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Target Snapshot

CHEMBL5251 Target Snapshot

Tyrosine-protein kinase BTK · SINGLE PROTEIN · Homo sapiens

14,839Compounds
1,626Assays
33Approved Drugs
23,795.0Activities
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

Tyrosine-protein kinase BTK shows approved-linked disease relevance led by chronic lymphocytic leukemia. 5 more disease programs remain visible in the same review block. 8 linked drugs keep the current disease frame grounded. Protein identity stays anchored to UniProt Q06187. Start with chronic lymphocytic leukemia, then reuse UniProt Q06187 as the stable protein anchor across project notes and exports.

Review focus
Review-ready target frame

Start with chronic lymphocytic leukemia, then reuse UniProt Q06187 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 8 linked drugs
Open source guide
Disease program
chronic lymphocytic leukemia

Tyrosine-protein kinase BTK shows approved-linked disease relevance led by chronic lymphocytic leukemia. 5 more disease programs remain visible in the same review block. 8 linked drugs remain visible in the same block.

Start review with chronic lymphocytic leukemia because it currently carries approved-linked support. Linked drugs include ACALABRUTINIB, ACALABRUTINIB MALEATE, EDRALBRUTINIB, IBRUTINIB. 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 8 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 Tyrosine-protein kinase BTK as ChEMBL target CHEMBL5251, mapped to UniProt Q06187. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
Tyrosine-protein kinase BTK
SINGLE PROTEIN · Homo sapiens
As of 2026-09-13
ChEMBL target ID
CHEMBL5251
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
Q06187
Tyrosine-protein kinase BTK
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 Tyrosine-protein kinase BTK is the right protein anchor across sources, using UniProt Q06187 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 chronic lymphocytic leukemia is currently framed as approved-linked support. It currently carries 8 linked drugs in the same disease frame.

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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 LabelTyrosine-protein kinase BTK
UniProt AccessionQ06187
Component TypeProtein
Sequence Length659 aa

Tyrosine-protein kinase BTK

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as Tyrosine-protein kinase BTK, mapped to UniProt Q06187. Sequence length is 659 aa.

Mapped IDQ06187
Review nameTyrosine-protein kinase BTK
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

Tyrosine-protein kinase BTK shows approved-linked disease relevance led by chronic lymphocytic leukemia. 5 more disease programs remain visible in the same review block.

Approved-linked Approved
chronic lymphocytic leukemia
8 linked drugs · 8 direct · 8 efficacy
Linked drugACALABRUTINIB
Linked drugACALABRUTINIB MALEATE
Linked drugEDRALBRUTINIB
Linked drugIBRUTINIB
Approved-linked Approved
neoplasm
8 linked drugs · 8 direct · 8 efficacy
Linked drugACALABRUTINIB
Linked drugEDRALBRUTINIB
Linked drugIBRUTINIB
Linked drugORELABRUTINIB
Approved-linked Approved
Mantle cell lymphoma
6 linked drugs · 6 direct · 6 efficacy
Linked drugACALABRUTINIB
Linked drugACALABRUTINIB MALEATE
Linked drugIBRUTINIB
Linked drugORELABRUTINIB
Approved-linked Approved
cancer
5 linked drugs · 5 direct · 5 efficacy
Linked drugACALABRUTINIB
Linked drugIBRUTINIB
Linked drugORELABRUTINIB
Linked drugTIRABRUTINIB
Approved-linked Approved
Waldenstrom macroglobulinemia
5 linked drugs · 5 direct · 5 efficacy
Linked drugACALABRUTINIB
Linked drugIBRUTINIB
Linked drugORELABRUTINIB
Linked drugPIRTOBRUTINIB
Approved-linked Approved
macroglobulinemia
1 linked drug · 1 direct · 1 efficacy
Linked drugIBRUTINIB
Source · ChEMBL drug mechanism + indication proxy
Review Cue

How to read disease relevance

Start review with chronic lymphocytic leukemia because it currently carries approved-linked support. Linked drugs include ACALABRUTINIB, ACALABRUTINIB MALEATE, EDRALBRUTINIB, IBRUTINIB. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.

Lead diseasechronic lymphocytic leukemia
Strongest levelApproved-linked
Block modeOpen Targets-ready proxy
Clinical Profile

Clinical Phase Distribution

33
Approved
25
Phase III
37
Phase II
16
Phase I
Assay Mix

Activity Type Distribution

IC5021,606.0
KI1,013.0
EC50733.0
KD443.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL4762397 10.85 IC50 0.014 Preclinical
CHEMBL5977366 10.54 IC50 0.029 Preclinical
CHEMBL5945342 10.4 IC50 0.04 Preclinical
CHEMBL5826570 10.4 IC50 0.04 Preclinical
CHEMBL5884405 10.35 IC50 0.045 Preclinical
CHEMBL5909954 10.34 IC50 0.046 Preclinical
CHEMBL5789446 10.33 IC50 0.047 Preclinical
CHEMBL5749648 10.31 IC50 0.049 Preclinical
CHEMBL5799170 10.3 IC50 0.05 Preclinical
CHEMBL5741138 10.3 IC50 0.05 Preclinical
Distribution

pChEMBL Value Distribution

692
5.0
532
5.5
2253
6.0
1591
6.5
2869
7.0
2135
7.5
2332
8.0
1891
8.5
1736
9.0
756
9.5
pChEMBL
Approved Drugs

Approved Drugs

RITLECITINIB
CHEMBL4085457
Approved 2023
FUTIBATINIB
CHEMBL3701238
Approved 2022
TIRABRUTINIB
CHEMBL4071161
Approved 2020
FEDRATINIB
CHEMBL1287853
Approved 2019
ENTRECTINIB
CHEMBL1983268
Approved 2019
ZANUBRUTINIB
CHEMBL3936761
Approved 2019
NERATINIB
CHEMBL180022
Approved 2017
BRIGATINIB
CHEMBL3545311
Approved 2017
ACALABRUTINIB
CHEMBL3707348
Approved 2017
OLMUTINIB
CHEMBL3786343
Approved 2016
OSIMERTINIB
CHEMBL3353410
Approved 2015
NINTEDANIB
CHEMBL502835
Approved 2014
IBRUTINIB
CHEMBL1873475
Approved 2013
BOSUTINIB
CHEMBL288441
Approved 2012
DASATINIB
CHEMBL5416410
Approved 2006
MITOXANTRONE
CHEMBL58
Approved 1987
Assay Landscape

Assay Landscape

1,626
Total Assays
11,109
Tested Compounds
3
Assay Types
Binding — 1,600 assays, 11,109 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 959 6,794 7.7
cell-based format 407 1,784 7.7
assay format 183 2,307 7.3
tissue-based format 33 192 7.2
subcellular format 16 31 6.3
cell membrane format 1 1 7.8
organism-based format 1 0
Functional — 23 assays, 147 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 14 3 6.8
assay format 3 143 6.2
organism-based format 3 0
tissue-based format 3 1 6.9
ADME — 3 assays, 0 compounds
BAO Format Assays Compounds Avg pChEMBL
assay format 2 0
single protein format 1 0

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine