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Protein / target

Mitogen-activated protein kinase kinase kinase 1

Encoded byMAP3K1Q13233Homo sapiensSwiss-Prot
UniProt: Q13233Ensembl: ENSG00000095015HGNC: HGNC:6848NCBI Gene: 4214
Clinical-stage
Therapeutic maturity
1
Clinical candidates
Small-molecule tractable
Druggability
Advanced Clinical
1
Research papers

Protein at a glance

Biological role

Protein serine/threonine kinase

Strongest disease association

Breast Neoplasms

Via encoding gene MAP3K1 · Genetic evidence · score 0.71

Therapeutic position

Clinically advancing target

Small molecules

Research activity

Emerging research

1 papers · latest 2012

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

Component of a protein kinase signal transduction cascade.

View complete UniProt function annotation

Component of a protein kinase signal transduction cascade (PubMed:9808624). Activates the ERK and JNK kinase pathways by phosphorylation of MAP2K1 and MAP2K4 (PubMed:9808624). May phosphorylate the MAPK8/JNK1 kinase (PubMed:17761173). Activates CHUK and IKBKB, the central protein kinases of the NF-kappa-B pathway (PubMed:9808624)

Domains and Gene Ontology detail (15)

Domains & features

Protein kinase

Gene Ontology

  • Ccytosol
  • Ctight junction
  • FATP binding
  • FMAP kinase kinase kinase activity
  • Fprotein kinase activity
  • Fprotein kinase binding
  • Fprotein serine kinase activity
  • Fprotein serine/threonine kinase activity
  • Fubiquitin protein ligase activity
  • Fzinc ion binding
  • Pcellular response to mechanical stimulus
  • PFc-epsilon receptor signaling pathway

1512 aa · 164 kDa

Biological roles

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Kinase signallingUniProt · GO
View supporting evidence

Kinase signalling

  • ·Component of a protein kinase signal transduction cascade (PubMed:9808624). Activates th…
  • ·MAP kinase kinase kinase activity
  • ·protein kinase activity
  • ·protein kinase binding

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene MAP3K1

Gene-level evidence surfaced through the gene MAP3K1that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Breast Neoplasms
0.84Well supported

Genetic evidence dominant · Open Targets 0.53

Prostate carcinoma
0.81Well supported

Genetic evidence dominant · Open Targets 0.51

Diabetes Mellitus, Type 2
0.67Moderately supported

Genetic evidence dominant · Open Targets 0.41

Ovarian Neoplasms
0.67Moderately supported

Somatic mutation evidence dominant · Open Targets 0.53

Breast adenocarcinoma
0.59Moderately supported

Somatic mutation evidence dominant · Open Targets 0.55

View evidence synthesis (5)
Breast NeoplasmsWell supported
0.84
agreement 0.73–0.96
Genetic57%Somatic mutation32%Literature11%Genetic literaturedup

Open Targets aggregate 0.53 · 3 independent evidence families · 1 not counted as duplicate

Prostate carcinomaWell supported
0.81
agreement 0.70–0.92
Genetic62%Somatic mutation36%Literature3%

Open Targets aggregate 0.51 · 3 independent evidence families

Diabetes Mellitus, Type 2Moderately supported
0.67
agreement 0.53–0.81
Genetic94%Literature6%

Open Targets aggregate 0.41 · 2 independent evidence families

Ovarian NeoplasmsModerately supported
0.67
agreement 0.56–0.78
Somatic mutation62%Genetic35%Literature3%

Open Targets aggregate 0.53 · 3 independent evidence families

Breast adenocarcinomaModerately supported
0.59
agreement 0.43–0.75
Somatic mutation100%Literature1%

Open Targets aggregate 0.55 · 2 independent evidence families

This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.

Show all associations
Breast adenocarcinoma0.55
Breast Neoplasms0.53
Ovarian Neoplasms0.53
Prostate carcinoma0.51
Diabetes Mellitus, Type 20.41

Drug development

1 compounds recorded · 1 in clinical development

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines.

View all recorded compounds (1)
E-6201Phase 2

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small molecules — Strong

Advanced Clinical and High-Quality Ligand support this modality.

Protein degraders — Emerging

Feasibility evidence (literature and database ubiquitination) — no clinical-stage drug of this modality recorded.

View underlying tractability evidence (6)
SM · Advanced ClinicalSM · High-Quality LigandSM · Druggable FamilyPR · LiteraturePR · Database UbiquitinationPR · Small Molecule Binder

Raw Open Targets tractability assessment buckets, by modality.

Research activity

1 papers · to 2012

Papers linked directly to this protein. This is the protein's own literature — descriptor-derived papers are kept separate below.

Most cited

Comprehensive molecular portraits of human breast tumours.9,720 cites

Nature · 2012

Recent

Comprehensive molecular portraits of human breast tumours.

Nature · 2012

Europe PMC papers linked directly to this protein.