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Target
Calcium/calmodulin-dependent protein kinase type II subunit alpha/beta/delta/gamma
Ligand
BDBM2579
Substrate
n/a
Meas. Tech.
ChEMBL_43111 (CHEMBL653818)
IC50
6±n/a nM
Citation
 Zhang, HC; White, KB; Ye, H; McComsey, DF; Derian, CK; Addo, MF; Andrade-Gordon, P; Eckardt, AJ; Conway, BR; Westover, L; Xu, JZ; Look, R; Demarest, KT; Emanuel, S; Maryanoff, BE Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3. Bioorg Med Chem Lett 13:3049-53 (2003) [PubMed]  Article 
Target
Name:
Calcium/calmodulin-dependent protein kinase type II subunit alpha/beta/delta/gamma
Synonyms:
CaM kinase II
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 368599
Components:
This complex has 4 components.
Component 1
Name:
Calcium/calmodulin-dependent protein kinase type II subunit alpha
Synonyms:
CAMK2A | CAMKA | CaM kinase II | CaM kinase II alpha | Calcium/calmodulin-dependent protein kinase type II subunit alpha (CAMK2a) | KCC2A_HUMAN | KIAA0968
Type:
Enzyme Catalytic Domain
Mol. Mass.:
54093.63
Organism:
Homo sapiens (Human)
Description:
gi_25952118
Residue:
478
Sequence:
MATITCTRFTEEYQLFEELGKGAFSVVRRCVKVLAGQEYAAKIINTKKLSARDHQKLEREARICRLLKHPNIVRLHDSISEEGHHYLIFDLVTGGELFEDIVAREYYSEADASHCIQQILEAVLHCHQMGVVHRDLKPENLLLASKLKGAAVKLADFGLAIEVEGEQQAWFGFAGTPGYLSPEVLRKDPYGKPVDLWACGVILYILLVGYPPFWDEDQHRLYQQIKAGAYDFPSPEWDTVTPEAKDLINKMLTINPSKRITAAEALKHPWISHRSTVASCMHRQETVDCLKKFNARRKLKGAILTTMLATRNFSGGKSGGNKKSDGVKESSESTNTTIEDEDTKVRKQEIIKVTEQLIEAISNGDFESYTKMCDPGMTAFEPEALGNLVEGLDFHRFYFENLWSRNSKPVHTTILNPHIHLMGDESACIAYIRITQYLDAGGIPRTAQSEETRVWHRRDGKWQIVHFHRSGAPSVLPH
  
Component 2
Name:
Calcium/calmodulin-dependent protein kinase type II subunit gamma
Synonyms:
2.7.11.17 | CAMK | CAMK-II | CAMK2G | CAMKG | CaM kinase II | CaM kinase II gamma | CaM kinase II subunit gamma | CaMK-II subunit gamma | Calcium/calmodulin-dependent protein kinase type II subunit gamma | Calcium/calmodulin-dependent protein kinase type II subunit gamma (CAMKllg) | KCC2G_HUMAN
Type:
Protein
Mol. Mass.:
62621.56
Organism:
Homo sapiens (Human)
Description:
Q13555
Residue:
558
Sequence:
MATTATCTRFTDDYQLFEELGKGAFSVVRRCVKKTSTQEYAAKIINTKKLSARDHQKLEREARICRLLKHPNIVRLHDSISEEGFHYLVFDLVTGGELFEDIVAREYYSEADASHCIHQILESVNHIHQHDIVHRDLKPENLLLASKCKGAAVKLADFGLAIEVQGEQQAWFGFAGTPGYLSPEVLRKDPYGKPVDIWACGVILYILLVGYPPFWDEDQHKLYQQIKAGAYDFPSPEWDTVTPEAKNLINQMLTINPAKRITADQALKHPWVCQRSTVASMMHRQETVECLRKFNARRKLKGAILTTMLVSRNFSAAKSLLNKKSDGGVKKRKSSSSVHLMPQSNNKNSLVSPAQEPAPLQTAMEPQTTVVHNATDGIKGSTESCNTTTEDEDLKGRVPEGRSSRDRTAPSAGMQPQPSLCSSAMRKQEIIKITEQLIEAINNGDFEAYTKICDPGLTSFEPEALGNLVEGMDFHKFYFENLLSKNSKPIHTTILNPHVHVIGEDAACIAYIRLTQYIDGQGRPRTSQSEETRVWHRRDGKWLNVHYHCSGAPAAPLQ
  
Component 3
Name:
Calcium/calmodulin-dependent protein kinase type II subunit beta
Synonyms:
CAM2 | CAMK2 | CAMK2B | CAMKB | CaM kinase II | CaM kinase II beta | CaM kinase II subunit beta | CaM-kinase II beta chain | CaMK-II subunit beta | Calcium/calmodulin-dependent protein kinase type II | Calcium/calmodulin-dependent protein kinase type II beta chain | KCC2B_HUMAN
Type:
Enzyme Catalytic Domain
Mol. Mass.:
72685.48
Organism:
Homo sapiens (Human)
Description:
gi_26051204
Residue:
666
Sequence:
MATTVTCTRFTDEYQLYEDIGKGAFSVVRRCVKLCTGHEYAAKIINTKKLSARDHQKLEREARICRLLKHSNIVRLHDSISEEGFHYLVFDLVTGGELFEDIVAREYYSEADASHCIQQILEAVLHCHQMGVVHRDLKPENLLLASKCKGAAVKLADFGLAIEVQGDQQAWFGFAGTPGYLSPEVLRKEAYGKPVDIWACGVILYILLVGYPPFWDEDQHKLYQQIKAGAYDFPSPEWDTVTPEAKNLINQMLTINPAKRITAHEALKHPWVCQRSTVASMMHRQETVECLKKFNARRKLKGAILTTMLATRNFSVGRQTTAPATMSTAASGTTMGLVEQAKSLLNKKADGVKPQTNSTKNSAAATSPKGTLPPAALEPQTTVIHNPVDGIKESSDSANTTIEDEDAKAPRVPDILSSVRRGSGAPEAEGPLPCPSPAPFSPLPAPSPRISDILNSVRRGSGTPEAEGPLSAGPPPCLSPALLGPLSSPSPRISDILNSVRRGSGTPEAEGPSPVGPPPCPSPTIPGPLPTPSRKQEIIKTTEQLIEAVNNGDFEAYAKICDPGLTSFEPEALGNLVEGMDFHRFYFENLLAKNSKPIHTTILNPHVHVIGEDAACIAYIRLTQYIDGQGRPRTSQSEETRVWHRRDGKWQNVHFHCSGAPVAPLQ
  
Component 4
Name:
Calcium/calmodulin-dependent protein kinase type II subunit delta
Synonyms:
CAMK2D | CAMKD | CaM kinase II | CaM kinase II delta | CaMK-II subunit delta | Calcium/calmodulin-dependent protein kinase type II subunit delta | Calcium/calmodulin-dependent protein kinase type II subunit delta (CAMK2D) | Calcium/calmodulin-dependent protein kinase type II subunit delta (CaMKII subunit delta) | KCC2D_HUMAN
Type:
Enzyme Catalytic Domain
Mol. Mass.:
56419.78
Organism:
Homo sapiens (Human)
Description:
Q13557
Residue:
499
Sequence:
MASTTTCTRFTDEYQLFEELGKGAFSVVRRCMKIPTGQEYAAKIINTKKLSARDHQKLEREARICRLLKHPNIVRLHDSISEEGFHYLVFDLVTGGELFEDIVAREYYSEADASHCIQQILESVNHCHLNGIVHRDLKPENLLLASKSKGAAVKLADFGLAIEVQGDQQAWFGFAGTPGYLSPEVLRKDPYGKPVDMWACGVILYILLVGYPPFWDEDQHRLYQQIKAGAYDFPSPEWDTVTPEAKDLINKMLTINPAKRITASEALKHPWICQRSTVASMMHRQETVDCLKKFNARRKLKGAILTTMLATRNFSAAKSLLKKPDGVKESTESSNTTIEDEDVKARKQEIIKVTEQLIEAINNGDFEAYTKICDPGLTAFEPEALGNLVEGMDFHRFYFENALSKSNKPIHTIILNPHVHLVGDDAACIAYIRLTQYMDGSGMPKTMQSEETRVWHRRDGKWQNVHFHRSGSPTVPIKPPCIPNGKENFSGGTSLWQNI
  
Inhibitor
Name:
BDBM2579
Synonyms:
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one | CHEMBL388978 | Staurosporin, 4 | Staurosporine | Staurosporine, 8 | US20240002365, Compound staurosporine | US9206188, Staurosporine | US9226923, Staurosporine
Type:
Small organic molecule
Emp. Form.:
C28H26N4O3
Mol. Mass.:
466.531
SMILES:
CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Structure:
Search PDB for entries with ligand similarity: