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MAP kinase ERK2 Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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StaurosporineIC50659.1 [1]
CID 24866313IC501.0 [1]
UlixertinibIC500.3 [1]
(3R)-N-(3-Chloro-4-hydroxyphenyl)-1-[2-oxo-2-[4-(4-phenylphenyl)piperazin-1-yl]ethyl]pyrrolidine-3-carboxamideIC504400.0 [1]
RavoxertinibIC500.3 [1], 3.3 [2], 86.0 [3], 140.0 [4]
1-[2-[4-(4-Acetylphenyl)piperazin-1-yl]-2-oxoethyl]-N-(4-hydroxyphenyl)pyrrolidine-3-carboxamideIC501060.0 [1], 1890.0 [2], 4000.0 [3], 15200.0 [4], 18600.0 [5]
N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]benzamideIC5025.0 [1], 10000.0 [2], 40000.0 [3]
5-(2-Phenylpyrazolo[1,5-A]pyridin-3-YL)-1H-pyrazolo[3,4-C]pyridazin-3-amineIC501200.0 [1], 1900.0 [2]
5-(2-Phenylpyrazolo[1,5-A]pyridin-3-YL)-1H-pyrazolo[3,4-C]pyridazin-3-amineKi310.0 [1]
(3R)-1-[2-[4-(4-Bromophenyl)piperazin-1-yl]-2-oxoethyl]-N-(3-chloro-4-hydroxyphenyl)pyrrolidine-3-carboxamideIC50930.0 [1], 2650.0 [2], 5000.0 [3], 8200.0 [4]
(3R)-1-[2-[4-(4-Acetylphenyl)piperazin-1-yl]-2-oxoethyl]-N-(3-fluoro-4-hydroxyphenyl)pyrrolidine-3-carboxamideIC50280.0 [1], 630.0 [2], 1300.0 [3], 11600.0 [4]
(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-oneIC500.3 [1], 310.0 [2], 380.0 [3]
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-oneIC500.3 [1], 110.0 [2], 1000.0 [3]
(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-oneIC500.3 [1], 0.5 [2], 12.0 [3], 62.0 [4]
(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-oneIC500.3 [1], 0.9 [2], 140.0 [3], 30000.0 [4]
2-[2-(Oxan-4-Ylamino)pyrimidin-4-Yl]-5-(Phenylmethyl)-6,7-Dihydro-1~{h}-Pyrrolo[3,2-C]pyridin-4-OneIC500.3 [1], 0.32 [2], 80.0 [3], 220.0 [4]
5-(2-Methoxyethyl)-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-oneIC501.13 [1], 4.8 [2], 600.0 [3], 18000.0 [4]
5-(2-Methoxyethyl)-2-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-oneIC502.5 [1], 5.39 [2], 1600.0 [3], 30000.0 [4]
(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-oneIC500.3 [1], 30.0 [2], 130.0 [3]
(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-oneIC500.3 [1], 200.0 [2], 8100.0 [3]
CID 126480565IC5023.0 [1], 240.0 [2], 4700.0 [3], 10000.0 [4]
7-[2-(Oxan-4-Ylamino)pyrimidin-4-Yl]-3,4-Dihydro-2~{h}-Pyrrolo[1,2-A]pyrazin-1-OneIC502.8 [1], 37.0 [2], 1100.0 [3], 25000.0 [4]
2-[2-[4-(4-Methylpiperazin-1-yl)anilino]pyrimidin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-oneIC5036.0 [1], 160.0 [2], 370.0 [3], 570.0 [4]
5-[(6-Methylpyridin-2-yl)methyl]-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-oneIC500.47 [1], 1.0 [2], 370.0 [3], 9400.0 [4]
(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-oneIC500.3 [1], 0.33 [2], 1100.0 [3], 29000.0 [4]
5-Methyl-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-oneIC5013.0 [1], 130.0 [2], 1900.0 [3], 10000.0 [4]
(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-oneIC500.2 [1], 0.3 [2], 130.0 [3], 22000.0 [4]
(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-oneIC501.9 [1], 14.0 [2], 1200.0 [3], 11700.0 [4]
2-(2-Methoxyethyl)-7-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-3,4-dihydropyrrolo[1,2-a]pyrazin-1-oneIC500.3 [1], 310.0 [2], 30000.0 [3]
2-[2-(Oxan-4-ylamino)pyrimidin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-oneIC501.2 [1], 9.2 [2], 940.0 [3], 960.0 [4]
3-Methyl-7-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-2-[(6-methylpyridin-2-yl)methyl]-3,4-dihydropyrrolo[1,2-a]pyrazin-1-oneIC500.35 [1], 0.39 [2], 330.0 [3], 30000.0 [4]
5-(2-Methoxyethyl)-1-methyl-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydropyrrolo[3,2-c]pyridin-4-oneIC502.7 [1], 24.0 [2], 1400.0 [3], 24000.0 [4]
5-[(1S)-2-Hydroxy-1-phenylethyl]-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-oneIC500.34 [1], 0.43 [2], 100.0 [3], 3500.0 [4]
1-Methyl-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydro-5H-pyrrolo[3,2-c]pyridin-4-oneIC501.4 [1], 7.9 [2], 340.0 [3], 570.0 [4]
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-oneIC500.31 [1], 0.72 [2], 130.0 [3], 3300.0 [4]
5-Benzyl-1-methyl-2-[2-(oxan-4-ylamino)pyrimidin-4-yl]-6,7-dihydropyrrolo[3,2-c]pyridin-4-oneIC500.48 [1], 1.6 [2], 69.0 [3], 9300.0 [4]
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-oneIC501.1 [1], 3.7 [2], 250.0 [3], 30000.0 [4]
(3R)-1-[2-[4-(4-Acetylphenyl)piperazin-1-yl]-2-oxoethyl]-N-(2-chloro-4-hydroxyphenyl)pyrrolidine-3-carboxamideIC5010000.0 [1], 12700.0 [2], 50000.0 [3]
(3R)-N-(3-Chloro-4-hydroxyphenyl)-1-[2-oxo-2-[4-(4-thiophen-3-ylphenyl)piperazin-1-yl]ethyl]pyrrolidine-3-carboxamideIC50290.0 [1], 980.0 [2], 2100.0 [3], 20000.0 [4]
(3S)-1-[2-[4-(4-Acetylphenyl)piperazin-1-yl]-2-oxoethyl]-N-(3-chloro-4-hydroxyphenyl)pyrrolidine-3-carboxamideIC50360.0 [1], 870.0 [2], 3600.0 [3], 32000.0 [4]
(3R)-1-[2-[4-(4-Acetylphenyl)piperazin-1-yl]-2-oxoethyl]-N-(3-chloro-4-hydroxyphenyl)pyrrolidine-3-carboxamideIC5050.0 [1], 140.0 [2], 360.0 [3], 2600.0 [4]
(3R)-N-(3-Chloro-4-hydroxyphenyl)-1-[2-[4-[4-(furan-3-yl)phenyl]piperazin-1-yl]-2-oxoethyl]pyrrolidine-3-carboxamideIC50120.0 [1], 330.0 [2], 1400.0 [3], 5500.0 [4]
(3R)-N-(3-Chloro-4-hydroxyphenyl)-1-[2-[4-(3-chlorophenyl)piperazin-1-yl]-2-oxoethyl]pyrrolidine-3-carboxamideIC5070.0 [1], 150.0 [2], 700.0 [3], 2100.0 [4]
(3R)-1-[2-[4-(1,3-Benzothiazol-2-yl)piperazin-1-yl]-2-oxoethyl]-N-(3-chloro-4-hydroxyphenyl)pyrrolidine-3-carboxamideIC50170.0 [1], 270.0 [2], 480.0 [3], 1600.0 [4]
1-[2-[4-(3-Chlorophenyl)piperazin-1-yl]-2-oxoethyl]-N-(4-hydroxyphenyl)pyrrolidine-3-carboxamideIC50920.0 [1], 1650.0 [2], 3400.0 [3], 12200.0 [4]
1-[2-[4-(4-Acetylphenyl)piperazin-1-yl]-2-oxoethyl]-N-(3-chloro-4-hydroxyphenyl)pyrrolidine-3-carboxamideIC50150.0 [1], 270.0 [2], 1200.0 [3], 4200.0 [4]
4-[3-Amino-6-(4-methylsulfonylcyclohexyl)pyrazin-2-yl]-N-benzyl-2-fluorobenzamideIC5029.7 [1], 64.4 [2], 197.0 [3], 206.0 [4]
SeliciclibIC5014000.0 [1], 25000.0 [2]
5Z-7-OxozeaenolIC5080.0 [1], 738.0 [2], 6800.0 [3]
(13R,15S)-13-Methyl-16-oxa-8,9,12,22,24-pentazahexacyclo[15.6.2.16,9.112,15.02,7.021,25]heptacosa-1(24),2,4,6,17,19,21(25)-heptaene-23,27-dioneIC501000.0 [1]
N-[(1S)-1-(3-Chloro-4-fluorophenyl)-2-hydroxyethyl]-2-(oxan-4-ylamino)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidine-7-carboxamideIC501.0 [1], 45.0 [2]
N-[(1S)-1-(3-Chloro-4-fluorophenyl)-2-hydroxyethyl]-2-(oxan-4-ylamino)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidine-7-carboxamideKi0.4 [1]
N-[(1S)-1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl]-2-(oxan-4-ylamino)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidine-7-carboxamideIC502.0 [1], 25.0 [2]
N-[(1S)-1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl]-2-(oxan-4-ylamino)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidine-7-carboxamideKi0.6 [1]
(4S,6E,9R,10S,12E)-9,10,18-Trihydroxy-16-methoxy-4-methyl-3-oxabicyclo[12.4.0]octadeca-1(14),6,12,15,17-pentaene-2,8-dioneIC501600.0 [1], 3700.0 [2], 5100.0 [3]
7-Ethenylsulfonyl-N-(oxan-4-yl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-2-amineIC50220.0 [1], 240.0 [2], 370.0 [3]
N-(3-Pyridin-4-yl-1H-indazol-5-yl)ethenesulfonamideIC507.5 [1], 17.0 [2], 120.0 [3]
5-Ethenylsulfonyl-3-(2-methylpyridin-4-yl)-1,4,6,7-tetrahydropyrazolo[4,3-c]pyridineIC5074.0 [1], 110.0 [2], 380.0 [3]
7-Ethylsulfonyl-N-(Oxan-4-Yl)-6,8-Dihydro-5h-Pyrido[3,4-D]pyrimidin-2-AmineIC509000.0 [1], 10000.0 [2]
N-(3-Pyridin-4-yl-1H-indazol-5-yl)ethanesulfonamideIC50280.0 [1], 1800.0 [2], 10000.0 [3]
4-Fluoro-N-methyl-2-[[2-(oxan-4-ylamino)-5-(trifluoromethyl)pyridin-4-yl]amino]benzamideIC5040.0 [1], 380.0 [2], 2100.0 [3]
N-[2-[[5-Chloro-2-(oxan-4-ylamino)pyridin-4-yl]amino]phenyl]prop-2-enamideIC5042.0 [1], 60.0 [2], 120.0 [3]
N-[2-[[5-Chloranyl-2-(Oxan-4-Ylamino)pyrimidin-4-Yl]amino]phenyl]propanamideIC50480.0 [1], 4000.0 [2], 30000.0 [3]
N-[4-[[5-Chloro-2-(oxan-4-ylamino)pyrimidin-4-yl]amino]pyridin-3-yl]prop-2-enamideIC503.0 [1], 3.1 [2], 6.7 [3]
N-[2-[[5-Methyl-2-(oxan-4-ylamino)pyrimidin-4-yl]amino]phenyl]prop-2-enamideIC5077.0 [1], 88.0 [2], 170.0 [3]
N-[2-[[5-Chloro-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]amino]phenyl]prop-2-enamideIC509.9 [1], 13.0 [2], 48.0 [3]
N-[2-[[5-Chloro-2-[[4-(dimethylamino)cyclohexyl]amino]pyrimidin-4-yl]amino]phenyl]prop-2-enamideIC5072.0 [1], 85.0 [2], 90.0 [3]
N-[2-[[5-Methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]amino]phenyl]prop-2-enamideIC5039.0 [1], 47.0 [2], 66.0 [3]
2-[[2-[(2,5-Dimethylpyrazol-3-yl)amino]-5-(trifluoromethyl)pyridin-4-yl]amino]-4-fluoro-N-methylbenzamideIC5044.0 [1], 340.0 [2], 8700.0 [3]
(3R)-1-[2-[4-(4-Acetylphenyl)piperazin-1-yl]-2-oxoethyl]-N-(3,5-dichloro-4-hydroxyphenyl)pyrrolidine-3-carboxamideIC5010000.0 [1]
1-[(1S)-1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-(oxan-4-ylamino)pyrimidin-4-yl]pyridin-2-oneIC503.9 [1]
1-[(1S)-1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-(oxan-4-ylamino)pyrimidin-4-yl]pyridin-2-oneKi0.6 [1]
1-[(1S)-1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[[(2R)-1-hydroxy-3-methoxypropan-2-yl]amino]pyrimidin-4-yl]pyridin-2-oneIC506.3 [1]
1-[(1S)-1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[[(2R)-1-hydroxy-3-methoxypropan-2-yl]amino]pyrimidin-4-yl]pyridin-2-oneKi3.0 [1]
1-[2-Hydroxy-1-(3-methylphenyl)ethyl]-4-[2-(oxan-4-ylamino)pyrimidin-4-yl]pyridin-2-oneIC503.0 [1]
1-[2-Hydroxy-1-(3-methylphenyl)ethyl]-4-[2-(oxan-4-ylamino)pyrimidin-4-yl]pyridin-2-oneKi1.6 [1]
1-[1-(3-Chloro-5-fluorophenyl)-2-hydroxyethyl]-4-[2-(oxan-4-ylamino)pyrimidin-4-yl]pyridin-2-oneIC503.8 [1]
1-[1-(3-Chloro-5-fluorophenyl)-2-hydroxyethyl]-4-[2-(oxan-4-ylamino)pyrimidin-4-yl]pyridin-2-oneKi0.1 [1]
1-[1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[5-methyl-2-(oxan-4-ylamino)pyrimidin-4-yl]pyridin-2-oneIC5051.8 [1]
1-[1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[5-methyl-2-(oxan-4-ylamino)pyrimidin-4-yl]pyridin-2-oneKi2.2 [1]
1-[1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-(oxan-4-ylamino)pyrimidin-4-yl]pyrimidin-2-oneIC5015.6 [1]
1-[1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-(oxan-4-ylamino)pyrimidin-4-yl]pyrimidin-2-oneKi1.7 [1]
1-[(1S)-1-(3-Chlorophenyl)-2-hydroxyethyl]-4-[2-(oxan-4-ylamino)pyrimidin-4-yl]pyridin-2-oneIC5035.7 [1]
1-[(1S)-1-(3-Chlorophenyl)-2-hydroxyethyl]-4-[2-(oxan-4-ylamino)pyrimidin-4-yl]pyridin-2-oneKi0.3 [1]
N-[2-[[5-Chloro-2-(oxan-4-ylamino)pyrimidin-4-yl]amino]phenyl]prop-2-enamideIC505.4 [1], 8.5 [2], 19.0 [3]
N-[(1S,2S)-1-(3-Chloro-4-fluorophenyl)-2-hydroxypropyl]-2-(propan-2-ylamino)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidine-7-carboxamideIC503.23 [1], 6.0 [2], 200.0 [3]
N-[(1S)-2-Amino-1-(3-chloro-4-fluorophenyl)ethyl]-2-(propan-2-ylamino)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidine-7-carboxamideIC501.9 [1], 2.0 [2], 356.0 [3]
N-[(1S)-1-(3-Chloro-4-fluorophenyl)-2-(methanesulfonamido)ethyl]-2-(propan-2-ylamino)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidine-7-carboxamideIC507.0 [1], 7.1 [2], 917.0 [3]
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-carboxamideIC5025.9 [1], 26.0 [2], 13238.0 [3]
N-[2-[[2-(Oxan-4-ylamino)-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamideIC506.9 [1], 8.5 [2], 22.0 [3]
4-[3-Amino-6-(4-hydroxycyclohexyl)pyrazin-2-yl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-2-fluorobenzamideIC500.09 [1], 0.69 [2], 1.28 [3]
4-[6-(4-Acetamidocyclohexyl)-3-aminopyrazin-2-yl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-2-fluorobenzamideIC500.56 [1], 1.11 [2], 1.19 [3]
4-(2-Amino-5-pyridin-4-ylpyridin-3-yl)-2-fluoro-N-[(1S)-2-hydroxy-1-phenylethyl]benzamideIC500.16 [1], 0.17 [2], 0.49 [3]
4-[3-Amino-6-(4-hydroxycyclohexyl)pyrazin-2-yl]-N-[(1S)-1-(3-bromo-5-fluorophenyl)-2-hydroxyethyl]-2-fluorobenzamideIC500.02 [1], 0.04 [2], 0.54 [3]
4-[3-Amino-6-[4-(methanesulfonamido)cyclohexyl]pyrazin-2-yl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-2-fluorobenzamideIC500.1 [1], 0.26 [2], 2.9 [3]
4-[3-Amino-6-(oxan-4-yl)pyrazin-2-yl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-2-fluorobenzamideIC500.03 [1], 0.09 [2], 0.11 [3]
4-[3-Amino-6-(oxan-4-yl)pyrazin-2-yl]-2-fluoro-N-[(1S,2R)-2-phenylcyclopropyl]benzamideIC500.08 [1], 0.18 [2], 0.21 [3]
Methyl N-[4-[5-amino-6-[4-[[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]carbamoyl]-3-fluorophenyl]pyrazin-2-yl]cyclohexyl]carbamateIC500.1 [1], 0.28 [2], 1.57 [3]
5-IodotubercidinIC501200.0 [1]
5-IodotubercidinKi530.0 [1]
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References

This online tool may be cited as follows

MLA

"Quest Database™ MAP kinase ERK2 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 8 May. 2024, https://www.aatbio.com/data-sets/map-kinase-erk2-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, May 8). Quest Database™ MAP kinase ERK2 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/map-kinase-erk2-inhibitors-ic50-ki.
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