Review anchor
Dual specificity mitogen-activated protein kinase kinase 1
SINGLE PROTEIN · Homo sapiens
As of 2026-09-14
Evidence Snapshot
Dual specificity mitogen-activated protein kinase kinase 1
CHEMBL3587
SINGLE PROTEIN
Homo sapiens
Identity Layer
Cross-source identity
Keep the review anchor, source IDs, and context contract aligned before reusing this target elsewhere.
This review treats Dual specificity mitogen-activated protein kinase kinase 1 as ChEMBL target CHEMBL3587, mapped to UniProt Q02750. Disease framing currently uses the Open Targets-ready proxy contract.
ChEMBL target ID
CHEMBL3587
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine
As of 2026-09-14
www.ebi.ac.uk
UniProt accession
Q02750
Dual specificity mitogen-activated protein kinase kinase 1
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.
Review-ready Target Rationale
Why Dual specificity mitogen-activated protein kinase kinase 1 matters
Dual specificity mitogen-activated protein kinase kinase 1 is reviewed as Dual specificity mitogen-activated protein kinase kinase 1 (UniProt Q02750); Dual specificity mitogen-activated protein kinase kinase 1 shows approved-linked disease relevance led by neoplasm. 5 more disease programs remain visible in the same review block.; 12 linked drugs keep this evidence frame grounded.; the current evidence base includes 22 approved drugs, 3197 compounds, and 897 assays, with lead potency reaching pChEMBL 10.8.
Protein context
Dual specificity mitogen-activated protein kinase kinase 1
Dual specificity mitogen-activated protein kinase kinase 1 Sequence length is 393 aa.
Review this target as Dual specificity mitogen-activated protein kinase kinase 1, mapped to UniProt Q02750. Sequence length is 393 aa.
Protein source · UniProt accession via ChEMBL component mapping
UniProt Q02750
Protein
Disease context
neoplasm
Dual specificity mitogen-activated protein kinase kinase 1 shows approved-linked disease relevance led by neoplasm. 5 more disease programs remain visible in the same review block. 12 linked drugs keep the rationale reviewable. 5 additional disease programs remain visible in the same card. Linked drugs include AS-703988, AVUTOMETINIB, BINIMETINIB.
Start review with neoplasm because it currently carries approved-linked support. Linked drugs include AS-703988, AVUTOMETINIB, BINIMETINIB, COBIMETINIB. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.
ChEMBL target record
Approved-linked
12 linked drugs
Activity base
Portfolio and assay base
ChEMBL currently tracks 22 approved drugs, 3197 compounds, and 897 assays for this target. The dominant activity type is IC50. CHEMBL3819302 is the current potency anchor at pChEMBL 10.8.
Use CHEMBL3819302 as the tractability anchor when discussing potency (pChEMBL 10.8).
Activity source · ChEMBL 36 via Core Engine
22 approved
pChEMBL 10.8
Source Guidance
Start with the right source
Pick the first block or linked source that matches the review question in front of you.
Need the shortest review narrative first?
Review-ready Target Rationale
One-page rationale with as-of-date and attribution
Start with the review rationale when you need to explain why Dual specificity mitogen-activated protein kinase kinase 1 matters before drilling into raw source blocks.
Jump to Review RationaleNeed stable protein naming or accession mapping?
UniProt Target Context
UniProt accession via ChEMBL component mapping
Go back to the target snapshot when you need the naming and mapping contract behind UniProt Q02750, not just the summarized rationale.
Open Protein ContextNeed disease fit or evidence level for program framing?
Disease Relevance & Evidence Level
ChEMBL drug mechanism + indication proxy
Use the target snapshot disease block when you need to see why neoplasm is currently treated as approved-linked support.
Open Disease ContextSnapshot State
No project snapshot selected. Export uses the live evidence card state.
3197
Total Compounds
897
Total Assays
22
Approved Drugs
IC50: 1459.0, KI: 351.0, EC50: 74.0, KD: 431.0
Activity Types
pChEMBL Activity Distribution
Top 5 Inhibitors (by pChEMBL)
| Structure | Compound | pChEMBL | Type | Phase |
|---|---|---|---|---|
|
|
No preferred name
CHEMBL3819302
|
10.8 | IC50 | — |
|
|
No preferred name
CHEMBL3818677
|
10.7 | IC50 | — |
|
|
No preferred name
CHEMBL2087076
|
9.7 | EC50 | — |
|
|
No preferred name
CHEMBL1614766
|
9.6 | Kd | — |
|
|
No preferred name
CHEMBL507361
|
9.5 | IC50 | Clinical |
Approved Drugs
| Structure | Compound | First Approval |
|---|---|---|
|
|
SELUMETINIB
CHEMBL1614701
|
2020 |
|
|
BINIMETINIB
CHEMBL3187723
|
2018 |
|
|
NERATINIB
CHEMBL180022
|
2017 |
|
|
COBIMETINIB
CHEMBL2146883
|
2015 |
|
|
NINTEDANIB
CHEMBL502835
|
2014 |
|
|
TRAMETINIB
CHEMBL2103875
|
2013 |
|
|
BOSUTINIB
CHEMBL288441
|
2012 |
|
|
TOFACITINIB
CHEMBL221959
|
2012 |
|
|
VANDETANIB
CHEMBL24828
|
2011 |
|
|
SUNITINIB
CHEMBL535
|
2006 |
|
|
DASATINIB
CHEMBL5416410
|
2006 |
Source Header