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Target Snapshot

CHEMBL2189116 Target Snapshot

Histone-lysine N-methyltransferase EZH1 · SINGLE PROTEIN · Homo sapiens

132Compounds
62Assays
1Approved Drugs
144.0Activities
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 2026-09-13

Protein identity stays anchored to UniProt Q92800. Use UniProt Q92800 as the stable identity anchor, then attach disease evidence before program review.

Review focus
Protein anchor ready

Use UniProt Q92800 as the stable identity anchor, then attach disease evidence before program review.

ChEMBL component mapping + Open Targets-ready proxy + ChEMBL 36 via Core Engine 2026-09-13
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 Histone-lysine N-methyltransferase EZH1 as ChEMBL target CHEMBL2189116, mapped to UniProt Q92800. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
Histone-lysine N-methyltransferase EZH1
SINGLE PROTEIN · Homo sapiens
As of 2026-09-13
ChEMBL target ID
CHEMBL2189116
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
Q92800
Histone-lysine N-methyltransferase EZH1
UniProt accession via ChEMBL component mapping As of 2026-09-13
www.uniprot.org
Disease evidence contract
Open Targets-ready proxy
ChEMBL drug mechanism + indication proxy
ChEMBL drug mechanism + indication proxy As of 2026-09-13
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 Histone-lysine N-methyltransferase EZH1 is the right protein anchor across sources, using UniProt Q92800 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 LabelHistone-lysine N-methyltransferase EZH1
UniProt AccessionQ92800
Component TypeProtein
Sequence Length747 aa

Histone-lysine N-methyltransferase EZH1

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as Histone-lysine N-methyltransferase EZH1, mapped to UniProt Q92800. Sequence length is 747 aa.

Mapped IDQ92800
Review nameHistone-lysine N-methyltransferase EZH1
OrganismHomo sapiens
Clinical Profile

Clinical Phase Distribution

1
Approved
2
Phase II
2
Phase I
Assay Mix

Activity Type Distribution

IC50140.0
KI2.0
EC502.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL4597193 9.36 IC50 0.44 Clinical
CHEMBL5197386 9.33 IC50 0.47 Preclinical
CHEMBL5185991 8.15 IC50 7.0 Preclinical
CHEMBL6032817 8.08 IC50 8.31 Preclinical
CHEMBL5289464 8.07 IC50 8.6 Preclinical
CHEMBL5840996 7.92 IC50 12.0 Preclinical
CHEMBL5922751 7.92 IC50 12.0 Preclinical
CHEMBL3414574 7.89 IC50 13.0 Preclinical
CHEMBL5791232 7.85 IC50 14.0 Preclinical
CHEMBL5956024 7.82 IC50 15.0 Preclinical
Distribution

pChEMBL Value Distribution

6
5.0
10
5.5
8
6.0
16
6.5
19
7.0
18
7.5
4
8.0
0
8.5
2
9.0
0
9.5
pChEMBL
Approved Drugs

Approved Drugs

TAZEMETOSTAT
CHEMBL3414621
Approved 2020
Assay Landscape

Assay Landscape

62
Total Assays
69
Tested Compounds
2
Assay Types
Binding — 59 assays, 69 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 51 67 6.9
assay format 4 1 6.8
cell-based format 4 1 7.1
Functional — 3 assays, 1 compounds
BAO Format Assays Compounds Avg pChEMBL
assay format 2 1 7.2
cell-based format 1 0

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine