Reaction Details |
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Target | Serine/threonine-protein kinase Chk1 |
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Ligand | BDBM15250 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_458388 (CHEMBL942709) |
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IC50 | 28±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 Lett17:6593-601 (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 |
Synonyms: | CHEK1 | CHK1 | CHK1 checkpoint homolog | CHK1_HUMAN | Checkpoint kinase-1 (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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BDBM15250 |
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n/a |
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Name | BDBM15250 |
Synonyms: | 7-chloro-3-oxo-11,18-dioxa-2,4,21,23-tetraazatricyclo[17.3.1.0^{5,10}]tricosa-1(22),5(10),6,8,19(23),20-hexaene-20-carbonitrile | CHEMBL374417 | macrocyclic inhibitor 5d |
Type | Small organic molecule |
Emp. Form. | C18H18ClN5O3 |
Mol. Mass. | 387.82 |
SMILES | Clc1ccc2OCCCCCCOc3nc(NC(=O)Nc2c1)cnc3C#N |
Structure |
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