PLIN5

Summary

PLIN5 (perilipin 5, HGNC:33196) is a protein-coding gene on chromosome 19p13.3, encoding Perilipin-5 (Q00G26). Lipid droplet-associated protein that maintains the balance between lipogenesis and lipolysis and also regulates fatty acid oxidation in oxidative tissues.

Predicted to enable identical protein binding activity and lipase binding activity. Predicted to be involved in several processes, including negative regulation of peroxisome proliferator activated receptor signaling pathway; positive regulation of triglyceride storage; and regulation of lipid metabolic process. Located in intracellular membrane-bounded organelle and lipid droplet.

Source: NCBI Gene 440503 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 145 total
• Druggable target: yes — 8 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001013706

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:33196
Approved symbol	PLIN5
Name	perilipin 5
Location	19p13.3
Locus type	gene with protein product
Status	Approved
Aliases	LSDP5, LSDA5, OXPAT, MLDP
Ensembl gene	ENSG00000214456
Ensembl biotype	protein_coding
OMIM	613248
Entrez	440503

Gene structure

Transcript identifiers

Ensembl transcripts: 26 — 23 protein_coding, 2 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000381848, ENST00000586133, ENST00000588887, ENST00000589728, ENST00000590350, ENST00000592610, ENST00000905182, ENST00000905183, ENST00000905184, ENST00000905185, ENST00000905186, ENST00000905187, ENST00000905188, ENST00000905189, ENST00000905190, ENST00000905191, ENST00000905192, ENST00000905193, ENST00000905194, ENST00000905195, ENST00000942350, ENST00000942351, ENST00000942352, ENST00000942353, ENST00000942354, ENST00000942355

RefSeq mRNA: 1 — MANE Select: NM_001013706 NM_001013706

CCDS: CCDS42473

Canonical transcript exons

ENST00000381848 — 8 exons

Exon	Start	End
ENSE00001490019	4529784	4529866
ENSE00001532857	4522531	4524085
ENSE00001532866	4525633	4525832
ENSE00001532876	4529073	4529253
ENSE00002941547	4535165	4535224
ENSE00003464420	4534015	4534095
ENSE00003471850	4531627	4531822
ENSE00003524826	4524963	4525076

Expression profiles

Bgee: expression breadth ubiquitous, 227 present calls, max score 98.85.

FANTOM5 (CAGE): breadth broad, TPM avg 2.1258 / max 291.2185, expressed in 441 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
178447	2.1258	441

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right lobe of liver	UBERON:0001114	98.85	gold quality
apex of heart	UBERON:0002098	98.37	gold quality
body of pancreas	UBERON:0001150	98.23	gold quality
gastrocnemius	UBERON:0001388	97.37	gold quality
left ovary	UBERON:0002119	96.88	gold quality
right ovary	UBERON:0002118	96.67	gold quality
hindlimb stylopod muscle	UBERON:0004252	95.96	gold quality
tibialis anterior	UBERON:0001385	95.89	gold quality
body of stomach	UBERON:0001161	95.70	gold quality
muscle of leg	UBERON:0001383	95.42	gold quality
liver	UBERON:0002107	94.66	gold quality
heart left ventricle	UBERON:0002084	94.26	gold quality
cardiac ventricle	UBERON:0002082	93.87	gold quality
omental fat pad	UBERON:0010414	92.64	gold quality
peritoneum	UBERON:0002358	92.59	gold quality
adipose tissue of abdominal region	UBERON:0007808	92.52	gold quality
quadriceps femoris	UBERON:0001377	92.41	silver quality
vastus lateralis	UBERON:0001379	92.28	silver quality
minor salivary gland	UBERON:0001830	92.15	gold quality
skeletal muscle tissue	UBERON:0001134	91.57	gold quality
saliva-secreting gland	UBERON:0001044	91.52	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	91.39	gold quality
biceps brachii	UBERON:0001507	91.24	gold quality
right atrium auricular region	UBERON:0006631	91.22	gold quality
deltoid	UBERON:0001476	91.08	silver quality
adipose tissue	UBERON:0001013	90.91	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	90.74	gold quality
cardiac atrium	UBERON:0002081	90.52	gold quality
subcutaneous adipose tissue	UBERON:0002190	90.40	gold quality
stomach	UBERON:0000945	90.37	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	11.72
E-CURD-135	no	481.19
E-MTAB-6379	no	28.10

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CEBPA, PPARA, PPARD, PPARG

miRNA regulators (miRDB)

37 targeting PLIN5, 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-3065-5P	99.97	71.56	3281
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-3912-5P	99.95	66.11	925
HSA-MIR-3119	99.92	71.34	2390
HSA-MIR-3529-3P	99.90	73.55	3045
HSA-MIR-4503	99.85	71.45	1869
HSA-MIR-7159-5P	99.53	72.12	2472
HSA-MIR-4437	99.52	65.29	1266
HSA-MIR-486-3P	99.51	66.82	1901
HSA-MIR-3612	99.45	66.02	1333
HSA-MIR-650	99.45	65.77	1309
HSA-MIR-330-3P	99.41	69.95	2521
HSA-MIR-4284	99.36	65.25	1293
HSA-MIR-6731-5P	99.28	67.42	2375
HSA-MIR-8085	99.28	67.56	2362
HSA-MIR-3978	99.24	68.39	2201
HSA-MIR-4263	99.18	69.25	2236
HSA-MIR-1286	99.09	66.23	1046
HSA-MIR-6830-5P	99.01	68.73	1884
HSA-MIR-520G-3P	98.91	67.38	1914
HSA-MIR-520H	98.91	67.38	1914
HSA-MIR-5000-3P	98.79	65.63	1251
HSA-MIR-3922-5P	98.77	66.53	1059
HSA-MIR-323A-5P	98.59	65.13	651
HSA-MIR-561-5P	98.25	68.13	1365
HSA-MIR-6773-3P	98.17	65.51	1213
HSA-MIR-124-5P	98.11	67.65	1095
HSA-MIR-4632-5P	97.82	65.38	1470
HSA-MIR-4733-5P	97.75	67.44	866
HSA-MIR-5699-5P	97.36	67.03	1014

Literature-anchored findings (GeneRIF, showing 20)

• Results indicate involvement of OXPAT and ADRP in muscular lipid accumulation and type 2 diabetes. (PMID:19602560)
• interaction of ATGL with CGI-58 increased lipolysis, whereas interaction of ATGL with perilipin 5 decreased lipolysis. (PMID:21393244)
• Perilipin 5 is the most recently established family member, highly expressed in oxidative tissues and could play an important role in regulating LD TAG hydrolysis in oxidative mammalian tissues. [Review] (PMID:21632259)
• The lipid droplet coat protein perilipin 5 also localizes to muscle mitochondria. (PMID:22127648)
• PLIN5 likely plays an important role in intramyocellular lipid accumulation and oxidation, both of which increase with endurance training in human skeletal muscle. (PMID:22667335)
• Sprint interval and traditional endurance training increase net intramuscular triglyceride breakdown and expression of perilipin 2 and 5 (PMID:23129790)
• Perilipin 5 as a lipid droplet protein adapted to mitochondrial energy utilization (PMID:24535284)
• PLIN5 was significantly colocated with ATGL, mitochondria and CGI-58, indicating a close association between the key lipolytic effectors in resting skeletal muscle. (PMID:25054327)
• High oxygen consumption in middle-aged men was reflected in higher perilipin 5 expression in skeletal muscle. (PMID:26447519)
• Notch1 expression is reduced and glucose-6-phosphatase and perilipin-5 (G6PC/PLIN5) are upregulated in liver biopsies from nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD) patients. (PMID:27428080)
• The data highlight a key role of PLIN5 in lipid droplets function, first by finely adjusting lipid droplets fatty acids supply to mitochondrial oxidation, and second acting as a protective factor against lipotoxicity in skeletal muscle. (PMID:27922115)
• Even though total PLIN5 protein content was almost double in Trained versus type 2 diabetes patients, PLIN5 coating did not affect lipid droplet number or size significantly. (PMID:29110300)
• perilipin 5 is not restricted to certain cell types but localizes to distinct lipid droplet subpopulations reflecting a possible function in oxidative energy supply in normal tissues and in diseases. (PMID:29752569)
• Using two super-resolution imaging approaches, the study shows that in sections of human skeletal muscle PLIN2 and PLIN5 localize to lipid droplets (LD) at distinct sites, with abundance of PLIN5 at LD-mitochondria tethering sites. (PMID:30591149)
• Lsdp5 expression is instrumental for reducing lipotoxicity in cultured liver cells. (PMID:31173228)
• Decoration of myocellular lipid droplets with perilipins as a marker for in vivo lipid droplet dynamics: A super-resolution microscopy study in trained athletes and insulin resistant individuals. (PMID:33160079)
• Enlarged PLIN5-uncoated lipid droplets in inner regions of skeletal muscle type II fibers associate with type 2 diabetes. (PMID:35220055)
• Plin5 Bidirectionally Regulates Lipid Metabolism in Oxidative Tissues. (PMID:35401929)
• Effects of perilipin-5 on lipid metabolism and high-sensitivity cardiac troponin I. (PMID:36134829)
• PLIN5 interacts with FATP4 at membrane contact sites to promote lipid droplet-to-mitochondria fatty acid transport. (PMID:37290445)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	plin3	ENSDARG00000013711
mus_musculus	Plin5	ENSMUSG00000011305
rattus_norvegicus	Plin5	ENSRNOG00000047860
drosophila_melanogaster	Lsd-2	FBGN0030608

Paralogs (4): PLIN3 (ENSG00000105355), PLIN2 (ENSG00000147872), PLIN1 (ENSG00000166819), PLIN4 (ENSG00000167676)

Protein

Protein identifiers

Perilipin-5 — Q00G26 (reviewed: Q00G26)

Alternative names: Lipid storage droplet protein 5

All UniProt accessions (2): Q00G26, K7EIX1

UniProt curated annotations — full annotation on UniProt →

Function. Lipid droplet-associated protein that maintains the balance between lipogenesis and lipolysis and also regulates fatty acid oxidation in oxidative tissues. Recruits mitochondria to the surface of lipid droplets and is involved in lipid droplet homeostasis by regulating both the storage of fatty acids in the form of triglycerides and the release of fatty acids for mitochondrial fatty acid oxidation. In lipid droplet triacylglycerol hydrolysis, plays a role as a scaffolding protein for three major key lipolytic players: ABHD5, PNPLA2 and LIPE. Reduces the triacylglycerol hydrolase activity of PNPLA2 by recruiting and sequestering PNPLA2 to lipid droplets. Phosphorylation by PKA enables lipolysis probably by promoting release of ABHD5 from the perilipin scaffold and by facilitating interaction of ABHD5 with PNPLA2. Also increases lipolysis through interaction with LIPE and upon PKA-mediated phosphorylation of LIPE.

Subunit / interactions. Homooligomer. Interacts with PNPLA2; prevents interaction of PNPLA2 with ABHD5. Interacts with ABHD5; targets ABHD5 to lipid droplets and promotes interaction of ABHD5 with PNPLA2. Interacts with LIPE.

Subcellular location. Lipid droplet. Cytoplasm. Mitochondrion.

Tissue specificity. Expressed in skeletal muscle, liver, heart and kidney.

Post-translational modifications. Phosphorylated by PKA. Phosphorylated on serine in skeletal muscle at rest or upon lipolytic stimulation.

Induction. Increased by endurance and sprint interval training.

Similarity. Belongs to the perilipin family.

RefSeq proteins (1): NP_001013728* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR004279	Perilipin	Family

Pfam: PF03036

UniProt features (11 total): region of interest 4, sequence variant 3, modified residue 3, chain 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q00G26-F1	66.54	0.11

Functional residue map

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

Post-translational modifications (3): 2, 148, 322

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 156 (showing top): GOBP_LIPID_MODIFICATION, GOBP_FATTY_ACID_CATABOLIC_PROCESS, GOBP_REGULATION_OF_LIPID_STORAGE, GOBP_REGULATION_OF_TRIGLYCERIDE_METABOLIC_PROCESS, GOBP_NEGATIVE_REGULATION_OF_LIPID_METABOLIC_PROCESS, GOBP_NEGATIVE_REGULATION_OF_REACTIVE_OXYGEN_SPECIES_METABOLIC_PROCESS, GOBP_NEGATIVE_REGULATION_OF_HYDROLASE_ACTIVITY, IVANOVA_HEMATOPOIESIS_LATE_PROGENITOR, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, GOBP_KETONE_METABOLIC_PROCESS, GOBP_REGULATION_OF_FATTY_ACID_METABOLIC_PROCESS, GOBP_NEGATIVE_REGULATION_OF_INTRACELLULAR_SIGNAL_TRANSDUCTION, GOBP_GLYCEROLIPID_METABOLIC_PROCESS, GOBP_REGULATION_OF_LIPID_BIOSYNTHETIC_PROCESS, GOBP_POSITIVE_REGULATION_OF_CATALYTIC_ACTIVITY

GO Biological Process (14): positive regulation of triglyceride biosynthetic process (GO:0010867), positive regulation of lipid storage (GO:0010884), positive regulation of triglyceride storage (GO:0010890), negative regulation of triglyceride catabolic process (GO:0010897), lipid storage (GO:0019915), negative regulation of fatty acid beta-oxidation (GO:0031999), positive regulation of fatty acid beta-oxidation (GO:0032000), lipid droplet organization (GO:0034389), negative regulation of peroxisome proliferator activated receptor signaling pathway (GO:0035359), mitochondrion localization (GO:0051646), negative regulation of lipase activity (GO:0060192), positive regulation of lipase activity (GO:0060193), negative regulation of reactive oxygen species metabolic process (GO:2000378), negative regulation of lipid catabolic process (GO:0050995)

GO Molecular Function (3): lipase binding (GO:0035473), identical protein binding (GO:0042802), protein binding (GO:0005515)

GO Cellular Component (4): cytoplasm (GO:0005737), mitochondrion (GO:0005739), lipid droplet (GO:0005811), cytosol (GO:0005829)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
negative regulation of lipid catabolic process	2
fatty acid beta-oxidation	2
regulation of fatty acid beta-oxidation	2
lipase activity	2
cellular anatomical structure	2
cytoplasm	2
regulation of triglyceride biosynthetic process	1
triglyceride biosynthetic process	1
positive regulation of lipid biosynthetic process	1
positive regulation of triglyceride metabolic process	1
regulation of lipid storage	1
lipid storage	1
positive regulation of cellular process	1
positive regulation of lipid localization	1
positive regulation of lipid storage	1
regulation of triglyceride storage	1
triglyceride storage	1
regulation of triglyceride catabolic process	1
triglyceride catabolic process	1
negative regulation of triglyceride metabolic process	1
nutrient storage	1
negative regulation of fatty acid oxidation	1
positive regulation of fatty acid oxidation	1
positive regulation of lipid catabolic process	1
organelle organization	1
peroxisome proliferator activated receptor signaling pathway	1
regulation of peroxisome proliferator activated receptor signaling pathway	1
negative regulation of intracellular signal transduction	1
organelle localization	1
negative regulation of hydrolase activity	1
positive regulation of hydrolase activity	1
negative regulation of metabolic process	1
reactive oxygen species metabolic process	1
regulation of reactive oxygen species metabolic process	1
negative regulation of catabolic process	1
lipid catabolic process	1
negative regulation of lipid metabolic process	1
regulation of lipid catabolic process	1
enzyme binding	1
protein binding	1

Protein interactions and networks

STRING

1385 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PLIN5	PNPLA2	Q96AD5	984
PLIN5	ABHD5	Q8WTS1	928
PLIN5	PPARA	Q07869	844
PLIN5	LIPE	Q05469	795
PLIN5	CIDEC	Q96AQ7	668
PLIN5	PPARGC1A	Q9UBK2	660
PLIN5	DGAT2	Q96PD7	603
PLIN5	PPARG	P37231	601
PLIN5	DGAT1	O75907	583
PLIN5	PLIN1	O60240	565
PLIN5	MFN2	O95140	557
PLIN5	SIRT1	Q96EB6	543
PLIN5	VPS13D	Q5THJ4	522
PLIN5	FITM2	Q8N6M3	518
PLIN5	CIDEA	O60543	510

IntAct

11 interactions, top by confidence:

A	B	Type	Score
PLIN5	ABHD5	psi-mi:“MI:0915”(physical association)	0.560
PLIN5	INPPL1	psi-mi:“MI:0914”(association)	0.530
ENC1	PLIN5	psi-mi:“MI:0914”(association)	0.530
CFLAR	PLIN5	psi-mi:“MI:0914”(association)	0.530
HTR3C	GET1	psi-mi:“MI:0914”(association)	0.350

BioGRID (18): METAP2 (Affinity Capture-MS), INPPL1 (Affinity Capture-MS), SAPCD2 (Affinity Capture-MS), PLIN5 (Affinity Capture-MS), PLIN5 (FRET), PLIN5 (Affinity Capture-Western), PLIN5 (Affinity Capture-MS), SAPCD2 (Affinity Capture-MS), PLIN5 (Affinity Capture-MS), METAP2 (Affinity Capture-MS), INPPL1 (Affinity Capture-MS), PLIN5 (Affinity Capture-MS), PLIN5 (Affinity Capture-MS), METAP2 (Affinity Capture-MS), PLIN5 (Affinity Capture-MS)

ESM2 similar proteins: A0A9P5BNK0, A2Y0H2, A6QLL0, B0FJL7, E9F970, F4JNX2, M0R7Z9, O48832, O60240, O60664, O82246, O82803, P0DKW0, P0DMN9, P0DMS3, P0DOC1, P0DP52, P0DTQ9, P0DUX6, P0DUX7, P0DUY0, P0DUY1, P12278, P15252, P18658, P19034, P29530, P43883, P43884, Q00368, Q00G26, Q41112, Q4PLW0, Q5BLZ2, Q5RAV8, Q69YL0, Q84K90, Q8BVZ1, Q8CGN5, Q99541

Diamond homologs: A6QLL0, B0FJL7, M0R7Z9, O60240, O60664, P43883, Q00G26, Q4PLW0, Q5BLZ2, Q5RAV8, Q8BVZ1, Q8CGN5, Q99541, Q9DBG5, Q9TUM6, Q96Q06, P43884, O88492, E9F970

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	124
Likely benign	8
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1678 predictions. Top by Δscore:

Variant	Effect	Δscore
19:4525073:CTAT:C	acceptor_gain	1.0000
19:4525074:TAT:T	acceptor_gain	1.0000
19:4525076:TCTG:T	acceptor_loss	1.0000
19:4525077:C:CA	acceptor_loss	1.0000
19:4525077:C:CC	acceptor_gain	1.0000
19:4525632:CCAG:C	donor_gain	1.0000
19:4529066:T:TA	donor_gain	1.0000
19:4529067:CCTCA:C	donor_loss	1.0000
19:4529068:CTCA:C	donor_loss	1.0000
19:4529069:TCAC:T	donor_loss	1.0000
19:4529070:CAC:C	donor_loss	1.0000
19:4529071:A:AC	donor_gain	1.0000
19:4529071:A:C	donor_loss	1.0000
19:4529072:C:CC	donor_gain	1.0000
19:4529072:C:G	donor_loss	1.0000
19:4529072:CCGAG:C	donor_gain	1.0000
19:4529081:T:TA	donor_gain	1.0000
19:4531625:A:AC	donor_gain	1.0000
19:4531626:C:CT	donor_gain	1.0000
19:4531626:CG:C	donor_gain	1.0000
19:4531819:CGTT:C	acceptor_gain	1.0000
19:4535160:CTCA:C	donor_loss	1.0000
19:4535161:TCACC:T	donor_loss	1.0000
19:4535162:CAC:C	donor_loss	1.0000
19:4535163:ACCT:A	donor_loss	1.0000
19:4525535:T:TA	donor_gain	0.9900
19:4525586:A:AC	donor_gain	0.9900
19:4525587:C:CC	donor_gain	0.9900
19:4525590:ATTGG:A	donor_gain	0.9900
19:4525628:CTCA:C	donor_loss	0.9900

AlphaMissense

2976 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
19:4523786:G:C	F378L	0.973
19:4523786:G:T	F378L	0.973
19:4523788:A:G	F378L	0.973
19:4523531:G:C	F463L	0.967
19:4523531:G:T	F463L	0.967
19:4523533:A:G	F463L	0.967
19:4523803:A:G	W373R	0.964
19:4523803:A:T	W373R	0.964
19:4529845:G:T	A93D	0.959
19:4525718:G:T	A212D	0.957
19:4531704:G:T	A60D	0.956
19:4525652:A:G	L234P	0.955
19:4523699:C:A	W407C	0.953
19:4523699:C:G	W407C	0.953
19:4523701:A:G	W407R	0.951
19:4523701:A:T	W407R	0.951
19:4523801:C:A	W373C	0.951
19:4523801:C:G	W373C	0.951
19:4531716:G:T	A56D	0.950
19:4531788:A:T	V32D	0.950
19:4531742:C:A	K47N	0.947
19:4531742:C:G	K47N	0.947
19:4523794:C:G	G376R	0.946
19:4523794:C:T	G376R	0.946
19:4529854:T:A	N90I	0.943
19:4525759:A:C	F198L	0.942
19:4525759:A:T	F198L	0.942
19:4525761:A:G	F198L	0.942
19:4525730:A:G	I208T	0.934
19:4523793:C:T	G376E	0.932

dbSNP variants (sampled 300 via entrez): RS1000183024 (19:4530825 A>G), RS1000344424 (19:4533244 C>T), RS1000404285 (19:4529006 G>C), RS1000579252 (19:4523076 G>A,T), RS1000634010 (19:4534209 G>A), RS1000784970 (19:4529926 G>A,T), RS1000947718 (19:4533785 A>G), RS1000998708 (19:4533604 G>C), RS1001059447 (19:4522904 C>G,T), RS1001069827 (19:4526229 T>G), RS1001272223 (19:4532019 T>C), RS1001320956 (19:4535082 G>A), RS1001519993 (19:4528204 C>A,T), RS1001686179 (19:4526929 GA>G), RS1001751843 (19:4524125 C>T)

Disease associations

OMIM: gene MIM:613248 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3885501 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

8 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 279,056 (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
CHEMBL12856	INAMRINONE	4	9,690
CHEMBL193	NIFEDIPINE	4	74,353
CHEMBL388590	BENZBROMARONE	4	8,245
CHEMBL456	ETHACRYNIC ACID	4	20,004
CHEMBL590	MENADIONE	4	21,034
CHEMBL964	DISULFIRAM	4	38,611
CHEMBL140	CURCUMIN	3	93,882
CHEMBL51085	EBSELEN	3	13,237

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

Binding affinities (BindingDB)

196 measured of 258 human assays (278 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
(4-acetyloxy-3-chloranyl-2-morpholin-4-yl-naphthalen-1-yl) ethanoate	EC50	0.133 nM
(5R)-6-[6-[(1E,3S,5Z)-3-hydroxyundeca-1,5-dienyl]pyridin-2-yl]hexane-1,5-diol	KI	25 nM
N-[4-(methoxymethyl)-1-(2-thiophen-2-ylethyl)piperidin-4-yl]-N-phenyl-propanamide;2-oxidanylpropane-1,2,3-tricarboxylic acid	KI	50 nM
SMR000469200	KI	126 nM
MLS000122969	IC50	127 nM
2-{2-ethoxy-5-[(4-ethylpiperazine-1-)sulfonyl]phenyl}-5-methyl-7-propyl-3H,4H-imidazo[1,5-a][1,2,4]triazin-4-one	IC50	300 nM
(3Z,5E)-1-ethyl-3,5-bis(3-hydroxy-4-methoxy-benzylidene)-4-piperidone	EC50	380 nM
2-butyl-4-thiazolidinecarboxylic acid	IC50	814 nM
N-cyclohexyl-2-[3-(2-furanyl)-2-oxo-1-quinoxalinyl]-2-phenylacetamide	IC50	817 nM
SMR001821229	IC50	828 nM
cid_53383152	IC50	970 nM
5-hydroxy-4-[[4-(2-hydroxyethyl)-1-piperazinyl]methyl]-2-methyl-3-benzo[g]benzofurancarboxylic acid ethyl ester	IC50	1130 nM
7-methyl-1,3-dinitro-acridine	EC50	1190 nM
MLS000684313	IC50	1230 nM
N-benzyl-2-(4-cyanophenyl)-2-[3-(furan-2-yl)-2-oxoquinoxalin-1-yl]acetamide	IC50	1300 nM
cid_53383173	IC50	1340 nM
cid_53383343	IC50	1400 nM
cid_53383347	IC50	1480 nM
N-cyclohexyl-2-[3-(2-furanyl)-2-oxo-1-quinoxalinyl]-2-(1-naphthalenyl)acetamide	IC50	1480 nM
cid_6377798	IC50	1560 nM
MLS000680483	IC50	1590 nM
(E)-2-cyano-3-[3-[(E)-2-cyano-3-(2-methoxyethylamino)-3-oxidanylidene-prop-1-enyl]phenyl]-N-(2-methoxyethyl)prop-2-enamide	EC50	1650 nM
N-tert-butyl-2-cyclopropyl-2-[3-(2-furanyl)-2-oxo-1-quinoxalinyl]acetamide	IC50	1720 nM
N-cyclohexyl-2-[3-(2-furanyl)-2-oxo-1-quinoxalinyl]-2-(4-methoxyphenyl)acetamide	IC50	1750 nM
N-tert-butyl-2-[3-(2-furanyl)-2-oxo-1-quinoxalinyl]-2-(4-methoxyphenyl)acetamide	IC50	1780 nM
MLS003674221	IC50	1810 nM
cid_53383334	IC50	1840 nM
N-tert-butyl-2-(2-fluorophenyl)-2-[3-(furan-2-yl)-2-oxoquinoxalin-1-yl]acetamide	IC50	1850 nM
MLS003674201	IC50	1860 nM
MLS003674212	IC50	1860 nM
N-Tosyl-L-phenylalanine chloromethyl ketone	IC50	1870 nM
MLS000779343	IC50	1870 nM
SMR000132574	IC50	1870 nM
1-(2-fluorophenyl)-5-{4-[(5-nitro-2-pyridinyl)oxy]benzylidene}-2,4,6(1H,3H,5H)-pyrimidinetrione	IC50	1880 nM
N-tert-butyl-2-[3-(furan-2-yl)-2-oxoquinoxalin-1-yl]-2-(4-phenylphenyl)acetamide	IC50	1910 nM
2-(1-benzofuran-2-yl)-2-[3-(furan-2-yl)-2-oxoquinoxalin-1-yl]-N-pentylacetamide	IC50	2000 nM
cid_53383163	IC50	2020 nM
methyl 1-(2-furylmethyl)-2-methyl-4-(4-nitrobenzylidene)-5-oxo-4,5-dihydro-1H-pyrrole-3-carboxylate	IC50	2070 nM
MLS000517420	IC50	2170 nM
cid_53383333	IC50	2170 nM
2-(1-benzofuran-2-yl)-N-cyclohexyl-2-[3-(furan-2-yl)-2-oxidanylidene-quinoxalin-1-yl]ethanamide	IC50	2190 nM
cid_2261569	IC50	2210 nM
N-cyclohexyl-2-[3-(furan-2-yl)-2-oxidanylidene-quinoxalin-1-yl]-2-quinolin-4-yl-ethanamide	IC50	2230 nM
2-(2-fluorophenyl)-2-[3-(furan-2-yl)-2-oxidanylidene-quinoxalin-1-yl]-N-(phenylmethyl)ethanamide	IC50	2240 nM
Cyclopentanone, 2-heptylidene-5-(1-pyrrolidinylmethyl)-, (E)-, hydrochloride	IC50	2250 nM
MLS000532188	IC50	2270 nM
N-tert-butyl-2-[3-(furan-2-yl)-2-oxoquinoxalin-1-yl]-2-naphthalen-1-ylacetamide	IC50	2270 nM
3-phenyl-1,4-benzodioxin-2-carboxaldehyde	EC50	2280 nM
MLS003674211	IC50	2400 nM
MLS003674210	IC50	2410 nM

ChEMBL bioactivities

32 potent at pChembl≥5 of 44 total, top 32 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
5.96	IC50	1101	nM	EBSELEN
5.95	IC50	1123	nM	CHEMBL1565221
5.83	IC50	1484	nM	CHEMBL17201
5.79	IC50	1622	nM	DISULFIRAM
5.72	IC50	1901	nM	TPCK
5.64	IC50	2269	nM	CHEMBL1500987
5.55	IC50	2798	nM	CHEMBL1535633
5.51	IC50	3103	nM	CHEMBL1369296
5.48	IC50	3300	nM	CHEMBL1462108
5.47	IC50	3408	nM	CHEMBL1363719
5.45	IC50	3573	nM	CHEMBL1598561
5.41	IC50	3906	nM	CHEMBL1352555
5.40	IC50	3942	nM	CHEMBL1414703
5.37	IC50	4245	nM	CHALCONE
5.33	IC50	4641	nM	CHEMBL1426508
5.32	IC50	4832	nM	ETHACRYNIC ACID
5.31	IC50	4850	nM	CHEMBL1498750
5.28	IC50	5240	nM	CHEMBL485636
5.28	IC50	5283	nM	CHEMBL1256923
5.24	IC50	5718	nM	CHEMBL1522846
5.21	IC50	6238	nM	CHEMBL1507428
5.19	IC50	6443	nM	9,10-PHENANTHRENEQUINONE
5.16	IC50	6958	nM	CHEMBL1519501
5.16	IC50	6970	nM	CHEMBL1478754
5.15	IC50	7133	nM	NIFEDIPINE
5.12	IC50	7587	nM	CHEMBL1308170
5.09	IC50	8122	nM	CHEMBL1366427
5.06	IC50	8697	nM	CHEMBL1433108
5.05	IC50	8908	nM	CHEMBL1548890
5.02	IC50	9468	nM	MENADIONE
5.01	IC50	9841	nM	CHEMBL1334291
5.00	IC50	9956	nM	CHEMBL1517036

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	affects binding, increases reaction, decreases expression, increases expression	3
triphenyl phosphate	decreases expression, increases abundance, affects expression	2
(+)-JQ1 compound	increases expression	2
Benzo(a)pyrene	decreases expression, decreases methylation, increases methylation	2
Estradiol	affects cotreatment, decreases expression, increases expression	2
OTX015	increases expression	1
mivebresib	increases expression	1
dicrotophos	decreases expression	1
methylmercuric chloride	increases expression	1
bisphenol A	affects cotreatment, decreases expression	1
trichostatin A	affects expression	1
di-n-butylphosphoric acid	affects expression	1
ICG 001	decreases expression	1
licochalcone B	increases expression	1
bisphenol S	affects cotreatment, decreases expression	1
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acid	increases expression	1
Temozolomide	decreases expression	1
Sunitinib	increases expression	1
Acetaminophen	increases expression	1
Dexamethasone	affects cotreatment, decreases expression, increases expression	1
Diethylhexyl Phthalate	decreases expression	1
Flame Retardants	decreases expression, increases abundance	1
Indomethacin	affects cotreatment, decreases expression, increases expression	1
N-Nitrosopyrrolidine	decreases expression	1
Nickel	decreases expression	1
Thiram	increases expression	1
Tobacco Smoke Pollution	decreases expression	1
Tretinoin	decreases expression	1
Triclosan	decreases expression	1
Urethane	increases expression	1

ChEMBL screening assays

1 unique, capped per target: 1 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1738081	Binding	PUBCHEM_BIOASSAY: Luminescence-based biochemical high throughput dose response assay for inhibitors of the interaction of the lipase co-activator protein, abhydrolase domain containing 5 (ABHD5) with perilipin-5 (MLDP; PLIN5) (2K validation	PubChem BioAssay data set

Clinical trials (associated diseases)

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