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Target Snapshot

CHEMBL252 Target Snapshot

Endothelin-1 receptor · SINGLE PROTEIN · Homo sapiens

3,414Compounds
383Assays
14Approved Drugs
3,672.0Activities
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

Endothelin-1 receptor shows approved-linked disease relevance led by IGA glomerulonephritis. 5 more disease programs remain visible in the same review block. 1 linked drug keeps the current disease frame grounded. Protein identity stays anchored to UniProt P25101. Start with IGA glomerulonephritis, then reuse UniProt P25101 as the stable protein anchor across project notes and exports.

Review focus
Review-ready target frame

Start with IGA glomerulonephritis, then reuse UniProt P25101 as the stable protein anchor across project notes and exports.

ChEMBL component mapping + Open Targets-ready proxy + ChEMBL 36 via Core Engine 2026-09-13 1 linked drug
Open source guide
Disease program
IGA glomerulonephritis

Endothelin-1 receptor shows approved-linked disease relevance led by IGA glomerulonephritis. 5 more disease programs remain visible in the same review block. 1 linked drug remains visible in the same block.

Start review with IGA glomerulonephritis because it currently carries approved-linked support. Linked drugs include SPARSENTAN. 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 1 linked drug
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 Endothelin-1 receptor as ChEMBL target CHEMBL252, mapped to UniProt P25101. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
Endothelin-1 receptor
SINGLE PROTEIN · Homo sapiens
As of 2026-09-13
ChEMBL target ID
CHEMBL252
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
P25101
Endothelin-1 receptor
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

Start with the right source

Choose the first block or source based on the question you are trying to answer.

Need stable target naming and protein identity?
UniProt Target Context
UniProt accession via ChEMBL component mapping

Start here when your first question is whether Endothelin-1 receptor is the right protein anchor across sources, using UniProt P25101 as the stable mapping.

Jump to Protein Context
Need disease fit before discussing compounds?
Disease Relevance & Evidence Level
ChEMBL drug mechanism + indication proxy

Use this block first when you need to confirm why IGA glomerulonephritis is currently framed as approved-linked support. It currently carries 1 linked drug in the same disease frame.

Jump to Disease Context
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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 LabelEndothelin-1 receptor
UniProt AccessionP25101
Component TypeProtein
Sequence Length427 aa

Endothelin-1 receptor

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as Endothelin-1 receptor, mapped to UniProt P25101. Sequence length is 427 aa.

Mapped IDP25101
Review nameEndothelin-1 receptor
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

Endothelin-1 receptor shows approved-linked disease relevance led by IGA glomerulonephritis. 5 more disease programs remain visible in the same review block.

Approved-linked Approved
IGA glomerulonephritis
1 linked drug · 1 direct · 1 efficacy
Linked drugSPARSENTAN
Late clinical Phase III
prostate cancer
3 linked drugs · 3 direct · 3 efficacy
Linked drugATRASENTAN HYDROCHLORIDE
Linked drugNEBENTAN
Linked drugZIBOTENTAN
Late clinical Phase III
cardiovascular disease
2 linked drugs · 2 direct · 2 efficacy
Linked drugBQ-123
Linked drugCLAZOSENTAN
Late clinical Phase III
heart failure
2 linked drugs · 2 direct · 2 efficacy
Linked drugBQ-123
Linked drugTEZOSENTAN
Late clinical Phase III
hypertension
2 linked drugs · 2 direct · 2 efficacy
Linked drugDARUSENTAN
Linked drugSPARSENTAN
Late clinical Phase III
diabetic nephropathy
1 linked drug · 1 direct · 1 efficacy
Linked drugAVOSENTAN
Source · ChEMBL drug mechanism + indication proxy
Review Cue

How to read disease relevance

Start review with IGA glomerulonephritis because it currently carries approved-linked support. Linked drugs include SPARSENTAN. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.

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

Clinical Phase Distribution

14
Approved
11
Phase III
8
Phase II
Assay Mix

Activity Type Distribution

IC502,535.0
KI1,118.0
EC5014.0
KD5.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL277447 11.0 Ki 0.01 Preclinical
CHEMBL440780 11.0 Ki 0.01 Preclinical
CHEMBL274489 11.0 Ki 0.01 Preclinical
CHEMBL411925 10.96 IC50 0.011 Preclinical
CHEMBL289634 10.96 IC50 0.011 Preclinical
CHEMBL286621 10.96 IC50 0.011 Preclinical
CHEMBL432856 10.85 IC50 0.014 Preclinical
CHEMBL287683 10.85 IC50 0.014 Preclinical
CHEMBL1627022 10.82 Ki 0.015 Preclinical
CHEMBL60058 10.7 IC50 0.02 Preclinical
Distribution

pChEMBL Value Distribution

130
5.0
135
5.5
180
6.0
195
6.5
194
7.0
218
7.5
248
8.0
176
8.5
128
9.0
77
9.5
pChEMBL
Approved Drugs

Approved Drugs

APROCITENTAN
CHEMBL2165326
Approved 2024
SPARSENTAN
CHEMBL539423
Approved 2023
MACITENTAN
CHEMBL2103873
Approved 2010
AMBRISENTAN
CHEMBL1111
Approved 2007
SITAXENTAN
CHEMBL282724
Approved 2006
BOSENTAN
CHEMBL957
Approved 2001
SULFISOXAZOLE
CHEMBL453
Approved 1971
Assay Landscape

Assay Landscape

383
Total Assays
1,453
Tested Compounds
4
Assay Types
Binding — 318 assays, 1,453 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 209 560 7.5
cell-based format 80 774 7.5
assay format 13 83 6.5
cell membrane format 8 13 7.4
tissue-based format 7 22 6.5
organism-based format 1 1 8.2
Functional — 62 assays, 249 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 29 131 7.7
assay format 26 101 7.6
tissue-based format 6 14 5.3
cell membrane format 1 3 8.3
Toxicity — 2 assays, 1 compounds
BAO Format Assays Compounds Avg pChEMBL
assay format 2 1 5.3
ADME — 1 assays, 0 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 1 0

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine