PIK3CG

Summary

PIK3CG (phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma, HGNC:8978) is a protein-coding gene on chromosome 7q22.3, encoding Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (P48736). Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3).

Phosphoinositide 3-kinases (PI3Ks) phosphorylate inositol lipids and are involved in the immune response. The protein encoded by this gene is a class I catalytic subunit of PI3K. Like other class I catalytic subunits (p110-alpha p110-beta, and p110-delta), the encoded protein binds a p85 regulatory subunit to form PI3K. This gene is located in a commonly deleted segment of chromosome 7 previously identified in myeloid leukemias. Several transcript variants encoding the same protein have been found for this gene.

Source: NCBI Gene 5294 — RefSeq curated summary.

At a glance

• Gene–disease (curated): immunodeficiency 97 with autoinflammation (Strong, GenCC)
• GWAS associations: 39
• Clinical variants (ClinVar): 157 total — 3 pathogenic, 1 likely-pathogenic
• Phenotypes (HPO): 41
• Druggable target: yes — 56 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001282426

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:8978
Approved symbol	PIK3CG
Name	phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma
Location	7q22.3
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000105851
Ensembl biotype	protein_coding
OMIM	601232
Entrez	5294

Gene structure

Transcript identifiers

Ensembl transcripts: 7 — 6 protein_coding, 1 protein_coding_CDS_not_defined

ENST00000359195, ENST00000440650, ENST00000466738, ENST00000473541, ENST00000496166, ENST00000851098, ENST00000953425

RefSeq mRNA: 3 — MANE Select: NM_001282426 NM_001282426, NM_001282427, NM_002649

CCDS: CCDS5739

Canonical transcript exons

ENST00000496166 — 11 exons

Exon	Start	End
ENSE00000715047	106883033	106883163
ENSE00000715048	106884155	106884266
ENSE00000715049	106886135	106886292
ENSE00000881746	106867550	106869556
ENSE00001209556	106874700	106874803
ENSE00001274489	106882117	106882207
ENSE00001274495	106879519	106879665
ENSE00001926728	106905109	106908980
ENSE00001952038	106865282	106865426
ENSE00003594341	106872537	106872602
ENSE00003648506	106872713	106872938

Expression profiles

Bgee: expression breadth ubiquitous, 201 present calls, max score 91.65.

FANTOM5 (CAGE): breadth broad, TPM avg 9.4322 / max 423.3138, expressed in 617 samples.

FANTOM5 promoters (8 alternative TSS)

Promoter ID	TPM avg	Samples expressed
80409	7.4458	607
80411	0.9856	184
80410	0.5214	189
80412	0.1558	73
80414	0.1277	57
80415	0.0994	37
80413	0.0601	33
80416	0.0363	16

Top tissues by expression

284 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
bone marrow	UBERON:0002371	91.65	gold quality
trabecular bone tissue	UBERON:0002483	89.58	gold quality
bone marrow cell	CL:0002092	88.97	gold quality
blood	UBERON:0000178	88.57	gold quality
monocyte	CL:0000576	87.03	gold quality
epithelium of nasopharynx	UBERON:0001951	86.51	gold quality
leukocyte	CL:0000738	86.50	gold quality
mononuclear cell	CL:0000842	86.20	gold quality
granulocyte	CL:0000094	83.46	gold quality
lymph node	UBERON:0000029	81.59	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	80.09	gold quality
visceral pleura	UBERON:0002401	79.75	gold quality
colonic epithelium	UBERON:0000397	78.18	gold quality
tonsil	UBERON:0002372	78.18	gold quality
vermiform appendix	UBERON:0001154	78.06	gold quality
pleura	UBERON:0000977	76.59	gold quality
parietal pleura	UBERON:0002400	76.51	gold quality
amniotic fluid	UBERON:0000173	76.20	gold quality
spleen	UBERON:0002106	75.53	gold quality
palpebral conjunctiva	UBERON:0001812	74.96	gold quality
jejunal mucosa	UBERON:0000399	74.59	gold quality
superficial temporal artery	UBERON:0001614	73.91	gold quality
rectum	UBERON:0001052	73.65	gold quality
buccal mucosa cell	CL:0002336	73.62	silver quality
caecum	UBERON:0001153	72.87	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	72.66	gold quality
calcaneal tendon	UBERON:0003701	72.37	gold quality
sperm	CL:0000019	71.75	silver quality
gall bladder	UBERON:0002110	71.51	gold quality
duodenum	UBERON:0002114	70.05	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	11.06
E-MTAB-6075	no	229.42
E-MTAB-8410	no	3.20

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CEBPE, RUNX1

miRNA regulators (miRDB)

167 targeting PIK3CG, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-29A-3P	100.00	73.11	1835
HSA-MIR-29B-3P	100.00	73.18	1833
HSA-MIR-29C-3P	100.00	73.15	1833
HSA-MIR-6876-5P	100.00	67.68	2126
HSA-MIR-4476	100.00	68.18	2030
HSA-MIR-574-5P	100.00	66.01	989
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-33A-5P	99.99	68.62	1055
HSA-MIR-33B-5P	99.99	68.58	1062
HSA-MIR-6077	99.99	68.04	2299
HSA-MIR-513B-5P	99.99	69.96	2150
HSA-MIR-3185	99.99	68.12	1959
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-507	99.97	70.11	1915
HSA-MIR-3658	99.96	73.87	4379
HSA-MIR-557	99.96	70.01	1640
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-1250-3P	99.96	70.04	4038
HSA-MIR-3910	99.95	71.13	2227
HSA-MIR-545-3P	99.95	70.74	2783
HSA-MIR-335-3P	99.93	73.36	4958
HSA-MIR-4760-3P	99.93	70.50	2385
HSA-MIR-205-3P	99.92	69.92	3165
HSA-MIR-515-5P	99.92	69.82	2343

Literature-anchored findings (GeneRIF, showing 40)

• PI3K promotes assembly of adherens junctions, which, in turn, control p38 MAPK activation and enterocyte differentiation. (PMID:11756422)
• activates phosphatidylinositol 3 (PI3) kinase and requires PI3 kinase to regulate the cell cycle [TEL/platelet-derived growth factor receptor beta] (PMID:11861293)
• PI3K inhibits HIV-1 transcription by targeting the viral protein Tat activation complex. (PMID:12077252)
• data indicated that the v-Crk-induced activation of PI3K/AKT pathway was cooperatively achieved by two distinct interactions (PMID:12242282)
• CB(1)-induced ERK activation was mediated by PI3K(IB) and this effect may have important consequences in the control of cell death/survival decision. (PMID:12435806)
• Bordetella pertussis infection of human monocytes resulted in a marked recruitment of cellular PI3-K to the sites of B. pertussis contact (PMID:12464013)
• Down-regulation of PIK3CG by CpG hypermethylation is associated with progression of colorectal cancer (PMID:12473596)
• higher protein levels of the PI3K subunit p110 in neutrophils from MDS patients (PMID:12529294)
• regulates human immunodeficiency virus type 1 replication following viral entry in primary CD4+ T lymphocytes and macrophages (PMID:12551992)
• PI3-K activation is signaled by rapid feedback amplification that involves P2Y(12) receptor-mediated activation of Syk. (PMID:12606772)
• migrating glioma cells activate the PI3-K survival pathway, protecting migrating cells from apoptosis (PMID:13130092)
• 1. the PI3K-Akt pathway plays an important role in preventing Fas-mediated apoptosis; and 2) a PI3 K inhibitor, such as LY294002, might be a useful anti-tumoral agent for gastric carcinoma (PMID:14605879)
• Vanadyl sulfate treatment also prolonged the insulin-stimulated activation of phosphatidylinositol 3-kinase (PI3-K). (PMID:14622970)
• Activation of hexosamine pathway affects glucose-induced phosphorylation of IRS-1. Impairs coupling of IRS-1 and PI 3-kinase and activativates Akt/mammalian target of rapamycin/phosphorylated heat- and acid-stable protein-1/p70S6 kinase pathway. (PMID:15001544)
• Thus, our results identified a functional region in the IL-1R AcP required for the recruitment and activation of PI 3-kinase. (PMID:15044087)
• PI3Kgamma appears to negatively control cardiac contractility through different signalling mechanisms [review] (PMID:15046613)
• In Goto-Kakizaki rat soleus muscle, chronic administration of antioxidant alpha -lipoic-acid partly ameliorated the diabetes-related deficit in glucose metabolism including the enzymes Akt/PKB and PI-3 kinase. (PMID:15326564)
• stromal cell-mediated apoptotic protection in B-lineage ALL is mediated by PI3K/mTOR and MEK via a synergistic mechanism (PMID:15496972)
• Amiloride enhances TRAIL-induced cytotoxicity by inhibiting phosphorylation of the PI 3-Kinase-Akt pathway-associated kinases and phosphatases. (PMID:15558024)
• there is a previously unknown, p101-related regulatory subunit for PI3Kgamma (PMID:15611065)
• activation of the PI3K/Akt pathway identified as an anti-inflammatory signal that may contribute to the establishment of Salmonella typhimurium in the intestine. (PMID:15668028)
• IL-4 > PI3K/Akt > NF-(kappa)B signaling pathways, which activate androgen receptor signaling, play an important role during the development of androgen independent prostate cancer cells. (PMID:15678501)
• PI3-K promotes the expression of TFF3 and MUC2 and that the PI3-K pathway may play a pivotal role in intestinal goblet cell differentiation. (PMID:15733066)
• p110gamma and p85alpha class Ia phosphoinositide 3-kinase (PI3K) subunits play roles in generating the antiapoptotic and chemoresistant phenotype associated with accelerated local tumor recurrence (PMID:15741161)
• Acanthamoeba castellani-mediated brain microvascular endothelial cell death is dependent on phosphatidylinositol 3-kinase (PMID:15845472)
• Stimulation of TNF-alpha-primed human neutrophils with fMLP results in biphasic activation of PI3K; the first phase is largely dependent on PI3Kgamma; the second phase is largely dependent on PI3Kdelta and regulates parallel activation of ROS production (PMID:15878979)
• the PI3-kinase/p38(MAPK)/CREB pathway contributes to the EGF activation of NF-IL6beta gene expression (PMID:15901830)
• the nSH2 domain of the p85 regulatory subumit is responsible for p110 regulatory contacts, and its disruption leads to constitutive p110 activity (PMID:15932879)
• In conclusion, erythropoietin may attenuate high glucose-induced endothelial cell apoptosis via PI-3 kinase pathway. (PMID:15993382)
• The protein phosphorylation activity of PIK3 plays an essential role in beta-adrenergic receptor internalization and identify non-muscle tropomyosin as a cellular substrate. (PMID:16094730)
• In human islets, activation of PPAR-gamma inhibits h-IAPP-induced islet cell apoptosis, and this action is at least in part mediated through activation of the phosphatidylinositol 3’-kinase-Akt cascade. (PMID:16204373)
• The TGFbeta(1)-induced destabilisation of E-cadherin-mediated cell-cell adhesion involves phosphorylation of beta-catenin, which is regulated by E-cadherin adhesion complex-associated PI3-kinase and PTEN. (PMID:16219695)
• as tumorigenesis progresses the addiction of cancers to their initiating oncogene is reduced to, at least in the case of Ras, the PI3K/AKT pathway. (PMID:16286246)
• this specific PI 3-kinase isoform is involved in both proliferation and the apoptosis resistance associated with chronic myeloid leukemia (PMID:16291747)
• These results suggest that the cytoprotective effect of deprenyl is, in part, dependent on Nrf2-mediated induction of antioxidative proteins, suggesting that activation of the PI3K-Nrf2 system may be a useful therapeutic strategy for PD. (PMID:16325767)
• Results showed that inhibition of PI-3 kinase with wortmannin was accompanied by a considerably reduced expression of beta-catenin. (PMID:16328013)
• analysis of a nuclear matrix attachment region like sequence in the last intron of PI3Kgamma (PMID:16430866)
• p110beta, -gamma, and -delta isoforms of class I phosphoinositide 3-kinase have roles in oncogenic transformation (PMID:16432180)
• Cellular responsiveness to Notch signals depends on the activity of the PI3K-Akt pathway in cells as diverse as CHO cells, primary T-cells and hippocampal neurons. (PMID:16507111)
• It is concluded that PI3-kinase induces or modulates the activity of recombinant TRPV2 channels; in contrast to the previously proposed mechanism, activation of TRPV2 channels by PI3-kinase is not due to channel translocation to the plasma membrane. (PMID:16533525)

Cross-species orthologs

7 orthologs

Organism	Symbol	Gene ID
danio_rerio	pik3cg	ENSDARG00000017757
mus_musculus	Pik3cg	ENSMUSG00000020573
rattus_norvegicus	Pik3cg	ENSRNOG00000009385
drosophila_melanogaster	Pi3K68D	FBGN0015278
drosophila_melanogaster	Pi3K92E	FBGN0015279
caenorhabditis_elegans		WBGENE00000090
caenorhabditis_elegans		WBGENE00009552

Paralogs (9): PIK3C2A (ENSG00000011405), PIK3CB (ENSG00000051382), PIK3C3 (ENSG00000078142), PIK3CA (ENSG00000121879), PIK3C2B (ENSG00000133056), PIK3C2G (ENSG00000139144), PI4KB (ENSG00000143393), PIK3CD (ENSG00000171608), PI4KA (ENSG00000241973)

Protein

Protein identifiers

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform — P48736 (reviewed: P48736)

Alternative names: Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma, Phosphoinositide-3-kinase catalytic gamma polypeptide, Serine/threonine protein kinase PIK3CG, p120-PI3K

All UniProt accessions (2): P48736, E9PDN7

UniProt curated annotations — full annotation on UniProt →

Function. Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Links G-protein coupled receptor activation to PIP3 production. Involved in immune, inflammatory and allergic responses. Modulates leukocyte chemotaxis to inflammatory sites and in response to chemoattractant agents. May control leukocyte polarization and migration by regulating the spatial accumulation of PIP3 and by regulating the organization of F-actin formation and integrin-based adhesion at the leading edge. Controls motility of dendritic cells. Together with PIK3CD is involved in natural killer (NK) cell development and migration towards the sites of inflammation. Participates in T-lymphocyte migration. Regulates T-lymphocyte proliferation, activation, and cytokine production. Together with PIK3CD participates in T-lymphocyte development. Required for B-lymphocyte development and signaling. Together with PIK3CD participates in neutrophil respiratory burst. Together with PIK3CD is involved in neutrophil chemotaxis and extravasation. Together with PIK3CB promotes platelet aggregation and thrombosis. Regulates alpha-IIb/beta-3 integrins (ITGA2B/ ITGB3) adhesive function in platelets downstream of P2Y12 through a lipid kinase activity-independent mechanism. May have also a lipid kinase activity-dependent function in platelet aggregation. Involved in endothelial progenitor cell migration. Negative regulator of cardiac contractility. Modulates cardiac contractility by anchoring protein kinase A (PKA) and PDE3B activation, reducing cAMP levels. Regulates cardiac contractility also by promoting beta-adrenergic receptor internalization by binding to GRK2 and by non-muscle tropomyosin phosphorylation. Also has serine/threonine protein kinase activity: both lipid and protein kinase activities are required for beta-adrenergic receptor endocytosis. May also have a scaffolding role in modulating cardiac contractility. Contributes to cardiac hypertrophy under pathological stress. Through simultaneous binding of PDE3B to RAPGEF3 and PIK3R6 is assembled in a signaling complex in which the PI3K gamma complex is activated by RAPGEF3 and which is involved in angiogenesis. In neutrophils, participates in a phospholipase C-activating N-formyl peptide-activated GPCR (G protein-coupled receptor) signaling pathway downstream of RASGRP4-mediated Ras-activation, to promote neutrophil functional responses.

Subunit / interactions. Heterodimer of a catalytic subunit PIK3CG and a PIK3R5 or PIK3R6 regulatory subunit. Interacts with GRK2 through the PIK helical domain. Interaction with GRK2 is required for targeting to agonist-occupied receptor. Interacts with PDE3B; regulates PDE3B activity and thereby cAMP levels in cells. Interacts with TPM2. Interacts with EPHA8; regulates integrin-mediated cell adhesion to substrate. Interacts with HRAS; the interaction is required for membrane recruitment and beta-gamma G protein dimer-dependent activation of the PI3K gamma complex PIK3CG:PIK3R6.

Subcellular location. Cytoplasm. Cell membrane.

Tissue specificity. Pancreas, skeletal muscle, liver and heart.

Post-translational modifications. Autophosphorylation at Ser-1101 has no effect on the phosphatidylinositol-4,5-bisphosphate 3-kinase activity.

Disease relevance. Immunodeficiency 97 with autoinflammation (IMD97) [MIM:619802] An autosomal recessive disorder with variable features. Affected individuals have childhood-onset antibody defects, cytopenias, and T lymphocytic pneumonitis and colitis. Some patients may have features of hemophagocytic lymphohistiocytosis. The disease is caused by variants affecting the gene represented in this entry.

Activity regulation. Activated by both the alpha and the beta-gamma G proteins following stimulation of G protein-coupled receptors (GPCRs). Activation by GPCRs is assisted by the regulatory subunits (PIK3R5 or PIK3R6) leading to the translocation from the cytosol to the plasma membrane and to kinase activation. Inhibited by AS-604850 and AS-605240.

Pathway. Phospholipid metabolism; phosphatidylinositol phosphate biosynthesis.

Miscellaneous. Candidate target in therapy for inflammatory diseases. Selective inhibitors and protein ablation are anti-inflammatory in multiple disease models such as asthma, rheumatoid arthritis, allergy, systemic lupus erythematosus, airway inflammation, lung injury and pancreatitis.

Similarity. Belongs to the PI3/PI4-kinase family.

RefSeq proteins (3): NP_001269355, NP_001269356, NP_002640 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000341	PI3K_Ras-bd_dom	Domain
IPR000403	PI3/4_kinase_cat_dom	Domain
IPR001263	PI3K_accessory_dom	Domain
IPR002420	PI3K-type_C2_dom	Domain
IPR003113	PI3K_ABD	Domain
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR015433	PI3/4_kinase	Family
IPR016024	ARM-type_fold	Homologous_superfamily
IPR018936	PI3/4_kinase_CS	Conserved_site
IPR029071	Ubiquitin-like_domsf	Homologous_superfamily
IPR035892	C2_domain_sf	Homologous_superfamily
IPR036940	PI3/4_kinase_cat_sf	Homologous_superfamily
IPR042236	PI3K_accessory_sf	Homologous_superfamily
IPR045580	PIK3CG_ABD	Domain

Pfam: PF00454, PF00613, PF00792, PF00794, PF19710

Enzyme classification (BRENDA):

• EC 2.7.1.137 — phosphatidylinositol 3-kinase (BRENDA: 29 organisms, 131 substrates, 146 inhibitors, 16 Km, 0 kcat entries)
• EC 2.7.1.153 — phosphatidylinositol-4,5-bisphosphate 3-kinase (BRENDA: 12 organisms, 48 substrates, 96 inhibitors, 1 Km, 0 kcat entries)
• EC 2.7.11.1 — non-specific serine/threonine protein kinase (BRENDA: 71 organisms, 682 substrates, 228 inhibitors, 23 Km, 6 kcat entries)

Substrate kinetics (BRENDA)

14 substrates with measured Km, best-characterized 14. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ATP	0.0007–0.64	11
ATP	0.03–44	7
PHOSPHATIDYLINOSITOL	0.034–64	3
KKRAARATSNVFA	0.013–0.045	3
PHOSPHATIDYLINOSITOL 4,5-BISPHOSPHATE	0.004–15	2
PHOSPHATIDYLINOSITOL 4-PHOSPHATE	0.009–10	2
PAH1 PHOSPHATIDATE PHOSPHATASE	0.0002	2
RRRLSSLRA	0.0036–0.0037	2
1,2-DIOCTANOYLPHOSPHATIDYLINOSITOL 4,5-DIPHOSPHA	0.05	1
PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE	0.011	1
GTP	0.46	1
KKRAARASSNVFA	0.02	1
LYS-LYS-PHE-ASN-ARG-THR-LEU-SER-VAL-ALA	0.0093	1
MYELIN BASIC PROTEIN	0.145	1

Catalyzed reactions (Rhea), 4 shown:

• a 1,2-diacyl-sn-glycero-3-phospho-(1D-myo-inositol) + ATP = a 1,2-diacyl-sn-glycero-3-phospho-(1D-myo-inositol-3-phosphate) + ADP + H(+) (RHEA:12709)
• L-seryl-[protein] + ATP = O-phospho-L-seryl-[protein] + ADP + H(+) (RHEA:17989)
• a 1,2-diacyl-sn-glycero-3-phospho-(1D-myo-inositol 4-phosphate) + ATP = a 1,2-diacyl-sn-glycero-3-phospho-(1D-myo-inositol-3,4-bisphosphate) + ADP + H(+) (RHEA:18373)
• a 1,2-diacyl-sn-glycero-3-phospho-(1D-myo-inositol-4,5-bisphosphate) + ATP = a 1,2-diacyl-sn-glycero-3-phospho-(1D-myo-inositol-3,4,5-trisphosphate) + ADP + H(+) (RHEA:21292)

UniProt features (130 total): helix 52, strand 45, turn 11, domain 5, binding site 3, sequence variant 3, mutagenesis site 3, region of interest 3, modified residue 2, sequence conflict 2, chain 1

Structure

Experimental structures (PDB)

107 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
1E8Y	X-RAY DIFFRACTION	2
6AUD	X-RAY DIFFRACTION	2.02
4ANV	X-RAY DIFFRACTION	2.13
3L54	X-RAY DIFFRACTION	2.3
4WWO	X-RAY DIFFRACTION	2.3
4ANW	X-RAY DIFFRACTION	2.31
6C1S	X-RAY DIFFRACTION	2.31
4HVB	X-RAY DIFFRACTION	2.35
1E8Z	X-RAY DIFFRACTION	2.4
3ENE	X-RAY DIFFRACTION	2.4
4WWP	X-RAY DIFFRACTION	2.4
3LJ3	X-RAY DIFFRACTION	2.43
4GB9	X-RAY DIFFRACTION	2.44
5G55	X-RAY DIFFRACTION	2.45
4FUL	X-RAY DIFFRACTION	2.47
5JHB	X-RAY DIFFRACTION	2.48
2CHX	X-RAY DIFFRACTION	2.5
2V4L	X-RAY DIFFRACTION	2.5
3R7Q	X-RAY DIFFRACTION	2.5
3T8M	X-RAY DIFFRACTION	2.5
3ZVV	X-RAY DIFFRACTION	2.5
5JHA	X-RAY DIFFRACTION	2.51
3APC	X-RAY DIFFRACTION	2.54
3APD	X-RAY DIFFRACTION	2.55
3ML9	X-RAY DIFFRACTION	2.55
3S2A	X-RAY DIFFRACTION	2.55
7JWE	X-RAY DIFFRACTION	2.55
2CHW	X-RAY DIFFRACTION	2.6
2CHZ	X-RAY DIFFRACTION	2.6
3NZU	X-RAY DIFFRACTION	2.6

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P48736-F1	88.13	0.69

Antibody-complex structures (SAbDab): 1 — 8DP0

Functional residue map

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

Ligand- & substrate-binding residues (3): 864–872; 961–969; 829–838

Post-translational modifications (2): 1024, 1101

Mutagenesis-validated functional residues (3):

Position	Phenotype
833	loss of kinase activity. loss of autophosphorylation. reduced inflammatory reactions but no alterations in cardiac contr
947	abolishes protein and lipid kinase activity. does not abolish interaction with grk2.
1101	loss of autophosphorylation. no effect on phosphatidylinositol-4,5-bisphosphate 3-kinase activity.

Function

Pathways and Gene Ontology

Reactome pathways

9 pathways

ID	Pathway
R-HSA-114604	GPVI-mediated activation cascade
R-HSA-1257604	PIP3 activates AKT signaling
R-HSA-1660499	Synthesis of PIPs at the plasma membrane
R-HSA-2219530	Constitutive Signaling by Aberrant PI3K in Cancer
R-HSA-389357	CD28 dependent PI3K/Akt signaling
R-HSA-392451	G beta:gamma signalling through PI3Kgamma
R-HSA-6811558	PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling
R-HSA-9027276	Erythropoietin activates Phosphoinositide-3-kinase (PI3K)
R-HSA-9927354	Co-stimulation by ICOS

MSigDB gene sets: 689 (showing top): BIOCARTA_GCR_PATHWAY, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_PHOSPHATIDYLINOSITOL_METABOLIC_PROCESS, GOBP_DENDRITIC_CELL_MIGRATION, GOBP_MYELOID_LEUKOCYTE_MIGRATION, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOBP_CELL_CHEMOTAXIS, GOBP_REGULATION_OF_PHOSPHORYLATION, BIOCARTA_EDG1_PATHWAY, REACTOME_ADAPTIVE_IMMUNE_SYSTEM, GOBP_INFLAMMATORY_RESPONSE, GOBP_NEGATIVE_REGULATION_OF_MUSCLE_CONTRACTION, REACTOME_PLATELET_ACTIVATION_SIGNALING_AND_AGGREGATION, GOBP_SPHINGOLIPID_MEDIATED_SIGNALING_PATHWAY

GO Biological Process (44): angiogenesis (GO:0001525), positive regulation of cytokine production (GO:0001819), adaptive immune response (GO:0002250), dendritic cell chemotaxis (GO:0002407), positive regulation of acute inflammatory response (GO:0002675), respiratory burst involved in defense response (GO:0002679), sphingosine-1-phosphate receptor signaling pathway (GO:0003376), endocytosis (GO:0006897), inflammatory response (GO:0006954), immune response (GO:0006955), G protein-coupled receptor signaling pathway (GO:0007186), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), positive regulation of cytosolic calcium ion concentration (GO:0007204), positive regulation of endothelial cell migration (GO:0010595), T cell chemotaxis (GO:0010818), negative regulation of triglyceride catabolic process (GO:0010897), cell migration (GO:0016477), neutrophil chemotaxis (GO:0030593), secretory granule localization (GO:0032252), regulation of cell adhesion mediated by integrin (GO:0033628), positive regulation of Rac protein signal transduction (GO:0035022), natural killer cell chemotaxis (GO:0035747), phosphatidylinositol-3-phosphate biosynthetic process (GO:0036092), T cell proliferation (GO:0042098), T cell activation (GO:0042110), mast cell degranulation (GO:0043303), positive regulation of MAP kinase activity (GO:0043406), phosphatidylinositol 3-kinase/protein kinase B signal transduction (GO:0043491), innate immune response (GO:0045087), regulation of angiogenesis (GO:0045765), phosphatidylinositol phosphate biosynthetic process (GO:0046854), phosphatidylinositol-mediated signaling (GO:0048015), positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction (GO:0051897), negative regulation of cardiac muscle contraction (GO:0055118), platelet aggregation (GO:0070527), cellular response to cAMP (GO:0071320), neutrophil extravasation (GO:0072672), hepatocyte apoptotic process (GO:0097284), regulation of calcium ion transmembrane transport (GO:1903169), negative regulation of fibroblast apoptotic process (GO:2000270)

GO Molecular Function (13): protein kinase activity (GO:0004672), protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), 1-phosphatidylinositol-3-kinase activity (GO:0016303), 1-phosphatidylinositol-4-phosphate 3-kinase activity (GO:0035005), identical protein binding (GO:0042802), ephrin receptor binding (GO:0046875), 1-phosphatidylinositol-4,5-bisphosphate 3-kinase activity (GO:0046934), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (7): cytoplasm (GO:0005737), cytosol (GO:0005829), plasma membrane (GO:0005886), phosphatidylinositol 3-kinase complex, class IA (GO:0005943), phosphatidylinositol 3-kinase complex, class IB (GO:0005944), membrane (GO:0016020), phosphatidylinositol 3-kinase complex (GO:0005942)

Reactome top-level categories

Rollup of top-9 pathways:

Category	Pathways
Platelet activation, signaling and aggregation	1
Intracellular signaling by second messengers	1
PI Metabolism	1
PI3K/AKT Signaling in Cancer	1
Co-stimulation by CD28	1
G-protein beta:gamma signalling	1
Negative regulation of the PI3K/AKT network	1
Signaling by Erythropoietin	1
Regulation of T cell activation by CD28 family	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
phosphatidylinositol kinase activity	3
cellular anatomical structure	3
defense response	2
G protein-coupled receptor signaling pathway	2
protein kinase activity	2
phosphatidylinositol 3-kinase complex, class I	2
blood vessel morphogenesis	1
anatomical structure formation involved in morphogenesis	1
cytokine production	1
regulation of cytokine production	1
positive regulation of gene expression	1
positive regulation of multicellular organismal process	1
immune response	1
leukocyte chemotaxis	1
dendritic cell migration	1
acute inflammatory response	1
regulation of acute inflammatory response	1
positive regulation of inflammatory response	1
immune effector process	1
respiratory burst	1
sphingolipid mediated signaling pathway	1
vesicle budding from membrane	1
membrane invagination	1
vesicle-mediated transport	1
import into cell	1
immune system process	1
response to stimulus	1
G protein-coupled receptor activity	1
signal transduction	1
phospholipase C activator activity	1
regulation of biological quality	1
regulation of endothelial cell migration	1
positive regulation of cell migration	1
endothelial cell migration	1
lymphocyte chemotaxis	1
T cell migration	1
regulation of triglyceride catabolic process	1
triglyceride catabolic process	1
negative regulation of lipid catabolic process	1
negative regulation of triglyceride metabolic process	1

Protein interactions and networks

STRING

2842 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PIK3CG	PIK3R5	Q8WYR1	998
PIK3CG	IMMT	Q16891	992
PIK3CG	PIK3R2	O00459	991
PIK3CG	PIK3R3	Q92569	991
PIK3CG	PPP1R12C	Q9BZL4	991
PIK3CG	PIK3R1	P27986	988
PIK3CG	PIK3R6	Q5UE93	988
PIK3CG	PIK3CB	P42338	976
PIK3CG	PIK3CA	P42336	973
PIK3CG	AKT1	P31749	948
PIK3CG	PIK3CD	O00329	923
PIK3CG	NRAS	P01111	870
PIK3CG	MTOR	P42345	837
PIK3CG	PTEN	P60484	818
PIK3CG	BECN1	Q14457	778

IntAct

61 interactions, top by confidence:

A	B	Type	Score
PDE3B	RAPGEF3	psi-mi:“MI:0914”(association)	0.640
PIK3CG	Pik3r6	psi-mi:“MI:0915”(physical association)	0.600
PIK3CG	Pik3r6	psi-mi:“MI:0407”(direct interaction)	0.600
PIK3CG	PIK3CG	psi-mi:“MI:0217”(phosphorylation reaction)	0.590
GABARAPL1	IPO5	psi-mi:“MI:0914”(association)	0.590
APP	PIK3CG	psi-mi:“MI:0915”(physical association)	0.560
PIK3CG	BRAF	psi-mi:“MI:0915”(physical association)	0.550
PIK3CG	BRAF	psi-mi:“MI:2364”(proximity)	0.550
PIK3CG	Prkcb	psi-mi:“MI:0915”(physical association)	0.520
PDE3B	PIK3CG	psi-mi:“MI:0915”(physical association)	0.500
PIK3R5	PIK3CG	psi-mi:“MI:2364”(proximity)	0.470
PIK3CG	PIK3R5	psi-mi:“MI:2364”(proximity)	0.470
PIK3CG	PIK3R5	psi-mi:“MI:0915”(physical association)	0.470
PIK3R5	PIK3CG	psi-mi:“MI:0915”(physical association)	0.470
PIK3CG	HRAS	psi-mi:“MI:0407”(direct interaction)	0.440
PRKCB	PIK3CG	psi-mi:“MI:0407”(direct interaction)	0.440
M	PIK3CG	psi-mi:“MI:0915”(physical association)	0.400
CD37	PIK3CG	psi-mi:“MI:0915”(physical association)	0.400

BioGRID (61): PIK3CG (Affinity Capture-MS), PIK3CG (Phenotypic Enhancement), GNB1 (Phenotypic Enhancement), GNG2 (Phenotypic Enhancement), PIK3CG (Phenotypic Enhancement), PIK3CG (Co-localization), PIK3CG (Co-localization), PIK3CG (Co-localization), PIK3CG (Affinity Capture-Western), PIK3R6 (Affinity Capture-Western), PIK3R5 (Affinity Capture-Western), PIK3R6 (FRET), PIK3R5 (FRET), GAB1 (Protein-peptide), PIK3CG (Protein-peptide)

ESM2 similar proteins: A0A0G2K344, D3ZGS3, F1M386, F1MSG6, F1PBJ0, G5EF51, O00329, O02697, O35242, O35904, O70481, O88763, O94830, P32871, P42336, P42337, P42338, P42339, P42347, P42348, P48736, P50520, P54676, P70600, Q01968, Q14289, Q14BI7, Q16JS8, Q3MHU3, Q3UYK3, Q4KWH5, Q4KWH8, Q5D891, Q5ZI89, Q6AZN6, Q6GQ76, Q6NVF0, Q6PF93, Q7Z392, Q80Y98

Diamond homologs: A0A0G2K344, O00329, O00443, O00750, O02697, O35904, O70167, O70173, O75747, P32871, P42336, P42337, P42338, P48736, P50520, P54673, P54674, P54675, P54676, Q0WPX9, Q22258, Q54UC0, Q5RAY1, Q61194, Q8BTI9, Q8WN22, Q9C680, Q9FMJ0, Q9JHG7, Q9VK45, Q9Z1L0, A4IID4, A4QPH2, A9X1A0, B0KWC1, B1MTG7, B2KI64, B3EX61, B4UT09, E9Q3L2

SIGNOR signaling

51 interactions.

A	Effect	B	Mechanism
IRS2	up-regulates	PIK3CG	binding
INS	up-regulates	PIK3CG
ERBB3	up-regulates	PIK3CG	binding
ERBB4	up-regulates	PIK3CG	binding
PIK3CG	up-regulates	PIP3	“chemical modification”
CD28	up-regulates	PIK3CG	binding
HRAS	up-regulates	PIK3CG	binding
KRAS	up-regulates	PIK3CG	binding
NRAS	up-regulates	PIK3CG	binding
dactolisib	down-regulates	PIK3CG	“chemical inhibition”
pictrelisib	down-regulates	PIK3CG	“chemical inhibition”
5-[(2,2-difluoro-1,3-benzodioxol-5-yl)methylidene]thiazolidine-2,4-dione	down-regulates	PIK3CG	“chemical inhibition”
AS-605240	down-regulates	PIK3CG	“chemical inhibition”
BKM120	down-regulates	PIK3CG	“chemical inhibition”
CAY10505	down-regulates	PIK3CG	“chemical inhibition”
CH5132799	down-regulates	PIK3CG	“chemical inhibition”
PIK3AP1	up-regulates	PIK3CG	binding
1-[4-[[2-(2-amino-5-pyrimidinyl)-7-methyl-4-(4-morpholinyl)-6-thieno[3,2-d]pyrimidinyl]methyl]-1-piperazinyl]-2-hydroxy-1-propanone	down-regulates	PIK3CG	“chemical inhibition”
GSK1059615	down-regulates	PIK3CG	“chemical inhibition”
GSK2126458	down-regulates	PIK3CG	“chemical inhibition”
3-methyladenine	down-regulates	PIK3CG	“chemical inhibition”
PKI-587	down-regulates	PIK3CG	“chemical inhibition”
PI-103	down-regulates	PIK3CG	“chemical inhibition”
IC-87114	down-regulates	PIK3CG	“chemical inhibition”
PIK-90	down-regulates	PIK3CG	“chemical inhibition”
PIK-93	down-regulates	PIK3CG	“chemical inhibition”
PKI-402	down-regulates	PIK3CG	“chemical inhibition”
PP121	down-regulates	PIK3CG	“chemical inhibition”
3-[2,4-diamino-7-(3-hydroxyphenyl)-6-pteridinyl]phenol	down-regulates	PIK3CG	“chemical inhibition”

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 31 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	5	18.6×	3e-03
PIP3 activates AKT signaling	5	12.8×	5e-03
Diseases of signal transduction by growth factor receptors and second messengers	5	10.9×	5e-03

GO biological processes:

GO term	Partners	Fold	FDR
positive regulation of ERK1 and ERK2 cascade	6	18.2×	6e-04
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	5	14.0×	2e-03
negative regulation of cell population proliferation	6	9.0×	3e-03
negative regulation of apoptotic process	6	7.5×	6e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	3
Likely pathogenic	1
Uncertain significance	103
Likely benign	24
Benign	10

Top pathogenic / likely-pathogenic (4)

Variant ID	HGVS	Classification
1675218	NM_001282426.2(PIK3CG):c.3062G>C (p.Arg1021Pro)	Pathogenic
1675219	NM_001282426.2(PIK3CG):c.3254A>G (p.Asn1085Ser)	Pathogenic
1675220	NM_001282426.2(PIK3CG):c.145C>A (p.Arg49Ser)	Pathogenic
3910977	NM_001282426.2(PIK3CG):c.211A>T (p.Lys71Ter)	Likely pathogenic

SpliceAI

1566 predictions. Top by Δscore:

Variant	Effect	Δscore
7:106882107:C:CA	acceptor_gain	1.0000
7:106883029:GTAGG:G	acceptor_loss	1.0000
7:106883030:TAG:T	acceptor_loss	1.0000
7:106883031:A:G	acceptor_loss	1.0000
7:106883162:AGGTG:A	donor_loss	1.0000
7:106883163:GGT:G	donor_loss	1.0000
7:106883164:G:GG	donor_gain	1.0000
7:106883164:GTGAG:G	donor_loss	1.0000
7:106883165:T:A	donor_loss	1.0000
7:106884262:GACAG:G	donor_gain	1.0000
7:106884263:ACAG:A	donor_loss	1.0000
7:106884265:AGG:A	donor_loss	1.0000
7:106884267:G:GA	donor_loss	1.0000
7:106884268:TGAG:T	donor_loss	1.0000
7:106884269:GAGT:G	donor_loss	1.0000
7:106886243:T:TA	acceptor_gain	1.0000
7:106886246:T:TA	acceptor_gain	1.0000
7:106886247:G:A	acceptor_gain	1.0000
7:106865348:TGGG:T	donor_loss	0.9900
7:106865349:GG:G	donor_gain	0.9900
7:106865350:GG:G	donor_gain	0.9900
7:106865351:G:GG	donor_gain	0.9900
7:106865351:GTAG:G	donor_loss	0.9900
7:106865352:TA:T	donor_loss	0.9900
7:106872740:T:TA	acceptor_gain	0.9900
7:106874698:A:AG	acceptor_gain	0.9900
7:106874699:G:GG	acceptor_gain	0.9900
7:106874699:GTT:G	acceptor_gain	0.9900
7:106874801:GCA:G	donor_gain	0.9900
7:106874804:G:GG	donor_gain	0.9900

AlphaMissense

7309 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
7:106879624:A:G	K833E	1.000
7:106879625:A:T	K833I	1.000
7:106879626:A:C	K833N	1.000
7:106879626:A:T	K833N	1.000
7:106879648:G:C	D841H	1.000
7:106879649:A:C	D841A	1.000
7:106879649:A:G	D841G	1.000
7:106879649:A:T	D841V	1.000
7:106882185:C:G	C869W	1.000
7:106882207:G:A	G877R	1.000
7:106882207:G:C	G877R	1.000
7:106883033:G:A	G877E	1.000
7:106883033:G:T	G877V	1.000
7:106883063:C:T	T887I	1.000
7:106884230:G:C	D946H	1.000
7:106884231:A:C	D946A	1.000
7:106884231:A:G	D946G	1.000
7:106884231:A:T	D946V	1.000
7:106884235:A:C	R947S	1.000
7:106884235:A:T	R947S	1.000
7:106884236:C:G	H948D	1.000
7:106884237:A:G	H948R	1.000
7:106884238:C:A	H948Q	1.000
7:106884238:C:G	H948Q	1.000
7:106884243:A:T	D950V	1.000
7:106884245:A:C	N951H	1.000
7:106884245:A:G	N951D	1.000
7:106884245:A:T	N951Y	1.000
7:106884246:A:T	N951I	1.000
7:106884247:T:A	N951K	1.000

dbSNP variants (sampled 300 via entrez): RS1000309944 (7:106872203 T>C), RS1000386783 (7:106898267 G>A,T), RS1000452287 (7:106906113 G>A), RS1000513467 (7:106893176 G>A), RS1000526867 (7:106878893 G>C,T), RS1000543821 (7:106870425 G>A), RS1000624805 (7:106865176 A>G), RS1000724433 (7:106907062 A>C,G), RS1000762503 (7:106870769 A>T), RS1000943916 (7:106900018 G>A), RS1000949341 (7:106886357 G>A,C,T), RS1000962098 (7:106884532 A>G), RS1001044762 (7:106878645 T>C), RS1001094723 (7:106906663 T>C), RS1001104782 (7:106885933 A>T)

Disease associations

OMIM: gene MIM:601232 | disease phenotypes: MIM:619802, MIM:219700, MIM:148300

GenCC curated gene-disease

Disease	Classification	Inheritance
immunodeficiency 97 with autoinflammation	Strong	Autosomal recessive

ClinGen Gene-Disease Validity (1)

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

Disease	Classification	Inheritance
immunodeficiency 97 with autoinflammation	Moderate	AR

Mondo (5): immunodeficiency 97 with autoinflammation (MONDO:0030717), cystic fibrosis (MONDO:0009061), long QT syndrome (MONDO:0002442), prostate cancer (MONDO:0008315), keratoconus (MONDO:0015486)

Orphanet (4): Cystic fibrosis (Orphanet:586), Familial prostate cancer (Orphanet:1331), OBSOLETE: Keratoconus (Orphanet:156071), NON RARE IN EUROPE: Isolated keratoconus (Orphanet:2335)

HPO phenotypes

41 total (30 of 41 shown, HPO-id order):

HPO	Term
HP:0000007	Autosomal recessive inheritance
HP:0000010	Recurrent urinary tract infections
HP:0000403	Recurrent otitis media
HP:0000964	Eczematoid dermatitis
HP:0001252	Hypotonia
HP:0001433	Hepatosplenomegaly
HP:0001581	Recurrent skin infections
HP:0001742	Nasal congestion
HP:0001744	Splenomegaly
HP:0001873	Thrombocytopenia
HP:0001880	Increased total eosinophil count
HP:0001888	Decreased total lymphocyte count
HP:0001890	Autoimmune hemolytic anemia
HP:0001904	Autoimmune neutropenia
HP:0001945	Fever
HP:0002014	Diarrhea
HP:0002027	Abdominal pain
HP:0002155	Hypertriglyceridemia
HP:0002583	Colitis
HP:0002716	Lymphadenopathy
HP:0002720	Decreased circulating IgA concentration
HP:0002850	Decreased circulating total IgM
HP:0002851	Elevated double-negative T cell proportion
HP:0003281	Increased circulating ferritin concentration
HP:0003621	Juvenile onset
HP:0003651	Foam cells
HP:0004313	Decreased circulating immunoglobulin concentration
HP:0004315	Decreased circulating IgG concentration
HP:0004387	Enterocolitis
HP:0005415	Decreased CD8+ T cell proportion

GWAS associations

39 associations (top):

Study	Trait	p-value
GCST000497_10	Mean platelet volume	2.000000e-33
GCST001231_4	Carotid intima media thickness	3.000000e-06
GCST001231_9	Carotid intima media thickness	2.000000e-12
GCST001235_3	Blood pressure	2.000000e-13
GCST001335_16	Mean platelet volume	7.000000e-57
GCST001337_21	Platelet count	6.000000e-25
GCST001439_1	Mean platelet volume	1.000000e-11
GCST002184_6	Mean platelet volume	5.000000e-22
GCST003274_11	Pulse pressure	4.000000e-12
GCST003274_2	Pulse pressure	4.000000e-06
GCST004775_27	Pulse pressure	4.000000e-22
GCST004776_49	Systolic blood pressure	1.000000e-13
GCST005054_3	Platelet count	3.000000e-10
GCST005991_91	Platelet count	2.000000e-11
GCST006009_6	Pulse pressure	1.000000e-08
GCST006168_21	Pulse pressure x alcohol consumption interaction (2df test)	1.000000e-99
GCST006168_47	Pulse pressure x alcohol consumption interaction (2df test)	2.000000e-97
GCST006170_27	Systolic blood pressure x alcohol consumption (light vs heavy) interaction (2df test)	1.000000e-14
GCST006171_10	Pulse pressure x alcohol consumption (light vs heavy) interaction (2df test)	5.000000e-32
GCST006171_2	Pulse pressure x alcohol consumption (light vs heavy) interaction (2df test)	4.000000e-33
GCST006188_35	Systolic blood pressure (cigarette smoking interaction)	2.000000e-38
GCST006434_109	Systolic blood pressure x alcohol consumption interaction (2df test)	1.000000e-24
GCST006434_50	Systolic blood pressure x alcohol consumption interaction (2df test)	6.000000e-35
GCST007095_132	Systolic blood pressure	2.000000e-10
GCST007095_133	Systolic blood pressure	2.000000e-08
GCST007096_78	Pulse pressure	4.000000e-100
GCST007097_122	Pulse pressure	9.000000e-30
GCST007097_123	Pulse pressure	1.000000e-34
GCST007099_225	Systolic blood pressure	3.000000e-36
GCST007435_2	Carotid plaque	4.000000e-11

EFO canonical traits (8, from GWAS)

EFO ID	Trait name
EFO:0005763	pulse pressure measurement
EFO:0004309	platelet count
EFO:0006335	systolic blood pressure
EFO:0004329	alcohol drinking
EFO:0006527	smoking status measurement
EFO:0009783	carotid atherosclerosis
EFO:0007969	cognitive inhibition measurement
EFO:0009792	valine measurement

MeSH disease descriptors (4)

Descriptor	Name	Tree numbers
D003550	Cystic Fibrosis	C06.689.202; C08.381.187; C16.320.190; C16.614.213
D007640	Keratoconus	C11.204.627
D008133	Long QT Syndrome	C14.280.067.565; C14.280.123.625; C16.131.240.400.715; C23.550.073.547
D011471	Prostatic Neoplasms	C04.588.945.440.770; C12.100.500.260.750; C12.100.500.565.625; C12.200.294.260.750; C12.200.294.565.625; C12.200.758.409.750; C12.900.619.750

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (8): CHEMBL3267 (SINGLE PROTEIN), CHEMBL3430881 (PROTEIN COMPLEX), CHEMBL3559703 (PROTEIN COMPLEX GROUP), CHEMBL3885617 (PROTEIN FAMILY), CHEMBL4296106 (PROTEIN COMPLEX), CHEMBL6193791 (PROTEIN-PROTEIN INTERACTION), CHEMBL6195503 (PROTEIN-PROTEIN INTERACTION), CHEMBL6195555 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

56 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 222,087 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1287853	FEDRATINIB	4	3,554
CHEMBL2216870	IDELALISIB	4	10,163
CHEMBL2396661	ALPELISIB	4	6,070
CHEMBL3039502	DUVELISIB	4	5,332
CHEMBL3218576	COPANLISIB	4	4,529
CHEMBL3545068	COPANLISIB HYDROCHLORIDE	4	1,306
CHEMBL3643413	LENIOLISIB	4	341
CHEMBL3948730	UMBRALISIB	4	2,833
CHEMBL4650215	INAVOLISIB	4	876
CHEMBL535	SUNITINIB	4	79,020
CHEMBL1879463	DACTOLISIB	3	7,988
CHEMBL2017974	BUPARLISIB	3	6,568
CHEMBL2387080	TASELISIB	3	3,473
CHEMBL50	QUERCETIN	3	74,559
CHEMBL592445	GEDATOLISIB	3	3,177
CHEMBL603469	LESTAURTINIB	3
CHEMBL1234354	PF-04691502	2	4,092
CHEMBL1236962	OMIPALISIB	2	3,989
CHEMBL1684984	IZORLISIB	2	1,147
CHEMBL1922094	APITOLISIB	2	3,070
CHEMBL2165191	AZD-6482	2
CHEMBL2216859	NEMIRALISIB	2
CHEMBL2216863	DEZAPELISIB	2
CHEMBL230011	TG100-115	2
CHEMBL2336325	VISTUSERTIB	2
CHEMBL3120215	OSI-027	2
CHEMBL3218578	BGT-226 FREE BASE	2
CHEMBL3360203	PILARALISIB	2
CHEMBL3545097	SAPANISERTIB	2
CHEMBL3545366	VOXTALISIB	2

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — Phosphatidylinositol kinases

Most potent curated ligand interactions (69 total), top 25:

Ligand	Action	Affinity	Parameter
eganelisib	Inhibition	9.54	pKd
AZD3458	Inhibition	9.1	pIC50
AZD8154	Inhibition	9.05	pIC50
compound 15a [PMID: 32069401]	Inhibition	8.92	pIC50
taselisib	Inhibition	8.84	pKi
compound 5d [PMID: 31335136]	Inhibition	8.8	pIC50
compound 22 [PMID: 24754609]	Inhibition	8.7	pKi
AZ2	Inhibition	8.65	pKd
neolymphostin A	Inhibition	8.46	pKd
compound 82 [PMID: 21332118]	Inhibition	8.33	pIC50
dactolisib	Inhibition	8.3	pIC50
copanlisib	Inhibition	8.19	pIC50
PI 3-Kg inhibitor	Inhibition	8.1	pIC50
NVP-CLR457	Inhibition	8.08	pIC50
apitolisib	Inhibition	7.85	pIC50
bosmolisib	Inhibition	7.82	pIC50
PI-103	Inhibition	7.82	pIC50
wortmannin	Inhibition	7.82	pKd
inavolisib	Inhibition	7.74	pKi
pilaralisib	Inhibition	7.64	pIC50
samotolisib	Inhibition	7.62	pIC50
omipalisib	Inhibition	7.62	pKi
tenalisib	Inhibition	7.62	pIC50
RV1729	Inhibition	7.6	pIC50
VS-5584	Inhibition	7.6	pIC50

Binding affinities (BindingDB)

1461 measured of 3136 human assays (3137 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
Inavolisib	KI	0.034 nM	US-10112932: Benzoxazepin oxazolidinone compounds and methods of use
(2S)-2-[[2-[(4S)-4-(fluoromethyl)-2-oxo-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]propanamide	KI	0.04 nM	US-10112932: Benzoxazepin oxazolidinone compounds and methods of use
(2S)-2-[[2-[(4S)-4-(difluoromethyl)-2-oxo-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]butanamide	KI	0.048 nM	US-10112932: Benzoxazepin oxazolidinone compounds and methods of use
(2S)-2-cyclopropyl-2-[[2-[(4S)-4-(fluoromethyl)-2-oxo-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]acetamide	KI	0.051 nM	US-10112932: Benzoxazepin oxazolidinone compounds and methods of use
(2S)-2-cyclopropyl-2-[[2-[(4S)-4-(difluoromethyl)-2-oxo-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]acetamide	KI	0.06 nM	US-10112932: Benzoxazepin oxazolidinone compounds and methods of use
Taselisib	KI	0.09 nM	US-10112932: Benzoxazepin oxazolidinone compounds and methods of use
4-amino-6-[2-(7-fluoro-2-piperidin-1-ylquinolin-3-yl)pyrrolidin-1-yl]pyrimidine-5-carbonitrile	IC50	0.1 nM	US-9637488: Heterocyclic compounds as inhibitors of class I PI3KS
(2S)-2-cyclopropyl-2-[[2-[(4R)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]acetamide	KI	0.464 nM	US-10112932: Benzoxazepin oxazolidinone compounds and methods of use
7-fluoro-2-(2-fluorophenyl)-3-[1-(7H-purin-6-yl)pyrrolidin-2-yl]quinoline	IC50	0.5 nM	US-9637488: Heterocyclic compounds as inhibitors of class I PI3KS
7-fluoro-2-phenyl-3-[1-(7H-purin-6-yl)pyrrolidin-2-yl]quinoline	IC50	0.7 nM	US-9637488: Heterocyclic compounds as inhibitors of class I PI3KS
7-fluoro-3-[1-(2-methyl-7H-purin-6-yl)pyrrolidin-2-yl]-2-piperidin-1-ylquinoline	IC50	0.9 nM	US-9637488: Heterocyclic compounds as inhibitors of class I PI3KS
(2S)-2-cyclobutyl-2-[[2-[(4R)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]acetamide	KI	0.949 nM	US-10112932: Benzoxazepin oxazolidinone compounds and methods of use
4-amino-6-[[(1S)-1-[3-chloro-6-(4-hydroxyphenyl)imidazo[1,2-b]pyridazin-7-yl]ethyl]amino]pyrimidine-5-carbonitrile	IC50	1 nM	US-10208066: Imidazopyridazine compounds and their use
(S)-4-amino-6-(0-(3-fluoro-6-phenylimidazo[1,2-b]pyridazin-7-yl)ethyl)amino)pyrimidine-5-carbonitrile	IC50	1 nM	US-10208066: Imidazopyridazine compounds and their use
DW12	IC50	1.4 nM
4-amino-6-(2-(7-fluoro-2-morpholinoquinolin-3-yl)pyrrolidin-1-yl)pyrimidine-5-carbonitrile	IC50	1.6 nM	US-9637488: Heterocyclic compounds as inhibitors of class I PI3KS
4-[8-methyl-3-[(2R)-1-(7H-purin-6-yl)pyrrolidin-2-yl]quinolin-2-yl]morpholine	IC50	1.6 nM	US-9637488: Heterocyclic compounds as inhibitors of class I PI3KS
5-ethynyl-6-[2-(7-fluoro-2-phenylquinolin-3-yl)pyrrolidin-1-yl]pyrimidin-4-amine	IC50	1.7 nM	US-9637488: Heterocyclic compounds as inhibitors of class I PI3KS
2,4-diamino-6-[[(1S)-1-[3-(5-aminopyrazin-2-yl)-5,8-dichloro-4-oxoquinazolin-2-yl]ethyl]amino]pyrimidine-5-carbonitrile	IC50	1.8 nM	US-9499523: Phosphatidylinositol 3-kinase inhibitors
4-[8-chloro-3-[1-(7H-purin-6-yl)pyrrolidin-2-yl]quinolin-2-yl]morpholine	IC50	1.8 nM	US-9637488: Heterocyclic compounds as inhibitors of class I PI3KS
ethyl 4-(7-oxo-5-thiomorpholin-4-ylthieno[3,2-b]pyran-3-yl)benzoate	IC50	1.87 nM	US-9505780: Thienopyranones as kinase and epigenetic inhibitors
6-{[(5Z)-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl}-4-{2-[4-(trifluoromethyl)phenyl]ethyl}-3,4-dihydro-2H-1,4-benzoxazin-3-one	IC50	1.92 nM
2,4-diamino-6-[[(1S)-1-[3-(5-aminopyrazin-2-yl)-5-chloro-4-oxoquinazolin-2-yl]ethyl]amino]pyrimidine-5-carbonitrile	IC50	2 nM	US-9499523: Phosphatidylinositol 3-kinase inhibitors
4-[[(1S)-1-(3-chloro-6-phenylimidazo[1,2-b]pyridazin-7-yl)ethyl]amino]-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile	IC50	2 nM	US-10208066: Imidazopyridazine compounds and their use
4-amino-6-[[(1S)-1-(3-methyl-6-phenylimidazo[1,2-b]pyridazin-7-yl)ethyl]amino]pyrimidine-5-carbonitrile	IC50	2 nM	US-10208066: Imidazopyridazine compounds and their use
7-fluoro-3-[1-(7H-purin-6-yl)pyrrolidin-2-yl]-2-pyridin-2-ylquinoline	IC50	2.2 nM	US-9637488: Heterocyclic compounds as inhibitors of class I PI3KS
4-[2-(4-bromophenyl)ethyl]-6-{[(5Z)-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl}-3,4-dihydro-2H-1,4-benzoxazin-3-one	IC50	2.34 nM
4-[(4-tert-butylphenyl)methyl]-6-{[(5Z)-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl}-3,4-dihydro-2H-1,4-benzoxazin-3-one	IC50	2.42 nM
4-[(3,4-dimethylphenyl)methyl]-6-{[(5Z)-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl}-3,4-dihydro-2H-1,4-benzoxazin-3-one	IC50	2.59 nM
4-[2-(3,5-dimethylphenyl)ethyl]-6-{[(5Z)-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl}-3,4-dihydro-2H-1,4-benzoxazin-3-one	IC50	2.65 nM
4-[2-(3-methoxyphenyl)ethyl]-6-{[(5Z)-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl}-3,4-dihydro-2H-1,4-benzoxazin-3-one	IC50	2.66 nM
4-[2-(3,5-dimethoxyphenyl)ethyl]-6-{[(5Z)-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl}-3,4-dihydro-2H-1,4-benzoxazin-3-one	IC50	2.79 nM
4-{6-chloroimidazo[1,2-a]pyridin-3-yl}-2-[(2-methyl-5-nitrobenzene)sulfonyl]-1,3-thiazole	IC50	2.8 nM
2-[(1S)-1-[[6-amino-5-(5-methyl-1,3,4-oxadiazol-2-yl)pyrimidin-4-yl]amino]propyl]-5-chloro-3-phenylquinazolin-4-one	IC50	3 nM	US-9670194: Substituted aminopyrimidine compounds and methods of use
N-[(1S)-1-(3-chloro-6-phenylimidazo[1,2-b]pyridazin-7-yl)ethyl]-7H-purin-6-amine	IC50	3 nM	US-10208066: Imidazopyridazine compounds and their use
N-[(1S)-1-[3-chloro-6-(2-fluorophenyl)imidazo[1,2-b]pyridazin-7-yl]ethyl]-7H-purin-6-amine	IC50	3 nM	US-10208066: Imidazopyridazine compounds and their use
N-[(1S)-1-[3-chloro-6-(3-fluorophenyl)imidazo[1,2-b]pyridazin-7-yl]ethyl]-7H-purin-6-amine	IC50	3 nM	US-10208066: Imidazopyridazine compounds and their use
2,4-diamino-6-[[(S)-[3-(5-aminopyrazin-2-yl)-5,8-dichloro-4-oxoquinazolin-2-yl]-cyclopropylmethyl]amino]pyrimidine-5-carbonitrile	IC50	3.6 nM	US-9499523: Phosphatidylinositol 3-kinase inhibitors
N-[1-(3-chloro-6-phenylimidazo[1,2-b]pyridazin-7-yl)propyl]-7H-purin-6-amine	IC50	4 nM	US-10208066: Imidazopyridazine compounds and their use
N-[1-[3-chloro-6-(2-fluorophenyl)imidazo[1,2-b]pyridazin-7-yl]propyl]-7H-purin-6-amine	IC50	4 nM	US-10208066: Imidazopyridazine compounds and their use
2,4-diamino-6-[[(S)-[3-(5-aminopyrazin-2-yl)-5-chloro-4-oxoquinazolin-2-yl]-cyclopropylmethyl]amino]pyrimidine-5-carbonitrile	IC50	4.2 nM	US-9499523: Phosphatidylinositol 3-kinase inhibitors
4-[2-(3-chlorophenyl)ethyl]-6-{[(5Z)-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl}-3,4-dihydro-2H-1,4-benzoxazin-3-one	IC50	4.27 nM
4-[2-(2,4-dichlorophenyl)ethyl]-6-{[(5Z)-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl}-3,4-dihydro-2H-1,4-benzoxazin-3-one	IC50	4.28 nM
4-[2-(3,4-dichlorophenyl)ethyl]-6-{[(5Z)-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl}-3,4-dihydro-2H-1,4-benzoxazin-3-one	IC50	4.36 nM
2,4-diamino-6-[[(1S)-1-[3-(5-aminopyrazin-2-yl)-5-chloro-8-fluoro-4-oxoquinazolin-2-yl]ethyl]amino]pyrimidine-5-carbonitrile	IC50	4.4 nM	US-9499523: Phosphatidylinositol 3-kinase inhibitors
CHEMBL3910904	IC50	4.6 nM
4-[2-(4-chlorophenyl)ethyl]-6-{[(5Z)-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl}-3,4-dihydro-2H-1,4-benzoxazin-3-one	IC50	4.76 nM
5-ethynyl-6-[2-[7-fluoro-2-(2-methoxyphenyl)quinolin-3-yl]pyrrolidin-1-yl]pyrimidin-4-amine	IC50	4.8 nM	US-9637488: Heterocyclic compounds as inhibitors of class I PI3KS
4-[2-(3,4-difluorophenyl)ethyl]-6-{[(5Z)-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl}-3,4-dihydro-2H-1,4-benzoxazin-3-one	IC50	4.84 nM
4-[2-(3-methylphenyl)ethyl]-6-{[(5Z)-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl}-3,4-dihydro-2H-1,4-benzoxazin-3-one	IC50	4.96 nM

ChEMBL bioactivities

5388 potent at pChembl≥5 of 5646 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	Ki	0.01	nM	CHEMBL3586674
10.96	Ki	0.011	nM	CHEMBL3586672
10.89	Ki	0.013	nM	CHEMBL3586668
10.80	Ki	0.016	nM	CHEMBL3586673
10.77	Ki	0.017	nM	CHEMBL3586670
10.62	Ki	0.024	nM	CHEMBL3586669
10.62	IC50	0.024	nM	OMIPALISIB
10.60	Ki	0.025	nM	CHEMBL3586680
10.47	Ki	0.034	nM	CHEMBL3586675
10.32	Ki	0.048	nM	CHEMBL3586666
10.22	Ki	0.06	nM	OMIPALISIB
10.18	Ki	0.066	nM	CHEMBL3586671
10.10	Ki	0.079	nM	TASELISIB
10.00	IC50	0.1	nM	CHEMBL5781674
9.96	Ki	0.111	nM	CHEMBL2331664
9.80	Ki	0.157	nM	CHEMBL3586665
9.77	Ki	0.17	nM	CHEMBL4878958
9.77	IC50	0.17	nM	CHEMBL5641901
9.62	IC50	0.24	nM	CHEMBL5646460
9.54	Kd	0.29	nM	EGANELISIB
9.54	IC50	0.29	nM	EGANELISIB
9.52	IC50	0.3	nM	CHEMBL4168702
9.52	IC50	0.3	nM	CHEMBL5639851
9.52	IC50	0.3	nM	CHEMBL5647196
9.48	Ki	0.33	nM	CHEMBL3586667
9.41	Ki	0.39	nM	CHEMBL5847452
9.40	IC50	0.398	nM	CHEMBL5914789
9.40	IC50	0.398	nM	CHEMBL5941326
9.39	IC50	0.41	nM	OMIPALISIB
9.38	Ki	0.417	nM	CHEMBL3770993
9.36	IC50	0.44	nM	OMIPALISIB
9.36	Ki	0.44	nM	CHEMBL4860369
9.30	IC50	0.5	nM	CHEMBL4217725
9.30	IC50	0.5	nM	CHEMBL5596530
9.30	IC50	0.5	nM	CHEMBL5994857
9.30	IC50	0.501	nM	CHEMBL5081600
9.29	Ki	0.51	nM	OMIPALISIB
9.26	Ki	0.55	nM	CHEMBL2381373
9.24	IC50	0.58	nM	CHEMBL4780201
9.22	IC50	0.6	nM	CHEMBL2381271
9.22	IC50	0.6	nM	OMIPALISIB
9.22	IC50	0.6	nM	CHEMBL3901855
9.21	IC50	0.61	nM	OMIPALISIB
9.21	IC50	0.62	nM	CHEMBL5639811
9.21	IC50	0.62	nM	CHEMBL5639738
9.20	IC50	0.631	nM	CHEMBL4127396
9.20	IC50	0.631	nM	CHEMBL4128537
9.20	IC50	0.631	nM	CHEMBL4126445
9.20	IC50	0.631	nM	CHEMBL5090959
9.20	IC50	0.631	nM	CHEMBL4126156

PubChem BioAssay actives

3368 with measured affinity, of 5009 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-[5-(6-chloro-5-methoxy-3-pyridinyl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]acetamide	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	<0.0001	uM
1-[5-(5-methoxy-3-pyridinyl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]-3-[2-(1-propan-2-ylimidazol-4-yl)ethyl]urea	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	<0.0001	uM
1-[5-(5-methoxy-3-pyridinyl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]-3-[2-(1-propylimidazol-4-yl)ethyl]urea	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	<0.0001	uM
1-[5-(5-methoxy-3-pyridinyl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]-3-[2-[1-(2-methylpropyl)imidazol-4-yl]ethyl]urea	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	<0.0001	uM
1-[2-[1-(2-fluoroethyl)imidazol-4-yl]ethyl]-3-[5-(5-methoxy-3-pyridinyl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]urea	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	<0.0001	uM
1-[2-[1-(2,2-difluoroethyl)imidazol-4-yl]ethyl]-3-[5-(5-methoxy-3-pyridinyl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]urea	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	<0.0001	uM
1-[2-[1-(2,2-difluoroethyl)imidazol-4-yl]ethyl]-3-[5-(6-methoxypyrazin-2-yl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]urea	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	<0.0001	uM
1-[5-(5-methoxy-3-pyridinyl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]-3-[2-[1-(2,2,2-trifluoroethyl)imidazol-4-yl]ethyl]urea	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	<0.0001	uM
1-[2-[1-(2-hydroxyethyl)imidazol-4-yl]ethyl]-3-[5-(5-methoxy-3-pyridinyl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]urea	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	<0.0001	uM
2,4-difluoro-N-[2-methoxy-5-(4-pyridazin-4-ylquinolin-6-yl)-3-pyridinyl]benzenesulfonamide	2091841: Inhibition of PI3Kgamma (unknown origin)	ic50	<0.0001	uM
N-[5-(5-methoxy-3-pyridinyl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]acetamide	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	<0.0001	uM
N-[5-(6-methoxypyrazin-2-yl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]acetamide	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	<0.0001	uM
1-[5-(6-chloro-5-methoxy-3-pyridinyl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]-3-[2-[1-(2,2-difluoroethyl)imidazol-4-yl]ethyl]urea	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	<0.0001	uM
1-[5-(5-methoxy-3-pyridinyl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]-3-(2-propoxyethyl)urea	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	<0.0001	uM
N-[5-(5,6-dimethoxy-3-pyridinyl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]acetamide	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	<0.0001	uM
1-[1-[(2S)-2-hydroxypropanoyl]piperidin-4-yl]-3-methyl-8-(6-methyl-3-pyridinyl)imidazo[4,5-c][1,5]naphthyridin-2-one	731923: Inhibition of human PI3Kgamma	ki	0.0001	uM
1-ethyl-3-[5-(5-methoxy-3-pyridinyl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]urea	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	0.0001	uM
N-[[6-[[5-(5,6-dimethoxy-3-pyridinyl)pyrazolo[1,5-a]pyrimidin-2-yl]amino]-2-pyridinyl]methyl]acetamide	2141196: Inhibition of PI3K gamma (unknown origin) incubated for 1 hr in presence of ATP by ADP-glo based luminescence assay	ic50	0.0002	uM
N-[[6-[[5-(5,6-dimethoxy-3-pyridinyl)pyrazolo[1,5-a]pyrimidin-2-yl]amino]-2-pyridinyl]methyl]-2-methoxyacetamide	2141196: Inhibition of PI3K gamma (unknown origin) incubated for 1 hr in presence of ATP by ADP-glo based luminescence assay	ic50	0.0002	uM
N-(5-pyridin-3-yl-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl)acetamide	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	0.0002	uM
18-fluoro-25-methoxy-31-methyl-22,22-dioxo-3,22lambda6,30-trithia-6,8,15,23,26-pentazahexacyclo[22.3.1.12,5.110,13.117,21.04,9]hentriaconta-1(28),2(31),4,6,8,10,12,17,19,21(29),24,26-dodecaen-16-one	1785808: Inhibition of human PI3Kgamma by HTRF assay	ki	0.0002	uM
N-[2-chloro-5-[3-(6-morpholin-4-yl-3-pyridinyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]-3-pyridinyl]benzenesulfonamide	2140011: Inhibition of PI3Kgamma (unknown origin)	ic50	0.0003	uM
N-[2-chloro-5-[3-[1-(2-morpholin-4-ylethyl)pyrazol-4-yl]-1H-pyrrolo[2,3-b]pyridin-5-yl]-3-pyridinyl]benzenesulfonamide	2140011: Inhibition of PI3Kgamma (unknown origin)	ic50	0.0003	uM
N-[5-(6-methoxy-3-pyridinyl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]acetamide	1231043: Inhibition of PI3Kgamma (unknown origin) using [33P]ATP and PIP2 incubated for 15 mins by liquid scintillation counting method	ki	0.0003	uM
2-[(1S)-1-[[5-(4-hydroxy-3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]ethyl]-5-methyl-3-phenylpyrrolo[2,1-f][1,2,4]triazin-4-one	1363651: Inhibition of recombinant human N-terminal His6-tagged full length p110gamma using PIP2 as substrate preincubated for 30 mins followed by substrate addition by HTRF assay	ic50	0.0003	uM
2-amino-N-[(1S)-1-[8-[2-(1-methylpyrazol-4-yl)ethynyl]-1-oxo-2-phenylisoquinolin-3-yl]ethyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide	1316853: Binding affinity to human recombinant full length N-terminal His-tagged PI3Kgamma expressed in Sf9 insect cells by equilibrium fluorescence titration analysis	kd	0.0003	uM
25-methoxy-31-methyl-22,22-dioxo-3,22lambda6,30-trithia-6,8,15,23,26-pentazahexacyclo[22.3.1.12,5.110,13.117,21.04,9]hentriaconta-1(28),2(31),4,6,8,10,12,17(29),18,20,24,26-dodecaen-16-one	1785808: Inhibition of human PI3Kgamma by HTRF assay	ki	0.0004	uM
N-[2-chloro-5-(3-pyridin-4-yl-1H-pyrrolo[2,3-b]pyridin-5-yl)-3-pyridinyl]benzenesulfonamide	1379439: Inhibition of recombinant full length His-tagged human PI3K p110gamma expressed in baculovirus expression system using PIP2/PS as substrate after 1 hr by ADP-Glo luminescence assay	ic50	0.0005	uM
1-[5-(5,6-dimethoxy-3-pyridinyl)pyrazolo[1,5-a]pyrimidin-2-yl]-3-(2-pyridin-3-yloxyethyl)urea	2122389: Inhibition of PI3Kgamma (unknown origin) using PI3:PS as substrate incubated for 1 hr in presence of ATP by ADP-glo kinase assay	ic50	0.0005	uM
N-[5-[2-[(1S)-1-cyclopropylethyl]-7-(methanesulfonamido)-1-oxo-3H-isoindol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide	1497485: Inhibition of recombinant human 6His-tagged PI3Kgamma (144 to 1102 residues) using DiC8-PIP2 as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by ADP-Glo assay	ic50	0.0006	uM
N-[5-[2-[(1S)-1-cyclopropylethyl]-1-oxo-7-sulfamoyl-3H-isoindol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide	1497485: Inhibition of recombinant human 6His-tagged PI3Kgamma (144 to 1102 residues) using DiC8-PIP2 as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by ADP-Glo assay	ic50	0.0006	uM
N-[5-[2-[(1S)-1-cyclopropylethyl]-7-methyl-1-oxo-3H-isoindol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide	1497485: Inhibition of recombinant human 6His-tagged PI3Kgamma (144 to 1102 residues) using DiC8-PIP2 as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by ADP-Glo assay	ic50	0.0006	uM
2,4-difluoro-N-[5-[4-[[1-(2-hydroxyethyl)pyrazol-4-yl]amino]quinazolin-6-yl]-2-methoxy-3-pyridinyl]benzenesulfonamide	1672939: Inhibition of PI3Kgamma (unknown origin) using lipid as substrate incubated for 15 mins followed by substrate addition and measured after 60 mins ADPGloTM reagent based assay	ic50	0.0006	uM
2-[(1S)-1-cyclopropylethyl]-5-[2-[[6-[4-(hydroxymethyl)-1,3-oxazol-5-yl]-2-pyridinyl]amino]-4-methyl-1,3-thiazol-5-yl]-7-methylsulfonyl-3H-isoindol-1-one	1807050: Inhibition of recombinant human PI3Kgamma assessed as reduction in ADP production using Dic8-PIP2 as substrate pre-treated for 15 mins followed by substrate addition measured after 60 mins by ADP-glo assay	ic50	0.0006	uM
N-[2-chloro-5-(3-pyridin-4-yl-2H-pyrazolo[3,4-b]pyridin-5-yl)-3-pyridinyl]-4-fluorobenzenesulfonamide	2133120: Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate incubated for 60 mins in presence of ATP by ADP-Glo assay	ic50	0.0006	uM
6-N-[5-(5,6-dimethoxy-3-pyridinyl)pyrazolo[1,5-a]pyrimidin-2-yl]pyridine-2,6-diamine	2141196: Inhibition of PI3K gamma (unknown origin) incubated for 1 hr in presence of ATP by ADP-glo based luminescence assay	ic50	0.0006	uM
N-[[6-[[5-(5,6-dimethoxy-3-pyridinyl)pyrazolo[1,5-a]pyrimidin-2-yl]amino]-2-pyridinyl]methyl]-1-methylimidazole-4-carboxamide	2141196: Inhibition of PI3K gamma (unknown origin) incubated for 1 hr in presence of ATP by ADP-glo based luminescence assay	ic50	0.0006	uM
2-[4-[2-(2-propan-2-yl-1,2,4-triazol-3-yl)-4,5-dihydro-[1]benzoxepino[5,4-d][1,3]thiazol-8-yl]pyrazol-1-yl]ethanol	746367: Inhibition of GST-fused human recombinant PI3Kgamma expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presence of [gamma-33P]-ATP	ki	0.0006	uM
8-(1-methylimidazol-4-yl)-2-(2-propan-2-yl-1,2,4-triazol-3-yl)-4,5-dihydro-[1]benzoxepino[5,4-d][1,3]thiazole	746367: Inhibition of GST-fused human recombinant PI3Kgamma expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presence of [gamma-33P]-ATP	ic50	0.0006	uM
2-[(1S)-1-[[5-(3-fluoro-5-hydroxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]ethyl]-5-methyl-3-phenylpyrrolo[2,1-f][1,2,4]triazin-4-one	1363651: Inhibition of recombinant human N-terminal His6-tagged full length p110gamma using PIP2 as substrate preincubated for 30 mins followed by substrate addition by HTRF assay	ic50	0.0006	uM
2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydro-1H-imidazo[1,2-c]quinazolin-5-ylidene]pyrimidine-5-carboxamide	1578117: Inhibition of PI3Kgamma (unknown origin)	ic50	0.0007	uM
N-[2-chloro-5-(3-pyridin-4-yl-1H-pyrrolo[2,3-b]pyridin-5-yl)-3-pyridinyl]-2-fluorobenzenesulfonamide	1379439: Inhibition of recombinant full length His-tagged human PI3K p110gamma expressed in baculovirus expression system using PIP2/PS as substrate after 1 hr by ADP-Glo luminescence assay	ic50	0.0007	uM
N-[2-chloro-5-(3-pyridin-4-yl-1H-pyrrolo[2,3-b]pyridin-5-yl)-3-pyridinyl]-4-fluorobenzenesulfonamide	1379439: Inhibition of recombinant full length His-tagged human PI3K p110gamma expressed in baculovirus expression system using PIP2/PS as substrate after 1 hr by ADP-Glo luminescence assay	ic50	0.0007	uM
2-amino-5-[2-[(1S)-1-cyclopropylethyl]-7-(difluoromethoxy)-1-oxo-3H-isoindol-5-yl]-N-(4-hydroxy-4-methylcyclohexyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide	1898686: Inhibition of PI3Kgamma (unknown origin) at 10 uM using PIP2 as substrate preincubated for 60 mins followed by substrate addition and measured after 45 mins in presence of ATP by TR-FRET analysis	ki	0.0007	uM
2,4-difluoro-N-[2-methoxy-5-[3-[1-(3-morpholin-4-ylpropyl)triazol-4-yl]imidazo[1,2-b]pyridazin-6-yl]-3-pyridinyl]benzenesulfonamide	2002974: Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate incubated for 1 hr in presence of ATP by ADP-Glo assay	ic50	0.0007	uM
N-[5-[3-(4-acetylpiperazin-1-yl)quinoxalin-6-yl]-2-chloro-3-pyridinyl]-4-fluorobenzenesulfonamide	1916686: Inhibition of PI3Kgamma (unknown origin) by TR-FRET assay	ic50	0.0007	uM
2-(2-propan-2-yl-1,2,4-triazol-3-yl)-8-(1H-pyrazol-4-yl)-4,5-dihydro-[1]benzoxepino[5,4-d][1,3]thiazole	746367: Inhibition of GST-fused human recombinant PI3Kgamma expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presence of [gamma-33P]-ATP	ic50	0.0007	uM
2-[(1S)-1-[[5-(4-hydroxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]ethyl]-5-methyl-3-phenylpyrrolo[2,1-f][1,2,4]triazin-4-one	1363651: Inhibition of recombinant human N-terminal His6-tagged full length p110gamma using PIP2 as substrate preincubated for 30 mins followed by substrate addition by HTRF assay	ic50	0.0007	uM
2,4-difluoro-N-[2-methoxy-5-[4-[4-(1,2,4-triazol-1-ylmethyl)phenyl]quinolin-6-yl]-3-pyridinyl]benzenesulfonamide	1327484: Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate after 1 hr in presence of ATP by ADP-glo based luminescence assay	ic50	0.0007	uM
N-[3-hydroxy-5-[4-[[(1S)-1-(5-methyl-4-oxo-3-phenylpyrrolo[2,1-f][1,2,4]triazin-2-yl)ethyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]phenyl]methanesulfonamide	1363651: Inhibition of recombinant human N-terminal His6-tagged full length p110gamma using PIP2 as substrate preincubated for 30 mins followed by substrate addition by HTRF assay	ic50	0.0007	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, increases expression, increases methylation, increases mutagenesis	4
Tretinoin	increases expression	4
sodium arsenite	affects methylation, decreases expression	2
tamibarotene	decreases reaction, increases activity, increases expression	2
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one	decreases reaction, increases activity, increases expression, decreases activity	2
GSK-J4	increases expression	1
triphenyl phosphate	affects expression	1
bis(tri-n-butyltin)oxide	increases expression	1
tributyltin	increases expression	1
mono-(2-ethylhexyl)phthalate	increases abundance, increases methylation	1
afimoxifene	decreases response to substance	1
cobaltous chloride	increases expression	1
ochratoxin A	increases expression	1
methylmercury II	increases expression	1
cyhalothrin	affects binding	1
cordycepin	affects binding	1
CGP 52608	affects binding, increases reaction	1
abrine	increases expression	1
2-(1H-indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-ylthieno(3,2-d)pyrimidine	affects activity	1
(+)-JQ1 compound	decreases expression	1
1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno(3,2-d)pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one	decreases activity	1
Resveratrol	decreases activity	1
Pioglitazone	affects cotreatment, decreases expression	1
Decitabine	increases expression	1
Arsenic Trioxide	decreases expression	1
Butyrates	decreases expression	1
Cadmium	decreases expression	1
Cisplatin	decreases response to substance	1
Cycloheximide	decreases expression, decreases reaction	1
Diethylhexyl Phthalate	increases methylation, increases abundance	1

ChEMBL screening assays

899 unique, capped per target: 888 binding, 8 admet, 2 functional, 1 toxicity

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1001353	Binding	Inhibition of PI3K gamma	Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines. — Bioorg Med Chem Lett
CHEMBL4005475	ADMET	Inhibition of human full length PI3Kgamma using PIP2/ATP as substrate after 30 mins by TR-FRET assay	Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856. — J Med Chem
CHEMBL5123069	Toxicity	Inhibition of human PI3Kgamma by ADP-Glo assay	Discovery of novel 7,8-dihydropteridine-6(5H)-one-based DNA-PK inhibitors as potential anticancer agents via scaffold hopping strategy. — Eur J Med Chem

Clinical trials (associated diseases)

300 trials via MONDO — disease-level, not drug-specific.

Trial	Phase	Status	Title
NCT00157690	PHASE4	COMPLETED	Study of Alendronate to Prevent and Treat Osteoporosis in Cystic Fibrosis Patients
NCT00208078	PHASE4	TERMINATED	Effect of Non-Invasive Ventilation in Cystic Fibrosis Patient With Chronic Respiratory Failure.
NCT00244270	PHASE4	COMPLETED	Cystic Fibrosis and Totally Implantable Vascular Access Devices
NCT00333385	PHASE4	TERMINATED	Continuous Versus Short Infusions of Ceftazidime in Cystic Fibrosis
NCT00411736	PHASE4	COMPLETED	Scandinavian Cystic Fibrosis Azithromycin Study
NCT00418470	PHASE4	TERMINATED	Prolonging the Duration of Peripheral Venous Catheters in Cystic Fibrosis People
NCT00431964	PHASE4	COMPLETED	Effect of Azithromycin on Lung Function in 6-18 Year-olds With Cystic Fibrosis (CF) Not Infected With P. Aeruginosa
NCT00434278	PHASE4	TERMINATED	A Trial of Pulmozyme Withdrawal on Exercise Tolerance in Cystic Fibrosis Subjects With Severe Lung Disease (TOPIC)
NCT00483769	PHASE4	COMPLETED	One Year Glargine Treatment in CFRD Children and Adolescents
NCT00528190	PHASE4	COMPLETED	Treatment of Aspergillus Fumigatus (a Fungal Infection) in Patients With Cystic Fibrosis
NCT00557089	PHASE4	COMPLETED	The Effect of rhDNase on Ventilation Inhomogeneity in Patients With Cystic Fibrosis
NCT00572975	PHASE4	COMPLETED	Malabsorption Blood Test:Toward a Novel Approach to Quantify Steatorrhea
NCT00680316	PHASE4	TERMINATED	A Study of Pulmozyme® (Dornase Alpha) in 3- to 5-Year-Old Patients With Cystic Fibrosis
NCT00685035	PHASE4	COMPLETED	Comparison of Airway Clearance Therapy in Cystic Fibrosis Using the Same VEST Therapy Device But With Different Settings
NCT00744250	PHASE4	TERMINATED	Intraduodenal Aspiration Study to Assess the Bioavailability of Oral Pancrecarb® Compared to Placebo Control
NCT00787917	PHASE4	TERMINATED	An Exploratory Study to Assess Multiple Doses of Omalizumab in Patients With Cystic Fibrosis Complicated by Acute Bronchopulmonary Aspergillosis (ABPA)
NCT00843817	PHASE4	COMPLETED	RhDNase and Biodistribution of PMN Serine Proteases in Cystic Fibrosis Sputum
NCT00890370	PHASE4	COMPLETED	Should Any One Airway Clearance Technique be Recommended for People With Cystic Fibrosis?
NCT00996424	PHASE4	TERMINATED	The Effect of Inhaled N-Acetylcysteine Compared to Normal Saline on Sputum Rheology and Lung Function
NCT01044719	PHASE4	UNKNOWN	Duration of Antibiotics in Infective Exacerbations of Cystic Fibrosis
NCT01100606	PHASE4	COMPLETED	A Study to Evaluate the Mode of Administration and Safety of EUR-1008 (APT-1008) in Infants 1 to 12 Months of Age
NCT01131507	PHASE4	COMPLETED	PR-018: An Open-Label, Safety Extension of Study PR-011
NCT01207245	PHASE4	COMPLETED	Circadian Rhythm In Tobramycin Elimination In Cystic Fibrosis
NCT01323101	PHASE4	COMPLETED	Doxycycline Effects on Inflammation in Cystic Fibrosis
NCT01327703	PHASE4	COMPLETED	Control of Steatorrhea in Participants With Cystic Fibrosis and Exocrine Pancreatic Insufficiency
NCT01377792	PHASE4	COMPLETED	Study of Long-term Treatment With Hypertonic Saline in Patients With Cystic Fibrosis
NCT01400750	PHASE4	COMPLETED	Comparison of 2 Treatment Regimens for Eradication of P Aeruginosa Infection in Children With Cystic Fibrosis
NCT01429259	PHASE4	COMPLETED	Population Pharmacokinetics of Prolonged Infusion Meropenem in Cystic Fibrosis (CF) Children
NCT01608555	PHASE4	COMPLETED	Tobramycin 300 mg Once-a-day (o.d.) Aerosol in Adults With Cystic Fibrosis
NCT01667094	PHASE4	UNKNOWN	A Study Comparing Continuous Infusion Antibiotics to Standard Treatment for Lung Infections in Cystic Fibrosis
NCT01694069	PHASE4	TERMINATED	Continuous Infusion Piperacillin-tazobactam for the Treatment of Cystic Fibrosis
NCT01702415	PHASE4	WITHDRAWN	Zoledronic Acid in Cystic Fibrosis
NCT01712334	PHASE4	COMPLETED	A Study of the Comparable Efficacy and Safety of Pulmozyme (Dornase Alfa) Delivered by the eRapid Nebulizer System in Patients With Cystic Fibrosis
NCT01737983	PHASE4	COMPLETED	Effect of Lactobacillus Reuteri in Cystic Fibrosis
NCT01844778	PHASE4	COMPLETED	Ease of Use and Microbial Contamination of Tobramycin Inhalation Powder (TIP) Versus Nebulised Tobramycin Inhalation Solution (TIS) and Nebulised Colistimethate (COLI)
NCT01880346	PHASE4	COMPLETED	Comparison of Absorption of Vitamin D in Cystic Fibrosis
NCT01882400	PHASE4	COMPLETED	Assessment of Response to Treatment of Osteoporosis With Oral Bisphosphonates in Patients With Muscular Dystrophy
NCT01937325	PHASE4	UNKNOWN	CPET in CF Patients With One G551D Mutation Taking VX770
NCT02015663	PHASE4	TERMINATED	Tobramycin Inhalation Powder (TIP) Administered Once Daily Continuously Versus TIP Administered BID in 28 Day on / 28 Day Off Cycles
NCT02048592	PHASE4	UNKNOWN	Impact of Immunonutrition on the Patients With Cystic Fibrosis