Buparlisib

Buparlisib

SCHEMBL143412

Cl.Nc1cc(C(F)(F)F)c(-c2cc(N3CCOCC3)nc(N3CCOCC3)n2)cn1

nearest known ligand 0.98

Full drug profile on Sugi Atlas →

Known targets — ChEMBL curated mechanism

PIK3CAPIK3CBPIK3CDPIK3CGPIK3R1PIK3R2PIK3R3PIK3R5

The experimentally established mechanism targets of Buparlisib. The predicted profile below is derived independently by chemical similarity — agreement is a validation signal, a miss is honest.

Predicted protein targets (top 16)

geneUniProtsupporting neighboursconfidence
PIK3CA known ✓ P42336 8/20 0.98
PIK3R1 known ✓ P27986 5/20 0.98
PIK3CG known ✓ P48736 3/20 0.98
PIK3CB known ✓ P42338 3/20 0.98
PIK3R5 known ✓ Q8WYR1 2/20 0.98
PIK3CD known ✓ O00329 2/20 0.98
MTOR P42345 11/20 0.98
PIK3C2B O00750 2/20 0.98
PRKDC P78527 2/20 0.98
PIK3C3 Q8NEB9 2/20 0.98
PI4KB Q9UBF8 2/20 0.98
AKR1C3 P42330 1/20 0.98
RICTOR Q6R327 1/20 0.70
RPTOR Q8N122 1/20 0.70
MAPKAP1 Q9BPZ7 1/20 0.70
MLST8 Q9BVC4 1/20 0.70

Click a target to see other patent compounds predicted against it — the reverse direction, in place.

Similar compounds — the chemically nearest patent molecules

Nearest neighbours by Morgan-fingerprint cosine across the patent-compound collection, with each neighbour's top predicted target and the predicted targets it shares with this molecule.

Compoundsimilaritytop predictedshared targets
Buparlisib SCHEMBL29412438 1.00 MTOR (0.98) MTORPIK3CAPIK3R1PIK3CGPIK3CB
Buparlisib SCHEMBL18528952 1.00 MTOR (0.98) MTORPIK3CAPIK3R1PIK3CGPIK3CB
Buparlisib SCHEMBL29493083 1.00 MTOR (0.98) MTORPIK3CAPIK3R1PIK3CGPIK3CB
Buparlisib SCHEMBL896994 0.99 MTOR (0.96) MTORPIK3CAPIK3R1PIK3CGPIK3CB
Buparlisib SCHEMBL146956 0.99 MTOR (1.00) MTORPIK3CAPIK3R1PIK3CGPIK3CB
Buparlisib SCHEMBL29351351 0.99 MTOR (1.00) MTORPIK3CAPIK3R1PIK3CGPIK3CB
Buparlisib SCHEMBL29350945 0.99 MTOR (1.00) MTORPIK3CAPIK3R1PIK3CGPIK3CB
Buparlisib SCHEMBL29387968 0.99 MTOR (1.00) MTORPIK3CAPIK3R1PIK3CGPIK3CB
Buparlisib SCHEMBL896966 0.98 MTOR (0.98) MTORPIK3CAPIK3R1PIK3CGPIK3CB
SCHEMBL19460575 0.97 MTOR (0.96) MTORPIK3CAPIK3R1PIK3CGPIK3CB

Similarity is cosine over the 2,048-bit Morgan fingerprint (≈ Tanimoto). Identical fingerprints score 1.00.

Patent provenance — the patents this molecule appears in, and who filed them

Claimed or disclosed in 29 patents — showing the first 20. claimed = in the patent's claims; disclosed = body only.

PatentTitleAssigneePublishedPriorityFilingCountryStatus
US-10377818-B2 Method of treating glioma THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY (US) 2019-08-13 US disclosed
US-10130629-B2 Pharmaceutical combinations NOVARTIS AG (CH) 2018-11-20 US disclosed
EP-3040333-B1 CRYSTALLINE FORMS OF 5-(2,6-DI-4-MORPHOLINYL-4-PYRIDMIDINYL)-4-TRIFLUOROMETHYLPYRIDIN-2-AMINE, A PIK3 INHIBITOR NOVARTIS AG (CH) 2018-09-12 EP disclosed
US-20180064709-A1 PHARMACEUTICAL COMBINATIONS BEIJING NOVARTIS PHARMA CO. LTD. (CN) 2018-03-08 US disclosed
EP-3273959-A1 PHARMACEUTICAL COMBINATIONS NOVARTIS AG (CH) 2018-01-31 EP disclosed
US-9637468-B2 Process for manufacturing 5-(2,6-di-4-morpholinyl-4-pyrimidinyl)-4-trifluoromethylpyridin-2-amine NOVARTIS AG (CH) 2017-05-02 US disclosed
EP-2964200-B1 FORMULATIONS OF ORGANIC COMPOUNDS NOVARTIS AG (CH) 2017-04-19 EP disclosed
WO-2017050111-A1 CRYSTAL FORM AND PREPARATION METHOD OF 5-[2,6-DI(4-MORPHOLINYL)-4-PYRIMIDINYL]-4-(TRIFLUOROMETHYL)-2-PYRIDINAMINE HYDROCHLORIDE 苏州晶云药物科技有限公司 2017-03-30 WO disclosed
US-20170056336-A1 CO-TARGETING ANDROGEN RECEPTOR SPLICE VARIANTS AND MTOR SIGNALING PATHWAY FOR THE TREATMENT OF CASTRATION-RESISTANT PROSTATE CANCER NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT 2017-03-02 US disclosed
US-9474534-B2 Formulations of organic compounds NOVARTIS AG (CH) 2016-10-25 US disclosed
US-9181215-B2 Manufacturing process for pyrimidine derivatives NOVARTIS AG (CH) 2015-11-10 US disclosed
US-20150246897-A1 Process for Manufacturing 5-(2,6-Di-4-morpholinyl-4-pyrimidinyl)-4-trifluoromethylpyridin-2-amine NOVARTIS PHARMA AG (CH) 2015-09-03 US disclosed
EP-2912030-A1 IMPROVED PROCESS FOR MANUFACTURING 5-(2,6-DI-4-MORPHOLINYL-4-PYRIMIDINYL)-4-TRIFLUOROMETHYLPYRIDIN-2-AMINE Novartis AG (CH) 2015-09-02 EP disclosed
US-20150232446-A1 MANUFACTURING PROCESS FOR PYRIMIDINE DERIVATIVES NOVARTIS AG (CH) 2015-08-20 US disclosed
WO-2014136048-A1 FORMULATIONS OF ORGANIC COMPOUNDS NOVARTIS AG (CH) 2014-09-12 WO disclosed
WO-2014064058-A1 IMPROVED PROCESS FOR MANUFACTURING 5-(2,6-DI-4-MORPHOLINYL-4-PYRIMIDINYL)-4-TRIFLUOROMETHYLPYRIDIN-2-AMINE NOVARTIS AG (CH) 2014-05-01 WO disclosed
US-20130225571-A1 MANUFACTURING PROCESS FOR PYRIMIDINE DERIVATIVES NOVARTIS AG (CH) 2013-08-29 US disclosed
EP-2621908-A2 MANUFACTURING PROCESS FOR PYRIMIDINE DERIVATIVES Novartis AG (CH) 2013-08-07 EP disclosed
WO-2012044727-A2 MANUFACTURING PROCESS FOR PYRIMIDINE DERIVATIVES NOVARTIS AG (CH) 2012-04-05 WO disclosed
US-20120059005-A1 COMBINATION OF (A) A PHOSPHOINOSITIDE 3-KINASE INHIBITOR AND (B) AN ANTIDIABETIC COMPOUND FOR USE IN THE TREATMENT OF PROLIFERATIVE DISEASES NOVARTIS AG (CH) 2012-03-08 US disclosed

Patent text — is the patent's own abstract consistent with the prediction?

For each of this compound's patents that has machine-readable text (7 of them — usually the abstract, not the full specification), we ask MedCPT which protein the text reads most about, and where the chemistry-predicted target lands among 4885 human targets. A high rank means the patent's own wording is consistent with the prediction — a weak, independent signal, not proof of activity.

PatentTitleText reads most aboutPredicted target · text-rank
US-20180064709-A1 PHARMACEUTICAL COMBINATIONS PKD1, SLC5A6, H4C1; H4C2; H4C3; H4C4; H4C5; H4C6; H4C8; H4C9; H4C11; H4C12; H4C13; H4C14; H4C15; H4C16 PIK3CA 2617/4885PIK3R1 3764/4885PIK3CG 3661/4885
US-20130225571-A1 MANUFACTURING PROCESS FOR PYRIMIDINE DERIVATIVES UMPS, HPRT1, TYMS PIK3CA 879/4885PIK3R1 4209/4885PIK3CG 2133/4885
US-20150246897-A1 Process for Manufacturing 5-(2,6-Di-4-morpholinyl-4-pyrimidinyl)-4-trifluoromethylpyridin-2-amine PAH, QDPR, NISCH PIK3CA 890/4885PIK3R1 3293/4885PIK3CG 689/4885
US-10130629-B2 Pharmaceutical combinations PKD1, SLC5A6, H4C1; H4C2; H4C3; H4C4; H4C5; H4C6; H4C8; H4C9; H4C11; H4C12; H4C13; H4C14; H4C15; H4C16 PIK3CA 2617/4885PIK3R1 3764/4885PIK3CG 3661/4885
US-20150232446-A1 MANUFACTURING PROCESS FOR PYRIMIDINE DERIVATIVES UMPS, HPRT1, NUDT1 PIK3CA 602/4885PIK3R1 4000/4885PIK3CG 1738/4885
US-20120059005-A1 COMBINATION OF (A) A PHOSPHOINOSITIDE 3-KINASE INHIBITOR AND (B) AN ANTIDIABETIC COMPOUND FOR USE IN THE TREATMENT OF PROLIFERATIVE DISEASES PIK3CA, PDPK1, PIK3CB PIK3CA 1/4885PIK3R1 79/4885PIK3CG 10/4885
US-20170056336-A1 CO-TARGETING ANDROGEN RECEPTOR SPLICE VARIANTS AND MTOR SIGNALING PATHWAY FOR THE TREATMENT OF CASTRATION-RESISTANT PROSTATE CANCER AR, MTOR, RICTOR PIK3CA 104/4885PIK3R1 7/4885PIK3CG 300/4885

“Text reads most about” is the patent abstract's nearest protein in MedCPT space (background-debiased). Only ~1.4% of patents have machine-readable text, so most compounds won't have this panel.