ID Source | ID |
---|---|
PubMed CID | 176155 |
CHEMBL ID | 10 |
CHEBI ID | 90705 |
SCHEMBL ID | 95208 |
MeSH ID | M0246906 |
Synonym |
---|
CBIOL_001970 |
K00038 |
4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)1h-imidazole |
HY-10256 |
adezmapimod |
HMS3267B07 |
BRD-A37704979-001-02-4 |
pyridine, 4-[5-(4-fluorophenyl)-2-[4-(methylsulfinyl)phenyl]-1h-imidazol-yl]- & z-100 |
sb 203580 & z-100 |
BIO1_000256 |
NCGC00025035-02 |
tocris-1402 |
BIO1_000745 |
NCGC00025035-01 |
tocris-1202 |
BIO1_001234 |
BSPBIO_001104 |
sb 203580 , |
sb203580 |
152121-47-6 |
pyridine, 4-[5-(4-fluorophenyl)-2-[4-(methylsulfinyl)phenyl]-1h-imidazol-yl]- |
4-[4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-1h-imidazol-5-yl]pyridine |
4-[5-(4-fluoro-phenyl)-2-(4-methanesulfinyl-phenyl)-3h-imidazol-4-yl]-pyridine |
sb 203580, solid, >=98% (hplc) |
4-[5-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-3h-imidazol-4-yl]pyridine |
1PME |
NCGC00025035-03 |
pyridine, 4-(5-(4-fluorophenyl)-2-(4-(methylsulfinyl)phenyl)-1h-imidazol-4-yl)- |
NCGC00025035-04 |
4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)-1h-imidazole |
4-[5-(4-fluorophenyl)-2-[4-(methylsulfonyl)phenyl]-1h-imidazol-4-yl]pyridine |
4-[4-(4-fluorophenyl)-2-(4-methanesulfinylphenyl)-1h-imidazol-5-yl]pyridine |
bdbm13336 |
cid_176155 |
4-{4-(4-fluorophenyl)-2-[4-(methylsulfinyl)phenyl]-1h-imidazol-5-yl}pyridine |
sb-203580 , |
chembl10 , |
HMS1990H05 |
chebi:90705 , |
AKOS005145971 |
HMS3229O04 |
HMS1792H05 |
EC-000.2318 |
KINOME_2521 |
4-(4-(4-fluorophenyl)-2-(4-(methylsulfinyl)phenyl)-1h-imidazol-5-yl)pyridine |
NCGC00025035-05 |
unii-ou13v1eywq |
ou13v1eywq , |
rwj 64809 |
4-(4-fluorophenyl)-2-[4-(methylsulfinyl)phenyl]-5-(4-pyridyl)-1h-imidazole |
4-(4-fluorophenyl)-2-[4-(methylsulfinyl)phenyl]-5-(4-pyridyl)-1h-imidazole;sb-203580 |
AKOS015994568 |
pb 203580 |
FT-0674525 |
HMS3244I16 |
HMS3244I15 |
HMS3244J15 |
BCPP000074 |
sb203580,rwj 64809,pb 203580 |
4-(5-(4-fluorophenyl)-2-(4-(methylsulfinyl)phenyl)-1h-imidazol-4-yl)pyridine |
CS-0140 |
S1076 |
c21h16fn3os |
gtpl5269 |
CCG-206878 |
SCHEMBL95208 |
CDMGBJANTYXAIV-UHFFFAOYSA-N |
MLS006010840 |
smr004701767 |
pyridine, 4-[4-(4-fluorophenyl)-2-[4-(methylsulfinyl)phenyl]-1h-imidazol-5-yl]- |
AM81234 |
ES-0013 |
pb-203580 |
rac-4-(5-(4-fluorophenyl)-2-(4-((r)- methanesulfinyl)phenyl)-1h-imidazol-4-yl)pyridine |
adezmapimod [inn] |
rwj-64809 |
birb203580 |
pyridine, 4-(4-(4-fluorophenyl)-2-(4-(methylsulfinyl)phenyl)-1h-imidazol-5-yl)- |
pb203580 |
rwj64809 |
birb-203580 |
HB1302 |
HMS3403H05 |
4-{4-(4-fluorophenyl)-2-[4-(methanesulfinyl)phenyl]-1h-imidazol-5-yl}pyridine |
bdbm192501 |
us9187470, 104 (sb203580) |
DTXSID2040577 |
mfcd00922198 |
bdbm50045333 |
J-513573 |
EX-A134 |
sr-01000597367 |
SR-01000597367-1 |
HMS3654M15 |
AC-32046 |
J-008891 |
NCGC00381704-12 |
SW218141-2 |
4-(4-(4-fluorophenyl)-2-(4-(methylsulfinyl)-phenyl)-1h-imidazol-5-yl)pyridine |
sb 203580 - cas 152121-47-6 |
F17411 |
HMS3676M17 |
BCP01763 |
HMS3412M17 |
Q7389023 |
BRD-A37704979-003-01-2 |
SB16633 |
HMS3295M11 |
nsc-755772 |
nsc755772 |
4-[5-(4-fluorophenyl)-2-[4-(methylsulfinyl)phenyl]-1h-imidazol-4-yl]pyridine |
F0864 |
SB 203580 is a pyridinyl imidazole compound which inhibits the release of pro-inflammatory cytokines, such as tumour necrosis factor-alpha (TNF-alpha) and interleukin-1 beta (IL-1beta) It is under intense study as a lead compound for developing novel anti-inflammatory agents.
Excerpt | Reference | Relevance |
---|---|---|
"SB 203580 is a highly selective inhibitor of p38MAPK in vitro and is under intense study as a lead compound for developing novel anti-inflammatory agents." | ( Activation of p90RSK and cAMP response element binding protein in stimulated neutrophils: novel effects of the pyridinyl imidazole SB 203580 on activation of the extracellular signal-regulated kinase cascade. Badwey, JA; Huang, R; Lian, JP; Robinson, D, 1999) | 1.23 |
"SB 203580 is a pyridinyl imidazole compound which inhibits the release of pro-inflammatory cytokines, such as tumour necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta), in vitro and in vivo by inhibiting p38 mitogen-activated protein kinase (MAPK). " | ( Effect of the p38 kinase inhibitor, SB 203580, on sephadex induced airway inflammation in the rat. Belvisi, MG; Birrell, M; Foster, M; Hele, D; McCluskie, K; Webber, S, 2000) | 2.02 |
SB 203580 has been widely used to specifically shut down the p38 MAP kinase-dependent pathway, although it is capable of inducing c-Raf kinase activity in cells. It has no inhibitory effects on the activity of coenzyme A-independent transacylase.
Excerpt | Reference | Relevance |
---|---|---|
"SB 203580 has been widely used to specifically shut down the p38 MAP kinase-dependent pathway, although it is capable of inducing c-Raf kinase activity in cells. " | ( Regulation of ERK-mediated signal transduction by p38 MAP kinase in human monocytic THP-1 cells. Izuno, M; Kurosawa, M; Nishimura, S; Numazawa, S; Watabe, M; Yoshida, T, 2003) | 1.76 |
"SB 203580 or PD 98059 has no inhibitory effects on the activity of coenzyme A-independent transacylase." | ( Phosphorylation of cytosolic phospholipase A2 and the release of arachidonic acid in human neutrophils. Hajjar, JJ; Molski, TF; Nagarkatti, D; Sha'afi, RI; Syrbu, SI; Waterman, WH, 1999) | 1.02 |
SB 203580 did not inhibit iNOS activity, as measured by the conversion of arginine to citrulline, when added directly to cultures where the enzyme had already been induced. It prevented the increase in collagenase-1 and stromelysin-1 mRNA stimulated by IL-1.
Treatment with SB 203580, a p38 MAPK inhibitor, reduced intestinal apoptosis (26.72+/-3.39% vs 62.50+/+3.08% in I/R vehicle, P<0.01) and decreased plasma D-lactate level. Light had no effect on the circadian oscillator in the presence of 100 microm SB 20 3580.
Excerpt | Reference | Relevance |
---|---|---|
" In the absence of inhibitors, JP-8 and to a lesser extent un and S-8, had the greatest toxic effect on cell viability and inflammation suggesting, as least in vitro, that synthetic S-8 fuel is less irritating than the currently used JP-8." | ( Inhibition of jet fuel aliphatic hydrocarbon induced toxicity in human epidermal keratinocytes. Inman, AO; Monteiro-Riviere, NA; Riviere, JE, 2008) | 0.35 |
" We investigated the hypotheses that these drugs (A) are less neurotoxic than the prototype local anesthetic, lidocaine (B) are selectively toxic for subcategories of dorsal root ganglion neurons and (C) induce activation of either p38 MAPK or related enzymes, such as the c-jun terminal N-kinase (JNK) and extracellular signal-regulated kinase (ERK)." | ( In vitro, inhibition of mitogen-activated protein kinase pathways protects against bupivacaine- and ropivacaine-induced neurotoxicity. Colvin, HP; Gerner, P; Haller, I; Klimaschewski, L; Lang, L; Lirk, P; Tomaselli, B, 2008) | 0.35 |
"The developing brain is very sensitive to damage by toxic agents, many of which only manifest in adulthood." | ( Neurotoxicity of cadmium on immature hippocampus and a neuroprotective role for p38 MAPK. Cordova, FM; Costa, AP; Leal, RB; Oliveira, CS; Posser, T; Rigon, AP; Rocha, JB; Rossi, FM; Santos, DA; Silva, IG, 2008) | 0.35 |
" In conclusion, deferoxamine is directly toxic on RPE cells, its toxicity depending on p38." | ( Deferoxamine mesylate is toxic for retinal pigment epithelium cells in vitro, and its toxicity is mediated by p38. Herdegen, T; Klettner, A; Koinzer, S; Roider, J; Waetzig, V, 2010) | 0.36 |
" In the mechanistic differentiation studies, p38 inhibitors displayed an increase in pJNK and caspase-3 activity in U937 cells and elevation in aspartate transaminase enzyme in HepG2 cells, whereas MK2 inhibitor did not show such adverse toxic effects." | ( Differential effect of p38 and MK2 kinase inhibitors on the inflammatory and toxicity biomarkers in vitro. Dastidar, SG; Diwan, M; Najmi, AK; Singh, RK, 2018) | 0.48 |
Excerpt | Reference | Relevance |
---|---|---|
"The addition of all-trans retinoic acid (ATRA) in combination with basic fibroblast growth factor (bFGF) to human fibroblasts results in a synergistic induction of tissue inhibitor of metalloproteinases-1 (TIMP-1) protein production." | ( Mechanisms of induction of human tissue inhibitor of metalloproteinases-1 (TIMP-1) gene expression by all-trans retinoic acid in combination with basic fibroblast growth factor. Bigg, HF; Cawston, TE; Clark, IM; McLeod, R; Waters, JG, 2000) | 0.31 |
" Agonist levels, which by themselves induced little or reversible aggregation, caused strong stable aggregation when combined with low levels of HOCl-LDL." | ( LDL oxidized by hypochlorous acid causes irreversible platelet aggregation when combined with low levels of ADP, thrombin, epinephrine, or macrophage-derived chemokine (CCL22). Coleman, LG; Gear, AR; Marcinkiewicz, M; Polanowska-Grabowska, RK, 2004) | 0.32 |
"The aim of the present study was to determine the effects of metformin, combined with a p38 mitogen‑activated protein kinase (MAPK) inhibitor, on the sensitivity of cisplatin‑resistant ovarian cancer to cisplatin." | ( Metformin combined with p38 MAPK inhibitor improves cisplatin sensitivity in cisplatin‑resistant ovarian cancer. Guo, H; Ji, M; Peng, Z; Shi, H; Shi, M; Xie, Y, 2014) | 0.4 |
" However, a PPARα-agonist (WY14643) failed to regulate the expression of the uncoupling protein 1(UCP1) gene unless combined with retinoic acid." | ( WY14643 combined with all-trans retinoic acid acts via p38 MAPK to induce "browning" of white adipocytes in mice. Cui, Y; Ding, J; Li, HR; Sun, GJ; Wang, J; Wang, SJ; Zhang, JX, 2015) | 0.42 |
"To investigate the molecular mechanisms of continuous venovenous hemofiltration (CVVH) combined with ulinastatin (ULI) (CVVH-ULI) for the treatment of septic shock." | ( [Mechanism of continuous venovenous hemofiltration combined with ulinastatin for the treatment of septic shock]. Guo, X; Liu, Y; Su, L; Wang, Z; Wu, F; Xu, Q, 2015) | 0.42 |
"Human umbilical endothelial cells (HUVECs) were incubated with serums isolated from normal healthy people (control), septic shock patients treated with conventional therapy (CT) or treated with CVVH combined with ULI (CVVH-ULI)." | ( [Mechanism of continuous venovenous hemofiltration combined with ulinastatin for the treatment of septic shock]. Guo, X; Liu, Y; Su, L; Wang, Z; Wu, F; Xu, Q, 2015) | 0.42 |
"CVVH combined with ulinastatin decreases endothelial hyperpermeability induced by septic shock through inhibiting p38 MAPK pathways." | ( [Mechanism of continuous venovenous hemofiltration combined with ulinastatin for the treatment of septic shock]. Guo, X; Liu, Y; Su, L; Wang, Z; Wu, F; Xu, Q, 2015) | 0.42 |
"Inhibitors of p38 (SB203580) and of signal transducer and activator of transcription 3 (stattic) were employed in combination with cisplatin in ovarian carcinoma cell lines." | ( AXL Downstream Targeting Unravels Synergistic Drug Combinations in Ovarian Carcinoma Cells. Alampi, DM; Carenini, N; Ciusani, E; Corna, E; Corno, C; Gatti, L, 2019) | 0.51 |
"SB203580 produced a synergistic effect in combination with cisplatin in cisplatin-resistant IGROV-1/Pt1 cells." | ( AXL Downstream Targeting Unravels Synergistic Drug Combinations in Ovarian Carcinoma Cells. Alampi, DM; Carenini, N; Ciusani, E; Corna, E; Corno, C; Gatti, L, 2019) | 0.51 |
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). |
Hsp90 inhibitor | An EC 3.6.4.10 (non-chaperonin molecular chaperone ATPase) inhibitor that blocks the action of heat shock protein 90. |
neuroprotective agent | Any compound that can be used for the treatment of neurodegenerative disorders. |
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | An EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of non-specific serine/threonine protein kinase (EC 2.7.11.1), a kinase enzyme involved in phosphorylation of hydroxy group of serine or threonine. |
geroprotector | Any compound that supports healthy aging, slows the biological aging process, or extends lifespan. |
[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 |
---|---|
imidazoles | A five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton. |
monofluorobenzenes | Any member of the class of fluorobenzenes containing a mono- or poly-substituted benzene ring carrying a single fluorine substitutent. |
pyridines | Any organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives. |
sulfoxide | An organosulfur compound having the structure R2S=O or R2C=S=O (R =/= H). |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 26.2000 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
Chain A, HADH2 protein | Homo sapiens (human) | Potency | 32.7992 | 0.0251 | 20.2376 | 39.8107 | AID886; AID893 |
Chain B, HADH2 protein | Homo sapiens (human) | Potency | 32.7992 | 0.0251 | 20.2376 | 39.8107 | AID886; AID893 |
Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 30.3001 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
15-lipoxygenase, partial | Homo sapiens (human) | Potency | 19.9526 | 0.0126 | 10.6917 | 88.5700 | AID887 |
Fumarate hydratase | Homo sapiens (human) | Potency | 67.9245 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
USP1 protein, partial | Homo sapiens (human) | Potency | 56.2341 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
PPM1D protein | Homo sapiens (human) | Potency | 7.3876 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
TDP1 protein | Homo sapiens (human) | Potency | 26.1056 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 30.6163 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 39.8107 | 0.0013 | 18.0743 | 39.8107 | AID926; AID938 |
regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 2.9935 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 0.5355 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
EWS/FLI fusion protein | Homo sapiens (human) | Potency | 44.3070 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
G | Vesicular stomatitis virus | Potency | 0.9522 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 6.7412 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
polyprotein | Zika virus | Potency | 67.9245 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 0.0020 | 7.5337 | 39.8107 | AID891 |
cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 0.0398 | 0.0025 | 5.8400 | 31.6228 | AID899 |
cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 1.9953 | 0.0063 | 6.9043 | 39.8107 | AID883 |
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 28.3709 | 0.0018 | 15.6638 | 39.8107 | AID894 |
vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 70.7946 | 0.3548 | 28.0659 | 89.1251 | AID504847 |
mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 18.8541 | 0.0398 | 16.7842 | 39.8107 | AID995 |
tyrosine-protein kinase Yes | Homo sapiens (human) | Potency | 10.9096 | 0.0000 | 5.0182 | 79.2586 | AID686947 |
DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 7.9433 | 0.0316 | 22.3146 | 100.0000 | AID588579 |
cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 0.8801 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 22.1061 | 0.0200 | 10.7869 | 31.6228 | AID912 |
Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 25.1189 | 0.3162 | 12.7657 | 31.6228 | AID881 |
Interferon beta | Homo sapiens (human) | Potency | 5.7787 | 0.0033 | 9.1582 | 39.8107 | AID1347411; AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 0.9522 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 11.2447 | 0.0063 | 8.2350 | 39.8107 | AID881; AID883 |
Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 0.9522 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 0.8801 | 1.0000 | 12.2248 | 31.6228 | AID885 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 0.9522 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, Erk2 | Homo sapiens (human) | Ki | 0.0004 | 0.0004 | 0.0004 | 0.0004 | AID977610 |
Citron Rho-interacting kinase | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.4580 | 0.8327 | 1.0400 | AID1646091 |
Cyclin-G-associated kinase | Homo sapiens (human) | IC50 (µMol) | 0.4133 | 0.0010 | 0.2972 | 1.1000 | AID1205969; AID1646094; AID242126 |
Mitogen-activated protein kinase 13 | Homo sapiens (human) | IC50 (µMol) | 0.2329 | 0.0007 | 0.4595 | 6.3000 | AID126948; AID127070; AID127071; AID127095; AID127097; AID127099; AID127105; AID127243; AID1444580; AID152778; AID152779; AID1638931; AID1876163; AID215099; AID216427; AID216428; AID222608; AID268710; AID286352; AID46887; AID90808 |
Mitogen-activated protein kinase 2 | Pneumocystis carinii | IC50 (µMol) | 0.1050 | 0.1050 | 0.1050 | 0.1050 | AID1876034 |
Receptor-interacting serine/threonine-protein kinase 2 | Homo sapiens (human) | IC50 (µMol) | 1.0359 | 0.0010 | 4.6143 | 100.0000 | AID1253622; AID1253623; AID1309961; AID1309962; AID1309963; AID1646096; AID242591 |
cGMP-specific 3',5'-cyclic phosphodiesterase | Homo sapiens (human) | IC50 (µMol) | 11.4760 | 0.0000 | 1.1843 | 9.6140 | AID625167 |
Serine/threonine-protein kinase D3 | Homo sapiens (human) | IC50 (µMol) | 75.0000 | 0.0001 | 1.1701 | 10.0000 | AID165149 |
Epidermal growth factor receptor | Homo sapiens (human) | IC50 (µMol) | 64.5000 | 0.0000 | 0.5369 | 10.0000 | AID241905; AID67274 |
RAF proto-oncogene serine/threonine-protein kinase | Homo sapiens (human) | IC50 (µMol) | 0.7575 | 0.0010 | 0.3349 | 8.9000 | AID166072; AID219504; AID241699; AID322453 |
Receptor tyrosine-protein kinase erbB-2 | Homo sapiens (human) | IC50 (µMol) | 18.8960 | 0.0001 | 0.5453 | 10.0000 | AID625186 |
Protein kinase C gamma type | Homo sapiens (human) | IC50 (µMol) | 75.0000 | 0.0001 | 1.0354 | 10.0000 | AID165149 |
Myeloperoxidase | Homo sapiens (human) | Ki | 0.0900 | 0.0019 | 0.1360 | 0.3162 | AID315938 |
Cytochrome P450 1A2 | Homo sapiens (human) | IC50 (µMol) | 2.0000 | 0.0001 | 1.7740 | 10.0000 | AID625245 |
Protein kinase C beta type | Homo sapiens (human) | IC50 (µMol) | 75.0000 | 0.0001 | 0.5542 | 10.0000 | AID165149 |
Tyrosine-protein kinase Lck | Homo sapiens (human) | IC50 (µMol) | 3.4500 | 0.0002 | 1.3173 | 10.0000 | AID224147 |
Neutrophil elastase | Homo sapiens (human) | IC50 (µMol) | 0.0250 | 0.0063 | 2.0734 | 22.3780 | AID222608 |
Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 0.0620 | 0.0001 | 1.7536 | 10.0000 | AID339980 |
Neuronal acetylcholine receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Ki | 0.0900 | 0.0000 | 0.1234 | 5.5000 | AID315938 |
Cytochrome P450 2D6 | Homo sapiens (human) | IC50 (µMol) | 2.0000 | 0.0000 | 2.0151 | 10.0000 | AID625249 |
Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | IC50 (µMol) | 10.6660 | 0.0000 | 1.4039 | 10.0000 | AID625151 |
Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | Ki | 2.5690 | 0.0000 | 0.5972 | 9.1201 | AID625151 |
Tyrosinase | Mus musculus (house mouse) | IC50 (µMol) | 0.0340 | 0.0300 | 2.2104 | 5.2300 | AID1611955 |
Cholesteryl ester transfer protein | Homo sapiens (human) | IC50 (µMol) | 0.0400 | 0.0030 | 0.2169 | 4.1000 | AID691521 |
Cytochrome P450 2C9 | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0000 | 2.8005 | 10.0000 | AID625248 |
Neuronal acetylcholine receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Ki | 0.0900 | 0.0000 | 0.1082 | 5.5000 | AID315938 |
Proto-oncogene tyrosine-protein kinase Src | Homo sapiens (human) | IC50 (µMol) | 5.0000 | 0.0002 | 0.5335 | 10.0000 | AID242316 |
Serine/threonine-protein kinase B-raf | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0001 | 0.2800 | 7.5890 | AID1646090 |
Protein kinase C alpha type | Homo sapiens (human) | IC50 (µMol) | 75.0000 | 0.0001 | 0.9720 | 10.0000 | AID165149 |
cAMP-dependent protein kinase catalytic subunit alpha | Homo sapiens (human) | IC50 (µMol) | 50.0000 | 0.0009 | 1.3241 | 9.0000 | AID164653 |
Amine oxidase [flavin-containing] B | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.3600 | 0.0004 | 0.7649 | 12.5000 | AID126948 |
cAMP-dependent protein kinase catalytic subunit gamma | Homo sapiens (human) | IC50 (µMol) | 50.0000 | 0.0009 | 1.5482 | 9.0000 | AID164653 |
cAMP-dependent protein kinase catalytic subunit beta | Homo sapiens (human) | IC50 (µMol) | 50.0000 | 0.0006 | 1.4848 | 9.0000 | AID164653 |
Prostaglandin G/H synthase 1 | Homo sapiens (human) | IC50 (µMol) | 3.5000 | 0.0002 | 1.5574 | 10.0000 | AID162316; AID162317 |
Thromboxane-A synthase | Homo sapiens (human) | IC50 (µMol) | 0.4940 | 0.0009 | 1.2304 | 10.0000 | AID625229 |
Protein kinase C eta type | Homo sapiens (human) | IC50 (µMol) | 75.0000 | 0.0001 | 0.7971 | 10.0000 | AID165149 |
Adenosine receptor A2a | Homo sapiens (human) | IC50 (µMol) | 6.0680 | 0.0007 | 1.5594 | 10.0000 | AID625195 |
Adenosine receptor A2a | Homo sapiens (human) | Ki | 3.4070 | 0.0000 | 1.0609 | 9.7920 | AID625195 |
Ephrin type-B receptor 2 | Homo sapiens (human) | IC50 (µMol) | 7.8000 | 0.0025 | 1.5875 | 8.5000 | AID240825 |
Adenosine receptor A1 | Homo sapiens (human) | IC50 (µMol) | 2.9500 | 0.0002 | 0.6818 | 7.7010 | AID625194 |
Adenosine receptor A1 | Homo sapiens (human) | Ki | 1.7210 | 0.0002 | 0.9316 | 10.0000 | AID625194 |
Sodium-dependent serotonin transporter | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0100 | 0.0003 | 0.8197 | 8.4900 | AID241741 |
Delta-type opioid receptor | Mus musculus (house mouse) | IC50 (µMol) | 0.0200 | 0.0001 | 0.7298 | 10.0000 | AID241747 |
Cytochrome P450 2C19 | Homo sapiens (human) | IC50 (µMol) | 0.8000 | 0.0000 | 2.3983 | 10.0000 | AID625247 |
Dual specificity mitogen-activated protein kinase kinase 2 | Homo sapiens (human) | IC50 (µMol) | 61.0000 | 0.0002 | 0.4653 | 9.7000 | AID126779 |
TGF-beta receptor type-1 | Homo sapiens (human) | IC50 (µMol) | 18.0000 | 0.0010 | 0.6436 | 10.0000 | AID210783; AID30869 |
Protein kinase C iota type | Homo sapiens (human) | IC50 (µMol) | 75.0000 | 0.0001 | 2.0378 | 10.0000 | AID165149 |
Mitogen-activated protein kinase 9 | Homo sapiens (human) | IC50 (µMol) | 2.3871 | 0.0050 | 0.7475 | 5.2000 | AID1646075; AID219483; AID219488; AID219491; AID219492; AID242421; AID468035 |
Mitogen-activated protein kinase 14 | Mus musculus (house mouse) | IC50 (µMol) | 0.0560 | 0.0008 | 0.2416 | 1.5000 | AID1797365 |
Casein kinase I isoform delta | Homo sapiens (human) | IC50 (µMol) | 0.4147 | 0.0040 | 1.1272 | 10.0000 | AID1645936; AID242035; AID448706 |
Casein kinase I isoform epsilon | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0040 | 1.1150 | 9.5000 | AID1646092 |
Mitogen-activated protein kinase 12 | Homo sapiens (human) | IC50 (µMol) | 0.2329 | 0.0007 | 0.4728 | 6.3000 | AID126948; AID127070; AID127071; AID127095; AID127097; AID127099; AID127105; AID127243; AID1444580; AID152778; AID152779; AID1638931; AID1876163; AID215099; AID216427; AID216428; AID222608; AID268710; AID286352; AID46887; AID90808 |
Mitogen-activated protein kinase 10 | Homo sapiens (human) | IC50 (µMol) | 0.6933 | 0.0020 | 1.7035 | 10.0000 | AID1646076; AID280498; AID444254 |
Mitogen-activated protein kinase 10 | Homo sapiens (human) | Ki | 0.0900 | 0.0900 | 0.5767 | 1.4000 | AID315938 |
Mitogen-activated protein kinase 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 500.0240 | 0.0020 | 0.0818 | 0.2200 | AID1797364 |
Protein kinase C epsilon type | Homo sapiens (human) | IC50 (µMol) | 75.0000 | 0.0001 | 0.8029 | 10.0000 | AID165149 |
Dual specificity mitogen-activated protein kinase kinase 1 | Homo sapiens (human) | IC50 (µMol) | 61.0000 | 0.0002 | 0.6813 | 9.7000 | AID126779 |
Angiopoietin-1 receptor | Homo sapiens (human) | IC50 (µMol) | 20.0000 | 0.0004 | 0.5553 | 9.0700 | AID300639 |
Protein kinase C theta type | Homo sapiens (human) | IC50 (µMol) | 75.0000 | 0.0001 | 0.9897 | 10.0000 | AID165149 |
Protein kinase C zeta type | Homo sapiens (human) | IC50 (µMol) | 75.0000 | 0.0001 | 2.4453 | 10.0000 | AID165149 |
Protein kinase C delta type | Homo sapiens (human) | IC50 (µMol) | 75.0000 | 0.0001 | 0.8448 | 10.0000 | AID165149 |
Myotonin-protein kinase | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.1050 | 0.4490 | 1.0000 | AID1646093 |
Serine/threonine-protein kinase D1 | Homo sapiens (human) | IC50 (µMol) | 75.0000 | 0.0001 | 1.2319 | 10.0000 | AID165149 |
Mitogen-activated protein kinase 11 | Homo sapiens (human) | IC50 (µMol) | 0.2646 | 0.0007 | 0.4754 | 6.3000 | AID126948; AID127070; AID127071; AID127095; AID127097; AID127099; AID127105; AID127243; AID127420; AID1337161; AID1444580; AID152778; AID152779; AID1638931; AID1645935; AID1876163; AID215099; AID216427; AID216428; AID222608; AID242384; AID268710; AID286352; AID46887; AID660758; AID90808 |
Mitogen-activated protein kinase 14 | Homo sapiens (human) | IC50 (µMol) | 15.3271 | 0.0001 | 0.7266 | 7.8000 | AID1053969; AID1053973; AID1071889; AID126603; AID126948; AID127070; AID127071; AID127085; AID127095; AID127097; AID127099; AID127105; AID127243; AID127255; AID127272; AID127407; AID127410; AID127411; AID127412; AID1337160; AID1444580; AID152778; AID152779; AID1540338; AID1596951; AID1597029; AID1638931; AID1732391; AID1797017; AID1797364; AID1797386; AID1799909; AID1876163; AID1876281; AID215099; AID216427; AID216428; AID222608; AID240921; AID241346; AID241741; AID241747; AID241943; AID242399; AID257469; AID268710; AID275050; AID280500; AID281717; AID286352; AID322018; AID322019; AID329649; AID339980; AID395288; AID428917; AID448705; AID462319; AID468034; AID46887; AID476334; AID492799; AID495020; AID495022; AID607540; AID625182; AID660757; AID691521; AID706189; AID721301; AID721302; AID749361; AID90808 |
Mitogen-activated protein kinase 14 | Homo sapiens (human) | Ki | 0.0375 | 0.0001 | 0.0749 | 0.3100 | AID315936; AID516347 |
P2X purinoceptor 7 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 30.0000 | 0.0047 | 0.4321 | 1.9000 | AID1238355 |
P2X purinoceptor 7 | Homo sapiens (human) | IC50 (µMol) | 5.0000 | 0.0008 | 0.2452 | 5.0000 | AID1238354 |
Serine/threonine-protein kinase 36 | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 1.0000 | 1.0000 | 1.0000 | AID1646097 |
Serine/threonine-protein kinase NLK | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0555 | 0.3778 | 1.0000 | AID1646095 |
TRAF2 and NCK-interacting protein kinase | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0003 | 0.2924 | 1.0000 | AID1646086 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID435854 | Percentage IKK-beta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID624924 | Binding constant for RIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625027 | Binding constant for MAP3K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720233 | Millipore: Percentage of residual kinase activity of PRKX at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID219488 | Inhibition of c-Jun N-terminal kinase 2-alpha 2 | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase. |
AID625094 | Binding constant for CDK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435904 | Binding constant for full-length CSK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID436037 | Percentage MAPKAPK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID624818 | Binding constant for ULK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625010 | Binding constant for FER kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID503307 | Antiproliferative activity against human PC3 cells at 25 uM after 120 hrs by MTT assay relative to DMSO | 2006 | Nature chemical biology, Jun, Volume: 2, Issue:6 | Identifying off-target effects and hidden phenotypes of drugs in human cells. |
AID256590 | Average Binding Constant for EPHB1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID127407 | In vitro inhibition of mitogen-activated protein kinase p38 alpha 2 derived from Escherichia coli | 2001 | Bioorganic & medicinal chemistry letters, Jan-08, Volume: 11, Issue:1 | p38 kinase inhibitors for the treatment of arthritis and osteoporosis: thienyl, furyl, and pyrrolyl ureas. |
AID256609 | Average Binding Constant for AAK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624772 | Binding constant for AURKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID767909 | Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced IL-6 production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA | 2013 | Journal of natural products, Sep-27, Volume: 76, Issue:9 | Anti-inflammatory asterosaponins from the starfish Astropecten monacanthus. |
AID256658 | Average Binding Constant for p38-beta; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID256610 | Average Binding Constant for Aurora3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624878 | Binding constant for PIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624992 | Binding constant for ABL1-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720069 | Millipore: Percentage of residual kinase activity of CDK7 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720157 | Millipore: Percentage of residual kinase activity of FER at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224770 | Delta TM value showing the stabilisation of JAK1~B produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624745 | Binding constant for PKN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720299 | Millipore: Percentage of residual kinase activity of CHUK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435197 | Binding constant for TEC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625073 | Binding constant for SGK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720158 | Millipore: Percentage of residual kinase activity of FER at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID30869 | Inhibition of Activin like receptor kinase 5, TGF beta type I receptor | 2002 | Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5 | Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5). |
AID435203 | Binding constant for TTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720116 | Millipore: Percentage of residual kinase activity of DMPK at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256602 | Average Binding Constant for EPHA2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720104 | Millipore: Percentage of residual kinase activity of CAMK4 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 40 mM HEPES pH 7.4, 5 mM CaCl2, 30 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720480 | Millipore: Percentage of residual kinase activity of PRKCD at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435827 | Binding constant for PDGFRA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256568 | Average Binding Constant for STK17A; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720437 | Millipore: Percentage of residual kinase activity of RPS6KB1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624832 | Binding constant for IKK-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435440 | Binding constant for PIM2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435826 | Binding constant for full-length PCTK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID75811 | Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the human glucagon receptor (hGLUR) expressed on CHO cells in absence of Mg+2 at 2 uM | 1999 | Bioorganic & medicinal chemistry letters, Mar-08, Volume: 9, Issue:5 | Potent, orally absorbed glucagon receptor antagonists. |
AID624991 | Binding constant for ABL1-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224756 | Delta TM value showing the stabilisation of CAMKK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID256670 | Average Binding Constant for ABL1(T315I); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435902 | Binding constant for BRAF(V600E) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625070 | Binding constant for PFTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720413 | Millipore: Percentage of residual kinase activity of VRK2 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720067 | Millipore: Percentage of residual kinase activity of CDK6 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435665 | Binding constant for NEK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID107309 | Effect in murine model of arthritis onset in mice immunized with bovine type II collagen at 50 mg/kg; Number of paws affected | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor. |
AID435718 | Percentage EF2K activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720272 | Millipore: Percentage of residual kinase activity of SIK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624862 | Binding constant for LYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436009 | Binding constant for full-length CAMK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1309961 | Competitive inhibition of full length FLAG-His-tagged RIP2K (unknown origin) expressed in baculovirus expression system preincubated for 10 mins followed by addition of fluorescent-labeled 2-Methyl-5-(2-propen-l-yloxy)aniline measured after 10 mins by flu | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase. |
AID624863 | Binding constant for MARK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435847 | Percentage DYRK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720477 | Millipore: Percentage of residual kinase activity of PRKCB at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720239 | Millipore: Percentage of residual kinase activity of ROCK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID241451 | Inhibition of mitogen-activated protein kinase p38 alpha | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2 | Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation. |
AID435541 | Percentage PKA activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID1645935 | Inhibition of human p38beta | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
AID720057 | Millipore: Percentage of residual kinase activity of CDK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224755 | Delta TM value showing the stabilisation of CAMK4 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1224783 | Delta TM value showing the stabilisation of PAK6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624803 | Binding constant for CHEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625011 | Binding constant for FGR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435156 | Binding constant for EGFR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID761959 | Antiinflammatory activity in human HL-60 derived macrophage-like cells assessed as inhibition of LPS-induced TNFalpha production treated 30 mins before LPS stimulation measured after 24 hrs by ELISA | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | First synthesis and biological evaluation of 4-amino-2-aryl-6,9-dichlorobenzo[g]pteridines as inhibitors of TNF-α and IL-6. |
AID256623 | Average Binding Constant for MYLK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720199 | Millipore: Percentage of residual kinase activity of PRKCZ at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720333 | Millipore: Percentage of residual kinase activity of LCK at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625136 | Binding constant for YSK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625046 | Binding constant for PIK3CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID660758 | Inhibition of p38beta kinase | 2011 | ACS medicinal chemistry letters, Oct-13, Volume: 2, Issue:10 | The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor. |
AID625055 | Binding constant for MST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720289 | Millipore: Percentage of residual kinase activity of TAOK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435176 | Percentage PIM2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID242384 | Inhibition of Mitogen-activated protein kinase 11 (P38 beta) at 100 uM ATP | 2005 | Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12 | Rapid computational identification of the targets of protein kinase inhibitors. |
AID624893 | Binding constant for MEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625111 | Binding constant for RIOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID512267 | Inhibition of His-tagged human S6K1 expressed in Escherichia coli at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID286352 | Inhibition of mitogen-activated protein kinase p38 at 100 uM ATP | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9 | Synthesis, biological testing, and binding mode prediction of 6,9-diarylpurin-8-ones as p38 MAP kinase inhibitors. |
AID435662 | Binding constant for MST2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624861 | Binding constant for LIMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256572 | Average Binding Constant for STK36; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720096 | Millipore: Percentage of residual kinase activity of CAMK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720342 | Millipore: Percentage of residual kinase activity of MAPKAPK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Na-?-glycerophosphate pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435198 | Binding constant for TIE1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435276 | Binding constant for BMPR1A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256603 | Average Binding Constant for FER; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624990 | Binding constant for ABL1(Y253F)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435415 | Binding constant for MYLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435661 | Binding constant for full-length MKNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720120 | Millipore: Percentage of residual kinase activity of DYRK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256596 | Average Binding Constant for CLK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID495020 | Inhibition of p38 alpha activity by ELISA | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Optimization of alpha-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site. |
AID720443 | Millipore: Percentage of residual kinase activity of NLK at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720238 | Millipore: Percentage of residual kinase activity of ROCK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256578 | Average Binding Constant for SLK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID1646090 | Inhibition of human BRAF | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
AID256577 | Average Binding Constant for CLK4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID322019 | Inhibition of human p38-alpha kinase phosphorylation | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors. |
AID720314 | Millipore: Percentage of residual kinase activity of JAK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624736 | Binding constant for RPS6KA5(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435165 | Binding constant for JAK1(Kin.Dom.1/JH2 - pseudokinase) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435545 | Binding constant for NEK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720136 | Millipore: Percentage of residual kinase activity of EPHA8 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435319 | Binding constant for PKN1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624766 | Binding constant for p38-gamma kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624916 | Binding constant for ULK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435283 | Binding constant for DAPK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID339968 | Inhibition of human SAPK4/p38delta at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID435731 | Percentage MNK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID624876 | Binding constant for PDPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624747 | Binding constant for SgK110 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720323 | Millipore: Percentage of residual kinase activity of MAPK10 at 10uM relative to control. Control inhibitor: JAK Inhibitor I at 30.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720311 | Millipore: Percentage of residual kinase activity of INSRR at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624705 | Binding constant for MYLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1645936 | Inhibition of human CK1delta | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
AID624981 | Binding constant for ABL1(F317L)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720190 | Millipore: Percentage of residual kinase activity of HIPK3 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624781 | Binding constant for CDK4-cyclinD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1876035 | Antiviral activity against HCoV-229E assessed as reduction of viral RNA level at 4 uM relative control | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID435396 | Binding constant for CHEK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624966 | Binding constant for DCAMKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1646097 | Inhibition of human STK36 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
AID256627 | Average Binding Constant for RPS6KA2 (Kin.Dom. 1); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624903 | Binding constant for SRPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID339955 | Inhibition of human SAPK2b/p38--beta-2 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID720185 | Millipore: Percentage of residual kinase activity of HIPK1 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720301 | Millipore: Percentage of residual kinase activity of IKBKB at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435803 | Binding constant for full-length LIMK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435328 | Binding constant for YES kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1638931 | Inhibition of p38alpha MAPK (unknown origin) using ATF-2 as substrate after 1 hr by ELISA | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Design and molecular modeling of novel P38α MAPK inhibitors targeting breast cancer, synthesized from oxygen heterocyclic natural compounds. |
AID720386 | Millipore: Percentage of residual kinase activity of NEK11 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID436072 | Percentage CK1delta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID435659 | Binding constant for full-length MARK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720124 | Millipore: Percentage of residual kinase activity of EPHA1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1597029 | Inhibition of human recombinant p38alpha MAPK using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate measured after 30 mins by LANCE assay relative to control | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Pyridinylimidazoles as dual glycogen synthase kinase 3β/p38α mitogen-activated protein kinase inhibitors. |
AID435823 | Binding constant for full-length PAK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435694 | Binding constant for TNK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID241346 | Inhibition of human Mitogen-activated protein kinase p38 alpha | 2004 | Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19 | The development of new bicyclic pyrazole-based cytokine synthesis inhibitors. |
AID435652 | Binding constant for EGFR(L747-E749del, A750P) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624967 | Binding constant for RPS6KA5(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID54378 | Inhibition of Cytochrome P450 2C19 at 10 uM | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15 | Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. |
AID625106 | Binding constant for MARK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID512274 | Inhibition of His-tagged human CHK1 expressed in Escherichia coli at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID624920 | Binding constant for MRCKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624702 | Binding constant for BRSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436053 | Binding constant for full-length STK33 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435713 | Percentage CHK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720156 | Millipore: Percentage of residual kinase activity of FGFR4 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256664 | Average Binding Constant for EGFR; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624853 | Binding constant for FLT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720194 | Millipore: Percentage of residual kinase activity of HCK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624800 | Binding constant for IGF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435979 | Percentage MST2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID183405 | Inhibition of secondary paw swelling in rat adjuvant arthritis model at 80 mg/kg b.i.d. | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | Pyrroles and other heterocycles as inhibitors of p38 kinase. |
AID435320 | Binding constant for PRKCE kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624969 | Binding constant for ROCK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624777 | Binding constant for DDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1646095 | Inhibition of human NLK | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
AID624950 | Binding constant for DMPK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720429 | Millipore: Percentage of residual kinase activity of SRC at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624866 | Binding constant for MLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID242421 | Inhibition of human mitogen-activated protein kinase 9 (JNK 2) at 100 uM ATP | 2005 | Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12 | Rapid computational identification of the targets of protein kinase inhibitors. |
AID435842 | Percentage Aurora C activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720079 | Millipore: Percentage of residual kinase activity of CSNK1G2 at 1uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435995 | Percentage SRPK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID256666 | Average Binding Constant for ABL1(Q252H); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID625047 | Binding constant for AMPK-alpha2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624711 | Binding constant for STK35 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625022 | Binding constant for MUSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720474 | Millipore: Percentage of residual kinase activity of PRKCB at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624841 | Binding constant for BLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID222608 | Inhibition of TNF-alpha production by lipopolysaccharide-stimulated human peripheral blood mononuclear cells | 1998 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 8, Issue:23 | Potent inhibitors of the MAP kinase p38. |
AID435193 | Binding constant for RPS6KA6(Kin.Dom.1 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720131 | Millipore: Percentage of residual kinase activity of EPHA5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435182 | Binding constant for full-length PKAC-beta | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1238354 | Inhibition of human P2X7 receptor | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Docking of competitive inhibitors to the P2X7 receptor family reveals key differences responsible for changes in response between rat and human. |
AID625026 | Binding constant for MAP3K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624875 | Binding constant for PDGFRB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1309962 | Inhibition of RIP2K in MDP-stimulated HEK-293 cells over-expressing NOD2 assessed as IL8 secretion | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase. |
AID435291 | Binding constant for FGFR3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435123 | Percentage NEK7 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID435650 | Binding constant for full-length CSNK1E | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256621 | Average Binding Constant for CAMK2A; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435734 | Percentage NEK6 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID256674 | Average Binding Constant for PKMYT1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID625001 | Binding constant for EGFR(L747-S752del, P753S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624749 | Binding constant for CASK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720082 | Millipore: Percentage of residual kinase activity of CSNK1G3 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720211 | Millipore: Percentage of residual kinase activity of PRKG1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 uM cGMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720446 | Millipore: Percentage of residual kinase activity of PAK3 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625078 | Binding constant for SRPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720154 | Millipore: Percentage of residual kinase activity of FGFR3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625137 | Binding constant for MEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435941 | Binding constant for ZAK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID127268 | Kd value and murine Mitogen-activated protein kinase p38 alpha complex was calculated | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22 | Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). |
AID720426 | Millipore: Percentage of residual kinase activity of KIT at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435747 | Percentage PRAK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID256612 | Average Binding Constant for GAK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435418 | Percentage PAK5 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720339 | Millipore: Percentage of residual kinase activity of MAPK3 at 10uM relative to control. Control inhibitor: ERK Inhibitor II at 30.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224750 | Delta TM value showing the stabilisation of CAMK1G produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720436 | Millipore: Percentage of residual kinase activity of RPS6KB1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435517 | Binding constant for AKT2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID436025 | Binding constant for NDR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720347 | Millipore: Percentage of residual kinase activity of MARK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID516347 | Binding affinity to full-length GST-tagged p38alpha after 2.5 hrs by TR-FRET competition binding assay | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19 | Biochemical and biophysical characterization of unique switch pocket inhibitors of p38α. |
AID527953 | Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated IL12 production at 50 uM treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Lupane-type triterpenoids from the steamed leaves of Acanthopanax koreanum and their inhibitory effects on the LPS-stimulated pro-inflammatory cytokine production in bone marrow-derived dendritic cells. |
AID240921 | Inhibitory concentration against p38 alpha MAP kinase (Experimental value) | 2005 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15 | The molecular basis for coxib inhibition of p38alpha MAP kinase. |
AID435829 | Binding constant for RPS6KA1(Kin.Dom.2 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435167 | Binding constant for KIT(V559D) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720135 | Millipore: Percentage of residual kinase activity of EPHA8 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID492799 | Inhibition of p38alpha | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Unexpected reaction of 2-alkylsulfanylimidazoles to imidazol-2-ones: pyridinylimidazol-2-ones as novel potent p38alpha mitogen-activated protein kinase inhibitors. |
AID435317 | Percentage PIM1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720379 | Millipore: Percentage of residual kinase activity of MERTK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: mM MOPS pH 7.0, 0.2 mM EDTA, 30 mM NaCl | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624707 | Binding constant for DCAMKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435238 | Percentage JNK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID241905 | Inhibitory concentration against Epidermal growth factor receptor tyrosine kinase activity | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase. |
AID436047 | Binding constant for full-length PRKX | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256659 | Average Binding Constant for DAPK3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435728 | Percentage JNK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID624901 | Binding constant for RSK1(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624751 | Binding constant for PIP5K1C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256624 | Average Binding Constant for FGFR3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720454 | Millipore: Percentage of residual kinase activity of MARK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435756 | Percentage Src activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID436051 | Binding constant for RPS6KA5(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435429 | Binding constant for FLT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625087 | Binding constant for MELK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720170 | Millipore: Percentage of residual kinase activity of CSF1R at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256584 | Average Binding Constant for CAMK1D; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720134 | Millipore: Percentage of residual kinase activity of EPHA7 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID251879 | Percent inhibition of staphylococcal enterotoxin B induced TNF-alpha production at 10 mg/kg concentration | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis. |
AID435679 | Binding constant for PIM3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720251 | Millipore: Percentage of residual kinase activity of RPS6KA1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID339974 | Inhibition of human LCK at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID625105 | Binding constant for EPHB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID223814 | Inhibition of p38 kinase at 2 uM | 1999 | Bioorganic & medicinal chemistry letters, Mar-08, Volume: 9, Issue:5 | Potent, orally absorbed glucagon receptor antagonists. |
AID435563 | Binding constant for TNIK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625071 | Binding constant for STK39 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625065 | Binding constant for CIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720263 | Millipore: Percentage of residual kinase activity of MAPK12 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435158 | Binding constant for EPHA5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720405 | Millipore: Percentage of residual kinase activity of NTRK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625104 | Binding constant for MYO3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720202 | Millipore: Percentage of residual kinase activity of PRKCQ at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256617 | Average Binding Constant for TEK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435289 | Binding constant for ERK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625044 | Binding constant for PIK3CA(M1043I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435663 | Binding constant for full-length MST4 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID275051 | Inhibition of CYP2C19 at 10 uM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Design, synthesis, and biological evaluation of phenylamino-substituted 6,11-dihydro-dibenzo[b,e]oxepin-11-ones and dibenzo[a,d]cycloheptan-5-ones: novel p38 MAP kinase inhibitors. |
AID435411 | Binding constant for KIT(D816V) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625124 | Binding constant for RET(V804M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624951 | Binding constant for EPHA2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID275052 | Inhibition of CYP2D6 at 10 uM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Design, synthesis, and biological evaluation of phenylamino-substituted 6,11-dihydro-dibenzo[b,e]oxepin-11-ones and dibenzo[a,d]cycloheptan-5-ones: novel p38 MAP kinase inhibitors. |
AID720458 | Millipore: Percentage of residual kinase activity of PDGFRA at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435911 | Binding constant for MEK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435987 | Percentage PRK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID624997 | Binding constant for EGFR(E746-A750del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256622 | Average Binding Constant for JNK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435797 | Binding constant for ERBB4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720421 | Millipore: Percentage of residual kinase activity of ZAP70 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435196 | Binding constant for full-length SRPK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624835 | Binding constant for ERN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720370 | Millipore: Percentage of residual kinase activity of SRPK3 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID54593 | Inhibition of Cytochrome P450 2D6 at 10 uM | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15 | Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. |
AID435801 | Binding constant for full-length GSK3A | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624963 | Binding constant for LATS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1071887 | Inhibition of TNFalpha-induced IL-6 gene expression in HUVEC at 10 uM | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5 | Syntheses and structure-activity relationships for some triazolyl p38α MAPK inhibitors. |
AID435546 | Binding constant for PRKG1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720455 | Millipore: Percentage of residual kinase activity of MARK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID395288 | Inhibition of p38alpha MAPK by cell-free enzyme immunosorbent assay | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Aza-analogue dibenzepinone scaffolds as p38 mitogen-activated protein kinase inhibitors: design, synthesis, and biological data of inhibitors with improved physicochemical properties. |
AID720329 | Millipore: Percentage of residual kinase activity of STK11 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.1% v/v Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID268709 | Inhibition of LPS-stimulated TNFalpha production in THP1 cells | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | The development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-alpha production. |
AID218679 | Inhibition of beta-lactamase from Escherichia coli | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | Kinase inhibitors: not just for kinases anymore. |
AID720280 | Millipore: Percentage of residual kinase activity of PLK2 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624839 | Binding constant for AKT2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720100 | Millipore: Percentage of residual kinase activity of CAMK2G at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720223 | Millipore: Percentage of residual kinase activity of PIM1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720072 | Millipore: Percentage of residual kinase activity of CDK9 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID749360 | Induction of cardiomyogenic activity in human embryonic stem cells assessed as cardiomyocyte yield at 5 uM measured on day 15 by FACS analysis relative to control | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Tri-substituted imidazole analogues of SB203580 as inducers for cardiomyogenesis of human embryonic stem cells. |
AID435408 | Binding constant for INSR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624956 | Binding constant for EPHB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720232 | Millipore: Percentage of residual kinase activity of PRKX at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625122 | Binding constant for RET(M918T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624982 | Binding constant for ABL1(F317L)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720176 | Millipore: Percentage of residual kinase activity of GRK5 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1646096 | Inhibition of human RIPK2 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
AID735307 | Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated IL12 production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA | 2013 | Journal of natural products, Apr-26, Volume: 76, Issue:4 | Diarylheptanoids and flavonoids from viscum album inhibit LPS-stimulated production of pro-inflammatory cytokines in bone marrow-derived dendritic cells. |
AID624812 | Binding constant for SBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID219353 | Inhibition of c-Jun N-terminal kinase 1-alpha 1 at 5 uM | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | Pyrroles and other heterocycles as inhibitors of p38 kinase. |
AID1224792 | Delta TM value showing the stabilisation of RIOK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1451481 | Binding affinity to wild type human biotin labelled p38 alpha (9 to 352 residues) expressed in sf21 insect cells SPR analysis | |||
AID127255 | Inhibitory concentration against mitogen-activated protein kinase p38 alpha | 2001 | Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9 | Phenoxypyrimidine inhibitors of p38alpha kinase: synthesis and statistical evaluation of the p38 inhibitory potencies of a series of 1-(piperidin-4-yl)-4-(4-fluorophenyl)-5-(2-phenoxypyrimidin-4-yl) imidazoles. |
AID435526 | Binding constant for FGFR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624910 | Binding constant for TTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID631225 | Inhibition of p38 MAPK phosphorylation in UVB irradiation-induced NHEK at 2 uM after 0.5 hrs by immunoblotting method | 2011 | Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21 | Sodium dl-α-tocopheryl-6-O-phosphate inhibits PGE₂ production in keratinocytes induced by UVB, IL-1β and peroxidants. |
AID720039 | Millipore: Percentage of residual kinase activity of AURKC at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl, 0.1% v/v Triton-X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624761 | Binding constant for CDC2L5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224754 | Delta TM value showing the stabilisation of CAMK2G produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID625081 | Binding constant for RSK4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256600 | Average Binding Constant for EPHA8; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624855 | Binding constant for FRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720353 | Millipore: Percentage of residual kinase activity of MINK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435805 | Binding constant for MAP4K5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435562 | Binding constant for STK36 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256636 | Average Binding Constant for JNK3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435677 | Binding constant for LOK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625085 | Binding constant for ULK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID164653 | Inhibition of Protein kinase A | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase. |
AID248204 | Inhibition of tumor necrosis factor alpha release by THP-1 cells | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2 | Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation. |
AID720062 | Millipore: Percentage of residual kinase activity of CDK3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720271 | Millipore: Percentage of residual kinase activity of SGK3 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720423 | Millipore: Percentage of residual kinase activity of DAPK3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624819 | Binding constant for ACVR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1451483 | Binding affinity to wild type biotin labelled human p38 alpha (9 to 352 residues) expressed in sf21 insect cells assessed as association rate constant by SPR analysis | |||
AID624925 | Binding constant for RIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625030 | Binding constant for LOK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435399 | Binding constant for DCAMKL3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224759 | Delta TM value showing the stabilisation of CDKL1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID436017 | Binding constant for ERK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435789 | Binding constant for full-length CSNK2A2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625007 | Binding constant for EGFR(T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720117 | Millipore: Percentage of residual kinase activity of STK17A at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID215251 | Percent inhibition of LPS-stimulated TNF-alpha release in fasted BALB/cJ mice at 10 mg/kg | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | 6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2, 3-b]pyridine (RWJ 68354): a potent and selective p38 kinase inhibitor. |
AID720114 | Millipore: Percentage of residual kinase activity of DDR2 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720181 | Millipore: Percentage of residual kinase activity of GSK3A at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435903 | Binding constant for CDK8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720020 | Millipore: Percentage of residual kinase activity of ALK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720261 | Millipore: Percentage of residual kinase activity of MAPK11 at 10uM relative to control. Control inhibitor: SB203580 at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224777 | Delta TM value showing the stabilisation of MST4(1) produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624808 | Binding constant for TRKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720400 | Millipore: Percentage of residual kinase activity of TEK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625138 | Binding constant for STK33 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID315938 | Inhibition of JNK3 | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode. |
AID339971 | Inhibition of human PKBalpha at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID435169 | Binding constant for full-length MEK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720266 | Millipore: Percentage of residual kinase activity of SGK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720300 | Millipore: Percentage of residual kinase activity of IKBKB at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435433 | Binding constant for full-length MST1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID596311 | Inhibition of p38 alpha MAPK in human whole blood assessed as phosphorylation of ATF-2 by immunosorbent non-radioactive enzyme assay | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9 | Chiral sulfoxides as metabolites of 2-thioimidazole-based p38α mitogen-activated protein kinase inhibitors: enantioselective synthesis and biological evaluation. |
AID720149 | Millipore: Percentage of residual kinase activity of FGFR1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435329 | Binding constant for YSK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435799 | Binding constant for FLT3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID183129 | Inhibition of secondary paw swelling in rat adjuvant arthritis model | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | Pyrroles and other heterocycles as inhibitors of p38 kinase. |
AID624906 | Binding constant for S6K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435804 | Binding constant for LYN kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720122 | Millipore: Percentage of residual kinase activity of EGFR at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID428917 | Inhibition of human recombinant p38alpha assessed as [gamma33P]ATP utilization by microplate scintillation counting | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection. |
AID256576 | Average Binding Constant for MKNK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435792 | Binding constant for EGFR(S752-I759del) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID339970 | Inhibition of human PKCalpha at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID435781 | Binding constant for full-length BMX | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID729897 | Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced IL1-beta release at 100 uM incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay relative to control | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Structure-activity relationships of 6-(aminomethylphenoxy)-benzoxaborole derivatives as anti-inflammatory agent. |
AID281718 | Inhibition of LPS-induced IL1 beta production in human whole blood | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Tetrasubstituted imidazole inhibitors of cytokine release: probing substituents in the N-1 position. |
AID720143 | Millipore: Percentage of residual kinase activity of EPHB4 at 1uM relative to control. Control inhibitor: PP2 at 30.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624756 | Binding constant for MAP4K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435905 | Binding constant for full-length CSNK1G3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1716410 | Binding affinity to Nluc-tagged MAPK14 (unknown origin) expressed in HeLa cells assessed as percentage of stability at 10 uM incubated for 3 mins by isothermal NaLTSA assay (Rvb = 32 +/- 2.1 %) | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID624838 | Binding constant for ACVR2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720196 | Millipore: Percentage of residual kinase activity of HCK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID216428 | Inhibition of p38-related TNF-alpha release by whole blood cells at 10 e-4 to 10 e-8 M | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15 | Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. |
AID436006 | Binding constant for full-length AURKC | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID668564 | Cytotoxicity against human HL60 cells at 50 uM by MTT assay relative to control | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and biological evaluation of 4-alkoxy-6,9-dichloro[1,2,4]triazolo[4,3-a]quinoxalines as inhibitors of TNF-α and IL-6. |
AID720442 | Millipore: Percentage of residual kinase activity of NLK at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625057 | Binding constant for TYRO3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624942 | Binding constant for DRAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720178 | Millipore: Percentage of residual kinase activity of GRK6 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID281723 | Inhibition of human liver CYP2D6 at 10 uM | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Tetrasubstituted imidazole inhibitors of cytokine release: probing substituents in the N-1 position. |
AID256585 | Average Binding Constant for EPHA7; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435184 | Binding constant for PTK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435431 | Binding constant for MAP4K1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435785 | Binding constant for full-length CDK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435166 | Binding constant for full-length JNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID126926 | Inhibition of Mitogen-activated protein kinase 1 (ERK-2 enzyme) at 10 uM | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | 6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2, 3-b]pyridine (RWJ 68354): a potent and selective p38 kinase inhibitor. |
AID435657 | Binding constant for full-length IKK-epsilon | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624989 | Binding constant for ABL1(T315I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720162 | Millipore: Percentage of residual kinase activity of FGR at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID127105 | Inhibition of Mitogen-activated protein kinase p38 | 2002 | Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5 | Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5). |
AID1337192 | Binding affinity to recombinant human His6-TEV protease-tagged BRDT bromodomain 1 expressed in bacteria assessed as change in melting temperature at 10 uM by SYPRO Orange probe-based Real-Time PCR method | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6 | Non-kinase targets of protein kinase inhibitors. |
AID512265 | Inhibition of human PKBalpha expressed in SF9 cells at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID720363 | Millipore: Percentage of residual kinase activity of CDC42BPA at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624717 | Binding constant for JNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436012 | Binding constant for full-length CSNK2A1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720095 | Millipore: Percentage of residual kinase activity of CAMK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID127099 | Inhibitory activity against mitogen-activated protein kinase p38 at 10 e-4 to 10 e-8 M concentration | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15 | Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. |
AID429178 | Inhibition of LPS-induced TNFalpha production in human whole blood by immunoassay | 2009 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16 | Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 1. |
AID435285 | Binding constant for DMPK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625135 | Binding constant for ADCK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID668560 | Antiinflammatory activity in PMA-stimulated human HL60 cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 30 mins before LPS challenge measured after 24 hrs by ELISA | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and biological evaluation of 4-alkoxy-6,9-dichloro[1,2,4]triazolo[4,3-a]quinoxalines as inhibitors of TNF-α and IL-6. |
AID720109 | Millipore: Percentage of residual kinase activity of DAPK2 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID339957 | Inhibition of IL1-beta release in human whole blood | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID624834 | Binding constant for DAPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624722 | Binding constant for MKK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720040 | Millipore: Percentage of residual kinase activity of AURKC at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl, 0.1% v/v Triton-X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256598 | Average Binding Constant for FRK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435794 | Binding constant for EPHA3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720192 | Millipore: Percentage of residual kinase activity of GSG2 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435814 | Percentage PIM3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID624965 | Binding constant for LZK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1475308 | In vivo inhibition of P38 MAPKalpha in Lewis rat assessed as decrease in LPS-stimulated TNFalpha level in serum at 30 mg/kg pretreated for 1 hrs followed by LPS addition measured after 1.5 hrs post dose | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases. |
AID761958 | Antiinflammatory activity in human HL-60 derived macrophage-like cells assessed as inhibition of LPS-induced IL-6 production at 50 uM treated 30 mins before LPS stimulation measured after 24 hrs by ELISA | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | First synthesis and biological evaluation of 4-amino-2-aryl-6,9-dichlorobenzo[g]pteridines as inhibitors of TNF-α and IL-6. |
AID720180 | Millipore: Percentage of residual kinase activity of GRK7 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720374 | Millipore: Percentage of residual kinase activity of STK3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624985 | Binding constant for ABL1(M351T)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435204 | Binding constant for WEE1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720264 | Millipore: Percentage of residual kinase activity of MAPK13 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625072 | Binding constant for TBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID93822 | Inhibition of LPS-induced IL1-beta production in human peripheral blood mononuclear cells(PBMCs) | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | 6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2, 3-b]pyridine (RWJ 68354): a potent and selective p38 kinase inhibitor. |
AID761957 | Antiinflammatory activity in human HL-60 derived macrophage-like cells assessed as inhibition of LPS-induced IL-6 production treated 30 mins before LPS stimulation measured after 24 hrs by ELISA | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | First synthesis and biological evaluation of 4-amino-2-aryl-6,9-dichlorobenzo[g]pteridines as inhibitors of TNF-α and IL-6. |
AID435432 | Binding constant for MLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720371 | Millipore: Percentage of residual kinase activity of SRPK3 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1253623 | Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells assessed as reduction in autophosphorylation pre-incubated for 30 mins followed by incubation with ATP for 2 hrs by ADP-Glo assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity. |
AID624880 | Binding constant for PIK4CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720459 | Millipore: Percentage of residual kinase activity of PDGFRA at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720076 | Millipore: Percentage of residual kinase activity of CHEK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720102 | Millipore: Percentage of residual kinase activity of CAMK2D at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID215252 | Percent inhibition of LPS-stimulated TNF-alpha release in fasted BALB/cJ mice at 25 mg/kg | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | 6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2, 3-b]pyridine (RWJ 68354): a potent and selective p38 kinase inhibitor. |
AID1224794 | Delta TM value showing the stabilisation of RSK2b produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID625018 | Binding constant for YES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435441 | Binding constant for RPS6KA4(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID219504 | Inhibition of human c-Raf kinase | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase. |
AID624723 | Binding constant for CSNK1A1L kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID54402 | Inhibition of Cytochrome P450 2C9 at 10 uM | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15 | Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. |
AID238116 | Binding constant for EphB2 tyrosine kinase | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Frontal affinity chromatography with MS detection of EphB2 tyrosine kinase receptor. 1. Comparison with conventional ELISA. |
AID625090 | Binding constant for ICK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID666744 | Antiinflammatory activity in BALB/c mouse peritoneal macrophages assessed as inhibition of LPS-induced TNFalpha production treated 1 hr before LPS challenge measured after 24 hrs by ELISA | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Docking, synthesis and pharmacological activity of novel urea-derivatives designed as p38 MAPK inhibitors. |
AID256675 | Average Binding Constant for PTK6; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720089 | Millipore: Percentage of residual kinase activity of CLK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID216427 | Inhibition of p38-related IL1-beta release by whole blood cells at 10 e-4 to 10 e-8 M | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15 | Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. |
AID720237 | Millipore: Percentage of residual kinase activity of RIPK2 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624713 | Binding constant for ERK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624944 | Binding constant for ALK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624948 | Binding constant for CSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID767910 | Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA | 2013 | Journal of natural products, Sep-27, Volume: 76, Issue:9 | Anti-inflammatory asterosaponins from the starfish Astropecten monacanthus. |
AID720022 | Millipore: Percentage of residual kinase activity of ACVR1B at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720070 | Millipore: Percentage of residual kinase activity of CDK7 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624921 | Binding constant for MAP4K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID468035 | Inhibition of JNK2 | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase. |
AID624804 | Binding constant for ERBB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435775 | Binding constant for ABL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624764 | Binding constant for CLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1516990 | Inhibition of LPS-induced TNFalpha production in human THP1 cells incubated for 1 hr followed by LPS stimulation and measured after 4 hrs by TR-FRET method | |||
AID720209 | Millipore: Percentage of residual kinase activity of PRKD2 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID315936 | Inhibition of purified human p38alpha | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode. |
AID625067 | Binding constant for NDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID339962 | Inhibition of human JNK1-alpha-1/SAPK1c at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID435294 | Binding constant for full-length LIMK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435539 | Percentage PHK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID435933 | Binding constant for PKN2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720439 | Millipore: Percentage of residual kinase activity of NEK6 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625052 | Binding constant for PRKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435370 | Percentage p38beta MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID624978 | Binding constant for ABL1(E255K)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625043 | Binding constant for PIK3CA(I800L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256644 | Average Binding Constant for CSNK1E; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435560 | Binding constant for SNF1LK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624807 | Binding constant for TNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435397 | Binding constant for CSNK1G1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720121 | Millipore: Percentage of residual kinase activity of EGFR at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624789 | Binding constant for KIT(D816V) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435393 | Binding constant for CAMK1D kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID155132 | Inhibition of the release of tumor necrosis factor alpha from peripheral blood mononuclear cells | 2002 | Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21 | Imidazole inhibitors of cytokine release: probing substituents in the 2 position. |
AID256645 | Average Binding Constant for JAK2 (Kin.Dom. 2); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720297 | Millipore: Percentage of residual kinase activity of IGF1R at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID495062 | Inhibition of interferon-gamma/anisomycin-induced p38 phosphorylation in human U937 cells by Phospho-Flow cytometry | 2008 | Nature chemical biology, Feb, Volume: 4, Issue:2 | High-content single-cell drug screening with phosphospecific flow cytometry. |
AID729551 | Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells at 10 uM by TR-FRET based binding assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay. |
AID256668 | Average Binding Constant for ABL1(H396P); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID256637 | Average Binding Constant for JNK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435325 | Binding constant for RPS6KA4(Kin.Dom.1 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435791 | Binding constant for EGFR(E746-A750del) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435164 | Binding constant for IGF1R kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID127420 | Inhibition of Mitogen-activated protein kinase p38 beta | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | Pyrroles and other heterocycles as inhibitors of p38 kinase. |
AID435200 | Binding constant for full-length TNNI3K | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720367 | Millipore: Percentage of residual kinase activity of RPS6KA5 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID339969 | Inhibition of human PKA at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID668561 | Antiinflammatory activity in PMA-stimulated human HL60 cells assessed as inhibition of LPS-induced IL-6 production at 50 uM preincubated for 30 mins before LPS challenge measured after 24 hrs by ELISA | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and biological evaluation of 4-alkoxy-6,9-dichloro[1,2,4]triazolo[4,3-a]quinoxalines as inhibitors of TNF-α and IL-6. |
AID624848 | Binding constant for CSNK2A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624718 | Binding constant for PFTAIRE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256564 | Average Binding Constant for MAP3K4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID625017 | Binding constant for TIE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID339965 | Inhibition of human JNK3 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID720193 | Millipore: Percentage of residual kinase activity of HCK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID215079 | Inhibition of staphylococcal enterotoxin B(SEB) stimulated tumor necrosis factor alpha (TNF-alpha) production by human peripheral blood mononuclear cells(PBMCs) | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | 6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2, 3-b]pyridine (RWJ 68354): a potent and selective p38 kinase inhibitor. |
AID668559 | Antiinflammatory activity in PMA-stimulated human HL60 cells assessed as inhibition of LPS-induced TNFalpha production at 10 uM preincubated for 30 mins before LPS challenge measured after 24 hrs by ELISA | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and biological evaluation of 4-alkoxy-6,9-dichloro[1,2,4]triazolo[4,3-a]quinoxalines as inhibitors of TNF-α and IL-6. |
AID720026 | Millipore: Percentage of residual kinase activity of PRKAA2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID322453 | Inhibition of Raf1 kinase | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Pharmacophore identification of Raf-1 kinase inhibitors. |
AID720428 | Millipore: Percentage of residual kinase activity of SRC at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1337160 | Inhibition of p38alpha (unknown origin) | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6 | Non-kinase targets of protein kinase inhibitors. |
AID435518 | Binding constant for AURKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435828 | Binding constant for full-length PIP5K2B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624733 | Binding constant for SIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1596969 | Inhibition of LPS-induced TNFalpha production in human whole blood preincubated with compound for 15 mins followed by LPS addition measured after 2.5 hrs by ELISA | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Pyridinylimidazoles as dual glycogen synthase kinase 3β/p38α mitogen-activated protein kinase inhibitors. |
AID624797 | Binding constant for PHKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720204 | Millipore: Percentage of residual kinase activity of PRKCI at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256633 | Average Binding Constant for PRKACA; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435375 | Percentage RSK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720396 | Millipore: Percentage of residual kinase activity of TSSK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624970 | Binding constant for CDK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624767 | Binding constant for MERTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720407 | Millipore: Percentage of residual kinase activity of TXK at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720360 | Millipore: Percentage of residual kinase activity of MAP3K9 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720080 | Millipore: Percentage of residual kinase activity of CSNK1G2 at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1205969 | Inhibition of GAK (unknown origin) | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8 | Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents. |
AID1224796 | Delta TM value showing the stabilisation of LOK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624795 | Binding constant for MET(M1250T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256638 | Average Binding Constant for PRKAA1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID749361 | Inhibition of recombinant GST-tagged p38alpha MAP kinase (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Tri-substituted imidazole analogues of SB203580 as inducers for cardiomyogenesis of human embryonic stem cells. |
AID435897 | Binding constant for ABL1(T315I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720376 | Millipore: Percentage of residual kinase activity of STK24 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435787 | Binding constant for CLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720425 | Millipore: Percentage of residual kinase activity of RAF1 at 10uM relative to control. Control inhibitor: SB203580 at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435233 | Percentage HIPK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID625025 | Binding constant for MAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624940 | Binding constant for FLT3(R834Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435409 | Binding constant for full-length JNK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624828 | Binding constant for CDK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624879 | Binding constant for PIK3CG kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720107 | Millipore: Percentage of residual kinase activity of DAPK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720127 | Millipore: Percentage of residual kinase activity of EPHA3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID468034 | Inhibition of p38alpha | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase. |
AID625056 | Binding constant for TESK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625088 | Binding constant for ARK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720035 | Millipore: Percentage of residual kinase activity of AURKA at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl, 0.1% v/v Triton-X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1202877 | Inhibition of p38 MAPK in HAEC assessed as reduction of L5-induced caspase-3 activation at 2 uM preincubated for 30 mins followed by L5 induction measured after 24 hrs by Western blot analysis | 2015 | Journal of natural products, Feb-27, Volume: 78, Issue:2 | Sesamol reduces the atherogenicity of electronegative L5 LDL in vivo and in vitro. |
AID720081 | Millipore: Percentage of residual kinase activity of CSNK1G3 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625114 | Binding constant for GSK3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720230 | Millipore: Percentage of residual kinase activity of PLK3 at 1uM relative to control. Control inhibitor: Wortmannin at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625143 | Binding constant for CAMKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624892 | Binding constant for p38-delta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720332 | Millipore: Percentage of residual kinase activity of LCK at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224762 | Delta TM value showing the stabilisation of CLK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID210783 | Inhibition of Transforming growth factor beta-1 receptor (TbetaRI) | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Successful shape-based virtual screening: the discovery of a potent inhibitor of the type I TGFbeta receptor kinase (TbetaRI). |
AID229248 | Ability to inhibit the release of tumor necrosis factor alpha (TNF-alpha) from whole blood | 2002 | Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21 | Imidazole inhibitors of cytokine release: probing substituents in the 2 position. |
AID281717 | Inhibition of mitogen-activated protein kinase p38 alpha | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Tetrasubstituted imidazole inhibitors of cytokine release: probing substituents in the N-1 position. |
AID339958 | Inhibition of human CAMK2 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID720392 | Millipore: Percentage of residual kinase activity of TLK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224765 | Delta TM value showing the stabilisation of CK1G2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID625039 | Binding constant for PIK3CA(E545A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720038 | Millipore: Percentage of residual kinase activity of AURKB at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl, 0.1% v/v Triton-X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720345 | Millipore: Percentage of residual kinase activity of MAPKAPK3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Na-?-glycerophosphate pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435199 | Binding constant for TLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID436055 | Binding constant for full-length YANK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720219 | Millipore: Percentage of residual kinase activity of FRK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624957 | Binding constant for EPHB6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720434 | Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624778 | Binding constant for ACVRL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435646 | Binding constant for BLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435350 | Percentage ERK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID256613 | Average Binding Constant for Aurora2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID625054 | Binding constant for MST2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436050 | Binding constant for RPS6KA2(Kin.Dom.1 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224784 | Delta TM value showing the stabilisation of PCTK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720284 | Millipore: Percentage of residual kinase activity of MAP3K7 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624732 | Binding constant for PYK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID54786 | Inhibition of Cytochrome P450 3A4 at 10 uM | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15 | Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. |
AID127071 | Inhibition of p38 MAP kinase related TNF-alpha release from peripheral blood mononuclear cells (PBMC) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | From imidazoles to pyrimidines: new inhibitors of cytokine release. |
AID599959 | Binding affinity to human KIT D816V mutant incubated for 1 hr by kinase binding assay | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. |
AID720417 | Millipore: Percentage of residual kinase activity of WNK3 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435727 | Percentage JNK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID435654 | Binding constant for full-length ERK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625099 | Binding constant for TAOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720142 | Millipore: Percentage of residual kinase activity of EPHB3 at 10uM relative to control. Control inhibitor: PP2 at 30.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625035 | Binding constant for PHKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID512259 | Inhibition of Gst-tagged human MAPKAPK2 expressed in Escherichia coli at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID624953 | Binding constant for EPHA7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720161 | Millipore: Percentage of residual kinase activity of FGR at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1253625 | Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells assessed as dissociation rate by fluorescent polarization assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity. |
AID624721 | Binding constant for MEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720141 | Millipore: Percentage of residual kinase activity of EPHB3 at 1uM relative to control. Control inhibitor: PP2 at 30.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624753 | Binding constant for PKNB(M.tuberculosis) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435151 | Binding constant for CAMK1G kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435830 | Binding constant for RPS6KA2(Kin.Dom.2 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624860 | Binding constant for VEGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224774 | Delta TM value showing the stabilisation of p38beta produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID706189 | Inhibition of MAP kinase p38alpha assessed as phosphorylation of ATF-2 | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Targeting the hinge glycine flip and the activation loop: novel approach to potent p38α inhibitors. |
AID512266 | Inhibition of His-tagged human SGK expressed in Sf9 cells at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID624934 | Binding constant for FLT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624763 | Binding constant for RIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID428941 | Antiprotozoal activity against 2000Toxoplasma gondii RH tachyzoites infected 30 days after initial 100 parasite infection in CBA/J mouse assessed as mouse survival time at 60 mg/kg, ip administered 2 hrs postinfection for 7 consecutive days | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection. |
AID720399 | Millipore: Percentage of residual kinase activity of TEC at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435292 | Binding constant for ITK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224791 | Delta TM value showing the stabilisation of PRKACA produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID512261 | Inhibition of His-tagged human PRAK expressed in Sf9 cells at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID625034 | Binding constant for PDGFRA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256561 | Average Binding Constant for BTK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435621 | Percentage p38alpha MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720027 | Millipore: Percentage of residual kinase activity of NUAK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720032 | Millipore: Percentage of residual kinase activity of ABL1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435401 | Binding constant for full-length DRAK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435444 | Binding constant for TYK2(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624941 | Binding constant for CDKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720110 | Millipore: Percentage of residual kinase activity of DAPK2 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624977 | Binding constant for OSR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720394 | Millipore: Percentage of residual kinase activity of TSSK1B at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720308 | Millipore: Percentage of residual kinase activity of IRAK4 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256589 | Average Binding Constant for EPHA4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720236 | Millipore: Percentage of residual kinase activity of RIPK2 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624785 | Binding constant for JAK3(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID248689 | Concentration required to inhibit production of Tumor necrosis factor, alpha in LPS-stimulated human monocytic cells (THP-1) | 2004 | Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19 | The development of new bicyclic pyrazole-based cytokine synthesis inhibitors. |
AID624762 | Binding constant for DLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435414 | Binding constant for MLK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625032 | Binding constant for TRKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720448 | Millipore: Percentage of residual kinase activity of PAK4 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720058 | Millipore: Percentage of residual kinase activity of CDK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625119 | Binding constant for CAMK1G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256640 | Average Binding Constant for PTK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624994 | Binding constant for AKT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720201 | Millipore: Percentage of residual kinase activity of PRKCH at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256619 | Average Binding Constant for RPS6KA3 (Kin.Dom. 1); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID256667 | Average Binding Constant for ABL1(E255K); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID625117 | Binding constant for PAK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625074 | Binding constant for IKK-epsilon kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID586672 | Activation of Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction at 10 uM after 5 hrs pretreated with p38 inhibitor SB203580 for 1 hr before compound addition by Western blot analysis | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Involvement of heme oxygenase-1 induction via Nrf2/ARE activation in protection against H2O2-induced PC12 cell death by a metabolite of sesamin contained in sesame seeds. |
AID720055 | Millipore: Percentage of residual kinase activity of CDK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720324 | Millipore: Percentage of residual kinase activity of KDR at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435530 | Binding constant for MAP3K4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID339967 | Inhibition of human SAPK3/p38gamma at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID624787 | Binding constant for KIT(A829P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624932 | Binding constant for CLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720364 | Millipore: Percentage of residual kinase activity of CDC42BPB at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435822 | Binding constant for MEK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID115509 | Effect in murine model of arthritis onset in mice immunized with bovine type II collagen at 50 mg/kg; Histopathology in interstitial edema | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor. |
AID516348 | Binding affinity to full-length GST-tagged p38alpha by surface plasmon resonance assay | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19 | Biochemical and biophysical characterization of unique switch pocket inhibitors of p38α. |
AID624780 | Binding constant for CDK4-cyclinD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625129 | Binding constant for HIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID492800 | Antiinflammatory activity in human whole blood assessed as inhibition of LPS-stimulated TNFalpha release after 15 mins by ELISA | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Unexpected reaction of 2-alkylsulfanylimidazoles to imidazol-2-ones: pyridinylimidazol-2-ones as novel potent p38alpha mitogen-activated protein kinase inhibitors. |
AID624868 | Binding constant for MST1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625059 | Binding constant for YSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID448714 | Inhibition of GST-fused human full length CK1delta expressed in Escherichia coli at 1 uM | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | 3,4-Diaryl-isoxazoles and -imidazoles as potent dual inhibitors of p38alpha mitogen activated protein kinase and casein kinase 1delta. |
AID435551 | Binding constant for full-length p38-beta | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID436048 | Binding constant for full-length PTK2B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256570 | Average Binding Constant for PIM2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720247 | Millipore: Percentage of residual kinase activity of ROS1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720316 | Millipore: Percentage of residual kinase activity of JAK3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224799 | Delta TM value showing the stabilisation of NDR1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720259 | Millipore: Percentage of residual kinase activity of MAPK14 at 10uM relative to control. Control inhibitor: SB203580 at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720403 | Millipore: Percentage of residual kinase activity of NTRK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID436084 | Percentage GAK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID435288 | Binding constant for EPHB2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1646075 | Inhibition of human JNK2 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
AID435149 | Binding constant for AMPK-alpha2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624743 | Binding constant for LTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID729900 | Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced IL1-beta release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Structure-activity relationships of 6-(aminomethylphenoxy)-benzoxaborole derivatives as anti-inflammatory agent. |
AID720441 | Millipore: Percentage of residual kinase activity of NEK7 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435931 | Binding constant for PIM1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435533 | Binding constant for NEK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID666741 | Antihypernociceptive activity in Wistar rat assessed as inhibition of capsaicin-induced thermal hypernociception by measuring paw withdrawal latency at 100 umol/kg, po administered 1 hr before capsaicin challenge measured after 10 mins | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Docking, synthesis and pharmacological activity of novel urea-derivatives designed as p38 MAPK inhibitors. |
AID242126 | Inhibition of human cyclin G associated kinase at 100 uM ATP | 2005 | Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12 | Rapid computational identification of the targets of protein kinase inhibitors. |
AID720453 | Millipore: Percentage of residual kinase activity of PAK6 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435934 | Binding constant for PLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720414 | Millipore: Percentage of residual kinase activity of WNK2 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624962 | Binding constant for ASK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID108872 | Effect on LPS-induced TNF-alpha production in mice at 30 mg/kg peroral dose | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor. |
AID241473 | Inhibition of Mitogen-activated protein kinase p38 alpha | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9 | The development of monocyclic pyrazolone based cytokine synthesis inhibitors. |
AID429179 | Inhibition of LPS-induced TNFalpha production in orally dosed mouse after 1 hr by ELISA | 2009 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16 | Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 1. |
AID720074 | Millipore: Percentage of residual kinase activity of CHEK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720408 | Millipore: Percentage of residual kinase activity of ULK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435798 | Binding constant for FGR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435925 | Binding constant for PCTK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624730 | Binding constant for CAMK2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624980 | Binding constant for ABL1(F317I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435524 | Binding constant for full-length CSNK1D | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624961 | Binding constant for TGFBR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720296 | Millipore: Percentage of residual kinase activity of IGF1R at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID721302 | Inhibition of p38alpha MAP kinase (unknown origin) in presence of 100 uM ATP | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Dibenzosuberones as p38 mitogen-activated protein kinase inhibitors with low ATP competitiveness and outstanding whole blood activity. |
AID256641 | Average Binding Constant for ABL2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720128 | Millipore: Percentage of residual kinase activity of EPHA3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435912 | Binding constant for MRCKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID242591 | Inhibition of human receptor-interacting serine-threonine kinase 2 (RIPK2) at 100 uM ATP | 2005 | Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12 | Rapid computational identification of the targets of protein kinase inhibitors. |
AID126779 | Inhibition of MEK-1, Mitogen activated protein kinase kinase 1 | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase. |
AID435776 | Binding constant for ABL1(Y253F) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625096 | Binding constant for STK36 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436014 | Binding constant for full-length DYRK1B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID248802 | Inhibitory activity against lipopolysaccharide stimulated TNF-alpha production in THP-1 cells (human monocytic cells) | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9 | The development of monocyclic pyrazolone based cytokine synthesis inhibitors. |
AID127410 | Inhibitory activity against Mitogen-activated protein kinase p38 alpha 2 | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor. |
AID435192 | Binding constant for ROS1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624813 | Binding constant for MINK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624988 | Binding constant for ABL1(T315I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1716408 | Binding affinity to Nluc-tagged MAPK14 (unknown origin) expressed in HeLa cells assessed as change in melting temperature at 50 uM by isothermal NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID512254 | Inhibition of Gst-tagged human SAPK2a/p38 expressed in Escherichia coli at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID729899 | Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced IL6 release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Structure-activity relationships of 6-(aminomethylphenoxy)-benzoxaborole derivatives as anti-inflammatory agent. |
AID720303 | Millipore: Percentage of residual kinase activity of INSR at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID732451 | Antiinflammatory activity against in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL6 production compound pre-incubated for 1 hr before LPS challenge by ELISA | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Anti-inflammatory norditerpenoids from the soft coral Sinularia maxima. |
AID256587 | Average Binding Constant for ACK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID436054 | Binding constant for TLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720281 | Millipore: Percentage of residual kinase activity of PLK2 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435834 | Binding constant for YANK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID607540 | Inhibition of human p38alpha by FRET assay | 2011 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14 | Indolin-2-one p38α inhibitors I: design, profiling and crystallographic binding mode. |
AID732450 | Antiinflammatory activity against in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated TNFalpha production compound pre-incubated for 1 hr before LPS challenge by ELISA | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Anti-inflammatory norditerpenoids from the soft coral Sinularia maxima. |
AID720218 | Millipore: Percentage of residual kinase activity of FRK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624815 | Binding constant for ERBB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1876163 | Inhibition of p38 MAPK (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1596951 | Inhibition of p38alpha MAPK (unknown origin) using ATF-2 as substrate after 1 hr by ELISA | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | Pyridinylimidazoles as dual glycogen synthase kinase 3β/p38α mitogen-activated protein kinase inhibitors. |
AID720447 | Millipore: Percentage of residual kinase activity of PAK3 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID436022 | Binding constant for full-length MEK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720312 | Millipore: Percentage of residual kinase activity of ITK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720397 | Millipore: Percentage of residual kinase activity of TSSK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720155 | Millipore: Percentage of residual kinase activity of FGFR4 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435807 | Binding constant for MARK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720203 | Millipore: Percentage of residual kinase activity of PRKCQ at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720420 | Millipore: Percentage of residual kinase activity of ZAP70 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID201878 | Compound was evaluated for its ability to inhibit IL-6 production in SW1353 cells treated with cytokines IL-1 and TNF | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18 | Discovery of a new class of p38 kinase inhibitors. |
AID435445 | Binding constant for ZAP70 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID668563 | Cytotoxicity against human HL60 cells at 10 uM by MTT assay relative to control | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and biological evaluation of 4-alkoxy-6,9-dichloro[1,2,4]triazolo[4,3-a]quinoxalines as inhibitors of TNF-α and IL-6. |
AID625086 | Binding constant for SLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720125 | Millipore: Percentage of residual kinase activity of EPHA2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID436015 | Binding constant for EPHA6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435403 | Binding constant for EPHB1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720318 | Millipore: Percentage of residual kinase activity of MAPK8 at 1uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ? -mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID155131 | Inhibition of the release of interleukin-1-beta from peripheral blood mononuclear cells | 2002 | Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21 | Imidazole inhibitors of cytokine release: probing substituents in the 2 position. |
AID435645 | Binding constant for ACVRL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624706 | Binding constant for MLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256662 | Average Binding Constant for ERBB2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720319 | Millipore: Percentage of residual kinase activity of MAPK8 at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ? -mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720433 | Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: PI-103 at 30.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435157 | Binding constant for EGFR(G719C) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624882 | Binding constant for PKAC-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435190 | Binding constant for full-length PIP5K1A | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435406 | Binding constant for FLT3(D835H) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720475 | Millipore: Percentage of residual kinase activity of PRKCB at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624881 | Binding constant for PKAC-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435704 | Percentage Aurora B activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID428943 | Antiprotozoal activity against 2000Toxoplasma gondii RH tachyzoites infected 30 days after initial 20 parasite infection in CBA/J mouse assessed as mouse survival time at 30 mg/kg, ip administered 2 hrs postinfection for 7 consecutive days | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection. |
AID435676 | Binding constant for LCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256579 | Average Binding Constant for MAP3K5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID625063 | Binding constant for PLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624983 | Binding constant for ABL1(H396P)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624824 | Binding constant for PIP5K1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624871 | Binding constant for PAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435883 | Percentage SGK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID625062 | Binding constant for MAP3K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624908 | Binding constant for TEC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720258 | Millipore: Percentage of residual kinase activity of MAPK14 at 1uM relative to control. Control inhibitor: SB203580 at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435554 | Binding constant for PRKD3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID691523 | Inhibition of p38alpha-dependent TNFalpha production in human whole blood | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12 | Design, synthesis, and biological evaluation of novel disubstituted dibenzosuberones as highly potent and selective inhibitors of p38 mitogen activated protein kinase. |
AID720351 | Millipore: Percentage of residual kinase activity of MELK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720030 | Millipore: Percentage of residual kinase activity of MAP3K5 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID339963 | Inhibition of human MEK1 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID720356 | Millipore: Percentage of residual kinase activity of MAP2K7 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol, 0.1 mM Na3VO4 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID127095 | Inhibition of Mitogen-activated protein kinase p38 | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | Kinase inhibitors: not just for kinases anymore. |
AID624900 | Binding constant for RSK1(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224768 | Delta TM value showing the stabilisation of DMPK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624872 | Binding constant for PAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720257 | Millipore: Percentage of residual kinase activity of RPS6KA6 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 30 mM NaCl | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625120 | Binding constant for EPHA8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1444580 | Inhibition of p38 MAPK (unknown origin) using ATF2 as substrate measured after 15 by ELISA | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8 | Synthesis and molecular docking studies of new furochromone derivatives as p38α MAPK inhibitors targeting human breast cancer MCF-7 cells. |
AID624794 | Binding constant for MET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624955 | Binding constant for EPHB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624775 | Binding constant for STK16 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720415 | Millipore: Percentage of residual kinase activity of WNK2 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256582 | Average Binding Constant for NEK9; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID436008 | Binding constant for full-length BTK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625051 | Binding constant for PRKCQ kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624928 | Binding constant for CDKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435529 | Binding constant for LATS1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720331 | Millipore: Percentage of residual kinase activity of STK10 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1451485 | Binding affinity to wild type human biotin labelled p38 alpha (9 to 352 residues) expressed in sf21 insect cells assessed as residence time by SPR analysis | |||
AID256649 | Average Binding Constant for CSK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435256 | Percentage p38-gamma MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID256650 | Average Binding Constant for PIM1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720235 | Millipore: Percentage of residual kinase activity of PTK2B at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435152 | Binding constant for CAMK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624814 | Binding constant for DCAMKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720249 | Millipore: Percentage of residual kinase activity of TYRO3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID512258 | Inhibition of MAPKAPK1b from rabbit skeletal muscle at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID624805 | Binding constant for RSK3(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720133 | Millipore: Percentage of residual kinase activity of EPHA7 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224797 | Delta TM value showing the stabilisation of MPSK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624947 | Binding constant for BRAF(V600E) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID281719 | Inhibition of LPS-induced TNFalpha production in human whole blood | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Tetrasubstituted imidazole inhibitors of cytokine release: probing substituents in the N-1 position. |
AID625053 | Binding constant for PRKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720242 | Millipore: Percentage of residual kinase activity of RET at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID538370 | Cytotoxicity against human LNCAP cells at 100 pM to 1 uM | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | Synthesis and biological analysis of prostate-specific membrane antigen-targeted anticancer prodrugs. |
AID1437537 | Anti-inflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-induced TNFalpha production pretreated for 1 hr followed by LPS-stimulation after 18 hrs by ELISA | 2017 | Journal of natural products, 01-27, Volume: 80, Issue:1 | Isochromans and Related Constituents from the Endophytic Fungus Annulohypoxylon truncatum of Zizania caduciflora and Their Anti-Inflammatory Effects. |
AID436036 | Percentage Lck activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID256569 | Average Binding Constant for PAK7/PAK5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720481 | Millipore: Percentage of residual kinase activity of PRKCD at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435779 | Binding constant for ALK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720092 | Millipore: Percentage of residual kinase activity of CLK3 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720153 | Millipore: Percentage of residual kinase activity of FGFR3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720344 | Millipore: Percentage of residual kinase activity of MAPKAPK3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Na-?-glycerophosphate pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435681 | Percentage MAPKAPK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID435820 | Percentage PKCalpha activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID599957 | Binding affinity to human KIT incubated for 1 hr by kinase binding assay | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. |
AID720327 | Millipore: Percentage of residual kinase activity of LIMK1 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625110 | Binding constant for TRPM6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720129 | Millipore: Percentage of residual kinase activity of EPHA4 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID761521 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IL-1beta release at 10 uM after 24 hrs by ELISA | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Inhibitory effect of resveratrol dimerized derivatives on nitric oxide production in lipopolysaccharide-induced RAW 264.7 cells. |
AID720049 | Millipore: Percentage of residual kinase activity of BMX at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625115 | Binding constant for PAK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720438 | Millipore: Percentage of residual kinase activity of NEK6 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624849 | Binding constant for CSNK2A2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624890 | Binding constant for p38-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720187 | Millipore: Percentage of residual kinase activity of HIPK2 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1646092 | Inhibition of human CK1epsilon | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
AID215078 | Inhibition of LPS-stimulated TH+NF-alphs production by human peripheral blood mononuclear cells (PBMCs) | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | 6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2, 3-b]pyridine (RWJ 68354): a potent and selective p38 kinase inhibitor. |
AID624923 | Binding constant for MAPKAPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435284 | Binding constant for DCAMKL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID281721 | Inhibition of human liver CYP2C9 at 10 uM | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Tetrasubstituted imidazole inhibitors of cytokine release: probing substituents in the N-1 position. |
AID624724 | Binding constant for TAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224753 | Delta TM value showing the stabilisation of CAMK2D produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID625083 | Binding constant for LATS2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435154 | Binding constant for DDR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256560 | Average Binding Constant for FGR; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435443 | Binding constant for TXK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435553 | Binding constant for PRKCD kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID406410 | Protection against Bacillus anthracis protective antigen and lethal toxin-diphtheria toxin chimeric protein mediated cytotoxicity in mouse RAW264.7 cells assessed as cell viability | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Amiodarone and bepridil inhibit anthrax toxin entry into host cells. |
AID625126 | Binding constant for TAOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID512255 | Inhibition of Gst-tagged human SAPK2b/p38--beta-2 expressed in Escherichia coli at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID720457 | Millipore: Percentage of residual kinase activity of PASK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435297 | Binding constant for MLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720406 | Millipore: Percentage of residual kinase activity of TXK at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435936 | Binding constant for full-length SRPK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624905 | Binding constant for CDKL5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624784 | Binding constant for INSR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624836 | Binding constant for IKK-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624865 | Binding constant for MAP3K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID761956 | Cytotoxicity against human HL-60 derived macrophage-like cells at 50 uM after 1 hr by MTT assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | First synthesis and biological evaluation of 4-amino-2-aryl-6,9-dichlorobenzo[g]pteridines as inhibitors of TNF-α and IL-6. |
AID720243 | Millipore: Percentage of residual kinase activity of RET at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435658 | Binding constant for JAK2(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720191 | Millipore: Percentage of residual kinase activity of GSG2 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435669 | Percentage PDK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID325680 | Inhibition of collagen-induced human platelet aggregation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720086 | Millipore: Percentage of residual kinase activity of CSNK2A1 at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 20 mM HEPES pH 7.6, 0.15 M NaCl, 0.1 mM EDTA, 5 mM DTT, 0.1% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1437536 | Anti-inflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-induced IL12 p40 production pretreated for 1 hr followed by LPS-stimulation after 18 hrs by ELISA | 2017 | Journal of natural products, 01-27, Volume: 80, Issue:1 | Isochromans and Related Constituents from the Endophytic Fungus Annulohypoxylon truncatum of Zizania caduciflora and Their Anti-Inflammatory Effects. |
AID720427 | Millipore: Percentage of residual kinase activity of KIT at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625040 | Binding constant for PIK3CA(E545K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720334 | Millipore: Percentage of residual kinase activity of LCK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720152 | Millipore: Percentage of residual kinase activity of FGFR2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720047 | Millipore: Percentage of residual kinase activity of BLK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256628 | Average Binding Constant for LYN; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720269 | Millipore: Percentage of residual kinase activity of SGK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624821 | Binding constant for YANK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720189 | Millipore: Percentage of residual kinase activity of HIPK3 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256660 | Average Binding Constant for KIT; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID512268 | Inhibition of His-tagged human GSK3b expressed in Sf21 cells at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID624931 | Binding constant for CLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720054 | Millipore: Percentage of residual kinase activity of BRSK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624845 | Binding constant for CDK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435674 | Binding constant for JAK3(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID339975 | Inhibition of CYP1A2 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID720375 | Millipore: Percentage of residual kinase activity of STK3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1516991 | Inhibition of recombinant Nanoluc-tagged p38alpha (unknown origin) expressed in HEK293 cells incubated for 2 to 3 mins by NanoBRET assay | |||
AID624731 | Binding constant for CAMK2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224760 | Delta TM value showing the stabilisation of CHEK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720179 | Millipore: Percentage of residual kinase activity of GRK7 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID219492 | Inhibition of c-Jun N-terminal kinase 2-beta 2 | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | Pyrroles and other heterocycles as inhibitors of p38 kinase. |
AID720389 | Millipore: Percentage of residual kinase activity of NEK2 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224763 | Delta TM value showing the stabilisation of CLK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1224781 | Delta TM value showing the stabilisation of PAK4 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID256632 | Average Binding Constant for CDK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID625107 | Binding constant for DMPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720302 | Millipore: Percentage of residual kinase activity of INSR at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID761960 | Antiinflammatory activity in human HL-60 derived macrophage-like cells assessed as inhibition of LPS-induced TNFalpha production at 50 uM treated 30 mins before LPS stimulation measured after 24 hrs by ELISA | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | First synthesis and biological evaluation of 4-amino-2-aryl-6,9-dichlorobenzo[g]pteridines as inhibitors of TNF-α and IL-6. |
AID435493 | Percentage PKD1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID624719 | Binding constant for GRK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256648 | Average Binding Constant for RPS6KA5 (Kin.Dom 1); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435250 | Percentage MSK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID624914 | Binding constant for WEE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624935 | Binding constant for FLT3(D835H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID165149 | Inhibition of Protein kinase C | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase. |
AID720206 | Millipore: Percentage of residual kinase activity of PRKD1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: mM HEPES pH 7.4, 0.03% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID126948 | Inhibition of Mitogen-activated protein kinase p38 | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | From imidazoles to pyrimidines: new inhibitors of cytokine release. |
AID241428 | Inhibition of EphB2 receptor tyrosine kinase in ELISA assay | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Frontal affinity chromatography with MS detection of EphB2 tyrosine kinase receptor. 1. Comparison with conventional ELISA. |
AID720274 | Millipore: Percentage of residual kinase activity of SRPK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID436033 | Binding constant for PIK3CA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624926 | Binding constant for RIOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID126603 | Inhibitory activity against mitogen activated protein (MAP) kinase p38 alpha. | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Benzimidazolone p38 inhibitors. |
AID720044 | Millipore: Percentage of residual kinase activity of PTK6 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720034 | Millipore: Percentage of residual kinase activity of ABL2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID339977 | Inhibition of CYP2C19 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID625084 | Binding constant for HUNK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720113 | Millipore: Percentage of residual kinase activity of DDR2 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256653 | Average Binding Constant for FGFR1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435800 | Binding constant for FYN kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256652 | Average Binding Constant for CAMK2B; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624833 | Binding constant for CSNK1G2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624793 | Binding constant for KIT(V559D,V654A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID339973 | Inhibition of human ROCK2 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID625038 | Binding constant for PIK3CA(E542K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224804 | Delta TM value showing the stabilisation of VRK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435901 | Binding constant for BRAF kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID162317 | Inhibition of Prostaglandin G/H synthase 1 at 5 uM | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | 6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2, 3-b]pyridine (RWJ 68354): a potent and selective p38 kinase inhibitor. |
AID625019 | Binding constant for AKT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435899 | Binding constant for AKT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720148 | Millipore: Percentage of residual kinase activity of PTK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435784 | Binding constant for CAMK2G kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720378 | Millipore: Percentage of residual kinase activity of MERTK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: mM MOPS pH 7.0, 0.2 mM EDTA, 30 mM NaCl | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624918 | Binding constant for DYRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435557 | Binding constant for RIPK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435183 | Binding constant for PLK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256631 | Average Binding Constant for FLT4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435696 | Selectivity for p38-alpha as proportion of 290 kinases in screen with similar potency; non-selective = 1 highly selective = 0 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435778 | Binding constant for full-length ADCK4 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720388 | Millipore: Percentage of residual kinase activity of NEK2 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID436013 | Binding constant for DMPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625140 | Binding constant for MARK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624949 | Binding constant for CSNK1G3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435400 | Binding constant for DDR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435552 | Binding constant for PIK3CA(E545K) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID224147 | Inhibition of p56 Lck tyrosine kinase | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase. |
AID256597 | Average Binding Constant for CLK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720276 | Millipore: Percentage of residual kinase activity of SRPK2 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720025 | Millipore: Percentage of residual kinase activity of PRKAA2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720087 | Millipore: Percentage of residual kinase activity of CSNK2A2 at 1uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 20 mM HEPES pH 7.6, 0.15 M NaCl, 0.1 mM EDTA, 5 mM DTT, 0.1% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435806 | Binding constant for MAPKAPK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720111 | Millipore: Percentage of residual kinase activity of DCLK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256661 | Average Binding Constant for PDGFRB; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720065 | Millipore: Percentage of residual kinase activity of CDK5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624806 | Binding constant for RPS6KA4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435378 | Percentage S6K1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID625125 | Binding constant for CLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720395 | Millipore: Percentage of residual kinase activity of TSSK1B at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID127411 | Inhibition of mitogen-activated protein kinase p38 alpha 2 | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18 | 1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors. |
AID624889 | Binding constant for JNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625013 | Binding constant for LCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624779 | Binding constant for BTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720241 | Millipore: Percentage of residual kinase activity of ROCK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720090 | Millipore: Percentage of residual kinase activity of CLK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID114908 | Percentage inhibition of LPS-induced TNF-alpha production in mice at 10 mg/kg peroral dose | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor. |
AID435647 | Binding constant for CAMK2D kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720278 | Millipore: Percentage of residual kinase activity of STK33 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435821 | Binding constant for GAK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720183 | Millipore: Percentage of residual kinase activity of GSK3B at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625134 | Binding constant for PIP5K2C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435373 | Percentage PKCzeta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720432 | Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: PI-103 at 30.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID127269 | Thermal denaturation temperature (Tm) of the inhibitor and murine pMitogen-activated protein kinase p38 alpha complex | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22 | Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). |
AID624729 | Binding constant for FAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625093 | Binding constant for TNIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624709 | Binding constant for MYLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435413 | Binding constant for MLCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624867 | Binding constant for MLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224776 | Delta TM value showing the stabilisation of ERK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720147 | Millipore: Percentage of residual kinase activity of PTK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID428942 | Antiprotozoal activity against 2000Toxoplasma gondii RH tachyzoites infected 30 days after initial 100 parasite infection in CBA/J mouse assessed as mouse survival time at 5 mg/kg, ip administered 2 hrs postinfection for 7 consecutive days | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection. |
AID435215 | Percentage AMPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720210 | Millipore: Percentage of residual kinase activity of PRKG1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 uM cGMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID209191 | Inhibition of LPS-induced tumor necrosis factor-alpha (TNF-alpha) production in THP-1 cells | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14 | Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
AID219663 | Inhibition of c-Src tyrosine kinase at 5 uM | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | 6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2, 3-b]pyridine (RWJ 68354): a potent and selective p38 kinase inhibitor. |
AID624913 | Binding constant for TYK2(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720411 | Millipore: Percentage of residual kinase activity of ULK3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID751226 | Inhibition of LPS-induced p38 MAPK phosphorylation in rat IEC-18 cells at 10 uM incubated for 1 hr prior to LPS challenge measured after 30 mins by Western blot analysis | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6 | Oleuropein protects against dextran sodium sulfate-induced chronic colitis in mice. |
AID720172 | Millipore: Percentage of residual kinase activity of FYN at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720283 | Millipore: Percentage of residual kinase activity of SYK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256642 | Average Binding Constant for VEGFR2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624712 | Binding constant for DYRK1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624765 | Binding constant for TRKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID729901 | Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced TNFalpha release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Structure-activity relationships of 6-(aminomethylphenoxy)-benzoxaborole derivatives as anti-inflammatory agent. |
AID720169 | Millipore: Percentage of residual kinase activity of CSF1R at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625128 | Binding constant for CSNK1G1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256630 | Average Binding Constant for FYN; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID256647 | Average Binding Constant for SYK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435374 | Percentage PLK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720445 | Millipore: Percentage of residual kinase activity of PAK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID512273 | Inhibition of His-tagged human LCK expressed in Sf9 cells at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID625029 | Binding constant for BRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435275 | Binding constant for BIKE kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625041 | Binding constant for PIK3CA(H1047L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720460 | Millipore: Percentage of residual kinase activity of PDGFRB at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720368 | Millipore: Percentage of residual kinase activity of RPS6KA4 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID339976 | Inhibition of CYP2C9 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID1269291 | Activation of p38 in human A549 cells assessed as downregulation of cytochrome c expression in mitochondria at 100 to 400 ug/ml by Western blot analysis | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | The anti-tumor activity and mechanism of alkaloids from Aconitum szechenyianum Gay. |
AID625048 | Binding constant for PRKCD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1527594 | Inhibition of LPS-induced TNFalpha production in human whole blood preincubated for 15 mins followed by LPS stimulation and measured after 2.5 hrs by ELISA | |||
AID435675 | Binding constant for KIT(V559D,T670I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624984 | Binding constant for ABL1(H396P)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435311 | Binding constant for HCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625042 | Binding constant for PIK3CA(H1047Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624826 | Binding constant for BMPR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID325676 | Inhibition of p38 MAP kinase | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435150 | Binding constant for ARK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256677 | Average Binding Constant for STK38L; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435909 | Binding constant for full-length LKB1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435180 | Binding constant for MAPKAPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435656 | Binding constant for FGFR4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720085 | Millipore: Percentage of residual kinase activity of CSNK2A1 at 1uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 20 mM HEPES pH 7.6, 0.15 M NaCl, 0.1 mM EDTA, 5 mM DTT, 0.1% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624754 | Binding constant for NEK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720244 | Millipore: Percentage of residual kinase activity of MST1R at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624907 | Binding constant for SYK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720341 | Millipore: Percentage of residual kinase activity of MAPK1 at 10uM relative to control. Control inhibitor: ERK Inhibitor II at 30.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625142 | Binding constant for TSSK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435191 | Binding constant for full-length RIOK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID445108 | Inhibition of CYP2D6 at 10 uM | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22 | Synthesis and biological evaluation of p38alpha kinase-targeting dialkynylimidazoles. |
AID624837 | Binding constant for IRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID735306 | Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated IL-12p40 production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA | 2013 | Journal of natural products, Apr-26, Volume: 76, Issue:4 | Diarylheptanoids and flavonoids from viscum album inhibit LPS-stimulated production of pro-inflammatory cytokines in bone marrow-derived dendritic cells. |
AID1224798 | Delta TM value showing the stabilisation of DRAK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID257469 | Inhibitory activity against p38-alpha MAPK | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Two classes of p38alpha MAP kinase inhibitors having a common diphenylether core but exhibiting divergent binding modes. |
AID720352 | Millipore: Percentage of residual kinase activity of MINK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625116 | Binding constant for ADCK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625127 | Binding constant for RSK3(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436019 | Binding constant for FRK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID339979 | Inhibition of CYP3A4 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID209183 | Inhibitory activity against TNF-alpha production using lipopolysaccharide stimulated human monocytic cells | 2003 | Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10 | The development of new triazole based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production. |
AID624909 | Binding constant for TGFBR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256655 | Average Binding Constant for CSNK1G1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID462319 | Inhibition of human MAPK p38alpha | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | In silico search for multi-target anti-inflammatories in Chinese herbs and formulas. |
AID1475427 | Binding affinity to p38alpha MAPK (unknown origin) by SPR assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases. |
AID720220 | Millipore: Percentage of residual kinase activity of PHKG2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256643 | Average Binding Constant for CAMK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624869 | Binding constant for NEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720362 | Millipore: Percentage of residual kinase activity of CDC42BPA at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID238118 | Equilibrium binding constant for EPH receptor B2 | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | Frontal affinity chromatography with MS detection of EphB2 tyrosine kinase receptor. 2. Identification of small-molecule inhibitors via coupling with virtual screening. |
AID624823 | Binding constant for MKNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID632580 | Antiinflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL-12p40 production preincubated for 1 hr before LPS-stimulation measured after 16 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | Chemical constituents of the rhizomes of Hedychium coronarium and their inhibitory effect on the pro-inflammatory cytokines production LPS-stimulated in bone marrow-derived dendritic cells. |
AID435937 | Binding constant for TESK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720024 | Millipore: Percentage of residual kinase activity of PRKAA1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435867 | Percentage NEK2a activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720053 | Millipore: Percentage of residual kinase activity of BRSK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720019 | Millipore: Percentage of residual kinase activity of ALK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720146 | Millipore: Percentage of residual kinase activity of ERBB4 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1253622 | Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells by fluorescent polarization assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity. |
AID256651 | Average Binding Constant for DAPK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435644 | Binding constant for ABL1(E255K) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID280498 | Inhibition of JNK3 by non-radioactive immunosorbent assay | 2007 | Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6 | From five- to six-membered rings: 3,4-diarylquinolinone as lead for novel p38MAP kinase inhibitors. |
AID90808 | Inhibition of LPS-induced p38-related TNF alpha release from human monocytes | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | Pyrroles and other heterocycles as inhibitors of p38 kinase. |
AID435274 | Binding constant for ACVR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID127272 | Inhibition of Mitogen-activated protein kinase p38 alpha | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | Pyrroles and other heterocycles as inhibitors of p38 kinase. |
AID720295 | Millipore: Percentage of residual kinase activity of TGFBR1 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625031 | Binding constant for MRCKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID660757 | Inhibition of p38alpha kinase | 2011 | ACS medicinal chemistry letters, Oct-13, Volume: 2, Issue:10 | The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor. |
AID624897 | Binding constant for RAF1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID632579 | Antiinflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL-6 production preincubated for 1 hr before LPS-stimulation measured after 16 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | Chemical constituents of the rhizomes of Hedychium coronarium and their inhibitory effect on the pro-inflammatory cytokines production LPS-stimulated in bone marrow-derived dendritic cells. |
AID720212 | Millipore: Percentage of residual kinase activity of PRKG1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 uM cGMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID732452 | Antiinflammatory activity against in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL12 production compound pre-incubated for 1 hr before LPS challenge by ELISA | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Anti-inflammatory norditerpenoids from the soft coral Sinularia maxima. |
AID720275 | Millipore: Percentage of residual kinase activity of SRPK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624811 | Binding constant for PAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID395286 | Aqueous solubility in HCl/H2O at pH 1 | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Aza-analogue dibenzepinone scaffolds as p38 mitogen-activated protein kinase inhibitors: design, synthesis, and biological data of inhibitors with improved physicochemical properties. |
AID435412 | Binding constant for MAP3K5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID512257 | Inhibition of Gst-tagged human SAPK4/p38delta expressed in Escherichia coli at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID720482 | Millipore: Percentage of residual kinase activity of PRKCE at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435819 | Percentage PKBbeta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID436007 | Binding constant for AXL kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624946 | Binding constant for BRAF kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720290 | Millipore: Percentage of residual kinase activity of TAOK3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 200 mM NaCl, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435777 | Binding constant for ABL2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435898 | Binding constant for ACVR1B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID92862 | Inhibition of LPS-induced release of Tumor necrosis factor-alpha (TNF-alpha) from human whole blood | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase. |
AID215099 | Inhibitory activity against LPS-stimulated TNF-alpha production in human monocytic cells (THP-1) | 2004 | Journal of medicinal chemistry, May-20, Volume: 47, Issue:11 | Development of orally bioavailable bicyclic pyrazolones as inhibitors of tumor necrosis factor-alpha production. |
AID1225272 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated IL-6 mRNA expression at 10 uM after 24 hrs by RT-qPCR analysis relative to control | 2015 | Journal of natural products, Mar-27, Volume: 78, Issue:3 | Monanchosterols A and B, bioactive bicyclo[4.3.1]steroids from a Korean sponge Monanchora sp. |
AID435434 | Binding constant for RET kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID281722 | Inhibition of human liver CYP2C19 at 10 uM | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Tetrasubstituted imidazole inhibitors of cytokine release: probing substituents in the N-1 position. |
AID435202 | Binding constant for TRKC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID322018 | Inhibition of human p38-alpha kinase | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors. |
AID256629 | Average Binding Constant for HCK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435280 | Binding constant for CSF1R kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625050 | Binding constant for PKN2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID241747 | Concentration required to inhibit human mitogen activated protein kinase p38 activity | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis. |
AID720401 | Millipore: Percentage of residual kinase activity of TEK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624873 | Binding constant for PAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720174 | Millipore: Percentage of residual kinase activity of GCK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 200 mM NaCl, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID436049 | Binding constant for PTK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID325678 | Inhibition of LPS-stimulated IL1 production in human THP1 cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID127436 | Inhibition of Mitogen-activated protein kinase p38 gamma at 40 uM | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | Pyrroles and other heterocycles as inhibitors of p38 kinase. |
AID720213 | Millipore: Percentage of residual kinase activity of PRKG1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 uM cGMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435155 | Binding constant for full-length DLK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435881 | Percentage ROCK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720430 | Millipore: Percentage of residual kinase activity of EEF2K at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID729898 | Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced TNFalpha release at 100 uM incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay relative to control | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Structure-activity relationships of 6-(aminomethylphenoxy)-benzoxaborole derivatives as anti-inflammatory agent. |
AID435321 | Binding constant for PRKCQ kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625009 | Binding constant for EPHA3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624952 | Binding constant for EPHA4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID761533 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production at 10 uM treated 2 hrs before LPS challenge measured after 24 hrs | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Inhibitory effect of resveratrol dimerized derivatives on nitric oxide production in lipopolysaccharide-induced RAW 264.7 cells. |
AID625131 | Binding constant for FGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435808 | Binding constant for full-length MEK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624976 | Binding constant for PRKX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625141 | Binding constant for RIOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435523 | Binding constant for CIT kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624864 | Binding constant for CTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435687 | Binding constant for PAK7/PAK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624816 | Binding constant for HPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID339964 | Inhibition of human JNK2alpha2 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID624770 | Binding constant for CAMK2D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720398 | Millipore: Percentage of residual kinase activity of TEC at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435833 | Binding constant for full-length TNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435181 | Binding constant for full-length p38-alpha | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720118 | Millipore: Percentage of residual kinase activity of STK17A at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID242399 | Inhibition of Mitogen-activated protein kinase 14 (P38 alpha) at 100 uM ATP | 2005 | Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12 | Rapid computational identification of the targets of protein kinase inhibitors. |
AID256676 | Average Binding Constant for SRC; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624790 | Binding constant for KIT(L576P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720277 | Millipore: Percentage of residual kinase activity of SRPK2 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID339978 | Inhibition of CYP2D6 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID720048 | Millipore: Percentage of residual kinase activity of BLK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625095 | Binding constant for SIK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624986 | Binding constant for ABL1(Q252H)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624927 | Binding constant for RPS6KA4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435398 | Binding constant for DAPK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624964 | Binding constant for DYRK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720292 | Millipore: Percentage of residual kinase activity of TBK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID436016 | Binding constant for full-length ERK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID771566 | Inhibition of p38 phosphorylation in LPS-stimulated mouse RAW264.7 cells at 10 uM incubated for 15 mins prior to LPS stimulation measured after 15 mins by Western blot analysis | 2013 | Journal of natural products, Sep-27, Volume: 76, Issue:9 | Vermelhotin, an anti-inflammatory agent, suppresses nitric oxide production in RAW 264.7 cells via p38 inhibition. |
AID720234 | Millipore: Percentage of residual kinase activity of PTK2B at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720041 | Millipore: Percentage of residual kinase activity of AXL at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720078 | Millipore: Percentage of residual kinase activity of CSNK1G1 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID114440 | Effect in murine model of arthritis onset in mice immunized with bovine type II collagen at 50 mg/kg; Histopathology in inflammatory cell | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor. |
AID720452 | Millipore: Percentage of residual kinase activity of PAK6 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624783 | Binding constant for FGFR3(G697C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435692 | Binding constant for STK16 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435363 | Percentage MELK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID435278 | Binding constant for full-length CDK7 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1475309 | In vivo inhibition of P38 MAPKalpha in Lewis rat assessed as decrease in LPS-stimulated TNFalpha level in serum at 30 mg/kg pretreated for 3 hrs followed by LPS addition measured after 1.5 hrs post dose | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases. |
AID624999 | Binding constant for EGFR(G719S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625028 | Binding constant for ASK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID586675 | Activation of Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction at 10 uM after 5 hrs pretreated with JNK inhibitor SP600125 for 1 hr before compound addition by Western blot analysis | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Involvement of heme oxygenase-1 induction via Nrf2/ARE activation in protection against H2O2-induced PC12 cell death by a metabolite of sesamin contained in sesame seeds. |
AID512272 | Inhibition of PHK from rabbit skeletal muscle at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID720228 | Millipore: Percentage of residual kinase activity of PLK1 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 20 mM DTT | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID735308 | Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated TNF-alpha production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA | 2013 | Journal of natural products, Apr-26, Volume: 76, Issue:4 | Diarylheptanoids and flavonoids from viscum album inhibit LPS-stimulated production of pro-inflammatory cytokines in bone marrow-derived dendritic cells. |
AID512264 | Inhibition of His-tagged human PDK1 expressed in Sf21 cells at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID435323 | Binding constant for RET(M918T) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624852 | Binding constant for FES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720098 | Millipore: Percentage of residual kinase activity of CAMK2B at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624954 | Binding constant for EPHB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435410 | Binding constant for KIT kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720037 | Millipore: Percentage of residual kinase activity of AURKB at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl, 0.1% v/v Triton-X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224787 | Delta TM value showing the stabilisation of PIM2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID625101 | Binding constant for TAOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID240825 | Inhibition of EPH receptor B2 using ELISA | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | Frontal affinity chromatography with MS detection of EphB2 tyrosine kinase receptor. 2. Identification of small-molecule inhibitors via coupling with virtual screening. |
AID720348 | Millipore: Percentage of residual kinase activity of MAP2K1 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 50 mM Tris pH 7.5, 0.2 mM EGTA, 0.1% ?-mercaptoethanol, 0.01% Brij-35 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID512256 | Inhibition of Gst-tagged human SAPK3/p38gamma expressed in Escherichia coli at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID436018 | Binding constant for FLT4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720354 | Millipore: Percentage of residual kinase activity of MAP2K6 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol, 0.1 mM Na3VO4, 1 mg/mL BSA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1451486 | Binding affinity to wild type human biotin labelled p38 alpha (9 to 352 residues) expressed in sf21 insect cells assessed as dissociation half life by SPR analysis | |||
AID435430 | Binding constant for INSRR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720198 | Millipore: Percentage of residual kinase activity of IGF1R at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624968 | Binding constant for DRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1309964 | Selectivity ratio, ratio of IC50 for RIP2K in MDP-stimulated HEK-293 cells over-expressing NOD2 assessed as IL8 secretion to IC50 for RIP2K in Pam2CSK4-stimulated HEK-293 cells over-expressing TLR2 assessed as IL8 secretion | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase. |
AID720286 | Millipore: Percentage of residual kinase activity of TAOK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624894 | Binding constant for MEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435693 | Binding constant for TGFBR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224772 | Delta TM value showing the stabilisation of MAP2K6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID127070 | Inhibition of p38 MAP kinase related TNF-alpha release from peripheral blood mononuclear cells (PBMC) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | From imidazoles to pyrimidines: new inhibitors of cytokine release. |
AID624846 | Binding constant for CSNK1A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720246 | Millipore: Percentage of residual kinase activity of ROS1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720304 | Millipore: Percentage of residual kinase activity of INSR at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435147 | Binding constant for ACVR2B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID325679 | Inhibition of LPS-stimulated TNFalpha production in human THP1 cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624769 | Binding constant for AURKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256672 | Average Binding Constant for CAMK2G; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720099 | Millipore: Percentage of residual kinase activity of CAMK2G at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720018 | Millipore: Percentage of residual kinase activity of TNK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624758 | Binding constant for RIPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1646086 | Inhibition of human TNIK | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
AID720195 | Millipore: Percentage of residual kinase activity of HCK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435790 | Binding constant for DRAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435146 | Binding constant for ABL1(H396P) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720173 | Millipore: Percentage of residual kinase activity of GCK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 200 mM NaCl, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625064 | Binding constant for PIM2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625130 | Binding constant for FGFR4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435324 | Binding constant for full-length RIOK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720260 | Millipore: Percentage of residual kinase activity of MAPK11 at 1uM relative to control. Control inhibitor: SB203580 at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624714 | Binding constant for p38-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID339966 | Inhibition of human SAPK2a/p38-alpha at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID436004 | Binding constant for ACVR2A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435522 | Binding constant for CDK11 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID691521 | Inhibition of p38alpha by immunosorbent based kinase assay | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12 | Design, synthesis, and biological evaluation of novel disubstituted dibenzosuberones as highly potent and selective inhibitors of p38 mitogen activated protein kinase. |
AID720224 | Millipore: Percentage of residual kinase activity of PIM2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720227 | Millipore: Percentage of residual kinase activity of PIM3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.1% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435831 | Binding constant for RPS6KA5(Kin.Dom.1 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID275053 | Inhibition of CYP3A4 at 10 uM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Design, synthesis, and biological evaluation of phenylamino-substituted 6,11-dihydro-dibenzo[b,e]oxepin-11-ones and dibenzo[a,d]cycloheptan-5-ones: novel p38 MAP kinase inhibitors. |
AID436071 | Percentage CHK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720293 | Millipore: Percentage of residual kinase activity of TBK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID127412 | Inhibitory activity against Mitogen-activated protein kinase p38 alpha 2 expressed in Escherichia coli. | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18 | Discovery of a new class of p38 kinase inhibitors. |
AID720473 | Millipore: Percentage of residual kinase activity of PRKCA at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720139 | Millipore: Percentage of residual kinase activity of EPHB2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435667 | Binding constant for full-length NLK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256669 | Average Binding Constant for ABL1(M351T); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435788 | Binding constant for CLK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624938 | Binding constant for FLT3(K663Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720346 | Millipore: Percentage of residual kinase activity of MARK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720091 | Millipore: Percentage of residual kinase activity of CLK3 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624936 | Binding constant for FLT3(D835Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624943 | Binding constant for ACVR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID495022 | Inhibition of phospho-p38 alpha activity by ELISA | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Optimization of alpha-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site. |
AID435678 | Binding constant for MUSK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624884 | Binding constant for PRKD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624959 | Binding constant for MAP4K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID428915 | Antiprotozoal activity against 1 MOI Toxoplasma gondii RH tachyzoites infected in confluent HFF assessed as inhibition of [3H]uracil incorporation into tachyzoites treated 4 hrs after infection measured after overnight incubation post uracil addition by l | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection. |
AID435930 | Binding constant for PHKG2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720391 | Millipore: Percentage of residual kinase activity of NEK3 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID46887 | In vitro inhibitory concentration against radioligand [3H]SB-202190 binding to CSBP kinase in human monocytic cell line, THP-1 | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | 1-substituted 4-aryl-5-pyridinylimidazoles: a new class of cytokine suppressive drugs with low 5-lipoxygenase and cyclooxygenase inhibitory potency. |
AID242035 | Inhibition of human casein kinase 1 delta at 100 uM ATP | 2005 | Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12 | Rapid computational identification of the targets of protein kinase inhibitors. |
AID624786 | Binding constant for KIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435322 | Binding constant for PRKG2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720416 | Millipore: Percentage of residual kinase activity of WNK3 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435706 | Percentage BRSK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID116871 | Percentage inhibition of LPS-induced TNF-alpha production in mice at 30 mg/kg peroral dose | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor. |
AID436045 | Binding constant for PRKD1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435338 | Percentage CaMK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID435910 | Binding constant for MAP4K4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID631280 | Protection against UVB irradiation-induced cell damage in NHEK assessed as inhibition of PGE2 production at 2 uM pretreated for 24 hrs before UVB irradiation measured after 24 hrs by enzymatic immunoassay | 2011 | Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21 | Sodium dl-α-tocopheryl-6-O-phosphate inhibits PGE₂ production in keratinocytes induced by UVB, IL-1β and peroxidants. |
AID720384 | Millipore: Percentage of residual kinase activity of MUSK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256607 | Average Binding Constant for STK18; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720042 | Millipore: Percentage of residual kinase activity of AXL at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624829 | Binding constant for CDK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1238355 | Inhibition of rat P2X7 receptor | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Docking of competitive inhibitors to the P2X7 receptor family reveals key differences responsible for changes in response between rat and human. |
AID435832 | Binding constant for SLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1071889 | Inhibition of p38a MAPK (unknown origin) by radiometric assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5 | Syntheses and structure-activity relationships for some triazolyl p38α MAPK inhibitors. |
AID720215 | Millipore: Percentage of residual kinase activity of MAPKAPK5 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Na-?-glycerophosphate pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435516 | Binding constant for ADCK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625139 | Binding constant for SNARK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1513827 | Cytotoxicity against human A549 cells assessed as reduction in cell viability at 10 to 25 uM after 8 hrs by Alamar blue assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
AID720393 | Millipore: Percentage of residual kinase activity of TLK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624773 | Binding constant for AMPK-alpha1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720449 | Millipore: Percentage of residual kinase activity of PAK4 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435655 | Binding constant for ERK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720298 | Millipore: Percentage of residual kinase activity of CHUK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435561 | Binding constant for SRMS kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624972 | Binding constant for MTOR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720167 | Millipore: Percentage of residual kinase activity of FLT4 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625000 | Binding constant for EGFR(L747-E749del, A750P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624902 | Binding constant for MEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624810 | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436011 | Binding constant for full-length CLK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625133 | Binding constant for CDC2L2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624725 | Binding constant for NEK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720052 | Millipore: Percentage of residual kinase activity of BRSK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624735 | Binding constant for ANKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625020 | Binding constant for ITK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720326 | Millipore: Percentage of residual kinase activity of LIMK1 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID749359 | Induction of cardiomyogenic activity in human embryonic stem cells assessed as cell growth at 5 uM measured on day 15 by FACS analysis | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Tri-substituted imidazole analogues of SB203580 as inducers for cardiomyogenesis of human embryonic stem cells. |
AID624996 | Binding constant for EGFR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624791 | Binding constant for KIT(V559D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624857 | Binding constant for HCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435148 | Binding constant for AMPK-alpha1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435286 | Binding constant for EPHA7 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624827 | Binding constant for CAMK2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256626 | Average Binding Constant for NTRK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720229 | Millipore: Percentage of residual kinase activity of PLK1 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 20 mM DTT | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624704 | Binding constant for NEK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435564 | Binding constant for TRKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256594 | Average Binding Constant for BMX; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720484 | Millipore: Percentage of residual kinase activity of PRKCZ at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720381 | Millipore: Percentage of residual kinase activity of MET at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID436086 | Percentage HIPK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID256565 | Average Binding Constant for MAP4K5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID428918 | Inhibition of Toxoplasma gondii recombinant MAPK1 expressed in Escherichia coli | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection. |
AID435531 | Binding constant for MKNK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435282 | Binding constant for full-length CSNK1G2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435723 | Percentage GSK3-beta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID1224773 | Delta TM value showing the stabilisation of ASK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624974 | Binding constant for PIK3CD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID242316 | Inhibition v-src sarcoma viral oncogene homolog (Src) at 100 uM ATP | 2005 | Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12 | Rapid computational identification of the targets of protein kinase inhibitors. |
AID720431 | Millipore: Percentage of residual kinase activity of EEF2K at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435786 | Binding constant for full-length CLK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1638929 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Design and molecular modeling of novel P38α MAPK inhibitors targeting breast cancer, synthesized from oxygen heterocyclic natural compounds. |
AID624727 | Binding constant for FYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435438 | Binding constant for full-length p38-gamma | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID436021 | Binding constant for LATS2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624792 | Binding constant for KIT(V559D,T670I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720137 | Millipore: Percentage of residual kinase activity of EPHB1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720412 | Millipore: Percentage of residual kinase activity of VRK2 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720164 | Millipore: Percentage of residual kinase activity of FLT1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624998 | Binding constant for EGFR(G719C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720372 | Millipore: Percentage of residual kinase activity of STK4 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624891 | Binding constant for JNK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624858 | Binding constant for JAK1(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435312 | Binding constant for MET kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720105 | Millipore: Percentage of residual kinase activity of CAMK1D at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID251866 | Percent inhibition of staphylococcal enterotoxin B induced TNF-alpha production at 3 mg/kg concentration | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis. |
AID625033 | Binding constant for PCTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256671 | Average Binding Constant for ABL1(Y253F); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720350 | Millipore: Percentage of residual kinase activity of MELK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435520 | Binding constant for CAMK2A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256571 | Average Binding Constant for BIKE; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435691 | Binding constant for SgK085 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID67274 | Inhibition of EGF receptor kinase | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase. |
AID624859 | Binding constant for JAK1(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256614 | Average Binding Constant for YES; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID339972 | Inhibition of human GSK3-beta at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID720151 | Millipore: Percentage of residual kinase activity of FGFR2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720138 | Millipore: Percentage of residual kinase activity of EPHB1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720270 | Millipore: Percentage of residual kinase activity of SGK3 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435277 | Binding constant for full-length CDK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624917 | Binding constant for MST3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID339956 | Inhibition of TNFalpha release in human whole blood | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID624930 | Binding constant for TNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435153 | Binding constant for full-length DAPK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720126 | Millipore: Percentage of residual kinase activity of EPHA2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256616 | Average Binding Constant for CDK5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720028 | Millipore: Percentage of residual kinase activity of NUAK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435783 | Binding constant for full-length BRSK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256583 | Average Binding Constant for CAMKK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624896 | Binding constant for PRKR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436032 | Binding constant for MYO3B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID54228 | Inhibition of Cytochrome P450 1A2 at 10 uM | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15 | Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. |
AID720385 | Millipore: Percentage of residual kinase activity of MUSK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624886 | Binding constant for ERK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256562 | Average Binding Constant for PAK4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID512251 | Inhibition of rabbit MKK1 expressed in Escherichia coli at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID720366 | Millipore: Percentage of residual kinase activity of RPS6KA5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224788 | Delta TM value showing the stabilisation of PIM3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435908 | Binding constant for EPHA2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625061 | Binding constant for MAP4K5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624993 | Binding constant for ABL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224782 | Delta TM value showing the stabilisation of PAK5 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720205 | Millipore: Percentage of residual kinase activity of PRKCI at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720023 | Millipore: Percentage of residual kinase activity of PRKAA1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624987 | Binding constant for ABL1(Q252H)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625005 | Binding constant for EGFR(L861Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625076 | Binding constant for PLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436023 | Binding constant for MERTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720216 | Millipore: Percentage of residual kinase activity of PKN2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435906 | Binding constant for EGFR(L747-T751del,Sins) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720317 | Millipore: Percentage of residual kinase activity of JAK3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256566 | Average Binding Constant for TNIK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624739 | Binding constant for GRK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624809 | Binding constant for MYLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435160 | Binding constant for FER kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256634 | Average Binding Constant for CSNK1G2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID339961 | Inhibition of human MAPK2/ERK2 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID625103 | Binding constant for MST4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256563 | Average Binding Constant for ULK3 m; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID721301 | Inhibition of p38alpha MAP kinase (unknown origin) in presence of 300 uM ATP | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Dibenzosuberones as p38 mitogen-activated protein kinase inhibitors with low ATP competitiveness and outstanding whole blood activity. |
AID435170 | Binding constant for MYO3A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID268710 | Inhibition of p38 | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | The development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-alpha production. |
AID624801 | Binding constant for MAP3K15 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720132 | Millipore: Percentage of residual kinase activity of EPHA5 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224769 | Delta TM value showing the stabilisation of GSK3B produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720060 | Millipore: Percentage of residual kinase activity of CDK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720093 | Millipore: Percentage of residual kinase activity of CSK at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720253 | Millipore: Percentage of residual kinase activity of RPS6KA3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624979 | Binding constant for ABL1(F317I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435327 | Binding constant for VEGFR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435514 | Binding constant for ABL1(M351T) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624708 | Binding constant for CDC2L1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625002 | Binding constant for EGFR(L747-T751del,Sins) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID512252 | Inhibition of Gst-tagged human MAPK2/ERK2 expressed in Escherichia coli at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID435461 | Percentage CK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720471 | Millipore: Percentage of residual kinase activity of AKT3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435515 | Binding constant for ABL1(Q252H) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720171 | Millipore: Percentage of residual kinase activity of FYN at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1337161 | Inhibition of p38beta (unknown origin) | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6 | Non-kinase targets of protein kinase inhibitors. |
AID436083 | Percentage ERK8 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID624799 | Binding constant for TIE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID127085 | Inhibition of Mitogen-activated protein kinase p38 (P38 MAPK) | 2002 | Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21 | Imidazole inhibitors of cytokine release: probing substituents in the 2 position. |
AID219483 | Inhibition of c-Jun N-terminal kinase 2-alpha 1 | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase. |
AID624759 | Binding constant for PFCDPK1(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435651 | Binding constant for DCAMKL2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720115 | Millipore: Percentage of residual kinase activity of DMPK at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1269279 | Activation of p38 in human A549 cells assessed as upregulation of TNF-R1 expression at 100 to 800 ug/ml by Western blot analysis | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | The anti-tumor activity and mechanism of alkaloids from Aconitum szechenyianum Gay. |
AID625098 | Binding constant for IRAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624831 | Binding constant for CHEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435300 | Percentage PAK6 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720343 | Millipore: Percentage of residual kinase activity of MAPKAPK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Na-?-glycerophosphate pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID229247 | Ability to inhibit the release of interleukin-1-beta (IL-1 beta) from whole blood | 2002 | Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21 | Imidazole inhibitors of cytokine release: probing substituents in the 2 position. |
AID720208 | Millipore: Percentage of residual kinase activity of PRKD2 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720390 | Millipore: Percentage of residual kinase activity of NEK3 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720033 | Millipore: Percentage of residual kinase activity of ABL2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID108871 | Effect on LPS-induced TNF-alpha production in mice at 10 mg/kg peroral dose | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor. |
AID720315 | Millipore: Percentage of residual kinase activity of JAK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625097 | Binding constant for TNNI3K kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720112 | Millipore: Percentage of residual kinase activity of DCLK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435326 | Binding constant for TYRO3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720322 | Millipore: Percentage of residual kinase activity of MAPK10 at 1uM relative to control. Control inhibitor: JAK Inhibitor I at 30.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224775 | Delta TM value showing the stabilisation of ERK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID256575 | Average Binding Constant for NEK6; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID1224766 | Delta TM value showing the stabilisation of CK1G3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435666 | Binding constant for full-length NEK7 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435660 | Binding constant for full-length MELK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625100 | Binding constant for NLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624802 | Binding constant for PIM3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625069 | Binding constant for TLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435664 | Binding constant for MYLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625023 | Binding constant for HIPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720279 | Millipore: Percentage of residual kinase activity of STK33 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720177 | Millipore: Percentage of residual kinase activity of GRK6 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224800 | Delta TM value showing the stabilisation of MST4 (2) produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624796 | Binding constant for MET(Y1235D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435962 | Percentage CDK2-cyclinA activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720359 | Millipore: Percentage of residual kinase activity of MYLK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625068 | Binding constant for NEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720140 | Millipore: Percentage of residual kinase activity of EPHB2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720387 | Millipore: Percentage of residual kinase activity of NEK11 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720328 | Millipore: Percentage of residual kinase activity of STK11 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.1% v/v Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID152779 | Inhibitory activity against TNF-alpha release in PBM cells | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15 | Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. |
AID729552 | Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells at 5 uM by TR-FRET based binding assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay. |
AID720463 | Millipore: Percentage of residual kinase activity of PDPK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435195 | Binding constant for SRC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1269282 | Activation of p38 in human A549 cells assessed as upregulation of p53 expression at 100 to 800 ug/ml by Western blot analysis | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | The anti-tumor activity and mechanism of alkaloids from Aconitum szechenyianum Gay. |
AID435795 | Binding constant for EPHA4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435189 | Binding constant for full-length PDPK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624904 | Binding constant for NEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624899 | Binding constant for ROS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID201674 | Inhibition of TNF and IL-1 induced IL-6 production in human chondro-sarcoma SW 1353 cells | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18 | 1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors. |
AID720245 | Millipore: Percentage of residual kinase activity of MST1R at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624960 | Binding constant for RSK2(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720101 | Millipore: Percentage of residual kinase activity of CAMK2D at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720335 | Millipore: Percentage of residual kinase activity of LCK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624842 | Binding constant for BMX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720056 | Millipore: Percentage of residual kinase activity of CDK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720291 | Millipore: Percentage of residual kinase activity of TAOK3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 200 mM NaCl, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720294 | Millipore: Percentage of residual kinase activity of TGFBR1 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720383 | Millipore: Percentage of residual kinase activity of MKNK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720050 | Millipore: Percentage of residual kinase activity of BMX at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625132 | Binding constant for FGFR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720222 | Millipore: Percentage of residual kinase activity of PIM1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435929 | Binding constant for PAK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624887 | Binding constant for ERK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624975 | Binding constant for PLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID329649 | Inhibition of p38-alpha MAPK | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Isoxazolone based inhibitors of p38 MAP kinases. |
AID436034 | Binding constant for PRKCH kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625014 | Binding constant for PRKCE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224757 | Delta TM value showing the stabilisation of CDK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624912 | Binding constant for TYK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256646 | Average Binding Constant for JAK1 (Kin.Dom. 1); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435501 | Percentage SmMLCK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID625112 | Binding constant for YANK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435780 | Binding constant for BMPR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624851 | Binding constant for ERBB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224786 | Delta TM value showing the stabilisation of PIM1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720467 | Millipore: Percentage of residual kinase activity of AKT1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624757 | Binding constant for PKMYT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625015 | Binding constant for ROCK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID476334 | Inhibition of MAPK14 | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Through the "gatekeeper door": exploiting the active kinase conformation. |
AID1224771 | Delta TM value showing the stabilisation of MEK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720262 | Millipore: Percentage of residual kinase activity of MAPK12 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1732391 | Inhibition of p38 alpha (unknown origin) | |||
AID512262 | Inhibition of bovine heart PKA at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID300639 | Inhibition of Tie2 kinase by autophosphorylation assay | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Pyridinylimidazole inhibitors of Tie2 kinase. |
AID1638930 | Antiproliferative activity against human MDA231 cells after 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Design and molecular modeling of novel P38α MAPK inhibitors targeting breast cancer, synthesized from oxygen heterocyclic natural compounds. |
AID435690 | Binding constant for RPS6KA1(Kin.Dom.1 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625016 | Binding constant for SRC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720071 | Millipore: Percentage of residual kinase activity of CDK9 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720108 | Millipore: Percentage of residual kinase activity of DAPK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID114904 | Percent inhibition of TNF-alpha-induced IL-6 production at 100 mg/kg peroral dose in mice | 2002 | Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12 | Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor. |
AID720462 | Millipore: Percentage of residual kinase activity of PDPK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720059 | Millipore: Percentage of residual kinase activity of CDK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720465 | Millipore: Percentage of residual kinase activity of PRKACA at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1269281 | Activation of p38 in human A549 cells assessed as upregulation of phosphorylated p53 expression at 100 to 800 ug/ml by Western blot analysis | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | The anti-tumor activity and mechanism of alkaloids from Aconitum szechenyianum Gay. |
AID435688 | Binding constant for full-length PCTK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624973 | Binding constant for JAK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435290 | Binding constant for FGFR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720182 | Millipore: Percentage of residual kinase activity of GSK3A at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625004 | Binding constant for EGFR(L858R,T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720410 | Millipore: Percentage of residual kinase activity of ULK3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624740 | Binding constant for LRRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720373 | Millipore: Percentage of residual kinase activity of STK4 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720064 | Millipore: Percentage of residual kinase activity of CDK5 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID767908 | Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced IL-12 p40 production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA | 2013 | Journal of natural products, Sep-27, Volume: 76, Issue:9 | Anti-inflammatory asterosaponins from the starfish Astropecten monacanthus. |
AID624958 | Binding constant for PIK3C2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435417 | Percentage PAK4 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720418 | Millipore: Percentage of residual kinase activity of YES1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435528 | Binding constant for IRAK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1475279 | Inhibition of PDE4 in LPS-stimulated human whole blood assessed as decrease in leukotriene B4 level in plasma | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases. |
AID720160 | Millipore: Percentage of residual kinase activity of FES at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720225 | Millipore: Percentage of residual kinase activity of PIM2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID436042 | Binding constant for full-length PHKG1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720119 | Millipore: Percentage of residual kinase activity of DYRK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435796 | Binding constant for ERBB2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID281720 | Inhibition of human liver CYP1A2 at 10 uM | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Tetrasubstituted imidazole inhibitors of cytokine release: probing substituents in the N-1 position. |
AID624883 | Binding constant for PRKCI kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID127243 | Inhibition of Mitogen-activated protein kinase p38 | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase. |
AID280500 | Inhibition of p38-alpha MAPK by non-radioactive immunosorbent assay | 2007 | Journal of medicinal chemistry, Mar-22, Volume: 50, Issue:6 | From five- to six-membered rings: 3,4-diarylquinolinone as lead for novel p38MAP kinase inhibitors. |
AID1869021 | Inhibition of LPS-induced p38 MAPK phosphorylation in mouse RAW264.7 cells pretreated with compound for 2 hrs followed by LPS-stimulation for 30 mins by Western blot analysis | 2022 | Bioorganic & medicinal chemistry, 07-15, Volume: 66 | Discovery of diarylheptanoids that activate α7 nAchR-JAK2-STAT3 signaling in macrophages with anti-inflammatory activity in vitro and in vivo. |
AID720451 | Millipore: Percentage of residual kinase activity of PAK7 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID448705 | Inhibition of p38alpha by Cherenkov counting | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | 3,4-Diaryl-isoxazoles and -imidazoles as potent dual inhibitors of p38alpha mitogen activated protein kinase and casein kinase 1delta. |
AID1224790 | Delta TM value showing the stabilisation of PLK4 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID256657 | Average Binding Constant for LCK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID127069 | Inhibition of p38 MAP kinase related TNF-alpha release from human whole blood | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | From imidazoles to pyrimidines: new inhibitors of cytokine release. |
AID1224780 | Delta TM value showing the stabilisation of OSR1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435318 | Binding constant for PAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624870 | Binding constant for NEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID512271 | Inhibition of His-tagged human CK2 expressed in Sf9 cells at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID1646091 | Inhibition of human CIT | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
AID1224802 | Delta TM value showing the stabilisation of TNIK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720175 | Millipore: Percentage of residual kinase activity of GRK5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID303553 | Inhibition of MK2 mediated HSP27 phosphorylation in immortalised WS cells assessed as reduction in F-actin stress fibres | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Synthesis and in vivo activity of MK2 and MK2 substrate-selective p38alpha(MAPK) inhibitors in Werner syndrome cells. |
AID720483 | Millipore: Percentage of residual kinase activity of PRKCE at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID241943 | Inhibitory concentration against p38 alpha MAP kinase calculated by CoMFA model; FlexX score = -22.2kcal/mol | 2005 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15 | The molecular basis for coxib inhibition of p38alpha MAP kinase. |
AID720255 | Millipore: Percentage of residual kinase activity of RPS6KA2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720380 | Millipore: Percentage of residual kinase activity of MET at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435940 | Binding constant for full-length TSSK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256665 | Average Binding Constant for ABL1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624850 | Binding constant for DDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720094 | Millipore: Percentage of residual kinase activity of CSK at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID395287 | Lipophilicity, CHI in methanol by fast-gradient HPLC | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Aza-analogue dibenzepinone scaffolds as p38 mitogen-activated protein kinase inhibitors: design, synthesis, and biological data of inhibitors with improved physicochemical properties. |
AID720325 | Millipore: Percentage of residual kinase activity of KDR at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256559 | Average Binding Constant for EPHB4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624820 | Binding constant for ACVR2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625008 | Binding constant for EPHA1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720268 | Millipore: Percentage of residual kinase activity of SGK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624720 | Binding constant for HIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224785 | Delta TM value showing the stabilisation of PDK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720338 | Millipore: Percentage of residual kinase activity of MAPK3 at 1uM relative to control. Control inhibitor: ERK Inhibitor II at 30.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID251880 | Percent inhibition of staphylococcal enterotoxin B induced TNF-alpha production at 30 mg/kg concentration | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis. |
AID624822 | Binding constant for CDKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624945 | Binding constant for BMPR1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435163 | Binding constant for full-length GSK3B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224803 | Delta TM value showing the stabilisation of PBK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720221 | Millipore: Percentage of residual kinase activity of PHKG2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435281 | Binding constant for full-length CSNK1A1L | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1527595 | Inhibition of LPS-induced TNFalpha production in human whole blood at 10 uM preincubated for 15 mins followed by LPS stimulation and measured after 2.5 hrs by ELISA relative to control | |||
AID625123 | Binding constant for RET(V804L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1475302 | In vivo inhibition of P38 MAPKalpha in Sprague-Dawley rat assessed as decrease in LPS-stimulated TNFalpha level in serum at 3 mg/kg, po pretreated for 1 hr followed by LPS addition measured after 2 hrs relative to control | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases. |
AID720361 | Millipore: Percentage of residual kinase activity of MAP3K9 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID166072 | Inhibition of RAF kinase | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | Pyrroles and other heterocycles as inhibitors of p38 kinase. |
AID127076 | Binding affinity for human recombinant Mitogen-activated protein kinase p38 in a fluorescent binding assay | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14 | Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
AID624744 | Binding constant for ZAP70 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624971 | Binding constant for DAPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256573 | Average Binding Constant for PAK6; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720349 | Millipore: Percentage of residual kinase activity of MAP2K1 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 50 mM Tris pH 7.5, 0.2 mM EGTA, 0.1% ?-mercaptoethanol, 0.01% Brij-35 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720461 | Millipore: Percentage of residual kinase activity of PDGFRB at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435900 | Binding constant for AKT3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435896 | Binding constant for AAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720273 | Millipore: Percentage of residual kinase activity of SIK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID512253 | Inhibition of Gst-tagged human JNK1a1 expressed in Escherichia coli at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID720330 | Millipore: Percentage of residual kinase activity of STK10 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID436046 | Binding constant for PRKD2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435171 | Binding constant for NEK9 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1053973 | Competitive inhibition of p38alpha MAP kinase (unknown origin) in presence of 100 uM ATP | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Metabolically stable dibenzo[b,e]oxepin-11(6H)-ones as highly selective p38 MAP kinase inhibitors: optimizing anti-cytokine activity in human whole blood. |
AID414669 | Binding affinity to ATP binding site of p38alpha MAP kinase | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Role of the hydrogen bonding heteroatom-Lys53 interaction between the p38alpha mitogen-activated protein (MAP) kinase and pyridinyl-substituted 5-membered heterocyclic ring inhibitors. |
AID625109 | Binding constant for BIKE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625058 | Binding constant for VRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625082 | Binding constant for RSK4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1876034 | Inhibition of MAPK (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1266416 | Induction of cardiogenesis in human embryonic stem cells by DAPI staining based immunofluorescence method relative to control | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24 | Medicinal Chemistry Approaches to Heart Regeneration. |
AID720045 | Millipore: Percentage of residual kinase activity of BTK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID275050 | Inhibition of p38 alpha | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Design, synthesis, and biological evaluation of phenylamino-substituted 6,11-dihydro-dibenzo[b,e]oxepin-11-ones and dibenzo[a,d]cycloheptan-5-ones: novel p38 MAP kinase inhibitors. |
AID720145 | Millipore: Percentage of residual kinase activity of ERBB4 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435926 | Binding constant for PDGFRB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720144 | Millipore: Percentage of residual kinase activity of EPHB4 at 10uM relative to control. Control inhibitor: PP2 at 30.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1409768 | Inhibition of sodium arsenate activated N-terminal GST-tagged Brugia malayi MPK1 expressed in HEK293F cells using FAM-p38tide as substrate by IMAP assay | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3 | Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis. |
AID256604 | Average Binding Constant for STK10; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435802 | Binding constant for KIT(V559D,V654A) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID436020 | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720083 | Millipore: Percentage of residual kinase activity of CSNK1D at 1uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1253624 | Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells assessed as residence time by by fluorescent polarization assay | 2015 | Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21 | Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity. |
AID248830 | Concentration required to inhibit lipopolysaccharide induced TNF-alpha release was determined in human peripheral blood mononuclear cells | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis. |
AID720029 | Millipore: Percentage of residual kinase activity of MAP3K5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720321 | Millipore: Percentage of residual kinase activity of MAPK9 at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720188 | Millipore: Percentage of residual kinase activity of HIPK2 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720309 | Millipore: Percentage of residual kinase activity of IRAK4 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224752 | Delta TM value showing the stabilisation of CAMK2B produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624760 | Binding constant for PFPK5(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624847 | Binding constant for CSNK1E kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID162316 | Inhibitory activity against Prostaglandin G/H synthase 1 (COX-1) | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | Kinase inhibitors: not just for kinases anymore. |
AID625108 | Binding constant for MKNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624755 | Binding constant for ZAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID596313 | Inhibition of p38 alpha MAPK in human whole blood assessed as suppression of LPS-induced TNF-alpha release by immunosorbent non-radioactive enzyme assay | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9 | Chiral sulfoxides as metabolites of 2-thioimidazole-based p38α mitogen-activated protein kinase inhibitors: enantioselective synthesis and biological evaluation. |
AID435168 | Binding constant for LTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720479 | Millipore: Percentage of residual kinase activity of PRKCG at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1269278 | Activation of p38 in human A549 cells assessed as upregulation of DR5 expression at 100 to 800 ug/ml by Western blot analysis | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | The anti-tumor activity and mechanism of alkaloids from Aconitum szechenyianum Gay. |
AID435865 | Percentage MKK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID256611 | Average Binding Constant for RIPK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435556 | Binding constant for RAF1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256592 | Average Binding Constant for LIMK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720464 | Millipore: Percentage of residual kinase activity of PRKACA at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1611955 | Inhibition of tyrosinase in mouse B16F10 cells assessed as reduction in melanin synthesis after 2 hrs by spectrophotometric analysis | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Inhibitors of Melanogenesis: An Updated Review. |
AID435442 | Binding constant for SYK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625079 | Binding constant for NEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720282 | Millipore: Percentage of residual kinase activity of SYK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435427 | Percentage PKBalpha activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID256595 | Average Binding Constant for CLK3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720207 | Millipore: Percentage of residual kinase activity of PRKD1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: mM HEPES pH 7.4, 0.03% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624798 | Binding constant for LKB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224764 | Delta TM value showing the stabilisation of CK1G1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1337162 | Binding affinity to recombinant human His6-TEV protease-tagged BRD4 bromodomain 1 expressed in bacteria assessed as change in melting temperature at 10 uM by SYPRO Orange probe-based Real-Time PCR method | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6 | Non-kinase targets of protein kinase inhibitors. |
AID720248 | Millipore: Percentage of residual kinase activity of TYRO3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID339959 | Inhibition of human c-RAF at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID1876333 | Antiviral activity against hCoV-229e at 4 uM assessed as reduction of viral RNA relative to control | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy. |
AID720084 | Millipore: Percentage of residual kinase activity of CSNK1D at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720382 | Millipore: Percentage of residual kinase activity of MKNK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720469 | Millipore: Percentage of residual kinase activity of AKT2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435653 | Binding constant for EGFR(L747-S752del, P753S) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435932 | Binding constant for PKAC-alpha kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256605 | Average Binding Constant for STK17B; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720310 | Millipore: Percentage of residual kinase activity of INSRR at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720150 | Millipore: Percentage of residual kinase activity of FGFR1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624933 | Binding constant for PLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625024 | Binding constant for PRKD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224751 | Delta TM value showing the stabilisation of CAMK2A produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435223 | Percentage CSK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID300816 | Inhibition of anisomycin-induced P38-alpha activation in human human TERT-immortalised WS cells assessed as HSP27 phosphorylation at 2.5 uM | 2007 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18 | Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells. |
AID625066 | Binding constant for IRAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624703 | Binding constant for MAPKAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256620 | Average Binding Constant for FLT3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID406411 | Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability at 0.125 to 12.5 uM relative to toxin-treated control | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Amiodarone and bepridil inhibit anthrax toxin entry into host cells. |
AID1646094 | Inhibition of human GAK | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
AID435293 | Binding constant for JNK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256591 | Average Binding Constant for EPHA5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720288 | Millipore: Percentage of residual kinase activity of TAOK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720444 | Millipore: Percentage of residual kinase activity of PAK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624716 | Binding constant for CSNK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720358 | Millipore: Percentage of residual kinase activity of MYLK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID436010 | Binding constant for full-length CDK5 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435649 | Binding constant for CDC2L2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625077 | Binding constant for DAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720424 | Millipore: Percentage of residual kinase activity of RAF1 at 1uM relative to control. Control inhibitor: SB203580 at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435296 | Binding constant for MARK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435782 | Binding constant for BRSK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256581 | Average Binding Constant for CAMK1G; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624752 | Binding constant for SNRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224806 | Delta TM value showing the stabilisation of VRK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624817 | Binding constant for MYO3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID729896 | Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced IL6 release at 100 uM incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay relative to control | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Structure-activity relationships of 6-(aminomethylphenoxy)-benzoxaborole derivatives as anti-inflammatory agent. |
AID720214 | Millipore: Percentage of residual kinase activity of MAPKAPK5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Na-?-glycerophosphate pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224767 | Delta TM value showing the stabilisation of DAPK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624840 | Binding constant for AXL kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224761 | Delta TM value showing the stabilisation of CLK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720165 | Millipore: Percentage of residual kinase activity of FLT3 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624776 | Binding constant for PCTK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID248021 | Concentration required to inhibit TNF-alpha production was determined in human whole blood | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase. |
AID720419 | Millipore: Percentage of residual kinase activity of YES1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720184 | Millipore: Percentage of residual kinase activity of GSK3B at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435194 | Binding constant for RPS6KA6(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720409 | Millipore: Percentage of residual kinase activity of ULK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224807 | Delta TM value showing the stabilisation of YSK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435394 | Binding constant for CAMK2B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624750 | Binding constant for PRP4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435439 | Binding constant for PAK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224795 | Delta TM value showing the stabilisation of SLK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1224801 | Delta TM value showing the stabilisation of MST1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720043 | Millipore: Percentage of residual kinase activity of PTK6 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224749 | Delta TM value showing the stabilisation of CAMK1D produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435689 | Binding constant for full-length PFTK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720031 | Millipore: Percentage of residual kinase activity of ABL1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435161 | Binding constant for FES kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID586673 | Activation of Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction at 10 uM after 5 hrs pretreated with MEK1 inhibitor PD98059 for 1 hr before compound addition by Western blot analysis | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Involvement of heme oxygenase-1 induction via Nrf2/ARE activation in protection against H2O2-induced PC12 cell death by a metabolite of sesamin contained in sesame seeds. |
AID720166 | Millipore: Percentage of residual kinase activity of FLT3 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID248535 | Concentration required to inhibit lipopolysaccharide induced TNF-alpha release was determined in human whole blood | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis. |
AID624854 | Binding constant for FLT4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624937 | Binding constant for FLT3(ITD) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720106 | Millipore: Percentage of residual kinase activity of CAMK1D at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435279 | Binding constant for full-length CDK9 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720197 | Millipore: Percentage of residual kinase activity of IGF1R at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720307 | Millipore: Percentage of residual kinase activity of IRAK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720256 | Millipore: Percentage of residual kinase activity of RPS6KA6 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 30 mM NaCl | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID16454 | Calculated partition coefficient (clogP) | 2001 | Bioorganic & medicinal chemistry letters, Jan-08, Volume: 11, Issue:1 | p38 kinase inhibitors for the treatment of arthritis and osteoporosis: thienyl, furyl, and pyrrolyl ureas. |
AID624885 | Binding constant for ERK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624995 | Binding constant for CSF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID512269 | Inhibition of rat ROCK2 expressed in Sf9 cells at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID632578 | Antiinflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated TNF-alpha production preincubated for 1 hr before LPS-stimulation measured after 16 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24 | Chemical constituents of the rhizomes of Hedychium coronarium and their inhibitory effect on the pro-inflammatory cytokines production LPS-stimulated in bone marrow-derived dendritic cells. |
AID303551 | Inhibition of p38 mediated MK2 activation | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Synthesis and in vivo activity of MK2 and MK2 substrate-selective p38alpha(MAPK) inhibitors in Werner syndrome cells. |
AID325677 | Inhibition of p38 MAP kinase in cell based assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624919 | Binding constant for AURKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720073 | Millipore: Percentage of residual kinase activity of CHEK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720130 | Millipore: Percentage of residual kinase activity of EPHA4 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720478 | Millipore: Percentage of residual kinase activity of PRKCG at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624830 | Binding constant for CDK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID201879 | Inhibition of IL-6 production by SW1353 cells treated with both cytokines IL-1 and TNF-alpha. | 2001 | Bioorganic & medicinal chemistry letters, Jan-08, Volume: 11, Issue:1 | p38 kinase inhibitors for the treatment of arthritis and osteoporosis: thienyl, furyl, and pyrrolyl ureas. |
AID256586 | Average Binding Constant for STK4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435939 | Binding constant for TIE2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256608 | Average Binding Constant for MARK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID625075 | Binding constant for INSRR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624742 | Binding constant for NEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224793 | Delta TM value showing the stabilisation of RSK2a produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720036 | Millipore: Percentage of residual kinase activity of AURKA at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl, 0.1% v/v Triton-X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID127097 | Inhibition of Mitogen-activated protein kinase p38 | 2002 | Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5 | Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5). |
AID435738 | Percentage p38delta MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID624825 | Binding constant for BMPR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720476 | Millipore: Percentage of residual kinase activity of PRKCB at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720377 | Millipore: Percentage of residual kinase activity of STK24 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1646093 | Inhibition of human DMPK | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
AID625080 | Binding constant for EIF2AK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624746 | Binding constant for WEE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID761522 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced iNOS expression at 10 uM after 24 hrs by Western blot analysis | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Inhibitory effect of resveratrol dimerized derivatives on nitric oxide production in lipopolysaccharide-induced RAW 264.7 cells. |
AID624915 | Binding constant for PIP5K2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720051 | Millipore: Percentage of residual kinase activity of BRSK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1646076 | Inhibition of human JNK3 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
AID243492 | Inhibition of ephrin-B1-mediated EPH receptor B2 autophosphorylation | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | Frontal affinity chromatography with MS detection of EphB2 tyrosine kinase receptor. 2. Identification of small-molecule inhibitors via coupling with virtual screening. |
AID256615 | Average Binding Constant for p38-gamma; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID625036 | Binding constant for PIK3CA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625113 | Binding constant for MARK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720402 | Millipore: Percentage of residual kinase activity of NTRK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720369 | Millipore: Percentage of residual kinase activity of RPS6KA4 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1053969 | Competitive inhibition of p38alpha MAP kinase (unknown origin) in presence of 300 uM ATP | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Metabolically stable dibenzo[b,e]oxepin-11(6H)-ones as highly selective p38 MAP kinase inhibitors: optimizing anti-cytokine activity in human whole blood. |
AID720450 | Millipore: Percentage of residual kinase activity of PAK7 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID448706 | Inhibition of CK1delta by Cherenkov counting in presence of 20 uM ATP | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | 3,4-Diaryl-isoxazoles and -imidazoles as potent dual inhibitors of p38alpha mitogen activated protein kinase and casein kinase 1delta. |
AID625006 | Binding constant for EGFR(S752-I759del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625118 | Binding constant for CAMK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720313 | Millipore: Percentage of residual kinase activity of ITK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435201 | Binding constant for TRKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256673 | Average Binding Constant for PAK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID625045 | Binding constant for PIK3CA(Q546K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720468 | Millipore: Percentage of residual kinase activity of AKT2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256580 | Average Binding Constant for CAMKK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720017 | Millipore: Percentage of residual kinase activity of TNK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720021 | Millipore: Percentage of residual kinase activity of ACVR1B at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720240 | Millipore: Percentage of residual kinase activity of ROCK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720306 | Millipore: Percentage of residual kinase activity of IRAK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224758 | Delta TM value showing the stabilisation of CDK6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID720088 | Millipore: Percentage of residual kinase activity of CSNK2A2 at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 20 mM HEPES pH 7.6, 0.15 M NaCl, 0.1 mM EDTA, 5 mM DTT, 0.1% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID729550 | Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells by TR-FRET based binding assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay. |
AID720217 | Millipore: Percentage of residual kinase activity of PKN2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID436005 | Binding constant for ANKK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720163 | Millipore: Percentage of residual kinase activity of FLT1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID512260 | Inhibition of His-tagged human MSK1 expressed in Sf9 cells at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID435454 | Percentage CaMKKalpha activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID625121 | Binding constant for RET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720123 | Millipore: Percentage of residual kinase activity of EPHA1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224805 | Delta TM value showing the stabilisation of VRK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID281724 | Inhibition of human liver CYP3A4 at 10 uM | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Tetrasubstituted imidazole inhibitors of cytokine release: probing substituents in the N-1 position. |
AID1224748 | Delta TM value showing the stabilisation of AMPKA2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1437535 | Anti-inflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-induced IL-6 production pretreated for 1 hr followed by LPS-stimulation after 18 hrs by ELISA | 2017 | Journal of natural products, 01-27, Volume: 80, Issue:1 | Isochromans and Related Constituents from the Endophytic Fungus Annulohypoxylon truncatum of Zizania caduciflora and Their Anti-Inflammatory Effects. |
AID625102 | Binding constant for PRKD2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435188 | Binding constant for PAK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1716409 | Binding affinity to Nluc-tagged MAPK14 (unknown origin) expressed in HeLa cells assessed as change in melting temperature at 50 uM by NaLTSA assay (Rvb = 50.2 degreeC) | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID256625 | Average Binding Constant for PAK3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624888 | Binding constant for ERK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435938 | Binding constant for TGFBR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435907 | Binding constant for EGFR(L861Q) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID428944 | Antiprotozoal activity against 2000Toxoplasma gondii RH tachyzoites infected 30 days after initial 20 parasite infection in CBA/J mouse assessed as mouse survival time at 60 mg/kg, ip administered 2 hrs postinfection for 7 consecutive days | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection. |
AID624771 | Binding constant for TLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624768 | Binding constant for SRPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435525 | Binding constant for EGFR(L858R) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1876234 | Antiviral activity against MERS-CoV infected in human HUh-7 cells at 10 uM measured after 1 to 24 hrs, pi | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID435793 | Binding constant for EPHA1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID241741 | Inhibitory concentration against alpha mitogen activated protein kinase p38 activity | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21 | Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase. |
AID720267 | Millipore: Percentage of residual kinase activity of SGK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256656 | Average Binding Constant for p38-alpha; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID436052 | Binding constant for full-length SNF1LK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720097 | Millipore: Percentage of residual kinase activity of CAMK2B at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624922 | Binding constant for CAMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436076 | Percentage DYRK1A activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID624877 | Binding constant for PIK3C2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624741 | Binding constant for LRRK2(G2019S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720285 | Millipore: Percentage of residual kinase activity of MAP3K7 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720466 | Millipore: Percentage of residual kinase activity of AKT1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256663 | Average Binding Constant for INSR; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID625089 | Binding constant for AAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624911 | Binding constant for TXK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624734 | Binding constant for YANK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720254 | Millipore: Percentage of residual kinase activity of RPS6KA2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435315 | Percentage MARK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID435225 | Percentage DYRK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID720357 | Millipore: Percentage of residual kinase activity of MAP2K7 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol, 0.1 mM Na3VO4 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID164793 | Inhibition of Protein kinase A at 5 uM | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | 6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2, 3-b]pyridine (RWJ 68354): a potent and selective p38 kinase inhibitor. |
AID720103 | Millipore: Percentage of residual kinase activity of CAMK4 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 40 mM HEPES pH 7.4, 5 mM CaCl2, 30 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1224789 | Delta TM value showing the stabilisation of PLK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435559 | Binding constant for SNARK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256567 | Average Binding Constant for EPHA6; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435260 | Percentage RSK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID390237 | Inhibition of Tat-induced HIV1 LTR transactivation in human HeLa cells assessed as CAT expression after 2 days | 2008 | Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22 | Novel piperidinylpyrimidine derivatives as inhibitors of HIV-1 LTR activation. |
AID625092 | Binding constant for NDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625037 | Binding constant for PIK3CA(C420R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720320 | Millipore: Percentage of residual kinase activity of MAPK9 at 1uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID436044 | Binding constant for PLK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624856 | Binding constant for GSK3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720265 | Millipore: Percentage of residual kinase activity of MAPK13 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435648 | Binding constant for CAMKK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625091 | Binding constant for MAST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256593 | Average Binding Constant for NEK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624788 | Binding constant for KIT(D816H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720066 | Millipore: Percentage of residual kinase activity of CDK5 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID322017 | Inhibition of LPS-induced TNFalpha production in human THP1 cells | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors. |
AID720200 | Millipore: Percentage of residual kinase activity of PRKCH at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID241699 | Inhibition of human RAF kinase at 100 uM ATP | 2005 | Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12 | Rapid computational identification of the targets of protein kinase inhibitors. |
AID720159 | Millipore: Percentage of residual kinase activity of FES at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256618 | Average Binding Constant for PHkg2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID256574 | Average Binding Constant for STK3_m; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720355 | Millipore: Percentage of residual kinase activity of MAP2K6 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol, 0.1 mM Na3VO4, 1 mg/mL BSA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720422 | Millipore: Percentage of residual kinase activity of DAPK3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720404 | Millipore: Percentage of residual kinase activity of NTRK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435555 | Binding constant for PRKR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435558 | Binding constant for RPS6KA3(Kin.Dom.1 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435404 | Binding constant for EPHB4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624738 | Binding constant for MLCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720226 | Millipore: Percentage of residual kinase activity of PIM3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.1% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435287 | Binding constant for EPHA8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID428916 | Antiprotozoal activity against 5 MOI Toxoplasma gondii Me49 tachyzoites infected in confluent HFF assessed as inhibition of [3H]uracil incorporation into tachyzoites treated 4 hrs after infection measured after overnight incubation post uracil addition by | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection. |
AID435295 | Binding constant for MAP4K3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435935 | Binding constant for RIPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1876281 | Inhibition of SAPK2a/p38 (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID720061 | Millipore: Percentage of residual kinase activity of CDK3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435613 | Percentage MNK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID625049 | Binding constant for PRKCH kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435532 | Binding constant for MST3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1513832 | Inhibition of BRD4 bromodomain 1 in human A549 cells assessed as reduction in TNFalpha-induced NFkappaB transcription at 1 to 25 uM after 8 hrs by bright-glo luciferase reporter gene assay relative to control | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. |
AID435339 | Percentage CaMKKbeta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID624939 | Binding constant for FLT3(N841I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID110755 | In vivo inhibition of LPS-induced TNF production in mice 50 mg/Kg. | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | 1-substituted 4-aryl-5-pyridinylimidazoles: a new class of cytokine suppressive drugs with low 5-lipoxygenase and cyclooxygenase inhibitory potency. |
AID435395 | Binding constant for CDC2L1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID303556 | Inhibition of p38 mediated MK2 activation in WS cells | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Synthesis and in vivo activity of MK2 and MK2 substrate-selective p38alpha(MAPK) inhibitors in Werner syndrome cells. |
AID300640 | Inhibition of P38 kinase | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Pyridinylimidazole inhibitors of Tie2 kinase. |
AID436024 | Binding constant for MRCKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256606 | Average Binding Constant for STK16; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID586674 | Activation of Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction at 10 uM after 5 hrs pretreated with MEK2 inhibitor U0126 for 1 hr before compound addition by Western blot analysis | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Involvement of heme oxygenase-1 induction via Nrf2/ARE activation in protection against H2O2-induced PC12 cell death by a metabolite of sesamin contained in sesame seeds. |
AID435521 | Binding constant for CAMKK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256635 | Average Binding Constant for CAMK2D; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID224150 | Inhibition of p56 Lck tyrosine kinase at 5 uM | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | 6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2, 3-b]pyridine (RWJ 68354): a potent and selective p38 kinase inhibitor. |
AID624748 | Binding constant for EPHA6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256601 | Average Binding Constant for EPHA3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624726 | Binding constant for HIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720287 | Millipore: Percentage of residual kinase activity of TAOK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720063 | Millipore: Percentage of residual kinase activity of CDK5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID625003 | Binding constant for EGFR(L858R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435534 | Binding constant for NEK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID751228 | Inhibition of p38 MAPK-induced COX-2 expression in rat IEC-18 cells at 10 uM incubated for 1 hr prior to LPS challenge measured after 24 hrs by Western blot analysis | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6 | Oleuropein protects against dextran sodium sulfate-induced chronic colitis in mice. |
AID435527 | Binding constant for FGFR3(G697C) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID732719 | Antiinflammatory activity in wild-type C57BL/6 mouse BMDCs assessed as inhibition of IL-12 p40 production incubated for 1 hr prior to LPS challenge measured after 16 hrs by ELISA | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Pyrrole and furan oligoglycosides from the starfish Asterina batheri and their inhibitory effect on the production of pro-inflammatory cytokines in lipopolysaccharide-stimulated bone marrow-derived dendritic cells. |
AID435405 | Binding constant for ERK8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720068 | Millipore: Percentage of residual kinase activity of CDK6 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720456 | Millipore: Percentage of residual kinase activity of PASK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720435 | Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID668562 | Antiinflammatory activity in PMA-stimulated human HL60 cells assessed as inhibition of LPS-induced IL-6 production preincubated for 30 mins before LPS challenge measured after 24 hrs by ELISA | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and biological evaluation of 4-alkoxy-6,9-dichloro[1,2,4]triazolo[4,3-a]quinoxalines as inhibitors of TNF-α and IL-6. |
AID1224779 | Delta TM value showing the stabilisation of NEK6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID256599 | Average Binding Constant for TTK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720470 | Millipore: Percentage of residual kinase activity of AKT3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435496 | Percentage RIP2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID624728 | Binding constant for NIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624737 | Binding constant for EPHA5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720186 | Millipore: Percentage of residual kinase activity of HIPK1 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720472 | Millipore: Percentage of residual kinase activity of PRKCA at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624774 | Binding constant for QSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625060 | Binding constant for CAMKK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720046 | Millipore: Percentage of residual kinase activity of BTK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720252 | Millipore: Percentage of residual kinase activity of RPS6KA3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435310 | Binding constant for FLT3(ITD) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720340 | Millipore: Percentage of residual kinase activity of MAPK1 at 1uM relative to control. Control inhibitor: ERK Inhibitor II at 30.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID256588 | Average Binding Constant for PCTK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID720305 | Millipore: Percentage of residual kinase activity of INSR at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID339980 | Inhibition of p38alpha | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
AID1309963 | Inhibition of RIP2K in Pam2CSK4-stimulated HEK-293 cells over-expressing TLR2 assessed as IL8 secretion | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase. |
AID435924 | Binding constant for MARK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435519 | Binding constant for AURKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID436043 | Binding constant for PKMYT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624843 | Binding constant for CAMK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID512270 | Inhibition of rat liver AMPK at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID624710 | Binding constant for SRMS kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625012 | Binding constant for GAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1451484 | Binding affinity to wild type human biotin labelled p38 alpha (9 to 352 residues) expressed in sf21 insect cells assessed as dissociation rate constant by SPR analysis | |||
AID219491 | Inhibition of c-Jun N-terminal kinase 2-beta 1 | 1998 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19 | Pyrroles and other heterocycles as inhibitors of p38 kinase. |
AID624782 | Binding constant for FGFR3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256654 | Average Binding Constant for FGFR2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435159 | Binding constant for EPHB3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624898 | Binding constant for GRK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1071888 | Inhibition of TNFalpha-induced COX2 gene expression in HUVEC at 10 uM | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5 | Syntheses and structure-activity relationships for some triazolyl p38α MAPK inhibitors. |
AID720337 | Millipore: Percentage of residual kinase activity of LYN at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720075 | Millipore: Percentage of residual kinase activity of CHEK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720077 | Millipore: Percentage of residual kinase activity of CSNK1G1 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID495061 | Inhibition of JAK-mediated interferon-gamma/anisomycin-induced Stat1 phosphorylation in human U937 cells by Phospho-Flow cytometry | 2008 | Nature chemical biology, Feb, Volume: 4, Issue:2 | High-content single-cell drug screening with phosphospecific flow cytometry. |
AID444254 | Inhibition of JNK3 by nonradioactive JNK3 assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Pyridinylquinoxalines and pyridinylpyridopyrazines as lead compounds for novel p38 alpha mitogen-activated protein kinase inhibitors. |
AID607539 | Inhibition of LPS-induced TNFalpha production in human whole blood after 24 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14 | Indolin-2-one p38α inhibitors I: design, profiling and crystallographic binding mode. |
AID1540338 | Inhibition of recombinant human full-length N-terminal GST-tagged P38 alpha MAPK expressed in baculovirus infected Sf9 insect cells using p38 peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins in presen | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of potent p38α MAPK inhibitors through a funnel like workflow combining in silico screening and in vitro validation. |
AID720168 | Millipore: Percentage of residual kinase activity of FLT4 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435407 | Binding constant for FLT3(D835Y) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256639 | Average Binding Constant for PHkg1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID1224778 | Delta TM value showing the stabilisation of NEK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624895 | Binding constant for MEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624929 | Binding constant for BRSK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720336 | Millipore: Percentage of residual kinase activity of LYN at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID512263 | Inhibition of His-tagged human PKCalpha expressed in Escherichia coli at 10 uM | 2000 | The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1 | Specificity and mechanism of action of some commonly used protein kinase inhibitors. |
AID720250 | Millipore: Percentage of residual kinase activity of RPS6KA1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID1876162 | Cytotoxicity against human L132 cells | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID435162 | Binding constant for FLT3(N841I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID720365 | Millipore: Percentage of residual kinase activity of CDC42BPB at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID624844 | Binding constant for CDK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID720440 | Millipore: Percentage of residual kinase activity of NEK7 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID720231 | Millipore: Percentage of residual kinase activity of PLK3 at 10uM relative to control. Control inhibitor: Wortmannin at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
AID435228 | Percentage ERK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
AID435402 | Binding constant for EGFR(G719S) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624874 | Binding constant for PCTK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID89421 | Inhibition of p38 MAP kinase related interleukin (IL1-beta (cytokine) release from human whole blood | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | From imidazoles to pyrimidines: new inhibitors of cytokine release. |
AID624715 | Binding constant for ERK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625021 | Binding constant for LIMK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID152778 | Inhibitory activity against induction of IL-1-beta release in PBMCs | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15 | Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. |
AID1347149 | Furin counterscreen qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347152 | Confirmatory screen NINDS AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347153 | Confirmatory screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347161 | Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347169 | Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Identification of potent Yes1 kinase inhibitors using a library screening approach. |
AID1347168 | HepG2 cells viability qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347167 | Vero cells viability qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID493040 | Navigating the Kinome | 2011 | Nature chemical biology, Apr, Volume: 7, Issue:4 | Navigating the kinome. |
AID1797316 | Thermal Denaturation Assay from Article 10.1021/jm030121k: \\Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796).\\ | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22 | Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). |
AID1797364 | Kinase Inhibition Assay from Article 10.1016/s0969-2126(98)00113-0: \\Structural basis of inhibitor selectivity in MAP kinases.\\ | 1998 | Structure (London, England : 1993), Sep-15, Volume: 6, Issue:9 | Structural basis of inhibitor selectivity in MAP kinases. |
AID1797365 | Enzyme Inhibition Scintillation Proximity Assay from Article 10.1038/nsb949: \\Structural basis for p38alpha MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity.\\ | 2003 | Nature structural biology, Sep, Volume: 10, Issue:9 | Structural basis for p38alpha MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity. |
AID1799909 | P38 MAP Kinase Assay from Article 10.1021/cc1000488: \\One-pot synthesis of 4,6-diaryl-2-oxo(imino)-1,2-dihydropyridine-3-carbonitrile; a New Scaffold for p38alpha MAP kinase inhibition.\\ | 2010 | Journal of combinatorial chemistry, Jul-12, Volume: 12, Issue:4 | One-pot synthesis of 4,6-diaryl-2-oxo(imino)-1,2-dihydropyridine-3-carbonitrile; a New Scaffold for p38alpha MAP kinase inhibition. |
AID1797017 | p38alpha Kinase Enzyme Assay from Article 10.1021/jm049575n: \\Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation.\\ | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2 | Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation. |
AID1797386 | Enzyme Inhibition Assay from Article 10.1016/j.bmcl.2003.12.023: \\Benzimidazolone p38 inhibitors.\\ | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Benzimidazolone p38 inhibitors. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 1998 | Protein science : a publication of the Protein Society, Nov, Volume: 7, Issue:11 | A single amino acid substitution makes ERK2 susceptible to pyridinyl imidazole inhibitors of p38 MAP kinase. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 1998 | Protein science : a publication of the Protein Society, Nov, Volume: 7, Issue:11 | A single amino acid substitution makes ERK2 susceptible to pyridinyl imidazole inhibitors of p38 MAP kinase. |
AID1345334 | Human mitogen-activated protein kinase 11 (p38 subfamily) | 1998 | Chemistry & biology, Jun, Volume: 5, Issue:6 | Conversion of SB 203580-insensitive MAP kinase family members to drug-sensitive forms by a single amino-acid substitution. |
AID1345304 | Human mitogen-activated protein kinase 14 (p38 subfamily) | 1998 | Chemistry & biology, Jun, Volume: 5, Issue:6 | Conversion of SB 203580-insensitive MAP kinase family members to drug-sensitive forms by a single amino-acid substitution. |
[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 | 242 (7.04) | 18.2507 |
2000's | 1890 (55.01) | 29.6817 |
2010's | 1221 (35.54) | 24.3611 |
2020's | 83 (2.42) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.
| This Compound (36.60) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 4 (0.11%) | 5.53% |
Reviews | 19 (0.54%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 3,466 (99.34%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |