Target
Voltage-dependent L-type calcium channel subunit alpha-1S
Ligand
BDBM50227967
Substrate
n/a
Meas. Tech.
ChEMBL_214797 (CHEMBL815533)
IC50
2.1±n/a nM
Citation
 Cho, HUeda, MShima, KMizuno, AHayashimatsu, MOhnaka, YTakeuchi, YHamaguchi, MAisaka, KHidaka, T Dihydropyrimidines: novel calcium antagonists with potent and long-lasting vasodilative and antihypertensive activity. J Med Chem 32:2399-406 (1989) [PubMed]
Target
Name:
Voltage-dependent L-type calcium channel subunit alpha-1S
Synonyms:
CAC1S_RAT | Cach1 | Cacn1 | Cacna1s | Cacnl1a3 | Calcium channel, L type, alpha-1 polypeptide, isoform 3, skeletal muscle | Cchl1a3 | ROB1 | Voltage-gated L-type calcium channel | Voltage-gated L-type calcium channel alpha-1S subunit | Voltage-gated calcium channel subunit alpha Cav1.1
Type:
PROTEIN
Mol. Mass.:
210392.58
Organism:
Rattus norvegicus
Description:
ChEMBL_92777
Residue:
1850
Sequence:
MEPSSPQDEGLRKKQPKKPVPEILPRPPRALFCLTLQNPLRKACISVVEWKPFETIILLTIFANCVALAVYLPMPEDDNNTLNLGLEKLEYFFLIVFSIEAAMKIIAYGFLFHQDAYLRSGWNVLDFIIVFLGVFTAILEQVNIIQTNTAPMSSKGAGLDVKALRAFRVLRPLRLVSGVPSLQVVLNSIFKAMLPLFHIALLVLFMVIIYAIIGLELFKGKMHKTCYFIGTDIVATVENEKPSPCARTGSGRPCTINGSECRGGWPGPNHGITHFDNFGFSMLTVYQCISMEGWTDVLYWVNDAIGNEWPWIYFVTLILLGSFFILNLVLGVLSGEFTKEREKAKSRGTFQKLREKQQLEEDLRGYMSWITQGEVMDVDDLREGKLSLDEGGSDTESLYEIEGLNKIIQFIRHWRQWNRVFRWKCHDLVKSKVFYWLVILIVALNTLSIASEHHNQPLWLTHLQDVANRVLLALFTIEMLMKMYGLGLRQYFMSIFNRFDCFVVCSGILEILLVESGAMTPLGISVLRCIRLLRLFKITKYWTSLSNLVASLLNSIRSIASLLLLLFLFMIIFALLGMQLFGGRYDFEDTEVRRSNFDNFPQALISVFQVLTGEDWNSVMYNGIMAYGGPSYPGVLVCIYFIILFVCGNYILLNVFLAIAVDNLAEAESLTSAQKAKAEERKRRKMSRGLPDKSEEERSTMTKKLEQKPKGEGIPTTAKLKIDEFESNVNEVKDPYPSADFPGDDEEDEPEIPASPRPRPLAELQLKEKAVPIPEASSFFIFSPTNKIRVLCHRIVNATWFTNFILLFILLSSAALAAEDPIRADSMRNQILEYFDYVFTAVFTVEIVLKMTTYGAFLHKGSFCRNYFNILDLLVVAVSLISMGLESSAISVVKILRVLRVLRPLRAINRAKGLKHVVQCVFVAIRTIGNIVLVTTLLQFMFACIGVQLFKGKFYSCNDLSKMTEEECRGYYYIYKDGDPTQIELRPRQWIHNDFHFDNVLSAMMSLFTVSTFEGWPQLLYKAIDSNEEDTGPVYNNRVEMAIFFIIYIILIAFFMMNIFVGFVIVTFQEQGETEYKNCELDKNQRQCVQYALKARPLRCYIPKNPYQYQVWYVVTSSYFEYLMFALIMLNTICLGMQHYNQSEQMNHISDILNVAFTIIFTLEMILKLIAFKPRGYFGDPWNVFDFLIVIGSIIDVILSEIDTLLASSGGLYCLGGGCGNVDPDESARISSAFFRLFRVMRLIKLLSRAEGVRTLLWTFIKSFQALPYVALLIVMLFFIYAVIGMQMFGKIAMVDGTQINRNNNFQTFPQAVLLLFRCATGEAWQEILLACSYGKRCDPESDYAPGEEYACGTNFAYYYFISFYMLCAFLIINLFVAVIMDNFDYLTRDWSILGPHHLDEFKAIWAEYDPEAKGRIKHLDVVTLLRRIQPPLGFGKFCPHRVACKRLVGMNMPLNSDGTVTFNATLFALVRTALKIKTEGNFEQANEELRAIIKKIWKRTSMKLLDQVIPPIGDDEVTVGKFYATFLIQEHFRKFMKRQEEYYGYRPKKDTVQIQAGLRTIEEEAAPEIHRAISGDLTAEEELERAMVEAAMEEGIFRRTGGLFGQVDNFLERTNSLPPVMANQRPLQFAEMEMEELESPVFLEDFPQNPGTHPLARANTNNANANVAYGNSSHRNSPVFSSIRYERELLEEAGRPVTREGPFSQPCSVSGVNSRSHVDKLERQMSQRRMPKGQVPPSPCQLSQEKHPVHEEGKGPRSWSTETSDSESFEERVPRNSAHKCTAPATTMLIQEALVRGGLDSLAADANFVMATGQALADACQMEPEEVEVAATELLKRESPKGGAMPREP
  
Inhibitor
Name:
BDBM50227967
Synonyms:
CHEMBL78973
Type:
Small organic molecule
Emp. Form.:
C33H34Cl2N4O6
Mol. Mass.:
653.552
SMILES:
CC(C)OC(=O)C1=C(C)N=C(C)N(C1c1ccccc1[N+]([O-])=O)C(=O)OCCN(Cc1ccccc1)Cc1ccc(Cl)c(Cl)c1 |c:6,t:9|
Structure:
Search PDB for entries with ligand similarity: