P42336 | PK3CA_HUMAN | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PIK3CA)

Pfam Domain Table

AccessionDomainRangeColor
PF00454PI3_PI4_kinase - Phosphatidylinositol 3- and 4-kinase798~1015
PF00613PI3Ka - Phosphoinositide 3-kinase family, accessory domain (PIK domain)520~703
PF00792PI3K_C2 - Phosphoinositide 3-kinase C2351~483
PF00794PI3K_rbd - PI3-kinase family, ras-binding domain174~291
PF02192PI3K_p85B - PI3-kinase family, p85-binding domain32~107

3D structures mapped by conservation among orthologs

[ Domain: "C2 domain" // PI3K_C2 ]

 PyMOL session

[ Domain: "ARM repeat" // PI3Ka ]

 PyMOL session

[ Domain: "Ubiquitin-like" // PI3K_rbd ]

 PyMOL session

[ Domain: "Ubiquitin-like" // PI3K_p85B ]

 PyMOL session

[ Domain: "Protein kinase" // PI3_PI4_kinase ]

 PyMOL session


[ Alpha Fold Model ] (go)



Known binders annotated in ChEMBL

 IC50 CSV    Ki CSV
Only the first 20 rows are shown.
molecule_chembl_idstructureassay_typerelation valueunitmol_wtsmilesorganism assay_chembl_idbao_label
CHEMBL1236962 IC50 = 0.04 nM 505.51 COc1ncc(-c2ccc3nccc(-c4ccnnc4)c3c2)cc1NS(=O)(=O)c1ccc(F)cc1F Homo sapiens CHEMBL3223603 single protein format
CHEMBL3577914 IC50 = 0.07 nM 520.52 COc1ncc(-c2ccc3nc(N)nc(-c4ccncc4)c3c2)cc1NS(=O)(=O)c1ccc(F)cc1F Homo sapiens CHEMBL3579761 single protein format
CHEMBL5422635 IC50 = 0.08 nM 597.61 COc1ncc(-c2ccc3ncc(-c4cn(CCN5CCOCC5)nn4)n3n2)cc1NS(=O)(=O)c1ccc(F)cc1F Homo sapiens CHEMBL5356226 single protein format
CHEMBL3577911 IC50 = 0.095 nM 505.51 COc1ncc(-c2ccc3ncnc(-c4ccncc4)c3c2)cc1NS(=O)(=O)c1ccc(F)cc1F Homo sapiens CHEMBL3579761 single protein format
CHEMBL3577908 IC50 = 0.1 nM 504.52 COc1ncc(-c2ccc3nccc(-c4ccncc4)c3c2)cc1NS(=O)(=O)c1ccc(F)cc1F Homo sapiens CHEMBL3579761 single protein format
CHEMBL5400439 IC50 = 0.11 nM 555.57 COc1ncc(-c2ccc3ncc(-c4cn(CCN(C)C)nn4)n3n2)cc1NS(=O)(=O)c1ccc(F)cc1F Homo sapiens CHEMBL5356226 single protein format
CHEMBL4878958 IC50 = 0.13 nM 567.65 COc1ncc2cc1NS(=O)(=O)c1ccc(F)c(c1)C(=O)NCc1ccc(s1)-c1ncnc3c(C)c-2sc13 Homo sapiens CHEMBL4845570 single protein format
CHEMBL3660111 IC50 = 0.14 nM 558.66 CCc1ncnc(N2CCN(S(C)(=O)=O)CC2)c1C#Cc1cnc(C)c(NS(=O)(=O)c2ccc(F)cc2)c1 Homo sapiens CHEMBL3705550 single protein format
CHEMBL3577927 IC50 = 0.15 nM 520.45 O=S(=O)(Nc1cc(-c2cc3c(-c4ccncc4)ncnc3s2)cnc1Cl)c1ccc(Cl)s1 Homo sapiens CHEMBL3579761 single protein format
CHEMBL5413309 IC50 = 0.16 nM 581.61 COc1ncc(-c2ccc3ncc(-c4cn(CCN5CCCC5)nn4)n3n2)cc1NS(=O)(=O)c1ccc(F)cc1F Homo sapiens CHEMBL5356226 single protein format
CHEMBL5401298 IC50 = 0.16 nM 593.65 COc1ncc(-c2ccc3ncc(-c4cn(CCCN5CCOCC5)nn4)n3n2)cc1NS(=O)(=O)c1ccc(F)cc1 Homo sapiens CHEMBL5356226 single protein format
CHEMBL1808977 IC50 = 0.2 nM 590.69 CN(C)CCN(C)C(=O)c1ccc(NC(=O)Nc2ccc(-c3nc(O[C@H]4CCOC4)nc(N4CCOCC4)n3)cc2)cc1 Homo sapiens CHEMBL1810228 cell-based format
CHEMBL3660114 IC50 = 0.2 nM 463.56 Cc1ncc(C#Cc2c(C)ncnc2N2CCOC[C@@H]2C)cc1NS(=O)(=O)c1ccccc1 Homo sapiens CHEMBL3705550 single protein format
CHEMBL4780201 IC50 = 0.2 nM 553.55 COc1ncc(-c2ccc3ncnc(Nc4cnn(CCO)c4)c3c2)cc1NS(=O)(=O)c1ccc(F)cc1F Homo sapiens CHEMBL4667358 single protein format
CHEMBL3577925 IC50 = 0.23 nM 515.95 O=S(=O)(Nc1cc(-c2cc3c(-c4ccncc4)ncnc3s2)cnc1Cl)c1ccc(F)cc1F Homo sapiens CHEMBL3579761 single protein format
CHEMBL4860369 IC50 = 0.23 nM 549.66 COc1ncc2cc1NS(=O)(=O)c1cccc(c1)C(=O)NCc1ccc(s1)-c1ncnc3c(C)c-2sc13 Homo sapiens CHEMBL4845570 single protein format
CHEMBL5431325 IC50 = 0.24 nM 564.57 COc1ncc(-c2ccc3ncc(C(=O)NCCc4ccccc4)n3n2)cc1NS(=O)(=O)c1ccc(F)cc1F Homo sapiens CHEMBL5356226 single protein format
CHEMBL3577913 IC50 = 0.27 nM 505.51 COc1ncc(-c2ccc3nncc(-c4ccncc4)c3c2)cc1NS(=O)(=O)c1ccc(F)cc1F Homo sapiens CHEMBL3579761 single protein format
CHEMBL3655894 IC50 = 0.28 nM 449.54 Cc1ncc(C#Cc2c(C)ncnc2N2CCOCC2)cc1NS(=O)(=O)c1ccccc1 Homo sapiens CHEMBL3705550 single protein format
CHEMBL3660127 IC50 = 0.3 nM 499.98 COc1ncc(C#Cc2c(C)ncnc2N2CCOCC2)cc1NS(=O)(=O)c1ccc(Cl)cc1 Homo sapiens CHEMBL3705550 single protein format