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Target
Casein kinase I isoform alpha/delta/epsilon/gamma-1/gamma-2
Ligand
BDBM2579
Substrate
n/a
Meas. Tech.
ChEMBL_46477 (CHEMBL658117)
IC50
1400±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:
Casein kinase I isoform alpha/delta/epsilon/gamma-1/gamma-2
Synonyms:
Casein kinase I
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 304706
Components:
This complex has 5 components.
Component 1
Name:
Casein kinase I isoform gamma-1
Synonyms:
CKI-gamma 1 | CSNK1G1 | Casein kinase I | Casein kinase I gamma 1 isoform | Casein kinase I isoform gamma-1 | KC1G1_HUMAN
Type:
PROTEIN
Mol. Mass.:
48530.93
Organism:
Homo sapiens (Human)
Description:
ChEMBL_774608
Residue:
422
Sequence:
MDHPSREKDERQRTTKPMAQRSAHCSRPSGSSSSSGVLMVGPNFRVGKKIGCGNFGELRLGKNLYTNEYVAIKLEPIKSRAPQLHLEYRFYKQLGSAGEGLPQVYYFGPCGKYNAMVLELLGPSLEDLFDLCDRTFTLKTVLMIAIQLLSRMEYVHSKNLIYRDVKPENFLIGRQGNKKEHVIHIIDFGLAKEYIDPETKKHIPYREHKSLTGTARYMSINTHLGKEQSRRDDLEALGHMFMYFLRGSLPWQGLKADTLKERYQKIGDTKRNTPIEALCENFPEEMATYLRYVRRLDFFEKPDYEYLRTLFTDLFEKKGYTFDYAYDWVGRPIPTPVGSVHVDSGASAITRESHTHRDRPSQQQPLRNQVVSSTNGELNVDDPTGAHSNAPITAHAEVEVVEEAKCCCFFKRKRKKTAQRHK
  
Component 2
Name:
Casein kinase I isoform delta
Synonyms:
CKI-delta | CKId | CSNK1D | Casein kinase 1 delta (CK1δ) | Casein kinase I delta | Casein kinase I isoform alpha/delta | Casein kinase I isoform delta (CK1D) | HCKID | KC1D_HUMAN | casein kinases 1 delta (CK1 delta)
Type:
Enzyme
Mol. Mass.:
47356.76
Organism:
Homo sapiens (Human)
Description:
P48730
Residue:
415
Sequence:
MELRVGNRYRLGRKIGSGSFGDIYLGTDIAAGEEVAIKLECVKTKHPQLHIESKIYKMMQGGVGIPTIRWCGAEGDYNVMVMELLGPSLEDLFNFCSRKFSLKTVLLLADQMISRIEYIHSKNFIHRDVKPDNFLMGLGKKGNLVYIIDFGLAKKYRDARTHQHIPYRENKNLTGTARYASINTHLGIEQSRRDDLESLGYVLMYFNLGSLPWQGLKAATKRQKYERISEKKMSTPIEVLCKGYPSEFATYLNFCRSLRFDDKPDYSYLRQLFRNLFHRQGFSYDYVFDWNMLKFGASRAADDAERERRDREERLRHSRNPATRGLPSTASGRLRGTQEVAPPTPLTPTSHTANTSPRPVSGMERERKVSMRLHRGAPVNISSSDLTGRQDTSRMSTSQIPGRVASSGLQSVVHR
  
Component 3
Name:
Casein kinase I isoform epsilon
Synonyms:
Axin-1/Casein kinase I epsilon | CKI-epsilon | CKIe | CSNK1E | Casein kinase 1 epsilon (CK1Ɛ) | Casein kinase I epsilon | Casein kinase I isoform epsilon (CK1 epsilon) | Casein kinase I isoform epsilon (CK1E) | Casein kinase I isoform epsilon (CK1epsilon) | KC1E_HUMAN
Type:
Protein
Mol. Mass.:
47340.25
Organism:
Homo sapiens (Human)
Description:
P49674
Residue:
416
Sequence:
MELRVGNKYRLGRKIGSGSFGDIYLGANIASGEEVAIKLECVKTKHPQLHIESKFYKMMQGGVGIPSIKWCGAEGDYNVMVMELLGPSLEDLFNFCSRKFSLKTVLLLADQMISRIEYIHSKNFIHRDVKPDNFLMGLGKKGNLVYIIDFGLAKKYRDARTHQHIPYRENKNLTGTARYASINTHLGIEQSRRDDLESLGYVLMYFNLGSLPWQGLKAATKRQKYERISEKKMSTPIEVLCKGYPSEFSTYLNFCRSLRFDDKPDYSYLRQLFRNLFHRQGFSYDYVFDWNMLKFGAARNPEDVDRERREHEREERMGQLRGSATRALPPGPPTGATANRLRSAAEPVASTPASRIQPAGNTSPRAISRVDRERKVSMRLHRGAPANVSSSDLTGRQEVSRIPASQTSVPFDHLGK
  
Component 4
Name:
Casein kinase I isoform gamma-2
Synonyms:
CK1G2 | CSNK1G2 | Casein kinase I | Casein kinase I gamma 2 | KC1G2_HUMAN
Type:
PROTEIN
Mol. Mass.:
47475.36
Organism:
Homo sapiens (Human)
Description:
ChEMBL_774313
Residue:
415
Sequence:
MDFDKKGGKGETEEGRRMSKAGGGRSSHGIRSSGTSSGVLMVGPNFRVGKKIGCGNFGELRLGKNLYTNEYVAIKLEPIKSRAPQLHLEYRFYKQLSATEGVPQVYYFGPCGKYNAMVLELLGPSLEDLFDLCDRTFTLKTVLMIAIQLITRMEYVHTKSLIYRDVKPENFLVGRPGTKRQHAIHIIDFGLAKEYIDPETKKHIPYREHKSLTGTARYMSINTHLGKEQSRRDDLEALGHMFMYFLRGSLPWQGLKADTLKERYQKIGDTKRATPIEVLCENFPEEMATYLRYVRRLDFFEKPDYDYLRKLFTDLFDRSGFVFDYEYDWAGKPLPTPIGTVHTDLPSQPQLRDKTQPHSKNQALNSTNGELNADDPTAGHSNAPITAPAEVEVADETKCCCFFKRRKRKSLQRHK
  
Component 5
Name:
Casein kinase I isoform alpha
Synonyms:
CK1 | CKI-alpha | CSNK1A1 | Casein Kinase I | Casein kinase 1 alpha (CK1 alpha) | Casein kinase I isoform alpha/delta | KC1A_HUMAN
Type:
Serine/threonine-protein kinase
Mol. Mass.:
38936.59
Organism:
Homo sapiens (Human)
Description:
P48729
Residue:
337
Sequence:
MASSSGSKAEFIVGGKYKLVRKIGSGSFGDIYLAINITNGEEVAVKLESQKARHPQLLYESKLYKILQGGVGIPHIRWYGQEKDYNVLVMDLLGPSLEDLFNFCSRRFTMKTVLMLADQMISRIEYVHTKNFIHRDIKPDNFLMGIGRHCNKLFLIDFGLAKKYRDNRTRQHIPYREDKNLTGTARYASINAHLGIEQSRRDDMESLGYVLMYFNRTSLPWQGLKAATKKQKYEKISEKKMSTPVEVLCKGFPAEFAMYLNYCRGLRFEEAPDYMYLRQLFRILFRTLNHQYDYTFDWTMLKQKAAQQAASSSGQGQQAQTPTGKQTDKTKSNMKGF
  
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:
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