| Reaction Details |
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 | Report a problem with these data |
| Target | DNA topoisomerase 2-alpha |
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| Ligand | BDBM50613099 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2290973 |
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| IC50 | 17000±n/a nM |
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| Citation |  Durcik, M; Cotman, AE; Toplak, ?; Mo?ina, ?; Skok, ?; Szili, PE; Czikkely, M; Maharramov, E; Vu, TH; Piras, MV; Zidar, N; Ila?, J; Zega, A; Trontelj, J; Pardo, LA; Hughes, D; Huseby, D; Berruga-Fernández, T; Cao, S; Simoff, I; Svensson, R; Korol, SV; Jin, Z; Vicente, F; Ramos, MC; Mundy, JEA; Maxwell, A; Stevenson, CEM; Lawson, DM; Glinghammar, B; Sjöström, E; Bohlin, M; Oreskär, J; Alvér, S; Janssen, GV; Sterk, GJ; Kikelj, D; Pal, C; Toma?i?, T; Peterlin Ma?i?, L New Dual Inhibitors of Bacterial Topoisomerases with Broad-Spectrum Antibacterial Activity and In Vivo Efficacy against Vancomycin-Intermediate J Med Chem66:3968-3994 (2023) [PubMed] |
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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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| BDBM50613099 |
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| n/a |
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| Name | BDBM50613099 |
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| Synonyms: | CHEMBL5288212 |
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| Type | Small organic molecule |
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| Emp. Form. | C18H16Cl2N4O4S |
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| Mol. Mass. | 455.315 |
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| SMILES | Cc1[nH]c(C(=O)Nc2nc3c(cc(cc3s2)C(O)=O)N2CCOCC2)c(Cl)c1Cl |
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| Structure | 
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