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Target
cGMP-dependent protein kinase 1
Ligand
BDBM50398379
Substrate
n/a
Meas. Tech.
ChEMBL_875871 (CHEMBL2187609)
IC50
98±n/a nM
Citation
Blake, JF; Xu, R; Bencsik, JR; Xiao, D; Kallan, NC; Schlachter, S; Mitchell, IS; Spencer, KL; Banka, AL; Wallace, EM; Gloor, SL; Martinson, M; Woessner, RD; Vigers, GP; Brandhuber, BJ; Liang, J; Safina, BS; Li, J; Zhang, B; Chabot, C; Do, S; Lee, L; Oeh, J; Sampath, D; Lee, BB; Lin, K; Liederer, BM; Skelton, NJ Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem 55:8110-27 (2012) [PubMed] Article
More Info.:
Target
Name:
cGMP-dependent protein kinase 1
Synonyms:
GMP-dependent protein kinase I | KGP1_HUMAN | PRKG1 | PRKG1B | PRKGR1A | PRKGR1B | Protein Kinase G | cGMP-dependent protein kinase | cGMP-dependent protein kinase 1 | cGMP-dependent protein kinase 1 beta
Type:
Protein
Mol. Mass.:
76358.04
Organism:
Human
Description:
Q13976
Residue:
671
Sequence:
MSELEEDFAKILMLKEERIKELEKRLSEKEEEIQELKRKLHKCQSVLPVPSTHIGPRTTRAQGISAEPQTYRSFHDLRQAFRKFTKSERSKDLIKEAILDNDFMKNLELSQIQEIVDCMYPVEYGKDSCIIKEGDVGSLVYVMEDGKVEVTKEGVKLCTMGPGKVFGELAILYNCTRTATVKTLVNVKLWAIDRQCFQTIMMRTGLIKHTEYMEFLKSVPTFQSLPEEILSKLADVLEETHYENGEYIIRQGARGDTFFIISKGTVNVTREDSPSEDPVFLRTLGKGDWFGEKALQGEDVRTANVIAAEAVTCLVIDRDSFKHLIGGLDDVSNKAYEDAEAKAKYEAEAAFFANLKLSDFNIIDTLGVGGFGRVELVQLKSEESKTFAMKILKKRHIVDTRQQEHIRSEKQIMQGAHSDFIVRLYRTFKDSKYLYMLMEACLGGELWTILRDRGSFEDSTTRFYTACVVEAFAYLHSKGIIYRDLKPENLILDHRGYAKLVDFGFAKKIGFGKKTWTFCGTPEYVAPEIILNKGHDISADYWSLGILMYELLTGSPPFSGPDPMKTYNIILRGIDMIEFPKKIAKNAANLIKKLCRDNPSERLGNLKNGVKDIQKHKWFEGFNWEGLRKGTLTPPIIPSVASPTDTSNFDSFPEDNDEPPPDDNSGWDIDF
Inhibitor
Name:
BDBM50398379
Synonyms:
CHEMBL2177390 | US10550114, Compound GDC-0068 | US20230286979, Positive control GDC-0068 | US20230321108, Positive control GDC-0068
Type:
Small organic molecule
Emp. Form.:
C24H32ClN5O2
Mol. Mass.:
457.996
SMILES:
CC(C)NC[C@@H](C(=O)N1CCN(CC1)c1ncnc2[C@H](O)C[C@@H](C)c12)c1ccc(Cl)cc1 |r|