PLAAT2

Summary

PLAAT2 (phospholipase A and acyltransferase 2, HGNC:17824) is a protein-coding gene on chromosome 11q12.3, encoding Phospholipase A and acyltransferase 2 (Q9NWW9). Exhibits both phospholipase A1/2 and acyltransferase activities.

The protein encoded by this gene has both phospholipase and acyltransferase activities and acts as a tumor suppressor. The encoded protein can hydrolyze dipalmitoylated phosphatidylcholine (PC) to palmitic acid and lyso-PC. In addition, this protein can catalyze the N-acylation of phosphatidylethanolamine and can catalyze the O-acylation of lyso-PC to form PC.

Source: NCBI Gene 54979 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 18 total
• Druggable target: yes
• MANE Select transcript: NM_017878

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:17824
Approved symbol	PLAAT2
Name	phospholipase A and acyltransferase 2
Location	11q12.3
Locus type	gene with protein product
Status	Approved
Aliases	FLJ20556, PLAAT-2
Ensembl gene	ENSG00000133328
Ensembl biotype	protein_coding
OMIM	613866
Entrez	54979

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 2 protein_coding

ENST00000255695, ENST00000947707

RefSeq mRNA: 1 — MANE Select: NM_017878 NM_017878

CCDS: CCDS8046

Canonical transcript exons

ENST00000255695 — 4 exons

Exon	Start	End
ENSE00000908985	63560085	63560193
ENSE00001289854	63552770	63553065
ENSE00001326482	63563316	63563379
ENSE00002495333	63558392	63558660

Expression profiles

Bgee: expression breadth ubiquitous, 184 present calls, max score 93.47.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.3214 / max 82.3066, expressed in 62 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
120290	0.1576	34
120291	0.1418	38
120293	0.0127	4
120292	0.0092	5

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
duodenum	UBERON:0002114	93.47	gold quality
jejunal mucosa	UBERON:0000399	91.49	gold quality
epithelium of bronchus	UBERON:0002031	90.27	gold quality
bronchus	UBERON:0002185	89.50	gold quality
bronchial epithelial cell	CL:0002328	89.40	gold quality
epithelium of nasopharynx	UBERON:0001951	86.51	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	85.27	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	84.60	silver quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	83.54	gold quality
nasal cavity epithelium	UBERON:0005384	83.20	gold quality
palpebral conjunctiva	UBERON:0001812	82.37	gold quality
rectum	UBERON:0001052	81.25	gold quality
colonic mucosa	UBERON:0000317	79.60	gold quality
jejunum	UBERON:0002115	79.19	gold quality
mucosa of sigmoid colon	UBERON:0004993	79.08	gold quality
small intestine	UBERON:0002108	78.58	gold quality
right uterine tube	UBERON:0001302	78.49	gold quality
nasal cavity mucosa	UBERON:0001826	77.96	gold quality
small intestine Peyer’s patch	UBERON:0003454	77.28	gold quality
mucosa of paranasal sinus	UBERON:0005030	76.98	gold quality
adult mammalian kidney	UBERON:0000082	76.57	gold quality
ileal mucosa	UBERON:0000331	76.30	gold quality
nephron tubule	UBERON:0001231	75.11	gold quality
pancreatic ductal cell	CL:0002079	74.90	silver quality
kidney epithelium	UBERON:0004819	73.84	gold quality
transverse colon	UBERON:0001157	73.40	gold quality
tongue squamous epithelium	UBERON:0006919	72.30	silver quality
diaphragm	UBERON:0001103	72.10	gold quality
olfactory bulb	UBERON:0002264	71.59	gold quality
renal glomerulus	UBERON:0000074	71.55	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	5.71

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

13 targeting PLAAT2, 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-5692A	100.00	74.40	6850
HSA-MIR-4425	100.00	67.59	1049
HSA-MIR-545-5P	99.66	70.18	2308
HSA-MIR-7152-5P	99.60	69.33	2094
HSA-MIR-136-5P	99.50	67.26	1153
HSA-MIR-5580-5P	99.38	66.96	1139
HSA-MIR-4711-3P	98.97	66.87	1020
HSA-MIR-876-3P	98.76	68.23	945
HSA-MIR-599	98.32	66.99	1037
HSA-MIR-1302	97.92	67.27	844
HSA-MIR-1914-5P	97.83	66.21	807
HSA-MIR-4298	97.26	66.59	765
HSA-MIR-4764-3P	96.81	67.94	580

Literature-anchored findings (GeneRIF, showing 3)

• HRASLS2 protein suppressed growth and RAS activities of cancer cells, and the C-terminal hydrophobic domain appeared to be indispensable for both activities. (PMID:18163183)
• The tumor suppressors TIG3, HRASLS2 and H-rev107 are involved in the phospholipid metabolism with different physiological roles. (PMID:19615464)
• Data show that acyl-modified forms of HRAS-like tumor suppressors HRASLS2 and HRASLS3 mimicking lipolytic activity of lecithin retinol acyltransferase LRAT. (PMID:22605381)

Cross-species orthologs

1 orthologs

Organism	Symbol	Gene ID
danio_rerio	lratb.2	ENSDARG00000077652

Paralogs (7): LRAT (ENSG00000121207), PLAAT1 (ENSG00000127252), PLAAT4 (ENSG00000133321), LRATD1 (ENSG00000162981), PLAAT5 (ENSG00000168004), LRATD2 (ENSG00000168672), PLAAT3 (ENSG00000176485)

Protein

Protein identifiers

Phospholipase A and acyltransferase 2 — Q9NWW9 (reviewed: Q9NWW9)

Alternative names: HRAS-like suppressor 2

All UniProt accessions (1): Q9NWW9

UniProt curated annotations — full annotation on UniProt →

Function. Exhibits both phospholipase A1/2 and acyltransferase activities. Shows phospholipase A1 (PLA1) and A2 (PLA2) activity, catalyzing the calcium-independent release of fatty acids from the sn-1 or sn-2 position of glycerophospholipids. For most substrates, PLA1 activity is much higher than PLA2 activity. Shows O-acyltransferase activity, catalyzing the transfer of a fatty acyl group from glycerophospholipid to the hydroxyl group of lysophospholipid. Shows N-acyltransferase activity, catalyzing the calcium-independent transfer of a fatty acyl group at the sn-1 position of phosphatidylcholine (PC) and other glycerophospholipids to the primary amine of phosphatidylethanolamine (PE), forming N-acylphosphatidylethanolamine (NAPE), which serves as precursor for N-acylethanolamines (NAEs). Catalyzes N-acylation of PE using both sn-1 and sn-2 palmitoyl groups of PC as acyl donor. Exhibits high phospholipase A1/2 activity and low N-acyltransferase activity.

Subcellular location. Cytoplasm. Membrane.

Tissue specificity. Expressed in liver, kidney, small intestine testis and colon. Undetectable in testis, placenta, salivary gland and fetal brain.

Similarity. Belongs to the H-rev107 family.

RefSeq proteins (1): NP_060348* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR007053	LRAT_dom	Domain
IPR051496	H-rev107_PLA/AT	Family

Pfam: PF04970

Enzyme classification (BRENDA):

• EC 2.7.1.22 — ribosylnicotinamide kinase (BRENDA: 8 organisms, 14 substrates, 1 inhibitors, 9 Km, 5 kcat entries)

Substrate kinetics (BRENDA)

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

Substrate	Km (mM)	Measurements
1-(BETA-D-RIBOFURANOSYL)-NICOTINAMIDE	0.068–30	4
ATP	1.2	1
N-RIBOSYLNICOTINAMIDE	0.08	1
NICOTINAMIDE MONONUCLEOTIDE	0.14	1
NICOTINAMIDE RIBOSIDE	1.1	1
PHOSPHATE	0.28	1

Catalyzed reactions (Rhea), 12 shown:

• a 1,2-diacyl-sn-glycero-3-phosphocholine + H2O = a 1-acyl-sn-glycero-3-phosphocholine + a fatty acid + H(+) (RHEA:15801)
• a 1,2-diacyl-sn-glycero-3-phosphocholine + H2O = a 2-acyl-sn-glycero-3-phosphocholine + a fatty acid + H(+) (RHEA:18689)
• 1-hexadecanoyl-2-(9Z-octadecenoyl)-sn-glycero-3-phosphocholine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphocholine + (9Z)-octadecenoate + H(+) (RHEA:38779)
• 1-hexadecanoyl-2-(9Z-octadecenoyl)-sn-glycero-3-phosphocholine + H2O = 2-(9Z-octadecenoyl)-sn-glycero-3-phosphocholine + hexadecanoate + H(+) (RHEA:38783)
• 1-hexadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycero-3-phosphoethanolamine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphoethanolamine + (5Z,8Z,11Z,14Z)-eicosatetraenoate + H(+) (RHEA:40431)
• 1,2-dihexadecanoyl-sn-glycero-3-phosphocholine + H2O = 2-hexadecanoyl-sn-glycero-3-phosphocholine + hexadecanoate + H(+) (RHEA:40487)
• 1-hexadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycero-3-phosphocholine + H2O = 2-(5Z,8Z,11Z,14Z)-eicosatetraenoyl-sn-glycero-3-phosphocholine + hexadecanoate + H(+) (RHEA:40571)
• 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphoethanolamine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphoethanolamine + (9Z,12Z)-octadecadienoate + H(+) (RHEA:40815)
• 1,2-dihexadecanoyl-sn-glycero-3-phosphocholine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphocholine + hexadecanoate + H(+) (RHEA:41223)
• 1-hexadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycero-3-phosphoethanolamine + H2O = 2-(5Z,8Z,11Z,14Z)-eicosatetraenoyl-sn-glycero-3-phosphoethanolamine + hexadecanoate + H(+) (RHEA:41348)
• 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphoethanolamine + H2O = 2-(9Z,12Z)-octadecadienoyl-sn-glycero-3-phosphoethanolamine + hexadecanoate + H(+) (RHEA:45164)
• 1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphoethanolamine + 1,2-dihexadecanoyl-sn-glycero-3-phosphocholine = N-hexadecanoyl-1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphoethanolamine + 2-hexadecanoyl-sn-glycero-3-phosphocholine + H(+) (RHEA:45172)

UniProt features (9 total): active site 3, topological domain 2, chain 1, transmembrane region 1, domain 1, mutagenesis site 1

Structure

Experimental structures (PDB)

1 structures.

PDB	Method	Resolution (Å)
4DPZ	X-RAY DIFFRACTION	1.25

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9NWW9-F1	79.40	0.56

Functional residue map

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

Catalytic / active sites (3): 23; 35; 113 (acyl-thioester intermediate)

Mutagenesis-validated functional residues (1):

Position	Phenotype
113	loss of n-acyltransferase activity.

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

ID	Pathway
R-HSA-1482839	Acyl chain remodelling of PE

MSigDB gene sets: 70 (showing top): GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_PHOSPHATIDYLCHOLINE_METABOLIC_PROCESS, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_GLYCEROLIPID_METABOLIC_PROCESS, SENGUPTA_NASOPHARYNGEAL_CARCINOMA_DN, GOBP_AMIDE_METABOLIC_PROCESS, GOBP_GLYCEROPHOSPHOLIPID_METABOLIC_PROCESS, GOBP_LIPID_METABOLIC_PROCESS, SABATES_COLORECTAL_ADENOMA_DN, GOBP_LIPID_CATABOLIC_PROCESS, GOBP_PHOSPHATIDYLETHANOLAMINE_ACYL_CHAIN_REMODELING, CHIANG_LIVER_CANCER_SUBCLASS_CTNNB1_UP, GOMF_HYDROLASE_ACTIVITY_ACTING_ON_ESTER_BONDS, GOMF_ACYLTRANSFERASE_ACTIVITY, GOMF_CARBOXYLIC_ESTER_HYDROLASE_ACTIVITY

GO Biological Process (4): lipid catabolic process (GO:0016042), phosphatidylethanolamine acyl-chain remodeling (GO:0036152), N-acylphosphatidylethanolamine metabolic process (GO:0070292), lipid metabolic process (GO:0006629)

GO Molecular Function (7): A2-type glycerophospholipase activity (GO:0004623), glycerophospholipid phospholipase A1 activity (GO:0008970), obsolete N-acyltransferase activity (GO:0016410), acyltransferase activity (GO:0016746), protein binding (GO:0005515), transferase activity (GO:0016740), hydrolase activity (GO:0016787)

GO Cellular Component (3): cytoplasm (GO:0005737), cytosol (GO:0005829), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
Glycerophospholipid biosynthesis	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
catalytic activity	2
lipid metabolic process	1
catabolic process	1
phosphatidylcholine metabolic process	1
phosphatidylethanolamine metabolic process	1
primary metabolic process	1
glycerophospholipase activity	1
carboxylic ester hydrolase activity	1
A1-type glycerophospholipase activity	1
transferase activity	1
binding	1
intracellular anatomical structure	1
cytoplasm	1

Protein interactions and networks

STRING

2506 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PLAAT2	LRATD2	Q96KN1	496
PLAAT2	SLC25A24	Q6NUK1	474
PLAAT2	DNAJC15	Q9Y5T4	462
PLAAT2	APOL2	Q9BQE5	456
PLAAT2	LAPTM4B	Q86VI4	433
PLAAT2	SSC4D	Q8WTU2	432
PLAAT2	FIG4	Q92562	429
PLAAT2	SEMA4A	Q9H3S1	423
PLAAT2	BCO1	Q9HAY6	421
PLAAT2	RPE65	Q16518	412
PLAAT2	ISX	Q2M1V0	410
PLAAT2	SAA4	P35542	406
PLAAT2	LRATD1	Q96KN4	401
PLAAT2	SPATA45	Q537H7	396
PLAAT2	OR6K3	Q8NGY3	396

IntAct

20 interactions, top by confidence:

A	B	Type	Score
PLAAT2	UBQLN2	psi-mi:“MI:0915”(physical association)	0.560
HPCAL1	PLAAT2	psi-mi:“MI:0915”(physical association)	0.560
NCALD	PLAAT2	psi-mi:“MI:0915”(physical association)	0.560
PLAAT2	UBQLN1	psi-mi:“MI:0915”(physical association)	0.560
ASPH	PLAAT2	psi-mi:“MI:0915”(physical association)	0.560
UBAC1	PLAAT2	psi-mi:“MI:0915”(physical association)	0.560
PLAAT2	COPS2	psi-mi:“MI:0914”(association)	0.350
PLAAT2	UBQLN2	psi-mi:“MI:0915”(physical association)	0.000
PLAAT2	HPCAL1	psi-mi:“MI:0915”(physical association)	0.000
PLAAT2	NCALD	psi-mi:“MI:0915”(physical association)	0.000
UBQLN1	PLAAT2	psi-mi:“MI:0915”(physical association)	0.000
UBAC1	PLAAT2	psi-mi:“MI:0915”(physical association)	0.000
NCALD	PLAAT2	psi-mi:“MI:0915”(physical association)	0.000
ASPH	PLAAT2	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (12): HRASLS2 (Two-hybrid), HRASLS2 (Two-hybrid), HRASLS2 (Two-hybrid), UBQLN1 (Two-hybrid), UBQLN2 (Two-hybrid), ASPH (Two-hybrid), COPS7A (Affinity Capture-MS), BTBD1 (Affinity Capture-MS), GHITM (Affinity Capture-MS), COPS2 (Affinity Capture-MS), RABGAP1 (Affinity Capture-MS), SCAF8 (Affinity Capture-MS)

ESM2 similar proteins: A0A0R4IY06, B8BKI7, D2KX21, D3ZLY0, E0CSI1, O54909, O75452, O88451, P00860, P09057, P11926, P14019, P17516, P27117, P27118, P27119, P27120, P50170, P53816, P53817, P55006, P70694, P97872, Q04799, Q1XAA8, Q2R483, Q3T067, Q3UFY7, Q571F8, Q5R611, Q6AY30, Q6AYP7, Q6P4H8, Q86TW2, Q86V88, Q8R127, Q8R2J9, Q8R3U1, Q8VDG3, Q93V51

Diamond homologs: A0A0R4IY06, D2KX21, P53816, P53817, Q4KLN5, Q5R611, Q8R3U1, Q96KN8, Q9BGL2, Q9CPX5, Q9HDD0, Q9JI61, Q9NWW9, Q9QZU4, Q9UL19, O95237, Q9JI60, Q3ZCA1, Q96KN1, Q96KN4, Q9D650

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	16
Likely benign	2
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

767 predictions. Top by Δscore:

Variant	Effect	Δscore
11:63560077:AT:A	donor_gain	1.0000
11:63560078:T:TA	donor_gain	1.0000
11:63560079:CCTTA:C	donor_loss	1.0000
11:63560080:CTTA:C	donor_loss	1.0000
11:63560081:TTA:T	donor_loss	1.0000
11:63560082:TA:T	donor_loss	1.0000
11:63560083:A:AC	donor_gain	1.0000
11:63560084:C:CG	donor_gain	1.0000
11:63560084:CTTG:C	donor_gain	1.0000
11:63560189:CTGGC:C	acceptor_gain	1.0000
11:63560190:TGGC:T	acceptor_gain	1.0000
11:63560191:GGC:G	acceptor_gain	1.0000
11:63560192:GC:G	acceptor_gain	1.0000
11:63560193:CC:C	acceptor_gain	1.0000
11:63560193:CCTG:C	acceptor_loss	1.0000
11:63560194:C:CC	acceptor_gain	1.0000
11:63560194:CT:C	acceptor_loss	1.0000
11:63560195:T:C	acceptor_loss	1.0000
11:63560201:A:T	acceptor_gain	1.0000
11:63558391:CCTGG:C	donor_gain	0.9900
11:63560197:C:CT	acceptor_gain	0.9900
11:63560198:A:T	acceptor_gain	0.9900
11:63560200:C:CT	acceptor_gain	0.9900
11:63563310:ACTT:A	donor_loss	0.9900
11:63563311:CTTA:C	donor_loss	0.9900
11:63563312:TTA:T	donor_loss	0.9900
11:63563313:TACCA:T	donor_loss	0.9900
11:63563314:A:AC	donor_gain	0.9900
11:63563314:ACCAA:A	donor_loss	0.9900
11:63563315:C:CC	donor_gain	0.9900

AlphaMissense

1029 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
11:63558418:G:T	R121S	0.990
11:63558431:G:C	F116L	0.984
11:63558431:G:T	F116L	0.984
11:63558433:A:G	F116L	0.984
11:63560156:A:G	I16T	0.984
11:63558443:G:C	N112K	0.981
11:63558443:G:T	N112K	0.981
11:63560131:C:A	W24C	0.980
11:63560131:C:G	W24C	0.980
11:63558432:A:G	F116S	0.979
11:63558398:A:C	S127R	0.978
11:63558398:A:T	S127R	0.978
11:63558400:T:G	S127R	0.978
11:63558437:C:A	E114D	0.978
11:63558437:C:G	E114D	0.978
11:63560102:A:T	V34D	0.977
11:63558432:A:C	F116C	0.976
11:63558600:A:T	V60E	0.976
11:63558441:C:T	C113Y	0.974
11:63558596:C:A	K61N	0.974
11:63558596:C:G	K61N	0.974
11:63558418:G:C	R121G	0.973
11:63558438:T:A	E114V	0.973
11:63560134:G:C	H23Q	0.973
11:63560134:G:T	H23Q	0.973
11:63558417:C:G	R121P	0.972
11:63560098:A:C	H35Q	0.972
11:63560098:A:T	H35Q	0.972
11:63558434:G:C	H115Q	0.971
11:63558434:G:T	H115Q	0.971

dbSNP variants (sampled 300 via entrez): RS1000200410 (11:63564175 A>C), RS1000374891 (11:63557478 G>T), RS1000407303 (11:63557776 G>A), RS1001346669 (11:63556382 A>G), RS1001420368 (11:63555989 A>G), RS1001709402 (11:63563759 T>C), RS1001964155 (11:63557312 G>A), RS1002156948 (11:63563573 G>T), RS1002652398 (11:63562483 A>G), RS1002936189 (11:63555228 G>T), RS1002967537 (11:63555393 A>C,G), RS1002983134 (11:63557643 G>A), RS1003054693 (11:63557292 G>A), RS1003263144 (11:63552545 A>G), RS1003316748 (11:63558908 T>C)

Disease associations

OMIM: gene MIM:613866 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST008972_211	Urate levels	1.000000e-76
GCST008972_64	Urate levels	2.000000e-101

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0004531	urate measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4630860 (SINGLE PROTEIN)

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

ChEMBL bioactivities

33 potent at pChembl≥5 of 33 total, top 33 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.30	IC50	50.12	nM	CHEMBL4643782
6.80	IC50	158.5	nM	CHEMBL4639199
6.70	IC50	199.5	nM	CHEMBL4649677
6.60	IC50	251.2	nM	CHEMBL4639478
6.30	IC50	501.2	nM	CHEMBL4645342
6.30	IC50	501.2	nM	CHEMBL4644464
6.20	IC50	631	nM	CHEMBL4643675
6.20	IC50	631	nM	CHEMBL4636463
6.20	IC50	631	nM	CHEMBL4636806
6.10	IC50	794.3	nM	CHEMBL4641977
5.90	IC50	1259	nM	CHEMBL4639235
5.90	IC50	1259	nM	CHEMBL4645578
5.90	IC50	1259	nM	CHEMBL4643099
5.80	IC50	1585	nM	CHEMBL4645552
5.80	IC50	1585	nM	CHEMBL4646429
5.80	IC50	1585	nM	CHEMBL4636379
5.70	IC50	1995	nM	CHEMBL4649884
5.70	IC50	1995	nM	CHEMBL4633449
5.70	IC50	1995	nM	CHEMBL4639242
5.70	IC50	1995	nM	CHEMBL4644324
5.60	IC50	2512	nM	CHEMBL4646350
5.60	IC50	2512	nM	CHEMBL4638043
5.60	IC50	2512	nM	CHEMBL4632512
5.60	IC50	2512	nM	CHEMBL4636282
5.50	IC50	3162	nM	CHEMBL4640863
5.50	IC50	3162	nM	CHEMBL4641818
5.40	IC50	3981	nM	CHEMBL4648272
5.30	IC50	5012	nM	CHEMBL4640676
5.30	IC50	5012	nM	CHEMBL4636625
5.30	IC50	5012	nM	CHEMBL4643908
5.20	IC50	6310	nM	CHEMBL4642795
5.10	IC50	7943	nM	CHEMBL4641304
5.10	IC50	7943	nM	CHEMBL4634598

PubChem BioAssay actives

33 with measured affinity, of 67 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
2-oxo-N-[2-(4-phenoxyphenyl)ethyl]-5-phenylpentanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	0.0501	uM
2-oxo-5-phenyl-N-[2-[4-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]ethyl]pentanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	0.1585	uM
2-oxo-5-phenyl-N-[2-[4-[[6-(trifluoromethyl)-3-pyridinyl]oxy]phenyl]ethyl]pentanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	0.1995	uM
N-[2-(4-bromophenyl)ethyl]-2-oxo-5-phenylpentanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	0.2512	uM
2-oxo-5-phenyl-N-[2-(4-pyrazin-2-yloxyphenyl)ethyl]pentanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	0.5012	uM
2-oxo-5-phenyl-N-(2-phenylethyl)pentanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	0.5012	uM
4-(4-chlorophenyl)-2-oxo-N-(4-phenylbutyl)butanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	0.6310	uM
N-[2-[4-(2-chloropyrimidin-4-yl)oxyphenyl]ethyl]-2-oxo-5-phenylpentanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	0.6310	uM
4-(4-chlorophenyl)-2-oxo-N-(2-phenylethyl)butanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	0.6310	uM
N-[2-(3-chlorophenyl)ethyl]-2-oxo-5-phenylpentanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	0.7943	uM
4-(2-chlorophenyl)-2-oxo-N-(2-phenylethyl)butanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	1.2589	uM
N-[2-(2,4-dichlorophenyl)ethyl]-2-oxo-5-phenylpentanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	1.2589	uM
N-[2-(4-hydroxyphenyl)ethyl]-2-oxo-5-phenylpentanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	1.2589	uM
N-[2-(4-methoxyphenyl)ethyl]-2-oxo-5-phenylpentanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	1.5849	uM
(E)-4-(4-methoxyphenyl)-2-oxo-N-(2-phenylethyl)but-3-enamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	1.5849	uM
(E)-4-(4-chlorophenyl)-2-oxo-N-(2-phenylethyl)but-3-enamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	1.5849	uM
4-(3,4-dichlorophenyl)-2-oxo-N-(2-phenylethyl)butanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	1.9953	uM
N-[2-(4-methylphenyl)ethyl]-2-oxo-5-phenylpentanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	1.9953	uM
2-oxo-5-phenyl-N-[2-(4-pyrimidin-2-yloxyphenyl)ethyl]pentanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	1.9953	uM
2-oxo-N-(2-phenylethyl)-4-[4-(trifluoromethyl)phenyl]butanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	1.9953	uM
4-(3-chlorophenyl)-2-oxo-N-(2-phenylethyl)butanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	2.5119	uM
4-(4-chlorophenyl)-N-ethyl-2-oxobutanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	2.5119	uM
(E)-2-oxo-N-(2-phenylethyl)-4-(3-phenylphenyl)but-3-enamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	2.5119	uM
N-benzyl-4-(4-chlorophenyl)-2-oxobutanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	2.5119	uM
2-oxo-6-phenyl-N-(2-phenylethyl)hexanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	3.1623	uM
4-(4-methoxyphenyl)-2-oxo-N-(2-phenylethyl)butanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	3.1623	uM
2-oxo-4-(4-phenoxyphenyl)-N-(2-phenylethyl)butanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	3.9811	uM
(E)-4-(4-bromophenyl)-2-oxo-N-(2-phenylethyl)but-3-enamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	5.0119	uM
4-(4-methylphenyl)-2-oxo-N-(2-phenylethyl)butanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	5.0119	uM
N-[2-(3,4-dimethoxyphenyl)ethyl]-2-oxo-5-phenylpentanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	5.0119	uM
N-[2-(2-chlorophenyl)ethyl]-2-oxo-5-phenylpentanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	6.3096	uM
(E)-2-oxo-4-phenyl-N-(2-phenylethyl)but-3-enamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	7.9433	uM
4-(4-fluorophenyl)-2-oxo-N-(2-phenylethyl)butanamide	1666051: Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	ic50	7.9433	uM

CTD chemical–gene interactions

21 total (human), top 21 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Cadmium Chloride	increases expression	2
bisphenol A	increases expression	1
arsenite	increases reaction, affects binding	1
sulforaphane	decreases expression	1
tris(1,3-dichloro-2-propyl)phosphate	decreases expression	1
sodium arsenite	increases expression	1
tamibarotene	increases expression	1
abrine	increases expression	1
jinfukang	increases expression, affects cotreatment	1
Benzo(a)pyrene	increases methylation	1
Cisplatin	increases expression, affects cotreatment	1
Demecolcine	increases expression	1
Hydrogen Peroxide	affects expression	1
Ibuprofen	increases expression	1
Metformin	increases expression	1
Rifampin	decreases expression	1
Silicon Dioxide	decreases expression	1
Tobacco Smoke Pollution	affects expression	1
Valproic Acid	decreases expression	1
Aflatoxin B1	increases expression	1
Okadaic Acid	increases expression	1

ChEMBL screening assays

12 unique, capped per target: 12 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4626912	Binding	Inhibition of full-length C-terminal FLAG-tagged human PLAAT2 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis	Structure-Activity Relationship Studies of α-Ketoamides as Inhibitors of the Phospholipase A and Acyltransferase Enzyme Family. — J Med Chem

Clinical trials (associated diseases)

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