Reaction Details |
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Target | Serine/threonine-protein kinase Chk1 |
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Ligand | BDBM50325163 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_651698 (CHEMBL1228388) |
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IC50 | 9±n/a nM |
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Citation | Oza, V; Ashwell, S; Brassil, P; Breed, J; Deng, C; Ezhuthachan, J; Haye, H; Horn, C; Janetka, J; Lyne, P; Newcombe, N; Otterbien, L; Pass, M; Read, J; Roswell, S; Su, M; Toader, D; Yu, D; Yu, Y; Valentine, A; Webborn, P; White, A; Zabludoff, S; Zheng, X Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration. Bioorg Med Chem Lett20:5133-8 (2010) [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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BDBM50325163 |
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n/a |
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Name | BDBM50325163 |
Synonyms: | 5-methyl-8-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-[1,2,4]triazolo[4,3-a]quinolin-1(2H)-one | CHEMBL1223386 |
Type | Small organic molecule |
Emp. Form. | C23H25N5O |
Mol. Mass. | 387.4775 |
SMILES | CN1CCN(Cc2ccc(cc2)-c2ccc3c(C)cc4n[nH]c(=O)n4c3c2)CC1 |
Structure |
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