Details of the Target

General Information of Target

Target ID LDTP00308
Target Name Voltage-dependent P/Q-type calcium channel subunit alpha-1A (CACNA1A)
Gene Name CACNA1A
Gene ID 773
Synonyms
CACH4; CACN3; CACNL1A4; Voltage-dependent P/Q-type calcium channel subunit alpha-1A; Brain calcium channel I; BI; Calcium channel, L type, alpha-1 polypeptide isoform 4; Voltage-gated calcium channel subunit alpha Cav2.1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MARFGDEMPARYGGGGSGAAAGVVVGSGGGRGAGGSRQGGQPGAQRMYKQSMAQRARTMA
LYNPIPVRQNCLTVNRSLFLFSEDNVVRKYAKKITEWPPFEYMILATIIANCIVLALEQH
LPDDDKTPMSERLDDTEPYFIGIFCFEAGIKIIALGFAFHKGSYLRNGWNVMDFVVVLTG
ILATVGTEFDLRTLRAVRVLRPLKLVSGIPSLQVVLKSIMKAMIPLLQIGLLLFFAILIF
AIIGLEFYMGKFHTTCFEEGTDDIQGESPAPCGTEEPARTCPNGTKCQPYWEGPNNGITQ
FDNILFAVLTVFQCITMEGWTDLLYNSNDASGNTWNWLYFIPLIIIGSFFMLNLVLGVLS
GEFAKERERVENRRAFLKLRRQQQIERELNGYMEWISKAEEVILAEDETDGEQRHPFDAL
RRTTIKKSKTDLLNPEEAEDQLADIASVGSPFARASIKSAKLENSTFFHKKERRMRFYIR
RMVKTQAFYWTVLSLVALNTLCVAIVHYNQPEWLSDFLYYAEFIFLGLFMSEMFIKMYGL
GTRPYFHSSFNCFDCGVIIGSIFEVIWAVIKPGTSFGISVLRALRLLRIFKVTKYWASLR
NLVVSLLNSMKSIISLLFLLFLFIVVFALLGMQLFGGQFNFDEGTPPTNFDTFPAAIMTV
FQILTGEDWNEVMYDGIKSQGGVQGGMVFSIYFIVLTLFGNYTLLNVFLAIAVDNLANAQ
ELTKDEQEEEEAANQKLALQKAKEVAEVSPLSAANMSIAVKEQQKNQKPAKSVWEQRTSE
MRKQNLLASREALYNEMDPDERWKAAYTRHLRPDMKTHLDRPLVVDPQENRNNNTNKSRA
AEPTVDQRLGQQRAEDFLRKQARYHDRARDPSGSAGLDARRPWAGSQEAELSREGPYGRE
SDHHAREGSLEQPGFWEGEAERGKAGDPHRRHVHRQGGSRESRSGSPRTGADGEHRRHRA
HRRPGEEGPEDKAERRARHREGSRPARGGEGEGEGPDGGERRRRHRHGAPATYEGDARRE
DKERRHRRRKENQGSGVPVSGPNLSTTRPIQQDLGRQDPPLAEDIDNMKNNKLATAESAA
PHGSLGHAGLPQSPAKMGNSTDPGPMLAIPAMATNPQNAASRRTPNNPGNPSNPGPPKTP
ENSLIVTNPSGTQTNSAKTARKPDHTTVDIPPACPPPLNHTVVQVNKNANPDPLPKKEEE
KKEEEEDDRGEDGPKPMPPYSSMFILSTTNPLRRLCHYILNLRYFEMCILMVIAMSSIAL
AAEDPVQPNAPRNNVLRYFDYVFTGVFTFEMVIKMIDLGLVLHQGAYFRDLWNILDFIVV
SGALVAFAFTGNSKGKDINTIKSLRVLRVLRPLKTIKRLPKLKAVFDCVVNSLKNVFNIL
IVYMLFMFIFAVVAVQLFKGKFFHCTDESKEFEKDCRGKYLLYEKNEVKARDREWKKYEF
HYDNVLWALLTLFTVSTGEGWPQVLKHSVDATFENQGPSPGYRMEMSIFYVVYFVVFPFF
FVNIFVALIIITFQEQGDKMMEEYSLEKNERACIDFAISAKPLTRHMPQNKQSFQYRMWQ
FVVSPPFEYTIMAMIALNTIVLMMKFYGASVAYENALRVFNIVFTSLFSLECVLKVMAFG
ILNYFRDAWNIFDFVTVLGSITDILVTEFGNNFINLSFLRLFRAARLIKLLRQGYTIRIL
LWTFVQSFKALPYVCLLIAMLFFIYAIIGMQVFGNIGIDVEDEDSDEDEFQITEHNNFRT
FFQALMLLFRSATGEAWHNIMLSCLSGKPCDKNSGILTRECGNEFAYFYFVSFIFLCSFL
MLNLFVAVIMDNFEYLTRDSSILGPHHLDEYVRVWAEYDPAAWGRMPYLDMYQMLRHMSP
PLGLGKKCPARVAYKRLLRMDLPVADDNTVHFNSTLMALIRTALDIKIAKGGADKQQMDA
ELRKEMMAIWPNLSQKTLDLLVTPHKSTDLTVGKIYAAMMIMEYYRQSKAKKLQAMREEQ
DRTPLMFQRMEPPSPTQEGGPGQNALPSTQLDPGGALMAHESGLKESPSWVTQRAQEMFQ
KTGTWSPEQGPPTDMPNSQPNSQSVEMREMGRDGYSDSEHYLPMEGQGRAASMPRLPAEN
QRRRGRPRGNNLSTISDTSPMKRSASVLGPKARRLDDYSLERVPPEENQRHHQRRRDRSH
RASERSLGRYTDVDTGLGTDLSMTTQSGDLPSKERDQERGRPKDRKHRQHHHHHHHHHHP
PPPDKDRYAQERPDHGRARARDQRWSRSPSEGREHMAHRQGSSSVSGSPAPSTSGTSTPR
RGRRQLPQTPSTPRPHVSYSPVIRKAGGSGPPQQQQQQQQQQQQQAVARPGRAATSGPRR
YPGPTAEPLAGDRPPTGGHSSGRSPRMERRVPGPARSESPRACRHGGARWPASGPHVSEG
PPGPRHHGYYRGSDYDEADGPGSGGGEEAMAGAYDAPPPVRHASSGATGRSPRTPRASGP
ACASPSRHGRRLPNGYYPAHGLARPRGPGSRKGLHEPYSESDDDWC
Target Type
Successful
Target Bioclass
Transporter and channel
Family
Calcium channel alpha-1 subunit (TC 1.A.1.11) family, CACNA1A subfamily
Subcellular location
Cell membrane
Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1A gives rise to P and/or Q-type calcium currents. P/Q-type calcium channels belong to the 'high-voltage activated' (HVA) group and are specifically blocked by the spider omega-agatoxin-IVA (AC P54282). They are however insensitive to dihydropyridines (DHP).
TTD ID
T34949
Uniprot ID
O00555
DrugMap ID
TTX4QDJ
Ensemble ID
ENST00000360228.11
HGNC ID
HGNC:1388
ChEMBL ID
CHEMBL4266

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Jackson_1
 Probe Info  		20.00  LDD0122  [1]
DBIA
 Probe Info  		C2462(1.86)  LDD3339  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A-549 C2462(1.70)  LDD2260  [2]
 LDCM0023  KB03 A-549 C2462(1.35)  LDD2677  [2]
 LDCM0024  KB05 NALM-6 C2462(1.86)  LDD3339  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Casein kinase II subunit beta (CSNK2B) Casein kinase 2 subunit beta family P67870
Cytochrome b-c1 complex subunit 2, mitochondrial (UQCRC2) Peptidase M16 family P22695
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Peripheral-type benzodiazepine receptor-associated protein 1 (TSPOAP1) RIMBP family O95153
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Zinc finger protein 40 (HIVEP1) . P15822
GPCR
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Adhesion G protein-coupled receptor L1 (ADGRL1) G-protein coupled receptor 2 family O94910
Immunoglobulin
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amphoterin-induced protein 2 (AMIGO2) AMIGO family Q86SJ2
Other
Click To Hide/Show 12 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Abl interactor 1 (ABI1) ABI family Q8IZP0
Progranulin (GRN) Granulin family P28799
Latent-transforming growth factor beta-binding protein 4 (LTBP4) LTBP family Q8N2S1
Poly(U)-binding-splicing factor PUF60 (PUF60) RRM half pint family Q9UHX1
Tubulin beta-2B chain (TUBB2B) Tubulin family Q9BVA1
DnaJ homolog subfamily B member 5 (DNAJB5) . O75953
Matrilin-2 (MATN2) . O00339
Multiple epidermal growth factor-like domains protein 6 (MEGF6) . O75095
Multiple epidermal growth factor-like domains protein 8 (MEGF8) . Q7Z7M0
Rho GTPase-activating protein 22 (ARHGAP22) . Q7Z5H3
RNA-binding protein 12B (RBM12B) . Q8IXT5
YLP motif-containing protein 1 (YLPM1) . P49750

The Drug(s) Related To This Target

Approved
Click To Hide/Show 20 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bepridil Small molecular drug DB01244
Calcium Phosphate Small molecular drug DB11348
Calcium Phosphate Dihydrate Small molecular drug DB14481
Drotaverine Small molecular drug DB06751
Enflurane Small molecular drug DB00228
Ergocalciferol Small molecular drug DB00153
Flunarizine Small molecular drug D05CEU
Levomenthol Small molecular drug DB00825
Loperamide Small molecular drug DB00836
Manidipine Small molecular drug DB09238
Nicardipine Small molecular drug DB00622
Nitrendipine Small molecular drug DB01054
Phenytoin Small molecular drug DB00252
Spironolactone Small molecular drug DB00421
Trimebutine Small molecular drug DB09089
Verapamil Small molecular drug DB00661
Ziconotide Small molecular drug DB06283
Bioallethrin . DB13746
Butamben . DB11148
Calcium Citrate . DB11093
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Xen007 . D0A3MJ
Investigative
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Alpha-eudesmol Small molecular drug D0N1MY
Cilnidipine Small molecular drug DB09232
Cpu-228 Small molecular drug D09YTH
Dotarizine Small molecular drug DB06446
Omega-conotoxin Gvia Small molecular drug D09LRA
Benidipine . DB09231
Efonidipine . DB09235
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Th-9229 . D0QQ7N

References

1 Appendage and Scaffold Diverse Fully Functionalized Small-Molecule Probes via a Minimalist Terminal Alkyne-Aliphatic Diazirine Isocyanide. J Org Chem. 2018 Sep 21;83(18):11245-11253. doi: 10.1021/acs.joc.8b01831. Epub 2018 Aug 31.
2 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840