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Target Snapshot

CHEMBL5393 Target Snapshot

Broad substrate specificity ATP-binding cassette transporter ABCG2 · SINGLE PROTEIN · Homo sapiens

2,195Compounds
865Assays
72Approved Drugs
2,639.0Activities
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 Q9UNQ0. Use UniProt Q9UNQ0 as the stable identity anchor, then attach disease evidence before program review.

Review focus
Protein anchor ready

Use UniProt Q9UNQ0 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 Broad substrate specificity ATP-binding cassette transporter ABCG2 as ChEMBL target CHEMBL5393, mapped to UniProt Q9UNQ0. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
Broad substrate specificity ATP-binding cassette transporter ABCG2
SINGLE PROTEIN · Homo sapiens
As of 2026-09-13
ChEMBL target ID
CHEMBL5393
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
Q9UNQ0
Broad substrate specificity ATP-binding cassette transporter ABCG2
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

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UniProt Target Context
UniProt accession via ChEMBL component mapping

Start here when your first question is whether Broad substrate specificity ATP-binding cassette transporter ABCG2 is the right protein anchor across sources, using UniProt Q9UNQ0 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

Verify identity, organism, and the fastest next research jumps from the same page.

UniProt Context

UniProt Target Context

Reviewable protein naming and mapping context for this target snapshot.

Protein LabelBroad substrate specificity ATP-binding cassette transporter ABCG2
UniProt AccessionQ9UNQ0
Component TypeProtein
Sequence Length655 aa

Broad substrate specificity ATP-binding cassette transporter ABCG2

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as Broad substrate specificity ATP-binding cassette transporter ABCG2, mapped to UniProt Q9UNQ0. Sequence length is 655 aa.

Mapped IDQ9UNQ0
Review nameBroad substrate specificity ATP-binding cassette transporter ABCG2
OrganismHomo sapiens
Clinical Profile

Clinical Phase Distribution

72
Approved
13
Phase III
13
Phase II
3
Phase I
Assay Mix

Activity Type Distribution

IC501,808.0
KI16.0
EC50815.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL2141796 10.99 EC50 0.01019 Preclinical
CHEMBL2145384 10.99 EC50 0.01013 Preclinical
CHEMBL2142245 10.96 EC50 0.01088 Preclinical
CHEMBL2137928 10.92 EC50 0.01209 Preclinical
CHEMBL2141666 10.64 EC50 0.02297 Preclinical
CHEMBL2130718 10.63 EC50 0.02338 Preclinical
CHEMBL2137680 10.39 EC50 0.04093 Preclinical
CHEMBL2140166 10.39 EC50 0.04032 Preclinical
CHEMBL2135227 10.35 EC50 0.04419 Preclinical
CHEMBL2133727 10.32 EC50 0.04775 Preclinical
Distribution

pChEMBL Value Distribution

286
5.0
346
5.5
449
6.0
377
6.5
235
7.0
132
7.5
72
8.0
23
8.5
3
9.0
1
9.5
pChEMBL
Approved Drugs

Approved Drugs

AVAPRITINIB
CHEMBL4204794
Approved 2020
FOSTAMATINIB
CHEMBL2103830
Approved 2018
TIVOZANIB
CHEMBL1289494
Approved 2017
PONATINIB
CHEMBL1171837
Approved 2012
VANDETANIB
CHEMBL24828
Approved 2011
FEBUXOSTAT
CHEMBL1164729
Approved 2008
ERLOTINIB
CHEMBL553
Approved 2004
GEFITINIB
CHEMBL939
Approved 2003
IMATINIB
CHEMBL941
Approved 2001
ATOVAQUONE
CHEMBL1450
Approved 1992
MITOXANTRONE
CHEMBL58
Approved 1987
CYCLOSPORINE
CHEMBL160
Approved 1983
VERAPAMIL
CHEMBL6966
Approved 1981
DIETHYLSTILBESTROL
CHEMBL411
Approved 1973
SULFASALAZINE
CHEMBL421
Approved 1950
Assay Landscape

Assay Landscape

867
Total Assays
1,414
Tested Compounds
4
Assay Types
Binding — 640 assays, 1,414 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 506 1,204 6.2
single protein format 60 61 6.3
assay format 50 87 7.1
cell membrane format 18 44 5.6
tissue-based format 6 18 6.3
ADME — 115 assays, 6 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 91 1 5.6
single protein format 17 3 4.8
assay format 2 2 4.8
cell membrane format 2 0
mitochondrion format 2 0
tissue-based format 1 0
Functional — 111 assays, 129 compounds
BAO Format Assays Compounds Avg pChEMBL
cell-based format 74 13 5.9
cell membrane format 33 4 5.9
assay format 4 112 7.2
Toxicity — 1 assays, 4 compounds
BAO Format Assays Compounds Avg pChEMBL
cell membrane format 1 4 4.6

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine