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Target Snapshot

CHEMBL1781 Target Snapshot

DNA topoisomerase 1 · SINGLE PROTEIN · Homo sapiens

4,594Compounds
1,172Assays
7Approved Drugs
915.0Activities
Free Research Context

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Broader Open DB context

Frame the target before identity details

Structured disease, protein, and project context should read before the lower-level identity rail.

As of 2026-09-13

DNA topoisomerase 1 shows approved-linked disease relevance led by neoplasm. 5 more disease programs remain visible in the same review block. 17 linked drugs keep the current disease frame grounded. Protein identity stays anchored to UniProt P11387. Start with neoplasm, then reuse UniProt P11387 as the stable protein anchor across project notes and exports.

Review focus
Review-ready target frame

Start with neoplasm, then reuse UniProt P11387 as the stable protein anchor across project notes and exports.

ChEMBL component mapping + Open Targets-ready proxy + ChEMBL 36 via Core Engine 2026-09-13 17 linked drugs
Open source guide
Disease program
neoplasm

DNA topoisomerase 1 shows approved-linked disease relevance led by neoplasm. 5 more disease programs remain visible in the same review block. 17 linked drugs remain visible in the same block.

Start review with neoplasm because it currently carries approved-linked support. Linked drugs include 7-ETHYL-10-HYDROXYCAMPTOTHECIN, AR-67, BECATECARIN, BELOTECAN. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.

Disease source · ChEMBL drug mechanism + indication proxy
Approved-linked Open Targets-ready proxy 17 linked drugs
Open disease block
Identity Layer

Cross-source identity

Keep the review anchor, source IDs, and context contract aligned before reusing this target elsewhere.

This review treats DNA topoisomerase 1 as ChEMBL target CHEMBL1781, mapped to UniProt P11387. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
DNA topoisomerase 1
SINGLE PROTEIN · Homo sapiens
As of 2026-09-13
ChEMBL target ID
CHEMBL1781
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
P11387
DNA topoisomerase 1
UniProt accession via ChEMBL component mapping As of 2026-09-13
www.uniprot.org
Disease evidence contract
Open Targets-ready proxy
ChEMBL drug mechanism + indication proxy
ChEMBL drug mechanism + indication proxy As of 2026-09-13
www.ebi.ac.uk

Reuse the same identifiers in notes, watch rules, exports, and review packs so provenance stays stable across surfaces.

Source Guidance

Start with the right source

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Need stable target naming and protein identity?
UniProt Target Context
UniProt accession via ChEMBL component mapping

Start here when your first question is whether DNA topoisomerase 1 is the right protein anchor across sources, using UniProt P11387 as the stable mapping.

Jump to Protein Context
Need disease fit before discussing compounds?
Disease Relevance & Evidence Level
ChEMBL drug mechanism + indication proxy

Use this block first when you need to confirm why neoplasm is currently framed as approved-linked support. It currently carries 17 linked drugs in the same disease frame.

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Evidence Card
Review-ready rationale with source-aware context

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Overview

Basic Information

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UniProt Context

UniProt Target Context

Reviewable protein naming and mapping context for this target snapshot.

Protein LabelDNA topoisomerase 1
UniProt AccessionP11387
Component TypeProtein
Sequence Length765 aa

DNA topoisomerase 1

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as DNA topoisomerase 1, mapped to UniProt P11387. Sequence length is 765 aa.

Mapped IDP11387
Review nameDNA topoisomerase 1
OrganismHomo sapiens
Disease Relevance

Disease Relevance & Evidence Level

Open Targets-ready disease context using the current target-indication evidence contract.

Approved-linked Open Targets-ready proxy

DNA topoisomerase 1 shows approved-linked disease relevance led by neoplasm. 5 more disease programs remain visible in the same review block.

Approved-linked Approved
neoplasm
17 linked drugs · 17 direct · 17 efficacy
Linked drug7-ETHYL-10-HYDROXYCAMPTOTHECIN
Linked drugAR-67
Linked drugBECATECARIN
Linked drugBELOTECAN
Approved-linked Approved
breast cancer
10 linked drugs · 10 direct · 10 efficacy
Linked drug7-ETHYL-10-HYDROXYCAMPTOTHECIN
Linked drugDATOPOTAMAB DERUXTECAN
Linked drugEDOTECARIN
Linked drugETIRINOTECAN PEGOL
Approved-linked Approved
cancer
9 linked drugs · 9 direct · 9 efficacy
Linked drug7-ETHYL-10-HYDROXYCAMPTOTHECIN
Linked drug9-AMINOCAMPTOTHECIN
Linked drugAR-67
Linked drugDATOPOTAMAB DERUXTECAN
Approved-linked Approved
small cell lung carcinoma
9 linked drugs · 9 direct · 9 efficacy
Linked drug7-ETHYL-10-HYDROXYCAMPTOTHECIN
Linked drugBECATECARIN
Linked drugBELOTECAN
Linked drugCAMPTOTHECIN-20-O-PROPIONATE
Approved-linked Approved
ovarian cancer
8 linked drugs · 8 direct · 8 efficacy
Linked drug9-AMINOCAMPTOTHECIN
Linked drugBECATECARIN
Linked drugBELOTECAN
Linked drugETIRINOTECAN PEGOL
Approved-linked Approved
cervical cancer
4 linked drugs · 4 direct · 4 efficacy
Linked drugBELOTECAN
Linked drugIRINOTECAN HYDROCHLORIDE
Linked drugSACITUZUMAB GOVITECAN
Linked drugTOPOTECAN HYDROCHLORIDE
Source · ChEMBL drug mechanism + indication proxy
Review Cue

How to read disease relevance

Start review with neoplasm because it currently carries approved-linked support. Linked drugs include 7-ETHYL-10-HYDROXYCAMPTOTHECIN, AR-67, BECATECARIN, BELOTECAN. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.

Lead diseaseneoplasm
Strongest levelApproved-linked
Block modeOpen Targets-ready proxy
Clinical Profile

Clinical Phase Distribution

7
Approved
3
Phase III
5
Phase II
Assay Mix

Activity Type Distribution

IC50735.0
KI1.0
EC50173.0
KD6.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL1813808 9.53 Kd 0.296 Preclinical
CHEMBL1813809 8.58 Kd 2.65 Preclinical
CHEMBL474561 8.48 EC50 3.3 Preclinical
CHEMBL5653589 8.19 Kd 6.526 Preclinical
CHEMBL135492 8.1 EC50 8.0 Preclinical
CHEMBL338843 7.96 IC50 11.0 Preclinical
CHEMBL507686 7.92 EC50 12.0 Preclinical
CHEMBL335455 7.82 IC50 15.0 Preclinical
CHEMBL503051 7.8 EC50 16.0 Preclinical
CHEMBL133209 7.77 EC50 17.0 Preclinical
Distribution

pChEMBL Value Distribution

72
5.0
83
5.5
64
6.0
64
6.5
45
7.0
44
7.5
3
8.0
1
8.5
0
9.0
1
9.5
pChEMBL
Approved Drugs

Approved Drugs

TOPOTECAN
CHEMBL84
Approved 1996
Assay Landscape

Assay Landscape

1,172
Total Assays
464
Tested Compounds
3
Assay Types
Binding — 1,133 assays, 464 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 945 362 5.7
cell-based format 138 86 5.9
assay format 46 16 4.3
subcellular format 2 0
tissue-based format 2 0
Functional — 38 assays, 45 compounds
BAO Format Assays Compounds Avg pChEMBL
assay format 38 45 6.8
ADME — 1 assays, 0 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 1 0

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine