KinasePro

Kinase Chemistry – Just a year and a half behind the times.

Archive for September, 2007

The Thursday List

Posted by kinasepro on September 29, 2007

So a handful of you want The Thursday list?

Send me your GMail address and I will share my Google-Doc.  If I like you I may even give you the ability to edit it.

 >> Update >> Perhaps I wasn’t clear above.  The thursday list is now being kept as a google document.  You’ll need a google or gmail account to access it.  You should note that through this system your gmail ‘name’ and / or email address may inadvertantly be made known to others on the list.  Keep this in mind, and if you would like to be taken off, or change the address you access the lists with just email me.

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Posted in Application List | 38 Comments »

PDB Update

Posted by kinasepro on September 26, 2007

VEGF: Amgen: J Med Chem; 2QU5; 2QU6 (C817A, V916T, E990V)

O=C(C1=NC=CC(OC2=CC=C3C(N=C(NC4=CC=C(Cl)C(C(F)(F)F)=C4)N3)=C2)=C1)NC

FGFR2: NYU: “A Molecular Brake” Mol. Cell
WT 2PSQ
WT 2PVF w/substrate
K659N 2PVY
N549H 2PWL
E565G 2PY3
N549T 2PZ5
K526E 2PZP
K641R 2PZR
E565A 2Q0B

CK2: 2OXD,2OXX,2OXY, ChemBiochem

EphA5: 2R2P (SGC)

Posted in PDB | 10 Comments »

Array: Bag ‘o’ cash en route

Posted by kinasepro on September 25, 2007

40M up front:

…Array will grant Celgene an option to select drugs developed under the collaboration that are directed to two of four mutually selected discovery targets

Looks like unpartnerds include: KSP, P38, P38/tie2, Erbb1-2RAF, TLR’s, etc

Posted in Array, Celgene, Deals | Leave a Comment »

Raf… Weird…

Posted by kinasepro on September 23, 2007

Wyeth’s got some new RAF stuff with US20070219186:

O=C(NC2=CC=CC(C3=CC=NC4=C(C5=CC=C(CN6CCCC6)C=C5)C=NN34)=C2)C1=CC=CC(C(F)(F)F)=C1

data on p19

This one’s got me wondering…

Posted in RAF, Wyeth | 7 Comments »

WO/2007/103308

Posted by kinasepro on September 19, 2007

It’s an Array / Genentech c-Met app:

CCN(CC3)C[C@H](F)[C@H]3NC1=NNC2=C1C(OC4=CC=C(N([H])C(C5=CC=NN(C6=CC=C(F)C=C6)C5=O)=O)C=C4F)=CC=N2

Posted in Array, c-Met, Genentech | 8 Comments »

PDB Update

Posted by kinasepro on September 18, 2007

Big week

2QOH; PPY-A bound to Abl via Ariad; Chem Biol Drug Des
2Z60; PPY-A bound to T315I Abl

O=C(C1=CC(C2=CN=C(NC=C3C4=CC=CC=C4OC)C3=C2)=CN=C1)N(C)C

(compounds from SGX)

2OH4; Benzimidazole bound to VEGF via GSK JP; J Med Chem

2V7A; PHA-739358 bound to T315I mutant of Abl via Nerviano; Cancer Res

2IN6 Wee1
2IO6 Wee1

Posted in bcr abl, PDB, VEGF | 5 Comments »

VX-702

Posted by kinasepro on September 15, 2007

Vertex’s Ph2 p38 inhibitor:

FC1=CC=CC(F)=C1N(C(N([H])[H])=O)C2=CC=C(C(N)=O)C(C3=CC=C(F)C=C3F)=N2

is described in WO/2007/103468; model below

Read the rest of this entry »

Posted in p38, Vertex | 24 Comments »

2V7O

Posted by kinasepro on September 11, 2007

2V7O is the structure of CAMK2-γ with BIM9 via the SGC.

O=C1C(C2=CN(C)C3=C2C=CC=C3)=C(C4=CN(CCCSC(N)=N)C5=C4C=CC=C5)C(N1)=O

Posted in PDB | Leave a Comment »

PDB Update

Posted by kinasepro on September 7, 2007

2E14 is ERK2 complexed to the macrocycle: FR-148083 via Astellas

BBRC: “Role of a cysteine residue in the active site of ERK and the MAPKK family”

O=C(C1=C(O[H])C=C(OC)C=C1/C=C/C[C@H](O)[C@@H]2O)O[C@@H](C)C\C=C/C2=O

related…

Posted in ERK, PDB | 16 Comments »

BIBW-2992

Posted by kinasepro on September 7, 2007

BI’s irreversible ErbB inhibitor to join the Ph3 club.

O=C(/C=C/CN(C)C)NC3=CC2=C(N=CN=C2C=C3O[C@H]4COCC4)NC1=CC=C(C(Cl)=C1)F

>> update they’ve named it Tovok

Posted in BI, EGF, Phase III | 4 Comments »