Target
Casein kinase I isoform epsilon
Ligand
BDBM302787
Substrate
n/a
Meas. Tech.
Kinase Assay
IC50
<10±n/a nM
Citation
 Velaparthi, UDarne, CPLiu, PWittman, MDPearce, BCAraujo, EMDasgupta, BNair, JSJanakiraman, SKRachamreddy, CRMettu, MRKaruppiah, AMReddy, BSNagalakshmi, PBora, ROMaheshwarappa, SHKumaravel, SMullick, DSistla, R Substituted 4,5,6,7-tetrahydropyrazolo[1,5-A]pyrazine derivatives as casein kinase 1 D/E inhibitors US Patent  US9598423 Publication Date 3/21/2017 
Target
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
  
Inhibitor
Name:
BDBM302787
Synonyms:
(R)-2-(3-Chloro-4- fluorophenyl)- N5-(4-cyano-3- fluorophenyl)-7- (fluoromethyl)- 6,7- dihydropyrazolo[1,5- a]pyrazine-3,5(4H)- dicarboxamide | US9598423, Example A17
Type:
Small organic molecule
Emp. Form.:
C22H16ClF3N6O2
Mol. Mass.:
488.85
SMILES:
NC(=O)c1c2CN(C[C@H](CF)n2nc1-c1ccc(F)c(Cl)c1)C(=O)Nc1ccc([N+]#[C-])c(F)c1 |r,$;;;;;;;;;;;;;;;;;;;;;;;;HN;;;;;;;;;$|
Structure:
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