CACNG1
gene geneOn this page
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
| Field | Value |
|---|---|
| HGNC ID | HGNC:1405 |
| Approved symbol | CACNG1 |
| Name | calcium voltage-gated channel auxiliary subunit gamma 1 |
| Location | 17q24.2 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000108878 |
| Ensembl biotype | protein_coding |
| OMIM | 114209 |
| Entrez | 786 |
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
| Exon | Start | End |
|---|---|---|
| ENSE00000742735 | 67053996 | 67054070 |
| ENSE00000742738 | 67055103 | 67055240 |
| ENSE00000837191 | 67044554 | 67044889 |
| ENSE00000837192 | 67056045 | 67056797 |
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 ID | TPM avg | Samples expressed |
|---|---|---|
| 162325 | 1.6426 | 76 |
| 162324 | 0.3270 | 53 |
| 162326 | 0.0522 | 20 |
| 162323 | 0.0347 | 19 |
| 162327 | 0.0318 | 16 |
| 162328 | 0.0141 | 4 |
Top tissues by expression
273 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| gastrocnemius | UBERON:0001388 | 98.26 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 97.78 | gold quality |
| triceps brachii | UBERON:0001509 | 96.35 | gold quality |
| muscle of leg | UBERON:0001383 | 96.01 | gold quality |
| muscle organ | UBERON:0001630 | 95.83 | gold quality |
| quadriceps femoris | UBERON:0001377 | 95.60 | gold quality |
| vastus lateralis | UBERON:0001379 | 95.56 | gold quality |
| skeletal muscle tissue | UBERON:0001134 | 95.25 | gold quality |
| skeletal muscle tissue of rectus abdominis | UBERON:0004511 | 95.20 | gold quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 95.08 | gold quality |
| biceps brachii | UBERON:0001507 | 94.24 | gold quality |
| gluteal muscle | UBERON:0002000 | 93.29 | gold quality |
| diaphragm | UBERON:0001103 | 92.80 | gold quality |
| deltoid | UBERON:0001476 | 92.71 | gold quality |
| tibialis anterior | UBERON:0001385 | 91.38 | silver quality |
| muscle tissue | UBERON:0002385 | 87.54 | gold quality |
| tongue squamous epithelium | UBERON:0006919 | 75.71 | gold quality |
| hair follicle | UBERON:0002073 | 73.13 | gold quality |
| body of tongue | UBERON:0011876 | 70.49 | gold quality |
| olfactory bulb | UBERON:0002264 | 70.24 | gold quality |
| type B pancreatic cell | CL:0000169 | 70.18 | gold quality |
| oocyte | CL:0000023 | 69.21 | gold quality |
| jejunum | UBERON:0002115 | 68.80 | silver quality |
| orbitofrontal cortex | UBERON:0004167 | 67.09 | gold quality |
| epithelial cell of pancreas | CL:0000083 | 65.56 | gold quality |
| tongue | UBERON:0001723 | 65.45 | gold quality |
| Brodmann (1909) area 46 | UBERON:0006483 | 65.07 | gold quality |
| cervix squamous epithelium | UBERON:0006922 | 65.06 | gold quality |
| nasal cavity epithelium | UBERON:0005384 | 64.91 | gold quality |
| cartilage tissue | UBERON:0002418 | 64.04 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 3.55 |
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):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-4725-3P | 99.96 | 69.53 | 2520 |
| HSA-MIR-6780B-5P | 99.96 | 69.60 | 2562 |
| HSA-MIR-6768-5P | 99.92 | 67.36 | 1942 |
| HSA-MIR-6783-3P | 99.89 | 67.92 | 2059 |
| HSA-MIR-4271 | 99.88 | 68.32 | 2244 |
| HSA-MIR-498-5P | 99.76 | 69.64 | 1807 |
| HSA-MIR-6764-5P | 99.75 | 67.89 | 2304 |
| HSA-MIR-4470 | 99.66 | 69.35 | 1767 |
| HSA-MIR-1915-3P | 99.58 | 66.79 | 1988 |
| HSA-MIR-671-5P | 99.52 | 67.11 | 1277 |
| HSA-MIR-486-3P | 99.51 | 66.82 | 1901 |
| HSA-MIR-4489 | 99.50 | 65.56 | 785 |
| HSA-MIR-5580-5P | 99.38 | 66.96 | 1139 |
| HSA-MIR-6852-5P | 99.17 | 66.69 | 2073 |
| HSA-MIR-328-5P | 99.08 | 64.65 | 1000 |
| HSA-MIR-374A-3P | 98.87 | 67.82 | 1531 |
| HSA-MIR-6761-5P | 98.71 | 68.03 | 1504 |
| HSA-MIR-6885-5P | 98.71 | 64.33 | 902 |
| HSA-MIR-3130-5P | 98.14 | 66.00 | 711 |
| HSA-MIR-9851-5P | 97.57 | 67.49 | 1067 |
| HSA-MIR-4482-5P | 97.53 | 65.68 | 598 |
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | cacng1a | ENSDARG00000008772 |
| danio_rerio | cacng1b | ENSDARG00000052360 |
| mus_musculus | Cacng1 | ENSMUSG00000020722 |
| rattus_norvegicus | Cacng1 | ENSRNOG00000003245 |
Paralogs (1): CACNG6 (ENSG00000130433)
Protein
Protein identifiers
Voltage-dependent calcium channel gamma-1 subunit — Q06432 (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)
| ID | Name | Type |
|---|---|---|
| IPR004031 | PMP22/EMP/MP20/Claudin | Family |
| IPR005421 | VDCC_g1su | Family |
| IPR008368 | VDCC_gsu | Family |
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)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q06432-F1 | 76.28 | 0.29 |
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:
| Category | Terms |
|---|---|
| calcium ion transport | 2 |
| calcium channel activity | 2 |
| cellular anatomical structure | 2 |
| muscle contraction | 1 |
| regulation of muscle contraction | 1 |
| positive regulation of multicellular organismal process | 1 |
| establishment of localization | 1 |
| cellular localization | 1 |
| monoatomic cation transmembrane transport | 1 |
| calcium ion transmembrane transport via high voltage-gated calcium channel | 1 |
| regulation of calcium ion transmembrane transport | 1 |
| transport | 1 |
| metal ion transport | 1 |
| monoatomic ion transport | 1 |
| transmembrane transport | 1 |
| voltage-gated monoatomic cation channel activity | 1 |
| ion channel regulator activity | 1 |
| monoatomic cation channel activity | 1 |
| calcium ion transmembrane transporter activity | 1 |
| binding | 1 |
| membrane | 1 |
| cell periphery | 1 |
| sarcolemma | 1 |
| plasma membrane | 1 |
| voltage-gated calcium channel complex | 1 |
| T-tubule | 1 |
| calcium channel complex | 1 |
| plasma membrane protein complex | 1 |
| transmembrane transporter complex | 1 |
Protein interactions and networks
STRING
1044 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CACNG1 | CACNB1 | Q02641 | 971 |
| CACNG1 | CACNG4 | Q9UBN1 | 952 |
| CACNG1 | CACNA2D1 | P54289 | 939 |
| CACNG1 | CACNA1D | Q01668 | 935 |
| CACNG1 | CACNG7 | P62955 | 917 |
| CACNG1 | CACNG5 | Q9UF02 | 916 |
| CACNG1 | CACNG3 | O60359 | 914 |
| CACNG1 | CACNG8 | Q8WXS5 | 891 |
| CACNG1 | CACNG2 | Q9Y698 | 871 |
| CACNG1 | CACNA1S | Q13698 | 842 |
| CACNG1 | CACNA2D2 | Q9NY47 | 816 |
| CACNG1 | CACNA2D3 | Q8IZS8 | 713 |
| CACNG1 | CACNA2D4 | Q7Z3S7 | 699 |
| CACNG1 | SCN4A | P35499 | 670 |
| CACNG1 | CACNA1A | P78510 | 615 |
IntAct
53 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CACNG1 | psi-mi:“MI:0915”(physical association) | 0.560 | |
| CACNG1 | BIK | psi-mi:“MI:0915”(physical association) | 0.560 |
| CACNG1 | REEP4 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CACNG1 | FNDC9 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CACNG1 | ERVFRD-1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CACNG1 | HSD17B13 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CACNG1 | VAPA | psi-mi:“MI:0915”(physical association) | 0.560 |
| ERVFRD-1 | CACNG1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| MUC1 | CACNG1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| MGST3 | CACNG1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CACNG1 | THAP4 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CACNG1 | CPLX4 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CACNG1 | GPX8 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CACNG1 | ODF4 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CACNG1 | TMEM45B | psi-mi:“MI:0915”(physical association) | 0.560 |
| CACNG1 | TLCD4 | psi-mi:“MI:0915”(physical association) | 0.560 |
| GAD2 | CACNG1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| FFAR2 | CACNG1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CACNG1 | TMEM120B | psi-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):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 40 |
| Likely benign | 2 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
512 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 17:67044886:GGGG:G | donor_gain | 1.0000 |
| 17:67044887:G:GT | donor_gain | 1.0000 |
| 17:67044887:GGG:G | donor_gain | 1.0000 |
| 17:67044888:GG:G | donor_gain | 1.0000 |
| 17:67044888:GGG:G | donor_gain | 1.0000 |
| 17:67044889:GG:G | donor_gain | 1.0000 |
| 17:67044890:G:GA | donor_loss | 1.0000 |
| 17:67053994:A:AG | acceptor_gain | 1.0000 |
| 17:67053995:G:GG | acceptor_gain | 1.0000 |
| 17:67053995:GA:G | acceptor_gain | 1.0000 |
| 17:67053995:GAGAA:G | acceptor_gain | 1.0000 |
| 17:67054066:GAAGG:G | donor_gain | 1.0000 |
| 17:67054069:GG:G | donor_gain | 1.0000 |
| 17:67054070:GG:G | donor_gain | 1.0000 |
| 17:67056039:CCCCA:C | acceptor_loss | 1.0000 |
| 17:67056040:CCCAG:C | acceptor_loss | 1.0000 |
| 17:67056041:CCA:C | acceptor_loss | 1.0000 |
| 17:67056044:G:GC | acceptor_loss | 1.0000 |
| 17:67044890:G:GG | donor_gain | 0.9900 |
| 17:67053990:TTGCA:T | acceptor_loss | 0.9900 |
| 17:67053991:TGCA:T | acceptor_loss | 0.9900 |
| 17:67053992:GCA:G | acceptor_loss | 0.9900 |
| 17:67053993:CA:C | acceptor_loss | 0.9900 |
| 17:67053993:CAG:C | acceptor_gain | 0.9900 |
| 17:67053994:A:AT | acceptor_loss | 0.9900 |
| 17:67053994:AGA:A | acceptor_gain | 0.9900 |
| 17:67053995:GAG:G | acceptor_gain | 0.9900 |
| 17:67053995:GAGA:G | acceptor_gain | 0.9900 |
| 17:67054067:AAGGG:A | donor_loss | 0.9900 |
| 17:67054069:GGGTG:G | donor_loss | 0.9900 |
AlphaMissense
1465 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 17:67054014:T:G | F83C | 0.995 |
| 17:67055138:A:C | S114R | 0.995 |
| 17:67055140:C:A | S114R | 0.995 |
| 17:67055140:C:G | S114R | 0.995 |
| 17:67044820:T:A | W54R | 0.994 |
| 17:67044820:T:C | W54R | 0.994 |
| 17:67044754:T:A | W32R | 0.993 |
| 17:67044754:T:C | W32R | 0.993 |
| 17:67044822:G:C | W54C | 0.993 |
| 17:67044822:G:T | W54C | 0.993 |
| 17:67055240:G:C | G148R | 0.993 |
| 17:67056050:T:C | C150R | 0.992 |
| 17:67044824:G:C | R55P | 0.991 |
| 17:67054013:T:C | F83L | 0.991 |
| 17:67054015:C:A | F83L | 0.991 |
| 17:67054015:C:G | F83L | 0.991 |
| 17:67055159:G:C | G121R | 0.991 |
| 17:67044715:G:C | G19R | 0.990 |
| 17:67044815:G:A | G52D | 0.990 |
| 17:67054004:T:A | C80S | 0.990 |
| 17:67054005:G:C | C80S | 0.990 |
| 17:67044756:G:C | W32C | 0.989 |
| 17:67044756:G:T | W32C | 0.989 |
| 17:67044829:T:A | C57S | 0.989 |
| 17:67044830:G:A | C57Y | 0.989 |
| 17:67044830:G:C | C57S | 0.989 |
| 17:67055108:A:C | S104R | 0.989 |
| 17:67055110:C:A | S104R | 0.989 |
| 17:67055110:C:G | S104R | 0.989 |
| 17:67044814:G:C | G52R | 0.988 |
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):
| Study | Trait | p-value |
|---|---|---|
| GCST009723_92 | Vertical cup-disc ratio (adjusted for vertical disc diameter) | 1.000000e-07 |
| GCST009724_72 | Vertical cup-disc ratio (multi-trait analysis) | 7.000000e-09 |
EFO canonical traits (1, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0006939 | cup-to-disc ratio measurement |
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| C535694 | Malignant 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).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL1428 | NIMODIPINE | 4 | 32,587 |
| CHEMBL95 | TACRINE | 4 | 35,360 |
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.
| Ligand | Measure | Value |
|---|---|---|
| SR 147778 | KI | 1000 nM |
| 3,5-diamino-6-chloro-N-(diaminomethylene)pyrazinamide;hydrochloride | IC50 | 6630 nM |
ChEMBL bioactivities
58 potent at pChembl≥5 of 75 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.82 | IC50 | 1.5 | nM | CHEMBL3891844 |
| 8.72 | IC50 | 1.9 | nM | CHEMBL3890624 |
| 8.62 | IC50 | 2.4 | nM | CHEMBL3973392 |
| 8.57 | IC50 | 2.7 | nM | CHEMBL3891844 |
| 8.52 | IC50 | 3 | nM | CHEMBL3919024 |
| 8.51 | IC50 | 3.1 | nM | CHEMBL3919898 |
| 8.35 | IC50 | 4.5 | nM | CHEMBL3965812 |
| 8.23 | IC50 | 5.9 | nM | CHEMBL3906126 |
| 8.22 | IC50 | 6 | nM | CHEMBL3890916 |
| 8.15 | IC50 | 7 | nM | CHEMBL3940577 |
| 8.14 | IC50 | 7.2 | nM | CHEMBL3969562 |
| 8.12 | IC50 | 7.6 | nM | CHEMBL3937280 |
| 8.12 | IC50 | 7.6 | nM | CHEMBL3965812 |
| 8.10 | IC50 | 8 | nM | CHEMBL3983323 |
| 8.05 | IC50 | 9 | nM | CHEMBL3942512 |
| 8.03 | IC50 | 9.4 | nM | CHEMBL3922498 |
| 8.01 | IC50 | 9.7 | nM | CHEMBL3897303 |
| 7.96 | IC50 | 11 | nM | CHEMBL3948329 |
| 7.92 | IC50 | 12 | nM | CHEMBL3898359 |
| 7.85 | IC50 | 14 | nM | CHEMBL3911369 |
| 7.85 | IC50 | 14 | nM | CHEMBL3913505 |
| 7.85 | IC50 | 14 | nM | CHEMBL3936725 |
| 7.82 | IC50 | 15 | nM | CHEMBL3984596 |
| 7.82 | IC50 | 15 | nM | CHEMBL3902376 |
| 7.67 | IC50 | 21.5 | nM | CHEMBL3952905 |
| 7.62 | IC50 | 24 | nM | CHEMBL3972896 |
| 7.58 | IC50 | 26 | nM | CHEMBL3889804 |
| 7.55 | IC50 | 28 | nM | CHEMBL3958844 |
| 7.55 | IC50 | 28 | nM | CHEMBL3973382 |
| 7.52 | IC50 | 30 | nM | CHEMBL3978200 |
| 7.52 | IC50 | 30 | nM | CHEMBL3985660 |
| 7.51 | IC50 | 31 | nM | CHEMBL3896861 |
| 7.51 | IC50 | 31 | nM | CHEMBL3951956 |
| 7.50 | IC50 | 31.4 | nM | CHEMBL3962403 |
| 7.44 | IC50 | 36 | nM | CHEMBL3953976 |
| 7.44 | IC50 | 36 | nM | CHEMBL3925140 |
| 7.41 | IC50 | 39 | nM | CHEMBL3900691 |
| 7.39 | IC50 | 41 | nM | CHEMBL3930781 |
| 7.30 | IC50 | 50 | nM | CHEMBL3921840 |
| 7.21 | IC50 | 62 | nM | CHEMBL3956991 |
| 7.17 | IC50 | 67 | nM | CHEMBL3965293 |
| 7.09 | IC50 | 81 | nM | CHEMBL3958264 |
| 7.07 | IC50 | 85 | nM | CHEMBL3964411 |
| 7.01 | IC50 | 98.5 | nM | CHEMBL3953031 |
| 6.40 | IC50 | 400 | nM | CHEMBL3974355 |
| 6.10 | IC50 | 800 | nM | CHEMBL3734797 |
| 5.75 | IC50 | 1800 | nM | CHEMBL4228929 |
| 5.66 | IC50 | 2200 | nM | CHEMBL4226021 |
| 5.52 | IC50 | 3000 | nM | CHEMBL4228209 |
| 5.52 | IC50 | 3000 | nM | CHEMBL4224773 |
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.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 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-carboxamide | 1262825: Inhibition of voltage-gated calcium channel (unknown origin) | ic50 | 0.8000 | uM |
| 5-methyl-1-[(2-nitrophenyl)methyl]-3-(piperidin-1-ylmethyl)indole | 1392176: Inhibition of KCl-induced cytosolic voltage gated calcium channel opening in human SH-SY5Y cells by Fluo-4 AM dye based fluorescence assay | ic50 | 1.8000 | uM |
| 1-[(3-chlorophenyl)methyl]-5-methyl-3-(piperidin-1-ylmethyl)indole | 1392176: Inhibition of KCl-induced cytosolic voltage gated calcium channel opening in human SH-SY5Y cells by Fluo-4 AM dye based fluorescence assay | ic50 | 2.2000 | uM |
| 5-methyl-1-[(3-nitrophenyl)methyl]-3-(piperidin-1-ylmethyl)indole | 1392176: Inhibition of KCl-induced cytosolic voltage gated calcium channel opening in human SH-SY5Y cells by Fluo-4 AM dye based fluorescence assay | ic50 | 3.0000 | uM |
| 1-[(4-chlorophenyl)methyl]-5-methyl-3-(piperidin-1-ylmethyl)indole | 1392176: Inhibition of KCl-induced cytosolic voltage gated calcium channel opening in human SH-SY5Y cells by Fluo-4 AM dye based fluorescence assay | ic50 | 3.0000 | uM |
| 1-benzyl-5-methyl-3-(piperidin-1-ylmethyl)indole | 1392176: Inhibition of KCl-induced cytosolic voltage gated calcium channel opening in human SH-SY5Y cells by Fluo-4 AM dye based fluorescence assay | ic50 | 3.4000 | uM |
| 5-methyl-1-[(4-methylphenyl)methyl]-3-(piperidin-1-ylmethyl)indole | 1392176: Inhibition of KCl-induced cytosolic voltage gated calcium channel opening in human SH-SY5Y cells by Fluo-4 AM dye based fluorescence assay | ic50 | 3.6000 | uM |
| 1-[(4-fluorophenyl)methyl]-5-methyl-3-(piperidin-1-ylmethyl)indole | 1392176: Inhibition of KCl-induced cytosolic voltage gated calcium channel opening in human SH-SY5Y cells by Fluo-4 AM dye based fluorescence assay | ic50 | 4.8000 | uM |
| 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-carboxamide | 1612587: 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 assay | ic50 | 9.0000 | uM |
| ethyl 5-amino-4-(3-methoxyphenyl)-2-methyl-7,8,9,10-tetrahydro-6H-cyclohepta[b][1,8]naphthyridine-3-carboxylate | 1653244: Inhibition of VGCC (unknown origin) | ic50 | 9.0000 | uM |
| ethyl 5-amino-4-(3,4-dimethoxyphenyl)-2-methyl-7,8,9,10-tetrahydro-6H-cyclohepta[b][1,8]naphthyridine-3-carboxylate | 1653244: Inhibition of VGCC (unknown origin) | ic50 | 9.0000 | uM |
| propan-2-yl 5-amino-2-methyl-4-phenyl-6,7,8,9-tetrahydrobenzo[b][1,8]naphthyridine-3-carboxylate | 1653244: Inhibition of VGCC (unknown origin) | ic50 | 10.0000 | uM |
| ethyl 5-amino-2-methyl-4-phenyl-6,7,8,9,10,11-hexahydrocycloocta[b][1,8]naphthyridine-3-carboxylate | 1653244: Inhibition of VGCC (unknown origin) | ic50 | 10.0000 | uM |
CTD chemical–gene interactions
11 total (human), top 11 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| aristolochic acid I | increases expression | 1 |
| incobotulinumtoxinA | decreases expression | 1 |
| Resveratrol | affects cotreatment, decreases expression | 1 |
| Aspirin | decreases expression | 1 |
| Benzo(a)pyrene | affects methylation | 1 |
| Niclosamide | increases expression | 1 |
| Plant Extracts | affects cotreatment, decreases expression | 1 |
| Rotenone | increases expression | 1 |
| Tobacco Smoke Pollution | decreases expression | 1 |
| Tretinoin | increases expression | 1 |
| Aflatoxin B1 | increases methylation | 1 |
ChEMBL screening assays
13 unique, capped per target: 13 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL3737861 | Binding | Inhibition 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):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_YA28 | IDG-HEK293T-CACNG1-V5-OE | Transformed cell line | Female |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): malignant hyperthermia, susceptibility to, 1