CYP4B1

Summary

CYP4B1 (cytochrome P450 family 4 subfamily B member 1, HGNC:2644) is a protein-coding gene on chromosome 1p33, encoding Cytochrome P450 4B1 (P13584). Cytochromes P450 are a group of heme-thiolate monooxygenases.

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. In rodents, the homologous protein has been shown to metabolize certain carcinogens; however, the specific function of the human protein has not been determined. Multiple transcript variants have been found for this gene.

Source: NCBI Gene 1580 — RefSeq curated summary.

At a glance

• GWAS associations: 4
• Clinical variants (ClinVar): 104 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001099772

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:2644
Approved symbol	CYP4B1
Name	cytochrome P450 family 4 subfamily B member 1
Location	1p33
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000142973
Ensembl biotype	protein_coding
OMIM	124075
Entrez	1580

Gene structure

Transcript identifiers

Ensembl transcripts: 24 — 15 protein_coding, 3 protein_coding_CDS_not_defined, 3 retained_intron, 3 nonsense_mediated_decay

ENST00000271153, ENST00000371919, ENST00000371923, ENST00000413093, ENST00000452782, ENST00000464439, ENST00000468637, ENST00000481248, ENST00000497005, ENST00000526297, ENST00000529715, ENST00000534708, ENST00000546128, ENST00000887998, ENST00000887999, ENST00000888000, ENST00000888001, ENST00000888002, ENST00000940943, ENST00000940944, ENST00000940945, ENST00000940946, ENST00000940947, ENST00000940948

RefSeq mRNA: 5 — MANE Select: NM_001099772 NM_000779, NM_001099772, NM_001319161, NM_001319162, NM_001319163

CCDS: CCDS41328, CCDS542, CCDS81318

Canonical transcript exons

ENST00000371923 — 12 exons

Exon	Start	End
ENSE00001456457	46813909	46814063
ENSE00001905451	46818631	46819413
ENSE00001935573	46799046	46799261
ENSE00003487657	46815074	46815264
ENSE00003538374	46812496	46812623
ENSE00003567596	46818131	46818213
ENSE00003580426	46810808	46810949
ENSE00003585841	46814209	46814315
ENSE00003616454	46813482	46813606
ENSE00003652252	46817048	46817181
ENSE00003673369	46811140	46811184
ENSE00003679874	46817965	46818029

Expression profiles

Bgee: expression breadth ubiquitous, 239 present calls, max score 99.83.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 1.5140 / max 260.9435, expressed in 173 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
2755	1.5140	173

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
bronchial epithelial cell	CL:0002328	99.83	gold quality
epithelium of bronchus	UBERON:0002031	99.65	gold quality
bronchus	UBERON:0002185	99.37	gold quality
right lung	UBERON:0002167	99.34	gold quality
nasal cavity epithelium	UBERON:0005384	99.20	gold quality
mucosa of paranasal sinus	UBERON:0005030	98.63	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	98.59	gold quality
lower lobe of lung	UBERON:0008949	98.39	gold quality
epithelium of nasopharynx	UBERON:0001951	98.36	gold quality
nasopharynx	UBERON:0001728	98.34	gold quality
right uterine tube	UBERON:0001302	98.11	gold quality
upper lobe of lung	UBERON:0008948	97.18	gold quality
upper lobe of left lung	UBERON:0008952	97.09	gold quality
tibial nerve	UBERON:0001323	96.57	gold quality
nasal cavity mucosa	UBERON:0001826	96.43	gold quality
lung	UBERON:0002048	95.15	gold quality
urinary bladder	UBERON:0001255	94.87	gold quality
palpebral conjunctiva	UBERON:0001812	94.16	gold quality
trachea	UBERON:0003126	93.87	gold quality
mammalian vulva	UBERON:0000997	93.16	gold quality
omental fat pad	UBERON:0010414	92.77	gold quality
peritoneum	UBERON:0002358	92.73	gold quality
urethra	UBERON:0000057	92.65	gold quality
calcaneal tendon	UBERON:0003701	92.57	gold quality
adipose tissue of abdominal region	UBERON:0007808	92.56	gold quality
esophagus mucosa	UBERON:0002469	92.30	gold quality
adult organism	UBERON:0007023	92.15	gold quality
visceral pleura	UBERON:0002401	91.72	gold quality
decidua	UBERON:0002450	91.71	gold quality
skin of abdomen	UBERON:0001416	91.39	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-GEOD-130148	yes	13.14
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AP1, JUN, NFKB

miRNA regulators (miRDB)

31 targeting CYP4B1, 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-8485	100.00	77.57	4731
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-8068	99.98	73.85	2376
HSA-MIR-3065-5P	99.97	71.56	3281
HSA-MIR-6825-5P	99.96	69.81	3431
HSA-MIR-1-3P	99.93	72.35	1914
HSA-MIR-206	99.93	72.50	1893
HSA-MIR-613	99.91	71.50	1710
HSA-MIR-153-5P	99.89	73.86	6317
HSA-LET-7A-2-3P	99.87	70.53	1921
HSA-LET-7G-3P	99.85	70.43	1929
HSA-MIR-4659A-3P	99.80	72.62	4248
HSA-MIR-4659B-3P	99.80	72.62	4248
HSA-MIR-7159-5P	99.53	72.12	2472
HSA-MIR-653-5P	99.46	67.35	1300
HSA-MIR-6071	99.16	67.77	1780
HSA-MIR-1178-3P	98.57	67.09	890
HSA-MIR-6852-3P	98.54	67.60	1468
HSA-MIR-654-3P	98.38	67.61	905
HSA-MIR-5088-3P	98.29	66.63	1310
HSA-MIR-4518	98.12	66.82	1030
HSA-MIR-556-5P	97.75	66.17	473
HSA-MIR-1266-5P	97.71	66.92	1052
HSA-MIR-6511A-3P	97.60	66.61	713
HSA-MIR-6511B-3P	97.60	66.61	713
HSA-MIR-3909	97.55	66.78	887
HSA-MIR-192-3P	97.52	67.66	1001
HSA-MIR-6509-5P	97.39	68.27	969
HSA-MIR-517-5P	97.13	68.43	781

Literature-anchored findings (GeneRIF, showing 15)

• polymorphism in humans: evidence for a non-functional allelic variant (PMID:12142726)
• CYP4B1 is a senescene-associated gene in normal human oral keratinocytes. (PMID:12837283)
• Results demostrated an increased risk of bladder cancer associated with the CYP4B1*1/*2 and *2/*2 genotypes. (PMID:18713828)
• Detected by polymerase chain reaction in prostate tissue. (PMID:19040121)
• A proline residue in the meander region at position 427 in human CYP4B1 and 422 in rabbit CYP4B1 is important for protein stability and rescues the 4-ipomeanol bioactivation. (PMID:25247810)
• Single nucleotide polymorphisms of CYP2C8,CYP2E1 and CYP4B1 are associated with susceptibility to gout in ethnic Han males population. (PMID:26252103)
• the Ser207 insertion does not rescue the P450 functional activity of human CYP4B1 that has been lost during evolution. (PMID:26355749)
• Loss of the CYP4B1 gene expression may play an important role in urothelial carcinoma progression. (PMID:30803053)
• oxidation of fatty acids and fatty alcohols by cytochrome P450 monooxygenase CYP4B1 (PMID:31801692)
• Cytochrome P450 4B1 (CYP4B1) as a target in cancer treatment. (PMID:32054340)
• CYP4B1 is a prognostic biomarker and potential therapeutic target in lung adenocarcinoma. (PMID:33592039)
• Case-control study on CYP4B1 gene polymorphism and susceptibility to gastric cancer in the chinese Han population. (PMID:36307788)
• reviews ability of CYP4B1 to hydroxylate fatty acids and fatty alcohols, its role in xenobiotic and endobiotic metabolism, and its unusual heme-binding characteristics (PMID:36768362)
• Missense variants in CYP4B1 associated with increased risk of lung cancer among Chinese Han population. (PMID:37950293)
• CYP4B1 polymorphisms and the risk of breast cancer in Chinese women: a case-control study. (PMID:38041008)

Cross-species orthologs

31 orthologs

Organism	Symbol	Gene ID
danio_rerio	cyp4f3	ENSDARG00000053530
mus_musculus	Cyp4b1	ENSMUSG00000028713
rattus_norvegicus	Cyp4b1	ENSRNOG00000055078
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), CYP4V2 (ENSG00000145476), CYP4A22 (ENSG00000162365), CYP4F11 (ENSG00000171903), CYP4F22 (ENSG00000171954), CYP4F2 (ENSG00000186115), CYP4Z1 (ENSG00000186160), CYP4F12 (ENSG00000186204), CYP4X1 (ENSG00000186377), CYP4F8 (ENSG00000186526), CYP4F3 (ENSG00000186529), CYP4A11 (ENSG00000187048)

Protein

Protein identifiers

Cytochrome P450 4B1 — P13584 (reviewed: P13584)

Alternative names: CYPIVB1, Cytochrome P450-HP

All UniProt accessions (6): P13584, E9PL36, E9PML0, F5H1Q8, F5H5Q6, Q8IZB0

UniProt curated annotations — full annotation on UniProt →

Function. Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.

Subcellular location. Endoplasmic reticulum membrane. Microsome membrane.

Tissue specificity. Detected in the liver and lung (at protein level).

Induction. P450 can be induced to high levels in liver and other tissues by various foreign compounds, including drugs, pesticides, and carcinogens.

Similarity. Belongs to the cytochrome P450 family.

Isoforms (2)

UniProt ID	Names	Canonical?
P13584-1	1	yes
P13584-2	2

RefSeq proteins (5): NP_000770, NP_001093242, NP_001306090, NP_001306091, NP_001306092 (=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

Catalyzed reactions (Rhea), 1 shown:

• an organic molecule + reduced [NADPH–hemoprotein reductase] + O2 = an alcohol + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:17149)

UniProt features (18 total): sequence variant 12, binding site 2, chain 1, sequence conflict 1, modified residue 1, splice variant 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P13584-F1	94.34	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.

Ligand- & substrate-binding residues (2): 315 (covalent); 453 (axial binding residue)

Post-translational modifications (1): 436

Function

Pathways and Gene Ontology

Reactome pathways

4 pathways

ID	Pathway
R-HSA-211935	Fatty acids
R-HSA-211958	Miscellaneous substrates
R-HSA-211979	Eicosanoids
R-HSA-2142691	Synthesis of Leukotrienes (LT) and Eoxins (EX)

MSigDB gene sets: 146 (showing top): MODULE_93, REACTOME_BIOLOGICAL_OXIDATIONS, GOMF_OXIDOREDUCTASE_ACTIVITY_ACTING_ON_PAIRED_DONORS_WITH_INCORPORATION_OR_REDUCTION_OF_MOLECULAR_OXYGEN, MODULE_45, SAENZ_DETOX_PATHWAY_AND_CARCINOGENESIS_DN, MOTAMED_RESPONSE_TO_ANDROGEN_UP, MODULE_16, SARRIO_EPITHELIAL_MESENCHYMAL_TRANSITION_DN, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, MARTINEZ_RB1_TARGETS_UP, CHEN_LVAD_SUPPORT_OF_FAILING_HEART_UP, MODULE_205, GATA3_01, SENGUPTA_NASOPHARYNGEAL_CARCINOMA_DN, GOBP_LIPID_METABOLIC_PROCESS

GO Biological Process (2): fatty acid metabolic process (GO:0006631), biphenyl metabolic process (GO:0018879)

GO Molecular Function (9): monooxygenase activity (GO:0004497), iron ion binding (GO:0005506), 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), oxygen binding (GO:0019825), heme binding (GO:0020037), heterocyclic compound binding (GO:1901363), oxidoreductase activity (GO:0016491), oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen (GO:0016705), metal ion binding (GO:0046872)

GO Cellular Component (3): endoplasmic reticulum membrane (GO:0005789), endoplasmic reticulum (GO:0005783), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Cytochrome P450 - arranged by substrate type	3
Arachidonate metabolism	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
oxidoreductase activity	2
small molecule binding	2
lipid metabolic process	1
monocarboxylic acid metabolic process	1
benzene-containing compound metabolic process	1
transition metal ion binding	1
monooxygenase activity	1
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen	1
tetrapyrrole binding	1
catalytic activity	1
cation binding	1
organelle membrane	1
nuclear outer membrane-endoplasmic reticulum membrane network	1
endoplasmic reticulum subcompartment	1
cytoplasm	1
endomembrane system	1
intracellular membrane-bounded organelle	1
cellular anatomical structure	1

Protein interactions and networks

STRING

1612 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CYP4B1	SULT1C2	O00338	514
CYP4B1	PPIG	Q13427	513
CYP4B1	HID1	Q8IV36	479
CYP4B1	CYB5A	P00167	459
CYP4B1	PTGS2	P35354	449
CYP4B1	CYB5B	O43169	425
CYP4B1	MYO18A	Q92614	408
CYP4B1	TAGAP	Q8N103	400
CYP4B1	TNXB	P22105	391
CYP4B1	CCRL2	O00421	383
CYP4B1	VNN2	O95498	380
CYP4B1	SWSAP1	Q6NVH7	375
CYP4B1	CHRNA4	P43681	374
CYP4B1	MMP12	P39900	374
CYP4B1	RETN	Q9HD89	364
CYP4B1	CAPN10	Q9HC96	364

IntAct

3 interactions, top by confidence:

A	B	Type	Score
	AP3B1	psi-mi:“MI:0914”(association)	0.350
DFFA	CYP4B1	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (2): PKLR (Affinity Capture-MS), CYP4B1 (Affinity Capture-MS)

ESM2 similar proteins: A2A974, F1Q8C3, H1A988, O18993, O35728, O88833, P00186, P04799, P08516, P08684, P13584, P14579, P14581, P15128, P15129, P20815, P20816, P20817, P24453, P24462, P24463, P24464, P33268, P33274, P51869, P51871, P78329, P79102, P79401, P98187, Q00557, Q08477, Q29496, Q3MID2, Q64391, Q64462, Q64464, Q6A152, Q6NT55, Q86W10

Diamond homologs: A0A017SFB8, A0A075TMP8, A0A075TRL5, A0A0U5CJM3, A0A1D6F9Y9, A0A1D6HSP4, A0A1L9WN31, A0A1L9WN72, A0A1U9YHZ8, A0A1V6NWJ0, A0A2B7YEY0, A0A2H3CNS9, A0A2H3CZX2, A0A2P1DP94, A0A6S6QPY4, A1CFL5, A1CFL6, A2A974, A2RRT9, A8NCK4, A8NCK6, C8VJR0, F1SY52, F1SY62, F1SY66, F1SY73, F1SY82, F1SY91, F1SY96, F1SYF1, F1SYI7, F2ZAF9, G1UB11, G1XU03, G3Y416, G9N4A8, H1A981, I3DZK9, O49394, O49396

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	76
Likely benign	4
Benign	8

Top pathogenic / likely-pathogenic (0)

SpliceAI

1905 predictions. Top by Δscore:

Variant	Effect	Δscore
1:46810803:TTCA:T	acceptor_loss	1.0000
1:46810804:TCA:T	acceptor_loss	1.0000
1:46810806:AGAT:A	acceptor_loss	1.0000
1:46810931:GCTGT:G	donor_gain	1.0000
1:46810932:C:G	donor_gain	1.0000
1:46810948:GG:G	donor_gain	1.0000
1:46810949:GG:G	donor_gain	1.0000
1:46810950:GTG:G	donor_loss	1.0000
1:46810951:T:A	donor_loss	1.0000
1:46810956:A:T	donor_gain	1.0000
1:46812494:A:AG	acceptor_gain	1.0000
1:46812494:AG:A	acceptor_gain	1.0000
1:46812495:G:GG	acceptor_gain	1.0000
1:46812495:GG:G	acceptor_gain	1.0000
1:46812495:GGGA:G	acceptor_gain	1.0000
1:46812620:GCTG:G	donor_gain	1.0000
1:46812622:TGGT:T	donor_loss	1.0000
1:46812623:GGTG:G	donor_loss	1.0000
1:46812624:GT:G	donor_loss	1.0000
1:46812625:T:G	donor_loss	1.0000
1:46813455:A:AG	acceptor_gain	1.0000
1:46813455:ACATT:A	acceptor_gain	1.0000
1:46813456:C:G	acceptor_gain	1.0000
1:46813457:A:AG	acceptor_gain	1.0000
1:46813457:ATT:A	acceptor_gain	1.0000
1:46813458:T:G	acceptor_gain	1.0000
1:46814061:CAGGT:C	donor_loss	1.0000
1:46814063:GGTG:G	donor_loss	1.0000
1:46814064:G:GC	donor_loss	1.0000
1:46814065:T:A	donor_loss	1.0000

AlphaMissense

3400 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
1:46812561:T:C	F145L	0.995
1:46812563:T:A	F145L	0.995
1:46812563:T:G	F145L	0.995
1:46812540:C:A	R138S	0.994
1:46817130:C:A	R385S	0.994
1:46817131:G:C	R385P	0.994
1:46812541:G:C	R138P	0.993
1:46818213:G:T	R451M	0.993
1:46818213:G:C	R451T	0.992
1:46818631:G:C	R451S	0.991
1:46818631:G:T	R451S	0.991
1:46811178:T:A	W121R	0.990
1:46811178:T:C	W121R	0.990
1:46812562:T:C	F145S	0.987
1:46815134:T:C	F314L	0.986
1:46815136:T:A	F314L	0.986
1:46815136:T:G	F314L	0.986
1:46818149:T:C	F430L	0.986
1:46818151:T:A	F430L	0.986
1:46818151:T:G	F430L	0.986
1:46815140:G:C	G316R	0.984
1:46811147:G:C	K110N	0.981
1:46811147:G:T	K110N	0.981
1:46813964:C:A	R225S	0.981
1:46814227:G:C	R264P	0.981
1:46818197:T:C	F446L	0.981
1:46818199:C:A	F446L	0.981
1:46818199:C:G	F446L	0.981
1:46813944:T:C	L218P	0.980
1:46817130:C:G	R385G	0.979

dbSNP variants (sampled 300 via entrez): RS1000057154 (1:46799973 C>A,T), RS1000095727 (1:46797239 C>A), RS1000166089 (1:46809430 G>C), RS1000173695 (1:46809726 T>G), RS1000340639 (1:46814542 G>A), RS1000540064 (1:46808063 A>C), RS1000541006 (1:46801342 T>C), RS1000716613 (1:46813682 C>A,T), RS1000848975 (1:46819070 G>A), RS1000933307 (1:46807746 C>T), RS1001143404 (1:46807926 G>A), RS1001343392 (1:46819377 G>C), RS1001398843 (1:46810381 T>G), RS1001654983 (1:46797249 G>A), RS1001684266 (1:46797487 A>G)

Disease associations

OMIM: gene MIM:124075 | disease phenotypes:

GenCC curated gene-disease

Mondo (1): pulmonary disease, chronic obstructive, susceptibility to (MONDO:0100167)

Orphanet (0):

HPO phenotypes

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

GWAS associations

4 associations (top):

Study	Trait	p-value
GCST001555_3	Testosterone levels	8.000000e-06
GCST005359_5	Disease progression in age-related macular degeneration	8.000000e-06
GCST006249_80	Serum metabolite levels	4.000000e-12
GCST009733_7	Urinary metabolite levels in chronic kidney disease	4.000000e-14

EFO canonical traits (3, from GWAS)

EFO ID	Trait name
EFO:0004908	testosterone measurement
EFO:0008336	disease progression measurement
EFO:0005116	urinary metabolite measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): 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

1 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs4646487	Toxicity	3	docetaxel;thalidomide	Prostatic Neoplasms

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs4646487	CYP4B1	3	2.00	1	docetaxel;thalidomide

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — CYP4 family

ChEMBL bioactivities

16 potent at pChembl≥5 of 17 total, top 16 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
6.60	IC50	251.2	nM	CHEMBL601428
6.16	IC50	700	nM	CHEMBL3330409
6.05	IC50	900	nM	CHEMBL3330410
5.96	IC50	1100	nM	CHEMBL2130955
5.72	IC50	1900	nM	CHEMBL2130955
5.60	IC50	2500	nM	CHEMBL5612347
5.55	IC50	2800	nM	CHEMBL2130955
5.43	IC50	3700	nM	CHEMBL5406721
5.43	IC50	3700	nM	CHEMBL46909
5.42	IC50	3800	nM	CHEMBL5418617
5.41	IC50	3900	nM	CHEMBL5429178
5.31	IC50	4900	nM	CHEMBL2130955
5.23	IC50	5900	nM	CHEMBL5406218
5.22	IC50	6053	nM	CHEMBL65590
5.10	IC50	7900	nM	PAZOPANIB
5.00	IC50	1e+04	nM	CHEMBL5395150

PubChem BioAssay actives

18 with measured affinity, of 466 total; 15 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
8-imidazol-1-yl-5,6,7,8-tetrahydroquinoline	2022035: Inhibition of CYP450 (unknown origin)	ic50	0.0335	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
2-(dimethylamino)-2-(2-ethylphenyl)-N-[3-(3-sulfamoylphenyl)-1H-indazol-5-yl]acetamide	2119433: Inhibition of CYP450 (unknown origin)	ic50	0.7000	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
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
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
(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
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

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

Chemical	Actions (top 5)	PubMed papers
Tobacco Smoke Pollution	decreases expression, increases expression	7
Air Pollutants	decreases expression, affects cotreatment, increases abundance, increases oxidation, increases expression	5
sodium arsenite	decreases expression, increases abundance, increases expression, affects methylation	4
Estradiol	affects cotreatment, decreases expression, increases expression	3
Tetrachlorodibenzodioxin	decreases expression	3
Resveratrol	affects cotreatment, decreases expression	2
Aerosols	decreases expression	2
Benzo(a)pyrene	affects methylation, decreases expression, increases methylation	2
Smoke	decreases expression, increases abundance, increases expression	2
Tretinoin	decreases expression, increases expression	2
Cadmium Chloride	increases expression, decreases expression	2
beta-Naphthoflavone	decreases expression	2
Particulate Matter	decreases expression, increases abundance, increases expression	2
methyleugenol	decreases expression	1
alpha-pinene	affects cotreatment, increases oxidation, increases abundance	1
propylparaben	decreases expression	1
1,12-benzoperylene	increases expression, decreases reaction	1
bisphenol A	affects cotreatment, increases expression	1
lead acetate	decreases expression	1
VX-agent	decreases expression	1
methylparaben	decreases expression	1
cupric chloride	decreases expression	1
methacrylaldehyde	increases abundance, affects cotreatment, increases oxidation	1
glycidamide	decreases expression	1
3-methyleneindolenine	increases chemical synthesis, increases metabolic processing	1
abrine	increases expression	1
2-methyl-2H-pyrazole-3-carboxylic acid (2-methyl-4-o-tolylazophenyl)amide	decreases reaction, increases expression	1
NSC668394	increases expression	1
walrycin A	increases expression	1
theaflavin-3,3’-digallate	affects expression	1

ChEMBL screening assays

183 unique, capped per target: 181 admet, 2 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2060324	ADMET	Inhibition of CYP450	Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR. — Bioorg Med Chem Lett
CHEMBL4614611	Binding	Drug metabolism in human liver microsomes assessed as Cytochrome P450-mediated formation of 12-OHNVP by measuring Kcat/Km ratio in presence of NADPH regenerating reagents by uHPLC-MS/MS analysis	Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death. — J Med Chem

Clinical trials (associated diseases)

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