Page last updated: 2024-08-01 13:18:30

ophiocordin

Description

ophiocordin: metabolite of Cordyceps ophioglossoides [MeSH]

Cross-References

ID SourceID
PubMed CID5490846
PubMed CID5287736
CHEMBL ID60254
SCHEMBL ID62128
MeSH IDM0064622

Synonyms (30)

Synonym
ophiocordin
(4z)-4-[(2-carboxy-6-hydroxyphenyl)-hydroxymethylidene]-3-hydroxy-1-[(3r,4r)-3-[(4-hydroxybenzoyl)amino]-2,3,4,5-tetrahydro-1h-azepin-4-yl]-5-oxocyclohex-2-ene-1-carboxylic acid
unii-o0n0e1mp23
benzoic acid, 4-(2-(((hexahydro-4-((4-hydroxybenzoyl)oxy)-1h-azepin-3-yl)amino)carbonyl)-6-hydroxybenzoyl)-3,5-dihydroxy-
63590-19-2
bdbm3149
2-{[2,6-dihydroxy-4-({[(3r,4r)-3-[(4-hydroxybenzene)amido]azepan-4-yl]oxy}carbonyl)phenyl]carbonyl}-3-hydroxybenzoic acid
balanol, 1
chembl60254 ,
MEGXM0_000504
ACON0_001438
balanol
2-[2,6-dihydroxy-4-[(3r,4r)-3-[(4-hydroxybenzoyl)amino]azepan-4-yl]oxycarbonylbenzoyl]-3-hydroxybenzoic acid
bdbm36607
(-)-balanol
azepinostatin
gtpl8142
SCHEMBL62128
2-(2,6-dihydroxy-4-(((3r,4r)-3-(4-hydroxybenzamido)azepan-4-yloxy)carbonyl)benzoyl)-3-hydroxybenzoic acid
2-{[2,6-dihydroxy-4-({[(3r,4r)-3-{[(4-hydroxyphenyl)carbonyl]amino}azepan-4-yl]oxy}carbonyl)phenyl]carbonyl}-3-hydroxybenzoic acid
167937-47-5
benzoic acid, 4-(2-carboxy-6-hydroxybenzoyl)-3,5-dihydroxy-, (3r,4r)-hexahydro-3-((4-hydroxybenzoyl)amino)-1h-azepin-4-yl ester
benzoic acid, 4-(2-carboxy-6-hydroxybenzoyl)-3,5-dihydroxy-, 1-(hexahydro-3-((4-hydroxybenzoyl)amino)-1h-azepin-4-yl) ester, (3r-trans)-
Q4850048
ophiocordin;azepinostatin
rac-balanol
DTXSID201318143
HY-121197
CS-0080790
AKOS040745594

Protein Targets (28)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Serine/threonine-protein kinase D3Homo sapiens (human)Ki0.0053AID254306
cAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)IC500.0400AID1795486
Protein kinase C gamma typeHomo sapiens (human)IC500.0148AID163879; AID164004; AID1795485
Protein kinase C gamma typeHomo sapiens (human)Ki0.0053AID254306
Protein kinase C beta typeHomo sapiens (human)IC500.0199AID163196; AID163200; AID163340; AID163351; AID1795485; AID1795494
Protein kinase C beta typeHomo sapiens (human)Ki0.0053AID254306
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)IC5010.0000AID205485
Protein kinase C alpha typeHomo sapiens (human)IC500.0248AID162844; AID165308; AID1795485; AID1795494
Protein kinase C alpha typeHomo sapiens (human)Ki0.0053AID254306
cAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)IC500.0270AID164608; AID1902445
cAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)Ki0.0047AID254305
Beta-adrenergic receptor kinase 1Bos taurus (cattle)IC500.0350AID1315720
cAMP-dependent protein kinase catalytic subunit gammaHomo sapiens (human)IC500.0040AID1902445
cAMP-dependent protein kinase catalytic subunit gammaHomo sapiens (human)Ki0.0047AID254305
cAMP-dependent protein kinase catalytic subunit betaHomo sapiens (human)IC500.0040AID1902445
cAMP-dependent protein kinase catalytic subunit betaHomo sapiens (human)Ki0.0047AID254305
Protein kinase C eta typeHomo sapiens (human)IC500.0113AID163860; AID164046; AID1795485; AID1902373
Protein kinase C eta typeHomo sapiens (human)Ki0.0053AID254306
Beta-adrenergic receptor kinase 1Homo sapiens (human)IC500.0420AID464308
Rhodopsin kinase GRK1Bos taurus (cattle)IC504.1000AID1315721
G protein-coupled receptor kinase 4Homo sapiens (human)IC500.2600AID464310
G protein-coupled receptor kinase 5Homo sapiens (human)IC500.1600AID464311
Beta-adrenergic receptor kinase 2Homo sapiens (human)IC500.0470AID464309
Protein kinase C iota typeHomo sapiens (human)Ki0.0053AID254306
G protein-coupled receptor kinase 5Bos taurus (cattle)IC500.4400AID1315722
G protein-coupled receptor kinase 6Homo sapiens (human)IC500.4900AID464312
Protein kinase C beta typeRattus norvegicus (Norway rat)Ki0.0053AID1799441
Protein kinase C epsilon typeHomo sapiens (human)IC500.0223AID163686; AID163694; AID1795485; AID1795494
Protein kinase C epsilon typeHomo sapiens (human)Ki0.0053AID254306
Protein kinase C theta typeHomo sapiens (human)Ki0.0053AID254306
Protein kinase C zeta typeHomo sapiens (human)IC507.4000AID164196
Protein kinase C zeta typeHomo sapiens (human)Ki0.0053AID254306
Protein kinase C delta typeHomo sapiens (human)IC500.0141AID163378; AID163505; AID1795485
Protein kinase C delta typeHomo sapiens (human)Ki0.0053AID254306
Serine/threonine-protein kinase D1Homo sapiens (human)Ki0.0053AID254306
Rhodopsin kinase GRK1Homo sapiens (human)IC500.3400AID464307
Rhodopsin kinase GRK7Homo sapiens (human)IC500.1800AID464313

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Protein kinase C beta typeHomo sapiens (human)Kd0.0018AID1315726
Protein kinase C alpha typeHomo sapiens (human)Kd0.0064AID1315725
cAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)Kd0.0039AID1315723
cGMP-dependent protein kinase 1 Homo sapiens (human)Kd0.0016AID1315724

Bioassays (60)

Assay IDTitleYearJournalArticle
AID1345341Human beta adrenergic receptor kinase 1 (Beta-adrenergic receptor kinases (betaARKs))2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
ISSN: 1520-4804
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
AID1345396Human protein kinase C eta (Eta subfamily)1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID1345398Human protein kinase C zeta (Iota subfamily)1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID1345307Human protein kinase C gamma (Alpha subfamily)1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID1345320Human G protein-coupled receptor kinase 7 (Opsin/rhodopsin kinases)2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
ISSN: 1520-4804
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
AID1345401Human G protein-coupled receptor kinase 6 (GRK4 subfamily)2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
ISSN: 1520-4804
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
AID1345313Human G protein-coupled receptor kinase 4 (GRK4 subfamily)2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
ISSN: 1520-4804
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
AID1345382Human protein kinase C delta (Delta subfamily)1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID1345308Human protein kinase C beta (Alpha subfamily)1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID1345397Human protein kinase C epsilon (Eta subfamily)1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID1345407Human protein kinase C alpha (Delta subfamily)1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID1345395Human beta adrenergic receptor kinase 2 (Beta-adrenergic receptor kinases (betaARKs))2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
ISSN: 1520-4804
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
AID1345331Human G protein-coupled receptor kinase 1 (Opsin/rhodopsin kinases)2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
ISSN: 1520-4804
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
AID1795485PKC assay from Article 10.1021/jm960581w: \\Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.\\1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID1795494PKC assay from Article 10.1021/jm020018f: \\Synthesis and protein kinase inhibitory activity of balanol analogues with modified benzophenone subunits.\\2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
ISSN: 0022-2623
Synthesis and protein kinase inhibitory activity of balanol analogues with modified benzophenone subunits.
AID1799441Inhibition Assay from Article 10.1016/1074-5521(95)90124-8: \\Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol.\\1995Chemistry & biology, Sep, Volume: 2, Issue:9
ISSN: 1074-5521
Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol.
AID1795486PKA assay from Article 10.1021/jm960581w: \\Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.\\1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID1799442Inhibition Assay from Article 10.1016/1074-5521(95)90124-8: \\Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol.\\1995Chemistry & biology, Sep, Volume: 2, Issue:9
ISSN: 1074-5521
Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol.
AID44948Inhibition of rat brain Ca 2+/Calmodulin dependent kinase1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID163694Inhibitory concentration against recombinant human Protein kinase C epsilon isozyme1997Journal of medicinal chemistry, Jan-17, Volume: 40, Issue:2
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.
AID165308Evaluated against recombinant human Protein kinase C alpha1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID1315721Inhibition of bovine C-terminal truncated GRK1 (535 residues) assessed as decrease in phosphorylation of urea-washed bovine rod outer segments preincubated for 30 mins followed by ATP addition and light exposure measured after 5 to 10 mins by SDS-PAGE ana2016Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20
ISSN: 1520-4804
G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.
AID1902373Inhibition of PKCeta (unknown origin) by IMAP kinase assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
ISSN: 1520-4804
Novel Aurora A and Protein Kinase C (α, β1, β2, and θ) Multitarget Inhibitors: Impact of Selenium Atoms on the Potency and Selectivity.
AID254306Inhibitory constant against protein kinase C2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
ISSN: 0022-2623
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.
AID163200Inhibitory concentration against recombinant human Protein kinase C beta 1 isozyme1997Journal of medicinal chemistry, Jan-17, Volume: 40, Issue:2
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.
AID464314Inhibition of PKA2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
ISSN: 1520-4804
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
AID49343Inhibition of rat brain Casein kinase II1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID1315720Inhibition of bovine GRK2 S670A mutant expressed in Baculovirus expression system assessed as decrease in phosphorylation of urea-washed bovine rod outer segments preincubated for 30 mins followed by ATP addition and light exposure measured after 5 to 10 2016Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20
ISSN: 1520-4804
G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.
AID254305Inhibitory constant against the protein kinase A2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
ISSN: 0022-2623
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.
AID163860Inhibitory concentration against recombinant human Protein kinase C eta isozyme1997Journal of medicinal chemistry, Jan-17, Volume: 40, Issue:2
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.
AID164609Evaluated against recombinant human Protein Kinase A (PKA)1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID164004Inhibitory concentration against recombinant human Protein kinase C gamma isozyme1997Journal of medicinal chemistry, Jan-17, Volume: 40, Issue:2
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.
AID464308Inhibition of GRK2-mediated bovine tubulin phosphorylation by scintillation counting2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
ISSN: 1520-4804
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
AID164046Evaluated against recombinant human Protein kinase C eta1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID711537Inhibition of Protein kinase C2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
ISSN: 1520-4804
Synopsis of some recent tactical application of bioisosteres in drug design.
AID163378Evaluated against recombinant human Protein kinase C delta1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID464313Inhibition of GRK7-mediated bovine tubulin phosphorylation by scintillation counting2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
ISSN: 1520-4804
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
AID205485Inhibition of src Protein Tyrosine Kinase1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID1315724Binding affinity to human recombinant N-terminal GST-tagged PKGalpha expressed in Baculovirus infected insect Sf9 cells using RKRSRAE as substrate in presence of [gamma-32P]ATP2016Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20
ISSN: 1520-4804
G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.
AID711536Inhibition of cAMP-dependent protein kinase2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
ISSN: 1520-4804
Synopsis of some recent tactical application of bioisosteres in drug design.
AID1902445Inhibition of PKA (unknown origin)2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
ISSN: 1520-4804
Novel Aurora A and Protein Kinase C (α, β1, β2, and θ) Multitarget Inhibitors: Impact of Selenium Atoms on the Potency and Selectivity.
AID1315726Binding affinity to PKCbeta2 (unknown origin) using Lys-Arg-Thr-Leu-Arg-Arg as substrate after 8 mins in presence of [gamma-32P]ATP by liquid scintillation spectrometry2016Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20
ISSN: 1520-4804
G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.
AID163351Inhibitory concentration against recombinant human Protein kinase C beta 2 isozyme1997Journal of medicinal chemistry, Jan-17, Volume: 40, Issue:2
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.
AID163196Evaluated against recombinant human Protein kinase C beta 11996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID1315723Binding affinity to PKAalpha (unknown origin) using Lys-Arg-Thr-Leu-Arg-Arg as substrate after 8 mins in presence of [gamma-32P]ATP by liquid scintillation spectrometry2016Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20
ISSN: 1520-4804
G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.
AID162844Inhibitory concentration against recombinant human Protein kinase C alpha isozyme1997Journal of medicinal chemistry, Jan-17, Volume: 40, Issue:2
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.
AID163010Inhibition of Protein kinase C alpha2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
ISSN: 0022-2623
Computational analysis of PKA-balanol interactions.
AID464310Inhibition of GRK4-mediated bovine tubulin phosphorylation by scintillation counting2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
ISSN: 1520-4804
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
AID163505Inhibitory concentration against recombinant human Protein kinase C delta isozyme1997Journal of medicinal chemistry, Jan-17, Volume: 40, Issue:2
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.
AID464309Inhibition of GRK3-mediated bovine tubulin phosphorylation by scintillation counting2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
ISSN: 1520-4804
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
AID464312Inhibition of GRK6-mediated bovine tubulin phosphorylation by scintillation counting2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
ISSN: 1520-4804
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
AID464311Inhibition of GRK5-mediated bovine tubulin phosphorylation by scintillation counting2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
ISSN: 1520-4804
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
AID163686Evaluated against recombinant human Protein kinase C epsilon1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID464307Inhibition of GRK1-mediated bovine tubulin phosphorylation by scintillation counting2010Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
ISSN: 1520-4804
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
AID1315725Binding affinity to PKCalpha (unknown origin) using Lys-Arg-Thr-Leu-Arg-Arg as substrate after 8 mins in presence of [gamma-32P]ATP by liquid scintillation spectrometry2016Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20
ISSN: 1520-4804
G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.
AID163340Evaluated against recombinant human Protein kinase C beta 21996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
AID1315722Inhibition of bovine C-terminal truncated GRK5 (561 residues) assessed as decrease in phosphorylation of urea-washed bovine rod outer segments preincubated for 30 mins followed by ATP addition and light exposure measured after 5 to 10 mins by SDS-PAGE ana2016Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20
ISSN: 1520-4804
G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.
AID164196Inhibitory concentration against recombinant human Protein kinase C zeta isozyme1997Journal of medicinal chemistry, Jan-17, Volume: 40, Issue:2
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.
AID164608Inhibitory concentration against recombinant human cAMP-dependent Protein kinase A1997Journal of medicinal chemistry, Jan-17, Volume: 40, Issue:2
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.
AID163879Evaluated against recombinant human Protein kinase C gamma1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
ISSN: 0022-2623
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.

Research

Studies (40)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's13 (32.50)18.2507
2000's15 (37.50)29.6817
2010's9 (22.50)24.3611
2020's3 (7.50)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews5 (10.64%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other42 (89.36%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
gamma-aminobutyric acidamino acid zwitterion;
gamma-amino acid;
monocarboxylic acid
human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
2011201113.0low000010
phenolphenolsantiseptic drug;
disinfectant;
human xenobiotic metabolite;
mouse metabolite
2011201113.0low000010
acetohydroxamic acidacetohydroxamic acids;
carbohydroximic acid
algal metabolite;
EC 3.5.1.5 (urease) inhibitor
2011201113.0low000010
celecoxiborganofluorine compound;
pyrazoles;
sulfonamide;
toluenes
cyclooxygenase 2 inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
2011201113.0low000010
haloperidolaromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol
antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
2011201113.0low000010
losartanbiphenylyltetrazole;
imidazoles
angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist
2011201113.0low000010
nimesulidearomatic ether;
C-nitro compound;
sulfonamide
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
2011201113.0low000010
pd 153035aromatic amine;
aromatic ether;
bromobenzenes;
quinazolines;
secondary amino compound
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist
2011201113.0low000010
trifluperidolaromatic ketone2011201113.0low000010
venlafaxinecyclohexanols;
monomethoxybenzene;
tertiary alcohol;
tertiary amino compound
adrenergic uptake inhibitor;
analgesic;
antidepressant;
dopamine uptake inhibitor;
environmental contaminant;
serotonin uptake inhibitor;
xenobiotic
2011201113.0low000010
estrone17-oxo steroid;
3-hydroxy steroid;
phenolic steroid;
phenols
antineoplastic agent;
bone density conservation agent;
estrogen;
human metabolite;
mouse metabolite
2011201113.0low000010
nifenalolC-nitro compound2011201113.0low000010
2'-deoxyadenosine triphosphate2'-deoxyadenosine 5'-phosphate;
purine 2'-deoxyribonucleoside 5'-triphosphate
Escherichia coli metabolite;
mouse metabolite
2011201113.0low000010
glutamic acidglutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid
Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
2011201113.0low000010
paclitaxeltaxane diterpenoid;
tetracyclic diterpenoid
antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
2005200519.0low000100
staurosporineindolocarbazole alkaloid;
organic heterooctacyclic compound
apoptosis inducer;
bacterial metabolite;
EC 2.7.11.13 (protein kinase C) inhibitor;
geroprotector
1995199529.0low001000
paroxetine hydrochloridehydrochlorideantidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
201620168.0low000010
thymidine 5'-triphosphatepyrimidine 2'-deoxyribonucleoside 5'-triphosphate;
thymidine phosphate
Escherichia coli metabolite;
mouse metabolite
2011201113.0low000010
2'-deoxycytidine 5'-triphosphate2'-deoxycytidine phosphate;
pyrimidine 2'-deoxyribonucleoside 5'-triphosphate
Escherichia coli metabolite;
human metabolite;
mouse metabolite
2011201113.0low000010
inositol hexasulfate201620168.0low000010
5,6,7,8-tetrahydro-1-naphtholtetralins2011201113.0medium000010
dmp 323diazepanone;
ureas
anti-HIV agent;
metabolite
2011201113.0low000010
estrone 3-methyl ether2011201113.0medium000010
inositol 1-phosphate201620168.0low000010
sc 58125organofluorine compound;
pyrazoles;
sulfone
antineoplastic agent;
cyclooxygenase 2 inhibitor
2011201113.0low000010
bmy 45778bisoxazolepartial prostacyclin agonist2011201113.0low000010
exp77112011201113.0low000010
bmy 423932011201113.0low000010
mk 9962011201113.0medium000010
ezetimibeazetidines;
beta-lactam;
organofluorine compound
anticholesteremic drug;
antilipemic drug;
antimetabolite
2011201113.0low000010
ruboxistaurin202220222.0low000001
enzastaurinindoles;
maleimides
202220222.0low000001
l 1588092011201113.0low000010
epothilone bepothilone;
epoxide
antineoplastic agent;
apoptosis inducer;
microtubule-stabilising agent
2005200519.0low000100
epothilone aepothilone;
epoxide
antineoplastic agent;
metabolite;
microtubule-stabilising agent;
tubulin modulator
2005200519.0low000100
telaprevircyclopentapyrrole;
cyclopropanes;
oligopeptide;
pyrazines
antiviral drug;
hepatitis C protease inhibitor;
peptidomimetic
2011201113.0low000010
chaetomellic acid a2011201113.0low000010
rottlerinaromatic ketone;
benzenetriol;
chromenol;
enone;
methyl ketone
anti-allergic agent;
antihypertensive agent;
antineoplastic agent;
apoptosis inducer;
K-ATP channel agonist;
metabolite
202220222.0low000001
sirolimusantibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol
antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
2005200519.0low000100
upf 5962011201113.0low000010
iloprostcarbobicyclic compound;
monocarboxylic acid;
secondary alcohol
platelet aggregation inhibitor;
vasodilator agent
2011201113.0low000010
fexaraminebiphenyls2005200519.0low000100
sarcodictyin a2005200519.0medium000100
vx680N-arylpiperazine202220222.0low000001
psammaplin a2005200519.0low000100
cyc 116202220222.0low000001
way 1335372011201113.0medium000010
dpc 4232011201113.0medium000010
hamigeran b2005200519.0low000100
snap 62012011201113.0high000010
sotrastaurinindoles;
maleimides;
N-alkylpiperazine;
N-arylpiperazine;
quinazolines
anticoronaviral agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
immunosuppressive agent
202220222.0low000001
apicularen a2005200519.0low000100
brevetoxin bciguatoxin2005200519.0low000100
103d5r2005200519.0high000100
danusertibpiperazines202220222.0low000001
somatostatinheterodetic cyclic peptide;
peptide hormone
2005200519.0low000100
mln 8237benzazepine202220222.0low000001
sns 314ureas202220222.0low000001
gsk 1070916pyrazoles;
ring assembly
202220222.0low000001
deoxyguanosine triphosphatedeoxyguanosine phosphate;
guanyl deoxyribonucleotide;
purine 2'-deoxyribonucleoside 5'-triphosphate
Arabidopsis thaliana metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
2011201113.0low000010
guanosine diphosphateguanosine 5'-phosphate;
purine ribonucleoside 5'-diphosphate
Escherichia coli metabolite;
mouse metabolite;
uncoupling protein inhibitor
2011201113.0low000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
bisindolylmaleimide i1999199925.0low001000
go 6976indolocarbazole;
organic heterohexacyclic compound
EC 2.7.11.13 (protein kinase C) inhibitor1999199925.0low001000
ro 31-8220imidothiocarbamic ester;
indoles;
maleimides
EC 2.7.11.13 (protein kinase C) inhibitor1999199925.0low001000
ethylene oxidegas molecular entity;
oxacycle;
saturated organic heteromonocyclic parent
allergen;
mouse metabolite;
mutagen
2008200816.0low000100
pyrrolespyrrole;
secondary amine
1999199925.0low001000
hexahydroazepineazacycloalkane;
azepanes;
saturated organic heteromonocyclic parent
2000200820.0medium001100
1,4-cyclohexadienecyclohexadiene2008200816.0low000100
palladiummetal allergen;
nickel group element atom;
platinum group metal atom
1999199925.0low001000
rutheniumiron group element atom;
platinum group metal atom
1999199925.0low001000
fluorinediatomic fluorine;
gas molecular entity
NMR chemical shift reference compound201720186.5low000020
alkenes1999199925.0low001000
ro 32-04321999199925.0low001000
ruboxistaurin1999199925.0low001000
h 89N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide201620168.0low000010
staurosporineammonium ion derivative2004200420.0low000100
riboseD-ribose;
ribopyranose
201920195.0low000010
bryostatin 11999199925.0low001000
aprinocarsen1999199925.0low001000
guanosine triphosphateguanosine 5'-phosphate;
purine ribonucleoside 5'-triphosphate
Escherichia coli metabolite;
mouse metabolite;
uncoupling protein inhibitor
1999199925.0low001000
inosine triphosphateinosine phosphate;
purine ribonucleoside 5'-triphosphate
Escherichia coli metabolite;
human metabolite;
mouse metabolite
1999199925.0low001000
magnesium itp1999199925.0medium001000
magnesium gtp1999199925.0low001000
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Breast Cancer0202220222.0high000001
Breast Neoplasms0202220222.0high000001
Colorectal Cancer0202320231.0high000001
Colorectal Neoplasms0202320231.0high000001