CACNG1

gene
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Summary

CACNG1 (calcium voltage-gated channel auxiliary subunit gamma 1, HGNC:1405) is a protein-coding gene on chromosome 17q24.2, encoding Voltage-dependent calcium channel gamma-1 subunit (Q06432). Regulatory subunit of the voltage-gated calcium channel that gives rise to L-type calcium currents in skeletal muscle.

Voltage-dependent calcium channels are composed of five subunits. The protein encoded by this gene represents one of these subunits, gamma, and is one of two known gamma subunit proteins. This particular gamma subunit is part of skeletal muscle 1,4-dihydropyridine-sensitive calcium channels and is an integral membrane protein that plays a role in excitation-contraction coupling. This gene is part of a functionally diverse eight-member protein subfamily of the PMP-22/EMP/MP20 family and is located in a cluster with two family members that function as transmembrane AMPA receptor regulatory proteins (TARPs).

Source: NCBI Gene 786 — RefSeq curated summary.

At a glance

  • GWAS associations: 2
  • Clinical variants (ClinVar): 46 total
  • Druggable target: yes — 2 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_000727

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:1405
Approved symbolCACNG1
Namecalcium voltage-gated channel auxiliary subunit gamma 1
Location17q24.2
Locus typegene with protein product
StatusApproved
Ensembl geneENSG00000108878
Ensembl biotypeprotein_coding
OMIM114209
Entrez786

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 2 protein_coding

ENST00000226021, ENST00000958687

RefSeq mRNA: 1 — MANE Select: NM_000727 NM_000727

CCDS: CCDS11668

Canonical transcript exons

ENST00000226021 — 4 exons

ExonStartEnd
ENSE000007427356705399667054070
ENSE000007427386705510367055240
ENSE000008371916704455467044889
ENSE000008371926705604567056797

Expression profiles

Bgee: expression breadth ubiquitous, 124 present calls, max score 98.26.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 2.1024 / max 685.4211, expressed in 85 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter IDTPM avgSamples expressed
1623251.642676
1623240.327053
1623260.052220
1623230.034719
1623270.031816
1623280.01414

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
gastrocnemiusUBERON:000138898.26gold quality
hindlimb stylopod muscleUBERON:000425297.78gold quality
triceps brachiiUBERON:000150996.35gold quality
muscle of legUBERON:000138396.01gold quality
muscle organUBERON:000163095.83gold quality
quadriceps femorisUBERON:000137795.60gold quality
vastus lateralisUBERON:000137995.56gold quality
skeletal muscle tissueUBERON:000113495.25gold quality
skeletal muscle tissue of rectus abdominisUBERON:000451195.20gold quality
skeletal muscle tissue of biceps brachiiUBERON:000450295.08gold quality
biceps brachiiUBERON:000150794.24gold quality
gluteal muscleUBERON:000200093.29gold quality
diaphragmUBERON:000110392.80gold quality
deltoidUBERON:000147692.71gold quality
tibialis anteriorUBERON:000138591.38silver quality
muscle tissueUBERON:000238587.54gold quality
tongue squamous epitheliumUBERON:000691975.71gold quality
hair follicleUBERON:000207373.13gold quality
body of tongueUBERON:001187670.49gold quality
olfactory bulbUBERON:000226470.24gold quality
type B pancreatic cellCL:000016970.18gold quality
oocyteCL:000002369.21gold quality
jejunumUBERON:000211568.80silver quality
orbitofrontal cortexUBERON:000416767.09gold quality
epithelial cell of pancreasCL:000008365.56gold quality
tongueUBERON:000172365.45gold quality
Brodmann (1909) area 46UBERON:000648365.07gold quality
cervix squamous epitheliumUBERON:000692265.06gold quality
nasal cavity epitheliumUBERON:000538464.91gold quality
cartilage tissueUBERON:000241864.04gold quality

Single-cell (SCXA)

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

ExperimentMarker?Max mean expression
E-ANND-3yes3.55

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

21 targeting CACNG1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-4725-3P99.9669.532520
HSA-MIR-6780B-5P99.9669.602562
HSA-MIR-6768-5P99.9267.361942
HSA-MIR-6783-3P99.8967.922059
HSA-MIR-427199.8868.322244
HSA-MIR-498-5P99.7669.641807
HSA-MIR-6764-5P99.7567.892304
HSA-MIR-447099.6669.351767
HSA-MIR-1915-3P99.5866.791988
HSA-MIR-671-5P99.5267.111277
HSA-MIR-486-3P99.5166.821901
HSA-MIR-448999.5065.56785
HSA-MIR-5580-5P99.3866.961139
HSA-MIR-6852-5P99.1766.692073
HSA-MIR-328-5P99.0864.651000
HSA-MIR-374A-3P98.8767.821531
HSA-MIR-6761-5P98.7168.031504
HSA-MIR-6885-5P98.7164.33902
HSA-MIR-3130-5P98.1466.00711
HSA-MIR-9851-5P97.5767.491067
HSA-MIR-4482-5P97.5365.68598

Cross-species orthologs

4 orthologs

OrganismSymbolGene ID
danio_reriocacng1aENSDARG00000008772
danio_reriocacng1bENSDARG00000052360
mus_musculusCacng1ENSMUSG00000020722
rattus_norvegicusCacng1ENSRNOG00000003245

Paralogs (1): CACNG6 (ENSG00000130433)

Protein

Protein identifiers

Voltage-dependent calcium channel gamma-1 subunitQ06432 (reviewed: Q06432)

Alternative names: Dihydropyridine-sensitive L-type, skeletal muscle calcium channel subunit gamma

All UniProt accessions (1): Q06432

UniProt curated annotations — full annotation on UniProt →

Function. Regulatory subunit of the voltage-gated calcium channel that gives rise to L-type calcium currents in skeletal muscle. Regulates channel inactivation kinetics.

Subunit / interactions. Component of a calcium channel complex consisting of a pore-forming alpha subunit (CACNA1S) and the ancillary subunits CACNB1 or CACNB2, CACNG1 and CACNA2D1. The channel complex contains alpha, beta, gamma and delta subunits in a 1:1:1:1 ratio, i.e. it contains either CACNB1 or CACNB2.

Subcellular location. Cell membrane. Sarcolemma.

Tissue specificity. Skeletal muscle.

Post-translational modifications. N-glycosylated.

Similarity. Belongs to the PMP-22/EMP/MP20 family. CACNG subfamily.

RefSeq proteins (1): NP_000718* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR004031PMP22/EMP/MP20/ClaudinFamily
IPR005421VDCC_g1suFamily
IPR008368VDCC_gsuFamily

Pfam: PF13903

UniProt features (14 total): topological domain 5, transmembrane region 4, glycosylation site 2, chain 1, disulfide bond 1, sequence variant 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q06432-F176.280.29

Functional residue map

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

Disulfide bonds (1): 57–80

Glycosylation sites (2): 43, 79

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 120 (showing top): KEGG_MAPK_SIGNALING_PATHWAY, MODULE_64, MODULE_329, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_POSITIVE_REGULATION_OF_MUSCLE_CONTRACTION, CAGCAGG_MIR370, GOBP_REGULATION_OF_MUSCLE_CONTRACTION, GOBP_MUSCLE_CONTRACTION, GOBP_REGULATION_OF_CALCIUM_ION_TRANSMEMBRANE_TRANSPORT, GOBP_SARCOPLASMIC_RETICULUM_CALCIUM_ION_TRANSPORT, GOBP_REGULATION_OF_SYSTEM_PROCESS, GOBP_MUSCLE_SYSTEM_PROCESS, MODULE_175, LEE_AGING_CEREBELLUM_DN, GOBP_REGULATION_OF_TRANSPORT

GO Biological Process (8): positive regulation of muscle contraction (GO:0045933), establishment of localization in cell (GO:0051649), sarcoplasmic reticulum calcium ion transport (GO:0070296), calcium ion transmembrane transport (GO:0070588), regulation of calcium ion transmembrane transport via high voltage-gated calcium channel (GO:1902514), monoatomic ion transport (GO:0006811), calcium ion transport (GO:0006816), monoatomic ion transmembrane transport (GO:0034220)

GO Molecular Function (4): voltage-gated calcium channel activity (GO:0005245), calcium channel regulator activity (GO:0005246), calcium channel activity (GO:0005262), protein binding (GO:0005515)

GO Cellular Component (7): plasma membrane (GO:0005886), T-tubule (GO:0030315), sarcolemma (GO:0042383), L-type voltage-gated calcium channel complex (GO:1990454), voltage-gated calcium channel complex (GO:0005891), membrane (GO:0016020), monoatomic ion channel complex (GO:0034702)

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
calcium ion transport2
calcium channel activity2
cellular anatomical structure2
muscle contraction1
regulation of muscle contraction1
positive regulation of multicellular organismal process1
establishment of localization1
cellular localization1
monoatomic cation transmembrane transport1
calcium ion transmembrane transport via high voltage-gated calcium channel1
regulation of calcium ion transmembrane transport1
transport1
metal ion transport1
monoatomic ion transport1
transmembrane transport1
voltage-gated monoatomic cation channel activity1
ion channel regulator activity1
monoatomic cation channel activity1
calcium ion transmembrane transporter activity1
binding1
membrane1
cell periphery1
sarcolemma1
plasma membrane1
voltage-gated calcium channel complex1
T-tubule1
calcium channel complex1
plasma membrane protein complex1
transmembrane transporter complex1

Protein interactions and networks

STRING

1044 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
CACNG1CACNB1Q02641971
CACNG1CACNG4Q9UBN1952
CACNG1CACNA2D1P54289939
CACNG1CACNA1DQ01668935
CACNG1CACNG7P62955917
CACNG1CACNG5Q9UF02916
CACNG1CACNG3O60359914
CACNG1CACNG8Q8WXS5891
CACNG1CACNG2Q9Y698871
CACNG1CACNA1SQ13698842
CACNG1CACNA2D2Q9NY47816
CACNG1CACNA2D3Q8IZS8713
CACNG1CACNA2D4Q7Z3S7699
CACNG1SCN4AP35499670
CACNG1CACNA1AP78510615

IntAct

53 interactions, top by confidence:

ABTypeScore
CACNG1psi-mi:“MI:0915”(physical association)0.560
CACNG1BIKpsi-mi:“MI:0915”(physical association)0.560
CACNG1REEP4psi-mi:“MI:0915”(physical association)0.560
CACNG1FNDC9psi-mi:“MI:0915”(physical association)0.560
CACNG1ERVFRD-1psi-mi:“MI:0915”(physical association)0.560
CACNG1HSD17B13psi-mi:“MI:0915”(physical association)0.560
CACNG1VAPApsi-mi:“MI:0915”(physical association)0.560
ERVFRD-1CACNG1psi-mi:“MI:0915”(physical association)0.560
MUC1CACNG1psi-mi:“MI:0915”(physical association)0.560
MGST3CACNG1psi-mi:“MI:0915”(physical association)0.560
CACNG1THAP4psi-mi:“MI:0915”(physical association)0.560
CACNG1CPLX4psi-mi:“MI:0915”(physical association)0.560
CACNG1GPX8psi-mi:“MI:0915”(physical association)0.560
CACNG1ODF4psi-mi:“MI:0915”(physical association)0.560
CACNG1TMEM45Bpsi-mi:“MI:0915”(physical association)0.560
CACNG1TLCD4psi-mi:“MI:0915”(physical association)0.560
GAD2CACNG1psi-mi:“MI:0915”(physical association)0.560
FFAR2CACNG1psi-mi:“MI:0915”(physical association)0.560
CACNG1TMEM120Bpsi-mi:“MI:0914”(association)0.350

BioGRID (43): VAPA (Two-hybrid), CACNG1 (Two-hybrid), CACNG1 (Synthetic Lethality), CACNG1 (Synthetic Lethality), CACNG1 (Two-hybrid), FFAR2 (Two-hybrid), GAD2 (Two-hybrid), MGST3 (Two-hybrid), TMEM45B (Two-hybrid), TMEM56 (Two-hybrid), GPX8 (Two-hybrid), CPLX4 (Two-hybrid), HSD17B13 (Two-hybrid), THAP4 (Two-hybrid), ODF4 (Two-hybrid)

ESM2 similar proteins: A0A1D5NY17, A4IF75, B2RVY9, B3SHH9, F6V1J6, O42281, O70578, P19518, P97707, Q06432, Q08CE6, Q08DE1, Q0D289, Q0V9E0, Q14714, Q2MJQ7, Q4R4Z3, Q4V922, Q5CZV0, Q5PRC1, Q5RDV7, Q5XGU1, Q62147, Q66IV3, Q68FV0, Q6AZD1, Q6P0C6, Q6R5J2, Q6ZP80, Q6ZUX7, Q7ZZL8, Q86WI0, Q8BGA2, Q8NBL3, Q8VHW3, Q8VHW4, Q8VHW7, Q8VHW8, Q91Y55, Q925N4

Diamond homologs: O70578, P19518, P97707, Q06432, Q08DE1, Q2MJQ7, Q8VHW3, Q8VHW7, Q9BXT2

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance40
Likely benign2
Benign0

Top pathogenic / likely-pathogenic (0)

SpliceAI

512 predictions. Top by Δscore:

VariantEffectΔscore
17:67044886:GGGG:Gdonor_gain1.0000
17:67044887:G:GTdonor_gain1.0000
17:67044887:GGG:Gdonor_gain1.0000
17:67044888:GG:Gdonor_gain1.0000
17:67044888:GGG:Gdonor_gain1.0000
17:67044889:GG:Gdonor_gain1.0000
17:67044890:G:GAdonor_loss1.0000
17:67053994:A:AGacceptor_gain1.0000
17:67053995:G:GGacceptor_gain1.0000
17:67053995:GA:Gacceptor_gain1.0000
17:67053995:GAGAA:Gacceptor_gain1.0000
17:67054066:GAAGG:Gdonor_gain1.0000
17:67054069:GG:Gdonor_gain1.0000
17:67054070:GG:Gdonor_gain1.0000
17:67056039:CCCCA:Cacceptor_loss1.0000
17:67056040:CCCAG:Cacceptor_loss1.0000
17:67056041:CCA:Cacceptor_loss1.0000
17:67056044:G:GCacceptor_loss1.0000
17:67044890:G:GGdonor_gain0.9900
17:67053990:TTGCA:Tacceptor_loss0.9900
17:67053991:TGCA:Tacceptor_loss0.9900
17:67053992:GCA:Gacceptor_loss0.9900
17:67053993:CA:Cacceptor_loss0.9900
17:67053993:CAG:Cacceptor_gain0.9900
17:67053994:A:ATacceptor_loss0.9900
17:67053994:AGA:Aacceptor_gain0.9900
17:67053995:GAG:Gacceptor_gain0.9900
17:67053995:GAGA:Gacceptor_gain0.9900
17:67054067:AAGGG:Adonor_loss0.9900
17:67054069:GGGTG:Gdonor_loss0.9900

AlphaMissense

1465 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
17:67054014:T:GF83C0.995
17:67055138:A:CS114R0.995
17:67055140:C:AS114R0.995
17:67055140:C:GS114R0.995
17:67044820:T:AW54R0.994
17:67044820:T:CW54R0.994
17:67044754:T:AW32R0.993
17:67044754:T:CW32R0.993
17:67044822:G:CW54C0.993
17:67044822:G:TW54C0.993
17:67055240:G:CG148R0.993
17:67056050:T:CC150R0.992
17:67044824:G:CR55P0.991
17:67054013:T:CF83L0.991
17:67054015:C:AF83L0.991
17:67054015:C:GF83L0.991
17:67055159:G:CG121R0.991
17:67044715:G:CG19R0.990
17:67044815:G:AG52D0.990
17:67054004:T:AC80S0.990
17:67054005:G:CC80S0.990
17:67044756:G:CW32C0.989
17:67044756:G:TW32C0.989
17:67044829:T:AC57S0.989
17:67044830:G:AC57Y0.989
17:67044830:G:CC57S0.989
17:67055108:A:CS104R0.989
17:67055110:C:AS104R0.989
17:67055110:C:GS104R0.989
17:67044814:G:CG52R0.988

dbSNP variants (sampled 300 via entrez): RS1000348210 (17:67054376 C>T), RS1000676404 (17:67049264 C>T), RS1000944843 (17:67044208 C>T), RS1000956594 (17:67055331 G>A,C,T), RS1001113253 (17:67049921 T>G), RS1001250993 (17:67056350 C>A,T), RS1001664931 (17:67050785 C>A), RS1001780903 (17:67051067 G>A), RS1001826344 (17:67051517 T>C), RS1001981837 (17:67045044 T>C), RS1002248382 (17:67046643 A>G), RS1002465428 (17:67045832 C>G,T), RS1003360737 (17:67053690 G>A), RS1003379060 (17:67054267 G>A), RS1003468908 (17:67047099 T>C)

Disease associations

OMIM: gene MIM:114209 | disease phenotypes: MIM:145600

GenCC curated gene-disease

Mondo (1): malignant hyperthermia, susceptibility to, 1 (MONDO:0007783)

Orphanet (1): Malignant hyperthermia of anesthesia (Orphanet:423)

HPO phenotypes

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

GWAS associations

2 associations (top):

StudyTraitp-value
GCST009723_92Vertical cup-disc ratio (adjusted for vertical disc diameter)1.000000e-07
GCST009724_72Vertical cup-disc ratio (multi-trait analysis)7.000000e-09

EFO canonical traits (1, from GWAS)

EFO IDTrait name
EFO:0006939cup-to-disc ratio measurement

MeSH disease descriptors (1)

DescriptorNameTree numbers
C535694Malignant hyperthermia susceptibility type 1 (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2363032 (PROTEIN COMPLEX GROUP)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 67,947 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL1428NIMODIPINE432,587
CHEMBL95TACRINE435,360

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

Binding affinities (BindingDB)

2 measured of 2 human assays (6 total across all organisms); most potent 2 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValue
SR 147778KI1000 nM
3,5-diamino-6-chloro-N-(diaminomethylene)pyrazinamide;hydrochlorideIC506630 nM

ChEMBL bioactivities

58 potent at pChembl≥5 of 75 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
8.82IC501.5nMCHEMBL3891844
8.72IC501.9nMCHEMBL3890624
8.62IC502.4nMCHEMBL3973392
8.57IC502.7nMCHEMBL3891844
8.52IC503nMCHEMBL3919024
8.51IC503.1nMCHEMBL3919898
8.35IC504.5nMCHEMBL3965812
8.23IC505.9nMCHEMBL3906126
8.22IC506nMCHEMBL3890916
8.15IC507nMCHEMBL3940577
8.14IC507.2nMCHEMBL3969562
8.12IC507.6nMCHEMBL3937280
8.12IC507.6nMCHEMBL3965812
8.10IC508nMCHEMBL3983323
8.05IC509nMCHEMBL3942512
8.03IC509.4nMCHEMBL3922498
8.01IC509.7nMCHEMBL3897303
7.96IC5011nMCHEMBL3948329
7.92IC5012nMCHEMBL3898359
7.85IC5014nMCHEMBL3911369
7.85IC5014nMCHEMBL3913505
7.85IC5014nMCHEMBL3936725
7.82IC5015nMCHEMBL3984596
7.82IC5015nMCHEMBL3902376
7.67IC5021.5nMCHEMBL3952905
7.62IC5024nMCHEMBL3972896
7.58IC5026nMCHEMBL3889804
7.55IC5028nMCHEMBL3958844
7.55IC5028nMCHEMBL3973382
7.52IC5030nMCHEMBL3978200
7.52IC5030nMCHEMBL3985660
7.51IC5031nMCHEMBL3896861
7.51IC5031nMCHEMBL3951956
7.50IC5031.4nMCHEMBL3962403
7.44IC5036nMCHEMBL3953976
7.44IC5036nMCHEMBL3925140
7.41IC5039nMCHEMBL3900691
7.39IC5041nMCHEMBL3930781
7.30IC5050nMCHEMBL3921840
7.21IC5062nMCHEMBL3956991
7.17IC5067nMCHEMBL3965293
7.09IC5081nMCHEMBL3958264
7.07IC5085nMCHEMBL3964411
7.01IC5098.5nMCHEMBL3953031
6.40IC50400nMCHEMBL3974355
6.10IC50800nMCHEMBL3734797
5.75IC501800nMCHEMBL4228929
5.66IC502200nMCHEMBL4226021
5.52IC503000nMCHEMBL4228209
5.52IC503000nMCHEMBL4224773

PubChem BioAssay actives

13 with measured affinity, of 101 total; 13 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
N-tert-butyl-8-[[[(1S,2S)-2-(3-methyl-1,2,4-oxadiazol-5-yl)cyclopropanecarbonyl]amino]methyl]-5-[3-(trifluoromethoxy)phenyl]-3,4-dihydro-1H-isoquinoline-2-carboxamide1262825: Inhibition of voltage-gated calcium channel (unknown origin)ic500.8000uM
5-methyl-1-[(2-nitrophenyl)methyl]-3-(piperidin-1-ylmethyl)indole1392176: Inhibition of KCl-induced cytosolic voltage gated calcium channel opening in human SH-SY5Y cells by Fluo-4 AM dye based fluorescence assayic501.8000uM
1-[(3-chlorophenyl)methyl]-5-methyl-3-(piperidin-1-ylmethyl)indole1392176: Inhibition of KCl-induced cytosolic voltage gated calcium channel opening in human SH-SY5Y cells by Fluo-4 AM dye based fluorescence assayic502.2000uM
5-methyl-1-[(3-nitrophenyl)methyl]-3-(piperidin-1-ylmethyl)indole1392176: Inhibition of KCl-induced cytosolic voltage gated calcium channel opening in human SH-SY5Y cells by Fluo-4 AM dye based fluorescence assayic503.0000uM
1-[(4-chlorophenyl)methyl]-5-methyl-3-(piperidin-1-ylmethyl)indole1392176: Inhibition of KCl-induced cytosolic voltage gated calcium channel opening in human SH-SY5Y cells by Fluo-4 AM dye based fluorescence assayic503.0000uM
1-benzyl-5-methyl-3-(piperidin-1-ylmethyl)indole1392176: Inhibition of KCl-induced cytosolic voltage gated calcium channel opening in human SH-SY5Y cells by Fluo-4 AM dye based fluorescence assayic503.4000uM
5-methyl-1-[(4-methylphenyl)methyl]-3-(piperidin-1-ylmethyl)indole1392176: Inhibition of KCl-induced cytosolic voltage gated calcium channel opening in human SH-SY5Y cells by Fluo-4 AM dye based fluorescence assayic503.6000uM
1-[(4-fluorophenyl)methyl]-5-methyl-3-(piperidin-1-ylmethyl)indole1392176: Inhibition of KCl-induced cytosolic voltage gated calcium channel opening in human SH-SY5Y cells by Fluo-4 AM dye based fluorescence assayic504.8000uM
N-heptyl-16,18-dioxo-17-azapentacyclo[6.6.5.02,7.09,14.015,19]nonadeca-2,4,6,9,11,13-hexaene-1-carboxamide1612587: Inhibition of K+-induced voltage gated calcium channel opening in human SH-SY5Y cells assessed as decrease in Ca2+ level after 10 mins by Fluo-4 dye-based fluorescence assayic509.0000uM
ethyl 5-amino-4-(3-methoxyphenyl)-2-methyl-7,8,9,10-tetrahydro-6H-cyclohepta[b][1,8]naphthyridine-3-carboxylate1653244: Inhibition of VGCC (unknown origin)ic509.0000uM
ethyl 5-amino-4-(3,4-dimethoxyphenyl)-2-methyl-7,8,9,10-tetrahydro-6H-cyclohepta[b][1,8]naphthyridine-3-carboxylate1653244: Inhibition of VGCC (unknown origin)ic509.0000uM
propan-2-yl 5-amino-2-methyl-4-phenyl-6,7,8,9-tetrahydrobenzo[b][1,8]naphthyridine-3-carboxylate1653244: Inhibition of VGCC (unknown origin)ic5010.0000uM
ethyl 5-amino-2-methyl-4-phenyl-6,7,8,9,10,11-hexahydrocycloocta[b][1,8]naphthyridine-3-carboxylate1653244: Inhibition of VGCC (unknown origin)ic5010.0000uM

CTD chemical–gene interactions

11 total (human), top 11 by PubMed support.

ChemicalActions (top 5)PubMed papers
aristolochic acid Iincreases expression1
incobotulinumtoxinAdecreases expression1
Resveratrolaffects cotreatment, decreases expression1
Aspirindecreases expression1
Benzo(a)pyreneaffects methylation1
Niclosamideincreases expression1
Plant Extractsaffects cotreatment, decreases expression1
Rotenoneincreases expression1
Tobacco Smoke Pollutiondecreases expression1
Tretinoinincreases expression1
Aflatoxin B1increases methylation1

ChEMBL screening assays

13 unique, capped per target: 13 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL3737861BindingInhibition of voltage-gated calcium channel (unknown origin)Discovery and Pharmacology of a Novel Class of Diacylglycerol Acyltransferase 2 Inhibitors. — J Med Chem

Cellosaurus cell lines

1 cell lines: 1 transformed cell line

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

CellosaurusNameCategorySex
CVCL_YA28IDG-HEK293T-CACNG1-V5-OETransformed cell lineFemale

Clinical trials (associated diseases)

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