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Target Snapshot

CHEMBL5330 Target Snapshot

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

2,062Compounds
284Assays
22Approved Drugs
1,358.0Activities
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 Q12851. Use UniProt Q12851 as the stable identity anchor, then attach disease evidence before program review.

Review focus
Protein anchor ready

Use UniProt Q12851 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 kinase 2 as ChEMBL target CHEMBL5330, mapped to UniProt Q12851. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
Mitogen-activated protein kinase kinase kinase kinase 2
SINGLE PROTEIN · Homo sapiens
As of 2026-09-14
ChEMBL target ID
CHEMBL5330
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-14
www.ebi.ac.uk
UniProt accession
Q12851
Mitogen-activated protein kinase 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 kinase 2 is the right protein anchor across sources, using UniProt Q12851 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 kinase 2
UniProt AccessionQ12851
Component TypeProtein
Sequence Length820 aa

Mitogen-activated protein kinase 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 kinase 2, mapped to UniProt Q12851. Sequence length is 820 aa.

Mapped IDQ12851
Review nameMitogen-activated protein kinase kinase kinase kinase 2
OrganismHomo sapiens
Clinical Profile

Clinical Phase Distribution

22
Approved
12
Phase III
22
Phase II
15
Phase I
Assay Mix

Activity Type Distribution

IC50109.0
KI911.0
EC501.0
KD337.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL388978 9.32 IC50 0.481 Preclinical
CHEMBL4214342 9.0 IC50 1.0 Preclinical
CHEMBL1994669 8.7 Ki 1.995 Preclinical
CHEMBL4202685 8.7 IC50 2.0 Preclinical
CHEMBL4207036 8.7 IC50 2.0 Preclinical
CHEMBL288441 8.51 Kd 3.1 Approved
CHEMBL1984548 8.5 Ki 3.162 Preclinical
CHEMBL244378 8.5 Ki 3.162 Preclinical
CHEMBL4116008 8.4 IC50 4.0 Clinical
CHEMBL603469 8.33 Kd 4.7 Clinical
Distribution

pChEMBL Value Distribution

73
5.0
160
5.5
124
6.0
88
6.5
86
7.0
40
7.5
24
8.0
6
8.5
2
9.0
0
9.5
pChEMBL
Approved Drugs

Approved Drugs

ENTRECTINIB
CHEMBL1983268
Approved 2019
GILTERITINIB
CHEMBL3301622
Approved 2018
NERATINIB
CHEMBL180022
Approved 2017
LENVATINIB
CHEMBL1289601
Approved 2015
NINTEDANIB
CHEMBL502835
Approved 2014
BOSUTINIB
CHEMBL288441
Approved 2012
PONATINIB
CHEMBL1171837
Approved 2012
CRIZOTINIB
CHEMBL601719
Approved 2011
SUNITINIB
CHEMBL535
Approved 2006
Assay Landscape

Assay Landscape

284
Total Assays
457
Tested Compounds
2
Assay Types
Binding — 283 assays, 163 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 205 120 6.8
cell-based format 29 3 7.2
assay format 27 4 7.0
subcellular format 22 36 6.2
Functional — 1 assays, 457 compounds
BAO Format Assays Compounds Avg pChEMBL
assay format 1 457 6.2

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine