| Reaction Details |
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 | Report a problem with these data |
| Target | DNA topoisomerase 2-alpha |
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| Ligand | BDBM50554226 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2048817 (CHEMBL4703516) |
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| IC50 | 20900±n/a nM |
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| Citation |  Ushiyama, F; Amada, H; Mihara, Y; Takeuchi, T; Tanaka-Yamamoto, N; Mima, M; Kamitani, M; Wada, R; Tamura, Y; Endo, M; Masuko, A; Takata, I; Hitaka, K; Sugiyama, H; Ohtake, N Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors. Bioorg Med Chem28:0 (2020) [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 |
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| 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) |
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| Type: | Protein |
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| Mol. Mass.: | 174415.30 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P11388 |
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| Residue: | 1531 |
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| 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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| BDBM50554226 |
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| n/a |
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| Name | BDBM50554226 |
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| Synonyms: | CHEMBL4740882 |
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| Type | Small organic molecule |
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| Emp. Form. | C20H20FN5O6S |
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| Mol. Mass. | 477.466 |
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| SMILES | CNc1cc(F)cc2c(O)c(C(=O)Nc3ccc(cc3)C(=O)NS(=O)(=O)N(C)C)c(=O)[nH]c12 |
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| Structure | 
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