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Evidence Snapshot

Endothelin-1 receptor

CHEMBL252 SINGLE PROTEIN Homo sapiens
Source Header

ChEMBL 36 via Core Engine

Target Snapshot 2026-09-13T20:44:05Z
Source · ChEMBL 36 via Core Engine
ChEMBL ChEMBL 36 CHEMBL252
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.

Review-ready Target Rationale

Why Endothelin-1 receptor matters

As of 2026-09-13

Endothelin-1 receptor is reviewed as Endothelin-1 receptor (UniProt P25101); 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 keep this evidence frame grounded.; the current evidence base includes 14 approved drugs, 3414 compounds, and 383 assays, with lead potency reaching pChEMBL 11.0.

Disease context
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 keep the rationale reviewable. 5 additional disease programs remain visible in the same card. Linked drugs include SPARSENTAN.

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.

ChEMBL target record
Approved-linked 1 linked drug
Activity base
Portfolio and assay base

ChEMBL currently tracks 14 approved drugs, 3414 compounds, and 383 assays for this target. The dominant activity type is IC50. CHEMBL277447 is the current potency anchor at pChEMBL 11.0.

Use CHEMBL277447 as the tractability anchor when discussing potency (pChEMBL 11.0).

Activity source · ChEMBL 36 via Core Engine
14 approved pChEMBL 11.0
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 Endothelin-1 receptor matters before drilling into raw source blocks.

Jump to Review Rationale
Need 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 P25101, not just the summarized rationale.

Open Protein Context
Need 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 IGA glomerulonephritis is currently treated as approved-linked support.

Open Disease Context

Snapshot State

No project snapshot selected. Export uses the live evidence card state.

3414
Total Compounds
383
Total Assays
14
Approved Drugs
IC50: 2535.0, KI: 1118.0, EC50: 14.0, KD: 5.0
Activity Types

pChEMBL Activity Distribution

Top 5 Inhibitors (by pChEMBL)

Structure Compound pChEMBL Type Phase
No preferred name
CHEMBL277447
 11.0 Ki —
No preferred name
CHEMBL440780
 11.0 Ki —
No preferred name
CHEMBL274489
 11.0 Ki —
No preferred name
CHEMBL411925
 11.0 IC50 —
No preferred name
CHEMBL289634
 11.0 IC50 —

Approved Drugs

Structure Compound First Approval
APROCITENTAN
CHEMBL2165326
 2024
SPARSENTAN
CHEMBL539423
 2023
MACITENTAN
CHEMBL2103873
 2010
AMBRISENTAN
CHEMBL1111
 2007
SITAXENTAN
CHEMBL282724
 2006
BOSENTAN
CHEMBL957
 2001
SULFISOXAZOLE
CHEMBL453
 1971
← Target Page
Source Header

ChEMBL 36 via Core Engine

Target Snapshot 2026-09-13T20:44:05Z
Source · ChEMBL 36 via Core Engine
ChEMBL ChEMBL 36 CHEMBL252