SCN2A

Summary

SCN2A (sodium voltage-gated channel alpha subunit 2, HGNC:10588) is a protein-coding gene on chromosome 2q24.3, encoding Sodium channel protein type 2 subunit alpha (Q99250). Mediates the voltage-dependent sodium ion permeability of excitable membranes. It is haploinsufficient (ClinGen: sufficient evidence).

Voltage-gated sodium channels are transmembrane glycoprotein complexes composed of a large alpha subunit with four repeat domains, each of which is composed of six membrane-spanning segments, and one or more regulatory beta subunits. Voltage-gated sodium channels function in the generation and propagation of action potentials in neurons and muscle. This gene encodes one member of the sodium channel alpha subunit gene family. Allelic variants of this gene are associated with seizure disorders and autism spectrum disorder. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 6326 — RefSeq curated summary.

At a glance

• Gene–disease (curated): complex neurodevelopmental disorder (Definitive, ClinGen) — +9 more curated relationships
• GWAS associations: 18
• Clinical variants (ClinVar): 3,105 total — 354 pathogenic, 321 likely-pathogenic (top 1% of genes corpus-wide)
• Regional missense constraint (gnomAD): 8 of 17 regions constrained (≈34% of expected missense variation)
• GTEx eGene: eQTL in 19 tissues, sQTL in 2 (q < 0.05)
• Phenotypes (HPO): 208
• Drug target: yes — 1 curated mechanism-of-action drug, 51 via a complex or family; 99 molecules with ChEMBL bioactivity (top 1% of genes corpus-wide)
• Approved drugs acting on a complex or family including it: 45 — Articaine Hydrochloride, Benoxinate Hydrochloride, Carbamazepine, +42 more (Sodium channel alpha subunit)
• Dosage sensitivity (ClinGen): haploinsufficiency sufficient evidence, triplosensitivity no evidence
• Constraint (gnomAD): pLI 1.00 (loss-of-function intolerant), LOEUF 0.16 (highly constrained)
• MANE Select transcript: NM_001040142
• Interaction hub: 1,970 STRING partners (top 8% of genes corpus-wide)

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:10588
Approved symbol	SCN2A
Name	sodium voltage-gated channel alpha subunit 2
Location	2q24.3
Locus type	gene with protein product
Status	Approved
Aliases	Nav1.2, HBSCII, HBSCI
Ensembl gene	ENSG00000136531
Ensembl biotype	protein_coding
OMIM	182390
Entrez	6326

Gene structure

Transcript identifiers

Ensembl transcripts: 23 — 11 protein_coding, 8 nonsense_mediated_decay, 3 protein_coding_CDS_not_defined, 1 retained_intron

MANE Select: ENST00000375437 · MANE Plus Clinical: ENST00000631182

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 3, TSL 5: 14

ENST00000375437, ENST00000631182, ENST00000283256, ENST00000424833, ENST00000480032, ENST00000486878, ENST00000635945, ENST00000636071, ENST00000636135, ENST00000636384, ENST00000636662, ENST00000636769, ENST00000636985, ENST00000637266, ENST00000637367, ENST00000638151, ENST00000640791, ENST00000673831, ENST00000673883, ENST00000674133, ENST00001113291, ENST00001137817, ENST00001137818

RefSeq mRNA: 5 — MANE Select: NM_001040142 NM_001040142, NM_001040143, NM_001371246, NM_001371247, NM_021007

CCDS: CCDS33313, CCDS33314

Canonical transcript exons

ENST00000375437 — 27 exons

Exon	Start	End
ENSE00003469366	165309352	165309443
ENSE00003476134	165312025	165312088
ENSE00003480100	165354192	165354671
ENSE00003515214	165367217	165367371
ENSE00003520813	165377597	165377650
ENSE00003534381	165326852	165326984
ENSE00003577130	165331330	165331568
ENSE00003578392	165344555	165344911
ENSE00003583124	165323156	165323500
ENSE00003607689	165295773	165296090
ENSE00003618158	165297017	165297135
ENSE00003622830	165313902	165314108
ENSE00003624540	165310323	165310595
ENSE00003632501	165342296	165342469
ENSE00003637082	165307848	165307937
ENSE00003646557	165308666	165308794
ENSE00003650170	165315471	165315758
ENSE00003667200	165313620	165313761
ENSE00003673050	165365143	165365263
ENSE00003692338	165374685	165374966
ENSE00003768497	165386746	165387016
ENSE00003793096	165380592	165380729
ENSE00003797234	165381093	165381197
ENSE00003797951	165370126	165370299
ENSE00003798346	165373225	165373347
ENSE00003843655	165239414	165239640
ENSE00003848820	165388629	165392304

Expression profiles

Bgee: expression breadth ubiquitous, 187 present calls, max score 98.77.

FANTOM5 (CAGE): breadth broad, TPM avg 15.1310 / max 2181.7494, expressed in 368 samples.

Highest expression (Bgee): middle temporal gyrus, Brodmann (1909) area 23, cerebellar vermis, entorhinal cortex, cerebellar cortex.

Genetic regulation across tissues (GTEx eQTL / sQTL)

SCN2A is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 19 tissues and its splicing (sQTL) in 2 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

showing 20 of 21 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Adipose Visceral Omentum	eqtl	3.0e-19	+0.30	2:165292137:C:T
Cells Cultured fibroblasts	eqtl	8.5e-14	-0.32	2:165291305:G:A
Skin Not Sun Exposed Suprapubic	eqtl	5.8e-11	+0.41	2:164995366:A:C
Artery Tibial	eqtl	9.9e-10	+0.26	2:165338306:C:T
Nerve Tibial	eqtl	1.1e-09	-0.23	2:164651333:C:T
Artery Aorta	eqtl	3.7e-09	+0.28	2:165332189:A:T
Testis	eqtl	1.3e-08	-0.39	2:164993823:C:T
Artery Coronary	eqtl	1.2e-06	-0.47	2:165335893:C:A
Uterus	eqtl	3.8e-06	-0.65	2:165296751:T:C
Brain Cerebellum	sqtl	2.5e-05	-0.85	2:165327179:C:G
Brain Cerebellar Hemisphere	eqtl	3.0e-05	+0.16	2:165383508:A:T
Brain Cerebellum	eqtl	1.2e-04	+0.16	2:165384762:G:A
Brain Cerebellar Hemisphere	sqtl	1.7e-04	-0.70	2:165327179:C:G
Esophagus Gastroesophageal Junction	eqtl	2.6e-04	-0.24	2:165363235:G:C
Bladder	eqtl	2.9e-04	+1.00	2:165332184:C:T
Esophagus Muscularis	eqtl	1.2e-03	-0.24	2:165511734:G:A
Skin Sun Exposed Lower leg	eqtl	5.1e-03	+0.22	2:164999669:G:A
Adipose Subcutaneous	eqtl	9.3e-03	-0.18	2:164900861:C:CA
Brain Cortex	eqtl	1.1e-02	+0.47	2:165437358:T:C
Vagina	eqtl	2.3e-02	+0.55	2:165029328:C:T

FANTOM5 promoters

7 alternative TSS:

Promoter ID	TPM avg	Samples expressed
23415	7.1018	138
23416	5.8147	137
23418	1.8434	304
23417	0.2913	68
23419	0.0336	17
23426	0.0286	13
23414	0.0175	9

Top tissues by expression

showing 100 of 289 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
middle temporal gyrus	UBERON:0002771	98.77	gold quality
Brodmann (1909) area 23	UBERON:0013554	98.30	gold quality
cerebellar vermis	UBERON:0004720	96.78	gold quality
entorhinal cortex	UBERON:0002728	96.62	gold quality
cerebellar cortex	UBERON:0002129	96.33	gold quality
parietal lobe	UBERON:0001872	96.27	gold quality
cerebellar hemisphere	UBERON:0002245	96.27	gold quality
postcentral gyrus	UBERON:0002581	96.21	gold quality
superior frontal gyrus	UBERON:0002661	96.17	gold quality
right hemisphere of cerebellum	UBERON:0014890	95.95	gold quality
cerebellum	UBERON:0002037	95.77	gold quality
endothelial cell	CL:0000115	95.41	gold quality
primary visual cortex	UBERON:0002436	94.15	gold quality
occipital lobe	UBERON:0002021	94.10	gold quality
pons	UBERON:0000988	93.83	gold quality
prefrontal cortex	UBERON:0000451	91.75	gold quality
cortical plate	UBERON:0005343	91.48	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	90.96	gold quality
Brodmann (1909) area 9	UBERON:0013540	90.83	gold quality
superior vestibular nucleus	UBERON:0007227	90.66	gold quality
frontal cortex	UBERON:0001870	90.52	gold quality
cerebral cortex	UBERON:0000956	89.86	gold quality
substantia nigra pars compacta	UBERON:0001965	89.69	gold quality
neocortex	UBERON:0001950	89.43	gold quality
lateral globus pallidus	UBERON:0002476	88.85	gold quality
telencephalon	UBERON:0001893	88.02	gold quality
temporal lobe	UBERON:0001871	87.96	gold quality
right frontal lobe	UBERON:0002810	87.72	gold quality
Brodmann (1909) area 46	UBERON:0006483	87.46	gold quality
Ammon’s horn	UBERON:0001954	87.33	gold quality
brain	UBERON:0000955	86.80	gold quality
nucleus accumbens	UBERON:0001882	86.64	gold quality
lateral nuclear group of thalamus	UBERON:0002736	86.35	gold quality
central nervous system	UBERON:0001017	86.26	gold quality
forebrain	UBERON:0001890	86.19	gold quality
cingulate cortex	UBERON:0003027	85.87	gold quality
anterior cingulate cortex	UBERON:0009835	85.66	gold quality
substantia nigra pars reticulata	UBERON:0001966	85.25	gold quality
caudate nucleus	UBERON:0001873	84.07	gold quality
ventral tegmental area	UBERON:0002691	83.69	gold quality
putamen	UBERON:0001874	83.42	gold quality
orbitofrontal cortex	UBERON:0004167	82.53	gold quality
medulla oblongata	UBERON:0001896	82.30	gold quality
amygdala	UBERON:0001876	82.20	gold quality
hypothalamus	UBERON:0001898	81.88	gold quality
frontal pole	UBERON:0002795	81.17	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	80.12	gold quality
paraflocculus	UBERON:0005351	79.78	gold quality
corpus callosum	UBERON:0002336	77.40	gold quality
buccal mucosa cell	CL:0002336	76.60	gold quality
midbrain	UBERON:0001891	76.54	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	76.46	gold quality
substantia nigra	UBERON:0002038	75.67	gold quality
dorsal plus ventral thalamus	UBERON:0001897	75.38	gold quality
metanephros cortex	UBERON:0010533	72.82	gold quality
adult organism	UBERON:0007023	72.80	gold quality
sural nerve	UBERON:0015488	71.36	gold quality
pituitary gland	UBERON:0000007	70.62	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	70.38	gold quality
adenohypophysis	UBERON:0002196	69.99	gold quality
spinal cord	UBERON:0002240	69.75	gold quality
middle frontal gyrus	UBERON:0002702	69.25	gold quality
adult mammalian kidney	UBERON:0000082	67.81	gold quality
subthalamic nucleus	UBERON:0001906	66.88	gold quality
CA1 field of hippocampus	UBERON:0003881	65.79	silver quality
ganglionic eminence	UBERON:0004023	65.62	gold quality
diaphragm	UBERON:0001103	64.90	gold quality
olfactory bulb	UBERON:0002264	64.19	gold quality
hair follicle	UBERON:0002073	64.15	gold quality
type B pancreatic cell	CL:0000169	63.90	gold quality
renal medulla	UBERON:0000362	63.60	gold quality
kidney	UBERON:0002113	63.52	gold quality
triceps brachii	UBERON:0001509	63.37	gold quality
gluteal muscle	UBERON:0002000	63.29	gold quality
islet of Langerhans	UBERON:0000006	63.08	gold quality
colonic epithelium	UBERON:0000397	62.87	silver quality
gall bladder	UBERON:0002110	62.21	gold quality
inferior olivary complex	UBERON:0002127	61.89	gold quality
embryo	UBERON:0000922	61.77	gold quality
Brodmann (1909) area 10	UBERON:0013541	61.48	silver quality
dorsal motor nucleus of vagus nerve	UBERON:0002870	61.28	gold quality
cortex of kidney	UBERON:0001225	60.25	gold quality
ventricular zone	UBERON:0003053	60.04	gold quality
globus pallidus	UBERON:0001875	59.91	gold quality
smooth muscle tissue	UBERON:0001135	59.77	gold quality
inferior vagus X ganglion	UBERON:0005363	59.74	silver quality
calcaneal tendon	UBERON:0003701	59.57	gold quality
right adrenal gland	UBERON:0001233	57.94	gold quality
cardiac muscle of right atrium	UBERON:0003379	57.59	gold quality
metanephros	UBERON:0000081	57.10	gold quality
left ventricle myocardium	UBERON:0006566	56.77	gold quality
right adrenal gland cortex	UBERON:0035827	56.76	gold quality
decidua	UBERON:0002450	56.55	gold quality
adrenal gland	UBERON:0002369	56.17	gold quality
myocardium	UBERON:0002349	55.92	gold quality
adrenal tissue	UBERON:0018303	55.24	gold quality
tibial nerve	UBERON:0001323	55.23	gold quality
left adrenal gland	UBERON:0001234	55.03	gold quality
medial globus pallidus	UBERON:0002477	54.86	gold quality
deltoid	UBERON:0001476	54.79	gold quality

Single-cell (SCXA)

Detected in 6 experiment(s), a significant marker in 6.

Experiment	Marker?	Max mean expression
E-GEOD-75140	yes	480.60
E-GEOD-93593	yes	309.30
E-CURD-119	yes	45.64
E-ANND-3	yes	7.71
E-GEOD-84465	yes	6.46
E-GEOD-83139	yes	3.96

HPA expression

RNA tissue specificity: Tissue enriched

showing 60 of 63 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Cerebellum	tissue	131.2	high
Cerebral cortex	tissue	118.9	medium
Somatosensory cortex	tissue	118.9
Occipital cortex	tissue	117.6
Motor cortex	tissue	116.8
Hippocampal formation	tissue	114.1
Entorhinal cortex	tissue	114.1
Prefrontal cortex	tissue	113.6
Retrosplenial and cingulate cortex	tissue	111.5
Temporal cortex	tissue	107.6
Retrosplenial cortex	tissue	98.3
Insular cortex	tissue	89.8
Putamen	tissue	85.3
Postcentral gyrus	tissue	80.7
Frontal cortex	tissue	77.8
Basal ganglia	tissue	77.8	low
Caudate putamen	tissue	77.4
Ventral forebrain	tissue	64.3
Amygdala	tissue	59.7
Septum	tissue	56.7
Pons	tissue	50.8
Nucleus accumbens	tissue	46.4
Hippocampus	tissue	45.2	low
Thalamus	tissue	44.0
Hypothalamus	tissue	43.8
Midbrain	tissue	42.5
Olfactory bulb	tissue	36.8
Locus coeruleus	tissue	34.8
Periaqueductal gray	tissue	33.7
Substantia nigra	tissue	29.5
Superior colliculi	tissue	21.7
Medulla oblongata	tissue	20.1
Spinal cord	tissue	10.9
Corpus callosum	tissue	8.8
Retina	tissue	3.8
Choroid plexus	tissue	3.7
Pituitary gland	tissue	3.4
Kidney	tissue	1.6	medium
Adrenal gland	tissue	1.1	not detected
Epididymis	tissue	0.9	not detected
Breast	tissue	0.7	not detected
Gallbladder	tissue	0.7	not detected
Smooth muscle	tissue	0.5	not detected
Endometrium 1	tissue	0.5	not detected
Ovary	tissue	0.3	not detected
Vagina	tissue	0.3	not detected
Seminal vesicle	tissue	0.3	not detected
Cervix	tissue	0.2	not detected
Testis	tissue	0.2	not detected
Stomach 1	tissue	0.2	not detected
Salivary gland	tissue	0.2	not detected
Lung	tissue	0.2	not detected
Small intestine	tissue	0.2	not detected
Duodenum	tissue	0.2	not detected
Thymus	tissue	0.2
Adipose tissue	tissue	0.1	not detected
Rectum	tissue	0.1	not detected
Colon	tissue	0.1	not detected
Urinary bladder	tissue	0.1	not detected
Spleen	tissue	0.1	not detected

Brain sub-regions (HPA Brain Atlas): detected in 189; highest nTPM — Dorsal hippocampus (100.5), Subiculum (93.4), Cerebellar cortex (92.1), Perirhinal gyrus (87.8), Olfactory area (83.6).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): IL10, KDM5C, KLF4, RCOR1, REST, TNF

miRNA regulators (miRDB)

Targeting SCN2A by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

showing 30 of 169 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-30A-5P	100.00	76.31	3233
HSA-MIR-30B-5P	100.00	76.29	3248
HSA-MIR-30C-5P	100.00	76.29	3248
HSA-MIR-30D-5P	100.00	76.32	3233
HSA-MIR-30E-5P	100.00	76.32	3242
HSA-MIR-6867-5P	100.00	82.21	3464
HSA-MIR-4533	100.00	69.48	2758
HSA-MIR-3924	100.00	72.09	2394
HSA-LET-7A-3P	100.00	74.03	3932
HSA-LET-7B-3P	100.00	74.08	3913
HSA-LET-7F-1-3P	100.00	74.02	3928
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-98-3P	100.00	74.08	3907
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-340-5P	100.00	72.50	4437
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-520D-5P	99.98	73.34	4883
HSA-MIR-524-5P	99.98	73.43	4882
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-103A-3P	99.98	69.14	1595
HSA-MIR-107	99.98	69.14	1595
HSA-MIR-4789-5P	99.98	70.76	2721
HSA-MIR-4803	99.98	71.99	3117
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-3148	99.97	75.06	6478

Functional genomics

gnomAD constraint: pLI 1, LOEUF 0.161, missense Z 8.73 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD)

ENST00000375437 splits into 17 regions with different missense tolerance; 8 are missense-constrained (≈34% 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
2:165,295,824–165,307,912	141 / 185.4	0.76	no
2:165,307,913–165,310,471	37 / 154.9	0.24	yes (p 2.7e-21)
2:165,310,472–165,312,052	45 / 58.1	0.77	no
2:165,312,053–165,314,068	42 / 137.3	0.31	yes (p 4.2e-16)
2:165,314,069–165,331,462	315 / 386.6	0.81	no
2:165,331,463–165,344,886	83 / 256.8	0.32	yes (p 2.1e-27)
2:165,344,887–165,354,240	0 / 27.9	0.00	yes (p 1.3e-07)
2:165,354,241–165,354,287	5 / 19.9	0.25	yes (p 8.4e-04)
2:165,354,288–165,370,195	228 / 297.3	0.77	no
2:165,370,196–165,374,795	39 / 130.2	0.30	yes (p 1.3e-15)
2:165,374,796–165,374,899	32 / 42.5	0.75	no
2:165,374,900–165,388,663	97 / 266.1	0.36	no
2:165,388,664–165,388,812	4 / 65.7	0.06	yes (p 2.7e-14)
2:165,388,813–165,389,078	47 / 109.0	0.43	no
2:165,389,079–165,389,154	0 / 34.1	0.00	yes (p 5.2e-09)
2:165,389,155–165,389,476	54 / 135.4	0.40	no
2:165,389,477–165,389,821	109 / 137.9	0.79	no
ClinGen dosage: haploinsufficiency 3 (sufficient evidence), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map

Literature-anchored findings (GeneRIF, showing 40)

• in autism families, the variant R1902C in SCN2A is located in the calmodulin binding site and was found to reduce binding affinity for calcium-bound calmodulin. (PMID:12610651)
• We found a nonsense mutation of SCN2A in a patient with intractable epilepsy and severe mental decline. The phenotype is like severe myoclonic epilepsy in infancy but distinct because of partial epilepsy, delayed onset and no temperature sensitivity (PMID:15028761)
• a role for the hemizygous deletion of not one but two sodium channel genes (SCN1A and SCN2A) in another complicated and more severe epileptic phenotype. (PMID:15249644)
• Calmodulin mediates Ca2+ sensitivity of Nav1.2 and Nav1.5 sodium channels (PMID:15316014)
• Although data suggest that SCN2A1 activity does not directly influence membrane potential, intracellular Ca(2+) release, or proliferation in normal human pulmonary artery smooth muscle cells, its physiological functions remain unresolved. (PMID:16052353)
• Genetic interaction between the combined mild alleles of monogenic epilepsy genes KCNQ2 and SCN2A1 results in severe epilepsy in transgenic mice. (PMID:16464983)
• Data show that the varied effects of beta1 and beta2 on Nav1.5 and Nav1.2 gating are apparently synergistic and highlight the complex manner, through subunit- and sugar-dependent mechanisms, by which Nav activity is modulated. (PMID:16847056)
• The SCN2A gene was tested for a possible role in hippocampal abnormalities in familial mesial temporal lobe epilepsy. We conclusively ruled out the SCN2A gene as a candidate in FMTLE. (PMID:16914293)
• two large families with benign familial neonatal-infantile seizure (BFNIS) and novel SCN2A mutations; the families had 12 & 9 affected individuals, respectively, with phenotypes consistent with BFNIS; two mutations were discovered in SCN2A (E430Q; I1596S) (PMID:17386050)
• analysis of neonatal & adult splice forms of NaV1.2 with a benign familial neonatal-infantile seizures mutation; developmentally regulated NaV1.2 splicing may be one mechanism that counters the normally high excitability of neonatal neurons (PMID:17467289)
• Characterization of 5’ untranslated regions SCN2A, and identification of cis-conserved noncoding sequences (PMID:17544618)
• In south china, the R188W mutation of the SCN2A gene not releate to children with febrile seizures. (PMID:17641256)
• Allele frequencies of both the D2S111 and the D2S124 polymorphisms of the SCN2A gene were not significantly different between cases with a specific idiopathic generalized epilepsy subtype (with generalized tonic-clonic seizures) and healthy controls. (PMID:17715289)
• Nav1.2 immunostaining was not observed along demyelinated axons in chronic lesions but was expressed by scar and reactive astrocytes within the plaque. (PMID:17805013)
• SCN2A gene mutations are associated with inherited benign neonatal-infantile epilepsy. (PMID:18479388)
• The association of antiepileptic drugs responsiveness with genetic polymorphisms was investigated and any association with mRNA expression of the neuronal sodium channels was correlated. (PMID:18784617)
• Clinically significant mutations identified in the C-terminal region of NaV1 sodium channels cluster in the helix I-IV interface and the helix II-III interhelical segment or in helices III and IV of the NaV1.2 (1777-1882) structure. (PMID:19129176)
• Data demonstrate that the two N-terminal alternatively spliced FGF14 variants, FGF14-1a and FGF14-1b, differentially regulate currents produced by Nav1.2 and Nav1.6 channels. (PMID:19465131)
• The direct effect of heat on Nav1.2 channels localized to the site of action potential initiation potentially causes a profound increase in neuronal excitability. This is likely to contribute to febrile seizure genesis. (PMID:19743470)
• This finding suggests that both nonsense mutations and missense SCN2A mutations cause Dravet syndrome. (PMID:19783390)
• de novo mutations SCN2A-E1211K, -I1473M, and -R102X indicate that SCN2A is an etiologic candidate underlying a variety of intractable childhood epilepsies (PMID:19786696)
• Deletions in SCN2A gene is associated with autistic features and developmental delay. (PMID:20346423)
• Transient expression of seizures occur due to a gain-of-function of mutant Na(V)1.2 channel. (PMID:20371507)
• Genetic variants in the voltage-gated ion channel SCN2A dramatically influence the phenotype of mice carrying an SCN1A mutation as well as the seizures caused by the SCN1A mutation. (PMID:21156207)
• We studied the developmental changes of Na(v)1.1 and Na(v)1.2 in the human hippocampus and temporal lobe (PMID:21377452)
• Thermodynamic and structural studies of Calmodulin (CaM)-Na(v)1.2(IQp) interactions show that apo and (Ca(2+))(4)-CaM adopt distinct conformations that both permit tight association with Na(v)1.2(IQp) during gating. (PMID:21439835)
• Environmental enrichment from birth reduces spontaneous seizures and neuronal damage in the Q54 model of temporal lobe epilepsy. (PMID:21762452)
• Functional studies of SCN2A mutations show that they can cause divergent biophysical defects in Na(V)1.2 and impair cell surface expressions[review] (PMID:22029951)
• association of the gene SCN2A, previously identified in epilepsy syndromes, with the risk of autism (PMID:22495306)
• The results of this study shown that both A1685V (GEFS+) and A1685D (SMEI) mutant Nav1.1 channels are characterized by complete loss of function when they are expressed alone (PMID:22525008)
• This finding suggests that SCN2A mutation is a predisposing factor for acute encephalopathy. (PMID:22591750)
• This study demonistrated the detailed functional analysis of Na(v)1.2 mutant, R1312T, which was originally found in a child with Dravet syndrome. (PMID:22677033)
• This study demonistrated that associated with a duplication of the SCN2A and SCN3A gene cluster on 2q24 in patient with early onset epilepsy. (PMID:23016767)
• Identification of a novel SCN2A mutation in a family with infantile seizures with onset between 6 and 8 months provides further confirmation that this gene is involved in families with a delayed age of onset. (PMID:23360469)
• study identified a de novo SCN2A mutation as the etiology for Ohtahara syndrome in monozygotic twins associated with a unique dentate-olivary dysplasia in the deceased twin (PMID:23550958)
• Mutation of SCN2A induces neuronal hyperexcitability, resulting in infantile epilepsy with favorable outcome (PMID:23758435)
• An SCN2A missense mutation is associated with infantile spasms and bitemporal hypometabolism. (PMID:23827426)
• Our data from the Hong Kong and Malaysia cohorts showed no significant allele, genotype and haplotype association of polymorphisms in the SCN1A, SCN2A, and SCN3A genes with drug responsiveness in epilepsy. (PMID:23859570)
• SCN2A mutations are an important genetic cause of Ohtahara syndrome. Given the wide clinical spectrum associated with SCN2A mutations, genetic testing for SCN2A should be considered for children with different epileptic conditions. (PMID:23935176)
• Following SCN2A knockdown, the concentration of Cu-Zn SOD declined and the si-SCN2A vector group showed a repeated discharge. (PMID:24220630)

Cross-species orthologs

2 orthologs

Organism	Symbol	Gene ID
mus_musculus	Scn2a	ENSMUSG00000075318
rattus_norvegicus	Scn2a	ENSRNOG00000005018

Paralogs (26): CACNA1G (ENSG00000006283), SCN4A (ENSG00000007314), CACNA1S (ENSG00000081248), CACNA1I (ENSG00000100346), CACNA1F (ENSG00000102001), NALCN (ENSG00000102452), SCN7A (ENSG00000136546), CACNA1A (ENSG00000141837), SCN1A (ENSG00000144285), CACNA1B (ENSG00000148408), CACNA1C (ENSG00000151067), CATSPER3 (ENSG00000152705), SCN3A (ENSG00000153253), CACNA1D (ENSG00000157388), TPCN2 (ENSG00000162341), CATSPER2 (ENSG00000166762), SCN11A (ENSG00000168356), SCN9A (ENSG00000169432), CATSPER1 (ENSG00000175294), SCN5A (ENSG00000183873), SCN10A (ENSG00000185313), TPCN1 (ENSG00000186815), CATSPER4 (ENSG00000188782), CACNA1H (ENSG00000196557), SCN8A (ENSG00000196876), CACNA1E (ENSG00000198216)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:98248) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 18 distinct phenotype terms.

Mouse phenotype (MP)	Records
weight loss	1
abnormal social investigation	1
decreased anxiety-related response	1
cyanosis	1
abnormal hemoglobin	1
respiratory distress	1
abnormal CNS synaptic transmission	1
abnormal nervous system electrophysiology	1
abnormal channel response	1
hypoxia	1
abnormal brainstem morphology	1
abnormal action potential	1
absent gastric milk in neonates	1
postnatal lethality, complete penetrance	1
perinatal lethality, complete penetrance	1
decreased excitatory postsynaptic current frequency	1
abnormal response to social novelty	1
increased locomotor activity	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
Oryctolagus cuniculus	Q28644	93.2%	Diamond
Gallus gallus	O73707	93.1%	Diamond
Onychomys torridus	P0DMA5	90.4%	Diamond
Equus caballus	Q28371	88.8%	Diamond
Tetraodon nigroviridis	Q2XVR4	88.2%	Diamond
Takifugu rubripes	Q2XVR6	88.2%	Diamond
Canis lupus familiaris	O46669	86.9%	Diamond
Diplobatis ommata	P56699	81.2%	Diamond
Danio rerio	Q2XVR3	73.3%	Diamond
Electrophorus electricus	P02719	68.2%	Diamond
Drosophila melanogaster	P35500	47.2%	Diamond
Periplaneta americana	D0E0C2	43.8%	Diamond
Heterololigo bleekeri	Q05973	40.5%	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
SLC38A11	protein-coding	151258
GALNT3	protein-coding	2591
SCN3A	protein-coding	6328
CSRNP3	protein-coding	80034
COBLL1	protein-coding	22837
TTC21B-AS1	ncRNA	100506134
TTC21B	protein-coding	79809

Protein

Protein identifiers

Sodium channel protein type 2 subunit alpha — Q99250 (reviewed: Q99250)

Alternative names: HBSC II, Sodium channel protein brain II subunit alpha, Sodium channel protein type II subunit alpha, Voltage-gated sodium channel subunit alpha Nav1.2

All UniProt accessions (11): A0A0D9SGG2, A0A1B0GTS6, A0A1B0GTX0, A0A1B0GW40, A0A1B0GW67, A0A1B0GWA6, A0A669KAR0, A0A669KBL5, A0A669KBM3, Q99250, F6U291

UniProt curated annotations — full annotation on UniProt →

Function. Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. Implicated in the regulation of hippocampal replay occurring within sharp wave ripples (SPW-R) important for memory.

Subunit / interactions. Heterooligomer of a large alpha subunit and a smaller beta subunit. Heterooligomer with SCN2B or SCN4B; disulfide-linked. Heterooligomer with SCN1B or SCN3B; non-covalently linked. Interacts with NEDD4L. Interacts with CALM. Interacts with TMEM233. Interacts with the conotoxin GVIIJ. Interacts with the spider beta/delta-theraphotoxin-Pre1a. Interacts with the conotoxin KIIIA. Interacts with the spider protoxin-II.

Subcellular location. Cell membrane.

Post-translational modifications. May be ubiquitinated by NEDD4L; which would promote its endocytosis. Phosphorylation at Ser-1506 by PKC in a highly conserved cytoplasmic loop slows inactivation of the sodium channel and reduces peak sodium currents. Sumoylated at Lys-38. Sumoylation is induced by hypoxia, increases voltage-gated sodium current and mediates the early response to acute hypoxia in neurons. Sumoylated SCN2A is located at the cell membrane.

Disease relevance. Seizures, benign familial infantile, 3 (BFIS3) [MIM:607745] A form of benign familial infantile epilepsy, a neurologic disorder characterized by afebrile seizures occurring in clusters during the first year of life, without neurologic sequelae. BFIS3 inheritance is autosomal dominant. The disease is caused by variants affecting the gene represented in this entry. Developmental and epileptic encephalopathy 11 (DEE11) [MIM:613721] An autosomal dominant seizure disorder characterized by neonatal or infantile onset of refractory seizures with resultant delayed neurologic development and persistent neurologic abnormalities. Patients may progress to West syndrome, which is characterized by tonic spasms with clustering, arrest of psychomotor development, and hypsarrhythmia on EEG. The disease is caused by variants affecting the gene represented in this entry. Defects in SCN2A are associated with genetic epilepsy with febrile seizures plus (GEFS+), a familial autosomal dominant epilepsy syndrome, a clinical subset of febrile seizures, characterized by frequent episodes after 6 years of age and various types of subsequent epilepsy. Defects in SCN2A are associated with autism spectrum disorders (ASD). It seems that mutations resulting in sodium channel gain of function and increased neuron excitability lead to infantile seizures, whereas variants resulting in sodium channel loss of function and decrease neuron excitability are associated with ASD. Episodic ataxia 9 (EA9) [MIM:618924] An autosomal dominant neurologic disorder characterized by episodic ataxia manifesting in the first years of life, early-onset seizures, difficulty walking, dizziness, slurred speech, headache, vomiting, and pain. The duration of ataxic episodes is heterogeneous. Most patients show episodes lasting minutes to maximum several hours, but periods lasting days up to weeks have been reported. Some patients have mildly delayed development with speech delay and/or autistic features or mildly impaired intellectual development. The disease is caused by variants affecting the gene represented in this entry.

Domain organisation. The sequence contains 4 internal repeats, each with 5 hydrophobic segments (S1, S2, S3, S5, S6) and one positively charged segment (S4). Segments S4 are probably the voltage-sensors and are characterized by a series of positively charged amino acids at every third position.

Similarity. Belongs to the sodium channel (TC 1.A.1.10) family. Nav1.2/SCN2A subfamily.

Isoforms (2)

UniProt ID	Names	Canonical?
Q99250-1	1, Adult, 6A	yes
Q99250-2	2, Neonatal, 6N

RefSeq proteins (5): NP_001035232, NP_001035233, NP_001358175, NP_001358176, NP_066287 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000048	IQ_motif_EF-hand-BS	Binding_site
IPR001696	Na_channel_asu	Family
IPR005821	Ion_trans_dom	Domain
IPR010526	Na_trans_assoc_dom	Domain
IPR024583	Na_trans_cytopl	Domain
IPR027359	Volt_channel_dom_sf	Homologous_superfamily
IPR043203	VGCC_Ca_Na	Family
IPR044564	Na_chnl_inactivation_gate	Domain
IPR058542	IQ_SCN5A_C	Domain

Pfam: PF00520, PF06512, PF11933, PF24609

Catalyzed reactions (Rhea)

• Na(+)(in) = Na(+)(out) (RHEA:34963)

UniProt features (352 total): sequence variant 112, helix 69, topological domain 29, transmembrane region 24, modified residue 24, strand 20, turn 19, site 11, glycosylation site 10, disulfide bond 7, region of interest 6, compositionally biased region 5, intramembrane region 4, sequence conflict 4, repeat 4, chain 1, cross-link 1, splice variant 1, domain 1

Structure

Experimental structures (PDB)

5 structures by resolution:

PDB	Title	Method	Resolution (Å)
4RLY	Crystal Structure of AnkB Ankyrin Repeats (R1-R9) in Complex with Nav1.2 Ankyrin Binding …	X-RAY DIFFRACTION	2.5
6J8E	Human Nav1.2-beta2-KIIIA ternary complex	ELECTRON MICROSCOPY	3
4JPZ	Voltage-gated sodium channel 1.2 C-terminal domain in complex with FGF13U and …	X-RAY DIFFRACTION	3.02
2KAV	Solution structure of the human Voltage-gated Sodium Channel, brain isoform (Nav1.2)	SOLUTION NMR
6BUT	Solution structure of full-length apo mammalian calmodulin bound to the IQ motif of the …	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q99250-F1	69.28	0.17

Human Protein Atlas

Protein class: Metabolic proteins, Transporters, Transporter channels and pores, Voltage-gated ion channels, Voltage-Gated Sodium Channels, Predicted membrane proteins, Disease related genes, FDA approved drug targets, Small molecule drugs, Human disease related genes, Epilepsy

Protein evidence: Evidence at protein level

Antibody reliability (HPA): IH enhanced

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 (11)

Position	Role
330	binds mu-conotoxin kiiia
362	binds mu-conotoxin kiiia
909	binds scn2b; via carbonyl oxygen
916	binds mu-conotoxin kiiia; via amide nitrogen
920	binds mu-conotoxin kiiia; via carbonyl oxygen
945	binds mu-conotoxin kiiia
949	binds mu-conotoxin kiiia
1374	binds mu-conotoxin kiiia; via amide nitrogen
1429	binds mu-conotoxin kiiia
1443	binds mu-conotoxin kiiia
1489	important for channel closure

Post-translational modifications (25)

Type	Positions
Phosphoserine	686, 687, 721, 1506, 1930, 1971, 4, 468, 471, 484, 526, 528, 531, 553, 554, 558, 573, 576, 589, 610, 623
Phosphothreonine	1943, 1963, 1966
Glycyl lysine isopeptide (lys-gly) (interchain with g-cter in sumo1)	38

Disulfide bonds (7)

Type	Positions
Disulfide bond	278–338, 912–918, 950–959, 1366–1386, 1731–1746
Interchain	910, 910

Glycosylation sites (10)

Type	Positions
N-linked (glcnac…) asparagine	212, 285, 291, 297, 303, 308, 340, 1368, 1382, 1393

Function

Pathways and Gene Ontology

Reactome pathways

1 curated (TAS) of 11; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

11 pathways:

ID	Pathway	Evidence
R-HSA-5576892	Phase 0 - rapid depolarisation	curated
R-HSA-422475	Axon guidance	—
R-HSA-5576891	Cardiac conduction	—
R-HSA-1266738	Developmental Biology	—
R-HSA-445095	Interaction between L1 and Ankyrins	electronic
R-HSA-373760	L1CAM interactions	—
R-HSA-397014	Muscle contraction	—
R-HSA-9675108	Nervous system development	—
R-HSA-9709957	Sensory Perception	—
R-HSA-9717207	Sensory perception of sweet, bitter, and umami (glutamate) taste	electronic
R-HSA-9717189	Sensory perception of taste	—

MSigDB gene sets: 599 (showing top): GOBP_MEMORY, GOBP_MEMBRANE_DEPOLARIZATION, GOBP_COGNITION, GOBP_BEHAVIOR, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOBP_SODIUM_ION_TRANSMEMBRANE_TRANSPORT, GOBP_MEMBRANE_DEPOLARIZATION_DURING_ACTION_POTENTIAL, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_LEVELS, GOBP_MUSCLE_CONTRACTION, GOBP_APOPTOTIC_SIGNALING_PATHWAY, GOBP_RESPONSE_TO_OXYGEN_LEVELS, GOBP_ENSHEATHMENT_OF_NEURONS, chr2q24, TAKEDA_TARGETS_OF_NUP98_HOXA9_FUSION_10D_UP

GO Biological Process (19): sodium ion transport (GO:0006814), nervous system development (GO:0007399), memory (GO:0007613), intrinsic apoptotic signaling pathway in response to osmotic stress (GO:0008627), neuronal action potential (GO:0019228), sodium ion transmembrane transport (GO:0035725), myelination (GO:0042552), neuron apoptotic process (GO:0051402), cellular response to hypoxia (GO:0071456), cardiac muscle cell action potential involved in contraction (GO:0086002), action potential (GO:0001508), regulation of heart rate (GO:0002027), monoatomic ion transport (GO:0006811), monoatomic ion transmembrane transport (GO:0034220), regulation of membrane potential (GO:0042391), transmembrane transport (GO:0055085), cardiac muscle cell action potential (GO:0086001), regulation of muscle system process (GO:0090257), monoatomic cation transmembrane transport (GO:0098655)

GO Molecular Function (6): voltage-gated sodium channel activity (GO:0005248), calmodulin binding (GO:0005516), monoatomic ion channel activity (GO:0005216), monoatomic cation channel activity (GO:0005261), sodium channel activity (GO:0005272), protein binding (GO:0005515)

GO Cellular Component (6): voltage-gated sodium channel complex (GO:0001518), plasma membrane (GO:0005886), membrane (GO:0016020), axon (GO:0030424), node of Ranvier (GO:0033268), monoatomic ion channel complex (GO:0034702)

Reactome top-level categories

8 top-level categories:

Category	Pathways
L1CAM interactions	1
Cardiac conduction	1
Sensory perception of taste	1
Axon guidance	1
Nervous system development	1
Muscle contraction	1
Developmental Biology	1
Sensory Perception	1

GO top-level categories

45 GO namespaces:

Category	Terms
action potential	2
regulation of biological quality	2
transport	2
monoatomic ion transmembrane transport	2
cellular anatomical structure	2
metal ion transport	1
system development	1
animal gross anatomical part developmental process	1
learning or memory	1
cellular response to osmotic stress	1
intrinsic apoptotic signaling pathway	1
transmission of nerve impulse	1
sodium ion transport	1
monoatomic cation transmembrane transport	1
axon ensheathment	1
apoptotic process	1
response to hypoxia	1
cellular response to stress	1
cellular response to decreased oxygen levels	1
cardiac muscle cell action potential	1
cardiac muscle cell contraction	1
regulation of membrane potential	1
regulation of heart contraction	1
monoatomic ion transport	1
transmembrane transport	1
cellular process	1
muscle system process	1
regulation of system process	1
monoatomic cation transport	1
sodium channel activity	1
protein binding	1
monoatomic ion transmembrane transporter activity	1
channel activity	1
monoatomic ion channel activity	1
monoatomic cation transmembrane transporter activity	1
monoatomic cation channel activity	1
sodium ion transmembrane transporter activity	1
binding	1
sodium channel complex	1
plasma membrane protein complex	1
membrane	1
cell periphery	1
neuron projection	1
main axon	1
transmembrane transporter complex	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 4 of 31 annotations. The rest are phylogenetic / computational / electronic (IEA).

4 experimentally-supported GO terms:

GO term	NS	Evidence
neuronal action potential	BP	mutant phenotype
plasma membrane	CC	direct assay
calmodulin binding	MF	mutant phenotype
voltage-gated sodium channel activity	MF	direct assay

Protein interactions and networks

STRING

showing 15 of 1,970 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SCN2A	SCN1B	Q07699	931
SCN2A	PRRT2	Q7Z6L0	911
SCN2A	KCNQ2	O43526	872
SCN2A	NAV1	Q8NEY1	861
SCN2A	PCDH19	Q8TAB3	848
SCN2A	STXBP1	P61764	835
SCN2A	CDKL5	O76039	818
SCN2A	SCN3B	Q9NY72	790
SCN2A	PCDH10	Q9P2E7	787
SCN2A	SCN4B	Q8IWT1	774
SCN2A	ANK3	Q12955	740
SCN2A	HBB	P02023	729
SCN2A	KCNT1	Q5JUK3	720
SCN2A	KCNA2	P16389	720
SCN2A	KCNQ3	O43525	716

IntAct

Human interaction partners of SCN2A in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

9 partners by confidence:

Partner	Interaction type	MIscore	Records
CALM1	physical association	0.690	1
ELAVL3	physical association	0.500	1
ATP5F1A	physical association	0.400	1
ATP5PD	physical association	0.400	1
IGF2BP3	association	0.350	1
IGLL5	association	0.350	1
ARHGEF10L	physical association	0.000	1
MPP3	physical association	0.000	1
RNF130	physical association	0.000	1

BioGRID (80 interactions; top human partners by supporting records): ATP5H (Cross-Linking-MS (XL-MS); 2 records), CALM2 (Affinity Capture-MS; 2 records), DNAJC5 (Cross-Linking-MS (XL-MS); 2 records), ELAVL2 (Affinity Capture-MS; 2 records), ELAVL3 (Affinity Capture-MS; 2 records), IGF2BP1 (Affinity Capture-MS; 2 records), IGF2BP2 (Affinity Capture-MS; 2 records), IGF2BP3 (Affinity Capture-MS; 2 records), SCN3A (Affinity Capture-MS; 2 records), SCN9A (Affinity Capture-MS; 2 records), ABCC8 (Affinity Capture-MS), AKAP1 (Affinity Capture-MS), ATP1A3 (Affinity Capture-MS), ATP1B1 (Affinity Capture-MS), ATP2B1 (Affinity Capture-MS)

SIGNOR signaling

showing 25 of 33 signaling interactions:

A	Effect	B	Mechanism
RCOR1	“down-regulates quantity by repression”	SCN2A	“transcriptional regulation”
REST	“down-regulates quantity by repression”	SCN2A	“transcriptional regulation”
SCN2A	“up-regulates quantity”	sodium(1+)	relocalization
FGF13	“down-regulates activity”	SCN2A	binding
FGF12	“down-regulates activity”	SCN2A	binding
FGF14	“down-regulates activity”	SCN2A	binding
FGF11	“down-regulates activity”	SCN2A	binding
SCN2A	up-regulates	Action_potential
“CoREST-HDAC complex”	“down-regulates quantity by repression”	SCN2A	“transcriptional regulation”
GSK3B	“down-regulates activity”	SCN2A	phosphorylation
PKA	“down-regulates activity”	SCN2A	phosphorylation
PKC	“down-regulates activity”	SCN2A	phosphorylation
CSNK2A3	“up-regulates activity”	SCN2A	phosphorylation
CSNK2B	“up-regulates activity”	SCN2A	phosphorylation
CSNK2A1	“up-regulates activity”	SCN2A	phosphorylation
CSNK2A2	“up-regulates activity”	SCN2A	phosphorylation
NEDD4L	“down-regulates quantity by destabilization”	SCN2A	ubiquitination
TNF	“up-regulates quantity by expression”	SCN2A	“transcriptional regulation”
TNF	“up-regulates activity”	SCN2A
KDM5C	“down-regulates quantity by repression”	SCN2A	“transcriptional regulation”
IL10	“down-regulates quantity by repression”	SCN2A	“transcriptional regulation”
phenytoin	“down-regulates activity”	SCN2A	“chemical inhibition”
carbamazepine	“down-regulates activity”	SCN2A	“chemical inhibition”
lidocaine	“down-regulates activity”	SCN2A	“chemical inhibition”
verapamil	“down-regulates activity”	SCN2A	“chemical inhibition”

Protein complexes (CORUM) (1)

Experimentally-characterized complexes this protein is a subunit of (★ = the complex contains a known drug target).

1 complexes by size:

Complex	Subunits	Members
★ SCN2A-SCN2B complex	2	SCN2A, SCN2B

Disease & clinical

Genetic variants

Variant evidence for SCN2A: 3,105 ClinVar records (675 pathogenic / likely pathogenic); 31 ClinGen expert-panel interpretations; 7 PharmGKB clinical annotations; 18 GWAS associations. Per-variant detail is on Sugi Variant.

ClinVar

3,105 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	354
Likely pathogenic	321
Uncertain significance	1300
Likely benign	719
Benign	123

Top pathogenic / likely-pathogenic (15)

Showing the 15 best-reviewed of 675 pathogenic / likely-pathogenic ClinVar records, ranked by ClinVar review status (expert panel → multiple submitters → single submitter), then by number of submitting labs.

Variant ID	HGVS	Classification	Review	Submitters
194555	NM_001040142.2(SCN2A):c.2558G>A (p.Arg853Gln)	Pathogenic	reviewed by expert panel	17
207024	NM_001040142.2(SCN2A):c.5317G>A (p.Ala1773Thr)	Pathogenic	reviewed by expert panel	14
207018	NM_001040142.2(SCN2A):c.4879G>A (p.Val1627Met)	Pathogenic	reviewed by expert panel	4
870190	NM_001040142.2(SCN2A):c.4832T>C (p.Leu1611Pro)	Pathogenic	reviewed by expert panel	3
3343696	NM_001040142.2(SCN2A):c.468G>C (p.Lys156Asn)	Pathogenic	reviewed by expert panel	2
1478168	NM_001040142.2(SCN2A):c.5636T>C (p.Met1879Thr)	Likely pathogenic	reviewed by expert panel	8
206972	NM_001040142.2(SCN2A):c.2657T>C (p.Leu886Ser)	Likely pathogenic	reviewed by expert panel	4
206975	NM_001040142.2(SCN2A):c.2696G>A (p.Gly899Asp)	Likely pathogenic	reviewed by expert panel	4
933619	NM_001040142.2(SCN2A):c.466A>C (p.Lys156Gln)	Likely pathogenic	reviewed by expert panel	4
984831	NM_001040142.2(SCN2A):c.3778A>G (p.Lys1260Glu)	Likely pathogenic	reviewed by expert panel	4
2435687	NM_001040142.2(SCN2A):c.1094C>T (p.Thr365Met)	Likely pathogenic	reviewed by expert panel	4
383825	NM_001040142.2(SCN2A):c.4782G>C (p.Trp1594Cys)	Likely pathogenic	reviewed by expert panel	3
984832	NM_001040142.2(SCN2A):c.3778A>C (p.Lys1260Gln)	Likely pathogenic	reviewed by expert panel	3
567919	NM_001040142.2(SCN2A):c.658A>G (p.Arg220Gly)	Likely pathogenic	reviewed by expert panel	2
1335404	NM_001040142.2(SCN2A):c.466A>G (p.Lys156Glu)	Likely pathogenic	reviewed by expert panel	2

Per-variant reference — Sugi Variant

Explore SCN2A’s pathogenic and likely-pathogenic variants individually — each with its ClinVar classification and conditions, applied ACMG criteria (ClinGen expert panel, where curated), the calibrated in-silico predictors (AlphaMissense, REVEL, SaProt, conservation), gnomAD frequency, and the predictor-disagreement QC signal — on Sugi Variant.

ClinGen expert-panel interpretations (31)

Expert ACMG interpretations from Epilepsy Sodium Channel VCEP for complex neurodevelopmental disorder — a higher-authority tier than individual ClinVar submissions.

Assertion	Variants
Pathogenic	6
Likely Pathogenic	10
Uncertain Significance	9
Likely Benign	2
Benign	4

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 26 predictions of 2,264):

Position(s)	Effect	Δscore	Sites
2:165296088	donor_gain	1.0000
2:165307859	acceptor_gain	1.0000
2:165307868	acceptor_gain	1.0000
2:165313900–165313901	acceptor_loss	1.0000	6
2:165314109–165314110	donor_loss	1.0000	4
2:165323153	acceptor_gain	1.0000
2:165323501–165323502	donor_loss	1.0000	5
2:165326985–165326986	donor_loss	1.0000	5
2:165342482	donor_gain	1.0000
2:165344548	acceptor_gain	1.0000

HPA cancer prognostics

RNA cancer specificity: Cancer enhanced (Glioblastoma Multiforme)

Disease associations

OMIM: gene MIM:182390 | disease phenotypes: MIM:607745, MIM:613721, MIM:618924, MIM:601764, MIM:604233, MIM:160120, MIM:616341, MIM:308350, MIM:209850, MIM:613863, MIM:201300, MIM:613722, MIM:128235, MIM:156200, MIM:117100, MIM:617080

GenCC curated gene-disease

10 curated gene-disease records:

Disease	Classification	Inheritance	Records
developmental and epileptic encephalopathy, 11	Definitive	Autosomal dominant	3
complex neurodevelopmental disorder	Definitive	Autosomal dominant	3
intellectual disability	Definitive	Autosomal dominant
seizures, benign familial infantile, 3	Strong	Autosomal dominant	2
episodic ataxia, type 9	Strong	Autosomal dominant
benign familial neonatal-infantile seizures	Supportive	Autosomal dominant
genetic developmental and epileptic encephalopathy	Supportive	Autosomal dominant
malignant migrating partial seizures of infancy	Supportive	Autosomal dominant
benign familial infantile epilepsy	Supportive	Autosomal dominant
Dravet syndrome	Supportive	Autosomal dominant

ClinGen Gene-Disease Validity

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

1 validity classifications:

Disease	Classification	Inheritance
complex neurodevelopmental disorder	Definitive	AD

Genomics England panels (PanelApp)

Clinical diagnostic gene panels including this gene (10 panels, 10 green/diagnostic-grade). Confidence: green = diagnostic, amber = moderate.

10 panels:

Panel	Rating
Ataxia and cerebellar anomalies - childhood onset	green
DDG2P	green
Early onset or syndromic epilepsy	green
Fetal anomalies	green
Hereditary ataxia and cerebellar anomalies, childhood onset	green
Hypotonic infant	green
Intellectual disability	green
Leukodystrophy, childhood onset	green
Paediatric disorders	green
Unexplained death in infancy and sudden unexplained death in childhood	green

Mondo (32): seizures, benign familial infantile, 3 (MONDO:0011904), developmental and epileptic encephalopathy, 11 (MONDO:0013388), neurodevelopmental disorder (MONDO:0700092), epilepsy (MONDO:0005027), SCN2A-related disorder (MONDO:1060245), episodic ataxia, type 9 (MONDO:0030064), benign familial infantile epilepsy (MONDO:0017615), complex neurodevelopmental disorder (MONDO:0100038), developmental and epileptic encephalopathy (MONDO:0100620), infantile spasms (MONDO:0018097), generalized epilepsy with febrile seizures plus (MONDO:0018214), autism spectrum disorder (MONDO:0005258), non-syndromic intellectual disability (MONDO:0000509), hereditary episodic ataxia (MONDO:0016227), developmental and epileptic encephalopathy, 30 (MONDO:0014595), benign familial neonatal-infantile seizures 1 (MONDO:0042499), genetic developmental and epileptic encephalopathy (MONDO:0100062), autism (MONDO:0005260), generalized epilepsy with febrile seizures plus, type 7 (MONDO:0013470), neuropathy, hereditary sensory and autonomic, type 2A (MONDO:0024309), developmental and epileptic encephalopathy, 12 (MONDO:0013389), dystonia 12 (MONDO:0007496), malignant migrating partial seizures of infancy (MONDO:0017385), focal epilepsy (MONDO:0005384), intellectual disability, autosomal dominant (MONDO:0100172), intellectual disability (MONDO:0001071), self-limited epilepsy with centrotemporal spikes (MONDO:0007295), seizures, benign familial infantile, 5 (MONDO:0014903), autosomal dominant non-syndromic intellectual disability (MONDO:0015802), movement disorder (MONDO:0005395), (MONDO:0011140), (MONDO:0011794)

Orphanet (15): Self-limited neonatal-infantile epilepsy (Orphanet:140927), Early infantile developmental and epileptic encephalopathy (Orphanet:1934), Self-limited infantile epilepsy (Orphanet:306), Non-specific syndromic intellectual disability (Orphanet:528084), West syndrome (Orphanet:3451), Infantile epileptic spasms syndrome (Orphanet:697160), Genetic epilepsy with febrile seizure plus (Orphanet:36387), Hereditary episodic ataxia (Orphanet:211062), Hereditary sensory and autonomic neuropathy type 2 (Orphanet:970), Rapid-onset dystonia-parkinsonism (Orphanet:71517), Epilepsy of infancy with migrating focal seizures (Orphanet:293181), Self-limited epilepsy with centrotemporal spikes (Orphanet:1945), Autosomal dominant non-syndromic intellectual disability (Orphanet:178469), NON RARE IN EUROPE: Autism (Orphanet:106), NON RARE IN EUROPE: Unexplained intellectual disability (Orphanet:319658)

HPO phenotypes

showing 60 of 208 phenotypes (HPO-id order):

HPO	Term
HP:0000006	Autosomal dominant inheritance
HP:0000054	Micropenis
HP:0000070	Ureterocele
HP:0000110	Renal dysplasia
HP:0000175	Cleft palate
HP:0000252	Microcephaly
HP:0000297	Facial hypotonia
HP:0000340	Sloping forehead
HP:0000348	High forehead
HP:0000463	Anteverted nares
HP:0000466	Limited neck range of motion
HP:0000486	Strabismus
HP:0000505	Visual impairment
HP:0000565	Esotropia
HP:0000577	Exotropia
HP:0000639	Nystagmus
HP:0000657	Oculomotor apraxia
HP:0000707	Abnormality of the nervous system
HP:0000708	Atypical behavior
HP:0000712	Emotional lability
HP:0000717	Autism
HP:0000718	Aggressive behavior
HP:0000729	Autistic behavior
HP:0000736	Short attention span
HP:0000739	Anxiety
HP:0000750	Delayed speech and language development
HP:0000752	Hyperactivity
HP:0000826	Precocious puberty
HP:0000961	Cyanosis
HP:0000975	Hyperhidrosis
HP:0000980	Pallor
HP:0001249	Intellectual disability
HP:0001250	Seizure
HP:0001251	Ataxia
HP:0001252	Hypotonia
HP:0001254	Lethargy
HP:0001257	Spasticity
HP:0001260	Dysarthria
HP:0001263	Global developmental delay
HP:0001266	Choreoathetosis
HP:0001268	Mental deterioration
HP:0001272	Cerebellar atrophy
HP:0001273	Abnormal corpus callosum morphology
HP:0001276	Hypertonia
HP:0001284	Areflexia
HP:0001298	Encephalopathy
HP:0001300	Parkinsonism
HP:0001302	Pachygyria
HP:0001327	Photosensitive myoclonic seizure
HP:0001332	Dystonia
HP:0001336	Myoclonus
HP:0001337	Tremor
HP:0001347	Hyperreflexia
HP:0001350	Slurred speech
HP:0001500	Broad finger
HP:0001508	Failure to thrive
HP:0001537	Umbilical hernia
HP:0001629	Ventricular septal defect
HP:0001638	Cardiomyopathy
HP:0001763	Pes planus

GWAS associations

18 associations:

Study	Trait	p-value
GCST007343_2	Epilepsy	2e-13
GCST010002_403	Refractive error	1e-11
GCST008647_50	Urinary sodium excretion	1e-10
GCST002672_4	Febrile seizures	3e-10
GCST006630_74	Diastolic blood pressure	3e-10
GCST008103_171	Bipolar disorder	2e-9
GCST011102_2	Bipolar disorder	2e-9
GCST007352_1	Focal epilepsy	7e-9
GCST90000047_207	Age at first sexual intercourse	1e-8
GCST010988_471	Adult body size	2e-8
GCST90000050_17	Age at first birth	2e-8
GCST012465_40	Bipolar disorder	3e-8
GCST007353_3	Generalized epilepsy	5e-8
GCST002673_3	Febrile seizures (MMR vaccine-unrelated)	2e-7
GCST007401_10	Factor VII activity	8e-7
GCST008154_44	Trunk fat mass	3e-6
GCST002674_5	Febrile seizures (MMR vaccine-related)	4e-6
GCST002129_12	Periodontitis (DPAL)	5e-6

EFO canonical traits (from GWAS)

6 canonical traits:

EFO ID	Trait name
EFO:0006519	MMR-related febrile seizures
EFO:0006336	diastolic blood pressure
EFO:0004619	factor VII measurement
EFO:0009282	sodium measurement
EFO:0009749	age at first sexual intercourse measurement
EFO:0009101	age at first birth measurement

MeSH disease descriptors

9 disease descriptors:

Descriptor	Name	Tree numbers
D001321	Autistic Disorder	F03.625.164.113.500
D004828	Epilepsies, Partial	C10.228.140.490.360
D004827	Epilepsy	C10.228.140.490
D008607	Intellectual Disability	C10.597.606.360; C23.888.592.604.646; F01.700.687; F03.625.539
D009069	Movement Disorders	C10.228.662
D065886	Neurodevelopmental Disorders	F03.625
C538001	Dystonia 12 *(supp.)*
C567827	Generalized Epilepsy With Febrile Seizures Plus, 7 *(supp.)*
C565808	Generalized Epilepsy with Febrile Seizures Plus *(supp.)*

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (4): CHEMBL2096682 (PROTEIN FAMILY), CHEMBL2331043 (PROTEIN FAMILY), CHEMBL4187 (SINGLE PROTEIN), CHEMBL4523672 (PROTEIN COMPLEX)

Drugs by curated mechanism of action (ChEMBL)

Drugs whose curated ChEMBL mechanism of action targets the SCN2A protein itself — single-protein targets only (drugs acting on a protein family or complex that merely includes it are excluded). Includes antibodies and oligonucleotides that bioactivity screening does not capture.

1 curated-mechanism drugs:

Drug	Modality	Max phase
ELPETRIGINE	Small molecule	2

Drugs acting on a complex or family that includes this protein

Curated ChEMBL mechanism-of-action drugs whose target is a protein complex or family of ≤10 members that includes SCN2A — the drug acts on the assembly or class, not necessarily on this subunit alone.

51 drugs via a complex or family:

Drug	Target (ChEMBL)	Members	Max phase
ARTICAINE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
BENOXINATE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
CARBAMAZEPINE	Sodium channel alpha subunit	10	4
CENOBAMATE	Sodium channel alpha subunit	10	4
CHLOROPROCAINE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
COCAINE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
DISOPYRAMIDE PHOSPHATE	Sodium channel alpha subunit	10	4
DRONEDARONE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
DYCLONINE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
ENCAINIDE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
ESLICARBAZEPINE	Sodium channel alpha subunit	10	4
ETHOTOIN	Sodium channel alpha subunit	10	4
ETIDOCAINE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
FOSPHENYTOIN SODIUM	Sodium channel alpha subunit	10	4
HEXYLCAINE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
INDECAINIDE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
LACOSAMIDE	Sodium channel alpha subunit	10	4
LAMOTRIGINE	Sodium channel alpha subunit	10	4
LIDOCAINE	Sodium channel alpha subunit	10	4
MEPHENYTOIN	Sodium channel alpha subunit	10	4
MEPIVACAINE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
MERETHOXYLLINE PROCAINE	Sodium channel alpha subunit	10	4
MEXILETINE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
MORICIZINE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
ORPHENADRINE CITRATE	Sodium channel alpha subunit	10	4
OXCARBAZEPINE	Sodium channel alpha subunit	10	4
PHENACEMIDE	Sodium channel alpha subunit	10	4
PHENAZOPYRIDINE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
PHENYTOIN	Sodium channel alpha subunit	10	4
PRILOCAINE	Sodium channel alpha subunit	10	4
PRIMIDONE	Sodium channel alpha subunit	10	4
PROCAINAMIDE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
PROCAINE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
PROPAFENONE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
PROPARACAINE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
PROPOXYCAINE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
QUINIDINE POLYGALACTURONATE	Sodium channel alpha subunit	10	4
QUINIDINE SULFATE	Sodium channel alpha subunit	10	4
RILUZOLE	Sodium channel alpha subunit	10	4
ROPIVACAINE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
RUFINAMIDE	Sodium channel alpha subunit	10	4
TETRACAINE	Sodium channel alpha subunit	10	4
TOCAINIDE HYDROCHLORIDE	Sodium channel alpha subunit	10	4
TOPIRAMATE	Sodium channel alpha subunit	10	4
ZONISAMIDE	Sodium channel alpha subunit	10	4
RALFINAMIDE	Sodium channel alpha subunit	10	3
EVENAMIDE	Sodium channel alpha subunit	10	2
IRAMPANEL	Sodium channel alpha subunit	10	2
NERISPIRDINE	Sodium channel alpha subunit	10	2
NKTR-171	Sodium channel alpha subunit	10	1
DICHLOROBENZYL ALCOHOL	Sodium channel alpha subunit	10	—

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 610,590 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

showing 60 of 99 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL633	AMIODARONE	4	30,023
CHEMBL629	AMITRIPTYLINE	4	53,007
CHEMBL1093	ARTICAINE	4	6,646
CHEMBL1200	BENOXINATE	4	6,775
CHEMBL1008	BEPRIDIL	4	11,851
CHEMBL811	BROMPHENIRAMINE	4	11,633
CHEMBL1098	BUPIVACAINE	4	38,262
CHEMBL505	CHLORPHENIRAMINE	4	40,568
CHEMBL71	CHLORPROMAZINE	4	46,206
CHEMBL43064	CINNARIZINE	4	16,783
CHEMBL370805	COCAINE	4	80,173
CHEMBL516	CYPROHEPTADINE	4	17,623
CHEMBL72	DESIPRAMINE	4	35,148
CHEMBL1086	DIBUCAINE	4	17,368
CHEMBL1123	DICYCLOMINE	4	8,759
CHEMBL23	DILTIAZEM	4	55,053
CHEMBL657	DIPHENHYDRAMINE	4	100,285
CHEMBL936	DIPHENIDOL	4	5,532
CHEMBL1108	DROPERIDOL	4	17,045
CHEMBL492	ETIDOCAINE	4	11,850
CHEMBL1480	FELODIPINE	4
CHEMBL726	FLUPHENAZINE	4
CHEMBL54	HALOPERIDOL	4
CHEMBL1197	HEXYLCAINE	4
CHEMBL11	IMIPRAMINE	4
CHEMBL741	LAMOTRIGINE	4
CHEMBL592	LEVORPHANOL	4
CHEMBL841	LOPERAMIDE	4
CHEMBL558	MEXILETINE	4
CHEMBL6437	MIANSERIN	4
CHEMBL45816	MIBEFRADIL	4
CHEMBL193	NIFEDIPINE	4
CHEMBL1726	NISOLDIPINE	4
CHEMBL1193	PHENIRAMINE	4
CHEMBL753	PHENOXYBENZAMINE	4
CHEMBL597	PHENTOLAMINE	4
CHEMBL16	PHENYTOIN	4
CHEMBL1423	PIMOZIDE	4
CHEMBL1198	PRAMOXINE	4
CHEMBL2	PRAZOSIN	4
CHEMBL24072	PRENYLAMINE	4
CHEMBL1194	PRILOCAINE	4
CHEMBL564	PROMAZINE	4
CHEMBL643	PROMETHAZINE	4
CHEMBL1196	PROPARACAINE	4
CHEMBL1195	PROPOXYCAINE	4
CHEMBL7568	QUINACRINE	4
CHEMBL1294	QUINIDINE	4
CHEMBL170	QUININE	4
CHEMBL772	RESERPINE	4
CHEMBL744	RILUZOLE	4
CHEMBL12713	SERTINDOLE	4
CHEMBL117785	TETRABENAZINE	4
CHEMBL698	TETRACAINE	4
CHEMBL479	THIORIDAZINE	4
CHEMBL422	TRIFLUOPERAZINE	4
CHEMBL6966	VERAPAMIL	4
CHEMBL5314404	AJMALINE	3
CHEMBL3707392	ELECLAZINE	3
CHEMBL475534	NITRENDIPINE	3

PharmGKB: 1 entry (CPIC guideline: no)

PharmGKB clinical annotations

7 annotations by evidence level (1 strongest → 4):

Variant	Association	Level	Drugs	Phenotypes
rs2304016	Efficacy	3	antiepileptics	Epilepsy
rs2304016	Efficacy	3	carbamazepine	Epilepsy
rs2304016	Efficacy	3	lamotrigine	Epilepsy
rs2304016	Efficacy	3	oxcarbazepine	Epilepsy
rs2304016	Efficacy	3	phenytoin	Epilepsy
rs2304016	Efficacy	3	topiramate	Epilepsy
rs17183814	Efficacy	4	antiepileptics;carbamazepine;phenobarbital;phenytoin;valproic acid	Epilepsy

PharmGKB variants

2 variants:

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2304016	SCN2A	3	3.25	6	oxcarbazepine;antiepileptics;carbamazepine;lamotrigine;phenytoin;topiramate
rs17183814	SCN2A	4	-2.50	1	antiepileptics;carbamazepine;phenobarbital;phenytoin;valproic acid

PharmGKB variant annotations

Per-publication pharmacogenomic findings for this gene (significant associations).

5 published findings:

Variant	Drug(s)	Category	Finding	PMID
rs2304016	antiepileptics	Efficacy	Allele A is associated with drug resistance when treated with antiepileptics in people with Epilepsy as compared to allele G.	PMID:18784617
rs17183814	valproic acid	Efficacy	Genotypes AA + AG is associated with increased resistance to valproic acid in children with Epilepsy as compared to genotype GG.	PMID:38837984
rs2304016	carbamazepine, lamotrigine, oxcarbazepine, phenytoin, topiramate	Efficacy	Allele A is associated with drug resistance when treated with carbamazepine, lamotrigine, oxcarbazepine, phenytoin or topiramate in people with Epilepsy as compared to allele G.	PMID:18784617
rs17183814	carbamazepine, phenobarbital, phenytoin, valproic acid	Efficacy	Allele A is associated with resistance to carbamazepine, phenobarbital, phenytoin or valproic acid as compared to allele G.	PMID:19694741
rs17183814	carbamazepine, phenytoin, valproic acid	Efficacy	Allele A is associated with non-response when treated with carbamazepine, phenytoin or valproic acid in people with Epilepsy as compared to allele G.	PMID:21747585

GtoPdb / IUPHAR curated pharmacology

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

Target class: vgic — Voltage-gated sodium channels (Na_V)

Most potent curated ligand interactions (27 total), top 25:

Ligand	Action	Affinity	Parameter
β-scorpion toxin Css IV	Partial agonist	9.7	pKd
batrachotoxin	Agonist	9.1	pKd
μ-conotoxin SmIIIA	Pore blocker	8.9	pKd
saxitoxin	Pore blocker	8.8	pIC50
α-scorpion toxin 2	Slows inactivation	8.7	pKd
μ-conotoxin KIIIA	Inhibition	8.3	pKd
GNE-131	Inhibition	8.15	pIC50
ATX-II	Slows inactivation	8.1	pEC50
tetrodotoxin	Pore blocker	8.0	pIC50
XPC-5462	Channel blocker	7.96	pIC50
GNE-616	Inhibition	7.92	pKd
huwentoxin IV	Voltage-dependent inhibition	7.8	pKd
C4Pen	Inhibition	7.48	pIC50
protoxin II	Voltage-dependent inhibition	7.4	pKi
relutrigine	Inhibition	6.76	pIC50
funapide	Inhibition	6.22	pIC50
etidocaine	Pore blocker	6.0	pIC50
aconitine	Partial agonist	5.9	pKd
Bc-III	Slows inactivation	5.8	pEC50
AFT-II	Slows inactivation	5.7	pEC50
cannabidiol	Channel blocker	5.54	pIC50
veratridine	Partial agonist	5.2	pKd
lidocaine	Pore blocker	5.0	pIC50
phenytoin	Pore blocker	4.9	pIC50
lacosamide	Antagonist	4.52	pIC50

Binding affinities (BindingDB)

836 measured of 929 human assays (952 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
CHEMBL3617050	IC50	0.006 nM
Fluperamide	KI	0.11 nM
CHEMBL4060338	IC50	0.28 nM
5-cyclopropyl-4-[(3R)-1-[(3,5-dichlorophenyl)methyl]piperidin-3-yl]oxy-2-fluoro-N-methylsulfonylbenzamide	IC50	0.3 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[2-(3-amino-1,2-benzoxazol-5-yl)-4-chlorophenoxy]-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide	IC50	0.6 nM	US-9481677: Biaryl ether sulfonamides and their use as therapeutic agents
5-cyclopropyl-N-cyclopropylsulfonyl-4-[[1-[(3,5-dichlorophenyl)-phenylmethyl]piperidin-4-yl]methoxy]-2-fluorobenzamide	IC50	0.8 nM	US-9694002: Substituted benzamides and methods of use thereof
N-(m-Tolyl)-6-(4-ethoxyphenyl)-pyrazine-2-carboxamide	IC50	1 nM
4-[(3R)-1-[[3-chloro-5-(trifluoromethoxy)phenyl]methyl]piperidin-3-yl]oxy-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamide	IC50	1.3 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[(3,5-dichlorophenyl)-phenylmethyl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamide	IC50	1.5 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[(2S)-2-(3,5-dichlorophenyl)-1-methoxypropan-2-yl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamide	IC50	1.6 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[(1S)-1-(3,5-dichlorophenyl)-2-methoxy-2-methylpropyl]piperidin-4-yl]methoxy]-N-ethylsulfonyl-2-fluorobenzamide	IC50	1.6 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[(1S)-1-(3,5-dichloro-2-fluorophenyl)ethyl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamide	IC50	1.6 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[[1-[1-(2-chloro-4-fluorophenyl)-2,2,2-trifluoroethyl]piperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamide	IC50	1.6 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[(3R)-1-[(2-chlorophenyl)methyl]piperidin-3-yl]oxy-5-cyclopropyl-N-cyclopropylsulfonyl-2-fluorobenzamide	IC50	1.7 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[(3R)-1-[(2,4-dichlorophenyl)methyl]piperidin-3-yl]oxy-2-fluoro-N-methylsulfonylbenzamide	IC50	1.7 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[(1R)-1-(3,5-dichlorophenyl)-2-methoxy-2-methylpropyl]piperidin-4-yl]methoxy]-N-ethylsulfonyl-2-fluorobenzamide	IC50	1.7 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[2-(3,5-dichlorophenyl)propan-2-yl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamide	IC50	1.7 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[(1S)-1-(3,5-dichlorophenyl)ethyl]-4-methylpiperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamide	IC50	1.7 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[(1S)-1-(3,5-dichlorophenyl)-2-methoxy-2-methylpropyl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamide	IC50	1.8 nM	US-9694002: Substituted benzamides and methods of use thereof
CHEBI:51137	KI	1.9 nM
5-cyclopropyl-2-fluoro-4-[(3R)-1-[[4-fluoro-2-(trifluoromethyl)phenyl]methyl]piperidin-3-yl]oxy-N-methylsulfonylbenzamide	IC50	1.9 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[(3R)-1-[(1S)-1-(3,5-dichlorophenyl)ethyl]piperidin-3-yl]oxy-2-fluoro-N-methylsulfonylbenzamide	IC50	1.9 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[[1-[[3-chloro-5-(trifluoromethoxy)phenyl]methyl]piperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamide	IC50	1.9 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[2-(3,5-dichlorophenyl)propan-2-yl]piperidin-4-yl]methoxy]-N-ethylsulfonyl-2-fluorobenzamide	IC50	1.9 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[1-(3,5-dichlorophenyl)-2,2,2-trifluoroethyl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamide	IC50	1.9 nM	US-9694002: Substituted benzamides and methods of use thereof
N-(azetidin-1-ylsulfonyl)-4-[(3R,6R)-1-[(2-chloro-4-fluorophenyl)methyl]-6-methylpiperidin-3-yl]oxy-5-cyclopropyl-2-fluorobenzamide	IC50	1.9 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[(3R,6R)-1-[(2-chloro-4-fluorophenyl)methyl]-6-methylpiperidin-3-yl]oxy-5-cyclopropyl-N-cyclopropylsulfonyl-2-fluorobenzamide	IC50	1.9 nM	US-9694002: Substituted benzamides and methods of use thereof
CHEMBL4070670	IC50	2 nM
5-(4-chlorophenyl)-N-(2-methylbenzyl)nicotinamide	IC50	2 nM
N-(2-Methylbenzyl)-6-(4-ethoxyphenyl)-pyrazine-2-carboxamide	IC50	2 nM
N-(3,5-Dimethylphenyl)-6-(4-ethoxyphenyl)-pyrazine-2-carboxamide	IC50	2 nM
5-cyclopropyl-4-[[1-[1-(3,5-dichlorophenyl)propyl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamide	IC50	2 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[[1-[bis(3-chlorophenyl)methyl]piperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamide	IC50	2 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[[1-[bis(2-chlorophenyl)methyl]piperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamide	IC50	2 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-N-cyclopropylsulfonyl-4-[(3R)-1-(3,5-dichlorophenyl)piperidin-3-yl]oxy-2-fluorobenzamide	IC50	2.1 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[[1-[[2,5-bis(trifluoromethyl)phenyl]methyl]-4-methylpiperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamide	IC50	2.1 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[[1-[[3-chloro-5-(trifluoromethyl)phenyl]methyl]piperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamide	IC50	2.1 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[[1-[bis(4-chlorophenyl)methyl]piperidin-4-yl]methoxy]-5-cyclopropyl-N-cyclopropylsulfonyl-2-fluorobenzamide	IC50	2.1 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[(3R)-1-[(2,4-dimethylphenyl)methyl]piperidin-3-yl]oxy-2-fluoro-N-methylsulfonylbenzamide	IC50	2.1 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[[1-[5-chloro-4-(trifluoromethyl)-2-pyridinyl]-4-methylpiperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamide	IC50	2.1 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[(1S)-1-(2,4-dichlorophenyl)ethyl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamide	IC50	2.2 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-N-cyclopropylsulfonyl-4-[[1-[(3,5-dichlorophenyl)methyl]piperidin-4-yl]methoxy]-2-fluorobenzamide	IC50	2.2 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[(3R)-1-[(2-chloro-4-fluorophenyl)methyl]piperidin-3-yl]oxy-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamide	IC50	2.2 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[[(1R,5S)-3-[3-chloro-5-(trifluoromethoxy)phenoxy]-8-azabicyclo[3.2.1]octan-8-yl]methyl]-5-cyclopropyl-N-cyclopropylsulfonyl-2-fluorobenzamide	IC50	2.2 nM	US-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[4-(3,5-dichlorophenyl)sulfanylpiperidin-1-yl]methyl]-2-fluorobenzamide	IC50	2.2 nM	US-9694002: Substituted benzamides and methods of use thereof
[(3aS,4R,10aS)-2,6-diamino-10,10-dihydroxy-3a,4,8,9-tetrahydro-1H-pyrrolo[1,2-c]purin-4-yl]methyl carbamate	IC50	2.3 nM	US-9174999: Methods and compositions for studying, imaging, and treating pain
5-cyclopropyl-N-cyclopropylsulfonyl-4-[[1-[(1S)-1-(3,5-dichlorophenyl)-2-methoxyethyl]piperidin-4-yl]methoxy]-2-fluorobenzamide	IC50	2.3 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[(3R)-1-[(1S)-1-(2-chloro-4-fluorophenyl)ethyl]piperidin-3-yl]oxy-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamide	IC50	2.3 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[(3R)-1-[(1S)-1-(5-chloro-6-cyclopropyl-2-pyridinyl)ethyl]piperidin-3-yl]oxy-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamide	IC50	2.3 nM	US-9694002: Substituted benzamides and methods of use thereof
4-[(3R)-1-[2-(3-chlorophenyl)propan-2-yl]piperidin-3-yl]oxy-5-cyclopropyl-2-fluorobenzamide	IC50	2.3 nM	US-9694002: Substituted benzamides and methods of use thereof

ChEMBL bioactivities

261 potent at pChembl≥5 of 343 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.70	IC50	0.2	nM	CHEMBL3617063
9.55	IC50	0.28	nM	CHEMBL4060338
9.35	IC50	0.45	nM	CHEMBL4060338
9.00	IC50	1	nM	SAXITOXIN
8.70	IC50	2	nM	CHEMBL4070670
8.70	IC50	2	nM	CHEMBL3662190
8.68	IC50	2.1	nM	CHEMBL4070670
8.60	IC50	2.519	nM	CHEMBL4217988
8.52	IC50	3	nM	CHEMBL4217988
8.38	IC50	4.2	nM	CHEMBL3341983
8.28	EC50	5.3	nM	CHEMBL4064160
8.22	IC50	6	nM	CHEMBL3662077
8.15	IC50	7	nM	CHEMBL4290579
8.12	IC50	7.5	nM	CHEMBL4082248
8.00	IC50	10	nM	CHEMBL4285790
7.92	EC50	12	nM	CHEMBL4060338
7.92	Kd	12	nM	CHEMBL4464990
7.92	IC50	12	nM	CHEMBL4854735
7.89	IC50	13	nM	CHEMBL4580996
7.85	IC50	14	nM	CHEMBL4279238
7.85	IC50	14	nM	TETRODOTOXIN
7.82	IC50	15.02	nM	BREVETOXIN B
7.82	IC50	15	nM	CHEMBL6143914
7.72	IC50	18.9	nM	CHEMBL3657855
7.70	IC50	20	nM	CHEMBL3657855
7.58	IC50	26	nM	CHEMBL4064160
7.54	IC50	29	nM	CHEMBL4068937
7.51	IC50	31	nM	CHEMBL4460028
7.46	IC50	35	nM	CHEMBL4082248
7.42	IC50	38	nM	CHEMBL5094715
7.39	IC50	41	nM	CHEMBL4224739
7.33	IC50	47	nM	CHEMBL4466858
7.30	IC50	50	nM	CHEMBL1269990
7.27	IC50	54	nM	PIMOZIDE
7.19	Kd	64	nM	CHEMBL4444707
7.19	IC50	65	nM	CHEMBL5598329
7.18	IC50	66	nM	CHEMBL4435054
7.16	IC50	70	nM	CHEMBL1270301
7.10	EC50	79	nM	CHEMBL4082248
7.10	IC50	79	nM	CHEMBL3318132
7.00	IC50	100	nM	CHEMBL486495
6.96	IC50	110	nM	PF-05089771
6.96	IC50	110	nM	CHEMBL1269882
6.92	EC50	120	nM	CHEMBL4070670
6.92	IC50	119	nM	PF-05089771
6.92	IC50	120	nM	CHEMBL4588728
6.92	IC50	120	nM	CHEMBL5598304
6.92	IC50	120	nM	CHEMBL1269991
6.90	IC50	125	nM	CHEMBL4471825
6.85	Kd	140	nM	CHEMBL4471012

PubChem BioAssay actives

260 with measured affinity, of 912 total; 50 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
[(3R,5S,6S,11R,12S,16S)-14,17-diamino-19,19-dihydroxy-6-(hydroxymethyl)-10-oxo-3-sulfooxy-8-oxa-1,9,13,15,18-pentazapentacyclo[9.5.2.13,16.05,9.012,16]nonadeca-14,17-dien-13-yl]methyl N-hydroxycarbamate	1246042: Inhibition of NaV1.2 channel (unknown origin) expressed in Xenopus laevis oocytes by two-electrode oocyte voltage-clamp method	ic50	<0.0001	uM
4-[2-(2-amino-3H-benzimidazol-5-yl)-4-chlorophenoxy]-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide	1300004: Inhibition of full length human Nav1.2 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis	ic50	0.0002	uM
(5R,7R)-7-decyl-1-oxa-8,10-diazaspiro[4.5]dec-8-en-9-amine	1432176: Antagonist activity at human Nav1.2 expressed in HEK293T cells assessed as inhibition of VTD-induced tail current by whole cell patch clamp method relative to control	ic50	0.0003	uM
[(3aS,4R,10aS)-2,6-diamino-10,10-dihydroxy-3a,4,8,9-tetrahydro-1H-pyrrolo[1,2-c]purin-4-yl]methyl carbamate	1525389: Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay	ic50	0.0010	uM
(5S,7S)-7-decyl-1-oxa-8,10-diazaspiro[4.5]dec-8-en-9-amine	1432176: Antagonist activity at human Nav1.2 expressed in HEK293T cells assessed as inhibition of VTD-induced tail current by whole cell patch clamp method relative to control	ic50	0.0020	uM
5-cyclopropyl-N-cyclopropylsulfonyl-2-fluoro-4-[(6-methylspiro[2.5]octan-6-yl)methoxy]benzamide	1525389: Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay	ic50	0.0020	uM
3-cyano-4-[2-[2-[(2-piperidin-4-ylethylamino)methyl]-4-pyridinyl]-4-[3-(trifluoromethyl)phenyl]phenoxy]-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide	1365875: Inhibition of human Nav1.2 expressed in HEK cells by patch clamp electrophysiology method	ic50	0.0025	uM
4-[2-(3-amino-1,2-benzoxazol-5-yl)-4-chlorophenoxy]-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide	1300004: Inhibition of full length human Nav1.2 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis	ic50	0.0042	uM
(5R,6S,7R)-9-amino-7-decyl-1-oxa-8,10-diazaspiro[4.5]dec-8-ene-6-carboxylic acid	1432177: Inhibition of Nav1.2 (unknown origin) by cell based assay	ec50	0.0053	uM
5-cyclopropyl-N-cyclopropylsulfonyl-4-[(4,4-difluoro-1-methylcyclohexyl)methoxy]-2-fluorobenzamide	1960144: Inhibition of human Nav1.2 alpha subunit expressed in HEK293 cells co-expressing beta1 subunit at -35 mV holding potential by PatchXpress automated voltage clamp electrophysiology technique	ic50	0.0060	uM
N-[7-(1-adamantylmethoxy)-6-cyclopropyl-[1,2,4]triazolo[4,3-a]pyridin-3-yl]cyclopropanesulfonamide	1410604: Inhibition of inactivated state of recombinant human NaV1.2 expressed in HEK293 cell membranes coexpressing Nav beta1 subunit assessed as decrease in sodium current amplitude at -35 mV holding potential by PX automated voltage clamp method	ic50	0.0070	uM
(5S,6R,7S)-9-amino-7-decyl-1-oxa-8,10-diazaspiro[4.5]dec-8-ene-6-carboxylic acid	1432157: Antagonist activity at human Nav1.2 expressed in HEK293T cells assessed as inhibition of VTD-induced sustained current by whole cell patch clamp method relative to control	ic50	0.0075	uM
N-[6-cyclopropyl-7-[(3,5-dichlorophenoxy)methyl]-[1,2,4]triazolo[4,3-a]pyridin-3-yl]methanesulfonamide	1410604: Inhibition of inactivated state of recombinant human NaV1.2 expressed in HEK293 cell membranes coexpressing Nav beta1 subunit assessed as decrease in sodium current amplitude at -35 mV holding potential by PX automated voltage clamp method	ic50	0.0100	uM
(4S)-6-fluoro-4-[(2R,4S)-2-pyridin-2-yl-4-(trifluoromethyl)piperidin-1-yl]-N-pyrimidin-4-yl-3,4-dihydro-2H-chromene-7-sulfonamide	1587753: Inhibition of full length human Nav1.2 expressed in HEK293 cells at -60 mV holding potential by manual patch clamp electrophysiology method	kd	0.0120	uM
4-[(3S,4S)-3-(3,4-difluorophenyl)-1-(2,2,2-trifluoroethyl)piperidin-4-yl]oxy-3,5-difluoro-N-(6-fluoro-2-pyridinyl)benzenesulfonamide	1754511: Inhibition of human Nav1.2 by V1/2 protocol based analysis	ic50	0.0120	uM
5-chloro-4-[[(1S)-1-(2,5-difluorophenyl)ethyl]amino]-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide	1616312: Inhibition of recombinant human full length Nav1.2 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential by whole cell patch clamp assay	ic50	0.0130	uM
(1R,5R,6R,7R,9S,11S,12S,13S,14S)-3-amino-14-(hydroxymethyl)-8,10-dioxa-2,4-diazatetracyclo[7.3.1.17,11.01,6]tetradec-3-ene-5,9,12,13,14-pentol	1525389: Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay	ic50	0.0140	uM
N-[7-(1-adamantylmethoxy)-6-cyclopropyl-[1,2,4]triazolo[4,3-a]pyridin-3-yl]methanesulfonamide	1410604: Inhibition of inactivated state of recombinant human NaV1.2 expressed in HEK293 cell membranes coexpressing Nav beta1 subunit assessed as decrease in sodium current amplitude at -35 mV holding potential by PX automated voltage clamp method	ic50	0.0140	uM
2-[[(1R,3S,5R,7S,9R,11S,12S,14R,16R,18S,20R,21Z,24S,26R,28S,30R,31R,33S,35R,37S,42R,44S,46R,48S)-12-hydroxy-1,3,11,24,31,41,44-heptamethyl-39-oxo-2,6,10,15,19,25,29,34,38,43,47-undecaoxaundecacyclo[26.22.0.03,26.05,24.07,20.09,18.011,16.030,48.033,46.035,44.037,42]pentaconta-21,40-dien-14-yl]methyl]prop-2-enal	254847: Inhibitory concentration against synaptosome using [3H]PbTx-3	ic50	0.0150	uM
(1S,2R,3S,5R)-5-[5-cyclopropyl-4-[[1-[(2,6-dichlorophenyl)methyl]piperidin-4-yl]methoxy]-2-fluorobenzoyl]-3-fluoro-2-methylcyclopentane-1-carboxylic acid	2218759: Inhibition of human Nav1.2 by patch clamp electrophysiology	ic50	0.0150	uM
4-(1-adamantylmethoxy)-N-(azetidin-1-ylsulfonyl)-5-cyclopropyl-2-fluorobenzamide	1831648: Inhibition of full length human Nav1.2 expressed in HEK cells by whole cell voltage clamp analysis	ic50	0.0189	uM
2-oxo-3-[(1R)-1-(1,2,3,4-tetrahydroisoquinolin-8-yl)ethyl]-N-(1,2,4-thiadiazol-5-yl)-1,3-benzoxazole-6-sulfonamide	1466785: Inhibition of Nav1.2 (unknown origin)	ic50	0.0290	uM
4-[[2-[(2,2-dimethylazetidin-1-yl)methyl]-6-fluorophenyl]methylamino]-2,6-difluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide	1616312: Inhibition of recombinant human full length Nav1.2 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential by whole cell patch clamp assay	ic50	0.0310	uM
5-cyclopropyl-4-[[1-[(1S)-1-(3,5-dichlorophenyl)ethyl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamide	1831648: Inhibition of full length human Nav1.2 expressed in HEK cells by whole cell voltage clamp analysis	ic50	0.0380	uM
(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(1R,4S,7S,13S,16R,21R,24S,27S,30S,33S,36S,39S,42R,45S,48S,51S,54S,57S,60R,65R,68S,71S,74S)-27,57-bis(4-aminobutyl)-21-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-24-(3-amino-3-oxopropyl)-54,74-bis(3-carbamimidamidopropyl)-13,51-bis(2-carboxyethyl)-45-(carboxymethyl)-39-[(1R)-1-hydroxyethyl]-48-(hydroxymethyl)-30,36,68-tris(1H-indol-3-ylmethyl)-71-(2-methylpropyl)-7,33-bis(2-methylsulfanylethyl)-3,6,9,12,15,22,25,28,31,34,37,40,43,46,49,52,55,58,67,70,73,76,81-tricosaoxo-4-propan-2-yl-18,19,62,63,78,79-hexathia-2,5,8,11,14,23,26,29,32,35,38,41,44,47,50,53,56,59,66,69,72,75,82-tricosazatricyclo[40.34.4.216,60]dooctacontane-65-carbonyl]amino]hexanoyl]amino]hexanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-indol-3-yl)propanoic acid	1388447: Inhibition of Nav1.2 (unknown origin) expressed in xenopus oocytes at -80 mV holding potential by two-electrode voltage-clamp method	ic50	0.0410	uM
2,6-difluoro-4-[[(1S)-1-(2-fluorophenyl)ethyl]amino]-N-(1,3-thiazol-4-yl)benzenesulfonamide	1616312: Inhibition of recombinant human full length Nav1.2 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential by whole cell patch clamp assay	ic50	0.0470	uM
5-(4-chlorophenyl)-N-[(2-piperidin-1-ylphenyl)methyl]pyridine-3-carboxamide	527217: Inhibition of human NaV1.2 by electrophysiology	ic50	0.0500	uM
Pimozide	1207165: Inhibition of Na channel (species unknown)	ic50	0.0540	uM
4-[[1-[[2-chloro-5-(trifluoromethyl)phenyl]methyl]piperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamide	1525419: Binding affinity to human recombinant Nav1.2 by radioligand binding assay	kd	0.0640	uM
4-(3-methoxyphenyl)-6-(8-methyl-1,3,4,5-tetrahydro-2-benzazepin-2-yl)pyrimidin-2-amine	2120760: Inhibition of human Nav1.2 expressed in HEK293 cells at -40 mv holding potential measured after 5 mins by whole cell voltage clamp electrophysiological analysis	ic50	0.0650	uM
2,6-difluoro-4-[[2-fluoro-6-[[methyl(propan-2-yl)amino]methyl]phenyl]methylamino]-N-(1,3-thiazol-4-yl)benzenesulfonamide	1616312: Inhibition of recombinant human full length Nav1.2 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential by whole cell patch clamp assay	ic50	0.0660	uM
5-(4-chlorophenyl)-N-[(2-piperidin-1-yl-3-pyridinyl)methyl]pyridine-3-carboxamide	527217: Inhibition of human NaV1.2 by electrophysiology	ic50	0.0700	uM
[5-(4-tert-butylphenyl)furan-2-yl]-(4-cyclohexylpiperazin-1-yl)methanone	404535: Inhibition of human recombinant Nav1.2 channel expressed in HEK293 cells by whole cell voltage clamp technique	ic50	0.1000	uM
4-[2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide	1525389: Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay	ic50	0.1100	uM
5-(4-chlorophenyl)-N-[(2-methylphenyl)methyl]pyridine-3-carboxamide	527217: Inhibition of human NaV1.2 by electrophysiology	ic50	0.1100	uM
(3S)-3-amino-4-oxo-4-[[(1R,4S,7S,10S,13S,16S,19R,24R,27S,30S,33S,36S,39S,42S,45R,51S,54S,57S,60R,65R,68S,71S,74S,77S,83S)-7,30,36,42,57-pentakis(4-aminobutyl)-77-benzyl-39,68-bis(3-carbamimidamidopropyl)-24-[[(2S)-1-[[(2S)-1-[[(2S)-3-carboxy-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(1S,2R)-1-carboxy-2-hydroxypropyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-4,13-bis(2-carboxyethyl)-10,16,83-tris(carboxymethyl)-27,71-bis[(4-hydroxyphenyl)methyl]-54-(1H-imidazol-5-ylmethyl)-51-(2-methylpropyl)-33,74-bis(2-methylsulfanylethyl)-2,5,8,11,14,17,26,29,32,35,38,41,44,47,50,53,56,59,66,69,72,75,78,81,84,91-hexacosaoxo-21,22,62,63,87,88-hexathia-3,6,9,12,15,18,25,28,31,34,37,40,43,46,49,52,55,58,67,70,73,76,79,82,85,90-hexacosazatricyclo[43.40.4.219,60]hennonacontan-65-yl]amino]butanoic acid	1525389: Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay	ic50	0.1200	uM
4-(3-methoxyphenyl)-6-(1,3,4,5-tetrahydro-2-benzazepin-2-yl)pyrimidin-2-amine	2120760: Inhibition of human Nav1.2 expressed in HEK293 cells at -40 mv holding potential measured after 5 mins by whole cell voltage clamp electrophysiological analysis	ic50	0.1200	uM
5-(4-chlorophenyl)-N-[(2-morpholin-4-ylphenyl)methyl]pyridine-3-carboxamide	527217: Inhibition of human NaV1.2 by electrophysiology	ic50	0.1200	uM
4-[[2-[[tert-butyl(methyl)amino]methyl]-6-fluorophenyl]methylamino]-2,6-difluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide	1616312: Inhibition of recombinant human full length Nav1.2 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential by whole cell patch clamp assay	ic50	0.1250	uM
N-cyclopropylsulfonyl-1-[(3R)-1-[(1R)-1-(3,5-dichlorophenyl)ethyl]pyrrolidin-3-yl]-6-fluoro-3-methylindazole-5-carboxamide	1525419: Binding affinity to human recombinant Nav1.2 by radioligand binding assay	kd	0.1400	uM
4-[4-chloro-2-(2-methylpyrazol-3-yl)phenoxy]-3-fluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide	1457691: Inhibition of human NaV1.2 expressed in HEK cells assessed as half inactivation potential at -120 mV holding potential by automated patch clamp method	ic50	0.1490	uM
2,6-ditert-butyl-4-[[3-(2,6-dimethylphenoxy)propylamino]methyl]phenol	2120835: Inhibition of Nav1.2 (unknown origin)	ic50	0.1800	uM
2,5-bis[3-(trifluoromethyl)phenyl]-1H-imidazole	351546: Inhibition of human Nav1.2 channel expressed in HEK cells by patch-clamp electrophysiology method	ic50	0.2000	uM
2,2-diphenyl-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]acetamide	1246060: Inhibition of human NaV1.2 channel by patch clamp electrophysiology assay	ic50	0.2400	uM
Loperamide	205267: Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex	ic50	0.2700	uM
4-[4-chloro-2-(2-methylpyrazol-3-yl)phenoxy]-3-cyano-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide	1457691: Inhibition of human NaV1.2 expressed in HEK cells assessed as half inactivation potential at -120 mV holding potential by automated patch clamp method	ic50	0.2760	uM
4-[4-[4-chloro-3-(trifluoromethyl)phenyl]-4-hydroxypiperidin-1-yl]-N,N-dimethyl-2,2-diphenylbutanamide	205267: Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex	ic50	0.2800	uM
3,3-diphenyl-N-(1-phenylpropan-2-yl)propan-1-amine	205267: Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex	ic50	0.3000	uM
[5-(4-chlorophenyl)furan-2-yl]-(4-cyclohexylpiperazin-1-yl)methanone	404535: Inhibition of human recombinant Nav1.2 channel expressed in HEK293 cells by whole cell voltage clamp technique	ic50	0.3500	uM
N-(3,5-dimethylphenyl)-6-(4-ethoxyphenyl)pyrazine-2-carboxamide	536195: Inhibition of human recombinant NaV1.2 by electrophysiology	ic50	0.3600	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
mercuric bromide	increases expression, affects cotreatment	2
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression	2
Ascorbic Acid	affects cotreatment, increases expression, affects binding	2
Benzo(a)pyrene	increases expression, increases methylation	2
Phenylmercuric Acetate	affects cotreatment, increases expression	2
Tretinoin	affects binding, increases reaction, affects reaction, affects cotreatment, increases expression	2
Valproic Acid	increases expression	2
ascorbate-2-phosphate	affects binding, affects cotreatment, increases expression	1
tris(2-butoxyethyl) phosphate	affects expression	1
decamethrin	decreases expression, decreases reaction	1
sodium arsenite	affects methylation	1
beta-methylcholine	affects expression	1
1,2-bis(2-aminophenoxy)ethane N,N,N’,N’-tetraacetic acid acetoxymethyl ester	decreases expression, decreases reaction	1
4-methoxycinnamate methyl ester	increases expression, increases reaction	1
CGP 52608	affects binding, increases reaction	1
PD 150606	decreases expression, decreases reaction	1
1-hydroxy-2-oxo-3,3-bis(2-aminoethyl)-1-triazene	affects cotreatment, increases expression	1
pinostrobin	increases phosphorylation	1
Chir 99021	increases expression, affects binding, affects cotreatment	1
Grape Seed Proanthocyanidins	decreases expression, affects cotreatment	1
dorsomorphin	affects cotreatment, increases expression	1
jinfukang	affects cotreatment, increases expression	1
XAV939	affects binding, affects cotreatment, increases expression	1
LDN 193189	affects cotreatment, increases expression	1
(+)-JQ1 compound	decreases expression	1
Temozolomide	decreases expression	1
Lamotrigine	decreases activity	1
Arsenic Trioxide	increases expression	1
Cyclic AMP	affects cotreatment, increases expression	1
Atrazine	decreases expression	1

ChEMBL screening assays

203 unique, capped per target: 172 binding, 20 functional, 10 admet, 1 toxicity

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL679768	Binding	Inhibition of [3H]BTX binding to guinea pig voltage-dependent sodium channel	Anticonvulsant activity of piperidinol and (dialkylamino)alkanol esters. — *J Med Chem*
CHEMBL749469	Functional	Antagonism of batrachotoxin-mediated sodium ion uptake into cultured neuroblastoma cells	Batrachotoxin binding site antagonists — *Bioorg Med Chem Lett*
CHEMBL3883160	ADMET	Inhibition of human Nav1.2 expressed in CHO cells assessed as reduction in peak frequency currents by whole-cell voltage-clamp method	Fused heterocyclic compounds as ion channel modulators

Cellosaurus cell lines

7 cell lines: 5 induced pluripotent stem cell, 2 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_C0Y9	B’SYS CHO Nav1.2	Spontaneously immortalized cell line	Female
CVCL_C8H7	FINi001-A	Induced pluripotent stem cell	Female
CVCL_C8SP	FINi003-A	Induced pluripotent stem cell	Male
CVCL_E4Q2	KOLF2.1J SCN2A 94.3kbdel DEL/DEL	Induced pluripotent stem cell	Male
CVCL_LC66	PrecisION hNav1.2-CHO	Spontaneously immortalized cell line	Female
CVCL_VE79	PFIZi031-A	Induced pluripotent stem cell	Male
CVCL_WN05	CBTCi008-A	Induced pluripotent stem cell	Female

Clinical trials (associated diseases)

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

showing 60 of 506 trials:

NCT	Phase	Status	Title
NCT05657860	Phase 4	COMPLETED	Guanfacine Extended Release for the Reduction of Aggression and Self-injurious Behavior Associated With Prader-Willi Syndrome
NCT05744479	Phase 4	RECRUITING	Metformin for Antipsychotic-induced Weight Gain in Adults With Intellectual Disability
NCT06107829	Phase 4	WITHDRAWN	Valbenazine Treatment of Tardive Dyskinesia in Adults With Intellectual/Developmental Disabilities
NCT06997198	Phase 4	RECRUITING	Deutetrabenazine Treatment for Tardive Dyskinesia in Intellectual/Developmental Disabilities
NCT04586348	Phase 4	UNKNOWN	Prenatal Iodine Supplementation and Early Childhood Neurodevelopment
NCT04873115	Phase 4	UNKNOWN	Double-blind, Placebo-controlled, Randomized Clinical Trial Comparing the Efficacy and Safety of Sialanar Plus orAl rehabiLitation Against Placebo Plus Oral Rehabilitation for chIldren and Adolescents With seVere Sialorrhoea and Neurodisabilties,
NCT00004637	Phase 4	COMPLETED	Double-Blind, Placebo-Controlled Trial of Vitamin E as Add-on Therapy for Children With Epilepsy
NCT00043914	Phase 4	COMPLETED	Measurement Of Serum Levels Of Two Antiepileptic Drugs During Conversion In Patients With Epilepsy
NCT00132223	Phase 4	UNKNOWN	Effects on the Diagnostic Accuracy of Magnetic Imaging Angiographies of the Supra-Aortic Vessels by Three Different Magnetic Resonance Contrast Agents in Patients
NCT00133081	Phase 4	UNKNOWN	Study to Improve the Treatment of Epilepsy (SITE)
NCT00137709	Phase 4	UNKNOWN	Hormone Profiles in Adults With Newly Diagnosed Epilepsy
NCT00154076	Phase 4	COMPLETED	A Multicenter Comparative Trial of Zonisamide and Topiramate as Initial Monotherapy in Untreated Epilepsies
NCT00165828	Phase 4	TERMINATED	Efficacy and Safety of an add-on Treatment With Zonisamide in Adults With Focal Epileptic Seizures With or Without Secondary Generalization
NCT00181116	Phase 4	COMPLETED	Levetiracetam for Benign Rolandic Epilepsy
NCT00207935	Phase 4	COMPLETED	Use of Sustained Release Antiepileptic Medication (Depakote® ER) for Pediatric Epilepsy in a Mental Retardation/Developmental Disorder Population
NCT00215592	Phase 4	COMPLETED	Open Label, Zonegran (Zonisamide) In Partial Onset Seizures
NCT00266604	Phase 4	COMPLETED	A Study to Evaluate the Dosing, Effectiveness and Safety of Topiramate for the Treatment of Epilepsy
NCT00288639	Phase 4	COMPLETED	Lyrica (Pregabalin) Administered as an Add-on Therapy for Partial Seizures (LEADER).
NCT00312676	Phase 4	UNKNOWN	Compare Tolerability of an Overnight Switch to Gradual Switch Between Two Different Forms of Depakote
NCT00323947	Phase 4	COMPLETED	Methylphenidate for Treating Attention Deficit Hyperactivity Disorder in Children With Both ADHD and Epilepsy
NCT00385411	Phase 4	COMPLETED	Study of Valproate in Young Patients Suffering From Epilepsy
NCT00522418	Phase 4	TERMINATED	Study Comparing Best Medical Practice With or Without VNS Therapy in Pharmacoresistant Partial Epilepsy Patients
NCT00537940	Phase 4	COMPLETED	Comparative Study Of Pregabalin And Gabapentin As Adjunctive Therapy In Subjects With Partial Seizures
NCT00552526	Phase 4	UNKNOWN	Ketogenic Diet vs.Antiepileptic Drug Treatment in Drug Resistant Epilepsy
NCT00564915	Phase 4	COMPLETED	RCT of the Efficacy of the Ketogenic Diet in the Treatment of Epilepsy
NCT00571155	Phase 4	COMPLETED	Trial of Levetiracetam in Patients With Primary Brain Tumors and Symptomatic Seizures Who Undergo Surgery
NCT00572195	Phase 4	COMPLETED	RNS® System LTT Study
NCT00610532	Phase 4	TERMINATED	Evaluating the Transporter Protein Inhibitor Probenecid In Patients With Epilepsy
NCT00630357	Phase 4	COMPLETED	Trial to Evaluate the Safety and Efficacy of Keppra After Conversion to Mono-therapy in Subjects With Partial Epilepsy
NCT00630630	Phase 4	COMPLETED	Study on Safety and Efficacy of Levetiracetam in the Adjunctive Treatment of Female Subjects With C1 Catamenial Epilepsy
NCT00630968	Phase 4	COMPLETED	S.K.A.T.E.: Safety of Keppra as Adjunctive Therapy in Epilepsy
NCT00631150	Phase 4	COMPLETED	A Phase IV-Pharmacovigilance Study of Keppra Greece - S.K.A.T.E.: Safety of Keppra as Adjunctive Therapy in Epilepsy
NCT00659958	Phase 4	COMPLETED	ZAGAL Study: Evaluating Effectiveness and Tolerability of Zonisamide as Adjunctive Therapy in Patients With Partial Onset Seizures Treated With Two Antiepileptic Drugs
NCT00713622	Phase 4	COMPLETED	Comparing The Effect On Cognition Of Adjunctive Therapy With Zonisamide Versus Sodium Valproate
NCT00807989	Phase 4	COMPLETED	The Efficacy and Safety of Low Dose Combination of LTG and VPA Compared to CBZ Monotherapy
NCT00832884	Phase 4	COMPLETED	The Safety of Intravenous Lacosamide
NCT00869622	Phase 4	COMPLETED	Antiepileptic Drugs and Osteoporotic Prevention Trial
NCT00896987	Phase 4	COMPLETED	Lamotrigine Cognitive Function Study in Adult Untreated Epilepsies
NCT00952081	Phase 4	COMPLETED	A Pilot Study to Evaluate Efficacy and Safety of Clevidipine in Neurosurgical Patients
NCT01118455	Phase 4	TERMINATED	Trial to Assess Vagus Nerve Stimulation Therapy vs. Anti-Epileptic Drug (AED) Treatment in Children With Refractory Seizures
NCT01127165	Phase 4	COMPLETED	Low and High Dose Zonisamide in Children as Monotherapy
NCT01127256	Phase 4	COMPLETED	Comparative Study of Zonisamide and Carbamazepine as an Initial Monotherapy: Efficacy and Safety Evaluation
NCT01140867	Phase 4	COMPLETED	Open-label, Multi-center Trial of Zonisamide as Adjunctive Therapy in Patients With Uncontrolled Partial Epilepsy
NCT01175954	Phase 4	COMPLETED	Cognitive and Behavioral Effects of Lacosamide
NCT01229735	Phase 4	COMPLETED	Levetiracetam Versus Topiramate as Adjunctive Therapy to Evaluate Efficacy and Safety in Subjects With Refractory Partial Onset Seizures
NCT01244724	Phase 4	TERMINATED	Lexapro for Major Depression in Patients With Epilepsy
NCT01309074	Phase 4	WITHDRAWN	Does Pregabalin Improve Symptoms of Anxiety in Patients With Epilepsy? A Comparison With Sertraline
NCT01318408	Phase 4	COMPLETED	Levetiracetam: The Anti-Convulsant of Choice for Elderly Patients With Dementia
NCT01498822	Phase 4	COMPLETED	Levetiracetam Versus Oxcarbazepine as Monotherapy to Evaluate Efficacy and Safety in Subjects With Newly or Recently Diagnosed Partial Epilepsy
NCT01546688	Phase 4	TERMINATED	A Study to Evaluate the Safety and Tolerability and Explore the Efficacy of Zonisamide as add-on Therapy in Elderly Patients With Refractory Partial Seizures
NCT01607346	Phase 4	TERMINATED	An Open Label Study to Evaluate the Effects of Ezogabine/Retigabine Added to Existing Anti-epileptic Drug(s) on Urinary Voiding Function in Subjects With Partial Onset Seizures
NCT01627860	Phase 4	COMPLETED	First Add-on vs. Mono-therapy Study of Topiramate in Neuro-Surgical Patients
NCT01689649	Phase 4	COMPLETED	A Study to Assess Tolerability and Efficacy of Topiramate Monotherapy in Recently Diagnosed Patients With Epilepsy
NCT01713777	Phase 4	COMPLETED	Equivalence Among Antiepileptic Drug Generic and Brand Products in People With Epilepsy: Chronic-Dose 4-Period Replicate Design
NCT01733394	Phase 4	COMPLETED	Equivalence Among Antiepileptic Drug Generic and Brand Products in People With Epilepsy: Single-Dose 6-Period Replicate Design (EQUIGEN Single-Dose Study)
NCT01804322	Phase 4	COMPLETED	Standardized Educational Plan for Epilepsy Patients With Comorbidities
NCT01932502	Phase 4	UNKNOWN	Evaluation of Onfi Conversion Therapy Replacing Clonazepam in Patients With Medically Refractory Epilepsy
NCT01995825	Phase 4	COMPLETED	Lamotrigine Bioequivalence
NCT02100644	Phase 4	COMPLETED	Valproate Dose Reduction and Its Clinical Evaluation by Introducing Lamotrigine in Japanese Women With Epilepsy - Single Arm, Multicenter, and Open-label Study
NCT02178995	Phase 4	COMPLETED	Methylphenidate Treatment of Attention Deficits in Epilepsy

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for SCN2A across ~30M SureChEMBL compounds — explore on Sugi Predict.