ABCG2

Summary

ABCG2 (ATP binding cassette subfamily G member 2 (JR blood group), HGNC:74) is a protein-coding gene on chromosome 4q22.1, encoding Broad substrate specificity ATP-binding cassette transporter ABCG2 (Q9UNQ0). Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells.

The membrane-associated protein encoded by this gene is included in the superfamily of ATP-binding cassette (ABC) transporters. ABC proteins transport various molecules across extra- and intra-cellular membranes. ABC genes are divided into seven distinct subfamilies (ABC1, MDR/TAP, MRP, ALD, OABP, GCN20, White). This protein is a member of the White subfamily. Alternatively referred to as a breast cancer resistance protein, this protein functions as a xenobiotic transporter which may play a major role in multi-drug resistance. It likely serves as a cellular defense mechanism in response to mitoxantrone and anthracycline exposure. Significant expression of this protein has been observed in the placenta, which may suggest a potential role for this molecule in placenta tissue. Multiple transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 9429 — RefSeq curated summary.

At a glance

• GWAS associations: 96 (top 1% of genes corpus-wide)
• Clinical variants (ClinVar): 107 total — 16 pathogenic, 1 likely-pathogenic
• GTEx eGene: eQTL in 25 tissues, sQTL in 1 (q < 0.05)
• Phenotypes (HPO): 5
• ChEMBL bioactivity: 92 clinical-phase molecules tested; no curated mechanism-of-action drug
• Pharmacogenomics (PharmGKB): 3 CPIC/DPWG dosing guidelines (e.g. rosuvastatin, atorvastatin;fluvastatin;lovastatin;pitavastatin;pravastatin;simvastatin, allopurinol)
• Constraint (gnomAD): pLI 0.00 (LoF-tolerant), LOEUF 1.31 (unconstrained)
• MANE Select transcript: NM_004827
• Interaction hub: 2,890 STRING partners (top 3% of genes corpus-wide)

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:74
Approved symbol	ABCG2
Name	ATP binding cassette subfamily G member 2 (JR blood group)
Location	4q22.1
Locus type	gene with protein product
Status	Approved
Aliases	EST157481, MXR, BCRP, ABCP, CD338
Ensembl gene	ENSG00000118777
Ensembl biotype	protein_coding
OMIM	603756
Entrez	9429

Gene structure

Transcript identifiers

Ensembl transcripts: 33 — 33 protein_coding

MANE Select: ENST00000237612

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 4

ENST00000237612, ENST00000503830, ENST00000505480, ENST00000515655, ENST00000650821, ENST00000889078, ENST00000889079, ENST00000889080, ENST00000889081, ENST00000889082, ENST00000889083, ENST00000889084, ENST00000889085, ENST00000889086, ENST00000889087, ENST00000889088, ENST00000889089, ENST00000889090, ENST00000889091, ENST00000889092, ENST00000889093, ENST00000889094, ENST00000889095, ENST00000889096, ENST00000889097, ENST00000889098, ENST00000889099, ENST00000889100, ENST00000962213, ENST00000962214, ENST00000962215, ENST00001112460, ENST00001140386

RefSeq mRNA: 13 — MANE Select: NM_004827 NM_001257386, NM_001348985, NM_001348986, NM_001348987, NM_001348988, NM_001348989, NM_001441208, NM_001441209, NM_001441210, NM_001441211, NM_001441212, NM_001441213, NM_004827

CCDS: CCDS3628, CCDS58910

Canonical transcript exons

ENST00000237612 — 16 exons

Exon	Start	End
ENSE00000801180	88095520	88095609
ENSE00000801181	88097453	88097607
ENSE00000801182	88099324	88099448
ENSE00000801183	88101230	88101319
ENSE00000801184	88107184	88107266
ENSE00000801185	88113303	88113553
ENSE00000801186	88114957	88115058
ENSE00000801187	88118109	88118260
ENSE00000801188	88121635	88121792
ENSE00000801189	88131061	88131213
ENSE00000801190	88131803	88131917
ENSE00000801191	88132576	88132635
ENSE00001196220	88090269	88092381
ENSE00001342969	88158386	88158639
ENSE00003465456	88139793	88140014
ENSE00003501294	88094577	88094659

Expression profiles

Bgee: expression breadth ubiquitous, 245 present calls, max score 98.97.

FANTOM5 (CAGE): breadth broad, TPM avg 4.4675 / max 251.9052, expressed in 755 samples.

Highest expression (Bgee): jejunal mucosa, ileal mucosa, endothelial cell, mucosa of transverse colon, seminal vesicle.

Genetic regulation across tissues (GTEx eQTL / sQTL)

ABCG2 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 25 tissues and its splicing (sQTL) in 1 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

showing 20 of 26 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Whole Blood	eqtl	2.0e-10	+0.25	4:88231566:A:G
Testis	eqtl	9.5e-09	-0.35	4:88206187:G:A
Thyroid	eqtl	1.6e-08	+0.27	4:88203626:C:T
Adipose Subcutaneous	eqtl	1.8e-06	+0.20	4:88201681:G:A
Artery Aorta	eqtl	8.6e-05	-0.27	4:88219681:A:C
Skin Not Sun Exposed Suprapubic	eqtl	1.0e-04	-0.27	4:88143807:AC:A
Artery Coronary	eqtl	3.4e-04	-0.26	4:88240750:C:T
Skin Sun Exposed Lower leg	eqtl	5.4e-04	+0.18	4:88144716:A:C
Spleen	eqtl	5.5e-04	-0.41	4:88242371:A:G
Adipose Visceral Omentum	eqtl	8.9e-04	+0.19	4:88205495:C:T
Esophagus Muscularis	eqtl	1.4e-03	+0.21	4:88206329:G:A
Brain Spinal cord cervical c-1	eqtl	9.8e-03	+2.37	4:87537090:G:T
Esophagus Gastroesophageal Junction	eqtl	1.0e-02	+0.21	4:88205615:C:T
Minor Salivary Gland	eqtl	1.1e-02	-1.08	4:87966021:C:T
Esophagus Mucosa	eqtl	1.3e-02	+0.17	4:88202773:C:T
Cells Cultured fibroblasts	eqtl	1.8e-02	-0.60	4:87966452:T:G
Stomach	eqtl	2.0e-02	+0.22	4:88234909:T:C
Liver	eqtl	2.4e-02	+0.27	4:88102072:G:A
Ovary	sqtl	3.0e-02	+0.68	4:88207261:T:C
Muscle Skeletal	eqtl	3.2e-02	+0.14	4:88234909:T:C

FANTOM5 promoters

showing 10 of 16 alternative TSS:

Promoter ID	TPM avg	Samples expressed
53072	1.3827	451
53070	1.1039	397
53066	0.4975	171
53069	0.3850	139
53076	0.3049	124
53067	0.2214	126
53071	0.1631	70
53075	0.1283	47
53068	0.1024	57
53078	0.0481	15

Top tissues by expression

showing 100 of 290 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
jejunal mucosa	UBERON:0000399	98.97	gold quality
ileal mucosa	UBERON:0000331	98.67	gold quality
endothelial cell	CL:0000115	95.45	gold quality
mucosa of transverse colon	UBERON:0004991	94.43	gold quality
seminal vesicle	UBERON:0000998	94.20	gold quality
duodenum	UBERON:0002114	93.87	gold quality
substantia nigra	UBERON:0002038	87.82	gold quality
medial globus pallidus	UBERON:0002477	87.80	gold quality
colonic mucosa	UBERON:0000317	87.50	gold quality
placenta	UBERON:0001987	87.32	gold quality
midbrain	UBERON:0001891	87.31	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	87.00	gold quality
inferior vagus X ganglion	UBERON:0005363	86.89	gold quality
subthalamic nucleus	UBERON:0001906	86.88	gold quality
spinal cord	UBERON:0002240	85.98	gold quality
globus pallidus	UBERON:0001875	85.81	gold quality
dorsal motor nucleus of vagus nerve	UBERON:0002870	85.53	gold quality
postcentral gyrus	UBERON:0002581	85.52	gold quality
putamen	UBERON:0001874	85.06	gold quality
rectum	UBERON:0001052	85.03	gold quality
caudate nucleus	UBERON:0001873	85.00	gold quality
prefrontal cortex	UBERON:0000451	84.87	gold quality
lateral nuclear group of thalamus	UBERON:0002736	84.87	gold quality
Ammon’s horn	UBERON:0001954	84.66	gold quality
hypothalamus	UBERON:0001898	84.63	gold quality
mucosa of sigmoid colon	UBERON:0004993	84.53	gold quality
medulla oblongata	UBERON:0001896	83.88	gold quality
parietal lobe	UBERON:0001872	83.83	gold quality
amygdala	UBERON:0001876	83.69	gold quality
superior vestibular nucleus	UBERON:0007227	83.32	gold quality
dorsal plus ventral thalamus	UBERON:0001897	83.20	gold quality
body of uterus	UBERON:0009853	83.15	gold quality
endocervix	UBERON:0000458	82.58	gold quality
cingulate cortex	UBERON:0003027	82.51	gold quality
anterior cingulate cortex	UBERON:0009835	82.48	gold quality
corpus callosum	UBERON:0002336	82.42	gold quality
telencephalon	UBERON:0001893	82.11	gold quality
frontal cortex	UBERON:0001870	82.09	gold quality
Brodmann (1909) area 46	UBERON:0006483	82.08	gold quality
superior frontal gyrus	UBERON:0002661	82.03	gold quality
ventral tegmental area	UBERON:0002691	81.93	gold quality
small intestine	UBERON:0002108	81.88	gold quality
liver	UBERON:0002107	81.81	gold quality
substantia nigra pars compacta	UBERON:0001965	81.74	gold quality
temporal lobe	UBERON:0001871	81.73	gold quality
forebrain	UBERON:0001890	81.73	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	81.59	gold quality
neocortex	UBERON:0001950	81.53	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	81.51	gold quality
cerebral cortex	UBERON:0000956	81.46	gold quality
substantia nigra pars reticulata	UBERON:0001966	81.24	gold quality
inferior olivary complex	UBERON:0002127	81.24	gold quality
choroid plexus epithelium	UBERON:0003911	81.21	gold quality
central nervous system	UBERON:0001017	80.99	gold quality
brain	UBERON:0000955	80.82	gold quality
visceral pleura	UBERON:0002401	80.78	gold quality
pons	UBERON:0000988	80.66	gold quality
small intestine Peyer’s patch	UBERON:0003454	80.57	gold quality
frontal pole	UBERON:0002795	80.50	gold quality
entorhinal cortex	UBERON:0002728	80.47	gold quality
nucleus accumbens	UBERON:0001882	80.45	gold quality
right frontal lobe	UBERON:0002810	80.33	gold quality
myometrium	UBERON:0001296	80.27	gold quality
paraflocculus	UBERON:0005351	80.21	gold quality
trigeminal ganglion	UBERON:0001675	79.90	gold quality
Brodmann (1909) area 9	UBERON:0013540	79.87	gold quality
middle frontal gyrus	UBERON:0002702	79.71	gold quality
jejunum	UBERON:0002115	79.52	gold quality
orbitofrontal cortex	UBERON:0004167	79.41	gold quality
right lobe of liver	UBERON:0001114	78.68	gold quality
adrenal tissue	UBERON:0018303	78.24	gold quality
smooth muscle tissue	UBERON:0001135	77.47	gold quality
ectocervix	UBERON:0012249	77.31	gold quality
trabecular bone tissue	UBERON:0002483	77.29	gold quality
primary visual cortex	UBERON:0002436	77.15	gold quality
sperm	CL:0000019	77.08	gold quality
occipital lobe	UBERON:0002021	77.06	gold quality
left uterine tube	UBERON:0001303	76.76	gold quality
Brodmann (1909) area 10	UBERON:0013541	76.70	gold quality
lateral globus pallidus	UBERON:0002476	76.31	gold quality
uterus	UBERON:0000995	75.97	gold quality
gall bladder	UBERON:0002110	75.37	gold quality
pituitary gland	UBERON:0000007	75.32	gold quality
male germ cell	CL:0000015	74.86	gold quality
adenohypophysis	UBERON:0002196	74.85	gold quality
urethra	UBERON:0000057	74.73	gold quality
female reproductive system	UBERON:0000474	74.51	gold quality
transverse colon	UBERON:0001157	74.47	gold quality
intestine	UBERON:0000160	74.39	gold quality
cerebellum	UBERON:0002037	73.53	gold quality
cerebellar cortex	UBERON:0002129	73.44	gold quality
right hemisphere of cerebellum	UBERON:0014890	73.33	gold quality
cerebellar hemisphere	UBERON:0002245	73.31	gold quality
CA1 field of hippocampus	UBERON:0003881	72.83	gold quality
endometrium	UBERON:0001295	72.29	gold quality
cerebellar vermis	UBERON:0004720	72.23	gold quality
ganglionic eminence	UBERON:0004023	72.07	gold quality
left ovary	UBERON:0002119	72.05	gold quality
large intestine	UBERON:0000059	71.72	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	71.62	gold quality

Single-cell (SCXA)

Detected in 8 experiment(s), a significant marker in 7.

Experiment	Marker?	Max mean expression
E-MTAB-6819	yes	387.44
E-MTAB-10018	yes	209.80
E-MTAB-6701	yes	45.98
E-GEOD-135922	yes	45.47
E-MTAB-9388	yes	7.38
E-GEOD-137537	yes	6.21
E-MTAB-2983	no	495.00
E-ANND-3	no	0.00

HPA expression

RNA tissue specificity: Tissue enhanced

showing 60 of 76 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Small intestine	tissue	83.2	high
Putamen	tissue	47.4
Substantia nigra	tissue	47.4
Medulla oblongata	tissue	45.6
Duodenum	tissue	45.4	high
Spinal cord	tissue	45.4
Thalamus	tissue	45.0
Cerebral cortex	tissue	44.6	low
Insular cortex	tissue	44.6
Motor cortex	tissue	44.4
Somatosensory cortex	tissue	43.9
Superior colliculi	tissue	43.7
Occipital cortex	tissue	43.7
Pons	tissue	43.4
Midbrain	tissue	42.3
Prefrontal cortex	tissue	41.6
Retrosplenial cortex	tissue	40.9
Retrosplenial and cingulate cortex	tissue	40.4
Temporal cortex	tissue	39.7
Ventral forebrain	tissue	39.0
Corpus callosum	tissue	38.3
Hypothalamus	tissue	38.2
Basal ganglia	tissue	38.0	not detected
Hippocampal formation	tissue	38.0
Entorhinal cortex	tissue	38.0
Amygdala	tissue	36.2
Septum	tissue	36.2
Olfactory bulb	tissue	35.4
Liver	tissue	33.7	not detected
Periaqueductal gray	tissue	32.8
Seminal vesicle	tissue	31.9	high
Cerebellum	tissue	29.8	not detected
Locus coeruleus	tissue	26.4
Hippocampus	tissue	25.6	not detected
Endometrium 1	tissue	21.6	not detected
Postcentral gyrus	tissue	21.6
Cervix	tissue	20.8	not detected
Nucleus accumbens	tissue	20.0
Smooth muscle	tissue	18.5	medium
Colon	tissue	14.7	high
Rectum	tissue	13.0	high
Placenta	tissue	11.0	medium
Choroid plexus	tissue	10.1
Ovary	tissue	9.8	not detected
Fallopian tube	tissue	9.2	not detected
Pituitary gland	tissue	7.9
Prostate	tissue	6.6	not detected
Epididymis	tissue	6.4	not detected
Thyroid gland	tissue	6.0	low
Lung	tissue	4.8	low
Gallbladder	tissue	4.8	not detected
Salivary gland	tissue	4.7	not detected
Parathyroid gland	tissue	4.2	not detected
Adrenal gland	tissue	3.8	low
Breast	tissue	3.7	not detected
Vagina	tissue	3.7	not detected
Kidney	tissue	3.3	medium
Testis	tissue	2.8	medium
Heart muscle	tissue	2.7	low
Retina	tissue	2.3

Brain sub-regions (HPA Brain Atlas): detected in 189; highest nTPM — Posterior thalamic nucleus (59.9), Dorsal cochlear nucleus (59.5), Nucleus cuneatus (56.3), Reticulotegmental nucleus (52.4), Inferior olive (51.1).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AHR, E2F1, ESR1, ESR2, FOXC1, GLI1, HIF1A, KLF5, MSX2, NFE2L2, NFKB1, NFKB, NR1I2, NR3C1, PGR, PPARA, PPARG, RARA, RELA, SALL4, SMAD2, SMARCA4, SP1, SP3, TP53

miRNA regulators (miRDB)

Targeting ABCG2 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

showing 30 of 104 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-6873-3P	100.00	71.42	2626
HSA-MIR-6833-3P	100.00	70.63	3197
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-4768-5P	100.00	69.49	2861
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-4747-5P	100.00	67.90	2681
HSA-MIR-5196-5P	100.00	67.98	2761
HSA-MIR-196A-1-3P	99.99	72.15	2772
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-548N	99.98	71.94	4170
HSA-MIR-4482-3P	99.98	72.50	3147
HSA-MIR-512-3P	99.97	67.35	1049
HSA-MIR-302E	99.96	70.74	2669
HSA-MIR-570-3P	99.96	72.41	4910
HSA-MIR-548AT-5P	99.96	70.83	2666
HSA-MIR-3143	99.93	71.96	3104
HSA-MIR-218-5P	99.93	72.22	2103
HSA-MIR-3119	99.92	71.34	2390
HSA-MIR-3529-3P	99.90	73.55	3045
HSA-MIR-302A-3P	99.89	71.23	1777
HSA-MIR-302B-3P	99.89	71.23	1777
HSA-MIR-302C-3P	99.89	71.20	1778
HSA-MIR-302D-3P	99.89	71.25	1777
HSA-MIR-7845-5P	99.88	64.88	771
HSA-MIR-12119	99.87	68.35	1653
HSA-MIR-579-3P	99.86	71.66	3628
HSA-MIR-520E-3P	99.84	70.55	1698
HSA-MIR-373-3P	99.84	70.68	1668

Functional genomics

gnomAD constraint: pLI 5.07e-29, LOEUF 1.31, missense Z 0.509 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000237612 — one region, missense o/e 1.01.

Literature-anchored findings (GeneRIF, showing 40)

• role in transport of 7-ethyl-10-hydroxycamptothecin (SN-38) in human lung cancer cells (PMID:11688982)
• ABCG2 protein effluxes hoechst 33342 in hematopoietic stem cells (PMID:11801536)
• homodimer formation is essential for BCRP drug resistance (PMID:11807788)
• There is no indication that elevated BCRP expression in breast carcinomas confers resistance to anthracyclines. (PMID:11948115)
• Increased expression in relapsed or refractory acute myeloid leukemia compared to level at diagnosis. (PMID:11986944)
• Expression of the BCRP gene reduces the response to chemotherapy in AML and that BCRP expression is higher at the time of relapse. (PMID:12145683)
• Overexpression of wild-type breast cancer resistance protein mediates methotrexate resistance. (PMID:12208758)
• involvement of ABCG2 in multidrug resistance in cancer, especially with regard to acute myeloid leukemia (PMID:12369998)
• characterization of different isoforms without possible endogenous dimerization partners (PMID:12374800)
• ABCG2 expression conferred resistance to mitoxantrone & topotecan, but not to idarubicin. High levels of ABCG2 mRNA expression in adult AML blast specimens are relatively uncommon. ABCG2 expression may be limited to a small cell subpopulation. (PMID:12393637)
• The breast cancer resistance protein protects against pheophorbide a, a major chlorophyll-derived dietary phototoxin, and protoporphyria. (PMID:12429862)
• In both normal and tumour brain tissue, BCRP is located at the blood-brain barrier, mainly at the luminal surface of microvessel endothelium. It may pose an additional barrier to drug access to the brain. (PMID:12438926)
• results showed that ABCG2 confers resistance to indolocarbazoles by transporting them in an energy-dependent manner (PMID:12459192)
• polymorphisms in BCRP1 result in low amounts of BCRP, which results in hypersensitivity of normal cells to such anticancer drugs as irinotecan and mitoxantrone (PMID:12479221)
• RNA expression of this protein in breast cancer correlates with response to chemotherapy. (PMID:12576456)
• Function of the ABC transporters, P-gp, multidrug resistance protein and BCRP, in minimal residual disease in acute myeloid leukemia (PMID:12604403)
• BCRP may play a role in the transport of sterols in human, in addition to its ability to transport multiple drugs and toxins. (PMID:12668685)
• transports sulfated conjugates of steroids and xenobiotics (PMID:12682043)
• functional study on polymorphism and determination of critical role of arginine-482 in methotrexate transport (PMID:12741957)
• Wld-type as well as R482T BCRP mediates cellular efflux of 9-AC but not 9-NC. Zplar groups at the 9 or 10 position of the CPT A ring facilitate interaction with BCRP. (PMID:12810652)
• ABCG2 is a component of the energy-dependent efflux system for certain folates and antifolates. (PMID:12874005)
• ABCG2 is expressed and functions as a transporter in the brain. (PMID:12958161)
• Single amino acid substitutions in the transmembrane domains of breast cancer resistance protein (BCRP) alter cross resistance patterns in transfectants (PMID:14566825)
• REVIEW: multidrug resistance in breast cancer (PMID:14576842)
• Higher ABCG2 expression is associated with T-lineage acute lymphoblastic leukemia (PMID:14613996)
• human ABCG2 likely exists and functions as a homotetramer (PMID:15001581)
• BCRP may serve as a molecular target for reducing drug resistance to chemotherapy in advanced lung cancer patients. (PMID:15014021)
• VX-710 modulates Pgp, MRP-1, and BCRP(R482), and has potential as a clinical broad-spectrum multidrug resistance modulator in malignancies. (PMID:15014037)
• ABCG2 overexpression is associated with drug resistance to SN38 in colon cancer cells and in irinotecan-treated metastases (PMID:15027118)
• Bcrp/ABCG2 enhances hypoxic cell survival through interactions with heme (PMID:15044468)
• subcellular localization of ABCG2 in gallbladder adenocarcinoma (PMID:15146167)
• As a method of circumventing ABCG2-associated drug resistance, low-polarity camptothecin analogues are considered to be potent lead compounds. (PMID:15170677)
• BCRP mRNA levels, antibody staining and function correlated strongly in cell lines but not in acute myeloid leukemia samples, suggesting complex biology of BCRP in AML and incomplete modeling by cell lines (PMID:15208643)
• imatinib is a substrate for BCRP; it competes with mitoxantrone for drug export (PMID:15251980)
• GXXXG motif promotes proper packing of the transmembrane segments in the functional ABCG2 homodimer, although it does not solely arbitrate dimerization (PMID:15260487)
• Results suggest that 1) the predominant allelic expression pattern of BCRP in placental samples is biallelic, and 2) the mutation C421A is not a genetic variant acting in cis, but is considered to influence translation efficiency. (PMID:15475413)
• conformational changes of the ABCG2 multidrug transporter modify its interaction with a monoclonal antibody on the cell surface (PMID:15557326)
• Cyclosporin A is neither a substrate nor an inhibitor of the human ABCG2 transporter. (PMID:15598974)
• The breast cancer resistance protein (BCRP) can be expressed in AML and BCRP mRNA expression was determined in samples from 40 AML patients by real-time RT-PCR. (PMID:15607361)
• The ABCG2, a member of the ATP binding cassette (ABC) transporters, has been identified as a molecular determinant for bone marrow stem cells and proposed as a universal marker for stem cells. (PMID:15625123)

Cross-species orthologs

12 orthologs

Organism	Symbol	Gene ID
danio_rerio	abcg2b	ENSDARG00000079361
mus_musculus	Abcg3	ENSMUSG00000029299
rattus_norvegicus	Abcg3l2	ENSRNOG00000064381
rattus_norvegicus	Abcg3l4	ENSRNOG00000065003
rattus_norvegicus	Abcg3l1	ENSRNOG00000069481
rattus_norvegicus	Abcg3	ENSRNOG00000070774
drosophila_melanogaster	CG31689	FBGN0031449
drosophila_melanogaster	CG31121	FBGN0051121
drosophila_melanogaster	CG32091	FBGN0052091
caenorhabditis_elegans		WBGENE00006522
caenorhabditis_elegans		WBGENE00015479
caenorhabditis_elegans		WBGENE00017179

Paralogs (4): ABCG5 (ENSG00000138075), ABCG8 (ENSG00000143921), ABCG1 (ENSG00000160179), ABCG4 (ENSG00000172350)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:1347061) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 37 distinct phenotype terms.

Mouse phenotype (MP)	Records
increased blood uric acid level	2
abnormal bile color	1
abnormal hepatocyte morphology	1
fused cornea and lens	1
increased circulating HDL cholesterol level	1
abnormal homeostasis	1
liver inflammation	1
abnormal glucose homeostasis	1
increased circulating insulin level	1
abnormal kidney physiology	1
abnormal hematopoietic system morphology/development	1
abnormal bone marrow cell morphology/development	1
hepatic steatosis	1
oxidative stress	1
increased porphyrin level	1
increased circulating insulin-like growth factor I level	1
increased circulating cholesterol level	1
impaired glucose tolerance	1
increased circulating bilirubin level	1
decreased renal glomerular filtration rate	1
increased circulating glucose level	1
decreased blood urea nitrogen level	1
increased circulating potassium level	1
phototoxicity	1
porphyria	1

+12 more (showing top 25).

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Macaca mulatta	Q5MB13	96.6%	Diamond
Cryptococcus deuterogattii R265	P9WEU3	92.9%	Diamond
Bos taurus	Q4GZT4	88.0%	Diamond
Sus scrofa	Q8MIB3	88.0%	Diamond
Anopheles albimanus	Q16928	87.6%	Diamond
Anopheles gambiae	Q27256	87.6%	Diamond
Arabidopsis thaliana	Q8RWI9	86.1%	Diamond
Lucilia cuprina	Q05360	82.7%	Diamond
Ceratitis capitata	Q17320	82.7%	Diamond
Nakaseomyces glabratus CBS 138	Q6FQN3	74.8%	Diamond
Saccharomyces cerevisiae S288C	P33302	74.1%	Diamond
Dictyostelium discoideum	Q86HQ2	72.5%	Diamond
Petunia x hybrida	A0A0M4FLW6	71.4%	Diamond
Medicago truncatula	A9YWR6	71.4%	Diamond
Oryza sativa Japonica Group	Q8GU82	53.8%	Diamond
Trichophyton benhamiae CBS 112371	D4AYW0	46.0%	Diamond
Penicillium crustosum	A0A481WQK1	43.8%	Diamond
Mycobacterium tuberculosis H37Rv	O65934	40.6%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
PKD2	protein-coding	5311
PPM1K	protein-coding	152926
PPM1K-DT	ncRNA	105369192
SPP1	protein-coding	6696

Protein

Protein identifiers

Broad substrate specificity ATP-binding cassette transporter ABCG2 — Q9UNQ0 (reviewed: Q9UNQ0)

Alternative names: ATP-binding cassette sub-family G member 2, Breast cancer resistance protein, CDw338, Mitoxantrone resistance-associated protein, Placenta-specific ATP-binding cassette transporter, Urate exporter

All UniProt accessions (2): F8S0F2, Q9UNQ0

UniProt curated annotations — full annotation on UniProt →

Function. Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells. Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme. Also mediates the efflux of sphingosine-1-P from cells. Acts as a urate exporter functioning in both renal and extrarenal urate excretion. In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate. Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates. Mediates the secretion of the vitamins riboflavin and biotin into milk. Involved in the excretion of the riboflavin-derived compound lumichrome into the intestinal lumen and in its secretion into milk. Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability. Plays an important role in the exclusion of xenobiotics from the brain. It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux. In placenta, it limits the penetration of drugs from the maternal plasma into the fetus. May play a role in early stem cell self-renewal by blocking differentiation. In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response.

Subunit / interactions. Homodimer; disulfide-linked. The minimal functional unit is a homodimer, but the major oligomeric form in plasma membrane is a homotetramer with possibility of higher order oligomerization up to homododecamers.

Subcellular location. Cell membrane. Apical cell membrane. Mitochondrion membrane.

Tissue specificity. Highly expressed in placenta. Low expression in small intestine, liver and colon. Expressed in brain (at protein level).

Post-translational modifications. N-glycosylated. Glycosylation-deficient ABCG2 is normally expressed and functional. Phosphorylated. Phosphorylation at Thr-362 by PIM1 is induced by drugs like mitoxantrone and is associated with cells increased drug resistance. It regulates the localization to the plasma membrane, the homooligomerization and therefore, the activity of the transporter.

Activity regulation. Specifically inhibited by the fungal toxin fumitremorgin C and Ko143.

Domain organisation. The extracellular loop 3 (ECL3) is involved in binding porphyrins and transfer them to other carriers, probably albumin.

Polymorphism. Genetic variations in ABCG2 define the blood group Junior system (JR) [MIM:614490]. Individuals with Jr(a-) blood group lack the Jr(a) antigen on their red blood cells. These individuals may have anti-Jr(a) antibodies in their serum, which can cause transfusion reactions or hemolytic disease of the fetus or newborn. Although the clinical significance of the Jr(a-) blood group has been controversial, severe fatal hemolytic disease of the newborn has been reported. The Jr(a-) phenotype has a higher frequency in individuals of Asian descent, compared to those of European descent. The Jr(a-) phenotype is inherited as an autosomal recessive trait. Genetic variations in ABCG2 influence the variance in serum uric acid concentrations and define the serum uric acid concentration quantitative trait locus 1 (UAQTL1) [MIM:138900]. Excess serum accumulation of uric acid can lead to the development of gout, a common disorder characterized by tissue deposition of monosodium urate crystals as a consequence of hyperuricemia.

Similarity. Belongs to the ABC transporter superfamily. ABCG family. Eye pigment precursor importer (TC 3.A.1.204) subfamily.

Isoforms (2)

UniProt ID	Names	Canonical?
Q9UNQ0-1	1	yes
Q9UNQ0-2	2

RefSeq proteins (13): NP_001244315, NP_001335914, NP_001335915, NP_001335916, NP_001335917, NP_001335918, NP_001428137, NP_001428138, NP_001428139, NP_001428140, NP_001428141, NP_001428142, NP_004818* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR003439	ABC_transporter-like_ATP-bd	Domain
IPR003593	AAA+_ATPase	Domain
IPR013525	ABC2_TM	Domain
IPR027417	P-loop_NTPase	Homologous_superfamily
IPR043926	ABCG_dom	Domain
IPR050352	ABCG_transporters	Family

Pfam: PF00005, PF01061, PF19055

Enzyme classification (BRENDA)

• EC 7.6.2.2 — ABC-type xenobiotic transporter (BRENDA: 49 organisms, 716 substrates, 471 inhibitors, 280 Km, 31 kcat entries)
• EC 7.6.2.3 — ABC-type glutathione-S-conjugate transporter (BRENDA: 8 organisms, 145 substrates, 63 inhibitors, 16 Km, 0 kcat entries)

Substrate kinetics (BRENDA)

75 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ATP	0.0009–9	105
VERAPAMIL/IN	0.0006–0.0058	11
VINBLASTINE/IN	0.0002–0.1455	11
ESTRADIOL 17-BETA-D-GLUCURONIDE/IN	0.013–0.17	7
LEUKOTRIENE C4/IN	—	7
METHOTREXATE/IN	0.24–0.776	6
NICARDIPINE/IN	0.0004–0.0026	6
PROGESTERONE/IN	0.0038–0.0207	6
CYCLIC GUANOSINE MONOPHOSPHATE/IN	0.36–2	5
VERAPAMIL	0.0022–0.0115	5
ATP	0.0865–0.91	5
COLCHICINE/IN	0.037–0.72	4
FOLIC ACID/IN	0.13–0.26	4
PACLITAXEL/IN	0.0007–0.0009	4
RHODAMINE 123/IN	0.0118–0.0354	4

Catalyzed reactions (Rhea)

• urate(in) + ATP + H2O = urate(out) + ADP + phosphate + H(+) (RHEA:16461)
• sphing-4-enine 1-phosphate(in) + ATP + H2O = sphing-4-enine 1-phosphate(out) + ADP + phosphate + H(+) (RHEA:38951)
• 17beta-estradiol 17-O-(beta-D-glucuronate)(in) + ATP + H2O = 17beta-estradiol 17-O-(beta-D-glucuronate)(out) + ADP + phosphate + H(+) (RHEA:60128)
• indoxyl sulfate(in) + ATP + H2O = indoxyl sulfate(out) + ADP + phosphate + H(+) (RHEA:61332)
• estrone 3-sulfate(in) + ATP + H2O = estrone 3-sulfate(out) + ADP + phosphate + H(+) (RHEA:61348)
• riboflavin(in) + ATP + H2O = riboflavin(out) + ADP + phosphate + H(+) (RHEA:61352)
• methotrexate(in) + ATP + H2O = methotrexate(out) + ADP + phosphate + H(+) (RHEA:61356)
• pheophorbide a(in) + ATP + H2O = pheophorbide a(out) + ADP + phosphate + H(+) (RHEA:61360)
• dehydroepiandrosterone 3-sulfate(in) + ATP + H2O = dehydroepiandrosterone 3-sulfate(out) + ADP + phosphate + H(+) (RHEA:61364)
• 4-methylumbelliferone sulfate(in) + ATP + H2O = 4-methylumbelliferone sulfate(out) + ADP + phosphate + H(+) (RHEA:61368)
• 4-methylumbelliferone beta-D-glucuronate(in) + ATP + H2O = 4-methylumbelliferone beta-D-glucuronate(out) + ADP + phosphate + H(+) (RHEA:61372)
• 5,7-dimethyl-2-methylamino-4-(3-pyridylmethyl)-1,3-benzothiazol-6-yl sulfate(in) + ATP + H2O = 5,7-dimethyl-2-methylamino-4-(3-pyridylmethyl)-1,3-benzothiazol-6-yl sulfate(out) + ADP + phosphate + H(+) (RHEA:61376)

UniProt features (142 total): helix 34, sequence variant 26, mutagenesis site 25, strand 17, topological domain 7, sequence conflict 7, transmembrane region 6, turn 5, binding site 4, domain 2, site 2, disulfide bond 2, splice variant 2, chain 1, modified residue 1, glycosylation site 1

Structure

Experimental structures (PDB)

29 structures by resolution:

PDB	Title	Method	Resolution (Å)
8QCM	ABCG2 in complex with MZ82 and 5D3 Fab	ELECTRON MICROSCOPY	2.39
8U2C	Gaussian mixture model based single particle refinement - ABC transporter …	ELECTRON MICROSCOPY	2.5
8Q7B	ABCG2 in complex with MZ29 and 5D3 Fab	ELECTRON MICROSCOPY	2.56
8PXO	ABCG2 in complex with AZ99 and 5D3 Fab	ELECTRON MICROSCOPY	3
8PY4	ABCG2 in complex with ko143 and 5D3 Fab	ELECTRON MICROSCOPY	3
8P7W	Structure of 5D3-Fab and nanobody(Nb8)-bound ABCG2	ELECTRON MICROSCOPY	3.04
6HBU	Cryo-EM structure of the ABCG2 E211Q mutant bound to ATP and Magnesium	ELECTRON MICROSCOPY	3.09
6HZM	Cryo-EM structure of the ABCG2 E211Q mutant bound to ATP and Magnesium (alternative …	ELECTRON MICROSCOPY	3.09
6ETI	Structure of inhibitor-bound ABCG2	ELECTRON MICROSCOPY	3.1
7OJH	ABCG2 topotecan turnover-1 state	ELECTRON MICROSCOPY	3.1
8BHT	ABCG2 turnover-1 state with tariquidar bound	ELECTRON MICROSCOPY	3.1
7NEQ	Structure of tariquidar-bound ABCG2	ELECTRON MICROSCOPY	3.12
8BI0	ABCG2 turnover-2 state with tariquidar bound	ELECTRON MICROSCOPY	3.2
8P8A	Structure of 5D3-Fab and nanobody(Nb17)-bound ABCG2	ELECTRON MICROSCOPY	3.2
7NEZ	Structure of topotecan-bound ABCG2	ELECTRON MICROSCOPY	3.39
7OJ8	ABCG2 E1S turnover-2 state	ELECTRON MICROSCOPY	3.4
7OJI	ABCG2 topotecan turnover-2 state	ELECTRON MICROSCOPY	3.4
8P8J	Structure of 5D3-Fab and nanobody(Nb96)-bound ABCG2	ELECTRON MICROSCOPY	3.49
6VXF	Structure of apo-closed ABCG2	ELECTRON MICROSCOPY	3.5
7NFD	Structure of mitoxantrone-bound ABCG2	ELECTRON MICROSCOPY	3.51
6FFC	Structure of an inhibitor-bound ABC transporter	ELECTRON MICROSCOPY	3.56
6HIJ	Cryo-EM structure of the human ABCG2-MZ29-Fab complex with cholesterol and PE lipids …	ELECTRON MICROSCOPY	3.56
6HCO	Cryo-EM structure of the ABCG2 E211Q mutant bound to estrone 3-sulfate and 5D3-Fab	ELECTRON MICROSCOPY	3.58
6FEQ	Structure of inhibitor-bound ABCG2	ELECTRON MICROSCOPY	3.6
6VXI	Structure of ABCG2 bound to mitoxantrone	ELECTRON MICROSCOPY	3.7
5NJ3	Structure of an ABC transporter: complete structure	ELECTRON MICROSCOPY	3.78
5NJG	Structure of an ABC transporter: part of the structure that could be built de novo	ELECTRON MICROSCOPY	3.78
6VXH	Structure of ABCG2 bound to imatinib	ELECTRON MICROSCOPY	4
6VXJ	Structure of ABCG2 bound to SN38	ELECTRON MICROSCOPY	4.1

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9UNQ0-F1	85.54	0.66

Antibody-complex structures (SAbDab)

16 antibodies co-crystallized with this protein: 5NJ3, 5NJG, 6ETI, 6FEQ, 6HCO, 7NEQ, 7NEZ, 7NFD, 8P7W, 8P8A, 8P8J, 8PXO, 8PY4, 8Q7B, 8QCM, 8U2C

Human Protein Atlas

Protein class: Enzymes, ENZYME proteins, Metabolic proteins, CD markers, Transporters, Primary Active Transporters, Predicted membrane proteins, Predicted intracellular proteins, Cancer-related genes, Candidate cancer biomarkers, Human disease related genes

Protein evidence: Evidence at protein level

Subcellular location (HPA, imaging): plasma membrane; nucleoplasm

Antibody reliability (HPA): IH enhanced · IF supported

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (2)

Position	Role
418	not glycosylated
557	not glycosylated

Ligand- & substrate-binding residues (4)

Position	Role
80–87	ATP
184–190	ATP
211	ATP
243	ATP

Post-translational modifications (1)

Type	Positions
Phosphothreonine	362

Disulfide bonds (2)

Type	Positions
Disulfide bond	592–608
Interchain	603

Glycosylation sites (1)

Type	Positions
N-linked (glcnac…) asparagine	596

Mutagenesis-validated functional residues (25)

Position	Phenotype
71	decreased protein abundance. no effect on substrate transmembrane transport.
86	decreased protein abundance. decreased localization to the plasma membrane and retained intracellularly. loss of atpase-coupled …
211	decreased estrone-3 sulfate atpase-coupled transmembrane transporter activity. decreased substrate-induced atp hydrolysis. loss of …
362	loss of phosphorylation by pim1. decreased localization to the plasma membrane. decreased homooligomerization. loss of function in …
362	loss of phosphorylation by pim1. constitutive drug resistance independent of pim1.
383	loss of protein expression.
418	no effect.
435	no effect on stability. increased estrone-3 sulfate atpase-coupled transmembrane transporter activity. increased substrate-induced atp …
435	no effect on stability. decreased estrone-3 sulfate atpase-coupled transmembrane transporter activity. decreased substrate-induced atp …
436	no effect on stability. decreased estrone-3 sulfate atpase-coupled transmembrane transporter activity. decreased substrate-induced atp …
439	no effect on stability. decreased estrone-3 sulfate atpase-coupled transmembrane transporter activity. decreased substrate-induced atp …
482	decreases atpase activity.
482	increases atpase activity.
482	no change in atpase activity.
482	decreases transport activity.
546	no effect on stability. no effect on estrone-3 sulfate atpase-coupled transmembrane transporter activity. no effect on substrate-induced …
546	no effect on stability. decreased estrone-3 sulfate atpase-coupled transmembrane transporter activity. increased basal and …
549	no effect on stability. no effect on estrone-3 sulfate atpase-coupled transmembrane transporter activity. no effect on substrate-induced …
554	no effect on stability. increased estrone-3 sulfate atpase-coupled transmembrane transporter activity. increased basal and …
555	loss of protein expression.
557	no effect.
583	strongly reduced binding to hemin but not to ppix.
596	loss of glycosylation.
603	strongly reduced binding to hemin but not to ppix.
605	no effect on hemin binding.

Function

Pathways and Gene Ontology

Reactome pathways

8 curated (TAS) of 24; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

24 pathways:

ID	Pathway	Evidence
R-HSA-9793528	Ciprofloxacin ADME	curated
R-HSA-9725554	Differentiation of Keratinocytes in Interfollicular Epidermis in Mammalian Skin	curated
R-HSA-189451	Heme biosynthesis	curated
R-HSA-189483	Heme degradation	curated
R-HSA-917937	Iron uptake and transport	curated
R-HSA-9818032	NFE2L2 regulating MDR associated enzymes	curated
R-HSA-9753281	Paracetamol ADME	curated
R-HSA-1660661	Sphingolipid de novo biosynthesis	curated
R-HSA-2161522	Abacavir ADME	—
R-HSA-2161517	Abacavir transmembrane transport	electronic
R-HSA-9711123	Cellular response to chemical stress	—
R-HSA-8953897	Cellular responses to stimuli	—
R-HSA-2262752	Cellular responses to stress	—
R-HSA-1266738	Developmental Biology	—
R-HSA-9734767	Developmental Cell Lineages	—
R-HSA-9734779	Developmental Cell Lineages of the Integumentary System	—
R-HSA-9748784	Drug ADME	—
R-HSA-9755511	KEAP1-NFE2L2 pathway	—
R-HSA-1430728	Metabolism	—
R-HSA-556833	Metabolism of lipids	—
R-HSA-189445	Metabolism of porphyrins	—
R-HSA-9759194	Nuclear events mediated by NFE2L2	—
R-HSA-428157	Sphingolipid metabolism	—
R-HSA-382551	Transport of small molecules	—

MSigDB gene sets: 315 (showing top): GSE18804_SPLEEN_MACROPHAGE_VS_TUMORAL_MACROPHAGE_UP, GOBP_EXCRETION, GOBP_CIRCULATORY_SYSTEM_PROCESS, PAL_PRMT5_TARGETS_UP, REACTOME_METABOLISM_OF_PORPHYRINS, VICENT_METASTASIS_UP, GOCC_CELL_SURFACE, GOBP_ORGANIC_ACID_TRANSPORT, KEGG_ABC_TRANSPORTERS, BOYAULT_LIVER_CANCER_SUBCLASS_G12_DN, OSWALD_HEMATOPOIETIC_STEM_CELL_IN_COLLAGEN_GEL_UP, GOBP_CELLULAR_RESPONSE_TO_TOXIC_SUBSTANCE, GOBP_SPHINGOLIPID_METABOLIC_PROCESS, BILD_E2F3_ONCOGENIC_SIGNATURE, ENGELMANN_CANCER_PROGENITORS_UP

GO Biological Process (15): biotin transport (GO:0015878), sphingolipid biosynthetic process (GO:0030148), riboflavin transport (GO:0032218), urate metabolic process (GO:0046415), transmembrane transport (GO:0055085), transepithelial transport (GO:0070633), renal urate salt excretion (GO:0097744), export across plasma membrane (GO:0140115), transport across blood-brain barrier (GO:0150104), cellular detoxification (GO:1990748), xenobiotic detoxification by transmembrane export across the plasma membrane (GO:1990961), xenobiotic transport across blood-brain barrier (GO:1990962), lipid transport (GO:0006869), urate transport (GO:0015747), sulfite export across plasma membrane (GO:0160244)

GO Molecular Function (17): ATP binding (GO:0005524), ABC-type xenobiotic transporter activity (GO:0008559), urate transmembrane transporter activity (GO:0015143), biotin transmembrane transporter activity (GO:0015225), efflux transmembrane transporter activity (GO:0015562), ATP hydrolysis activity (GO:0016887), transmembrane transporter activity (GO:0022857), riboflavin transmembrane transporter activity (GO:0032217), ATPase-coupled transmembrane transporter activity (GO:0042626), identical protein binding (GO:0042802), protein homodimerization activity (GO:0042803), xenobiotic transmembrane transporter activity (GO:0042910), sphingolipid intramembrane carrier activity (GO:0046624), nucleotide binding (GO:0000166), protein binding (GO:0005515), protein dimerization activity (GO:0046983), ABC-type transporter activity (GO:0140359)

GO Cellular Component (7): plasma membrane (GO:0005886), apical plasma membrane (GO:0016324), brush border membrane (GO:0031526), mitochondrial membrane (GO:0031966), membrane raft (GO:0045121), external side of apical plasma membrane (GO:0098591), membrane (GO:0016020)

Reactome top-level categories

12 top-level categories:

Category	Pathways
Drug ADME	3
Metabolism of porphyrins	2
Metabolism	2
Sphingolipid metabolism	1
Abacavir ADME	1
Transport of small molecules	1
Developmental Cell Lineages of the Integumentary System	1
Nuclear events mediated by NFE2L2	1
Cellular responses to stimuli	1
Metabolism of lipids	1
Cellular responses to stress	1
Developmental Biology	1

GO top-level categories

showing 60 of 62 GO namespaces:

Category	Terms
nitrogen compound transport	3
transport	3
vitamin transport	2
cellular process	2
transmembrane transport	2
detoxification	2
export across plasma membrane	2
xenobiotic transport	2
vitamin transmembrane transporter activity	2
transmembrane transporter activity	2
ATP-dependent activity	2
protein binding	2
apical plasma membrane	2
monocarboxylic acid transport	1
sulfur compound transport	1
sphingolipid metabolic process	1
lipid biosynthetic process	1
small molecule metabolic process	1
purine-containing compound metabolic process	1
renal tubular secretion	1
export from cell	1
vascular transport	1
cellular response to toxic substance	1
xenobiotic export from cell	1
transport across blood-brain barrier	1
lipid localization	1
sulfite transmembrane transport	1
detoxification of sulfite	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
anion binding	1
xenobiotic transmembrane transporter activity	1
ABC-type transporter activity	1
urate transport	1
salt transmembrane transporter activity	1
monocarboxylic acid transmembrane transporter activity	1
biotin transport	1
sulfur compound transmembrane transporter activity	1
ribonucleoside triphosphate phosphatase activity	1
transporter activity	1
riboflavin transport	1
primary active transmembrane transporter activity	1
ATP hydrolysis activity	1
identical protein binding	1
protein dimerization activity	1
intramembrane lipid carrier activity	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
binding	1
ATPase-coupled transmembrane transporter activity	1
membrane	1
cell periphery	1
apical part of cell	1
plasma membrane region	1
brush border	1
cell projection membrane	1
mitochondrion	1
mitochondrial envelope	1
organelle membrane	1
membrane microdomain	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 18 of 40 annotations. The rest are phylogenetic / computational / electronic (IEA).

18 experimentally-supported GO terms:

GO term	NS	Evidence
cellular detoxification	BP	direct assay
renal urate salt excretion	BP	mutant phenotype
riboflavin transport	BP	direct assay
transepithelial transport	BP	direct assay
transmembrane transport	BP	mutant phenotype
urate metabolic process	BP	mutant phenotype
xenobiotic detoxification by transmembrane export across the plasma membrane	BP	mutant phenotype
xenobiotic transport across blood-brain barrier	BP	direct assay
brush border membrane	CC	direct assay
membrane raft	CC	direct assay
plasma membrane	CC	direct assay
ABC-type xenobiotic transporter activity	MF	direct assay
ATPase-coupled transmembrane transporter activity	MF	mutant phenotype
efflux transmembrane transporter activity	MF	mutant phenotype
identical protein binding	MF	physical interaction
protein homodimerization activity	MF	direct assay
riboflavin transmembrane transporter activity	MF	direct assay
urate transmembrane transporter activity	MF	direct assay

Protein interactions and networks

STRING

showing 15 of 2,890 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ABCG2	ABCC1	P33527	942
ABCG2	ABCC2	Q92887	888
ABCG2	SLCO1B1	Q9Y6L6	800
ABCG2	SLC2A9	Q9NRM0	783
ABCG2	MRPS7	Q9Y2R9	779
ABCG2	SLC22A8	Q8TCC7	776
ABCG2	SLCO1B3	Q9NPD5	773
ABCG2	SLC22A12	Q96S37	770
ABCG2	CYP3A4	P05184	770
ABCG2	PROM1	O43490	759
ABCG2	SLCO2B1	O94956	746
ABCG2	SLCO1A2	P46721	742
ABCG2	NR1I2	O75469	740
ABCG2	CD44	P16070	734
ABCG2	SLC47A1	Q96FL8	727

IntAct

Human interaction partners of ABCG2 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

4 partners by confidence:

Partner	Interaction type	MIscore	Records
PIM1	physical association	0.640	5
ENPP1	direct interaction	0.600	4
UBC	physical association	0.400	2
SCAMP1	association	0.350	2

BioGRID (82 interactions; top human partners by supporting records): BAG6 (Affinity Capture-Western; 4 records), RNF126 (Affinity Capture-Western; 3 records), DNAJB1 (Affinity Capture-MS; 2 records), HSP90AA1 (Affinity Capture-MS; 2 records), HSPA8 (Affinity Capture-MS; 2 records), ANLN (Affinity Capture-MS), ARRDC5 (Affinity Capture-MS), ATP5B (Affinity Capture-MS), ATP8A1 (Co-fractionation), BAG2 (Affinity Capture-MS), CHMP4B (Affinity Capture-MS), CHMP4C (Affinity Capture-MS), CIT (Affinity Capture-MS), CLPP (Affinity Capture-MS), CRAT (Co-fractionation)

SIGNOR signaling

4 signaling interactions:

A	Effect	B	Mechanism
PPARG	“up-regulates quantity by expression”	ABCG2	“transcriptional regulation”
SALL4	“up-regulates quantity by expression”	ABCG2	“transcriptional regulation”
SMARCA4	“up-regulates quantity by expression”	ABCG2	“transcriptional regulation”
PIM1	“up-regulates activity”	ABCG2	phosphorylation

Disease & clinical

Genetic variants

Variant evidence for ABCG2: 107 ClinVar records (17 pathogenic / likely pathogenic); 1 CIViC cancer variant; 3 PharmGKB dosing guidelines; 96 GWAS associations. Per-variant detail is on Sugi Variant.

ClinVar

107 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	16
Likely pathogenic	1
Uncertain significance	47
Likely benign	11
Benign	10

Top pathogenic / likely-pathogenic (15)

Showing the 15 best-reviewed of 17 pathogenic / likely-pathogenic ClinVar records, ranked by ClinVar review status (expert panel → multiple submitters → single submitter), then by number of submitting labs.

Variant ID	HGVS	Classification	Review	Submitters
59455	GRCh38/hg38 4q21.21-22.1(chr4:79575748-92412449)x1	Pathogenic	criteria provided, single submitter	1
1527097	GRCh37/hg19 4q13.3-22.1(chr4:75737340-91131156)x3	Pathogenic	criteria provided, single submitter	1
1527100	GRCh37/hg19 4q21.21-22.2(chr4:79780152-94873225)x1	Pathogenic	criteria provided, single submitter	1
1527103	GRCh37/hg19 4q21.21-22.1(chr4:81054789-90667421)x1	Pathogenic	criteria provided, single submitter	1
1527108	GRCh37/hg19 4q21.23-22.1(chr4:85839771-93071150)x1	Pathogenic	criteria provided, single submitter	1
2498966	GRCh37/hg19 4q22.1(chr4:88344058-89061168)x1	Pathogenic	criteria provided, single submitter	1
2579270	GRCh38/hg38 4q21.21-23(chr4:79123548-99457773)x1	Pathogenic	criteria provided, single submitter	1
3062764	GRCh37/hg19 4q21.21-22.3(chr4:81558759-95965995)x1	Pathogenic	criteria provided, single submitter	1
4851157	GRCh37/hg19 4q13.3-22.1(chr4:70910927-92961027)x1	Pathogenic	criteria provided, single submitter	1
4974698	GRCh38/hg38 4q22.1(chr4:87353588-91785400)x1	Pathogenic	criteria provided, single submitter	1
3062760	GRCh37/hg19 4q21.23-22.3(chr4:85139670-96295033)x3	Likely pathogenic	criteria provided, single submitter	1
145649	GRCh38/hg38 4q21.21-22.3(chr4:80879777-94809447)x1	Pathogenic	no assertion criteria provided	1
148194	GRCh38/hg38 4q21.21-24(chr4:80427023-100855441)x1	Pathogenic	no assertion criteria provided	1
152923	GRCh38/hg38 4q21.23-22.2(chr4:85449365-93973194)x1	Pathogenic	no assertion criteria provided	1
394976	GRCh37/hg19 4q21.21-22.1(chr4:82283358-90341831)x1	Pathogenic	no assertion criteria provided	1

Per-variant reference — Sugi Variant

Explore ABCG2’s pathogenic and likely-pathogenic variants individually — each with its ClinVar classification and conditions, applied ACMG criteria (ClinGen expert panel, where curated), the calibrated in-silico predictors (AlphaMissense, REVEL, SaProt, conservation), gnomAD frequency, and the predictor-disagreement QC signal — on Sugi Variant.

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 26 predictions of 1,148):

Position(s)	Effect	Δscore	Sites
4:88094660–88094661	acceptor_loss	1.0000	4
4:88095610–88095611	acceptor_loss	1.0000	6
4:88097615	acceptor_gain	1.0000
4:88107283	acceptor_gain	1.0000
4:88113363	donor_gain	1.0000
4:88113564	acceptor_gain	1.0000
4:88113569	acceptor_gain	1.0000
4:88114955–88114956	donor_loss	1.0000	4
4:88131801–88131802	donor_loss	1.0000	5
4:88132636	acceptor_loss	1.0000	2

AlphaMissense

1,638 missense substitutions predicted likely pathogenic (of 4,276 scored), across 425 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:

Residue	Likely-pathogenic substitutions	Mean am_pathogenicity	Max am_pathogenicity
M548	9	0.841	0.990
D217	8	0.999	0.999
D210	8	0.995	0.998
H243	8	0.988	1.000
D292	8	0.977	0.993
D296	8	0.975	0.989
F208	8	0.952	0.997
D91	8	0.948	0.980
F253	8	0.940	0.982
D128	8	0.926	0.973
F455	8	0.921	0.987
F551	8	0.901	0.984
F277	8	0.888	0.975
F439	8	0.886	0.968
S572	8	0.876	0.998
D477	8	0.872	0.951
F448	8	0.857	0.953
F432	8	0.845	0.959
H457	8	0.798	0.950
E211	7	0.998	0.999

HPA cancer prognostics

RNA cancer specificity: Cancer enhanced (Glioblastoma Multiforme)

Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.

3 prognostic cancer types:

Cancer	Prognostic	p-value
Kidney Renal Clear Cell Carcinoma (TCGA)	favorable	3.55e-15
Kidney Renal Clear Cell Carcinoma (validation)	favorable	5.94e-05
Glioblastoma Multiforme (TCGA)	favorable	0.000242

Disease associations

OMIM: gene MIM:603756 | disease phenotypes:

HPO phenotypes

5 phenotypes (HPO-id order):

HPO	Term
HP:0000006	Autosomal dominant inheritance
HP:0000951	Abnormality of the skin
HP:0001369	Arthritis
HP:0002149	Hyperuricemia
HP:0033073	Urate tophus

GWAS associations

showing 30 of 96 associations:

Study	Trait	p-value
GCST008971_71	Urate levels	0.000000e+00
GCST008972_60	Urate levels	0.000000e+00
GCST008970_3	Gout	1e-290
GCST012338_14	Gout	3e-255
GCST007725_21	Serum uric acid levels	2e-149
GCST007733_1	Serum uric acid levels	1e-148
GCST010637_8	Urate levels	2e-135
GCST001791_31	Urate levels	1e-134
GCST005983_46	Serum uric acid levels	2e-132
GCST007733_2	Serum uric acid levels	5e-128
GCST008972_234	Urate levels	2e-122
GCST012339_2	Gout vs asymptomatic hyperuricemia	3e-109
GCST010277_1	Gout	2e-101
GCST012020_593	Serum metabolite levels	7e-91
GCST000818_5	Urate levels	1e-75
GCST000242_3	Urate levels	3e-60
GCST010274_1	Gout (combined type)	2e-56
GCST002773_1	Gout	7e-54
GCST010275_1	Renal overload gout	1e-45
GCST008971_64	Urate levels	8e-44
GCST005799_2	Gout	2e-42
GCST002355_1	Serum uric acid levels	3e-42
GCST005793_1	Uric acid levels	3e-39
GCST008139_1	Gout	4e-35
GCST003925_5	Gout	9e-35
GCST003924_3	Renal overload gout	5e-33
GCST001790_4	Gout	2e-32
GCST002829_29	Urate levels in overweight individuals	2e-30
GCST001608_3	Renal function-related traits (urate)	4e-30
GCST002830_4	Urate levels in lean individuals	2e-29

EFO canonical traits (from GWAS)

13 canonical traits:

EFO ID	Trait name
EFO:0004531	urate measurement
EFO:0004761	uric acid measurement
EFO:0007804	LDL cholesterol change measurement
EFO:0004746	lipoprotein-associated phospholipase A(2) measurement
EFO:0004330	coffee consumption
EFO:0006782	cups of coffee per day measurement
EFO:0007677	LDL peak particle diameter measurement
EFO:0007678	total fat intake measurement
EFO:0009104	hyperuricemia
EFO:0010089	bitter beverage consumption measurement
EFO:0006781	coffee consumption measurement
EFO:0010091	tea consumption measurement
EFO:0004346	neuroimaging measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5393 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 837,801 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

showing 60 of 92 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL1738797	ALECTINIB	4	7,111
CHEMBL1163	ATAZANAVIR	4	22,353
CHEMBL1487	ATORVASTATIN	4	69,270
CHEMBL1450	ATOVAQUONE	4	14,731
CHEMBL4204794	AVAPRITINIB	4	1,416
CHEMBL388590	BENZBROMARONE	4	8,286
CHEMBL288441	BOSUTINIB	4	12,869
CHEMBL1014	CANDESARTAN CILEXETIL	4	11,240
CHEMBL1630575	CASPOFUNGIN	4	14
CHEMBL908	CHLORPROTHIXENE	4	9,392
CHEMBL1292	CLOFAZIMINE	4	15,677
CHEMBL2095208	COBICISTAT	4	2,928
CHEMBL160	CYCLOSPORINE	4	169,776
CHEMBL5416410	DASATINIB	4	674
CHEMBL593	DELAVIRDINE	4	25,680
CHEMBL411	DIETHYLSTILBESTROL	4	373,838
CHEMBL932	DIPYRIDAMOLE	4	52,091
CHEMBL1229211	DOLUTEGRAVIR	4	3,506
CHEMBL223228	EFAVIRENZ	4	36,324
CHEMBL461101	ELTROMBOPAG	4	625
CHEMBL553	ERLOTINIB	4
CHEMBL1405	ESTRONE	4
CHEMBL308954	ETRAVIRINE	4
CHEMBL1164729	FEBUXOSTAT	4
CHEMBL672	FENOFIBRATE	4
CHEMBL2103830	FOSTAMATINIB	4
CHEMBL35	FUROSEMIDE	4
CHEMBL374975	FUSIDIC ACID	4
CHEMBL939	GEFITINIB	4
CHEMBL941	IMATINIB	4
CHEMBL64391	ITRACONAZOLE	4
CHEMBL157101	KETOCONAZOLE	4
CHEMBL480	LANSOPRAZOLE	4
CHEMBL554	LAPATINIB	4
CHEMBL729	LOPINAVIR	4
CHEMBL191	LOSARTAN	4
CHEMBL457547	MICAFUNGIN	4
CHEMBL608533	MIDOSTAURIN	4
CHEMBL58	MITOXANTRONE	4
CHEMBL584	NELFINAVIR	4
CHEMBL1484	NICARDIPINE	4
CHEMBL193	NIFEDIPINE	4
CHEMBL255863	NILOTINIB	4
CHEMBL1428	NIMODIPINE	4
CHEMBL36506	NOVOBIOCIN	4
CHEMBL1503	OMEPRAZOLE	4
CHEMBL1502	PANTOPRAZOLE	4
CHEMBL1171837	PONATINIB	4
CHEMBL1397	POSACONAZOLE	4
CHEMBL1219	RABEPRAZOLE	4
CHEMBL1946170	REGORAFENIB	4
CHEMBL772	RESERPINE	4
CHEMBL374478	RIFAMPIN	4
CHEMBL175691	RILPIVIRINE	4
CHEMBL163	RITONAVIR	4
CHEMBL114	SAQUINAVIR	4
CHEMBL413	SIROLIMUS	4
CHEMBL1336	SORAFENIB	4
CHEMBL421	SULFASALAZINE	4
CHEMBL535	SUNITINIB	4

CIViC curated variants (1)

Named clinical variants curated in CIViC for this gene (the catalogue beneath the predictive evidence above):

Q141K (missense variant).

PharmGKB: 1 entry (CPIC guideline: yes)

PharmGKB clinical annotations

53 annotations by evidence level (1 strongest → 4):

Variant	Association	Level	Drugs	Phenotypes
rs2231142	Metabolism/PK	1A	rosuvastatin
rs2231142	Toxicity	1A	rosuvastatin	statin-related myopathy
rs2231142	Efficacy	1A	allopurinol	Gout
rs2231142	Dosage	1A	allopurinol	Gout
rs2231142	Efficacy	2A	rosuvastatin	Hypercholesterolemia;Myocardial Infarction
rs1061018	Other	3	dasatinib;imatinib;nilotinib
rs12505410	Efficacy	3	imatinib	Chronic myelogenous leukemia;BCR-ABL1 positive
rs12505410	Metabolism/PK	3	methotrexate	Osteosarcoma
rs13120400	Efficacy	3	methotrexate	Psoriasis
rs13120400	Efficacy	3	imatinib	Chronic myelogenous leukemia;BCR-ABL1 positive
rs13120400	Efficacy,Metabolism/PK	3	deferasirox	Beta-thalassemia and related diseases
rs13120400	Metabolism/PK	3	ceftriaxone	Central Nervous System Infectious Disorder
rs13120400	Metabolism/PK	3	methotrexate	Osteosarcoma
rs13137622	Metabolism/PK	3	methotrexate	Osteosarcoma
rs17731538	Efficacy	3	methotrexate	Psoriasis
rs2199936	Efficacy	3	rosuvastatin
rs2231135	Toxicity	3	methotrexate	Osteosarcoma
rs2231137	Toxicity	3	irinotecan	Non-Small Cell Lung Carcinoma
rs2231137	Other	3	dasatinib;imatinib;nilotinib
rs2231137	Dosage	3	imatinib	Drug Toxicity;Gastrointestinal Stromal Tumors
rs2231142	Metabolism/PK	3	tenofovir	HIV infectious disease
rs2231142	Metabolism/PK	3	dolutegravir	HIV infectious disease
rs2231142	Toxicity	3	methotrexate	Rheumatoid arthritis
rs2231142	Metabolism/PK	3	apixaban	Atrial Fibrillation
rs2231142	Efficacy,Toxicity	3	gemcitabine	Non-Small Cell Lung Carcinoma
rs2231142	Efficacy	3	Opioid anesthetics;Other general anesthetics;volatile anesthetics
rs2231142	Toxicity	3	cyclophosphamide;doxorubicin;fluorouracil	Breast Neoplasms
rs2231142	Toxicity	3	sunitinib	Neoplasms
rs2231142	Metabolism/PK	3	lamotrigine	Epilepsy
rs2231142	Other	3	atorvastatin
rs2231142	Metabolism/PK	3	simvastatin
rs2231142	Metabolism/PK	3	fluvastatin
rs2231142	Toxicity	3	atorvastatin
rs2231142	Toxicity	3	efavirenz	HIV infectious disease
rs2231142	Efficacy	3	sulfasalazine	Rheumatoid arthritis
rs2231142	Metabolism/PK	3	imatinib
rs2231142	Metabolism/PK	3	sulfasalazine
rs2725252	Efficacy	3	imatinib	Chronic myelogenous leukemia;BCR-ABL1 positive
rs3114020	Metabolism/PK	3	lamotrigine	Epilepsy
rs41282401	Other	3	dasatinib;imatinib;nilotinib
rs4148155	Efficacy	3	allopurinol
rs4148157	Metabolism/PK	3	topotecan	Brain Neoplasms
rs4148157	Efficacy	3	allopurinol
rs45605536	Other	3	dasatinib;imatinib
rs58818712	Other	3	dasatinib;imatinib
rs72552713	Metabolism/PK	3	sulfasalazine
rs76979899	Efficacy	3	allopurinol
rs7699188	Efficacy,Toxicity	3	fluorouracil;irinotecan;leucovorin	Colorectal Neoplasms
rs10011796	Efficacy	4	allopurinol
rs2231142	Toxicity	4	gefitinib	Lung Neoplasms
rs2231142	Efficacy	4	capecitabine;fluorouracil;leucovorin;oxaliplatin	Colorectal Neoplasms
rs2231142	Metabolism/PK	4	methotrexate	Acute lymphoblastic leukemia;Burkitt Lymphoma;Lymphoma;T-Cell;Osteosarcoma
rs2231142	Toxicity	4	methotrexate	Acute lymphoblastic leukemia;Burkitt Lymphoma;Drug Toxicity;Lymphoma;T-Cell;Osteosarcoma

PharmGKB variants

20 variants:

Variant	Genes	Level	Score	#Clin annots	Drugs
rs1061018	ABCG2	3	0.00	1	dasatinib;imatinib;nilotinib
rs2231135	ABCG2	3	2.25	1	methotrexate
rs2231137	ABCG2	3	3.75	3	irinotecan;dasatinib;imatinib;nilotinib;imatinib
rs2231142	ABCG2	1A	115.62	26	rosuvastatin;atorvastatin;cyclophosphamide;doxorubicin;fluorouracil;allopurinol;simvastatin;fluvastatin;efavirenz;tenofovir;dolutegravir;Opioid anesthetics;Other general anesthetics;volatile anesthetics
rs2725252	ABCG2	3	2.00	1	imatinib
rs3114020	ABCG2	3	0.75	1	lamotrigine
rs4148157	ABCG2	3	1.75	2	allopurinol;topotecan
rs7699188	ABCG2	3	6.00	1	fluorouracil;irinotecan;leucovorin
rs10011796	ABCG2	4	-1.50	1	allopurinol
rs12505410	ABCG2	3	2.00	2	methotrexate;imatinib
rs13120400	ABCG2	3	4.25	5	methotrexate;ceftriaxone;imatinib;deferasirox
rs17731538	ABCG2	3	2.75	1	methotrexate
rs41282401	ABCG2	3	0.00	1	dasatinib;imatinib;nilotinib
rs45605536	ABCG2	3	0.00	1	dasatinib;imatinib
rs58818712	ABCG2	3	0.00	1	dasatinib;imatinib
rs72552713	ABCG2	3	0.12	1	sulfasalazine
rs13137622	ABCG2	3	2.00	1	methotrexate
rs4148155	ABCG2	3	0.00	1	allopurinol
rs76979899	ABCG2	3	0.00	1	allopurinol
rs2199936	ABCG2	3	0.00	1	rosuvastatin

PharmGKB variant annotations

Per-publication pharmacogenomic findings for this gene (significant associations).

showing 58 of 131 published findings:

Variant	Drug(s)	Category	Finding	PMID
rs2231142	fluvastatin	Metabolism/PK	Genotype TT is associated with increased exposure to drug when treated with fluvastatin in healthy individuals as compared to genotypes GG + GT.	PMID:19842935
rs2231142	simvastatin	Metabolism/PK	Genotype TT is associated with increased exposure to drug when treated with simvastatin in healthy individuals as compared to genotypes GG + GT.	PMID:19842935
rs7699188	fluorouracil, irinotecan, leucovorin	Efficacy	Allele A is associated with increased tumor response rate when treated with fluorouracil, irinotecan and leucovorin in people with Colorectal Neoplasms as compared to allele G.	PMID:24018773
rs7699188	fluorouracil, irinotecan, leucovorin	Toxicity	Allele A is associated with increased risk of grade 3-4 nonhematological toxicity when treated with fluorouracil, irinotecan and leucovorin in people with Colorectal Neoplasms as compared to allele G.	PMID:24018773
rs2231142	rosuvastatin	Metabolism/PK	Genotype TT is associated with increased plasma concentrations of rosuvastatin when treated with rosuvastatin in people with Hypercholesterolemia as compared to genotype GG.	PMID:23930675
rs2231142	rosuvastatin	Efficacy	Genotype GG is associated with decreased percentage change in LDL-cholesterol levels when treated with rosuvastatin in people with Hypercholesterolemia as compared to genotype TT.	PMID:23930675
rs2231142	rosuvastatin	Metabolism/PK	Allele T is associated with increased plasma concentrations of rosuvastatin as compared to allele G.	PMID:23876492
rs2231142	sunitinib	Toxicity	Genotype TT is associated with increased risk of Thrombocytopenia when treated with sunitinib in people with Carcinoma, Renal Cell as compared to genotypes GG + GT.	PMID:24013576
rs2231142	sunitinib	Toxicity	Genotype TT is associated with increased risk of Neutropenia when treated with sunitinib in people with Carcinoma, Renal Cell as compared to genotypes GG + GT.	PMID:24013576
rs2231142	sunitinib	Toxicity	Genotype TT is associated with increased risk of hand-foot syndrome when treated with sunitinib in people with Carcinoma, Renal Cell as compared to genotypes GG + GT.	PMID:24013576
rs2231142	sunitinib	Toxicity	Genotype TT is associated with increased risk of Drug Toxicity when treated with sunitinib in people with Carcinoma, Renal Cell as compared to genotypes GG + GT.	PMID:24013576
rs12505410	imatinib	Efficacy	Allele G is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to allele T.	PMID:24123600
rs12505410	imatinib	Efficacy	Genotypes GG + GT is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotype TT.	PMID:24123600
rs13120400	imatinib	Efficacy	Genotypes CC + CT is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotype TT.	PMID:24123600
rs2725252	imatinib	Efficacy	Genotypes AC + CC is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotype AA.	PMID:24123600
rs2725252	imatinib	Efficacy	Allele C is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to allele A.	PMID:24123600
rs2231142	antineoplastic agents	Efficacy	Genotype GG is associated with decreased response to antineoplastic agents in people with Colorectal Neoplasms as compared to genotypes GT + TT.	PMID:24338217
rs2231142	sulfasalazine	Efficacy	Genotypes GT + TT are associated with increased response to sulfasalazine in people with Arthritis, Rheumatoid as compared to genotype GG.	PMID:24394199
rs2231142	allopurinol	Efficacy	Allele T is associated with decreased response to allopurinol in people with Gout as compared to allele G.	PMID:25676789
rs2231142	sunitinib	Toxicity	Genotype TT is associated with decreased risk of Neutropenia when treated with sunitinib in people with Carcinoma, Renal Cell as compared to genotypes GG + GT.	PMID:26244574
rs2231142	sunitinib	Metabolism/PK	Genotypes GT + TT is associated with increased exposure to sunitinib in people with Neoplasms as compared to genotype GG.	PMID:25344452
rs2231137	sunitinib	Efficacy	Genotype CT is associated with increased progression-free survival when treated with sunitinib in people with Carcinoma, Renal Cell as compared to genotype CC.	PMID:21097692
rs2231135	methotrexate	Toxicity	Genotype AG is associated with increased risk of mucositis when treated with methotrexate in people with Osteosarcoma as compared to genotype AA.	PMID:25778468
rs2231142	imatinib	Efficacy	Genotype TT is associated with increased progression-free survival when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes GG + GT.	PMID:25417047
rs2231142	atorvastatin	Toxicity	Genotypes GT + TT is associated with increased likelihood of Drug Toxicity, Muscular Diseases, Rhabdomyolysis or Toxic liver disease when treated with atorvastatin as compared to genotype GG.	PMID:26086347
rs1481012	rosuvastatin	Efficacy	Genotypes AG + GG are associated with increased response to rosuvastatin as compared to genotype AA.	PMID:22331829
rs4148157	topotecan	Metabolism/PK	Genotypes AA + AG is associated with increased concentrations of topotecan in children with Brain Neoplasms as compared to genotype GG.	PMID:27052877
rs2231142	allopurinol	Efficacy	Genotypes GT + TT are associated with decreased response to allopurinol in people with Gout as compared to genotype GG.	PMID:26810134
rs13120400	deferasirox	Metabolism/PK	Genotype CC is associated with increased concentrations of deferasirox in people with beta-Thalassemia as compared to genotypes CT + TT.	PMID:27043265
rs2231142	HMG-CoA reductase inhibitors	Efficacy	Allele G is associated with decreased response to hmg coa reductase inhibitors as compared to allele T.	PMID:27045730
rs3114020	lamotrigine	Metabolism/PK	Genotypes CC + CT are associated with increased concentrations of lamotrigine in people with Epilepsy as compared to genotype TT.	PMID:26213157
rs2231142	lamotrigine	Metabolism/PK	Genotypes GT + TT are associated with increased concentrations of lamotrigine in people with Epilepsy as compared to genotype GG.	PMID:26213157
rs13120400	deferasirox	Metabolism/PK	Genotype CC is associated with increased concentrations of deferasirox in people with beta-Thalassemia as compared to genotypes CT + TT.	PMID:27193993
rs2231142	pazopanib, simvastatin	Toxicity	Genotypes GT + TT is associated with increased likelihood of Toxic liver disease when treated with pazopanib and simvastatin in people with Neoplasms as compared to genotype GG.	PMID:22918879
rs2231142	rosuvastatin	Efficacy	Allele T is associated with increased response to rosuvastatin in people with Myocardial Infarction as compared to allele G.	PMID:20207952
rs2231142	lamotrigine	Metabolism/PK	Genotype TT is associated with increased concentrations of lamotrigine in people with Epilepsy as compared to genotypes GG + GT.	PMID:27610747
rs2231142	sunitinib	Toxicity	Allele T is associated with increased severity of Thrombocytopenia when treated with sunitinib in people with Carcinoma, Renal Cell as compared to allele G.	PMID:26914831
rs2231142	imatinib	Efficacy	Allele T is associated with decreased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to allele G.	PMID:27991849
rs2231142	felodipine	Metabolism/PK	Genotype TT is associated with increased exposure to felodipine in healthy individuals as compared to genotypes GG + GT.	PMID:28244604
rs13120400	deferasirox	Metabolism/PK	Genotypes CT + TT is associated with increased exposure to deferasirox in children with beta-Thalassemia as compared to genotype CC.	PMID:28346059
rs2231137	sorafenib	Metabolism/PK	Genotype CT is associated with concentrations of sorafenib in people with Carcinoma, Hepatocellular as compared to genotype CC.	PMID:28289864
rs2231142	sorafenib	Metabolism/PK	Genotype GT is associated with concentrations of sorafenib in people with Carcinoma, Hepatocellular as compared to genotype GG.	PMID:28289864
rs2231142	apixaban	Metabolism/PK	Genotype TT is associated with increased concentrations of apixaban in people with Atrial Fibrillation as compared to genotype GG.	PMID:28678049
rs2231142	tenofovir	Metabolism/PK	Genotypes GT + TT are associated with increased concentrations of tenofovir in women with HIV Infections as compared to genotype GG.	PMID:28462920
rs2231142	dolutegravir	Metabolism/PK	Genotype TT is associated with increased concentrations of dolutegravir in people with HIV Infections as compared to genotypes GG + GT.	PMID:28858994
rs2725263		Other	Allele C is associated with increased expression of ABCG2 in HepG2 and HEK293 cells as compared to allele A.	PMID:28930109
rs2231142	risperidone	Metabolism/PK	Genotypes GT + TT is associated with decreased dose-adjusted trough concentrations of risperidone in children as compared to genotype GG.	PMID:28719598
rs2231142	risperidone	Toxicity	Genotypes GT + TT is associated with increased risk of adverse events when treated with risperidone in children as compared to genotype GG.	PMID:28719598
rs2231142	clozapine	Metabolism/PK	Genotypes GT + TT is associated with increased dose-adjusted trough concentrations of clozapine in people with Schizophrenia as compared to genotype GG.	PMID:27932669
rs2231142	allopurinol	Dosage	Allele T is associated with increased dose of allopurinol in people with Gout as compared to allele G.	PMID:29341237
rs2231142	methotrexate	Metabolism/PK	Allele T is associated with decreased metabolism of methotrexate in children with Osteosarcoma as compared to allele G.	PMID:27566582
rs2231142	iguratimod	Efficacy	Genotypes GT + TT is associated with increased clinical benefit to iguratimod in people with Arthritis, Rheumatoid as compared to genotype GG.	PMID:29517409
rs2231142	axitinib	Metabolism/PK	Allele T is associated with concentrations of axitinib in people with Carcinoma, Renal Cell as compared to allele G.	PMID:29682213
rs2231142	gemcitabine	Efficacy	Genotypes GT + TT are associated with increased progression-free survival when treated with gemcitabine in people with Carcinoma, Non-Small-Cell Lung as compared to genotype GG.	PMID:29751792
rs2231142	gemcitabine	Toxicity	Genotypes GT + TT are associated with increased severity of Thrombocytopenia when treated with gemcitabine in people with Carcinoma, Non-Small-Cell Lung as compared to genotype GG.	PMID:29751792
rs2231142	lamotrigine	Metabolism/PK	Allele T is associated with increased concentrations of lamotrigine in people with Epilepsy as compared to allele G.	PMID:29791014
rs13120400	voriconazole	Metabolism/PK	Genotype CC is associated with increased trough concentration of voriconazole in children as compared to genotypes CT + TT.	PMID:29914286
rs2231142	Opioid anesthetics, Other general anesthetics, volatile anesthetics	Efficacy	Genotype TT is associated with increased response to Opioid anesthetics, Other general anesthetics or volatile anesthetics as compared to genotypes GG + GT.	PMID:30136624

PharmGKB dosing guidelines

CPIC / DPWG genotype-guided dosing for this gene (drug × pharmacogene).

3 dosing guidelines:

Guideline	Source	Drug	Dosing?	Recommendation?
Annotation of CPIC Guideline for atorvastatin, fluvastatin, lovastatin	CPIC	atorvastatin;fluvastatin;lovastatin;pitavastatin;pravastatin;simvastatin
Annotation of CPIC Guideline for rosuvastatin and ABCG2, SLCO1B1	CPIC	rosuvastatin	yes	yes
Annotation of DPWG Guideline for allopurinol and ABCG2	DPWG	allopurinol	yes	yes

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: transporter — ABCG subfamily

Most potent curated ligand interactions (5 total), top 5:

Ligand	Action	Affinity	Parameter
elacridar	Inhibition	6.71	pIC50
cyclosporin A	Inhibition	6.3	pKi
KS 176	Inhibition	6.23	pIC50
compound 14 [PMID: 30925062]	Non-competitive	5.62	pIC50
nobiletin	Inhibition	5.36	pIC50

Binding affinities (BindingDB)

1259 measured of 1446 human assays (1469 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide	EC50	0.05 nM
Alectinib	IC50	0.59 nM	US-9126931: Tetracyclic compound
CHEMBL4168440	EC50	0.6 nM
CHEMBL4585968	EC50	0.6 nM
CHEMBL4458009	EC50	0.9 nM
CHEMBL4434729	EC50	0.97 nM
(2S)-1-[[2-(difluoromethyl)-6-[2-(difluoromethyl)-4-pyridinyl]-3-pyridinyl]oxy]-2,4-dimethylpentan-2-amine	IC50	1.2 nM	US-10155760: Biaryl kinase inhibitors
CHEMBL4547419	EC50	1.3 nM
Avapritinib	IC50	1.5 nM	US-10807985: Compositions useful for treating disorders related to kit
REGORAFENIB	IC50	1.5 nM
CHEMBL5089855	IC50	1.8 nM
CHEMBL4101737	EC50	2 nM
CHEMBL4172744	EC50	2 nM
CHEMBL5631325	EC50	2 nM
CHEMBL5088809	IC50	2.2 nM
2-(3-CYANO-4-ISOBUTOXY-PHENYL)-4-METHYL-5-THIAZOLE-CARBOXYLIC ACID	IC50	2.9 nM
(3Z)-3-(2-chloro-9H-thioxanthen-9-ylidene)-N,N-dimethylpropan-1-amine	KI	3 nM
CHEMBL4073213	EC50	3 nM
CHEMBL5631270	EC50	3 nM
CHEMBL4081708	EC50	4 nM
CHEMBL4082228	EC50	4 nM
CHEMBL4094899	EC50	4 nM
CHEMBL4091528	EC50	4 nM
CHEMBL4072298	EC50	4 nM
CHEMBL4176228	EC50	4 nM
CHEMBL4074563	EC50	5 nM
CHEMBL4161427	EC50	5 nM
CHEMBL4166863	EC50	6 nM
CHEMBL4083491	EC50	7 nM
CHEMBL4081623	EC50	8 nM
CHEMBL4064296	EC50	8 nM
CHEMBL4165918	EC50	10 nM
CHEMBL4163310	EC50	10 nM
(3-Chloro-phenyl)-(2-phenyl-quinazolin-4-yl)-amine; hydrochloride	EC50	11 nM
CHEMBL4082782	EC50	11 nM
CHEMBL4176534	EC50	11 nM
CHEMBL4172203	EC50	11 nM
CHEMBL4751863	EC50	11 nM
CI 981	IC50	11.6 nM	US-9353061: 3,5,N-trihydroxy-alkanamide and derivatives: method for making same and use thereof
CHEMBL4099250	EC50	12 nM
CHEMBL4567446	IC50	12 nM
CHEMBL5632630	EC50	12 nM
CHEMBL4075328	EC50	13 nM
MMV665798	EC50	13 nM
CHEMBL4073354	EC50	13 nM
CHEMBL5173341	EC50	13 nM
ELACRIDAR HYDROCHLORIDE	EC50	14 nM
CHEMBL4075963	EC50	14 nM
CHEMBL4160887	EC50	14 nM
CHEMBL2158558	EC50	14 nM

ChEMBL bioactivities

1955 potent at pChembl≥5 of 2203 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.99	EC50	0.01019	nM	CHEMBL2141796
10.99	EC50	0.01013	nM	CHEMBL2145384
10.96	EC50	0.01088	nM	CHEMBL2142245
10.92	EC50	0.01209	nM	CHEMBL2137928
10.64	EC50	0.02297	nM	CHEMBL2141666
10.63	EC50	0.02338	nM	CHEMBL2130718
10.39	EC50	0.04032	nM	CHEMBL2140166
10.39	EC50	0.04093	nM	CHEMBL2137680
10.35	EC50	0.04419	nM	CHEMBL2135227
10.32	EC50	0.04775	nM	CHEMBL2133727
9.60	EC50	0.254	nM	CHEMBL2132526
9.22	EC50	0.6	nM	CHEMBL4168440
9.05	EC50	0.9	nM	CHEMBL4561302
9.05	EC50	0.9	nM	CHEMBL4584493
8.96	EC50	1.1	nM	CHEMBL4453052
8.92	EC50	1.2	nM	CHEMBL4159635
8.85	EC50	1.4	nM	CHEMBL4561302
8.85	EC50	1.4	nM	CHEMBL4860031
8.82	IC50	1.5	nM	AVAPRITINIB
8.80	EC50	1.6	nM	CHEMBL4860031
8.77	EC50	1.7	nM	CHEMBL4454217
8.70	EC50	1.999	nM	CHEMBL2133413
8.70	EC50	2	nM	CHEMBL4101737
8.70	EC50	2	nM	CHEMBL4172744
8.70	EC50	2	nM	CHEMBL4591134
8.70	EC50	2	nM	CHEMBL4454217
8.68	EC50	2.1	nM	CHEMBL4474920
8.66	EC50	2.2	nM	CHEMBL4442810
8.66	EC50	2.2	nM	CHEMBL4453052
8.64	EC50	2.3	nM	CHEMBL4591134
8.62	EC50	2.4	nM	CHEMBL4440681
8.62	EC50	2.4	nM	CHEMBL4592756
8.60	EC50	2.5	nM	CHEMBL4453052
8.55	EC50	2.8	nM	CHEMBL4545977
8.55	EC50	2.8	nM	CHEMBL4584493
8.52	EC50	3	nM	CHEMBL4073213
8.51	EC50	3.1	nM	CHEMBL4291291
8.48	EC50	3.3	nM	CHEMBL4454945
8.48	EC50	3.3	nM	CHEMBL4589907
8.46	EC50	3.5	nM	CHEMBL3092485
8.46	EC50	3.5	nM	CHEMBL4463713
8.46	EC50	3.5	nM	CHEMBL4877122
8.44	EC50	3.6	nM	CHEMBL4564209
8.41	EC50	3.9	nM	CHEMBL4472194
8.40	EC50	4	nM	CHEMBL4082228
8.40	EC50	4	nM	CHEMBL4081708
8.40	EC50	4	nM	CHEMBL4094899
8.40	EC50	4	nM	CHEMBL4091528
8.40	EC50	4	nM	CHEMBL4072298
8.40	EC50	4	nM	CHEMBL4176228

PubChem BioAssay actives

1926 with measured affinity, of 5077 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
N-(3-methylsulfanylphenyl)-2-(3-nitrophenyl)quinazolin-4-amine	1501277: Activation of ABCG2 ATPase activity (unknown origin) expressed in baculovirus infected high5 cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction based colorimetric assay	ec50	0.0006	uM
methyl 3-[[2-[4-[2-[2-[2-[4-[4-[4-(6-methyl-4-oxochromen-2-yl)phenoxy]butyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1525920: Inhibition of BCRP in human MCF7/MX100 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0009	uM
methyl 3-[[4-oxo-2-[4-[2-[2-[2-[4-[4-(4-oxo-2-phenylchromen-7-yl)oxybutyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]phenyl]chromen-3-yl]oxymethyl]benzoate	1525919: Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0009	uM
methyl 3-[[2-[4-[2-[2-[4-[3-[1-[2-[2-[4-[3-[(3-methoxycarbonylphenyl)methoxy]-4-oxochromen-2-yl]phenoxy]ethoxy]ethyl]triazol-4-yl]phenyl]triazol-1-yl]ethoxy]ethoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1525920: Inhibition of BCRP in human MCF7/MX100 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0011	uM
N-(3,4-dimethoxyphenyl)-2-(4-methoxyphenyl)quinazolin-4-amine	1501277: Activation of ABCG2 ATPase activity (unknown origin) expressed in baculovirus infected high5 cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction based colorimetric assay	ec50	0.0012	uM
methyl 3-[[2-[4-[2-[2-[2-[4-[[benzyl(2-hydroxyethyl)amino]methyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1769259: Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0014	uM
Avapritinib	1916975: Inhibition of ABCG2 (unknown origin)	ic50	0.0015	uM
methyl 3-[[4-oxo-2-[4-[2-[2-[2-[4-[2-(4-oxo-2-phenylchromen-7-yl)oxyethoxymethyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]phenyl]chromen-3-yl]oxymethyl]benzoate	1525919: Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0017	uM
4-[[2-(3-methoxyphenyl)pyrido[2,3-d]pyrimidin-4-yl]amino]phenol	1479734: Activation of recombinant human ABCG2 ATPase activity expressed in baculovirus infected High five insect cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction-based colorimetric method	ec50	0.0020	uM
N,2-bis(3-nitrophenyl)quinazolin-4-amine	1501277: Activation of ABCG2 ATPase activity (unknown origin) expressed in baculovirus infected high5 cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction based colorimetric assay	ec50	0.0020	uM
methyl 3-[[2-[4-[2-[2-[2-[4-[3-[4-(7-fluoro-4-oxochromen-2-yl)phenoxy]propyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1525919: Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0020	uM
methyl 3-[[2-[4-[2-[2-[4-[[1-[2-[2-[4-[3-[(3-methoxycarbonylphenyl)methoxy]-4-oxochromen-2-yl]phenoxy]ethoxy]ethyl]triazol-4-yl]methoxymethyl]triazol-1-yl]ethoxy]ethoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1525920: Inhibition of BCRP in human MCF7/MX100 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0021	uM
methyl 3-[[2-[4-[2-[2-[4-[[N-[[1-[2-[2-[4-[3-[(3-methoxycarbonylphenyl)methoxy]-4-oxochromen-2-yl]phenoxy]ethoxy]ethyl]triazol-4-yl]methyl]anilino]methyl]triazol-1-yl]ethoxy]ethoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1525920: Inhibition of BCRP in human MCF7/MX100 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0022	uM
methyl 3-[[2-[4-[2-[2-[4-[3-[1-[2-[2-[4-[3-[(3-methoxycarbonylphenyl)methoxy]-4-oxochromen-2-yl]phenoxy]ethoxy]ethyl]triazol-4-yl]propyl]triazol-1-yl]ethoxy]ethoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1525920: Inhibition of BCRP in human MCF7/MX100 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0024	uM
methyl 3-[[2-[4-[2-[2-[2-[4-[4-[1-[2-[2-[2-[4-[3-[(3-methoxycarbonylphenyl)methoxy]-4-oxochromen-2-yl]phenoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]phenyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1525919: Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0024	uM
methyl 3-[[2-[4-[2-[2-[2-[4-[3-[1-[2-[2-[2-[4-[3-[(3-methoxycarbonylphenyl)methoxy]-4-oxochromen-2-yl]phenoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]phenyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1525919: Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0028	uM
4-[[2-(3-methoxyphenyl)pyrido[2,3-d]pyrimidin-4-yl]amino]benzonitrile	1479734: Activation of recombinant human ABCG2 ATPase activity expressed in baculovirus infected High five insect cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction-based colorimetric method	ec50	0.0030	uM
7-fluoro-2-[4-[3-[1-[2-[2-[2-[4-(6-fluoro-4-oxochromen-2-yl)phenoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]propoxy]phenyl]chromen-4-one	1525919: Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0031	uM
methyl 3-[[2-[4-[2-[2-[2-[4-[[benzyl-[[1-[2-[2-[2-[4-[3-[(3-methoxycarbonylphenyl)methoxy]-4-oxochromen-2-yl]phenoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]methyl]amino]methyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1525919: Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0033	uM
methyl 3-[[2-[4-[2-[2-[4-[[benzyl-[[1-[2-[2-[4-[3-[(3-methoxycarbonylphenyl)methoxy]-4-oxochromen-2-yl]phenoxy]ethoxy]ethyl]triazol-4-yl]methyl]amino]methyl]triazol-1-yl]ethoxy]ethoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1525920: Inhibition of BCRP in human MCF7/MX100 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0033	uM
methyl 3-[[4-oxo-2-[4-[2-[2-[2-[4-[3-(4-oxo-2-phenylchromen-7-yl)oxypropyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]phenyl]chromen-3-yl]oxymethyl]benzoate	1525919: Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0035	uM
methyl 3-[[2-[4-[2-[2-[4-[[benzyl(methyl)amino]methyl]triazol-1-yl]ethoxy]ethoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1769261: Inhibition of BCRP (unknown origin) expressed in MCF7/MX100 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0035	uM
2-(3,4-dimethoxyphenyl)-N-(3-nitrophenyl)quinazolin-4-amine	1501277: Activation of ABCG2 ATPase activity (unknown origin) expressed in baculovirus infected high5 cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction based colorimetric assay	ec50	0.0035	uM
methyl 3-[[2-[4-[2-[2-[4-[4-[4-(6-methyl-4-oxochromen-2-yl)phenoxy]butyl]triazol-1-yl]ethoxy]ethoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1525919: Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0036	uM
methyl 3-[[2-[4-[2-[2-[2-[4-[[N-[[1-[2-[2-[2-[4-[3-[(3-methoxycarbonylphenyl)methoxy]-4-oxochromen-2-yl]phenoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]methyl]anilino]methyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1525920: Inhibition of BCRP in human MCF7/MX100 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0039	uM
tert-butyl 3-[(2S,5S,8S)-14-methoxy-2-(2-methylpropyl)-4,7-dioxo-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraen-5-yl]propanoate	1635795: Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive basal ATPase activity after 20 mins by colorimetric method	ic50	0.0040	uM
N-(3-nitrophenyl)-2-pyridin-3-ylpyrido[2,3-d]pyrimidin-4-amine	1479734: Activation of recombinant human ABCG2 ATPase activity expressed in baculovirus infected High five insect cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction-based colorimetric method	ec50	0.0040	uM
N-(3-nitrophenyl)-2-pyridin-4-ylquinazolin-4-amine	1447895: Activation of ABCG2 (unknown origin) ATPase activity expressed in baculovirus infected high five cell membranes by ascorbic acid/ammonia molybdate reaction-based colorimetric analysis	ec50	0.0040	uM
4-[(2-pyridin-3-ylquinazolin-4-yl)amino]benzonitrile	1447895: Activation of ABCG2 (unknown origin) ATPase activity expressed in baculovirus infected high five cell membranes by ascorbic acid/ammonia molybdate reaction-based colorimetric analysis	ec50	0.0040	uM
N-(4-fluorophenyl)-2-(3-methoxyphenyl)pyrido[2,3-d]pyrimidin-4-amine	1479734: Activation of recombinant human ABCG2 ATPase activity expressed in baculovirus infected High five insect cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction-based colorimetric method	ec50	0.0040	uM
3-[[2-(3-methoxyphenyl)pyrido[2,3-d]pyrimidin-4-yl]amino]benzonitrile	1479734: Activation of recombinant human ABCG2 ATPase activity expressed in baculovirus infected High five insect cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction-based colorimetric method	ec50	0.0040	uM
N-(3,4-dimethoxyphenyl)-2-(3-methoxyphenyl)quinazolin-4-amine	1501277: Activation of ABCG2 ATPase activity (unknown origin) expressed in baculovirus infected high5 cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction based colorimetric assay	ec50	0.0040	uM
N-(4-bromo-3-methoxyphenyl)-2-(3,4-dimethoxyphenyl)quinazolin-4-amine	1501277: Activation of ABCG2 ATPase activity (unknown origin) expressed in baculovirus infected high5 cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction based colorimetric assay	ec50	0.0040	uM
2-(3-methoxyphenyl)-N-(3-nitrophenyl)quinazolin-4-amine	1501277: Activation of ABCG2 ATPase activity (unknown origin) expressed in baculovirus infected high5 cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction based colorimetric assay	ec50	0.0040	uM
methyl 3-[[4-oxo-2-[4-[2-[2-[4-[2-(4-oxo-2-phenylchromen-7-yl)oxyethoxymethyl]triazol-1-yl]ethoxy]ethoxy]phenyl]chromen-3-yl]oxymethyl]benzoate	1525919: Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0041	uM
2-[(2S,5S,8S)-14-methoxy-2-(2-methylpropyl)-4,7-dioxo-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraen-5-yl]ethyl 2,2-dimethylpropanoate	1668468: Reversal of human ABCG2-mediated multidrug resistance in HEK293/R482 cells assessed as effect on mitoxantrone-induced cytotoxicity by measuring mitoxantrone IC50 at 1 uM after 72 hrs by CCK8 assay (Rvb = 50.66 +/- 6.88 nM)	ic50	0.0046	uM
2-(3,4-dimethoxyphenyl)-N-(4-nitrophenyl)quinazolin-4-amine	1501277: Activation of ABCG2 ATPase activity (unknown origin) expressed in baculovirus infected high5 cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction based colorimetric assay	ec50	0.0047	uM
N-(4-nitrophenyl)-2-phenylpyrido[2,3-d]pyrimidin-4-amine	1479734: Activation of recombinant human ABCG2 ATPase activity expressed in baculovirus infected High five insect cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction-based colorimetric method	ec50	0.0050	uM
2-nitro-4-[[2-(3-nitrophenyl)quinazolin-4-yl]amino]phenol	1501277: Activation of ABCG2 ATPase activity (unknown origin) expressed in baculovirus infected high5 cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction based colorimetric assay	ec50	0.0050	uM
tert-butyl 3-[(2S,5S,8S)-14-methoxy-2-(2-methylpropyl)-7-oxo-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraen-5-yl]propanoate	1769268: Inhibition of BCRP (unknown origin) expressed in human HEK293/R2 cells assessed as reversal of mitoxantrone resistance after 5 days by MTS/PMS assay	ec50	0.0050	uM
methyl 3-[[4-oxo-2-[4-[2-[2-[4-[4-(4-oxo-2-phenylchromen-7-yl)oxybutyl]triazol-1-yl]ethoxy]ethoxy]phenyl]chromen-3-yl]oxymethyl]benzoate	1525919: Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0052	uM
2-(3-methoxyphenyl)-N-(4-nitrophenyl)quinazolin-4-amine	1501277: Activation of ABCG2 ATPase activity (unknown origin) expressed in baculovirus infected high5 cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction based colorimetric assay	ec50	0.0060	uM
methyl 3-[[2-[4-[4-(1-benzyltriazol-4-yl)butoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1769261: Inhibition of BCRP (unknown origin) expressed in MCF7/MX100 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0060	uM
(E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one	1668466: Reversal of human ABCG2-mediated multidrug resistance in HEK293/R482 cells assessed as effect on mitoxantrone-induced cytotoxicity by measuring mitoxantrone IC50 at 3 uM after 72 hrs by CCK8 assay (Rvb = 50.66 +/- 6.88 nM)	ic50	0.0062	uM
7-[2-[2-[4-[3-[4-(7-fluoro-4-oxochromen-2-yl)phenoxy]propyl]triazol-1-yl]ethoxy]ethoxy]-2-phenylchromen-4-one	1525919: Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0064	uM
methyl 3-[[2-[4-[2-[2-[4-[3-[4-(7-fluoro-4-oxochromen-2-yl)phenoxy]propyl]triazol-1-yl]ethoxy]ethoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate	1525920: Inhibition of BCRP in human MCF7/MX100 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0065	uM
2-nitro-4-[(2-pyridin-3-ylquinazolin-4-yl)amino]phenol	1447895: Activation of ABCG2 (unknown origin) ATPase activity expressed in baculovirus infected high five cell membranes by ascorbic acid/ammonia molybdate reaction-based colorimetric analysis	ec50	0.0070	uM
methyl 3-[[4-oxo-2-[4-[2-[2-[4-[3-(4-oxo-2-phenylchromen-7-yl)oxypropyl]triazol-1-yl]ethoxy]ethoxy]phenyl]chromen-3-yl]oxymethyl]benzoate	1525919: Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0072	uM
7-fluoro-2-[4-[3-[1-[2-[2-[4-(4-oxochromen-2-yl)phenoxy]ethoxy]ethyl]triazol-4-yl]propoxy]phenyl]chromen-4-one	1525919: Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0072	uM
7-fluoro-2-[4-[3-[1-[2-[2-[2-[4-(4-oxochromen-2-yl)phenoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]propoxy]phenyl]chromen-4-one	1525920: Inhibition of BCRP in human MCF7/MX100 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay	ec50	0.0074	uM

CTD chemical–gene interactions

309 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Mitoxantrone	affects activity, decreases activity, decreases response to substance, increases reaction, affects uptake (+12 more)	24
3-(6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino(1’,2’-1,6)pyrido(3,4-b)indol-3-yl)propionic acid tert-butyl ester	decreases export, decreases activity, affects reaction, increases secretion, increases reaction (+6 more)	14
Tetrachlorodibenzodioxin	decreases reaction, increases expression, affects cotreatment	12
Benzo(a)pyrene	decreases transport, increases transport, decreases methylation, increases reaction, affects cotreatment (+4 more)	11
Estradiol	affects reaction, affects cotreatment, affects expression, affects binding, decreases activity (+6 more)	11
Cisplatin	decreases reaction, affects expression, affects response to substance, decreases expression, affects cotreatment (+2 more)	10
Methotrexate	decreases response to substance, increases export, increases expression, affects response to substance, affects transport (+3 more)	10
tryptoquivaline	increases export, affects transport, affects uptake, decreases activity, decreases export (+2 more)	9
bisbenzimide ethoxide trihydrochloride	decreases reaction, increases export, decreases activity, decreases abundance, increases transport (+6 more)	9
Irinotecan	decreases reaction, affects response to substance, affects metabolic processing, increases response to substance, affects export (+2 more)	9
Doxorubicin	affects cotreatment, decreases response to substance, affects response to substance, increases export, increases expression (+7 more)	9
Topotecan	affects transport, decreases response to substance, increases export, increases response to substance, increases transport (+6 more)	9
estrone sulfate	increases uptake, affects cotreatment, decreases reaction, affects export, affects transport (+2 more)	7
Sulfasalazine	decreases reaction, increases expression, increases uptake, increases activity, increases reaction (+4 more)	7
Valproic Acid	affects cotreatment, increases expression, affects expression	7
Cyclosporine	decreases reaction, increases export, increases transport, decreases activity, increases expression (+2 more)	7
2-amino-1-methyl-6-phenylimidazo(4,5-b)pyridine	decreases reaction, increases export, decreases activity, affects transport, decreases expression (+4 more)	6
Resveratrol	increases expression, increases reaction, decreases reaction, increases export, decreases expression (+2 more)	5
Arsenic Trioxide	affects expression, decreases expression, increases expression, decreases reaction, increases reaction	5
Fulvestrant	affects reaction, decreases expression, decreases reaction, affects cotreatment, increases expression (+1 more)	5
Cadmium	decreases reaction, increases abundance, decreases response to substance, decreases uptake, increases expression (+3 more)	5
Fluorouracil	affects cotreatment, affects response to substance, increases expression, decreases expression, decreases reaction (+1 more)	5
Tobacco Smoke Pollution	increases expression, increases reaction, affects expression, decreases reaction, increases export	5
Cadmium Chloride	affects cotreatment, decreases reaction, affects response to substance, affects uptake, decreases uptake (+7 more)	5
bisphenol A	increases transport, decreases activity, decreases transport, decreases expression, affects reaction (+1 more)	4
chrysin	decreases expression, increases expression, decreases reaction, increases secretion, increases transport (+2 more)	4
Acetaminophen	increases expression, decreases expression, decreases activity	4
Chlorpyrifos	increases expression, affects cotreatment, affects expression, decreases response to substance	4
Novobiocin	increases abundance, increases uptake, decreases activity, decreases reaction, decreases export	4
Phenobarbital	increases expression, affects expression	4

ChEMBL screening assays

878 unique, capped per target: 651 binding, 115 admet, 111 functional, 1 toxicity

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1035250	Binding	Inhibition of BCRP expressed in human MCF7 MX cells at 31.6 uM by Hoechst 33342 staining relative to 10 uM XR9577	Aromatic 2-(thio)ureidocarboxylic acids as a new family of modulators of multidrug resistance-associated protein 1: synthesis, biological evaluation, and structure-activity relationships. — *J Med Chem*
CHEMBL1743158	ADMET	Substrates of transporters of clinical importance in the absorption and disposition of drugs, BCRP	Membrane transporters in drug development. — *Nat Rev Drug Discov*
CHEMBL2075183	Functional	TP_TRANSPORTER: inhibition of mitoxantrone efflux in BCRP-expressing MCF7-MX cells	Transport of glyburide by placental ABC transporters: implications in fetal drug exposure. — *Placenta*

Cellosaurus cell lines

20 cell lines: 16 cancer cell line, 2 spontaneously immortalized cell line, 1 induced pluripotent stem cell, 1 transformed cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_0H87	S1-M1-80	Cancer cell line	Female
CVCL_5227	OCI-AML3/HaABCG2 clone 6.2	Cancer cell line	Male
CVCL_A2KC	MDCK-hBCRP cMDR1-KO	Spontaneously immortalized cell line	Female
CVCL_A5XR	NCI-H460/TPT10 ABCG2 KO	Cancer cell line	Male
CVCL_B1EH	Abcam A-549 ABCG2 KO	Cancer cell line	Male
CVCL_B5ZS	C2BBe1 BCRP KO	Cancer cell line	Male
CVCL_B5ZU	C2BBe1 MDR1/BCRP KO	Cancer cell line	Male
CVCL_B5ZX	C2BBe1 MRP2/BCRP KO	Cancer cell line	Male
CVCL_B6A8	HepaRG BCRP KO	Cancer cell line	Female
CVCL_D6NG	OCI-AML3/HaABCG2 clone 3.3	Cancer cell line	Male

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

showing 60 of 168 trials:

NCT	Phase	Status	Title
NCT00414440	Phase 4	COMPLETED	Efficacy, Safety and Tolerability of Everolimus in Preventing End-stage Renal Disease in Patients With Autosomal Dominant Polycystic Kidney Disease
NCT03273413	Phase 4	ACTIVE_NOT_RECRUITING	Statin Therapy in Patients With Early Stage ADPKD
NCT03949894	Phase 4	COMPLETED	Evaluating the Safety and effectivenesS in Adult KorEaN Patients Treated With Tolvaptan for Management of Autosomal domInAnt poLycystic Kidney Disease
NCT02562170	Phase 4	COMPLETED	Protexa® Versus TiLoopBra® in Immediate Breast Reconstruction- A Pilot Study
NCT00309283	Phase 3	COMPLETED	Somatostatin in Polycystic Kidney: a Long-term Three Year Follow up Study
NCT00346918	Phase 3	COMPLETED	Sirolimus (Rapamune®) for Autosomal Dominant Polycystic Kidney Disease (ADPKD)
NCT00428948	Phase 3	COMPLETED	Tolvaptan Phase 3 Efficacy and Safety Study in Autosomal Dominant Polycystic Kidney Disease (ADPKD)
NCT01022424	Phase 3	COMPLETED	A Long-term Administration Study of OPC-41061 in Patients With Autosomal Dominant Polycystic Kidney Disease (ADPKD) (2) [Extension of Study 156-05-002]
NCT01214421	Phase 3	COMPLETED	Tolvaptan Extension Study in Participants With ADPKD
NCT01377246	Phase 3	COMPLETED	Somatostatin In Patients With Autosomal Dominant Polycystic Kidney Disease And Moderate To Severe Renal Insufficiency
NCT01616927	Phase 3	UNKNOWN	Study of Lanreotide to Treat Polycystic Kidney Disease
NCT01853553	Phase 3	COMPLETED	Mineralocorticoid Antagonism and Endothelial Dysfunction in Autosomal Dominant Polycystic Kidney Disease (ADPKD)
NCT02115659	Phase 3	UNKNOWN	Triptolide-Containing Formulation as Treatment for Autosomal Dominant Polycystic Kidney Disease (ADPKD)
NCT02134899	Phase 3	COMPLETED	The Efficacy of Everolimus in Reducing Total Native Kidney Volume in Polycystic Kidney Disease Transplanted Recipients
NCT02160145	Phase 3	COMPLETED	Efficacy and Safety of Tolvaptan in Subjects With Chronic Kidney Disease Between Late Stage 2 to Early Stage 4 Due to Autosomal Dominant Polycystic Kidney Disease
NCT02964273	Phase 3	COMPLETED	Safety, Pharmacokinetics, Tolerability and Efficacy of Tolvaptan in Children and Adolescents With ADPKD (Autosomal Dominant Polycystic Kidney Disease)
NCT03764605	Phase 3	UNKNOWN	Metformin vs Tolvaptan for Treatment of Autosomal Dominant Polycystic Kidney Disease
NCT03918447	Phase 3	TERMINATED	A Trial of Bardoxolone Methyl in Patients With ADPKD - FALCON
NCT04064346	Phase 3	TERMINATED	Efficacy and Safety of Lixivaptan in the Treatment of Autosomal Dominant Polycystic Kidney Disease
NCT04152837	Phase 3	TERMINATED	Safety of Lixivaptan in Subjects Previously Treated With Tolvaptan for Autosomal Dominant Polycystic Kidney Disease
NCT04939935	Phase 3	RECRUITING	Implementation of Metformin theraPy to Ease Decline of Kidney Function in Polycystic Kidney Disease (IMPEDE-PKD)
NCT05373264	Phase 3	RECRUITING	HYDROchlorothiazide to PROTECT Polycystic Kidney Disease Patients and Improve Their Quality of Life
NCT00673335	Phase 3	COMPLETED	Letrozole in Preventing Breast Cancer in Postmenopausal Women With a BRCA1 or BRCA2 Mutation
NCT00685256	Phase 3	COMPLETED	Standard Genetic Counseling With or Without a Decision Guide in Improving Communication Between Mothers Undergoing BRCA1/2 Testing and Their Minor-Age Children
NCT03162276	Phase 3	UNKNOWN	Trial of Inquiry Based Stress Reduction (IBSR) Program for BRCA1/2 Mutation Carriers
NCT00841568	Phase 2	COMPLETED	A Long-term Administration Study of OPC-41061 in Patients With Autosomal Dominant Polycystic Kidney Disease (ADPKD) [Extension of Study 156-04-001]
NCT01210560	Phase 2	COMPLETED	Dose-finding Study of New Tolvaptan Formulation in Subjects With ADPKD
NCT01336972	Phase 2	COMPLETED	Short-term Renal Hemodynamic Effects of Tolvaptan in Subjects With Autosomal Dominant Polycystic Kidney Disease (ADPKD)
NCT01451827	Phase 2	COMPLETED	8-Week Study of Tolvaptan Dose Forms in Autosomal Dominant Polycystic Kidney Disease (ADPKD)
NCT01670110	Phase 2	COMPLETED	Pasireotide LAR in Severe Polycystic Liver Disease
NCT01932450	Phase 2	UNKNOWN	Radiofrequency Ablation for ADPKD Blood Pressure and Disease Progression Control
NCT02527863	Phase 2	COMPLETED	Effect of the Aquaretic Tolvaptan on Nitric Oxide System
NCT02616055	Phase 2	TERMINATED	Long-Term Treatment and Follow up of Subjects Completing 24 Months of Treatment With Tesevatinib on Study KD019-101
NCT03203642	Phase 2	COMPLETED	Study of the Efficacy and Safety of Tesevatinib in Subjects With ADPKD
NCT03487913	Phase 2	COMPLETED	The ELiSA Study - Evaluation of Lixivaptan in Subjects With Autosomal Dominant Polycystic Kidney Disease
NCT03541447	Phase 2	COMPLETED	Tolvaptan-Octreotide LAR Combination in ADPKD
NCT04284657	Phase 2	COMPLETED	Pravastatin and Alkali Therapy in Patients With Autosomal Dominant Polycystic Kidney Disease
NCT04578548	Phase 2	TERMINATED	A Study to Evaluate the Effects of GLPG2737 in Participants With Autosomal Dominant Polycystic Kidney Disease (ADPKD)
NCT05190744	Phase 2	COMPLETED	Probenecid (PB) to Treat Hereditary Nephrogenic Diabetes Insipidus (NDI), ADPKD Treated With Tolvaptan, and Severely Polyuric Patients With Previous Lithium Administration
NCT05870007	Phase 2	ENROLLING_BY_INVITATION	Atorvastatin and Alkali Therapy in Patients With Autosomal Dominant Polycystic Kidney Disease
NCT06100133	Phase 2	UNKNOWN	Treat Autosomal Dominant Polycystic Kidney Disease With Oral Ketone Ester?
NCT06289998	Phase 2	ACTIVE_NOT_RECRUITING	Study of Tamibarotene in Patients With ADPKD
NCT06435858	Phase 2	COMPLETED	Short-term Effects of an SGLT2 Inhibitor on Divalent Ions in Autosomal Dominant Polycystic Kidney Disease
NCT06800651	Phase 2	RECRUITING	Trial of JMKX003142 in Participants With Rapidly Progressive Autosomal Dominant Polycystic Kidney Disease (ADPKD)
NCT06902558	Phase 2	RECRUITING	ANCHOR Study: A Study to Assess the Safety and Efficacy of ABBV-CLS-628 in Adult Participants With Autosomal Dominant Polycystic Kidney Disease (ADPKD)
NCT07161037	Phase 2	ACTIVE_NOT_RECRUITING	Phase 2a Study of VX-407 in Participants With ADPKD Who Have a Subset of PKD1 Gene Variants (AGLOW)
NCT07282821	Phase 2	NOT_YET_RECRUITING	Bempedoic Acid Therapy for Polycystic Kidney Disease
NCT00253539	Phase 2	COMPLETED	Arzoxifene or Tamoxifen in Preventing Breast Cancer in Premenopausal Women at High Risk for Breast Cancer
NCT00305695	Phase 2	COMPLETED	Zoledronate or Observation in Maintaining Bone Mineral Density in Patients Who Are Undergoing Surgery to Remove Both Ovaries
NCT00321633	Phase 2	COMPLETED	Carboplatin or Docetaxel in Treating Women With Metastatic Genetic Breast Cancer
NCT01333748	Phase 2	COMPLETED	Search Allelic Imbalance of Expression of BRCA Genes in Hereditary Risk of Breast and/or Ovarian Cancer
NCT01367639	Phase 2	COMPLETED	Trial of Inquiry Based Stress Reduction (IBSR) Program for BRCA1/2 Mutation Carriers
NCT00345137	Phase 1	COMPLETED	Effects of Systemic NO-Inhibition on Renal Hemodynamics in Patiens With Polycystic Kidney Disease and Chronic Glomerulonephritis
NCT04536688	Phase 1	COMPLETED	A Study of RGLS4326 in Patients With Autosomal Dominant Polycystic Kidney Disease
NCT05521191	Phase 1	COMPLETED	A Study of RGLS8429 in Patients With Autosomal Dominant Polycystic Kidney Disease
NCT06345755	Phase 1	COMPLETED	A Phase 1 Study to Evaluate Safety, Tolerability, and Pharmacokinetics of VX-407 in Healthy Participants
NCT06658964	Phase 1	NOT_YET_RECRUITING	Study to Evaluate the Drug-drug Interaction of JMKX003142 in Healthy Subjects
NCT06714006	Phase 1	RECRUITING	Phase 1 Study to Evaluate the Safety and Tolerability of Intravenously Administered PYC-003
NCT07022119	Phase 1	COMPLETED	A Phase 1 Study Evaluating Safety, Tolerability, and Pharmacokinetics of VX-407 in Healthy Participants
NCT07074327	Phase 1	COMPLETED	Effects of VX-407 on the Pharmacokinetics of Oral Contraceptives in Healthy Participants

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for ABCG2 across ~30M SureChEMBL compounds — explore on Sugi Predict.