General Information of Drug (ID: DMMESBW)

Drug Name
PMID20005102C1 Drug Info
Synonyms GTPL8181; BDBM50305878; B99
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
46225540
TTD Drug ID
DMMESBW

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Investigative Drug(s)
Approved Drug(s)
Discontinued Drug(s)
Patented Agent(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
AR-12 DM4RK6P Lymphoma 2A80-2A86 Phase 1 [2]
L-serine-O-phosphate DMTJ1NH Discovery agent N.A. Investigative [3]
BX-912 DMZA45C Discovery agent N.A. Investigative [4]
BX-795 DMRIMLJ Discovery agent N.A. Investigative [4]
PHT-427 DMI96Y3 Discovery agent N.A. Investigative [5]
PF-5177624 DMUOFT0 Solid tumour/cancer 2A00-2F9Z Investigative [6]
GSK-2334470 DM3BI7R Solid tumour/cancer 2A00-2F9Z Investigative [7]
⏷ Show the Full List of 7 Drug(s)
Drug(s) Targeting PAK-1 protein kinase (PAK1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
RKI-1447 DMGTAWC Discovery agent N.A. Investigative [8]
Il-94 DMPNQ27 Discovery agent N.A. Investigative [9]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Capivasertib DM9SKW8 Breast cancer 2C60-2C65 Approved [10]
Enzastaurin DM5H0R9 Diffuse large B-cell lymphoma 2A81 Phase 3 [10]
GDC-0068 DMWBZJD Breast cancer 2C60-2C65 Phase 3 [10]
CI-1033 DMSI8N3 Lymphoma 2A80-2A86 Phase 2 [11]
CMX-2043 DMPSCVY Cardiac disease BA00-BE2Z Phase 2 [12]
ARQ 092 DM5WK0J Proteus syndrome LD2C Phase 2 [13]
GSK2110183 DMZHB37 leukaemia 2A60-2B33 Phase 2 [14]
RX-0201 DMTBAV3 Pancreatic cancer 2C10 Phase 2 [15]
PTX-200 DM0ZIT2 Breast cancer 2C60-2C65 Phase 2 [10]
Triciribine prodrug DMBN1XS Solid tumour/cancer 2A00-2F9Z Phase 1/2 [14]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Capivasertib DM9SKW8 Breast cancer 2C60-2C65 Approved [16]
ARQ 092 DM5WK0J Proteus syndrome LD2C Phase 2 [2]
MK-2206 DMT1OZ6 Rectal adenocarcinoma 2B92 Phase 2 [17]
GSK2141795 DMSHE70 Colorectal cancer 2B91.Z Phase 2 [18]
M2698 DM3PVBJ Solid tumour/cancer 2A00-2F9Z Phase 1 [10]
LYS-6KAKT1 DMLXGAI Solid tumour/cancer 2A00-2F9Z Phase 1 [19]
LY2780301 DM93AJW Solid tumour/cancer 2A00-2F9Z Phase 1 [20]
XL418 DME0F5W Solid tumour/cancer 2A00-2F9Z Phase 1 [21]
SR13668 DMO5760 Solid tumour/cancer 2A00-2F9Z Phase 1 [22]
TCN-P DMV0AH8 Acute myeloid leukaemia 2A60 Phase 1 [23]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BALANOL DMDLN9E N. A. N. A. Terminated [24]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol DMSKJ1X Discovery agent N.A. Investigative [25]
Ro-4396686 DM5DMCH Discovery agent N.A. Investigative [26]
[3H]cAMP DMZRQU7 Discovery agent N.A. Investigative [27]
PMID19364658C33 DMSE1C3 Discovery agent N.A. Investigative [28]
BX-912 DMZA45C Discovery agent N.A. Investigative [4]
BX-795 DMRIMLJ Discovery agent N.A. Investigative [4]
chelerythrine DMCP1G9 Discovery agent N.A. Investigative [29]
PMID21742770C1 DME3JMH Discovery agent N.A. Investigative [30]
Rp-adenosine 3',5'-cyclic monophosphothioate triethylamine (Rp-cAMPS) DM1JWGH Discovery agent N.A. Investigative [31]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
M2698 DM3PVBJ Solid tumour/cancer 2A00-2F9Z Phase 1 [10]
NNI-362 DMPCV65 Alzheimer disease 8A20 Phase 1 [32]
PF-4708671 DMO0892 Ulcerative colitis DD71 Clinical trial [33]
PMID27410995-Compound-Figure3c DMDQMZT N. A. N. A. Patented [34]
Pyrimido[4,5-d] pyrimidines and pyrido[4,3-d] pyrimidine derivative 1 DM6O2Q9 N. A. N. A. Patented [34]
RO-316233 DMAGLPW Discovery agent N.A. Investigative [35]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol DMSKJ1X Discovery agent N.A. Investigative [25]
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole DMN9YOB Discovery agent N.A. Investigative [36]
CI-1040 DMF3DZX Discovery agent N.A. Investigative [35]
KN-62 DMLZ89P Discovery agent N.A. Investigative [35]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Akt inhibitor VIII DMDVIT1 Discovery agent N.A. Investigative [37]
PHT-427 DMI96Y3 Discovery agent N.A. Investigative [5]

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Fungal Protein kinase A (Fung ypkA) TTYVI76 Q56921_YEREN Inhibitor [1]
PAK-1 protein kinase (PAK1) TTFN95D PAK1_HUMAN Inhibitor [1]
Phosphoinositide dependent protein kinase-1 (PDPK1) TT9QBI6 PDPK1_HUMAN Inhibitor [1]
RAC-alpha serine/threonine-protein kinase (AKT1) TTWTSCV AKT1_HUMAN Inhibitor [1]
RAC-beta serine/threonine-protein kinase (AKT2) TTH24WI AKT2_HUMAN Inhibitor [1]
RAC-gamma serine/threonine-protein kinase (AKT3) TTAZ05C AKT3_HUMAN Inhibitor [1]
Ribosomal protein S6 kinase beta-1 (S6K1) TTG0U4H KS6B1_HUMAN Inhibitor [1]

References

1 2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles. Bioorg Med Chem Lett. 2010 Jan 15;20(2):679-83.
2 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
3 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
4 Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74.
5 Molecular pharmacology and antitumor activity of PHT-427, a novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor. Mol Cancer Ther. 2010 Mar;9(3):706-17.
6 Targeting 3-phosphoinoside-dependent kinase-1 to inhibit insulin-like growth factor-I induced AKT and p70 S6 kinase activation in breast cancer cells. PLoS One. 2012;7(10):e48402.
7 Genetic inactivation or pharmacological inhibition of Pdk1 delays development and inhibits metastasis of Braf(V600E)::Pten(-/-) melanoma. Oncogene. 2014 Aug 21;33(34):4330-9.
8 Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2). Medchemcomm. 2012 Jun 1;3(6):699-709.
9 PAK1: A Therapeutic Target for Cancer Treatment. ACS Med Chem Lett. 2013 Mar 19;4(5):431-2.
10 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
11 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
12 Pre-clinical and Clinical Safety Studies of CMX-2043: a cytoprotective lipoic acid analogue for ischaemia-reperfusion injury. Basic Clin Pharmacol Toxicol. 2014 Nov;115(5):456-64.
13 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
14 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1479).
15 CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008.
16 The novel AKT inhibitor afuresertib shows favorable safety, pharmacokinetics, and clinical activity in multiple myeloma. Blood. 2014 Oct 2;124(14):2190-5.
17 First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors.J Clin Oncol.2011 Dec 10;29(35):4688-95.
18 Inhibiting the akt pathway in cancer treatment: three leading candidates. P T. 2011 Apr;36(4):225-7.
19 DOI: 10.1016/S1359-6349(10)71767-5
20 A first-in-human phase I trial of LY2780301, a dual p70 S6 kinase and Akt Inhibitor, in patients with advanced or metastatic cancer. Invest New Drugs. 2015 Jun;33(3):710-9.
21 Targeting the phosphoinositide 3-kinase (PI3K) pathway in cancer
22 Phase 0 clinical chemoprevention trial of the Akt inhibitor SR13668. Cancer Prev Res (Phila). 2011 Mar;4(3):347-53.
23 Phase I pharmacokinetic and pharmacodynamic study of triciribine phosphate monohydrate, a small-molecule inhibitor of AKT phosphorylation, in adult subjects with solid tumors containing activated AKT.Invest New Drugs.2011 Dec;29(6):1381-9.
24 Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry. J Med Chem. 2005 Sep 8;48(18):5613-38. Address;
25 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006 Nov 2;49(22):6500-9.
26 Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3.
27 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1694).
28 Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). Bioorg Med Chem. 2009 May 1;17(9):3342-51.
29 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8.
30 A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells. ACS Med Chem Lett. 2012 Dec 13;3(12):1034-1038.
31 Inhibition of protein kinase A activity interferes with long-term, but not short-term, memory of conditioned taste aversions. Behav Neurosci. 2002 Dec;116(6):1070-4.
32 Novel pharmacotherapy: NNI-362, an allosteric p70S6 kinase stimulator, reverses cognitive and neural regenerative deficits in models of aging and disease. Stem Cell Res Ther. 2021 Jan 13;12(1):59.
33 Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). Biochem J. 2010 Oct 15;431(2):245-55.
34 Ribosomal S6 kinase (RSK) modulators: a patent review.Expert Opin Ther Pat. 2016 Sep;26(9):1061-78.
35 Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
36 Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47.
37 Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg Med Chem Lett. 2005 Feb 1;15(3):761-4.