General Information of the Protein
Protein ID
PT01934
Protein Name
Serine/threonine-protein kinase ATR
Secondarily
Protein Name
Ataxia telangiectasia and Rad3-related protein
FRAP-related protein 1
Gene Name
ATR
Secondarily
Gene Name
FRP1
Sequence
MGEHGLELASMIPALRELGSATPEEYNTVVQKPRQILCQFIDRILTDVNVVAVELVKKTDSQPTSVMLLDFIQHIMKSSPLMFVNVSGSHEAKGSCIEFSNWIITRLLRIAATPSCHLLHKKICEVICSLLFLFKSKSPAIFGVLTKELLQLFEDLVYLHRRNVMGHAVEWPVVMSRFLSQLDEHMGYLQSAPLQLMSMQNLEFIEVTLLMVLTRIIAIVFFRRQELLLWQIGCVLLEYGSPKIKSLAISFLTELFQLGGLPAQPASTFFSSFLELLKHLVEMDTDQLKLYEEPLSKLIKTLFPFEAEAYRNIEPVYLNMLLEKLCVMFEDGVLMRLKSDLLKAALCHLLQYFLKFVPAGYESALQVRKVYVRNICKALLDVLGIEVDAEYLLGPLYAALKMESMEIIEEIQCQTQQENLSSNSDGISPKRRRLSSSLNPSKRAPKQTEEIKHVDMNQKSILWSALKQKAESLQISLEYSGLKNPVIEMLEGIAVVLQLTALCTVHCSHQNMNCRTFKDCQHKSKKKPSVVITWMSLDFYTKVLKSCRSLLESVQKLDLEATIDKVVKIYDALIYMQVNSSFEDHILEDLCGMLSLPWIYSHSDDGCLKLTTFAANLLTLSCRISDSYSPQAQSRCVFLLTLFPRRIFLEWRTAVYNWALQSSHEVIRASCVSGFFILLQQQNSCNRVPKILIDKVKDDSDIVKKEFASILGQLVCTLHGMFYLTSSLTEPFSEHGHVDLFCRNLKATSQHECSSSQLKASVCKPFLFLLKKKIPSPVKLAFIDNLHHLCKHLDFREDETDVKAVLGTLLNLMEDPDKDVRVAFSGNIKHILESLDSEDGFIKELFVLRMKEAYTHAQISRNNELKDTLILTTGDIGRAAKGDLVPFALLHLLHCLLSKSASVSGAAYTEIRALVAAKSVKLQSFFSQYKKPICQFLVESLHSSQMTALPNTPCQNADVRKQDVAHQREMALNTLSEIANVFDFPDLNRFLTRTLQVLLPDLAAKASPAASALIRTLGKQLNVNRREILINNFKYIFSHLVCSCSKDELERALHYLKNETEIELGSLLRQDFQGLHNELLLRIGEHYQQVFNGLSILASFASSDDPYQGPRDIISPELMADYLQPKLLGILAFFNMQLLSSSVGIEDKKMALNSLMSLMKLMGPKHVSSVRVKMMTTLRTGLRFKDDFPELCCRAWDCFVRCLDHACLGSLLSHVIVALLPLIHIQPKETAAIFHYLIIENRDAVQDFLHEIYFLPDHPELKKIKAVLQEYRKETSESTDLQTTLQLSMKAIQHENVDVRIHALTSLKETLYKNQEKLIKYATDSETVEPIISQLVTVLLKGCQDANSQARLLCGECLGELGAIDPGRLDFSTTETQGKDFTFVTGVEDSSFAYGLLMELTRAYLAYADNSRAQDSAAYAIQELLSIYDCREMETNGPGHQLWRRFPEHVREILEPHLNTRYKSSQKSTDWSGVKKPIYLSKLGSNFAEWSASWAGYLITKVRHDLASKIFTCCSIMMKHDFKVTIYLLPHILVYVLLGCNQEDQQEVYAEIMAVLKHDDQHTINTQDIASDLCQLSTQTVFSMLDHLTQWARHKFQALKAEKCPHSKSNRNKVDSMVSTVDYEDYQSVTRFLDLIPQDTLAVASFRSKAYTRAVMHFESFITEKKQNIQEHLGFLQKLYAAMHEPDGVAGVSAIRKAEPSLKEQILEHESLGLLRDATACYDRAIQLEPDQIIHYHGVVKSMLGLGQLSTVITQVNGVHANRSEWTDELNTYRVEAAWKLSQWDLVENYLAADGKSTTWSVRLGQLLLSAKKRDITAFYDSLKLVRAEQIVPLSAASFERGSYQRGYEYIVRLHMLCELEHSIKPLFQHSPGDSSQEDSLNWVARLEMTQNSYRAKEPILALRRALLSLNKRPDYNEMVGECWLQSARVARKAGHHQTAYNALLNAGESRLAELYVERAKWLWSKGDVHQALIVLQKGVELCFPENETPPEGKNMLIHGRAMLLVGRFMEETANFESNAIMKKYKDVTACLPEWEDGHFYLAKYYDKLMPMVTDNKMEKQGDLIRYIVLHFGRSLQYGNQFIYQSMPRMLTLWLDYGTKAYEWEKAGRSDRVQMRNDLGKINKVITEHTNYLAPYQFLTAFSQLISRICHSHDEVFVVLMEIIAKVFLAYPQQAMWMMTAVSKSSYPMRVNRCKEILNKAIHMKKSLEKFVGDATRLTDKLLELCNKPVDGSSSTLSMSTHFKMLKKLVEEATFSEILIPLQSVMIPTLPSILGTHANHASHEPFPGHWAYIAGFDDMVEILASLQKPKKISLKGSDGKFYIMMCKPKDDLRKDCRLMEFNSLINKCLRKDAESRRRELHIRTYAVIPLNDECGIIEWVNNTAGLRPILTKLYKEKGVYMTGKELRQCMLPKSAALSEKLKVFREFLLPRHPPIFHEWFLRTFPDPTSWYSSRSAYCRSTAVMSMVGYILGLGDRHGENILFDSLTGECVHVDFNCLFNKGETFEVPEIVPFRLTHNMVNGMGPMGTEGLFRRACEVTMRLMRDQREPLMSVLKTFLHDPLVEWSKPVKGHSKAPLNETGEVVNEKAKTHVLDIEQRLQGVIKTRNRVTGLPLSIEGHVHYLIQEATDENLLCQMYLGWTPYM
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
Atypical protein kinase group
>
Atypical protein kinase PIKK family
Function
Serine/threonine protein kinase which activates checkpoint signaling upon genotoxic stresses such as ionizing radiation (IR), ultraviolet light (UV), or DNA replication stalling, thereby acting as a DNA damage sensor (PubMed:10597277, PubMed:10608806, PubMed:10859164, PubMed:11721054, PubMed:12791985, PubMed:12814551, PubMed:14657349, PubMed:14729973, PubMed:14742437, PubMed:15210935, PubMed:15496423, PubMed:16260606, PubMed:21144835, PubMed:27723717, PubMed:27723720, PubMed:33848395, PubMed:9427750, PubMed:9636169, PubMed:21777809). Recognizes the substrate consensus sequence [ST]-Q (PubMed:10597277, PubMed:10608806, PubMed:10859164, PubMed:11721054, PubMed:12791985, PubMed:12814551, PubMed:14657349, PubMed:14729973, PubMed:14742437, PubMed:15210935, PubMed:15496423, PubMed:16260606, PubMed:21144835, PubMed:27723717, PubMed:27723720, PubMed:33848395, PubMed:9427750, PubMed:9636169). Phosphorylates BRCA1, CHEK1, MCM2, RAD17, RPA2, SMC1 and p53/TP53, which collectively inhibit DNA replication and mitosis and promote DNA repair, recombination and apoptosis (PubMed:9925639, PubMed:11114888, PubMed:11418864, PubMed:11865061, PubMed:21777809). Phosphorylates 'Ser-139' of histone variant H2AX at sites of DNA damage, thereby regulating DNA damage response mechanism (PubMed:11673449). Required for FANCD2 ubiquitination (PubMed:15314022). Critical for maintenance of fragile site stability and efficient regulation of centrosome duplication (PubMed:12526805). Positively regulates the restart of stalled replication forks following activation by the KHDC3L-OOEP scaffold complex (By similarity).
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Uniprot ID
Primary ID:
Q13535

Secondarily ID:
Q59HB2
Q7KYL3
Q93051
Q9BXK4
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HGNC ID
HGNC:882
Subcellular Location
Nucleus
Chromosome
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: CL000007 , HT-29
Compound ID Compound Name Compound Formula
CP0068245
N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
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C21H26N6O3S
 1
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0669285
US8552004, 2.03
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C21H27N7O2S
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0393368
N-methyl-4-[(10S,14R)-14-methyl-6-(2-methylsulfonylpropan-2-yl)-8,12-dioxa-1,3,5-triazatricyclo[8.4.0.02,7]tetradeca-2,4,6-trien-4-yl]-1H-pyrrolo[2,3-b]pyridin-5-amine
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C22H28N6O4S
 1
1
IC50 < 10 nM
   TI
   LI
   LO
   TS
CP0393370
N-methyl-1-[(10S,14R)-14-methyl-6-(2-methylsulfonylpropan-2-yl)-8,12-dioxa-1,3,5-triazatricyclo[8.4.0.02,7]tetradeca-2,4,6-trien-4-yl]imidazol-2-amine
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C18H26N6O4S
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0445759
2-[(10S,14R)-14-methyl-4-[5-(methylamino)-1H-pyrrolo[2,3-b]pyridin-4-yl]-8,12-dioxa-1,3,5-triazatricyclo[8.4.0.02,7]tetradeca-2,4,6-trien-6-yl]propan-2-ol
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C21H26N6O3
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0493027
(10S,14R)-N,14-dimethyl-6-(2-methylsulfonylpropan-2-yl)-N-(1H-pyrazol-5-yl)-8,12-dioxa-1,3,5-triazatricyclo[8.4.0.02,7]tetradeca-2,4,6-trien-4-amine
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C18H26N6O4S
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0566052
N-methyl-1-[(10S,14R)-14-methyl-6-(2-methylsulfonylpropan-2-yl)-8,12-dioxa-1,3,5-triazatricyclo[8.4.0.02,7]tetradeca-2,4,6-trien-4-yl]benzimidazol-2-amine
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C22H28N6O4S
 1
1
IC50 < 10 nM
   TI
   LI
   LO
   TS
CP0567492
N-ethyl-4-[(10S,14R)-14-methyl-6-(2-methylsulfonylpropan-2-yl)-8,12-dioxa-1,3,5-triazatricyclo[8.4.0.02,7]tetradeca-2,4,6-trien-4-yl]-1H-pyrrolo[2,3-b]pyridin-5-amine
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C23H30N6O4S
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0068244
(3R)-3-methyl-4-[6-(1-methylsulfonylcyclopropyl)-2-(1H-pyrrolo[2,3-c]pyridin-4-yl)pyrimidin-4-yl]morpholine
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C20H23N5O3S
 1
1
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0402721
US9428503, CN102399218A: Compound 94
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C20H20N6O2
 1
1
IC50 = 12.9 nM
   TI
   LI
   LO
   TS
CP0893331
(3R)-3-methyl-4-(6-(1-(S-methylsulfonimidoyl)cyclopropyl)-2-(1H-pyrrolo[2,3-c]pyridin-4-yl)pyrimidin-4-yl)morpholine
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C20H24N6O2S
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0354837
1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
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C20H24N6O3S
 1
1
IC50 = 15 nM
   TI
   LI
   LO
   TS
CP0076584
N-[1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-yl]acetamide
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C22H26N6O4S
 1
1
IC50 = 17 nM
   TI
   LI
   LO
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CP0168855
N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[1-(methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl]benzimidazol-2-amine
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C21H27N7O2S
 1
1
IC50 = 23 nM
   TI
   LI
   LO
   TS
CP0928862
4-{[Diethyl(oxido)-lambda6-sulfanylidene]amino}-2-[(3R)-3-methylmorpholin-4-yl]-8-(1H-pyrazol-5-yl)-1,7-naphthyridine
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C20H26N6O2S
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
CP0946954
3,3-Dimethyl-2-{2-[(3R)-3-methylmorpholin-4-yl]-8-(1H-pyrazol-5-yl)-1,7-naphthyridin-4-yl}butan-2-ol
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C22H29N5O2
 1
1
IC50 = 34 nM
   TI
   LI
   LO
   TS
CP0168728
5-fluoro-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
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C20H23FN6O3S
 1
1
IC50 = 35 nM
   TI
   LI
   LO
   TS
CP0639539
2-[(3R)-3-Methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-5-yl)-1,7-naphthyridine
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C20H21N7O
 1
1
IC50 = 36 nM
   TI
   LI
   LO
   TS
CP0946950
4-(2-Fluoropyridin-3-yl)-2-[(3R)-3-methylmorpholin-4-yl]-8-(1H-pyrazol-5-yl)-1,7-naphthyridine
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C21H19FN6O
 1
1
IC50 = 44 nM
   TI
   LI
   LO
   TS
CP0068243
(3R)-4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]-3-methylmorpholine
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C21H24N4O3S
 2
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
2
IC50 = 61 nM
   TI
   LI
   LO
   TS
CP0472913
1-(oxan-4-yl)-8-pyridin-3-yl-3H-imidazo[4,5-c]quinolin-2-one
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C20H18N4O2
 1
1
IC50 = 51 nM
   TI
   LI
   LO
   TS
CP0076577
1-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]benzimidazol-2-amine
   Show/Hide
C19H22N6O3S
 1
1
IC50 = 51 nM
   TI
   LI
   LO
   TS
CP0413611
US9428503, CN102399218A: Compound 62
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C21H17N5O
 1
1
IC50 = 55.3 nM
   TI
   LI
   LO
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CP0904636
2-[(3R)-3-Methylmorpholin-4-yl]-4-[4-(methylsulfonyl)piperazin-1-yl]-8-(1H-pyrazol-5-yl)-1,7-naphthyridine
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C21H27N7O3S
 1
1
IC50 = 59 nM
   TI
   LI
   LO
   TS
CP0529511
US9428503, CN102372711A: Compound 5
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C24H25N5O3
 1
1
IC50 = 64.4 nM
   TI
   LI
   LO
   TS
CP0958487
2-[(3R)-3-Methylmorpholin-4-yl]-8-(1H-pyrazol-5-yl)-4-(tetrahydro-2H-pyran-4-yl)-1,7-naphthyridine
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C21H25N5O2
 1
1
IC50 = 66 nM
   TI
   LI
   LO
   TS
CP0495550
US9428503, CN102399218A: Compound 114
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C23H23N5O4S
 1
1
IC50 = 68.6 nM
   TI
   LI
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CP0518461
US9428503, CN102372711A: Compound 4
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C24H25N5O4
 1
1
IC50 = 68.6 nM
   TI
   LI
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CP0901623
N-(4-Fluorophenyl)-N-methyl-2-[(3R)-3-methylmorpholin-4-yl]-8-(1H-pyrazol-5-yl)-1,7-naphthyridin-4-amine
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C23H23FN6O
 1
1
IC50 = 70 nM
   TI
   LI
   LO
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CP0808811
CERALASERTIB
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C20H24N6O2S
 1
1
IC50 = 74 nM
   TI
   LI
   LO
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CP0912067
4-(2-Methyl-1H-imidazol-1-yl)-2-[(3R)-3-methylmorpholin-4-yl]-8-(1H-pyrazol-5-yl)-1,7-naphthyridine
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C20H21N7O
 1
1
IC50 = 76 nM
   TI
   LI
   LO
   TS
CP0901624
4-(6,7-Dihydro-5H-pyrrolo[1,2-a]imidazol-3-yl)-2-[(3R)-3-methylmorpholin-4-yl]-8-(1H-pyrazol-5-yl)-1,7-naphthyridine
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C22H23N7O
 1
1
IC50 = 82 nM
   TI
   LI
   LO
   TS
CP0076581
4-[6-(1-methylsulfonylcyclopropyl)-2-(1H-pyrrolo[2,3-c]pyridin-4-yl)pyrimidin-4-yl]morpholine
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C19H21N5O3S
 1
1
IC50 = 85 nM
   TI
   LI
   LO
   TS
CP0081365
3-[6-(1-methylsulfonylcyclopropyl)-2-(1H-pyrrolo[2,3-c]pyridin-4-yl)pyrimidin-4-yl]-8-oxa-3-azabicyclo[3.2.1]octane
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C21H23N5O3S
 1
1
IC50 = 86 nM
   TI
   LI
   LO
   TS
CP0867459
2-[(3R)-3-Methylmorpholin-4-yl]-4-[1-(methylsulfonyl)-cyclopropyl]-8-(1H-pyrazol-5-yl)-1,7-naphthyridine
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C20H23N5O3S
 1
1
IC50 = 86 nM
   TI
   LI
   LO
   TS
CP0412368
3-methyl-1-(oxan-4-yl)-8-pyridin-3-ylimidazo[4,5-c]quinolin-2-one
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C21H20N4O2
 1
1
IC50 = 87 nM
   TI
   LI
   LO
   TS
CP0314495
(3R)-3-methyl-4-[6-[1-[(S)-methylsulfinyl]cyclopropyl]-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl]morpholine
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C20H23N5O2S
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0076580
(3R)-3-methyl-4-[6-(1-methylsulfonylcyclopropyl)-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl]morpholine
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C20H23N5O3S
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0145081
3-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]-8-oxa-3-azabicyclo[3.2.1]octane
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C22H24N4O3S
 2
1
IC50 = 110 nM
   TI
   LI
   LO
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2
IC50 = 350 nM
   TI
   LI
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   TS
CP0514493
6-fluoro-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
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C20H23FN6O3S
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0102647
4-fluoro-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
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C20H23FN6O3S
 1
1
IC50 = 130 nM
   TI
   LI
   LO
   TS
CP0130832
4-[2-(6-fluoro-1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
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C20H21FN4O3S
 2
1
IC50 = 130 nM
   TI
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2
IC50 = 440 nM
   TI
   LI
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CP0958488
4-Isopropoxy-2-[(3R)-3-methylmorpholin-4-yl]-8-(1H-pyrazol-5-yl)-1,7-naphthyridine
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C19H23N5O2
 1
1
IC50 = 154 nM
   TI
   LI
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CP0406920
US9428503, CN102399218A: Compound 64
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C18H16N6O
 1
1
IC50 = 162 nM
   TI
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CP0085622
4-[2-(1H-indol-4-yl)-6-(4-methylsulfonyloxan-4-yl)pyrimidin-4-yl]morpholine
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C22H26N4O4S
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0168854
(3R)-3-methyl-4-[6-[1-[(R)-methylsulfinyl]cyclopropyl]-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl]morpholine
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C20H23N5O2S
 1
1
IC50 = 180 nM
   TI
   LI
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CP0895134
2-[(3R)-3-Methylmorpholin-4-yl]-8-(1H-pyrazol-5-yl)-4-(pyridin-3-ylethynyl)-1,7-naphthyridine
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C23H20N6O
 1
1
IC50 = 227 nM
   TI
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CP0241870
BDBM103466
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C20H24N6O2S
 1
1
IC50 = 240 nM
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CP0081366
8-[6-(1-methylsulfonylcyclopropyl)-2-(1H-pyrrolo[2,3-c]pyridin-4-yl)pyrimidin-4-yl]-3-oxa-8-azabicyclo[3.2.1]octane
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C21H23N5O3S
 1
1
IC50 = 260 nM
   TI
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CP0902619
4-[2-Methyl-6-(S-methylsulfonimidoyl)pyridin-3-yl]-2-[(3R)-3-methylmorpholin-4-yl]-8-(1H-pyrazol-5-yl)-1,7-naphthyridine
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C23H25N7O2S
 1
1
IC50 = 266 nM
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CP0565273
4-[4-(3,6-dihydro-2H-pyran-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]-1H-indole
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C21H21N3O3S
 1
1
IC50 = 270 nM
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   TS
CP0157307
4-[2-(1H-indol-4-yl)-6-(2-methylsulfonylpropan-2-yl)pyrimidin-4-yl]morpholine
   Show/Hide
C20H24N4O3S
 1
1
IC50 = 280 nM
   TI
   LI
   LO
   TS
CP0413610
US9428503, CN102372711A: Compound 1
   Show/Hide
C22H23N5O2
 1
1
IC50 = 281 nM
   TI
   LI
   LO
   TS
CP0939308
4-(Diethylphosphoryl)-2-[(3R)-3-methylmorpholin-4-yl]-8-(1H-pyrazol-5-yl)-1,7-naphthyridine
   Show/Hide
C20H26N5O2P
 1
1
IC50 = 289 nM
   TI
   LI
   LO
   TS
CP0102640
4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C20H22N4O3S
 2
1
IC50 = 290 nM
   TI
   LI
   LO
   TS
2
IC50 = 360 nM
   TI
   LI
   LO
   TS
CP0404754
4-[6-(1-methylsulfonylcyclopropyl)-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl]morpholine
   Show/Hide
C19H21N5O3S
 1
1
IC50 = 350 nM
   TI
   LI
   LO
   TS
CP0514510
(3S)-3-methyl-4-[6-(1-methylsulfonylcyclopropyl)-2-(1H-pyrrolo[2,3-c]pyridin-4-yl)pyrimidin-4-yl]morpholine
   Show/Hide
C20H23N5O3S
 1
1
IC50 = 360 nM
   TI
   LI
   LO
   TS
CP0287648
3-amino-6-(4-((4-hydroxybutan-2-yl)sulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C21H22N4O4S
 1
1
IC50 = 380 nM
   TI
   LI
   LO
   TS
CP0421059
US10772893, Example 7
   Show/Hide
C22H21N5O3S
 1
1
IC50 = 380 nM
   TI
   LI
   LO
   TS
CP0563148
US9428503, CN102399218A: Compound 60
   Show/Hide
C22H25N5O3
 1
1
IC50 = 418 nM
   TI
   LI
   LO
   TS
CP0050427
3-amino-6-(4-((1-(dimethylamino)propan-2-yl)sulfonyl)-phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C22H25N5O3S
 1
1
IC50 = 420 nM
   TI
   LI
   LO
   TS
CP0076974
4-[2-(1H-indol-4-yl)-6-(4-methylsulfonylpiperidin-4-yl)pyrimidin-4-yl]morpholine
   Show/Hide
C22H27N5O3S
 1
1
IC50 = 420 nM
   TI
   LI
   LO
   TS
CP0527886
US10772893, Example 40
   Show/Hide
C18H21N5O2
 1
1
IC50 = 424 nM
   TI
   LI
   LO
   TS
CP0222476
(R)-3-amino-N-phenyl-6-(4-((tetrahydrofuran-3-yl)sulfonyl)-phenyl)pyrazine-2-carboxamide
   Show/Hide
C21H20N4O4S
 1
1
IC50 = 460 nM
   TI
   LI
   LO
   TS
CP0186550
4-[2-(6-methyl-1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C21H24N4O3S
 1
1
IC50 = 490 nM
   TI
   LI
   LO
   TS
CP0256504
4-[6-[1-(benzenesulfonyl)cyclopropyl]-2-(1H-indol-4-yl)pyrimidin-4-yl]morpholine
   Show/Hide
C25H24N4O3S
 1
1
IC50 = 590 nM
   TI
   LI
   LO
   TS
CP0362355
4-[[(1S)-1-(1-methylpyrazol-3-yl)ethyl]amino]-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C21H20N6O
 1
1
IC50 = 640 nM
   TI
   LI
   LO
   TS
CP0130830
4-[2-(6-chloro-1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C20H21ClN4O3S
 1
1
IC50 = 720 nM
   TI
   LI
   LO
   TS
CP0480277
4-(2-ethylbutylamino)-6-pyridin-4-ylquinoline-3-carboxamide
   Show/Hide
C21H24N4O
 1
1
IC50 = 730 nM
   TI
   LI
   LO
   TS
CP0345264
4-[2-(1H-indol-4-yl)-6-(1-propan-2-ylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C22H26N4O3S
 1
1
IC50 = 770 nM
   TI
   LI
   LO
   TS
CP0304424
4-[2-(6-methoxy-1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C21H24N4O4S
 1
1
IC50 = 800 nM
   TI
   LI
   LO
   TS
CP0249222
5-chloro-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
   Show/Hide
C20H23ClN6O3S
 1
1
IC50 = 870 nM
   TI
   LI
   LO
   TS
CP0180289
3-amino-6-(4-(isopropylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C20H20N4O3S
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0212807
3-amino-6-(4-(tert-butylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C21H22N4O3S
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0341198
3-amino-6-(4-(azetidine-1-carbonyl)phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C21H19N5O2
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0085620
4-[2-(1H-indol-4-yl)-6-(methylsulfonylmethyl)pyrimidin-4-yl]morpholine
   Show/Hide
C18H20N4O3S
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0364430
4-(cyclopentylamino)-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C20H20N4O
 1
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0480891
US9428503, 40
   Show/Hide
C25H29N5O3
 1
1
IC50 = 1330 nM
   TI
   LI
   LO
   TS
CP0271874
3-amino-N-phenyl-6-(4-(pyrrolidine-1-carbonyl)phenyl)-pyrazine-2-carboxamide
   Show/Hide
C22H21N5O2
 1
1
IC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0508027
US9428503, CN102399218A: Compound 61
   Show/Hide
C21H18N6O
 1
1
IC50 = 1480 nM
   TI
   LI
   LO
   TS
CP0199334
3-amino-6-(4-(ethylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C19H18N4O3S
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0130833
4-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]-1H-indole-6-carbonitrile
   Show/Hide
C21H21N5O3S
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0199392
3-amino-6-(4-(sec-butylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C21H22N4O3S
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0234613
4-[[(1R)-1-(4-chlorophenyl)ethyl]amino]-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C23H19ClN4O
 1
1
IC50 = 1900 nM
   TI
   LI
   LO
   TS
CP0050429
3-amino-6-(4-(dimethylcarbamoyl)phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C20H19N5O2
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0171816
3-amino-N-phenyl-6-(4-(propylsulfonyl)phenyl)pyrazine-2-carboxamide
   Show/Hide
C20H20N4O3S
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0076973
4-[2-(1H-indol-4-yl)-6-(1-pyridin-2-ylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C24H23N5O3S
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0427439
8-[6-[3-(dimethylamino)propoxy]pyridin-3-yl]-3-methyl-1-(oxan-4-yl)imidazo[4,5-c][1,5]naphthyridin-2-one
   Show/Hide
C25H30N6O3
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0265453
4-[2-(2-methyl-1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C21H24N4O3S
 1
1
IC50 = 2500 nM
   TI
   LI
   LO
   TS
CP0473927
4-(2-ethylbutylamino)-6-pyridazin-4-ylquinoline-3-carboxamide
   Show/Hide
C20H23N5O
 1
1
IC50 = 2600 nM
   TI
   LI
   LO
   TS
CP0474996
US9428503, 43
   Show/Hide
C25H29N5O3
 1
1
IC50 = 2690 nM
   TI
   LI
   LO
   TS
CP0130834
4-[2-(1H-indol-4-yl)-6-[1-(oxan-4-ylsulfonyl)cyclopropyl]pyrimidin-4-yl]morpholine
   Show/Hide
C24H28N4O4S
 1
1
IC50 = 2800 nM
   TI
   LI
   LO
   TS
CP0310474
4-[2-(1H-indol-4-yl)-6-(1-piperidin-4-ylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C24H29N5O3S
 1
1
IC50 = 2900 nM
   TI
   LI
   LO
   TS
CP0265668
4-(cyclohexylmethylamino)-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C22H24N4O
 1
1
IC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0164861
4-(oxan-4-ylamino)-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C20H20N4O2
 1
1
IC50 = 3100 nM
   TI
   LI
   LO
   TS
CP0556348
4-(cyclohexylamino)-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C21H22N4O
 1
1
IC50 = 3200 nM
   TI
   LI
   LO
   TS
CP0473945
4-[[(1R)-1-(oxan-4-yl)ethyl]amino]-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C22H24N4O2
 1
1
IC50 = 3500 nM
   TI
   LI
   LO
   TS
CP0130829
(3S)-4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]-3-methylmorpholine
   Show/Hide
C21H24N4O3S
 1
1
IC50 = 3700 nM
   TI
   LI
   LO
   TS
CP0333714
4-[2-(1H-indol-4-yl)-6-(1-methyl-4-methylsulfonylpiperidin-4-yl)pyrimidin-4-yl]morpholine
   Show/Hide
C23H29N5O3S
 1
1
IC50 = 3700 nM
   TI
   LI
   LO
   TS
CP0451943
US9428503, 41
   Show/Hide
C25H29N5O3
 1
1
IC50 = 3940 nM
   TI
   LI
   LO
   TS
CP0472916
US9428503, 42
   Show/Hide
C25H29N5O3
 2
1
IC50 = 4370 nM
   TI
   LI
   LO
   TS
2
IC50 = 4400 nM
   TI
   LI
   LO
   TS
CP0130828
(3R)-3-ethyl-4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C22H26N4O3S
 1
1
IC50 = 4400 nM
   TI
   LI
   LO
   TS
CP0180782
6-cyano-4-(2-ethylbutylamino)quinoline-3-carboxamide
   Show/Hide
C17H20N4O
 1
1
IC50 = 4400 nM
   TI
   LI
   LO
   TS
CP0180780
4-[[(1R)-1-(4-chlorophenyl)ethyl]amino]-6-cyanoquinoline-3-carboxamide
   Show/Hide
C19H15ClN4O
 1
1
IC50 = 4700 nM
   TI
   LI
   LO
   TS
CP0533485
7-fluoro-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
   Show/Hide
C20H23FN6O3S
 1
1
IC50 = 5100 nM
   TI
   LI
   LO
   TS
CP0136765
4-methoxy-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
   Show/Hide
C21H26N6O4S
 1
1
IC50 = 5300 nM
   TI
   LI
   LO
   TS
CP0249202
4-chloro-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
   Show/Hide
C20H23ClN6O3S
 1
1
IC50 = 5300 nM
   TI
   LI
   LO
   TS
CP0160334
3-amino-6-(4-(methylsulfinyl)phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C18H16N4O2S
 1
1
IC50 = 5400 nM
   TI
   LI
   LO
   TS
CP0364431
4-(2-ethylbutylamino)-6-(6-methylpyridin-3-yl)quinoline-3-carboxamide
   Show/Hide
C22H26N4O
 1
1
IC50 = 5500 nM
   TI
   LI
   LO
   TS
CP0839448
2-((2S,3R)-2-Benzyl-3-methylpyrrolidin-1-yl)-6-morpholinopyrimidin-4(3H)-one
   Show/Hide
C20H26N4O2
 1
1
IC50 = 5500 nM
   TI
   LI
   LO
   TS
CP0127298
US9428503, 1
   Show/Hide
C26H31N5O3
 2
1
IC50 = 6160 nM
   TI
   LI
   LO
   TS
2
IC50 = 6200 nM
   TI
   LI
   LO
   TS
CP0314494
4-[2-(1H-benzimidazol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C19H21N5O3S
 2
1
IC50 = 6200 nM
   TI
   LI
   LO
   TS
2
IC50 = 8900 nM
   TI
   LI
   LO
   TS
CP0256503
4-[2-(7-methyl-1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C21H24N4O3S
 1
1
IC50 = 6300 nM
   TI
   LI
   LO
   TS
CP0199330
3-amino-N-phenyl-6-(4-(piperidine-1-carbonyl)phenyl)pyrazine-2-carboxamide
   Show/Hide
C23H23N5O2
 1
1
IC50 = 6500 nM
   TI
   LI
   LO
   TS
CP0534989
4-(2-ethylbutylamino)-6-(1-methylpyrazol-4-yl)quinoline-3-carboxamide
   Show/Hide
C20H25N5O
 1
1
IC50 = 7100 nM
   TI
   LI
   LO
   TS
CP0193494
4-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]-1H-indole-2-carbonitrile
   Show/Hide
C21H21N5O3S
 1
1
IC50 = 7200 nM
   TI
   LI
   LO
   TS
CP0457022
US9428503, 66
   Show/Hide
C29H35N5O3
 1
1
IC50 = 7850 nM
   TI
   LI
   LO
   TS
CP0955420
(R)-6-(2-Benzylpiperidin-1-yl)-4-morpholinopyridin-2(1H)-one
   Show/Hide
C21H27N3O2
 1
1
IC50 = 8000 nM
   TI
   LI
   LO
   TS
CP0180814
2-morpholin-4-yl-6-(9H-thioxanthen-4-yl)pyran-4-one
   Show/Hide
C22H19NO3S
 1
1
IC50 = 8500 nM
   TI
   LI
   LO
   TS
CP0333713
4-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]-1H-indole-6-carboxamide
   Show/Hide
C21H23N5O4S
 1
1
IC50 = 9200 nM
   TI
   LI
   LO
   TS
CP0476587
US9428503, 45
   Show/Hide
C25H29N5O3
 1
1
IC50 = 9600 nM
   TI
   LI
   LO
   TS
CP0470735
N,N-dimethyl-3-[5-[3-methyl-1-(oxan-4-yl)-2-oxoimidazo[4,5-c]quinolin-8-yl]pyridin-2-yl]oxypropan-1-amine oxide
   Show/Hide
C26H31N5O4
 1
1
IC50 = 10000 nM
   TI
   LI
   LO
   TS
CP0457002
US9428503, 39
   Show/Hide
C27H31N5O3
 1
1
IC50 = 10700 nM
   TI
   LI
   LO
   TS
CP0451374
US9428503, 7
   Show/Hide
C27H33N5O3
 1
1
IC50 = 10800 nM
   TI
   LI
   LO
   TS
CP0446983
4-(oxan-4-ylmethylamino)-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C21H22N4O2
 1
1
IC50 = 11000 nM
   TI
   LI
   LO
   TS
CP0558413
4-(2-ethylbutylamino)-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C21H24N4O
 1
1
IC50 > 11000 nM
   TI
   LI
   LO
   TS
CP0291454
3-amino-6-(3-chloro-4-(dimethylcarbamoyl)phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C20H18ClN5O2
 1
1
IC50 = 12000 nM
   TI
   LI
   LO
   TS
CP0315929
4-[2-(1H-indazol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C19H21N5O3S
 1
1
IC50 = 13000 nM
   TI
   LI
   LO
   TS
CP0145049
8-[6-(methoxymethyl)pyridin-3-yl]-3-methyl-1-(oxan-4-yl)imidazo[4,5-c]quinolin-2-one
   Show/Hide
C23H24N4O3
 1
1
IC50 > 13000 nM
   TI
   LI
   LO
   TS
CP0180774
4-(2-ethylbutylamino)-6-[6-(hydroxymethyl)pyridin-3-yl]quinoline-3-carboxamide
   Show/Hide
C22H26N4O2
 1
1
IC50 > 13000 nM
   TI
   LI
   LO
   TS
CP0953819
6-((1S,2S,5R)-2-Benzyl-3-azabicyclo[3.1.0]hexan-3-yl)-4-((R)-2-methylmorpholino)pyridin-2(1H)-one
   Show/Hide
C22H27N3O2
 1
1
IC50 = 13000 nM
   TI
   LI
   LO
   TS
CP0180772
4-[[(1S)-1-(oxan-4-yl)ethyl]amino]-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C22H24N4O2
 1
1
IC50 > 14000 nM
   TI
   LI
   LO
   TS
CP0076582
N-methyl-4-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]-1H-indole-6-carboxamide
   Show/Hide
C22H25N5O4S
 2
1
IC50 = 15000 nM
   TI
   LI
   LO
   TS
2
IC50 = 16500 nM
   TI
   LI
   LO
   TS
CP0438313
7-fluoro-8-[6-(hydroxymethyl)pyridin-3-yl]-1-(3-methoxycyclobutyl)-3-methylimidazo[4,5-c]quinolin-2-one
   Show/Hide
C22H21FN4O3
 1
1
IC50 = 15000 nM
   TI
   LI
   LO
   TS
CP0444138
5-methoxy-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
   Show/Hide
C21H26N6O4S
 1
1
IC50 = 15000 nM
   TI
   LI
   LO
   TS
CP0549742
4-(2-ethylbutylamino)-6-pyridazin-3-ylquinoline-3-carboxamide
   Show/Hide
C20H23N5O
 1
1
IC50 > 15000 nM
   TI
   LI
   LO
   TS
CP0497632
US9428503, 67
   Show/Hide
C29H35N5O3
 1
1
IC50 = 15200 nM
   TI
   LI
   LO
   TS
CP0145086
4-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]-1,3-dihydroindol-2-one
   Show/Hide
C20H22N4O4S
 1
1
IC50 = 16000 nM
   TI
   LI
   LO
   TS
CP0232291
7-fluoro-1-(3-methoxycyclobutyl)-3-methyl-8-[6-(methylsulfonylmethyl)pyridin-3-yl]imidazo[4,5-c]quinolin-2-one
   Show/Hide
C23H23FN4O4S
 1
1
IC50 > 16000 nM
   TI
   LI
   LO
   TS
CP0497631
US9428503, 55
   Show/Hide
C28H33N5O3
 1
1
IC50 > 16100 nM
   TI
   LI
   LO
   TS
CP0861326
US9428503, 35
   Show/Hide
C27H31N5O3
 1
1
IC50 = 17800 nM
   TI
   LI
   LO
   TS
CP0180773
4-(2-ethylbutylamino)-6-pyrimidin-5-ylquinoline-3-carboxamide
   Show/Hide
C20H23N5O
 1
1
IC50 > 18000 nM
   TI
   LI
   LO
   TS
CP0259633
4-[[(1R)-1-(1-methylpyrazol-3-yl)ethyl]amino]-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C21H20N6O
 1
1
IC50 > 18000 nM
   TI
   LI
   LO
   TS
CP0563158
US9428503, 24
   Show/Hide
C28H32FN5O3
 1
1
IC50 > 18800 nM
   TI
   LI
   LO
   TS
CP0483520
US9428503, 29
   Show/Hide
C28H33N5O3
 1
1
IC50 = 19000 nM
   TI
   LI
   LO
   TS
CP0518510
US9428503, 30
   Show/Hide
C28H33N5O3
 1
1
IC50 = 19000 nM
   TI
   LI
   LO
   TS
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 > 19000 nM
   TI
   LI
   LO
   TS
CP0474997
US9428503, 59
   Show/Hide
C28H33N5O3
 1
1
IC50 > 19100 nM
   TI
   LI
   LO
   TS
CP0474823
US9428503, 44
   Show/Hide
C25H29N5O3
 1
1
IC50 > 19200 nM
   TI
   LI
   LO
   TS
CP0164866
7-fluoro-8-[6-(methoxymethyl)pyridin-3-yl]-3-methyl-1-(oxan-4-yl)imidazo[4,5-c]quinolin-2-one
   Show/Hide
C23H23FN4O3
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0480889
US9428503, 25
   Show/Hide
C27H33N5O3
 1
1
IC50 > 20700 nM
   TI
   LI
   LO
   TS
CP0457001
US9428503, 26
   Show/Hide
C27H33N5O3
 1
1
IC50 > 21800 nM
   TI
   LI
   LO
   TS
CP0483112
US9428503, 54
   Show/Hide
C28H33N5O3
 1
1
IC50 > 22400 nM
   TI
   LI
   LO
   TS
CP0145048
US9428503, 16
   Show/Hide
C26H31N5O3
 2
1
IC50 > 22800 nM
   TI
   LI
   LO
   TS
2
IC50 > 23000 nM
   TI
   LI
   LO
   TS
CP0393906
US9428503, 28
   Show/Hide
C28H33N5O3
 2
1
IC50 > 22800 nM
   TI
   LI
   LO
   TS
2
IC50 > 24000 nM
   TI
   LI
   LO
   TS
CP0491233
4-cyclopentylsulfanyl-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C20H19N3OS
 1
1
IC50 > 23000 nM
   TI
   LI
   LO
   TS
CP0480890
US9428503, 27
   Show/Hide
C28H32FN5O3
 1
1
IC50 > 23300 nM
   TI
   LI
   LO
   TS
CP0315928
N,N-dimethyl-4-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]-1H-indole-6-carboxamide
   Show/Hide
C23H27N5O4S
 1
1
IC50 = 24000 nM
   TI
   LI
   LO
   TS
CP0164887
US9428503, 38
   Show/Hide
C27H31N5O3
 2
1
IC50 > 24000 nM
   TI
   LI
   LO
   TS
2
IC50 > 24400 nM
   TI
   LI
   LO
   TS
CP0457004
US9428503, 64
   Show/Hide
C30H38N6O2
 1
1
IC50 > 24100 nM
   TI
   LI
   LO
   TS
CP0246126
US9428503, 33
   Show/Hide
C29H35N5O3
 2
1
IC50 > 24700 nM
   TI
   LI
   LO
   TS
2
IC50 > 2600 nM
   TI
   LI
   LO
   TS
CP0512613
US9428503, 70
   Show/Hide
C27H32FN5O3
 1
1
IC50 > 24900 nM
   TI
   LI
   LO
   TS
CP0180778
6-[2-fluoro-6-(methoxymethyl)pyridin-3-yl]-4-[[(1S)-1-(1-methylpyrazol-3-yl)ethyl]amino]quinoline-3-carboxamide
   Show/Hide
C23H23FN6O2
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0907953
US9428503, 12
   Show/Hide
C25H29N5O3
 1
1
IC50 > 25200 nM
   TI
   LI
   LO
   TS
CP0497634
US9428503, 46
   Show/Hide
C25H29N5O2
 1
1
IC50 > 26000 nM
   TI
   LI
   LO
   TS
CP0235599
7-fluoro-1-(4-methoxycyclohexyl)-8-[6-(methoxymethyl)pyridin-3-yl]-3-methylimidazo[4,5-c]quinolin-2-one
   Show/Hide
C25H27FN4O3
 1
1
IC50 > 26000 nM
   TI
   LI
   LO
   TS
CP0406927
US9428503, 65
   Show/Hide
C30H38N6O2
 1
1
IC50 > 26600 nM
   TI
   LI
   LO
   TS
CP0451372
US9428503, 53
   Show/Hide
C29H34FN5O3
 2
1
IC50 > 27100 nM
   TI
   LI
   LO
   TS
2
IC50 > 29000 nM
   TI
   LI
   LO
   TS
CP0538859
1-(oxan-4-yl)-3-propan-2-yl-8-pyridin-3-ylimidazo[4,5-c]quinolin-2-one
   Show/Hide
C23H24N4O2
 1
1
IC50 > 27600 nM
   TI
   LI
   LO
   TS
CP0164867
7-fluoro-1-(3-methoxycyclobutyl)-8-[6-(methoxymethyl)pyridin-3-yl]-3-methylimidazo[4,5-c]quinolin-2-one
   Show/Hide
C23H23FN4O3
 1
1
IC50 > 28000 nM
   TI
   LI
   LO
   TS
CP0451373
US9428503, 58
   Show/Hide
C27H31N5O2
 1
1
IC50 > 28100 nM
   TI
   LI
   LO
   TS
CP0472915
US9428503, 2
   Show/Hide
C26H31N5O3
 2
1
IC50 > 29000 nM
   TI
   LI
   LO
   TS
2
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0476588
US9428503, 68
   Show/Hide
C27H32FN5O3
 1
1
IC50 > 29000 nM
   TI
   LI
   LO
   TS
CP0473312
7-methyl-2-((7-methyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino)-9-(tetrahydro-2H-pyran-4-yl)-7,9-dihydro-8H-purin-8-one
   Show/Hide
C18H20N8O2
 1
1
IC50 > 29000 nM
   TI
   LI
   LO
   TS
CP0483521
US9428503, 37
   Show/Hide
C29H35N5O3
 1
1
IC50 > 29400 nM
   TI
   LI
   LO
   TS
CP0476585
US9428503, 11
   Show/Hide
C26H30FN5O3
 1
1
IC50 > 29600 nM
   TI
   LI
   LO
   TS
CP0085621
4-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]-1H-indole-2-carboxamide
   Show/Hide
C21H23N5O4S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0123538
4-[2-(1H-indol-5-yl)-6-(methylsulfonylmethyl)pyrimidin-4-yl]morpholine
   Show/Hide
C18H20N4O3S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0145082
4-[2-(3-methyl-1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C21H24N4O3S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0193495
4-[2-(1H-indol-7-yl)-6-(methylsulfonylmethyl)pyrimidin-4-yl]morpholine
   Show/Hide
C18H20N4O3S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0265455
4-[2-(1-methylindol-4-yl)-6-(methylsulfonylmethyl)pyrimidin-4-yl]morpholine
   Show/Hide
C19H22N4O3S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0315930
3-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]aniline
   Show/Hide
C18H22N4O3S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0333715
4-[2-(1H-indol-6-yl)-6-(methylsulfonylmethyl)pyrimidin-4-yl]morpholine
   Show/Hide
C18H20N4O3S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0345262
4-[2-(5-methyl-1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C21H24N4O3S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0345263
4-[6-(1-methylsulfonylcyclopropyl)-2-phenylpyrimidin-4-yl]morpholine
   Show/Hide
C18H21N3O3S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0093702
US9156831, 1
   Show/Hide
C21H29N9O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0093703
US9156831, 7
   Show/Hide
C22H31N9O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0143273
US9156831, 3
   Show/Hide
C22H31N9O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0173540
US9156831, 6
   Show/Hide
C22H31N9O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0283502
US9156831, 8
   Show/Hide
C21H27N9O4
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0068686
US9428503, 18
   Show/Hide
C26H30FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0081675
US9428503, 4
   Show/Hide
C24H27N5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0145046
US9428503, 17
   Show/Hide
C26H31N5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0164865
US9428503, 8
   Show/Hide
C26H30FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0228362
US9428503, 5
   Show/Hide
C25H29N5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0438311
US9428503, 19
   Show/Hide
C26H29F2N5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0438312
US9428503, 6
   Show/Hide
C26H30FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0445207
US9428503, 31
   Show/Hide
C29H35N5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0451370
US9428503, 47
   Show/Hide
C29H34FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0451371
US9428503, 52
   Show/Hide
C24H26FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0457000
US9428503, 22
   Show/Hide
C26H30FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0457005
US9428503, 71
   Show/Hide
C27H32FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0457020
US9428503, 20
   Show/Hide
C26H30FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0457021
US9428503, 49
   Show/Hide
C25H28FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0457024
US9428503, 3
   Show/Hide
C27H32FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0457026
US9428503, 10
   Show/Hide
C26H30FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0474824
US9428503, 56
   Show/Hide
C27H31N5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0474994
US9428503, 14
   Show/Hide
C26H29N5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0474995
US9428503, 15
   Show/Hide
C27H31N5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0476586
US9428503, 13
   Show/Hide
C25H29N5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0480888
US9428503, 9
   Show/Hide
C24H26FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0481097
US9428503, 57
   Show/Hide
C28H33N5O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0483063
US9428503, 48
   Show/Hide
C26H29F2N5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0483510
US9428503, 32
   Show/Hide
C29H35N5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0483512
US9428503, 51
   Show/Hide
C25H28FN5O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0483519
US9428503, 21
   Show/Hide
C26H30FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0483523
US9428503, 50
   Show/Hide
C25H28FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0491473
US9428503, 23
   Show/Hide
C28H32FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0492967
US9428503, 69
   Show/Hide
C27H32FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0507339
US9428503, 36
   Show/Hide
C28H33N5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0512612
US9428503, 61
   Show/Hide
C28H32FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0518509
US9428503, 63
   Show/Hide
C27H32FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0164862
8-[6-[2-(dimethylamino)ethoxy]pyridin-3-yl]-7-fluoro-1-(3-methoxycyclobutyl)-3-methylimidazo[4,5-c]quinolin-2-one
   Show/Hide
C25H28FN5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0164863
8-[6-[2-(dimethylamino)ethyl-methylamino]pyridin-3-yl]-7-fluoro-1-(3-methoxycyclobutyl)-3-methylimidazo[4,5-c]quinolin-2-one
   Show/Hide
C26H31FN6O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0164864
7-fluoro-8-[6-(methoxymethyl)pyridin-3-yl]-3-methyl-1-[(1S)-1-(oxan-4-yl)ethyl]imidazo[4,5-c]quinolin-2-one
   Show/Hide
C25H27FN4O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0164868
7-fluoro-1-(3-methoxycyclobutyl)-8-[6-(methoxymethyl)pyridin-3-yl]-3-methylimidazo[4,5-c]quinolin-2-one
   Show/Hide
C23H23FN4O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0235616
8-[6-[2-(dimethylamino)ethylamino]pyridin-3-yl]-7-fluoro-1-(3-methoxycyclobutyl)-3-methylimidazo[4,5-c]quinolin-2-one
   Show/Hide
C25H29FN6O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0427440
8-[6-[3-(dimethylamino)propoxy]pyridin-3-yl]-3-methyl-1-(oxan-4-yl)imidazo[4,5-c]cinnolin-2-one
   Show/Hide
C25H30N6O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0427456
1-(3-methoxycyclobutyl)-3-methyl-8-[6-(3-morpholin-4-ylpropoxy)pyridin-3-yl]imidazo[4,5-c]quinolin-2-one
   Show/Hide
C28H33N5O4
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0438314
4-(dimethylamino)-N-[5-[7-fluoro-1-(3-methoxycyclobutyl)-3-methyl-2-oxoimidazo[4,5-c]quinolin-8-yl]pyridin-2-yl]butanamide
   Show/Hide
C27H31FN6O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0470728
8-[6-[3-(4-hydroxypiperidin-1-yl)propoxy]pyridin-3-yl]-1-(3-methoxycyclobutyl)-3-methylimidazo[4,5-c]quinolin-2-one
   Show/Hide
C29H35N5O4
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0474725
4-(2-ethylbutylamino)-7-fluoro-6-[2-(2-pyrrolidin-1-ylethylamino)pyrimidin-5-yl]quinoline-3-carboxamide
   Show/Hide
C26H34FN7O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0542830
CHEMBL4176135
   Show/Hide
C22H21FN4O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0548185
N-[2-(dimethylamino)ethyl]-5-[7-fluoro-1-(3-methoxycyclobutyl)-3-methyl-2-oxoimidazo[4,5-c]quinolin-8-yl]pyridine-2-carboxamide
   Show/Hide
C26H29FN6O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
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 > 30000 nM
   TI
   LI
   LO
   TS
CP0180776
6-[6-(methoxymethyl)pyridin-3-yl]-4-[[(1S)-1-(oxan-4-yl)ethyl]amino]quinoline-3-carboxamide
   Show/Hide
C24H28N4O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
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 > 30000 nM
   TI
   LI
   LO
   TS
CP0362301
4-[[(1S)-1-(1,4-dimethylpyrazol-3-yl)ethyl]amino]-7-fluoro-6-[6-(methoxymethyl)pyridin-3-yl]quinoline-3-carboxamide
   Show/Hide
C24H25FN6O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0387521
6-[6-[2-(dimethylamino)ethylamino]pyridin-3-yl]-4-[[(1S)-1-(oxan-4-yl)ethyl]amino]cinnoline-3-carboxamide
   Show/Hide
C25H33N7O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0429517
6-[6-(methoxymethyl)pyridin-3-yl]-4-[[(1S)-1-(1-methylpyrazol-3-yl)ethyl]amino]cinnoline-3-carboxamide
   Show/Hide
C22H23N7O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0456091
4-[[(1S)-1-(oxan-4-yl)ethyl]amino]-6-[6-(3-pyrrolidin-1-ylpropoxy)pyridin-3-yl]cinnoline-3-carboxamide
   Show/Hide
C28H36N6O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0456092
6-[6-(methoxymethyl)pyridin-3-yl]-4-[[(1S)-1-(oxan-4-yl)ethyl]amino]cinnoline-3-carboxamide
   Show/Hide
C23H27N5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0456093
4-[[(1S)-1-(1,4-dimethylpyrazol-3-yl)ethyl]amino]-6-[6-(methoxymethyl)pyridin-3-yl]cinnoline-3-carboxamide
   Show/Hide
C23H25N7O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0456094
6-[6-(methoxymethyl)pyridin-3-yl]-N-methyl-4-[[(1S)-1-(oxan-4-yl)ethyl]amino]cinnoline-3-carboxamide
   Show/Hide
C24H29N5O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0474081
4-[[(1S)-1-(1-methylpyrazol-3-yl)ethyl]amino]-6-[6-(3-pyrrolidin-1-ylpropoxy)pyridin-3-yl]cinnoline-3-carboxamide
   Show/Hide
C27H32N8O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0474082
6-[6-[2-(dimethylamino)ethoxy]pyridin-3-yl]-N-methyl-4-[[(1S)-1-(oxan-4-yl)ethyl]amino]cinnoline-3-carboxamide
   Show/Hide
C26H34N6O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0474083
6-[6-[3-(dimethylamino)propoxy]pyridin-3-yl]-4-[[(1S)-1-(1,4-dimethylpyrazol-3-yl)ethyl]amino]-N-methylcinnoline-3-carboxamide
   Show/Hide
C27H34N8O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0545150
6-[6-[3-(dimethylamino)propoxy]pyridin-3-yl]-4-[[(1S)-1-(1,4-dimethylpyrazol-3-yl)ethyl]amino]cinnoline-3-carboxamide
   Show/Hide
C26H32N8O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0545151
4-[[(1S)-1-(1,4-dimethylpyrazol-3-yl)ethyl]amino]-6-[6-(3-pyrrolidin-1-ylpropoxy)pyridin-3-yl]cinnoline-3-carboxamide
   Show/Hide
C28H34N8O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0547086
6-[6-[3-(dimethylamino)propoxy]pyridin-3-yl]-4-[[(1S)-1-(1-methylpyrazol-3-yl)ethyl]amino]cinnoline-3-carboxamide
   Show/Hide
C25H30N8O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0552478
6-[6-[2-(dimethylamino)ethoxy]pyridin-3-yl]-4-[[(1S)-1-(1-methylpyrazol-3-yl)ethyl]amino]cinnoline-3-carboxamide
   Show/Hide
C24H28N8O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0354838
2-amino-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazole-5-carbonitrile
   Show/Hide
C21H23N7O3S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0016003
2-morpholin-4-yl-6-thianthren-1-yl-pyran-4-one
   Show/Hide
C21H17NO3S2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0180775
4-(2-ethylbutylamino)-8-methyl-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C22H26N4O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0180813
2-(6,7-dimethoxyquinazolin-4-yl)-5-pyridin-2-yl-1,2,4-triazol-3-amine
   Show/Hide
C17H15N7O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0234610
4-(2-ethylbutylamino)-6-[4-(methylsulfonylmethyl)phenyl]quinoline-3-carboxamide
   Show/Hide
C24H29N3O3S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0234614
4-(2-ethylbutylamino)-6-[6-(methoxymethyl)pyridin-3-yl]quinoline-3-carboxamide
   Show/Hide
C23H28N4O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0236325
4-(2-ethylbutylamino)-6-[6-(methylsulfonylmethyl)pyridin-3-yl]quinoline-3-carboxamide
   Show/Hide
C23H28N4O3S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0259634
7-fluoro-4-[[(1S)-1-(4-fluoro-1-methylpyrazol-3-yl)ethyl]amino]-6-[6-(methoxymethyl)pyridin-3-yl]quinoline-3-carboxamide
   Show/Hide
C23H22F2N6O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0362298
8-chloro-4-(oxan-4-ylamino)-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C20H19ClN4O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0362300
7-fluoro-6-[6-(methoxymethyl)pyridin-3-yl]-4-[[(1S)-1-(oxan-4-yl)ethyl]amino]quinoline-3-carboxamide
   Show/Hide
C24H27FN4O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0362356
7-chloro-4-(oxan-4-ylamino)-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C20H19ClN4O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0364433
4-(2-ethylbutylamino)-2-methyl-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C22H26N4O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0446981
4-[[(1R)-1-(4-chlorophenyl)ethyl]amino]-6-pyridin-3-ylquinoline-3-carboxylic acid
   Show/Hide
C23H18ClN3O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0446982
4-[[(1R)-1-(4-chlorophenyl)ethyl]amino]-N-methyl-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C24H21ClN4O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0491228
8-fluoro-4-(oxan-4-ylamino)-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C20H19FN4O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0491230
4-(2-ethylbutoxy)-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C21H23N3O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0537595
4-(2-ethylbutylamino)-6-[4-(methoxymethyl)phenyl]quinoline-3-carboxamide
   Show/Hide
C24H29N3O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0537597
7-fluoro-6-[2-fluoro-6-(methoxymethyl)pyridin-3-yl]-4-[[(1S)-1-(1-methylpyrazol-3-yl)ethyl]amino]quinoline-3-carboxamide
   Show/Hide
C23H22F2N6O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0558418
5-fluoro-4-(oxan-4-ylamino)-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C20H19FN4O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0559691
N-[(1R)-1-(4-chlorophenyl)ethyl]-6-pyridin-3-ylquinolin-4-amine
   Show/Hide
C22H18ClN3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0561273
7-fluoro-4-(oxan-4-ylamino)-6-pyridin-3-ylquinoline-3-carboxamide
   Show/Hide
C20H19FN4O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0946565
(R)-6-(2-Benzylazepan-1-yl)-4-morpholinopyridin-2(1H)-one
   Show/Hide
C22H29N3O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0953820
6-((1R,2S,5S)-2-Benzyl-3-azabicyclo[3.1.0]hexan-3-yl)-4-morpholinopyridin-2(1H)-one
   Show/Hide
C21H25N3O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0571634
9-[(3R,4R)-4-fluoropyrrolidin-3-yl]-7-methyl-2-[(7-methylquinolin-6-yl)amino]purin-8-one
   Show/Hide
C20H20FN7O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0257340
3-amino-N,6-diphenylpyrazine-2-carboxamide
   Show/Hide
C17H14N4O
 1
1
IC50 > 2500 nM
   TI
   LI
   LO
   TS
CP0540068
US10772893, Example 41
   Show/Hide
C19H22N4O2
 1
1
IC50 > 3000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0354837
1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
   Show/Hide
C20H24N6O3S
 1
1 IC50 = 1 nM
CP0068244
(3R)-3-methyl-4-[6-(1-methylsulfonylcyclopropyl)-2-(1H-pyrrolo[2,3-c]pyridin-4-yl)pyrimidin-4-yl]morpholine
   Show/Hide
C20H23N5O3S
 1
1 IC50 = 2 nM
CP0068245
N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
   Show/Hide
C21H26N6O3S
 1
1 IC50 = 2 nM
CP0168728
5-fluoro-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
   Show/Hide
C20H23FN6O3S
 1
1 IC50 = 2 nM
CP0157307
4-[2-(1H-indol-4-yl)-6-(2-methylsulfonylpropan-2-yl)pyrimidin-4-yl]morpholine
   Show/Hide
C20H24N4O3S
 1
1 IC50 = 3 nM
CP0076577
1-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]benzimidazol-2-amine
   Show/Hide
C19H22N6O3S
 1
1 IC50 = 3 nM
CP0085622
4-[2-(1H-indol-4-yl)-6-(4-methylsulfonyloxan-4-yl)pyrimidin-4-yl]morpholine
   Show/Hide
C22H26N4O4S
 1
1 IC50 = 4 nM
CP0808811
CERALASERTIB
   Show/Hide
C20H24N6O2S
 2
1 IC50 = 4 nM
2 IC50 = 18 nM
CP0068243
(3R)-4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]-3-methylmorpholine
   Show/Hide
C21H24N4O3S
 2
1 IC50 = 5 nM
2 IC50 = 61 nM
CP0256504
4-[6-[1-(benzenesulfonyl)cyclopropyl]-2-(1H-indol-4-yl)pyrimidin-4-yl]morpholine
   Show/Hide
C25H24N4O3S
 1
1 IC50 = 5 nM
CP0076580
(3R)-3-methyl-4-[6-(1-methylsulfonylcyclopropyl)-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl]morpholine
   Show/Hide
C20H23N5O3S
 1
1 IC50 = 5 nM
CP0076581
4-[6-(1-methylsulfonylcyclopropyl)-2-(1H-pyrrolo[2,3-c]pyridin-4-yl)pyrimidin-4-yl]morpholine
   Show/Hide
C19H21N5O3S
 1
1 IC50 = 5 nM
CP0669285
US8552004, 2.03
   Show/Hide
C21H27N7O2S
 3
1 IC50 = 5.607 nM
2 IC50 = 6 nM
3 IC50 = 7.053 nM
CP0212807
3-amino-6-(4-(tert-butylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C21H22N4O3S
 1
1 IC50 = 6 nM
CP0145081
3-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]-8-oxa-3-azabicyclo[3.2.1]octane
   Show/Hide
C22H24N4O3S
 1
1 IC50 = 7 nM
CP0180289
3-amino-6-(4-(isopropylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C20H20N4O3S
 1
1 IC50 = 8 nM
CP0287648
3-amino-6-(4-((4-hydroxybutan-2-yl)sulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C21H22N4O4S
 1
1 IC50 = 8 nM
CP0102640
4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C20H22N4O3S
 1
1 IC50 = 8 nM
CP0186550
4-[2-(6-methyl-1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C21H24N4O3S
 1
1 IC50 = 8 nM
CP0514493
6-fluoro-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
   Show/Hide
C20H23FN6O3S
 1
1 IC50 = 8 nM
CP0076974
4-[2-(1H-indol-4-yl)-6-(4-methylsulfonylpiperidin-4-yl)pyrimidin-4-yl]morpholine
   Show/Hide
C22H27N5O3S
 1
1 IC50 = 9 nM
CP0021486
3-[3-[4-[dideuterio(methylamino)methyl]phenyl]isoxazol-5-yl]-5-(4-isopropylsulfonylphenyl)pyrazin-2-amine
   Show/Hide
C24H25N5O3S
 2
1 IC50 = 9 nM
2 IC50 = 19 nM
CP0199392
3-amino-6-(4-(sec-butylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C21H22N4O3S
 1
1 IC50 = 10 nM
CP0222476
(R)-3-amino-N-phenyl-6-(4-((tetrahydrofuran-3-yl)sulfonyl)-phenyl)pyrazine-2-carboxamide
   Show/Hide
C21H20N4O4S
 1
1 IC50 = 10 nM
CP0102647
4-fluoro-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
   Show/Hide
C20H23FN6O3S
 1
1 IC50 = 10 nM
CP0314495
(3R)-3-methyl-4-[6-[1-[(S)-methylsulfinyl]cyclopropyl]-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl]morpholine
   Show/Hide
C20H23N5O2S
 1
1 IC50 = 11 nM
CP0050427
3-amino-6-(4-((1-(dimethylamino)propan-2-yl)sulfonyl)-phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C22H25N5O3S
 2
1 IC50 = 12 nM
2 Ki = 6 nM
CP0199334
3-amino-6-(4-(ethylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide
   Show/Hide
C19H18N4O3S
 1
1 IC50 = 12 nM
CP0345264
4-[2-(1H-indol-4-yl)-6-(1-propan-2-ylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C22H26N4O3S
 1
1 IC50 = 13 nM
CP0171816
3-amino-N-phenyl-6-(4-(propylsulfonyl)phenyl)pyrazine-2-carboxamide
   Show/Hide
C20H20N4O3S
 1
1 IC50 = 14 nM
CP0076584
N-[1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-yl]acetamide
   Show/Hide
C22H26N6O4S
 1
1 IC50 = 14 nM
CP0130832
4-[2-(6-fluoro-1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C20H21FN4O3S
 1
1 IC50 = 15 nM
CP0130830
4-[2-(6-chloro-1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C20H21ClN4O3S
 1
1 IC50 = 16 nM
CP0168854
(3R)-3-methyl-4-[6-[1-[(R)-methylsulfinyl]cyclopropyl]-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl]morpholine
   Show/Hide
C20H23N5O2S
 1
1 IC50 = 16 nM
CP0249202
4-chloro-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
   Show/Hide
C20H23ClN6O3S
 1
1 IC50 = 17 nM
CP0565273
4-[4-(3,6-dihydro-2H-pyran-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]-1H-indole
   Show/Hide
C21H21N3O3S
 1
1 IC50 = 18 nM
CP0249222
5-chloro-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
   Show/Hide
C20H23ClN6O3S
 1
1 IC50 = 21 nM
CP0304424
4-[2-(6-methoxy-1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C21H24N4O4S
 1
1 IC50 = 23 nM
CP0199330
3-amino-N-phenyl-6-(4-(piperidine-1-carbonyl)phenyl)pyrazine-2-carboxamide
   Show/Hide
C23H23N5O2
 1
1 IC50 = 26 nM
CP0265453
4-[2-(2-methyl-1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C21H24N4O3S
 1
1 IC50 = 28 nM
CP0085620
4-[2-(1H-indol-4-yl)-6-(methylsulfonylmethyl)pyrimidin-4-yl]morpholine
   Show/Hide
C18H20N4O3S
 1
1 IC50 = 30 nM
CP0076973
4-[2-(1H-indol-4-yl)-6-(1-pyridin-2-ylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
   Show/Hide
C24H23N5O3S
 1
1 IC50 = 33 nM
CP0130834
4-[2-(1H-indol-4-yl)-6-[1-(oxan-4-ylsulfonyl)cyclopropyl]pyrimidin-4-yl]morpholine
   Show/Hide
C24H28N4O4S
 1
1 IC50 = 33 nM
CP0130829
(3S)-4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]-3-methylmorpholine
   Show/Hide
C21H24N4O3S
 1
1 IC50 = 34 nM
CP0404754
4-[6-(1-methylsulfonylcyclopropyl)-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl]morpholine
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C19H21N5O3S
 1
1 IC50 = 37 nM
CP0333713
4-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]-1H-indole-6-carboxamide
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C21H23N5O4S
 1
1 IC50 = 41 nM
CP0310474
4-[2-(1H-indol-4-yl)-6-(1-piperidin-4-ylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
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C24H29N5O3S
 1
1 IC50 = 46 nM
CP0291454
3-amino-6-(3-chloro-4-(dimethylcarbamoyl)phenyl)-N-phenylpyrazine-2-carboxamide
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C20H18ClN5O2
 1
1 IC50 = 48 nM
CP0050429
3-amino-6-(4-(dimethylcarbamoyl)phenyl)-N-phenylpyrazine-2-carboxamide
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C20H19N5O2
 1
1 IC50 = 54 nM
CP0271874
3-amino-N-phenyl-6-(4-(pyrrolidine-1-carbonyl)phenyl)-pyrazine-2-carboxamide
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C22H21N5O2
 1
1 IC50 = 54 nM
CP0160334
3-amino-6-(4-(methylsulfinyl)phenyl)-N-phenylpyrazine-2-carboxamide
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C18H16N4O2S
 1
1 IC50 = 56 nM
CP0333714
4-[2-(1H-indol-4-yl)-6-(1-methyl-4-methylsulfonylpiperidin-4-yl)pyrimidin-4-yl]morpholine
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C23H29N5O3S
 1
1 IC50 = 61 nM
CP0130833
4-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]-1H-indole-6-carbonitrile
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C21H21N5O3S
 1
1 IC50 = 66 nM
CP0533485
7-fluoro-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
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C20H23FN6O3S
 1
1 IC50 = 90 nM
CP0341198
3-amino-6-(4-(azetidine-1-carbonyl)phenyl)-N-phenylpyrazine-2-carboxamide
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C21H19N5O2
 1
1 IC50 = 100 nM
CP0145086
4-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]-1,3-dihydroindol-2-one
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C20H22N4O4S
 1
1 IC50 = 120 nM
CP0315929
4-[2-(1H-indazol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
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C19H21N5O3S
 1
1 IC50 = 130 nM
CP0076582
N-methyl-4-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]-1H-indole-6-carboxamide
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C22H25N5O4S
 1
1 IC50 = 140 nM
CP0130828
(3R)-3-ethyl-4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
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C22H26N4O3S
 1
1 IC50 = 170 nM
CP0193495
4-[2-(1H-indol-7-yl)-6-(methylsulfonylmethyl)pyrimidin-4-yl]morpholine
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C18H20N4O3S
 1
1 IC50 = 180 nM
CP0314494
4-[2-(1H-benzimidazol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
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C19H21N5O3S
 1
1 IC50 = 180 nM
CP0256503
4-[2-(7-methyl-1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
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C21H24N4O3S
 1
1 IC50 = 220 nM
CP0136765
4-methoxy-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
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C21H26N6O4S
 1
1 IC50 = 270 nM
CP0193494
4-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]-1H-indole-2-carbonitrile
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C21H21N5O3S
 1
1 IC50 = 300 nM
CP0345263
4-[6-(1-methylsulfonylcyclopropyl)-2-phenylpyrimidin-4-yl]morpholine
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C18H21N3O3S
 1
1 IC50 = 360 nM
CP0444138
5-methoxy-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazol-2-amine
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C21H26N6O4S
 1
1 IC50 = 550 nM
CP0257340
3-amino-N,6-diphenylpyrazine-2-carboxamide
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C17H14N4O
 1
1 IC50 = 620 nM
CP0315928
N,N-dimethyl-4-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]-1H-indole-6-carboxamide
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C23H27N5O4S
 1
1 IC50 = 720 nM
CP0085621
4-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]-1H-indole-2-carboxamide
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C21H23N5O4S
 1
1 IC50 = 1100 nM
CP0315930
3-[4-(1-methylsulfonylcyclopropyl)-6-morpholin-4-ylpyrimidin-2-yl]aniline
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C18H22N4O3S
 1
1 IC50 = 1200 nM
CP0333715
4-[2-(1H-indol-6-yl)-6-(methylsulfonylmethyl)pyrimidin-4-yl]morpholine
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C18H20N4O3S
 1
1 IC50 = 1500 nM
CP0123538
4-[2-(1H-indol-5-yl)-6-(methylsulfonylmethyl)pyrimidin-4-yl]morpholine
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C18H20N4O3S
 1
1 IC50 = 1700 nM
CP0265455
4-[2-(1-methylindol-4-yl)-6-(methylsulfonylmethyl)pyrimidin-4-yl]morpholine
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C19H22N4O3S
 1
1 IC50 = 3300 nM
CP0354838
2-amino-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-(1-methylsulfonylcyclopropyl)pyrimidin-2-yl]benzimidazole-5-carbonitrile
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C21H23N7O3S
 1
1 IC50 = 4000 nM
CP0287511
3,4,5,19-tetramethoxy-9,10-dimethyl-15,17-dioxatetracyclo[10.7.0.02,7.014,18]nonadeca-1(19),2,4,6,12,14(18)-hexaene
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C23H28O6
 1
1 IC50 = 7200 nM
CP0145082
4-[2-(3-methyl-1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)pyrimidin-4-yl]morpholine
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C21H24N4O3S
 1
1 IC50 = 14000 nM
CP0016003
2-morpholin-4-yl-6-thianthren-1-yl-pyran-4-one
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C21H17NO3S2
 1
1 IC50 > 100000 nM
CP0238623
US8846917, I-1
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C21H20N6O2S
 1
1 Ki = 6 nM
CP0639539
2-[(3R)-3-Methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-5-yl)-1,7-naphthyridine
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C20H21N7O
 1
1 Ki = 7 nM
CP0141550
3-(3-phenyl-4,5-dihydro-1,2-oxazol-5-yl)-5-(4-propan-2-ylsulfonylphenyl)pyrazin-2-amine
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C22H22N4O3S
 1
1 Ki = 90 nM
Clinical Information about the Protein
Target 1 ( Serine/threonine-protein kinase ATR (FRP1) )
Target Type Clinical trial Target
Disease 3 Target-related Diseases  3
1 Small-cell lung cancer [ICD-11: 2C25.Y]
2 Lymphoma [ICD-11: 2A80-2A86]
3 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Clinical Trial Drug(s) 4 Clinical Trial Drugs  4
1 AZD6738 Phase 2
Small-cell lung cancer
2 BAY1895344 Phase 1
Lymphoma
3 M4344 Phase 1
Solid tumour/cancer
4 VX-970 Phase 1
Solid tumour/cancer
Investigative Drug(s) 1 Investigative Drug  1
1 VE-821 Investigative
Solid tumour/cancer