KYAT1

Summary

KYAT1 (kynurenine aminotransferase 1, HGNC:1564) is a protein-coding gene on chromosome 9q34.11, encoding Kynurenine–oxoglutarate transaminase 1 (Q16773). Catalyzes the irreversible transamination of the L-tryptophan metabolite L-kynurenine to form kynurenic acid (KA), an intermediate in the tryptophan catabolic pathway which is also a broad spectrum antagonist of the three ionotropic excitatory amino acid receptors among others.

This gene encodes a cytosolic enzyme that is responsible for the metabolism of cysteine conjugates of certain halogenated alkenes and alkanes. This metabolism can form reactive metabolites leading to nephrotoxicity and neurotoxicity. Increased levels of this enzyme have been linked to schizophrenia. Multiple transcript variants that encode different isoforms have been identified for this gene.

Source: NCBI Gene 883 — RefSeq curated summary.

At a glance

• GWAS associations: 9
• Clinical variants (ClinVar): 19 total
• Druggable target: yes
• MANE Select transcript: NM_004059

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:1564
Approved symbol	KYAT1
Name	kynurenine aminotransferase 1
Location	9q34.11
Locus type	gene with protein product
Status	Approved
Aliases	KATI, GTK
Ensembl gene	ENSG00000171097
Ensembl biotype	protein_coding
OMIM	600547
Entrez	883

Gene structure

Transcript identifiers

Ensembl transcripts: 51 — 47 protein_coding, 4 protein_coding_CDS_not_defined

ENST00000302586, ENST00000320665, ENST00000416084, ENST00000427720, ENST00000436267, ENST00000451800, ENST00000462722, ENST00000466418, ENST00000474824, ENST00000483599, ENST00000896293, ENST00000896294, ENST00000896295, ENST00000896296, ENST00000896297, ENST00000896298, ENST00000896299, ENST00000896300, ENST00000896301, ENST00000896302, ENST00000896303, ENST00000896304, ENST00000896305, ENST00000896306, ENST00000896307, ENST00000896308, ENST00000896309, ENST00000896310, ENST00000929023, ENST00000929024, ENST00000929025, ENST00000929026, ENST00000929027, ENST00000964593, ENST00000964594, ENST00000964595, ENST00000964596, ENST00000964597, ENST00000964598, ENST00000964599, ENST00000964600, ENST00000964601, ENST00000964602, ENST00000964603, ENST00000964604, ENST00000964605, ENST00000964606, ENST00000964607, ENST00000964608, ENST00000964609, ENST00000964610

RefSeq mRNA: 14 — MANE Select: NM_004059 NM_001122671, NM_001122672, NM_001287390, NM_001352988, NM_001352989, NM_001352990, NM_001352991, NM_001352992, NM_001352993, NM_001352994, NM_001352997, NM_001352998, NM_001352999, NM_004059

CCDS: CCDS43884, CCDS48038, CCDS75915

Canonical transcript exons

ENST00000302586 — 13 exons

Exon	Start	End
ENSE00001704435	128835997	128836073
ENSE00001766968	128832942	128833643
ENSE00001851283	128881897	128881950
ENSE00003492296	128836802	128836922
ENSE00003559446	128835779	128835868
ENSE00003561407	128838051	128838137
ENSE00003565251	128835323	128835402
ENSE00003582125	128837685	128837813
ENSE00003589920	128845353	128845411
ENSE00003594463	128835481	128835667
ENSE00003624347	128833740	128833826
ENSE00003633499	128842654	128842801
ENSE00003656584	128838218	128838367

Expression profiles

Bgee: expression breadth ubiquitous, 138 present calls, max score 86.78.

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right hemisphere of cerebellum	UBERON:0014890	86.78	gold quality
cerebellar hemisphere	UBERON:0002245	86.21	gold quality
cerebellar cortex	UBERON:0002129	86.11	gold quality
cerebellum	UBERON:0002037	86.09	gold quality
Brodmann (1909) area 9	UBERON:0013540	85.96	gold quality
right frontal lobe	UBERON:0002810	85.91	gold quality
prefrontal cortex	UBERON:0000451	85.62	gold quality
frontal cortex	UBERON:0001870	85.60	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	84.92	gold quality
apex of heart	UBERON:0002098	84.59	gold quality
primary visual cortex	UBERON:0002436	84.55	gold quality
nucleus accumbens	UBERON:0001882	84.47	gold quality
cerebral cortex	UBERON:0000956	84.43	gold quality
telencephalon	UBERON:0001893	83.93	gold quality
brain	UBERON:0000955	83.79	gold quality
hindlimb stylopod muscle	UBERON:0004252	83.66	gold quality
putamen	UBERON:0001874	83.63	gold quality
heart left ventricle	UBERON:0002084	83.60	gold quality
anterior cingulate cortex	UBERON:0009835	83.37	gold quality
stromal cell of endometrium	CL:0002255	83.18	gold quality
right lobe of liver	UBERON:0001114	82.92	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	82.89	gold quality
substantia nigra	UBERON:0002038	82.88	gold quality
caudate nucleus	UBERON:0001873	82.85	gold quality
cortical plate	UBERON:0005343	82.67	gold quality
superior frontal gyrus	UBERON:0002661	82.55	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	82.51	gold quality
skeletal muscle tissue	UBERON:0001134	82.32	gold quality
heart	UBERON:0000948	82.04	gold quality
temporal lobe	UBERON:0001871	81.90	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	3.05

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

16 targeting KYAT1, 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-5680	99.91	69.83	3421
HSA-MIR-182-3P	99.57	67.57	825
HSA-MIR-302A-5P	99.39	68.21	1913
HSA-MIR-423-5P	98.69	67.48	1522
HSA-MIR-4710	98.61	65.96	1048
HSA-MIR-2117	98.48	67.97	1307
HSA-MIR-654-3P	98.38	67.61	905
HSA-MIR-6793-3P	97.66	65.78	1084
HSA-MIR-1224-3P	97.24	65.92	851
HSA-MIR-597-5P	96.82	67.57	732
HSA-MIR-597-3P	96.46	68.03	1035
HSA-MIR-3690	96.44	65.18	737
HSA-MIR-152-5P	96.42	66.59	960
HSA-MIR-3918	96.13	64.65	1300
HSA-MIR-6796-5P	95.37	66.08	1120
HSA-MIR-4734	88.28	63.44	87

Literature-anchored findings (GeneRIF, showing 6)

• major biological roles of glutamine transaminase K are to maintain low levels of phenylpyruvate and to close the methionine salvage pathway–REVIEW (PMID:15016471)
• We found elevated cerebellar KAT-1 activities in post-mortem brain samples from schizophrenic versus normal individuals. (PMID:16828464)
• alpha-keto acids generated by transamination/l-amino acid oxidase activity of the two catechol cysteine S-conjugates are unstable (PMID:18342615)
• CH(3)Hg-S-Cys and Cys-S-Hg-S-Cys are substrates and reversible inhibitors of GTK. (PMID:22093698)
• Immunohistochemical analysis revealed the presence of KAT I, II, and III in all examined corneal sections. (PMID:28706436)
• genetic suppression of glutamine transaminase K (GTK), a key enzyme of the glutaminase II pathway, leads to the complete inhibition of pancreatic tumorigenesis in vivo unveiling GTK as a new metabolic target for cancer therapy (PMID:31231915)

Cross-species orthologs

8 orthologs

Organism	Symbol	Gene ID
danio_rerio	kyat1	ENSDARG00000023645
mus_musculus	Kyat1	ENSMUSG00000039648
rattus_norvegicus	Kyat1	ENSRNOG00000016097
drosophila_melanogaster	CG1640	FBGN0030478
drosophila_melanogaster	CG6321	FBGN0036117
caenorhabditis_elegans		WBGENE00009232
caenorhabditis_elegans		WBGENE00010984
caenorhabditis_elegans	C32F10.8	WBGENE00016333

Paralogs (7): AADAT (ENSG00000109576), ACCS (ENSG00000110455), KYAT3 (ENSG00000137944), GPT2 (ENSG00000166123), GPT (ENSG00000167701), TAT (ENSG00000198650), ACCSL (ENSG00000205126)

Protein

Protein identifiers

Kynurenine–oxoglutarate transaminase 1 — Q16773 (reviewed: Q16773)

Alternative names: Cysteine-S-conjugate beta-lyase, Glutamine transaminase K, Glutamine–phenylpyruvate transaminase, Kynurenine aminotransferase 1, Kynurenine aminotransferase I, Kynurenine–oxoglutarate transaminase I

All UniProt accessions (6): A8K563, B7Z4W5, Q16773, Q5T276, Q5T277, Q5T278

UniProt curated annotations — full annotation on UniProt →

Function. Catalyzes the irreversible transamination of the L-tryptophan metabolite L-kynurenine to form kynurenic acid (KA), an intermediate in the tryptophan catabolic pathway which is also a broad spectrum antagonist of the three ionotropic excitatory amino acid receptors among others. Also metabolizes the cysteine conjugates of certain halogenated alkenes and alkanes to form reactive metabolites. Catalyzes the beta-elimination of S-conjugates and Se-conjugates of L-(seleno)cysteine, resulting in the cleavage of the C-S or C-Se bond.

Subunit / interactions. Homodimer.

Subcellular location. Cytoplasm. Cytosol.

Activity regulation. Inhibited by tryptophan, indole-3-pyruvic acid, 3-indolepropionic acid, DL-indole-3-lactic acid, indole-3-acetic acid (IAC), amino-oxyacetate (AOAA), aminooxy-phenylpropionic acid (AOPP) and Tris.

Pathway. Amino-acid degradation; L-kynurenine degradation; kynurenate from L-kynurenine: step 1/2.

Similarity. Belongs to the class-I pyridoxal-phosphate-dependent aminotransferase family.

Isoforms (3)

UniProt ID	Names	Canonical?
Q16773-1	1	yes
Q16773-2	2
Q16773-3	3

RefSeq proteins (14): NP_001116143, NP_001116144, NP_001274319, NP_001339917, NP_001339918, NP_001339919, NP_001339920, NP_001339921, NP_001339922, NP_001339923, NP_001339926, NP_001339927, NP_001339928, NP_004050* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR004839	Aminotransferase_I/II_large	Domain
IPR015421	PyrdxlP-dep_Trfase_major	Homologous_superfamily
IPR015422	PyrdxlP-dep_Trfase_small	Homologous_superfamily
IPR015424	PyrdxlP-dep_Trfase	Homologous_superfamily
IPR051326	Kynurenine-oxoglutarate_AT	Family

Pfam: PF00155

Enzyme classification (BRENDA):

• EC 2.6.1.7 — kynurenine-oxoglutarate transaminase (BRENDA: 24 organisms, 197 substrates, 229 inhibitors, 160 Km, 93 kcat entries)

Substrate kinetics (BRENDA)

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

Substrate	Km (mM)	Measurements
L-KYNURENINE	0.083–27	28
2-OXOGLUTARATE	0.013–8.1	15
PYRUVATE	0.0175–12.1	12
L-3-HYDROXYKYNURENINE	1.36–6.3	6
2-OXOBUTYRATE	0.0002–42.2	5
L-METHIONINE	0.9–6.4	5
L-TRYPTOPHAN	1.2–12.9	5
PHENYLPYRUVATE	0.6–1.8	5
2-OXO-4-METHYLTHIOBUTYRATE	0.0024–5.7	4
GLYOXYLATE	0.4–18	4
L-LEUCINE	5–34.5	4
MERCAPTOPYRUVATE	2.4–3.2	4
OXALOACETATE	0.9–16.8	4
2-OXOISOCAPROATE	1	3
2-OXOVALERATE	1.2–10.9	3

Catalyzed reactions (Rhea), 3 shown:

• 3-phenylpyruvate + L-glutamine = 2-oxoglutaramate + L-phenylalanine (RHEA:17593)
• an S-substituted L-cysteine + H2O = a thiol + pyruvate + NH4(+) (RHEA:18121)
• L-kynurenine + 2-oxoglutarate = kynurenate + L-glutamate + H2O (RHEA:65560)

UniProt features (51 total): helix 22, strand 12, turn 8, binding site 3, splice variant 3, chain 1, modified residue 1, sequence conflict 1

Structure

Experimental structures (PDB)

9 structures.

PDB	Method	Resolution (Å)
4WLH	X-RAY DIFFRACTION	1.28
3FVS	X-RAY DIFFRACTION	1.5
3FVX	X-RAY DIFFRACTION	1.5
4WLJ	X-RAY DIFFRACTION	1.54
3FVU	X-RAY DIFFRACTION	1.55
1W7L	X-RAY DIFFRACTION	2
1W7M	X-RAY DIFFRACTION	2.7
1W7N	X-RAY DIFFRACTION	2.9
4WP0	X-RAY DIFFRACTION	3

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q16773-F1	97.90	0.96

Functional residue map

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

Ligand- & substrate-binding residues (3): 36; 185; 398

Post-translational modifications (1): 247

Function

Pathways and Gene Ontology

Reactome pathways

6 pathways

ID	Pathway
R-HSA-71240	Tryptophan catabolism
R-HSA-8964208	Phenylalanine metabolism
R-HSA-8964539	Glutamate and glutamine metabolism
R-HSA-1430728	Metabolism
R-HSA-71291	Metabolism of amino acids and derivatives
R-HSA-8963691	Phenylalanine and tyrosine metabolism

MSigDB gene sets: 154 (showing top): GOBP_ALPHA_AMINO_ACID_METABOLIC_PROCESS, REACTOME_TRYPTOPHAN_CATABOLISM, CREBP1_Q2, GGGTGGRR_PAX4_03, GOBP_KETONE_METABOLIC_PROCESS, CREB_Q4, MODULE_66, GOBP_ORGANIC_ACID_CATABOLIC_PROCESS, E4F1_Q6, CREB_Q2_01, GOBP_ORGANIC_ACID_METABOLIC_PROCESS, GOBP_SMALL_MOLECULE_CATABOLIC_PROCESS, GOBP_BENZENE_CONTAINING_COMPOUND_METABOLIC_PROCESS, GOBP_AMINO_ACID_CATABOLIC_PROCESS, MODULE_11

GO Biological Process (4): response to bacterium (GO:0009617), obsolete kynurenine metabolic process (GO:0070189), obsolete L-kynurenine catabolic process (GO:0097053), biosynthetic process (GO:0009058)

GO Molecular Function (9): L-kynurenine:2-oxoglutarate transaminase activity (GO:0016212), pyridoxal phosphate binding (GO:0030170), protein homodimerization activity (GO:0042803), L-glutamine:phenylpyruvate transaminase activity (GO:0047316), cysteine-S-conjugate beta-lyase activity (GO:0047804), protein binding (GO:0005515), transaminase activity (GO:0008483), transferase activity (GO:0016740), lyase activity (GO:0016829)

GO Cellular Component (3): cytoplasm (GO:0005737), mitochondrion (GO:0005739), cytosol (GO:0005829)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Metabolism of amino acids and derivatives	3
Phenylalanine and tyrosine metabolism	1
Metabolism	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
catalytic activity	2
cellular anatomical structure	2
cytoplasm	2
response to other organism	1
metabolic process	1
transaminase activity	1
anion binding	1
vitamin B6 binding	1
identical protein binding	1
protein dimerization activity	1
amino acid transaminase activity	1
carbon-sulfur lyase activity	1
binding	1
transferase activity, transferring nitrogenous groups	1
intracellular anatomical structure	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

1734 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
KYAT1	AADAT	Q8N5Z0	995
KYAT1	SPOUT1	Q5T280	906
KYAT1	TBC1D13	Q9NVG8	901
KYAT1	KMO	O15229	795
KYAT1	ENDOG	Q14249	783
KYAT1	KYNU	Q16719	774
KYAT1	GOT2	P00505	717
KYAT1	HAAO	P46952	716
KYAT1	TDO2	P48775	712
KYAT1	QPRT	Q15274	668
KYAT1	AFMID	Q63HM1	658
KYAT1	GPR35	Q9HC97	627
KYAT1	IDO1	P14902	623
KYAT1	TRABD2B	A6NFA1	583
KYAT1	IDO2	Q6ZQW0	567

IntAct

12 interactions, top by confidence:

A	B	Type	Score
VAC14	KYAT1	psi-mi:“MI:0915”(physical association)	0.670
KYAT1	VAC14	psi-mi:“MI:0915”(physical association)	0.670
KYAT1	TRIP13	psi-mi:“MI:0915”(physical association)	0.560
TRIP13	KYAT1	psi-mi:“MI:0915”(physical association)	0.560
GRIN2C	KYAT1	psi-mi:“MI:0915”(physical association)	0.400
ECE1	KYAT1	psi-mi:“MI:0915”(physical association)	0.370
KYAT1	ZNF318	psi-mi:“MI:0914”(association)	0.350
KYAT1	IGHG1	psi-mi:“MI:0914”(association)	0.350

BioGRID (24): TRIP13 (Two-hybrid), VAC14 (Two-hybrid), CCBL1 (Affinity Capture-RNA), CCBL1 (Affinity Capture-RNA), CCBL1 (Co-fractionation), ZNF318 (Affinity Capture-MS), YEATS2 (Affinity Capture-MS), ZZZ3 (Affinity Capture-MS), MBIP (Affinity Capture-MS), CCBL1 (Two-hybrid), CCBL1 (Two-hybrid), CCBL1 (Two-hybrid), ZZZ3 (Affinity Capture-MS), YEATS2 (Affinity Capture-MS), MBIP (Affinity Capture-MS)

ESM2 similar proteins: A0A0P0UZP7, A0A0P0VI36, A0A0P0WIY3, A2XFC1, A2XLL2, A2YTP9, A4IFH5, C6JS30, P18485, P23279, P23599, P24298, P27486, P31531, P37821, Q00257, Q00379, Q01912, Q06402, Q06429, Q07262, Q0DKE8, Q0DSV9, Q0DWQ1, Q10DK7, Q16773, Q28DB5, Q37001, Q42881, Q43309, Q43654, Q58CZ9, Q5VQG8, Q5W6F9, Q6GM82, Q6NYL5, Q6UTZ2, Q7T3E5, Q7XQ85, Q8BGT5

Diamond homologs: A1ADA5, A1VDD3, A3PMF8, A4QAL4, A7ZP71, A8A2C0, A9N5B4, B1I544, B1IXT4, B1X8W6, B2A250, B4SYW9, B4TBG4, B4TPI0, B5BCP8, B5EZH6, B5FNT7, B5R270, B5RCC2, B6I7J6, B7LAR8, B7LM78, B7M5T5, B7MG20, B7MXT4, B7N5L8, B7NNT2, B7UFR5, B8DJJ6, C0Q071, C4ZU95, C6BUK3, C6C2Z3, E9L7A5, H3ZPU1, O31665, O33822, O58489, O67781, O86459

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

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

Top pathogenic / likely-pathogenic (0)

SpliceAI

5200 predictions. Top by Δscore:

Variant	Effect	Δscore
9:128820737:A:AC	acceptor_loss	1.0000
9:128820737:A:AG	acceptor_gain	1.0000
9:128820738:G:GG	acceptor_gain	1.0000
9:128823902:A:C	acceptor_gain	1.0000
9:128824764:T:TA	donor_gain	1.0000
9:128824767:TTA:T	donor_loss	1.0000
9:128824768:TA:T	donor_loss	1.0000
9:128824769:A:AC	donor_gain	1.0000
9:128824769:ACT:A	donor_loss	1.0000
9:128824770:C:CA	donor_gain	1.0000
9:128824770:CT:C	donor_gain	1.0000
9:128824770:CTG:C	donor_gain	1.0000
9:128824770:CTGAG:C	donor_gain	1.0000
9:128824968:T:A	donor_gain	1.0000
9:128824973:ATAC:A	donor_loss	1.0000
9:128824974:TACC:T	donor_loss	1.0000
9:128824975:ACCTG:A	donor_loss	1.0000
9:128824976:C:A	donor_loss	1.0000
9:128825047:CTC:C	acceptor_gain	1.0000
9:128826016:TCCTA:T	donor_loss	1.0000
9:128826017:CCTAC:C	donor_loss	1.0000
9:128826018:CTA:C	donor_loss	1.0000
9:128826019:TAC:T	donor_loss	1.0000
9:128826020:A:T	donor_loss	1.0000
9:128826021:C:CA	donor_loss	1.0000
9:128826150:GCC:G	acceptor_gain	1.0000
9:128826151:CC:C	acceptor_gain	1.0000
9:128826151:CCC:C	acceptor_gain	1.0000
9:128826152:CC:C	acceptor_gain	1.0000
9:128826153:C:CC	acceptor_gain	1.0000

AlphaMissense

2821 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
9:128835862:A:G	W258R	0.996
9:128835862:A:T	W258R	0.996
9:128836002:A:G	W254R	0.994
9:128836002:A:T	W254R	0.994
9:128835573:C:G	R317P	0.993
9:128833740:C:A	K403N	0.992
9:128833740:C:G	K403N	0.992
9:128833749:A:C	C400W	0.992
9:128836853:C:G	D213H	0.992
9:128838114:A:C	F125L	0.992
9:128838114:A:T	F125L	0.992
9:128838116:A:G	F125L	0.992
9:128836030:G:C	S244R	0.991
9:128836030:G:T	S244R	0.991
9:128836032:T:G	S244R	0.991
9:128836852:T:A	D213V	0.991
9:128833756:C:G	R398P	0.990
9:128835506:G:C	F339L	0.990
9:128835506:G:T	F339L	0.990
9:128835508:A:G	F339L	0.990
9:128837697:G:C	N185K	0.990
9:128837697:G:T	N185K	0.990
9:128835512:G:C	S337R	0.989
9:128835512:G:T	S337R	0.989
9:128835514:T:G	S337R	0.989
9:128836853:C:A	D213Y	0.988
9:128837716:A:T	V179D	0.988
9:128836862:A:G	C210R	0.987
9:128836852:T:G	D213A	0.986
9:128835552:A:G	L324P	0.985

dbSNP variants (sampled 300 via entrez): RS1000269770 (9:128866458 G>A), RS1000270972 (9:128868689 A>C), RS1000271816 (9:128837114 A>T), RS1000411635 (9:128843098 C>A,T), RS1000424572 (9:128860583 T>G), RS1000447903 (9:128847718 C>T), RS1000580338 (9:128864394 A>C,T), RS1000604085 (9:128835617 G>A,C), RS1000629123 (9:128879881 G>A,C), RS1000652862 (9:128877826 T>C), RS1000724028 (9:128879136 C>G), RS1000754412 (9:128883742 A>C), RS1000754929 (9:128860264 T>A), RS1000825894 (9:128841453 G>A), RS1000896186 (9:128842782 C>A)

Disease associations

OMIM: gene MIM:600547 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

9 associations (top):

Study	Trait	p-value
GCST006879_1	Blood metabolite levels	1.000000e-09
GCST006879_18	Blood metabolite levels	3.000000e-43
GCST006879_19	Blood metabolite levels	4.000000e-83
GCST006879_2	Blood metabolite levels	2.000000e-12
GCST006879_20	Blood metabolite levels	5.000000e-12
GCST006879_21	Blood metabolite levels	2.000000e-22
GCST006879_22	Blood metabolite levels	2.000000e-20
GCST012020_521	Serum metabolite levels	4.000000e-11
GCST012021_62	Serum metabolite levels	4.000000e-11

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3962 (SINGLE PROTEIN)

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — Hydrogen sulphide synthesis

Binding affinities (BindingDB)

2 measured of 2 human assays (2 total across all organisms); most potent 2 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
Acid, 7	IC50	140000 nM
DL-indole-3-lactic acid	IC50	220000 nM

ChEMBL bioactivities

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

pChembl	Type	Value	Unit	Molecule
5.69	IC50	2040	nM	CHEMBL2321944

PubChem BioAssay actives

1 with measured affinity, of 98 total; 1 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
(3S)-3-amino-1-hydroxy-6-phenoxy-3,4-dihydroquinolin-2-one	727189: Inhibition of human KAT1 using L-kynurenine as substrate measured after 16 hrs by SpectraMax plate reader analysis	ic50	2.0400	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Air Pollutants	decreases expression, increases abundance, increases expression	2
Cisplatin	increases expression, affects expression, affects cotreatment	2
Aflatoxin B1	increases methylation, decreases expression	2
lanthionine	increases amination	1
bismuth tripotassium dicitrate	decreases expression	1
bisphenol A	decreases methylation	1
senecionine	decreases expression	1
beta-lapachone	decreases expression	1
tris(1,3-dichloro-2-propyl)phosphate	decreases expression	1
cobaltous chloride	decreases expression	1
methylmercury cysteine	increases amination, decreases activity	1
S-(1,2-dichlorovinyl)cysteine	decreases reaction, increases expression	1
avobenzone	increases expression	1
di-n-butylphosphoric acid	affects expression	1
perfluorooctane sulfonic acid	decreases expression	1
pentabromodiphenyl ether	increases expression	1
K 7174	decreases expression	1
jinfukang	affects cotreatment, increases expression	1
Decitabine	affects expression	1
Sunitinib	decreases expression	1
Allergens	increases expression	1
Benzo(a)pyrene	decreases expression	1
Cannabidiol	decreases expression	1
Coal	increases abundance, increases expression	1
Cystathionine	increases amination	1
Cysteine	affects cotreatment, increases amination	1
Cystine	increases amination	1
Colforsin	increases expression, decreases reaction	1
Mercuric Chloride	affects cotreatment, increases amination	1
Methionine	increases amination	1

ChEMBL screening assays

14 unique, capped per target: 14 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1002981	Binding	Inhibition of human recombinant KAT1 expressed in Sf9 cells assessed as decrease in enzyme activity at 25 % ligand concentration	Structural insight into the inhibition of human kynurenine aminotransferase I/glutamine transaminase K. — J Med Chem

Clinical trials (associated diseases)

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