Reaction Details |
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Target | Serine/threonine-protein kinase Chk1 |
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Ligand | BDBM50221589 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_457662 (CHEMBL923939) |
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IC50 | 5±n/a nM |
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Citation | Tao, ZF; Li, G; Tong, Y; Stewart, KD; Chen, Z; Bui, MH; Merta, P; Park, C; Kovar, P; Zhang, H; Sham, HL; Rosenberg, SH; Sowin, TJ; Lin, NH Discovery of 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-benzonitriles and 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-pyridine-2'-carbonitriles as potent checkpoint kinase 1 (Chk1) inhibitors. Bioorg Med Chem Lett17:5944-51 (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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BDBM50221589 |
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n/a |
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Name | BDBM50221589 |
Synonyms: | 4-((6,7-dimethoxy-1,4-dihydroindeno[1,2-c]pyrazol-3-yl)ethynyl)-2-methoxyphenol | 4-(6,7-dimethoxy-2,4-dihydro-indeno[1,2-c]pyrazol-3-ylethynyl)-2-methoxy-phenol | CHEMBL248396 | Chk1_146 |
Type | Small organic molecule |
Emp. Form. | C21H18N2O4 |
Mol. Mass. | 362.3786 |
SMILES | COc1cc2Cc3c(n[nH]c3C#Cc3ccc(O)c(OC)c3)-c2cc1OC |
Structure |
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