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Couple-a-new-PDB’s

2BDF, and 2BDJ These are the SRC / Abl phosphine oxide bearing purines from Ariad. Good stuff with a free bonus link to the published discussion: Chem Biol Drug Des 2006, 46. x-ray crystallography,...

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US7125875

The claims are basically: Swallow Dasatinib wherein the cancer is Gleevec resistant. Read the J Med Chems (here, and here). BMS has been prolific in writing about their aminothiazoles and there’s...

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TG100801

Hi TargeGen. So whats with the new VEGF compound, eh?  Oh well. I also see you’ve disclosed that it’s an ester prodrug that hits VEGFR2 / PDGFR / SRC so its either a pyrimidine from WO2006101977 or a...

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US20060247217

Not terribly new, but none-the-less entertaining. This is a divisional application of Wyeth’s 6,6,6 5,6,6 and 6,5,6 tricycles. They are SRC inhibitors, and there’s already a J. Med. Chem....

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US20060247250

Hi TargeGen, I see you’ve got another handful of compounds in another SRC inhibitor application. I guess selectivity has never been a real big thing down there in San Diego. These look suspiciously...

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2 PDBs today

Today’s update to the PDB contains two interesting SRC / Abl inhibitors. BMS’s dasatinib in Abl is 2GQG Astra’s AZD0530 in SRC is 2H8H

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Who’s in CA?

No, not Canada, A? SF, CA – Here, have a sequal to the Prague entry: This is what you’re missing at YawnFest ’07, err I mean: the MMTC: Wyeth talks Src/Abl: SKI-606 (American Cyanamid: WO/2000/018740)...

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KX2-391

Kinex filed an IND today for this ‘ere compound: KX-01, KX2-391, ALB-30350, wait, ALB-30350? yah… from WO/2006/071960: Note that KX2-391 has weak activity against isolated kinases because the peptide...

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TargaGen closes…

Closes a 40M series D that is. Kudos Pros. Some of the more recent thiazole apps like US20070161645 appear to my eye to be the Src/Abl backup brigade. wt Abl 1.5 nM T315I 18 nM So you like pictures?...

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PDB Update

Aurora A + 680: 3E5A; Protien Sci Aurora B: 2VGO; Mol Cell Ther SRC: 3EL7 & 3EL8; Chem Biol; EPHB4: 2VWX; 2VWY; 2VX0, 2VX1 Posted in Aurora, EphB4, PDB, SRC

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