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Target Snapshot

CHEMBL5914 Target Snapshot

Mitogen-activated protein kinase kinase kinase 2 · SINGLE PROTEIN · Homo sapiens

553Compounds
218Assays
13Approved Drugs
354.0Activities
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 2026-09-14

Protein identity stays anchored to UniProt Q9Y2U5. Use UniProt Q9Y2U5 as the stable identity anchor, then attach disease evidence before program review.

Review focus
Protein anchor ready

Use UniProt Q9Y2U5 as the stable identity anchor, then attach disease evidence before program review.

ChEMBL component mapping + Open Targets-ready proxy + ChEMBL 36 via Core Engine 2026-09-14
Open source guide
Identity Layer

Cross-source identity

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

This review treats Mitogen-activated protein kinase kinase kinase 2 as ChEMBL target CHEMBL5914, mapped to UniProt Q9Y2U5. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
Mitogen-activated protein kinase kinase kinase 2
SINGLE PROTEIN · Homo sapiens
As of 2026-09-14
ChEMBL target ID
CHEMBL5914
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-14
www.ebi.ac.uk
UniProt accession
Q9Y2U5
Mitogen-activated protein kinase kinase kinase 2
UniProt accession via ChEMBL component mapping As of 2026-09-14
www.uniprot.org
Disease evidence contract
Open Targets-ready proxy
ChEMBL drug mechanism + indication proxy
ChEMBL drug mechanism + indication proxy As of 2026-09-14
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 Mitogen-activated protein kinase kinase kinase 2 is the right protein anchor across sources, using UniProt Q9Y2U5 as the stable mapping.

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Disease Relevance & Evidence Level
ChEMBL drug mechanism + indication proxy

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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 LabelMitogen-activated protein kinase kinase kinase 2
UniProt AccessionQ9Y2U5
Component TypeProtein
Sequence Length619 aa

Mitogen-activated protein kinase kinase kinase 2

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as Mitogen-activated protein kinase kinase kinase 2, mapped to UniProt Q9Y2U5. Sequence length is 619 aa.

Mapped IDQ9Y2U5
Review nameMitogen-activated protein kinase kinase kinase 2
OrganismHomo sapiens
Clinical Profile

Clinical Phase Distribution

13
Approved
6
Phase III
7
Phase II
5
Phase I
Assay Mix

Activity Type Distribution

IC5021.0
KD333.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL388978 8.62 Kd 2.4 Preclinical
CHEMBL603469 8.32 Kd 4.8 Clinical
CHEMBL502835 8.03 Kd 9.4 Approved
CHEMBL4554938 7.72 Kd 19.0 Preclinical
CHEMBL388978 7.63 IC50 23.5 Preclinical
CHEMBL288441 7.52 Kd 30.0 Approved
CHEMBL4465866 7.42 Kd 38.0 Preclinical
CHEMBL1789941 7.39 Kd 41.0 Approved
CHEMBL4576489 7.28 Kd 53.0 Preclinical
CHEMBL535 7.24 Kd 57.0 Approved
Distribution

pChEMBL Value Distribution

11
5.0
11
5.5
15
6.0
9
6.5
16
7.0
4
7.5
3
8.0
1
8.5
0
9.0
0
9.5
pChEMBL
Approved Drugs

Approved Drugs

FEDRATINIB
CHEMBL1287853
Approved 2019
GILTERITINIB
CHEMBL3301622
Approved 2018
MIDOSTAURIN
CHEMBL608533
Approved 2017
NERATINIB
CHEMBL180022
Approved 2017
NINTEDANIB
CHEMBL502835
Approved 2014
BOSUTINIB
CHEMBL288441
Approved 2012
RUXOLITINIB
CHEMBL1789941
Approved 2011
CRIZOTINIB
CHEMBL601719
Approved 2011
PAZOPANIB
CHEMBL477772
Approved 2009
SUNITINIB
CHEMBL535
Approved 2006
DASATINIB
CHEMBL5416410
Approved 2006
Assay Landscape

Assay Landscape

218
Total Assays
61
Tested Compounds
1
Assay Types
Binding — 218 assays, 61 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 138 41 6.7
subcellular format 30 16 5.9
cell-based format 29 4 6.5
assay format 21 0

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine