pamapimod profile

pamapimod : A member of the class of pyridopyrimidines that is 8-methylpyrido[2,3-d]pyrimidin-7(8H)-one carrying additional (1,5-dihydroxypentan-3-yl)amino and 2,4-difluorophenoxy substituents at positions 2 and 6 respectively. It is a potent inhibitor of MAPK and is used for treatment of rheumatoid arthritis. [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]

ID Source	ID
PubMed CID	16220188
CHEMBL ID	1090089
CHEBI ID	90685
SCHEMBL ID	3636701
MeSH ID	M0527875

Synonym
6-(2,4-difluorophenoxy)-2-{[3-hydroxy-1-(2-hydroxyethyl)propyl]amino}-8-methylpyrido[2,3-d]pyrimidin-7(8h)-one
FLW ,
pamapimod (inn/usan)
449811-01-2
D08963
6-(2,4-difluorophenoxy)-2-[[3-hydroxy-1-(2-hydroxyethyl)propyl]amino]-8-methylpyrido[2,3-d]pyrimidin-7(8h)-one
r 1503
SCHEMBL3636701
bdbm50314070
R1503 ,
pamapimod
r-1503
ro-4402257
CHEMBL1090089 ,
chebi:90685 ,
ro 4402257
6-(2,4-difluorophenoxy)-2-((3-hydroxy-1-(2-hydroxyethyl)propyl)amino)-8-methylpyrido(2,3-d)pyrimidin-7(8h)-one
pyrido(2,3-d)pyrimidin-7(8h)-one, 6-(2,4-difluorophenoxy)-2-((3-hydroxy-1-(2-hydroxyethyl)propyl)amino)-8-methyl-
unii-8s2c9v11k4
pamapimod [usan:inn]
8s2c9v11k4 ,
FT-0673504
S8125
pamapimod [usan]
pamapimod [inn]
pamapimod [who-dd]
AC-33182
6-(2,4-difluorophenoxy)-2-[(1,5-dihydroxypentan-3-yl)amino]-8-methylpyrido[2,3-d]pyrimidin-7(8h)-one
HY-10405
EX-A1084
6-(2,4-difluorophenoxy)-2-[(1,5-dihydroxypentan-3-yl)amino]-8-methyl-7h,8h-pyrido[2,3-d]pyrimidin-7-one
CS-5965
mfcd25976551
6-(2,4-difluorophenoxy)-2-((1,5-dihydroxypentan-3-yl)amino)-8-methylpyrido[2,3-d]pyrimidin-7(8h)-one
pamapimodr-1503
compound 2b [pmid: 21375264]
gtpl9915
6-(2,4-difluorophenoxy)-2-(1,5-dihydroxypentan-3-ylamino)-8-methylpyrido[2,3-d]pyrimidin-7-one
AKOS032944999
BCP17491
Q27162644
pamapimod (r-1503, ro4402257)
ro4402257
6-(2,4-difluorophenoxy)-2-[(1,5-dihydroxypentan-3-yl)imino]-8-methyl-2,8-dihydropyrido[2,3-d]pyrimidin-7(3h)-one
DTXSID90963312
CCG-268715
AS-56094

Excerpt	Reference	Relevance
"Pamapimod (PAM) is a novel selective p38 mitogen-activated protein (MAP) kinase inhibitor proved to be effective in rheumatoid arthritis in phase 2 clinical trial. "	( The Novel p38 Inhibitor, Pamapimod, Inhibits Osteoclastogenesis and Counteracts Estrogen-Dependent Bone Loss in Mice. Fan, S; Huang, B; Jie, Z; Li, X; Ma, Y; Ning, L; Qin, A; Shen, S; Song, L; Sun, X; Tang, P; Wan, S; Wan, X; Xie, Z; Zhao, X, 2019)	2.26

Excerpt	Reference	Relevance
" Safety monitoring included recording of adverse events (AEs), laboratory testing, immunology assessments, administration of electrocardiograms, and assessment of vital signs."	( Evaluation of the efficacy and safety of pamapimod, a p38 MAP kinase inhibitor, in a double-blind, methotrexate-controlled study of patients with active rheumatoid arthritis. Burgos-Vargas, R; Caulfield, JP; Cheng, TT; Chindalore, V; Cohen, SB; Damjanov, N; Delora, P; Travers, H; Zimany, K, 2009)	0.62
" Pamapimod was generally well tolerated, but the 300-mg dose appeared to be more toxic than either the 2 lower doses or MTX."	( Evaluation of the efficacy and safety of pamapimod, a p38 MAP kinase inhibitor, in a double-blind, methotrexate-controlled study of patients with active rheumatoid arthritis. Burgos-Vargas, R; Caulfield, JP; Cheng, TT; Chindalore, V; Cohen, SB; Damjanov, N; Delora, P; Travers, H; Zimany, K, 2009)	1.53
" Safety measures included adverse events (AEs), laboratory testing and immunology assessments."	( Efficacy and safety of pamapimod in patients with active rheumatoid arthritis receiving stable methotrexate therapy. Alten, RE; Bertasso, A; Caulfield, JP; Emery, P; Irazoque, F; Jeka, S; Khatib, F; Rabbia, M; Zerbini, C, 2010)	0.67

Role	Description
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor	An EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of mitogen-activated protein kinase (EC 2.7.11.24).
antirheumatic drug	A drug used to treat rheumatoid arthritis.
[role 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]

Class	Description
pyridopyrimidine	Any organic heterobicyclic compound consisting of a pyridine ring ortho-fused at any position to a pyrimidine ring.
aromatic ether	Any ether in which the oxygen is attached to at least one aryl substituent.
difluorobenzene	Any member of the class of fluorobenzenes containing a mono- or poly-substituted benzene ring carrying two fluorine atoms.
aromatic amine	An amino compound in which the amino group is linked directly to an aromatic system.
secondary amino compound	A compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
primary alcohol	A primary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has either three hydrogen atoms attached to it or only one other carbon atom and two hydrogen atoms attached to it.
diol	A compound that contains two hydroxy groups, generally assumed to be, but not necessarily, alcoholic. Aliphatic diols are also called glycols.
[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 Targets (19)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Cytochrome P450 1A2	Homo sapiens (human)	IC50 (µMol)	29.0000	0.0001	1.7740	10.0000	AID592484
Cytochrome P450 3A4	Homo sapiens (human)	IC50 (µMol)	29.0000	0.0001	1.7536	10.0000	AID592488
Cytochrome P450 2D6	Homo sapiens (human)	IC50 (µMol)	29.0000	0.0000	2.0151	10.0000	AID592487
Cytochrome P450 2C9	Homo sapiens (human)	IC50 (µMol)	29.0000	0.0000	2.8005	10.0000	AID592485
Substance-P receptor	Cavia porcellus (domestic guinea pig)	IC50 (µMol)	29.0000	0.0000	2.7518	10.0000	AID592488
Cytochrome P450 2C19	Homo sapiens (human)	IC50 (µMol)	29.0000	0.0000	2.3983	10.0000	AID592486
Mitogen-activated protein kinase 8	Homo sapiens (human)	IC50 (µMol)	5.4200	0.0020	1.0173	5.4200	AID1269008
Mitogen-activated protein kinase 14	Homo sapiens (human)	IC50 (µMol)	0.0140	0.0001	0.7266	7.8000	AID476311; AID592303
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Cyclin-G-associated kinase	Homo sapiens (human)	Kd	1.0000	0.0003	0.9086	28.6510	AID592323
Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)	Kd	0.1500	0.0120	1.6396	7.2000	AID592376
Mitogen-activated protein kinase 8	Homo sapiens (human)	Kd	0.1900	0.0110	2.0965	26.0590	AID476307; AID592324
Mitogen-activated protein kinase 9	Homo sapiens (human)	Kd	0.0160	0.0020	1.4596	8.1000	AID476302; AID592325
Casein kinase I isoform epsilon	Homo sapiens (human)	Kd	0.2600	0.0130	1.4086	12.4090	AID476308; AID592321
Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)	Kd	0.3000	0.0170	2.8896	37.6050	AID592375
Mitogen-activated protein kinase 10	Homo sapiens (human)	Kd	0.0190	0.0010	1.6354	5.9000	AID476303; AID592326
Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)	Kd	1.0000	0.0002	1.6314	71.4840	AID592322
Mitogen-activated protein kinase 11	Homo sapiens (human)	Kd	0.1200	0.0001	0.4610	3.7430	AID476301; AID592319
Mitogen-activated protein kinase 14	Homo sapiens (human)	Kd	0.0013	0.0000	0.5036	8.5000	AID476300; AID592305
Atypical kinase COQ8A, mitochondrial	Homo sapiens (human)	Kd	1.0000	0.0940	5.1673	65.3020	AID592320
Serine/threonine-protein kinase 36	Homo sapiens (human)	Kd	1.0000	0.1800	2.7651	8.3000	AID592377
Serine/threonine-protein kinase NLK	Homo sapiens (human)	Kd	0.1700	0.0060	1.0226	4.4000	AID476305; AID592374
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (229)

Process	via Protein(s)	Taxonomy
receptor-mediated endocytosis	Cyclin-G-associated kinase	Homo sapiens (human)
endoplasmic reticulum organization	Cyclin-G-associated kinase	Homo sapiens (human)
Golgi organization	Cyclin-G-associated kinase	Homo sapiens (human)
negative regulation of neuron projection development	Cyclin-G-associated kinase	Homo sapiens (human)
synaptic vesicle uncoating	Cyclin-G-associated kinase	Homo sapiens (human)
protein localization to Golgi apparatus	Cyclin-G-associated kinase	Homo sapiens (human)
intracellular transport	Cyclin-G-associated kinase	Homo sapiens (human)
clathrin coat assembly	Cyclin-G-associated kinase	Homo sapiens (human)
chaperone cofactor-dependent protein refolding	Cyclin-G-associated kinase	Homo sapiens (human)
clathrin coat disassembly	Cyclin-G-associated kinase	Homo sapiens (human)
clathrin-dependent endocytosis	Cyclin-G-associated kinase	Homo sapiens (human)
protein localization to plasma membrane	Cyclin-G-associated kinase	Homo sapiens (human)
Golgi to lysosome transport	Cyclin-G-associated kinase	Homo sapiens (human)
regulation of clathrin coat assembly	Cyclin-G-associated kinase	Homo sapiens (human)
negative regulation of cytokine production	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
chromatin remodeling	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
regulation of DNA-templated transcription	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
protein phosphorylation	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
inflammatory response	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
positive regulation of CREB transcription factor activity	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
intracellular signal transduction	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
post-translational protein modification	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activity	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
interleukin-1-mediated signaling pathway	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
peptidyl-serine phosphorylation	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 1A2	Homo sapiens (human)
porphyrin-containing compound metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
toxin biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
post-embryonic development	Cytochrome P450 1A2	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
regulation of gene expression	Cytochrome P450 1A2	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
dibenzo-p-dioxin metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 1A2	Homo sapiens (human)
lung development	Cytochrome P450 1A2	Homo sapiens (human)
methylation	Cytochrome P450 1A2	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 1A2	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
cellular respiration	Cytochrome P450 1A2	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
hydrogen peroxide biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 1A2	Homo sapiens (human)
cellular response to cadmium ion	Cytochrome P450 1A2	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 1A2	Homo sapiens (human)
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
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)
xenobiotic metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
urea metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
amide metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
icosanoid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2C9	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C19	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C19	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C19	Homo sapiens (human)
JUN phosphorylation	Mitogen-activated protein kinase 8	Homo sapiens (human)
response to UV	Mitogen-activated protein kinase 8	Homo sapiens (human)
negative regulation of apoptotic process	Mitogen-activated protein kinase 8	Homo sapiens (human)
cellular response to lipopolysaccharide	Mitogen-activated protein kinase 8	Homo sapiens (human)
protein phosphorylation	Mitogen-activated protein kinase 8	Homo sapiens (human)
response to oxidative stress	Mitogen-activated protein kinase 8	Homo sapiens (human)
JNK cascade	Mitogen-activated protein kinase 8	Homo sapiens (human)
JUN phosphorylation	Mitogen-activated protein kinase 8	Homo sapiens (human)
positive regulation of gene expression	Mitogen-activated protein kinase 8	Homo sapiens (human)
regulation of macroautophagy	Mitogen-activated protein kinase 8	Homo sapiens (human)
peptidyl-serine phosphorylation	Mitogen-activated protein kinase 8	Homo sapiens (human)
peptidyl-threonine phosphorylation	Mitogen-activated protein kinase 8	Homo sapiens (human)
positive regulation of cyclase activity	Mitogen-activated protein kinase 8	Homo sapiens (human)
positive regulation of cell killing	Mitogen-activated protein kinase 8	Homo sapiens (human)
negative regulation of protein binding	Mitogen-activated protein kinase 8	Homo sapiens (human)
regulation of protein localization	Mitogen-activated protein kinase 8	Homo sapiens (human)
cellular response to amino acid starvation	Mitogen-activated protein kinase 8	Homo sapiens (human)
cellular response to oxidative stress	Mitogen-activated protein kinase 8	Homo sapiens (human)
cellular response to reactive oxygen species	Mitogen-activated protein kinase 8	Homo sapiens (human)
Fc-epsilon receptor signaling pathway	Mitogen-activated protein kinase 8	Homo sapiens (human)
regulation of circadian rhythm	Mitogen-activated protein kinase 8	Homo sapiens (human)
positive regulation of apoptotic process	Mitogen-activated protein kinase 8	Homo sapiens (human)
negative regulation of apoptotic process	Mitogen-activated protein kinase 8	Homo sapiens (human)
rhythmic process	Mitogen-activated protein kinase 8	Homo sapiens (human)
positive regulation of protein metabolic process	Mitogen-activated protein kinase 8	Homo sapiens (human)
stress-activated MAPK cascade	Mitogen-activated protein kinase 8	Homo sapiens (human)
cellular response to mechanical stimulus	Mitogen-activated protein kinase 8	Homo sapiens (human)
cellular response to cadmium ion	Mitogen-activated protein kinase 8	Homo sapiens (human)
cellular senescence	Mitogen-activated protein kinase 8	Homo sapiens (human)
energy homeostasis	Mitogen-activated protein kinase 8	Homo sapiens (human)
positive regulation of NLRP3 inflammasome complex assembly	Mitogen-activated protein kinase 8	Homo sapiens (human)
response to mechanical stimulus	Mitogen-activated protein kinase 8	Homo sapiens (human)
positive regulation of establishment of protein localization to mitochondrion	Mitogen-activated protein kinase 8	Homo sapiens (human)
protein phosphorylation	Mitogen-activated protein kinase 9	Homo sapiens (human)
JNK cascade	Mitogen-activated protein kinase 9	Homo sapiens (human)
positive regulation of gene expression	Mitogen-activated protein kinase 9	Homo sapiens (human)
positive regulation of macrophage derived foam cell differentiation	Mitogen-activated protein kinase 9	Homo sapiens (human)
positive regulation of protein ubiquitination	Mitogen-activated protein kinase 9	Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic process	Mitogen-activated protein kinase 9	Homo sapiens (human)
cellular response to reactive oxygen species	Mitogen-activated protein kinase 9	Homo sapiens (human)
Fc-epsilon receptor signaling pathway	Mitogen-activated protein kinase 9	Homo sapiens (human)
regulation of circadian rhythm	Mitogen-activated protein kinase 9	Homo sapiens (human)
rhythmic process	Mitogen-activated protein kinase 9	Homo sapiens (human)
modulation of chemical synaptic transmission	Mitogen-activated protein kinase 9	Homo sapiens (human)
protein localization to tricellular tight junction	Mitogen-activated protein kinase 9	Homo sapiens (human)
cellular response to cadmium ion	Mitogen-activated protein kinase 9	Homo sapiens (human)
positive regulation of podosome assembly	Mitogen-activated protein kinase 9	Homo sapiens (human)
cellular senescence	Mitogen-activated protein kinase 9	Homo sapiens (human)
inflammatory response to wounding	Mitogen-activated protein kinase 9	Homo sapiens (human)
apoptotic signaling pathway	Mitogen-activated protein kinase 9	Homo sapiens (human)
positive regulation of cytokine production involved in inflammatory response	Mitogen-activated protein kinase 9	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Mitogen-activated protein kinase 9	Homo sapiens (human)
DNA repair	Casein kinase I isoform epsilon	Homo sapiens (human)
protein phosphorylation	Casein kinase I isoform epsilon	Homo sapiens (human)
protein localization	Casein kinase I isoform epsilon	Homo sapiens (human)
negative regulation of Wnt signaling pathway	Casein kinase I isoform epsilon	Homo sapiens (human)
negative regulation of protein binding	Casein kinase I isoform epsilon	Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic process	Casein kinase I isoform epsilon	Homo sapiens (human)
regulation of protein localization	Casein kinase I isoform epsilon	Homo sapiens (human)
circadian regulation of gene expression	Casein kinase I isoform epsilon	Homo sapiens (human)
regulation of circadian rhythm	Casein kinase I isoform epsilon	Homo sapiens (human)
circadian behavior	Casein kinase I isoform epsilon	Homo sapiens (human)
canonical Wnt signaling pathway	Casein kinase I isoform epsilon	Homo sapiens (human)
positive regulation of amyloid-beta formation	Casein kinase I isoform epsilon	Homo sapiens (human)
cellular response to nerve growth factor stimulus	Casein kinase I isoform epsilon	Homo sapiens (human)
positive regulation of non-canonical Wnt signaling pathway	Casein kinase I isoform epsilon	Homo sapiens (human)
peptidyl-serine phosphorylation	Casein kinase I isoform epsilon	Homo sapiens (human)
endocytosis	Casein kinase I isoform epsilon	Homo sapiens (human)
positive regulation of canonical Wnt signaling pathway	Casein kinase I isoform epsilon	Homo sapiens (human)
signal transduction	Casein kinase I isoform epsilon	Homo sapiens (human)
skeletal system development	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
toll-like receptor signaling pathway	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
signal transduction	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
chemical synaptic transmission	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
central nervous system development	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
peptidyl-serine phosphorylation	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
positive regulation of cell growth	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
response to lipopolysaccharide	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
intracellular signal transduction	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
negative regulation of apoptotic process	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic process	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
regulation of translation in response to stress	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
positive regulation of cell differentiation	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
protein phosphorylation	Mitogen-activated protein kinase 10	Homo sapiens (human)
signal transduction	Mitogen-activated protein kinase 10	Homo sapiens (human)
JNK cascade	Mitogen-activated protein kinase 10	Homo sapiens (human)
response to light stimulus	Mitogen-activated protein kinase 10	Homo sapiens (human)
Fc-epsilon receptor signaling pathway	Mitogen-activated protein kinase 10	Homo sapiens (human)
regulation of circadian rhythm	Mitogen-activated protein kinase 10	Homo sapiens (human)
rhythmic process	Mitogen-activated protein kinase 10	Homo sapiens (human)
cellular senescence	Mitogen-activated protein kinase 10	Homo sapiens (human)
regulation of cell growth	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
regulation of cell-matrix adhesion	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
cell adhesion	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
embryo implantation	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
lactation	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
cell population proliferation	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
negative regulation of cell population proliferation	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
regulation of extracellular matrix disassembly	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
smooth muscle cell migration	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
collagen-activated tyrosine kinase receptor signaling pathway	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
peptidyl-tyrosine autophosphorylation	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
ear development	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
wound healing, spreading of cells	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
protein autophosphorylation	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
branching involved in mammary gland duct morphogenesis	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
mammary gland alveolus development	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
smooth muscle cell-matrix adhesion	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
axon development	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
neuron projection extension	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathway	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
multicellular organism development	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
positive regulation of kinase activity	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
positive regulation of neuron projection development	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
positive regulation of erythrocyte differentiation	Mitogen-activated protein kinase 11	Homo sapiens (human)
osteoblast differentiation	Mitogen-activated protein kinase 11	Homo sapiens (human)
positive regulation of gene expression	Mitogen-activated protein kinase 11	Homo sapiens (human)
stress-activated protein kinase signaling cascade	Mitogen-activated protein kinase 11	Homo sapiens (human)
positive regulation of interleukin-12 production	Mitogen-activated protein kinase 11	Homo sapiens (human)
p38MAPK cascade	Mitogen-activated protein kinase 11	Homo sapiens (human)
positive regulation of muscle cell differentiation	Mitogen-activated protein kinase 11	Homo sapiens (human)
stress-activated MAPK cascade	Mitogen-activated protein kinase 11	Homo sapiens (human)
cardiac muscle cell proliferation	Mitogen-activated protein kinase 11	Homo sapiens (human)
negative regulation of cardiac muscle cell proliferation	Mitogen-activated protein kinase 11	Homo sapiens (human)
bone development	Mitogen-activated protein kinase 11	Homo sapiens (human)
cellular response to interleukin-1	Mitogen-activated protein kinase 11	Homo sapiens (human)
cellular response to UV-B	Mitogen-activated protein kinase 11	Homo sapiens (human)
cellular senescence	Mitogen-activated protein kinase 11	Homo sapiens (human)
cellular response to virus	Mitogen-activated protein kinase 11	Homo sapiens (human)
intracellular signal transduction	Mitogen-activated protein kinase 11	Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration	Mitogen-activated protein kinase 14	Homo sapiens (human)
cellular response to lipopolysaccharide	Mitogen-activated protein kinase 14	Homo sapiens (human)
DNA damage checkpoint signaling	Mitogen-activated protein kinase 14	Homo sapiens (human)
cell morphogenesis	Mitogen-activated protein kinase 14	Homo sapiens (human)
cartilage condensation	Mitogen-activated protein kinase 14	Homo sapiens (human)
angiogenesis	Mitogen-activated protein kinase 14	Homo sapiens (human)
osteoblast differentiation	Mitogen-activated protein kinase 14	Homo sapiens (human)
placenta development	Mitogen-activated protein kinase 14	Homo sapiens (human)
response to dietary excess	Mitogen-activated protein kinase 14	Homo sapiens (human)
chondrocyte differentiation	Mitogen-activated protein kinase 14	Homo sapiens (human)
negative regulation of inflammatory response to antigenic stimulus	Mitogen-activated protein kinase 14	Homo sapiens (human)
glucose metabolic process	Mitogen-activated protein kinase 14	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Mitogen-activated protein kinase 14	Homo sapiens (human)
transcription by RNA polymerase II	Mitogen-activated protein kinase 14	Homo sapiens (human)
apoptotic process	Mitogen-activated protein kinase 14	Homo sapiens (human)
chemotaxis	Mitogen-activated protein kinase 14	Homo sapiens (human)
signal transduction	Mitogen-activated protein kinase 14	Homo sapiens (human)
cell surface receptor signaling pathway	Mitogen-activated protein kinase 14	Homo sapiens (human)
cell surface receptor protein serine/threonine kinase signaling pathway	Mitogen-activated protein kinase 14	Homo sapiens (human)
skeletal muscle tissue development	Mitogen-activated protein kinase 14	Homo sapiens (human)
positive regulation of gene expression	Mitogen-activated protein kinase 14	Homo sapiens (human)
positive regulation of myotube differentiation	Mitogen-activated protein kinase 14	Homo sapiens (human)
peptidyl-serine phosphorylation	Mitogen-activated protein kinase 14	Homo sapiens (human)
fatty acid oxidation	Mitogen-activated protein kinase 14	Homo sapiens (human)
platelet activation	Mitogen-activated protein kinase 14	Homo sapiens (human)
regulation of ossification	Mitogen-activated protein kinase 14	Homo sapiens (human)
osteoclast differentiation	Mitogen-activated protein kinase 14	Homo sapiens (human)
stress-activated protein kinase signaling cascade	Mitogen-activated protein kinase 14	Homo sapiens (human)
positive regulation of cyclase activity	Mitogen-activated protein kinase 14	Homo sapiens (human)
lipopolysaccharide-mediated signaling pathway	Mitogen-activated protein kinase 14	Homo sapiens (human)
response to muramyl dipeptide	Mitogen-activated protein kinase 14	Homo sapiens (human)
positive regulation of interleukin-12 production	Mitogen-activated protein kinase 14	Homo sapiens (human)
response to insulin	Mitogen-activated protein kinase 14	Homo sapiens (human)
negative regulation of hippo signaling	Mitogen-activated protein kinase 14	Homo sapiens (human)
intracellular signal transduction	Mitogen-activated protein kinase 14	Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulus	Mitogen-activated protein kinase 14	Homo sapiens (human)
response to muscle stretch	Mitogen-activated protein kinase 14	Homo sapiens (human)
p38MAPK cascade	Mitogen-activated protein kinase 14	Homo sapiens (human)
positive regulation of protein import into nucleus	Mitogen-activated protein kinase 14	Homo sapiens (human)
signal transduction in response to DNA damage	Mitogen-activated protein kinase 14	Homo sapiens (human)
positive regulation of erythrocyte differentiation	Mitogen-activated protein kinase 14	Homo sapiens (human)
positive regulation of myoblast differentiation	Mitogen-activated protein kinase 14	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Mitogen-activated protein kinase 14	Homo sapiens (human)
glucose import	Mitogen-activated protein kinase 14	Homo sapiens (human)
positive regulation of glucose import	Mitogen-activated protein kinase 14	Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathway	Mitogen-activated protein kinase 14	Homo sapiens (human)
stem cell differentiation	Mitogen-activated protein kinase 14	Homo sapiens (human)
striated muscle cell differentiation	Mitogen-activated protein kinase 14	Homo sapiens (human)
positive regulation of muscle cell differentiation	Mitogen-activated protein kinase 14	Homo sapiens (human)
stress-activated MAPK cascade	Mitogen-activated protein kinase 14	Homo sapiens (human)
positive regulation of cardiac muscle cell proliferation	Mitogen-activated protein kinase 14	Homo sapiens (human)
bone development	Mitogen-activated protein kinase 14	Homo sapiens (human)
3'-UTR-mediated mRNA stabilization	Mitogen-activated protein kinase 14	Homo sapiens (human)
cellular response to lipoteichoic acid	Mitogen-activated protein kinase 14	Homo sapiens (human)
cellular response to tumor necrosis factor	Mitogen-activated protein kinase 14	Homo sapiens (human)
cellular response to ionizing radiation	Mitogen-activated protein kinase 14	Homo sapiens (human)
cellular response to UV-B	Mitogen-activated protein kinase 14	Homo sapiens (human)
negative regulation of canonical Wnt signaling pathway	Mitogen-activated protein kinase 14	Homo sapiens (human)
positive regulation of brown fat cell differentiation	Mitogen-activated protein kinase 14	Homo sapiens (human)
cellular senescence	Mitogen-activated protein kinase 14	Homo sapiens (human)
stress-induced premature senescence	Mitogen-activated protein kinase 14	Homo sapiens (human)
cellular response to virus	Mitogen-activated protein kinase 14	Homo sapiens (human)
regulation of synaptic membrane adhesion	Mitogen-activated protein kinase 14	Homo sapiens (human)
regulation of cytokine production involved in inflammatory response	Mitogen-activated protein kinase 14	Homo sapiens (human)
positive regulation of myoblast fusion	Mitogen-activated protein kinase 14	Homo sapiens (human)
positive regulation of reactive oxygen species metabolic process	Mitogen-activated protein kinase 14	Homo sapiens (human)
protein phosphorylation	Atypical kinase COQ8A, mitochondrial	Homo sapiens (human)
ubiquinone biosynthetic process	Atypical kinase COQ8A, mitochondrial	Homo sapiens (human)
phosphorylation	Atypical kinase COQ8A, mitochondrial	Homo sapiens (human)
epithelial cilium movement involved in extracellular fluid movement	Serine/threonine-protein kinase 36	Homo sapiens (human)
protein phosphorylation	Serine/threonine-protein kinase 36	Homo sapiens (human)
smoothened signaling pathway	Serine/threonine-protein kinase 36	Homo sapiens (human)
brain development	Serine/threonine-protein kinase 36	Homo sapiens (human)
post-embryonic development	Serine/threonine-protein kinase 36	Homo sapiens (human)
axoneme assembly	Serine/threonine-protein kinase 36	Homo sapiens (human)
positive regulation of smoothened signaling pathway	Serine/threonine-protein kinase 36	Homo sapiens (human)
regulation of DNA-binding transcription factor activity	Serine/threonine-protein kinase 36	Homo sapiens (human)
cilium assembly	Serine/threonine-protein kinase 36	Homo sapiens (human)
MAPK cascade	Serine/threonine-protein kinase NLK	Homo sapiens (human)
regulation of DNA-templated transcription	Serine/threonine-protein kinase NLK	Homo sapiens (human)
protein phosphorylation	Serine/threonine-protein kinase NLK	Homo sapiens (human)
transforming growth factor beta receptor signaling pathway	Serine/threonine-protein kinase NLK	Homo sapiens (human)
Wnt signaling pathway, calcium modulating pathway	Serine/threonine-protein kinase NLK	Homo sapiens (human)
peptidyl-threonine phosphorylation	Serine/threonine-protein kinase NLK	Homo sapiens (human)
negative regulation of Wnt signaling pathway	Serine/threonine-protein kinase NLK	Homo sapiens (human)
intracellular signal transduction	Serine/threonine-protein kinase NLK	Homo sapiens (human)
protein stabilization	Serine/threonine-protein kinase NLK	Homo sapiens (human)
cellular response to osmotic stress	Serine/threonine-protein kinase NLK	Homo sapiens (human)
negative regulation of TORC1 signaling	Serine/threonine-protein kinase NLK	Homo sapiens (human)
positive regulation of receptor signaling pathway via STAT	Serine/threonine-protein kinase NLK	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (68)

Process	via Protein(s)	Taxonomy
protein serine/threonine kinase activity	Cyclin-G-associated kinase	Homo sapiens (human)
protein binding	Cyclin-G-associated kinase	Homo sapiens (human)
ATP binding	Cyclin-G-associated kinase	Homo sapiens (human)
cyclin binding	Cyclin-G-associated kinase	Homo sapiens (human)
protein-folding chaperone binding	Cyclin-G-associated kinase	Homo sapiens (human)
protein serine kinase activity	Cyclin-G-associated kinase	Homo sapiens (human)
clathrin binding	Cyclin-G-associated kinase	Homo sapiens (human)
magnesium ion binding	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
protein serine/threonine kinase activity	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
ribosomal protein S6 kinase activity	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
protein binding	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
ATP binding	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
histone H3S10 kinase activity	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
histone H3S28 kinase activity	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
protein serine kinase activity	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 1A2	Homo sapiens (human)
iron ion binding	Cytochrome P450 1A2	Homo sapiens (human)
protein binding	Cytochrome P450 1A2	Homo sapiens (human)
electron transfer activity	Cytochrome P450 1A2	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 1A2	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 1A2	Homo sapiens (human)
enzyme binding	Cytochrome P450 1A2	Homo sapiens (human)
heme binding	Cytochrome P450 1A2	Homo sapiens (human)
demethylase activity	Cytochrome P450 1A2	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 1A2	Homo sapiens (human)
aromatase activity	Cytochrome P450 1A2	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 1A2	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 1A2	Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activity	Cytochrome P450 1A2	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
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)
monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 2C9	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C9	Homo sapiens (human)
heme binding	Cytochrome P450 2C9	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 2C9	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C19	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C19	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C19	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
oxygen binding	Cytochrome P450 2C19	Homo sapiens (human)
enzyme binding	Cytochrome P450 2C19	Homo sapiens (human)
heme binding	Cytochrome P450 2C19	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C19	Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activity	Cytochrome P450 2C19	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C19	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 2C19	Homo sapiens (human)
protein serine/threonine kinase activity	Mitogen-activated protein kinase 8	Homo sapiens (human)
JUN kinase activity	Mitogen-activated protein kinase 8	Homo sapiens (human)
protein binding	Mitogen-activated protein kinase 8	Homo sapiens (human)
ATP binding	Mitogen-activated protein kinase 8	Homo sapiens (human)
enzyme binding	Mitogen-activated protein kinase 8	Homo sapiens (human)
protein phosphatase binding	Mitogen-activated protein kinase 8	Homo sapiens (human)
histone deacetylase regulator activity	Mitogen-activated protein kinase 8	Homo sapiens (human)
histone deacetylase binding	Mitogen-activated protein kinase 8	Homo sapiens (human)
protein serine kinase activity	Mitogen-activated protein kinase 8	Homo sapiens (human)
protein serine/threonine kinase binding	Mitogen-activated protein kinase 8	Homo sapiens (human)
protein serine/threonine kinase activity	Mitogen-activated protein kinase 9	Homo sapiens (human)
JUN kinase activity	Mitogen-activated protein kinase 9	Homo sapiens (human)
protein serine/threonine/tyrosine kinase activity	Mitogen-activated protein kinase 9	Homo sapiens (human)
protein binding	Mitogen-activated protein kinase 9	Homo sapiens (human)
ATP binding	Mitogen-activated protein kinase 9	Homo sapiens (human)
protein serine kinase activity	Mitogen-activated protein kinase 9	Homo sapiens (human)
RNA binding	Casein kinase I isoform epsilon	Homo sapiens (human)
protein kinase activity	Casein kinase I isoform epsilon	Homo sapiens (human)
protein serine/threonine kinase activity	Casein kinase I isoform epsilon	Homo sapiens (human)
protein binding	Casein kinase I isoform epsilon	Homo sapiens (human)
ATP binding	Casein kinase I isoform epsilon	Homo sapiens (human)
protein serine kinase activity	Casein kinase I isoform epsilon	Homo sapiens (human)
magnesium ion binding	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
protein kinase activity	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
protein serine/threonine kinase activity	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
protein binding	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
ATP binding	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
protein kinase binding	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic process	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
protein serine kinase activity	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
ribosomal protein S6 kinase activity	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
JUN kinase activity	Mitogen-activated protein kinase 10	Homo sapiens (human)
MAP kinase kinase activity	Mitogen-activated protein kinase 10	Homo sapiens (human)
protein binding	Mitogen-activated protein kinase 10	Homo sapiens (human)
ATP binding	Mitogen-activated protein kinase 10	Homo sapiens (human)
protein serine kinase activity	Mitogen-activated protein kinase 10	Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activity	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
protein binding	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
collagen binding	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
ATP binding	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
protein tyrosine kinase collagen receptor activity	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
metal ion binding	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
protein serine/threonine kinase activity	Mitogen-activated protein kinase 11	Homo sapiens (human)
MAP kinase activity	Mitogen-activated protein kinase 11	Homo sapiens (human)
protein binding	Mitogen-activated protein kinase 11	Homo sapiens (human)
ATP binding	Mitogen-activated protein kinase 11	Homo sapiens (human)
protein serine kinase activity	Mitogen-activated protein kinase 11	Homo sapiens (human)
protein serine/threonine kinase activity	Mitogen-activated protein kinase 14	Homo sapiens (human)
MAP kinase activity	Mitogen-activated protein kinase 14	Homo sapiens (human)
MAP kinase kinase activity	Mitogen-activated protein kinase 14	Homo sapiens (human)
protein binding	Mitogen-activated protein kinase 14	Homo sapiens (human)
ATP binding	Mitogen-activated protein kinase 14	Homo sapiens (human)
enzyme binding	Mitogen-activated protein kinase 14	Homo sapiens (human)
protein phosphatase binding	Mitogen-activated protein kinase 14	Homo sapiens (human)
mitogen-activated protein kinase p38 binding	Mitogen-activated protein kinase 14	Homo sapiens (human)
NFAT protein binding	Mitogen-activated protein kinase 14	Homo sapiens (human)
protein serine kinase activity	Mitogen-activated protein kinase 14	Homo sapiens (human)
protein kinase activity	Atypical kinase COQ8A, mitochondrial	Homo sapiens (human)
protein binding	Atypical kinase COQ8A, mitochondrial	Homo sapiens (human)
ATP binding	Atypical kinase COQ8A, mitochondrial	Homo sapiens (human)
kinase activity	Atypical kinase COQ8A, mitochondrial	Homo sapiens (human)
ADP binding	Atypical kinase COQ8A, mitochondrial	Homo sapiens (human)
transcription corepressor binding	Serine/threonine-protein kinase 36	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase 36	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase 36	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase 36	Homo sapiens (human)
metal ion binding	Serine/threonine-protein kinase 36	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase 36	Homo sapiens (human)
magnesium ion binding	Serine/threonine-protein kinase NLK	Homo sapiens (human)
protein kinase activity	Serine/threonine-protein kinase NLK	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase NLK	Homo sapiens (human)
MAP kinase activity	Serine/threonine-protein kinase NLK	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase NLK	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase NLK	Homo sapiens (human)
ubiquitin protein ligase binding	Serine/threonine-protein kinase NLK	Homo sapiens (human)
SH2 domain binding	Serine/threonine-protein kinase NLK	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase NLK	Homo sapiens (human)
DNA-binding transcription factor binding	Serine/threonine-protein kinase NLK	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (35)

Process	via Protein(s)	Taxonomy
Golgi apparatus	Cyclin-G-associated kinase	Homo sapiens (human)
cytosol	Cyclin-G-associated kinase	Homo sapiens (human)
focal adhesion	Cyclin-G-associated kinase	Homo sapiens (human)
membrane	Cyclin-G-associated kinase	Homo sapiens (human)
clathrin-coated vesicle	Cyclin-G-associated kinase	Homo sapiens (human)
vesicle	Cyclin-G-associated kinase	Homo sapiens (human)
intracellular membrane-bounded organelle	Cyclin-G-associated kinase	Homo sapiens (human)
perinuclear region of cytoplasm	Cyclin-G-associated kinase	Homo sapiens (human)
presynapse	Cyclin-G-associated kinase	Homo sapiens (human)
vesicle	Cyclin-G-associated kinase	Homo sapiens (human)
cytoplasm	Cyclin-G-associated kinase	Homo sapiens (human)
intracellular membrane-bounded organelle	Cyclin-G-associated kinase	Homo sapiens (human)
nucleus	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
nucleoplasm	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
cytosol	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
synapse	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
cytoplasm	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
nucleoplasm	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 1A2	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 1A2	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 1A2	Homo sapiens (human)
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
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)
endoplasmic reticulum membrane	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C19	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C19	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C19	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C19	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C19	Homo sapiens (human)
cytoplasm	Mitogen-activated protein kinase 8	Homo sapiens (human)
nucleus	Mitogen-activated protein kinase 8	Homo sapiens (human)
nucleoplasm	Mitogen-activated protein kinase 8	Homo sapiens (human)
cytosol	Mitogen-activated protein kinase 8	Homo sapiens (human)
axon	Mitogen-activated protein kinase 8	Homo sapiens (human)
synapse	Mitogen-activated protein kinase 8	Homo sapiens (human)
basal dendrite	Mitogen-activated protein kinase 8	Homo sapiens (human)
nucleus	Mitogen-activated protein kinase 8	Homo sapiens (human)
nucleoplasm	Mitogen-activated protein kinase 9	Homo sapiens (human)
mitochondrion	Mitogen-activated protein kinase 9	Homo sapiens (human)
cytosol	Mitogen-activated protein kinase 9	Homo sapiens (human)
plasma membrane	Mitogen-activated protein kinase 9	Homo sapiens (human)
nuclear speck	Mitogen-activated protein kinase 9	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Mitogen-activated protein kinase 9	Homo sapiens (human)
cytoplasm	Mitogen-activated protein kinase 9	Homo sapiens (human)
nucleus	Mitogen-activated protein kinase 9	Homo sapiens (human)
nucleus	Casein kinase I isoform epsilon	Homo sapiens (human)
nucleoplasm	Casein kinase I isoform epsilon	Homo sapiens (human)
cytoplasm	Casein kinase I isoform epsilon	Homo sapiens (human)
cytosol	Casein kinase I isoform epsilon	Homo sapiens (human)
growth cone	Casein kinase I isoform epsilon	Homo sapiens (human)
neuronal cell body	Casein kinase I isoform epsilon	Homo sapiens (human)
ribonucleoprotein complex	Casein kinase I isoform epsilon	Homo sapiens (human)
cytoplasm	Casein kinase I isoform epsilon	Homo sapiens (human)
nucleus	Casein kinase I isoform epsilon	Homo sapiens (human)
nucleoplasm	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
nucleolus	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
cytosol	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
synapse	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
cytoplasm	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
nucleoplasm	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
nucleoplasm	Mitogen-activated protein kinase 10	Homo sapiens (human)
cytoplasm	Mitogen-activated protein kinase 10	Homo sapiens (human)
mitochondrion	Mitogen-activated protein kinase 10	Homo sapiens (human)
cytosol	Mitogen-activated protein kinase 10	Homo sapiens (human)
plasma membrane	Mitogen-activated protein kinase 10	Homo sapiens (human)
nucleus	Mitogen-activated protein kinase 10	Homo sapiens (human)
cytoplasm	Mitogen-activated protein kinase 10	Homo sapiens (human)
extracellular space	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
plasma membrane	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
extracellular exosome	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
receptor complex	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
plasma membrane	Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)
nucleoplasm	Mitogen-activated protein kinase 11	Homo sapiens (human)
cytosol	Mitogen-activated protein kinase 11	Homo sapiens (human)
cytoplasm	Mitogen-activated protein kinase 11	Homo sapiens (human)
nucleus	Mitogen-activated protein kinase 11	Homo sapiens (human)
cytosol	Mitogen-activated protein kinase 14	Homo sapiens (human)
spindle pole	Mitogen-activated protein kinase 14	Homo sapiens (human)
extracellular region	Mitogen-activated protein kinase 14	Homo sapiens (human)
nucleus	Mitogen-activated protein kinase 14	Homo sapiens (human)
nucleoplasm	Mitogen-activated protein kinase 14	Homo sapiens (human)
cytoplasm	Mitogen-activated protein kinase 14	Homo sapiens (human)
mitochondrion	Mitogen-activated protein kinase 14	Homo sapiens (human)
cytosol	Mitogen-activated protein kinase 14	Homo sapiens (human)
nuclear speck	Mitogen-activated protein kinase 14	Homo sapiens (human)
secretory granule lumen	Mitogen-activated protein kinase 14	Homo sapiens (human)
glutamatergic synapse	Mitogen-activated protein kinase 14	Homo sapiens (human)
ficolin-1-rich granule lumen	Mitogen-activated protein kinase 14	Homo sapiens (human)
nucleus	Mitogen-activated protein kinase 14	Homo sapiens (human)
cytoplasm	Mitogen-activated protein kinase 14	Homo sapiens (human)
mitochondrion	Atypical kinase COQ8A, mitochondrial	Homo sapiens (human)
membrane	Atypical kinase COQ8A, mitochondrial	Homo sapiens (human)
extracellular region	Serine/threonine-protein kinase 36	Homo sapiens (human)
nucleus	Serine/threonine-protein kinase 36	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase 36	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase 36	Homo sapiens (human)
cytoskeleton	Serine/threonine-protein kinase 36	Homo sapiens (human)
cell projection	Serine/threonine-protein kinase 36	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase 36	Homo sapiens (human)
nucleus	Serine/threonine-protein kinase NLK	Homo sapiens (human)
nucleoplasm	Serine/threonine-protein kinase NLK	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase NLK	Homo sapiens (human)
nucleus	Serine/threonine-protein kinase NLK	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase NLK	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID592468	Clearance in Hanover-Wistar rat at 5 mg/kg, iv	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592487	Inhibition of human CYP2D6	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592322	Inhibition of DDR1	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592384	Inhibition of LPS-induced TNFalpha production in rat serum at 3 mg/kg, po administered 30 mins before LPS challenge measured after 1.5 hrs by ELISA	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592374	Inhibition of NLK	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592471	Cmax in cynomolgus monkey at 5 mg/kg, po	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592484	Inhibition of human CYP1A2	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592469	Volume of distribution at steady state in Hanover-Wistar rat at 5 mg/kg, iv	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID476311	Inhibition of human recombinant p38alpha by liquid scintillation counting	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID592485	Inhibition of human CYP2C9	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592325	Inhibition of JNK2	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592483	Volume of distribution at steady state in Beagle dog at 5 mg/kg, iv	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID476318	Inhibition of collagen-induced arthritis in intradermally dosed DBA/1J mouse	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID592303	Inhibition of human recombinant p38alpha assessed as incorporation of 33P from gamma-[33P]ATP into myelin basic protein after 30 mins by scintillation counting	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592463	Tmax in Hanover-Wistar rat at 5 mg/kg, po	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592307	Inhibition of P38beta at 10 uM	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592387	Inhibition of TNF-alpha-induced IL-6 production in po dosed rat plasma administered 30 mins before TNFalpha challenge measured after 2 hrs by ELISA	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592305	Inhibition of p38alpha	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID1269008	Inhibition of JNK1 (unknown origin)	2016	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2	Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes.
AID592466	AUC (0 to last) in Hanover-Wistar rat at 5 mg/kg, po after 24 hrs	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592474	Oral bioavailability in cynomolgus monkey at 5 mg/kg	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID476319	Analgesic activity in po dosed Sprague-Dawley rat assessed as inhibition of mechanical hyperalgesia by Randall-Selitto test	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID592478	Cmax in Beagle dog at 5 mg/kg, po	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592482	Clearance in Beagle dog at 5 mg/kg, iv	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID1269087	Cytotoxicity against HEK293 after 24 hrs by CellTiter-Glo luminescent cell viability assay	2016	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2	Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes.
AID476300	Binding affinity to p38alpha	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID592318	Inhibition of STK36 at 10 uM	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592317	Inhibition of RSK4 at 10 uM	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592480	AUC (0 to last) in Beagle dog at 5 mg/kg, po	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592385	Inhibition of LPS-induced TNFalpha production in human THP1 cells after 2 hrs by ELISA	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592310	Inhibition of DDR1 at 10 uM	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592311	Inhibition of GAK at 10 uM	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592314	Inhibition of JNK3 at 10 uM	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592403	Plasma protein binding in cynomolgus monkey by untrafiltration method	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592467	Oral bioavailability in Hanover-Wistar rat at 5 mg/kg	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592319	Inhibition of P38beta	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592388	Analgesic activity in po dosed rat inflammatory yeast hyperalgesia model assessed as increase in tolerance to pressure	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592379	Aqueous solubility of the compound in phosphate buffer at pH 6.5	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592320	Inhibition of ADCK3	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592380	Permeability of the compound from apical to basolateral side of human Caco2 cells at 10 uM after 21 days	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID476313	Inhibition of LPS-induced IL1-beta production in human whole blood by ELISA	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID592488	Inhibition of human CYP3A4	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID476316	Inhibition of TNF-alpha-induced IL6 production in po BALB/c mouse by ELISA	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID592313	Inhibition of JNK2 at 10 uM	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592323	Inhibition of GAK	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592383	Inhibition of LPS-induced TNFalpha production in po dosed rat serum administered 30 mins before LPS challenge measured after 1.5 hrs by ELISA	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592470	Tmax in cynomolgus monkey at 5 mg/kg, po	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592386	Inhibition of LPS-induced IL-6 production in po dosed rat serum administered 30 mins before LPS challenge measured after 1.5 hrs by ELISA	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592306	Inhibition of human recombinant p38alpha assessed as incorporation of 33P from gamma-[33P]ATP into myelin basic protein at 10 uM after 30 mins by scintillation counting	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592308	Inhibition of ADCK3 at 10 uM	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID476301	Binding affinity to p38beta	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID476315	Inhibition of LPS-induced TNFalpha production in po BALB/c mouse by ELISA	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID592312	Inhibition of JNK1 at 10 uM	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID476303	Binding affinity to JNK3	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID592321	Inhibition of CSNK1epsilon	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID476302	Binding affinity to JNK2	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID592381	Permeability of the compound from basolateral to apical side of human Caco2 cells at 10 uM after 21 days	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592464	Cmax in Hanover-Wistar rat at 5 mg/kg, po	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592479	Half life in Beagle dog at 5 mg/kg, po	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592476	Volume of distribution at steady state in cynomolgus monkey at 5 mg/kg, iv	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID1269010	Inhibition of JNK1 (unknown origin) expressed in HEK293 cells assessed as anisomycin-induced c-Jun phosphorylation at 10 uM incubated for 30 mins by Western blot analysis relative to anisomycin	2016	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2	Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes.
AID476305	Binding affinity to NLK	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID592316	Inhibition of RSK2 at 10 uM	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID476308	Binding affinity to CSNK1epsilon	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID592324	Inhibition of JNK1	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592376	Inhibition of RSK4	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592326	Inhibition of JNK3	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592395	Plasma protein binding in Hanover-Wistar rat by untrafiltration method	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592377	Inhibition of STK36	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID476307	Binding affinity to JNK1	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID592465	Half life in Hanover-Wistar rat at 5 mg/kg, po	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592473	AUC (0 to last) in cynomolgus monkey at 5 mg/kg, po after 72 hrs	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID476310	Binding affinity to RSK3beta	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID476314	Inhibition of LPS-induced TNFalpha production in po dosed rat by ELISA	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID476312	Inhibition of LPS-induced TNFalpha production in human THP1 cells by ELISA	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID476317	Inhibition of LPS-induced IL6 production in po BALB/c mouse by ELISA	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID1269009	Inhibition of JNK1 (unknown origin) expressed in HEK293 cells assessed as anisomycin-induced IRS-1(Ser307) phosphorylation at 10 uM incubated for 30 mins by Western blot analysis relative to anisomycin	2016	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2	Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes.
AID592315	Inhibition of NLK at 10 uM	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592378	Inhibition of TNFalpha-induced IL1-beta production in human whole blood after 2 to 5 hrs by ELISA	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592477	Tmax in Beagle dog at 5 mg/kg, po	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592375	Inhibition of RSK2	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592309	Inhibition of CSNK1epsilon at 10 uM	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592481	Oral bioavailability in Beagle dog at 5 mg/kg	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID476309	Binding affinity to RSK4beta	2010	Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6	Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
AID592475	Clearance in cynomolgus monkey at 5 mg/kg, iv	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592472	Half life in cynomolgus monkey at 5 mg/kg, po	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592486	Inhibition of human CYP2C19	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID592382	Plasma protein binding in human by ultrafiltration method	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID1345333	Human mitogen-activated protein kinase 8 (JNK subfamily)	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID1345334	Human mitogen-activated protein kinase 11 (p38 subfamily)	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID1345304	Human mitogen-activated protein kinase 14 (p38 subfamily)	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID1345355	Human mitogen-activated protein kinase 9 (JNK subfamily)	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
AID1345347	Human mitogen-activated protein kinase 10 (JNK subfamily)	2011	Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7	Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally
[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	3 (27.27)	29.6817
2010's	7 (63.64)	24.3611
2020's	1 (9.09)	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	4 (36.36%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	7 (63.64%)	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
pioglitazone Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.. pioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity.	7.41	1	0	aromatic ether; pyridines; thiazolidinediones	antidepressant; cardioprotective agent; EC 2.7.1.33 (pantothenate kinase) inhibitor; EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; geroprotector; hypoglycemic agent; insulin-sensitizing drug; PPARgamma agonist; xenobiotic
methotrexate [no description available]	5.05	3	3	dicarboxylic acid; monocarboxylic acid amide; pteridines	abortifacient; antimetabolite; antineoplastic agent; antirheumatic drug; dermatologic drug; DNA synthesis inhibitor; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; immunosuppressive agent
birb 796 [no description available]	2.05	1	0	aromatic ether; morpholines; naphthalenes; pyrazoles; ureas	EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; immunomodulator
bi-78d3 [no description available]	2.13	1	0	aryl sulfide
vx-745 [no description available]	2.46	2	0	aryl sulfide; dichlorobenzene; difluorobenzene; pyrimidopyridazine	anti-inflammatory drug; apoptosis inducer; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
scio-469 SCIO-469: a small-molecule p38 mitogen-activated protein (MAP) kinase inhibitor for potential oral therapy for inflammatory disorders; in phase lib clinical trials for rheumatoid arthritis 4/2004. talmapimod : An indolecarboxamide obtained by formal condensation of the carboxy group of 6-chloro-3-[(dimethylamino)(oxo)acetyl]-1-methylindole-5-carboxylic acid with the secondary amino group of (2S,5R)-1-[(4-fluorophenyl)methyl]-2,5-dimethylpiperazine. It is a potent inhibitor of MAPK and exhibits anti-cancer properties.	2.46	2	0	aromatic amide; aromatic ketone; chloroindole; dicarboxylic acid diamide; indolecarboxamide; monofluorobenzenes; N-acylpiperazine; N-alkylpiperazine	antineoplastic agent; apoptosis inducer; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
vx 702 VX 702: a p38 MAP kinase inhibitor	2.46	2	0	phenylpyridine
r 1487 [no description available]	2.06	1	0
6-(5-((cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl)-n-(2,2-dimethylprpyl)-3-pyridinecarboxamide [no description available]	2.05	1	0	phenylpyridine
2-({2-[(3-hydroxyphenyl)amino]pyrimidin-4-yl}amino)benzamide [no description available]	2.13	1	0	aminopyrimidine; benzamides	protein kinase inhibitor
ph 797804 PH 797804: an NSAID; structure in first source. PH 797804 : A member of the class of benzamides obtained by formal condensation of the carboxy group of 3-{3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1-yl}-4-methylbenzoic acid with the amino group of methylamine.	2.05	1	0	aromatic ether; benzamides; organobromine compound; organofluorine compound; pyridone	anti-inflammatory agent; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
arry-371797 ARRY-371797: a p38 MAP kinase inhibitor	2.05	1	0

Condition	Relationship Strength	Studies	Trials
Chronic Illness [description not available]	2.05	1	0
Rheumatoid Arthritis [description not available]	5.74	7	3
Palmoplantaris Pustulosis [description not available]	2.05	1	0
Bowel Diseases, Inflammatory [description not available]	2.05	1	0
Arthritis, Rheumatoid A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.	5.74	7	3
Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).	2.05	1	0
Psoriasis A common genetically determined, chronic, inflammatory skin disease characterized by rounded erythematous, dry, scaling patches. The lesions have a predilection for nails, scalp, genitalia, extensor surfaces, and the lumbosacral region. Accelerated epidermopoiesis is considered to be the fundamental pathologic feature in psoriasis.	2.05	1	0
Inflammatory Bowel Diseases Chronic, non-specific inflammation of the GASTROINTESTINAL TRACT. Etiology may be genetic or environmental. This term includes CROHN DISEASE and ULCERATIVE COLITIS.	2.05	1	0
Diabetes Mellitus, Adult-Onset [description not available]	2.61	2	0
Diabetes Mellitus, Type 2 A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.	2.61	2	0
Age-Related Osteoporosis [description not available]	2.49	2	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.	2.49	2	0
Innate Inflammatory Response [description not available]	2.04	1	0
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	2.04	1	0
Kidney Diseases Pathological processes of the KIDNEY or its component tissues.	2.04	1	0

pamapimod

Description

Cross-References

Synonyms (47)

Research Excerpts

Overview

Toxicity

Roles (2)

Drug Classes (7)

Protein Targets (19)

Inhibition Measurements

Activation Measurements

Biological Processes (229)

Molecular Functions (68)

Ceullar Components (35)

Bioassays (93)

Research

Studies (11)

Market Indicators

Research Demand Index: 22.32

Study Types

pamapimod

Description

Cross-References

Synonyms (47)

Research Excerpts

Overview

Toxicity

Roles (2)

Drug Classes (7)

Protein Targets (19)

Inhibition Measurements

Activation Measurements

Biological Processes (229)

Molecular Functions (68)

Ceullar Components (35)

Bioassays (93)

Research

Studies (11)

Market Indicators

Research Demand Index: 22.32

Study Types

Related Drugs (12)

Related Conditions (15)