Details of the Target

General Information of Target

Target ID LDTP05968
Target Name Voltage-dependent L-type calcium channel subunit alpha-1S (CACNA1S)
Gene Name CACNA1S
Gene ID 779
Synonyms
CACH1; CACN1; CACNL1A3; Voltage-dependent L-type calcium channel subunit alpha-1S; Calcium channel, L type, alpha-1 polypeptide, isoform 3, skeletal muscle; Voltage-gated calcium channel subunit alpha Cav1.1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEPSSPQDEGLRKKQPKKPVPEILPRPPRALFCLTLENPLRKACISIVEWKPFETIILLT
IFANCVALAVYLPMPEDDNNSLNLGLEKLEYFFLIVFSIEAAMKIIAYGFLFHQDAYLRS
GWNVLDFTIVFLGVFTVILEQVNVIQSHTAPMSSKGAGLDVKALRAFRVLRPLRLVSGVP
SLQVVLNSIFKAMLPLFHIALLVLFMVIIYAIIGLELFKGKMHKTCYFIGTDIVATVENE
EPSPCARTGSGRRCTINGSECRGGWPGPNHGITHFDNFGFSMLTVYQCITMEGWTDVLYW
VNDAIGNEWPWIYFVTLILLGSFFILNLVLGVLSGEFTKEREKAKSRGTFQKLREKQQLD
EDLRGYMSWITQGEVMDVEDFREGKLSLDEGGSDTESLYEIAGLNKIIQFIRHWRQWNRI
FRWKCHDIVKSKVFYWLVILIVALNTLSIASEHHNQPLWLTRLQDIANRVLLSLFTTEML
MKMYGLGLRQYFMSIFNRFDCFVVCSGILEILLVESGAMTPLGISVLRCIRLLRIFKITK
YWTSLSNLVASLLNSIRSIASLLLLLFLFIVIFALLGMQLFGGRYDFEDTEVRRSNFDNF
PQALISVFQVLTGEDWTSMMYNGIMAYGGPSYPGMLVCIYFIILFVCGNYILLNVFLAIA
VDNLAEAESLTSAQKAKAEEKKRRKMSKGLPDKSEEEKSTMAKKLEQKPKGEGIPTTAKL
KIDEFESNVNEVKDPYPSADFPGDDEEDEPEIPLSPRPRPLAELQLKEKAVPIPEASSFF
IFSPTNKIRVLCHRIVNATWFTNFILLFILLSSAALAAEDPIRADSMRNQILKHFDIGFT
SVFTVEIVLKMTTYGAFLHKGSFCRNYFNMLDLLVVAVSLISMGLESSAISVVKILRVLR
VLRPLRAINRAKGLKHVVQCMFVAISTIGNIVLVTTLLQFMFACIGVQLFKGKFFRCTDL
SKMTEEECRGYYYVYKDGDPMQIELRHREWVHSDFHFDNVLSAMMSLFTVSTFEGWPQLL
YKAIDSNAEDVGPIYNNRVEMAIFFIIYIILIAFFMMNIFVGFVIVTFQEQGETEYKNCE
LDKNQRQCVQYALKARPLRCYIPKNPYQYQVWYIVTSSYFEYLMFALIMLNTICLGMQHY
NQSEQMNHISDILNVAFTIIFTLEMILKLMAFKARGYFGDPWNVFDFLIVIGSIIDVILS
EIDTFLASSGGLYCLGGGCGNVDPDESARISSAFFRLFRVMRLIKLLSRAEGVRTLLWTF
IKSFQALPYVALLIVMLFFIYAVIGMQMFGKIALVDGTQINRNNNFQTFPQAVLLLFRCA
TGEAWQEILLACSYGKLCDPESDYAPGEEYTCGTNFAYYYFISFYMLCAFLVINLFVAVI
MDNFDYLTRDWSILGPHHLDEFKAIWAEYDPEAKGRIKHLDVVTLLRRIQPPLGFGKFCP
HRVACKRLVGMNMPLNSDGTVTFNATLFALVRTALKIKTEGNFEQANEELRAIIKKIWKR
TSMKLLDQVIPPIGDDEVTVGKFYATFLIQEHFRKFMKRQEEYYGYRPKKDIVQIQAGLR
TIEEEAAPEICRTVSGDLAAEEELERAMVEAAMEEGIFRRTGGLFGQVDNFLERTNSLPP
VMANQRPLQFAEIEMEEMESPVFLEDFPQDPRTNPLARANTNNANANVAYGNSNHSNSHV
FSSVHYEREFPEETETPATRGRALGQPCRVLGPHSKPCVEMLKGLLTQRAMPRGQAPPAP
CQCPRVESSMPEDRKSSTPGSLHEETPHSRSTRENTSRCSAPATALLIQKALVRGGLGTL
AADANFIMATGQALADACQMEPEEVEIMATELLKGREAPEGMASSLGCLNLGSSLGSLDQ
HQGSQETLIPPRL
Target Type
Literature-reported
Target Bioclass
Transporter and channel
Family
Calcium channel alpha-1 subunit (TC 1.A.1.11) family, CACNA1S subfamily
Subcellular location
Cell membrane, sarcolemma, T-tubule
Function
Pore-forming, alpha-1S subunit of the voltage-gated calcium channel that gives rise to L-type calcium currents in skeletal muscle. Calcium channels containing the alpha-1S subunit play an important role in excitation-contraction coupling in skeletal muscle via their interaction with RYR1, which triggers Ca(2+) release from the sarcoplasmic reticulum and ultimately results in muscle contraction. Long-lasting (L-type) calcium channels belong to the 'high-voltage activated' (HVA) group.
TTD ID
T24965
Uniprot ID
Q13698
DrugMap ID
TT94HRF
Ensemble ID
ENST00000362061.4
HGNC ID
HGNC:1397
ChEMBL ID
CHEMBL3805

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Acrolein
 Probe Info  		N.A.  LDD0217  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0107  IAA HeLa N.A.  LDD0221  [1]
 LDCM0109  NEM HeLa N.A.  LDD0224  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Poly [ADP-ribose] polymerase tankyrase-2 (TNKS2) ARTD/PARP family Q9H2K2
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cysteine-rich tail protein 1 (CYSRT1) CYSRT1 family A8MQ03
Coiled-coil domain-containing protein 106 (CCDC106) . Q9BWC9
Na(+)/H(+) exchange regulatory cofactor NHE-RF4 (NHERF4) . Q86UT5

The Drug(s) Related To This Target

Approved
Click To Hide/Show 32 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Amiodarone Small molecular drug DB01118
Calcium Phosphate Small molecular drug DB11348
Calcium Phosphate Dihydrate Small molecular drug DB14481
Cinnarizine Small molecular drug DB00568
Clevidipine Small molecular drug DB04920
Dronedarone Small molecular drug DB04855
Drotaverine Small molecular drug DB06751
Enflurane Small molecular drug DB00228
Ergocalciferol Small molecular drug DB00153
Ethanol Small molecular drug DB00898
Felodipine Small molecular drug DB01023
Isradipine Small molecular drug DB00270
Levomenthol Small molecular drug DB00825
Manidipine Small molecular drug DB09238
Miconazole Small molecular drug DB01110
Nicardipine Small molecular drug DB00622
Nifedipine Small molecular drug DB01115
Nilvadipine Small molecular drug DB06712
Nimodipine Small molecular drug DB00393
Nisoldipine Small molecular drug DB00401
Nitrendipine Small molecular drug DB01054
Phenytoin Small molecular drug DB00252
Ranolazine Small molecular drug DB00243
Spironolactone Small molecular drug DB00421
Topiramate Small molecular drug DB00273
Trimebutine Small molecular drug DB09089
Verapamil Small molecular drug DB00661
Bioallethrin . DB13746
Butamben . DB11148
Calcium Citrate . DB11093
Fish Oil . DB13961
Pinaverium . DB09090
Investigative
Click To Hide/Show 11 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(-)-(S)-bayk8644 Small molecular drug D02RIH
Cilnidipine Small molecular drug DB09232
Fpl64176 Small molecular drug D06XTT
Mibefradil Small molecular drug DB01388
Sz(+)-(S)-202-791 Small molecular drug D0U7BI
[3h](+)-cis-diltiazem Small molecular drug D04ALU
[3h](+)-isradipine Small molecular drug D0S3YP
[3h](-)Devapamil Small molecular drug D03UJT
Aranidipine . DB09229
Benidipine . DB09231
Efonidipine . DB09235

References

1 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.