Compounds > bix 02188
Page last updated: 2024-10-15

bix 02188

Description

BIX 02188: a MEK5 inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID135398492
CHEMBL ID4303171
SCHEMBL ID16685266
SCHEMBL ID16685268
SCHEMBL ID16685264
SCHEMBL ID21143306
MeSH IDM0527063

Synonyms (48)

Synonym
HY-12055
bix02188 ,
1094614-84-2
3-[[[3-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1h-indole-6-carboxamide;(z)-3-((3-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxamide
bix 02188
bix-02188
BCP9000421
AKOS015966567
4y3vyy2x83 ,
unii-4y3vyy2x83
3-[[[3-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1h-indole-6-carboxamide
CS-0214
(z)-3-((3-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxamide
(3z)-3-[[[3-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1h-indole-6-carboxamide
334949-59-6
gtpl8064
(3z)-3-[[3-[(dimethylamino)methyl]anilino]-phenylmethylidene]-2-oxo-1h-indole-6-carboxamide
1h-indole-6-carboxamide, 3-(((3-((dimethylamino)methyl)phenyl)amino)phenylmethylene)-2,3-dihydro-2-oxo-, (3z)-
(z)-3-(((3-((dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxamide
J-501300
AKOS025117452
3,3,3-trifluoroalaninehydrochloride
AC-28462
SCHEMBL16685266
SCHEMBL16685268
SCHEMBL16685264
EX-A221
AKOS030255959
3-[({3-[(dimethylamino)methyl]phenyl}amino)(phenyl)methylidene]-2-oxo-2,3-dihydro-1h-indole-6-carboxamide
AS-74756
bix02188 (bix 02188
FT-0773373
bix-02188 (random configuration)
bdbm50559802
3-(((3-((dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxamide
Q27075324
BCP11305
SCHEMBL21143306
SB19418
HMS3674E11
CHEMBL4303171 ,
NCGC00389358-01
A875276
3-[n-[3-[(dimethylamino)methyl]phenyl]-c-phenylcarbonimidoyl]-2-hydroxy-1h-indole-6-carboxamide
AS-82731
(e/z)-bix02188
CS-0028992
HY-107622

Bioavailability

ExcerptReference
"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)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Dual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)IC50 (µMol)0.00430.00150.81995.7000AID1720300
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
negative regulation of transcription by RNA polymerase IIDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
MAPK cascadeDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
signal transductionDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
heart developmentDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
positive regulation of cell growthDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activityDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
negative regulation of interleukin-8 productionDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
negative regulation of heterotypic cell-cell adhesionDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
negative regulation of smooth muscle cell apoptotic processDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
positive regulation of MAP kinase activityDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
insulin-like growth factor receptor signaling pathwayDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
positive regulation of epithelial cell proliferationDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
positive regulation of protein metabolic processDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
negative regulation of response to cytokine stimulusDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
ERK5 cascadeDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
cellular response to growth factor stimulusDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
cellular response to laminar fluid shear stressDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
negative regulation of cell migration involved in sprouting angiogenesisDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
negative regulation of chemokine (C-X-C motif) ligand 2 productionDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
protein kinase activityDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
protein serine/threonine kinase activityDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
protein tyrosine kinase activityDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
protein bindingDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
ATP bindingDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
metal ion bindingDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
protein serine kinase activityDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
MAP kinase kinase activityDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
spindleDual specificity mitogen-activated protein kinase kinase 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID1720302Selectivity ratio of IC50 for TGFbetaR1 (unknown origin) to IC50 for MEK5 (unknown origin)2020Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13
Non-'classical' MEKs: A review of MEK3-7 inhibitors.
AID1720301Selectivity ratio of IC50 for ERK5 (unknown origin) to IC50 for MEK5 (unknown origin)2020Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13
Non-'classical' MEKs: A review of MEK3-7 inhibitors.
AID1720300Inhibition of MEK5 (unknown origin)2020Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13
Non-'classical' MEKs: A review of MEK3-7 inhibitors.
AID1347411qHTS 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) Libary2020ACS 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.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1345731Human mitogen-activated protein kinase kinase 5 (STE7 family)2008Biochemical and biophysical research communications, Dec-05, Volume: 377, Issue:1
Identification of pharmacological inhibitors of the MEK5/ERK5 pathway.
AID1345738Human mitogen-activated protein kinase 7 (ERK subfamily)2008Biochemical and biophysical research communications, Dec-05, Volume: 377, Issue:1
Identification of pharmacological inhibitors of the MEK5/ERK5 pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (11.11)29.6817
2010's6 (66.67)24.3611
2020's2 (22.22)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (22.22%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (77.78%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
ethacrynic acid
Ethacrynic Acid: A compound that inhibits symport of sodium, potassium, and chloride primarily in the ascending limb of Henle, but also in the proximal and distal tubules. This pharmacological action results in excretion of these ions, increased urinary output, and reduction in extracellular fluid. This compound has been classified as a loop or high ceiling diuretic.. etacrynic acid : An aromatic ether that is phenoxyacetic acid in which the phenyl ring is substituted by chlorines at positions 2 and 3, and by a 2-methylidenebutanoyl group at position 4. It is a loop diuretic used to treat high blood pressure resulting from diseases such as congestive heart failure, liver failure, and kidney failure. It is also a glutathione S-transferase (EC 2.5.1.18) inhibitor.		3.3510aromatic ether;
aromatic ketone;
dichlorobenzene;
monocarboxylic acid		EC 2.5.1.18 (glutathione transferase) inhibitor;
ion transport inhibitor;
loop diuretic
sorbitol
D-glucitol : The D-enantiomer of glucitol (also known as D-sorbitol).		2.0410glucitolcathartic;
Escherichia coli metabolite;
food humectant;
human metabolite;
laxative;
metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite;
sweetening agent
u 0126
U 0126: protein kinase kinase inhibitor; structure in first source		2.0710aryl sulfide;
dinitrile;
enamine;
substituted aniline		antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
osteogenesis regulator;
vasoconstrictor agent
genistein
[no description available]		3.35107-hydroxyisoflavonesantineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
morphine
Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.		2.0610morphinane alkaloid;
organic heteropentacyclic compound;
tertiary amino compound		anaesthetic;
drug allergen;
environmental contaminant;
geroprotector;
mu-opioid receptor agonist;
opioid analgesic;
plant metabolite;
vasodilator agent;
xenobiotic
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.		2.0710
bix 02189
[no description available]		4.3930
ConditionIndicatedRelationship StrengthStudiesTrials
Degenerative Disc Disease
[description not available]		02.110
Intervertebral Disc Degeneration
Degenerative changes in the INTERVERTEBRAL DISC due to aging or structural damage, especially to the vertebral end-plates.		02.110
Morphine Abuse
[description not available]		02.0610
Morphine Dependence
Strong dependence, both physiological and emotional, upon morphine.		02.0610
Leucocythaemia
[description not available]		02.0610
Leukemia
A progressive, malignant disease of the blood-forming organs, characterized by distorted proliferation and development of leukocytes and their precursors in the blood and bone marrow. Leukemias were originally termed acute or chronic based on life expectancy but now are classified according to cellular maturity. Acute leukemias consist of predominately immature cells; chronic leukemias are composed of more mature cells. (From The Merck Manual, 2006)		02.0610