Reaction Details |
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Target | DNA topoisomerase 2-alpha |
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Ligand | BDBM50600008 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2232376 (CHEMBL5146148) |
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IC50 | >100000±n/a nM |
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Citation | Lyons, A; Kirkham, J; Blades, K; Orr, D; Dauncey, E; Smith, O; Dick, E; Walker, R; Matthews, T; Bunt, A; Finlayson, J; Morrison, I; Savage, VJ; Moyo, E; Butler, HS; Newman, R; Ooi, N; Smith, A; Charrier, C; Ratcliffe, AJ; Stokes, NR; Best, S; Salisbury, AM; Craighead, M; Cooper, IR Discovery and structure-activity relationships of a novel oxazolidinone class of bacterial type II topoisomerase inhibitors. Bioorg Med Chem Lett65:0 (2022) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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DNA topoisomerase 2-alpha |
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Name: | DNA topoisomerase 2-alpha |
Synonyms: | DNA topoisomerase 2-alpha | DNA topoisomerase II | DNA topoisomerase II (Topo II) | DNA topoisomerase II alpha | DNA topoisomerase II, alpha isozyme | TOP2 | TOP2A | TOP2A_HUMAN | Topoisomerase I/II | Topoisomerase II alpha (HuTopoIIα) |
Type: | Protein |
Mol. Mass.: | 174415.30 |
Organism: | Homo sapiens (Human) |
Description: | P11388 |
Residue: | 1531 |
Sequence: | MEVSPLQPVNENMQVNKIKKNEDAKKRLSVERIYQKKTQLEHILLRPDTYIGSVELVTQQ
MWVYDEDVGINYREVTFVPGLYKIFDEILVNAADNKQRDPKMSCIRVTIDPENNLISIWN
NGKGIPVVEHKVEKMYVPALIFGQLLTSSNYDDDEKKVTGGRNGYGAKLCNIFSTKFTVE
TASREYKKMFKQTWMDNMGRAGEMELKPFNGEDYTCITFQPDLSKFKMQSLDKDIVALMV
RRAYDIAGSTKDVKVFLNGNKLPVKGFRSYVDMYLKDKLDETGNSLKVIHEQVNHRWEVC
LTMSEKGFQQISFVNSIATSKGGRHVDYVADQIVTKLVDVVKKKNKGGVAVKAHQVKNHM
WIFVNALIENPTFDSQTKENMTLQPKSFGSTCQLSEKFIKAAIGCGIVESILNWVKFKAQ
VQLNKKCSAVKHNRIKGIPKLDDANDAGGRNSTECTLILTEGDSAKTLAVSGLGVVGRDK
YGVFPLRGKILNVREASHKQIMENAEINNIIKIVGLQYKKNYEDEDSLKTLRYGKIMIMT
DQDQDGSHIKGLLINFIHHNWPSLLRHRFLEEFITPIVKVSKNKQEMAFYSLPEFEEWKS
STPNHKKWKVKYYKGLGTSTSKEAKEYFADMKRHRIQFKYSGPEDDAAISLAFSKKQIDD
RKEWLTNFMEDRRQRKLLGLPEDYLYGQTTTYLTYNDFINKELILFSNSDNERSIPSMVD
GLKPGQRKVLFTCFKRNDKREVKVAQLAGSVAEMSSYHHGEMSLMMTIINLAQNFVGSNN
LNLLQPIGQFGTRLHGGKDSASPRYIFTMLSSLARLLFPPKDDHTLKFLYDDNQRVEPEW
YIPIIPMVLINGAEGIGTGWSCKIPNFDVREIVNNIRRLMDGEEPLPMLPSYKNFKGTIE
ELAPNQYVISGEVAILNSTTIEISELPVRTWTQTYKEQVLEPMLNGTEKTPPLITDYREY
HTDTTVKFVVKMTEEKLAEAERVGLHKVFKLQTSLTCNSMVLFDHVGCLKKYDTVLDILR
DFFELRLKYYGLRKEWLLGMLGAESAKLNNQARFILEKIDGKIIIENKPKKELIKVLIQR
GYDSDPVKAWKEAQQKVPDEEENEESDNEKETEKSDSVTDSGPTFNYLLDMPLWYLTKEK
KDELCRLRNEKEQELDTLKRKSPSDLWKEDLATFIEELEAVEAKEKQDEQVGLPGKGGKA
KGKKTQMAEVLPSPRGQRVIPRITIEMKAEAEKKNKKKIKNENTEGSPQEDGVELEGLKQ
RLEKKQKREPGTKTKKQTTLAFKPIKKGKKRNPWSDSESDRSSDESNFDVPPRETEPRRA
ATKTKFTMDLDSDEDFSDFDEKTDDEDFVPSDASPPKTKTSPKLSNKELKPQKSVVSDLE
ADDVKGSVPLSSSPPATHFPDETEITNPVPKKNVTVKKTAAKSQSSTSTTGAKKRAAPKG
TKRDPALNSGVSQKPDPAKTKNRRKRKPSTSDDSDSNFEKIVSKAVTSKKSKGESDDFHM
DFDSAVAPRAKSVRAKKPIKYLEESDEDDLF
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BDBM50600008 |
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n/a |
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Name | BDBM50600008 |
Synonyms: | CHEMBL5198597 |
Type | Small organic molecule |
Emp. Form. | C26H28N6O6 |
Mol. Mass. | 520.5371 |
SMILES | [H][C@]12C[C@H](CC[C@]1([H])N(C(=O)O2)c1ccc2OCC(=O)Nc2n1)NCCCn1c2cc(OC)cnc2ccc1=O |r| |
Structure |
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