 2 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-psicosyl)-L-lysyl-[protein] + ATP = N(6)-(3-O-phospho-D-psicosyl)-L-lysyl-[protein] + ADP + H(+) (RHEA:61392)

UniProt features (8 total): sequence conflict 3, chain 1, active site 1, binding site 1, modified residue 1, sequence variant 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9HA64-F1	94.55	0.89

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): 20

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-163841	Gamma carboxylation, hypusinylation, hydroxylation, and arylsulfatase activation
R-HSA-392499	Metabolism of proteins
R-HSA-597592	Post-translational protein modification

MSigDB gene sets: 77 (showing top): ACEVEDO_NORMAL_TISSUE_ADJACENT_TO_LIVER_TUMOR_DN, GOBP_POST_TRANSLATIONAL_PROTEIN_MODIFICATION, FISCHER_DREAM_TARGETS, GCM_NF2, NIKOLSKY_BREAST_CANCER_17Q21_Q25_AMPLICON, GOMF_KINASE_ACTIVITY, GOMF_ADENYL_NUCLEOTIDE_BINDING, GOMF_TRANSFERASE_ACTIVITY_TRANSFERRING_PHOSPHORUS_CONTAINING_GROUPS, REACTOME_POST_TRANSLATIONAL_PROTEIN_MODIFICATION, GCM_RAN, PURBEY_TARGETS_OF_CTBP1_AND_SATB1_DN, FORTSCHEGGER_PHF8_TARGETS_DN, REACTOME_GAMMA_CARBOXYLATION_HYPUSINYLATION_HYDROXYLATION_AND_ARYLSULFATASE_ACTIVATION, EIF4E_UP, CDC5L_TARGET_GENES

GO Biological Process (1): post-translational protein modification (GO:0043687)

GO Molecular Function (5): ATP binding (GO:0005524), kinase activity (GO:0016301), protein-ribulosamine 3-kinase activity (GO:0102193), nucleotide binding (GO:0000166), transferase activity (GO:0016740)

GO Cellular Component (2): cytosol (GO:0005829), cytoplasm (GO:0005737)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Post-translational protein modification	1
Metabolism of proteins	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	2
protein modification process	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
transferase activity, transferring phosphorus-containing groups	1
phosphotransferase activity, alcohol group as acceptor	1
catalytic activity, acting on a protein	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
catalytic activity	1
cytoplasm	1
intracellular anatomical structure	1

Protein interactions and networks

STRING

842 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
FN3KRP	QTGAL	Q67FW5	461
FN3KRP	GPATCH11	Q8N954	453
FN3KRP	PGP	A6NDG6	452
FN3KRP	CCDC167	Q9P0B6	445
FN3KRP	TBCD	Q9BTW9	436
FN3KRP	CTXN1	P60606	428
FN3KRP	YJU2B	P13994	412
FN3KRP	METRNL	Q641Q3	376
FN3KRP	ZNF750	Q32MQ0	369
FN3KRP	ADCK1	Q86TW2	351
FN3KRP	ZMAT4	Q9H898	338
FN3KRP	HSPB6	O14558	332
FN3KRP	NRDC	O43847	328
FN3KRP	GPR151	Q8TDV0	324
FN3KRP	F6RGN5	F6RGN5	317
FN3KRP	SLC25A10	Q9UBX3	317

IntAct

25 interactions, top by confidence:

A	B	Type	Score
USP43	YWHAB	psi-mi:“MI:0914”(association)	0.640
FN3KRP	LTF	psi-mi:“MI:0914”(association)	0.530
HSCB	RBP5	psi-mi:“MI:0914”(association)	0.350
ORF69	PEPD	psi-mi:“MI:0914”(association)	0.350
CUL4B	APBB1	psi-mi:“MI:0914”(association)	0.350
CUL3	PXDNL	psi-mi:“MI:0914”(association)	0.350
FN3KRP	IGHA1	psi-mi:“MI:0914”(association)	0.350
ENG	IGKV2-28	psi-mi:“MI:0914”(association)	0.350
S	COPE	psi-mi:“MI:0914”(association)	0.350
rep	VWA8	psi-mi:“MI:0914”(association)	0.350
HLA-A	AIP	psi-mi:“MI:0914”(association)	0.350
CAPZB	ENAH	psi-mi:“MI:0914”(association)	0.350
CLTA	CLTB	psi-mi:“MI:0914”(association)	0.350
FN3KRP	SRC	psi-mi:“MI:0914”(association)	0.350
MFSD14A	FAM171A2	psi-mi:“MI:0914”(association)	0.350
SLC12A1	ELOVL7	psi-mi:“MI:0914”(association)	0.350
SLC16A5	NDUFB3	psi-mi:“MI:0914”(association)	0.350
PIDD1	IPO5	psi-mi:“MI:0914”(association)	0.350

BioGRID (81): FN3KRP (Affinity Capture-MS), LTF (Affinity Capture-MS), LACRT (Affinity Capture-MS), PIGR (Affinity Capture-MS), IGHA1 (Affinity Capture-MS), FN3KRP (Affinity Capture-MS), FN3KRP (Affinity Capture-MS), LTF (Affinity Capture-MS), LACRT (Affinity Capture-MS), DOHH (Affinity Capture-MS), IGHA1 (Affinity Capture-MS), FN3KRP (Affinity Capture-MS), FN3KRP (Affinity Capture-MS), FN3KRP (Affinity Capture-MS), FN3KRP (Affinity Capture-MS)

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

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	79
Likely benign	4
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1393 predictions. Top by Δscore:

Variant	Effect	Δscore
17:82716862:G:GT	donor_gain	1.0000
17:82716876:A:T	donor_gain	1.0000
17:82716894:G:GT	donor_gain	1.0000
17:82719046:GCATC:G	donor_gain	1.0000
17:82720348:G:GT	donor_gain	1.0000
17:82720360:GTGG:G	donor_gain	1.0000
17:82722794:T:TA	acceptor_gain	1.0000
17:82722798:T:TA	acceptor_gain	1.0000
17:82722801:A:AG	acceptor_gain	1.0000
17:82722801:AAG:A	acceptor_gain	1.0000
17:82722801:AAGG:A	acceptor_gain	1.0000
17:82722802:A:G	acceptor_gain	1.0000
17:82722803:G:A	acceptor_gain	1.0000
17:82722803:GGGA:G	acceptor_gain	1.0000
17:82722884:CAG:C	donor_loss	1.0000
17:82722887:G:GG	donor_gain	1.0000
17:82722887:GT:G	donor_loss	1.0000
17:82722888:T:G	donor_loss	1.0000
17:82723014:T:A	acceptor_gain	1.0000
17:82726471:ACTGT:A	acceptor_gain	1.0000
17:82726473:T:A	acceptor_gain	1.0000
17:82726474:GTGCA:G	acceptor_loss	1.0000
17:82726475:T:TA	acceptor_gain	1.0000
17:82726476:GCA:G	acceptor_loss	1.0000
17:82726477:CAG:C	acceptor_loss	1.0000
17:82726478:A:AG	acceptor_gain	1.0000
17:82726478:AG:A	acceptor_gain	1.0000
17:82726478:AGGT:A	acceptor_gain	1.0000
17:82726478:AGGTG:A	acceptor_loss	1.0000
17:82726479:G:GC	acceptor_gain	1.0000

AlphaMissense

2035 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
17:82718936:A:C	S58R	0.997
17:82718938:T:A	S58R	0.997
17:82718938:T:G	S58R	0.997
17:82726891:A:T	D217V	0.997
17:82722849:G:A	G144E	0.996
17:82726891:A:C	D217A	0.996
17:82726896:T:A	W219R	0.996
17:82726896:T:C	W219R	0.996
17:82726907:C:A	N222K	0.996
17:82726907:C:G	N222K	0.996
17:82727115:T:C	F292L	0.996
17:82727117:T:A	F292L	0.996
17:82727117:T:G	F292L	0.996
17:82716878:A:C	K41N	0.995
17:82716878:A:T	K41N	0.995
17:82726501:T:A	W164R	0.995
17:82726501:T:C	W164R	0.995
17:82726888:G:T	G216V	0.995
17:82726891:A:G	D217G	0.995
17:82726892:C:A	D217E	0.995
17:82726892:C:G	D217E	0.995
17:82726995:T:C	F252L	0.995
17:82726997:T:A	F252L	0.995
17:82726997:T:G	F252L	0.995
17:82722873:G:A	G152E	0.994
17:82726887:G:T	G216W	0.994
17:82726888:G:A	G216E	0.994
17:82716831:A:C	S26R	0.993
17:82716833:C:A	S26R	0.993
17:82716833:C:G	S26R	0.993

dbSNP variants (sampled 300 via entrez): RS1000646661 (17:82724850 C>T), RS1000857036 (17:82716366 A>G), RS1000939777 (17:82716019 G>A), RS1000964359 (17:82725498 A>G,T), RS1001006191 (17:82720539 A>G), RS1001357507 (17:82717312 A>G,T), RS1001484766 (17:82717159 T>C,G), RS1001951935 (17:82725499 G>A,C), RS1002246653 (17:82720938 T>A), RS1002355103 (17:82716692 C>A,G,T), RS1002489415 (17:82716468 G>C), RS1002548677 (17:82723459 C>A,T), RS1002573464 (17:82727598 C>T), RS1002625815 (17:82727478 G>A,C,T), RS1002908912 (17:82722961 C>A,G,T)

Disease associations

OMIM: gene MIM:611683 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

5 associations (top):

Study	Trait	p-value
GCST005145_4	Glycated hemoglobin levels	6.000000e-17
GCST005914_1	Glycated hemoglobin levels	4.000000e-07
GCST007951_1	Glycated hemoglobin levels	7.000000e-07
GCST007953_3	Glycated hemoglobin levels	7.000000e-10
GCST007954_27	Glycated hemoglobin levels	4.000000e-64

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0004541	HbA1c measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4295947 (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: 1,538 (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
CHEMBL1232461	MOLIBRESIB	2	1,538

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

ChEMBL bioactivities

3 potent at pChembl≥5 of 4 total, top 3 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.84	Kd	14.53	nM	CHEMBL5653589
7.74	ED50	18.31	nM	CHEMBL5653589
5.27	IC50	5340	nM	MOLIBRESIB

PubChem BioAssay actives

2 with measured affinity, of 19 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	2148398: Binding affinity to human FN3KRP incubated for 45 mins by Kinobead based pull down assay	kd	0.0145	uM
2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide	2178942: Inhibition of FN3KRP (unknown origin) incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysis	ic50	5.3400	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
bisphenol A	decreases expression, increases expression, affects expression	3
sodium arsenite	affects cotreatment, decreases expression, increases abundance, increases expression	2
Air Pollutants	affects cotreatment, increases abundance, increases oxidation, decreases expression	2
aristolochic acid I	increases expression	1
methylmercuric chloride	decreases expression	1
alpha-pinene	affects cotreatment, increases oxidation, increases abundance	1
arsenite	increases reaction, affects binding	1
tris(1,3-dichloro-2-propyl)phosphate	decreases expression	1
manganese chloride	affects cotreatment, decreases expression, increases abundance	1
methacrylaldehyde	affects cotreatment, increases oxidation, increases abundance	1
di-n-butylphosphoric acid	affects expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression	1
nutlin 3	increases expression, increases secretion, affects cotreatment	1
ICG 001	increases expression	1
bisphenol S	increases expression	1
LDN 193189	affects cotreatment, increases expression	1
bisphenol AF	increases 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	increases expression	1
Resveratrol	affects cotreatment, increases expression	1
Temozolomide	increases expression	1
Arsenic Trioxide	increases expression	1
Acetaminophen	increases expression	1
Acrolein	affects cotreatment, increases oxidation, increases abundance	1
Arsenic	increases abundance, affects cotreatment, decreases expression	1
Ascorbic Acid	increases expression	1
Benzo(a)pyrene	affects methylation	1
Cadmium	increases abundance, increases expression	1
Cisplatin	increases expression	1
Dactinomycin	increases secretion, affects cotreatment, increases expression	1
Ivermectin	decreases expression	1

ChEMBL screening assays

16 unique, capped per target: 16 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4118968	Binding	Binding affinity to FN3KRP in human NCI-H358 cells at 1 uM by mass spectrometry based pull down assay	Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors. — Bioorg Med Chem

Clinical trials (associated diseases)

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