General Information of the Protein
Protein ID
PT04520
Protein Name
Serine/threonine-protein kinase SMG1
Secondarily
Protein Name
Lambda/iota protein kinase C-interacting protein
Nonsense mediated mRNA decay-associated PI3K-related kinase SMG1
Gene Name
SMG1
Secondarily
Gene Name
ATX
KIAA0421
LIP
Sequence
MSRRAPGSRLSSGGGGGGTKYPRSWNDWQPRTDSASADPDNLKYSSSRDRGGSSSYGLQPSNSAVVSRQRHDDTRVHADIQNDEKGGYSVNGGSGENTYGRKSLGQELRVNNVTSPEFTSVQHGSRALATKDMRKSQERSMSYSDESRLSNLLRRITREDDRDRRLATVKQLKEFIQQPENKLVLVKQLDNILAAVHDVLNESSKLLQELRQEGACCLGLLCASLSYEAEKIFKWIFSKFSSSAKDEVKLLYLCATYKALETVGEKKAFSSVMQLVMTSLQSILENVDTPELLCKCVKCILLVARCYPHIFSTNFRDTVDILVGWHIDHTQKPSLTQQVSGWLQSLEPFWVADLAFSTTLLGQFLEDMEAYAEDLSHVASGESVDEDVPPPSVSLPKLAALLRVFSTVVRSIGERFSPIRGPPITEAYVTDVLYRVMRCVTAANQVFFSEAVLTAANECVGVLLGSLDPSMTIHCDMVITYGLDQLENCQTCGTDYIISVLNLLTLIVEQINTKLPSSFVEKLFIPSSKLLFLRYHKEKEVVAVAHAVYQAVLSLKNIPVLETAYKLILGEMTCALNNLLHSLQLPEACSEIKHEAFKNHVFNVDNAKFVVIFDLSALTTIGNAKNSLIGMWALSPTVFALLSKNLMIVHSDLAVHFPAIQYAVLYTLYSHCTRHDHFISSSLSSSSPSLFDGAVISTVTTATKKHFSIILNLLGILLKKDNLNQDTRKLLMTWALEAAVLMKKSETYAPLFSLPSFHKFCKGLLANTLVEDVNICLQACSSLHALSSSLPDDLLQRCVDVCRVQLVHSGTRIRQAFGKLLKSIPLDVVLSNNNHTEIQEISLALRSHMSKAPSNTFHPQDFSDVISFILYGNSHRTGKDNWLERLFYSCQRLDKRDQSTIPRNLLKTDAVLWQWAIWEAAQFTVLSKLRTPLGRAQDTFQTIEGIIRSLAAHTLNPDQDVSQWTTADNDEGHGNNQLRLVLLLQYLENLEKLMYNAYEGCANALTSPPKVIRTFFYTNRQTCQDWLTRIRLSIMRVGLLAGQPAVTVRHGFDLLTEMKTTSLSQGNELEVTIMMVVEALCELHCPEAIQGIAVWSSSIVGKNLLWINSVAQQAEGRFEKASVEYQEHLCAMTGVDCCISSFDKSVLTLANAGRNSASPKHSLNGESRKTVLSKPTDSSPEVINYLGNKACECYISIADWAAVQEWQNAIHDLKKSTSSTSLNLKADFNYIKSLSSFESGKFVECTEQLELLPGENINLLAGGSKEKIDMKKLLPNMLSPDPRELQKSIEVQLLRSSVCLATALNPIEQDQKWQSITENVVKYLKQTSRIAIGPLRLSTLTVSQSLPVLSTLQLYCSSALENTVSNRLSTEDCLIPLFSEALRSCKQHDVRPWMQALRYTMYQNQLLEKIKEQTVPIRSHLMELGLTAAKFARKRGNVSLATRLLAQCSEVQLGKTTTAQDLVQHFKKLSTQGQVDEKWGPELDIEKTKLLYTAGQSTHAMEMLSSCAISFCKSVKAEYAVAKSILTLAKWIQAEWKEISGQLKQVYRAQHQQNFTGLSTLSKNILTLIELPSVNTMEEEYPRIESESTVHIGVGEPDFILGQLYHLSSVQAPEVAKSWAALASWAYRWGRKVVDNASQGEGVRLLPREKSEVQNLLPDTITEEEKERIYGILGQAVCRPAGIQDEDITLQITESEDNEEDDMVDVIWRQLISSCPWLSELDESATEGVIKVWRKVVDRIFSLYKLSCSAYFTFLKLNAGQIPLDEDDPRLHLSHRVEQSTDDMIVMATLRLLRLLVKHAGELRQYLEHGLETTPTAPWRGIIPQLFSRLNHPEVYVRQSICNLLCRVAQDSPHLILYPAIVGTISLSSESQASGNKFSTAIPTLLGNIQGEELLVSECEGGSPPASQDSNKDEPKSGLNEDQAMMQDCYSKIVDKLSSANPTMVLQVQMLVAELRRVTVLWDELWLGVLLQQHMYVLRRIQQLEDEVKRVQNNNTLRKEEKIAIMREKHTALMKPIVFALEHVRSITAAPAETPHEKWFQDNYGDAIENALEKLKTPLNPAKPGSSWIPFKEIMLSLQQRAQKRASYILRLEEISPWLAAMTNTEIALPGEVSARDTVTIHSVGGTITILPTKTKPKKLLFLGSDGKSYPYLFKGLEDLHLDERIMQFLSIVNTMFATINRQETPRFHARHYSVTPLGTRSGLIQWVDGATPLFGLYKRWQQREAALQAQKAQDSYQTPQNPGIVPRPSELYYSKIGPALKTVGLSLDVSRRDWPLHVMKAVLEELMEATPPNLLAKELWSSCTTPDEWWRVTQSYARSTAVMSMVGYIIGLGDRHLDNVLIDMTTGEVVHIDYNVCFEKGKSLRVPEKVPFRMTQNIETALGVTGVEGVFRLSCEQVLHIMRRGRETLLTLLEAFVYDPLVDWTAGGEAGFAGAVYGGGGQQAESKQSKREMEREITRSLFSSRVAEIKVNWFKNRDEMLVVLPKLDGSLDEYLSLQEQLTDVEKLQGKLLEEIEFLEGAEGVDHPSHTLQHRYSEHTQLQTQQRAVQEAIQVKLNEFEQWITHYQAAFNNLEATQLASLLQEISTQMDLGPPSYVPATAFLQNAGQAHLISQCEQLEGEVGALLQQRRSVLRGCLEQLHHYATVALQYPKAIFQKHRIEQWKTWMEELICNTTVERCQELYRKYEMQYAPQPPPTVCQFITATEMTLQRYAADINSRLIRQVERLKQEAVTVPVCEDQLKEIERCIKVFLHENGEEGSLSLASVIISALCTLTRRNLMMEGAASSAGEQLVDLTSRDGAWFLEELCSMSGNVTCLVQLLKQCHLVPQDLDIPNPMEASETVHLANGVYTSLQELNSNFRQIIFPEALRCLMKGEYTLESMLHELDGLIEQTTDGVPLQTLVESLQAYLRNAAMGLEEETHAHYIDVARLLHAQYGELIQPRNGSVDETPKMSAGQMLLVAFDGMFAQVETAFSLLVEKLNKMEIPIAWRKIDIIREARSTQVNFFDDDNHRQVLEEIFFLKRLQTIKEFFRLCGTFSKTLSGSSSLEDQNTVNGPVQIVNVKTLFRNSCFSEDQMAKPIKAFTADFVRQLLIGLPNQALGLTLCSFISALGVDIIAQVEAKDFGAESKVSVDDLCKKAVEHNIQIGKFSQLVMNRATVLASSYDTAWKKHDLVRRLETSISSCKTSLQRVQLHIAMFQWQHEDLLINRPQAMSVTPPPRSAILTSMKKKLHTLSQIETSIATVQEKLAALESSIEQRLKWAGGANPALAPVLQDFEATIAERRNLVLKESQRASQVTFLCSNIIHFESLRTRTAEALNLDAALFELIKRCQQMCSFASQFNSSVSELELRLLQRVDTGLEHPIGSSEWLLSAHKQLTQDMSTQRAIQTEKEQQIETVCETIQNLVDNIKTVLTGHNRQLGDVKHLLKAMAKDEEAALADGEDVPYENSVRQFLGEYKSWQDNIQTVLFTLVQAMGQVRSQEHVEMLQEITPTLKELKTQSQSIYNNLVSFASPLVTDATNECSSPTSSATYQPSFAAAVRSNTGQKTQPDVMSQNARKLIQKNLATSADTPPSTVPGTGKSVACSPKKAVRDPKTGKAVQERNSYAVSVWKRVKAKLEGRDVDPNRRMSVAEQVDYVIKEATNLDNLAQLYEGWTAWV
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
Function
Serine/threonine protein kinase involved in both mRNA surveillance and genotoxic stress response pathways. Recognizes the substrate consensus sequence [ST]-Q. Plays a central role in nonsense-mediated decay (NMD) of mRNAs containing premature stop codons by phosphorylating UPF1/RENT1. Recruited by release factors to stalled ribosomes together with SMG8 and SMG9 (forming the SMG1C protein kinase complex), and UPF1 to form the transient SURF (SMG1-UPF1-eRF1-eRF3) complex. In EJC-dependent NMD, the SURF complex associates with the exon junction complex (EJC) through UPF2 and allows the formation of an UPF1-UPF2-UPF3 surveillance complex which is believed to activate NMD. Also acts as a genotoxic stress-activated protein kinase that displays some functional overlap with ATM. Can phosphorylate p53/TP53 and is required for optimal p53/TP53 activation after cellular exposure to genotoxic stress. Its depletion leads to spontaneous DNA damage and increased sensitivity to ionizing radiation (IR). May activate PRKCI but not PRKCZ.
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Uniprot ID
Primary ID:
Q96Q15

Secondarily ID:
O43305
Q13284
Q8NFX2
Q96QV0
Q96RW3
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Ensembl ID
ENSG00000157106
HGNC ID
HGNC:30045
Subcellular Location
Nucleus
Cytoplasm
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0178303
1-methyl-3-[4-[4-[2-[4-methyl-3-(methylsulfamoyl)anilino]pyrimidin-4-yl]pyridin-2-yl]phenyl]urea
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C25H25N7O3S
 1
1
IC50 < 0.05 nM
   TI
   LI
   LO
   TS
CP0178304
1-methyl-3-[4-[4-[2-(3-sulfamoylanilino)pyrimidin-4-yl]pyridin-2-yl]phenyl]urea
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C23H21N7O3S
 1
1
IC50 < 0.05 nM
   TI
   LI
   LO
   TS
CP0186436
1-methyl-3-[4-[4-[2-(4-methyl-3-sulfamoylanilino)pyrimidin-4-yl]pyridin-2-yl]phenyl]urea
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C24H23N7O3S
 1
1
IC50 < 0.05 nM
   TI
   LI
   LO
   TS
CP0200088
1-[4-[4-[2-[4-chloro-3-(dimethylsulfamoyl)anilino]pyrimidin-4-yl]pyridin-2-yl]phenyl]-3-methylurea
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C25H24ClN7O3S
 1
1
IC50 < 0.05 nM
   TI
   LI
   LO
   TS
CP0247761
1-[4-[4-[2-[4-chloro-3-(methylsulfamoyl)anilino]pyrimidin-4-yl]pyridin-2-yl]phenyl]-3-methylurea
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C24H22ClN7O3S
 1
1
IC50 < 0.05 nM
   TI
   LI
   LO
   TS
CP0253446
1-[4-[4-[2-[3-(dimethylsulfamoyl)-4-methylanilino]pyrimidin-4-yl]pyridin-2-yl]phenyl]-3-methylurea
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C26H27N7O3S
 1
1
IC50 < 0.05 nM
   TI
   LI
   LO
   TS
CP0178296
1-methyl-3-[4-[4-[2-[3-(methylsulfamoyl)anilino]pyrimidin-4-yl]pyridin-2-yl]phenyl]urea
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C24H23N7O3S
 1
1
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
CP0120603
1-[4-[4-[2-[4-chloro-3-(diethylsulfamoyl)anilino]pyrimidin-4-yl]pyridin-2-yl]phenyl]-3-methylurea
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C27H28ClN7O3S
 1
1
IC50 = 0.11 nM
   TI
   LI
   LO
   TS
CP0178300
1-[4-[4-[2-[3-(diethylsulfamoyl)anilino]pyrimidin-4-yl]pyridin-2-yl]phenyl]-3-methylurea
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C27H29N7O3S
 1
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
CP0191346
1-[4-[4-[2-[3-(diethylsulfamoyl)-4-methylanilino]pyrimidin-4-yl]pyridin-2-yl]phenyl]-3-methylurea
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C28H31N7O3S
 1
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
CP0197606
3-[[4-(2-piperidin-1-ylpyridin-4-yl)pyrimidin-2-yl]amino]benzenesulfonamide
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C20H22N6O2S
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0252578
3-[[4-[2-(diethylamino)pyridin-4-yl]pyrimidin-2-yl]amino]benzenesulfonamide
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C19H22N6O2S
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0252576
3-[[4-[2-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)pyridin-4-yl]pyrimidin-2-yl]amino]benzenesulfonamide
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C21H22N6O3S
 1
1
IC50 = 6 nM
   TI
   LI
   LO
   TS
CP0252577
3-[[4-(2-morpholin-4-ylpyridin-4-yl)pyrimidin-2-yl]amino]benzenesulfonamide
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C19H20N6O3S
 1
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
CP0178274
3-[[4-[2-(3-hydroxypropylamino)pyridin-4-yl]pyrimidin-2-yl]amino]benzenesulfonamide
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C18H20N6O3S
 1
1
IC50 = 22 nM
   TI
   LI
   LO
   TS
CP0282623
3-[[4-[2-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)pyridin-4-yl]pyrimidin-2-yl]amino]benzenesulfonamide
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C21H22N6O3S
 1
1
IC50 = 25 nM
   TI
   LI
   LO
   TS
CP0087616
3-[[4-(2-morpholin-4-ylpyridin-4-yl)pyrimidin-2-yl]amino]benzonitrile
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C20H18N6O
 1
1
IC50 = 80 nM
   TI
   LI
   LO
   TS
CP0004084
3-[[4-[2-(3-chloroanilino)-4-pyrimidinyl]-2-pyridinyl]amino]-1-propanol
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C18H18ClN5O
 1
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0087619
4-(2-morpholin-4-ylpyridin-4-yl)-N-[3-(trifluoromethyl)phenyl]pyrimidin-2-amine
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C20H18F3N5O
 1
1
IC50 = 250 nM
   TI
   LI
   LO
   TS
CP0191344
N-(3-chlorophenyl)-4-(2-morpholin-4-ylpyridin-4-yl)pyrimidin-2-amine
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C19H18ClN5O
 1
1
IC50 = 280 nM
   TI
   LI
   LO
   TS
CP0120601
3-[[4-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]pyrimidin-2-yl]amino]benzenesulfonamide
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C20H23N7O2S
 1
1
IC50 = 310 nM
   TI
   LI
   LO
   TS
CP0178298
N-(3-methylphenyl)-4-(2-morpholin-4-ylpyridin-4-yl)pyrimidin-2-amine
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C20H21N5O
 1
1
IC50 = 330 nM
   TI
   LI
   LO
   TS
CP0191343
4-[[4-(2-morpholin-4-ylpyridin-4-yl)pyrimidin-2-yl]amino]benzenesulfonamide
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C19H20N6O3S
 1
1
IC50 = 370 nM
   TI
   LI
   LO
   TS
CP0192166
4-[[4-[3-(piperidine-1-carbonyl)phenyl]pyrimidin-2-yl]amino]benzenesulfonamide
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C22H23N5O3S
 1
1
IC50 = 450 nM
   TI
   LI
   LO
   TS
CP0087618
N-(4-chlorophenyl)-4-(2-morpholin-4-ylpyridin-4-yl)pyrimidin-2-amine
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C19H18ClN5O
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0247762
N-(3-methoxyphenyl)-4-(2-morpholin-4-ylpyridin-4-yl)pyrimidin-2-amine
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C20H21N5O2
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0247763
4-(2-morpholin-4-ylpyridin-4-yl)-N-phenylpyrimidin-2-amine
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C19H19N5O
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS