1. Chemogenomics
2. PIK3CA

PIK3CA

NCBI gene ID HGNC ID UniProt ID SwissProt ID Description Protein family

5290

8975

P42336

PK3CA_HUMAN

phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha

lipid-kinase

Compounds

Compound EUbOPEN ID Compound name Compound image SMILES / InChIKey Mode of action Main target Chem QC data available Incucyte cytotox data available Multiplex data available Other annotation data available

EUB0000049b

Pictilisib (GDC-0941)

CS(=O)(=O)N1CCN(Cc2cc3nc(-c4cccc5[nH]ncc45)nc(N4CCOCC4)c3s2)CC1

LHNIIDJUOCFXAP-UHFFFAOYSA-N

PIK3CA

,

PIK3CB

,

PIK3CD

,

PIK3CG

Yes

Yes

No

Yes

EUB0000656a

ZSTK474

FC(F)C1=NC(C=CC=C2)=C2N1C3=NC(N4CCOCC4)=NC(N5CCOCC5)=N3

HGVNLRPZOWWDKD-UHFFFAOYSA-N

PIK3CA

,

PIK3CB

,

PIK3CD

,

PIK3CG

Yes

Yes

No

Yes

EUB0000658a

PI-103

Oc1cccc(c1)c1nc(N2CCOCC2)c2oc3ncccc3c2n1

TUVCWJQQGGETHL-UHFFFAOYSA-N

PIK3C2B

,

PIK3CA

,

PIK3CB

,

PIK3CD

,

PIK3CG

,

PRKDC

Yes

Yes

Yes

Yes

EUB0000680aBDA

BGT226

COC(N=C1)=CC=C1C2=CC3=C(C=C2)N=CC4=C3N(C5=CC=C(N6CCNCC6)C(C(F)(F)F)=C5)C(N4C)=O.OC(/C=C\C(O)=O)=O

YUXMAKUNSXIEKN-BTJKTKAUSA-N

PIK3C3

,

PIK3CA

,

PIK3CB

,

PIK3CG

Yes

Yes

Yes

Yes

EUB0000685a

Taselisib

CC1=NN(C(C)C)C(C2=CN(CCO3)C(C4=C3C=C(C5=CN(C(C)(C)C(N)=O)N=C5)C=C4)=N2)=N1

BEUQXVWXFDOSAQ-UHFFFAOYSA-N

PIK3CA

,

PIK3CD

,

PIK3CG

No

Yes

No

Yes

EUB0000689a

Alpelisib

CC1=C(SC(=N1)NC(=O)N2CCC[C@H]2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F

STUWGJZDJHPWGZ-LBPRGKRZSA-N

PIK3CA

Yes

Yes

No

Yes

EUB0000691a

Omipalisib

COC1=C(NS(C2=CC=C(F)C=C2F)(=O)=O)C=C(C3=CC(C(C4=CC=NN=C4)=CC=N5)=C5C=C3)C=N1

CGBJSGAELGCMKE-UHFFFAOYSA-N

PIK3CA

,

PIK3CB

,

PIK3CD

,

PIK3CG

Yes

Yes

Yes

Yes