Target
cGMP-dependent protein kinase 1
Ligand
BDBM3049
Substrate
Histone II-A
Meas. Tech.
cGPK assay
IC50
4800±n/a nM
Citation
 Kleinschroth, JHartenstein, JRudolph, CSchachtele, C Novel Indolocarbazole protein kinase C inhibitors with improved biochemical and physicochemical properties. Bioorg Med Chem Lett 5:55-60 (1995)    Article 
Target
Name:
cGMP-dependent protein kinase 1
Synonyms:
CGK 1 alpha | KGP1_BOVIN | PRKG1 | PRKG1B | PRKGR1A | PRKGR1B | cGMP-Dependent Protein Kinase | cGMP-dependent protein kinase 1 alpha | cGMP-dependent protein kinase 1, alpha isozyme
Type:
Enzyme
Mol. Mass.:
76413.14
Organism:
Bos taurus (bovine)
Description:
n/a
Residue:
671
Sequence:
MSELEEDFAKILMLKEERIKELEKRLSEKEEEIQELKRKLHKCQSVLPVPSTHIGPRTTRAQGISAEPQTYRSFHDLRQAFRKFTKSERSKDLIKEAILDNDFMKNLELSQIQEIVDCMYPVEYGKDSCIIKEGDVGSLVYVMEDGKVEVTKEGVKLCTMGPGKVFGELAILYNCTRTATVKTLVNVKLWAIDRQCFQTIMMRTGLIKHTEYMEFLKSVPTFQSLPEEILSKLADVLEETHYENGEYIIRQGARGDTFFIISKGKVNVTREDSPNEDPVFLRTLGKGDWFGEKALQGEDVRTANVIAAEAVTCLVIDRDSFKHLIGGLDDVSNKAYEDAEAKAKYEAEAAFFANLKLSDFNIIDTLGVGGFGRVELVQLKSEESKTFAMKILKKRHIVDTRQQEHIRSEKQIMQGAHSDFIVRLYRTFKDSKYLYMLMEACLGGELWTILRDRGSFEDSTTRFYTACVVEAFAYLHSKGIIYRDLKPENLILDHRGYAKLVDFGFAKKIGFGKKTWTFCGTPEYVAPEIILNKGHDISADYWSLGILMYELLTGSPPFSGPDPMKTYNIILRGIDMIEFPKKIAKNAANLIKKLCRDNPSERLGNLKNGVKDIQKHKWFEGFNWEGLRKGTLTPPIIPSVASPTDTSNFDSFPEDNDEPPPDDNSGWDIDF
  
Inhibitor
Name:
BDBM3049
Synonyms:
23-[3-(dimethylamino)-2-hydroxypropyl]-7-methoxy-3-methyl-3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^{11,15}.0^{17,22}]tricosa-1(16),2(10),4,6,8,11(15),17(22),18,20-nonaene-12,14-dione | Go 7874 | Indolocarbazole deriv.
Type:
Small organic molecule
Emp. Form.:
C27H26N4O4
Mol. Mass.:
470.5197
SMILES:
COc1ccc2n(C)c3c(c4C(=O)NC(=O)c4c4c5ccccc5n(CC(O)CN(C)C)c34)c2c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Histone II-A
Synonyms:
n/a
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
n/a
Description:
Unfractionated whole histone. 10 uM ATP (0.3 uCi [gamma-32P]ATP) as co-substrate.
Residue:
3
Sequence:
NA