General Information of the Protein
Protein ID
PT00850
Protein Name
Mitogen-activated protein kinase 1
Secondarily
Protein Name
ERT1
Extracellular signal-regulated kinase 2
MAP kinase isoform p42
Mitogen-activated protein kinase 2
Gene Name
MAPK1
Secondarily
Gene Name
ERK2
PRKM1
PRKM2
Sequence
MAAAAAAGAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNVNKVRVAIKKISPFEHQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQHLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHKRIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
CMGC protein kinase group
>
CMGC protein kinase MAPK family
>
CMGC protein kinase ERK subfamily
Function
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. MAPK1/ERK2 and MAPK3/ERK1 are the 2 MAPKs which play an important role in the MAPK/ERK cascade. They participate also in a signaling cascade initiated by activated KIT and KITLG/SCF. Depending on the cellular context, the MAPK/ERK cascade mediates diverse biological functions such as cell growth, adhesion, survival and differentiation through the regulation of transcription, translation, cytoskeletal rearrangements. The MAPK/ERK cascade also plays a role in initiation and regulation of meiosis, mitosis, and postmitotic functions in differentiated cells by phosphorylating a number of transcription factors. About 160 substrates have already been discovered for ERKs. Many of these substrates are localized in the nucleus, and seem to participate in the regulation of transcription upon stimulation. However, other substrates are found in the cytosol as well as in other cellular organelles, and those are responsible for processes such as translation, mitosis and apoptosis. Moreover, the MAPK/ERK cascade is also involved in the regulation of the endosomal dynamics, including lysosome processing and endosome cycling through the perinuclear recycling compartment (PNRC); as well as in the fragmentation of the Golgi apparatus during mitosis. The substrates include transcription factors (such as ATF2, BCL6, ELK1, ERF, FOS, HSF4 or SPZ1), cytoskeletal elements (such as CANX, CTTN, GJA1, MAP2, MAPT, PXN, SORBS3 or STMN1), regulators of apoptosis (such as BAD, BTG2, CASP9, DAPK1, IER3, MCL1 or PPARG), regulators of translation (such as EIF4EBP1 and FXR1) and a variety of other signaling-related molecules (like ARHGEF2, DCC, FRS2 or GRB10). Protein kinases (such as RAF1, RPS6KA1/RSK1, RPS6KA3/RSK2, RPS6KA2/RSK3, RPS6KA6/RSK4, SYK, MKNK1/MNK1, MKNK2/MNK2, RPS6KA5/MSK1, RPS6KA4/MSK2, MAPKAPK3 or MAPKAPK5) and phosphatases (such as DUSP1, DUSP4, DUSP6 or DUSP16) are other substrates which enable the propagation the MAPK/ERK signal to additional cytosolic and nuclear targets, thereby extending the specificity of the cascade. Mediates phosphorylation of TPR in response to EGF stimulation. May play a role in the spindle assembly checkpoint. Phosphorylates PML and promotes its interaction with PIN1, leading to PML degradation. Phosphorylates CDK2AP2 (By similarity).
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Uniprot ID
Primary ID:
P28482

Secondarily ID:
A8CZ64
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Ensembl ID
ENSG00000100030
HGNC ID
HGNC:6871
Subcellular Location
Cytoplasm
Cytoskeleton
Spindle
Nucleus
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
Cytoplasm
Membrane
Caveola
Cell junction
Focal adhesion
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: CL000045 , A-375
Compound ID Compound Name Compound Formula
CP0072527
SCH772984
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C33H33N9O2
 2
1
IC50 = 4 nM
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2
IC50 = 20 nM
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CP0674370
N-(4-((5-chloro-2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)amino)pyridin-3-yl)acrylamide
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C17H19ClN6O2
 1
1
IC50 = 6.7 nM
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CP0096302
(3R)-3-methyl-7-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-2-[(6-methylpyridin-2-yl)methyl]-3,4-dihydropyrrolo[1,2-a]pyrazin-1-one
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C24H26N8O
 2
1
IC50 = 12 nM
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2
IC50 = 62 nM
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CP0667349
N-(2-((5-chloro-2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)amino)phenyl)acrylamide
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C18H20ClN5O2
 1
1
IC50 = 19 nM
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CP0072523
N-[2-[[2-(oxan-4-ylamino)-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide
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C19H20F3N5O2
 1
1
IC50 = 22 nM
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CP0180353
(6R)-5-(2-methoxyethyl)-6-methyl-2-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C20H25N7O2
 2
1
IC50 = 30 nM
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2
IC50 = 130 nM
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CP0649592
ULIXERTINIB
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C21H22Cl2N4O2
 2
1
IC50 = 31 nM
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2
IC50 = 4100 nM
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CP0676203
N-(2-((5-chloro-2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)amino)phenyl)acrylamide
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C17H16ClN7O
 1
1
IC50 = 48 nM
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CP0318103
N-[2-[[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]amino]phenyl]prop-2-enamide
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C18H19N7O
 1
1
IC50 = 66 nM
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CP0109825
5-benzyl-1-methyl-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydropyrrolo[3,2-c]pyridin-4-one
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C24H27N5O2
 2
1
IC50 = 69 nM
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2
IC50 = 9300 nM
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CP0115031
N-[2-[[5-chloro-2-[[4-(dimethylamino)cyclohexyl]amino]pyrimidin-4-yl]amino]phenyl]prop-2-enamide
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C21H27ClN6O
 1
1
IC50 = 72 nM
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CP0241368
5-benzyl-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C23H25N5O2
 2
1
IC50 = 80 nM
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2
IC50 = 220 nM
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CP0095473
US10525036, Example GDC-0994
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C21H18ClFN6O2
 2
1
IC50 = 86 nM
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2
IC50 = 140 nM
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CP0109840
5-[(1S)-2-hydroxy-1-phenylethyl]-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C24H27N5O3
 2
1
IC50 = 100 nM
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2
IC50 = 3500 nM
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CP0364731
7-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-2-[(6-methylpyridin-2-yl)methyl]-3,4-dihydropyrrolo[1,2-a]pyrazin-1-one
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C23H24N8O
 2
1
IC50 = 110 nM
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2
IC50 > 1000 nM
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CP0667326
N-(3-(pyridin-4-yl)-1H-indazol-5-yl)ethenesulfonamide
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C14H12N4O2S
 1
1
IC50 = 120 nM
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CP0721177
N-(2-((5-chloro-2-((tetrahydro-2H-pyran-4-yl)amino)pyridin-4-yl)amino)phenyl)acrylamide
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C19H21ClN4O2
 1
1
IC50 = 120 nM
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CP0326387
(3R)-2-(2-methoxyethyl)-3-methyl-7-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-3,4-dihydropyrrolo[1,2-a]pyrazin-1-one
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C20H25N7O2
 2
1
IC50 = 130 nM
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2
IC50 = 22000 nM
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CP0408200
5-[(1S)-1-(3-chloro-4-fluorophenyl)-2-hydroxyethyl]-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C24H25ClFN5O3
 2
1
IC50 = 130 nM
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2
IC50 = 3300 nM
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CP0180385
(3S)-3-methyl-7-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-2-[(6-methylpyridin-2-yl)methyl]-3,4-dihydropyrrolo[1,2-a]pyrazin-1-one
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C24H26N8O
 2
1
IC50 = 140 nM
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2
IC50 > 30000 nM
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CP0241366
2-[2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one
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C22H25N7O
 2
1
IC50 = 160 nM
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2
IC50 = 570 nM
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CP0072522
N-[2-[[5-methyl-2-(oxan-4-ylamino)pyrimidin-4-yl]amino]phenyl]prop-2-enamide
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C19H23N5O2
 1
1
IC50 = 170 nM
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CP0180354
(6S)-5-(2-methoxyethyl)-6-methyl-2-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C20H25N7O2
 2
1
IC50 = 200 nM
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2
IC50 = 8100 nM
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CP0664804
N-(tetrahydro-2H-pyran-4-yl)-7-(vinylsulfonyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-amine
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C14H20N4O3S
 1
1
IC50 = 240 nM
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CP0326385
5-[(1S)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C24H25ClFN5O3
 2
1
IC50 = 250 nM
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2
IC50 > 30000 nM
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CP0180352
(3S)-2-(2-methoxyethyl)-3-methyl-7-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-3,4-dihydropyrrolo[1,2-a]pyrazin-1-one
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C20H25N7O2
 2
1
IC50 = 310 nM
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2
IC50 = 380 nM
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CP0241372
2-(2-methoxyethyl)-7-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-3,4-dihydropyrrolo[1,2-a]pyrazin-1-one
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C19H23N7O2
 2
1
IC50 = 310 nM
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2
IC50 > 30000 nM
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CP0085671
1-methyl-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-5H-pyrrolo[3,2-c]pyridin-4-one
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C17H21N5O2
 2
1
IC50 = 340 nM
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2
IC50 = 570 nM
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CP0072557
5-[(6-methylpyridin-2-yl)methyl]-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C23H26N6O2
 2
1
IC50 = 370 nM
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2
IC50 = 9400 nM
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CP0733191
3-(2-methylpyridin-4-yl)-5-(vinylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
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C14H16N4O2S
 1
1
IC50 = 380 nM
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CP0180387
5-(2-methoxyethyl)-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C19H25N5O3
 2
1
IC50 = 600 nM
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2
IC50 = 18000 nM
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CP0109841
2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one
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C16H19N5O2
 2
1
IC50 = 940 nM
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2
IC50 = 960 nM
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CP0241369
(6S)-5-(2-methoxyethyl)-6-methyl-2-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C19H23N7O2
 2
1
IC50 = 1100 nM
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2
IC50 = 29000 nM
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CP0241373
7-[2-(oxan-4-ylamino)pyrimidin-4-yl]-3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one
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C16H19N5O2
 2
1
IC50 = 1100 nM
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2
IC50 = 25000 nM
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CP0072317
(6R)-5-(2-methoxyethyl)-6-methyl-2-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C19H23N7O2
 2
1
IC50 = 1200 nM
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2
IC50 = 11700 nM
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CP0328082
5-(2-methoxyethyl)-1-methyl-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydropyrrolo[3,2-c]pyridin-4-one
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C20H27N5O3
 2
1
IC50 = 1400 nM
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2
IC50 = 24000 nM
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CP0674360
(3S,5E,8R,9S,11E)-8,9,16-trihydroxy-14-methoxy-3-methyl-3,4,9,10-tetrahydro-1H-benzo[c][1]oxacyclotetradecine-1,7(8H)-dione
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C19H22O7
 1
1
IC50 = 1600 nM
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CP0109828
5-(2-methoxyethyl)-2-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C18H21N7O2
 2
1
IC50 = 1600 nM
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2
IC50 > 30000 nM
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CP0241367
5-methyl-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C17H21N5O2
 2
1
IC50 = 1900 nM
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2
IC50 > 10000 nM
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CP0725021
4-fluoro-N-methyl-2-(2-(tetrahydro-2H-pyran-4-ylamino)-5-(trifluoromethyl)pyridin-4-ylamino)benzamide
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C19H20F4N4O2
 1
1
IC50 = 2100 nM
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CP0180390
5-(2-methoxyethyl)-1-methyl-2-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-6,7-dihydropyrrolo[3,2-c]pyridin-4-one
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C19H23N7O2
 2
1
IC50 = 4700 nM
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2
IC50 > 10000 nM
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CP0788339
2-(5-chloro-2-(tetrahydro-2H-pyran-4-ylamino)pyridin-4-ylamino)-N-methylbenzamide
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C18H21ClN4O2
 1
1
IC50 = 7500 nM
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CP0733193
2-(2-(1,3-dimethyl-1H-pyrazol-5-ylamino)-5-(trifluoromethyl)pyridin-4-ylamino)-4-fluoro-N-methylbenzamide
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C19H18F4N6O
 1
1
IC50 = 8700 nM
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CP0733190
N-(3-(pyridin-4-yl)-1H-indazol-5-yl)ethanesulfonamide
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C14H14N4O2S
 1
1
IC50 = 10000 nM
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CP0733192
7-(ethylsulfonyl)-N-(tetrahydro-2H-pyran-4-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-amine
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C14H22N4O3S
 1
1
IC50 = 10000 nM
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CP0806313
N-(2-(5-chloro-2-(tetrahydro-2H-pyran-4-ylamino)pyrimidin-4-ylamino)phenyl)propionamide
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C18H22ClN5O2
 1
1
IC50 > 30000 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0649592
ULIXERTINIB
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C21H22Cl2N4O2
 6
1 IC50 = 0.03 nM
2 IC50 < 0.3 nM
3 IC50 = 10.6 nM
4 Kd = 0.3162 nM
5 Kd = 10 nM
6 Ki = 0.04 nM
CP0041086
8-[2-[[(1R,3S,4S)-3-fluoro-4-hydroxycyclopentyl]amino]pyrimidin-4-yl]-2-[(1S)-2-hydroxy-1-phenylethyl]-4,5-dihydro-3H-pyrrolo[1,2-a][1,4]diazepin-1-one
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C25H28FN5O3
 1
1 IC50 = 0.19 nM
CP0345626
2-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-8-[2-[[(1S,3R)-3-hydroxycyclopentyl]amino]pyrimidin-4-yl]-4,5-dihydro-3H-pyrrolo[1,2-a][1,4]diazepin-1-one
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C25H28ClN5O3
 1
1 IC50 = 0.19 nM
CP0326387
(3R)-2-(2-methoxyethyl)-3-methyl-7-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-3,4-dihydropyrrolo[1,2-a]pyrazin-1-one
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C20H25N7O2
 2
1 IC50 = 0.2 nM
2 IC50 < 0.3 nM
CP0235673
2-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-8-[2-[[(1R,4S)-3,3-difluoro-4-hydroxycyclopentyl]amino]pyrimidin-4-yl]-4,5-dihydro-3H-pyrrolo[1,2-a][1,4]diazepin-1-one
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C25H26ClF2N5O3
 1
1 IC50 = 0.26 nM
CP0072527
SCH772984
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C33H33N9O2
 5
1 IC50 < 0.3 nM
2 IC50 = 0.4 nM
3 IC50 = 1 nM
4 Kd = 0.05012 nM
5 Kd = 0.1 nM
CP0095473
US10525036, Example GDC-0994
   Show/Hide
C21H18ClFN6O2
 4
1 IC50 = 0.3 nM
2 IC50 = 3.1 nM
3 IC50 = 3.3 nM
4 Kd = 1.585 nM
CP0180352
(3S)-2-(2-methoxyethyl)-3-methyl-7-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-3,4-dihydropyrrolo[1,2-a]pyrazin-1-one
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C20H25N7O2
 1
1 IC50 < 0.3 nM
CP0180353
(6R)-5-(2-methoxyethyl)-6-methyl-2-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C20H25N7O2
 1
1 IC50 < 0.3 nM
CP0180354
(6S)-5-(2-methoxyethyl)-6-methyl-2-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C20H25N7O2
 1
1 IC50 < 0.3 nM
CP0241368
5-benzyl-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C23H25N5O2
 2
1 IC50 < 0.3 nM
2 IC50 < 0.32 nM
CP0241372
2-(2-methoxyethyl)-7-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-3,4-dihydropyrrolo[1,2-a]pyrazin-1-one
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C19H23N7O2
 1
1 IC50 < 0.3 nM
CP0364731
7-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-2-[(6-methylpyridin-2-yl)methyl]-3,4-dihydropyrrolo[1,2-a]pyrazin-1-one
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C23H24N8O
 2
1 IC50 = 0.3 nM
2 IC50 < 0.3 nM
CP0096302
(3R)-3-methyl-7-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-2-[(6-methylpyridin-2-yl)methyl]-3,4-dihydropyrrolo[1,2-a]pyrazin-1-one
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C24H26N8O
 4
1 IC50 < 0.3 nM
2 IC50 = 0.5 nM
3 Kd = 0.1585 nM
4 Kd = 0.7943 nM
CP0180385
(3S)-3-methyl-7-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-2-[(6-methylpyridin-2-yl)methyl]-3,4-dihydropyrrolo[1,2-a]pyrazin-1-one
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C24H26N8O
 2
1 IC50 < 0.3 nM
2 IC50 = 0.9 nM
CP0241369
(6S)-5-(2-methoxyethyl)-6-methyl-2-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C19H23N7O2
 2
1 IC50 < 0.3 nM
2 IC50 < 0.33 nM
CP0408200
5-[(1S)-1-(3-chloro-4-fluorophenyl)-2-hydroxyethyl]-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C24H25ClFN5O3
 2
1 IC50 < 0.31 nM
2 IC50 = 0.72 nM
CP0109840
5-[(1S)-2-hydroxy-1-phenylethyl]-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C24H27N5O3
 2
1 IC50 < 0.34 nM
2 IC50 = 0.43 nM
CP0072557
5-[(6-methylpyridin-2-yl)methyl]-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C23H26N6O2
 2
1 IC50 = 0.47 nM
2 IC50 = 1 nM
CP0109825
5-benzyl-1-methyl-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydropyrrolo[3,2-c]pyridin-4-one
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C24H27N5O2
 2
1 IC50 < 0.48 nM
2 IC50 = 1.6 nM
CP0326385
5-[(1S)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C24H25ClFN5O3
 2
1 IC50 = 1.1 nM
2 IC50 = 3.7 nM
CP0180387
5-(2-methoxyethyl)-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C19H25N5O3
 2
1 IC50 < 1.13 nM
2 IC50 = 4.8 nM
CP0109841
2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one
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C16H19N5O2
 2
1 IC50 = 1.2 nM
2 IC50 = 9.2 nM
CP0085671
1-methyl-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-5H-pyrrolo[3,2-c]pyridin-4-one
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C17H21N5O2
 2
1 IC50 = 1.4 nM
2 IC50 = 7.9 nM
CP0272776
N-[(1S)-2-amino-1-(3-chloro-4-fluorophenyl)ethyl]-2-(propan-2-ylamino)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidine-7-carboxamide
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C19H24ClFN6O
 1
1 IC50 = 1.9 nM
CP0072317
(6R)-5-(2-methoxyethyl)-6-methyl-2-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C19H23N7O2
 2
1 IC50 = 1.9 nM
2 IC50 = 14 nM
CP0534588
8-[2-[[(1S,3R)-3-hydroxycyclopentyl]amino]pyrimidin-4-yl]-2-[(1S)-2-hydroxy-1-phenylethyl]-4,5-dihydro-3H-pyrrolo[1,2-a][1,4]diazepin-1-one
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C25H29N5O3
 1
1 IC50 = 2.26 nM
CP0109828
5-(2-methoxyethyl)-2-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C18H21N7O2
 2
1 IC50 = 2.5 nM
2 IC50 = 5.39 nM
CP0328082
5-(2-methoxyethyl)-1-methyl-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydropyrrolo[3,2-c]pyridin-4-one
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C20H27N5O3
 2
1 IC50 = 2.7 nM
2 IC50 = 24 nM
CP0241373
7-[2-(oxan-4-ylamino)pyrimidin-4-yl]-3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one
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C16H19N5O2
 2
1 IC50 = 2.8 nM
2 IC50 = 37 nM
CP0674370
N-(4-((5-chloro-2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)amino)pyridin-3-yl)acrylamide
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C17H19ClN6O2
 2
1 IC50 = 3 nM
2 IC50 = 3.1 nM
CP0283608
N-[(1S,2S)-1-(3-chloro-4-fluorophenyl)-2-hydroxypropyl]-2-(propan-2-ylamino)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidine-7-carboxamide
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C20H25ClFN5O2
 1
1 IC50 = 3.23 nM
CP0252998
4-(3-pyridin-4-yl-1,4,6,7-tetrahydropyrazolo[4,3-c]pyridin-5-yl)-1H-pyridin-2-one
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C16H15N5O
 1
1 IC50 = 5 nM
CP0667349
N-(2-((5-chloro-2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)amino)phenyl)acrylamide
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C18H20ClN5O2
 2
1 IC50 = 5.4 nM
2 IC50 = 8.5 nM
CP0072523
N-[2-[[2-(oxan-4-ylamino)-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide
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C19H20F3N5O2
 2
1 IC50 = 6.9 nM
2 IC50 = 8.5 nM
CP0132840
N-[(1S)-1-(3-chloro-4-fluorophenyl)-2-(methanesulfonamido)ethyl]-2-(propan-2-ylamino)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidine-7-carboxamide
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C20H26ClFN6O3S
 1
1 IC50 = 7.1 nM
CP0667326
N-(3-(pyridin-4-yl)-1H-indazol-5-yl)ethenesulfonamide
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C14H12N4O2S
 2
1 IC50 = 7.5 nM
2 IC50 = 17 nM
CP0676203
N-(2-((5-chloro-2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)amino)phenyl)acrylamide
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C17H16ClN7O
 2
1 IC50 = 9.9 nM
2 IC50 = 13 nM
CP0241367
5-methyl-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one
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C17H21N5O2
 2
1 IC50 = 13 nM
2 IC50 = 130 nM
CP0180390
5-(2-methoxyethyl)-1-methyl-2-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-6,7-dihydropyrrolo[3,2-c]pyridin-4-one
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C19H23N7O2
 2
1 IC50 = 23 nM
2 IC50 = 240 nM
CP0097585
N-[(1S)-1-(3-chloro-4-fluorophenyl)-2-hydroxyethyl]-2-[(3,5-dimethyl-1,2-oxazol-4-yl)amino]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidine-7-carboxamide
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C21H22ClFN6O3
 1
1 IC50 = 25.9 nM
CP0241366
2-[2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one
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C22H25N7O
 2
1 IC50 = 36 nM
2 IC50 = 370 nM
CP0318103
N-[2-[[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]amino]phenyl]prop-2-enamide
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C18H19N7O
 2
1 IC50 = 39 nM
2 IC50 = 47 nM
CP0725021
4-fluoro-N-methyl-2-(2-(tetrahydro-2H-pyran-4-ylamino)-5-(trifluoromethyl)pyridin-4-ylamino)benzamide
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C19H20F4N4O2
 2
1 IC50 = 40 nM
2 IC50 = 380 nM
CP0721177
N-(2-((5-chloro-2-((tetrahydro-2H-pyran-4-yl)amino)pyridin-4-yl)amino)phenyl)acrylamide
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C19H21ClN4O2
 2
1 IC50 = 42 nM
2 IC50 = 60 nM
CP0733193
2-(2-(1,3-dimethyl-1H-pyrazol-5-ylamino)-5-(trifluoromethyl)pyridin-4-ylamino)-4-fluoro-N-methylbenzamide
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C19H18F4N6O
 2
1 IC50 = 44 nM
2 IC50 = 340 nM
CP0733191
3-(2-methylpyridin-4-yl)-5-(vinylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
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C14H16N4O2S
 2
1 IC50 = 74 nM
2 IC50 = 110 nM
CP0072522
N-[2-[[5-methyl-2-(oxan-4-ylamino)pyrimidin-4-yl]amino]phenyl]prop-2-enamide
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C19H23N5O2
 2
1 IC50 = 77 nM
2 IC50 = 88 nM
CP0115031
CHEMBL3590124
   Show/Hide
C21H27ClN6O
 2
1 IC50 = 85 nM
2 IC50 = 90 nM
CP0664804
N-(tetrahydro-2H-pyran-4-yl)-7-(vinylsulfonyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-amine
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C14H20N4O3S
 2
1 IC50 = 220 nM
2 IC50 = 370 nM
CP0788339
2-(5-chloro-2-(tetrahydro-2H-pyran-4-ylamino)pyridin-4-ylamino)-N-methylbenzamide
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C18H21ClN4O2
 1
1 IC50 = 260 nM
CP0733190
N-(3-(pyridin-4-yl)-1H-indazol-5-yl)ethanesulfonamide
   Show/Hide
C14H14N4O2S
 2
1 IC50 = 280 nM
2 IC50 = 1800 nM
CP0806313
N-(2-(5-chloro-2-(tetrahydro-2H-pyran-4-ylamino)pyrimidin-4-ylamino)phenyl)propionamide
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C18H22ClN5O2
 2
1 IC50 = 480 nM
2 IC50 = 4000 nM
CP0644710
ERKi_NC
   Show/Hide
C15H16N6O2
 2
1 IC50 = 1780 nM
2 IC50 ~ 1780 nM
CP0674360
(3S,5E,8R,9S,11E)-8,9,16-trihydroxy-14-methoxy-3-methyl-3,4,9,10-tetrahydro-1H-benzo[c][1]oxacyclotetradecine-1,7(8H)-dione
   Show/Hide
C19H22O7
 2
1 IC50 = 3700 nM
2 IC50 = 5100 nM
CP0733192
7-(ethylsulfonyl)-N-(tetrahydro-2H-pyran-4-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-amine
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C14H22N4O3S
 2
1 IC50 = 9000 nM
2 IC50 > 10000 nM
CP0645110
ERKi
   Show/Hide
C16H17N5O2
 4
1 IC50 ~ 1.8 nM
2 IC50 ~ 4 nM
3 IC50 ~ 850 nM
4 Kd = 4.8 nM
Clinical Information about the Protein
Target 1 ( Extracellular signal-regulated kinase 2 (ERK2) )
Target Type Clinical trial Target
Disease 4 Target-related Diseases  4
1 Melanoma [ICD-11: 2C30]
2 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
3 Graft rejection [ICD-11: NE84]
4 Arthritis [ICD-11: FA20]
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 BVD-523 Phase 2
Melanoma
2 GDC-0994 Phase 1
Solid tumour/cancer
3 LY3214996 Phase 1
Solid tumour/cancer
Discontinued Drug(s) 1 Discontinued Drug  1
1 SB220025 Terminated
Arthritis
Patented Agent(s) 1 Patented Agent  1
1 CHIR-99021 Patented
Graft rejection
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01069 Mitogen-activated protein kinase 3 Homo sapiens, Human