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Epidermal growth factor receptor Inhibitors (IC50, Ki)

Structure
▲
▼
Compound Name
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▼
Standard Type
▲
▼
Standard Values (in nM)
▲
▼
GefitinibIC50845.0 [1]
WZ4002IC503.82 [1]
ErlotinibIC5068.0 [1]
ErlotinibKi95.0 [1]
OsimertinibIC5017.0 [1]
OsimertinibKi2.2 [1], 3.2 [2]
RociletinibIC5046.0 [1]
RociletinibKi1.65 [1], 1.75 [2]
AfatinibIC500.97 [1]
CID 78209992IC502.4 [1]
Unii-5IE92SK9EBIC507.0 [1], 13.0 [2], 21.0 [3], 90.0 [4], 140.0 [5]
Unii-5IE92SK9EBKi4.0 [1]
N-(1H-Indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5H-furo[3,4-d]pyrimidin-4-amineIC50600.0 [1]
N-(1H-Indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5H-furo[3,4-d]pyrimidin-4-amineKi0.2 [1], 0.5 [2], 1.6 [3], 2.0 [4]
N-(7-Chloro-1H-indazol-3-yl)-2-[5-(difluoromethyl)-1H-pyrazol-4-yl]-7,7-dimethyl-5H-furo[3,4-d]pyrimidin-4-amineIC50370.0 [1]
N-(7-Chloro-1H-indazol-3-yl)-2-[5-(difluoromethyl)-1H-pyrazol-4-yl]-7,7-dimethyl-5H-furo[3,4-d]pyrimidin-4-amineKi1.7 [1], 2.5 [2], 3.4 [3], 9.0 [4]
N-(1H-Indazol-3-yl)-7,7-dimethyl-2-(2-methylpyrazol-3-yl)-5H-furo[3,4-d]pyrimidin-4-amineIC503000.0 [1]
N-(1H-Indazol-3-yl)-7,7-dimethyl-2-(2-methylpyrazol-3-yl)-5H-furo[3,4-d]pyrimidin-4-amineKi0.5 [1], 21.3 [2], 34.3 [3]
NaquotinibIC508.0 [1]
CID 71496460IC502.0 [1], 2000.0 [2]
N-[(3R,4R)-4-Fluoro-1-[6-[(1-methylpyrazol-4-yl)amino]-9-propan-2-ylpurin-2-yl]pyrrolidin-3-yl]prop-2-enamideIC502.0 [1], 7.0 [2], 9.0 [3]
N-[4-Methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]-2-[methyl-[2-(methylamino)ethyl]amino]phenyl]prop-2-enamideIC5026.0 [1], 45.0 [2], 26000.0 [3], 45000.0 [4]
N-[5-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-ylpyrimidin-2-yl)amino]-4-methoxy-2-(4-methylpiperazin-1-yl)phenyl]prop-2-enamideIC5019.0 [1], 140.0 [2]
N-[5-[[4-(1H-Indol-3-yl)pyrimidin-2-yl]amino]-4-methoxy-2-(4-methylpiperazin-1-yl)phenyl]prop-2-enamideIC5015.0 [1], 17.0 [2], 63.0 [3], 68.0 [4]
(E)-N-[3-[(5-Chloro-4-pyrazolo[1,5-a]pyridin-3-ylpyrimidin-2-yl)amino]-4-methoxyphenyl]-4-(dimethylamino)but-2-enamideIC5091.0 [1], 96.0 [2], 388.0 [3], 400.0 [4]
1-[(3As,6aR)-2-[6-[4-(4-methylpiperazin-1-yl)anilino]-9-propan-2-ylpurin-2-yl]-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]prop-2-en-1-oneIC508.0 [1], 14.0 [2], 18.0 [3]
N-[(3R,4R)-1-[6-[(1-Ethyl-3-methoxypyrazol-4-yl)amino]-9-methylpurin-2-yl]-4-fluoropyrrolidin-3-yl]prop-2-enamideIC501.0 [1], 2.0 [2], 6.0 [3]
N-[(3R,4R)-4-Fluoro-1-[6-[[3-methoxy-1-(1-methylpyrrolidin-3-yl)pyrazol-4-yl]amino]-9-propan-2-ylpurin-2-yl]pyrrolidin-3-yl]prop-2-enamideIC502.0 [1], 3.0 [2], 5.0 [3], 6.0 [4]
N-[3-[4-(4-Methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]oxyphenyl]prop-2-enamideIC5030.0 [1], 500.0 [2]
N-[3-[4-(4-Methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]oxyphenyl]prop-2-enamideKi0.64 [1], 70.2 [2]
N-[3-[4-(1H-Indazol-3-ylamino)-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl]oxyphenyl]prop-2-enamideIC5070.0 [1], 500.0 [2]
N-[3-[4-(1H-Indazol-3-ylamino)-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl]oxyphenyl]prop-2-enamideKi0.32 [1], 833.0 [2]
N-[3-[7-[2-Methoxy-4-(4-methyl-1,4-diazepan-1-yl)anilino]-3-methyl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC502.11 [1], 2.75 [2], 5.17 [3], 11.0 [4]
N-[3-[7-[4-[4-(Dimethylamino)piperidin-1-yl]-2-methoxyanilino]-3-methyl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC502.41 [1], 2.83 [2], 5.2 [3], 9.52 [4]
N-[3-(7-Anilino-3-methyl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl)phenyl]prop-2-enamideIC5010.9 [1], 12.1 [2], 28.3 [3], 45.7 [4]
N-[3-[3-Methyl-7-(methylamino)-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC50837.1 [1], 1000.0 [2]
N-[3-[3-Methyl-7-[4-(4-methylpiperazin-1-yl)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC500.53 [1], 0.56 [2], 1.19 [3], 1.66 [4]
N-[3-[7-[3-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-3-methyl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC500.63 [1], 1.67 [2], 2.04 [3], 2.31 [4]
N-[3-[7-[2-Ethoxy-4-(4-methylpiperazin-1-yl)anilino]-3-methyl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC502.68 [1], 3.02 [2], 7.1 [3], 12.7 [4]
N-[3-[3-Methyl-7-[4-(4-methylpiperazin-1-yl)-2-propan-2-yloxyanilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC5013.5 [1], 13.7 [2], 36.3 [3], 39.9 [4]
N-[3-[3-Methyl-7-[2-methyl-4-(4-methylpiperazin-1-yl)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC501.21 [1], 1.31 [2], 4.18 [3], 9.37 [4]
N-[3-[7-[2-Fluoro-4-(4-methylpiperazin-1-yl)anilino]-3-methyl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC501000.0 [1]
N-[3-[7-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-2-oxo-3-propan-2-yl-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC500.45 [1], 0.46 [2], 4.42 [3], 6.02 [4]
N-[3-[3-Cyclopropyl-7-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC500.66 [1], 0.73 [2], 6.02 [3], 10.5 [4]
N-[3-[7-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-2-oxo-3-phenyl-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC500.46 [1], 0.51 [2], 0.93 [3], 0.98 [4]
N-[3-[7-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-3-naphthalen-2-yl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC501.16 [1], 1.34 [2], 1.59 [3], 2.44 [4]
N-[3-[3-Benzyl-7-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC500.38 [1], 0.67 [2], 0.72 [3], 0.93 [4]
N-[3-[7-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-2-oxo-3-(4-phenylphenyl)-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC501.67 [1], 3.43 [2], 4.64 [3], 5.24 [4]
N-[3-[7-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-2-oxo-3-(4-phenoxyphenyl)-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC501.66 [1], 2.03 [2], 2.31 [3], 3.57 [4]
N-[3-[7-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-2-oxo-3-(4-phenylmethoxyphenyl)-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC502.42 [1], 2.43 [2], 2.56 [3], 6.31 [4]
1-(3-Aminophenyl)-7-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-3-methyl-4H-pyrimido[4,5-d]pyrimidin-2-oneIC50478.0 [1], 1000.0 [2]
N-[3-[7-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-3-methyl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]propanamideIC501000.0 [1]
N-[3-[7-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-3-methyl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC501.08 [1], 1.21 [2], 3.14 [3], 6.56 [4]
N-[3-[7-[4-(Dimethylamino)-2-methoxyanilino]-3-methyl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC504.95 [1], 6.22 [2], 11.5 [3], 24.9 [4]
N-[3-[7-(2-Methoxy-4-piperidin-1-ylanilino)-3-methyl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC5010.42 [1], 15.4 [2], 36.43 [3], 95.71 [4]
N-[3-[7-(2-Methoxy-4-morpholin-4-ylanilino)-3-methyl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]phenyl]prop-2-enamideIC5010.33 [1], 12.74 [2], 28.85 [3], 60.31 [4]
7-[3-Methyl-4-(4-methylpiperazin-1-yl)anilino]-3-phenyl-1-[(3S)-1-prop-2-enoylpyrrolidin-3-yl]-4H-pyrimido[4,5-d]pyrimidin-2-oneIC503.0 [1], 9.2 [2], 10.0 [3]
N-[4-Methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]-2-(4-methylpiperazin-1-yl)phenyl]prop-2-enamideIC501.0 [1]
N-[4-Methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]-2-(4-methylpiperazin-1-yl)phenyl]prop-2-enamideKi1.46 [1], 1.58 [2]
N-(7-Chloro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5H-furo[3,4-d]pyrimidin-4-amineKi0.4 [1], 1.3 [2], 2.0 [3]
N-[3-[2-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-6-methyl-5,8-dioxo-7H-pyrimido[4,5-e][1,4]diazepin-9-yl]phenyl]prop-2-enamideIC5015.11 [1], 22.34 [2], 52.63 [3], 110.1 [4]
N-[3-[12-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-2,8-dioxo-3,9,11,13-tetrazatricyclo[8.4.0.03,7]tetradeca-1(14),10,12-trien-9-yl]phenyl]prop-2-enamideIC501000.0 [1]
N-[3-[6-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-2,10-dioxo-1,5,7,9-tetrazatricyclo[9.4.0.03,8]pentadeca-3,5,7-trien-9-yl]phenyl]prop-2-enamideIC502.74 [1], 4.3 [2], 40.73 [3], 114.99 [4]
N-[3-[2-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-6,7-dimethyl-5,8-dioxo-7H-pyrimido[4,5-e][1,4]diazepin-9-yl]phenyl]prop-2-enamideIC506.02 [1], 41.59 [2], 50.85 [3], 122.45 [4]
N-[3-[2-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-6-methyl-5,8-dioxo-7-propan-2-yl-7H-pyrimido[4,5-e][1,4]diazepin-9-yl]phenyl]prop-2-enamideIC5024.11 [1], 24.83 [2], 44.05 [3], 56.49 [4]
N-[3-[7-Butan-2-yl-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-6-methyl-5,8-dioxo-7H-pyrimido[4,5-e][1,4]diazepin-9-yl]phenyl]prop-2-enamideIC507.25 [1], 13.25 [2], 86.76 [3], 87.45 [4]
N-[3-[2-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-6-methyl-5,8-dioxo-7-phenyl-7H-pyrimido[4,5-e][1,4]diazepin-9-yl]phenyl]prop-2-enamideIC5077.09 [1], 173.73 [2], 778.15 [3], 1000.0 [4]
N-[3-[2-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-5,8-dioxo-6-phenyl-7H-pyrimido[4,5-e][1,4]diazepin-9-yl]phenyl]prop-2-enamideIC506.86 [1], 30.74 [2], 193.97 [3], 221.2 [4]
N-[3-[7-Benzyl-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-6-methyl-5,8-dioxo-7H-pyrimido[4,5-e][1,4]diazepin-9-yl]phenyl]prop-2-enamideIC505.3 [1], 8.33 [2], 8.95 [3], 16.46 [4]
N-[3-[2-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-7-[(4-methoxyphenyl)methyl]-6-methyl-5,8-dioxo-7H-pyrimido[4,5-e][1,4]diazepin-9-yl]phenyl]prop-2-enamideIC5050.02 [1], 53.94 [2], 88.34 [3], 97.12 [4]
N-[3-[7-[(4-Chlorophenyl)methyl]-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-6-methyl-5,8-dioxo-7H-pyrimido[4,5-e][1,4]diazepin-9-yl]phenyl]prop-2-enamideIC5034.67 [1], 59.36 [2], 62.19 [3], 87.23 [4]
N-[3-[7-[(4-Fluorophenyl)methyl]-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-6-methyl-5,8-dioxo-7H-pyrimido[4,5-e][1,4]diazepin-9-yl]phenyl]prop-2-enamideIC507.57 [1], 14.08 [2], 17.91 [3], 24.53 [4]
N-[3-[6-Benzyl-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-5,8-dioxo-7H-pyrimido[4,5-e][1,4]diazepin-9-yl]phenyl]prop-2-enamideIC508.4 [1], 9.12 [2], 32.83 [3], 84.25 [4]
StaurosporineIC500.6 [1], 1.1 [2], 10.6 [3]
4-[(3-Bromophenyl)amino]-6-acrylamidoquinazolineIC501.0 [1], 1.1 [2], 28.0 [3]
NazartinibIC509.0 [1], 11.0 [2], 25.0 [3]
N-[(3R,4R)-1-[6-[(1,3-Dimethylpyrazol-4-yl)amino]-9-propan-2-ylpurin-2-yl]-4-fluoropyrrolidin-3-yl]prop-2-enamideIC502127.0 [1], 6138.0 [2], 6651.0 [3]
CID 46864270IC50231.0 [1], 3000.0 [2]
N-[3-[2-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]prop-2-enamideIC500.8 [1], 4.0 [2], 12.0 [3]
N-[2-(4-Methoxypiperidin-1-yl)pyrimidin-4-yl]-1-propan-2-ylimidazo[4,5-c]pyridin-6-amineKi40.0 [1], 211.0 [2]
N-[(3S)-1-[9-(2-Hydroxyethyl)-6-[4-(4-methylpiperazin-1-yl)anilino]purin-2-yl]pyrrolidin-3-yl]prop-2-enamideIC507.0 [1], 31.0 [2], 387.0 [3]
(1R)-1-[6-[[2-[(3R,4S)-3-Fluoro-4-methoxypiperidin-1-yl]pyrimidin-4-yl]amino]-1-[(2R)-1,1,1-trifluoropropan-2-yl]imidazo[4,5-c]pyridin-2-yl]ethanolIC5027.0 [1]
(1R)-1-[6-[[2-[(3R,4S)-3-Fluoro-4-methoxypiperidin-1-yl]pyrimidin-4-yl]amino]-1-[(2R)-1,1,1-trifluoropropan-2-yl]imidazo[4,5-c]pyridin-2-yl]ethanolKi1.1 [1], 7.0 [2]
N-[3-[[5-Chloro-2-[(2E)-2-[1-(4-fluorophenyl)ethylidene]hydrazinyl]pyrimidin-4-yl]amino]phenyl]prop-2-enamideIC501290.0 [1], 1680.0 [2], 2530.0 [3]
(E)-N-[3-[[2-[(2E)-2-[(1-Benzylindol-3-yl)methylidene]hydrazinyl]-5-chloropyrimidin-4-yl]amino]phenyl]-4-(dimethylamino)but-2-enamideIC50760.0 [1], 790.0 [2], 880.0 [3]
(E)-N-[3-[[5-Chloro-2-[(2E)-2-[1-(2,4-difluorophenyl)ethylidene]hydrazinyl]pyrimidin-4-yl]amino]phenyl]-4-(dimethylamino)but-2-enamideIC50720.0 [1], 820.0 [2], 1250.0 [3]
(E)-N-[3-[[5-Chloro-2-[(2E)-2-[(2-fluorophenyl)methylidene]hydrazinyl]pyrimidin-4-yl]amino]phenyl]-4-(dimethylamino)but-2-enamideIC50790.0 [1], 1560.0 [2], 3270.0 [3]
(E)-N-[3-[[5-Chloro-2-[(2E)-2-[(4-fluorophenyl)methylidene]hydrazinyl]pyrimidin-4-yl]amino]phenyl]-4-(dimethylamino)but-2-enamideIC50680.0 [1], 1490.0 [2], 2230.0 [3]
(E)-N-[3-[[5-Chloro-2-[(2E)-2-[(2,4-difluorophenyl)methylidene]hydrazinyl]pyrimidin-4-yl]amino]phenyl]-4-(dimethylamino)but-2-enamideIC502510.0 [1], 2520.0 [2], 5110.0 [3]
N-[3-[[5-Chloro-2-[(2E)-2-[(4-fluorophenyl)methylidene]hydrazinyl]pyrimidin-4-yl]amino]phenyl]prop-2-enamideIC50570.0 [1], 860.0 [2], 1120.0 [3]
N-[3-[[5-Chloro-2-[(2E)-2-[(2-fluorophenyl)methylidene]hydrazinyl]pyrimidin-4-yl]amino]phenyl]prop-2-enamideIC501510.0 [1], 1910.0 [2], 4740.0 [3]
1-[4-[3-Chloro-4-[(3-fluorophenyl)methoxy]anilino]quinazolin-6-yl]-3-(2-piperidin-1-ylethyl)ureaIC50500.0 [1], 2030.0 [2], 2380.0 [3]
1-[4-[3-Chloro-4-[(3-fluorophenyl)methoxy]anilino]quinazolin-6-yl]-3-(2-piperidin-1-ylethyl)thioureaIC50500.0 [1], 1760.0 [2], 2310.0 [3]
N-[3-[2-[2-Methoxy-4-(4-methylpiperazin-1-yl)anilino]-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]prop-2-enamideIC500.5 [1], 3.0 [2]
9-[[8-Fluoro-6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl]sulfanyl]-4-methyl-[1,4]oxazino[3,2-c]quinolin-3-oneIC5030000.0 [1]
(3R,4S)-3-Fluoro-1-[4-[[2-[(1R)-1-hydroxyethyl]-1-[(2R)-1,1,1-trifluoropropan-2-yl]imidazo[4,5-c]pyridin-6-yl]amino]pyrimidin-2-yl]piperidin-4-olIC5081.0 [1]
(3R,4S)-3-Fluoro-1-[4-[[2-[(1R)-1-hydroxyethyl]-1-[(2R)-1,1,1-trifluoropropan-2-yl]imidazo[4,5-c]pyridin-6-yl]amino]pyrimidin-2-yl]piperidin-4-olKi2.5 [1], 6.0 [2]
NeratinibIC503.0 [1], 66.0 [2]
DacomitinibIC500.63 [1], 42.0 [2]
CanertinibIC503.0 [1]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Epidermal growth factor receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 9 May. 2024, https://www.aatbio.com/data-sets/epidermal-growth-factor-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, May 9). Quest Database™ Epidermal growth factor receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/epidermal-growth-factor-receptor-inhibitors-ic50-ki.
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