DNA topoisomerase 1
Named enzymes, including the metabolising cytochromes and the monoamine oxidases.
- Measurements
- 3
- Compounds
- 2
- Binding constants
- 0
- Median pX
- —
I · Identity
What this target is
Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.
DNA topoisomerase 1
Releases the supercoiling and torsional tension of DNA introduced during the DNA replication and transcription by transiently cleaving and rejoining one strand of the DNA duplex. Introduces a single-strand break via transesterification at a target site in duplex DNA. The scissile phosphodiester is attacked by the catalytic tyrosine of the enzyme, resulting in the formation of a DNA-(3'-phosphotyrosyl)-enzyme intermediate and the expulsion of a 5'-OH DNA strand. The free DNA strand then rotates around the intact phosphodiester bond on the opposing strand, thus removing DNA supercoils. Finally, in the religation step, the DNA 5'-OH attacks the covalent intermediate to expel the active-site tyrosine and restore the DNA phosphodiester backbone (By similarity). Regulates the alternative splicing of tissue factor (F3) pre-mRNA in endothelial cells. Involved in the circadian transcription of the core circadian clock component BMAL1 by altering the chromatin structure around the ROR response elements (ROREs) on the BMAL1 promoter
Quoted from UniProt’s FUNCTION annotation for P11387 (reviewed).
What it acts with
STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.
Where it sits in the cell
- Nucleoplasm
- Nucleoli fibrillar center
Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.
UniProt, curated Nucleus, nucleolus · Nucleus, nucleoplasm
Expression by cell type
Single cell type RNA, the 3 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.
- Syncytiotrophoblasts1,442.3 nCPM
- Alveolar cells type 21,249.6 nCPM
- Neutrophils1,184.4 nCPM
IV · Evidence
Every measurement at this target
Each row links to the ChEMBL assay it came from.
Functional readouts 1
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| DNA topoisomerase 1 | Enzymes | IC50 | 31,000 | 4.51 | Homo sapiens | CHEMBL5242304 |
Other measurements 2
Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| DNA topoisomerase 1 | Enzymes | ED50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5150780 |
| DNA topoisomerase 1 | Enzymes | ED50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5150780 |