gdc-0068 profile

ipatasertib: an Akt kinase inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	24788740
CHEMBL ID	2177390
CHEBI ID	95089
SCHEMBL ID	191659
MeSH ID	M0587982

Synonym
gdc 0068
rg-7440
rg7440
1001264-89-6
BCP9000712
bdbm50398379
chembl2177390 ,
ipatasertib
HY-15186
CS-0975
0rf ,
(2s)-2-(4-chlorophenyl)-1-{4-[(5r,7r)-7-hydroxy-5-methyl-6,7-dihydro-5h-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl}-3-(propan-2-ylamino)propan-1-one
gdc-0068
BCP0726000195
NCGC00346714-01
S2808
(2s)-2-(4-chlorophenyl)-1-(4-((5r,7r)-7-hydroxy-5-methyl-6,7-dihydro-5h-cyclopenta(d)pyrimidin-4-yl)piperazin-1-yl(-3-((propan-2-yl)amino)propan-1-one
ipatasertib [usan:inn]
1-propanone, 2-(4-chlorophenyl)-1-(4-((5r,7r)-6,7-dihydro-7-hydroxy-5-methyl-5h-cyclopentapyrimidin-4-yl)-1-piperazinyl)-3-((1-methylethyl)amino)-, (2s)-
rg 7440
gdc0068
2-(4-chlorophenyl)-1-(4-(7-hydroxy-5-methyl-6,7-dihydro-5h-cyclopenta(d)pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one
unii-524y3ib4hq
524y3ib4hq ,
(s)-2-(4-chlorophenyl)-1-(4-((5r,7r)-7-hydroxy-5-methyl-6,7-dihydro-5h-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one
GRZXWCHAXNAUHY-NSISKUIASA-N
(2s)-2-(4-chlorophenyl)-1-[4-[(5r,7r)-7-hydroxy-5-methyl-6,7-dihydro-5h-cyclopenta[e]pyrimidin-4-yl]piperazin-1-yl]-3-(propan-2-ylamino)propan-1-one
gtpl7887
SCHEMBL191659
ipatasertib [who-dd]
ipatasertib [usan]
ipatasertib [inn]
D10641
ipatasertib (usan/inn)
AC-28420
ipatasertib (gdc-0068)
(2s)-2-(4-chlorophenyl)-1-[4-[(5r,7r)-6,7-dihydro-7-hydroxy-5-methyl-5h-cyclopentapyrimidin-4-yl]-1-piperazinyl]-3-[(1-methylethyl)amino]-1-propanone
AKOS025396463
CHEBI:95089
DB11743
mfcd22124514
ipatasertib; gdc-0068
EX-A2077
Q27078088
AS-17027
1-propanone, 2-(4-chlorophenyl)-1-[4-[(5r,7r)-6,7-dihydro-7-hydroxy-5-methyl-5h-cyclopentapyrimidin-4-yl]-1-piperazinyl]-3-[(1-methylethyl)amino]-, (2s)-
CCG-269312
nsc-800986
nsc800986
gdc-0068 di-hcl
nsc832484
gdc0068 di-hcl
rg-7440 di-hcl
nsc-832484
(2s)-2-(4-chlorophenyl)-1-[4-[(5r,7r)-7-hydroxy-5-methyl-6,7-dihydro-5h-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl]-3-(propan-2-ylamino)propan-1-one
nsc-767898
nsc-781451
nsc767898
nsc781451
DTXSID101025595

Excerpt	Reference	Relevance
" In this phase I study, ipatasertib was well tolerated; most adverse events were gastrointestinal and grade 1-2 in severity."	( A First-in-Human Phase I Study of the ATP-Competitive AKT Inhibitor Ipatasertib Demonstrates Robust and Safe Targeting of AKT in Patients with Solid Tumors. Baselga, J; Budha, N; Cervantes, A; Chan, WY; Lin, K; Macarulla, T; Meng, RD; Morales-Barrera, R; Musib, L; Nannini, M; Oliveira, M; Patel, P; Pérez-Fidalgo, JA; Roda, D; Roselló, S; Sanabria Bohórquez, SM; Sanchis-García, JM; Saura, C; Tabernero, J; Yan, Y; Zhu, J, 2017)	0.46
"Among 66 patients who received ≥1 dose of study drug, all experienced an adverse event (AE)."	( A phase Ib open-label dose escalation study of the safety, pharmacokinetics, and pharmacodynamics of cobimetinib (GDC-0973) and ipatasertib (GDC-0068) in patients with locally advanced or metastatic solid tumors. Bendell, JC; Chan, IT; Chang, I; Cho, DC; LoRusso, P; Meng, RD; Musib, L; Patel, P; Sanabria-Bohorquez, S; Shapiro, GI; Wongchenko, M; Yan, Y, 2021)	0.82
" Here we characterise the safety of these agents in subpopulations and assess manageability of key adverse events (AEs)."	( Safety Profile of Ipatasertib Plus Abiraterone vs Placebo Plus Abiraterone in Metastatic Castration-resistant Prostate Cancer. Bracarda, S; Chen, G; Chi, KN; de Bono, J; Garcia, J; Harris, A; Hinton, H; Massard, C; Matsubara, N; Olmos, D; Sandhu, S; Sane, R; Schenkel, F; Sternberg, CN; Sweeney, C, 2023)	0.91
" Grade 3/4 adverse events occurred in 46% (17/37) of patients, with one grade 4 adverse event (anemia, deemed related to rucaparib) and no deaths."	( A Phase Ib, Open-label Study Evaluating the Safety and Efficacy of Ipatasertib plus Rucaparib in Patients with Metastatic Castration-resistant Prostate Cancer. Barve, M; Bracarda, S; Carles, J; de Braud, F; Fang, B; Gallo, JD; Geynisman, DM; Gurney, H; Harris, A; Huang, KC; Joshua, AM; Kerloeguen, Y; Kim, M; Llácer Pérez, C; Maruzzo, M; Maund, SL; Pérez-Gracia, JL; Pook, D; Poon, V; Shin, SJ; Sutaria, DS, 2023)	0.91

Excerpt	Reference	Relevance
" Secondary objectives included analysis of pharmacokinetic parameters, MAPK and PI3K pathway alterations, changes in tissue biomarkers, and preliminary anti-tumor efficacy."	( A phase Ib open-label dose escalation study of the safety, pharmacokinetics, and pharmacodynamics of cobimetinib (GDC-0973) and ipatasertib (GDC-0068) in patients with locally advanced or metastatic solid tumors. Bendell, JC; Chan, IT; Chang, I; Cho, DC; LoRusso, P; Meng, RD; Musib, L; Patel, P; Sanabria-Bohorquez, S; Shapiro, GI; Wongchenko, M; Yan, Y, 2021)	0.82
" No pharmacokinetic interactions were identified."	( A phase Ib open-label dose escalation study of the safety, pharmacokinetics, and pharmacodynamics of cobimetinib (GDC-0973) and ipatasertib (GDC-0068) in patients with locally advanced or metastatic solid tumors. Bendell, JC; Chan, IT; Chang, I; Cho, DC; LoRusso, P; Meng, RD; Musib, L; Patel, P; Sanabria-Bohorquez, S; Shapiro, GI; Wongchenko, M; Yan, Y, 2021)	0.82
" Nonetheless, pharmacodynamic analyses indicated target engagement and suggest rationale for further exploration of cobimetinib or ipatasertib in combination with other anticancer agents."	( A phase Ib open-label dose escalation study of the safety, pharmacokinetics, and pharmacodynamics of cobimetinib (GDC-0973) and ipatasertib (GDC-0068) in patients with locally advanced or metastatic solid tumors. Bendell, JC; Chan, IT; Chang, I; Cho, DC; LoRusso, P; Meng, RD; Musib, L; Patel, P; Sanabria-Bohorquez, S; Shapiro, GI; Wongchenko, M; Yan, Y, 2021)	0.82
" This study was undertaken to characterize pharmacokinetic profiles of ipatasertib and its metabolite M1 (G-037720) and to understand the sources of variability."	( Population Pharmacokinetics of Ipatasertib and Its Metabolite in Cancer Patients. Chanu, P; Kotani, N; Sane, R; Wade, JR; Wang, N; Wilkins, J; Winkler, J; Yoshida, K, 2021)	0.62
" To assess the DDI risk of ipatasertib at the intended clinical dose of 400 mg with CYP3A4 inhibitors, inducers, and substrates, a fit-for-purpose physiologically based pharmacokinetic (PBPK) model of ipatasertib was developed."	( Assessment of cytochrome P450 3A4-mediated drug-drug interactions for ipatasertib using a fit-for-purpose physiologically based pharmacokinetic model. Chen, Y; Cheung, KWK; Jin, JY; Jing, J; Musib, L; Sane, R; Yoshida, K, 2022)	0.72

Excerpt	Reference	Relevance
" We have previously demonstrated the anti-tumor efficacy of these anti-PI3K/AKT-inibitors in combination with anti-microtubule drugs in human BC cell lines, through a complete cytoskeleton disorganization."	( Three dimensional primary cultures for selecting human breast cancers that are sensitive to the anti-tumor activity of ipatasertib or taselisib in combination with anti-microtubule cytotoxic drugs. Caraglia, M; Ciaramella, V; Ciardiello, F; De Vita, F; Della Corte, CM; Diana, A; Famiglietti, V; Franco, R; Franzese, E; Grimaldi, A; Lieto, E; Lombardi, A; Maiello, E; Morgillo, F; Orditura, M; Panarese, I; Procaccini, E; Santoriello, A, 2018)	0.48
" The maximum assessed dose of ipatasertib 600 mg combined with docetaxel or enzalutamide was well tolerated."	( Antitumor activity of ipatasertib combined with chemotherapy: results from a phase Ib study in solid tumors. Argilés, G; Baron, A; Bendell, J; Cervantes, A; Chan, W; Conkling, PR; Gendreau, S; Hussain, M; Isakoff, SJ; Lin, K; Ma, H; Maslyar, D; Molife, LR; Musib, L; Patel, MR; Patel, P; Sampath, D; Soria, JC; Tabernero, J; Vogelzang, NJ; Xu, N, 2020)	0.56
"Ipatasertib in combination with chemotherapy or hormonal therapy was well tolerated with a safety profile consistent with that of ATP-competitive AKT inhibitors."	( Antitumor activity of ipatasertib combined with chemotherapy: results from a phase Ib study in solid tumors. Argilés, G; Baron, A; Bendell, J; Cervantes, A; Chan, W; Conkling, PR; Gendreau, S; Hussain, M; Isakoff, SJ; Lin, K; Ma, H; Maslyar, D; Molife, LR; Musib, L; Patel, MR; Patel, P; Sampath, D; Soria, JC; Tabernero, J; Vogelzang, NJ; Xu, N, 2020)	0.56
"Our results indicate that IPAT combined with carboplatin at low doses was more effective at reducing proliferation, inducing apoptosis and causing cellular stress than IPAT or carboplatin alone."	( Ipatasertib, an oral AKT inhibitor, in combination with carboplatin exhibits anti-proliferative effects in uterine serous carcinoma. Bae-Jump, V; Burkett, WC; Deng, B; Newton, MA; Secord, AA; Sun, W; Zhao, Z; Zhou, C, 2023)	0.91

Excerpt	Reference	Relevance
"GDC-0068 is a highly selective, orally bioavailable Akt kinase inhibitor that shows pharmacodynamic inhibition of Akt signaling and robust antitumor activity in human cancer cells in vitro and in vivo."	( Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Belvin, M; Degtyarev, M; Friedman, LS; Gross, S; Guan, Z; Hong, R; Kassees, R; Koeppen, H; Lee, BB; Lee, LB; Liederer, BM; Lin, J; Lin, K; Nannini, MA; Oeh, J; Punnoose, E; Risom, T; Sampath, D; Savage, H; Skelton, NJ; Wallin, JJ, 2013)	2.12
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51
" Ipatasertib bioavailability and M1 formation increased after multiple dosing, resulting in an increase in exposure beyond that expected from accumulation alone."	( Population Pharmacokinetics of Ipatasertib and Its Metabolite in Cancer Patients. Chanu, P; Kotani, N; Sane, R; Wade, JR; Wang, N; Wilkins, J; Winkler, J; Yoshida, K, 2021)	0.62
" Ipatasertib (IPAT) is an orally bioavailable pan‑AKT inhibitor, which targets all three AKT isoforms and has demonstrated anti‑tumor activity in pre‑clinical models, with clinical trials emerging for many cancer types."	( Ipatasertib exhibits anti‑tumorigenic effects and enhances sensitivity to paclitaxel in endometrial cancer Bae-Jump, VL; Buckingham, L; Deng, B; Fan, Y; Hao, T; John, C; O'Donnell, J; Secord, AA; Shen, X; Sun, W; Suo, H; Zhang, X; Zhao, Z; Zhou, C, 2023)	0.91

Excerpt	Relevance	Reference
" Despite a steeper E-R relationship when accounting for dose modifications, similar dose-response projections were generated."	( Exposure-Response-Based Product Profile-Driven Clinical Utility Index for Ipatasertib Dose Selection in Prostate Cancer. Budha, N; Cho, E; Jin, JY; Liu, Q; Ma, H; Maslyar, D; Musib, L; Poland, B; Wada, R; Yu, W; Zhu, R, 2019)	0.51
"This Phase Ib study explored combination dosing of the allosteric MEK1/2 inhibitor cobimetinib and the ATP-competitive pan-AKT inhibitor ipatasertib."	( A phase Ib open-label dose escalation study of the safety, pharmacokinetics, and pharmacodynamics of cobimetinib (GDC-0973) and ipatasertib (GDC-0068) in patients with locally advanced or metastatic solid tumors. Bendell, JC; Chan, IT; Chang, I; Cho, DC; LoRusso, P; Meng, RD; Musib, L; Patel, P; Sanabria-Bohorquez, S; Shapiro, GI; Wongchenko, M; Yan, Y, 2021)	0.82
" Patients aged 18 years or older with previously untreated asymptomatic or mildly symptomatic mCRPC who had progressive disease and Eastern Collaborative Oncology Group performance status of 0 or 1 were randomly assigned (1:1; permuted block method) to receive ipatasertib (400 mg once daily orally) plus abiraterone (1000 mg once daily orally) and prednisolone (5 mg twice a day orally) or placebo plus abiraterone and prednisolone (with the same dosing schedule)."	( Ipatasertib plus abiraterone and prednisolone in metastatic castration-resistant prostate cancer (IPATential150): a multicentre, randomised, double-blind, phase 3 trial. Alekseev, B; Alves, GV; Atduev, V; Borre, M; Bournakis, E; Bracarda, S; Buchschacher, GL; Chen, G; Chi, KN; Corrales, L; de Bono, JS; Gafanov, R; Gallo, J; Garcia, J; Hanover, J; Harle-Yge, ML; Massard, C; Matsubara, N; Olmos, D; Parnis, F; Puente, J; Sandhu, S; Sternberg, CN; Stroyakovskiy, D; Sweeney, C; Wongchenko, MJ, 2021)	0.62
"The Phase I dose-escalation study enrolled patients with solid tumors in a standard 3 + 3 design with a 1 week washout after the first dose, followed by once-daily dosing on a 3-week-on/1-week-off schedule."	( Single- and multiple-dose pharmacokinetics, potential for CYP3A inhibition, and food effect in patients with cancer and healthy subjects receiving ipatasertib. Budha, N; Cervantes, A; Deng, Y; Huang, J; Liederer, B; Malhi, V; Meng, R; Musib, L; Patel, P; Sane, R; Tabernero, J, 2021)	0.62
"This study demonstrates the value of using a fit-for-purpose PBPK model to assess the clinical DDIs for ipatasertib and to provide dosing strategies for the concurrent use of other CYP3A4 perpetrators or victims."	( Assessment of cytochrome P450 3A4-mediated drug-drug interactions for ipatasertib using a fit-for-purpose physiologically based pharmacokinetic model. Chen, Y; Cheung, KWK; Jin, JY; Jing, J; Musib, L; Sane, R; Yoshida, K, 2022)	0.72
" The results from this study suggest that dosing ipatasertib after an evening meal followed by overnight fasting can be an effective strategy for managing increased glucose levels."	( Mitigating ipatasertib-induced glucose increase through dose and meal timing modifications. Agarwal, P; Gallo, JD; Hinton, H; Huang, KC; Miles, DR; Rasuo, G; Rotmensch, J; Sane, RS; Sutaria, DS, 2022)	0.72
"Continuous dosing of ipatasertib with chemotherapy was safe and well-tolerated."	( Phase I Trial of Ipatasertib Plus Carboplatin, Carboplatin/Paclitaxel, or Capecitabine and Atezolizumab in Metastatic Triple-Negative Breast Cancer. Bozoghlanian, M; Cui, Y; Frankel, PH; Martinez, N; Murga, M; Patel, N; Ruel, C; Schmolze, D; Stewart, D; Tang, A; Tumyan, L; Vora, L; Waisman, J; Yost, SE; Yuan, Y, 2023)	0.91

Class	Description
N-arylpiperazine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Fumarate hydratase	Homo sapiens (human)	Potency	33.1734	0.0030	8.7949	48.0869	AID1347053
EWS/FLI fusion protein	Homo sapiens (human)	Potency	5.1885	0.0013	10.1577	42.8575	AID1259252; AID1259253; AID1259255; AID1259256
polyprotein	Zika virus	Potency	33.1734	0.0030	8.7949	48.0869	AID1347053
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Cytochrome P450 2D6	Homo sapiens (human)	IC50 (µMol)	0.1570	0.0000	2.0151	10.0000	AID708170
RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)	IC50 (µMol)	0.0418	0.0002	0.7387	10.0000	AID1770729; AID1912109; AID708154; AID708170
RAC-beta serine/threonine-protein kinase	Homo sapiens (human)	IC50 (µMol)	0.0255	0.0005	0.5013	7.6000	AID1690018; AID1770730; AID1912110; AID708169
cGMP-dependent protein kinase 1	Homo sapiens (human)	IC50 (µMol)	0.0835	0.0011	0.0267	0.0980	AID708127; AID708128
RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)	IC50 (µMol)	0.0187	0.0006	0.4743	4.0000	AID1690019; AID1912111; AID708171
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)	Kd	0.0006	0.0006	1.0621	4.4000	AID1831406
RAC-beta serine/threonine-protein kinase	Homo sapiens (human)	Kd	0.0350	0.0021	1.6196	8.7000	AID1831407
RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)	Kd	0.0025	0.0025	1.7646	6.2000	AID1831408
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
xenobiotic metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
coumarin metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
isoquinoline alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of cellular organofluorine metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
arachidonic acid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
protein phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
activation-induced cell death of T cells	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
intracellular signal transduction	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
osteoblast differentiation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
maternal placenta development	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of protein phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of endothelial cell proliferation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cell migration involved in sprouting angiogenesis	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
glycogen biosynthetic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of glycogen biosynthetic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
glucose metabolic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of translation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of protein kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein import into nucleus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
nitric oxide biosynthetic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
inflammatory response	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to oxidative stress	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
signal transduction	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
epidermal growth factor receptor signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
G protein-coupled receptor signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
canonical NF-kappaB signal transduction	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cell population proliferation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
insulin receptor signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
apoptotic mitochondrial changes	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to heat	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
gene expression	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of autophagy	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of endothelial cell migration	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of gene expression	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of gene expression	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of long-chain fatty acid import across plasma membrane	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
fibroblast migration	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of fibroblast migration	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of sodium ion transport	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of glucose metabolic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of endopeptidase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of neuron projection development	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of macroautophagy	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein ubiquitination	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
peptidyl-serine phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
peptidyl-threonine phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
virus-mediated perturbation of host defense response	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cytokine-mediated signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
mammalian oogenesis stage	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cell differentiation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of cell growth	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of cell migration	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of cell migration	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
T cell costimulation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of protein ubiquitination	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of myelination	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
lipopolysaccharide-mediated signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
TOR signaling	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of fatty acid beta-oxidation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of endodeoxyribonuclease activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of protein binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to food	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
peripheral nervous system myelin maintenance	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to insulin stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to fluid shear stress	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to reactive oxygen species	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
interleukin-18-mediated signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to decreased oxygen levels	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
non-canonical NF-kappaB signal transduction	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
glucose homeostasis	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of apoptotic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of apoptotic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
anoikis	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of mRNA stability	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of nitric oxide biosynthetic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of fat cell differentiation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of glycogen biosynthetic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of Notch signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of proteolysis	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of DNA-templated transcription	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of glucose import	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of organ growth	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein autophosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of lipid biosynthetic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
insulin-like growth factor receptor signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
behavioral response to pain	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of smooth muscle cell proliferation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of nitric-oxide synthase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of DNA-binding transcription factor activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
striated muscle cell differentiation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of protein metabolic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
excitatory postsynaptic potential	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to growth hormone	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
mammary gland epithelial cell differentiation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
labyrinthine layer blood vessel development	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to UV-A	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to growth factor	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to cadmium ion	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to tumor necrosis factor	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to epidermal growth factor stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to prostaglandin E stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of protein serine/threonine kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
establishment of protein localization to mitochondrion	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
maintenance of protein location in mitochondrion	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of release of cytochrome c from mitochondria	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to granulocyte macrophage colony-stimulating factor stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
execution phase of apoptosis	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of postsynapse organization	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of tRNA methylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to oxidised low-density lipoprotein particle stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of protein localization to lysosome	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of cGAS/STING signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycle	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of protein localization to nucleus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to peptide	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of signal transduction by p53 class mediator	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of cilium assembly	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of oxidative stress-induced intrinsic apoptotic signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of leukocyte cell-cell adhesion	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of protein localization to plasma membrane	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of I-kappaB phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of TORC1 signaling	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of protein localization to endoplasmic reticulum	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to nerve growth factor stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to insulin-like growth factor stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of protein localization to cell surface	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of type B pancreatic cell development	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of lymphocyte migration	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligand	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
intracellular signal transduction	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
glycogen biosynthetic process	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
glucose metabolic process	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
regulation of translation	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
signal transduction	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
insulin receptor signaling pathway	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of long-chain fatty acid import across plasma membrane	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of glucose metabolic process	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
regulation of cell migration	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of cell migration	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of fatty acid beta-oxidation	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
peripheral nervous system myelin maintenance	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
cellular response to insulin stimulus	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
protein modification process	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
fat cell differentiation	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of glycogen biosynthetic process	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of glucose import	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
regulation of cell cycle	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
mammary gland epithelial cell differentiation	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
cellular response to high light intensity	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
organic substance transport	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
protein localization to plasma membrane	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of protein targeting to membrane	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
retinal rod cell apoptotic process	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of cell motility	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
intracellular signal transduction	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
peptidyl-serine phosphorylation	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
protein phosphorylation	cGMP-dependent protein kinase 1	Homo sapiens (human)
neuron migration	cGMP-dependent protein kinase 1	Homo sapiens (human)
signal transduction	cGMP-dependent protein kinase 1	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	cGMP-dependent protein kinase 1	Homo sapiens (human)
spermatid development	cGMP-dependent protein kinase 1	Homo sapiens (human)
negative regulation of inositol phosphate biosynthetic process	cGMP-dependent protein kinase 1	Homo sapiens (human)
negative regulation of glutamate secretion	cGMP-dependent protein kinase 1	Homo sapiens (human)
dendrite development	cGMP-dependent protein kinase 1	Homo sapiens (human)
cGMP-mediated signaling	cGMP-dependent protein kinase 1	Homo sapiens (human)
cerebellum development	cGMP-dependent protein kinase 1	Homo sapiens (human)
actin cytoskeleton organization	cGMP-dependent protein kinase 1	Homo sapiens (human)
forebrain development	cGMP-dependent protein kinase 1	Homo sapiens (human)
positive regulation of circadian rhythm	cGMP-dependent protein kinase 1	Homo sapiens (human)
regulation of GTPase activity	cGMP-dependent protein kinase 1	Homo sapiens (human)
collateral sprouting	cGMP-dependent protein kinase 1	Homo sapiens (human)
relaxation of vascular associated smooth muscle	cGMP-dependent protein kinase 1	Homo sapiens (human)
cell growth involved in cardiac muscle cell development	cGMP-dependent protein kinase 1	Homo sapiens (human)
negative regulation of platelet aggregation	cGMP-dependent protein kinase 1	Homo sapiens (human)
negative regulation of vascular associated smooth muscle cell proliferation	cGMP-dependent protein kinase 1	Homo sapiens (human)
negative regulation of vascular associated smooth muscle cell migration	cGMP-dependent protein kinase 1	Homo sapiens (human)
regulation of testosterone biosynthetic process	cGMP-dependent protein kinase 1	Homo sapiens (human)
protein kinase A signaling	cGMP-dependent protein kinase 1	Homo sapiens (human)
mitochondrial genome maintenance	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of endothelial cell proliferation	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
protein phosphorylation	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
signal transduction	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of TOR signaling	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of angiogenesis	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of cell size	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
brain morphogenesis	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
homeostasis of number of cells within a tissue	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesis	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of vascular endothelial cell proliferation	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of artery morphogenesis	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of cellular senescence	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
intracellular signal transduction	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
peptidyl-serine phosphorylation	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
monooxygenase activity	Cytochrome P450 2D6	Homo sapiens (human)
iron ion binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2D6	Homo sapiens (human)
heme binding	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
protein kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein serine/threonine kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein serine/threonine/tyrosine kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
calmodulin binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
ATP binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
phosphatidylinositol-3,4,5-trisphosphate binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
enzyme binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein kinase binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
nitric-oxide synthase regulator activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein serine/threonine kinase inhibitor activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
identical protein binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein homodimerization activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
phosphatidylinositol-3,4-bisphosphate binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
14-3-3 protein binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
potassium channel activator activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein serine kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein serine/threonine kinase activity	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
protein binding	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
ATP binding	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
metal ion binding	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
protein serine kinase activity	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
molecular function activator activity	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
protein kinase activity	cGMP-dependent protein kinase 1	Homo sapiens (human)
cGMP-dependent protein kinase activity	cGMP-dependent protein kinase 1	Homo sapiens (human)
calcium channel regulator activity	cGMP-dependent protein kinase 1	Homo sapiens (human)
protein binding	cGMP-dependent protein kinase 1	Homo sapiens (human)
ATP binding	cGMP-dependent protein kinase 1	Homo sapiens (human)
cGMP binding	cGMP-dependent protein kinase 1	Homo sapiens (human)
identical protein binding	cGMP-dependent protein kinase 1	Homo sapiens (human)
mitogen-activated protein kinase p38 binding	cGMP-dependent protein kinase 1	Homo sapiens (human)
protein serine kinase activity	cGMP-dependent protein kinase 1	Homo sapiens (human)
protein kinase activity	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
protein serine/threonine kinase activity	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
protein binding	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
ATP binding	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
protein serine kinase activity	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
mitochondrion	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2D6	Homo sapiens (human)
cytoplasm	Cytochrome P450 2D6	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2D6	Homo sapiens (human)
cytoplasm	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
mitochondrial intermembrane space	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
membrane	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
nucleus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
nucleoplasm	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cytoplasm	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
spindle	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cytosol	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
plasma membrane	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cell-cell junction	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cell cortex	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
microtubule cytoskeleton	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
lamellipodium	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
vesicle	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
ciliary basal body	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
postsynapse	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
glutamatergic synapse	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein-containing complex	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
nucleus	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
nucleoplasm	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
early endosome	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
cytosol	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
plasma membrane	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
cell cortex	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
ruffle membrane	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
intracellular membrane-bounded organelle	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
acrosomal vesicle	cGMP-dependent protein kinase 1	Homo sapiens (human)
nucleoplasm	cGMP-dependent protein kinase 1	Homo sapiens (human)
cytoplasm	cGMP-dependent protein kinase 1	Homo sapiens (human)
Golgi apparatus	cGMP-dependent protein kinase 1	Homo sapiens (human)
cytosol	cGMP-dependent protein kinase 1	Homo sapiens (human)
plasma membrane	cGMP-dependent protein kinase 1	Homo sapiens (human)
sarcolemma	cGMP-dependent protein kinase 1	Homo sapiens (human)
nucleus	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
cytoplasm	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
membrane	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
nucleoplasm	RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (127)

Assay ID	Title	Year	Journal	Article
AID708169	Competitive inhibition of wild-type full-length amino-terminal polyhistidine-tagged human Akt2 expressed in recombinant baculovirus system using fluorescence labeled substrate after 60 mins by fluorescence polarization assay in presence of ATP	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708127	Inhibition of PRKG1beta	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1690019	Inhibition of full length human Akt3 S472D mutant using GRPRTSSFAEGKK as substrate incubated for 40 mins by scintillation counting method	2020	European journal of medicinal chemistry, Mar-01, Volume: 189	Discovery of novel akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells.
AID1831444	Antiproliferative activity against human BT-474 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis	2021	Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24	Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders.
AID1831406	Binding affinity to wild-type human partial length AKT1 expressed in bacterial expression system assessed as residual binding level by Kinomescan method	2021	Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24	Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders.
AID708135	Antitumor activity against human PC3 xenografted in nu/nu mouse assessed as inhibition of tumor growth at 100 mg/kg, po qd after 11 days	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708140	Inhibition of Akt in nu/nu mouse xenografted with human PC3 cells assessed as decrease in tumor p-PRAS40 level at 100 mg/kg, po at 8 hrs by ELISA relative to total PRAS40	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1690020	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay	2020	European journal of medicinal chemistry, Mar-01, Volume: 189	Discovery of novel akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells.
AID708128	Inhibition of PRKG1alpha	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708166	Inhibition of PRKG1beta at 1 uM	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1690023	Cytotoxicity against human SMMC-7721 cells assessed as reduction in cell viability by MTT assay	2020	European journal of medicinal chemistry, Mar-01, Volume: 189	Discovery of novel akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells.
AID708157	Cytotoxicity against human PC3 cells assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708155	Cytotoxicity against human BT474M1 cells assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708149	Inhibition of Akt1-mediated PRAS40 phosphorylation in human PC3 cells	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708171	Competitive inhibition of wild-type full-length amino-terminal polyhistidine-tagged human Akt3 expressed in recombinant baculovirus system using fluorescence labeled Crosstide as substrate after 60 mins by fluorescence polarization assay in presence of AT	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708151	Induction of necrosis in human MCF7 cells overexpressing Her2	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708156	Cytotoxicity against human MCF7 cells overexpressing Her2 assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708138	Toxicity in nu/nu mouse xenografted with human PC3 cells assessed as loss in body weight at 1 to 100 mg/kg, po qd relative to vehicle-treated control	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1912205	Upregulation of Akt phosphorylation in human LNCap cells at 0.25 to 2.5 uM measured after 1 to 4 hrs by Western blot analysis	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
AID1831408	Binding affinity to wild-type human partial length AKT3 expressed in bacterial expression system assessed as residual binding level by Kinomescan method	2021	Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24	Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders.
AID1912134	Antiproliferative activity against human PC-3 habouring PTEN deletion and PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
AID708130	Induction of cell cycle arrest in human BT474M1 cells assessed as accumulation at G1 phase	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708153	Induction of apoptosis in human MCF7 cells overexpressing Her2	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708139	Inhibition of Akt in nu/nu mouse xenografted with human PC3 cells assessed as decrease in tumor p-S6RP level at 100 mg/kg, po at 8 hrs by ELISA relative to total S6RP	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708146	Plasma concentration in nu/nu mouse xenografted with human PC3 cells at 12.5 mg/kg, po within 1 hr by LC/MS/MS analysis	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1770730	Inhibition of N-terminal GST-tagged human AKT2 (120 to 481 residues) expressed in baculovirus infected Sf21 cells incubated for 1 hr in presence of ATP by mobility shift assay	2021	Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16	Discovery of
AID708158	Cytotoxicity against human LNCAP cells assessed as reduction of resazurin to resorufin after 72 hrs	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708152	Induction of apoptosis in human BT474M1 cells	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708167	Inhibition of PRKG1alpha at 1 uM	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1831379	Protac activity at VHL/AKT in human BT-474 cells assessed as reduction in PRAS40 phosphorylation at 1 uM after 24 hrs by Western blot analysis	2021	Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24	Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders.
AID1912111	Inhibition of recombinant N-terminal GST tagged AKT2 (108 to 479 end residues) (unknown origin) catalytic domain expressed in Sf21 cells using peptide substrate incubated for 1 hr in presence of ATP by caliper off-chip mobility shift assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
AID708133	Competitive inhibition of PKA expressed in Escherichia coli assessed as fluorescence labeled peptide substrate phosphorylation after 60 mins in presence of ATP	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1912110	Inhibition of recombinant AKT2 (120 to 481 end residues) (unknown origin) catalytic domain expressed in Sf21 cells using peptide substrate incubated for 1 hr in presence of ATP by caliper off-chip mobility shift assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
AID708132	Induction of necrosis in human BT474M1 cells	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1912135	Antiproliferative activity against human CAL-51 habouring PTEN deletion and PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
AID1690022	Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability by MTT assay	2020	European journal of medicinal chemistry, Mar-01, Volume: 189	Discovery of novel akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells.
AID1831445	Antiproliferative activity against human PC-3 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis	2021	Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24	Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders.
AID708129	Antitumor activity against human PC3 xenografted in po dosed nu/nu mouse assessed as inhibition of tumor growth administered once daily measured after 11 days	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708147	Inhibition of Akt1-mediated PRAS40 phosphorylation in human BT474M1 cells	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708165	Inhibition of p70S6K at 1 uM	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1912139	Antiproliferative activity against human RL95-2 habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
AID708136	Antitumor activity against human PC3 xenografted in nu/nu mouse assessed as inhibition of tumor growth at 25 mg/kg, po qd after 11 days	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1912104	Antiproliferative activity against human COLO-704 habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
AID1690021	Cytotoxicity against human Hep3B cells assessed as reduction in cell viability by MTT assay	2020	European journal of medicinal chemistry, Mar-01, Volume: 189	Discovery of novel akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells.
AID708144	Plasma concentration in nu/nu mouse xenografted with human PC3 cells at 50 mg/kg, po at 1 hr by LC/MS/MS analysis	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708148	Inhibition of Akt1-mediated PRAS40 phosphorylation in human MCF7 cells overexpressing Her2	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1690048	Induction of autophagy flux arrest in human Huh-7 cells assessed as reduction in LC3 by immunofluorescence staining based assay	2020	European journal of medicinal chemistry, Mar-01, Volume: 189	Discovery of novel akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells.
AID708159	Solubility of the compound at pH 1.2 to 7.4	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708150	Inhibition of Akt1-mediated PRAS40 phosphorylation in human LNCAP cells	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1912137	Antiproliferative activity against human TOV-21G habouring PTEN deletion and PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
AID708134	Antitumor activity against human PC3 xenografted in nu/nu mouse assessed as inhibition of tumor growth at 50 mg/kg, po bid after 11 days	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1857187	Antiproliferative activity against human osimertinib resistant NCI-H1975 cells assessed as reduction in cell viability measured after 24 hrs by CCK-8 assay
AID708154	Competitive inhibition of wild-type full-length amino-terminal polyhistidine-tagged human Akt1 expressed in recombinant baculovirus system using fluorescence labeled substrate after 60 mins by fluorescence polarization assay in presence of ATP	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1912109	Inhibition of recombinant AKT1 (104 to 480 end residues) (unknown origin) catalytic domain expressed in Sf21 cells using peptide substrate incubated for 1 hr in presence of ATP by caliper off-chip mobility shift assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
AID1690018	Inhibition of full length human Akt2 S474D mutant using GRPRTSSFAEGKK as substrate incubated for 40 mins by scintillation counting method	2020	European journal of medicinal chemistry, Mar-01, Volume: 189	Discovery of novel akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells.
AID1912138	Antiproliferative activity against human C-33-A habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
AID1770729	Inhibition of N-terminal GST-tagged human AKT1 (104 to 408 residues) expressed in baculovirus infected Sf21 cells incubated for 1 hr in presence of ATP by mobility shift assay	2021	Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16	Discovery of
AID1690017	Inhibition of full length human Akt1 S478G mutant using GRPRTSSFAEGKK as substrate incubated for 40 mins by scintillation counting method	2020	European journal of medicinal chemistry, Mar-01, Volume: 189	Discovery of novel akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells.
AID1831378	Protac activity at VHL/AKT in human BT-474 cells assessed as reduction in total AKT level at 1 uM after 24 hrs by Western blot analysis	2021	Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24	Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders.
AID1912108	Antiproliferative activity against human ZR-75-1 habouring PTEN deletion mutant assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
AID1912136	Antiproliferative activity against human T47D habouring PIK3CA mutation/amplication assessed as reduction in cell viability incubated for 72 hrs by Cell Titer Glo luminescent assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
AID708131	Induction of cell cycle arrest in human MCF7 cells overexpressing Her2 assessed as accumulation at G1 phase	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1831446	Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis	2021	Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24	Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders.
AID708126	Inhibition of p70S6K	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708143	Plasma concentration in nu/nu mouse xenografted with human PC3 cells at 50 mg/kg, po at 9 hrs by LC/MS/MS analysis	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1831407	Binding affinity to wild-type human partial length AKT2 expressed in bacterial expression system assessed as residual binding level by Kinomescan method	2021	Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24	Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders.
AID708141	Plasma concentration in nu/nu mouse xenografted with human PC3 cells at 100 mg/kg, po at 8 hrs by LC/MS/MS analysis	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708142	Inhibition of Akt in nu/nu mouse xenografted with human PC3 cells assessed as decrease in tumor p-PRAS40 level at 100 mg/kg, po within 3 hrs by ELISA relative to total PRAS40	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708145	Plasma concentration in nu/nu mouse xenografted with human PC3 cells at 50 mg/kg, po within 1 hr by LC/MS/MS analysis	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1831380	Protac activity at VHL/AKT in human BT-474 cells assessed as reduction in S6 phosphorylation at 1 uM after 24 hrs by Western blot analysis	2021	Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24	Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders.
AID708170	Inhibition of Akt1 in human LNCAP cells assessed as phosphorylation of PRAS40 at Thr246 after 1.5 hrs	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID708137	Toxicity in nu/nu mouse xenografted with human PC3 cells assessed as loss in body weight at 150 mg/kg, po qd after 8 days relative to vehicle-treated control	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1690049	Induction of autophagy flux arrest in human Huh-7 cells assessed as reduction in LAMP1 by immunofluorescence staining based assay	2020	European journal of medicinal chemistry, Mar-01, Volume: 189	Discovery of novel akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347126	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347122	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1347123	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347121	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347127	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1345374	Human AKT serine/threonine kinase 1 (Akt (Protein kinase B))	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1345349	Human AKT serine/threonine kinase 2 (Akt (Protein kinase B))	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1345391	Human Protein kinase G (PKG) 1 (Protein kinase G (PKG))	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1345907	Human AKT serine/threonine kinase 3 (Akt (Protein kinase B))	2012	Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	23 (37.10)	24.3611
2020's	39 (62.90)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	17 (27.42%)	5.53%
Reviews	3 (4.84%)	6.00%
Case Studies	1 (1.61%)	4.05%
Observational	0 (0.00%)	0.25%
Other	41 (66.13%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
fluorouracil Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.	4.51	1	1	nucleobase analogue; organofluorine compound	antimetabolite; antineoplastic agent; environmental contaminant; immunosuppressive agent; radiosensitizing agent; xenobiotic
pd 98059 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one: inhibits MAP kinase kinase (MEK) activity, p42 MAPK and p44 MAPK; structure in first source. 2-(2-amino-3-methoxyphenyl)chromen-4-one : A member of the class of monomethoxyflavones that is 3'-methoxyflavone bearing an additional amino substituent at position 2'.	2.21	1	0	aromatic amine; monomethoxyflavone	EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector
prednisolone Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone.	7.23	4	4	11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone	adrenergic agent; anti-inflammatory drug; antineoplastic agent; drug metabolite; environmental contaminant; immunosuppressive agent; xenobiotic
prednisone Prednisone: A synthetic anti-inflammatory glucocorticoid derived from CORTISONE. It is biologically inert and converted to PREDNISOLONE in the liver.. prednisone : A synthetic glucocorticoid drug that is particularly effective as an immunosuppressant, and affects virtually all of the immune system. Prednisone is a prodrug that is converted by the liver into prednisolone (a beta-hydroxy group instead of the oxo group at position 11), which is the active drug and also a steroid.	4.84	2	2	11-oxo steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone	adrenergic agent; anti-inflammatory drug; antineoplastic agent; immunosuppressive agent; prodrug
quinoxalines quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.	3.82	2	0	mancude organic heterobicyclic parent; naphthyridine; ortho-fused heteroarene
pyrroles 1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.	3.35	1	0	pyrrole; secondary amine
thiophenes Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.	3.78	2	0	mancude organic heteromonocyclic parent; monocyclic heteroarene; thiophenes; volatile organic compound	non-polar solvent
pyrazolanthrone pyrazolanthrone: JNK (c-Jun N-terminal kinase) inhibitor; structure in first source. anthra[1,9-cd]pyrazol-6(2H)-one : A member of the class of anthrapyrazoles that is anthra[1,9-cd]pyrazole substituted at position 6 by an oxo group. An inhibitor of c-Jun N-terminal kinase.	2.21	1	0	anthrapyrazole; aromatic ketone; cyclic ketone	antineoplastic agent; c-Jun N-terminal kinase inhibitor; geroprotector
indazoles Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.	2.54	2	0	indazole
thiazoles [no description available]	2.31	1	0	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
imperatorin imperatorin: tumor necrosis factor antagonist; furanocoumarin from West African medicinal plant Clausena anisata; structure in Negwer, 5th ed, #3005. imperatorin : A member of the class of psoralens that is psoralen substituted by a prenyloxy group at position 8. Isolated from Angelica dahurica and Angelica koreana, it acts as a acetylcholinesterase inhibitor.	2.25	1	0	psoralens	EC 3.1.1.7 (acetylcholinesterase) inhibitor; metabolite
tetradecanoylphorbol acetate Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.. phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.	2.21	1	0	acetate ester; diester; phorbol ester; tertiary alpha-hydroxy ketone; tetradecanoate ester	antineoplastic agent; apoptosis inducer; carcinogenic agent; mitogen; plant metabolite; protein kinase C agonist; reactive oxygen species generator
paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).	8.08	7	6	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
capecitabine Capecitabine: A deoxycytidine derivative and fluorouracil PRODRUG that is used as an ANTINEOPLASTIC ANTIMETABOLITE in the treatment of COLON CANCER; BREAST CANCER and GASTRIC CANCER.. capecitabine : A carbamate ester that is cytidine in which the hydrogen at position 5 is replaced by fluorine and in which the amino group attached to position 4 is converted into its N-(penyloxy)carbonyl derivative. Capecitabine is a antineoplastic agent used in the treatment of cancers.	3.99	1	1	carbamate ester; cytidines; organofluorine compound	antimetabolite; antineoplastic agent; prodrug
fulvestrant Fulvestrant: An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.. fulvestrant : A 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer.	2.31	1	0	17beta-hydroxy steroid; 3-hydroxy steroid; organofluorine compound; sulfoxide	antineoplastic agent; estrogen antagonist; estrogen receptor antagonist
abiraterone [no description available]	7.57	5	5	3beta-hydroxy-Delta(5)-steroid; 3beta-sterol; pyridines	antineoplastic agent; EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor
pomalidomide 3-aminophthalimidoglutarimide: structure in first source	2.31	1	0	aromatic amine; dicarboximide; isoindoles; piperidones	angiogenesis inhibitor; antineoplastic agent; immunomodulator
sb 203580 [no description available]	2.21	1	0	imidazoles; monofluorobenzenes; pyridines; sulfoxide	EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector; Hsp90 inhibitor; neuroprotective agent
carboplatin [no description available]	4.4	2	1
u 0126 U 0126: protein kinase kinase inhibitor; structure in first source	2.21	1	0	aryl sulfide; dinitrile; enamine; substituted aniline	antineoplastic agent; antioxidant; apoptosis inducer; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; osteogenesis regulator; vasoconstrictor agent
dasatinib N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).	2.31	1	0	1,3-thiazoles; aminopyrimidine; monocarboxylic acid amide; N-(2-hydroxyethyl)piperazine; N-arylpiperazine; organochlorine compound; secondary amino compound; tertiary amino compound	anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor
su 11248 [no description available]	2.31	1	0	monocarboxylic acid amide; pyrroles	angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist
palbociclib [no description available]	2.31	1	0	aminopyridine; aromatic ketone; cyclopentanes; piperidines; pyridopyrimidine; secondary amino compound; tertiary amino compound	antineoplastic agent; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
everolimus [no description available]	2.31	1	0	cyclic acetal; cyclic ketone; ether; macrolide lactam; primary alcohol; secondary alcohol	anticoronaviral agent; antineoplastic agent; geroprotector; immunosuppressive agent; mTOR inhibitor
axitinib [no description available]	2.21	1	0	aryl sulfide; benzamides; indazoles; pyridines	antineoplastic agent; tyrosine kinase inhibitor; vascular endothelial growth factor receptor antagonist
abiraterone acetate Abiraterone Acetate: An androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic castration-resistant PROSTATE CANCER.. abiraterone acetate : A sterol ester obtained by formal condensation of the 3-hydroxy group of abiraterone with the carboxy group of acetic acid. A prodrug that is converted in vivo into abiraterone. Used for treatment of metastatic castrate-resistant prostate cancer.	3.99	1	1	pyridines; sterol ester	antineoplastic agent; EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor; prodrug
rucaparib AG14447: Poly(ADP-ribose) polymerase inhibitor; structure in first source	3.99	1	1	azepinoindole; caprolactams; organofluorine compound; secondary amino compound	antineoplastic agent; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor
nu 7441 8-dibenzothiophen-4-yl-2-morpholin-4-yl-chromen-4-one: structure in first source	2.15	1	0	dibenzothiophenes
trametinib [no description available]	2.25	1	0	acetamides; aromatic amine; cyclopropanes; organofluorine compound; organoiodine compound; pyridopyrimidine; ring assembly	anticoronaviral agent; antineoplastic agent; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector
mdv 3100 [no description available]	2.25	1	0	(trifluoromethyl)benzenes; benzamides; imidazolidinone; monofluorobenzenes; nitrile; thiocarbonyl compound	androgen antagonist; antineoplastic agent
gdc-0973 cobimetinib: has antineoplastic activity; structure in first source. cobimetinib : A member of the class of N-acylazetidines obtained by selective formal condensation of the carboxy group of 3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzoic acid with the secondary amino group from the azetidine ring of 3-[(2S)-piperidin-2-yl]azetidin-3-ol. An inhibitor of mitogen-activated protein kinase that is used (as its fumarate salt) in combination with vemurafenib for the treatment of patients with unresectable or metastatic melanoma.	9.62	1	1	aromatic amine; difluorobenzene; N-acylazetidine; organoiodine compound; piperidines; secondary amino compound; tertiary alcohol	antineoplastic agent; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
mk 2206 MK 2206: a protein kinase inhibitor and antineoplastic agent	4.01	3	0	organic heterotricyclic compound	EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
piperidines Piperidines: A family of hexahydropyridines.	4.62	1	1
pht 427 4-dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide: an antineoplastic agent; structure in first source	3.35	1	0
afuresertib [no description available]	3.35	1	0	amphetamines
xmd 8-92 XMD8-92 : A dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one carrying at C-2 on the pyrimidine ring a [2-ethoxy-4-(4-hydroxypiperidin-1-yl)phenyl]amino substituent. It is an inhibitor of the BMK1 kinase pathway.	2.25	1	0	pyrimidobenzodiazepine	protein kinase inhibitor
abt-199 venetoclax: A BCL-2 inhibitor with antineoplastic activity that is used in the treatment of CHRONIC LYMPHOCYTIC LEUKEMIA associated with chromosome 17p deletion; structure in first source.. venetoclax : A member of the class of pyrrolopyridines that is a potent inhibitor of the antiapoptotic protein B-cell lymphoma 2. It is used for treamtment of chronic lymphocytic leukemia with 17p deletion.	2.31	1	0	aromatic ether; C-nitro compound; monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; N-sulfonylcarboxamide; oxanes; pyrrolopyridine	antineoplastic agent; apoptosis inducer; B-cell lymphoma 2 inhibitor
gsk2141795 GSK2141795: an Akt inhibitor with antineoplastic activity; structure in first source	3.35	1	0
byl719 [no description available]	2.31	1	0	proline derivative
epidermal growth factor Epidermal Growth Factor: A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form.	2.1	1	0
erdafitinib erdafitinib: inhibitor of fibroblast growth factor receptors	7.41	1	0
akt-i-1,2 compound Akt-I-1,2 compound: an aminopeptidase P inhibitor; structure in first source	3.35	1	0
levoleucovorin Levoleucovorin: A folate analog consisting of the pharmacologically active isomer of LEUCOVORIN.. (6S)-5-formyltetrahydrofolic acid : The pharmacologically active (6S)-stereoisomer of 5-formyltetrahydrofolic acid.	4.51	1	1	5-formyltetrahydrofolic acid	antineoplastic agent; metabolite
pyrimidinones Pyrimidinones: Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O.	2.25	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Hepatocellular Carcinoma [description not available]	0	2.25	1	0
Cancer of Liver [description not available]	0	4.94	2	1
Carcinoma, Hepatocellular A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.	0	2.25	1	0
Liver Neoplasms Tumors or cancer of the LIVER.	0	4.94	2	1
Congenital Zika Syndrome [description not available]	0	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.54	2	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	0	2.25	1	0
Exanthem [description not available]	0	4.21	2	1
Benign Neoplasms [description not available]	0	9.7	11	8
Exanthema Diseases in which skin eruptions or rashes are a prominent manifestation. Classically, six such diseases were described with similar rashes; they were numbered in the order in which they were reported. Only the fourth (Duke's disease), fifth (ERYTHEMA INFECTIOSUM), and sixth (EXANTHEMA SUBITUM) numeric designations survive as occasional synonyms in current terminology.	0	4.21	2	1
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	1	13.67	22	16
Breast Cancer [description not available]	0	11.51	7	2
Local Neoplasm Recurrence [description not available]	0	4.72	1	1
Breast Neoplasms Tumors or cancer of the human BREAST.	1	11.31	21	6
ER-Negative PR-Negative HER2-Negative Breast Cancer [description not available]	0	6.98	6	4
Triple Negative Breast Neoplasms Breast neoplasms that do not express ESTROGEN RECEPTORS; PROGESTERONE RECEPTORS; and do not overexpress the NEU RECEPTOR/HER-2 PROTO-ONCOGENE PROTEIN.	1	8.98	6	4
Bladder Cancer [description not available]	0	7.41	1	0
Urinary Bladder Neoplasms Tumors or cancer of the URINARY BLADDER.	0	2.41	1	0
Androgen-Independent Prostatic Cancer [description not available]	0	9.1	9	8
Prostatic Neoplasms, Castration-Resistant Tumors or cancer of the PROSTATE which can grow in the presence of low or residual amount of androgen hormones such as TESTOSTERONE.	1	11.1	9	8
Hyperglycemia, Postprandial Abnormally high BLOOD GLUCOSE level after a meal.	0	4.4	2	1
Hyperglycemia Abnormally high BLOOD GLUCOSE level.	0	4.4	2	1
Carcinoma, Anaplastic [description not available]	0	5.27	3	1
Cancer of the Uterus [description not available]	0	2.6	1	0
Carcinoma A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for cancer.	0	5.27	3	1
Uterine Neoplasms Tumors or cancer of the UTERUS.	0	2.6	1	0
Cancer of Prostate [description not available]	0	3.9	3	0
Prostatic Neoplasms Tumors or cancer of the PROSTATE.	1	5.9	3	0
Cancer of Endometrium [description not available]	0	2.6	1	0
Endometrial Neoplasms Tumors or cancer of ENDOMETRIUM, the mucous lining of the UTERUS. These neoplasms can be benign or malignant. Their classification and grading are based on the various cell types and the percent of undifferentiated cells.	1	4.6	1	0
Benign Neoplasms, Brain [description not available]	0	2.61	2	0
Brain Neoplasms Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.	0	2.61	2	0
Cancer of Colon [description not available]	0	2.21	1	0
Colonic Neoplasms Tumors or cancer of the COLON.	0	2.21	1	0
Age-Related Osteoporosis [description not available]	0	2.25	1	0
Osteoporosis Reduction of bone mass without alteration in the composition of bone, leading to fractures. Primary osteoporosis can be of two major types: postmenopausal osteoporosis (OSTEOPOROSIS, POSTMENOPAUSAL) and age-related or senile osteoporosis.	0	2.25	1	0
Carcinoma, Non-Small Cell Lung [description not available]	0	2.31	1	0
Cancer of Lung [description not available]	0	4.96	2	1
Carcinoma, Non-Small-Cell Lung A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.	1	4.31	1	0
Lung Neoplasms Tumors or cancer of the LUNG.	0	4.96	2	1
Metastase [description not available]	0	4.6	2	2
Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.	0	4.6	2	2
Hepatic Failure [description not available]	0	3.8	1	1
Liver Failure Severe inability of the LIVER to perform its normal metabolic functions, as evidenced by severe JAUNDICE and abnormal serum levels of AMMONIA; BILIRUBIN; ALKALINE PHOSPHATASE; ASPARTATE AMINOTRANSFERASE; LACTATE DEHYDROGENASES; and albumin/globulin ratio. (Blakiston's Gould Medical Dictionary, 4th ed)	0	3.8	1	1
Bone Cancer [description not available]	0	4.51	1	1
Cancer of Stomach [description not available]	0	4.51	1	1
Bone Neoplasms Tumors or cancer located in bone tissue or specific BONES.	0	4.51	1	1
Stomach Neoplasms Tumors or cancer of the STOMACH.	1	7.94	2	2
Disease Exacerbation [description not available]	0	2.21	1	0

gdc-0068

Description

Cross-References

Synonyms (60)

Research Excerpts

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (8)

Potency Measurements

Inhibition Measurements

Activation Measurements

Biological Processes (191)

Molecular Functions (32)

Ceullar Components (26)

Bioassays (127)

Research

Studies (62)

Market Indicators

Research Demand Index: 27.19

Study Types

gdc-0068

Description

Cross-References

Synonyms (60)

Research Excerpts

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (8)

Potency Measurements

Inhibition Measurements

Activation Measurements

Biological Processes (191)

Molecular Functions (32)

Ceullar Components (26)

Bioassays (127)

Research

Studies (62)

Market Indicators

Research Demand Index: 27.19

Study Types

Related Drugs (44)

Related Conditions (49)