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Voltage-dependent L-type calcium channel subunit alpha-1C
Ligand
BDBM50566512
Substrate
n/a
Meas. Tech.
ChEMBL_2101023 (CHEMBL4809419)
IC50
>500000±n/a nM
Citation
Lapointe, G; Skepper, CK; Holder, LM; Armstrong, D; Bellamacina, C; Blais, J; Bussiere, D; Bian, J; Cepura, C; Chan, H; Dean, CR; De Pascale, G; Dhumale, B; Fisher, LM; Fulsunder, M; Kantariya, B; Kim, J; King, S; Kossy, L; Kulkarni, U; Lakshman, J; Leeds, JA; Ling, X; Lvov, A; Ma, S; Malekar, S; McKenney, D; Mergo, W; Metzger, L; Mhaske, K; Moser, HE; Mostafavi, M; Namballa, S; Noeske, J; Osborne, C; Patel, A; Patel, D; Patel, T; Piechon, P; Polyakov, V; Prajapati, K; Prosen, KR; Reck, F; Richie, DL; Sanderson, MR; Satasia, S; Savani, B; Selvarajah, J; Sethuraman, V; Shu, W; Tashiro, K; Thompson, KV; Vaarla, K; Vala, L; Veselkov, DA; Vo, J; Vora, B; Wagner, T; Wedel, L; Williams, SL; Yendluri, S; Yue, Q; Yifru, A; Zhang, Y; Rivkin, A Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria. J Med Chem 64:6329-6357 (2021) [PubMed] ArticleMore Info.:
Target
Name:
Voltage-dependent L-type calcium channel subunit alpha-1C
Synonyms:
CAC1C_HUMAN | CACH2 | CACN2 | CACNA1C | CACNL1A1 | CCHL1A1 | Calcium channel (Type L) | Calcium channel, L type, alpha-1 polypeptide, isoform 1, cardiac muscle | L-type calcium channel alpha-1c/beta-2/alpha2delta-1 | Voltage-dependent L-type calcium channel subunit alpha-1C | Voltage-gated L-type calcium channel | Voltage-gated L-type calcium channel alpha-1C subunit | Voltage-gated calcium channel | Voltage-gated calcium channel subunit alpha Cav1.2
Type:
Enzyme Catalytic Domain
Mol. Mass.:
248979.79
Organism:
Homo sapiens (Human)
Description:
Calcium channel (Type L) 0 HUMAN::Q13936
Residue:
2221
Sequence:
MVNENTRMYIPEENHQGSNYGSPRPAHANMNANAAAGLAPEHIPTPGAALSWQAAIDAARQAKLMGSAGNATISTVSSTQRKRQQYGKPKKQGSTTATRPPRALLCLTLKNPIRRACISIVEWKPFEIIILLTIFANCVALAIYIPFPEDDSNATNSNLERVEYLFLIIFTVEAFLKVIAYGLLFHPNAYLRNGWNLLDFIIVVVGLFSAILEQATKADGANALGGKGAGFDVKALRAFRVLRPLRLVSGVPSLQVVLNSIIKAMVPLLHIALLVLFVIIIYAIIGLELFMGKMHKTCYNQEGIADVPAEDDPSPCALETGHGRQCQNGTVCKPGWDGPKHGITNFDNFAFAMLTVFQCITMEGWTDVLYWVNDAVGRDWPWIYFVTLIIIGSFFVLNLVLGVLSGEFSKEREKAKARGDFQKLREKQQLEEDLKGYLDWITQAEDIDPENEDEGMDEEKPRNMSMPTSETESVNTENVAGGDIEGENCGARLAHRISKSKFSRYWRRWNRFCRRKCRAAVKSNVFYWLVIFLVFLNTLTIASEHYNQPNWLTEVQDTANKALLALFTAEMLLKMYSLGLQAYFVSLFNRFDCFVVCGGILETILVETKIMSPLGISVLRCVRLLRIFKITRYWNSLSNLVASLLNSVRSIASLLLLLFLFIIIFSLLGMQLFGGKFNFDEMQTRRSTFDNFPQSLLTVFQILTGEDWNSVMYDGIMAYGGPSFPGMLVCIYFIILFICGNYILLNVFLAIAVDNLADAESLTSAQKEEEEEKERKKLARTASPEKKQELVEKPAVGESKEEKIELKSITADGESPPATKINMDDLQPNENEDKSPYPNPETTGEEDEEEPEMPVGPRPRPLSELHLKEKAVPMPEASAFFIFSSNNRFRLQCHRIVNDTIFTNLILFFILLSSISLAAEDPVQHTSFRNHILFYFDIVFTTIFTIEIALKILGNADYVFTSIFTLEIILKMTAYGAFLHKGSFCRNYFNILDLLVVSVSLISFGIQSSAINVVKILRVLRVLRPLRAINRAKGLKHVVQCVFVAIRTIGNIVIVTTLLQFMFACIGVQLFKGKLYTCSDSSKQTEAECKGNYITYKDGEVDHPIIQPRSWENSKFDFDNVLAAMMALFTVSTFEGWPELLYRSIDSHTEDKGPIYNYRVEISIFFIIYIIIIAFFMMNIFVGFVIVTFQEQGEQEYKNCELDKNQRQCVEYALKARPLRRYIPKNQHQYKVWYVVNSTYFEYLMFVLILLNTICLAMQHYGQSCLFKIAMNILNMLFTGLFTVEMILKLIAFKPKGYFSDPWNVFDFLIVIGSIIDVILSETNHYFCDAWNTFDALIVVGSIVDIAITEVNPAEHTQCSPSMNAEENSRISITFFRLFRVMRLVKLLSRGEGIRTLLWTFIKSFQALPYVALLIVMLFFIYAVIGMQVFGKIALNDTTEINRNNNFQTFPQAVLLLFRCATGEAWQDIMLACMPGKKCAPESEPSNSTEGETPCGSSFAVFYFISFYMLCAFLIINLFVAVIMDNFDYLTRDWSILGPHHLDEFKRIWAEYDPEAKGRIKHLDVVTLLRRIQPPLGFGKLCPHRVACKRLVSMNMPLNSDGTVMFNATLFALVRTALRIKTEGNLEQANEELRAIIKKIWKRTSMKLLDQVVPPAGDDEVTVGKFYATFLIQEYFRKFKKRKEQGLVGKPSQRNALSLQAGLRTLHDIGPEIRRAISGDLTAEEELDKAMKEAVSAASEDDIFRRAGGLFGNHVSYYQSDGRSAFPQTFTTQRPLHINKAGSSQGDTESPSHEKLVDSTFTPSSYSSTGSNANINNANNTALGRLPRPAGYPSTVSTVEGHGPPLSPAIRVQEVAWKLSSNRERHVPMCEDLELRRDSGSAGTQAHCLLLRKANPSRCHSRESQAAMAGQEETSQDETYEVKMNHDTEACSEPSLLSTEMLSYQDDENRQLTLPEEDKRDIRQSPKRGFLRSASLGRRASFHLECLKRQKDRGGDISQKTVLPLHLVHHQALAVAGLSPLLQRSHSPASFPRPFATPPATPGSRGWPPQPVPTLRLEGVESSEKLNSSFPSIHCGSWAETTPGGGGSSAARRVRPVSLMVPSQAGAPGRQFHGSASSLVEAVLISEGLGQFAQDPKFIEVTTQELADACDMTIEEMESAADNILSGGAPQSPNGALLPFVNCRDAGQDRAGGEEDAGCVRARGRPSEEELQDSRVYVSSL
Inhibitor
Name:
BDBM50566512
Synonyms:
CHEMBL4857241
Type:
Small organic molecule
Emp. Form.:
C21H24FN3O3
Mol. Mass.:
385.432
SMILES:
Cc1c(N2CC[C@H](C2)C2(N)CC2)c(F)cc2cc(C(O)=O)c(=O)n(C3CC3)c12 |r|
Structure:
