| Reaction Details |
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 | Report a problem with these data |
| Target | DNA topoisomerase 2-alpha |
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| Ligand | BDBM50505821 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1824282 (CHEMBL4324046) |
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| EC50 | 9000±n/a nM |
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| Citation |  Abraham, AD; Esquer, H; Zhou, Q; Tomlinson, N; Hamill, BD; Abbott, JM; Li, L; Pike, LA; Rinaldetti, S; Ramirez, DA; Lunghofer, PJ; Gomez, JD; Schaack, J; Nemkov, T; D'Alessandro, A; Hansen, KC; Gustafson, DL; Messersmith, WA; LaBarbera, DV Drug Design Targeting T-Cell Factor-Driven Epithelial-Mesenchymal Transition as a Therapeutic Strategy for Colorectal Cancer. J Med Chem62:10182-10203 (2019) [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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| BDBM50505821 |
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| n/a |
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| Name | BDBM50505821 |
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| Synonyms: | CHEMBL4457343 |
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| Type | Small organic molecule |
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| Emp. Form. | C25H21N3O4 |
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| Mol. Mass. | 427.4519 |
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| SMILES | COc1cc(NC(C)=O)c(O)c2nccc(-c3ccccc3NC(=O)c3ccccc3)c12 |
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| Structure | 
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