Recent developments in fragment-based drug discovery.

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Congreve M, Chessari G, Tisi D, Woodhead AJ

Recent developments in fragment-based drug discovery.

J Med Chem. 2008 Jul 10;51(13):3661-80. doi: 10.1021/jm8000373. Epub 2008 May 6.

PubMed ID
18457385 [ View in PubMed
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Abstract

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DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
(2R)-1-(2,6-dimethylphenoxy)propan-2-amineUrokinase-type plasminogen activatorIC 50 (nM)>1000000N/AN/ADetails
(S)-2-[(R)-3-amino-4-(2-fluorophenyl)butyryl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamideDipeptidyl peptidase 4IC 50 (nM)23N/AN/ADetails
1-(1-phenylcyclopentyl)methylamineDipeptidyl peptidase 4IC 50 (nM)40000N/AN/ADetails
2-(4-hydroxyphenyl)benzo[b]thiophen-6-olEstrogen receptor alphaEC 50 (nM)1400N/AN/ADetails
2-Amino-1H-benzimidazol-5-olUrokinase-type plasminogen activatorIC 50 (nM)200000N/AN/ADetails
2-Amino-3-Methyl-1-Pyrrolidin-1-Yl-Butan-1-OneDipeptidyl peptidase 4Ki (nM)2000N/AN/ADetails
2-Amino-6-ChloropyrazineCyclin-dependent kinase 2IC 50 (nM)350000N/AN/ADetails
4-(2-aminoethoxy)-N-(3-chloro-2-ethoxy-5-piperidin-1-ylphenyl)-3,5-dimethylbenzamideUrokinase-type plasminogen activatorIC 50 (nM)72N/AN/ADetails
4-[(6-chloropyrazin-2-yl)amino]benzenesulfonamideCyclin-dependent kinase 2IC 50 (nM)9100N/AN/ADetails
6-(4-{(1S,2S)-2-AMINO-1-[(DIMETHYLAMINO)CARBONYL]-3-[(3S)-3-FLUOROPYRROLIDIN-1-YL]-3-OXOPROPYL}PHENYL)-1H-[1,2,4]TRIAZOLO[1,5-A]PYRIDIN-4-IUMDipeptidyl peptidase 4Ki (nM)4.3N/AN/ADetails
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolinePhenylethanolamine N-methyltransferaseIC 50 (nM)3N/AN/ADetails
N-[(2R,3S)-3-AMINO-2-HYDROXY-4-PHENYLBUTYL]-4-METHOXY-2,3,6-TRIMETHYLBENZENESULFONAMIDEProthrombinIC 50 (nM)12000N/AN/ADetails
N-[3-(aminomethyl)benzyl]acetamidineNitric oxide synthase, brainKi (nM)7300N/AN/ADetails
RaloxifeneEstrogen receptor alphaEC 50 (nM)22N/AN/ADetails