CYP51A1

Summary

CYP51A1 (cytochrome P450 family 51 subfamily A member 1, HGNC:2649) is a protein-coding gene on chromosome 7q21.2, encoding Lanosterol 14-alpha demethylase (Q16850). Sterol 14alpha-demethylase that plays a critical role in the cholesterol biosynthesis pathway, being cholesterol the major sterol component in mammalian membranes as well as a precursor for bile acid and steroid hormone synthesis.

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 endoplasmic reticulum protein participates in the synthesis of cholesterol by catalyzing the removal of the 14alpha-methyl group from lanosterol. Homologous genes are found in all three eukaryotic phyla, fungi, plants, and animals, suggesting that this is one of the oldest cytochrome P450 genes. Two transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 1595 — RefSeq curated summary.

At a glance

• Gene–disease (curated): cataract (Definitive, GenCC)
• GWAS associations: 3
• Clinical variants (ClinVar): 132 total — 1 likely-pathogenic
• Druggable target: yes — 12 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000786

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:2649
Approved symbol	CYP51A1
Name	cytochrome P450 family 51 subfamily A member 1
Location	7q21.2
Locus type	gene with protein product
Status	Approved
Aliases	CP51, CYPL1, P450L1, LDM, P450-14DM
Ensembl gene	ENSG00000001630
Ensembl biotype	protein_coding
OMIM	601637
Entrez	1595

Gene structure

Transcript identifiers

Ensembl transcripts: 9 — 8 protein_coding, 1 retained_intron

ENST00000003100, ENST00000422867, ENST00000450723, ENST00000482924, ENST00000691309, ENST00000856111, ENST00000856112, ENST00000856113, ENST00000962380

RefSeq mRNA: 2 — MANE Select: NM_000786 NM_000786, NM_001146152

CCDS: CCDS55123, CCDS5623

Canonical transcript exons

ENST00000003100 — 10 exons

Exon	Start	End
ENSE00001216550	92134173	92134477
ENSE00001813804	92112153	92113843
ENSE00003462720	92123120	92123315
ENSE00003489134	92117044	92117212
ENSE00003498850	92126253	92126427
ENSE00003512266	92118520	92118615
ENSE00003572925	92127505	92127631
ENSE00003580461	92123734	92123853
ENSE00003588081	92131774	92131872
ENSE00003693314	92128880	92129056

Expression profiles

Bgee: expression breadth ubiquitous, 142 present calls, max score 99.64.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 55.1165 / max 740.3065, expressed in 1819 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter ID	TPM avg	Samples expressed
84772	45.1568	1816
84775	5.6847	1610
84777	2.3967	1259
84771	1.1897	689
84774	0.4488	241
84776	0.2398	69

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
adrenal tissue	UBERON:0018303	99.64	gold quality
ventricular zone	UBERON:0003053	98.02	gold quality
islet of Langerhans	UBERON:0000006	97.62	gold quality
embryo	UBERON:0000922	97.59	gold quality
ganglionic eminence	UBERON:0004023	97.59	gold quality
corpus callosum	UBERON:0002336	97.19	gold quality
cortical plate	UBERON:0005343	96.93	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	96.02	gold quality
right testis	UBERON:0004534	95.54	gold quality
duodenum	UBERON:0002114	95.47	gold quality
left testis	UBERON:0004533	95.18	gold quality
liver	UBERON:0002107	94.87	gold quality
testis	UBERON:0000473	94.20	gold quality
superior frontal gyrus	UBERON:0002661	93.97	gold quality
prefrontal cortex	UBERON:0000451	93.73	gold quality
right adrenal gland	UBERON:0001233	93.61	gold quality
right adrenal gland cortex	UBERON:0035827	93.60	gold quality
right lobe of liver	UBERON:0001114	93.55	gold quality
rectum	UBERON:0001052	93.49	gold quality
adrenal gland	UBERON:0002369	93.46	gold quality
pancreas	UBERON:0001264	93.14	gold quality
left adrenal gland	UBERON:0001234	92.89	gold quality
Brodmann (1909) area 9	UBERON:0013540	92.70	gold quality
hypothalamus	UBERON:0001898	92.66	gold quality
mucosa of transverse colon	UBERON:0004991	92.48	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	92.47	gold quality
left adrenal gland cortex	UBERON:0035825	92.44	gold quality
frontal cortex	UBERON:0001870	92.38	gold quality
frontal lobe	UBERON:0016525	92.38	gold quality
esophagus mucosa	UBERON:0002469	92.31	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	17.32
E-GEOD-130148	yes	9.38
E-MTAB-7051	no	637.04

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): BHLHE40, BHLHE41, CNBP, CREB1, CREM, EPAS1, FOXO4, JUN, ONECUT1, RUNX2, SP1, SREBF1, SREBF2, TCF3

miRNA regulators (miRDB)

79 targeting CYP51A1, 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-656-3P	100.00	72.15	2788
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-518D-5P	100.00	67.51	979
HSA-MIR-518E-5P	100.00	67.66	954
HSA-MIR-518F-5P	100.00	67.51	979
HSA-MIR-519A-5P	100.00	67.66	954
HSA-MIR-519B-5P	100.00	67.66	954
HSA-MIR-519C-5P	100.00	67.66	954
HSA-MIR-520C-5P	100.00	67.51	979
HSA-MIR-522-5P	100.00	67.66	954
HSA-MIR-523-5P	100.00	67.66	954
HSA-MIR-526A-5P	100.00	67.51	979
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-6758-5P	100.00	66.21	1470
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-6856-5P	100.00	65.47	1298
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-570-3P	99.96	72.41	4910
HSA-MIR-5688	99.96	73.23	4504
HSA-MIR-6835-3P	99.93	70.49	2904
HSA-MIR-3119	99.92	71.34	2390
HSA-MIR-10527-5P	99.91	72.28	3754
HSA-MIR-3671	99.90	73.04	3897
HSA-MIR-380-3P	99.89	70.18	1978
HSA-MIR-6780A-5P	99.88	66.69	2776

Literature-anchored findings (GeneRIF, showing 22)

• A cAMP-responsive element binding site is essential for sterol regulation of the human lanosterol 14alpha-demethylase gene. (PMID:12145339)
• Plays primary roles in determining strength of interactions with azoles (PMID:15611056)
• the liver X receptor alpha directly silencing the expression of two key cholesterologenic enzymes (lanosterol 14alpha-demethylase (CYP51A1), and squalene synthase (farnesyl diphosphate farnesyl transferase 1)) via novel negative LXR DNA response elements (PMID:18676367)
• The substantial conformational changes in the B’ helix and F-G loop regions are induced upon ligand binding, consistent with the membrane nature of the protein and its substrate. (PMID:20149798)
• Studies indicate that CPY51 structures from various eukaryotic organisms are strikingly similar. (PMID:20547249)
• The new CYP51A1 inhibitor 2-((3,4-dichlorophenethyl)(propyl)amino)-1-(pyridin-3-yl)ethanol (LEK-935) on the proteome of primary human hepatocytes were analyzed. (PMID:22180046)
• Data show that forkhead transcription factor 4 (FoxO4) interacts with sterol regulatory element binding protein (SREBP)2 and hypoxia inducible factor (HIF)2alpha to modulate lanosterol 14alpha demethylase (CYP51) promoter activity. (PMID:24353279)
• Our results indicate a new link between a cholesterol synthesis gene CYP51A1 and pregnancy pathologies. (PMID:24358204)
• Low nucleotide variability of CYP51A1 is seen in cholesterol and bile acid synthesis and xenobiotic metabolism pathways. (PMID:24362992)
• The studied azoles selectively interacted with human cytochrome P450 51A1, which showed the highest affinity towards ketoconazole. (PMID:24502137)
• Suggest that GDF9, possibly with FSH, may play significant roles in the regulation of cholesterol biosynthesis and the expression of CYP51A1 in granulosa cells which might be a predictor for unfertilization. (PMID:24711211)
• Acyl-Carbon Bond Cleaving Cytochrome P450 Enzymes: CYP17A1, CYP19A1 and CYP51A1. (PMID:26002733)
• Molecular insights regarding substrate profile, faster catalysis, and weaker susceptibility of human CYP51 to inhibition. (PMID:27313059)
• the regulation of expression of human CYP51A1, the lanosterol 14alpha-demethylase, is reported. (PMID:28830911)
• Analysis of molecular docking data demonstrated the ability of abiraterone and galeterone to bind to the active site of CYP51A1, but abiraterone occupies the position closer to the heme. (PMID:29807244)
• the E3 ubiquitin ligase membrane-associated ring-CH-type finger 6 (MARCH6), known to control earlier rate-limiting steps in cholesterol synthesis, also control levels of LDM and the terminal cholesterol synthesis enzyme, 24-dehydrocholesterol reductase. (PMID:31904814)
• A requirement for an active proton delivery network supports a compound I-mediated C-C bond cleavage in CYP51 catalysis. (PMID:32493730)
• Concerning P450 Evolution: Structural Analyses Support Bacterial Origin of Sterol 14alpha-Demethylases. (PMID:33031537)
• CYP51-mediated cholesterol biosynthesis is required for the proliferation of CD4[+] T cells in Sjogren’s syndrome. (PMID:36413274)
• Revealing substrate-induced structural changes in active site of human CYP51 in the presence of its physiological substrates. (PMID:36870163)
• Processive kinetics in the three-step lanosterol 14alpha-demethylation reaction catalyzed by human cytochrome P450 51A1. (PMID:37209823)
• The effect of membrane composition on the interaction between human CYP51 and its flavonoid inhibitor - luteolin 7,3’-disulfate. (PMID:38272204)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	cyp51	ENSDARG00000042641
mus_musculus	Cyp51	ENSMUSG00000001467
rattus_norvegicus	Cyp51	ENSRNOG00000007234

Protein

Protein identifiers

Lanosterol 14-alpha demethylase — Q16850 (reviewed: Q16850)

Alternative names: CYPLI, Cytochrome P450 51A1, Cytochrome P450-14DM, Cytochrome P450LI, Sterol 14-alpha demethylase

All UniProt accessions (3): A0A8I5KRT9, Q16850, H7C0D0

UniProt curated annotations — full annotation on UniProt →

Function. Sterol 14alpha-demethylase that plays a critical role in the cholesterol biosynthesis pathway, being cholesterol the major sterol component in mammalian membranes as well as a precursor for bile acid and steroid hormone synthesis. Cytochrome P450 monooxygenase that catalyzes the three-step oxidative removal of the 14alpha-methyl group (C-32) of sterols such as lanosterol (lanosta-8,24-dien-3beta-ol) and 24,25-dihydrolanosterol (DHL) in the form of formate, and converts the sterols to 4,4-dimethyl-5alpha-cholesta-8,14,24-trien-3beta-ol and 4,4-dimethyl-8,14-cholestadien-3beta-ol, respectively, which are intermediates of cholesterol biosynthesis. Can also demethylate substrates not intrinsic to mammals, such as eburicol (24-methylene-24,25-dihydrolanosterol), but at a lower rate than DHL.

Subcellular location. Endoplasmic reticulum membrane. Microsome membrane.

Tissue specificity. Ubiquitously expressed with highest levels in testis, ovary, adrenal, prostate, liver, kidney and lung.

Post-translational modifications. Ubiquitinated by MARCHF6, leading to proteasomal degradation.

Activity regulation. Inhibited by azalanstat. Inhibited by azole antifungal agents ketoconazole, itraconazole and fluconazole.

Pathway. Steroid biosynthesis; zymosterol biosynthesis; zymosterol from lanosterol: step 1/6.

Similarity. Belongs to the cytochrome P450 family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q16850-1	1	yes
Q16850-2	2

RefSeq proteins (2): NP_000777, NP_001139624 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001128	Cyt_P450	Family
IPR002403	Cyt_P450_E_grp-IV	Family
IPR017972	Cyt_P450_CS	Conserved_site
IPR036396	Cyt_P450_sf	Homologous_superfamily
IPR050529	CYP51A1-like	Family

Pfam: PF00067

Enzyme classification (BRENDA):

• EC 1.14.13.70 — sterol 14alpha-demethylase (BRENDA: 0 organisms, 0 substrates, 0 inhibitors, 0 Km, 0 kcat entries)
• EC 1.14.14.154 — sterol 14alpha-demethylase (BRENDA: 79 organisms, 152 substrates, 488 inhibitors, 40 Km, 7 kcat entries)

Substrate kinetics (BRENDA)

11 substrates with measured Km, best-characterized 11. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
LANOSTEROL	0.0017–0.0551	13
OBTUSIFOLIOL	0.0113–0.16	4
EBURICOL	0.0041–0.0559	3
24,25-DIHYDROLANOSTEROL	0.017–0.02	2
24-METHYLENE-24,25-DIHYDROLANOSTEROL	0.0077–0.0087	2
(3BETA,4ALPHA,5ALPHA)-4,14-DIMETHYLCHOLEST-8-EN-	0.116	1
14ALPHA-METHYLZYMOSTEROL	0.0091	1
4ALPHA,14ALPHA-DIMETHYL-5ALPHA-ERGOSTA-8,24(28)-	0.008	1
7-LANOSTENE-3BETA,32-DIOL	0.003	1
8-LANOSTENE-3BETA,32-DIOL	0.0001	1
NORLANOSTEROL	0.0185	1

Catalyzed reactions (Rhea), 12 shown:

• lanosterol + 3 reduced [NADPH–hemoprotein reductase] + 3 O2 = 4,4-dimethyl-5alpha-cholesta-8,14,24-trien-3beta-ol + formate + 3 oxidized [NADPH–hemoprotein reductase] + 4 H2O + 4 H(+) (RHEA:25286)
• 24,25-dihydrolanosterol + 3 reduced [NADPH–hemoprotein reductase] + 3 O2 = 4,4-dimethyl-8,14-cholestadien-3beta-ol + formate + 3 oxidized [NADPH–hemoprotein reductase] + 4 H2O + 4 H(+) (RHEA:45960)
• a 14alpha-methyl steroid + 3 reduced [NADPH–hemoprotein reductase] + 3 O2 = a Delta(14) steroid + formate + 3 oxidized [NADPH–hemoprotein reductase] + 4 H2O + 4 H(+) (RHEA:54028)
• a 14alpha-methyl steroid + reduced [NADPH–hemoprotein reductase] + O2 = a 14alpha-hydroxymethyl steroid + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:68060)
• a 14alpha-hydroxymethyl steroid + reduced [NADPH–hemoprotein reductase] + O2 = a 14alpha-formyl steroid + oxidized [NADPH–hemoprotein reductase] + 2 H2O + H(+) (RHEA:68064)
• a 14alpha-formyl steroid + reduced [NADPH–hemoprotein reductase] + O2 = a Delta(14) steroid + formate + oxidized [NADPH–hemoprotein reductase] + H2O + 2 H(+) (RHEA:68068)
• 24,25-dihydrolanosterol + reduced [NADPH–hemoprotein reductase] + O2 = 32-hydroxy-24,25-dihydrolanosterol + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:75079)
• 32-oxo-24,25-dihydrolanosterol + reduced [NADPH–hemoprotein reductase] + O2 = 4,4-dimethyl-8,14-cholestadien-3beta-ol + formate + oxidized [NADPH–hemoprotein reductase] + H2O + 2 H(+) (RHEA:75083)
• 32-hydroxy-24,25-dihydrolanosterol + reduced [NADPH–hemoprotein reductase] + O2 = 32-oxo-24,25-dihydrolanosterol + oxidized [NADPH–hemoprotein reductase] + 2 H2O + H(+) (RHEA:75087)
• lanosterol + reduced [NADPH–hemoprotein reductase] + O2 = 32-hydroxylanosterol + oxidized [NADPH–hemoprotein reductase] + H2O + H(+) (RHEA:75103)
• 32-hydroxylanosterol + reduced [NADPH–hemoprotein reductase] + O2 = 32-oxolanosterol + oxidized [NADPH–hemoprotein reductase] + 2 H2O + H(+) (RHEA:75107)
• 32-oxolanosterol + reduced [NADPH–hemoprotein reductase] + O2 = 4,4-dimethyl-5alpha-cholesta-8,14,24-trien-3beta-ol + formate + oxidized [NADPH–hemoprotein reductase] + H2O + 2 H(+) (RHEA:75111)

UniProt features (53 total): helix 23, strand 16, turn 5, sequence conflict 4, chain 1, transmembrane region 1, binding site 1, splice variant 1, sequence variant 1

Structure

Experimental structures (PDB)

10 structures.

PDB	Method	Resolution (Å)
6UEZ	X-RAY DIFFRACTION	1.98
4UHI	X-RAY DIFFRACTION	2.04
8SS0	X-RAY DIFFRACTION	2.25
4UHL	X-RAY DIFFRACTION	2.5
8SBI	X-RAY DIFFRACTION	2.73
3LD6	X-RAY DIFFRACTION	2.8
6Q2T	X-RAY DIFFRACTION	2.8
3JUS	X-RAY DIFFRACTION	2.9
3JUV	X-RAY DIFFRACTION	3.12
8YQO	ELECTRON MICROSCOPY	3.52

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q16850-F1	91.17	0.78

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 (1): 455 (axial binding residue)

Function

Pathways and Gene Ontology

Reactome pathways

6 pathways

ID	Pathway
R-HSA-211976	Endogenous sterols
R-HSA-2426168	Activation of gene expression by SREBF (SREBP)
R-HSA-6807047	Cholesterol biosynthesis via desmosterol (Bloch pathway)
R-HSA-6807062	Zymostenol biosynthesis via lathosterol (Kandutsch-Russell pathway)
R-HSA-9619665	EGR2 and SOX10-mediated initiation of Schwann cell myelination
R-HSA-191273	Cholesterol biosynthesis

MSigDB gene sets: 324 (showing top): GSE45365_NK_CELL_VS_CD8_TCELL_UP, REACTOME_BIOLOGICAL_OXIDATIONS, JI_RESPONSE_TO_FSH_UP, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_UP, GOMF_OXIDOREDUCTASE_ACTIVITY_ACTING_ON_PAIRED_DONORS_WITH_INCORPORATION_OR_REDUCTION_OF_MOLECULAR_OXYGEN, SHEPARD_CRASH_AND_BURN_MUTANT_UP, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, REACTOME_ENDOGENOUS_STEROLS, SHAFFER_IRF4_TARGETS_IN_ACTIVATED_B_LYMPHOCYTE, KYNG_DNA_DAMAGE_DN, KYNG_DNA_DAMAGE_BY_4NQO, GOBP_NEGATIVE_REGULATION_OF_PROTEIN_LOCALIZATION, GOBP_NEGATIVE_REGULATION_OF_PROTEIN_CATABOLIC_PROCESS, GOBP_SMALL_MOLECULE_BIOSYNTHETIC_PROCESS

GO Biological Process (12): steroid biosynthetic process (GO:0006694), cholesterol biosynthetic process (GO:0006695), sterol metabolic process (GO:0016125), obsolete cholesterol biosynthetic process via 24,25-dihydrolanosterol (GO:0033488), negative regulation of protein catabolic process (GO:0042177), negative regulation of protein secretion (GO:0050709), negative regulation of amyloid-beta clearance (GO:1900222), lipid metabolic process (GO:0006629), steroid metabolic process (GO:0008202), cholesterol metabolic process (GO:0008203), sterol biosynthetic process (GO:0016126), small molecule biosynthetic process (GO:0044283)

GO Molecular Function (8): iron ion binding (GO:0005506), sterol 14-demethylase activity (GO:0008398), oxidoreductase activity (GO:0016491), 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), heme binding (GO:0020037), monooxygenase activity (GO:0004497), 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), membrane (GO:0016020), endoplasmic reticulum (GO:0005783)

Reactome top-level categories

Rollup of top-5 pathways:

Category	Pathways
Cholesterol biosynthesis	2
Cytochrome P450 - arranged by substrate type	1
Regulation of cholesterol biosynthesis by SREBP (SREBF)	1
Nervous system development	1
Metabolism of steroids	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
steroid metabolic process	2
sterol metabolic process	2
oxidoreductase activity	2
lipid biosynthetic process	1
cholesterol metabolic process	1
sterol biosynthetic process	1
secondary alcohol biosynthetic process	1
negative regulation of catabolic process	1
protein catabolic process	1
regulation of protein catabolic process	1
negative regulation of protein metabolic process	1
protein secretion	1
regulation of protein secretion	1
negative regulation of protein transport	1
negative regulation of secretion by cell	1
negative regulation of multicellular organismal process	1
amyloid-beta clearance	1
regulation of amyloid-beta clearance	1
primary metabolic process	1
lipid metabolic process	1
secondary alcohol metabolic process	1
steroid biosynthetic process	1
biosynthetic process	1
small molecule metabolic process	1
transition metal ion binding	1
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	1
demethylase activity	1
catalytic activity	1
monooxygenase activity	1
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen	1
tetrapyrrole binding	1
cation binding	1
organelle membrane	1
nuclear outer membrane-endoplasmic reticulum membrane network	1
endoplasmic reticulum subcompartment	1
cellular anatomical structure	1
cytoplasm	1
endomembrane system	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

2396 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CYP51A1	POR	P16435	950
CYP51A1	SC5D	O75845	908
CYP51A1	SQLE	Q14534	908
CYP51A1	FDFT1	P37268	896
CYP51A1	PPIG	Q13427	890
CYP51A1	HMGCS1	Q01581	872
CYP51A1	ERG28	Q9UKR5	865
CYP51A1	NSDHL	Q15738	857
CYP51A1	HSD17B7	P56937	853
CYP51A1	MSMO1	Q15800	832
CYP51A1	DHCR7	Q9UBM7	799
CYP51A1	HMGCR	P04035	797
CYP51A1	PGRMC1	O00264	784
CYP51A1	TM7SF2	O76062	782
CYP51A1	CYB5R3	P00387	777

IntAct

117 interactions, top by confidence:

A	B	Type	Score
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
ADCY9	NEMP1	psi-mi:“MI:0914”(association)	0.640
SPINT2	UPK3BL1	psi-mi:“MI:0914”(association)	0.530
TSPAN17	UPK3BL1	psi-mi:“MI:0914”(association)	0.530
SLC31A1	C2orf72	psi-mi:“MI:0914”(association)	0.530
KCNS3	UPK3BL1	psi-mi:“MI:0914”(association)	0.530
CYP51A1	POTEI	psi-mi:“MI:0914”(association)	0.530
EVA1C	STK25	psi-mi:“MI:0914”(association)	0.530
KCNA2	FADS1	psi-mi:“MI:0914”(association)	0.530
KCNK16	B3GAT3	psi-mi:“MI:0914”(association)	0.530
LPAR1	TMEM223	psi-mi:“MI:0914”(association)	0.530
PCDHA3	CYP51A1	psi-mi:“MI:0914”(association)	0.530
SLC31A1	PRORP	psi-mi:“MI:0914”(association)	0.530
CYP51A1	HRAS	psi-mi:“MI:0914”(association)	0.480
NRAS	ESYT2	psi-mi:“MI:2364”(proximity)	0.480
CYP51A1	SHANK3	psi-mi:“MI:0915”(physical association)	0.370
ZNF420	CYP51A1	psi-mi:“MI:0915”(physical association)	0.370
HSCB	RBP5	psi-mi:“MI:0914”(association)	0.350
RRP1B	ZNF785	psi-mi:“MI:0914”(association)	0.350
PSEN1	PGRMC1	psi-mi:“MI:0914”(association)	0.350
LRRK2		psi-mi:“MI:0914”(association)	0.350
PCDHGB4	FAM171A2	psi-mi:“MI:0914”(association)	0.350
PCDHA3	ABCD4	psi-mi:“MI:0914”(association)	0.350
NS3	C15orf61	psi-mi:“MI:0914”(association)	0.350
sseG	PSMD12	psi-mi:“MI:0914”(association)	0.350

BioGRID (235): CYP51A1 (Affinity Capture-MS), CYP51A1 (Affinity Capture-MS), CYP51A1 (Affinity Capture-MS), CYP51A1 (Affinity Capture-MS), CYP51A1 (Affinity Capture-MS), CYP51A1 (Affinity Capture-MS), CYP51A1 (Affinity Capture-MS), CYP51A1 (Affinity Capture-MS), CYP51A1 (Affinity Capture-MS), CYP51A1 (Affinity Capture-MS), CYP51A1 (Affinity Capture-MS), POTEI (Affinity Capture-MS), YES1 (Affinity Capture-MS), HRAS (Affinity Capture-MS), CCNY (Affinity Capture-MS)

ESM2 similar proteins: A0A098DJ84, A0A0L1JEW4, A0A0U2V7I8, A0A1V1FNZ5, B8N0E9, B8N2C8, B8NFL5, B8NUK6, E9QY26, G1UB11, I1RBR4, I1RE80, I1RJR2, I1S2M5, O13820, O14442, O23365, O46420, O48921, O64697, O64698, P0DXU9, P0DXV0, P10613, P10614, P14263, P18125, P49602, P50859, P54781, Q02315, Q078T0, Q09736, Q12664, Q16850, Q1JPY5, Q1T7C2, Q40778, Q43078, Q4PJW3

Diamond homologs: A0A097ZPE4, A0A0B5KYT4, A0A0C3HJL3, A0A0C5Q4Y6, A0A1D6F9Y9, A0A1D6GQ67, A0A2U8U2M8, A0A343URW7, A0A516F411, A0A8D5RWG4, B4FVP3, B8M9J6, B8NM64, B8NYW9, C8V0D4, C8VI81, D7PHZ6, D7PI20, F1SYC2, I7LRH3, K3VFR8, O16805, O46420, O64635, O64637, O64900, P33269, P38364, P9WEG0, P9WEG2, Q0CRQ3, Q12645, Q16850, Q2U0K1, Q3LFT9, Q4PJW3, Q4R8S6, Q4WZ68, Q5RE72, Q5Z5R7

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 149 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Regulation of RAS by GAPs	5	10.6×	3e-03

GO biological processes:

GO term	Partners	Fold	FDR
potassium ion transmembrane transport	7	7.5×	1e-02

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	1
Uncertain significance	75
Likely benign	18
Benign	24

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
3393179	NM_000786.4(CYP51A1):c.695T>C (p.Leu232Pro)	Likely pathogenic

SpliceAI

2936 predictions. Top by Δscore:

Variant	Effect	Δscore
7:92085489:TTCCA:T	acceptor_loss	1.0000
7:92085490:TCCAG:T	acceptor_loss	1.0000
7:92085491:CCAG:C	acceptor_loss	1.0000
7:92085492:CA:C	acceptor_loss	1.0000
7:92085493:A:T	acceptor_loss	1.0000
7:92086224:CTA:C	acceptor_loss	1.0000
7:92086225:TA:T	acceptor_loss	1.0000
7:92086227:G:GT	acceptor_loss	1.0000
7:92086412:AACAG:A	donor_loss	1.0000
7:92086413:ACAG:A	donor_loss	1.0000
7:92086414:CAGG:C	donor_loss	1.0000
7:92086415:AG:A	donor_loss	1.0000
7:92086416:GG:G	donor_loss	1.0000
7:92086417:GTATA:G	donor_loss	1.0000
7:92086418:T:G	donor_loss	1.0000
7:92089377:T:TA	acceptor_gain	1.0000
7:92089380:TACA:T	acceptor_loss	1.0000
7:92089381:ACAG:A	acceptor_gain	1.0000
7:92089382:CAGGG:C	acceptor_loss	1.0000
7:92089383:AG:A	acceptor_gain	1.0000
7:92089383:AGG:A	acceptor_gain	1.0000
7:92089383:AGGGT:A	acceptor_gain	1.0000
7:92089384:GG:G	acceptor_gain	1.0000
7:92089384:GGG:G	acceptor_gain	1.0000
7:92089384:GGGT:G	acceptor_gain	1.0000
7:92089384:GGGTG:G	acceptor_gain	1.0000
7:92089527:AAGGT:A	donor_loss	1.0000
7:92089528:AGGTA:A	donor_loss	1.0000
7:92089529:GGTA:G	donor_loss	1.0000
7:92089530:G:GA	donor_loss	1.0000

AlphaMissense

3338 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000189717 (7:92128324 T>C), RS1000284599 (7:92128018 T>C), RS1000457167 (7:92114277 C>T), RS1000488498 (7:92134605 G>A), RS1000539717 (7:92121061 G>A), RS1000886139 (7:92115898 G>A), RS1001067097 (7:92127752 C>T), RS1001173900 (7:92128717 G>A), RS1001360225 (7:92120292 G>T), RS1001810606 (7:92119562 T>A), RS1002075080 (7:92119939 A>G), RS1002304216 (7:92119041 T>C), RS1002500755 (7:92123971 C>G), RS1002636390 (7:92123490 C>T), RS1002707219 (7:92130147 G>A,T)

Disease associations

OMIM: gene MIM:601637 | disease phenotypes:

GenCC curated gene-disease

Disease	Classification	Inheritance
cataract	Definitive	Autosomal recessive

Mondo (1): cataract (MONDO:0005129)

Orphanet (0):

HPO phenotypes

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

GWAS associations

3 associations (top):

Study	Trait	p-value
GCST002846_5	Lifespan	2.000000e-08
GCST006993_10	Hippocampal volume in Alzheimer’s disease dementia	2.000000e-07
GCST007269_215	Pulse pressure	3.000000e-09

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0005035	hippocampal volume
EFO:0005763	pulse pressure measurement

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
D002386	Cataract	C11.510.245

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3849 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

12 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 554,178 (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
CHEMBL104	CLOTRIMAZOLE	4	56,325
CHEMBL106	FLUCONAZOLE	4	58,942
CHEMBL157101	KETOCONAZOLE	4	75,361
CHEMBL1714574	TERCONAZOLE	4	21
CHEMBL277535	BIFONAZOLE	4	12,513
CHEMBL374478	RIFAMPIN	4	93,834
CHEMBL386630	TESTOSTERONE	4	129,997
CHEMBL562	GRISEOFULVIN	4	36,847
CHEMBL64391	ITRACONAZOLE	4	606
CHEMBL808	ECONAZOLE	4	24,813
CHEMBL91	MICONAZOLE	4	45,914
CHEMBL83668	TOLNAFTATE	3	19,005

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

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs7793861	CYP51A1		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — CYP39, CYP46 and CYP51 families

Most potent curated ligand interactions (2 total), top 2:

Ligand	Action	Affinity	Parameter
azalanstat	Inhibition	9.1	pKi
compound 10 [PMID: 31663733]	Irreversible inhibition	6.0	pIC50

ChEMBL bioactivities

45 potent at pChembl≥5 of 65 total, top 44 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.75	Ki	17.7	nM	CHEMBL305220
7.70	Kd	20	nM	CHEMBL4461447
7.61	Ki	24.5	nM	KETOCONAZOLE
7.39	Ki	40.4	nM	CHEMBL305220
7.30	IC50	50	nM	ECONAZOLE
7.22	Kd	60	nM	CHEMBL4277680
7.20	Ki	63.5	nM	KETOCONAZOLE
7.05	Kd	90	nM	CHEMBL3629567
7.05	Kd	90	nM	CHEMBL4522116
6.96	Kd	110	nM	KETOCONAZOLE
6.89	Kd	130	nM	CHEMBL4439225
6.89	IC50	130	nM	CLOTRIMAZOLE
6.82	Kd	150	nM	CHEMBL4435160
6.72	IC50	190	nM	KETOCONAZOLE
6.70	IC50	200	nM	MICONAZOLE
6.52	IC50	300	nM	ANALOGUE A
6.47	IC50	342	nM	BIFONAZOLE
6.47	Kd	340	nM	CHEMBL535872
6.40	Kd	400	nM	CHEMBL537002
6.33	Kd	470	nM	CHEMBL4444489
6.10	IC50	800	nM	CHEMBL259552
6.04	IC50	910	nM	CHEMBL409630
5.94	Kd	1150	nM	CHEMBL4593688
5.89	IC50	1300	nM	CHEMBL258892
5.85	Kd	1400	nM	CHEMBL127866
5.82	IC50	1500	nM	CHEMBL4458275
5.78	Kd	1650	nM	CHEMBL4458275
5.63	Kd	2320	nM	CHEMBL4472919
5.60	Kd	2500	nM	CHEMBL4466288
5.60	IC50	2500	nM	CHEMBL259288
5.52	IC50	3000	nM	CHEMBL4593688
5.52	IC50	3000	nM	TERCONAZOLE
5.51	IC50	3100	nM	CHEMBL317410
5.48	Kd	3300	nM	CHEMBL558189
5.44	IC50	3600	nM	CHEMBL4439225
5.44	IC50	3600	nM	ITRACONAZOLE
5.41	Kd	3900	nM	CHEMBL4452294
5.40	IC50	4000	nM	CHEMBL99889
5.36	IC50	4400	nM	CHEMBL4461447
5.35	IC50	4500	nM	CHEMBL265700
5.28	IC50	5200	nM	CHEMBL4452294
5.23	IC50	5900	nM	CHEMBL4277680
5.10	Kd	8000	nM	KETOCONAZOLE
5.01	IC50	9700	nM	CHEMBL410331

PubChem BioAssay actives

55 with measured affinity, of 148 total; 33 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-[[(2R,4R)-2-[2-(4-chlorophenyl)ethyl]-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methylsulfanyl]aniline	221160: Inhibition of lanosterol 14-alpha-demethylase in hamster hepatic microsomes	ki	0.0177	uM
N-[(1R)-1-[2-chloro-4-(4-fluorophenyl)phenyl]-2-imidazol-1-ylethyl]-4-[5-(3-methylsulfonyl-5-pyridin-2-ylphenyl)-1,3,4-oxadiazol-2-yl]benzamide	1527137: Binding affinity to recombinant full length human CYP51 expressed in Escherichia coli incubated for 30 sec using [3H] labelled substrate by HPLC analysis	kd	0.0200	uM
1-[4-[4-[[2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]ethanone	221159: Inhibition of lanosterol 14-alpha-demethylase in hamster hepatic microsomes	ki	0.0245	uM
N-[4-(trifluoromethyl)phenyl]-N-[1-[5-(trifluoromethyl)-2-pyridinyl]piperidin-4-yl]pyridin-3-amine	1802428: CYP51 Inhibition Assay from Article 10.1074/jbc.M113.497990: “Complexes of Trypanosoma cruzi sterol 14a-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: structural basis for pathogen selectivity.”	kd	0.0260	uM
Econazole	322753: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay	ic50	0.0500	uM
N-[(1R)-1-[2-chloro-4-(4-fluorophenyl)phenyl]-2-imidazol-1-ylethyl]-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide	1527137: Binding affinity to recombinant full length human CYP51 expressed in Escherichia coli incubated for 30 sec using [3H] labelled substrate by HPLC analysis	kd	0.0600	uM
(2S)-2-(4-chlorophenyl)-2-pyridin-3-yl-1-[4-[4-(trifluoromethyl)phenyl]piperazin-1-yl]ethanone	1802428: CYP51 Inhibition Assay from Article 10.1074/jbc.M113.497990: “Complexes of Trypanosoma cruzi sterol 14a-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: structural basis for pathogen selectivity.”	kd	0.0690	uM
N-[(1R)-1-[2-fluoro-4-(4-fluorophenyl)phenyl]-2-imidazol-1-ylethyl]-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide	1527137: Binding affinity to recombinant full length human CYP51 expressed in Escherichia coli incubated for 30 sec using [3H] labelled substrate by HPLC analysis	kd	0.0900	uM
N-[(1R)-1-[2-chloro-4-(4-fluorophenyl)phenyl]-2-imidazol-1-ylethyl]-4-[5-[3-fluoro-5-(5-fluoropyrimidin-4-yl)phenyl]-1,3,4-oxadiazol-2-yl]benzamide	1527137: Binding affinity to recombinant full length human CYP51 expressed in Escherichia coli incubated for 30 sec using [3H] labelled substrate by HPLC analysis	kd	0.0900	uM
4-[5-(3-bromo-5-methylsulfonylphenyl)-1,3,4-oxadiazol-2-yl]-N-[(1R)-1-[2-chloro-4-(4-fluorophenyl)phenyl]-2-imidazol-1-ylethyl]benzamide	1527137: Binding affinity to recombinant full length human CYP51 expressed in Escherichia coli incubated for 30 sec using [3H] labelled substrate by HPLC analysis	kd	0.1300	uM
Clotrimazole	322753: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay	ic50	0.1300	uM
N-[(1R)-1-[2-chloro-4-(4-fluorophenyl)phenyl]-2-imidazol-1-ylethyl]-4-[5-(3-fluoro-5-pyridin-2-ylphenyl)-1,3,4-oxadiazol-2-yl]benzamide	1527137: Binding affinity to recombinant full length human CYP51 expressed in Escherichia coli incubated for 30 sec using [3H] labelled substrate by HPLC analysis	kd	0.1500	uM
Miconazole	322753: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay	ic50	0.2000	uM
5-chloro-N-[(2S)-3-(2-chlorophenyl)-1-(4-hydroxypiperidin-1-yl)-1-oxopropan-2-yl]-1H-indole-2-carboxamide	322753: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay	ic50	0.3000	uM
2-[2-naphthalen-2-ylethyl(propyl)amino]-1-pyridin-3-ylethanol;hydrobromide	322375: Binding affinity to human His-tagged CYP51 expressed in Escherichia coli	kd	0.3400	uM
1-[phenyl-(4-phenylphenyl)methyl]imidazole	322753: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay	ic50	0.3420	uM
2-[2-(3,4-dichlorophenyl)ethyl-propylamino]-1-pyridin-3-ylethanol;hydrobromide	322375: Binding affinity to human His-tagged CYP51 expressed in Escherichia coli	kd	0.4000	uM
4-[5-(3-bromonaphthalen-1-yl)-1,3,4-oxadiazol-2-yl]-N-[(1R)-1-[2-chloro-4-(4-fluorophenyl)phenyl]-2-imidazol-1-ylethyl]benzamide	1527137: Binding affinity to recombinant full length human CYP51 expressed in Escherichia coli incubated for 30 sec using [3H] labelled substrate by HPLC analysis	kd	0.4700	uM
N-[(1R)-1-[2-chloro-4-(4-fluorophenyl)phenyl]-2-imidazol-1-ylethyl]-4-[5-(2-fluoro-5-pyridin-2-ylphenyl)-1,3,4-oxadiazol-2-yl]benzamide	1527139: Inhibition of recombinant full length human CYP51 expressed in Escherichia coli incubated for 1 min using [3H] lanosterol as substrate by HPLC analysis	ic50	0.5000	uM
5-chloro-N-[(2S)-3-(2-fluorophenyl)-1-(4-hydroxypiperidin-1-yl)-1-oxopropan-2-yl]-1H-indole-2-carboxamide	322753: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay	ic50	0.8000	uM
N-[(2S)-1-(4-hydroxypiperidin-1-yl)-1-oxo-3-phenylpropan-2-yl]-1H-indole-2-carboxamide	322753: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay	ic50	0.9100	uM
N-[(1R)-1-[4-(4-fluorophenyl)naphthalen-1-yl]-2-imidazol-1-ylethyl]-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide	1527137: Binding affinity to recombinant full length human CYP51 expressed in Escherichia coli incubated for 30 sec using [3H] labelled substrate by HPLC analysis	kd	1.1500	uM
5-chloro-N-[(2S)-1-(4-hydroxypiperidin-1-yl)-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-1H-indole-2-carboxamide	322753: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay	ic50	1.3000	uM
N-[(1R)-1-[4-(4-fluorophenyl)-2-phenylphenyl]-2-imidazol-1-ylethyl]-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide	1527139: Inhibition of recombinant full length human CYP51 expressed in Escherichia coli incubated for 1 min using [3H] lanosterol as substrate by HPLC analysis	ic50	1.5000	uM
N-[(1R)-1-[4-(4-fluorophenyl)-2-(4-methoxyphenyl)phenyl]-2-imidazol-1-ylethyl]-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide	1527137: Binding affinity to recombinant full length human CYP51 expressed in Escherichia coli incubated for 30 sec using [3H] labelled substrate by HPLC analysis	kd	2.3200	uM
5-chloro-N-[(2S)-3-(4-hydroxyphenyl)-1-(4-hydroxypiperidin-1-yl)-1-oxopropan-2-yl]-1H-indole-2-carboxamide	322753: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay	ic50	2.5000	uM
5-chloro-N-[(2S)-1-(4-hydroxypiperidin-1-yl)-1-oxo-3-phenylpropan-2-yl]-1H-indole-2-carboxamide	322753: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay	ic50	3.1000	uM
2-[2-(4-chlorophenyl)ethyl-propylamino]-1-pyridin-4-ylethanol;hydrobromide	322375: Binding affinity to human His-tagged CYP51 expressed in Escherichia coli	kd	3.3000	uM
2-butan-2-yl-4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one	322753: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay	ic50	3.6000	uM
N-[(1R)-1-[4-(4-fluorophenyl)-2-(furan-2-yl)phenyl]-2-imidazol-1-ylethyl]-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide	1527137: Binding affinity to recombinant full length human CYP51 expressed in Escherichia coli incubated for 30 sec using [3H] labelled substrate by HPLC analysis	kd	3.9000	uM
5-chloro-N-[(2S)-3-(4-fluorophenyl)-1-(4-hydroxypiperidin-1-yl)-1-oxopropan-2-yl]-1H-indole-2-carboxamide	322753: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay	ic50	4.0000	uM
5-chloro-N-[(2S)-1-(4-hydroxypiperidin-1-yl)-3-(4-methoxyphenyl)-1-oxopropan-2-yl]-1H-indole-2-carboxamide	322753: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay	ic50	4.5000	uM
5-chloro-N-[(2S)-3-(4-chlorophenyl)-1-(4-hydroxypiperidin-1-yl)-1-oxopropan-2-yl]-1H-indole-2-carboxamide	322753: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay	ic50	9.7000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
perfluorooctanoic acid	decreases expression, increases expression	4
Benzo(a)pyrene	decreases expression, decreases methylation	4
Valproic Acid	affects expression, decreases expression, decreases methylation	4
bisphenol A	decreases expression, increases expression	3
perfluorooctane sulfonic acid	decreases expression	3
bisphenol S	affects expression, increases expression, affects cotreatment	3
sodium arsenite	decreases expression, increases expression	2
epoxiconazole	decreases activity, increases expression	2
Acetaminophen	decreases expression	2
Clotrimazole	decreases activity, decreases response to substance	2
Hydrogen Peroxide	affects cotreatment, increases expression, affects expression	2
Ketoconazole	decreases chemical synthesis, decreases reaction, decreases metabolic processing, increases abundance, decreases response to substance (+1 more)	2
Miconazole	decreases response to substance, decreases activity	2
Rotenone	decreases expression, increases expression	2
Tobacco Smoke Pollution	decreases expression, increases expression	2
Fluconazole	decreases activity, decreases chemical synthesis, decreases reaction, decreases metabolic processing, increases abundance (+1 more)	2
Cyclosporine	decreases expression, increases expression	2
Itraconazole	decreases response to substance, decreases activity, decreases chemical synthesis, decreases reaction, decreases metabolic processing (+1 more)	2
Particulate Matter	affects expression, increases reaction, decreases expression	2
22-hydroxycholesterol	decreases expression	1
tremortin	increases expression	1
triphenyl phosphate	affects expression	1
deoxynivalenol	decreases expression	1
dodecyldimethylamine oxide	increases expression	1
lanostenol	decreases abundance	1
isoquercitrin	affects cotreatment, increases expression	1
enilconazole	decreases activity	1
cobaltous chloride	decreases expression	1
9,10-dihydro-9,10-dihydroxybenzo(a)pyrene	decreases expression	1
periodate-oxidized adenosine	affects expression	1

ChEMBL screening assays

21 unique, capped per target: 21 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1022141	Binding	Inhibition of human sterol 14-alpha-demethylase assessed as drug/enzyme molar ratio required to produce 50 percent decrease in turnover number	Rational modification of a candidate cancer drug for use against Chagas disease. — J Med Chem

Cellosaurus cell lines

5 cell lines: 4 cancer cell line, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_D8JU	Ubigene HCT 116 CYP51A1 KO	Cancer cell line	Male
CVCL_E0TX	Ubigene Hep G2 CYP51A1 KO	Cancer cell line	Male
CVCL_E1CD	Ubigene SRA01/04 CYP51A1 KO	Transformed cell line	Male
CVCL_SK26	HAP1 CYP51A1 (-) 1	Cancer cell line	Male
CVCL_SK27	HAP1 CYP51A1 (-) 2	Cancer cell line	Male

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00273221	PHASE4	UNKNOWN	Combined Phacotube vs Phacotrabeculectomy:A Randomized Controlled Trial
NCT00312299	PHASE4	COMPLETED	Posterior Capsule Opacification Study
NCT00345046	PHASE4	COMPLETED	A Comparison of Three Different Formulations of Prednisolone Acetate 1%
NCT00347243	PHASE4	COMPLETED	Wavefront Analisys and Contrast Sensitivity of Spherical and Aspherical Intraocular Lenses
NCT00347503	PHASE4	COMPLETED	Aqueous Concentrations and PGE2 Inhibition of Ketorolac 0.4% vs. Bromfenac 0.09% in Cataract Patients
NCT00348244	PHASE4	COMPLETED	Ketorolac vs. Steroid in the Prevention of CME
NCT00348270	PHASE4	COMPLETED	Comparison of the Quality of Vision Provided by AMO Tecnis Z9000 and Alcon Laboratories MA60 Acrysof Posterior Chamber Intraocular Lenses
NCT00348582	PHASE4	COMPLETED	Acular LS vs. Nevanac in Post op Inflammation Following Cataract Surgery
NCT00348621	PHASE4	COMPLETED	A Study of Interventions to Reduce Disability From Visual Loss in Nursing Home Residents
NCT00349583	PHASE4	COMPLETED	Efficacy of Topical Cyclosporine Versus Tears for Improving Visual Outcomes Following Multifocal IOL Implantation
NCT00355446	PHASE4	COMPLETED	Bioavailability of Bimatoprost Ophthalmic Solution in Human Aqueous.
NCT00386438	PHASE4	COMPLETED	Efficacy of Honan Balloon in Intraocular Pressure Reduction Before Phacoemulsification
NCT00392275	PHASE4	COMPLETED	Penetrance of Third Generation Fluoroquinolones in Eyes With Functioning Filtering Blebs
NCT00428363	PHASE4	COMPLETED	Effect of Optic Edge Design in a Silicone Intraocular Lens on Posterior Capsule Opacification
NCT00449267	PHASE4	COMPLETED	Aurolab Hydrophobic Foldable Intraocular Lens Study
NCT00459303	PHASE4	COMPLETED	Comparison of Functional Vision Provided by AMO Tecnis Z9000 and Alcon SA60AT Acrysof
NCT00469690	PHASE4	COMPLETED	Aqueous Concentrations and PGE2 Inhibition of Ketorolac 0.4% vs. Bromfenac 0.09% in Cataract Patients: Trough Drug Effects
NCT00576485	PHASE4	COMPLETED	Spherical Aberration and Contrast Sensitivity in IOLs
NCT00612729	PHASE4	COMPLETED	Light Filters in Intraocular Lenses (IOLs) and Its Influence on Colour and Contrast Vision.
NCT00612781	PHASE4	COMPLETED	Yellow Versus White Study
NCT00630019	PHASE4	COMPLETED	Ocular Tissue Levels of 1.5% Levofloxacin Ophthalmic Solution Compared to an Active Comparator
NCT00673803	PHASE4	COMPLETED	Influence of Two Different Preloaded Intraocular Lens (IOLs) on Posterior Capsule Opacification
NCT00684138	PHASE4	COMPLETED	ACRYSOF® ReSTOR® Aspheric +3.0 D Add Power Intraocular Lens (IOL)
NCT00698724	PHASE4	COMPLETED	Comparing Optical Coherence Tomography (OCT) and Visual Acuity Outcomes in Subjects Undergoing Cataract Surgery, Who Receive Xibrom Ophthalmic Solution and Standard Presurgical Care vs. Xibrom Ophthalmic Solution Plus Prednisolone Acetate 1% and Standard Presurgical Care
NCT00710905	PHASE4	TERMINATED	Visual Function With Contralateral AcrySof® ReSTOR® Aspheric SN6AD1 and SN6AD3
NCT00710931	PHASE4	COMPLETED	Visual Function With Bilateral AcrySof® ReSTOR® Aspheric SN6AD1
NCT00711347	PHASE4	COMPLETED	Intraoperative Floppy Iris Syndrome
NCT00712244	PHASE4	COMPLETED	DisCoVisc Versus DuoVisc, Healon5 and AmVisc Plus
NCT00717080	PHASE4	COMPLETED	The Role of Capsular Tension Ring (CTR) in Anterior Capsular Contraction
NCT00719732	PHASE4	COMPLETED	Visual Function After Implantation of Bilateral AcrySof ReSTOR Aspheric +3
NCT00721253	PHASE4	COMPLETED	Visual Outcomes of Subjects Bilaterally Implanted With ReSTOR Aspheric +4 vs. Tecnis or Acri.LISA
NCT00731640	PHASE4	COMPLETED	Contralateral ReSTOR / Monofocal or Phakic Eye
NCT00732030	PHASE4	COMPLETED	Low Cylinder Toric
NCT00758199	PHASE4	COMPLETED	Determination of Optimum Duration of Treatment With Bromfenac (Xibrom) Eyedrops Following Cataract Surgery
NCT00760058	PHASE4	WITHDRAWN	Visual Outcome and Visual Quality After Bilateral Implantation of the AcrySof® IQ IOL Compared to MI60® and Tecnis® IOL
NCT00760487	PHASE4	COMPLETED	Visual Function After Implantation of Bilateral AcrySof® Toric Natural Intraocular Lens
NCT00761488	PHASE4	WITHDRAWN	Recommendations for Monitoring Clinical Experience Following Implantation of the AcrySof® Toric
NCT00763360	PHASE4	COMPLETED	To Compare the Ability of DiscoVisc® OVD to Protect the Corneal Endothelium and Maintain Anterior Chamber Space With Healon® and Amvisc® PLUS During Cataract Surgery.
NCT00786370	PHASE4	COMPLETED	Dexmedetomidine vs. Propofol for Cataract Surgery
NCT00786565	PHASE4	COMPLETED	Clinical Evaluation of a New Aspheric Intraocular Lens.