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Target Snapshot

CHEMBL3788 Target Snapshot

Serine/threonine-protein kinase PLK4 · SINGLE PROTEIN · Homo sapiens

2,057Compounds
276Assays
22Approved Drugs
1,988.0Activities
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

Serine/threonine-protein kinase PLK4 shows clinical signal disease relevance led by neoplasm. 3 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 O00444. Start with neoplasm, then reuse UniProt O00444 as the stable protein anchor across project notes and exports.

Review focus
Review-ready target frame

Start with neoplasm, then reuse UniProt O00444 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
neoplasm

Serine/threonine-protein kinase PLK4 shows clinical signal disease relevance led by neoplasm. 3 more disease programs remain visible in the same review block. 2 linked drugs remain visible in the same block.

Start review with neoplasm because it currently carries clinical signal support. Linked drugs include OCIFISERTIB, RG-1530. 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 PLK4 as ChEMBL target CHEMBL3788, mapped to UniProt O00444. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
Serine/threonine-protein kinase PLK4
SINGLE PROTEIN · Homo sapiens
As of 2026-09-13
ChEMBL target ID
CHEMBL3788
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
O00444
Serine/threonine-protein kinase PLK4
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 PLK4 is the right protein anchor across sources, using UniProt O00444 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 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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UniProt Context

UniProt Target Context

Reviewable protein naming and mapping context for this target snapshot.

Protein LabelSerine/threonine-protein kinase PLK4
UniProt AccessionO00444
Component TypeProtein
Sequence Length970 aa

Serine/threonine-protein kinase PLK4

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as Serine/threonine-protein kinase PLK4, mapped to UniProt O00444. Sequence length is 970 aa.

Mapped IDO00444
Review nameSerine/threonine-protein kinase PLK4
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 PLK4 shows clinical signal disease relevance led by neoplasm. 3 more disease programs remain visible in the same review block.

Clinical signal Phase II
neoplasm
2 linked drugs · 2 direct · 2 efficacy
Linked drugOCIFISERTIB
Linked drugRG-1530
Clinical signal Phase II
breast cancer
1 linked drug · 1 direct · 1 efficacy
Linked drugCFI-400945
Clinical signal Phase II
prostate cancer
1 linked drug · 1 direct · 1 efficacy
Linked drugCFI-400945
Clinical signal Phase I
cancer
1 linked drug · 1 direct · 1 efficacy
Linked drugCFI-400945
Source · ChEMBL drug mechanism + indication proxy
Review Cue

How to read disease relevance

Start review with neoplasm because it currently carries clinical signal support. Linked drugs include OCIFISERTIB, RG-1530. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.

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

Clinical Phase Distribution

22
Approved
11
Phase III
27
Phase II
20
Phase I
Assay Mix

Activity Type Distribution

IC50856.0
KI732.0
EC502.0
KD398.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL3408945 10.0 Ki 0.1 Preclinical
CHEMBL5209160 10.0 IC50 0.1 Preclinical
CHEMBL5185225 9.8 Ki 0.16 Preclinical
CHEMBL5185001 9.7 IC50 0.2 Preclinical
CHEMBL3408947 9.59 Ki 0.26 Clinical
CHEMBL5171469 9.52 IC50 0.3 Preclinical
CHEMBL5404983 9.52 IC50 0.3 Preclinical
CHEMBL5428085 9.52 IC50 0.3 Preclinical
CHEMBL2407898 9.49 IC50 0.32 Preclinical
CHEMBL3353348 9.43 IC50 0.37 Preclinical
Distribution

pChEMBL Value Distribution

48
5.0
135
5.5
158
6.0
119
6.5
110
7.0
87
7.5
81
8.0
69
8.5
37
9.0
9
9.5
pChEMBL
Approved Drugs

Approved Drugs

MOMELOTINIB
CHEMBL1078178
Approved 2023
ENTRECTINIB
CHEMBL1983268
Approved 2019
FEDRATINIB
CHEMBL1287853
Approved 2019
GILTERITINIB
CHEMBL3301622
Approved 2018
FOSTAMATINIB
CHEMBL2103830
Approved 2018
MIDOSTAURIN
CHEMBL608533
Approved 2017
NINTEDANIB
CHEMBL502835
Approved 2014
DABRAFENIB
CHEMBL2028663
Approved 2013
AXITINIB
CHEMBL1289926
Approved 2012
CRIZOTINIB
CHEMBL601719
Approved 2011
RUXOLITINIB
CHEMBL1789941
Approved 2011
VANDETANIB
CHEMBL24828
Approved 2011
PAZOPANIB
CHEMBL477772
Approved 2009
SUNITINIB
CHEMBL535
Approved 2006
SORAFENIB
CHEMBL1336
Approved 2005
Assay Landscape

Assay Landscape

276
Total Assays
474
Tested Compounds
2
Assay Types
Binding — 275 assays, 474 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 217 348 7.3
assay format 32 78 7.4
cell-based format 20 5 7.4
subcellular format 6 43 6.6
Functional — 1 assays, 306 compounds
BAO Format Assays Compounds Avg pChEMBL
assay format 1 306 6.5

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine