DGKA

Summary

DGKA (diacylglycerol kinase alpha, HGNC:2849) is a protein-coding gene on chromosome 12q13.2, encoding Diacylglycerol kinase alpha (P23743). Diacylglycerol kinase that converts diacylglycerol/DAG into phosphatidic acid/phosphatidate/PA and regulates the respective levels of these two bioactive lipids.

The protein encoded by this gene belongs to the eukaryotic diacylglycerol kinase family. It acts as a modulator that competes with protein kinase C for the second messenger diacylglycerol in intracellular signaling pathways. It also plays an important role in the resynthesis of phosphatidylinositols and phosphorylating diacylglycerol to phosphatidic acid. Several transcript variants encoding different isoforms have been identified for this gene.

Source: NCBI Gene 1606 — RefSeq curated summary.

At a glance

• GWAS associations: 3
• Clinical variants (ClinVar): 114 total
• Regional missense constraint (gnomAD): 1 of 3 regions constrained (≈2% of expected missense variation)
• GTEx eGene: eQTL in 17 tissues, sQTL in 24 (q < 0.05)
• ChEMBL bioactivity: 1 clinical-phase molecule tested; no curated mechanism-of-action drug
• Constraint (gnomAD): pLI 1.00 (loss-of-function intolerant), LOEUF 0.42 (moderately constrained)
• MANE Select transcript: NM_001345
• Notable: 114 clinical variants but no curated precision-oncology (CIViC) evidence yet

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:2849
Approved symbol	DGKA
Name	diacylglycerol kinase alpha
Location	12q13.2
Locus type	gene with protein product
Status	Approved
Aliases	DGK-alpha
Ensembl gene	ENSG00000065357
Ensembl biotype	protein_coding
OMIM	125855
Entrez	1606

Gene structure

Transcript identifiers

Ensembl transcripts: 52 — 24 retained_intron, 18 protein_coding, 6 nonsense_mediated_decay, 4 protein_coding_CDS_not_defined

MANE Select: ENST00000331886

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 6, TSL 2: 6, TSL 3: 8, TSL 4: 15, TSL 5: 14

ENST00000331886, ENST00000394147, ENST00000402956, ENST00000432422, ENST00000546878, ENST00000546895, ENST00000546995, ENST00000547015, ENST00000547324, ENST00000547358, ENST00000547535, ENST00000548047, ENST00000548378, ENST00000548407, ENST00000548479, ENST00000548491, ENST00000548549, ENST00000549079, ENST00000549085, ENST00000549097, ENST00000549323, ENST00000549368, ENST00000549629, ENST00000549986, ENST00000550115, ENST00000550484, ENST00000550888, ENST00000550957, ENST00000551156, ENST00000551296, ENST00000551585, ENST00000551615, ENST00000551707, ENST00000551739, ENST00000552335, ENST00000552478, ENST00000552652, ENST00000552687, ENST00000552903, ENST00000553084, ENST00000553783, ENST00000554434, ENST00000555025, ENST00000555090, ENST00000555218, ENST00000556001, ENST00000556344, ENST00000557080, ENST00000557180, ENST00000879156, ENST00001007838, ENST00001143538

RefSeq mRNA: 21 — MANE Select: NM_001345 NM_001345, NM_001351033, NM_001351034, NM_001351035, NM_001351036, NM_001351037, NM_001351038, NM_001351039, NM_001351040, NM_001413596, NM_001413597, NM_001413598, NM_001413599, NM_001413600, NM_001413601, NM_001413602, NM_001413603, NM_001413604, NM_201444, NM_201445, NM_201554

CCDS: CCDS8896

Canonical transcript exons

ENST00000331886 — 24 exons

Exon	Start	End
ENSE00001292720	55931162	55931344
ENSE00002324565	55953685	55954023
ENSE00003468510	55937017	55937090
ENSE00003478536	55938915	55938989
ENSE00003480327	55940897	55940980
ENSE00003488180	55953040	55953160
ENSE00003490063	55953350	55953410
ENSE00003494686	55942174	55942263
ENSE00003500650	55939186	55939305
ENSE00003509930	55940314	55940433
ENSE00003531973	55952035	55952099
ENSE00003540649	55941998	55942083
ENSE00003586579	55952341	55952431
ENSE00003590549	55940082	55940170
ENSE00003602142	55941252	55941325
ENSE00003607289	55937408	55937543
ENSE00003613637	55951623	55951783
ENSE00003641213	55940624	55940722
ENSE00003655489	55939415	55939529
ENSE00003659879	55941510	55941584
ENSE00003671883	55952734	55952932
ENSE00003785907	55938511	55938560
ENSE00003787684	55937978	55938052
ENSE00003798460	55936423	55936567

Expression profiles

Bgee: expression breadth ubiquitous, 264 present calls, max score 99.32.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 29.9528 / max 953.9898, expressed in 1760 samples.

Highest expression (Bgee): lower esophagus mucosa, skin of abdomen, esophagus mucosa, skin of leg, granulocyte.

Genetic regulation across tissues (GTEx eQTL / sQTL)

DGKA is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 17 tissues and its splicing (sQTL) in 24 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

showing 20 of 41 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Skin Not Sun Exposed Suprapubic	sqtl	1.1e-40	-0.80	12:55941323:A:G
Skin Sun Exposed Lower leg	sqtl	7.0e-33	-0.70	12:55915071:C:T
Esophagus Mucosa	sqtl	1.7e-24	+0.62	12:55879225:T:G
Nerve Tibial	eqtl	4.7e-17	-0.29	12:55935753:C:T
Whole Blood	sqtl	2.0e-15	-0.49	12:55873729:A:T
Lung	sqtl	3.1e-11	-0.60	12:55952024:G:A
Brain Cerebellar Hemisphere	eqtl	4.5e-11	+0.39	12:55880211:G:A
Brain Cerebellum	eqtl	2.2e-09	+0.42	12:55890222:T:C
Artery Tibial	eqtl	3.8e-09	-0.42	12:55923804:G:A
Artery Aorta	sqtl	2.9e-07	-0.58	12:55909972:G:A
Artery Tibial	sqtl	7.6e-07	-0.42	12:55941323:A:G
Spleen	sqtl	1.6e-06	-0.97	12:55952024:G:A
Adipose Subcutaneous	sqtl	7.3e-06	-0.40	12:55918259:G:A
Skin Sun Exposed Lower leg	eqtl	1.3e-05	-0.10	12:55863919:C:CA
Nerve Tibial	sqtl	1.3e-05	-0.58	12:55952024:G:A
Cells Cultured fibroblasts	sqtl	1.5e-05	-0.49	12:55918259:G:A
Whole Blood	eqtl	1.5e-05	-0.25	12:55923804:G:A
Cells EBV-transformed lymphocytes	sqtl	3.6e-05	-0.55	12:55862478:T:C
Colon Transverse	sqtl	5.6e-05	-0.44	12:55915071:C:T
Brain Cerebellar Hemisphere	sqtl	5.6e-05	-0.63	12:55952024:G:A

FANTOM5 promoters

9 alternative TSS:

Promoter ID	TPM avg	Samples expressed
126003	14.8307	1727
126000	13.6834	1035
126007	0.5517	263
126006	0.5375	256
126001	0.1281	58
125999	0.1125	53
126004	0.0475	20
126005	0.0461	17
126002	0.0152	8

Top tissues by expression

showing 100 of 290 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
lower esophagus mucosa	UBERON:0035834	99.32	gold quality
skin of abdomen	UBERON:0001416	98.46	gold quality
esophagus mucosa	UBERON:0002469	98.44	gold quality
skin of leg	UBERON:0001511	98.32	gold quality
granulocyte	CL:0000094	98.20	gold quality
small intestine Peyer’s patch	UBERON:0003454	97.57	gold quality
spleen	UBERON:0002106	96.97	gold quality
lymph node	UBERON:0000029	96.94	gold quality
mucosa of transverse colon	UBERON:0004991	96.91	gold quality
minor salivary gland	UBERON:0001830	96.88	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	96.84	gold quality
zone of skin	UBERON:0000014	96.69	gold quality
small intestine	UBERON:0002108	96.52	gold quality
tonsil	UBERON:0002372	96.48	gold quality
mouth mucosa	UBERON:0003729	96.00	gold quality
rectum	UBERON:0001052	95.92	gold quality
descending thoracic aorta	UBERON:0002345	95.73	gold quality
transverse colon	UBERON:0001157	95.71	gold quality
vermiform appendix	UBERON:0001154	95.62	gold quality
jejunal mucosa	UBERON:0000399	95.60	gold quality
saliva-secreting gland	UBERON:0001044	95.50	gold quality
thymus	UBERON:0002370	95.48	gold quality
ileal mucosa	UBERON:0000331	95.34	gold quality
ascending aorta	UBERON:0001496	95.34	gold quality
thoracic aorta	UBERON:0001515	95.29	gold quality
vagina	UBERON:0000996	95.28	gold quality
esophagus	UBERON:0001043	95.21	gold quality
duodenum	UBERON:0002114	94.88	gold quality
ectocervix	UBERON:0012249	94.83	gold quality
blood	UBERON:0000178	94.82	gold quality
right lung	UBERON:0002167	94.72	gold quality
bone marrow cell	CL:0002092	94.69	gold quality
gall bladder	UBERON:0002110	94.52	gold quality
colonic epithelium	UBERON:0000397	94.24	gold quality
upper leg skin	UBERON:0004262	94.11	gold quality
body of pancreas	UBERON:0001150	93.97	gold quality
left uterine tube	UBERON:0001303	93.96	gold quality
right coronary artery	UBERON:0001625	93.82	gold quality
stromal cell of endometrium	CL:0002255	93.52	gold quality
caecum	UBERON:0001153	93.27	gold quality
right hemisphere of cerebellum	UBERON:0014890	93.23	gold quality
endocervix	UBERON:0000458	93.11	gold quality
oral cavity	UBERON:0000167	93.07	gold quality
right ovary	UBERON:0002118	92.96	gold quality
mucosa of stomach	UBERON:0001199	92.92	gold quality
intestine	UBERON:0000160	92.87	gold quality
right frontal lobe	UBERON:0002810	92.79	gold quality
upper arm skin	UBERON:0004263	92.78	gold quality
cerebellar hemisphere	UBERON:0002245	92.74	gold quality
cerebellar cortex	UBERON:0002129	92.71	gold quality
body of uterus	UBERON:0009853	92.71	gold quality
leukocyte	CL:0000738	92.41	gold quality
left coronary artery	UBERON:0001626	92.41	gold quality
tibial nerve	UBERON:0001323	92.26	gold quality
upper lobe of left lung	UBERON:0008952	92.23	gold quality
colon	UBERON:0001155	92.09	gold quality
left ovary	UBERON:0002119	92.07	gold quality
mononuclear cell	CL:0000842	91.96	gold quality
monocyte	CL:0000576	91.87	gold quality
large intestine	UBERON:0000059	91.85	gold quality
aorta	UBERON:0000947	91.84	gold quality
esophagus squamous epithelium	UBERON:0006920	91.58	gold quality
epithelium of esophagus	UBERON:0001976	91.54	gold quality
body of stomach	UBERON:0001161	91.53	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	91.53	gold quality
lower esophagus	UBERON:0013473	91.51	gold quality
lower esophagus muscularis layer	UBERON:0035833	91.48	gold quality
omental fat pad	UBERON:0010414	91.46	gold quality
urinary bladder	UBERON:0001255	91.41	gold quality
peritoneum	UBERON:0002358	91.40	gold quality
tongue squamous epithelium	UBERON:0006919	91.39	gold quality
coronary artery	UBERON:0001621	91.38	gold quality
sural nerve	UBERON:0015488	91.12	gold quality
prostate gland	UBERON:0002367	91.11	gold quality
buccal mucosa cell	CL:0002336	90.92	gold quality
muscle layer of sigmoid colon	UBERON:0035805	90.90	gold quality
cerebellum	UBERON:0002037	90.84	gold quality
upper lobe of lung	UBERON:0008948	90.80	gold quality
nucleus accumbens	UBERON:0001882	90.78	gold quality
anterior cingulate cortex	UBERON:0009835	90.64	gold quality
cingulate cortex	UBERON:0003027	90.63	gold quality
pancreas	UBERON:0001264	90.40	gold quality
left adrenal gland cortex	UBERON:0035825	90.22	gold quality
adipose tissue of abdominal region	UBERON:0007808	90.18	gold quality
right adrenal gland cortex	UBERON:0035827	90.03	gold quality
skin of hip	UBERON:0001554	90.00	gold quality
right adrenal gland	UBERON:0001233	89.99	gold quality
parotid gland	UBERON:0001831	89.98	gold quality
bone marrow	UBERON:0002371	89.95	gold quality
left adrenal gland	UBERON:0001234	89.88	gold quality
stomach	UBERON:0000945	89.84	gold quality
sigmoid colon	UBERON:0001159	89.78	gold quality
nasal cavity epithelium	UBERON:0005384	89.71	gold quality
gingiva	UBERON:0001828	89.48	gold quality
popliteal artery	UBERON:0002250	89.41	gold quality
tibial artery	UBERON:0007610	89.41	gold quality
adenohypophysis	UBERON:0002196	89.33	gold quality
gingival epithelium	UBERON:0001949	89.22	gold quality
adrenal gland	UBERON:0002369	89.17	gold quality
right lobe of thyroid gland	UBERON:0001119	89.10	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-CURD-122	yes	32.98
E-ANND-3	no	0.00

HPA expression

RNA tissue specificity: Tissue enhanced

showing 60 of 79 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Thymus	tissue	184.5
Tonsil	tissue	95.4	high
Lymph node	tissue	89.0	medium
Skin 1	tissue	79.7	medium
Esophagus	tissue	53.0	medium
Duodenum	tissue	48.0	medium
Appendix	tissue	47.1	low
Small intestine	tissue	38.2	medium
Spleen	tissue	36.8	high
Vagina	tissue	36.5	medium
Bone marrow	tissue	30.0	low
Urinary bladder	tissue	26.5	medium
Rectum	tissue	25.3	low
Colon	tissue	23.9	low
Salivary gland	tissue	18.9	medium
Nucleus accumbens	tissue	18.9
Spinal cord	tissue	17.3
Cerebellum	tissue	17.2	medium
Cerebral cortex	tissue	15.7	medium
Somatosensory cortex	tissue	15.7
Substantia nigra	tissue	15.6
Prefrontal cortex	tissue	15.1
Gallbladder	tissue	14.8	medium
Retrosplenial and cingulate cortex	tissue	14.4
Occipital cortex	tissue	14.3
Placenta	tissue	14.0	medium
Temporal cortex	tissue	14.0
Retrosplenial cortex	tissue	13.6
Insular cortex	tissue	13.6
Motor cortex	tissue	13.5
Smooth muscle	tissue	13.2	medium
Choroid plexus	tissue	13.2
Hippocampal formation	tissue	13.0
Entorhinal cortex	tissue	13.0
Medulla oblongata	tissue	12.9
Pancreas	tissue	12.3	low
Midbrain	tissue	12.1
Prostate	tissue	11.9	not detected
Ventral forebrain	tissue	11.8
Corpus callosum	tissue	11.7
Stomach 1	tissue	11.6	medium
Testis	tissue	11.5	medium
Amygdala	tissue	11.5
Parathyroid gland	tissue	11.2	medium
Pons	tissue	11.1
Basal ganglia	tissue	11.0	low
Thalamus	tissue	10.8
Septum	tissue	10.7
Superior colliculi	tissue	10.6
Olfactory bulb	tissue	10.5
Hippocampus	tissue	10.4	medium
Postcentral gyrus	tissue	10.2
Adipose tissue	tissue	9.7	not detected
Lung	tissue	9.7	medium
Epididymis	tissue	9.4	not detected
Hypothalamus	tissue	9.4
Cervix	tissue	9.2	not detected
Putamen	tissue	9.1
Periaqueductal gray	tissue	9.1
Seminal vesicle	tissue	9.0

Brain sub-regions (HPA Brain Atlas): detected in 192; highest nTPM — Blood vessel (24.6), Ventral spinal cord (17.3), Temporal pole (16.4), Dorsal spinal cord (14.9), Caudate nucleus (14.6).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): FOXO1, FOXO3

miRNA regulators (miRDB)

Targeting DGKA by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

showing 30 of 36 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-200B-3P	100.00	73.31	2693
HSA-MIR-200C-3P	100.00	73.35	2685
HSA-MIR-429	100.00	73.44	2698
HSA-MIR-6867-5P	100.00	82.21	3464
HSA-MIR-4455	100.00	65.48	1587
HSA-MIR-1827	99.63	68.57	3265
HSA-MIR-6134	99.63	65.68	1537
HSA-MIR-892A	99.54	68.16	1141
HSA-MIR-1207-5P	99.49	69.11	2983
HSA-MIR-297	99.40	69.58	1418
HSA-MIR-4318	99.38	66.94	1505
HSA-MIR-892C-5P	99.16	70.56	2116
HSA-MIR-3688-5P	99.12	69.67	1091
HSA-MIR-4763-3P	99.10	67.83	2649
HSA-MIR-6868-5P	99.06	65.69	1284
HSA-MIR-4260	98.78	65.37	848
HSA-MIR-5572	98.55	65.84	970
HSA-MIR-4722-5P	98.46	66.34	1611
HSA-MIR-6804-5P	98.39	65.77	1084
HSA-MIR-4664-5P	98.17	65.07	1020
HSA-MIR-891A-3P	98.05	67.99	970
HSA-MIR-4443	98.02	66.25	1928
HSA-MIR-6819-5P	97.96	66.59	1071
HSA-MIR-4736	97.96	65.89	1287
HSA-MIR-450A-2-3P	97.91	67.56	1459
HSA-MIR-7113-5P	97.88	67.33	1735
HSA-MIR-6737-5P	97.75	66.54	1044
HSA-MIR-4433A-3P	97.75	62.82	1435
HSA-MIR-4733-5P	97.75	67.44	866
HSA-MIR-6783-5P	97.67	67.21	1528

Functional genomics

gnomAD constraint: pLI 1, LOEUF 0.419, missense Z 3.55 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD)

ENST00000331886 splits into 3 regions with different missense tolerance; 1 is missense-constrained (≈2% of the expected missense variation). Missense variants in a constrained region (low observed/expected) are more likely to be pathogenic. gnomAD

Region (GRCh38)	Missense obs / exp	o/e	Constrained
12:55,936,504–55,952,096	504 / 681.2	0.74	no
12:55,952,097–55,952,388	3 / 20.4	0.15	yes (p 1.2e-04)
12:55,952,389–55,953,765	158 / 213.4	0.74	no

Literature-anchored findings (GeneRIF, showing 36)

• Defects in both polymorphonuclear neutrophil (PMN) transendothelial migration and PMN diacylglycerol kinase alpha signaling are implicated as disordered functions in subjects with localized aggressive periodontitis. (PMID:14734770)
• PPARgamma agonists upregulate DGKalpha production.This suppresses the diacylglycerol/protein-kinase-C signaling pathway. (PMID:15117825)
• DGKalpha is crucial for the control of cell activation and also for the regulation of the secretion of lethal exosomes, which in turn controls cell death. (PMID:15870081)
• ALK-mediated alphaDGK activation is dependent on p60src tyrosine kinase, with which alphaDGK forms a complex; alphaDGK activation is involved in the control of ALK-mediated mitogenic properties. (PMID:15928040)
• These results strongly suggest that DGKalpha is a novel positive regulator of NF-kappaB, which suppresses TNF-alpha-induced melanoma cell apoptosis. (PMID:17276726)
• diacylglycerol kinase alpha-conserved domains have a role in membrane targeting in intact T cells (PMID:17911109)
• 2,3-dioleoylglycerol binds to a site on the alpha and zeta isoforms of diacylglycerol kinase that is exposed as a consequence of the substrate binding to the active site. (PMID:18004883)
• Lck-dependent tyrosine phosphorylation of diacylglycerol kinase alpha regulates its membrane association in T cells.( (PMID:18424699)
• These results strongly suggest that DGKalpha positively regulates TNF-alpha-dependent NF-kappaB activation via the PKCzeta-mediated Ser311 phosphorylation of p65/RelA. (PMID:19751727)
• Diacylglycerol kinase alpha is a key regulator of the polarised secretion of exosomes. (PMID:21252909)
• findings further suggest that DGL-alpha and -beta may regulate neurite outgrowth by engaging temporally and spatially distinct molecular pathways (PMID:21493725)
• SAP-mediated inhibition of DGKalpha sustains diacylglycerol signaling, thereby regulating T cell activation (PMID:22048771)
• Antigen-specific CD8-positive T cells from DGKalpha-deficient transgenic mice show enhanced expansion and increased cytokine production after lymphocytic choriomeningitis virus infection, yet DGK-deficient memory CD8+ T cells exhibit impaired expansion. (PMID:22271650)
• DGKalpha is involved in hepatocellular carcinoma progression by activation of the MAPK pathway. (PMID:22425622)
• DGK-alpha was more highly expressed in CD8-tumor-infiltrating T cellscompared with that in CD8non-tumor kidney-infiltrating lymphocytes. (PMID:22573804)
• High diacylglycerol kinase alpha expression is associated with glioblastoma. (PMID:24158111)
• These data indicates the existence of a SDF-1alpha induced DGKalpha - atypical PKC - beta1 integrin signaling pathway, which is essential for matrix invasion of carcinoma cells. (PMID:24887021)
• DGKalpha generates phosphatidic acid to drive its own recruitment to tubular recycling endosomes via its interaction with MICAL-L1 (PMID:25248744)
• Redundant and specialized roles for diacylglycerol kinases alpha and zeta in the control of T cell functions. (PMID:25921290)
• An abandoned compound that also inhibits serotonin receptors may have more translational potential as a DGKa inhibitor, but more potent and specific DGKa inhibitors are sorely needed (PMID:26420856)
• Decreased DNA methylation at this enhancer enables recruitment of the profibrotic transcription factor early growth response 1 (EGR1) and facilitates radiation-induced DGKA transcription in cells from patients later developing fibrosis. (PMID:26964756)
• LIPFDGKA might serve as a potential possible biomarkers for diagnosis of gastric cancer, and their downregulation may bring new perspective into the investigation of gastric cancer prognosis (PMID:27498782)
• Diacylglycerol kinases alpha and zeta are up-regulated in cancer in cancer, and contribute towards tumor immune evasion and T cells clonal anergy. (Review) (PMID:27697466)
• DGKalpha isoform is highly expressed in the nuclei of human erythroleukemia cell line K562, and its nuclear activity drives K562 cells through the G1/S transition during cell cycle progression. (PMID:27731506)
• This novel study demonstrates efficient ablation of diacylglycerol kinase in human CAR-T cells that leads to improved antitumor immunity and may have significant impact in human cancer immunotherapy (PMID:29967261)
• This study presents the first crystal structure of EF-hand domains of diacylglycerol kinase alpha in its Ca(2+) bound form and characterize Ca(2+) -induced conformational changes, which likely regulates intra-molecular interactions. (PMID:30653270)
• Upon neutrophil stimulation, DGK-alpha activation is necessary for migration and a productive response. This paper focuses on the role of DGK-alpha in obstructive respiratory diseases, including asthma and chronic obstructive pulmonary disease, but also rare genetic diseases such as alpha-1-antitrypsin deficiency. [review] (PMID:31766109)
• DGKA Provides Platinum Resistance in Ovarian Cancer Through Activation of c-JUN-WEE1 Signaling. (PMID:32341033)
• Diacylglycerol kinases regulate TRPV1 channel activity. (PMID:32345612)
• DGKA Mediates Resistance to PD-1 Blockade. (PMID:33608256)
• Diacylglycerol Kinase Inhibition Reduces Airway Contraction by Negative Feedback Regulation of Gq-Signaling. (PMID:34293268)
• DGKA interacts with SRC/FAK to promote the metastasis of non-small cell lung cancer. (PMID:35131384)
• Targeting diacylglycerol kinase alpha impairs lung tumorigenesis by inhibiting cyclin D3. (PMID:36965165)
• Multiomics analysis reveals metabolic subtypes and identifies diacylglycerol kinase alpha (DGKA) as a potential therapeutic target for intrahepatic cholangiocarcinoma. (PMID:38143235)
• Tumor-associated macrophage (TAM)-secreted CCL22 confers cisplatin resistance of esophageal squamous cell carcinoma (ESCC) cells via regulating the activity of diacylglycerol kinase alpha (DGKalpha)/NOX4 axis. (PMID:38387281)
• Diacylglycerol kinase alpha is a proliferation marker of intrahepatic cholangiocarcinoma associated with the prognosis. (PMID:38716625)

Cross-species orthologs

8 orthologs

Organism	Symbol	Gene ID
danio_rerio	dgkaa	ENSDARG00000060626
danio_rerio	dgkab	ENSDARG00000098175
mus_musculus	Dgka	ENSMUSG00000025357
rattus_norvegicus	Dgka	ENSRNOG00000022943
drosophila_melanogaster	CG34384	FBGN0085413
drosophila_melanogaster	rdgA	FBGN0261549
caenorhabditis_elegans		WBGENE00006483
caenorhabditis_elegans		WBGENE00019428

Paralogs (9): DGKG (ENSG00000058866), DGKD (ENSG00000077044), DGKH (ENSG00000102780), DGKB (ENSG00000136267), DGKQ (ENSG00000145214), DGKZ (ENSG00000149091), DGKE (ENSG00000153933), DGKI (ENSG00000157680), DGKK (ENSG00000274588)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:102952) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 3 distinct phenotype terms.

Mouse phenotype (MP)	Records
abnormal lymphocyte anergy	1
increased T cell number	1
increased interleukin-2 secretion	1

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Drosophila sechellia	B4I4Y1	98.1%	Diamond
Drosophila simulans	B4R0A5	98.1%	Diamond
Drosophila yakuba	B4PRE2	97.6%	Diamond
Bos taurus	A0JN54	97.1%	Diamond
Drosophila erecta	B3NYS4	97.1%	Diamond
Sus scrofa	P20192	97.1%	Diamond
Drosophila ananassae	B3LXF2	90.2%	Diamond
Drosophila grimshawi	B4JHJ7	87.6%	Diamond
Drosophila mojavensis	B4K6T8	87.6%	Diamond
Debaryomyces hansenii CBS767	Q6BWS8	78.2%	Diamond
Arabidopsis thaliana	Q39017	51.5%	Diamond
Dictyostelium discoideum	P34125	47.6%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
RAB5B	protein-coding	5869
PMEL	protein-coding	6490
SUOX	protein-coding	6821
PYM1	protein-coding	84305
CDK2	protein-coding	1017

Protein

Protein identifiers

Diacylglycerol kinase alpha — P23743 (reviewed: P23743)

Alternative names: 80 kDa diacylglycerol kinase, Diglyceride kinase alpha

All UniProt accessions (12): C9JM35, P23743, F8VNZ9, F8VWX8, F8W1H7, F8W1M3, G3V312, G3V327, G3V4E1, G3V4I3, H0YJE7, H0YJH4

UniProt curated annotations — full annotation on UniProt →

Function. Diacylglycerol kinase that converts diacylglycerol/DAG into phosphatidic acid/phosphatidate/PA and regulates the respective levels of these two bioactive lipids. Thereby, acts as a central switch between the signaling pathways activated by these second messengers with different cellular targets and opposite effects in numerous biological processes. Also plays an important role in the biosynthesis of complex lipids. Can also phosphorylate 1-alkyl-2-acylglycerol in vitro as efficiently as diacylglycerol provided it contains an arachidonoyl group. Also involved in the production of alkyl-lysophosphatidic acid, another bioactive lipid, through the phosphorylation of 1-alkyl-2-acetyl glycerol.

Subunit / interactions. Monomer.

Subcellular location. Cytoplasm. Cytosol.

Tissue specificity. Expressed in lymphocytes.

Activity regulation. Stimulated by calcium and phosphatidylserine.

Pathway. Lipid metabolism; glycerolipid metabolism.

Miscellaneous. May be produced at very low levels due to a premature stop codon in the mRNA, leading to nonsense-mediated mRNA decay.

Similarity. Belongs to the eukaryotic diacylglycerol kinase family.

Isoforms (3)

UniProt ID	Names	Canonical?
P23743-1	1	yes
P23743-2	2
P23743-3	3

RefSeq proteins (21): NP_001336, NP_001337962, NP_001337963, NP_001337964, NP_001337965, NP_001337966, NP_001337967, NP_001337968, NP_001337969, NP_001400525, NP_001400526, NP_001400527, NP_001400528, NP_001400529, NP_001400530, NP_001400531, NP_001400532, NP_001400533, NP_958852, NP_958853, NP_963848 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000756	Diacylglycerol_kin_accessory	Domain
IPR001206	Diacylglycerol_kinase_cat_dom	Domain
IPR002048	EF_hand_dom	Domain
IPR002219	PKC_DAG/PE	Domain
IPR011992	EF-hand-dom_pair	Homologous_superfamily
IPR016064	NAD/diacylglycerol_kinase_sf	Homologous_superfamily
IPR017438	ATP-NAD_kinase_N	Homologous_superfamily
IPR018247	EF_Hand_1_Ca_BS	Binding_site
IPR029477	DAG_kinase_typeI_N	Domain
IPR037607	DGK	Family
IPR038199	DGK_typeI_N_sf	Homologous_superfamily
IPR046349	C1-like_sf	Homologous_superfamily
IPR047469	C1_DGKalpha_rpt2	Domain

Pfam: PF00130, PF00609, PF00781, PF14513

Enzyme classification (BRENDA)

• EC 2.7.1.107 — diacylglycerol kinase (ATP) (BRENDA: 27 organisms, 171 substrates, 108 inhibitors, 81 Km, 16 kcat entries)

Substrate kinetics (BRENDA)

16 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ATP	0.05–4.8	46
GTP	0.03–8.7	5
DIOLEIN	0.05–0.08	3
1,2-DIARACHIDONOYL-GLYCEROL	0.09–0.14	2
1-STEAROYL-2-ARACHIDONOYL-SN-GLYCEROL	0.07–0.09	2
SN-1,2-DIOLEOYLGLYCEROL	0.1–0.125	2
1,2-DIACYL-SN-GLYCEROL	0.25	1
1,2-DIOLEIN	0.45	1
1,2-DIOLEOYL-SN-GLYCEROL	0.125	1
2’-DEOXY-ATP	4.2	1
ADP	1	1
CERAMIDE	0.23	1
DIOLEOYLGLYCEROL	0.9	1
ITP	5.9	1
1-STEAROYL-2-LINOLEOYL-SN-GLYCEROL	—	0

Catalyzed reactions (Rhea)

• a 1,2-diacyl-sn-glycerol + ATP = a 1,2-diacyl-sn-glycero-3-phosphate + ADP + H(+) (RHEA:10272)
• a 1-O-alkyl-sn-glycerol + ATP = a 1-O-alkyl-sn-glycero-3-phosphate + ADP + H(+) (RHEA:16937)
• 1-octadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycerol + ATP = 1-octadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycero-3-phosphate + ADP + H(+) (RHEA:40323)
• 1,2-di-(9Z-octadecenoyl)-sn-glycerol + ATP = 1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphate + ADP + H(+) (RHEA:40327)
• 1-O-hexadecyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycerol + ATP = 1-O-hexadecyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycero-3-phosphate + ADP + H(+) (RHEA:40403)
• 1-O-hexadecyl-2-(9Z-octadecenoyl)-sn-glycerol + ATP = 1-O-hexadecyl-2-(9Z-octadecenoyl)-sn-glycero-3-phosphate + ADP + H(+) (RHEA:40407)
• 1-O-hexadecyl-sn-glycerol + ATP = 1-O-hexadecyl-sn-glycero-3-phosphate + ADP + H(+) (RHEA:41672)
• 1-O-hexadecyl-2-acetyl-sn-glycerol + ATP = 1-O-hexadecyl-2-acetyl-sn-glycero-3-phosphate + ADP + H(+) (RHEA:41676)
• 1-hexadecanoyl-2-(9Z-octadecenoyl)-sn-glycerol + ATP = 1-hexadecanoyl-2-(9Z-octadecenoyl)-sn-glycero-3-phosphate + ADP + H(+) (RHEA:43416)
• 1,2-didecanoyl-sn-glycerol + ATP = 1,2-didecanoyl-sn-glycero-3-phosphate + ADP + H(+) (RHEA:43428)
• 1-O-alkyl-2-acyl-sn-glycerol + ATP = 1-O-alkyl-2-acyl-sn-glycero-3-phosphate + ADP + H(+) (RHEA:44072)
• 1,2-dihexadecanoyl-sn-glycerol + ATP = 1,2-dihexadecanoyl-sn-glycero-3-phosphate + ADP + H(+) (RHEA:63324)

UniProt features (43 total): helix 11, binding site 9, sequence conflict 6, splice variant 4, domain 3, mutagenesis site 2, strand 2, zinc finger region 2, chain 1, modified residue 1, sequence variant 1, turn 1

Structure

Experimental structures (PDB)

2 structures by resolution:

PDB	Title	Method	Resolution (Å)
6IIE	Crystal structure of human diacylglycerol kinase alpha EF-hand domains bound to Ca2+	X-RAY DIFFRACTION	2.14
1TUZ	NMR Structure of the Diacylglycerol kinase alpha, NESGC target HR532	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P23743-F1	82.51	0.45

Human Protein Atlas

Protein class: Enzymes, ENZYME proteins, Transferases, Metabolic proteins, Predicted intracellular proteins

Protein evidence: Evidence at protein level

Subcellular location (HPA, imaging): vesicles; mitochondria; nucleoplasm

Antibody reliability (HPA): IH approved · IF approved

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 (9)

Position	Role
168	Ca(2+)
170	Ca(2+)
172	Ca(2+)
174	Ca(2+)
179	Ca(2+)
123	Ca(2+)
125	Ca(2+)
127	Ca(2+)
134	Ca(2+)

Post-translational modifications (1)

Type	Positions
N6-acetyllysine	484

Mutagenesis-validated functional residues (2)

Position	Phenotype
134	binds calcium but with decreased affinity.
179	loss of calcium-binding.

Function

Pathways and Gene Ontology

Reactome pathways

1 curated (TAS) of 7; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

7 pathways:

ID	Pathway	Evidence
R-HSA-114508	Effects of PIP2 hydrolysis	curated
R-HSA-416476	G alpha (q) signalling events	—
R-HSA-388396	GPCR downstream signalling	—
R-HSA-109582	Hemostasis	—
R-HSA-76002	Platelet activation, signaling and aggregation	—
R-HSA-162582	Signal Transduction	—
R-HSA-372790	Signaling by GPCR	—

MSigDB gene sets: 385 (showing top): GOBP_LIPID_MODIFICATION, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, JAEGER_METASTASIS_DN, REACTOME_PLATELET_ACTIVATION_SIGNALING_AND_AGGREGATION, GOBP_PLATELET_ACTIVATION, MODULE_45, AREB6_03, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_UP, LINDGREN_BLADDER_CANCER_CLUSTER_3_DN, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_ORGANOPHOSPHATE_BIOSYNTHETIC_PROCESS, GOBP_PHOSPHOLIPID_BIOSYNTHETIC_PROCESS, GOBP_GLYCEROLIPID_METABOLIC_PROCESS, GOBP_WOUND_HEALING

GO Biological Process (9): phosphatidic acid biosynthetic process (GO:0006654), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), platelet activation (GO:0030168), intracellular signal transduction (GO:0035556), diacylglycerol metabolic process (GO:0046339), glycerolipid metabolic process (GO:0046486), lipid phosphorylation (GO:0046834), lipid metabolic process (GO:0006629), signal transduction (GO:0007165)

GO Molecular Function (11): ATP-dependent diacylglycerol kinase activity (GO:0004143), calcium ion binding (GO:0005509), ATP binding (GO:0005524), phospholipid binding (GO:0005543), zinc ion binding (GO:0008270), lipid binding (GO:0008289), kinase activity (GO:0016301), alkylglycerol kinase activity (GO:0047649), nucleotide binding (GO:0000166), transferase activity (GO:0016740), metal ion binding (GO:0046872)

GO Cellular Component (3): cytosol (GO:0005829), plasma membrane (GO:0005886), membrane (GO:0016020)

Reactome top-level categories

6 top-level categories:

Category	Pathways
G alpha (q) signalling events	1
Platelet activation, signaling and aggregation	1
Signal Transduction	1
Signaling by GPCR	1
GPCR downstream signalling	1
Hemostasis	1

GO top-level categories

37 GO namespaces:

Category	Terms
phosphotransferase activity, alcohol group as acceptor	2
cellular anatomical structure	2
phosphatidic acid metabolic process	1
glycerophospholipid biosynthetic process	1
G protein-coupled receptor signaling pathway	1
phospholipase C activator activity	1
cell activation	1
blood coagulation	1
intracellular anatomical structure	1
signal transduction	1
acylglycerol metabolic process	1
lipid metabolic process	1
phosphorylation	1
lipid modification	1
primary metabolic process	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
lipid kinase activity	1
metal ion binding	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
anion binding	1
lipid binding	1
transition metal ion binding	1
binding	1
transferase activity, transferring phosphorus-containing groups	1
kinase activity	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
catalytic activity	1
cation binding	1
cytoplasm	1
membrane	1
cell periphery	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 9 of 23 annotations. The rest are phylogenetic / computational / electronic (IEA).

9 experimentally-supported GO terms:

GO term	NS	Evidence
diacylglycerol metabolic process	BP	direct assay
glycerolipid metabolic process	BP	direct assay
lipid phosphorylation	BP	direct assay
phosphatidic acid biosynthetic process	BP	direct assay
cytosol	CC	direct assay
membrane	CC	high-throughput assay
ATP-dependent diacylglycerol kinase activity	MF	direct assay
kinase activity	MF	direct assay
lipid binding	MF	direct assay

Protein interactions and networks

STRING

showing 15 of 792 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
DGKA	CERK	Q8TCT0	767
DGKA	RASGRP1	O95267	748
DGKA	PFKM	P08237	726
DGKA	SPHK1	Q9NYA1	707
DGKA	SPHK2	Q9NRA0	559
DGKA	PLEK2	Q9NYT0	529
DGKA	PLEK	P08567	504
DGKA	PFKP	Q01813	501
DGKA	ARRB1	P49407	479
DGKA	ATOSB	Q7L5A3	450
DGKA	PLD2	O14939	427
DGKA	LMOD1	P29536	427
DGKA	VAV1	P15498	421
DGKA	ARRB2	P32121	417
DGKA	MBOAT2	Q6ZWT7	396

IntAct

Human interaction partners of DGKA in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

3 partners by confidence:

Partner	Interaction type	MIscore	Records
SRC	association	0.460	2
DHRS4	physical association	0.400	1
IL21	proximity	0.270	1

BioGRID (17 interactions; top human partners by supporting records): CTTN (Cross-Linking-MS (XL-MS)), DHRS4 (Affinity Capture-MS), EGFR (Affinity Capture-MS), FKBP4 (Proximity Label-MS), FKBP5 (Proximity Label-MS), FUS (Affinity Capture-MS), IL21 (Co-localization), METTL21B (Affinity Capture-MS), ORC5 (Co-fractionation), OTUD3 (Cross-Linking-MS (XL-MS)), RNF123 (Affinity Capture-MS), RPL22L1 (Affinity Capture-MS), SMAD2 (Affinity Capture-MS), STX7 (Cross-Linking-MS (XL-MS)), TOPBP1 (Proximity Label-MS)

SIGNOR signaling

1 signaling interactions:

A	Effect	B	Mechanism
SRC	up-regulates	DGKA	phosphorylation

Disease & clinical

Genetic variants

Variant evidence for DGKA: 114 ClinVar records (0 pathogenic / likely pathogenic); 3 GWAS associations.

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	60
Likely benign	8
Benign	7

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 27 predictions of 2,183):

Position(s)	Effect	Δscore	Sites
12:55937011	acceptor_gain	1.0000
12:55939184	acceptor_loss	1.0000	3
12:55939244	donor_gain	1.0000
12:55939306–55939307	donor_loss	1.0000	5
12:55939413	acceptor_loss	1.0000	2
12:55939530–55939531	donor_loss	1.0000	2
12:55940622	acceptor_loss	1.0000	2
12:55940723–55940724	donor_loss	1.0000	5
12:55940957	donor_gain	1.0000
12:55941326–55941327	donor_loss	1.0000	5

HPA cancer prognostics

RNA cancer specificity: Low cancer specificity

Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.

1 prognostic cancer types:

Cancer	Prognostic	p-value
Breast Invasive Carcinoma (validation)	favorable	0.0001

Disease associations

OMIM: gene MIM:125855 | disease phenotypes:

GWAS associations

3 associations:

Study	Trait	p-value
GCST010002_69	Refractive error	6e-174
GCST001670_1	Vitiligo	8e-12
GCST004367_1	Anorexia nervosa	4e-9

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL4105787 (SINGLE PROTEIN), CHEMBL4630754 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 4,811 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

1 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL267777	RITANSERIN	2	4,811

PharmGKB: 1 entry (CPIC guideline: no)

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — Diacylglycerol kinases

Most potent curated ligand interactions (4 total), top 4:

Ligand	Action	Affinity	Parameter
compound 16 [PMID: 40916365]	Inhibition	9.57	pIC50
pasodacigib	Inhibition	9.3	pIC50
BMS-502	Inhibition	8.34	pIC50
BMS-684	Inhibition	7.82	pIC50

Binding affinities (BindingDB)

3670 measured of 4304 human assays (4305 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
3-(2-hydroxyethylamino)-5-methyl-8-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-6-oxo-1,5-naphthyridine-2-carbonitrile	IC50	0.1 nM	US-20240051958: DIACYLGLYCEROL KINASE (DGK) ALPHA INHIBITORS AND USES THEREOF
1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(oxolan-3-yloxy)quinoline-3,6-dicarbonitrile	IC50	0.1 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
7-[2-hydroxyethyl(methyl)amino]-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxoquinoline-3-carbonitrile	IC50	0.1 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(oxolan-3-yloxy)quinoline-3-carboxamide	IC50	0.1 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
6-chloro-7-(2-hydroxyethylamino)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-1,5-naphthyridin-2-one	IC50	0.12 nM	US-20240051958: DIACYLGLYCEROL KINASE (DGK) ALPHA INHIBITORS AND USES THEREOF
6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-(oxolan-3-yloxy)-1,5-naphthyridin-2-one	IC50	0.13 nM	US-20240051958: DIACYLGLYCEROL KINASE (DGK) ALPHA INHIBITORS AND USES THEREOF
5-methyl-8-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-6-oxo-3-[(3R)-oxolan-3-yl]oxy-1,5-naphthyridine-2-carbonitrile	IC50	0.14 nM	US-20240051958: DIACYLGLYCEROL KINASE (DGK) ALPHA INHIBITORS AND USES THEREOF
6-chloro-7-(2-hydroxyethoxy)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-1,5-naphthyridin-2-one	IC50	0.15 nM	US-20240051958: DIACYLGLYCEROL KINASE (DGK) ALPHA INHIBITORS AND USES THEREOF
6-chloro-7-(2-methoxyethoxy)-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-1,5-naphthyridin-2-one	IC50	0.19 nM	US-20240051958: DIACYLGLYCEROL KINASE (DGK) ALPHA INHIBITORS AND USES THEREOF
1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(oxolan-3-yloxy)quinoline-3,6-dicarbonitrile	IC50	0.2 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
6-bromo-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(oxolan-3-yloxy)quinoline-3-carboxamide	IC50	0.2 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
6-bromo-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-[(3R)-oxolan-3-yl]oxyquinoline-3-carbonitrile	IC50	0.2 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
6-cyano-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(oxolan-3-yloxy)quinoline-3-carboxamide	IC50	0.2 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(oxolan-3-yloxy)quinoline-3-carboxamide	IC50	0.2 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
7-(2-hydroxyethylamino)-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxoquinoline-3-carbonitrile	IC50	0.2 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
5-methyl-8-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-6-oxo-3-(oxolan-3-yloxy)-1,5-naphthyridine-2-carbonitrile	IC50	0.23 nM	US-20240051958: DIACYLGLYCEROL KINASE (DGK) ALPHA INHIBITORS AND USES THEREOF
3-(2-hydroxyethoxy)-5-methyl-8-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-6-oxo-1,5-naphthyridine-2-carbonitrile	IC50	0.27 nM	US-20240051958: DIACYLGLYCEROL KINASE (DGK) ALPHA INHIBITORS AND USES THEREOF
1-methyl-2-oxo-4-[4-(4-propan-2-yloxyphenyl)piperidin-1-yl]quinoline-3-carboxamide	IC50	0.3 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
7-(methoxymethyl)-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxoquinoline-3-carbonitrile	IC50	0.3 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
6-bromo-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(oxolan-3-yloxy)quinoline-3-carbonitrile	IC50	0.3 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(oxolan-3-yloxy)quinoline-3-carbonitrile	IC50	0.3 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
6-cyano-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(oxolan-3-yloxy)quinoline-3-carboxamide	IC50	0.3 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
7-(3-hydroxyazetidin-1-yl)-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxoquinoline-3-carbonitrile	IC50	0.3 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
6-chloro-7-methoxy-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxoquinoline-3-carbonitrile	IC50	0.3 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(oxolan-3-yloxy)quinoline-3-carbonitrile	IC50	0.3 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
3-(3-hydroxypropoxy)-5-methyl-8-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-6-oxo-1,5-naphthyridine-2-carbonitrile	IC50	0.31 nM	US-20240051958: DIACYLGLYCEROL KINASE (DGK) ALPHA INHIBITORS AND USES THEREOF
3-(2-methoxyethoxy)-5-methyl-8-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-6-oxo-1,5-naphthyridine-2-carbonitrile	IC50	0.35 nM	US-20240051958: DIACYLGLYCEROL KINASE (DGK) ALPHA INHIBITORS AND USES THEREOF
6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-1,5-naphthyridin-2-one	IC50	0.36 nM	US-20240051958: DIACYLGLYCEROL KINASE (DGK) ALPHA INHIBITORS AND USES THEREOF
6-fluoro-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxoquinoline-3-carbonitrile	IC50	0.4 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-6-fluoro-1-methyl-2-oxoquinoline-3-carbonitrile	IC50	0.4 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(oxolan-3-yloxy)quinoline-3-carbonitrile	IC50	0.4 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxo-7-(oxolan-3-ylmethoxy)quinoline-3-carboxamide	IC50	0.4 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
6-chloro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]quinolin-2-one	IC50	0.47 nM	US-20240051958: DIACYLGLYCEROL KINASE (DGK) ALPHA INHIBITORS AND USES THEREOF
4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-6-bromo-1-methyl-2-oxoquinoline-3-carbonitrile	IC50	0.5 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-6-fluoro-1-methyl-2-oxoquinoline-3-carboxamide	IC50	0.5 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
6-fluoro-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxoquinoline-3-carboxamide	IC50	0.5 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
7-[2-hydroxyethyl(methyl)amino]-1-methyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxoquinoline-3-carbonitrile	IC50	0.5 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
1-methyl-4-[4-(2-methyl-2,3-dihydro-1-benzofuran-5-yl)piperidin-1-yl]-2-oxoquinoline-3-carboxamide	IC50	0.5 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
8-[(4R)-4-(3-cyclopropylphenoxy)-3-methylpiperidin-1-yl]-5-methyl-6-oxo-1,5-naphthyridine-2-carbonitrile	IC50	0.51 nM	US-11964973: Substituted bicyclic compounds useful as T cell activators
1-methyl-4-[4-methyl-4-(5-propan-2-yl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxoquinoline-3-carboxamide	IC50	0.6 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
4-[4-(1,3-benzoxazol-2-yl)piperidin-1-yl]-7-bromo-1-methyl-2-oxoquinoline-3-carboxamide	IC50	0.6 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
4-[4-(1,3-benzothiazol-2-yl)piperidin-1-yl]-6-bromo-1-methyl-2-oxoquinoline-3-carbonitrile	IC50	0.6 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-1,7-dimethyl-2-oxoquinoline-3-carbonitrile	IC50	0.6 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
7-[(1-hydroxycyclopropyl)methoxy]-1-methyl-4-[4-methyl-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxoquinoline-3-carbonitrile	IC50	0.6 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
4-[4-(1,3-benzoxazol-2-yl)-4-methylpiperidin-1-yl]-7-chloro-1-methyl-2-oxoquinoline-3-carboxamide	IC50	0.6 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
1-methyl-4-[4-(2-methyl-2,3-dihydro-1-benzofuran-5-yl)piperidin-1-yl]-2-oxoquinoline-3-carbonitrile	IC50	0.6 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
6-bromo-4-[4-fluoro-4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-methoxy-1-methyl-2-oxoquinoline-3-carbonitrile	IC50	0.6 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
7-hydroxy-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxoquinoline-3-carbonitrile	IC50	0.6 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
7-(2-methoxyethylamino)-1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-2-oxoquinoline-3-carbonitrile	IC50	0.6 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation
1,6-dimethyl-4-[4-(5-methyl-1,3-benzoxazol-2-yl)piperidin-1-yl]-7-(oxetan-3-ylamino)-2-oxoquinoline-3-carbonitrile	IC50	0.6 nM	US-11998539: Substituted aminoquinolones as DGKalpha inhibitors for immune activation

ChEMBL bioactivities

215 potent at pChembl≥5 of 229 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.70	IC50	2	nM	CHEMBL6027746
8.70	IC50	2	nM	CHEMBL5781357
8.70	IC50	2	nM	CHEMBL5768187
8.30	IC50	5	nM	CHEMBL5424446
8.30	IC50	5	nM	CHEMBL5818523
8.15	IC50	7	nM	CHEMBL5915983
8.02	IC50	9.6	nM	CHEMBL4633304
8.00	IC50	10	nM	CHEMBL5919576
8.00	IC50	10	nM	CHEMBL5845562
7.85	IC50	14	nM	CHEMBL5849375
7.82	IC50	15	nM	CHEMBL5408449
7.80	IC50	16	nM	CHEMBL5767075
7.80	IC50	16	nM	CHEMBL5993135
7.80	IC50	16	nM	CHEMBL6012969
7.80	IC50	16	nM	CHEMBL6046889
7.66	IC50	22	nM	CHEMBL5788045
7.58	IC50	26	nM	CHEMBL4648848
7.58	IC50	26	nM	CHEMBL6053165
7.55	IC50	28	nM	CHEMBL4647083
7.55	IC50	28	nM	CHEMBL5904241
7.55	IC50	28	nM	CHEMBL5865642
7.54	IC50	29	nM	CHEMBL5999766
7.54	IC50	29	nM	CHEMBL5749461
7.54	IC50	29	nM	CHEMBL5798900
7.52	IC50	30	nM	CHEMBL5771377
7.52	IC50	30	nM	CHEMBL5918545
7.52	IC50	30	nM	CHEMBL5828074
7.52	IC50	30	nM	CHEMBL5846539
7.50	IC50	32	nM	CHEMBL5767075
7.50	IC50	32	nM	CHEMBL5919513
7.47	IC50	34	nM	CHEMBL5402920
7.47	IC50	34	nM	CHEMBL5758324
7.44	IC50	36	nM	CHEMBL5916345
7.43	IC50	37	nM	CHEMBL5793843
7.43	IC50	37	nM	CHEMBL5860953
7.42	IC50	38	nM	CHEMBL5907037
7.41	IC50	39	nM	CHEMBL4646970
7.41	IC50	39	nM	CHEMBL5816364
7.41	IC50	39	nM	CHEMBL5963493
7.40	IC50	40	nM	CHEMBL5868935
7.40	IC50	40	nM	CHEMBL5915810
7.37	IC50	43	nM	CHEMBL4645744
7.37	IC50	43	nM	CHEMBL5794331
7.35	IC50	45	nM	CHEMBL5798900
7.33	IC50	47	nM	CHEMBL5794331
7.33	IC50	47	nM	CHEMBL5870719
7.28	IC50	53	nM	CHEMBL5413938
7.28	IC50	52	nM	CHEMBL5828074
7.28	IC50	52	nM	CHEMBL5741470
7.26	IC50	55	nM	CHEMBL5969668

PubChem BioAssay actives

30 with measured affinity, of 99 total; 17 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
8-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-5-methyl-7-nitro-6-oxo-1,5-naphthyridine-2-carbonitrile	2010060: Inhibition of human DGK alpha using 1, 2-Dilauroyl-sn-glycerol as substrate by ADP-Glo assay	ic50	0.0050	uM
8-[(3R)-4-[(4-chlorophenyl)-phenylmethyl]-3-methylpiperazin-1-yl]-5-methyl-6-oxo-1,5-naphthyridine-2,7-dicarbonitrile	1658256: Inhibition of DGKA/DGKZ in human CD8 cells assessed as induction of CD8 activation by measuring IFNgamma level after 20 hrs by AlphaLISA assay	ic50	0.0096	uM
4-(4-benzhydrylpiperazin-1-yl)-1-methyl-3-nitroquinolin-2-one	2010060: Inhibition of human DGK alpha using 1, 2-Dilauroyl-sn-glycerol as substrate by ADP-Glo assay	ic50	0.0150	uM
8-[(2S,5R)-4-[(2-fluorophenyl)-(4-fluorophenyl)methyl]-2,5-dimethylpiperazin-1-yl]-5-methyl-6-oxo-1,5-naphthyridine-2-carbonitrile	1658256: Inhibition of DGKA/DGKZ in human CD8 cells assessed as induction of CD8 activation by measuring IFNgamma level after 20 hrs by AlphaLISA assay	ic50	0.0260	uM
8-[(3R)-4-[bis(4-chlorophenyl)methyl]-3-methylpiperazin-1-yl]-5-methyl-6-oxo-1,5-naphthyridine-2,7-dicarbonitrile	1658256: Inhibition of DGKA/DGKZ in human CD8 cells assessed as induction of CD8 activation by measuring IFNgamma level after 20 hrs by AlphaLISA assay	ic50	0.0280	uM
4-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-1-methyl-3-nitro-2-oxoquinoline-6-carbonitrile	2010060: Inhibition of human DGK alpha using 1, 2-Dilauroyl-sn-glycerol as substrate by ADP-Glo assay	ic50	0.0340	uM
8-[(2S,5R)-4-[(2,2-difluoro-1,3-benzodioxol-5-yl)methyl]-2,5-dimethylpiperazin-1-yl]-5-methyl-6-oxo-1,5-naphthyridine-2-carbonitrile	1658256: Inhibition of DGKA/DGKZ in human CD8 cells assessed as induction of CD8 activation by measuring IFNgamma level after 20 hrs by AlphaLISA assay	ic50	0.0390	uM
8-[(2S,5R)-4-[bis(4-fluorophenyl)methyl]-2,5-dimethylpiperazin-1-yl]-5-methyl-6-oxo-1,5-naphthyridine-2-carbonitrile	1658256: Inhibition of DGKA/DGKZ in human CD8 cells assessed as induction of CD8 activation by measuring IFNgamma level after 20 hrs by AlphaLISA assay	ic50	0.0430	uM
4-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-1-methyl-3-nitro-1,5-naphthyridin-2-one	2010060: Inhibition of human DGK alpha using 1, 2-Dilauroyl-sn-glycerol as substrate by ADP-Glo assay	ic50	0.0530	uM
8-[(2R)-4-[bis(4-fluorophenyl)methyl]-2-ethylpiperazin-1-yl]-5-methyl-6-oxo-1,5-naphthyridine-2-carbonitrile	1658256: Inhibition of DGKA/DGKZ in human CD8 cells assessed as induction of CD8 activation by measuring IFNgamma level after 20 hrs by AlphaLISA assay	ic50	0.1900	uM
3-[2-[4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl]ethyl]-2-sulfanylidene-1H-quinazolin-4-one	1613990: Inhibition of DGKalpha in human erythrocytes using OAG as substrate preincubated for 1 min followed by OAG addition and measured after 8 mins in presence of [gamma-32P]ATP	ic50	0.3000	uM
N-[(5Z)-5-[(E)-3-(furan-2-yl)prop-2-enylidene]-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]benzenesulfonamide	2010060: Inhibition of human DGK alpha using 1, 2-Dilauroyl-sn-glycerol as substrate by ADP-Glo assay	ic50	0.6000	uM
8-[(3S)-4-[bis(4-fluorophenyl)methyl]-3-methylpiperazin-1-yl]-7-chloro-5-methyl-6-oxo-1,5-naphthyridine-2-carbonitrile	1658256: Inhibition of DGKA/DGKZ in human CD8 cells assessed as induction of CD8 activation by measuring IFNgamma level after 20 hrs by AlphaLISA assay	ic50	1.2000	uM
[(2S,3R,4S)-2-[(3R,4aR,6aR,12S,12aS,12bR)-12-hydroxy-3-(2-hydroxypropan-2-yl)-6a,12b-dimethyl-8,11-dioxo-1,2,3,4a,5,6,12,12a-octahydropyrano[3,2-a]xanthen-9-yl]-4-methylhexan-3-yl] acetate	1613990: Inhibition of DGKalpha in human erythrocytes using OAG as substrate preincubated for 1 min followed by OAG addition and measured after 8 mins in presence of [gamma-32P]ATP	ki	2.2600	uM
[(E,2S,3S)-2-[(3R,4aR,6aR,12S,12aS,12bR)-12-hydroxy-3-(2-hydroxypropan-2-yl)-6a,12b-dimethyl-8,11-dioxo-1,2,3,4a,5,6,12,12a-octahydropyrano[3,2-a]xanthen-9-yl]-4-methylhex-4-en-3-yl] acetate	1613990: Inhibition of DGKalpha in human erythrocytes using OAG as substrate preincubated for 1 min followed by OAG addition and measured after 8 mins in presence of [gamma-32P]ATP	ki	3.3200	uM
6-[2-[4-[(4-fluorophenyl)-phenylmethylidene]piperidin-1-yl]ethyl]-7-methyl-[1,3]thiazolo[3,2-a]pyrimidin-5-one	1613990: Inhibition of DGKalpha in human erythrocytes using OAG as substrate preincubated for 1 min followed by OAG addition and measured after 8 mins in presence of [gamma-32P]ATP	ic50	3.8000	uM
1-(2,6-dimethyl-1H-indol-3-yl)-2-[4-(furan-2-carbonyl)piperazin-1-yl]ethanone	1613974: Inhibition of OST-tagged DGKalpha (unknown origin) expressed in MDCK cell homogenates using DAG as substrate measured after 5 mins in presence of [gamma-32P]ATP by TLC analysis	ic50	4.2810	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, decreases expression, decreases methylation, increases expression, increases methylation	5
Aflatoxin B1	affects expression, increases expression	4
Cisplatin	affects cotreatment, increases expression	3
Air Pollutants	increases oxidation, increases expression, affects cotreatment, increases abundance	2
Testosterone	affects cotreatment, increases expression, decreases expression	2
Tetrachlorodibenzodioxin	increases expression	2
Tobacco Smoke Pollution	decreases expression	2
Particulate Matter	increases abundance, increases expression	2
bisphenol F	affects cotreatment, increases expression	1
chloroacetaldehyde	affects expression	1
alpha phellandrene	increases expression	1
alpha-pinene	affects cotreatment, increases oxidation, increases abundance	1
uranyl acetate	affects expression	1
propionaldehyde	increases expression	1
pirinixic acid	affects binding, decreases expression, increases activity	1
pyrogallol 1,3-dimethyl ether	affects cotreatment, decreases expression, affects localization, increases expression	1
decabromobiphenyl ether	decreases expression	1
pyrazolo(3,4-d)pyrimidine	affects expression	1
arsenite	affects binding, decreases reaction	1
sodium arsenite	increases expression	1
tetrabromobisphenol A	increases expression	1
nickel sulfate	decreases expression	1
methacrylaldehyde	affects cotreatment, increases oxidation, increases abundance	1
di-n-butylphosphoric acid	affects expression	1
perfluorooctane sulfonic acid	increases expression	1
CGP 52608	affects binding, increases reaction	1
adefovir dipivoxil	increases expression	1
erucylphospho-N,N,N-trimethylpropylammonium	increases expression	1
nutlin 3	affects cotreatment, increases expression	1
bisphenol B	increases expression	1

ChEMBL screening assays

43 unique, capped per target: 43 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4034309	Binding	Inhibition of DGKA (unknown origin) at 10 uM	Developing DYRK inhibitors derived from the meridianins as a means of increasing levels of NFAT in the nucleus. — *Bioorg Med Chem Lett*

Cellosaurus cell lines

7 cell lines: 6 cancer cell line, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_D1M9	Abcam K-562 DGKA KO	Cancer cell line	Female
CVCL_D2IU	Abcam Raji DGKA KO	Cancer cell line	Male
CVCL_D7NI	Ubigene A-549 DGKA KO	Cancer cell line	Male
CVCL_D8JY	Ubigene HCT 116 DGKA KO	Cancer cell line	Male
CVCL_D9D7	Ubigene HEK293 DGKA KO	Transformed cell line	Female
CVCL_E0BM	Ubigene HeLa DGKA KO	Cancer cell line	Female
CVCL_UQ41	Abcam Jurkat DGKA KO	Cancer cell line	Male

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for DGKA across ~30M SureChEMBL compounds — explore on Sugi Predict.