Reaction Details |
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Target | Serine/threonine-protein kinase Chk1 |
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Ligand | BDBM50204715 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_442099 (CHEMBL891237) |
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IC50 | 7.4±n/a nM |
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Citation | Tong, Y; Claiborne, A; Stewart, KD; Park, C; Kovar, P; Chen, Z; Credo, RB; Gu, WZ; Gwaltney, SL; Judge, RA; Zhang, H; Rosenberg, SH; Sham, HL; Sowin, TJ; Lin, NH Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors. Bioorg Med Chem15:2759-67 (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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BDBM50204715 |
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n/a |
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Name | BDBM50204715 |
Synonyms: | 4'-(6-{[(5-methyl-pyrazin-2-ylmethyl)-amino]-methyl}-1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-biphenyl-4-ol | CHEMBL242536 |
Type | Small organic molecule |
Emp. Form. | C29H25N5O |
Mol. Mass. | 459.5417 |
SMILES | Cc1cnc(CNCc2ccc-3c(Cc4c(n[nH]c-34)-c3ccc(cc3)-c3ccc(O)cc3)c2)cn1 |
Structure |
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