CACNG6
gene geneOn this page
Summary
CACNG6 (calcium voltage-gated channel auxiliary subunit gamma 6, HGNC:13625) is a protein-coding gene on chromosome 19q13.42, encoding Voltage-dependent calcium channel gamma-6 subunit (Q9BXT2). Regulates the activity of L-type calcium channels that contain CACNA1C as pore-forming subunit.
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 an integral membrane protein that is thought to stabilize the calcium channel in an inactive (closed) state. 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). Alternative splicing results in multiple transcript variants. Variants in this gene have been associated with aspirin-intolerant asthma.
Source: NCBI Gene 59285 — RefSeq curated summary.
At a glance
- Clinical variants (ClinVar): 69 total — 1 pathogenic
- Druggable target: yes — 2 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_145814
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:13625 |
| Approved symbol | CACNG6 |
| Name | calcium voltage-gated channel auxiliary subunit gamma 6 |
| Location | 19q13.42 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000130433 |
| Ensembl biotype | protein_coding |
| OMIM | 606898 |
| Entrez | 59285 |
Gene structure
Transcript identifiers
Ensembl transcripts: 4 — 4 protein_coding
ENST00000252729, ENST00000346968, ENST00000352529, ENST00000955412
RefSeq mRNA: 3 — MANE Select: NM_145814
NM_031897, NM_145814, NM_145815
CCDS: CCDS12870, CCDS12871
Canonical transcript exons
ENST00000252729 — 4 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000895267 | 53999634 | 53999771 |
| ENSE00000895269 | 53998239 | 53998313 |
| ENSE00001854002 | 54011951 | 54012666 |
| ENSE00003915662 | 53991637 | 53993208 |
Expression profiles
Bgee: expression breadth ubiquitous, 124 present calls, max score 93.29.
FANTOM5 (CAGE): breadth broad, TPM avg 0.5243 / max 49.8471, expressed in 191 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 177458 | 0.4603 | 173 |
| 177459 | 0.0640 | 25 |
Top tissues by expression
216 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| hindlimb stylopod muscle | UBERON:0004252 | 93.29 | gold quality |
| gastrocnemius | UBERON:0001388 | 93.15 | gold quality |
| muscle of leg | UBERON:0001383 | 91.32 | gold quality |
| skeletal muscle tissue of rectus abdominis | UBERON:0004511 | 88.16 | gold quality |
| sperm | CL:0000019 | 87.45 | silver quality |
| right uterine tube | UBERON:0001302 | 87.07 | gold quality |
| tibialis anterior | UBERON:0001385 | 86.63 | silver quality |
| olfactory segment of nasal mucosa | UBERON:0005386 | 84.48 | gold quality |
| skeletal muscle tissue | UBERON:0001134 | 83.62 | gold quality |
| mucosa of paranasal sinus | UBERON:0005030 | 82.48 | silver quality |
| superficial temporal artery | UBERON:0001614 | 81.07 | gold quality |
| quadriceps femoris | UBERON:0001377 | 78.59 | silver quality |
| vastus lateralis | UBERON:0001379 | 77.61 | silver quality |
| deltoid | UBERON:0001476 | 77.54 | silver quality |
| biceps brachii | UBERON:0001507 | 77.04 | gold quality |
| muscle tissue | UBERON:0002385 | 76.69 | gold quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 75.00 | silver quality |
| oocyte | CL:0000023 | 73.26 | silver quality |
| bronchial epithelial cell | CL:0002328 | 72.97 | gold quality |
| upper leg skin | UBERON:0004262 | 72.67 | gold quality |
| bronchus | UBERON:0002185 | 72.30 | gold quality |
| nasal cavity mucosa | UBERON:0001826 | 70.69 | gold quality |
| gingival epithelium | UBERON:0001949 | 68.74 | gold quality |
| skin of hip | UBERON:0001554 | 67.74 | gold quality |
| gingiva | UBERON:0001828 | 65.41 | gold quality |
| nasal cavity epithelium | UBERON:0005384 | 64.93 | gold quality |
| right lung | UBERON:0002167 | 63.37 | gold quality |
| body of tongue | UBERON:0011876 | 63.22 | gold quality |
| cardia of stomach | UBERON:0001162 | 62.65 | silver quality |
| germinal epithelium of ovary | UBERON:0001304 | 62.40 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 2.08 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
29 targeting CACNG6, 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-4510 | 100.00 | 66.60 | 2050 |
| HSA-MIR-6127 | 100.00 | 66.76 | 2188 |
| HSA-MIR-6129 | 100.00 | 66.46 | 2080 |
| HSA-MIR-6130 | 100.00 | 66.69 | 2012 |
| HSA-MIR-6133 | 100.00 | 66.48 | 2064 |
| HSA-MIR-3919 | 99.87 | 69.45 | 2489 |
| HSA-MIR-7110-5P | 99.80 | 67.84 | 1712 |
| HSA-MIR-4516 | 99.61 | 67.78 | 3390 |
| HSA-MIR-6751-5P | 99.56 | 64.99 | 1145 |
| HSA-MIR-513A-3P | 99.39 | 70.63 | 3620 |
| HSA-MIR-513C-3P | 99.39 | 70.63 | 3620 |
| HSA-MIR-6803-5P | 99.19 | 63.90 | 1026 |
| HSA-MIR-6760-5P | 98.87 | 66.73 | 1515 |
| HSA-MIR-7851-3P | 98.72 | 64.88 | 980 |
| HSA-MIR-4700-5P | 98.63 | 67.43 | 1915 |
| HSA-MIR-6878-5P | 98.49 | 67.91 | 2142 |
| HSA-MIR-4691-3P | 98.11 | 66.83 | 1204 |
| HSA-MIR-204-3P | 97.80 | 66.84 | 1656 |
| HSA-MIR-4733-5P | 97.75 | 67.44 | 866 |
| HSA-MIR-8089 | 97.74 | 66.21 | 1698 |
| HSA-MIR-296-5P | 97.61 | 64.02 | 851 |
| HSA-MIR-4667-5P | 97.61 | 66.67 | 1683 |
| HSA-MIR-493-3P | 97.50 | 66.44 | 731 |
| HSA-MIR-558 | 97.50 | 67.16 | 977 |
| HSA-MIR-3184-3P | 96.96 | 66.91 | 845 |
| HSA-MIR-3059-3P | 96.71 | 67.08 | 606 |
| HSA-MIR-3675-5P | 95.90 | 65.80 | 474 |
| HSA-MIR-6835-5P | 95.81 | 64.27 | 500 |
| HSA-MIR-1282 | 91.07 | 71.26 | 99 |
Literature-anchored findings (GeneRIF, showing 2)
- CACNG6 variants might be associated with the risk of aspirin-intolerant asthma in a Korean population. (PMID:20860846)
- 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
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | cacng6a | ENSDARG00000036457 |
| danio_rerio | cacng6b | ENSDARG00000046079 |
| mus_musculus | Cacng6 | ENSMUSG00000078815 |
| rattus_norvegicus | Cacng6 | ENSRNOG00000063051 |
Paralogs (1): CACNG1 (ENSG00000108878)
Protein
Protein identifiers
Voltage-dependent calcium channel gamma-6 subunit — Q9BXT2 (reviewed: Q9BXT2)
Alternative names: Neuronal voltage-gated calcium channel gamma-6 subunit
All UniProt accessions (3): Q9BXT2, A6NFR2, A6NP74
UniProt curated annotations — full annotation on UniProt →
Function. Regulates the activity of L-type calcium channels that contain CACNA1C as pore-forming subunit.
Subunit / interactions. Interacts with CACNA1C. Identified in a complex with the L-type calcium channel subunits CACNA1C, CACNA2D1 and either CACNB1 or CACNB2.
Subcellular location. Cell membrane.
Tissue specificity. Detected in heart left ventricle.
Similarity. Belongs to the PMP-22/EMP/MP20 family. CACNG subfamily.
RefSeq proteins (3): NP_114103, NP_665813, NP_665814 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR004031 | PMP22/EMP/MP20/Claudin | Family |
| IPR008368 | VDCC_gsu | Family |
| IPR008370 | VDCC_g6su | Family |
Pfam: PF13903
UniProt features (8 total): transmembrane region 4, chain 1, region of interest 1, compositionally biased region 1, sequence variant 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9BXT2-F1 | 76.94 | 0.30 |
Function
Pathways and Gene Ontology
Reactome pathways
4 pathways
| ID | Pathway |
|---|---|
| R-HSA-5576892 | Phase 0 - rapid depolarisation |
| R-HSA-5576893 | Phase 2 - plateau phase |
| R-HSA-397014 | Muscle contraction |
| R-HSA-5576891 | Cardiac conduction |
MSigDB gene sets: 93 (showing top):
KEGG_MAPK_SIGNALING_PATHWAY, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_REGULATION_OF_CALCIUM_ION_TRANSMEMBRANE_TRANSPORT, ROZANOV_MMP14_TARGETS_UP, GOBP_REGULATION_OF_TRANSPORT, GOBP_CALCIUM_ION_TRANSMEMBRANE_TRANSPORT, GOBP_REGULATION_OF_MONOATOMIC_ION_TRANSPORT, GOBP_TRANSMEMBRANE_TRANSPORT, KEGG_ARRHYTHMOGENIC_RIGHT_VENTRICULAR_CARDIOMYOPATHY_ARVC, AP4_01, GOBP_REGULATION_OF_TRANSMEMBRANE_TRANSPORT, GOCC_VOLTAGE_GATED_CALCIUM_CHANNEL_COMPLEX, GOCC_CATION_CHANNEL_COMPLEX, GOCC_TRANSPORTER_COMPLEX, GOCC_MEMBRANE_PROTEIN_COMPLEX
GO Biological Process (5): calcium ion transport (GO:0006816), regulation of calcium ion transmembrane transport via high voltage-gated calcium channel (GO:1902514), monoatomic ion transport (GO:0006811), monoatomic ion transmembrane transport (GO:0034220), calcium ion transmembrane transport (GO:0070588)
GO Molecular Function (3): voltage-gated calcium channel activity (GO:0005245), calcium channel regulator activity (GO:0005246), calcium channel activity (GO:0005262)
GO Cellular Component (5): plasma membrane (GO:0005886), voltage-gated calcium channel complex (GO:0005891), 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-2 pathways:
| Category | Pathways |
|---|---|
| Cardiac conduction | 2 |
| Muscle contraction | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| calcium channel activity | 2 |
| metal ion transport | 1 |
| calcium ion transmembrane transport via high voltage-gated calcium channel | 1 |
| regulation of calcium ion transmembrane transport | 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 |
| monoatomic cation channel activity | 1 |
| calcium ion transmembrane transporter activity | 1 |
| membrane | 1 |
| cell periphery | 1 |
| calcium channel complex | 1 |
| plasma membrane protein complex | 1 |
| voltage-gated calcium channel complex | 1 |
| T-tubule | 1 |
| cellular anatomical structure | 1 |
| transmembrane transporter complex | 1 |
Protein interactions and networks
STRING
357 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CACNG6 | CACNB4 | O00305 | 503 |
| CACNG6 | CACNA2D3 | Q8IZS8 | 487 |
| CACNG6 | CACNB2 | Q08289 | 486 |
| CACNG6 | ATP2A1 | O14983 | 474 |
| CACNG6 | KCNS2 | Q9ULS6 | 356 |
| CACNG6 | LRTM1 | Q9HBL6 | 353 |
| CACNG6 | FSIP1 | Q8NA03 | 324 |
| CACNG6 | ILDR2 | Q71H61 | 311 |
| CACNG6 | KCNK15 | Q9H427 | 309 |
| CACNG6 | KCNA7 | Q96RP8 | 301 |
| CACNG6 | TCTN3 | Q6NUS6 | 300 |
| CACNG6 | KCNU1 | A8MYU2 | 275 |
| CACNG6 | KCNK13 | Q9HB14 | 273 |
| CACNG6 | BAIAP3 | O94812 | 272 |
| CACNG6 | PLA2G4E | Q3MJ16 | 272 |
IntAct
5 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CACNG6 | HSPD1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| TMEM223 | psi-mi:“MI:0914”(association) | 0.350 | |
| PRR27 | VWA8 | psi-mi:“MI:0914”(association) | 0.350 |
| CACNG6 | TSPAN3 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (34): CACNG6 (Affinity Capture-MS), CACNG6 (Proximity Label-MS), CDS1 (Affinity Capture-MS), SLC5A3 (Affinity Capture-MS), CACNG6 (Affinity Capture-MS), FITM2 (Affinity Capture-MS), TNPO3 (Affinity Capture-MS), MSMO1 (Affinity Capture-MS), XPO6 (Affinity Capture-MS), SLC7A2 (Affinity Capture-MS), GOLGA5 (Affinity Capture-MS), MFSD5 (Affinity Capture-MS), SLC38A3 (Affinity Capture-MS), LGALS3 (Affinity Capture-MS), TTYH3 (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: O70578, P19518, P97707, Q06432, Q08DE1, Q2MJQ7, Q8VHW3, Q8VHW7, Q9BXT2
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
69 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 1 |
| Likely pathogenic | 0 |
| Uncertain significance | 61 |
| Likely benign | 1 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (1)
| Variant ID | HGVS | Classification |
|---|---|---|
| 253434 | GRCh37/hg19 19q13.42(chr19:54280799-54635178)x1 | Pathogenic |
SpliceAI
636 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 19:53998228:T:A | acceptor_gain | 1.0000 |
| 19:53998237:A:AG | acceptor_gain | 1.0000 |
| 19:53998238:G:GA | acceptor_gain | 1.0000 |
| 19:53998238:GA:G | acceptor_gain | 1.0000 |
| 19:53998238:GAA:G | acceptor_gain | 1.0000 |
| 19:53998238:GAAGC:G | acceptor_gain | 1.0000 |
| 19:53998309:GAAAG:G | donor_gain | 1.0000 |
| 19:53998314:G:T | donor_loss | 1.0000 |
| 19:54011945:CCGCA:C | acceptor_loss | 1.0000 |
| 19:54011946:CGCAG:C | acceptor_loss | 1.0000 |
| 19:54011947:GCA:G | acceptor_loss | 1.0000 |
| 19:54011948:CAGG:C | acceptor_loss | 1.0000 |
| 19:54011949:A:AC | acceptor_loss | 1.0000 |
| 19:54011949:A:AG | acceptor_gain | 1.0000 |
| 19:54011950:G:GT | acceptor_gain | 1.0000 |
| 19:54011950:GGC:G | acceptor_gain | 1.0000 |
| 19:54011950:GGCCT:G | acceptor_gain | 1.0000 |
| 19:53999625:T:TA | acceptor_gain | 0.9900 |
| 19:54011946:C:A | acceptor_gain | 0.9900 |
| 19:54011949:AG:A | acceptor_gain | 0.9900 |
| 19:54011950:GG:G | acceptor_gain | 0.9900 |
| 19:54011950:GGCC:G | acceptor_gain | 0.9900 |
| 19:53998236:C:G | acceptor_gain | 0.9800 |
| 19:53999628:T:A | acceptor_gain | 0.9800 |
| 19:53999631:CAG:C | acceptor_gain | 0.9800 |
| 19:53999632:AGA:A | acceptor_gain | 0.9800 |
| 19:53999633:GAG:G | acceptor_gain | 0.9800 |
| 19:53999725:TGCA:T | donor_gain | 0.9800 |
| 19:53999726:GCAG:G | donor_gain | 0.9800 |
| 19:53999767:CTCAG:C | donor_loss | 0.9800 |
AlphaMissense
1631 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 19:53993129:G:C | W84C | 0.996 |
| 19:53993129:G:T | W84C | 0.996 |
| 19:53993127:T:A | W84R | 0.995 |
| 19:53993127:T:C | W84R | 0.995 |
| 19:53993058:T:C | F61L | 0.994 |
| 19:53993060:C:A | F61L | 0.994 |
| 19:53993060:C:G | F61L | 0.994 |
| 19:53993144:G:C | K89N | 0.992 |
| 19:53993144:G:T | K89N | 0.992 |
| 19:53993184:T:A | C103S | 0.992 |
| 19:53993185:G:A | C103Y | 0.992 |
| 19:53993185:G:C | C103S | 0.992 |
| 19:53998247:T:A | C114S | 0.991 |
| 19:53998248:G:C | C114S | 0.991 |
| 19:54011968:A:C | S188R | 0.991 |
| 19:54011970:C:A | S188R | 0.991 |
| 19:54011970:C:G | S188R | 0.991 |
| 19:53993137:G:A | C87Y | 0.990 |
| 19:53993138:C:G | C87W | 0.990 |
| 19:53993184:T:C | C103R | 0.989 |
| 19:53998248:G:A | C114Y | 0.989 |
| 19:53993121:G:A | G82R | 0.988 |
| 19:53993121:G:C | G82R | 0.988 |
| 19:53993122:G:A | G82E | 0.988 |
| 19:53998249:C:G | C114W | 0.988 |
| 19:53993187:G:T | G104C | 0.987 |
| 19:53998257:T:G | F117C | 0.987 |
| 19:53993022:G:C | G49R | 0.986 |
| 19:53993063:G:C | W62C | 0.986 |
| 19:53993063:G:T | W62C | 0.986 |
dbSNP variants (sampled 300 via entrez): RS1000047377 (19:53999673 T>C), RS1000190008 (19:54006620 C>T), RS1000201341 (19:54006233 G>C), RS1000240971 (19:53991552 G>T), RS1000355786 (19:54012557 C>T), RS1000397291 (19:53999994 G>A), RS1000486907 (19:53996784 T>C), RS1000524202 (19:54004669 C>G), RS1000535634 (19:54004464 C>A,G,T), RS1000598830 (19:54011560 A>T), RS1000711919 (19:54002082 T>G), RS1000744436 (19:54002266 G>A,T), RS1000946960 (19:54006844 TTATTTTGTTA>T), RS1000992544 (19:53995890 G>C), RS1001094663 (19:54010944 T>C)
Disease associations
OMIM: gene MIM:606898 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
0 associations (top):
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
29 total (human), top 29 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Benzo(a)pyrene | affects methylation, decreases methylation | 2 |
| Cisplatin | increases expression, affects expression, affects cotreatment | 2 |
| Particulate Matter | decreases expression, increases abundance, affects expression | 2 |
| afuresertib | increases expression | 1 |
| methylethyl ketone | decreases expression | 1 |
| deoxynivalenol | decreases expression | 1 |
| 11-nor-delta(9)-tetrahydrocannabinol-9-carboxylic acid | affects methylation, increases abundance | 1 |
| tris(1,3-dichloro-2-propyl)phosphate | increases expression | 1 |
| sodium arsenite | decreases expression | 1 |
| butyraldehyde | decreases expression | 1 |
| benzo(e)pyrene | increases methylation | 1 |
| aflatoxin B2 | increases methylation | 1 |
| polyhexamethyleneguanidine | affects expression | 1 |
| CGP 52608 | increases reaction, affects binding | 1 |
| abrine | decreases expression | 1 |
| jinfukang | affects cotreatment, increases expression | 1 |
| (+)-JQ1 compound | decreases expression | 1 |
| Decitabine | affects expression | 1 |
| Air Pollutants | decreases expression, increases abundance | 1 |
| Aspirin | affects response to substance | 1 |
| Cannabinoids | increases abundance, affects methylation | 1 |
| Diethylhexyl Phthalate | decreases expression | 1 |
| Hydralazine | affects cotreatment, increases expression | 1 |
| Methapyrilene | increases methylation | 1 |
| Pesticides | increases methylation | 1 |
| Silicon Dioxide | decreases expression | 1 |
| Tobacco Smoke Pollution | decreases expression | 1 |
| Triclosan | decreases expression | 1 |
| Valproic Acid | affects cotreatment, increases 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
1 cell lines: 1 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_D7LF | Ubigene A-549 CACNG6 KO | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.