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108 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1.EBI
National Cancer Institute-Frederick
Design of potent protein kinase inhibitors using the bisubstrate approach.EBI
Ura Cnrs 1309
Synthesis of quaternary amine ether lipids and evaluation of neoplastic cell growth inhibitory properties.EBI
University Of North Carolina
Synthesis of N-alkyl substituted indolocarbazoles as potent inhibitors of human cytomegalovirus replication.EBI
Glaxosmithkline
Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).EBI
Icahn School Of Medicine At Mount Sinai
Discovery of selective and orally bioavailable protein kinase C¿ (PKC¿) inhibitors from a fragment hit.EBI
Abbvie Bioresearch Center
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI
Exelixis
Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases.EBI
Vertex Pharmaceuticals
Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases.EBI
Martin-Luther-University Halle-Wittenberg
Structure-activity studies on the spiroketal moiety of a simplified analogue of debromoaplysiatoxin with antiproliferative activity.EBI
Kyoto University
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.EBI
University Of California
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI
University Of Oxford
Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction.EBI
Kyoto University
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI
Abbott Laboratories
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.EBI
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Kinase inhibitors: not just for kinases anymore.EBI
Northwestern University
Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.EBI
Johnson And Johnson Pharmaceutical Research And Development
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.EBI
Millennium Pharmaceuticals
New hexahydroxybiphenyl derivatives as inhibitors of protein kinase C.EBI
University Of North Carolina
Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V.EBI
Kyoto University
Structure-activity relationship studies of flavopiridol analogues.EBI
Mitotix
 
Synthesis and PKC inhibitory activities of balanol analogs with a cyclopentane substructureEBI
TBA
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).EBI
Ansaris
Generation of 'Unnatural Natural Product' library and identification of a small molecule inhibitor of XIAP.EBI
Keio University
Hippolides A-H, acyclic manoalide derivatives from the marine sponge Hippospongia lachne.EBI
Second Military Medical University
Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors.EBI
Martin-Luther-University Halle-Wittenberg
Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.EBI
Kyoto University
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.EBI
Abbott Laboratories
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI
Abbott Laboratories
Anti-AIDS Agents, 11. Betulinic Acid and Platanic Acid as Anti-HIV Principles from Syzigium claviflorum, and the Anti-HIV Activity of Structurally Related TriterpenoidsEBI
TBA
 
Benzo[c]quinoliziniums: A new family of inhibitors for protein kinase CK IIEBI
TBA
 
A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylationEBI
TBA
 
Synthesis and protein kinase C inhibitory activities of indane analogs of balanolEBI
TBA
 
Potent and selective PKC inhibitory 5-membered ring analogs of balanol with replacement of the carboxamide moietyEBI
TBA
 
Heteroatom effect in the PKC inhibitory activities of perhydroazepine analogs of balanolEBI
TBA
 
Novel PKC inhibitory analogs of balanol with replacement of the ester functionalityEBI
TBA
 
Conformationally constrained analogues of diacylglycerol (DAG). 4. Interaction of α-alkylidene-γ-lactones with protein kinase C (PK-C)EBI
TBA
Conformationally constrained analogues of diacylglycerol (DAG). 31. Modulation of the biological properties of diacylgycerol lactones (DAG-lactones) containing rigid-rod acyl groups separated from the core lactone by spacer units of different lengths.EBI
National Cancer Institute-Frederick
(-)-Cercosporamide derivatives as novel antihyperglycemic agents.EBI
Daiichi Sankyo
Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits.EBI
University Of California San Francisco
Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes.EBI
Kyoto University
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.EBI
Abbott Laboratories
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.EBI
Abbott Laboratories
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Design and synthesis of 8-octyl-benzolactam-V9, a selective activator for protein kinase C epsilon and eta.EBI
Kyoto University
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.EBI
Abbott Bioresearch Center
Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.EBI
Johnson & Johnson Pharmaceutical Research & Development
Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.EBI
Johnson & Johnson Pharmaceutical Research & Development
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.EBI
Eli Lilly
New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity.EBI
Georgetown University Medical Center
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.EBI
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and binding selectivity of 7- and 15-decylbenzolactone-V8 for the C1 domains of protein kinase C isozymes.EBI
Kyoto University
Novel IKK inhibitors: beta-carbolines.EBI
Millennium Pharmaceuticals
Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.EBI
Eli Lilly
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI
Boehringer Ingelheim Pharmaceuticals
Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a.EBI
Cephalon
Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.EBI
Abbott Bioresearch Center
Beta-carbolines as specific inhibitors of cyclin-dependent kinases.EBI
Institute Of Molecular And Cell Biology
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.EBI
Georgetotwn University
The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities.EBI
Kyoto University
The C4 hydroxyl group of phorbol esters is not necessary for protein kinase C binding.EBI
Kyoto University
Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.EBI
Basf Bioresearch
Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952.EBI
Japan Tobacco
Synthesis and biological activities of NB-506 analogues modified at the glucose group.EBI
Banyu Tsukuba Research Institute
4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: potent and selective inhibitors of ZAP 70.EBI
Celltech Therapeutics
Synthesis and biological activities of NB-506 analogues: Effects of the positions of two hydroxyl groups at the indole rings.EBI
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.EBI
Chinese Academy Of Sciences
Selective binding of bryostatin analogues to the cysteine rich domains of protein kinase C isozymes.EBI
Stanford University
Discovery of 4EBI
TBA
Synthesis and Structure-Activity Relationship Correlations of Gnidimacrin Derivatives as Potent HIV-1 Inhibitors and HIV Latency Reversing Agents.EBI
Toho University
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.EBI
China Pharmaceutical University
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.EBI
University Of Florida
Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivity.EBI
Georgetown University Medical Center
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.EBI
Takeda Pharmaceutical
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.EBI
Eli Lilly
(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.EBI
Eli Lilly
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.EBI
Abbvie Bioresearch Center
Effects of the methoxy group in the side chain of debromoaplysiatoxin on its tumor-promoting and anti-proliferative activities.EBI
Kyoto University
Glycoglycerolipid analogues inhibit PKC translocation to the plasma membrane and downstream signaling pathways in PMA-treated fibroblasts and human glioblastoma cells, U87MG.EBI
University Of Milan
Bioactive peroxides as potential therapeutic agents.EBI
The Hebrew University Of Jerusalem
Syntheses and biological activities of rebeccamycin analogues. Introduction of a halogenoacetyl substituent.EBI
Universit£
Syntheses and biological evaluation of indolocarbazoles, analogues of rebeccamycin, modified at the imide heterocycle.EBI
Universit£
An aminopyridazine-based inhibitor of a pro-apoptotic protein kinase attenuates hypoxia-ischemia induced acute brain injury.EBI
Northwestern University
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.EBI
Kaohsiung Medical University
A novel 2,4-diaminopyrimidine derivative as selective inhibitor of protein kinase C theta prevents allograft rejection in a rat heart transplant model.EBI
Astellas Pharma
Natural Products with Heteroatom-Rich Ring Systems.EBI
University Of Auckland
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.EBI
Vertex Pharmaceuticals
Synthesis and anticancer activity of novel bisindolylhydroxymaleimide derivatives with potent GSK-3 kinase inhibition.EBI
University College Cork
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.EBI
Vertex Pharmaceuticals
Discovery of Novel Small-Molecule Inhibitors of NF-?B Signaling with Antiinflammatory and Anticancer Properties.EBI
University Of Colorado
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.EBI
The Ohio State University
Methyl 3-(3-(4-(2,4,4-Trimethylpentan-2-yl)phenoxy)-propanamido)benzoate as a Novel and Dual Malate Dehydrogenase (MDH) 1/2 Inhibitor Targeting Cancer Metabolism.EBI
Dongguk University
Hexosaminidase inhibitors as new drug candidates for the therapy of osteoarthritis.BDB
The Scripps Research Institute
Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.BDB
Shanghai Institute Of Materia Medica
Specificity and affinity of natural product cyclopentapeptide inhibitors against A. fumigatus, human, and bacterial chitinases.BDB
University Of Dundee
Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.BDB
Cnrs
 
DISCOVERY AND STRUCTURE-ACTIVITY STUDIES OF A NOVEL SERIES OF PYRIDO[2,3-d]PYRIMIDINE TYROSINE KINASE INHIBITORSBDB
Parke-Davis Pharmaceutical Research