CYP4A11

Summary

CYP4A11 (cytochrome P450 family 4 subfamily A member 11, HGNC:2642) is a protein-coding gene on chromosome 1p33, encoding Cytochrome P450 4A11 (Q02928). A cytochrome P450 monooxygenase involved in the metabolism of fatty acids and their oxygenated derivatives (oxylipins).

This gene encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. This protein localizes to the endoplasmic reticulum and hydroxylates medium-chain fatty acids such as laurate and myristate. Multiple transcript variants have been found for this gene.

Source: NCBI Gene 1579 — RefSeq curated summary.

At a glance

• GWAS associations: 11
• Clinical variants (ClinVar): 101 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000778

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:2642
Approved symbol	CYP4A11
Name	cytochrome P450 family 4 subfamily A member 11
Location	1p33
Locus type	gene with protein product
Status	Approved
Aliases	CYP4AII
Ensembl gene	ENSG00000187048
Ensembl biotype	protein_coding
OMIM	601310
Entrez	1579

Gene structure

Transcript identifiers

Ensembl transcripts: 45 — 40 protein_coding, 4 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000310638, ENST00000371905, ENST00000462347, ENST00000465874, ENST00000468629, ENST00000474458, ENST00000475477, ENST00000496519, ENST00000909022, ENST00000909023, ENST00000909024, ENST00000909025, ENST00000909026, ENST00000909027, ENST00000909028, ENST00000909029, ENST00000909030, ENST00000909031, ENST00000909032, ENST00000909033, ENST00000909034, ENST00000909035, ENST00000909036, ENST00000909037, ENST00000909038, ENST00000909039, ENST00000909040, ENST00000909041, ENST00000909042, ENST00000909043, ENST00000909044, ENST00000909045, ENST00000909046, ENST00000909047, ENST00000909048, ENST00000909049, ENST00000909050, ENST00000909051, ENST00000909052, ENST00000909053, ENST00000909054, ENST00000909055, ENST00000909056, ENST00000909057, ENST00000909058

RefSeq mRNA: 3 — MANE Select: NM_000778 NM_000778, NM_001319155, NM_001363587

CCDS: CCDS543, CCDS85973

Canonical transcript exons

ENST00000310638 — 12 exons

Exon	Start	End
ENSE00001668297	46935000	46935154
ENSE00001823232	46941239	46941476
ENSE00003464743	46929188	46930310
ENSE00003702632	46932761	46932837
ENSE00003702714	46934176	46934366
ENSE00003703300	46933946	46934079
ENSE00003705717	46936664	46936791
ENSE00003706092	46937302	46937346
ENSE00003706637	46932983	46933047
ENSE00003707341	46935523	46935647
ENSE00003708613	46937996	46938137
ENSE00003710677	46934453	46934559

Expression profiles

Bgee: expression breadth ubiquitous, 117 present calls, max score 99.18.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.2421 / max 74.3163, expressed in 13 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
12208	0.1623	13
12207	0.0550	11
12206	0.0192	8
201501	0.0055	5

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right lobe of liver	UBERON:0001114	99.18	gold quality
liver	UBERON:0002107	98.88	gold quality
adult mammalian kidney	UBERON:0000082	94.68	gold quality
kidney	UBERON:0002113	87.97	gold quality
calcaneal tendon	UBERON:0003701	83.75	gold quality
sural nerve	UBERON:0015488	83.51	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	79.48	gold quality
cortex of kidney	UBERON:0001225	74.55	gold quality
metanephros cortex	UBERON:0010533	72.79	gold quality
duodenum	UBERON:0002114	66.47	gold quality
cortical plate	UBERON:0005343	64.70	gold quality
gall bladder	UBERON:0002110	63.68	gold quality
colonic epithelium	UBERON:0000397	63.06	silver quality
subcutaneous adipose tissue	UBERON:0002190	60.63	gold quality
adipose tissue	UBERON:0001013	56.15	gold quality
superior frontal gyrus	UBERON:0002661	55.45	gold quality
skeletal muscle tissue	UBERON:0001134	55.29	gold quality
hypothalamus	UBERON:0001898	53.96	gold quality
tibial nerve	UBERON:0001323	53.71	gold quality
thoracic mammary gland	UBERON:0005200	53.61	gold quality
nucleus accumbens	UBERON:0001882	53.11	gold quality
right lung	UBERON:0002167	52.77	gold quality
body of stomach	UBERON:0001161	52.61	gold quality
small intestine	UBERON:0002108	52.10	gold quality
muscle tissue	UBERON:0002385	51.79	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	51.56	gold quality
small intestine Peyer’s patch	UBERON:0003454	51.25	gold quality
hindlimb stylopod muscle	UBERON:0004252	50.97	gold quality
muscle of leg	UBERON:0001383	50.92	gold quality
stomach	UBERON:0000945	50.90	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	6.42

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): JUN, POU2F1, PPARA

miRNA regulators (miRDB)

37 targeting CYP4A11, 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-4692	100.00	67.32	2066
HSA-MIR-4514	99.99	67.10	1870
HSA-MIR-150-5P	99.99	66.69	1976
HSA-MIR-6721-5P	99.93	68.92	2981
HSA-MIR-4496	99.88	68.89	2236
HSA-MIR-4447	99.85	67.81	2900
HSA-MIR-629-3P	99.85	67.99	1875
HSA-MIR-6842-5P	99.80	67.54	1587
HSA-MIR-7110-5P	99.80	67.84	1712
HSA-MIR-4713-5P	99.78	67.80	1794
HSA-MIR-4524A-3P	99.72	66.85	2406
HSA-MIR-3934-5P	99.67	64.04	846
HSA-MIR-4690-5P	99.65	66.24	813
HSA-MIR-6752-5P	99.59	67.32	1243
HSA-MIR-4472	99.56	66.08	1478
HSA-MIR-4519	99.48	66.10	859
HSA-MIR-1324	99.46	66.57	1302
HSA-MIR-940	99.37	66.14	2064
HSA-MIR-6808-5P	99.31	66.23	2150
HSA-MIR-6893-5P	99.31	66.25	2119
HSA-MIR-10399-5P	99.17	69.87	2610
HSA-MIR-6504-3P	99.17	69.31	2891
HSA-MIR-4254	99.11	65.15	1315
HSA-MIR-3154	98.94	66.55	1455
HSA-MIR-887-5P	98.82	65.90	1347
HSA-MIR-34B-3P	98.70	67.40	1171
HSA-MIR-4717-5P	98.19	67.97	894
HSA-MIR-3129-3P	97.85	67.63	1246
HSA-MIR-5583-5P	97.85	67.61	1243
HSA-MIR-7855-5P	97.39	67.18	925

Literature-anchored findings (GeneRIF, showing 40)

• CYP4A11 expression can be induced by glucocorticoids and peroxisome proliferators (PMID:12464261)
• gene and protein analysis of CYP4A11 show that it is expressed in kidney (PMID:12464262)
• A variant of the human CYP4A11 (T8590C) encodes for a monooxygenase with reduced 20-HETE synthase activity. The association of the T8590C variant with hypertension supports its role as a polygenic determinant of blood pressure control in humans. (PMID:15611369)
• Our data strengthen the association between the T8590C polymorphism of CYP4A11 and hypertension and suggest a recessive mode of inheritance. (PMID:16144986)
• Genetic (T8590C) and environmental (insulin) factors impair 20-HETE responses to salt in human hypertension. The T8590C polymorphism of CYP4A11 encodes an enzyme with reduced catalytic activity. (PMID:18227405)
• Essential hypertension is associated with the TC + TT genotype of rs1126742 in the human CYP4A11 gene (PMID:18300855)
• The CYP4A11 8590CC genotype is associated with increased blood pressure in black men with hypertensive nephrosclerosis and is associated with adverse clinical outcomes in those with baseline proteinuria. (PMID:18385420)
• In humans that polymorphisms of the CYP4F2 and CYP4A11 genes have opposite effects on 20-hydroxyeicosatetraenoic acid excretion. (PMID:18391101)
• a functional variant (-845A/G) of CYP4A11 is significantly associated with hypertension and appears to be a novel candidate for a predisposing factor for hypertension (PMID:18936345)
• PPARalpha contributes to the maintenance of basal CYP4A11 expression and mediates CYP4A11 induction in response to fibrates or fasting; increased exposure to growth hormone down-regulates CYP4A11 expression in liver (PMID:19366684)
• In patients with established and stable coronary artery disease the 434SS variant of CYP4A11 F434 is associated with pronounced coronary vasoconstriction. (PMID:19615687)
• Association of common variants of CYP4A11 with stroke in Han Chinese population is reported. (PMID:20130494)
• In normotensive individuals, the CYP4A11 rs4660980 polymophism was associated with both systolic and diastolic blood pressure in men. A common variant on CYP4A11 was associated with blood pressure in a Chinese population. (PMID:21326303)
• We confirmed that the CYP4A11 (8590T>C) functional polymorphism exhibits inter-ethnic frequency differences and an association with hypertension. (PMID:21617944)
• Data suggest that results could be helpful for further investigations of the potential role of CYP4A variants in the genetic susceptibility to cardiovascular diseases such as arterial hypertension. (PMID:21820496)
• The loss-of-function CYP4A11 8590C allele is associated with a diagnosis of hypertension and, in normotensive individuals, with higher blood pressure regardless of salt intake. (PMID:21873888)
• The CYP4A11 8590C allele was also associated with low HDL-C in women. (PMID:21912424)
• rs3890011 maybe a novel polymorphism of the CYP4A11 gene associated with CAD in a Han Chinese population. (PMID:22327816)
• Single-nucleotide polymorphisms of the human CYP4A11 gene appear to have no association with myocardial infarction in Japanese. (PMID:22804341)
• The GG genotype of rs3890011 and the G-G-T haplotype in the CYP4A11 gene could be a useful genetic marker of CAD in Han populations in China. (PMID:23085321)
• This meta-analysis revealed that the RGS2 1891-1892del TC polymorphism and CYP4A11 T8590C polymorphism were associated with hypertension risk. (PMID:23859711)
• The CC genotype and C allele of the CYP4A11 gene were associated with essential hypertension in the male western Chinese Han population. (PMID:24164311)
• suggests there is a significant association between the CYP4A11 T8590C variant and essential hypertension, especially in Caucasians. The case-control study did not find a significant association among the Han Chinese population (PMID:24278241)
• The results suggest that the CYP4A11 GG genotype was a high risk factor for hypertension. (PMID:24535879)
• This meta-analysis suggests the CYP4A11 T8590C polymorphism may be a risk factor for hypertension. (PMID:24931260)
• individuals homozygous for the CYP4A11 rs3890011 C allele, blood pressure is resistant to mineralocorticoid receptor antagonism, but sensitive to ENaC inhibition, consistent with ENaC activation. (PMID:25064769)
• Results indicate that both the transfer of an electron to the ferrous.O2 complex and C-H bond-breaking limit the rate of CYP4A11 ( cytochrome P450 4A11) omega-oxidation. (PMID:25203493)
• To evaluate the associations between four single-nucleotide polymorphisms (SNPs) in CYP4A11 and CYP4F2 and ischemic stroke (IS) (PMID:25734770)
• The present study focused on 10 CYP4A11 variant alleles and evaluated their functional characteristics using arachidonic acid as the substrate in a COS-7 cell-based expression system. (PMID:25760539)
• Interaction among CYP2C8, EPHX2, and CYP4A11 Gene Variants Significantly Increases the Risk for Ischemic Stroke. (PMID:25947240)
• Single nucleotide polymorphism of CYP4A11 gene is associated with Plaque in Patients with Ischemic Stroke. (PMID:26423716)
• CYP4A1l rs9333025 GG and CYP4F2 rs2108622 GG two-loci interaction significantly increases the risk for IS and an elevated 20-HETE level. (PMID:26959478)
• CYP4A11 Variants are associated with Ischemic Stroke. (PMID:27087514)
• These results point to a potential 20-HETE dependence of intrarenal angiotensinogen production and ANGII receptor type 1 activation that are associated with increases in NCC and SGK1 and identify elevated P450 4A11 activity and 20-HETE as potential risk factors for salt-sensitive human hypertension by perturbation of the renal renin-angiotensin axis. (PMID:27298316)
• The DEGs, such as AGTR1, CYP3A4 and CYP4A11 may play critical roles in the development of HTN likely via the regulation by hsa-miR-26b-5p and taking part in some pathways. (PMID:27756246)
• The results suggest that individuals carrying the alleles, K276T and S353G, might exhibit higher catalysis of CYP4A11 (PMID:27793475)
• Heme-thiolate sulfenylation of human cytochrome P450 4A11 functions as a redox switch for catalytic inhibition. (PMID:28533430)
• Gene-gene interaction between rs1126742 and rs3890011 and gene-environment interaction between rs1126742 and smoking were associated with increased EH risk. (PMID:28534704)
• Haplotype G-C-A of CYP4A11 was associated with increased risk of coronary artery disease. (PMID:29484037)
• The rs1126742 T/C polymorphism of CYP4A11 is more likely to be a genetic risk factor for the hypertension cases in the Caucasian population. Moreover, whereas the AG genotype of CYP4A11 rs9332978 may be associated with an increased risk of hypertension, the AA genotype of rs9333025 may be linked to a decreased risk of cardiovascular and cerebrovascular diseases. [meta-analysis] (PMID:30132788)

Cross-species orthologs

36 orthologs

Organism	Symbol	Gene ID
danio_rerio	cyp4t8	ENSDARG00000004964
danio_rerio	cyp4f3	ENSDARG00000053530
mus_musculus	Cyp4a31	ENSMUSG00000028712
mus_musculus	Cyp4a32	ENSMUSG00000063929
mus_musculus	Cyp4a10	ENSMUSG00000066072
mus_musculus	Cyp4a30b	ENSMUSG00000084346
rattus_norvegicus	Cyp4a1	ENSRNOG00000009597
rattus_norvegicus	Cyp4a3	ENSRNOG00000066878
drosophila_melanogaster	Cyp4d1	FBGN0005670
drosophila_melanogaster	Cyp4d2	FBGN0011576
drosophila_melanogaster	Cyp4e2	FBGN0014469
drosophila_melanogaster	Cyp4c3	FBGN0015032
drosophila_melanogaster	Cyp4d8	FBGN0015033
drosophila_melanogaster	Cyp4e1	FBGN0015034
drosophila_melanogaster	Cyp4e3	FBGN0015035
drosophila_melanogaster	Cyp4ae1	FBGN0015036
drosophila_melanogaster	Cyp4p1	FBGN0015037
drosophila_melanogaster	Cyp4d14	FBGN0023541
drosophila_melanogaster	Cyp4s3	FBGN0030615
drosophila_melanogaster	Cyp4ac1	FBGN0031693
drosophila_melanogaster	Cyp4ac2	FBGN0031694
drosophila_melanogaster	Cyp4ac3	FBGN0031695
drosophila_melanogaster	Cyp4d21	FBGN0031925
drosophila_melanogaster	Cyp4ad1	FBGN0033292
drosophila_melanogaster	Cyp4p2	FBGN0033395
drosophila_melanogaster	Cyp4p3	FBGN0033397
drosophila_melanogaster	Cyp4aa1	FBGN0034053
drosophila_melanogaster	Cyp4d20	FBGN0035344
drosophila_melanogaster	Cyp312a1	FBGN0036778
caenorhabditis_elegans		WBGENE00007140
caenorhabditis_elegans		WBGENE00009226
caenorhabditis_elegans		WBGENE00010354
caenorhabditis_elegans		WBGENE00013381
caenorhabditis_elegans		WBGENE00016147
caenorhabditis_elegans		WBGENE00021200
caenorhabditis_elegans		WBGENE00021412

Paralogs (12): CYP19A1 (ENSG00000137869), CYP4B1 (ENSG00000142973), CYP4V2 (ENSG00000145476), CYP4A22 (ENSG00000162365), CYP4F11 (ENSG00000171903), CYP4F22 (ENSG00000171954), CYP4F2 (ENSG00000186115), CYP4Z1 (ENSG00000186160), CYP4F12 (ENSG00000186204), CYP4X1 (ENSG00000186377), CYP4F8 (ENSG00000186526), CYP4F3 (ENSG00000186529)

Protein

Protein identifiers

Cytochrome P450 4A11 — Q02928 (reviewed: Q02928)

Alternative names: 20-hydroxyeicosatetraenoic acid synthase, CYP4AII, CYPIVA11, Cytochrome P-450HK-omega, Cytochrome P450HL-omega, Fatty acid omega-hydroxylase, Lauric acid omega-hydroxylase, Long-chain fatty acid omega-monooxygenase

All UniProt accessions (7): A0A0C4DFV7, Q02928, V9GY41, V9GYC6, V9GYK4, V9GYQ2, V9GZ77

UniProt curated annotations — full annotation on UniProt →

Function. A cytochrome P450 monooxygenase involved in the metabolism of fatty acids and their oxygenated derivatives (oxylipins). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (CPR; NADPH-ferrihemoprotein reductase). Catalyzes predominantly the oxidation of the terminal carbon (omega-oxidation) of saturated and unsaturated fatty acids, the catalytic efficiency decreasing in the following order: dodecanoic > tetradecanoic > (9Z)-octadecenoic > (9Z,12Z)-octadecadienoic > hexadecanoic acid. Acts as a major omega-hydroxylase for dodecanoic (lauric) acid in liver. Participates in omega-hydroxylation of (5Z,8Z,11Z,14Z)-eicosatetraenoic acid (arachidonate) to 20-hydroxyeicosatetraenoic acid (20-HETE), a signaling molecule acting both as vasoconstrictive and natriuretic with overall effect on arterial blood pressure. Can also catalyze the oxidation of the penultimate carbon (omega-1 oxidation) of fatty acids with lower efficiency. May contribute to the degradation of saturated very long-chain fatty acids (VLCFAs) such as docosanoic acid, by catalyzing successive omega-oxidations to the corresponding dicarboxylic acid, thereby initiating chain shortening. Omega-hydroxylates (9R,10S)-epoxy-octadecanoate stereoisomer. Plays a minor role in omega-oxidation of long-chain 3-hydroxy fatty acids. Has little activity toward prostaglandins A1 and E1.

Subcellular location. Endoplasmic reticulum membrane. Microsome membrane.

Tissue specificity. Expressed in liver. Expressed in S2 and S3 segments of proximal tubules in cortex and outer medulla of kidney.

Activity regulation. Activated by cytochrome b5.

Pathway. Lipid metabolism; arachidonate metabolism. Lipid metabolism; oxylipin biosynthesis.

Polymorphism. CYP4A11v seems to be a rare allelic variant of CYP4A11, it seems to be unstable and not to metabolize lauric acid.

Similarity. Belongs to the cytochrome P450 family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q02928-1	1	yes
Q02928-2	2

RefSeq proteins (3): NP_000769, NP_001306084, NP_001350516 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001128	Cyt_P450	Family
IPR002401	Cyt_P450_E_grp-I	Family
IPR017972	Cyt_P450_CS	Conserved_site
IPR036396	Cyt_P450_sf	Homologous_superfamily
IPR050196	Cytochrome_P450_Monoox	Family

Pfam: PF00067

Enzyme classification (BRENDA):

• EC 1.14.14.80 — long-chain fatty acid omega-monooxygenase (BRENDA: 7 organisms, 59 substrates, 1 inhibitors, 46 Km, 39 kcat entries)

Substrate kinetics (BRENDA)

6 substrates with measured Km, best-characterized 6. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ARACHIDONIC ACID	0.003–0.25	11
MYRISTIC ACID	0.004–0.07	11
LAURIC ACID	0.019–0.14	10
PALMITIC ACID	0.014–0.43	8
OLEIC ACID	0.018–0.136	4
LINOLEIC ACID	0.068	1

Catalyzed reactions (Rhea), 11 shown:

• an organic molecule + reduced [NADPH–hemoprotein reductase] + O2 = an alcohol + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:17149)
• dodecanoate + reduced [NADPH–hemoprotein reductase] + O2 = 12-hydroxydodecanoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:38947)
• 22-oxodocosanoate + reduced [NADPH–hemoprotein reductase] + O2 = docosanedioate + oxidized [NADPH–hemoprotein reductase] + H2O + 2 H(+) (RHEA:39043)
• 22-hydroxydocosanoate + reduced [NADPH–hemoprotein reductase] + O2 = 22-oxodocosanoate + oxidized [NADPH–hemoprotein reductase] + 2 H2O + H(+) (RHEA:39055)
• 3-hydroxyhexadecanoate + reduced [NADPH–hemoprotein reductase] + O2 = 3,16-dihydroxyhexadecanoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:39731)
• (5Z,8Z,11Z,14Z)-eicosatetraenoate + reduced [NADPH–hemoprotein reductase] + O2 = 20-hydroxy-(5Z,8Z,11Z,14Z)-eicosatetraenoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:39755)
• hexadecanoate + reduced [NADPH–hemoprotein reductase] + O2 = 16-hydroxyhexadecanoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:40199)
• tetradecanoate + reduced [NADPH–hemoprotein reductase] + O2 = 14-hydroxytetradecanoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:40203)
• (9Z)-octadecenoate + reduced [NADPH–hemoprotein reductase] + O2 = 18-hydroxy-(9Z)-octadecenoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:41728)
• (9R,10S)-epoxy-octadecanoate + reduced [NADPH–hemoprotein reductase] + O2 = 18-hydroxy-(9R,10S)-epoxy-octadecanoate + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:53556)
• an omega-methyl-long-chain fatty acid + reduced [NADPH–hemoprotein reductase] + O2 = an omega-hydroxy-long-chain fatty acid + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:56748)

UniProt features (16 total): sequence conflict 4, sequence variant 4, mutagenesis site 2, binding site 2, propeptide 1, chain 1, modified residue 1, splice variant 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q02928-F1	91.54	0.80

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 (2): 321 (covalent); 457 (axial binding residue)

Post-translational modifications (1): 440

Mutagenesis-validated functional residues (2):

Position	Phenotype
130	loss of activity.
321	loss of covalent heme binding.

Function

Pathways and Gene Ontology

Reactome pathways

6 pathways

ID	Pathway
R-HSA-1989781	PPARA activates gene expression
R-HSA-211935	Fatty acids
R-HSA-211958	Miscellaneous substrates
R-HSA-211979	Eicosanoids
R-HSA-2142691	Synthesis of Leukotrienes (LT) and Eoxins (EX)
R-HSA-2142816	Synthesis of (16-20)-hydroxyeicosatetraenoic acids (HETE)

MSigDB gene sets: 195 (showing top): MODULE_93, GOBP_FATTY_ACID_CATABOLIC_PROCESS, REACTOME_BIOLOGICAL_OXIDATIONS, GOBP_REGULATION_OF_ICOSANOID_SECRETION, GOBP_REGULATION_OF_BLOOD_PRESSURE, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOBP_REGULATION_OF_ORGANIC_ACID_TRANSPORT, GOMF_OXIDOREDUCTASE_ACTIVITY_ACTING_ON_PAIRED_DONORS_WITH_INCORPORATION_OR_REDUCTION_OF_MOLECULAR_OXYGEN, GNF2_GSTM1, GOBP_RENAL_SYSTEM_PROCESS_INVOLVED_IN_REGULATION_OF_BLOOD_VOLUME, GNF2_HPN, GOBP_REGULATION_OF_SYSTEMIC_ARTERIAL_BLOOD_PRESSURE, GOBP_LONG_CHAIN_FATTY_ACID_METABOLIC_PROCESS, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, GOBP_ORGANIC_ACID_BIOSYNTHETIC_PROCESS

GO Biological Process (17): long-chain fatty acid metabolic process (GO:0001676), kidney development (GO:0001822), renal water homeostasis (GO:0003091), pressure natriuresis (GO:0003095), fatty acid metabolic process (GO:0006631), leukotriene metabolic process (GO:0006691), arachidonate metabolic process (GO:0019369), epoxygenase P450 pathway (GO:0019373), oxylipin biosynthetic process (GO:0031408), positive regulation of icosanoid secretion (GO:0032305), linoleic acid metabolic process (GO:0043651), icosanoid biosynthetic process (GO:0046456), lauric acid metabolic process (GO:0048252), sodium ion homeostasis (GO:0055078), omega-hydroxylase P450 pathway (GO:0097267), lipid metabolic process (GO:0006629), leukotriene B4 catabolic process (GO:0036101)

GO Molecular Function (13): monooxygenase activity (GO:0004497), iron ion binding (GO:0005506), arachidonate monooxygenase activity (GO:0008391), arachidonate epoxygenase activity (GO:0008392), alkane 1-monooxygenase activity (GO:0018685), heme binding (GO:0020037), leukotriene-B4 20-monooxygenase activity (GO:0050051), arachidonate omega-hydroxylase activity (GO:0052869), long-chain fatty acid omega-hydroxylase activity (GO:0102033), oxidoreductase activity (GO:0016491), oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen (GO:0016705), oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen (GO:0016712), metal ion binding (GO:0046872)

GO Cellular Component (6): cytoplasm (GO:0005737), endoplasmic reticulum membrane (GO:0005789), apical plasma membrane (GO:0016324), intracellular membrane-bounded organelle (GO:0043231), endoplasmic reticulum (GO:0005783), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Cytochrome P450 - arranged by substrate type	3
Arachidonate metabolism	2
Regulation of lipid metabolism by PPARalpha	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
icosanoid metabolic process	3
renal system process	2
long-chain fatty acid metabolic process	2
unsaturated fatty acid metabolic process	2
olefinic compound metabolic process	2
arachidonate metabolic process	2
carboxylic acid biosynthetic process	2
oxidoreductase activity	2
monooxygenase activity	2
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen	2
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	2
intracellular anatomical structure	2
cellular anatomical structure	2
fatty acid metabolic process	1
animal organ development	1
renal system development	1
multicellular organismal-level water homeostasis	1
regulation of body fluid levels	1
lipid metabolic process	1
monocarboxylic acid metabolic process	1
oxylipin metabolic process	1
regulation of icosanoid secretion	1
icosanoid secretion	1
positive regulation of secretion	1
positive regulation of fatty acid transport	1
medium-chain fatty acid metabolic process	1
monoatomic cation homeostasis	1
inorganic ion homeostasis	1
primary metabolic process	1
leukotriene catabolic process	1
leukotriene B4 metabolic process	1
long-chain fatty acid catabolic process	1
icosanoid catabolic process	1
transition metal ion binding	1
arachidonate monooxygenase activity	1
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced iron-sulfur protein as one donor, and incorporation of one atom of oxygen	1
tetrapyrrole binding	1
leukotriene B4 catabolic process	1
fatty acid omega-hydroxylase activity	1
catalytic activity	1

Protein interactions and networks

STRING

1858 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CYP4A11	SCNN1D	P51172	815
CYP4A11	B3GAT2	Q9NPZ5	725
CYP4A11	PPIG	Q13427	662
CYP4A11	MEX3C	Q5U5Q3	548
CYP4A11	GNB3	P16520	546
CYP4A11	ERAP1	Q9NZ08	546
CYP4A11	CYP2A6	P00190	538
CYP4A11	ADD1	P35611	536
CYP4A11	EPHX2	P34913	536
CYP4A11	ATP1B1	P05026	532
CYP4A11	CYP1A2	P05177	521
CYP4A11	PLA2G1B	P04054	518
CYP4A11	PPARA	Q07869	502
CYP4A11	ACE	P12821	499
CYP4A11	KCNMB1	P78475	493

IntAct

3 interactions, top by confidence:

A	B	Type	Score
CYP4A22	CYP4A11	psi-mi:“MI:0915”(physical association)	0.400
PIK3R5	CYP4A11	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (5): CYP4A11 (Affinity Capture-MS), CYP4A11 (Two-hybrid), PDR (Biochemical Activity), CYB5A (Biochemical Activity), CYP4A11 (Co-purification)

ESM2 similar proteins: A2A974, O35728, O88833, P00184, P00186, P04799, P08516, P08684, P10611, P13584, P14579, P14581, P15128, P15129, P20815, P20816, P20817, P24453, P24462, P24463, P24464, P33268, P51869, P56592, P78329, P79102, P79401, Q00557, Q02928, Q06367, Q08477, Q0IIF9, Q29496, Q3LFT9, Q4V8D1, Q5KQT6, Q5TCH4, Q64391, Q64462, Q64464

Diamond homologs: A0A067DT54, A0A067E1K2, A0A0S2II38, A0A140JWM8, A0A1B4XBH8, A0A1W5T1Y6, A0A3Q7HBJ5, A0A517FNB9, A0A517FNC6, A0A5B8ND22, A0A9Y1LLN2, A0AAW1NEA3, A2QTE8, A2RRT9, A2Z212, A9QNE7, B0XZV0, B1NF18, B5BSX1, B6SSW8, B8AJL3, B8AV52, B8QHP1, B8QHP5, B9X287, F1SY66, G3XMC3, I1GQE7, K4CI52, L7T720, L7T8H2, O23051, O35728, O49858, O61387, O81077, O88833, P08682, P0DXH4, P14137

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	87
Likely benign	5
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

1332 predictions. Top by Δscore:

Variant	Effect	Δscore
1:46930317:C:CT	acceptor_gain	1.0000
1:46932758:CAC:C	donor_loss	1.0000
1:46934377:C:CT	acceptor_gain	1.0000
1:46934451:A:AC	donor_gain	1.0000
1:46934452:C:CA	donor_gain	1.0000
1:46934555:TTGGT:T	acceptor_gain	1.0000
1:46934556:TGGT:T	acceptor_gain	1.0000
1:46934557:GGT:G	acceptor_gain	1.0000
1:46934558:GT:G	acceptor_gain	1.0000
1:46934559:TC:T	acceptor_loss	1.0000
1:46934560:C:CC	acceptor_gain	1.0000
1:46934566:C:CT	acceptor_gain	1.0000
1:46934567:A:T	acceptor_gain	1.0000
1:46936659:CTCA:C	donor_loss	1.0000
1:46936660:TCAC:T	donor_loss	1.0000
1:46936661:CA:C	donor_loss	1.0000
1:46936662:A:AC	donor_gain	1.0000
1:46936663:C:CA	donor_loss	1.0000
1:46936663:C:CC	donor_gain	1.0000
1:46936663:CCAG:C	donor_gain	1.0000
1:46941240:T:TA	donor_gain	1.0000
1:46930318:A:T	acceptor_gain	0.9900
1:46932834:ACACC:A	acceptor_loss	0.9900
1:46932835:CAC:C	acceptor_gain	0.9900
1:46932835:CACCT:C	acceptor_loss	0.9900
1:46932836:ACCTG:A	acceptor_loss	0.9900
1:46932837:CCTGC:C	acceptor_loss	0.9900
1:46932838:CTGCA:C	acceptor_loss	0.9900
1:46932839:T:A	acceptor_loss	0.9900
1:46933942:ATACC:A	donor_loss	0.9900

AlphaMissense

3421 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
1:46932775:G:C	F450L	0.998
1:46932775:G:T	F450L	0.998
1:46932777:A:G	F450L	0.998
1:46936724:G:C	F150L	0.996
1:46936724:G:T	F150L	0.996
1:46936726:A:G	F150L	0.996
1:46934290:G:A	T325I	0.995
1:46935641:A:G	W173R	0.994
1:46935641:A:T	W173R	0.994
1:46934026:C:G	R381T	0.993
1:46936746:C:G	R143P	0.993
1:46932817:A:C	F436L	0.992
1:46932817:A:T	F436L	0.992
1:46932819:A:G	F436L	0.992
1:46934285:C:G	A327P	0.992
1:46934025:C:A	R381S	0.991
1:46934025:C:G	R381S	0.991
1:46934035:T:A	E378V	0.991
1:46934221:C:G	R348P	0.991
1:46930299:C:T	G459E	0.990
1:46930300:C:A	G459W	0.990
1:46934026:C:A	R381M	0.990
1:46930304:G:C	C457W	0.989
1:46933995:T:A	R391S	0.989
1:46933995:T:G	R391S	0.989
1:46934270:A:G	W332R	0.989
1:46934270:A:T	W332R	0.989
1:46936725:A:G	F150S	0.989
1:46934252:C:G	A338P	0.988
1:46930310:C:A	R455S	0.987

dbSNP variants (sampled 300 via entrez): RS1000057858 (1:46937560 A>G), RS1000395436 (1:46942821 T>A), RS1000665662 (1:46932660 C>A), RS1001002790 (1:46941673 T>A), RS1001005229 (1:46936012 G>C), RS1001059019 (1:46936295 C>T), RS1001324926 (1:46938224 T>C,G), RS1001481904 (1:46933219 A>C), RS1002169173 (1:46941980 T>C), RS1002320821 (1:46936856 A>C,G), RS1002891845 (1:46931969 C>T), RS1002944601 (1:46939174 C>G), RS1003098093 (1:46933949 T>C), RS1003797878 (1:46942893 G>A,T), RS1004027217 (1:46942017 T>C)

Disease associations

OMIM: gene MIM:601310 | 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
GCST006249_80	Serum metabolite levels	4.000000e-12
GCST009733_207	Urinary metabolite levels in chronic kidney disease	5.000000e-13
GCST009733_8	Urinary metabolite levels in chronic kidney disease	6.000000e-20
GCST012020_30	Serum metabolite levels	6.000000e-14
GCST012020_31	Serum metabolite levels	5.000000e-12
GCST012020_72	Serum metabolite levels	1.000000e-13
GCST012020_73	Serum metabolite levels	6.000000e-23
GCST012020_74	Serum metabolite levels	4.000000e-16
GCST012020_75	Serum metabolite levels	6.000000e-61
GCST012353_8	Serum metabolite concentrations in chronic kidney disease	4.000000e-14
GCST012353_9	Serum metabolite concentrations in chronic kidney disease	6.000000e-12

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0005116	urinary metabolite measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL3978 (SINGLE PROTEIN), CHEMBL4523986 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 15,540 (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
CHEMBL477772	PAZOPANIB	4	15,540

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

PharmGKB clinical annotations

2 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs1126742	Efficacy	3	amiloride;spironolactone	Hypertension
rs3890011	Efficacy	3	spironolactone	Hypertension

PharmGKB variants

3 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs1126742	CYP4A11	3	2.25	1	amiloride;spironolactone
rs9332978	CYP4A11		0.00	0
rs3890011	CYP4A11	3	2.00	1	spironolactone

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — CYP4 family

Most potent curated ligand interactions (3 total), top 3:

Ligand	Action	Affinity	Parameter
HET0016	Inhibition	7.74	pIC50
TP0472993	Inhibition	6.85	pIC50
epalrestat	Inhibition	5.74	pIC50

ChEMBL bioactivities

497 potent at pChembl≥5 of 503 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.28	IC50	5.3	nM	CHEMBL5958917
8.16	IC50	6.9	nM	CHEMBL5870367
8.11	IC50	7.7	nM	CHEMBL5923864
8.09	IC50	8.2	nM	CHEMBL5859173
8.09	IC50	8.1	nM	CHEMBL5969801
8.03	IC50	9.3	nM	CHEMBL6000751
8.02	IC50	9.5	nM	CHEMBL5985192
8.01	IC50	9.8	nM	CHEMBL6024341
8.00	IC50	9.9	nM	CHEMBL6051897
7.96	IC50	11	nM	CHEMBL5982248
7.92	IC50	12	nM	CHEMBL5810262
7.92	IC50	12	nM	CHEMBL5796122
7.89	IC50	13	nM	CHEMBL5774352
7.89	IC50	13	nM	CHEMBL5824435
7.85	IC50	14	nM	CHEMBL6012007
7.85	IC50	14	nM	CHEMBL5955238
7.85	IC50	14	nM	CHEMBL5938653
7.82	IC50	15	nM	CHEMBL5848080
7.82	IC50	15	nM	CHEMBL5918498
7.82	IC50	15	nM	CHEMBL6015416
7.82	IC50	15	nM	CHEMBL5992460
7.82	IC50	15	nM	CHEMBL5828253
7.80	IC50	16	nM	CHEMBL5758549
7.80	IC50	16	nM	CHEMBL5994548
7.80	IC50	16	nM	CHEMBL5848340
7.80	IC50	16	nM	CHEMBL5745213
7.80	IC50	16	nM	CHEMBL5937645
7.80	IC50	16	nM	CHEMBL5997414
7.77	IC50	17	nM	CHEMBL5869080
7.75	IC50	18	nM	CHEMBL6009649
7.75	IC50	18	nM	CHEMBL5795280
7.72	IC50	19	nM	CHEMBL5204432
7.72	IC50	19	nM	CHEMBL5870889
7.72	IC50	19	nM	CHEMBL5992460
7.70	IC50	20	nM	CHEMBL5995019
7.70	IC50	20	nM	CHEMBL6008827
7.70	IC50	20	nM	CHEMBL5872848
7.70	IC50	20	nM	CHEMBL5929669
7.68	IC50	21	nM	CHEMBL5828627
7.68	IC50	21	nM	CHEMBL5846030
7.68	IC50	21	nM	CHEMBL5777357
7.68	IC50	21	nM	CHEMBL6021694
7.66	IC50	22	nM	CHEMBL6018521
7.66	IC50	22	nM	CHEMBL5772711
7.66	IC50	22	nM	CHEMBL5854968
7.66	IC50	22	nM	CHEMBL5929406
7.66	IC50	22	nM	CHEMBL5780188
7.64	IC50	23	nM	CHEMBL6055323
7.64	IC50	23	nM	CHEMBL5986439
7.64	IC50	23	nM	CHEMBL5834431

PubChem BioAssay actives

42 with measured affinity, of 516 total; 38 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-5-[2-[4-(1H-pyrazol-5-yl)phenoxy]ethyl]-1,3-thiazole	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.0190	uM
(3S)-N,N-dimethyl-3-[[6-(1H-pyrazol-5-yl)-3-pyridinyl]oxymethyl]piperidine-1-sulfonamide	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.0290	uM
8-imidazol-1-yl-5,6,7,8-tetrahydroquinoline	2022035: Inhibition of CYP450 (unknown origin)	ic50	0.0335	uM
5-[[(3R)-1-methylsulfonylpiperidin-3-yl]methoxy]-2-(1H-pyrazol-5-yl)pyridine	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.0380	uM
5-[[(3S)-1-methylsulfonylpiperidin-3-yl]methoxy]-2-(1H-pyrazol-5-yl)pyridine	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.0410	uM
5-[(3-methylsulfonylphenyl)methoxy]-2-(1H-pyrazol-5-yl)pyridine	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.0630	uM
1-[(3R)-3-[[6-(1H-pyrazol-5-yl)-3-pyridinyl]oxymethyl]piperidin-1-yl]ethanone	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.0700	uM
1-[4-[[6-(1H-pyrazol-5-yl)-3-pyridinyl]oxymethyl]piperidin-1-yl]ethanone	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.1400	uM
4-methyl-5-[2-[[6-(1H-pyrazol-5-yl)-3-pyridinyl]oxy]ethyl]-1,3-thiazole	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.1600	uM
3-methylsulfonyl-5-[[6-(1H-pyrazol-5-yl)-3-pyridinyl]oxymethyl]phenol	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.2100	uM
1-[(3S)-3-[[6-(1H-pyrazol-5-yl)-3-pyridinyl]oxymethyl]piperidin-1-yl]ethanone	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.2200	uM
N-(4-chlorophenyl)-5-ethyl-N-methyl-3-phenyl-1,2-oxazole-4-carboxamide	2108148: Inhibition of CYP450 (unknown origin)	ic50	0.2512	uM
4-methyl-5-[2-[2-(1H-pyrazol-5-yl)pyrimidin-5-yl]oxyethyl]-1,3-thiazole	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.2600	uM
methyl 4-[[6-(1H-pyrazol-5-yl)-3-pyridinyl]oxymethyl]piperidine-1-carboxylate	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.3100	uM
5-[(4-fluorophenyl)methoxy]-2-(1H-pyrazol-5-yl)pyridine	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.3700	uM
3-[[6-(1H-pyrazol-5-yl)-3-pyridinyl]oxymethyl]benzonitrile	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.3900	uM
N-[4-[[6-(1H-pyrazol-5-yl)-3-pyridinyl]oxymethyl]cyclohexyl]acetamide	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.4100	uM
cyclopropyl-[4-[[6-(1H-pyrazol-5-yl)-3-pyridinyl]oxymethyl]piperidin-1-yl]methanone	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.5300	uM
N,N-dimethyl-4-[[6-(1H-pyrazol-5-yl)-3-pyridinyl]oxymethyl]piperidine-1-carboxamide	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.6400	uM
2-(dimethylamino)-2-(2-ethylphenyl)-N-[3-(3-sulfamoylphenyl)-1H-indazol-5-yl]acetamide	2119433: Inhibition of CYP450 (unknown origin)	ic50	0.7000	uM
5-[(1-methylsulfonylpiperidin-4-yl)methoxy]-2-(1H-pyrazol-5-yl)pyridine	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	0.8600	uM
2-pyrrolidin-1-yl-N-[3-(3-sulfamoylphenyl)-1H-indazol-5-yl]-2-thiophen-3-ylacetamide	2119433: Inhibition of CYP450 (unknown origin)	ic50	0.9000	uM
2-[4-(trifluoromethyl)phenyl]chromen-4-one	1860369: Inhibition of CYP450 in human HCT-116 cells assessed as 20-HETE formation in presence of arachidonic acid incubated for 15 mins by multi-enzyme assay based LC-MS/MS analysis	ic50	1.1000	uM
N-methyl-4-[[6-(1H-pyrazol-5-yl)-3-pyridinyl]oxymethyl]piperidine-1-carboxamide	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	1.3000	uM
4-[[6-(1H-pyrazol-5-yl)-3-pyridinyl]oxymethyl]benzonitrile	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	1.6000	uM
4-N-[(1S)-1,2,3,4-tetrahydronaphthalen-1-yl]-4-N-[[(7R)-5,6,7,8-tetrahydro-1,6-naphthyridin-7-yl]methyl]cyclohexane-1,4-diamine	2124397: Inhibition of CYP450 (unknown origin)	ic50	2.5000	uM
1-[3-(2,4-dimethoxyphenyl)phenyl]-2,4-dimethoxybenzene	1973305: Inhibition of CYP450 in pooled human liver microsomes in presence of NADPH measured every 3 mins for 120 mins by fluorescence based analysis	ic50	3.7000	uM
1-[(E)-2-(2,4-dimethoxyphenyl)ethenyl]-3,5-dimethoxybenzene	1973305: Inhibition of CYP450 in pooled human liver microsomes in presence of NADPH measured every 3 mins for 120 mins by fluorescence based analysis	ic50	3.7000	uM
2,4-bis(3,5-dimethoxyphenyl)pyrimidine	1973305: Inhibition of CYP450 in pooled human liver microsomes in presence of NADPH measured every 3 mins for 120 mins by fluorescence based analysis	ic50	3.8000	uM
2,5-bis(3,5-dimethoxyphenyl)thiophene	1973305: Inhibition of CYP450 in pooled human liver microsomes in presence of NADPH measured every 3 mins for 120 mins by fluorescence based analysis	ic50	3.9000	uM
4-[2-(2,4-dimethoxyphenyl)-1,3-thiazol-4-yl]phenol	1973305: Inhibition of CYP450 in pooled human liver microsomes in presence of NADPH measured every 3 mins for 120 mins by fluorescence based analysis	ic50	5.9000	uM
5-[(4-methylsulfonylphenyl)methoxy]-2-(1H-pyrazol-5-yl)pyridine	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	6.0000	uM
1-pyridin-4-yl-1a,2,3,7b-tetrahydro-1H-cyclopropa[a]naphthalen-4-ol	2022025: Inhibition of CYP450 in human liver microsomes	ic50	6.0534	uM
ethyl 4-[2-[4-(1H-pyrazol-5-yl)phenoxy]ethyl]piperazine-1-carboxylate	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	7.4000	uM
(5R)-3-[1-(1H-indol-2-ylmethyl)piperidin-4-yl]-5-(6-methoxyquinolin-4-yl)-1,3-oxazolidin-2-one	306257: Inhibition of CYP450	ic50	7.9433	uM
1-[4-[[6-(1H-pyrazol-5-yl)-3-pyridinyl]oxy]piperidin-1-yl]ethanone	1858241: Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	ic50	9.3000	uM
3-[1-[(3,4-dimethylphenyl)methyl]piperidin-4-yl]-5-(6-methoxyquinolin-4-yl)-1,3-oxazolidin-2-one	306257: Inhibition of CYP450	ic50	10.0000	uM
1-[3-(3,5-dimethoxyphenyl)phenyl]-3,5-dimethoxybenzene	1973305: Inhibition of CYP450 in pooled human liver microsomes in presence of NADPH measured every 3 mins for 120 mins by fluorescence based analysis	ic50	10.0000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
perfluorooctanoic acid	increases expression	6
Bezafibrate	increases expression, increases reaction, decreases reaction	3
Clofibrate	increases expression	3
pirinixic acid	increases expression	2
isoliquiritigenin	decreases reaction, increases secretion, decreases expression	2
20-hydroxy-5,8,11,14-eicosatetraenoic acid	decreases reaction, increases chemical synthesis, increases secretion	2
perfluorooctane sulfonic acid	increases expression	2
perfluoro-n-heptanoic acid	increases expression	2
perfluoroundecanoic acid	increases expression	2
Benzo(a)pyrene	affects methylation, decreases expression, increases methylation	2
Tretinoin	decreases reaction, increases expression, decreases expression	2
Aflatoxin B1	decreases methylation, decreases expression	2
HET0016	decreases expression	1
perfluorodecanesulfonic acid	increases expression	1
4-oxoretinoic acid	decreases expression	1
lasiocarpine	decreases expression	1
methyleugenol	decreases expression	1
nuciferine	increases metabolic processing, increases abundance	1
senecionine	decreases expression	1
senkirkine	decreases expression	1
VX-agent	decreases expression	1
heliotrine	decreases expression	1
3-phenoxybenzoic acid	increases expression	1
sodium arsenite	decreases expression	1
2-bromopalmitate	increases expression	1
sulindac sulfide	decreases activity	1
sulindac sulfone	affects activity	1
lauric acid	increases metabolic processing	1
perfluorobutyric acid	increases expression	1
1,4-naphthoquinone	increases abundance	1

ChEMBL screening assays

203 unique, capped per target: 199 admet, 4 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3509251	ADMET	Enzyme kinetics constant (Km value) for CYP4A11 was determined in human liver microsome incubated with [14C]SPP100 hemifumarate	FDA drug approval package for Aliskiren hemifumarate
CHEMBL5113119	Binding	Inhibition of human recombinant CYP4A11 using Luciferin-4A as substrate incubated for 60 mins in presence of NADPH regenerating system by luminescence based assay	Discovery of Novel Pyrazolylpyridine Derivatives for 20-Hydroxyeicosatetraenoic Acid Synthase Inhibitors with Selective CYP4A11/4F2 Inhibition. — J Med Chem

Cellosaurus cell lines

1 cell lines: 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_UH21	HEK293 CYP4A11*1-V5	Transformed cell line	Female

Clinical trials (associated diseases)

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