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Target
Myosin light chain kinase, smooth muscle
Ligand
BDBM3049
Substrate
Myosin Light-Chain
Meas. Tech.
MLCK assay
pH
7.2±n/a
Temperature
303.15±n/a K
IC50
120±n/a nM
Citation
 Kleinschroth, J; Hartenstein, J; Rudolph, C; Schachtele, C Novel Indolocarbazole protein kinase C inhibitors with improved biochemical and physicochemical properties. Bioorg Med Chem Lett 5:55-60 (1995)    Article 
Target
Name:
Myosin light chain kinase, smooth muscle
Synonyms:
MLCK | MYLK_CHICK | Mylk | Myosin Light-Chain Kinase | Telokin
Type:
Enzyme
Mol. Mass.:
210423.57
Organism:
Gallus gallus (chicken)
Description:
n/a
Residue:
1906
Sequence:
MGDVKLVTSTRVSKTSLTLSPSVPAEAPAFTLPPRNIRVQLGATARFEGKVRGYPEPQITWYRNGHPLPEGDHYVVDHSIRGIFSLVIKGVQEGDSGKYTCEAANDGGVRQVTVELTVEGNSLKKYSLPSSAKTPGGRLSVPPVEHRPSIWGESPPKFATKPNRVVVREGQTGRFSCKITGRPQPQVTWTKGDIHLQQNERFNMFEKTGIQYLEIQNVQLADAGIYTCTVVNSAGKASVSAELTVQGPDKTDTHAQPLCMPPKPTTLATKAIENSDFKQATSNGIAKELKSTSTELMVETKDRLSAKKETFYTSREAKDGKQGQNQEANAVPLQESRGTKGPQVLQKTSSTITLQAVKAQPEPKAEPQTTFIRQAEDRKRTVQPLMTTTTQENPSLTGQVSPRSRETENRAGVRKSVKEEKREPLGIPPQFESRPQSLEASEGQEIKFKSKVSGKPKPDVEWFKEGVPIKTGEGIQIYEEDGTHCLWLKKACLGDSGSYSCAAFNPRGQTSTSWLLTVKRPKVEEVAPCFSSVLKGCTVSEGQDFVLQCYVGGVPVPEITWLLNEQPIQYAHSTFEAGVAKLTVQDALPEDDGIYTCLAENNAGRASCSAQVTVKEKKSSKKAEGTQAAKLNKTFAPIFLKGLTDLKVMDGSQVIMTVEVSANPCPEIIWLHNGKEIQETEDFHFEKKGNEYSLYIQEVFPEDTGKYTCEAWNELGETQTQATLTVQEPQDGIQPWFISKPRSVTAAAGQNVLISCAIAGDPFPTVHWFKDGQEITPGTGCEILQNEDIFTLILRNVQSRHAGQYEIQLRNQVGECSCQVSLMLRESSASRAEMLRDGRESASSGERRDGGNYGALTFGRTSGFKKSSSETRAAEEEQEDVRGVLKRRVETREHTEESLRQQEAEQLDFRDILGKKVSTKSFSEEDLKEIPAEQMDFRANLQRQVKPKTLSEEERKVHAPQQVDFRSVLAKKGTPKTPLPEKVPPPKPAVTDFRSVLGAKKKPPAENGSASTPAPNARAGSEAQNATPNSEAPAPKPVVKKEEKNDRKCEHGCAVVDGGIIGKKAENKPAASKPTPPPSKGTAPSFTEKLQDAKVADGEKLVLQCRISSDPPASVSWTLDSKAIKSSKSIVISQEGTLCSLTIEKVMPEDGGEYKCIAENAAGKAECACKVLVEDTSSTKAAKPAEKKTKKPKTTLPPVLSTESSEATVKKKPAPKTPPKAATPPQITQFPEDRKVRAGESVELFAKVVGTAPITCTWMKFRKQIQENEYIKIENAENSSKLTISSTKQEHCGCYTLVVENKLGSRQAQVNLTVVDKPDPPAGTPCASDIRSSSLTLSWYGSSYDGGSAVQSYTVEIWNSVDNKWTDLTTCRSTSFNVQDLQADREYKFRVRAANVYGISEPSQESEVVKVGEKQEEELKEEEAELSDDEGKETEVNYRTVTINTEQKVSDVYNIEERLGSGKFGQVFRLVEKKTGKVWAGKFFKAYSAKEKENIRDEISIMNCLHHPKLVQCVDAFEEKANIVMVLEMVSGGELFERIIDEDFELTERECIKYMRQISEGVEYIHKQGIVHLDLKPENIMCVNKTGTSIKLIDFGLARRLESAGSLKVLFGTPEFVAPEVINYEPIGYETDMWSIGVICYILVSGLSPFMGDNDNETLANVTSATWDFDDEAFDEISDDAKDFISNLLKKDMKSRLNCTQCLQHPWLQKDTKNMEAKKLSKDRMKKYMARRKWQKTGHAVRAIGRLSSMAMISGMSGRKASGSSPTSPINADKVENEDAFLEEVAEEKPHVKPYFTKTILDMEVVEGSAARFDCKIEGYPDPEVMWYKDDQPVKESRHFQIDYDEEGNCSLTISEVCGDDDAKYTCKAVNSLGEATCTAELLVETMGKEGEGEGEGEEDEEEEEE
  
Inhibitor
Name:
BDBM3049
Synonyms:
23-[3-(dimethylamino)-2-hydroxypropyl]-7-methoxy-3-methyl-3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^{11,15}.0^{17,22}]tricosa-1(16),2(10),4,6,8,11(15),17(22),18,20-nonaene-12,14-dione | Go 7874 | Indolocarbazole deriv.
Type:
Small organic molecule
Emp. Form.:
C27H26N4O4
Mol. Mass.:
470.5197
SMILES:
COc1ccc2n(C)c3c(c4C(=O)NC(=O)c4c4c5ccccc5n(CC(O)CN(C)C)c34)c2c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Myosin Light-Chain
Synonyms:
MYL6 | MYL6_CHICK
Type:
Peptide
Mol. Mass.:
16974.98
Organism:
Gallus gallus (chicken)
Description:
250 uM ATP (0.3 uCi [gamma-32P]ATP) as co-substrate.
Residue:
151
Sequence:
MCDFSEEQTAEFKEAFQLFDRTGDGKILYSQCGDVMRALGQNPTNAEVMKVLGNPKSDEMNLKTLKFEQFLPMMQTIAKNKDQGCFEDYVEGLRVFDKEGNGTVMGAEIRHVLVTLGEKMTEEEVEQLVAGHEDSNGCINYEELVRMVLSG