General Information of the Protein
Protein ID
PT01045
Protein Name
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Secondarily
Protein Name
Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha
Phosphoinositide 3-kinase alpha
Phosphoinositide-3-kinase catalytic alpha polypeptide
Serine/threonine protein kinase PIK3CA
Gene Name
PIK3CA
Sequence
MPPRPSSGELWGIHLMPPRILVECLLPNGMIVTLECLREATLITIKHELFKEARKYPLHQLLQDESSYIFVSVTQEAEREEFFDETRRLCDLRLFQPFLKVIEPVGNREEKILNREIGFAIGMPVCEFDMVKDPEVQDFRRNILNVCKEAVDLRDLNSPHSRAMYVYPPNVESSPELPKHIYNKLDKGQIIVVIWVIVSPNNDKQKYTLKINHDCVPEQVIAEAIRKKTRSMLLSSEQLKLCVLEYQGKYILKVCGCDEYFLEKYPLSQYKYIRSCIMLGRMPNLMLMAKESLYSQLPMDCFTMPSYSRRISTATPYMNGETSTKSLWVINSALRIKILCATYVNVNIRDIDKIYVRTGIYHGGEPLCDNVNTQRVPCSNPRWNEWLNYDIYIPDLPRAARLCLSICSVKGRKGAKEEHCPLAWGNINLFDYTDTLVSGKMALNLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWFSSVVKFPDMSVIEEHANWSVSREAGFSYSHAGLSNRLARDNELRENDKEQLKAISTRDPLSEITEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQMYCLVKDWPPIKPEQAMELLDCNYPDPMVRGFAVRCLEKYLTDDKLSQYLIQLVQVLKYEQYLDNLLVRFLLKKALTNQRIGHFFFWHLKSEMHNKTVSQRFGLLLESYCRACGMYLKHLNRQVEAMEKLINLTDILKQEKKDETQKVQMKFLVEQMRRPDFMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLWLNWENPDIMSELLFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLSIGDCVGLIEVVRNSHTIMQIQCKGGLKGALQFNSHTLHQWLKDKNKGEIYDAAIDLFTRSCAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLDHKKKKFGYKRERVPFVLTQDFLIVISKGAQECTKTREFERFQEMCYKAYLAIRQHANLFINLFSMMLGSGMPELQSFDDIAYIRKTLALDKTEQEALEYFMKQMNDAHHGGWTTKMDWIFHTIKQHALN
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Transferase
Function
Phosphoinositide-3-kinase (PI3K) phosphorylates phosphatidylinositol (PI) and its phosphorylated derivatives at position 3 of the inositol ring to produce 3-phosphoinositides (PubMed:15135396, PubMed:23936502, PubMed:28676499). Uses ATP and PtdIns(4,5)P2 (phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3) (PubMed:15135396, PubMed:28676499). 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. Participates in cellular signaling in response to various growth factors. Involved in the activation of AKT1 upon stimulation by receptor tyrosine kinases ligands such as EGF, insulin, IGF1, VEGFA and PDGF. Involved in signaling via insulin-receptor substrate (IRS) proteins. Essential in endothelial cell migration during vascular development through VEGFA signaling, possibly by regulating RhoA activity. Required for lymphatic vasculature development, possibly by binding to RAS and by activation by EGF and FGF2, but not by PDGF. Regulates invadopodia formation through the PDPK1-AKT1 pathway. Participates in cardiomyogenesis in embryonic stem cells through a AKT1 pathway. Participates in vasculogenesis in embryonic stem cells through PDK1 and protein kinase C pathway. In addition to its lipid kinase activity, it displays a serine-protein kinase activity that results in the autophosphorylation of the p85alpha regulatory subunit as well as phosphorylation of other proteins such as 4EBP1, H-Ras, the IL-3 beta c receptor and possibly others (PubMed:23936502, PubMed:28676499). Plays a role in the positive regulation of phagocytosis and pinocytosis (By similarity).
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Uniprot ID
Primary ID:
P42336

Secondarily ID:
Q14CW1
Q99762
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Ensembl ID
ENSG00000121879
HGNC ID
HGNC:8975
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: CL000072 , A2780
Compound ID Compound Name Compound Formula
CP0355792
6-(2-aminopyrimidin-5-yl)-N-[6-(1-methylpiperidin-4-yl)oxypyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-amine
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C23H29N9O2
 1
1
EC50 = 10 nM
   TI
   LI
   LO
   TS
CP0067162
2-morpholino-N6-(quinolin-3-yl)-4,5'-bipyrimidine-2',6-diamine
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C21H20N8O
 1
1
EC50 = 40 nM
   TI
   LI
   LO
   TS
CP0066324
N-[6-[6-amino-5-(trifluoromethyl)pyridin-3-yl]imidazo[1,2-b]pyridazin-2-yl]acetamide
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C14H11F3N6O
 1
1
EC50 < 40 nM
   TI
   LI
   LO
   TS
CP0074362
N-[6-(5-amino-6-ethoxypyrazin-2-yl)imidazo[1,2-a]pyridin-2-yl]acetamide
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C15H16N6O2
 1
1
EC50 < 40 nM
   TI
   LI
   LO
   TS
CP0074363
N-[6-(6-amino-5-ethoxypyridin-3-yl)imidazo[1,2-b]pyridazin-2-yl]acetamide
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C15H16N6O2
 1
1
EC50 < 40 nM
   TI
   LI
   LO
   TS
CP0099482
N-[6-[5-amino-6-(1,1,1-trifluoropropan-2-yloxy)pyrazin-2-yl]imidazo[1,2-a]pyridin-2-yl]acetamide
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C16H15F3N6O2
 1
1
EC50 < 40 nM
   TI
   LI
   LO
   TS
CP0133918
N-[6-[5-amino-6-(2,2,2-trifluoroethoxy)pyrazin-2-yl]imidazo[1,2-a]pyridin-2-yl]acetamide
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C15H13F3N6O2
 1
1
EC50 < 40 nM
   TI
   LI
   LO
   TS
CP0403436
N-[6-(5-amino-6-propan-2-yloxypyrazin-2-yl)imidazo[1,2-a]pyridin-2-yl]acetamide
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C16H18N6O2
 1
1
EC50 < 40 nM
   TI
   LI
   LO
   TS
CP0067896
N-[6-(5-amino-6-methoxypyrazin-2-yl)imidazo[1,2-a]pyridin-2-yl]acetamide
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C14H14N6O2
 1
1
EC50 = 60 nM
   TI
   LI
   LO
   TS
CP0044152
N-[6-[6-amino-5-(trifluoromethyl)pyridin-3-yl]imidazo[1,2-a]pyridin-2-yl]acetamide
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C15H12F3N5O
 1
1
EC50 = 80 nM
   TI
   LI
   LO
   TS
CP0057731
6-(2-aminopyrimidin-5-yl)-N-(6-methoxypyridin-3-yl)-2-morpholin-4-ylpyrimidin-4-amine
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C18H20N8O2
 1
1
EC50 = 90 nM
   TI
   LI
   LO
   TS
CP0455105
N-[6-(6-amino-5-methoxypyridin-3-yl)imidazo[1,2-a]pyridin-2-yl]acetamide
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C15H15N5O2
 1
1
EC50 = 90 nM
   TI
   LI
   LO
   TS
CP0067148
2-morpholino-N6-(6-phenoxypyridin-3-yl)-4,5'-bipyrimidine-2',6-diamine
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C23H22N8O2
 1
1
EC50 = 110 nM
   TI
   LI
   LO
   TS
CP0267762
N-[6-[2-(methylamino)pyrimidin-5-yl]-2-morpholin-4-ylpyrimidin-4-yl]quinolin-3-amine
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C22H22N8O
 1
1
EC50 = 110 nM
   TI
   LI
   LO
   TS
CP0350954
N-[6-(6-amino-5-methoxypyridin-3-yl)imidazo[1,2-b]pyridazin-2-yl]acetamide
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C14H14N6O2
 1
1
EC50 = 110 nM
   TI
   LI
   LO
   TS
CP0014549
2-morpholino-4,5'-bipyrimidin-2'-amine
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C12H14N6O
 1
1
EC50 = 130 nM
   TI
   LI
   LO
   TS
CP0350953
N-[6-[6-amino-5-(2-methoxyethoxy)pyridin-3-yl]imidazo[1,2-b]pyridazin-2-yl]acetamide
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C16H18N6O3
 1
1
EC50 = 150 nM
   TI
   LI
   LO
   TS
CP0429707
N-[6-[5-amino-6-(2-methoxyethoxy)pyrazin-2-yl]imidazo[1,2-a]pyridin-2-yl]acetamide
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C16H18N6O3
 1
1
EC50 = 170 nM
   TI
   LI
   LO
   TS
CP0353573
2-morpholino-N6-(tetrahydro-2H-pyran-4-yl)-4,5'-bipyrimidine-2',6-diamine
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C17H23N7O2
 1
1
EC50 = 220 nM
   TI
   LI
   LO
   TS
CP0447635
N-[6-(6-amino-5-ethoxypyridin-3-yl)imidazo[1,2-a]pyridin-2-yl]acetamide
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C16H17N5O2
 1
1
EC50 = 270 nM
   TI
   LI
   LO
   TS
CP0355469
N-[6-(6-aminopyridin-3-yl)-2-morpholin-4-ylpyrimidin-4-yl]quinolin-3-amine
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C22H21N7O
 1
1
EC50 = 310 nM
   TI
   LI
   LO
   TS
CP0264752
3-(2-morpholino-6-(quinolin-3-ylamino)pyrimidin-4-yl)phenol
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C23H21N5O2
 1
1
EC50 = 370 nM
   TI
   LI
   LO
   TS
CP0287208
N-(2-morpholin-4-yl-6-pyrazin-2-ylpyrimidin-4-yl)quinolin-3-amine
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C21H19N7O
 1
1
EC50 = 390 nM
   TI
   LI
   LO
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CP0492328
N-(2-morpholin-4-yl-6-pyrimidin-5-ylpyrimidin-4-yl)quinolin-3-amine
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C21H19N7O
 1
1
EC50 = 450 nM
   TI
   LI
   LO
   TS
CP0492327
N-(2-morpholin-4-yl-6-pyridin-3-ylpyrimidin-4-yl)quinolin-3-amine
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C22H20N6O
 1
1
EC50 = 650 nM
   TI
   LI
   LO
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CP0322007
N-[6-(5-aminopyrazin-2-yl)-2-morpholin-4-ylpyrimidin-4-yl]quinolin-3-amine
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C21H20N8O
 1
1
EC50 = 3300 nM
   TI
   LI
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0007933
2-(difluoromethyl)-1-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)-1H-benzimidazole
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C19H21F2N7O2
 8
1 EC50 = 50 nM
2 IC50 = 5 nM
3 IC50 = 6 nM
4 IC50 = 8.9 nM
5 IC50 = 12 nM
6 IC50 = 16 nM
7 IC50 = 25 nM
8 IC50 = 26 nM
CP0017744
GSK2126458
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C25H17F2N5O3S
 9
1 IC50 = 0.04 nM
2 IC50 = 0.3 nM
3 IC50 = 0.34 nM
4 IC50 = 0.41 nM
5 IC50 = 0.55 nM
6 IC50 = 0.63 nM
7 IC50 = 1.02 nM
8 IC50 = 1.1 nM
9 Ki = 0.019 nM
CP0007893
4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpiperazin-1-yl)methyl]thieno[3,2-d]pyrimidin-4-yl]morpholine
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C23H27N7O3S2
 18
1 IC50 = 0.1 nM
2 IC50 = 3 nM
3 IC50 = 4.7 nM
4 IC50 = 6.5 nM
5 IC50 = 7 nM
6 IC50 = 33 nM
7 IC50 = 50.12 nM
8 IC50 = 251.19 nM
9 Kd = 0.76 nM
10 Kd = 0.86 nM
11 Kd = 1.1 nM
12 Kd = 1.2 nM
13 Kd = 1.5 nM
14 Kd = 1.7 nM
15 Kd = 3.7 nM
16 Kd = 4.1 nM
17 Kd = 4.5 nM
18 Kd = 7.1 nM
CP0071769
2-(difluoromethyl)-1-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)benzimidazol-4-ol
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C19H21F2N7O3
 3
1 IC50 = 0.12 nM
2 IC50 = 0.53 nM
3 IC50 = 0.83 nM
CP0108539
1-(4-{[4-(Dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea
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C32H41N9O4
 3
1 IC50 = 0.4 nM
2 IC50 = 6 nM
3 IC50 = 6.04 nM
CP0167775
6-(2-aminopyrimidin-5-yl)-8-morpholin-4-ylimidazo[1,2-a]pyrazine-2-carboxamide
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C15H16N8O2
 1
1 IC50 = 0.4 nM
CP0184421
2-[4-(2-chlorophenyl)-5-oxo-1H-1,2,4-triazol-3-yl]-4,5-dihydrothieno[3,2-d][1]benzoxepine-8-carboxamide
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C21H15ClN4O3S
 1
1 IC50 < 0.5 nM
CP0205588
2-[1-(2-chlorophenyl)tetrazol-5-yl]-4,5-dihydrothieno[3,2-d][1]benzoxepine-8-carboxamide
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C20H14ClN5O2S
 1
1 IC50 < 0.5 nM
CP0283411
2-[2-(2,4-difluorophenyl)-1,2,4-triazol-3-yl]-4,5-dihydrothieno[3,2-d][1]benzoxepine-8-carboxamide
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C21H14F2N4O2S
 1
1 IC50 < 0.5 nM
CP0333718
5-(2-chlorophenyl)-4-(4,5-dihydrothieno[3,2-d][1]benzoxepin-2-yl)-1,3-thiazol-2-amine
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C21H15ClN2OS2
 1
1 IC50 < 0.5 nM
CP0522710
2-[4-(2-chlorophenyl)-1,2,4-triazol-3-yl]-4,5-dihydrothieno[3,2-d][1]benzoxepine-8-carboxamide
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C21H15ClN4O2S
 1
1 IC50 < 0.5 nM
CP0558428
4-[5-(2,4-difluorophenyl)-2H-triazol-4-yl]-9-oxa-3-thia-14-azatricyclo[8.4.0.02,6]tetradeca-1(10),2(6),4,11,13-pentaene-12-carboxamide
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C20H13F2N5O2S
 1
1 IC50 < 0.5 nM
CP0085320
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
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C21H22N6O2S
 1
1 IC50 < 0.5 nM
CP0169553
6-(2-aminopyrimidin-5-yl)-N-[3-(dimethylamino)propyl]-8-morpholin-4-ylimidazo[1,2-a]pyrazine-2-carboxamide
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C20H27N9O2
 1
1 IC50 = 0.6 nM
CP0101176
2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide
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C24H28N8O2
 4
1 IC50 < 0.7 nM
2 Ki = 0.09 nM
3 Ki = 0.29 nM
4 Ki = 0.3 nM
CP0066248
N-[(E)-(5-cyanopyrazolo[1,5-a]pyridin-3-yl)methylideneamino]-N,2-dimethyl-5-nitrobenzenesulfonamide
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C17H14N6O4S
 1
1 IC50 = 0.9 nM
CP0154471
6-(2-aminopyrimidin-5-yl)-N-(2-methoxyethyl)-3-methyl-8-morpholin-4-ylimidazo[1,2-a]pyrazine-2-carboxamide
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C19H24N8O3
 5
1 IC50 = 0.9 nM
2 Ki = 1.9 nM
3 Ki = 2.3 nM
4 Ki = 2.4 nM
5 Ki = 3.1 nM
CP0071675
2-(difluoromethyl)-3-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)-7-methoxybenzimidazol-5-amine
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C20H24F2N8O3
 3
1 IC50 = 0.95 nM
2 IC50 = 1 nM
3 IC50 = 3.1 nM
CP0020505
(1R,3R,5S,9R,18S)-18-(methoxymethyl)-1,5-dimethyl-6,11,16-trioxo-13,17-dioxapentacyclo[10.6.1.0^{2,10}.0^{5,9}.0^{15,19}]nonadeca-2(10),12(19),14-trien-3-yl acetate
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C23H24O8
 6
1 IC50 = 1 nM
2 IC50 = 12 nM
3 IC50 = 13 nM
4 IC50 = 17.6 nM
5 IC50 >= 1000 nM
6 Kd = 5.4 nM
CP0205610
2-[4-(2-chlorophenyl)-1H-pyrazol-5-yl]-4,5-dihydrothieno[3,2-d][1]benzoxepine-8-carboxamide
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C22H16ClN3O2S
 1
1 IC50 = 1 nM
CP0085563
4-(2-chlorophenyl)-3-(4,5-dihydrothieno[3,2-d][1]benzoxepin-2-yl)-1H-1,2,4-triazol-5-one
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C20H14ClN3O2S
 1
1 IC50 = 1.2 nM
CP0487811
1-(2,4-difluorophenyl)-5-(4,5-dihydrothieno[3,2-d][1]benzoxepin-2-yl)-1,2,4-triazole
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C20H13F2N3OS
 1
1 IC50 = 1.2 nM
CP0011997
N-[(E)-(5-cyanopyrazolo[1,5-a]pyridin-3-yl)methylideneamino]-N-(2-hydroxyethyl)-2-methyl-5-nitrobenzenesulfonamide
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C18H16N6O5S
 1
1 IC50 = 1.3 nM
CP0095286
1-[4-(3-Ethyl-7-morpholin-4-yl-3H-[1,2,3]triazolo-[4,5-d]pyrimidin-5-yl)phenyl]-3-{4-[(4-methylpiperazin-1-yl)carbonyl]-phenyl}urea
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C29H34N10O3
 2
1 IC50 = 1.4 nM
2 IC50 = 2 nM
CP0278460
N-[4-(2-chlorophenyl)-5-(9-oxa-3-thia-14-azatricyclo[8.4.0.02,6]tetradeca-1(10),2(6),4,11,13-pentaen-4-yl)-1H-imidazol-2-yl]acetamide
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C22H17ClN4O2S
 1
1 IC50 < 1.4 nM
CP0184542
2-N-(2-chlorophenyl)-2-N-methyl-4,5-dihydrothieno[3,2-d][1]benzoxepine-2,8-dicarboxamide
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C21H17ClN2O3S
 2
1 IC50 = 1.5 nM
2 Ki = 1.2 nM
CP0013755
3-(4-morpholin-4-ylpyrido[2,3]furo[2,4-b]pyrimidin-2-yl)phenol
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C19H16N4O3
 30
1 IC50 = 1.76 nM
2 IC50 = 2 nM
3 IC50 = 3.22 nM
4 IC50 = 3.8 nM
5 IC50 = 3.9 nM
6 IC50 = 4 nM
7 IC50 = 4.4 nM
8 IC50 = 4.5 nM
9 IC50 = 5.8 nM
10 IC50 = 6 nM
11 IC50 = 6.1 nM
12 IC50 = 6.8 nM
13 IC50 = 7.5 nM
14 IC50 = 8 nM
15 IC50 = 8.7 nM
16 IC50 = 11 nM
17 IC50 = 12 nM
18 IC50 = 16.8 nM
19 IC50 = 17 nM
20 IC50 = 19.7 nM
21 IC50 = 75 nM
22 IC50 = 150 nM
23 IC50 = 5300 nM
24 Kd = 1.3 nM
25 Kd = 1.4 nM
26 Kd = 1.5 nM
27 Kd = 2.9 nM
28 Kd = 3 nM
29 Kd = 3.2 nM
30 Kd = 3.4 nM
CP0068590
(2R)-3-[6-[5-[(2-chloro-4-fluorophenyl)sulfonylamino]-6-methoxypyridin-3-yl]-4-oxoquinazolin-3-yl]-N,2-dimethylpropanamide
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C25H23ClFN5O5S
 1
1 IC50 = 1.8 nM
CP0057731
6-(2-aminopyrimidin-5-yl)-N-(6-methoxypyridin-3-yl)-2-morpholin-4-ylpyrimidin-4-amine
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C18H20N8O2
 1
1 IC50 < 2 nM
CP0067148
2-morpholino-N6-(6-phenoxypyridin-3-yl)-4,5'-bipyrimidine-2',6-diamine
   Show/Hide
C23H22N8O2
 1
1 IC50 < 2 nM
CP0067162
2-morpholino-N6-(quinolin-3-yl)-4,5'-bipyrimidine-2',6-diamine
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C21H20N8O
 1
1 IC50 < 2 nM
CP0355792
6-(2-aminopyrimidin-5-yl)-N-[6-(1-methylpiperidin-4-yl)oxypyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-amine
   Show/Hide
C23H29N9O2
 1
1 IC50 < 2 nM
CP0066324
N-[6-[6-amino-5-(trifluoromethyl)pyridin-3-yl]imidazo[1,2-b]pyridazin-2-yl]acetamide
   Show/Hide
C14H11F3N6O
 1
1 IC50 = 2 nM
CP0245774
3-(4-morpholin-4-ylthieno[3,2-d]pyrimidin-2-yl)phenol
   Show/Hide
C16H15N3O2S
 2
1 IC50 = 2 nM
2 IC50 = 41 nM
CP0403436
N-[6-(5-amino-6-propan-2-yloxypyrazin-2-yl)imidazo[1,2-a]pyridin-2-yl]acetamide
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C16H18N6O2
 1
1 IC50 = 2 nM
CP0169552
6-(2-aminopyrimidin-5-yl)-N-(2-methoxyethyl)-8-morpholin-4-ylimidazo[1,2-a]pyrazine-2-carboxamide
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C18H22N8O3
 1
1 IC50 = 2.7 nM
CP0075331
4-[4-[4-(difluoromethoxy)-2-(difluoromethyl)benzimidazol-1-yl]-6-morpholin-4-yl-1,3,5-triazin-2-yl]morpholine
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C20H21F4N7O3
 3
1 IC50 = 3 nM
2 IC50 = 4.7 nM
3 IC50 = 8.5 nM
CP0067896
N-[6-(5-amino-6-methoxypyrazin-2-yl)imidazo[1,2-a]pyridin-2-yl]acetamide
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C14H14N6O2
 1
1 IC50 = 3 nM
CP0074362
N-[6-(5-amino-6-ethoxypyrazin-2-yl)imidazo[1,2-a]pyridin-2-yl]acetamide
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C15H16N6O2
 1
1 IC50 = 3 nM
CP0099482
N-[6-[5-amino-6-(1,1,1-trifluoropropan-2-yloxy)pyrazin-2-yl]imidazo[1,2-a]pyridin-2-yl]acetamide
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C16H15F3N6O2
 1
1 IC50 = 3 nM
CP0133918
N-[6-[5-amino-6-(2,2,2-trifluoroethoxy)pyrazin-2-yl]imidazo[1,2-a]pyridin-2-yl]acetamide
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C15H13F3N6O2
 1
1 IC50 = 3 nM
CP0540714
2,4-difluoro-N-[2-methoxy-5-(4-oxopyrido[1,2-a]pyrimidin-7-yl)pyridin-3-yl]benzenesulfonamide
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C20H14F2N4O4S
 1
1 IC50 = 3.1 nM
CP0157210
6-(2-aminopyrimidin-5-yl)-N-(3-methoxypropyl)-8-morpholin-4-ylimidazo[1,2-a]pyrazine-2-carboxamide
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C19H24N8O3
 1
1 IC50 = 3.2 nM
CP0022562
N-[5-(3-chloro-4-oxopyrido[1,2-a]pyrimidin-7-yl)-2-methoxypyridin-3-yl]-2,4-difluorobenzenesulfonamide
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C20H13ClF2N4O4S
 1
1 IC50 = 3.4 nM
CP0044152
N-[6-[6-amino-5-(trifluoromethyl)pyridin-3-yl]imidazo[1,2-a]pyridin-2-yl]acetamide
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C15H12F3N5O
 4
1 IC50 = 3.6 nM
2 IC50 = 4 nM
3 IC50 = 5.9 nM
4 IC50 = 12 nM
CP0279244
2-[2-(2-methylpropyl)-1,2,4-triazol-3-yl]-4,5-dihydrothieno[3,2-d][1]benzoxepine-8-carboxamide
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C19H20N4O2S
 1
1 IC50 = 4 nM
CP0333717
2-(2-propan-2-yl-1,2,4-triazol-3-yl)-4,5-dihydrothieno[3,2-d][1]benzoxepine-8-carboxamide
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C18H18N4O2S
 1
1 IC50 = 4 nM
CP0465619
2-[2-(2-hydroxy-2-methylpropyl)-1,2,4-triazol-3-yl]-4,5-dihydrothieno[3,2-d][1]benzoxepine-8-carboxamide
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C19H20N4O3S
 1
1 IC50 = 4 nM
CP0055472
(2S)-1-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)pyrrolidine-1,2-dicarboxamide
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C19H24N6O2S
 1
1 IC50 = 4 nM
CP0055473
(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
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C21H29N7O2S
 1
1 IC50 = 4 nM
CP0154469
6-(2-aminopyrimidin-5-yl)-N-[2-(dimethylamino)ethyl]-8-morpholin-4-ylimidazo[1,2-a]pyrazine-2-carboxamide
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C19H25N9O2
 1
1 IC50 = 4.6 nM
CP0008405
(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
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C19H22F3N5O2S
 4
1 IC50 = 4.6 nM
2 IC50 = 5 nM
3 IC50 = 9.5 nM
4 IC50 = 17.8 nM
CP0066777
(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
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C20H22F3N5O3S
 1
1 IC50 = 5 nM
CP0124222
(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
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C20H23F3N6O2S
 1
1 IC50 = 5 nM
CP0176371
(2S)-1-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)-2-methylpyrrolidine-1,2-dicarboxamide
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C20H26N6O2S
 1
1 IC50 = 5 nM
CP0215337
(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
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C22H31N7O2S
 1
1 IC50 = 5 nM
CP0350954
N-[6-(6-amino-5-methoxypyridin-3-yl)imidazo[1,2-b]pyridazin-2-yl]acetamide
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C14H14N6O2
 1
1 IC50 = 5 nM
CP0125424
1-[4-[5-[5-amino-6-(benzotriazol-1-yl)pyrazin-2-yl]-1-methylpyrazol-3-yl]piperidin-1-yl]-2-(dimethylamino)ethanone
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C23H28N10O
 1
1 IC50 = 6 nM
CP0099116
(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
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C20H24N6O2S
 1
1 IC50 = 6 nM
CP0144577
(2S,3R)-1-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)-3-methylpyrrolidine-1,2-dicarboxamide
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C20H26N6O2S
 1
1 IC50 = 6 nM
CP0350953
N-[6-[6-amino-5-(2-methoxyethoxy)pyridin-3-yl]imidazo[1,2-b]pyridazin-2-yl]acetamide
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C16H18N6O3
 1
1 IC50 = 6 nM
CP0090916
6-(1H-indazol-4-yl)-1-methyl-4-(4-(methylsulfonyl)phenoxy)-1H-pyrazolo[3,4-b]pyridine
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C21H17N5O3S
 2
1 IC50 = 6.8 nM
2 IC50 = 7 nM
CP0065610
1-[4-[[2-(1H-indazol-4-yl)-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-6-methylhept-5-ene-1,4-dione
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C30H35N7O3S
 1
1 IC50 = 6.8 nM
CP0267762
N-[6-[2-(methylamino)pyrimidin-5-yl]-2-morpholin-4-ylpyrimidin-4-yl]quinolin-3-amine
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C22H22N8O
 1
1 IC50 = 7 nM
CP0214220
2-[2-(2,2,2-trifluoroethyl)-1,2,4-triazol-3-yl]-4,5-dihydrothieno[3,2-d][1]benzoxepine-8-carboxamide
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C17H13F3N4O2S
 1
1 IC50 = 7 nM
CP0232134
N-(2-chlorophenyl)-N-methyl-9-oxa-3-thia-14-azatricyclo[8.4.0.02,6]tetradeca-1(10),2(6),4,11,13-pentaene-4-carboxamide
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C19H15ClN2O2S
 1
1 IC50 = 7 nM
CP0109038
(2S)-1-N-[5-(2-tert-butylpyrimidin-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C18H24N6O2S
 3
1 IC50 = 7 nM
2 IC50 = 7.5 nM
3 IC50 = 20 nM
CP0145100
4-(2-chlorophenyl)-3-(4,5-dihydrothieno[3,2-d][1]benzoxepin-2-yl)-1,2,4-triazole
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C20H14ClN3OS
 1
1 IC50 = 7.3 nM
CP0492328
N-(2-morpholin-4-yl-6-pyrimidin-5-ylpyrimidin-4-yl)quinolin-3-amine
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C21H19N7O
 1
1 IC50 = 8 nM
CP0205608
2-(2-cyclobutyl-1,2,4-triazol-3-yl)-4,5-dihydrothieno[3,2-d][1]benzoxepine-8-carboxamide
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C19H18N4O2S
 1
1 IC50 = 8 nM
CP0059183
(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
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C19H25N5O2S2
 1
1 IC50 = 8 nM
CP0429707
N-[6-[5-amino-6-(2-methoxyethoxy)pyrazin-2-yl]imidazo[1,2-a]pyridin-2-yl]acetamide
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C16H18N6O3
 1
1 IC50 = 8 nM
CP0120405
(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
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C19H22F3N5O2S2
 1
1 IC50 = 9 nM
CP0176375
(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
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C19H23N5O2S2
 1
1 IC50 = 9 nM
CP0157490
(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
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C18H20F3N5O2S
 1
1 IC50 = 9.5 nM
CP0238435
CHEMBL2058168
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C21H26N8O3
 1
1 IC50 = 10 nM
CP0055471
(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
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C21H30N6O2S2
 1
1 IC50 = 10 nM
CP0074912
8-[(3,5-difluoro-N-methylanilino)methyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide
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C24H25F2N3O4
 2
1 IC50 = 10 nM
2 IC50 = 25 nM
CP0167773
6-(2-aminopyrimidin-5-yl)-8-morpholin-4-yl-N-(2-morpholin-4-ylethyl)imidazo[1,2-a]pyrazine-2-carboxamide
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C21H27N9O3
 1
1 IC50 = 10.4 nM
CP0095462
(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
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C19H25N5O2S2
 1
1 IC50 = 11 nM
CP0074363
N-[6-(6-amino-5-ethoxypyridin-3-yl)imidazo[1,2-b]pyridazin-2-yl]acetamide
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C15H16N6O2
 1
1 IC50 = 11 nM
CP0238436
6-(2-aminopyrimidin-5-yl)-5-chloro-N-(2-methoxyethyl)-8-morpholin-4-ylimidazo[1,2-a]pyrazine-2-carboxamide
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C18H21ClN8O3
 1
1 IC50 = 11.2 nM
CP0145099
4-[5-(2-chlorophenyl)-1,3-oxazol-4-yl]-9-oxa-3-thia-14-azatricyclo[8.4.0.02,6]tetradeca-1(10),2(6),4,11,13-pentaene
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C20H13ClN2O2S
 1
1 IC50 = 12 nM
CP0102055
(2S)-1-N-[4-methyl-5-[2-(1-methylcyclopropyl)pyrimidin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C18H22N6O2S
 1
1 IC50 = 12 nM
CP0283808
8-[(1R)-1-(3,5-difluoroanilino)ethyl]-N,N-dimethyl-2-[(2S)-2-methylmorpholin-4-yl]-4-oxochromene-6-carboxamide
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C25H27F2N3O4
 1
1 IC50 = 12 nM
CP0353573
2-morpholino-N6-(tetrahydro-2H-pyran-4-yl)-4,5'-bipyrimidine-2',6-diamine
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C17H23N7O2
 1
1 IC50 = 13 nM
CP0055470
(2S)-1-N-(7-tert-butyl-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl)pyrrolidine-1,2-dicarboxamide
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C18H23N5O2S2
 1
1 IC50 = 13 nM
CP0099118
(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
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C19H25N5O2S2
 1
1 IC50 = 13 nM
CP0455105
N-[6-(6-amino-5-methoxypyridin-3-yl)imidazo[1,2-a]pyridin-2-yl]acetamide
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C15H15N5O2
 1
1 IC50 = 13 nM
CP0001930
5-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine
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C18H21F3N6O2
 9
1 IC50 = 13 nM
2 IC50 = 20 nM
3 IC50 = 25 nM
4 IC50 = 30 nM
5 IC50 = 44 nM
6 IC50 = 45 nM
7 IC50 = 52 nM
8 IC50 = 52.48 nM
9 Ki = 20 nM
CP0167778
6-(2-aminopyrimidin-5-yl)-8-morpholin-4-yl-N-(oxan-4-yl)imidazo[1,2-a]pyrazine-2-carboxamide
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C20H24N8O3
 1
1 IC50 = 13.1 nM
CP0014549
2-morpholino-4,5'-bipyrimidin-2'-amine
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C12H14N6O
 1
1 IC50 = 14 nM
CP0107865
(2S)-1-N-[5-(2-tert-butylpyridin-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C19H25N5O2S
 1
1 IC50 = 14 nM
CP0099117
(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
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C22H31N7O2S
 1
1 IC50 = 14 nM
CP0184540
2-[2-(2-hydroxyethyl)-1,2,4-triazol-3-yl]-4,5-dihydrothieno[3,2-d][1]benzoxepine-8-carboxamide
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C17H16N4O3S
 1
1 IC50 = 15 nM
CP0054682
(2S)-1-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C17H23N5O2S2
 2
1 IC50 = 15 nM
2 IC50 = 32 nM
CP0038259
(3-(9-(1-(4-(3-(dimethylamino)propoxy)benzyl)piperidin-4-yl)-6-morpholino-9H-purin-2-yl)phenyl)methanol
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C33H43N7O3
 1
1 IC50 = 16 nM
CP0184539
N-(2-chlorophenyl)-N-methyl-4,5-dihydrothieno[3,2-d][1]benzoxepine-2-carboxamide
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C20H16ClNO2S
 4
1 IC50 = 16 nM
2 IC50 = 24 nM
3 Ki = 16 nM
4 Ki = 16.3 nM
CP0102057
(2S)-1-N-[4-methyl-5-(2-propan-2-ylpyrimidin-4-yl)-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C17H22N6O2S
 1
1 IC50 = 16 nM
CP0107860
(2S)-1-N-[5-[2-(diethylamino)pyrimidin-4-yl]-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C18H25N7O2S
 1
1 IC50 = 16 nM
CP0072499
1-[4-[4-[5-amino-6-(benzotriazol-1-yl)pyrazin-2-yl]pyrazol-1-yl]piperidin-1-yl]-2-(dimethylamino)ethanone
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C22H26N10O
 1
1 IC50 = 16 nM
CP0447635
N-[6-(6-amino-5-ethoxypyridin-3-yl)imidazo[1,2-a]pyridin-2-yl]acetamide
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C16H17N5O2
 1
1 IC50 = 16 nM
CP0006058
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
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C30H24N8O2
 1
1 IC50 = 17 nM
CP0177294
8-[(1R)-1-(3,5-difluoroanilino)ethyl]-N-methyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide
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C23H23F2N3O4
 1
1 IC50 = 18 nM
CP0107861
(2S)-1-N-[5-[2-(1-cyanocyclopropyl)pyridin-4-yl]-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C19H20N6O2S
 1
1 IC50 = 19 nM
CP0116057
(2S)-1-N-[5-(2-tert-butylpyrimidin-4-yl)-4-methyl-1,3-thiazol-2-yl]azetidine-1,2-dicarboxamide
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C17H22N6O2S
 1
1 IC50 = 19 nM
CP0078092
(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
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C20H24F3N5O2S
 1
1 IC50 = 19 nM
CP0057012
(2S)-1-N-[5-(2-cyclobutylpyrimidin-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C18H22N6O2S
 1
1 IC50 = 20 nM
CP0674357
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
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C21H25N11O
 1
1 IC50 = 21 nM
CP0674930
(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
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C18H24N6O2S
 1
1 IC50 = 22 nM
CP0177288
8-[(1R)-1-(3-chloro-5-fluoroanilino)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide
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C24H25ClFN3O4
 1
1 IC50 = 25 nM
CP0689001
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
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C22H26N10O
 1
1 IC50 = 27 nM
CP0258576
8-[(1R)-1-(3-chloro-2-fluoroanilino)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide
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C24H25ClFN3O4
 1
1 IC50 = 28 nM
CP0354016
(2S)-1-[[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]carbamoyl]pyrrolidine-2-carboxylic acid
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C19H21F3N4O3S
 1
1 IC50 = 28.6 nM
CP0089056
6-(azetidine-1-carbonyl)-8-[(1R)-1-(3,5-difluoroanilino)ethyl]-2-morpholin-4-ylchromen-4-one
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C25H25F2N3O4
 1
1 IC50 = 29 nM
CP0072498
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
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C22H27N11O
 1
1 IC50 = 29 nM
CP0142914
2-(4-(2-(3-hydroxyphenylamino)-1H-benzo[d]imidazol-1-yl)-6-methyl-1,3,5-triazin-2-ylamino)acetonitrile
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C19H16N8O
 1
1 IC50 = 32 nM
CP0009496
N-[3-(dimethylamino)propyl]-6-(1H-indazol-4-yl)-8-morpholin-4-ylimidazo[1,2-a]pyrazine-2-carboxamide
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C23H28N8O2
 1
1 IC50 = 35 nM
CP0014178
8-[(1R)-1-(3,5-difluoroanilino)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide
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C24H25F2N3O4
 1
1 IC50 = 35 nM
CP0300568
4-[2-(1H-indazol-4-yl)thieno[3,2-d]pyrimidin-4-yl]morpholine
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C17H15N5OS
 1
1 IC50 = 36 nM
CP0051959
(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 = 39 nM
CP0330198
US8653092, 68
   Show/Hide
C24H29F3N6O3
 2
1 IC50 = 43 nM
2 IC50 = 44 nM
CP0322007
N-[6-(5-aminopyrazin-2-yl)-2-morpholin-4-ylpyrimidin-4-yl]quinolin-3-amine
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C21H20N8O
 1
1 IC50 = 44 nM
CP0071674
2-(difluoromethyl)-1-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)-5-methoxybenzimidazol-4-ol
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C20H23F2N7O4
 3
1 IC50 = 49 nM
2 IC50 = 70 nM
3 IC50 = 158 nM
CP0094320
(S)-2-(3-((1H-indol-3-yl)methyl)morpholino)-5,5-dimethyl-5,6-dihydrobenzo[d]thiazol-7(4H)-one
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C22H25N3O2S
 1
1 IC50 = 51 nM
CP0145096
N-(2,4-difluorophenyl)-N-methyl-4,5-dihydrothieno[3,2-d][1]benzoxepine-2-carboxamide
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C20H15F2NO2S
 1
1 IC50 = 52 nM
CP0355469
N-[6-(6-aminopyridin-3-yl)-2-morpholin-4-ylpyrimidin-4-yl]quinolin-3-amine
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C22H21N7O
 2
1 IC50 = 55 nM
2 IC50 = 110 nM
CP0177291
US8673906, 4.15
   Show/Hide
C25H27F2N3O5
 1
1 IC50 = 57 nM
CP0094325
(S)-2-(3-((1H-indol-3-yl)methyl)morpholino)-7,7-dimethyl-5,6,7,8-tetrahydrothiazolo[5,4-c]azepin-4-one
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C22H26N4O2S
 1
1 IC50 = 59 nM
CP0089057
US8673906, 4.17
   Show/Hide
C24H25F2N3O4
 1
1 IC50 = 59 nM
CP0264752
3-(2-morpholino-6-(quinolin-3-ylamino)pyrimidin-4-yl)phenol
   Show/Hide
C23H21N5O2
 1
1 IC50 = 61 nM
CP0249149
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 = 64 nM
CP0124221
(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 = 70 nM
CP0053978
9-[(1R)-1-(3,5-difluoroanilino)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidine-7-carboxamide
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C23H25F2N5O3
 1
1 IC50 = 75 nM
CP0068001
US8653092, 67
   Show/Hide
C21H25F3N6O2
 3
1 IC50 = 75.5 nM
2 IC50 = 244 nM
3 IC50 = 262 nM
CP0258575
US8673906, 3.09
   Show/Hide
C24H26ClN3O4
 1
1 IC50 = 85 nM
CP0086020
US8673906, 4.07
   Show/Hide
C25H27F2N3O5
 1
1 IC50 = 90 nM
CP0114229
9-[1-(3-chloro-2-fluoroanilino)ethyl]-N-[2-(dimethylamino)ethyl]-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidine-7-carboxamide
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C25H30ClFN6O3
 1
1 IC50 = 92 nM
CP0258574
8-[(3,5-difluoroanilino)methyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide
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C23H23F2N3O4
 1
1 IC50 = 93 nM
CP0091859
US8673906, 4.02
   Show/Hide
C26H27F2N3O4
 1
1 IC50 = 98 nM
CP0265356
(4aS,7R,12cS)-10,11-Dihydroxy-4,4,7,12c-tetramethyl-2,3,4,4a,5,6,7,12c-octahydro-1H-8-oxa-dibenzo[a,h]azulene-9-carbaldehyde
   Show/Hide
C22H28O4
 1
1 IC50 = 100 nM
CP0086018
N,N-dimethyl-2-morpholin-4-yl-4-oxo-8-[(1R)-1-(3,4,5-trifluoroanilino)ethyl]chromene-6-carboxamide
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C24H24F3N3O4
 1
1 IC50 = 110 nM
CP0086019
US8673906, 3.33
   Show/Hide
C24H25Cl2N3O4
 1
1 IC50 = 110 nM
CP0302579
US8673906, 4.11
   Show/Hide
C25H27F2N3O4
 1
1 IC50 = 110 nM
CP0419316
1-[(3S)-3-[6-(3,4-dimethoxyphenyl)quinazolin-4-yl]oxypyrrolidin-1-yl]ethanone
   Show/Hide
C22H23N3O4
 1
1 IC50 = 126 nM
CP0345063
1-[4-[3-[6-(3,4-dimethoxyphenyl)quinazolin-4-yl]benzoyl]piperazin-1-yl]ethanone
   Show/Hide
C29H28N4O4
 1
1 IC50 = 127 nM
CP0089058
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 = 130 nM
CP0258577
US8673906, 3.16
   Show/Hide
C25H28FN3O4
 1
1 IC50 = 130 nM
CP0492327
N-(2-morpholin-4-yl-6-pyridin-3-ylpyrimidin-4-yl)quinolin-3-amine
   Show/Hide
C22H20N6O
 1
1 IC50 = 135 nM
CP0283805
N,N-dimethyl-2-morpholin-4-yl-4-oxo-8-[(1R)-1-(2,3,5-trifluoroanilino)ethyl]chromene-6-carboxamide
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C24H24F3N3O4
 1
1 IC50 = 140 nM
CP0085980
tert-butyl (3S)-3-[6-(3,4-dimethoxyphenyl)quinazolin-4-yl]oxypyrrolidine-1-carboxylate
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C25H29N3O5
 1
1 IC50 = 148 nM
CP0086022
US8673906, 4.01
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C26H29F2N3O4
 1
1 IC50 = 150 nM
CP0177287
US8673906, 3.3
   Show/Hide
C25H28FN3O5
 1
1 IC50 = 160 nM
CP0086017
8-[(1R)-1-(3,4-difluoroanilino)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide
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C24H25F2N3O4
 1
1 IC50 = 170 nM
CP0227062
US8673906, 3.05
   Show/Hide
C24H25ClFN3O4
 1
1 IC50 = 170 nM
CP0010760
5-fluoro-3-phenyl-2-[(1S)-1-(7H-purin-6-ylamino)propyl]quinazolin-4-one
   Show/Hide
C22H18FN7O
 13
1 IC50 = 177.2 nM
2 IC50 = 306.4 nM
3 IC50 = 391.3 nM
4 IC50 = 467 nM
5 IC50 = 583 nM
6 IC50 = 737 nM
7 IC50 = 800 nM
8 IC50 = 820 nM
9 IC50 = 822 nM
10 IC50 = 1650 nM
11 IC50 = 9700 nM
12 IC50 = 10000 nM
13 IC50 > 500 nM
CP0302544
8-[(1R)-1-(3,5-difluoro-N-methylanilino)ethyl]-N-(2-hydroxyethyl)-N-methyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide
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C26H29F2N3O5
 1
1 IC50 = 180 nM
CP0002420
2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
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C19H17NO3
 15
1 IC50 = 200 nM
2 IC50 = 300 nM
3 IC50 = 356 nM
4 IC50 = 480 nM
5 IC50 = 481 nM
6 IC50 = 500 nM
7 IC50 = 550 nM
8 IC50 = 600 nM
9 IC50 = 630 nM
10 IC50 = 720 nM
11 IC50 = 730 nM
12 IC50 = 2300 nM
13 IC50 = 4000 nM
14 IC50 = 6180 nM
15 IC50 = 62800 nM
CP0088830
US8673906, 4.1
   Show/Hide
C27H29F2N3O4
 1
1 IC50 = 200 nM
CP0237222
1-[(3S)-3-[6-(6-methoxypyridin-3-yl)quinazolin-4-yl]oxypyrrolidin-1-yl]propan-1-one
   Show/Hide
C21H22N4O3
 1
1 IC50 = 218 nM
CP0182845
US8673906, 3.12
   Show/Hide
C24H26FN3O4
 1
1 IC50 = 220 nM
CP0214687
1-[(3S)-3-[6-(6-methoxypyridin-3-yl)quinolin-4-yl]oxypyrrolidin-1-yl]propan-1-one
   Show/Hide
C22H23N3O3
 1
1 IC50 = 220 nM
CP0213155
US8673906, 4.09
   Show/Hide
C27H29F2N3O5
 1
1 IC50 = 230 nM
CP0287208
N-(2-morpholin-4-yl-6-pyrazin-2-ylpyrimidin-4-yl)quinolin-3-amine
   Show/Hide
C21H19N7O
 1
1 IC50 = 231 nM
CP0140244
5-[4-[3-(4-acetylpiperazine-1-carbonyl)phenyl]quinazolin-6-yl]-2-methoxypyridine-3-carbonitrile
   Show/Hide
C28H24N6O3
 1
1 IC50 = 262 nM
CP0066459
US8653092, 63
   Show/Hide
C21H24F3N5O3
 3
1 IC50 = 262 nM
2 IC50 = 791 nM
3 IC50 = 792 nM
CP0086021
8-[(1R)-1-(3,5-difluoro-N-methylanilino)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide
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C25H27F2N3O4
 1
1 IC50 = 280 nM
CP0116954
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 = 280 nM
CP0300738
US8673906, 4.24
   Show/Hide
C26H29F2N3O5
 1
1 IC50 = 290 nM
CP0091860
US8673906, 2.07
   Show/Hide
C26H27F2N3O5
 1
1 IC50 = 300 nM
CP0050326
2-(4-(2-(3-hydroxyphenylamino)-1H-benzo[d]imidazol-1-yl)-1,3,5-triazin-2-ylamino)acetonitrile
   Show/Hide
C18H14N8O
 1
1 IC50 = 320 nM
CP0102054
(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 = 320 nM
CP0258835
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 = 340 nM
CP0132804
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 = 370 nM
2 IC50 = 2300 nM
CP0177292
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 = 370 nM
CP0274584
US8673906, 3.1
   Show/Hide
C24H25F2N3O4
 1
1 IC50 = 370 nM
CP0303600
US8653092, 83
   Show/Hide
C24H32N6O3
 2
1 IC50 = 373 nM
2 IC50 = 432 nM
CP0140106
2-methoxy-5-[4-[(3S)-1-propanoylpyrrolidin-3-yl]oxyquinazolin-6-yl]pyridine-3-carbonitrile
   Show/Hide
C22H21N5O3
 1
1 IC50 = 386 nM
CP0131435
1-[4-[3-[6-(6-methoxypyridin-3-yl)quinazolin-4-yl]benzoyl]piperazin-1-yl]ethanone
   Show/Hide
C27H25N5O3
 1
1 IC50 = 418 nM
CP0140243
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 = 424 nM
CP0180777
7-fluoro-6-[6-(methoxymethyl)pyridin-3-yl]-4-[[(1S)-1-(1-methylpyrazol-3-yl)ethyl]amino]quinoline-3-carboxamide
   Show/Hide
C23H23FN6O2
 1
1 IC50 = 445 nM
CP0213052
US8673906, 3.15
   Show/Hide
C24H25F2N3O4
 1
1 IC50 = 450 nM
CP0140107
1-[(3R)-3-[7-(3,4-dimethoxyphenyl)quinoxalin-2-yl]oxypyrrolidin-1-yl]propan-1-one
   Show/Hide
C23H25N3O4
 1
1 IC50 = 491 nM
CP0205068
US8673906, 6
   Show/Hide
C27H29F2N3O4
 1
1 IC50 = 510 nM
CP0086623
9-(1-anilinoethyl)-N,N-dimethyl-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidine-7-carboxamide
   Show/Hide
C23H27N5O3
 2
1 IC50 = 560 nM
2 IC50 = 2500 nM
CP0068002
US8653092, 61
   Show/Hide
C24H28F3N5O4
 2
1 IC50 = 589 nM
2 IC50 = 590 nM
CP0107863
N-[5-(2-tert-butylpyridin-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1-carboxamide
   Show/Hide
C18H24N4OS
 1
1 IC50 = 620 nM
CP0067930
US8653092, 81
   Show/Hide
C21H28N6O2
 1
1 IC50 = 651 nM
CP0177296
US8673906, 2.01
   Show/Hide
C24H26FN3O4
 1
1 IC50 = 810 nM
CP0177298
8-[(1R)-1-(3,5-difluorophenoxy)ethyl]-N,N-dimethyl-2-morpholin-4-yl-4-oxochromene-6-carboxamide
   Show/Hide
C24H24F2N2O5
 1
1 IC50 = 970 nM
CP0094318
2-morpholin-4-yl-5,6-dihydro-4H-benzothiazol-7-one
   Show/Hide
C13H18N2O2S
 2
1 IC50 = 975 nM
2 IC50 = 1333 nM
CP0688695
7-methyl-9-(2-methylbenzylamino)-2-morpholino-4H-pyrido[1,2-a]pyrimidin-4-one
   Show/Hide
C21H24N4O2
 1
1 IC50 = 1100 nM
CP0371471
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 = 1300 nM
CP0043078
US8653092, 1
   Show/Hide
C24H31N5O4
 3
1 IC50 = 1940 nM
2 IC50 = 2037.8 nM
3 IC50 = 2038 nM
CP0249954
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 = 2020 nM
CP0180776
6-[6-(methoxymethyl)pyridin-3-yl]-4-[[(1S)-1-(oxan-4-yl)ethyl]amino]quinoline-3-carboxamide
   Show/Hide
C24H28N4O3
 1
1 IC50 = 2110 nM
CP0186648
2-(4-morpholin-4-yl-6-oxo-1H-pyrimidin-2-yl)-N-phenylacetamide
   Show/Hide
C16H18N4O3
 1
1 IC50 = 2138 nM
CP0123998
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 = 2200 nM
CP0084873
8-(1-anilinoethyl)-6-methyl-2-morpholin-4-ylchromen-4-one
   Show/Hide
C22H24N2O3
 1
1 IC50 = 2600 nM
CP0051973
(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 = 2700 nM
CP0128743
(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 = 3500 nM
2 IC50 = 8200 nM
CP0189386
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 = 3800 nM
CP0569111
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 = 4425 nM
CP0105849
(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 = 4700 nM
2 IC50 = 12000 nM
CP0231955
1-[(3S)-3-[6-(6-methoxypyridin-3-yl)cinnolin-4-yl]oxypyrrolidin-1-yl]propan-1-one
   Show/Hide
C21H22N4O3
 1
1 IC50 = 5080 nM
CP0003061
9-(1-anilinoethyl)-7-methyl-2-morpholin-4-ylpyrido[1,2-a]pyrimidin-4-one
   Show/Hide
C21H24N4O2
 2
1 IC50 = 5800 nM
2 IC50 > 1000 nM
CP0157447
(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 = 6300 nM
2 IC50 = 9200 nM
CP0241717
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 = 6660 nM
CP0067931
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 = 6940 nM
CP0053343
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 = 7900 nM
CP0068243
(3R)-4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]-3-methylmorpholine
   Show/Hide
C21H24N4O3S
 1
1 IC50 = 13000 nM
CP0003452
1-(4-(4-Propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one
   Show/Hide
C35H28F3N5O2
 1
1 Kd = 23 nM
CP0543864
(S)-2-((2-((S)-4-(difluoromethyl)- 2-oxooxazolidin-3-yl)-5,6- dihydrobenzo[f]imidazo[1,2- d][1,4]oxazepin-9- yl)amino)propanamide
   Show/Hide
C18H19F2N5O4
 1
1 Ki = 0.034 nM
CP0579285
(S)-2-cyclopropyl-2-((2-((S)-4- (fluoromethyl)-2-oxooxazolidin-3- yl)-5,6- dihydrobenzo[f]imidazo[1,2- d][1,4]oxazepin-9- yl)amino)acetamide
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C20H22FN5O4
 1
1 Ki = 0.051 nM
CP0567669
(S)-2-cyclopropyl-2-((2-((S)-4- (difluoromethyl)-2-oxooxazolidin- 3-yl)-5,6- dihydrobenzo[f]imidazo[1,2- d][1,4]oxazepin-9- yl)amino)acetamide
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C20H21F2N5O4
 1
1 Ki = 0.06 nM
CP0576041
(2S)-2-[[2-[5-(hydroxymethyl)-2-(2,2,2-trifluoroethyl)-1,2,4-triazol-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]oxy]propanamide
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C19H19F3N6O4
 1
1 Ki = 0.062 nM
CP0579284
(2S)-2-[[2-[(4S)-2-oxo-4-(trifluoromethyl)-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]propanamide
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C18H18F3N5O4
 1
1 Ki = 0.095 nM
CP0569719
(2S)-2-cyclopropyl-2-[[2-[(4S)-2-oxo-4-(trifluoromethyl)-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]acetamide
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C20H20F3N5O4
 1
1 Ki = 0.1 nM
CP0579283
(2S)-2-[[2-(5-amino-2-propan-2-yl-1,2,4-triazol-3-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]oxy]propanamide
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C19H23N7O3
 1
1 Ki = 0.107 nM
CP0209641
2-[3-[4-[2-(5-methyl-2-propan-2-yl-1,2,4-triazol-3-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]pyrazol-1-yl]azetidin-1-yl]ethanol
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C25H30N8O2
 1
1 Ki = 0.11 nM
CP0199042
2-methyl-1-[4-[2-(2-propan-2-yl-1,2,4-triazol-3-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]pyrazol-1-yl]propan-2-ol
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C23H27N7O2
 1
1 Ki = 0.14 nM
CP0550609
(2S)-1-[2-[(4S)-2-oxo-4-(trifluoromethyl)-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]pyrrolidine-2-carboxamide
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C20H20F3N5O4
 1
1 Ki = 0.15 nM
CP0580037
(2S)-2-[[2-[(4S)-2-oxo-4-(trifluoromethyl)-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]butanamide
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C19H20F3N5O4
 1
1 Ki = 0.157 nM
CP0057541
2-[4-[2-(2-propan-2-yl-1,2,4-triazol-3-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]pyrazol-1-yl]ethanol
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C21H23N7O2
 1
1 Ki = 0.17 nM
CP0212773
(2S)-2-[[2-(2-propan-2-yl-1,2,4-triazol-3-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]oxy]propanamide
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C19H22N6O3
 2
1 Ki = 0.2 nM
2 Ki = 0.346 nM
CP0199043
2-(5-methyl-2-propan-2-yl-1,2,4-triazol-3-yl)-9-(1-methylpyrazol-4-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine
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C21H23N7O
 1
1 Ki = 0.29 nM
CP0195833
4-amino-2,6-dimethyl-N-(1H-pyrrolo[2,3-b]pyridin-5-yl)quinazoline-8-carboxamide
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C18H16N6O
 1
1 Ki = 0.3 nM
CP0363073
2-(5-methyl-2-propan-2-yl-1,2,4-triazol-3-yl)-9-[1-(2-morpholin-4-ylethyl)pyrazol-4-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine
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C26H32N8O2
 1
1 Ki = 0.3 nM
CP0339746
(2S)-2-hydroxy-1-[3-[4-[2-(5-methyl-2-propan-2-yl-1,2,4-triazol-3-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]pyrazol-1-yl]azetidin-1-yl]propan-1-one
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C26H30N8O3
 1
1 Ki = 0.34 nM
CP0576522
(2S)-1-[2-[(3S)-3-hydroxy-2-oxopyrrolidin-1-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]pyrrolidine-2-carboxamide
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C20H23N5O4
 1
1 Ki = 0.355 nM
CP0085319
2-[4-[2-(5-methyl-2-propan-2-yl-1,2,4-triazol-3-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]pyrazol-1-yl]ethanol
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C22H25N7O2
 1
1 Ki = 0.4 nM
CP0054466
4-amino-2-methyl-N-(6-methylpyridin-3-yl)quinazoline-8-carboxamide
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C16H15N5O
 1
1 Ki = 0.5 nM
CP0282725
4-amino-2,6-dimethyl-N-(6-methylpyridin-3-yl)quinazoline-8-carboxamide
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C17H17N5O
 1
1 Ki = 0.5 nM
CP0578777
(2S)-3-methyl-2-[[2-[(4S)-2-oxo-4-(trifluoromethyl)-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]butanamide
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C20H22F3N5O4
 1
1 Ki = 0.692 nM
CP0057540
2-[4-[2-[2-(2,2,2-trifluoroethyl)-1,2,4-triazol-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]pyrazol-1-yl]ethanol
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C20H18F3N7O2
 1
1 Ki < 1 nM
CP0198652
5-[6-(2-methoxypropan-2-yl)-4-morpholin-4-ylthieno[3,2-d]pyrimidin-2-yl]pyrimidin-2-amine
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C18H22N6O2S
 1
1 Ki = 1 nM
CP0199338
N-[6-[6-chloro-5-[(4-fluorophenyl)sulfonylamino]pyridin-3-yl]-1,3-benzothiazol-2-yl]acetamide
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C20H14ClFN4O3S2
 1
1 Ki = 1.2 nM
CP0015891
5-[5-chloro-2-[(4-methylsulfonylpiperazin-1-yl)methyl]-8-morpholin-4-ylimidazo[1,2-a]pyrazin-6-yl]pyrimidin-2-amine
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C20H26ClN9O3S
 3
1 Ki = 1.73 nM
2 Ki = 2.77 nM
3 Ki = 3.07 nM
CP0002073
5-[2-[(4-methylsulfonylpiperazin-1-yl)methyl]-8-morpholin-4-ylimidazo[1,2-a]pyrazin-6-yl]pyrimidin-2-amine
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C20H27N9O3S
 3
1 Ki = 1.77 nM
2 Ki = 1.89 nM
3 Ki = 2.33 nM
CP0057249
2-amino-4-[5-chloro-2-[[6-chloro-5-(dimethylsulfamoylamino)pyridin-3-yl]amino]pyridin-3-yl]-6-methyl-1,3,5-triazine
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C16H17Cl2N9O2S
 1
1 Ki = 2 nM
CP0330594
4-[2-[(6-methoxypyridin-3-yl)amino]-5-[(4-methylsulfonylphenyl)methyl]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C23H23N7O3S
 1
1 Ki = 2 nM
CP0371423
N-[5-[[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-5-(oxan-4-yl)pyridin-2-yl]amino]-2-chloropyridin-3-yl]methanesulfonamide
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C20H23ClN8O3S
 1
1 Ki = 2 nM
CP0204864
5-[6-(3-methoxyoxetan-3-yl)-7-methyl-4-morpholin-4-ylthieno[3,2-d]pyrimidin-2-yl]pyrimidin-2-amine
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C19H22N6O3S
 1
1 Ki = 2 nM
CP0292752
N-[5-[[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-5-(morpholin-4-ylmethyl)pyridin-2-yl]amino]-2-chloropyridin-3-yl]methanesulfonamide
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C20H24ClN9O3S
 1
1 Ki = 4 nM
CP0054465
4-amino-2,6-dimethyl-N-(1H-pyrazol-4-yl)quinazoline-8-carboxamide
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C14H14N6O
 1
1 Ki = 5 nM
CP0047685
(2S)-1-N-[4-methyl-5-(4-pyrazol-1-ylphenyl)-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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C19H20N6O2S
 1
1 Ki = 5 nM
CP0172054
4-[5-(3,6-dihydro-2H-pyran-4-yl)-2-[(6-methoxypyridin-3-yl)amino]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C20H21N7O2
 1
1 Ki = 5 nM
CP0279598
N-[5-[[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-5-(2-methoxyethoxy)pyridin-2-yl]amino]-2-chloropyridin-3-yl]methanesulfonamide
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C18H21ClN8O4S
 1
1 Ki = 5 nM
CP0395569
N-[5-[[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)pyridin-2-yl]amino]-2-chloropyridin-3-yl]-4-fluorobenzenesulfonamide
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C20H16ClFN8O2S
 1
1 Ki = 5 nM
CP0295372
N-[5-(2-amino-1,3-benzothiazol-6-yl)-2-chloropyridin-3-yl]-4-fluorobenzenesulfonamide
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C18H12ClFN4O2S2
 1
1 Ki = 5.6 nM
CP0252600
3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-N-(1H-indazol-4-yl)imidazo[1,2-a]pyridin-2-amine
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C18H15N9
 1
1 Ki = 5.6 nM
CP0750882
3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-N-(5-fluoro-6-methoxypyridin-3-yl)-6-(piperazin-1-yl)imidazo[1,2-a]pyridin-2-amine
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C21H23FN10O
 1
1 Ki = 5.7 nM
CP0174697
N-[5-[[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)pyridin-2-yl]amino]-2-chloropyridin-3-yl]cyclopropanesulfonamide
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C17H17ClN8O2S
 1
1 Ki = 6 nM
CP0688569
4-(3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-2-(5-fluoro-6-methoxypyridin-3-ylamino)imidazo[1,2-a]pyridin-6-yl)-N,N-dimethylpiperazine-1-carboxamide
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C24H28FN11O2
 1
1 Ki = 6.1 nM
CP0750883
3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-N-(5-fluoro-6-methoxypyridin-3-yl)-6-(4-(2-methoxyethyl)piperazin-1-yl)imidazo[1,2-a]pyridin-2-amine
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C24H29FN10O2
 1
1 Ki = 6.3 nM
CP0765233
3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-N-(5-fluoro-6-methoxypyridin-3-yl)-6-(4-isopropylpiperazin-1-yl)imidazo[1,2-a]pyridin-2-amine
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C24H29FN10O
 1
1 Ki = 6.5 nM
CP0195835
4-amino-2,6-dimethyl-N-(1H-pyrazol-5-yl)quinazoline-8-carboxamide
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C14H14N6O
 1
1 Ki = 7 nM
CP0131208
N-[5-[[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-5-methoxypyridin-2-yl]amino]-2-chloropyridin-3-yl]methanesulfonamide
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C16H17ClN8O3S
 1
1 Ki = 7 nM
CP0191321
4-[2-[(6-methoxypyridin-3-yl)amino]-5-(6-methylpyridin-3-yl)pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C21H20N8O
 1
1 Ki = 8 nM
CP0192152
4-[2-[(6-methoxypyridin-3-yl)amino]-5-(1-methylpyrazol-4-yl)pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C19H19N9O
 1
1 Ki = 8 nM
CP0717560
4-(3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-2-(6-methoxypyridin-3-ylamino)imidazo[1,2-a]pyridin-6-yl)-N,N-dimethylpiperazine-1-carboxamide
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C24H29N11O2
 1
1 Ki = 8.3 nM
CP0009370
4-[2-[(6-methoxypyridin-3-yl)amino]-5-[(4-methylsulfonylpiperazin-1-yl)methyl]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C21H27N9O3S
 1
1 Ki = 9 nM
CP0087634
4-[2-[(6-methoxypyridin-3-yl)amino]-5-[(1-methylsulfonylpiperidin-4-yl)methyl]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C22H28N8O3S
 1
1 Ki = 9 nM
CP0093388
N-[5-[[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-5-chloropyridin-2-yl]amino]-2-methoxypyridin-3-yl]methanesulfonamide
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C16H17ClN8O3S
 1
1 Ki = 10 nM
CP0072230
2-[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-2-[(5-fluoro-6-methoxypyridin-3-yl)amino]imidazo[1,2-a]pyridin-6-yl]propan-2-ol
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C20H21FN8O2
 1
1 Ki = 11 nM
CP0330470
N-[5-[[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-5-methoxypyridin-2-yl]amino]-2-chloropyridin-3-yl]morpholine-4-sulfonamide
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C19H22ClN9O4S
 1
1 Ki = 11 nM
CP0191632
N-[5-(1,3-benzothiazol-6-yl)-2-chloropyridin-3-yl]-4-fluorobenzenesulfonamide
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C18H11ClFN3O2S2
 1
1 Ki = 13 nM
CP0284307
3-[[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)pyridin-2-yl]amino]phenol
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C15H14N6O
 1
1 Ki = 13 nM
CP0252602
3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-N-(5-fluoro-6-methoxypyridin-3-yl)imidazo[1,2-a]pyridin-2-amine
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C17H15FN8O
 1
1 Ki = 14 nM
CP0093391
N-[5-[[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)pyridin-2-yl]amino]-2-chloropyridin-3-yl]morpholine-4-sulfonamide
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C18H20ClN9O3S
 1
1 Ki = 14 nM
CP0218104
2-amino-4-[2-[[6-chloro-5-(dimethylsulfamoylamino)pyridin-3-yl]amino]-5-methoxypyridin-3-yl]-6-methyl-1,3,5-triazine
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C17H20ClN9O3S
 1
1 Ki = 14 nM
CP0087633
4-[2-[(6-methoxypyridin-3-yl)amino]-5-[(3-methylsulfonylpyrrolidin-1-yl)methyl]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C21H26N8O3S
 1
1 Ki = 16 nM
CP0174686
4-[[5-(4-amino-6-methyl-1,3,5-triazin-2-yl)-6-[(6-methoxypyridin-3-yl)amino]pyridin-3-yl]methyl]-N,N-dimethylpiperazine-1-sulfonamide
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C22H30N10O3S
 1
1 Ki = 17 nM
CP0076062
4-[4-[(6-methoxypyridin-3-yl)amino]pyrimidin-5-yl]-6-methyl-1,3,5-triazin-2-amine
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C14H14N8O
 1
1 Ki = 18 nM
CP0338291
4-[2-[(6-methoxypyridin-3-yl)amino]-5-[(4-methylsulfonylpiperidin-1-yl)methyl]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C22H28N8O3S
 1
1 Ki = 22 nM
CP0087590
3-[[3-(6-amino-2-methylpyrimidin-4-yl)pyridin-2-yl]amino]phenol
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C16H15N5O
 1
1 Ki = 24 nM
CP0711390
2-(3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-2-(6-methoxypyridin-3-ylamino)imidazo[1,2-a]pyridin-6-yl)propan-2-ol
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C20H22N8O2
 1
1 Ki = 26 nM
CP0177940
3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-N-(6-methoxypyridin-3-yl)imidazo[1,2-a]pyridin-2-amine
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C17H16N8O
 1
1 Ki = 29 nM
CP0143583
N-[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)pyridin-2-yl]-1H-indazol-4-amine
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C16H14N8
 1
1 Ki = 33 nM
CP0282689
N-[3-(2-methyl-7H-purin-6-yl)pyridin-2-yl]-1H-indazol-4-amine
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C18H14N8
 1
1 Ki = 36 nM
CP0649593
N-(3-(4-amino-6-methyl-1,3,5-triazin-2-yl)imidazo[1,2-a]pyridin-2-yl)quinolin-7-amine
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C20H16N8
 1
1 Ki = 43 nM
CP0731810
3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-N-(6-methoxypyridin-3-yl)-6-(piperazin-1-yl)imidazo[1,2-a]pyridin-2-amine
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C21H24N10O
 1
1 Ki = 43 nM
CP0499598
2-amino-4-[2-[[6-chloro-5-[[methyl(propan-2-yl)sulfamoyl]amino]pyridin-3-yl]amino]pyridin-3-yl]-6-methyl-1,3,5-triazine
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C18H22ClN9O2S
 1
1 Ki = 44 nM
CP0218935
N-[6-(2-methylsulfanylpyrimidin-4-yl)-1,3-benzothiazol-2-yl]acetamide
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C14H12N4OS2
 1
1 Ki = 53 nM
CP0192153
4-[5-methoxy-2-[(6-methoxypyridin-3-yl)amino]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C16H17N7O2
 1
1 Ki = 55 nM
CP0139562
6-[3-[(6-methoxypyridin-3-yl)amino]pyrazin-2-yl]-2-methylpyrimidin-4-amine
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C15H15N7O
 1
1 Ki = 59 nM
CP0192150
4-[2-[(6-methoxypyridin-3-yl)amino]-5-(piperazin-1-ylmethyl)pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C20H25N9O
 1
1 Ki = 61 nM
CP0188464
N-(6-methoxypyridin-3-yl)-3-(2-methyl-7H-purin-6-yl)pyridin-2-amine
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C17H15N7O
 1
1 Ki = 62 nM
CP0172047
[5-(4-amino-6-methyl-1,3,5-triazin-2-yl)-6-[(6-methoxypyridin-3-yl)amino]pyridin-3-yl]methanol
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C16H17N7O2
 1
1 Ki = 63 nM
CP0282688
4-[5-benzyl-2-[(6-methoxypyridin-3-yl)amino]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C22H21N7O
 1
1 Ki = 65 nM
CP0369237
4-[5-chloro-2-[(6-methoxypyridin-3-yl)amino]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C15H14ClN7O
 1
1 Ki = 70 nM
CP0284209
N-[5-[[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-5-chloropyridin-2-yl]amino]-2-methylpyridin-3-yl]methanesulfonamide
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C16H17ClN8O2S
 1
1 Ki = 85 nM
CP0192151
4-[2-[(6-methoxypyridin-3-yl)amino]-5-(morpholin-4-ylmethyl)pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C20H24N8O2
 1
1 Ki = 104 nM
CP0349679
4-[2-[(6-methoxypyridin-3-yl)amino]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C15H15N7O
 1
1 Ki = 107 nM
CP0143584
N-[3-(6-amino-2-methylpyrimidin-4-yl)pyridin-2-yl]-1H-indazol-4-amine
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C17H15N7
 1
1 Ki = 130 nM
CP0173323
3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-N-(6-ethoxypyridin-3-yl)imidazo[1,2-a]pyridin-2-amine
   Show/Hide
C18H18N8O
 1
1 Ki = 148 nM
CP0339164
4-[2-[(6-methoxypyridin-3-yl)amino]-5-(piperidin-1-ylmethyl)pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C21H26N8O
 1
1 Ki = 153 nM
CP0343352
4-[5-(azetidin-1-ylmethyl)-2-[(6-methoxypyridin-3-yl)amino]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C19H22N8O
 1
1 Ki = 160 nM
CP0302072
N-[3-(2-methyl-7H-purin-6-yl)pyridin-2-yl]-1H-indol-4-amine
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C19H15N7
 1
1 Ki = 181 nM
CP0142948
N-[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)pyridin-2-yl]-1H-indol-4-amine
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C17H15N7
 1
1 Ki = 187 nM
CP0087588
1-[[5-(4-amino-6-methyl-1,3,5-triazin-2-yl)-6-[(6-methoxypyridin-3-yl)amino]pyridin-3-yl]methyl]piperidin-4-ol
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C21H26N8O2
 1
1 Ki = 199 nM
CP0131195
4-[2-[(6-methoxypyridin-3-yl)amino]-5-methylpyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C16H17N7O
 1
1 Ki = 242 nM
CP0292692
4-[5-bromo-2-[(6-methoxypyridin-3-yl)amino]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C15H14BrN7O
 1
1 Ki = 247 nM
CP0172042
4-[2-[(6-methoxypyridin-3-yl)amino]-5-[(4-methylpiperazin-1-yl)methyl]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C21H27N9O
 1
1 Ki = 258 nM
CP0313976
4-[2-[(6-methoxypyridin-3-yl)amino]-5-(pyrrolidin-1-ylmethyl)pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C20H24N8O
 1
1 Ki = 266 nM
CP0087587
[(3R)-1-[[5-(4-amino-6-methyl-1,3,5-triazin-2-yl)-6-[(6-methoxypyridin-3-yl)amino]pyridin-3-yl]methyl]pyrrolidin-3-yl]methanol
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C21H26N8O2
 1
1 Ki = 278 nM
CP0191322
4-[5-[(2-methoxyethylamino)methyl]-2-[(6-methoxypyridin-3-yl)amino]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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C19H24N8O2
 1
1 Ki = 283 nM
CP0346732
5-N-[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)pyridin-2-yl]-2-chloropyridine-3,5-diamine
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C14H13ClN8
 1
1 Ki = 324 nM
CP0064828
4-[3-[(6-methoxypyridin-3-yl)amino]pyrazin-2-yl]-6-methyl-1,3,5-triazin-2-amine
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C14H14N8O
 1
1 Ki = 327 nM
CP0330553
4-[2-[(6-methoxypyridin-3-yl)amino]phenyl]-6-methyl-1,3,5-triazin-2-amine
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C16H16N6O
 1
1 Ki = 396 nM
CP0041963
N-[3-(4-amino-6-methyl-1,3,5-triazin-2-yl)imidazo[1,2-a]pyridin-2-yl]quinolin-6-amine
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C20H16N8
 1
1 Ki = 529 nM
CP0346280
N-[3-(6-amino-5-fluoro-2-methylpyrimidin-4-yl)pyridin-2-yl]-1H-indazol-4-amine
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C17H14FN7
 1
1 Ki = 802 nM
CP0328888
4-[3-[(6-methoxypyridin-3-yl)amino]pyridin-4-yl]-6-methyl-1,3,5-triazin-2-amine
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C15H15N7O
 1
1 Ki = 868 nM
CP0191327
N-[3-(6-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl)pyridin-2-yl]-1H-indazol-4-amine
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C18H14N8
 1
1 Ki = 1411 nM
CP0174742
N-[3-[6-amino-2-(trifluoromethyl)pyrimidin-4-yl]pyridin-2-yl]-1H-indazol-4-amine
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C17H12F3N7
 1
1 Ki = 3139 nM
CP0229154
N-(6-methoxypyridin-3-yl)-3-(7H-purin-6-yl)pyridin-2-amine
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C16H13N7O
 1
1 Ki = 7277 nM
CP0087589
N-[3-(7H-purin-6-yl)pyridin-2-yl]-1H-indazol-4-amine
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C17H12N8
 1
1 Ki = 22621 nM
Clinical Information about the Protein
Target 1 ( PI3-kinase alpha (PIK3CA) )
Target Type Successful Target
Disease 4 Target-related Diseases  4
1 Breast cancer [ICD-11: 2C60-2C65]
2 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
3 Colorectal cancer [ICD-11: 2B91.Z]
4 Rheumatoid arthritis [ICD-11: FA20]
Approved Drug(s) 1 Approved Drug  1
1 Alpelisib Approved
Breast cancer
Clinical Trial Drug(s) 5 Clinical Trial Drugs  5
1 Buparlisib Phase 3
Breast cancer
2 GDC-0032 Phase 3
Breast cancer
3 HHCYH33 Phase 1
Breast cancer
4 MLN1117 Phase 1/2
Solid tumour/cancer
5 PA-799 Phase 1/2
Colorectal cancer
Investigative Drug(s) 1 Investigative Drug  1
1 ETP-46321 Investigative
Rheumatoid arthritis
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01368 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Bos taurus, Bovine
PT03525 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Mus musculus, Mouse
PT07498 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Rattus norvegicus, Rat