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Target Snapshot

CHEMBL3587 Target Snapshot

Dual specificity mitogen-activated protein kinase kinase 1 · SINGLE PROTEIN · Homo sapiens

3,197Compounds
897Assays
22Approved Drugs
2,315.0Activities
Free Research Context

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Broader Open DB context

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Structured disease, protein, and project context should read before the lower-level identity rail.

As of 2026-09-14

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 current disease frame grounded. Protein identity stays anchored to UniProt Q02750. Start with neoplasm, then reuse UniProt Q02750 as the stable protein anchor across project notes and exports.

Review focus
Review-ready target frame

Start with neoplasm, then reuse UniProt Q02750 as the stable protein anchor across project notes and exports.

ChEMBL component mapping + Open Targets-ready proxy + ChEMBL 36 via Core Engine 2026-09-14 12 linked drugs
Open source guide
Disease program
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 remain visible in the same block.

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.

Disease source · ChEMBL drug mechanism + indication proxy
Approved-linked Open Targets-ready proxy 12 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 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.

Review anchor
Dual specificity mitogen-activated protein kinase kinase 1
SINGLE PROTEIN · Homo sapiens
As of 2026-09-14
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.

Source Guidance

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UniProt Target Context
UniProt accession via ChEMBL component mapping

Start here when your first question is whether Dual specificity mitogen-activated protein kinase kinase 1 is the right protein anchor across sources, using UniProt Q02750 as the stable mapping.

Jump to Protein Context
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Disease Relevance & Evidence Level
ChEMBL drug mechanism + indication proxy

Use this block first when you need to confirm why neoplasm is currently framed as approved-linked support. It currently carries 12 linked drugs in the same disease frame.

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Evidence Card
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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 LabelDual specificity mitogen-activated protein kinase kinase 1
UniProt AccessionQ02750
Component TypeProtein
Sequence Length393 aa

Dual specificity mitogen-activated protein kinase kinase 1

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as Dual specificity mitogen-activated protein kinase kinase 1, mapped to UniProt Q02750. Sequence length is 393 aa.

Mapped IDQ02750
Review nameDual specificity mitogen-activated protein kinase kinase 1
OrganismHomo sapiens
Disease Relevance

Disease Relevance & Evidence Level

Open Targets-ready disease context using the current target-indication evidence contract.

Approved-linked Open Targets-ready proxy

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.

Approved-linked Approved
neoplasm
12 linked drugs · 12 direct · 12 efficacy
Linked drugAS-703988
Linked drugAVUTOMETINIB
Linked drugBINIMETINIB
Linked drugCOBIMETINIB
Approved-linked Approved
cancer
9 linked drugs · 9 direct · 9 efficacy
Linked drugAZD-8330
Linked drugBINIMETINIB
Linked drugCOBIMETINIB
Linked drugMIRDAMETINIB
Approved-linked Approved
melanoma
7 linked drugs · 7 direct · 7 efficacy
Linked drugAVUTOMETINIB
Linked drugBINIMETINIB
Linked drugCOBIMETINIB
Linked drugCOBIMETINIB FUMARATE
Approved-linked Approved
metastatic melanoma
6 linked drugs · 6 direct · 6 efficacy
Linked drugBINIMETINIB
Linked drugCOBIMETINIB
Linked drugCOBIMETINIB FUMARATE
Linked drugSELUMETINIB
Approved-linked Approved
cutaneous melanoma
5 linked drugs · 5 direct · 5 efficacy
Linked drugBINIMETINIB
Linked drugCOBIMETINIB
Linked drugPIMASERTIB
Linked drugSELUMETINIB
Approved-linked Approved
lung cancer
4 linked drugs · 4 direct · 4 efficacy
Linked drugBINIMETINIB
Linked drugCI-1040
Linked drugSELUMETINIB
Linked drugTRAMETINIB DIMETHYL SULFOXIDE
Source · ChEMBL drug mechanism + indication proxy
Review Cue

How to read disease relevance

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.

Lead diseaseneoplasm
Strongest levelApproved-linked
Block modeOpen Targets-ready proxy
Clinical Profile

Clinical Phase Distribution

22
Approved
8
Phase III
23
Phase II
12
Phase I
Assay Mix

Activity Type Distribution

IC501,459.0
KI351.0
EC5074.0
KD431.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL3819302 10.82 IC50 0.015 Preclinical
CHEMBL3818677 10.72 IC50 0.019 Preclinical
CHEMBL2087076 9.7 EC50 0.2 Preclinical
CHEMBL1614766 9.62 Kd 0.24 Preclinical
CHEMBL507361 9.48 IC50 0.33 Clinical
CHEMBL2087080 9.4 EC50 0.4 Preclinical
CHEMBL507361 9.4 Kd 0.4 Clinical
CHEMBL2103875 9.32 IC50 0.48 Approved
CHEMBL3819622 9.3 IC50 0.5 Preclinical
CHEMBL2087461 9.22 EC50 0.6 Preclinical
Distribution

pChEMBL Value Distribution

67
5.0
149
5.5
213
6.0
178
6.5
283
7.0
249
7.5
184
8.0
54
8.5
25
9.0
2
9.5
pChEMBL
Approved Drugs

Approved Drugs

SELUMETINIB
CHEMBL1614701
Approved 2020
BINIMETINIB
CHEMBL3187723
Approved 2018
NERATINIB
CHEMBL180022
Approved 2017
COBIMETINIB
CHEMBL2146883
Approved 2015
NINTEDANIB
CHEMBL502835
Approved 2014
TRAMETINIB
CHEMBL2103875
Approved 2013
BOSUTINIB
CHEMBL288441
Approved 2012
TOFACITINIB
CHEMBL221959
Approved 2012
VANDETANIB
CHEMBL24828
Approved 2011
SUNITINIB
CHEMBL535
Approved 2006
DASATINIB
CHEMBL5416410
Approved 2006
Assay Landscape

Assay Landscape

897
Total Assays
1,000
Tested Compounds
3
Assay Types
Binding — 876 assays, 1,000 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 648 828 7.2
cell-based format 103 49 7.2
assay format 94 91 6.2
subcellular format 29 32 6.2
organism-based format 2 0
Functional — 20 assays, 212 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 16 4 8.0
assay format 4 208 6.1
ADME — 1 assays, 0 compounds
BAO Format Assays Compounds Avg pChEMBL
assay format 1 0

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine