General Information of the Protein
Protein ID
PT01218
Protein Name
DNA topoisomerase 2-alpha
Secondarily
Protein Name
DNA topoisomerase II
alpha isozyme
Gene Name
TOP2A
Secondarily
Gene Name
TOP2
Sequence
MEVSPLQPVNENMQVNKIKKNEDAKKRLSVERIYQKKTQLEHILLRPDTYIGSVELVTQQMWVYDEDVGINYREVTFVPGLYKIFDEILVNAADNKQRDPKMSCIRVTIDPENNLISIWNNGKGIPVVEHKVEKMYVPALIFGQLLTSSNYDDDEKKVTGGRNGYGAKLCNIFSTKFTVETASREYKKMFKQTWMDNMGRAGEMELKPFNGEDYTCITFQPDLSKFKMQSLDKDIVALMVRRAYDIAGSTKDVKVFLNGNKLPVKGFRSYVDMYLKDKLDETGNSLKVIHEQVNHRWEVCLTMSEKGFQQISFVNSIATSKGGRHVDYVADQIVTKLVDVVKKKNKGGVAVKAHQVKNHMWIFVNALIENPTFDSQTKENMTLQPKSFGSTCQLSEKFIKAAIGCGIVESILNWVKFKAQVQLNKKCSAVKHNRIKGIPKLDDANDAGGRNSTECTLILTEGDSAKTLAVSGLGVVGRDKYGVFPLRGKILNVREASHKQIMENAEINNIIKIVGLQYKKNYEDEDSLKTLRYGKIMIMTDQDQDGSHIKGLLINFIHHNWPSLLRHRFLEEFITPIVKVSKNKQEMAFYSLPEFEEWKSSTPNHKKWKVKYYKGLGTSTSKEAKEYFADMKRHRIQFKYSGPEDDAAISLAFSKKQIDDRKEWLTNFMEDRRQRKLLGLPEDYLYGQTTTYLTYNDFINKELILFSNSDNERSIPSMVDGLKPGQRKVLFTCFKRNDKREVKVAQLAGSVAEMSSYHHGEMSLMMTIINLAQNFVGSNNLNLLQPIGQFGTRLHGGKDSASPRYIFTMLSSLARLLFPPKDDHTLKFLYDDNQRVEPEWYIPIIPMVLINGAEGIGTGWSCKIPNFDVREIVNNIRRLMDGEEPLPMLPSYKNFKGTIEELAPNQYVISGEVAILNSTTIEISELPVRTWTQTYKEQVLEPMLNGTEKTPPLITDYREYHTDTTVKFVVKMTEEKLAEAERVGLHKVFKLQTSLTCNSMVLFDHVGCLKKYDTVLDILRDFFELRLKYYGLRKEWLLGMLGAESAKLNNQARFILEKIDGKIIIENKPKKELIKVLIQRGYDSDPVKAWKEAQQKVPDEEENEESDNEKETEKSDSVTDSGPTFNYLLDMPLWYLTKEKKDELCRLRNEKEQELDTLKRKSPSDLWKEDLATFIEELEAVEAKEKQDEQVGLPGKGGKAKGKKTQMAEVLPSPRGQRVIPRITIEMKAEAEKKNKKKIKNENTEGSPQEDGVELEGLKQRLEKKQKREPGTKTKKQTTLAFKPIKKGKKRNPWSDSESDRSSDESNFDVPPRETEPRRAATKTKFTMDLDSDEDFSDFDEKTDDEDFVPSDASPPKTKTSPKLSNKELKPQKSVVSDLEADDVKGSVPLSSSPPATHFPDETEITNPVPKKNVTVKKTAAKSQSSTSTTGAKKRAAPKGTKRDPALNSGVSQKPDPAKTKNRRKRKPSTSDDSDSNFEKIVSKAVTSKKSKGESDDFHMDFDSAVAPRAKSVRAKKPIKYLEESDEDDLF
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Isomerase
Function
Key decatenating enzyme that alters DNA topology by binding to two double-stranded DNA molecules, generating a double-stranded break in one of the strands, passing the intact strand through the broken strand, and religating the broken strand (PubMed:17567603, PubMed:18790802, PubMed:22013166, PubMed:22323612). May play a role in regulating the period length of BMAL1 transcriptional oscillation (By similarity).
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Uniprot ID
Primary ID:
P11388

Secondarily ID:
B2RTS1
Q71UN1
Q71UQ5
Q9HB24
Q9HB25
Q9HB26
Q9UP44
Q9UQP9
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Ensembl ID
ENSG00000131747
HGNC ID
HGNC:11989
Subcellular Location
Cytoplasm
Nucleus
Nucleoplasm
Nucleus
Nucleus
Nucleolus
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000073 , A-498
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0001940
 Compound Info 
(8S,10S)-10-{[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy}-6,8,11-trihydroxy-8-(2-hydroxyacetyl)-1-methoxy-5,7,8,9,10,12-hexahydrotetracene-5,12-dione
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C27H29NO11
  1
1
IC50 = 990 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0564213
 Compound Info 
2-amino-4-(1-benzothiophen-2-yl)-5-oxo-4H-pyrano[3,2-c]chromene-3-carbonitrile
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C21H12N2O3S
  1
1
IC50 = 10280 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0964647
 Compound Info 
2-amino-4-(1H-indol-2-yl)-5-oxo-4,5-dihydropyrano[3,2-c]chromene-3-carbonitrile
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C21H13N3O3
  1
1
IC50 = 12380 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0514615
 Compound Info 
2-amino-5-oxo-4-quinolin-3-yl-4H-pyrano[3,2-c]chromene-3-carbonitrile
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C22H13N3O3
  1
1
IC50 = 16660 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0578729
 Compound Info 
3-[1-(4-bromophenyl)-4,5-diphenylimidazol-2-yl]-6-chloro-7-methylchromen-4-one
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C31H20BrClN2O2
  1
1
IC50 = 17120 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0563042
 Compound Info 
2-amino-5-oxo-4-(4-oxochromen-2-yl)-4H-pyrano[3,2-c]chromene-3-carbonitrile
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C22H12N2O5
  1
1
IC50 = 26420 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0569851
 Compound Info 
6-chloro-3-[1-(3,4-dichlorophenyl)-4,5-diphenylimidazol-2-yl]-7-methylchromen-4-one
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C31H19Cl3N2O2
  1
1
IC50 = 39880 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0573445
 Compound Info 
6-chloro-7-methyl-3-[1-(4-nitrophenyl)-4,5-diphenylimidazol-2-yl]chromen-4-one
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C31H20ClN3O4
  1
1
IC50 = 48400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0001940
 Compound Info 
(8S,10S)-10-{[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy}-6,8,11-trihydroxy-8-(2-hydroxyacetyl)-1-methoxy-5,7,8,9,10,12-hexahydrotetracene-5,12-dione
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C27H29NO11
  3
1 IC50 = 600 nM
2 IC50 = 880 nM
3 IC50 = 3000 nM
Clinical Information about the Protein
Target 1 ( DNA topoisomerase II alpha (TOP2A) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 PK1
 Drug Info 
Phase 2
Solid tumour/cancer