Reaction Details |
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Target | Serine/threonine-protein kinase Chk1 |
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Ligand | BDBM50224893 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_458388 |
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IC50 | 0.300000±n/a nM |
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Citation | Tao ZF; Chen Z; Bui MH; Kovar P; Johnson E; Bouska J; Zhang H; Rosenberg S; Sowin T; Lin NH Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. Bioorg Med Chem Lett 17:6593-601 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Serine/threonine-protein kinase Chk1 |
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Name: | Serine/threonine-protein kinase Chk1/2 |
Synonyms: | CHK1 checkpoint homolog | Checkpoint kinase-1 (CHK1) | Serine/threonine-protein kinase Chk1 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 54443.02 |
Organism: | Homo sapiens (Human) |
Description: | gi_166295192 |
Residue: | 476 |
Sequence: | MAVPFVEDWDLVQTLGEGAYGEVQLAVNRVTEEAVAVKIVDMKRAVDCPENIKKEICINK
MLNHENVVKFYGHRREGNIQYLFLEYCSGGELFDRIEPDIGMPEPDAQRFFHQLMAGVVY
LHGIGITHRDIKPENLLLDERDNLKISDFGLATVFRYNNRERLLNKMCGTLPYVAPELLK
RREFHAEPVDVWSCGIVLTAMLAGELPWDQPSDSCQEYSDWKEKKTYLNPWKKIDSAPLA
LLHKILVENPSARITIPDIKKDRWYNKPLKKGAKRPRVTSGGVSESPSGFSKHIQSNLDF
SPVNSASSEENVKYSSSQPEPRTGLSLWDTSPSYIDKLVQGISFSQPTCPDHMLLNSQLL
GTPGSSQNPWQRLVKRMTRFFTKLDADKSYQCLKETCEKLGYQWKKSCMNQVTISTTDRR
NNKLIFKVNLLEMDDKILVDFRLSKGDGLEFKRHFLKIKGKLIDIVSSQKIWLPAT
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BDBM50224893 |
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n/a |
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Name | BDBM50224893 |
Synonyms: | 7-chloro-8-hydroxy-3-oxo-11,16-dioxa-2,4,19,21-tetraaza-tricyclo[15.3.1.0*5,10*]henicosa-1(21),5,7,9,17,19-hexaene-18-carbonitrile | CHEMBL400805 |
Type | Small organic molecule |
Emp. Form. | C16H14ClN5O4 |
Mol. Mass. | 375.766 |
SMILES | Oc1cc2OCCCCOc3nc(NC(=O)Nc2cc1Cl)cnc3C#N |
Structure |
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