Details of the Target

General Information of Target

Target ID LDTP01517
Target Name Voltage-dependent T-type calcium channel subunit alpha-1H (CACNA1H)
Gene Name CACNA1H
Gene ID 8912
Synonyms
Voltage-dependent T-type calcium channel subunit alpha-1H; Low-voltage-activated calcium channel alpha1 3.2 subunit; Voltage-gated calcium channel subunit alpha Cav3.2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTEGARAADEVRVPLGAPPPGPAALVGASPESPGAPGREAERGSELGVSPSESPAAERGA
ELGADEEQRVPYPALAATVFFCLGQTTRPRSWCLRLVCNPWFEHVSMLVIMLNCVTLGMF
RPCEDVECGSERCNILEAFDAFIFAFFAVEMVIKMVALGLFGQKCYLGDTWNRLDFFIVV
AGMMEYSLDGHNVSLSAIRTVRVLRPLRAINRVPSMRILVTLLLDTLPMLGNVLLLCFFV
FFIFGIVGVQLWAGLLRNRCFLDSAFVRNNNLTFLRPYYQTEEGEENPFICSSRRDNGMQ
KCSHIPGRRELRMPCTLGWEAYTQPQAEGVGAARNACINWNQYYNVCRSGDSNPHNGAIN
FDNIGYAWIAIFQVITLEGWVDIMYYVMDAHSFYNFIYFILLIIVGSFFMINLCLVVIAT
QFSETKQRESQLMREQRARHLSNDSTLASFSEPGSCYEELLKYVGHIFRKVKRRSLRLYA
RWQSRWRKKVDPSAVQGQGPGHRQRRAGRHTASVHHLVYHHHHHHHHHYHFSHGSPRRPG
PEPGACDTRLVRAGAPPSPPSPGRGPPDAESVHSIYHADCHIEGPQERARVAHAAATAAA
SLRLATGLGTMNYPTILPSGVGSGKGSTSPGPKGKWAGGPPGTGGHGPLSLNSPDPYEKI
PHVVGEHGLGQAPGHLSGLSVPCPLPSPPAGTLTCELKSCPYCTRALEDPEGELSGSESG
DSDGRGVYEFTQDVRHGDRWDPTRPPRATDTPGPGPGSPQRRAQQRAAPGEPGWMGRLWV
TFSGKLRRIVDSKYFSRGIMMAILVNTLSMGVEYHEQPEELTNALEISNIVFTSMFALEM
LLKLLACGPLGYIRNPYNIFDGIIVVISVWEIVGQADGGLSVLRTFRLLRVLKLVRFLPA
LRRQLVVLVKTMDNVATFCTLLMLFIFIFSILGMHLFGCKFSLKTDTGDTVPDRKNFDSL
LWAIVTVFQILTQEDWNVVLYNGMASTSSWAALYFVALMTFGNYVLFNLLVAILVEGFQA
EGDANRSDTDEDKTSVHFEEDFHKLRELQTTELKMCSLAVTPNGHLEGRGSLSPPLIMCT
AATPMPTPKSSPFLDAAPSLPDSRRGSSSSGDPPLGDQKPPASLRSSPCAPWGPSGAWSS
RRSSWSSLGRAPSLKRRGQCGERESLLSGEGKGSTDDEAEDGRAAPGPRATPLRRAESLD
PRPLRPAALPPTKCRDRDGQVVALPSDFFLRIDSHREDAAELDDDSEDSCCLRLHKVLEP
YKPQWCRSREAWALYLFSPQNRFRVSCQKVITHKMFDHVVLVFIFLNCVTIALERPDIDP
GSTERVFLSVSNYIFTAIFVAEMMVKVVALGLLSGEHAYLQSSWNLLDGLLVLVSLVDIV
VAMASAGGAKILGVLRVLRLLRTLRPLRVISRAPGLKLVVETLISSLRPIGNIVLICCAF
FIIFGILGVQLFKGKFYYCEGPDTRNISTKAQCRAAHYRWVRRKYNFDNLGQALMSLFVL
SSKDGWVNIMYDGLDAVGVDQQPVQNHNPWMLLYFISFLLIVSFFVLNMFVGVVVENFHK
CRQHQEAEEARRREEKRLRRLERRRRSTFPSPEAQRRPYYADYSPTRRSIHSLCTSHYLD
LFITFIICVNVITMSMEHYNQPKSLDEALKYCNYVFTIVFVFEAALKLVAFGFRRFFKDR
WNQLDLAIVLLSLMGITLEEIEMSAALPINPTIIRIMRVLRIARVLKLLKMATGMRALLD
TVVQALPQVGNLGLLFMLLFFIYAALGVELFGRLECSEDNPCEGLSRHATFSNFGMAFLT
LFRVSTGDNWNGIMKDTLRECSREDKHCLSYLPALSPVYFVTFVLVAQFVLVNVVVAVLM
KHLEESNKEAREDAELDAEIELEMAQGPGSARRVDADRPPLPQESPGARDAPNLVARKVS
VSRMLSLPNDSYMFRPVVPASAPHPRPLQEVEMETYGAGTPLGSVASVHSPPAESCASLQ
IPLAVSSPARSGEPLHALSPRGTARSPSLSRLLCRQEAVHTDSLEGKIDSPRDTLDPAEP
GEKTPVRPVTQGGSLQSPPRSPRPASVRTRKHTFGQRCVSSRPAAPGGEEAEASDPADEE
VSHITSSACPWQPTAEPHGPEASPVAGGERDLRRLYSVDAQGFLDKPGRADEQWRPSAEL
GSGEPGEAKAWGPEAEPALGARRKKKMSPPCISVEPPAEDEGSARPSAAEGGSTTLRRRT
PSCEATPHRDSLEPTEGSGAGGDPAAKGERWGQASCRAEHLTVPSFAFEPLDLGVPSGDP
FLDGSHSVTPESRASSSGAIVPLEPPESEPPMPVGDPPEKRRGLYLTVPQCPLEKPGSPS
ATPAPGGGADDPV
Target Type
Successful
Target Bioclass
Transporter and channel
Family
Calcium channel alpha-1 subunit (TC 1.A.1.11) family, CACNA1H subfamily
Subcellular location
Cell membrane
Function
Voltage-sensitive calcium channel that gives rise to T-type calcium currents. T-type calcium channels belong to the 'low-voltage activated (LVA)' group. A particularity of this type of channel is an opening at quite negative potentials, and a voltage-dependent inactivation. T-type channels serve pacemaking functions in both central neurons and cardiac nodal cells and support calcium signaling in secretory cells and vascular smooth muscle (Probable). They may also be involved in the modulation of firing patterns of neurons. In the adrenal zona glomerulosa, participates in the signaling pathway leading to aldosterone production in response to either AGT/angiotensin II, or hyperkalemia.
TTD ID
T54644
Uniprot ID
O95180
DrugMap ID
TTZPWGN
Ensemble ID
ENST00000348261.11
HGNC ID
HGNC:1395
ChEMBL ID
CHEMBL1859

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
769P SNV: p.A900S .
A172 SNV: p.T1657I .
A498 SNV: p.G665V .
CCLP1 SNV: p.E1164G .
GB2 SNV: p.K1730N .
HCT15 SNV: p.T170K; p.G773C .
HEC1 SNV: p.R1482Ter .
HEC1B SNV: p.Y1004H .
HLF SNV: p.S455N .
HT SNV: p.V812A .
HT115 SNV: p.S475N .
IM95 Deletion: p.S558RfsTer25 .
Ishikawa (Heraklio) 02 ER SNV: p.V591E .
JHH4 Substitution: p.A1594F .
KPL1 SNV: p.M611I .
LOXIMVI SNV: p.D877N .
LUDLU1 SNV: p.F929L .
MCF7 SNV: p.M611I .
MEWO SNV: p.E729K .
MFE319 SNV: p.R1718C .
NCIH1666 SNV: p.I964L .
NCIH1993 SNV: p.S1110T; p.D1112G .
NCIN87 SNV: p.M151I .
OVK18 SNV: p.A1358V .
RKO SNV: p.F177L; p.V179F .
RL952 SNV: p.P18S; p.E31Ter; p.R761Q .
SKMEL2 SNV: p.N232S .
SKMEL30 SNV: p.A1081T .
SKNSH SNV: p.P100Q; p.P562Q .
SUIT2 SNV: p.P14S .
TOV21G Substitution: p.R1715D .
TYKNU SNV: p.M775L .
UACC257 SNV: p.W779Ter .

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.  LDD0222  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [1]
 LDCM0109  NEM HeLa N.A.  LDD0224  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 23 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
Cannabidiol Small molecular drug DB09061
Cinnarizine Small molecular drug DB00568
Enflurane Small molecular drug DB00228
Ergocalciferol Small molecular drug DB00153
Felodipine Small molecular drug DB01023
Flunarizine Small molecular drug D05CEU
Isradipine Small molecular drug DB00270
Manidipine Small molecular drug DB09238
Nicardipine Small molecular drug DB00622
Nifedipine Small molecular drug DB01115
Nilvadipine Small molecular drug DB06712
Nitrendipine Small molecular drug DB01054
Sodium Bicarbonate Small molecular drug D02FLB
Spironolactone Small molecular drug DB00421
Trimebutine Small molecular drug DB09089
Verapamil Small molecular drug DB00661
Zonisamide Small molecular drug DB00909
Bioallethrin . DB13746
Butamben . DB11148
Calcium Citrate . DB11093
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Abt-639 Small molecular drug D04TNT
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Mibefradil Small molecular drug D0W8XT
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tta-a8 Small molecular drug D0X5OV
Investigative
Click To Hide/Show 22 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cis-n,5-dibenzyl-6-oxomorpholine-3-carboxamide Small molecular drug D07UBR
Gnf-pf-1967 Small molecular drug D06HWI
Gnf-pf-4599 Small molecular drug D05NSP
Kys-05001 Small molecular drug D02DUO
Kys-05040 Small molecular drug D0S5QB
Kys-05050 Small molecular drug D0K5RX
Kys-05077 Small molecular drug D02SSG
Kys-05080 Small molecular drug D06UAX
Ml218 Small molecular drug D09PWJ
Nabiximols Small molecular drug DB14011
Aranidipine . DB09229
Barnidipine . DB09227
Benidipine . DB09231
Dp-3005 . D0TW1Q
Efonidipine . DB09235
Hyp-10 . D08NRG
Kst-5468 . D0YF6L
Kys-05041 . D0N5RQ
Kys-05042 . D0M2EZ
Medical Cannabis . DB14009
Ttl-1177 . D0Y5WL
Z 944 . D0T6NE
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
U-92032 Small molecular drug D0OW2O

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.