Protein Information

General Information of the Protein

Protein ID	PT01033
Protein Name	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform
Secondarily Protein Name	Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit beta Serine/threonine protein kinase PIK3CB
Gene Name	PIK3CB
Secondarily Gene Name	PIK3C1
Sequence	MCFSFIMPPAMADILDIWAVDSQIASDGSIPVDFLLPTGIYIQLEVPREATISYIKQMLWKQVHNYPMFNLLMDIDSYMFACVNQTAVYEELEDETRRLCDVRPFLPVLKLVTRSCDPGEKLDSKIGVLIGKGLHEFDSLKDPEVNEFRRKMRKFSEEKILSLVGLSWMDWLKQTYPPEHEPSIPENLEDKLYGGKLIVAVHFENCQDVFSFQVSPNMNPIKVNELAIQKRLTIHGKEDEVSPYDYVLQVSGRVEYVFGDHPLIQFQYIRNCVMNRALPHFILVECCKIKKMYEQEMIAIEAAINRNSSNLPLPLPPKKTRIISHVWENNNPFQIVLVKGNKLNTEETVKVHVRAGLFHGTELLCKTIVSSEVSGKNDHIWNEPLEFDINICDLPRMARLCFAVYAVLDKVKTKKSTKTINPSKYQTIRKAGKVHYPVAWVNTMVFDFKGQLRTGDIILHSWSSFPDELEEMLNPMGTVQTNPYTENATALHVKFPENKKQPYYYPPFDKIIEKAAEIASSDSANVSSRGGKKFLPVLKEILDRDPLSQLCENEMDLIWTLRQDCREIFPQSLPKLLLSIKWNKLEDVAQLQALLQIWPKLPPREALELLDFNYPDQYVREYAVGCLRQMSDEELSQYLLQLVQVLKYEPFLDCALSRFLLERALGNRRIGQFLFWHLRSEVHIPAVSVQFGVILEAYCRGSVGHMKVLSKQVEALNKLKTLNSLIKLNAVKLNRAKGKEAMHTCLKQSAYREALSDLQSPLNPCVILSELYVEKCKYMDSKMKPLWLVYNNKVFGEDSVGVIFKNGDDLRQDMLTLQMLRLMDLLWKEAGLDLRMLPYGCLATGDRSGLIEVVSTSETIADIQLNSSNVAAAAAFNKDALLNWLKEYNSGDDLDRAIEEFTLSCAGYCVASYVLGIGDRHSDNIMVKKTGQLFHIDFGHILGNFKSKFGIKRERVPFILTYDFIHVIQQGKTGNTEKFGRFRQCCEDAYLILRRHGNLFITLFALMLTAGLPELTSVKDIQYLKDSLALGKSEEEALKQFKQKFDEALRESWTTKVNWMAHTVRKDYRS Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Transferase
Function	Phosphoinositide-3-kinase (PI3K) phosphorylates phosphatidylinositol derivatives at position 3 of the inositol ring to produce 3-phosphoinositides (PubMed:15135396). Uses ATP and PtdIns(4,5)P2 (phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3) (PubMed:15135396). 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. Involved in the activation of AKT1 upon stimulation by G-protein coupled receptors (GPCRs) ligands such as CXCL12, sphingosine 1-phosphate, and lysophosphatidic acid. May also act downstream receptor tyrosine kinases. Required in different signaling pathways for stable platelet adhesion and aggregation. Plays a role in platelet activation signaling triggered by GPCRs, alpha-IIb/beta-3 integrins (ITGA2B/ ITGB3) and ITAM (immunoreceptor tyrosine-based activation motif)-bearing receptors such as GP6. Regulates the strength of adhesion of ITGA2B/ ITGB3 activated receptors necessary for the cellular transmission of contractile forces. Required for platelet aggregation induced by F2 (thrombin) and thromboxane A2 (TXA2). Has a role in cell survival. May have a role in cell migration. Involved in the early stage of autophagosome formation. Modulates the intracellular level of PtdIns3P (phosphatidylinositol 3-phosphate) and activates PIK3C3 kinase activity. May act as a scaffold, independently of its lipid kinase activity to positively regulate autophagy. May have a role in insulin signaling as scaffolding protein in which the lipid kinase activity is not required. May have a kinase-independent function in regulating cell proliferation and in clathrin-mediated endocytosis. Mediator of oncogenic signal in cell lines lacking PTEN. The lipid kinase activity is necessary for its role in oncogenic transformation. Required for the growth of ERBB2 and RAS driven tumors. Has also a protein kinase activity showing autophosphorylation (PubMed:12502714). Show/Hide
Uniprot ID	Primary ID: P42338 Secondarily ID: D3DNF0 Q24JU2 Show/Hide
Ensembl ID	ENSG00000051382
HGNC ID	HGNC:8976
Subcellular Location	Cytoplasm Nucleus

Map of Molecular Bioactivity Related to the Protein

Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity

Table of Molecular Bioactivities Related to the Protein

Cell Line ID: CL000144 , 3T3 MEFs WT

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0003061 Compound Info	9-(1-anilinoethyl)-7-methyl-2-morpholin-4-ylpyrido[1,2-a]pyrimidin-4-one Show/Hide	C21H24N4O2	1
1	IC50 = 11 nM Bioactivity Info	TI LI LO TS
CP0111428 Compound Info	2-[(1-methylbenzimidazol-2-yl)methyl]-4-morpholin-4-yl-1H-pyrimidin-6-one Show/Hide	C17H19N5O2	1
1	IC50 = 86 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000244 , 786-O

Cell Line Info

Cell Line ID: CL000023 , BTI-Tn-5B1-4

Cell Line Info

Cell Line ID: CL000481 , HCC1954

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000749 , HUVEC-C

Cell Line Info

Cell Line ID: CL000111 , MDA-MB-231

Cell Line Info

Cell Line ID: CL000196 , MDA-MB-468

Cell Line Info

Cell Line ID: CL000048 , PC-3

Cell Line Info

Cell Line ID: CL000019 , Rat1

Cell Line Info

Cell Line ID: CL000146 , S21

Cell Line Info

Cell Line ID: CL000012 , Sf21

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Cell Line ID: CL000366 , UACC-62

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0007933 Compound Info	2-(difluoromethyl)-1-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)-1H-benzimidazole Show/Hide	C19H21F2N7O2	5
1	EC50 = 44 nM
2	IC50 = 6 nM
3	IC50 = 15.2 nM
4	IC50 = 44 nM
5	IC50 = 58 nM
CP0126150 Compound Info	4-[(3-chloro-2-methylphenyl)methyl]-5-(hydroxymethyl)-2-morpholin-4-yl-[1,3]thiazolo[4,5-d]pyrimidin-7-one Show/Hide	C18H19ClN4O3S	1
1	IC50 = 0.1 nM
CP0179766 Compound Info	5-amino-4-[(3-chloro-2-methylphenyl)methyl]-2-morpholin-4-yl-[1,3]thiazolo[4,5-d]pyrimidin-7-one Show/Hide	C17H18ClN5O2S	1
1	IC50 = 0.2 nM
CP0140197 Compound Info	4-[(3-chloro-2-methylphenyl)methyl]-5-methoxy-2-morpholin-4-yl-[1,3]thiazolo[4,5-d]pyrimidin-7-one Show/Hide	C18H19ClN4O3S	1
1	IC50 = 0.3 nM
CP0067451 Compound Info	CHEMBL2322340 Show/Hide	C18H15Cl2F3N4O2	1
1	IC50 = 0.3981 nM
CP0142386 Compound Info	CHEMBL2322331 Show/Hide	C20H21F3N4O2	1
1	IC50 = 0.3981 nM
CP0267652 Compound Info	2-methylsulfanyl-3-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-5-morpholin-4-yl-[1,2,4]triazolo[1,5-a]pyrimidin-7-one Show/Hide	C19H20F3N5O2S	1
1	IC50 = 0.4 nM
CP0088734 Compound Info	4-[(3-chloro-2-methylphenyl)methyl]-5-methyl-2-morpholin-4-yl-[1,3]thiazolo[4,5-d]pyrimidin-7-one Show/Hide	C18H19ClN4O2S	1
1	IC50 = 0.5 nM
CP0126151 Compound Info	5-ethyl-4-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-2-morpholin-4-yl-[1,3]thiazolo[4,5-d]pyrimidin-7-one Show/Hide	C20H21F3N4O2S	1
1	IC50 = 0.5 nM
CP0140199 Compound Info	5-cyclopropyl-4-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-2-morpholin-4-yl-[1,3]thiazolo[4,5-d]pyrimidin-7-one Show/Hide	C21H21F3N4O2S	1
1	IC50 = 0.5 nM
CP0093019 Compound Info	2-methyl-3-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-5-morpholin-4-yl-[1,2,4]triazolo[1,5-a]pyrimidin-7-one Show/Hide	C19H20F3N5O2	1
1	IC50 = 0.6 nM
CP0165847 Compound Info	5-methyl-4-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-2-morpholin-4-yl-[1,3]thiazolo[4,5-d]pyrimidin-7-one Show/Hide	C19H19F3N4O2S	3
1	IC50 = 0.6 nM
2	IC50 = 0.631 nM
3	IC50 = 16 nM
CP0193724 Compound Info	CHEMBL2322338 Show/Hide	C20H16Cl2N4O	1
1	IC50 = 0.631 nM
CP0010347 Compound Info	GSK-2636771 Show/Hide	C22H22F3N3O3	2
1	IC50 = 0.89 nM
2	IC50 = 21.7 nM
CP0077449 Compound Info	2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-7-morpholin-4-ylimidazo[1,2-a]pyrimidin-5-one Show/Hide	C20H21F3N4O2	2
1	IC50 = 1 nM
2	IC50 = 1.3 nM
CP0202817 Compound Info	7-[(2R)-2-methylmorpholin-4-yl]-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]imidazo[1,2-a]pyrimidin-5-one Show/Hide	C20H21F3N4O2	1
1	IC50 = 1 nM
CP0153351 Compound Info	CHEMBL2322332 Show/Hide	C22H22N4O2	1
1	IC50 = 1 nM
CP0153354 Compound Info	CHEMBL2322344 Show/Hide	C19H14Cl2N4O2	1
1	IC50 = 1.259 nM
CP0160611 Compound Info	3-[(2,3-dichlorophenyl)methyl]-2-methyl-5-morpholin-4-yl-[1,2,4]triazolo[1,5-a]pyrimidin-7-one Show/Hide	C17H17Cl2N5O2	1
1	IC50 = 1.3 nM
CP0163638 Compound Info	2-cyclopropyl-3-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-5-morpholin-4-yl-[1,2,4]triazolo[1,5-a]pyrimidin-7-one Show/Hide	C21H22F3N5O2	1
1	IC50 = 1.3 nM
CP0101920 Compound Info	3-[(3-chloro-2-methylphenyl)methyl]-2-methyl-5-morpholin-4-ylimidazo[4,5-b]pyridine-7-carboxylic acid Show/Hide	C20H21ClN4O3	1
1	IC50 = 1.585 nM
CP0093016 Compound Info	3-[(2,3-dichlorophenyl)methyl]-2-methylsulfanyl-5-morpholin-4-yl-[1,2,4]triazolo[1,5-a]pyrimidin-7-one Show/Hide	C17H17Cl2N5O2S	1
1	IC50 = 1.6 nM
CP0126587 Compound Info	2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-7-morpholin-4-yl-[1,2,4]triazolo[1,5-c]pyrimidin-5-one Show/Hide	C19H20F3N5O2	1
1	IC50 = 2 nM
CP0302579 Compound Info	US8673906, 4.11 Show/Hide	C25H27F2N3O4	2
1	IC50 = 2 nM
2	IC50 = 8 nM
CP0126629 Compound Info	2-cyclopropyl-3-[(2,3-dichlorophenyl)methyl]-5-morpholin-4-yl-[1,2,4]triazolo[1,5-a]pyrimidin-7-one Show/Hide	C19H19Cl2N5O2	1
1	IC50 = 2.5 nM
CP0085472 Compound Info	CHEMBL2322337 Show/Hide	C20H15F3N4O	1
1	IC50 = 2.512 nM
CP0642162 Compound Info	3-(4-morpholin-4-yl-pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl)-phenol Show/Hide	C19H17ClN4O3	1
1	IC50 = 3 nM
CP0081482 Compound Info	1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-7-morpholin-4-ylimidazo[1,2-a]pyrimidin-5-one Show/Hide	C19H19F3N4O2	1
1	IC50 = 3 nM
CP0213155 Compound Info	US8673906, 4.09 Show/Hide	C27H29F2N3O5	2
1	IC50 = 3 nM
2	IC50 = 11 nM
CP0007893 Compound Info	4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpiperazin-1-yl)methyl]thieno[3,2-d]pyrimidin-4-yl]morpholine Show/Hide	C23H27N7O3S2	9
1	IC50 = 3 nM
2	IC50 = 31 nM
3	IC50 = 32 nM
4	IC50 = 33 nM
5	IC50 = 181 nM
6	IC50 = 251.19 nM
7	IC50 = 324 nM
8	Kd = 2.1 nM
9	Kd = 16 nM
CP0071769 Compound Info	2-(difluoromethyl)-1-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)benzimidazol-4-ol Show/Hide	C19H21F2N7O3	1
1	IC50 = 3.5 nM
CP0085474 Compound Info	CHEMBL2322333 Show/Hide	C21H22F3N3O2	1
1	IC50 = 3.981 nM
CP0014178 Compound Info	8-[(1R)-1-(3,5-difluoroanilino)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide Show/Hide	C24H25F2N3O4	1
1	IC50 = 4 nM
CP0089056 Compound Info	6-(azetidine-1-carbonyl)-8-[(1R)-1-(3,5-difluoroanilino)ethyl]-2-morpholin-4-ylchromen-4-one Show/Hide	C25H25F2N3O4	1
1	IC50 = 4 nM
CP0283808 Compound Info	8-[(1R)-1-(3,5-difluoroanilino)ethyl]-N,N-dimethyl-2-[(2S)-2-methylmorpholin-4-yl]-4-oxochromene-6-carboxamide Show/Hide	C25H27F2N3O4	1
1	IC50 = 4 nM
CP0086020 Compound Info	US8673906, 4.07 Show/Hide	C25H27F2N3O5	2
1	IC50 = 4 nM
2	IC50 = 10 nM
CP0086022 Compound Info	US8673906, 4.01 Show/Hide	C26H29F2N3O4	2
1	IC50 = 4 nM
2	IC50 = 10 nM
CP0091859 Compound Info	US8673906, 4.02 Show/Hide	C26H27F2N3O4	2
1	IC50 = 4 nM
2	IC50 = 9 nM
CP0177287 Compound Info	US8673906, 3.3 Show/Hide	C25H28FN3O5	2
1	IC50 = 4 nM
2	IC50 = 10 nM
CP0177291 Compound Info	US8673906, 4.15 Show/Hide	C25H27F2N3O5	2
1	IC50 = 4 nM
2	IC50 = 9 nM
CP0258575 Compound Info	US8673906, 3.09 Show/Hide	C24H26ClN3O4	2
1	IC50 = 4 nM
2	IC50 = 10 nM
CP0274584 Compound Info	US8673906, 3.1 Show/Hide	C24H25F2N3O4	2
1	IC50 = 4 nM
2	IC50 = 13 nM
CP0300738 Compound Info	US8673906, 4.24 Show/Hide	C26H29F2N3O5	2
1	IC50 = 4 nM
2	IC50 = 11 nM
CP0053978 Compound Info	9-[(1R)-1-(3,5-difluoroanilino)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidine-7-carboxamide Show/Hide	C23H25F2N5O3	1
1	IC50 = 5 nM
CP0086018 Compound Info	N,N-dimethyl-2-morpholin-4-yl-4-oxo-8-[(1R)-1-(3,4,5-trifluoroanilino)ethyl]chromene-6-carboxamide Show/Hide	C24H24F3N3O4	1
1	IC50 = 5 nM
CP0177288 Compound Info	8-[(1R)-1-(3-chloro-5-fluoroanilino)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide Show/Hide	C24H25ClFN3O4	1
1	IC50 = 5 nM
CP0258576 Compound Info	8-[(1R)-1-(3-chloro-2-fluoroanilino)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide Show/Hide	C24H25ClFN3O4	1
1	IC50 = 5 nM
CP0086019 Compound Info	US8673906, 3.33 Show/Hide	C24H25Cl2N3O4	2
1	IC50 = 5 nM
2	IC50 = 10 nM
CP0088830 Compound Info	US8673906, 4.1 Show/Hide	C27H29F2N3O4	2
1	IC50 = 5 nM
2	IC50 = 12 nM
CP0089057 Compound Info	US8673906, 4.17 Show/Hide	C24H25F2N3O4	2
1	IC50 = 5 nM
2	IC50 = 9 nM
CP0091860 Compound Info	US8673906, 2.07 Show/Hide	C26H27F2N3O5	2
1	IC50 = 5 nM
2	IC50 = 11 nM
CP0205068 Compound Info	US8673906, 6 Show/Hide	C27H29F2N3O4	2
1	IC50 = 5 nM
2	IC50 = 13 nM
CP0258577 Compound Info	US8673906, 3.16 Show/Hide	C25H28FN3O4	2
1	IC50 = 5 nM
2	IC50 = 15 nM
CP0085471 Compound Info	2-methyl-3-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-5-morpholin-4-ylpyrazolo[1,5-a]pyrimidine-7-carboxylic acid Show/Hide	C21H21F3N4O3	1
1	IC50 = 5.012 nM
CP0153352 Compound Info	CHEMBL2322336 Show/Hide	C19H19F3N4O2	1
1	IC50 = 5.012 nM
CP0073798 Compound Info	2-methyl-3-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-5-morpholin-4-ylimidazo[4,5-b]pyridine-7-carboxylic acid Show/Hide	C21H21F3N4O3	1
1	IC50 = 5.012 nM
CP0508638 Compound Info	3-[(2,3-dichlorophenyl)methyl]-2-methyl-5-morpholin-4-ylimidazo[4,5-b]pyridine-7-carboxylic acid Show/Hide	C19H18Cl2N4O3	1
1	IC50 = 5.012 nM
CP0177294 Compound Info	8-[(1R)-1-(3,5-difluoroanilino)ethyl]-N-methyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide Show/Hide	C23H23F2N3O4	1
1	IC50 = 6 nM
CP0302544 Compound Info	8-[(1R)-1-(3,5-difluoro-N-methylanilino)ethyl]-N-(2-hydroxyethyl)-N-methyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide Show/Hide	C26H29F2N3O5	1
1	IC50 = 6 nM
CP0227062 Compound Info	US8673906, 3.05 Show/Hide	C24H25ClFN3O4	2
1	IC50 = 6 nM
2	IC50 = 12 nM
CP0046476 Compound Info	8-[(6,8-difluoro-2,3-dihydro-1,4-benzoxazin-4-yl)methyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide Show/Hide	C25H25F2N3O5	2
1	IC50 = 6 nM
2	IC50 = 10 nM
CP0174499 Compound Info	8-[(6,8-difluoro-2,3-dihydro-1,4-benzoxazin-4-yl)methyl]-N,N-dimethyl-2-[(2R)-2-methylmorpholin-4-yl]-4-oxochromene-6-carboxamide Show/Hide	C26H27F2N3O5	2
1	IC50 = 6 nM
2	IC50 = 10 nM
CP0114229 Compound Info	9-[1-(3-chloro-2-fluoroanilino)ethyl]-N-[2-(dimethylamino)ethyl]-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidine-7-carboxamide Show/Hide	C25H30ClFN6O3	1
1	IC50 = 7 nM
CP0258835 Compound Info	9-[1-(3,4-difluoroanilino)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidine-7-carboxamide Show/Hide	C23H25F2N5O3	1
1	IC50 = 7 nM
CP0074912 Compound Info	8-[(3,5-difluoro-N-methylanilino)methyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide Show/Hide	C24H25F2N3O4	2
1	IC50 = 7 nM
2	IC50 = 10 nM
CP0086017 Compound Info	8-[(1R)-1-(3,4-difluoroanilino)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide Show/Hide	C24H25F2N3O4	1
1	IC50 = 7 nM
CP0086021 Compound Info	8-[(1R)-1-(3,5-difluoro-N-methylanilino)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide Show/Hide	C25H27F2N3O4	1
1	IC50 = 7 nM
CP0177292 Compound Info	8-[(1R)-1-(3,5-difluoro-N-methylanilino)ethyl]-6-(4-hydroxypiperidine-1-carbonyl)-2-morpholin-4-ylchromen-4-one Show/Hide	C28H31F2N3O5	1
1	IC50 = 7 nM
CP0177296 Compound Info	US8673906, 2.01 Show/Hide	C24H26FN3O4	2
1	IC50 = 7 nM
2	IC50 = 18 nM
CP0094801 Compound Info	8-[(6-fluoro-2,3-dihydro-1,4-benzoxazin-4-yl)methyl]-N,N-dimethyl-2-[(2R)-2-methylmorpholin-4-yl]-4-oxochromene-6-carboxamide Show/Hide	C26H28FN3O5	2
1	IC50 = 7 nM
2	IC50 = 10 nM
CP0094802 Compound Info	8-[(3,5-difluoro-N-methylanilino)methyl]-N,N-dimethyl-2-[(2R)-2-methylmorpholin-4-yl]-4-oxochromene-6-carboxamide Show/Hide	C25H27F2N3O4	2
1	IC50 = 7 nM
2	IC50 = 10 nM
CP0108529 Compound Info	8-[(8-fluoro-2,3-dihydro-1,4-benzoxazin-4-yl)methyl]-N,N-dimethyl-2-[(2R)-2-methylmorpholin-4-yl]-4-oxochromene-6-carboxamide Show/Hide	C26H28FN3O5	2
1	IC50 = 7 nM
2	IC50 = 10 nM
CP0142384 Compound Info	CHEMBL2322345 Show/Hide	C18H18Cl2N4O2	1
1	IC50 = 7.943 nM
CP0174459 Compound Info	4-[2-(4-chloro-2-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxylic acid Show/Hide	C19H20ClN3O4S	1
1	IC50 = 8 nM
CP0132804 Compound Info	9-(1-anilinoethyl)-N-[2-(dimethylamino)ethyl]-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidine-7-carboxamide Show/Hide	C25H32N6O3	2
1	IC50 = 8 nM
2	IC50 = 35 nM
CP0258574 Compound Info	8-[(3,5-difluoroanilino)methyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide Show/Hide	C23H23F2N3O4	1
1	IC50 = 8 nM
CP0283805 Compound Info	N,N-dimethyl-2-morpholin-4-yl-4-oxo-8-[(1R)-1-(2,3,5-trifluoroanilino)ethyl]chromene-6-carboxamide Show/Hide	C24H24F3N3O4	1
1	IC50 = 8 nM
CP0046475 Compound Info	8-[(8-fluoro-2,3-dihydro-1,4-benzoxazin-4-yl)methyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide Show/Hide	C25H26FN3O5	2
1	IC50 = 8 nM
2	IC50 = 10 nM
CP0089058 Compound Info	8-[(1S)-1-(3,5-difluoroanilino)ethyl]-N,N-dimethyl-2-[(2S)-2-methylmorpholin-4-yl]-4-oxochromene-6-carboxamide Show/Hide	C25H27F2N3O4	1
1	IC50 = 9 nM
CP0046478 Compound Info	8-[(6-fluoro-2,3-dihydro-1,4-benzoxazin-4-yl)methyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide Show/Hide	C25H26FN3O5	2
1	IC50 = 9 nM
2	IC50 = 10 nM
CP0174458 Compound Info	4-[2-(4-chloro-2-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxamide Show/Hide	C19H21ClN4O3S	1
1	IC50 = 10 nM
CP0094342 Compound Info	2-[[(1R)-1-(7-methyl-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidin-9-yl)ethyl]amino]benzoic acid Show/Hide	C22H24N4O4	2
1	IC50 = 10 nM
2	IC50 = 40 nM
CP0213052 Compound Info	US8673906, 3.15 Show/Hide	C24H25F2N3O4	2
1	IC50 = 10 nM
2	IC50 = 19 nM
CP0056280 Compound Info	4-[2-(4-bromo-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxylic acid Show/Hide	C18H18BrN3O4S	1
1	IC50 = 11 nM
CP0084826 Compound Info	4-[2-(4-bromo-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxamide Show/Hide	C18H19BrN4O3S	1
1	IC50 = 11 nM
CP0086623 Compound Info	9-(1-anilinoethyl)-N,N-dimethyl-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidine-7-carboxamide Show/Hide	C23H27N5O3	2
1	IC50 = 11 nM
2	IC50 = 68 nM
CP0182845 Compound Info	US8673906, 3.12 Show/Hide	C24H26FN3O4	1
1	IC50 = 12 nM
CP0298597 Compound Info	1-[(2,3-dichlorophenyl)methyl]-7-morpholin-4-ylimidazo[1,2-a]pyrimidin-5-one Show/Hide	C17H16Cl2N4O2	1
1	IC50 = 13 nM
CP0084833 Compound Info	4-[2-(5-fluoro-2-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxylic acid Show/Hide	C19H20FN3O4S	1
1	IC50 = 15 nM
CP0640938 Compound Info	3-(4-morpholinothieno[3,2-d]pyrimidin-2-yl)phenol Show/Hide	C16H16ClN3O2S	1
1	IC50 = 16 nM
CP0003676 Compound Info	N-hydroxy-2-[[2-(6-methoxypyridin-3-yl)-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl-methylamino]pyrimidine-5-carboxamide Show/Hide	C23H24N8O4S	3
1	IC50 = 16 nM
2	IC50 = 21 nM
3	IC50 = 54 nM
CP0177298 Compound Info	8-[(1R)-1-(3,5-difluorophenoxy)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide Show/Hide	C24H24F2N2O5	1
1	IC50 = 17 nM
CP0142382 Compound Info	[2-methyl-3-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-5-morpholin-4-ylpyrazolo[1,5-a]pyrimidin-7-yl]urea Show/Hide	C21H23F3N6O2	1
1	IC50 = 19.95 nM
CP0135450 Compound Info	4-[2-(5-fluoro-2-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxamide Show/Hide	C19H21FN4O3S	1
1	IC50 = 20 nM
CP0084825 Compound Info	4-[2-(5-fluoro-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxamide Show/Hide	C18H19FN4O3S	1
1	IC50 = 22 nM
CP0084830 Compound Info	4-[2-(4-chloro-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxylic acid Show/Hide	C18H18ClN3O4S	1
1	IC50 = 23 nM
CP0209381 Compound Info	4-[2-(5-fluoro-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxylic acid Show/Hide	C18H18FN3O4S	1
1	IC50 = 25 nM
CP0207212 Compound Info	2-methyl-3-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-5-morpholin-4-ylpyrazolo[1,5-a]pyrimidine-7-carboxamide Show/Hide	C21H22F3N5O2	1
1	IC50 = 25.12 nM
CP0071675 Compound Info	2-(difluoromethyl)-3-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)-7-methoxybenzimidazol-5-amine Show/Hide	C20H24F2N8O3	1
1	IC50 = 27 nM
CP0128743 Compound Info	(2S)-2-amino-1-[4-[4-[2-(difluoromethyl)benzimidazol-1-yl]-6-morpholin-4-yl-1,3,5-triazin-2-yl]piperazin-1-yl]propan-1-one Show/Hide	C22H27F2N9O2	2
1	IC50 = 31 nM
2	IC50 = 62 nM
CP0371471 Compound Info	9-[1-(4-fluoroanilino)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidine-7-carboxamide Show/Hide	C23H26FN5O3	1
1	IC50 = 37 nM
CP0153348 Compound Info	2-methyl-3-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-5-morpholin-4-ylpyrazolo[1,5-a]pyrimidin-7-amine Show/Hide	C20H22F3N5O	1
1	IC50 = 39.81 nM
CP0186648 Compound Info	2-(4-morpholin-4-yl-6-oxo-1H-pyrimidin-2-yl)-N-phenylacetamide Show/Hide	C16H18N4O3	1
1	IC50 = 42 nM
CP0071674 Compound Info	2-(difluoromethyl)-1-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)-5-methoxybenzimidazol-4-ol Show/Hide	C20H23F2N7O4	1
1	IC50 = 44 nM
CP0106231 Compound Info	4-[2-(4-chloro-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxamide Show/Hide	C18H19ClN4O3S	1
1	IC50 = 49 nM
CP0003061 Compound Info	9-(1-anilinoethyl)-7-methyl-2-morpholin-4-ylpyrido[1,2-a]pyrimidin-4-one Show/Hide	C21H24N4O2	3
1	IC50 = 49 nM
2	IC50 = 65 nM
3	IC50 = 2000 nM
CP0084873 Compound Info	8-(1-anilinoethyl)-6-methyl-2-morpholin-4-ylchromen-4-one Show/Hide	C22H24N2O3	1
1	IC50 = 57 nM
CP0087779 Compound Info	4-[1-(7-fluoro-3-methyl-2-pyridin-2-ylquinolin-4-yl)-3,3-dimethyl-2H-indol-6-yl]morpholine Show/Hide	C29H29FN4O	1
1	IC50 = 58 nM
CP0105849 Compound Info	(2S)-2-amino-1-[4-[4-[2-(difluoromethyl)benzimidazol-1-yl]-6-morpholin-4-yl-1,3,5-triazin-2-yl]piperazin-1-yl]-3-phenylpropan-1-one Show/Hide	C28H31F2N9O2	2
1	IC50 = 63 nM
2	IC50 = 74 nM
CP0157447 Compound Info	(2S,3S)-2-amino-1-[4-[4-[2-(difluoromethyl)benzimidazol-1-yl]-6-morpholin-4-yl-1,3,5-triazin-2-yl]piperazin-1-yl]-3-methylpentan-1-one Show/Hide	C25H33F2N9O2	2
1	IC50 = 67 nM
2	IC50 = 140 nM
CP0174462 Compound Info	4-[2-(2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxamide Show/Hide	C18H20N4O3S	1
1	IC50 = 71 nM
CP0176371 Compound Info	(2S)-1-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)-2-methylpyrrolidine-1,2-dicarboxamide Show/Hide	C20H26N6O2S	1
1	IC50 = 75 nM
CP0124222 Compound Info	(2S,3R)-3-methyl-1-N-[8-(1,1,1-trifluoro-2-methylpropan-2-yl)-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C20H23F3N6O2S	1
1	IC50 = 81 nM
CP0006058 Compound Info	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 Show/Hide	C30H24N8O2	1
1	IC50 = 82 nM
CP0688695 Compound Info	7-methyl-9-(2-methylbenzylamino)-2-morpholino-4H-pyrido[1,2-a]pyrimidin-4-one Show/Hide	C21H24N4O2	1
1	IC50 = 110 nM
CP0010760 Compound Info	5-fluoro-3-phenyl-2-[(1S)-1-(7H-purin-6-ylamino)propyl]quinazolin-4-one Show/Hide	C22H18FN7O	15
1	IC50 = 120.1 nM
2	IC50 = 129 nM
3	IC50 = 134 nM
4	IC50 = 139.1 nM
5	IC50 = 281 nM
6	IC50 = 380 nM
7	IC50 = 562 nM
8	IC50 = 565 nM
9	IC50 = 571 nM
10	IC50 = 669 nM
11	IC50 = 845.5 nM
12	IC50 = 1400 nM
13	IC50 = 1995.26 nM
14	IC50 = 4000 nM
15	IC50 > 500 nM
CP0221013 Compound Info	4-[2-(3-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxamide Show/Hide	C19H22N4O3S	1
1	IC50 = 130 nM
CP0056282 Compound Info	4-[2-(4-fluoro-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxamide Show/Hide	C18H19FN4O3S	1
1	IC50 = 138 nM
CP0056279 Compound Info	4-[2-(5-chloro-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxamide Show/Hide	C18H19ClN4O3S	1
1	IC50 = 166 nM
CP0084990 Compound Info	4-[2-(2-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxamide Show/Hide	C19H22N4O3S	1
1	IC50 = 178 nM
CP0008405 Compound Info	(2S)-1-N-[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C19H22F3N5O2S	2
1	IC50 = 190 nM
2	IC50 = 1200 nM
CP0055472 Compound Info	(2S)-1-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)pyrrolidine-1,2-dicarboxamide Show/Hide	C19H24N6O2S	1
1	IC50 = 220 nM
CP0174456 Compound Info	4-[2-(5-bromo-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxamide Show/Hide	C18H19BrN4O3S	1
1	IC50 = 240 nM
CP0176936 Compound Info	2,4-diamino-6-[[(1S)-1-[7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenylquinolizin-2-yl]ethyl]amino]pyrimidine-5-carbonitrile Show/Hide	C28H21F2N7O	1
1	IC50 = 241.6 nM
CP0002420 Compound Info	2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one Show/Hide	C19H17NO3	12
1	IC50 = 270 nM
2	IC50 = 306 nM
3	IC50 = 310 nM
4	IC50 = 340 nM
5	IC50 = 736 nM
6	IC50 = 900 nM
7	IC50 = 970 nM
8	IC50 = 980 nM
9	IC50 = 983 nM
10	IC50 = 3000 nM
11	IC50 = 13100 nM
12	IC50 = 16000 nM
CP0209379 Compound Info	4-[2-(2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxylic acid Show/Hide	C18H19N3O4S	1
1	IC50 = 270 nM
CP0099116 Compound Info	(1S,5R)-2-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)-2-azabicyclo[3.1.0]hexane-1,2-dicarboxamide Show/Hide	C20H24N6O2S	1
1	IC50 = 290 nM
CP0330198 Compound Info	US8653092, 68 Show/Hide	C24H29F3N6O3	1
1	IC50 = 300 nM
CP0419316 Compound Info	1-[(3S)-3-[6-(3,4-dimethoxyphenyl)quinazolin-4-yl]oxypyrrolidin-1-yl]ethanone Show/Hide	C22H23N3O4	1
1	IC50 = 304 nM
CP0084824 Compound Info	4-[2-(5-bromo-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxylic acid Show/Hide	C18H18BrN3O4S	1
1	IC50 = 308 nM
CP0144577 Compound Info	(2S,3R)-1-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)-3-methylpyrrolidine-1,2-dicarboxamide Show/Hide	C20H26N6O2S	1
1	IC50 = 320 nM
CP0056281 Compound Info	4-[2-(2-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-2-morpholin-4-yl-1,3-thiazole-5-carboxylic acid Show/Hide	C19H21N3O4S	1
1	IC50 = 340 nM
CP0140106 Compound Info	2-methoxy-5-[4-[(3S)-1-propanoylpyrrolidin-3-yl]oxyquinazolin-6-yl]pyridine-3-carbonitrile Show/Hide	C22H21N5O3	1
1	IC50 = 360 nM
CP0068001 Compound Info	US8653092, 67 Show/Hide	C21H25F3N6O2	2
1	IC50 = 363 nM
2	IC50 = 424 nM
CP0569111 Compound Info	5-chloro-3-(3-fluorophenyl)-2-[(2S,5S)-5-methyl-1-(7H-purin-6-yl)pyrrolidin-2-yl]quinazolin-4-one Show/Hide	C24H19ClFN7O	1
1	IC50 = 375 nM
CP0050326 Compound Info	2-(4-(2-(3-hydroxyphenylamino)-1H-benzo[d]imidazol-1-yl)-1,3,5-triazin-2-ylamino)acetonitrile Show/Hide	C18H14N8O	1
1	IC50 = 380 nM
CP0125424 Compound Info	1-[4-[5-[5-amino-6-(benzotriazol-1-yl)pyrazin-2-yl]-1-methylpyrazol-3-yl]piperidin-1-yl]-2-(dimethylamino)ethanone Show/Hide	C23H28N10O	1
1	IC50 = 380 nM
CP0674357 Compound Info	1-(4-(4-(5-amino-6-(1H-benzo[d][1,2,3]triazol-1-yl)pyrazin-2-yl)-2H-1,2,3-triazol-2-yl)piperidin-1-yl)-2-(dimethylamino)ethanone Show/Hide	C21H25N11O	1
1	IC50 = 650 nM
CP0214687 Compound Info	1-[(3S)-3-[6-(6-methoxypyridin-3-yl)quinolin-4-yl]oxypyrrolidin-1-yl]propan-1-one Show/Hide	C22H23N3O3	1
1	IC50 = 655 nM
CP0237222 Compound Info	1-[(3S)-3-[6-(6-methoxypyridin-3-yl)quinazolin-4-yl]oxypyrrolidin-1-yl]propan-1-one Show/Hide	C21H22N4O3	1
1	IC50 = 669 nM
CP0066777 Compound Info	(2S,3R)-3-methyl-1-N-[12-(1,1,1-trifluoro-2-methylpropan-2-yl)-8-oxa-3-thia-5,11-diazatricyclo[7.4.0.02,6]trideca-1(13),2(6),4,9,11-pentaen-4-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C20H22F3N5O3S	1
1	IC50 = 670 nM
CP0059183 Compound Info	(2S)-1-N-(7-tert-butyl-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl)-2-methylpyrrolidine-1,2-dicarboxamide Show/Hide	C19H25N5O2S2	1
1	IC50 = 720 nM
CP0215337 Compound Info	(2S,3S)-1-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)-3-[(dimethylamino)methyl]pyrrolidine-1,2-dicarboxamide Show/Hide	C22H31N7O2S	1
1	IC50 = 770 nM
CP0140107 Compound Info	1-[(3R)-3-[7-(3,4-dimethoxyphenyl)quinoxalin-2-yl]oxypyrrolidin-1-yl]propan-1-one Show/Hide	C23H25N3O4	1
1	IC50 = 860 nM
CP0072499 Compound Info	1-[4-[4-[5-amino-6-(benzotriazol-1-yl)pyrazin-2-yl]pyrazol-1-yl]piperidin-1-yl]-2-(dimethylamino)ethanone Show/Hide	C22H26N10O	1
1	IC50 = 900 nM
CP0120405 Compound Info	(2S,3R)-3-methyl-1-N-[7-(1,1,1-trifluoro-2-methylpropan-2-yl)-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C19H22F3N5O2S2	1
1	IC50 = 930 nM
CP0067930 Compound Info	US8653092, 81 Show/Hide	C21H28N6O2	1
1	IC50 = 951 nM
CP0085980 Compound Info	tert-butyl (3S)-3-[6-(3,4-dimethoxyphenyl)quinazolin-4-yl]oxypyrrolidine-1-carboxylate Show/Hide	C25H29N3O5	1
1	IC50 = 956 nM
CP0574226 Compound Info	1-[(3S)-3-[[6-(5,6-dimethoxypyridin-3-yl)thieno[2,3-d]pyrimidin-4-yl]amino]pyrrolidin-1-yl]propan-1-one Show/Hide	C20H23N5O3S	1
1	IC50 = 972.5 nM
CP0072498 Compound Info	1-[4-[5-[5-amino-6-(benzotriazol-1-yl)pyrazin-2-yl]-1-methyl-1,2,4-triazol-3-yl]piperidin-1-yl]-2-(dimethylamino)ethanone Show/Hide	C22H27N11O	1
1	IC50 = 1000 nM
CP0055473 Compound Info	(2S,4R)-1-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)-4-(dimethylamino)pyrrolidine-1,2-dicarboxamide Show/Hide	C21H29N7O2S	1
1	IC50 = 1000 nM
CP0140243 Compound Info	1-[(3S)-3-[[6-(6-methoxypyridin-3-yl)-1,5-naphthyridin-4-yl]oxy]pyrrolidin-1-yl]propan-1-one Show/Hide	C21H22N4O3	1
1	IC50 = 1030 nM
CP0078092 Compound Info	(2S,3R)-3-methyl-1-N-[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C20H24F3N5O2S	1
1	IC50 = 1040 nM
CP0107860 Compound Info	(2S)-1-N-[5-[2-(diethylamino)pyrimidin-4-yl]-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C18H25N7O2S	1
1	IC50 = 1200 nM
CP0116057 Compound Info	(2S)-1-N-[5-(2-tert-butylpyrimidin-4-yl)-4-methyl-1,3-thiazol-2-yl]azetidine-1,2-dicarboxamide Show/Hide	C17H22N6O2S	1
1	IC50 = 1200 nM
CP0249149 Compound Info	1-[4-[2-[5-amino-6-(benzotriazol-1-yl)pyrazin-2-yl]-1-methylimidazol-4-yl]piperidin-1-yl]-2-(dimethylamino)ethanone Show/Hide	C23H28N10O	1
1	IC50 = 1300 nM
CP0068002 Compound Info	US8653092, 61 Show/Hide	C24H28F3N5O4	1
1	IC50 = 1330 nM
CP0551744 Compound Info	cyclobutyl-[(3S)-3-[[6-(5,6-dimethoxypyridin-3-yl)thieno[2,3-d]pyrimidin-4-yl]amino]pyrrolidin-1-yl]methanone Show/Hide	C22H25N5O3S	1
1	IC50 = 1365.5 nM
CP0099117 Compound Info	(2R)-1-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)-2-[(dimethylamino)methyl]pyrrolidine-1,2-dicarboxamide Show/Hide	C22H31N7O2S	1
1	IC50 = 1400 nM
CP0140244 Compound Info	5-[4-[3-(4-acetylpiperazine-1-carbonyl)phenyl]quinazolin-6-yl]-2-methoxypyridine-3-carbonitrile Show/Hide	C28H24N6O3	1
1	IC50 = 1650 nM
CP0689001 Compound Info	1-(4-(3-(5-amino-6-(1H-benzo[d][1,2,3]triazol-1-yl)pyrazin-2-yl)-1H-pyrazol-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone Show/Hide	C22H26N10O	1
1	IC50 = 1700 nM
CP0066459 Compound Info	US8653092, 63 Show/Hide	C21H24F3N5O3	1
1	IC50 = 1710 nM
CP0057012 Compound Info	(2S)-1-N-[5-(2-cyclobutylpyrimidin-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C18H22N6O2S	1
1	IC50 = 1800 nM
CP0109038 Compound Info	(2S)-1-N-[5-(2-tert-butylpyrimidin-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C18H24N6O2S	3
1	IC50 = 1800 nM
2	IC50 = 1900 nM
3	IC50 = 2010 nM
CP0099118 Compound Info	(2S,3S)-1-N-(7-tert-butyl-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl)-3-methylpyrrolidine-1,2-dicarboxamide Show/Hide	C19H25N5O2S2	1
1	IC50 = 1800 nM
CP0345063 Compound Info	1-[4-[3-[6-(3,4-dimethoxyphenyl)quinazolin-4-yl]benzoyl]piperazin-1-yl]ethanone Show/Hide	C29H28N4O4	1
1	IC50 = 1940 nM
CP0543235 Compound Info	cyclobutyl-[(3S)-3-[6-(5,6-dimethoxypyridin-3-yl)thieno[2,3-d]pyrimidin-4-yl]oxypyrrolidin-1-yl]methanone Show/Hide	C22H24N4O4S	1
1	IC50 = 1962.5 nM
CP0303600 Compound Info	US8653092, 83 Show/Hide	C24H32N6O3	1
1	IC50 = 2020 nM
CP0674930 Compound Info	(2S)-N1-[4-methyl-5-[2-[2,2,2-trideuterio-1,1-bis(trideuteriomethyl)ethyl]pyrimidin-4-yl]thiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C18H24N6O2S	1
1	IC50 = 2070 nM
CP0095462 Compound Info	(2S,3R)-1-N-(7-tert-butyl-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl)-3-methylpyrrolidine-1,2-dicarboxamide Show/Hide	C19H25N5O2S2	1
1	IC50 = 2300 nM
CP0116954 Compound Info	1-[4-[5-[5-amino-6-(benzotriazol-1-yl)pyrazin-2-yl]-2-methyl-1,2,4-triazol-3-yl]piperidin-1-yl]-2-(dimethylamino)ethanone Show/Hide	C22H27N11O	1
1	IC50 = 2400 nM
CP0055470 Compound Info	(2S)-1-N-(7-tert-butyl-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl)pyrrolidine-1,2-dicarboxamide Show/Hide	C18H23N5O2S2	1
1	IC50 = 2500 nM
CP0053343 Compound Info	4-amino-6-[[(1S)-1-(6-fluoro-3,4-dipyridin-2-ylquinolin-2-yl)ethyl]amino]pyrimidine-5-carbonitrile Show/Hide	C26H19FN8	1
1	IC50 = 2800 nM
CP0102055 Compound Info	(2S)-1-N-[4-methyl-5-[2-(1-methylcyclopropyl)pyrimidin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C18H22N6O2S	1
1	IC50 = 3100 nM
CP0157490 Compound Info	(2S)-1-N-[5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C18H20F3N5O2S	1
1	IC50 = 3900 nM
CP0102057 Compound Info	(2S)-1-N-[4-methyl-5-(2-propan-2-ylpyrimidin-4-yl)-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C17H22N6O2S	1
1	IC50 = 4000 nM
CP0107861 Compound Info	(2S)-1-N-[5-[2-(1-cyanocyclopropyl)pyridin-4-yl]-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C19H20N6O2S	1
1	IC50 = 4100 nM
CP0043078 Compound Info	US8653092, 1 Show/Hide	C24H31N5O4	1
1	IC50 = 4150 nM
CP0107865 Compound Info	(2S)-1-N-[5-(2-tert-butylpyridin-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C19H25N5O2S	1
1	IC50 = 4400 nM
CP0176375 Compound Info	(1S,5R)-2-N-(7-tert-butyl-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl)-2-azabicyclo[3.1.0]hexane-1,2-dicarboxamide Show/Hide	C19H23N5O2S2	1
1	IC50 = 4500 nM
CP0131435 Compound Info	1-[4-[3-[6-(6-methoxypyridin-3-yl)quinazolin-4-yl]benzoyl]piperazin-1-yl]ethanone Show/Hide	C27H25N5O3	1
1	IC50 = 4840 nM
CP0107863 Compound Info	N-[5-(2-tert-butylpyridin-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1-carboxamide Show/Hide	C18H24N4OS	1
1	IC50 = 4900 nM
CP0124221 Compound Info	(2S)-1-N-[7-(cyclopropylmethyl)-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C18H21N5O2S2	1
1	IC50 = 5100 nM
CP0051959 Compound Info	(2S)-1-N-[4-chloro-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C18H19ClF3N5O2S	1
1	IC50 = 5500 nM
CP0055471 Compound Info	(2S,3S)-1-N-(7-tert-butyl-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl)-3-[(dimethylamino)methyl]pyrrolidine-1,2-dicarboxamide Show/Hide	C21H30N6O2S2	1
1	IC50 = 5500 nM
CP0054682 Compound Info	(2S)-1-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C17H23N5O2S2	1
1	IC50 = 6500 nM
CP0123998 Compound Info	6-[6-[3-(dimethylamino)propoxy]pyridin-3-yl]-4-[[(1S)-1-(oxan-4-yl)ethyl]amino]cinnoline-3-carboxamide Show/Hide	C26H34N6O3	1
1	IC50 = 8100 nM
CP0241717 Compound Info	1-[(3S)-3-[[6-(6-methoxypyridin-3-yl)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]oxy]pyrrolidin-1-yl]propan-1-one Show/Hide	C20H25N5O3	1
1	IC50 = 8940 nM
CP0231955 Compound Info	1-[(3S)-3-[6-(6-methoxypyridin-3-yl)cinnolin-4-yl]oxypyrrolidin-1-yl]propan-1-one Show/Hide	C21H22N4O3	1
1	IC50 = 9010 nM
CP0189386 Compound Info	6-[6-[3-(dimethylamino)propoxy]pyridin-3-yl]-N-methyl-4-[[(1S)-1-(oxan-4-yl)ethyl]amino]cinnoline-3-carboxamide Show/Hide	C27H36N6O3	1
1	IC50 = 10300 nM
CP0075331 Compound Info	4-[4-[4-(difluoromethoxy)-2-(difluoromethyl)benzimidazol-1-yl]-6-morpholin-4-yl-1,3,5-triazin-2-yl]morpholine Show/Hide	C20H21F4N7O3	1
1	IC50 > 2500 nM
CP0051973 Compound Info	(2S)-1-N-[5-(2-tert-butylpyridin-4-yl)-4-methyl-1,3-thiazol-2-yl]-2-N-methylpyrrolidine-1,2-dicarboxamide Show/Hide	C20H27N5O2S	1
1	IC50 > 9100 nM
CP0102054 Compound Info	(2S)-1-N-[4-methyl-5-(6-propan-2-ylpyrimidin-4-yl)-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C17H22N6O2S	1
1	IC50 > 9100 nM
CP0067931 Compound Info	1-[4-[3-[6-(6-methoxypyridin-3-yl)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]benzoyl]piperazin-1-yl]ethanone Show/Hide	C26H28N6O3	1
1	IC50 > 9100 nM
CP0249954 Compound Info	1-[4-[3-[6-(6-methoxypyridin-3-yl)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]phenoxy]piperidin-1-yl]ethanone Show/Hide	C26H29N5O3	1
1	IC50 > 9100 nM
CP0087784 Compound Info	4-[1-(7-fluoro-3-methyl-2-pyridin-2-ylquinolin-4-yl)-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-6-yl]pyrimidin-2-amine Show/Hide	C28H24FN7	1
1	Ki = 18 nM
CP0160603 Compound Info	4-[1-(7-fluoro-3-methyl-2-pyridin-2-ylquinolin-4-yl)-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-6-yl]morpholine Show/Hide	C28H28FN5O	1
1	Ki = 30 nM
CP0013647 Compound Info	1-(7-fluoro-3-methyl-2-pyridin-2-ylquinolin-4-yl)-6-morpholin-4-ylspiro[2H-pyrrolo[3,2-b]pyridine-3,4'-oxane] Show/Hide	C30H30FN5O2	1
1	Ki = 44 nM
CP0047685 Compound Info	(2S)-1-N-[4-methyl-5-(4-pyrazol-1-ylphenyl)-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide Show/Hide	C19H20N6O2S	1
1	Ki = 2000 nM

Clinical Information about the Protein

Target 1 ( PI3-kinase beta (PIK3CB) )

Target Type	Clinical trial Target
Disease	5 Target-related Diseases				5
1	Breast cancer [ICD-11: 2C60-2C65]
2	Solid tumour/cancer [ICD-11: 2A00-2F9Z]
3	Colorectal cancer [ICD-11: 2B91.Z]
4	Squamous head and neck cell carcinom [ICD-11: 2D60.0]
5	Thrombosis [ICD-11: DB61-GB90]
Clinical Trial Drug(s)	5 Clinical Trial Drugs				5
1	Buparlisib	Drug Info	Phase 3	Breast cancer
2	AZD8186	Drug Info	Phase 1	Solid tumour/cancer
3	GSK2636771	Drug Info	Phase 1	Solid tumour/cancer
4	PA-799	Drug Info	Phase 1/2	Colorectal cancer
5	PQR309	Drug Info	Phase 2	Squamous head and neck cell carcinom
Discontinued Drug(s)	1 Discontinued Drug				1
1	AZD6482	Drug Info	Terminated	Thrombosis

Target 2 ( PI3K p110 beta messenger RNA (PIK3CB mRNA) )

Target Type	Literature-reported Target

Similar Protein(s) and Bioactivity Statistics

90% Identity

Protein ID	Protein Name	Protein Organism
PT06232	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform	Rattus norvegicus, Rat	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han