General Information of the Protein
Protein ID
PT03462
Protein Name
GTPase KRas
Secondarily
Protein Name
K-Ras 2
Ki-Ras
c-K-ras
c-Ki-ras
Gene Name
KRAS
Secondarily
Gene Name
KRAS2
RASK2
Sequence
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Hydrolase
Function
Ras proteins bind GDP/GTP and possess intrinsic GTPase activity (PubMed:20949621). Plays an important role in the regulation of cell proliferation (PubMed:23698361, PubMed:22711838). Plays a role in promoting oncogenic events by inducing transcriptional silencing of tumor suppressor genes (TSGs) in colorectal cancer (CRC) cells in a ZNF304-dependent manner (PubMed:24623306).
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Uniprot ID
Primary ID:
P01116

Secondarily ID:
A8K8Z5
B0LPF9
P01118
Q96D10
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Ensembl ID
ENSG00000133703
HGNC ID
HGNC:6407
Subcellular Location
Cell membrane
Endomembrane system
Cytoplasm
Cytosol
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: CL000275 , AGS
Compound ID Compound Name Compound Formula
CP0575124
4-[4-[(1R,5S)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-[[(2R,8S)-2-fluoro-1,2,3,5,6,7-hexahydropyrrolizin-8-yl]methoxy]pyrido[4,3-d]pyrimidin-7-yl]-5-ethynyl-6-fluoronaphthalen-2-ol
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C33H31F3N6O2
 1
1
IC50 = 2 nM
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CP0571951
4-[4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)pyrido[4,3-d]pyrimidin-7-yl]-5-ethynylnaphthalen-2-ol
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C33H33FN6O2
 1
1
IC50 = 14 nM
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CP0573768
4-[(1R,5S)-3,8-diazabicyclo[3.2.1]octan-3-yl]-7-(8-ethynyl-7-fluoronaphthalen-1-yl)-8-fluoro-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)pyrido[4,3-d]pyrimidine
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C33H32F2N6O
 1
1
IC50 = 24 nM
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CP0577514
4-[4-[(1R,5S)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-[[(2R,8S)-2-fluoro-1,2,3,5,6,7-hexahydropyrrolizin-8-yl]methoxy]pyrido[4,3-d]pyrimidin-7-yl]naphthalen-2-ol
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C31H32F2N6O2
 1
1
IC50 = 24 nM
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CP0579154
5-chloro-4-[4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)pyrido[4,3-d]pyrimidin-7-yl]naphthalen-2-ol
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C31H32ClFN6O2
 1
1
IC50 = 63 nM
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CP0551801
4-[4-[(1R,5S)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-[[(2S,8R)-2-fluoro-1,2,3,5,6,7-hexahydropyrrolizin-8-yl]methoxy]pyrido[4,3-d]pyrimidin-7-yl]naphthalen-2-ol
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C31H32F2N6O2
 1
1
IC50 = 64 nM
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CP0572594
4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-7-(8-ethynylnaphthalen-1-yl)-8-fluoro-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)pyrido[4,3-d]pyrimidine
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C33H33FN6O
 1
1
IC50 = 71 nM
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CP0575123
4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-7-(7,8-difluoronaphthalen-1-yl)-8-fluoro-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)pyrido[4,3-d]pyrimidine
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C31H31F3N6O
 1
1
IC50 = 97 nM
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CP0571909
7-(8-chloronaphthalen-1-yl)-4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)pyrido[4,3-d]pyrimidine
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C31H32ClFN6O
 1
1
IC50 = 190 nM
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CP0567531
4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-7-(8-ethylnaphthalen-1-yl)-8-fluoro-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)pyrido[4,3-d]pyrimidine
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C33H37FN6O
 1
1
IC50 = 200 nM
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CP0572593
4-[4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)pyrido[4,3-d]pyrimidin-7-yl]naphthalen-2-ol
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C31H33FN6O2
 1
1
IC50 = 270 nM
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CP0579153
4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-7-(7-fluoronaphthalen-1-yl)-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)pyrido[4,3-d]pyrimidine
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C31H32F2N6O
 1
1
IC50 = 370 nM
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CP0573914
4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-7-(8-fluoronaphthalen-1-yl)-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)pyrido[4,3-d]pyrimidine
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C31H32F2N6O
 1
1
IC50 = 380 nM
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CP0567429
4-[4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-[[(2S)-1-methylpyrrolidin-2-yl]methoxy]pyrido[4,3-d]pyrimidin-7-yl]naphthalen-2-ol
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C29H31FN6O2
 1
1
IC50 = 530 nM
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CP0579152
4-[4-(3,8-diazabicyclo[3.2.1]octan-3-yl)-8-fluoro-2-(2,3,5,6,7,8-hexahydro-1H-indolizin-8a-ylmethoxy)pyrido[4,3-d]pyrimidin-7-yl]naphthalen-2-ol
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C32H35FN6O2
 1
1
IC50 = 650 nM
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CP0543340
4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)-7-(8-methoxynaphthalen-1-yl)pyrido[4,3-d]pyrimidine
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C32H35FN6O2
 1
1
IC50 = 1200 nM
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CP0577513
US11453683, Example 120
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C28H30FN7O
 1
1
IC50 = 1300 nM
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CP0543339
4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)-7-(8-methylnaphthalen-1-yl)pyrido[4,3-d]pyrimidine
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C32H35FN6O
 1
1
IC50 = 2500 nM
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CP0545185
4-[4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-[2-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]ethoxy]pyrido[4,3-d]pyrimidin-7-yl]naphthalen-2-ol
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C30H31FN6O3
 1
1
IC50 = 3000 nM
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CP0571949
4-[4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-[2-(1-methylimidazol-2-yl)ethoxy]pyrido[4,3-d]pyrimidin-7-yl]naphthalen-2-ol
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C29H28FN7O2
 1
1
IC50 = 3500 nM
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CP0547020
[8-[4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)pyrido[4,3-d]pyrimidin-7-yl]naphthalen-1-yl]methanol
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C32H35FN6O2
 1
1
IC50 > 10000 nM
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CP0567532
US11453683, Example 181
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C23H20FN5O
 1
1
IC50 > 10000 nM
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CP0571952
4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-ylmethoxy)-7-naphthalen-1-ylpyrido[4,3-d]pyrimidine
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C31H33FN6O
 1
1
IC50 > 10000 nM
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CP0572595
8-[[4-(3,8-diazabicyclo[3.2.1]octan-3-yl)-8-fluoro-7-(3-hydroxynaphthalen-1-yl)pyrido[4,3-d]pyrimidin-2-yl]oxymethyl]-2,5,6,7-tetrahydro-1H-pyrrolizin-3-one
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C31H31FN6O3
 1
1
IC50 > 10000 nM
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CP0579155
4-[4-[(1S,5R)-3,8-diazabicyclo[3.2.1]octan-3-yl]-2-[2-(dimethylamino)ethoxy]-8-fluoropyrido[4,3-d]pyrimidin-7-yl]naphthalen-2-ol
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C27H29FN6O2
 1
1
IC50 > 10000 nM
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CP0349547
1-[4-[7-(3-hydroxynaphthalen-1-yl)-2-[[(2S)-1-methylpyrrolidin-2-yl]methoxy]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]piperazin-1-yl]prop-2-en-1-one
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C30H36N6O3
 1
1
IC50 > 16000 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0015072
Adagrasib
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C32H35ClFN7O2
 2
1 EC50 = 10 nM
2 Ki = 3700 nM
CP0544029
2-[(3R,8R,11S,14S,20S,23S,26S,29S,32S,35S,38S,39R)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-6-azidohexanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-8-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-26-(hydroxymethyl)-23-[(4-hydroxyphenyl)methyl]-29-methyl-35-(2-methylpropyl)-2,10,13,19,22,25,28,31,34,37-decaoxo-39-phenyl-32-[(4-phenylphenyl)methyl]-11-propan-2-yl-5,6-dithia-1,9,12,18,21,24,27,30,33,36-decazatricyclo[36.3.0.014,18]hentetracontan-20-yl]acetic acid
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C99H146N32O21S2
 1
1 IC50 < 1 nM
CP0544030
2-[(4R,9R,12S,15S,21S,24S,27S,30S,33S,36S,39S,40R)-4-[[(2S)-2-[[(2S)-2-acetamido-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-9-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-30-[(2S)-butan-2-yl]-27-(hydroxymethyl)-24-[(4-hydroxyphenyl)methyl]-36-(2-methylpropyl)-3,11,14,20,23,26,29,32,35,38-decaoxo-40-phenyl-33-[(4-phenylphenyl)methyl]-12-propan-2-yl-6,7-dithia-1,10,13,19,22,25,28,31,34,37-decazatricyclo[37.3.0.015,19]dotetracontan-21-yl]acetic acid
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C97H144N28O20S2
 1
1 IC50 < 1 nM
CP0567489
2-[(4R,9R,12S,15S,21S,24S,27S,30S,33S,36S,39S,40S)-4-[[(2S)-2-[[(2S)-2-acetamido-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-9-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-30-[(2S)-butan-2-yl]-27-(hydroxymethyl)-24-[(4-hydroxyphenyl)methyl]-36-(2-methylpropyl)-3,11,14,20,23,26,29,32,35,38-decaoxo-33-[(4-phenylphenyl)methyl]-12-propan-2-yl-40-prop-2-enyl-6,7-dithia-1,10,13,19,22,25,28,31,34,37-decazatricyclo[37.3.0.015,19]dotetracontan-21-yl]acetic acid
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C94H144N28O20S2
 1
1 IC50 < 1 nM
CP0568539
2-[(4R,9R,12S,15S,21S,24S,27S,30S,33S,36S,39S,40R)-4-[[(2S)-2-[[(2S)-2-acetamido-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-9-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-30-[(2S)-butan-2-yl]-27-(hydroxymethyl)-24-[(4-hydroxyphenyl)methyl]-36-(2-methylpropyl)-3,11,14,20,23,26,29,32,35,38-decaoxo-12-pentyl-40-phenyl-33-[(4-phenylphenyl)methyl]-6,7-dithia-1,10,13,19,22,25,28,31,34,37-decazatricyclo[37.3.0.015,19]dotetracontan-21-yl]acetic acid
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C99H148N28O20S2
 1
1 IC50 < 1 nM
CP0569904
2-[(3R,8R,11S,14S,20S,23S,26S,29S,32S,35S,38S,39S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-6-azidohexanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-8-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-29-[(2S)-butan-2-yl]-26-(hydroxymethyl)-23-[(4-hydroxyphenyl)methyl]-35-(2-methylpropyl)-2,10,13,19,22,25,28,31,34,37-decaoxo-39-phenyl-32-[(4-phenylphenyl)methyl]-11-propan-2-yl-5,6-dithia-1,9,12,18,21,24,27,30,33,36-decazatricyclo[36.3.0.014,18]hentetracontan-20-yl]acetic acid
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C102H152N32O21S2
 1
1 IC50 < 1 nM
CP0571629
2-[(4R,9R,12S,15S,21S,24S,27S,30S,33S,36S,39S,40S)-4-[[(2S)-2-[[(2S)-2-acetamido-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-9-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-30-[(2S)-butan-2-yl]-27-(hydroxymethyl)-24-[(4-hydroxyphenyl)methyl]-36-(2-methylpropyl)-3,11,14,20,23,26,29,32,35,38-decaoxo-12-pentyl-33-[(4-phenylphenyl)methyl]-40-prop-2-enyl-6,7-dithia-1,10,13,19,22,25,28,31,34,37-decazatricyclo[37.3.0.015,19]dotetracontan-21-yl]acetic acid
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C96H148N28O20S2
 1
1 IC50 < 1 nM
CP0579406
2-[(3R,8R,11S,14S,20S,23S,26S,29S,32S,35S,38S,41S,42S)-3-[[(2S)-2-[[(2S)-2-acetamido-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-8-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-32-[(2S)-butan-2-yl]-26-(hydroxymethyl)-23-[(4-hydroxyphenyl)methyl]-29-methyl-38-(2-methylpropyl)-2,10,13,19,22,25,28,31,34,37,40-undecaoxo-42-phenyl-35-[(4-phenylphenyl)methyl]-11-propan-2-yl-5,6-dithia-1,9,12,18,21,24,27,30,33,36,39-undecazatricyclo[39.3.0.014,18]tetratetracontan-20-yl]acetic acid
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C99H147N29O21S2
 1
1 IC50 < 1 nM
CP0533768
7-(2-amino-3,5-dichloro-6-fluorophenyl)-6-chloro-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(3R)-3-methyl-4-prop-2-enoylpiperazin-1-yl]-2-oxo-1,8-naphthyridine-3-carbonitrile
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C32H29Cl3FN7O2
 1
1 IC50 = 2.535 nM
CP0570618
7-(2-amino-6-fluorophenyl)-6-chloro-1-[4,6-di(propan-2-yl)pyrimidin-5-yl]-2-oxo-4-(4-prop-2-enoylpiperazin-1-yl)-1,8-naphthyridine-3-carbonitrile
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C32H32ClFN8O2
 1
1 IC50 = 2.77 nM
CP0533767
7-(2-amino-3,5-dichloro-6-fluorophenyl)-6-chloro-4-[(3S,5R)-3,5-dimethyl-4-prop-2-enoylpiperazin-1-yl]-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-2-oxo-1,8-naphthyridine-3-carbonitrile
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C33H31Cl3FN7O2
 1
1 IC50 = 2.832 nM
CP0563420
6-chloro-7-(2-fluorophenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-2-oxo-4-(4-prop-2-enoylpiperazin-1-yl)-1,8-naphthyridine-3-carbonitrile
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C31H28ClFN6O2
 1
1 IC50 = 4.4 nM
CP0444490
7-(2-amino-3,5-dichloro-6-fluorophenyl)-6-chloro-1-[4,6-di(propan-2-yl)pyrimidin-5-yl]-2-oxo-4-(4-prop-2-enoylpiperazin-1-yl)-1,8-naphthyridine-3-carbonitrile
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C32H30Cl3FN8O2
 1
1 IC50 = 4.737 nM
CP0130475
ethyl (2R,3R)-3-[(3S)-4-[6-chloro-7-(2-fluorophenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-2-oxopyrido[2,3-d]pyrimidin-4-yl]-3-methylpiperazine-1-carbonyl]oxirane-2-carboxylate
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C33H34ClFN6O5
 2
1 IC50 = 5 nM
2 IC50 = 216 nM
CP0575124
4-[4-[(1R,5S)-3,8-diazabicyclo[3.2.1]octan-3-yl]-8-fluoro-2-[[(2R,8S)-2-fluoro-1,2,3,5,6,7-hexahydropyrrolizin-8-yl]methoxy]pyrido[4,3-d]pyrimidin-7-yl]-5-ethynyl-6-fluoronaphthalen-2-ol
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C33H31F3N6O2
 1
1 IC50 = 5 nM
CP0444489
7-(2-amino-3,5-dichloro-6-fluorophenyl)-6-chloro-4-[3-(cyanomethyl)-4-prop-2-enoylpiperazin-1-yl]-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-2-oxo-1,8-naphthyridine-3-carbonitrile
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C33H28Cl3FN8O2
 1
1 IC50 = 5.188 nM
CP0552434
7-(2-amino-3,5-dichloro-6-fluorophenyl)-6-chloro-4-[(3S)-3-(cyanomethyl)-4-prop-2-enoylpiperazin-1-yl]-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-2-oxo-1,8-naphthyridine-3-carbonitrile
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C33H28Cl3FN8O2
 1
1 IC50 = 6.66 nM
CP0232483
6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one
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C30H30F2N6O3
 3
1 IC50 = 9.66 nM
2 Ki = 12200 nM
3 Ki = 86000 nM
CP0418887
methyl (E)-4-[(3S)-4-[6-chloro-7-(2-fluorophenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-2-oxopyrido[2,3-d]pyrimidin-4-yl]-3-methylpiperazin-1-yl]-4-oxobut-2-enoate
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C32H32ClFN6O4
 2
1 IC50 = 26 nM
2 IC50 = 95 nM
CP0271490
2-[(3S)-4-[6-chloro-7-(2-fluorophenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-2-oxopyrido[2,3-d]pyrimidin-4-yl]-3-methylpiperazin-1-yl]-2-oxoacetaldehyde
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C29H28ClFN6O3
 2
1 IC50 = 39 nM
2 IC50 = 610 nM
CP0546998
4-[6-chloro-2-[2-(dimethylamino)ethoxy]-4-(3-ethenyl-6,8-dihydro-5H-imidazo[1,5-a]pyrazin-7-yl)-8-fluoroquinazolin-7-yl]naphthalen-2-ol
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C30H28ClFN6O2
 1
1 IC50 = 100 nM
CP0550168
4-[6-chloro-4-(3-ethenyl-6,8-dihydro-5H-imidazo[1,5-a]pyrazin-7-yl)-8-fluoro-2-[(1-methylpyrrolidin-2-yl)methoxy]quinazolin-7-yl]naphthalen-2-ol
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C32H30ClFN6O2
 1
1 IC50 <= 100 nM
CP0564522
4-(3-ethenyl-6,8-dihydro-5H-imidazo[1,5-a]pyrazin-7-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2-one
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C30H27F2N7O2
 1
1 IC50 = 100 nM
CP0564523
4-(3-ethenyl-6,8-dihydro-5H-imidazo[1,5-a]pyrazin-7-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-propan-2-ylpyrido[2,3-d]pyrimidin-2-one
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C24H22F2N6O2
 1
1 IC50 = 100 nM
CP0569576
4-[6-chloro-4-(3-ethenyl-6,8-dihydro-5H-imidazo[1,5-a]pyrazin-7-yl)-8-fluoro-2-(2-morpholin-4-ylethoxy)quinazolin-7-yl]naphthalen-2-ol
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C32H30ClFN6O3
 1
1 IC50 = 100 nM
CP0569979
4-[6-chloro-4-(3-ethenyl-6,8-dihydro-5H-imidazo[1,5-a]pyrazin-7-yl)-8-fluoro-2-(1-methylpiperidin-4-yl)oxyquinazolin-7-yl]naphthalen-2-ol
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C32H30ClFN6O2
 1
1 IC50 = 100 nM
CP0572231
4-[6-chloro-4-(3-ethenyl-6,8-dihydro-5H-imidazo[1,5-a]pyrazin-7-yl)-8-fluoro-2-[[(2S)-1-methylpyrrolidin-2-yl]methoxy]quinazolin-7-yl]naphthalen-2-ol
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C32H30ClFN6O2
 1
1 IC50 = 100 nM
CP0575858
4-[6-chloro-4-(3-ethenyl-6,8-dihydro-5H-imidazo[1,5-a]pyrazin-7-yl)-8-fluoro-2-(1-methylpiperidin-3-yl)oxyquinazolin-7-yl]naphthalen-2-ol
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C32H30ClFN6O2
 1
1 IC50 = 100 nM
CP0579117
1-(cyclopropylmethyl)-4-(3-ethenyl-6,8-dihydro-5H-imidazo[1,5-a]pyrazin-7-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)pyrido[2,3-d]pyrimidin-2-one
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C25H22F2N6O2
 1
1 IC50 = 100 nM
CP0579118
2-[6-chloro-4-(3-ethenyl-6,8-dihydro-5H-imidazo[1,5-a]pyrazin-7-yl)-8-fluoro-2-[(1-methylpyrrolidin-2-yl)methoxy]quinazolin-7-yl]-3-fluorophenol
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C28H27ClF2N6O2
 1
1 IC50 = 100 nM
CP0970169
6-chloro-8-fluoro-7-(5-methyl-1H-indazol-4-yl)-2-((1-methylpyrrolidin-2-yl)methoxy)-4-(3-vinyl-5,6-dihydroimidazo[1,5-a]pyrazin-7(8H)-yl)quinazoline
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C30H30ClFN8O
 1
1 IC50 = 100 nM
CP0964491
1-((1-acryloyl-3-fluoroazetidin-3-yl)methyl)-6-(2-amino-6-fluorophenyl)-7-chloro-4-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-b]pyrazine-2,3(1H,4H)-dione
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C29H27ClF2N6O3
 1
1 IC50 <= 100 nM
CP0964923
1-((1-acryloyl-3-fluoroazetidin-3-yl)methyl)-7-chloro-4-(2,6-diisopropylphenyl)-6-(3-hydroxynaphthalen-1-yl)pyrido[2,3-b]pyrazine-2,3(1H,4H)-dione
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C36H34ClFN4O4
 1
1 IC50 <= 100 nM
CP0969459
1-((1-acryloyl-3-fluoroazetidin-3-yl)methyl)-7-chloro-6-(2-fluorophenyl)-4-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-b]pyrazine-2,3(1H,4H)-dione
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C29H26ClF2N5O3
 1
1 IC50 <= 100 nM
CP0970148
1-((1-acryloyl-3-fluoroazetidin-3-yl)methyl)-7-chloro-6-(5-chlorobenzo[d][1,3]dioxol-4-yl)-4-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-b]pyrazine-2,3(1H,4H)-dione
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C30H26Cl2FN5O5
 1
1 IC50 <= 100 nM
CP0970268
1-((1-acryloyl-3-fluoroazetidin-3-yl)methyl)-7-chloro-6-(3,6-difluoro-2-hydroxyphenyl)-4-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-b]pyrazine-2,3(1H,4H)-dione
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C29H25ClF3N5O4
 1
1 IC50 <= 100 nM
CP0970352
1-((1-acryloyl-3-fluoroazetidin-3-yl)methyl)-7-chloro-6-(2,3-dichlorophenyl)-4-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-b]pyrazine-2,3(1H,4H)-dione
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C29H25Cl3FN5O3
 1
1 IC50 <= 100 nM
CP0169187
2-[5-bromo-3-(5-methoxy-3,4-dihydro-1H-isoquinoline-2-carbonyl)-2,7-dimethylindol-1-yl]-N-(1-prop-2-enoylazetidin-3-yl)acetamide
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C29H31BrN4O4
 1
1 IC50 = 109 nM
CP0152940
2-[5-chloro-2-cyclopropyl-3-(5-methoxy-3,4-dihydro-1H-isoquinoline-2-carbonyl)-7-methylindol-1-yl]-N-(1-prop-2-enoylazetidin-3-yl)acetamide
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C31H33ClN4O4
 2
1 IC50 = 115 nM
2 Kd = 20000 nM
CP0169183
2-[5-bromo-2-cyclopropyl-3-(5-methoxy-3,4-dihydro-1H-isoquinoline-2-carbonyl)indol-1-yl]-N-(1-prop-2-enoylazetidin-3-yl)acetamide
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C30H31BrN4O4
 1
1 IC50 = 139 nM
CP0152939
2-[5-chloro-3-(5-methoxy-3,4-dihydro-1H-isoquinoline-2-carbonyl)-2,7-dimethylindol-1-yl]-N-(1-prop-2-enoylazetidin-3-yl)acetamide
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C29H31ClN4O4
 1
1 IC50 = 150 nM
CP0158949
2-[5-bromo-3-(5-methoxy-3,4-dihydro-1H-isoquinoline-2-carbonyl)-7-methylindol-1-yl]-N-(1-prop-2-enoylazetidin-3-yl)acetamide
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C28H29BrN4O4
 1
1 IC50 = 174 nM
CP0152945
2-[5-bromo-3-(5-methoxy-3,4-dihydro-1H-isoquinoline-2-carbonyl)-2-methylindol-1-yl]-N-(1-prop-2-enoylazetidin-3-yl)acetamide
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C28H29BrN4O4
 1
1 IC50 = 299 nM
CP0158917
2-[5-chloro-3-(5-methoxy-3,4-dihydro-1H-isoquinoline-2-carbonyl)-2-methylindol-1-yl]-N-(1-prop-2-enoylazetidin-3-yl)acetamide
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C28H29ClN4O4
 1
1 IC50 = 369 nM
CP0158948
2-[5-bromo-3-(5-methoxy-3,4-dihydro-1H-isoquinoline-2-carbonyl)indol-1-yl]-N-(1-prop-2-enoylazetidin-3-yl)acetamide
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C27H27BrN4O4
 1
1 IC50 = 638 nM
CP0339057
1-[4-[6-chloro-8-fluoro-7-(2-fluoro-6-hydroxyphenyl)quinazolin-4-yl]piperazin-1-yl]prop-2-en-1-one
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C21H17ClF2N4O2
 2
1 IC50 = 939 nM
2 Ki = 31000 nM
CP0158916
2-[5-bromo-3-(3,4-dihydro-1H-isoquinoline-2-carbonyl)indol-1-yl]-N-(1-prop-2-enoylazetidin-3-yl)acetamide
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C26H25BrN4O3
 1
1 IC50 = 1270 nM
CP0169186
2-[5-bromo-3-(5-chloro-3,4-dihydro-1H-isoquinoline-2-carbonyl)indol-1-yl]-N-(1-prop-2-enoylazetidin-3-yl)acetamide
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C26H24BrClN4O3
 1
1 IC50 = 1290 nM
CP0238937
2-[5-bromo-3-(6-fluoro-3,4-dihydro-1H-isoquinoline-2-carbonyl)indol-1-yl]-N-(1-prop-2-enoylazetidin-3-yl)acetamide
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C26H24BrFN4O3
 1
1 IC50 = 1370 nM
CP0152944
2-[5-bromo-3-(6-chloro-3,4-dihydro-1H-isoquinoline-2-carbonyl)indol-1-yl]-N-(1-prop-2-enoylazetidin-3-yl)acetamide
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C26H24BrClN4O3
 1
1 IC50 = 2000 nM
CP0169174
2-[5-bromo-3-(5-fluoro-3,4-dihydro-1H-isoquinoline-2-carbonyl)indol-1-yl]-N-(1-prop-2-enoylazetidin-3-yl)acetamide
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C26H24BrFN4O3
 1
1 IC50 = 2120 nM
CP0572675
2-[4-bromo-2-(3-phenyl-2,5-dihydropyrrole-1-carbonyl)phenoxy]-N-(1-prop-2-enoylazetidin-3-yl)acetamide
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C25H24BrN3O4
 1
1 IC50 = 2780 nM
CP0152942
5-bromo-1-[2-oxo-2-[(1-prop-2-enoylazetidin-3-yl)amino]ethyl]-N-(2-phenylethyl)indole-3-carboxamide
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C25H25BrN4O3
 1
1 IC50 = 4260 nM
CP0169173
N-benzyl-5-bromo-N-methyl-1-[2-oxo-2-[(1-prop-2-enoylazetidin-3-yl)amino]ethyl]indole-3-carboxamide
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C25H25BrN4O3
 1
1 IC50 = 6630 nM
CP0158915
N-benzyl-5-bromo-1-[2-oxo-2-[(1-prop-2-enoylazetidin-3-yl)amino]ethyl]indole-3-carboxamide
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C24H23BrN4O3
 1
1 IC50 = 14200 nM
CP0355547
(7S,10S,13R,16S,19R,22S,25S,28R,31S,34S,37R)-N-[(2S)-5-amino-1-[[(2R)-1-[[(2S)-1-[[(2R)-1-amino-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]-31-(2-amino-2-oxoethyl)-16-(3-amino-3-oxopropyl)-19-benzyl-10,13-bis(3-carbamimidamidopropyl)-34-(hydroxymethyl)-28,37-bis(naphthalen-2-ylmethyl)-4,9,12,15,18,21,24,27,30,33,36,39,42-tridecaoxo-25-phenyl-5,8,11,14,17,20,23,26,29,32,35,38,43-tridecazatricyclo[20.19.6.13,40]octatetraconta-1,3(48),40-triene-7-carboxamide
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C108H138N30O21
 3
1 Kd = 21 nM
2 Kd = 42 nM
3 Kd = 230 nM
Clinical Information about the Protein
Target 1 ( GTPase KRas (KRAS) )
Target Type Clinical trial Target
Target 2 ( KRAS messenger RNA (KRAS mRNA) )
Target Type Literature-reported Target
Target 3 ( KRAS G12D mutant messenger RNA (KRAS mRNA) )
Target Type Clinical trial Target
Target 4 ( KRAS G12C mutant (KRAS G12C) )
Target Type Successful Target
Disease 1 Target-related Disease  1
1 Non-small-cell lung cancer [ICD-11: 2C25]
Approved Drug(s) 2 Approved Drugs  2
1 Adagrasib Approved
Non-small-cell lung cancer
2 Sotorasib Approved
Non-small-cell lung cancer
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 JDQ443 Phase 3
Non-small-cell lung cancer
Target 5 ( KRas D816V mutant (KRAS D816V) )
Target Type Clinical trial Target