CACNG7
gene geneOn this page
Summary
CACNG7 (calcium voltage-gated channel auxiliary subunit gamma 7, HGNC:13626) is a protein-coding gene on chromosome 19q13.42, encoding Voltage-dependent calcium channel gamma-7 subunit (P62955). Regulates the activity of L-type calcium channels that contain CACNA1C as pore-forming subunit.
The protein encoded by this gene is a type II transmembrane AMPA receptor regulatory protein (TARP). TARPs regulate both trafficking and channel gating of the AMPA receptors. 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, a type I TARP and a calcium channel gamma subunit.
Source: NCBI Gene 59284 — RefSeq curated summary.
At a glance
- Clinical variants (ClinVar): 41 total — 1 likely-pathogenic
- Druggable target: yes — 2 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_031896
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:13626 |
| Approved symbol | CACNG7 |
| Name | calcium voltage-gated channel auxiliary subunit gamma 7 |
| Location | 19q13.42 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000105605 |
| Ensembl biotype | protein_coding |
| OMIM | 606899 |
| Entrez | 59284 |
Gene structure
Transcript identifiers
Ensembl transcripts: 4 — 3 protein_coding, 1 protein_coding_CDS_not_defined
ENST00000222212, ENST00000391766, ENST00000391767, ENST00000468076
RefSeq mRNA: 2 — MANE Select: NM_031896
NM_001384801, NM_031896
CCDS: CCDS12868
Canonical transcript exons
ENST00000391767 — 6 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000724876 | 53914500 | 53914586 |
| ENSE00001122959 | 53941470 | 53941615 |
| ENSE00001509686 | 53942036 | 53943950 |
| ENSE00001509687 | 53912803 | 53913027 |
| ENSE00003606090 | 53915365 | 53915505 |
| ENSE00003911033 | 53909278 | 53909517 |
Expression profiles
Bgee: expression breadth ubiquitous, 110 present calls, max score 97.19.
FANTOM5 (CAGE): breadth broad, TPM avg 2.9562 / max 75.7450, expressed in 487 samples.
FANTOM5 promoters (3 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 177435 | 2.6092 | 472 |
| 177436 | 0.2943 | 188 |
| 177434 | 0.0526 | 21 |
Top tissues by expression
233 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| cortical plate | UBERON:0005343 | 97.19 | gold quality |
| right frontal lobe | UBERON:0002810 | 96.30 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 95.57 | gold quality |
| anterior cingulate cortex | UBERON:0009835 | 95.50 | gold quality |
| Brodmann (1909) area 9 | UBERON:0013540 | 95.19 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 94.85 | gold quality |
| cerebellar cortex | UBERON:0002129 | 94.69 | gold quality |
| prefrontal cortex | UBERON:0000451 | 94.23 | gold quality |
| C1 segment of cervical spinal cord | UBERON:0006469 | 93.21 | gold quality |
| amygdala | UBERON:0001876 | 91.56 | gold quality |
| ganglionic eminence | UBERON:0004023 | 91.53 | gold quality |
| cerebellum | UBERON:0002037 | 91.18 | gold quality |
| hypothalamus | UBERON:0001898 | 90.34 | gold quality |
| putamen | UBERON:0001874 | 89.31 | gold quality |
| nucleus accumbens | UBERON:0001882 | 88.50 | gold quality |
| spinal cord | UBERON:0002240 | 88.46 | gold quality |
| caudate nucleus | UBERON:0001873 | 88.21 | gold quality |
| dorsolateral prefrontal cortex | UBERON:0009834 | 87.88 | gold quality |
| neocortex | UBERON:0001950 | 87.64 | gold quality |
| ventricular zone | UBERON:0003053 | 87.57 | gold quality |
| frontal cortex | UBERON:0001870 | 86.66 | gold quality |
| cerebral cortex | UBERON:0000956 | 82.68 | gold quality |
| brain | UBERON:0000955 | 82.33 | gold quality |
| forebrain | UBERON:0001890 | 82.04 | gold quality |
| substantia nigra | UBERON:0002038 | 80.70 | gold quality |
| pancreatic ductal cell | CL:0002079 | 78.58 | silver quality |
| Ammon’s horn | UBERON:0001954 | 78.58 | gold quality |
| midbrain | UBERON:0001891 | 76.27 | gold quality |
| temporal lobe | UBERON:0001871 | 73.19 | gold quality |
| adenohypophysis | UBERON:0002196 | 73.01 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 1.46 |
Regulation
Is transcription factor: no
Cross-species orthologs
6 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | cacng7a | ENSDARG00000063006 |
| danio_rerio | cacng7b | ENSDARG00000070624 |
| mus_musculus | Cacng7 | ENSMUSG00000069806 |
| rattus_norvegicus | Cacng7 | ENSRNOG00000056257 |
| drosophila_melanogaster | stg1 | FBGN0288700 |
| caenorhabditis_elegans | WBGENE00007670 |
Paralogs (5): CACNG3 (ENSG00000006116), CACNG5 (ENSG00000075429), CACNG4 (ENSG00000075461), CACNG8 (ENSG00000142408), CACNG2 (ENSG00000166862)
Protein
Protein identifiers
Voltage-dependent calcium channel gamma-7 subunit — P62955 (reviewed: P62955)
Alternative names: Neuronal voltage-gated calcium channel gamma-7 subunit, Transmembrane AMPAR regulatory protein gamma-7
All UniProt accessions (2): P62955, A0A0C4DFY2
UniProt curated annotations — full annotation on UniProt →
Function. Regulates the activity of L-type calcium channels that contain CACNA1C as pore-forming subunit. Regulates the trafficking and gating properties of AMPA-selective glutamate receptors (AMPARs). Promotes their targeting to the cell membrane and synapses and modulates their gating properties by slowing their rates of activation, deactivation and desensitization and by mediating their resensitization. Displays subunit-specific AMPA receptor regulation. Shows specificity only for GRIA1 and GRIA2.
Subunit / interactions. Interacts with CACNA1C. Identified in a complex with the L-type calcium channel subunits CACNA1C, CACNA2D1 and either CACNB1 or CACNB2. Acts as an auxiliary subunit for AMPA-selective glutamate receptors (AMPARs), such as GRIA1 and GRIA2.
Subcellular location. Cell membrane.
Tissue specificity. Detected in heart left ventricle. Widely expressed.
Similarity. Belongs to the PMP-22/EMP/MP20 family. CACNG subfamily.
RefSeq proteins (2): NP_001371730, NP_114102* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR004031 | PMP22/EMP/MP20/Claudin | Family |
| IPR008368 | VDCC_gsu | Family |
| IPR008371 | VDCC_g7su | Family |
| IPR051072 | CACNG_subunit | Family |
Pfam: PF13903
UniProt features (9 total): transmembrane region 4, modified residue 3, chain 1, sequence conflict 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P62955-F1 | 71.34 | 0.25 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Post-translational modifications (3): 222, 225, 273
Function
Pathways and Gene Ontology
Reactome pathways
7 pathways
| ID | Pathway |
|---|---|
| R-HSA-5576892 | Phase 0 - rapid depolarisation |
| R-HSA-5576893 | Phase 2 - plateau phase |
| R-HSA-9856532 | Mechanical load activates signaling by PIEZO1 and integrins in osteocytes |
| R-HSA-397014 | Muscle contraction |
| R-HSA-5576891 | Cardiac conduction |
| R-HSA-8953897 | Cellular responses to stimuli |
| R-HSA-9855142 | Cellular responses to mechanical stimuli |
MSigDB gene sets: 168 (showing top):
GOBP_POSITIVE_REGULATION_OF_SYNAPTIC_TRANSMISSION_GLUTAMATERGIC, GOBP_REGULATION_OF_CELL_MORPHOGENESIS, GOBP_NEURON_PROJECTION_EXTENSION, GOBP_REGULATION_OF_MRNA_CATABOLIC_PROCESS, GOBP_REGULATION_OF_DEVELOPMENTAL_GROWTH, GOBP_REGULATION_OF_SYNAPTIC_TRANSMISSION_GLUTAMATERGIC, KEGG_MAPK_SIGNALING_PATHWAY, GOBP_GROWTH, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, GOBP_NEUROGENESIS, HATADA_METHYLATED_IN_LUNG_CANCER_DN, GOBP_PROTEIN_LOCALIZATION_TO_CELL_PERIPHERY, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_CELL_CELL_SIGNALING, GOBP_POST_TRANSCRIPTIONAL_REGULATION_OF_GENE_EXPRESSION
GO Biological Process (11): calcium ion transport (GO:0006816), transmission of nerve impulse (GO:0019226), regulation of mRNA stability (GO:0043488), positive regulation of synaptic transmission, glutamatergic (GO:0051968), postsynaptic neurotransmitter receptor diffusion trapping (GO:0098970), neurotransmitter receptor localization to postsynaptic specialization membrane (GO:0099645), positive regulation of dendrite extension (GO:1903861), regulation of AMPA receptor activity (GO:2000311), monoatomic ion transport (GO:0006811), monoatomic ion transmembrane transport (GO:0034220), calcium ion transmembrane transport (GO:0070588)
GO Molecular Function (5): voltage-gated calcium channel activity (GO:0005245), calcium channel regulator activity (GO:0005246), channel regulator activity (GO:0016247), calcium channel activity (GO:0005262), protein binding (GO:0005515)
GO Cellular Component (11): early endosome (GO:0005769), plasma membrane (GO:0005886), voltage-gated calcium channel complex (GO:0005891), AMPA glutamate receptor complex (GO:0032281), neuronal cell body (GO:0043025), cerebellar mossy fiber (GO:0044300), postsynaptic density membrane (GO:0098839), glutamatergic synapse (GO:0098978), L-type voltage-gated calcium channel complex (GO:1990454), membrane (GO:0016020), monoatomic ion channel complex (GO:0034702)
Reactome top-level categories
Rollup of top-4 pathways:
| Category | Pathways |
|---|---|
| Cardiac conduction | 2 |
| Cellular responses to mechanical stimuli | 1 |
| Muscle contraction | 1 |
| Cellular responses to stimuli | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| postsynaptic membrane | 2 |
| receptor localization to synapse | 2 |
| regulation of postsynaptic membrane neurotransmitter receptor levels | 2 |
| postsynaptic specialization membrane | 2 |
| calcium channel activity | 2 |
| metal ion transport | 1 |
| action potential | 1 |
| cell communication | 1 |
| chemical synaptic transmission | 1 |
| nervous system process | 1 |
| regulation of RNA stability | 1 |
| regulation of mRNA catabolic process | 1 |
| synaptic transmission, glutamatergic | 1 |
| positive regulation of synaptic transmission | 1 |
| regulation of synaptic transmission, glutamatergic | 1 |
| neurotransmitter receptor diffusion trapping | 1 |
| protein-containing complex localization | 1 |
| protein localization to postsynaptic specialization membrane | 1 |
| positive regulation of cell growth | 1 |
| positive regulation of developmental growth | 1 |
| dendrite extension | 1 |
| regulation of dendrite extension | 1 |
| AMPA glutamate receptor activity | 1 |
| regulation of transmembrane transporter activity | 1 |
| regulation of neurotransmitter receptor activity | 1 |
| transport | 1 |
| monoatomic ion transport | 1 |
| transmembrane transport | 1 |
| calcium ion transport | 1 |
| monoatomic cation transmembrane transport | 1 |
| voltage-gated monoatomic cation channel activity | 1 |
| ion channel regulator activity | 1 |
| channel activity | 1 |
| transporter regulator activity | 1 |
| monoatomic cation channel activity | 1 |
| calcium ion transmembrane transporter activity | 1 |
| binding | 1 |
| endosome | 1 |
| membrane | 1 |
| cell periphery | 1 |
Protein interactions and networks
STRING
2128 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CACNG7 | CACNG1 | Q06432 | 917 |
| CACNG7 | PRKCG | P05129 | 802 |
| CACNG7 | CACNA1D | Q01668 | 783 |
| CACNG7 | CACNB1 | Q02641 | 751 |
| CACNG7 | DLG4 | P78352 | 650 |
| CACNG7 | CACNA2D2 | Q9NY47 | 645 |
| CACNG7 | CACNA2D1 | P54289 | 644 |
| CACNG7 | CACNA1E | Q15878 | 543 |
| CACNG7 | CNIH2 | Q6PI25 | 520 |
| CACNG7 | CACNA1G | O43497 | 512 |
| CACNG7 | CACNA1B | Q00975 | 500 |
| CACNG7 | CNIH4 | Q9P003 | 477 |
| CACNG7 | CACNG4 | Q9UBN1 | 475 |
| CACNG7 | AVPI1 | Q5T686 | 464 |
| CACNG7 | ELOC | Q15369 | 461 |
IntAct
5 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CACNG7 | SPACA1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| CACNG7 | PLD2 | psi-mi:“MI:0914”(association) | 0.350 |
| CACNG7 | SPACA1 | psi-mi:“MI:0915”(physical association) | 0.000 |
BioGRID (19): SPACA1 (Two-hybrid), SLC25A4 (Affinity Capture-MS), TSPYL1 (Affinity Capture-MS), RAB29 (Affinity Capture-MS), CYBA (Affinity Capture-MS), HLA-DRB1 (Affinity Capture-MS), FBXL6 (Affinity Capture-MS), ACSL1 (Affinity Capture-MS), SLC25A6 (Affinity Capture-MS), IQSEC1 (Affinity Capture-MS), HSPA5 (Affinity Capture-MS), KIRREL (Affinity Capture-MS), FUT8 (Affinity Capture-MS), SAMM50 (Affinity Capture-MS), SLC38A5 (Affinity Capture-MS)
ESM2 similar proteins: A2AIR5, A5PK40, A6NFX1, B9EKX1, D2HKB0, D3ZG27, F1NCD6, O60242, P23979, P46098, P62955, P62956, P62957, Q08DW9, Q0VBU9, Q13635, Q14B62, Q3T9X0, Q4R766, Q504N2, Q5H8A4, Q5RB09, Q5RIV7, Q5T4D3, Q5VTY9, Q5VYX0, Q5VZY2, Q5ZIN0, Q61115, Q66H95, Q6AYT7, Q6ZW05, Q80ZF8, Q8BG19, Q8BWB6, Q8IZD6, Q8N2K0, Q8N6M3, Q8NEB5, Q8NHX9
Diamond homologs: O60359, O88602, P62955, P62956, P62957, Q0VD05, Q4R589, Q5R5X2, Q71RJ2, Q8VHW2, Q8VHW4, Q8VHW5, Q8VHW8, Q8VHW9, Q8VHX0, Q8WXS5, Q9JJV4, Q9JJV5, Q9UBN1, Q9UF02, Q9Y698
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
41 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 1 |
| Uncertain significance | 37 |
| Likely benign | 0 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (1)
| Variant ID | HGVS | Classification |
|---|---|---|
| 996577 | NM_031896.5(CACNG7):c.784A>G (p.Ile262Val) | Likely pathogenic |
SpliceAI
1123 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 19:53909516:AGGTG:A | donor_loss | 1.0000 |
| 19:53909518:G:GA | donor_loss | 1.0000 |
| 19:53913009:C:T | donor_gain | 1.0000 |
| 19:53913025:CAGGT:C | donor_loss | 1.0000 |
| 19:53913027:GG:G | donor_loss | 1.0000 |
| 19:53913028:GTA:G | donor_loss | 1.0000 |
| 19:53913029:T:A | donor_loss | 1.0000 |
| 19:53914583:C:G | donor_gain | 1.0000 |
| 19:53914585:GA:G | donor_gain | 1.0000 |
| 19:53914587:G:GG | donor_gain | 1.0000 |
| 19:53915363:A:AG | acceptor_gain | 1.0000 |
| 19:53915364:G:GG | acceptor_gain | 1.0000 |
| 19:53915364:GA:G | acceptor_gain | 1.0000 |
| 19:53915504:GG:G | donor_gain | 1.0000 |
| 19:53915505:GG:G | donor_gain | 1.0000 |
| 19:53915506:G:GC | donor_loss | 1.0000 |
| 19:53915506:G:GG | donor_gain | 1.0000 |
| 19:53915507:T:G | donor_loss | 1.0000 |
| 19:53942031:CGCAG:C | acceptor_loss | 1.0000 |
| 19:53942032:GCAGG:G | acceptor_loss | 1.0000 |
| 19:53942034:A:AG | acceptor_gain | 1.0000 |
| 19:53942034:AG:A | acceptor_gain | 1.0000 |
| 19:53942034:AGG:A | acceptor_gain | 1.0000 |
| 19:53942035:G:GG | acceptor_gain | 1.0000 |
| 19:53942035:GG:G | acceptor_gain | 1.0000 |
| 19:53942035:GGG:G | acceptor_gain | 1.0000 |
| 19:53909513:GCGAG:G | donor_gain | 0.9900 |
| 19:53912801:A:AG | acceptor_gain | 0.9900 |
| 19:53912802:G:GA | acceptor_loss | 0.9900 |
| 19:53912802:G:GG | acceptor_gain | 0.9900 |
AlphaMissense
1806 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 19:53914517:T:A | C72S | 1.000 |
| 19:53914518:G:C | C72S | 1.000 |
| 19:53915400:A:C | S107R | 1.000 |
| 19:53915402:C:A | S107R | 1.000 |
| 19:53915402:C:G | S107R | 1.000 |
| 19:53915484:G:C | G135R | 1.000 |
| 19:53915485:G:A | G135D | 1.000 |
| 19:53915497:T:A | I139K | 1.000 |
| 19:53915505:G:C | G142R | 1.000 |
| 19:53941487:G:C | G148R | 1.000 |
| 19:53942043:G:A | G193D | 1.000 |
| 19:53912868:A:C | S13R | 0.999 |
| 19:53912870:C:A | S13R | 0.999 |
| 19:53912870:C:G | S13R | 0.999 |
| 19:53912881:G:A | G17D | 0.999 |
| 19:53912889:G:C | G20R | 0.999 |
| 19:53912904:G:C | G25R | 0.999 |
| 19:53912911:C:A | A27E | 0.999 |
| 19:53912916:A:C | S29R | 0.999 |
| 19:53912918:C:A | S29R | 0.999 |
| 19:53912918:C:G | S29R | 0.999 |
| 19:53912920:C:T | T30I | 0.999 |
| 19:53912923:A:T | D31V | 0.999 |
| 19:53912928:T:A | W33R | 0.999 |
| 19:53912928:T:C | W33R | 0.999 |
| 19:53912930:G:C | W33C | 0.999 |
| 19:53912930:G:T | W33C | 0.999 |
| 19:53912932:T:C | L34P | 0.999 |
| 19:53913000:G:C | G57R | 0.999 |
| 19:53913000:G:T | G57C | 0.999 |
dbSNP variants (sampled 300 via entrez): RS1000073509 (19:53928600 T>C), RS1000133518 (19:53913697 T>A,C), RS1000140909 (19:53926092 T>C), RS1000164686 (19:53918849 A>C,G), RS1000195198 (19:53925900 C>T), RS1000209109 (19:53916193 G>A), RS1000247390 (19:53925726 G>A,C,T), RS1000309496 (19:53913129 G>A,C), RS1000398555 (19:53931135 G>A,T), RS1000646668 (19:53911715 G>A,T), RS1000680830 (19:53929934 T>C), RS1000829273 (19:53917313 T>C), RS1000841551 (19:53936938 C>G), RS1000874020 (19:53936758 A>G), RS1000891901 (19:53918684 C>T)
Disease associations
OMIM: gene MIM:606899 | disease phenotypes:
GenCC curated gene-disease
Mondo (1): intellectual disability (MONDO:0001071)
Orphanet (1): NON RARE IN EUROPE: Unexplained intellectual disability (Orphanet:319658)
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
0 associations (top):
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D008607 | Intellectual Disability | C10.597.606.360; C23.888.592.604.646; F01.700.687; F03.625.539 |
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)
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
17 total (human), top 17 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| propionaldehyde | increases expression | 1 |
| pirinixic acid | affects binding, increases activity, increases expression | 1 |
| ethyl-p-hydroxybenzoate | decreases expression | 1 |
| butyraldehyde | increases expression | 1 |
| pentanal | increases expression | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| abrine | decreases expression | 1 |
| jinfukang | increases expression | 1 |
| Resveratrol | affects cotreatment, decreases expression | 1 |
| Arbutin | decreases expression | 1 |
| Benzo(a)pyrene | affects methylation | 1 |
| Diethylhexyl Phthalate | decreases expression | 1 |
| Plant Extracts | decreases expression, affects cotreatment | 1 |
| Silicon Dioxide | increases expression | 1 |
| Dronabinol | increases expression | 1 |
| Aflatoxin B1 | decreases methylation | 1 |
| Acrylamide | decreases expression | 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
2 cell lines: 1 cancer cell line, 1 transformed cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_D7LG | Ubigene A-549 CACNG7 KO | Cancer cell line | Male |
| CVCL_YA31 | IDG-HEK293T-CACNG7-V5-OE | Transformed cell line | Female |
Clinical trials (associated diseases)
197 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT05657860 | PHASE4 | COMPLETED | Guanfacine Extended Release for the Reduction of Aggression and Self-injurious Behavior Associated With Prader-Willi Syndrome |
| NCT05744479 | PHASE4 | RECRUITING | Metformin for Antipsychotic-induced Weight Gain in Adults With Intellectual Disability |
| NCT06107829 | PHASE4 | WITHDRAWN | Valbenazine Treatment of Tardive Dyskinesia in Adults With Intellectual/Developmental Disabilities |
| NCT06997198 | PHASE4 | NOT_YET_RECRUITING | Deutetrabenazine Treatment for Tardive Dyskinesia in Intellectual/Developmental Disabilities |
| NCT02270736 | PHASE3 | COMPLETED | Clinical Study to Investigate the Efficacy and Safety of NT 201 Compared to Placebo in the Treatment of Chronic Troublesome Drooling Associated With Neurological Disorders and/or Intellectual Disability |
| NCT02304302 | PHASE2 | COMPLETED | Down Syndrome Memantine Follow-up Study |
| NCT03862950 | PHASE2 | COMPLETED | A Trial of Metformin in Individuals With Fragile X Syndrome (Met) |
| NCT04529226 | PHASE2 | UNKNOWN | Study to Compare Clozapine vs Treatment as Usual in People With Intellectual Disability & Treatment-resistant Psychosis |
| NCT04821856 | PHASE2 | COMPLETED | Evaluation of the Effectiveness of Cannabidiol in Treating Severe Behavioural Problems in Children and Adolescents With Intellectual Disability |
| NCT05273320 | PHASE1 | COMPLETED | Clinical Trial of Nabilone for Aggression in Adults With Intellectual and Developmental Disabilities |
| NCT05301361 | PHASE1 | ENROLLING_BY_INVITATION | Sensitivity of the NIH Toolbox to Stimulant Treatment in Intellectual Disabilities |
| NCT06016764 | PHASE1 | COMPLETED | Use of MRI and cTBS for Catatonia in Autism |
| NCT06586827 | PHASE1 | COMPLETED | Impact of Competency-Based Training and Technical Assistance Employment Outcomes of Individuals With ID/DD |
| NCT07531940 | PHASE1 | NOT_YET_RECRUITING | Escalating Doses of Memantine in Down Syndrome (MEDS-123) |
| NCT03479476 | PHASE2/PHASE3 | COMPLETED | A Trial of Metformin in Individuals With Fragile X Syndrome |
| NCT02616796 | PHASE1/PHASE2 | COMPLETED | Effects of Social Gaze Training on Brain and Behavior in Fragile X Syndrome |
| NCT06860672 | EARLY_PHASE1 | RECRUITING | Clinical Trial of the Dual Vector Base Editor for the Treatment of the CHD3-R1025W Mutation |
| NCT00597948 | Not specified | COMPLETED | Healthy Lifestyles for People With Intellectual Disabilities |
| NCT01087320 | Not specified | RECRUITING | Genome Medical Sequencing for Gene Discovery |
| NCT01652963 | Not specified | UNKNOWN | Picture-based Computerised Assessment and Training of Cognitive Behaviour Therapy Skills |
| NCT01695395 | Not specified | COMPLETED | Mental Health Care Provision for Adults With Intellectual Disability and a Mental Disorder |
| NCT01867554 | Not specified | COMPLETED | Research and Characterization of New Genes Involved in Intellectual Disability |
| NCT01915381 | Not specified | COMPLETED | Improving Adherence Healthy Lifestyle With a Smartphone Application Based on Adults With Intellectual Disabilities |
| NCT01988623 | Not specified | COMPLETED | Pivotal Response Treatment for Individuals With Intellectual Disabilities |
| NCT02099773 | Not specified | COMPLETED | Support Staff-client Interactions With Augmentative and Alternative Communication |
| NCT02136849 | Not specified | COMPLETED | Inter-regional Project of the Great Western Exploration Approach for Exome Molecular Causes Severe Intellectual Disability Isolated or Syndromic |
| NCT02225041 | Not specified | COMPLETED | Sedation Strategy and Cognitive Outcome After Critical Illness in Early Childhood |
| NCT02414438 | Not specified | COMPLETED | Establishing the Clinical Utility of First StepDx PLUS and NextStepDx PLUS Study |
| NCT02451761 | Not specified | COMPLETED | Apparently Balanced Chromosomal Translocation/ Next-generation Sequencing/ Intellectual Disability |
| NCT02461420 | Not specified | ACTIVE_NOT_RECRUITING | Mapping the Genotype, Phenotype, and Natural History of Phelan-McDermid Syndrome |
| NCT02461459 | Not specified | ACTIVE_NOT_RECRUITING | Autism Spectrum Disorder (ASD) and Intellectual Disability (ID) Determinants in Tuberous Sclerosis Complex (TSC) |
| NCT02486081 | Not specified | COMPLETED | Development and Application-Smart Football for Movement Evaluation and Training in the Special Education Population |
| NCT02504502 | Not specified | COMPLETED | Enhancing Genomic Laboratory Reports to Enhance Communication and Empower Patients |
| NCT02513277 | Not specified | COMPLETED | Diabetes Screening & Prevention for People With Learning (Intellectual) Disabilities:STOP Diabetes Study |
| NCT02561754 | Not specified | COMPLETED | Weight Management for Adolescents With IDD |
| NCT02591446 | Not specified | COMPLETED | Transcranial Magnetic Stimulation Studies in Autism Spectrum Disorders |
| NCT02714868 | Not specified | COMPLETED | Evaluation of Project TEAM (Teens Making Environmental and Activity Modifications) |
| NCT02721394 | Not specified | UNKNOWN | FCT With Young Children With ID in the UK: A Feasibility Project V.1 |
| NCT02746614 | Not specified | COMPLETED | Psychomotor Therapy Effects in Adaptive Behavior and Motor Proficiency in Intellectual Disability |
| NCT02836405 | Not specified | COMPLETED | TMS for the Investigation of Brain Plasticity in Autism Spectrum Disorders |
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.