Reaction Details |
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Target | Casein kinase I isoform alpha/delta/epsilon/gamma-1/gamma-2 |
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Ligand | BDBM2579 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_46477 (CHEMBL658117) |
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IC50 | 1400±n/a nM |
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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 Lett13:3049-53 (2003) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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Casein kinase I isoform alpha/delta/epsilon/gamma-1/gamma-2 |
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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: | MDHPSREKDERQRTTKPMAQRSAHCSRPSGSSSSSGVLMVGPNFRVGKKIGCGNFGELRL
GKNLYTNEYVAIKLEPIKSRAPQLHLEYRFYKQLGSAGEGLPQVYYFGPCGKYNAMVLEL
LGPSLEDLFDLCDRTFTLKTVLMIAIQLLSRMEYVHSKNLIYRDVKPENFLIGRQGNKKE
HVIHIIDFGLAKEYIDPETKKHIPYREHKSLTGTARYMSINTHLGKEQSRRDDLEALGHM
FMYFLRGSLPWQGLKADTLKERYQKIGDTKRNTPIEALCENFPEEMATYLRYVRRLDFFE
KPDYEYLRTLFTDLFEKKGYTFDYAYDWVGRPIPTPVGSVHVDSGASAITRESHTHRDRP
SQQQPLRNQVVSSTNGELNVDDPTGAHSNAPITAHAEVEVVEEAKCCCFFKRKRKKTAQR
HK
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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: | MELRVGNRYRLGRKIGSGSFGDIYLGTDIAAGEEVAIKLECVKTKHPQLHIESKIYKMMQ
GGVGIPTIRWCGAEGDYNVMVMELLGPSLEDLFNFCSRKFSLKTVLLLADQMISRIEYIH
SKNFIHRDVKPDNFLMGLGKKGNLVYIIDFGLAKKYRDARTHQHIPYRENKNLTGTARYA
SINTHLGIEQSRRDDLESLGYVLMYFNLGSLPWQGLKAATKRQKYERISEKKMSTPIEVL
CKGYPSEFATYLNFCRSLRFDDKPDYSYLRQLFRNLFHRQGFSYDYVFDWNMLKFGASRA
ADDAERERRDREERLRHSRNPATRGLPSTASGRLRGTQEVAPPTPLTPTSHTANTSPRPV
SGMERERKVSMRLHRGAPVNISSSDLTGRQDTSRMSTSQIPGRVASSGLQSVVHR
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Component 3 |
Name: | Casein kinase I isoform epsilon |
Synonyms: | Axin-1/Casein kinase I epsilon | CKI-epsilon | CKIe | CSNK1E | Casein kinase 1 epsilon (CK1Æ) | 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: | MELRVGNKYRLGRKIGSGSFGDIYLGANIASGEEVAIKLECVKTKHPQLHIESKFYKMMQ
GGVGIPSIKWCGAEGDYNVMVMELLGPSLEDLFNFCSRKFSLKTVLLLADQMISRIEYIH
SKNFIHRDVKPDNFLMGLGKKGNLVYIIDFGLAKKYRDARTHQHIPYRENKNLTGTARYA
SINTHLGIEQSRRDDLESLGYVLMYFNLGSLPWQGLKAATKRQKYERISEKKMSTPIEVL
CKGYPSEFSTYLNFCRSLRFDDKPDYSYLRQLFRNLFHRQGFSYDYVFDWNMLKFGAARN
PEDVDRERREHEREERMGQLRGSATRALPPGPPTGATANRLRSAAEPVASTPASRIQPAG
NTSPRAISRVDRERKVSMRLHRGAPANVSSSDLTGRQEVSRIPASQTSVPFDHLGK
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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: | MDFDKKGGKGETEEGRRMSKAGGGRSSHGIRSSGTSSGVLMVGPNFRVGKKIGCGNFGEL
RLGKNLYTNEYVAIKLEPIKSRAPQLHLEYRFYKQLSATEGVPQVYYFGPCGKYNAMVLE
LLGPSLEDLFDLCDRTFTLKTVLMIAIQLITRMEYVHTKSLIYRDVKPENFLVGRPGTKR
QHAIHIIDFGLAKEYIDPETKKHIPYREHKSLTGTARYMSINTHLGKEQSRRDDLEALGH
MFMYFLRGSLPWQGLKADTLKERYQKIGDTKRATPIEVLCENFPEEMATYLRYVRRLDFF
EKPDYDYLRKLFTDLFDRSGFVFDYEYDWAGKPLPTPIGTVHTDLPSQPQLRDKTQPHSK
NQALNSTNGELNADDPTAGHSNAPITAPAEVEVADETKCCCFFKRRKRKSLQRHK
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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: | MASSSGSKAEFIVGGKYKLVRKIGSGSFGDIYLAINITNGEEVAVKLESQKARHPQLLYE
SKLYKILQGGVGIPHIRWYGQEKDYNVLVMDLLGPSLEDLFNFCSRRFTMKTVLMLADQM
ISRIEYVHTKNFIHRDIKPDNFLMGIGRHCNKLFLIDFGLAKKYRDNRTRQHIPYREDKN
LTGTARYASINAHLGIEQSRRDDMESLGYVLMYFNRTSLPWQGLKAATKKQKYEKISEKK
MSTPVEVLCKGFPAEFAMYLNYCRGLRFEEAPDYMYLRQLFRILFRTLNHQYDYTFDWTM
LKQKAAQQAASSSGQGQQAQTPTGKQTDKTKSNMKGF
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BDBM2579 |
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n/a |
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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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