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Target Snapshot

CHEMBL2527 Target Snapshot

Serine/threonine-protein kinase Chk2 · SINGLE PROTEIN · Homo sapiens

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2,871Compounds
677Assays
7Approved Drugs
1,588.0Activities
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Broader Open DB context

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

As of 2026-09-13

Serine/threonine-protein kinase Chk2 shows clinical signal disease relevance led by cancer. 5 more disease programs remain visible in the same review block. 2 linked drugs keep the current disease frame grounded. Protein identity stays anchored to UniProt O96017. Start with cancer, then reuse UniProt O96017 as the stable protein anchor across project notes and exports.

Review focus
Review-ready target frame

Start with cancer, then reuse UniProt O96017 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 2 linked drugs
Open source guide
Disease program
cancer

Serine/threonine-protein kinase Chk2 shows clinical signal disease relevance led by cancer. 5 more disease programs remain visible in the same review block. 2 linked drugs remain visible in the same block.

Start review with cancer because it currently carries clinical signal support. Linked drugs include PREXASERTIB, XL-844. 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
Clinical signal Open Targets-ready proxy 2 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 Serine/threonine-protein kinase Chk2 as ChEMBL target CHEMBL2527, mapped to UniProt O96017. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
Serine/threonine-protein kinase Chk2
SINGLE PROTEIN · Homo sapiens
As of 2026-09-13
ChEMBL target ID
CHEMBL2527
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
O96017
Serine/threonine-protein kinase Chk2
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

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UniProt Target Context
UniProt accession via ChEMBL component mapping

Start here when your first question is whether Serine/threonine-protein kinase Chk2 is the right protein anchor across sources, using UniProt O96017 as the stable mapping.

Jump to Protein Context
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Disease Relevance & Evidence Level
ChEMBL drug mechanism + indication proxy

Use this block first when you need to confirm why cancer is currently framed as clinical signal support. It currently carries 2 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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Preferred NameSerine/threonine-protein kinase Chk2
Target TypeSINGLE PROTEIN
OrganismHomo sapiens
UniProtO96017
ChEMBL ↗ UniProt ↗ NCBI Protein ↗

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UniProt Context

UniProt Target Context

Reviewable protein naming and mapping context for this target snapshot.

Protein LabelSerine/threonine-protein kinase Chk2
UniProt AccessionO96017
Component TypeProtein
Sequence Length543 aa

Serine/threonine-protein kinase Chk2

Source · UniProt accession via ChEMBL component mapping
UniProt Context ↗
Review Cue

How to read this target

Review this target as Serine/threonine-protein kinase Chk2, mapped to UniProt O96017. Sequence length is 543 aa.

Mapped IDO96017
Review nameSerine/threonine-protein kinase Chk2
OrganismHomo sapiens
Disease Relevance

Disease Relevance & Evidence Level

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

Clinical signal Open Targets-ready proxy

Serine/threonine-protein kinase Chk2 shows clinical signal disease relevance led by cancer. 5 more disease programs remain visible in the same review block.

Clinical signal Phase II
cancer
2 linked drugs · 2 direct · 2 efficacy
Linked drugPREXASERTIB
Linked drugXL-844
Clinical signal Phase II
breast cancer
1 linked drug · 1 direct · 1 efficacy
Linked drugPREXASERTIB
Clinical signal Phase II
neoplasm
1 linked drug · 1 direct · 1 efficacy
Linked drugPREXASERTIB
Clinical signal Phase II
ovarian cancer
1 linked drug · 1 direct · 1 efficacy
Linked drugPREXASERTIB
Clinical signal Phase II
small cell lung carcinoma
1 linked drug · 1 direct · 1 efficacy
Linked drugPREXASERTIB
Clinical signal Phase I
acute myeloid leukemia
1 linked drug · 1 direct · 1 efficacy
Linked drugPREXASERTIB
Source · ChEMBL drug mechanism + indication proxy
ChEMBL target record ↗
Review Cue

How to read disease relevance

Start review with cancer because it currently carries clinical signal support. Linked drugs include PREXASERTIB, XL-844. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.

Lead diseasecancer
Strongest levelClinical signal
Block modeOpen Targets-ready proxy
Clinical Profile

Clinical Phase Distribution

7
Approved
5
Phase III
11
Phase II
13
Phase I
Assay Mix

Activity Type Distribution

IC50796.0
KI705.0
EC504.0
KD83.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL1988594 9.2 Ki 0.631 Preclinical
CHEMBL509032 8.9 Ki 1.259 Preclinical
CHEMBL1970203 8.8 Ki 1.585 Preclinical
CHEMBL195041 8.7 IC50 2.0 Preclinical
CHEMBL5812190 8.7 IC50 2.0 Preclinical
CHEMBL1967878 8.6 Ki 2.512 Clinical
CHEMBL179717 8.52 IC50 3.0 Preclinical
CHEMBL195177 8.52 IC50 3.0 Preclinical
CHEMBL1236782 8.52 IC50 3.0 Preclinical
CHEMBL3980850 8.52 IC50 3.0 Preclinical
Distribution

pChEMBL Value Distribution

65
5.0
102
5.5
149
6.0
132
6.5
202
7.0
132
7.5
66
8.0
13
8.5
1
9.0
0
9.5
pChEMBL
Approved Drugs

Approved Drugs

BRIGATINIB
CHEMBL3545311
Approved 2017
Properties Compare Identifier
NERATINIB
CHEMBL180022
Approved 2017
Properties Compare Identifier
BOSUTINIB
CHEMBL288441
Approved 2012
Properties Compare Identifier
SUNITINIB
CHEMBL535
Approved 2006
Properties Compare Identifier
GEFITINIB
CHEMBL939
Approved 2003
Properties Compare Identifier
Assay Landscape

Assay Landscape

677
Total Assays
596
Tested Compounds
3
Assay Types
Binding — 674 assays, 596 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 503 583 6.7
assay format 74 6 6.6
cell-based format 71 7 6.2
subcellular format 26 0 —
Functional — 2 assays, 205 compounds
BAO Format Assays Compounds Avg pChEMBL
assay format 1 204 6.3
cell-based format 1 1 7.4
ADME — 1 assays, 0 compounds
BAO Format Assays Compounds Avg pChEMBL
assay format 1 0 —

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine