CACNG5
gene geneOn this page
Summary
CACNG5 (calcium voltage-gated channel auxiliary subunit gamma 5, HGNC:1409) is a protein-coding gene on chromosome 17q24.2, encoding Voltage-dependent calcium channel gamma-5 subunit (Q9UF02). Regulates the gating properties of AMPA-selective glutamate receptors (AMPARs).
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. This gene is a susceptibility locus for schizophrenia and bipolar disorder.
Source: NCBI Gene 27091 — RefSeq curated summary.
At a glance
- GWAS associations: 3
- Clinical variants (ClinVar): 51 total
- Druggable target: yes — 2 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_145811
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:1409 |
| Approved symbol | CACNG5 |
| Name | calcium voltage-gated channel auxiliary subunit gamma 5 |
| Location | 17q24.2 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000075429 |
| Ensembl biotype | protein_coding |
| OMIM | 606405 |
| Entrez | 27091 |
Gene structure
Transcript identifiers
Ensembl transcripts: 3 — 3 protein_coding
ENST00000307139, ENST00000533854, ENST00000673855
RefSeq mRNA: 2 — MANE Select: NM_145811
NM_001371476, NM_145811
CCDS: CCDS11665, CCDS92382
Canonical transcript exons
ENST00000533854 — 6 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000406082 | 66878972 | 66879058 |
| ENSE00000742698 | 66884516 | 66884661 |
| ENSE00002142694 | 66884983 | 66894751 |
| ENSE00002148235 | 66835117 | 66835250 |
| ENSE00002200600 | 66877230 | 66877528 |
| ENSE00002472944 | 66880557 | 66880697 |
Expression profiles
Bgee: expression breadth broad, 46 present calls, max score 66.84.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.3061 / max 58.0704, expressed in 107 samples.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 162318 | 0.3061 | 107 |
Top tissues by expression
233 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 66.84 | silver quality |
| anterior cingulate cortex | UBERON:0009835 | 65.21 | gold quality |
| Brodmann (1909) area 9 | UBERON:0013540 | 64.15 | gold quality |
| prefrontal cortex | UBERON:0000451 | 63.76 | gold quality |
| islet of Langerhans | UBERON:0000006 | 63.69 | gold quality |
| putamen | UBERON:0001874 | 63.67 | gold quality |
| ganglionic eminence | UBERON:0004023 | 63.02 | gold quality |
| dorsolateral prefrontal cortex | UBERON:0009834 | 62.91 | gold quality |
| nucleus accumbens | UBERON:0001882 | 62.86 | gold quality |
| amygdala | UBERON:0001876 | 62.09 | gold quality |
| right frontal lobe | UBERON:0002810 | 61.89 | gold quality |
| jejunal mucosa | UBERON:0000399 | 61.67 | gold quality |
| caudate nucleus | UBERON:0001873 | 61.61 | gold quality |
| neocortex | UBERON:0001950 | 60.05 | gold quality |
| parotid gland | UBERON:0001831 | 59.72 | gold quality |
| nasal cavity epithelium | UBERON:0005384 | 59.40 | gold quality |
| frontal cortex | UBERON:0001870 | 59.05 | gold quality |
| cerebral cortex | UBERON:0000956 | 57.98 | gold quality |
| hypothalamus | UBERON:0001898 | 57.69 | gold quality |
| ventricular zone | UBERON:0003053 | 57.66 | silver quality |
| myocardium | UBERON:0002349 | 57.35 | gold quality |
| forebrain | UBERON:0001890 | 56.77 | gold quality |
| primary visual cortex | UBERON:0002436 | 56.37 | gold quality |
| tendon of biceps brachii | UBERON:0008188 | 55.88 | gold quality |
| C1 segment of cervical spinal cord | UBERON:0006469 | 55.54 | gold quality |
| brain | UBERON:0000955 | 55.40 | gold quality |
| vena cava | UBERON:0004087 | 55.04 | gold quality |
| seminal vesicle | UBERON:0000998 | 54.49 | gold quality |
| temporal lobe | UBERON:0001871 | 54.37 | gold quality |
| spinal cord | UBERON:0002240 | 54.13 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 1.14 |
Regulation
Is transcription factor: no
Literature-anchored findings (GeneRIF, showing 1)
- These results indicate that CACNG4, CACNG5, CACNG6 and CACNG8 may contribute to the risk of SCZ. The statistical epistasis identified between CACNG5 and CACNG6 suggests that there may be an underlying biological interaction between the two genes. (PMID:27102562)
Cross-species orthologs
6 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | cacng5a | ENSDARG00000003326 |
| danio_rerio | cacng5b | ENSDARG00000039240 |
| mus_musculus | Cacng5 | ENSMUSG00000040373 |
| rattus_norvegicus | Cacng5 | ENSRNOG00000003288 |
| drosophila_melanogaster | stg1 | FBGN0288700 |
| caenorhabditis_elegans | WBGENE00007670 |
Paralogs (5): CACNG3 (ENSG00000006116), CACNG4 (ENSG00000075461), CACNG7 (ENSG00000105605), CACNG8 (ENSG00000142408), CACNG2 (ENSG00000166862)
Protein
Protein identifiers
Voltage-dependent calcium channel gamma-5 subunit — Q9UF02 (reviewed: Q9UF02)
Alternative names: Neuronal voltage-gated calcium channel gamma-5 subunit, Transmembrane AMPAR regulatory protein gamma-5
All UniProt accessions (2): Q9UF02, A0A669KBF6
UniProt curated annotations — full annotation on UniProt →
Function. Regulates the gating properties of AMPA-selective glutamate receptors (AMPARs). Modulates their gating properties by accelerating their rates of activation, deactivation and desensitization. Displays subunit-specific AMPA receptor regulation. Shows specificity for GRIA1, GRIA4 and the long isoform of GRIA2. Thought to stabilize the calcium channel in an inactivated (closed) state.
Subunit / interactions. The L-type calcium channel is composed of five subunits: alpha-1, alpha-2/delta, beta and gamma. Acts as an auxiliary subunit for AMPA-selective glutamate receptors (AMPARs). Found in a complex with GRIA1, GRIA2, GRIA3, GRIA4, CNIH2, CNIH3, CACNG2, CACNG3, CACNG4, CACNG7 and CACNG8. Interacts with GRIA1, GRIA2, GRIA3 and GRIA4.
Subcellular location. Membrane. Postsynaptic density membrane.
Similarity. Belongs to the PMP-22/EMP/MP20 family. CACNG subfamily.
RefSeq proteins (2): NP_001358405, NP_665810* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR004031 | PMP22/EMP/MP20/Claudin | Family |
| IPR008368 | VDCC_gsu | Family |
| IPR008369 | VDCC_g5su | Family |
| IPR051072 | CACNG_subunit | Family |
Pfam: PF13903
UniProt features (6 total): transmembrane region 4, chain 1, sequence conflict 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9UF02-F1 | 72.86 | 0.26 |
Function
Pathways and Gene Ontology
Reactome pathways
0 pathways
MSigDB gene sets: 105 (showing top):
GOBP_POSITIVE_REGULATION_OF_SYNAPTIC_TRANSMISSION_GLUTAMATERGIC, GOBP_REGULATION_OF_SYNAPTIC_TRANSMISSION_GLUTAMATERGIC, KEGG_MAPK_SIGNALING_PATHWAY, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_CELL_CELL_SIGNALING, GOBP_SYNAPTIC_SIGNALING, GOBP_POSITIVE_REGULATION_OF_SYNAPTIC_TRANSMISSION, GOBP_SYNAPTIC_TRANSMISSION_GLUTAMATERGIC, GOBP_REGULATION_OF_NEUROTRANSMITTER_RECEPTOR_ACTIVITY, GOBP_LOCALIZATION_WITHIN_MEMBRANE, GOBP_REGULATION_OF_TRANSPORT, GOBP_CALCIUM_ION_TRANSMEMBRANE_TRANSPORT, NIKOLSKY_BREAST_CANCER_17Q21_Q25_AMPLICON, GOBP_TRANSMEMBRANE_TRANSPORT, KEGG_ARRHYTHMOGENIC_RIGHT_VENTRICULAR_CARDIOMYOPATHY_ARVC
GO Biological Process (7): transmission of nerve impulse (GO:0019226), positive regulation of synaptic transmission, glutamatergic (GO:0051968), postsynaptic neurotransmitter receptor diffusion trapping (GO:0098970), regulation of AMPA receptor activity (GO:2000311), calcium ion transport (GO:0006816), monoatomic ion transmembrane transport (GO:0034220), calcium ion transmembrane transport (GO:0070588)
GO Molecular Function (3): voltage-gated calcium channel activity (GO:0005245), monoatomic ion transmembrane transporter activity (GO:0015075), channel regulator activity (GO:0016247)
GO Cellular Component (8): postsynaptic density (GO:0014069), AMPA glutamate receptor complex (GO:0032281), postsynaptic density membrane (GO:0098839), glutamatergic synapse (GO:0098978), plasma membrane (GO:0005886), membrane (GO:0016020), synapse (GO:0045202), postsynaptic membrane (GO:0045211)
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| postsynaptic membrane | 2 |
| postsynaptic specialization membrane | 2 |
| action potential | 1 |
| cell communication | 1 |
| chemical synaptic transmission | 1 |
| nervous system process | 1 |
| synaptic transmission, glutamatergic | 1 |
| positive regulation of synaptic transmission | 1 |
| regulation of synaptic transmission, glutamatergic | 1 |
| receptor localization to synapse | 1 |
| regulation of postsynaptic membrane neurotransmitter receptor levels | 1 |
| neurotransmitter receptor diffusion trapping | 1 |
| AMPA glutamate receptor activity | 1 |
| regulation of transmembrane transporter activity | 1 |
| regulation of neurotransmitter receptor activity | 1 |
| metal ion transport | 1 |
| monoatomic ion transport | 1 |
| transmembrane transport | 1 |
| calcium ion transport | 1 |
| monoatomic cation transmembrane transport | 1 |
| calcium channel activity | 1 |
| voltage-gated monoatomic cation channel activity | 1 |
| transmembrane transporter activity | 1 |
| monoatomic ion transmembrane transport | 1 |
| channel activity | 1 |
| transporter regulator activity | 1 |
| asymmetric synapse | 1 |
| postsynaptic specialization | 1 |
| ionotropic glutamate receptor complex | 1 |
| postsynaptic density | 1 |
| synapse | 1 |
| membrane | 1 |
| cell periphery | 1 |
| cellular anatomical structure | 1 |
| cell junction | 1 |
| synaptic membrane | 1 |
| postsynapse | 1 |
Protein interactions and networks
STRING
1151 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CACNG5 | CACNG1 | Q06432 | 916 |
| CACNG5 | CACNB1 | Q02641 | 809 |
| CACNG5 | CACNA2D1 | P54289 | 705 |
| CACNG5 | CACNA1D | Q01668 | 672 |
| CACNG5 | CACNA1B | Q00975 | 595 |
| CACNG5 | GRIA2 | P42262 | 551 |
| CACNG5 | PRKCG | P05129 | 506 |
| CACNG5 | PRKCA | P17252 | 440 |
| CACNG5 | CACNG4 | Q9UBN1 | 421 |
| CACNG5 | CACNA2D3 | Q8IZS8 | 395 |
| CACNG5 | CACNB4 | O00305 | 391 |
| CACNG5 | GSG1L | Q6UXU4 | 360 |
| CACNG5 | TRPV2 | Q9Y5S1 | 358 |
| CACNG5 | CNIH1 | O95406 | 351 |
| CACNG5 | GRIA4 | P48058 | 349 |
IntAct
4 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CACNG5 | ZNF316 | psi-mi:“MI:0914”(association) | 0.530 |
| CACNG5 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (76): HELZ2 (Affinity Capture-MS), ZNF142 (Affinity Capture-MS), SCAI (Affinity Capture-MS), PLD1 (Affinity Capture-MS), ARHGEF39 (Affinity Capture-MS), MIS18BP1 (Affinity Capture-MS), PRKRIR (Affinity Capture-MS), MBLAC2 (Affinity Capture-MS), MCM10 (Affinity Capture-MS), PLD2 (Affinity Capture-MS), ZC3H3 (Affinity Capture-MS), SGPL1 (Affinity Capture-MS), ZNF865 (Affinity Capture-MS), TTLL5 (Affinity Capture-MS), ZNF445 (Affinity Capture-MS)
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: O60359, O88602, Q0VD05, Q4R589, Q5R5X2, Q71RJ2, Q8VHW2, Q8VHW4, Q8VHW5, Q8VHW8, Q8VHW9, Q8VHX0, Q8WXS5, Q9JJV4, Q9JJV5, Q9UBN1, Q9UF02, Q9Y698, P62955, P62956, P62957
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
51 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 50 |
| Likely benign | 0 |
| Benign | 1 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
1123 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 17:66835246:GCGAG:G | donor_gain | 1.0000 |
| 17:66835249:AGG:A | donor_loss | 1.0000 |
| 17:66835250:GGTAA:G | donor_loss | 1.0000 |
| 17:66835251:G:GA | donor_loss | 1.0000 |
| 17:66835252:T:A | donor_loss | 1.0000 |
| 17:66879059:G:GG | donor_gain | 1.0000 |
| 17:66880694:TCAGG:T | donor_loss | 1.0000 |
| 17:66880696:AGGT:A | donor_loss | 1.0000 |
| 17:66880697:GGTA:G | donor_loss | 1.0000 |
| 17:66880698:GTAA:G | donor_loss | 1.0000 |
| 17:66884505:T:A | acceptor_gain | 1.0000 |
| 17:66884528:T:TA | acceptor_gain | 1.0000 |
| 17:66884531:T:TA | acceptor_gain | 1.0000 |
| 17:66884537:T:TA | acceptor_gain | 1.0000 |
| 17:66884613:G:GG | donor_gain | 1.0000 |
| 17:66884620:T:TA | donor_gain | 1.0000 |
| 17:66884621:G:GA | donor_gain | 1.0000 |
| 17:66884659:G:GT | donor_gain | 1.0000 |
| 17:66884982:GA:G | acceptor_gain | 1.0000 |
| 17:66835248:GAG:G | donor_gain | 0.9900 |
| 17:66835251:G:GG | donor_gain | 0.9900 |
| 17:66877524:TGCAG:T | donor_loss | 0.9900 |
| 17:66877526:CAGG:C | donor_loss | 0.9900 |
| 17:66877527:AGG:A | donor_loss | 0.9900 |
| 17:66877528:GGTA:G | donor_loss | 0.9900 |
| 17:66878966:CCACA:C | acceptor_loss | 0.9900 |
| 17:66878967:CACAG:C | acceptor_loss | 0.9900 |
| 17:66878968:ACAG:A | acceptor_loss | 0.9900 |
| 17:66878969:CAG:C | acceptor_loss | 0.9900 |
| 17:66878970:A:AT | acceptor_loss | 0.9900 |
AlphaMissense
1808 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 17:66877429:T:A | W33R | 0.999 |
| 17:66877429:T:C | W33R | 0.999 |
| 17:66877433:T:C | L34P | 0.999 |
| 17:66880592:A:C | S107R | 0.999 |
| 17:66880594:C:A | S107R | 0.999 |
| 17:66880594:C:G | S107R | 0.999 |
| 17:66880613:G:A | G114R | 0.999 |
| 17:66880613:G:C | G114R | 0.999 |
| 17:66880613:G:T | G114W | 0.999 |
| 17:66880614:G:A | G114E | 0.999 |
| 17:66880676:G:C | G135R | 0.999 |
| 17:66880677:G:A | G135D | 0.999 |
| 17:66880697:G:C | G142R | 0.999 |
| 17:66884519:T:C | L143P | 0.999 |
| 17:66884533:G:C | G148R | 0.999 |
| 17:66884537:T:C | L149P | 0.999 |
| 17:66884989:G:A | G193R | 0.999 |
| 17:66884989:G:C | G193R | 0.999 |
| 17:66884989:G:T | G193W | 0.999 |
| 17:66884990:G:A | G193E | 0.999 |
| 17:66877369:A:C | S13R | 0.998 |
| 17:66877371:C:A | S13R | 0.998 |
| 17:66877371:C:G | S13R | 0.998 |
| 17:66877412:C:A | A27E | 0.998 |
| 17:66877431:G:C | W33C | 0.998 |
| 17:66877431:G:T | W33C | 0.998 |
| 17:66877501:G:C | G57R | 0.998 |
| 17:66877501:G:T | G57C | 0.998 |
| 17:66877502:G:A | G57D | 0.998 |
| 17:66877507:T:A | W59R | 0.998 |
dbSNP variants (sampled 300 via entrez): RS1000064415 (17:66865512 T>C), RS1000090500 (17:66845470 A>AC), RS1000140606 (17:66859547 T>C), RS1000155128 (17:66893648 A>G), RS1000222477 (17:66885524 G>A), RS1000271448 (17:66851431 T>G), RS1000437405 (17:66876966 G>T), RS1000467590 (17:66888585 A>C,G), RS1000558802 (17:66881955 T>C), RS1000633389 (17:66841138 C>T), RS1000649708 (17:66849119 C>T), RS1000670613 (17:66871157 G>T), RS1000731636 (17:66835458 GTGTC>G), RS1000757439 (17:66887307 A>C), RS1000843459 (17:66867097 G>A)
Disease associations
OMIM: gene MIM:606405 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
3 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST000862_2 | Bipolar disorder and schizophrenia | 6.000000e-07 |
| GCST003365_6 | Systolic blood pressure (cigarette smoking interaction) | 2.000000e-06 |
| GCST005944_4 | Viral capsid antigen IgG seropositivity | 2.000000e-09 |
EFO canonical traits (2, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0006335 | systolic blood pressure |
| EFO:0009272 | Epstein Barr viral capsid antigen seropositivity |
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
13 total (human), top 13 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| bisphenol A | affects cotreatment, increases methylation | 1 |
| cobaltous chloride | affects expression | 1 |
| S-(1,2-dichlorovinyl)cysteine | decreases expression | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| Resveratrol | affects cotreatment, decreases expression | 1 |
| Arsenic Trioxide | increases expression | 1 |
| Fulvestrant | affects cotreatment, increases methylation | 1 |
| Arsenic | affects methylation | 1 |
| Benzo(a)pyrene | decreases methylation, affects methylation | 1 |
| Diethylhexyl Phthalate | decreases expression | 1 |
| Plant Extracts | affects cotreatment, decreases expression | 1 |
| 1-Methyl-4-phenylpyridinium | 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_YA30 | IDG-HEK293T-CACNG5-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): mental disorder