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TargetCasein kinase I isoform alpha/delta/epsilon/gamma-1/gamma-2
LigandBDBM50179207
Substrate/Competitorn/a
Meas. Tech.ChEMBL_325239 (CHEMBL861600)
IC50 7200±n/a nM
Citation Ho, CY; Ludovici, DW; Maharoof, US; Mei, J; Sechler, JL; Tuman, RW; Strobel, ED; Andraka, L; Yen, HK; Leo, G; Li, J; Almond, H; Lu, H; DeVine, A; Tominovich, RM; Baker, J; Emanuel, S; Gruninger, RH; Middleton, SA; Johnson, DL; Galemmo, RA (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. J Med Chem48:8163-73 (2005) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Casein kinase I isoform alpha/delta/epsilon/gamma-1/gamma-2
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 (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:
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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BDBM50179207
n/a
NameBDBM50179207
Synonyms:3-fluoro-N-(6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine | CHEMBL120077 | JNJ-10198409
TypeSmall organic molecule
Emp. Form.C18H16FN3O2
Mol. Mass.325.3369
SMILESCOc1cc2Cc3c(Nc4cccc(F)c4)[nH]nc3-c2cc1OC
Structure
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