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Target Snapshot

CHEMBL5014 Target Snapshot

Receptor-interacting serine/threonine-protein kinase 2 · SINGLE PROTEIN · Homo sapiens

1,598Compounds
417Assays
31Approved Drugs
1,476.0Activities
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 O43353. Use UniProt O43353 as the stable identity anchor, then attach disease evidence before program review.

Review focus
Protein anchor ready

Use UniProt O43353 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 Receptor-interacting serine/threonine-protein kinase 2 as ChEMBL target CHEMBL5014, mapped to UniProt O43353. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
Receptor-interacting serine/threonine-protein kinase 2
SINGLE PROTEIN · Homo sapiens
As of 2026-09-13
ChEMBL target ID
CHEMBL5014
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
O43353
Receptor-interacting serine/threonine-protein kinase 2
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 Receptor-interacting serine/threonine-protein kinase 2 is the right protein anchor across sources, using UniProt O43353 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 LabelReceptor-interacting serine/threonine-protein kinase 2
UniProt AccessionO43353
Component TypeProtein
Sequence Length540 aa

Receptor-interacting serine/threonine-protein kinase 2

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as Receptor-interacting serine/threonine-protein kinase 2, mapped to UniProt O43353. Sequence length is 540 aa.

Mapped IDO43353
Review nameReceptor-interacting serine/threonine-protein kinase 2
OrganismHomo sapiens
Clinical Profile

Clinical Phase Distribution

31
Approved
12
Phase III
21
Phase II
9
Phase I
Assay Mix

Activity Type Distribution

IC501,048.0
KI1.0
KD427.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL4531690 10.96 IC50 0.011 Preclinical
CHEMBL4857880 10.0 IC50 0.1 Preclinical
CHEMBL4866182 9.8 IC50 0.1585 Preclinical
CHEMBL5177284 9.55 Kd 0.28 Preclinical
CHEMBL5177284 9.22 IC50 0.6 Preclinical
CHEMBL5742848 9.21 IC50 0.61 Preclinical
CHEMBL4596287 9.11 Kd 0.78 Preclinical
CHEMBL5187454 9.1 IC50 0.8 Preclinical
CHEMBL5840021 9.09 IC50 0.81 Preclinical
CHEMBL6002258 9.05 IC50 0.9 Preclinical
Distribution

pChEMBL Value Distribution

39
5.0
51
5.5
106
6.0
135
6.5
123
7.0
172
7.5
183
8.0
97
8.5
16
9.0
2
9.5
pChEMBL
Approved Drugs

Approved Drugs

ENCORAFENIB
CHEMBL3301612
Approved 2018
DACOMITINIB ANHYDROUS
CHEMBL2110732
Approved 2018
GILTERITINIB
CHEMBL3301622
Approved 2018
TIVOZANIB
CHEMBL1289494
Approved 2017
LENVATINIB
CHEMBL1289601
Approved 2015
IBRUTINIB
CHEMBL1873475
Approved 2013
DABRAFENIB
CHEMBL2028663
Approved 2013
REGORAFENIB
CHEMBL1946170
Approved 2012
PONATINIB
CHEMBL1171837
Approved 2012
CABOZANTINIB
CHEMBL2105717
Approved 2012
VEMURAFENIB
CHEMBL1229517
Approved 2011
VANDETANIB
CHEMBL24828
Approved 2011
CRIZOTINIB
CHEMBL601719
Approved 2011
PAZOPANIB
CHEMBL477772
Approved 2009
DASATINIB
CHEMBL5416410
Approved 2006
SORAFENIB
CHEMBL1336
Approved 2005
ERLOTINIB
CHEMBL553
Approved 2004
GEFITINIB
CHEMBL939
Approved 2003
Assay Landscape

Assay Landscape

417
Total Assays
724
Tested Compounds
2
Assay Types
Binding — 414 assays, 724 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 307 483 7.5
cell-based format 55 108 7.3
assay format 37 71 7.0
subcellular format 11 49 6.6
tissue-based format 4 13 6.6
ADME — 3 assays, 7 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 2 5 5.6
cell-based format 1 2 6.5

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine