nintedanib : A member of the class of oxindoles that is a kinase inhibitor used (in the form of its ethylsulfonate salt) for the treatment of idiopathic pulmonary fibrosis and cancer. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
ID Source | ID |
---|---|
PubMed CID | 135423438 |
CHEMBL ID | 2136735 |
CHEBI ID | 85164 |
CHEBI ID | 91413 |
SCHEMBL ID | 431007 |
SCHEMBL ID | 431006 |
SCHEMBL ID | 1535871 |
MeSH ID | M0549010 |
Synonym |
---|
HY-50904 |
cid 9809715 |
vargatef |
nintedanib |
intedanib |
bibf-1120 |
bibf 1120 , |
chebi:85164 , |
bibf1120 |
AKOS005145820 |
928326-83-4 |
1160294-26-7 |
BCP9000405 |
(z)-methyl 3-((4-(n-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxylate |
hsdb 8339 |
methyl (3z)-3-(((4-(n-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylidene)-2-oxo-2,3-dihydro-1h-indole-6-carboxylate |
nintedanib [usan:inn] |
unii-g6hrd2p839 |
g6hrd2p839 , |
656247-17-5 |
FT-0670358 |
HMS3244B14 |
HMS3244B10 |
HMS3244B06 |
bibf1120,vargatef |
D10481 |
nintedanib (usan/inn) |
NCGC00263156-02 |
NCGC00263156-01 |
AM84929 |
CS-0104 |
S1010 |
gtpl5936 |
BRD-K49075727-001-01-0 |
methyl (3z)-3-[({4-[n-methyl-2-(4-methylpiperazin-1-yl)acetamido]phenyl}amino)(phenyl)methylidene]-2-oxo-2,3-dihydro-1h-indole-6-carboxylate |
nintedanib [who-dd] |
intedanib [mi] |
nintedanib [vandf] |
nintedanib [usan] |
nintedanib component of ofev |
nintedanib [inn] |
ofev component nintedanib |
SCHEMBL431007 |
SCHEMBL431006 |
smr004701273 |
MLS006010165 |
J-502642 |
XZXHXSATPCNXJR-ZIADKAODSA-N |
3-z-[1-(4-(n-((4-methyl-piperazin-1-yl)-methylcarbonyl)-n-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone |
SCHEMBL1535871 |
CHEMBL2136735 |
methyl (3z)-3-[(4-{methyl[(4-methylpiperazin-1-yl)acetyl]amino}anilino)(phenyl)methylidene]-2-oxo-2,3-dihydro-1h-indole-6-carboxylate |
KS-1434 |
AC-25071 |
nintedanib (bibf 1120) |
mfcd11974012 |
AKOS025401745 |
DB09079 |
AKOS026750205 |
EX-A341 |
bdbm50026612 |
methyl (3z)-3-[[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]anilino]-phenylmethylidene]-2-oxo-1h-indole-6-carboxylate |
CHEBI:91413 |
HMS3654A05 |
bdbm445209 |
us10669235, nintedanib |
1h-indole-6-carboxylic acid, 2,3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-, methyl ester, (3z)-; 1h-indole-6-carboxylic acid, 2,3-dihydro-3-[[[4-[methyl[(4-methyl-1-piperazinyl)acetyl]amino]phenyl]a |
NCGC00389321-03 |
SW218301-2 |
methyl 2-hydroxy-3-[(4-{methyl[(4-methylpiperazin-1-yl)acetyl]amino}anilino)(phenyl)methylidene]-3h-indole-6-carboxylate |
DTXSID20918936 |
FT-0772497 |
Q27163267 |
3-[[4-[methyl-[2-(4-methyl-1-piperazinyl)-1-oxoethyl]amino]anilino]-phenylmethylidene]-2-oxo-1h-indole-6-carboxylic acid methyl ester |
(z)-methyl 3-((4-(n-methyl-2-(4-methylpiperazin-1-yl)acetamido)-phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxylate |
BCP01744 |
BCP09316 |
vargatef base |
EX-A2818 |
Q15149723 |
SB11190 |
HMS3295K01 |
(z)-methyl 3-(((4-(n-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate |
AMY9163 |
CCG-264775 |
NCGC00263156-14 |
methyl 2-hydroxy-3-[n-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-c-phenylcarbonimidoyl]-1h-indole-6-carboxylate |
nsc757442 |
nsc756659 |
nsc800805 |
nsc-757442 |
nsc-756659 |
nsc-800805 |
NCGC00263156-13 |
nintedanib- bio-x |
BN164249 |
DTXSID201025948 |
nintedanib (free base) |
nintedanib, free base |
EN300-188528 |
methyl 3-[({4-[n-methyl-2-(4-methylpiperazin-1-yl)acetamido]phenyl}amino)(phenyl)methylidene]-2-oxo-2,3-dihydro-1h-indole-6-carboxylate |
Z2756516920 |
1h-indole-6-carboxylic acid, 2,3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-, methyl ester |
Nintedanib (N.T.B) is an orally administered tyrosine kinase inhibitor that has been approved recently by U.S.F.A for idiopathic pulmonary fibrosis (I.P.F) and systemic sclerosis-associated interstitial lung disease (S.Sc-I.L.D). NintedAnib is an antifibrotic drug that has an inhibitory effect on growth factor tyrosin kinases.
Nintedanib has a beneficial effect on slowing disease progression in patients with IPF. The drug has a low potential for drug-drug interactions, especially with drugs metabolised by cytochrome P450 enzymes.
Nintedanib (NTD) has been shown to be effective in systemic sclerosis (SSc)-interstitial lung disease (ILD) The drug has been approved for the treatment of idiopathic pulmonary fibrosis.
Nintedanib can inhibit processes involved in the progression of fibrosis. It can reduce the decline in forced vital capacity in patients with idiopathic pulmonary fibrosis (IPF)
Excerpt | Reference |
---|---|
"As nintedanib may cause foetal harm, patients taking nintedanib should avoid pregnancy." | ( A Drug-Drug Interaction Study to Investigate the Effect of Nintedanib on the Pharmacokinetics of Microgynon (Ethinylestradiol and Levonorgestrel) in Female Patients with Systemic Sclerosis-Associated Interstitial Lung Disease. Avis, M; Gahlemann, M; Guillén-Del-Castillo, A; Kreuter, M; Mack, SR; Marzin, K; Vonk, MC; Wind, S, 2022) |
"Nintedanib can inhibit processes involved in the progression of fibrosis and can reduce the decline in forced vital capacity in patients with idiopathic pulmonary fibrosis (IPF) and fibrotic-interstitial lung disease (fibrotic-ILDs). " | ( The safety of nintedanib for the treatment of interstitial lung disease: A systematic review and meta-analysis of randomized controlled trials. Chen, CH; Lai, CC; Lin, HC; Lin, YS; Wang, CY; Wang, YH, 2021) |
Nintedanib is a licensed treatment for pulmonary fibrosis in adults. Treatment with nintedAnib may slow decline in lung function, decrease the frequency of exacerbations, and improve quality of life in subjects with IPF. Nintinganib treatment has shown to be a promising approach for prostate cancer therapy.
Nintedanib is effective and safe in patients with IPF aged >80 years. No significant differences were found when clinical outcomes were compared with those of younger patients. Placebo-controlled trials showed that the adverse event profile was characterised mainly by gastrointestinal events, particularly diarrhoea.
A population pharmacokinetic model was developed for nintedanib in patients with non-small cell lung cancer (NSCLC) or idiopathic pulmonary fibrosis (IPF) Pharmacokinetic analysis indicated oral-delivered nintinganib plasma exposure and lung tissue partitioning were not dose-proportional and resulting lung levels were substantially higher than blood.
Nintedanib is a triple angiokinase inhibitor that has been approved by the European Agency Medicines (EMA) in combination with docetaxel for the treatment of adult patients with locally advanced, metastatic or locally recurrent lung cancer.
Nintedanib esylate is a kinase inhibitor designated for the cure of non-small cell lung cancer suffered from first-pass metabolism.
In children and adolescents with fibrosing ILD, a weight-based dosing regimen resulted in exposure to nintedanib similar to adults and an acceptable safety profile. Annual rate of decline in forced vital capacity and the duration of ninteganib administration were not significantly different between groups with and without dosage reduction.
Pathway | Proteins | Compounds |
---|---|---|
Endometrial cancer | 0 | 4 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
PPM1D protein | Homo sapiens (human) | Potency | 16.5388 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 3.3786 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
EWS/FLI fusion protein | Homo sapiens (human) | Potency | 1.4225 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
tyrosine-protein kinase Yes | Homo sapiens (human) | Potency | 0.0056 | 0.0000 | 5.0182 | 79.2586 | AID686947; AID686948 |
Interferon beta | Homo sapiens (human) | Potency | 16.5388 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
[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) |
---|---|---|---|---|---|---|---|
Serine/threonine-protein kinase Chk1 | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0001 | 0.4530 | 8.8300 | AID1662309 |
Epidermal growth factor receptor | Homo sapiens (human) | IC50 (µMol) | 30.0000 | 0.0000 | 0.5369 | 10.0000 | AID397043; AID507197 |
Receptor tyrosine-protein kinase erbB-2 | Homo sapiens (human) | IC50 (µMol) | 30.0000 | 0.0001 | 0.5453 | 10.0000 | AID397044; AID507198 |
Platelet-derived growth factor receptor beta | Mus musculus (house mouse) | IC50 (µMol) | 0.0850 | 0.0018 | 0.7552 | 9.5000 | AID1504565 |
Insulin receptor | Homo sapiens (human) | IC50 (µMol) | 7.0000 | 0.0017 | 0.8479 | 10.0000 | AID397040; AID507195 |
Tyrosine-protein kinase Lck | Homo sapiens (human) | IC50 (µMol) | 0.0160 | 0.0002 | 1.3173 | 10.0000 | AID397077; AID507203 |
Cyclin-dependent kinase 1 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0004 | 1.3452 | 10.0000 | AID397041; AID507199 |
Tyrosine-protein kinase Lyn | Homo sapiens (human) | IC50 (µMol) | 0.1483 | 0.0002 | 0.5594 | 5.2000 | AID1662305; AID397078; AID507204 |
Insulin-like growth factor 1 receptor | Homo sapiens (human) | IC50 (µMol) | 5.5000 | 0.0003 | 0.4308 | 8.0000 | AID397039; AID507196 |
Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0001 | 1.7536 | 10.0000 | AID1662309 |
Platelet-derived growth factor receptor beta | Homo sapiens (human) | IC50 (µMol) | 0.0133 | 0.0006 | 0.8007 | 8.5000 | AID1427154; AID1501068; AID1504563; AID1662299; AID507194; AID761354 |
Fibroblast growth factor receptor 1 | Homo sapiens (human) | IC50 (µMol) | 0.0680 | 0.0002 | 0.9420 | 10.0000 | AID1427162; AID1501094; AID1504562; AID1662303; AID1845296; AID1876271; AID397047; AID507189; AID761353 |
Cyclin-dependent kinase 4 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0006 | 0.5706 | 10.0000 | AID397042; AID507201 |
Proto-oncogene tyrosine-protein kinase Src | Homo sapiens (human) | IC50 (µMol) | 0.1093 | 0.0002 | 0.5335 | 10.0000 | AID1662304; AID397076; AID507205 |
Platelet-derived growth factor receptor alpha | Homo sapiens (human) | IC50 (µMol) | 0.0170 | 0.0001 | 0.4912 | 10.0000 | AID1427161; AID1501092; AID397048; AID507193; AID761356 |
Vascular endothelial growth factor receptor 1 | Homo sapiens (human) | IC50 (µMol) | 0.0395 | 0.0001 | 0.2914 | 7.0000 | AID1427159; AID1510861; AID1662300; AID397049; AID507185 |
Fibroblast growth factor receptor 2 | Homo sapiens (human) | IC50 (µMol) | 0.0370 | 0.0004 | 0.3276 | 8.6200 | AID1845297; AID1876272; AID507190 |
Fibroblast growth factor receptor 4 | Homo sapiens (human) | IC50 (µMol) | 0.6100 | 0.0008 | 0.6217 | 8.6200 | AID1845299; AID507192 |
Fibroblast growth factor receptor 3 | Homo sapiens (human) | IC50 (µMol) | 0.1080 | 0.0004 | 0.2863 | 8.6200 | AID1845298; AID1876273; AID507191 |
Cyclin-dependent kinase 2 | Homo sapiens (human) | IC50 (µMol) | 5.5000 | 0.0004 | 1.0444 | 10.0000 | AID1662307; AID507200 |
Platelet-derived growth factor receptor alpha | Mus musculus (house mouse) | IC50 (µMol) | 0.0850 | 0.0018 | 0.8572 | 9.5000 | AID1504565 |
Vascular endothelial growth factor receptor 3 | Homo sapiens (human) | IC50 (µMol) | 0.0116 | 0.0001 | 0.2264 | 4.9000 | AID1427160; AID1501093; AID1510862; AID397050; AID507188 |
Vascular endothelial growth factor receptor 2 | Mus musculus (house mouse) | IC50 (µMol) | 0.0130 | 0.0015 | 0.3672 | 5.1286 | AID507186 |
Vascular endothelial growth factor receptor 2 | Homo sapiens (human) | IC50 (µMol) | 0.0090 | 0.0000 | 0.4830 | 8.8000 | AID1427153; AID1478069; AID1501066; AID1504564; AID1510860; AID1662298; AID397037; AID507187; AID761355 |
Receptor-type tyrosine-protein kinase FLT3 | Homo sapiens (human) | IC50 (µMol) | 0.0260 | 0.0001 | 0.3275 | 9.5480 | AID397079; AID507202 |
Serine/threonine-protein kinase PLK1 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0001 | 0.7734 | 9.0000 | AID397045 |
Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 0.0026 | 0.0009 | 1.9014 | 10.0000 | AID1504566 |
Maternal embryonic leucine zipper kinase | Homo sapiens (human) | IC50 (µMol) | 0.0430 | 0.0004 | 0.3577 | 0.7600 | AID1474637 |
Maternal embryonic leucine zipper kinase | Homo sapiens (human) | Ki | 0.0056 | 0.0056 | 0.0056 | 0.0056 | AID1474637 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1645848 | NCATS Kinetic Aqueous Solubility Profiling | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14 | Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity. |
AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 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. |
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. |
AID1345514 | Human fibroblast growth factor receptor 1 (Type V RTKs: FGF (fibroblast growth factor) receptor family) | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1345563 | Human platelet derived growth factor receptor alpha (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1345506 | Human kinase insert domain receptor (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family) | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1345520 | Human fms related tyrosine kinase 4 (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family) | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1345590 | Human platelet derived growth factor receptor beta (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1345535 | Human fibroblast growth factor receptor 3 (Type V RTKs: FGF (fibroblast growth factor) receptor family) | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1345517 | Human fibroblast growth factor receptor 2 (Type V RTKs: FGF (fibroblast growth factor) receptor family) | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1345568 | Human fibroblast growth factor receptor 4 (Type V RTKs: FGF (fibroblast growth factor) receptor family) | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1345548 | Human fms related tyrosine kinase 1 (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family) | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID507214 | Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced apoptosis by [3H]thymidine incorporation assay | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID625018 | Binding constant for YES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624759 | Binding constant for PFCDPK1(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624717 | Binding constant for JNK2 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. |
AID1692004 | Cytotoxicity against rat NRK-49F cells assessed as cell survival rate at 10 uM incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Design, synthesis and discovery of 2(1H)-quinolone derivatives for the treatment of pulmonary fibrosis through inhibition of TGF-β/smad dependent and independent pathway. |
AID1425122 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624787 | Binding constant for KIT(A829P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425150 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625035 | Binding constant for PHKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID625136 | Binding constant for YSK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425146 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424992 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507218 | Inhibition of VEGF-induced Akt phosphorylation in HUVEC at 100 nM treated 2 hrs before VEGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624840 | Binding constant for AXL kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424891 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624990 | Binding constant for ABL1(Y253F)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID397066 | Antitumor activity against human FADU cells xenografted NMRI nu/nu mouse assessed as inhibition of mean tumor volume growth at 25 mg/kg, po qd after 21 days relative to control | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID507220 | Inhibition of VEGF-induced MAPK phosphorylation in HUASMC at 100 nM treated 2 hrs before VEGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1519459 | Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells incubated for 2 days by PSR staining based microscopic analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis and discovery of new compounds bearing coumarin scaffold for the treatment of pulmonary fibrosis. |
AID507225 | Inhibition of bFGF-induced MAPK phosphorylation in BRP treated 2 hrs before bFGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1708225 | Inhibition of JAK2 pathway in human TF-1 cells assessed as decrease in IL3-induced STAT5 phosphorylation preincubated for 1 hr followed by IL-3 stimulation and measured after 20 mins by immunoassay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery and Biological Evaluation of |
AID624895 | Binding constant for MEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425142 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424947 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625102 | Binding constant for PRKD2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424988 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425175 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425036 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624866 | Binding constant for MLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425008 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1654027 | Antifibrotic activity against bleomycin-induced pulmonary fibrosis C57BL/6J mouse model assessed as reduction in alveolar septal swelling at 60 mg/kg, po administered via gavage qd for 14 days at 3 days post bleomycin challenge by hematoxylin and eosin st | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2 | Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis. |
AID624841 | Binding constant for BLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425062 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1662302 | Inhibition of N-terminal GST-tagged human recombinant PDGFRalpha D842I mutant expressed in baculovirus-infected Sf9 cells using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobilit | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID624969 | Binding constant for ROCK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID397069 | Antitumor activity against human Caki1 cells xenografted NMRI nu/nu mouse assessed as inhibition of mean tumor volume growth at 50 mg/kg, po qd after 21 days relative to control | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1425069 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624834 | Binding constant for DAPK3 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. |
AID1424985 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624835 | Binding constant for ERN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425023 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625034 | Binding constant for PDGFRA 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. |
AID1425007 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624996 | Binding constant for EGFR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1519472 | Oral bioavailability in Sprague-Dawley rat 10 mg/kg measured upto 24 hrs | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis and discovery of new compounds bearing coumarin scaffold for the treatment of pulmonary fibrosis. |
AID1425009 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625033 | Binding constant for PCTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425190 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624749 | Binding constant for CASK 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. |
AID1424908 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID624852 | Binding constant for FES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID624957 | Binding constant for EPHB6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624745 | Binding constant for PKN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1441674 | Anti-inflammatory activity in BLM-induced C57BL/6 mouse model of acute lung neutrophilic inflammation assessed as reduction in number of neutrophils in BALF at 30 mg/kg, ip qd for 7 days post BLM challenge measured on day 7 | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
AID624923 | Binding constant for MAPKAPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625107 | Binding constant for DMPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624837 | Binding constant for IRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624855 | Binding constant for FRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424924 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624929 | Binding constant for BRSK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425135 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425162 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1427156 | Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors. |
AID624836 | Binding constant for IKK-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507243 | Antitumor activity against human FADU cells xenografted in NMRI nu/nu mouse assessed as reduction of Meca 32-positive cells at 100 mg/kg, po qd for 5 days by double immunofluorescence staining | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID625040 | Binding constant for PIK3CA(E545K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID624767 | Binding constant for MERTK 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. |
AID625048 | Binding constant for PRKCD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425093 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1662306 | Inhibition of c-Kit (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobility shift assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID397067 | Antitumor activity against human FADU cells xenografted NMRI nu/nu mouse assessed as inhibition of mean tumor volume growth at 10 mg/kg, po qd after 21 days relative to control | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID507204 | Inhibition of human Lyn | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID625128 | Binding constant for CSNK1G1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425131 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507208 | Antiangiogenic activity in HSMEC assessed as inhibition of VEGF-induced cell proliferation by [3H]thymidine incorporation assay | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1425129 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1692030 | Anti-fibrotic activity in C57BL/6 mouse model of bleomycin-induced lung fibrosis assessed as protection of alveolar tissue structure at 50 mg/kg, po administered for 21 days starting from day 8 post bleomycin treatment by hematoxylin and eosin staining ba | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Design, synthesis and discovery of 2(1H)-quinolone derivatives for the treatment of pulmonary fibrosis through inhibition of TGF-β/smad dependent and independent pathway. |
AID397086 | Inhibition of human GSK3-beta at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1424909 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397077 | Inhibition of human Lck | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1425141 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624778 | Binding constant for ACVRL1 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. |
AID1424983 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397050 | Inhibition of human VEGFR3 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624710 | Binding constant for SRMS kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID507252 | Antitumor activity against human Caki1 cells xenografted in NMRI nu/nu mouse assessed as inhibition of tumor growth at 100 mg/kg, po qd for 5 days relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1425067 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425154 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625134 | Binding constant for PIP5K2C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425116 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624738 | Binding constant for MLCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425181 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624845 | Binding constant for CDK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425128 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507202 | Inhibition of human Flt3 | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID507238 | Antitumor activity against human FADU cells xenografted in NMRI nu/nu mouse assessed as reduction of tumor perfusion at 100 mg/kg, po qd for 3 days by DCE-MRI analysis | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1425189 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1662358 | Toxicity in nu/nu mouse xenografted with human HT-29 cells assessed as effect on body weight at 100 mg/kg, po qd for 18 days | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID625022 | Binding constant for MUSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425001 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624921 | Binding constant for MAP4K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424898 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624998 | Binding constant for EGFR(G719C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID761353 | Inhibition of FGFR1 (unknown origin) using poly (Glu, Tyr)4:1 as substrate by ELISA | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Naphthalimides exhibit in vitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs). |
AID624930 | Binding constant for TNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID624723 | Binding constant for CSNK1A1L kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425064 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397078 | Inhibition of human Lyn | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624765 | Binding constant for TRKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625017 | Binding constant for TIE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1519474 | Antifibrotic activity against C57BL/6 mouse pulmonary fibrosis model assessed as reduction in bleomycin-iduced hydroxyproline level at 50 mg/kg, po administered for 28 days and measured on day 14 and 28 by spectrophotometry | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis and discovery of new compounds bearing coumarin scaffold for the treatment of pulmonary fibrosis. |
AID624935 | Binding constant for FLT3(D835H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507187 | Inhibition of human GST-fused VEGFR2 expressed in Sf9 insect cells after 20 mins by scintillation counting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID625061 | Binding constant for MAP4K5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID397040 | Inhibition of human InsR | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID625027 | Binding constant for MAP3K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID397082 | Antiangiogenic activity BRP cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1662357 | Antitumor activity against human HT-29 cells xenografted in nu/nu mouse assessed as tumour growth inhibition at 100 mg/kg, po qd for 18 days and measured twice per week by vernier caliper method | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID1424960 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624946 | Binding constant for BRAF 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. |
AID1424963 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625043 | Binding constant for PIK3CA(I800L) 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. |
AID625119 | Binding constant for CAMK1G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424961 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624982 | Binding constant for ABL1(F317L)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625097 | Binding constant for TNNI3K kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425100 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424975 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625055 | Binding constant for MST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624918 | Binding constant for DYRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425086 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507250 | Antitumor activity against human FADU cells xenografted in NMRI nu/nu mouse assessed as inhibition of tumor growth at 25 mg/kg, po qd for 5 days relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID507224 | Inhibition of VEGF-induced MAPK phosphorylation in BRP treated 2 hrs before VEGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID625114 | Binding constant for GSK3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507253 | Antitumor activity against human Caki1 cells xenografted in NMRI nu/nu mouse assessed as inhibition of tumor growth at 50 mg/kg, po qd for 5 days relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1425037 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424938 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624909 | Binding constant for TGFBR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1510862 | Inhibition of VEGFR3 (unknown origin) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma. |
AID1876272 | Inhibition of FGFR2 (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID1425019 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1504563 | Inhibition of recombinant PDGFRbeta (unknown origin) by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID624997 | Binding constant for EGFR(E746-A750del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424981 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624719 | Binding constant for GRK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425070 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625103 | Binding constant for MST4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1692021 | Anti-fibrotic activity in C57BL/6 mouse model of bleomycin-induced lung fibrosis assessed as reduction in collagen deposition by measuring hydroxyproline content in lung at 50 mg/kg, po administered for 30 days starting from day 1 post bleomycin treatment | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Design, synthesis and discovery of 2(1H)-quinolone derivatives for the treatment of pulmonary fibrosis through inhibition of TGF-β/smad dependent and independent pathway. |
AID1519486 | Antifibrotic activity against BLM-induced C57BL/6 mouse pulmonary fibrosis model assessed as reduction in lymphocytes in BALF at 50 mg/kg, po administered for 28 days and measured on day 28 | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis and discovery of new compounds bearing coumarin scaffold for the treatment of pulmonary fibrosis. |
AID624812 | Binding constant for SBK1 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. |
AID1425094 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1427152 | Inhibition of human N-terminal GST-tagged VEGFR2 cytoplasmic domain (790 to 1356 residues) expressed in baculovirus expression system at 1 uM preincubated for 10 mins followed by FAM-labeled peptide substrate addition measured after 1 hr by mobility shift | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors. |
AID625106 | Binding constant for MARK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1510861 | Inhibition of VEGFR1 (unknown origin) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma. |
AID397048 | Inhibition of human PDGFRalpha | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID625126 | Binding constant for TAOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507209 | Antiangiogenic activity in BRP assessed as inhibition of PDGF BB-induced cell proliferation by [3H]thymidine incorporation assay | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1587789 | Inhibition of Rho/MRTF/SRF pathway (unknown origin) expressed in human PC3 cells assessed as reduction in Galpha12 Q231L-stimulated MRTF-selective SRE.L promoter-driven luciferase activity after overnight incubation by luminescence assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | 5-Aryl-1,3,4-oxadiazol-2-ylthioalkanoic Acids: A Highly Potent New Class of Inhibitors of Rho/Myocardin-Related Transcription Factor (MRTF)/Serum Response Factor (SRF)-Mediated Gene Transcription as Potential Antifibrotic Agents for Scleroderma. |
AID1425049 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425153 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397065 | Antitumor activity against human FADU cells xenografted NMRI nu/nu mouse assessed as inhibition of mean tumor volume growth at 50 mg/kg, po bid after 21 days relative to control | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID625120 | Binding constant for EPHA8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625090 | Binding constant for ICK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID1425005 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625124 | Binding constant for RET(V804M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID397038 | Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation by [3H]thymidine incorporation assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID625089 | Binding constant for AAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID397061 | Antiangiogenic activity against human Calu6 cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624789 | Binding constant for KIT(D816V) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424965 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625068 | Binding constant for NEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID1425055 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424916 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624958 | Binding constant for PIK3C2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID625069 | Binding constant for TLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424896 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424996 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624742 | Binding constant for NEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507232 | Inhibition of bFGF-induced MAPK phosphorylation in BRP treated 2 hrs before bFGF challenge by Western blotting in presence of 5% fetal calf serum | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624879 | Binding constant for PIK3CG kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424931 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397052 | Half life in NMRI nu/nu mouse at 50 mg/kg, po administered as single dose | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1519477 | Antifibrotic activity against BLM-induced C57BL/6 mouse pulmonary fibrosis model assessed as decrease in bronchioles inflammatory cell infiltration at 50 mg/kg, po administered for 28 days and measured on day 14 and 28 by HE staining based fluorescence mi | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis and discovery of new compounds bearing coumarin scaffold for the treatment of pulmonary fibrosis. |
AID1662300 | Inhibition of GST-tagged human recombinant VEGFR1 cytoplasmic domain (781 to 1338 residues) expressed in baculovirus expression system using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID1474637 | Inhibition of His6-tagged MELK catalytic domain (1 to 340 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells using Bcl-GL as substrate measured after 30 mins in presence of [gamma32P]ATP by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9 | Discovery of a potent inhibitor of MELK that inhibits expression of the anti-apoptotic protein Mcl-1 and TNBC cell growth. |
AID624965 | Binding constant for LZK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID507254 | Antitumor activity against human Caki1 cells xenografted in NMRI nu/nu mouse assessed as inhibition of tumor growth at 10 mg/kg, po qd for 5 days relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624985 | Binding constant for ABL1(M351T)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425060 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507231 | Inhibition of PDGF-BB-induced MAPK phosphorylation in BRP at 100 nM treated 2 hrs before PDGF-BB challenge by Western blotting in presence of 5% fetal calf serum | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624825 | Binding constant for BMPR1B 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. |
AID397076 | Inhibition of human Src | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID397088 | Inhibition of human DYRK1A at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1424899 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625129 | Binding constant for HIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID625137 | Binding constant for MEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID1425157 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624878 | Binding constant for PIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424944 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425145 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425208 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1654033 | Antifibrotic activity against bleomycin-induced pulmonary fibrosis C57BL/6J mouse model assessed as reduction in collagen deposition by measuring hydroxyproline content in lungs at 60 mg/kg, po administered via gavage qd for 14 days at 3 days post bleomyc | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2 | Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis. |
AID625009 | Binding constant for EPHA3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624915 | Binding constant for PIP5K2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425004 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424895 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624971 | Binding constant for DAPK1 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. |
AID1504576 | Inhibition of recombinant PDGFRalpha (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID1504567 | Inhibition of recombinant ABL (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID624821 | Binding constant for YANK1 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. |
AID1425207 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507197 | Inhibition of human EGFR | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624779 | Binding constant for BTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425174 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624828 | Binding constant for CDK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID624762 | Binding constant for DLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507192 | Inhibition of human FGFR4 | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1425057 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425127 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1662301 | Inhibition of GST-tagged human recombinant VEGFR3 cytoplasmic domain (800 to 1297 residues) Q890H/V1128L/H1146R mutant expressed in baculovirus expression system using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID397245 | Inhibition of human S6K1 at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1424948 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507261 | Antitumor activity against human PAC120 cells xenografted in NMRI nu/nu mouse assessed as inhibition of tumor growth at 100 mg/kg, po qd for 5 days relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
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. |
AID624860 | Binding constant for VEGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625053 | Binding constant for PRKG2 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. |
AID1425028 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425046 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624734 | Binding constant for YANK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625109 | Binding constant for BIKE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1662323 | Inhibition of colony formation in human MKN74 cells at 1 uM measured after 14 days by crystal violet staining-based assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID625117 | Binding constant for PAK7 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. |
AID1424923 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625135 | Binding constant for ADCK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624739 | Binding constant for GRK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424956 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507237 | Inhibition of bFGF-induced apoptosis in HUASMC assessed as increase of cleaved caspase 3 level at 100 nM treated 2 hrs before bFGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1425078 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624711 | Binding constant for STK35 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424942 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425156 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425186 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425077 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624702 | Binding constant for BRSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424990 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424897 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425102 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1504599 | Antifibrotic activity in BLM-induced chronic pulmonary fibrosis C57 mouse model assessed as increase in survival rate at 100 mg/kg, po administered qd measured up to 28 days | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID625123 | Binding constant for RET(V804L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424991 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397090 | Inhibition of human MAPK2 at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1425073 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624853 | Binding constant for FLT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625003 | Binding constant for EGFR(L858R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624758 | Binding constant for RIPK5 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. |
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. |
AID507242 | Antitumor activity against human FADU cells xenografted in NMRI nu/nu mouse assessed as reduction of PDGFR-beta-positive mural cells at 100 mg/kg, po qd for 5 days by DCE-MRI analysis relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1424979 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624776 | Binding constant for PCTK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624889 | Binding constant for JNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507201 | Inhibition of human CDK4 | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID625046 | Binding constant for PIK3CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507188 | Inhibition of human VEGFR3 | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624793 | Binding constant for KIT(V559D,V654A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID397042 | Inhibition of human CDK4 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624813 | Binding constant for MINK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424970 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1478069 | Inhibition of human VEGFR2 | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1 | Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
AID625065 | Binding constant for CIT 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. |
AID1425194 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625092 | Binding constant for NDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID397039 | Inhibition of human IGFR1 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1504573 | Inhibition of recombinant c-KIT (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID625045 | Binding constant for PIK3CA(Q546K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425161 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507193 | Inhibition of human PDGFRalpha | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624937 | Binding constant for FLT3(ITD) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1699266 | Antifibrotic activity in bleomycin-induced C57BL/6N mouse model of pulmonary fibrosis assessed as reduction in lung-fibrosis at 100 mg/kg, po qd administered from 7th day post-bleomycin challenge and measured post last dose | |||
AID397043 | Inhibition of human EGFR | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624933 | Binding constant for PLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID507259 | Antitumor activity against human SKOV3 cells xenografted in NMRI nu/nu mouse assessed as inhibition of tumor growth at 50 mg/kg, po qd for 5 days relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID625079 | Binding constant for NEK6 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. |
AID397054 | Clearance in NMRI nu/nu mouse at 50 mg/kg, po or 10 mg/kg, iv administered as single dose | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624940 | Binding constant for FLT3(R834Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425188 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624703 | Binding constant for MAPKAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1654037 | Antifibrotic activity against bleomycin-induced pulmonary fibrosis C57BL/6J mouse model assessed as reduction in oxidative stress by measuring reduction in MDA level in plasma at 60 mg/kg, po administered via gavage qd for 14 days at 3 days post bleomycin | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2 | Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis. |
AID397075 | Inhibition of VEGF-stimulated human VEGFR2 phosphorylation expressed in mouse NIH3T3 cells pretreated for 1 hr measured 32 hrs after drug dose by immunoprecipitation based pulse-chase experiment | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID397053 | AUC in NMRI nu/nu mouse at 50 mg/kg, po administered as single dose | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID625044 | Binding constant for PIK3CA(M1043I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624854 | Binding constant for FLT4 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. |
AID507244 | Antitumor activity against human FADU cells xenografted in NMRI nu/nu mouse assessed as reduction of PDGFR-beta-positive mural cells at 100 mg/kg, po qd for 5 days by double immunofluorescence staining | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1504582 | Inhibition of recombinant RET (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID1425173 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1876273 | Inhibition of FGFR3 (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID1424984 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424929 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424919 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425124 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624873 | Binding constant for PAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507185 | Inhibition of human VEGFR1 | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1425038 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425125 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1692028 | Anti-fibrotic activity in C57BL/6 mouse model of bleomycin-induced lung fibrosis assessed as protection of alveolar tissue structure at 50 mg/kg, po administered for 30 days starting from day 1 post bleomycin treatment by hematoxylin and eosin staining ba | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Design, synthesis and discovery of 2(1H)-quinolone derivatives for the treatment of pulmonary fibrosis through inhibition of TGF-β/smad dependent and independent pathway. |
AID624704 | Binding constant for NEK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625121 | Binding constant for RET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425163 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425170 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425106 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625012 | Binding constant for GAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625063 | Binding constant for PLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425147 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397247 | Inhibition of human CK1 at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1425084 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397091 | Inhibition of human ERK2 at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624989 | Binding constant for ABL1(T315I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID397092 | Inhibition of human MSK1 at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624748 | Binding constant for EPHA6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425117 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624869 | Binding constant for NEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624934 | Binding constant for FLT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425024 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425167 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1662299 | Inhibition of N-terminal GST-fused human PDGFRbeta cytoplasmic domain (557 to 1106 (end) residues) expressed in baculovirus expression system using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured a | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID507186 | Inhibition of mouse GST-fused VEGFR2 expressed in Sf9 insect cells after 20 mins by scintillation counting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624887 | Binding constant for ERK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1504581 | Inhibition of recombinant HCK (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID1425042 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1501092 | Inhibition of N-terminal GST tagged human PDGFRalpha (550 to 1089 end residues) cytoplasmic domain expressed in baculovirus expression system preincubated for 10 mins followed by fluorescein amidite-labelled peptide substrate addition measured after 1 hr | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel methyl indolinone-6-carboxylates containing an indole moiety as angiokinase inhibitors. |
AID1424905 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625020 | Binding constant for ITK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625122 | Binding constant for RET(M918T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425072 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625132 | Binding constant for FGFR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425053 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425058 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425074 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624857 | Binding constant for HCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424910 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1504578 | Inhibition of recombinant FGR (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID625075 | Binding constant for INSRR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425166 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1708217 | Antiproliferative activity human LX2 cells assessed as inhibition of TGF-beta induced hepatic stellate cell growth incubated for upto 72 hrs by CCK8 assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery and Biological Evaluation of |
AID625105 | Binding constant for EPHB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424950 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424930 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624760 | Binding constant for PFPK5(P.falciparum) 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. |
AID397059 | Plasma concentration in NMRI nu/nu mouse at 50 mg/kg, po administered as single dose after 2 hrs | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID507251 | Antitumor activity against human FADU cells xenografted in NMRI nu/nu mouse assessed as inhibition of tumor growth at 10 mg/kg, po qd for 5 days relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID761356 | Inhibition of PDGFRalpha (unknown origin) using poly (Glu, Tyr)4:1 as substrate by ELISA | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Naphthalimides exhibit in vitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs). |
AID1425165 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1504565 | Inhibition of PDGFR in mouse NIH/3T3 cells assessed as reduction in recombinant human PDGF-BB-induced cell proliferation after 42 hrs by cell titer 96 aqueous one solution based assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID624831 | Binding constant for CHEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625084 | Binding constant for HUNK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425022 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1427162 | Inhibition of recombinant human GST-tagged FGFR1 cytoplasmic domain (398 to 822 residues) expressed in baculovirus expression system preincubated for 10 mins followed by FAM-labeled peptide substrate addition measured after 1 hr by mobility shift assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors. |
AID624720 | Binding constant for HIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507191 | Inhibition of human FGFR3 | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1425202 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507205 | Inhibition of human Src | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1425045 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397060 | Plasma concentration in NMRI nu/nu mouse at 50 mg/kg, po administered as single dose after 24 hrs | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID625138 | Binding constant for STK33 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID1845299 | Inhibition of GST-tagged FGFR4 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
AID507190 | Inhibition of human FGFR2 | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1425133 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1662298 | Inhibition of N-terminal GST fused human VEGFR2 cytoplasmic domain (790 to 1356 (end) residues) expressed in baculovirus expression system using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured afte | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID397252 | Inhibition of human JNK1A1 at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624826 | Binding constant for BMPR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624728 | Binding constant for NIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624712 | Binding constant for DYRK1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1708216 | Antiproliferative activity human LX2 cells assessed as inhibition of TGF-beta induced hepatic stellate cells activation by CCK8 assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery and Biological Evaluation of |
AID624730 | Binding constant for CAMK2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID775337 | Binding affinity to human MLK3 | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
AID625101 | Binding constant for TAOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507222 | Inhibition of VEGF-induced Akt phosphorylation in HUASMC at 100 nM treated 2 hrs before VEGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1425031 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624815 | Binding constant for ERBB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425144 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1708218 | Cytotoxicity against human LX2 cells assessed as cell viability incubated for 48 hrs by YOYO1 dye based fluorescence analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery and Biological Evaluation of |
AID397085 | Induction of apoptosis in BRP cells assessed as caspase-3 cleavage | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1424941 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424977 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425193 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1427157 | Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors. |
AID1425126 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624974 | Binding constant for PIK3CD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425199 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424925 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624975 | Binding constant for PLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625054 | Binding constant for MST2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425054 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425191 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624777 | Binding constant for DDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425085 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507219 | Inhibition of bFGF-induced Akt phosphorylation in HUVEC at 100 nM treated 2 hrs before bFGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID625096 | Binding constant for STK36 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425033 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425065 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625098 | Binding constant for IRAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507241 | Antitumor activity against human FADU cells xenografted in NMRI nu/nu mouse assessed as reduction of tumor vessel density at 100 mg/kg, po qd for 5 days by DCE-MRI analysis relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624706 | Binding constant for MLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425087 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624882 | Binding constant for PKAC-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1501094 | Inhibition of N-terminal GST tagged human FGFR1 (398 to 822 end residues) cytoplasmic domain expressed in baculovirus expression system preincubated for 10 mins followed by fluorescein amidite-labelled peptide substrate addition measured after 1 hr by mob | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel methyl indolinone-6-carboxylates containing an indole moiety as angiokinase inhibitors. |
AID507239 | Inhibition of VEGFR2 transfected in mouse NIH3T3 cells at 50 nM incubated for 1 hr measured after 32 hrs washout followed by VEGF stimulation for 10 mins by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
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. |
AID625112 | Binding constant for YANK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1845297 | Inhibition of GST-tagged FGFR2 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
AID1425081 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624999 | Binding constant for EGFR(G719S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425050 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624715 | Binding constant for ERK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424952 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID775336 | Binding affinity to human FLT3 | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
AID624868 | Binding constant for MST1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID1425051 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1587792 | Cytotoxicity against human PC3 cells assessed as reduction in cell viability by CellTiter-Fluor assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | 5-Aryl-1,3,4-oxadiazol-2-ylthioalkanoic Acids: A Highly Potent New Class of Inhibitors of Rho/Myocardin-Related Transcription Factor (MRTF)/Serum Response Factor (SRF)-Mediated Gene Transcription as Potential Antifibrotic Agents for Scleroderma. |
AID507240 | Antitumor activity against human FADU cells xenografted in NMRI nu/nu mouse assessed as reduction of tumor vascular permeability at 100 mg/kg, po qd for 3 days by DCE-MRI analysis | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624823 | Binding constant for MKNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624881 | Binding constant for PKAC-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507206 | Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation by [3H]thymidine incorporation assay | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1425111 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID1425209 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1519491 | Antifibrotic activity against BLM-induced C57BL/6 mouse pulmonary fibrosis model assessed as decrease in destruction alveolar structure at 50 mg/kg, po administered for 28 days and measured on day 14 and 28 by HE staining based fluorescence microscopy | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis and discovery of new compounds bearing coumarin scaffold for the treatment of pulmonary fibrosis. |
AID1501068 | Inhibition of N-terminal GST tagged human PDGFRbeta (557 to 1106 end residues) cytoplasmic domain expressed in baculovirus expression system preincubated for 10 mins followed by fluorescein amidite-labelled peptide substrate addition measured after 1 hr b | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel methyl indolinone-6-carboxylates containing an indole moiety as angiokinase inhibitors. |
AID624808 | Binding constant for TRKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425137 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425183 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397045 | Inhibition of human Plk1 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID625094 | Binding constant for CDK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507227 | Inhibition of bFGF-induced Akt phosphorylation in BRP treated 2 hrs before bFGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1510860 | Inhibition of VEGFR2 (unknown origin) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma. |
AID397051 | Cmax in NMRI nu/nu mouse at 50 mg/kg, po administered as single dose | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1424889 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397244 | Inhibition of human SAPK2A/P38 at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624753 | Binding constant for PKNB(M.tuberculosis) 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. |
AID1424995 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624788 | Binding constant for KIT(D816H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1662310 | Inhibition of B-Raf (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobility shift assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID1845298 | Inhibition of GST-tagged FGFR3 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
AID397041 | Inhibition of human CDK1 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID625088 | Binding constant for ARK5 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. |
AID1425013 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425048 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507212 | Antiangiogenic activity in human Calu6 assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay in presence of fetal calf serum | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624847 | Binding constant for CSNK1E kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624876 | Binding constant for PDPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625031 | Binding constant for MRCKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425148 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425104 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624897 | Binding constant for RAF1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1504566 | Inhibition of human ERG | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID1424894 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397250 | Inhibition of human SAPK2B/P38-beta-2 at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1654030 | Antifibrotic activity against bleomycin-induced pulmonary fibrosis C57BL/6J mouse model assessed as reduction in lung coefficient at 30 to 60 mg/kg, po administered via gavage qd for 14 days at 3 days post bleomycin challenge | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2 | Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis. |
AID1425158 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425063 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624838 | Binding constant for ACVR2A 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. |
AID1662304 | Inhibition of SRC (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobility shift assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID1424946 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624792 | Binding constant for KIT(V559D,T670I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1501070 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel methyl indolinone-6-carboxylates containing an indole moiety as angiokinase inhibitors. |
AID624973 | Binding constant for JAK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425149 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624735 | Binding constant for ANKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624799 | Binding constant for TIE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624713 | Binding constant for ERK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424967 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624732 | Binding constant for PYK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424953 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397070 | Antitumor activity against human Caki1 cells xenografted NMRI nu/nu mouse assessed as inhibition of mean tumor volume growth at 10 mg/kg, po qd after 21 days relative to control | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624851 | Binding constant for ERBB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1427159 | Inhibition of recombinant human GST-tagged VEGFR1 cytoplasmic domain (781 to 1338 residues) expressed in baculovirus expression system preincubated for 10 mins followed by FAM-labeled peptide substrate addition measured after 1 hr by mobility shift assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors. |
AID624829 | Binding constant for CDK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID624791 | Binding constant for KIT(V559D) 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. |
AID397073 | Antitumor activity against human Calu6 cells xenografted NMRI nu/nu mouse assessed as inhibition of mean tumor volume growth at 50 mg/kg, po qd after 21 days relative to control | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1692007 | Inhibition of TGF-beta-induced collagen-1 protein expression in rat NRK-49F cells at 20 to 40 uM incubated for 24 hrs by Western blotting analysis | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Design, synthesis and discovery of 2(1H)-quinolone derivatives for the treatment of pulmonary fibrosis through inhibition of TGF-β/smad dependent and independent pathway. |
AID1519490 | Antifibrotic activity against BLM-induced C57BL/6 mouse pulmonary fibrosis model assessed as increase in time for reduction of alveoli at 50 mg/kg, po administered for 28 days and measured on day 14 and 28 by HE staining based fluorescence microscopy | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis and discovery of new compounds bearing coumarin scaffold for the treatment of pulmonary fibrosis. |
AID624931 | Binding constant for CLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624798 | Binding constant for LKB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424976 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624954 | Binding constant for EPHB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425052 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424945 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424911 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507200 | Inhibition of human CDK2 | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID625026 | Binding constant for MAP3K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424922 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424921 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624705 | Binding constant for MYLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425012 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1519478 | Antifibrotic activity against BLM-induced C57BL/6 mouse pulmonary fibrosis model assessed as decrease in perivascular inflammatory cell infiltration at 50 mg/kg, po administered for 28 days and measured on day 14 and 28 by HE staining based fluorescence m | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis and discovery of new compounds bearing coumarin scaffold for the treatment of pulmonary fibrosis. |
AID624718 | Binding constant for PFTAIRE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID397074 | Antitumor activity against human PAC120 cells xenografted NMRI nu/nu mouse assessed as inhibition of mean tumor volume growth at 100 mg/kg, po qd after 21 days relative to control | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1425059 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624818 | Binding constant for ULK3 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. |
AID1692008 | Inhibition of TGF-beta-induced alpha-SMA protein expression in rat NRK-49F cells at 20 to 40 uM incubated for 24 hrs by Western blotting analysis | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Design, synthesis and discovery of 2(1H)-quinolone derivatives for the treatment of pulmonary fibrosis through inhibition of TGF-β/smad dependent and independent pathway. |
AID507203 | Inhibition of human Lck | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1662308 | Inhibition of CDK4 (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobility shift assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID397055 | Volume of distribution in NMRI nu/nu mouse at 50 mg/kg, po or 10 mg/kg, iv administered as single dose | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1425176 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624977 | Binding constant for OSR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624761 | Binding constant for CDC2L5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID624756 | Binding constant for MAP4K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624783 | Binding constant for FGFR3(G697C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1427160 | Inhibition of recombinant human GST-tagged VEGFR3 cytoplasmic domain expressed in baculovirus expression system preincubated for 10 mins followed by FAM-labeled peptide substrate addition measured after 1 hr by mobility shift assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors. |
AID1662303 | Inhibition of N-terminal GST fused human recombinant FGFR1 cytoplasmic domain (398 to 822 (end) residues) expressed in baculovirus expression system using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition mea | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID624938 | Binding constant for FLT3(K663Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425035 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397084 | Induction of apoptosis in HUASMC assessed as caspase-3 cleavage | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID507210 | Antiangiogenic activity in HUASMC assessed as inhibition of PDGF BB-induced cell proliferation by [3H]thymidine incorporation assay | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1425160 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624962 | Binding constant for ASK2 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. |
AID1425076 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1427153 | Inhibition of human N-terminal GST-tagged VEGFR2 cytoplasmic domain (790 to 1356 residues) expressed in baculovirus expression system preincubated for 10 mins followed by FAM-labeled peptide substrate addition measured after 1 hr by mobility shift assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors. |
AID624903 | Binding constant for SRPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425068 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425025 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425113 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625047 | Binding constant for AMPK-alpha2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624804 | Binding constant for ERBB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425134 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624754 | Binding constant for NEK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425044 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507236 | Inhibition of bFGF-induced apoptosis in BRP assessed as increase of cleaved caspase 3 level at 100 nM treated 2 hrs before bFGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1425018 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID397249 | Inhibition of human PKA at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID625086 | Binding constant for SLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624782 | Binding constant for FGFR3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424955 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425138 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424904 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624961 | Binding constant for TGFBR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625131 | Binding constant for FGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425003 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624905 | Binding constant for CDKL5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1504580 | Inhibition of recombinant FYN (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID1424987 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425169 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424962 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425040 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624993 | Binding constant for ABL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID397071 | Antitumor activity against human HT-29 cells xenografted NMRI nu/nu mouse assessed as inhibition of mean tumor volume growth at 100 mg/kg, po qd after 21 days relative to control | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID507234 | Inhibition of bFGF-induced Akt phosphorylation in BRP at 100 nM treated 2 hrs before bFGF challenge by Western blotting in presence of 5% fetal calf serum | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
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. |
AID624907 | Binding constant for SYK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1587829 | Inhibition of Rho/MRTF/SRF pathway in human primary dermal fibroblasts assessed as reduction in LPA-stimulated CTGF mRNA expression by measuring CTGF mRNA level at 10'-6 M preincubated for 72 hrs followed by LPA stimulation and measured after 1 hr by qPCR | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | 5-Aryl-1,3,4-oxadiazol-2-ylthioalkanoic Acids: A Highly Potent New Class of Inhibitors of Rho/Myocardin-Related Transcription Factor (MRTF)/Serum Response Factor (SRF)-Mediated Gene Transcription as Potential Antifibrotic Agents for Scleroderma. |
AID1504585 | Inhibition of recombinant LYN-A (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID397056 | Oral bioavailability in NMRI nu/nu mouse at 50 mg/kg administered as single dose | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID397241 | Inhibition of human PDK1 at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1425172 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507262 | Plasma concentration in NMRI nu/nu mouse at 50 mg/kg, po after 1 hr | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1424907 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424937 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425105 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625140 | Binding constant for MARK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1662305 | Inhibition of LYN (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobility shift assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID1425115 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624952 | Binding constant for EPHA4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425000 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625007 | Binding constant for EGFR(T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507246 | Antitumor activity against human FADU cells xenografted in NMRI nu/nu mouse assessed as inhibition of tumor growth at 100 mg/kg, po qd for 5 days relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1504574 | Inhibition of recombinant YES (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID625049 | Binding constant for PRKCH kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1504570 | Inhibition of recombinant BTK (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID624795 | Binding constant for MET(M1250T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624785 | Binding constant for JAK3(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425210 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424935 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425130 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624994 | Binding constant for AKT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID624752 | Binding constant for SNRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507211 | Antiangiogenic activity in human FADU assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay in presence of fetal calf serum | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624786 | Binding constant for KIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425071 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID625073 | Binding constant for SGK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624757 | Binding constant for PKMYT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624832 | Binding constant for IKK-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625057 | Binding constant for TYRO3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624919 | Binding constant for AURKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425151 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425108 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424890 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624920 | Binding constant for MRCKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID624781 | Binding constant for CDK4-cyclinD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425039 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624709 | Binding constant for MYLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID397251 | Inhibition of human SAPK3/P38gamma at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1425200 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1504572 | Inhibition of recombinant ITK (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID1424980 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625021 | Binding constant for LIMK2 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. |
AID624803 | Binding constant for CHEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425119 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424958 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425205 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1654036 | Antifibrotic activity against bleomycin-induced pulmonary fibrosis C57BL/6J mouse model assessed as reduction in TNF-alpha expression in plasma at 30 to 60 mg/kg, po administered via gavage qd for 14 days at 3 days post bleomycin challenge by FACSCalibur | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2 | Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis. |
AID397047 | Inhibition of human FGFR1 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1425177 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625013 | Binding constant for LCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624833 | Binding constant for CSNK1G2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1504569 | Inhibition of recombinant BLK (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID1425056 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1662354 | Intrinsic clearance in human liver microsomes | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID1425029 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425061 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424951 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1519476 | Antifibrotic activity against BLM-induced C57BL/6 mouse pulmonary fibrosis model assessed as decrease in bronchiolar epithelial cell shedding at 50 mg/kg, po administered for 28 days and measured on day 14 and 28 by HE staining based fluorescence microsco | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis and discovery of new compounds bearing coumarin scaffold for the treatment of pulmonary fibrosis. |
AID624914 | Binding constant for WEE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624987 | Binding constant for ABL1(Q252H)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424971 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624947 | Binding constant for BRAF(V600E) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425101 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424940 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507198 | Inhibition of human HER2 | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624924 | Binding constant for RIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1654035 | Antifibrotic activity against bleomycin-induced pulmonary fibrosis C57BL/6J mouse model assessed as reduction in IL17A expression in plasma at 30 to 60 mg/kg, po administered via gavage qd for 14 days at 3 days post bleomycin challenge by FACSCalibur flow | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2 | Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis. |
AID507189 | Inhibition of human FGFR1 | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1519484 | Antifibrotic activity against BLM-induced C57BL/6 mouse pulmonary fibrosis model assessed as reduction in total white blood cells in BALF at 50 mg/kg, po administered for 28 days and measured on day 28 | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis and discovery of new compounds bearing coumarin scaffold for the treatment of pulmonary fibrosis. |
AID507249 | Antitumor activity against human FADU cells xenografted in NMRI nu/nu mouse assessed as inhibition of tumor growth at 50 mg/kg, po qd for 2 days relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624908 | Binding constant for TEC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624950 | Binding constant for DMPK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424900 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507245 | Antitumor activity against human FADU cells xenografted in NMRI nu/nu mouse assessed as inhibition of tumor growth at 50 mg/kg, po qd for 5 days relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID507226 | Inhibition of VEGF-induced Akt phosphorylation in BRP treated 2 hrs before VEGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID625070 | Binding constant for PFTK1 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. |
AID1692025 | Anti-fibrotic activity in C57BL/6 mouse model of bleomycin-induced lung fibrosis assessed as survival rate at 50 mg/kg, po administered for 30 days starting from day 1 post bleomycin treatment | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Design, synthesis and discovery of 2(1H)-quinolone derivatives for the treatment of pulmonary fibrosis through inhibition of TGF-β/smad dependent and independent pathway. |
AID625083 | Binding constant for LATS2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425047 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624867 | Binding constant for MLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625004 | Binding constant for EGFR(L858R,T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624991 | Binding constant for ABL1-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424893 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1692019 | Oral bioavailability in Sprague-Dawley rat at 5 mg/kg | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Design, synthesis and discovery of 2(1H)-quinolone derivatives for the treatment of pulmonary fibrosis through inhibition of TGF-β/smad dependent and independent pathway. |
AID624721 | Binding constant for MEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID624707 | Binding constant for DCAMKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID624716 | Binding constant for CSNK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1504579 | Inhibition of recombinant FLT3 (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID1424974 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425182 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625019 | Binding constant for AKT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507248 | Toxicity in human FADU cells xenografted in NMRI nu/nu mouse assessed weight loss at 100 mg/kg, po qd for 5 days | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID625006 | Binding constant for EGFR(S752-I759del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425017 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397087 | Inhibition of human ROCK2 at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID625010 | Binding constant for FER kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424928 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624743 | Binding constant for LTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625115 | Binding constant for PAK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1519485 | Antifibrotic activity against BLM-induced C57BL/6 mouse pulmonary fibrosis model assessed as reduction in neutrophils in BALF at 50 mg/kg, po administered for 28 days and measured on day 28 | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis and discovery of new compounds bearing coumarin scaffold for the treatment of pulmonary fibrosis. |
AID1504577 | Inhibition of recombinant FER (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID625110 | Binding constant for TRPM6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625080 | Binding constant for EIF2AK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425089 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID1424915 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424968 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624906 | Binding constant for S6K1 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. |
AID624849 | Binding constant for CSNK2A2 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. |
AID624740 | Binding constant for LRRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507217 | Inhibition of bFGF-induced MAPK phosphorylation in HUVEC at 100 nM treated 2 hrs before bFGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID507263 | Trough plasma concentration in NMRI nu/nu mouse at 50 mg/kg, po after 24 hrs | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
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. |
AID624948 | Binding constant for CSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID624769 | Binding constant for AURKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624724 | Binding constant for TAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425164 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624774 | Binding constant for QSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1501071 | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel methyl indolinone-6-carboxylates containing an indole moiety as angiokinase inhibitors. |
AID1692023 | Anti-fibrotic activity in C57BL/6 mouse model of bleomycin-induced lung fibrosis assessed as reduction in collagen deposition by measuring hydroxyproline content in lung at 50 mg/kg, po administered for 21 days starting from day 8 post bleomycin treatment | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Design, synthesis and discovery of 2(1H)-quinolone derivatives for the treatment of pulmonary fibrosis through inhibition of TGF-β/smad dependent and independent pathway. |
AID624830 | Binding constant for CDK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425026 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624770 | Binding constant for CAMK2D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424892 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624780 | Binding constant for CDK4-cyclinD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID1425021 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1519457 | Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells at 10 uM incubated for 2 days by PSR staining based microscopic analysis relative to control | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis and discovery of new compounds bearing coumarin scaffold for the treatment of pulmonary fibrosis. |
AID624859 | Binding constant for JAK1(JH1domain-catalytic) 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. |
AID397089 | Inhibition of human PKCalpha at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624984 | Binding constant for ABL1(H396P)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425136 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624822 | Binding constant for CDKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424998 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1823957 | Antifibrotic activity against Hypo fractionated palliative 17 Gy radiotherapy-induced C57BL/6J mouse lung fibrosis model assessed as reduction in collagen deposition at 60 mg/kg, po qd administered for 25 days starting from 16 weeks post irradiation by he | |||
AID624884 | Binding constant for PRKD1 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. |
AID507235 | Inhibition of PDGF-BB-induced apoptosis in BRP assessed as increase of cleaved caspase 3 level at 100 nM treated 2 hrs before PDGF-BB challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1501066 | Inhibition of N-terminal biotinylated DYKDDDDK tagged human VEGFR2 (790 to 1356 end residues) cytoplasmic domain expressed in baculovirus expression system preincubated for 10 mins followed by fluorescein amidite-labelled peptide substrate addition measur | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel methyl indolinone-6-carboxylates containing an indole moiety as angiokinase inhibitors. |
AID624964 | Binding constant for DYRK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507216 | Inhibition of VEGF-induced MAPK phosphorylation in HUVEC at 100 nM treated 2 hrs before VEGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID397254 | Inhibition of human PHK at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624936 | Binding constant for FLT3(D835Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624896 | Binding constant for PRKR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507194 | Inhibition of human PDGFRbeta | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624842 | Binding constant for BMX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507247 | Toxicity in human FADU cells xenografted in NMRI nu/nu mouse assessed mortality at 100 mg/kg, po qd for 5 days | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID397068 | Antitumor activity against human Caki1 cells xenografted NMRI nu/nu mouse assessed as inhibition of mean tumor volume growth at 100 mg/kg, po qd after 21 days relative to control | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID507256 | Antitumor activity against rat GL-9L cells xenografted in NMRI nu/nu mouse assessed as inhibition of tumor growth at 25 mg/kg, po qd for 5 days relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624802 | Binding constant for PIM3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425043 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425197 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624926 | Binding constant for RIOK3 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. |
AID624913 | Binding constant for TYK2(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425140 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424966 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424939 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425083 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624772 | Binding constant for AURKB 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. |
AID1425206 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397049 | Inhibition of human VEGFR1 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1425120 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1504564 | Inhibition of recombinant VEGFR2 (unknown origin) by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID397079 | Inhibition of human Flt3 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID507199 | Inhibition of human CDK1 | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1427161 | Inhibition of PDGFRalpha (unknown origin) preincubated for 10 mins followed by FAM-labeled peptide substrate addition measured after 1 hr by mobility shift assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors. |
AID625072 | Binding constant for TBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624726 | Binding constant for HIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624846 | Binding constant for CSNK1A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625095 | Binding constant for SIK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507213 | Antiangiogenic activity in human HeLa assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay in presence of fetal calf serum | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1662307 | Inhibition of CDK2 (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobility shift assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID1425016 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624814 | Binding constant for DCAMKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624744 | Binding constant for ZAP70 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624953 | Binding constant for EPHA7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID1425155 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425082 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397248 | Inhibition of human CK2 at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1425090 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425079 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625041 | Binding constant for PIK3CA(H1047L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424913 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625039 | Binding constant for PIK3CA(E545A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625078 | Binding constant for SRPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625066 | Binding constant for IRAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624925 | Binding constant for RIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624888 | Binding constant for ERK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425097 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424912 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625113 | Binding constant for MARK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425159 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624893 | Binding constant for MEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1519458 | Cytotoxicity against rat NRK-49F cells assessed as cell viability at 10 uM incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis and discovery of new compounds bearing coumarin scaffold for the treatment of pulmonary fibrosis. |
AID507228 | Inhibition of VEGF-induced apoptosis in HUVEC assessed as increase of cleaved caspase 3 level treated 2 hrs before VEGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID507257 | Antitumor activity against rat GL-9L cells xenografted in NMRI nu/nu mouse assessed as inhibition of tumor growth at 10 mg/kg, po qd for 5 days relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1425171 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425179 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624741 | Binding constant for LRRK2(G2019S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425121 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624872 | Binding constant for PAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624731 | Binding constant for CAMK2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1501093 | Inhibition of N-terminal GST tagged human VEGFR3 (798 to 1298 end residues) cytoplasmic domain expressed in baculovirus expression system preincubated for 10 mins followed by fluorescein amidite-labelled peptide substrate addition measured after 1 hr by m | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel methyl indolinone-6-carboxylates containing an indole moiety as angiokinase inhibitors. |
AID624819 | Binding constant for ACVR1 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. |
AID625028 | Binding constant for ASK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID761355 | Inhibition of KDR (unknown origin) using poly (Glu, Tyr)4:1 as substrate by ELISA | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Naphthalimides exhibit in vitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs). |
AID1424964 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1623456 | Inhibition of ABCB1 in human A2780/ADR cells assessed as potentiation of daunorubicin-induced cytotoxicity measured after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Novel chalcone and flavone derivatives as selective and dual inhibitors of the transport proteins ABCB1 and ABCG2. |
AID624844 | Binding constant for CDK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507196 | Inhibition of human IGF1R | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624922 | Binding constant for CAMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425041 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625029 | Binding constant for BRK 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. |
AID1501069 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel methyl indolinone-6-carboxylates containing an indole moiety as angiokinase inhibitors. |
AID624862 | Binding constant for LYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1654034 | Antifibrotic activity against bleomycin-induced pulmonary fibrosis C57BL/6J mouse model assessed as reduction in IL6 expression in plasma at 30 to 60 mg/kg, po administered via gavage qd for 14 days at 3 days post bleomycin challenge by FACSCalibur flow c | 2020 | Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2 | Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis. |
AID625064 | Binding constant for PIM2 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. |
AID507230 | Induction of apoptosis in HUVEC at 50 nM by TUNEL assay (Rvb = 2%) | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
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. |
AID624951 | Binding constant for EPHA2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624912 | Binding constant for TYK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507221 | Inhibition of bFGF-induced MAPK phosphorylation in HUASMC at >300 nM treated 2 hrs before bFGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID625042 | Binding constant for PIK3CA(H1047Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID625085 | Binding constant for ULK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1504562 | Inhibition of recombinant FGFR1 (unknown origin) by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID1424902 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424972 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625111 | Binding constant for RIOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424917 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624790 | Binding constant for KIT(L576P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1692032 | Anti-fibrotic activity in C57BL/6 mouse model of bleomycin-induced lung fibrosis assessed as reduction in inflammatory cell infiltration at 50 mg/kg, po administered for 30 days starting from day 1 post bleomycin treatment by hematoxylin and eosin stainin | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Design, synthesis and discovery of 2(1H)-quinolone derivatives for the treatment of pulmonary fibrosis through inhibition of TGF-β/smad dependent and independent pathway. |
AID625118 | Binding constant for CAMK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624863 | Binding constant for MARK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624839 | Binding constant for AKT2 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. |
AID1504575 | Inhibition of recombinant JAK3 (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID624737 | Binding constant for EPHA5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1692006 | Antimigratory activity in mouse L929 cells assessed as inhibition of TGF-beta-induced cell migration at 10 uM incubated for 24 hrs by wound healing assay | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Design, synthesis and discovery of 2(1H)-quinolone derivatives for the treatment of pulmonary fibrosis through inhibition of TGF-β/smad dependent and independent pathway. |
AID507258 | Antitumor activity against human HT-29 cells xenografted in NMRI nu/nu mouse assessed as inhibition of tumor growth at 100 mg/kg, po qd for 5 days relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID625116 | Binding constant for ADCK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID397064 | Antitumor activity against human FADU cells xenografted NMRI nu/nu mouse assessed as inhibition of mean tumor volume growth at 50 mg/kg, po qd after 21 days relative to control | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1425034 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425032 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424920 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1504568 | Inhibition of recombinant ALK (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID624875 | Binding constant for PDGFRB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624970 | Binding constant for CDK5 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. |
AID1504571 | Inhibition of recombinant INSR (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID625142 | Binding constant for TSSK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624848 | Binding constant for CSNK2A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624978 | Binding constant for ABL1(E255K)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624773 | Binding constant for AMPK-alpha1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID1425143 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425103 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424949 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625062 | Binding constant for MAP3K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625025 | Binding constant for MAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424934 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624928 | Binding constant for CDKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425213 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624939 | Binding constant for FLT3(N841I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425112 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425110 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1662309 | Inhibition of CHK (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobility shift assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID1424957 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507223 | Inhibition of bFGF-induced Akt phosphorylation in HUASMC at 100 nM treated 2 hrs before bFGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624911 | Binding constant for TXK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624877 | Binding constant for PIK3C2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID397063 | Antitumor activity against human FADU cells xenografted NMRI nu/nu mouse assessed as inhibition of mean tumor volume growth at 100 mg/kg, po qd after 21 days relative to control | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624972 | Binding constant for MTOR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1823954 | Antifibrotic activity against intranasal bleomycin-induced C57BL/6N mouse pulmonary fibrosis model assessed as reduction in Ashcroft score at 60 mg/kg, po qd administered for 15 days starting from 7 days post induction | |||
AID625087 | Binding constant for MELK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID397046 | Antiangiogenic activity against human HeLa cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1425178 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625125 | Binding constant for CLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID397243 | Inhibition of human MAPKAPK2 at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
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. |
AID1425203 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625104 | Binding constant for MYO3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID397246 | Inhibition of human SGK at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID397242 | Inhibition of human CHK1 at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624892 | Binding constant for p38-delta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625067 | Binding constant for NDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624797 | Binding constant for PHKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624883 | Binding constant for PRKCI kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625036 | Binding constant for PIK3CA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424989 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625051 | Binding constant for PRKCQ kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624811 | Binding constant for PAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID507215 | Antiangiogenic activity in HSMEC assessed as inhibition of VEGF-induced apoptosis by [3H]thymidine incorporation assay | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1692005 | Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells incubated for 2 days by PSR staining based microscopic analysis | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Design, synthesis and discovery of 2(1H)-quinolone derivatives for the treatment of pulmonary fibrosis through inhibition of TGF-β/smad dependent and independent pathway. |
AID507255 | Antitumor activity against rat GL-9L cells xenografted in NMRI nu/nu mouse assessed as inhibition of tumor growth at 50 mg/kg, po qd for 5 days relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID1876271 | Inhibition of FGFR1 (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID397080 | Antiangiogenic activity against HMSEC assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID397072 | Antitumor activity against human SKOV3 cells xenografted NMRI nu/nu mouse assessed as inhibition of mean tumor volume growth at 50 mg/kg, po qd after 21 days relative to control | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID625091 | Binding constant for MAST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625056 | Binding constant for TESK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425168 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID624820 | Binding constant for ACVR2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424933 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425014 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1504583 | Inhibition of recombinant C-SRC (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID624885 | Binding constant for ERK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624800 | Binding constant for IGF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425196 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625060 | Binding constant for CAMKK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624796 | Binding constant for MET(Y1235D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1504584 | Inhibition of recombinant LCK (unknown origin) at 1 uM by off-chip mobility shift assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11 | Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
AID507233 | Inhibition of PDGF-BB-induced Akt phosphorylation in BRP at 100 nM treated 2 hrs before PDGF-BB challenge by Western blotting in presence of 5% fetal calf serum | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624727 | Binding constant for FYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425010 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425027 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624801 | Binding constant for MAP3K15 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625052 | Binding constant for PRKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624880 | Binding constant for PIK4CB 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. |
AID1425198 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624817 | Binding constant for MYO3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424973 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625108 | Binding constant for MKNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625038 | Binding constant for PIK3CA(E542K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425123 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1692003 | Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells at 10 uM incubated for 2 days by PSR staining based microscopic analysis relative to control | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Design, synthesis and discovery of 2(1H)-quinolone derivatives for the treatment of pulmonary fibrosis through inhibition of TGF-β/smad dependent and independent pathway. |
AID624891 | Binding constant for JNK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625143 | Binding constant for CAMKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1845296 | Inhibition of GST-tagged FGFR1 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
AID1424901 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425201 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624794 | Binding constant for MET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425098 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424969 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507260 | Antitumor activity against human Calu6 cells xenografted in NMRI nu/nu mouse assessed as inhibition of tumor growth at 50 mg/kg, po qd for 5 days relative to control | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID397081 | Antiangiogenic activity against HUASMC assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1425095 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID1424997 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624729 | Binding constant for FAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID397253 | Inhibition of human SAPK4/P38delta at 10 umol/L | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1425118 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1427155 | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors. |
AID624771 | Binding constant for TLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1662353 | Half life in human liver microsomes | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11 | Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity. |
AID1427154 | Inhibition of human N-terminal GST-tagged PDGFRbeta cytoplasmic domain (557 to 1106 residues) expressed in baculovirus expression system preincubated for 10 mins followed by FAM-labeled peptide substrate addition measured after 1 hr by mobility shift assa | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors. |
AID624714 | Binding constant for p38-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424978 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425080 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624894 | Binding constant for MEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID397044 | Inhibition of human HER2 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1519479 | Antifibrotic activity against BLM-induced C57BL/6 mouse pulmonary fibrosis model assessed as decrease in bronchial epithelial vacuolar degeneration at 50 mg/kg, po administered for 28 days and measured on day 14 and 28 by HE staining based fluorescence mi | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Synthesis and discovery of new compounds bearing coumarin scaffold for the treatment of pulmonary fibrosis. |
AID1425192 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507229 | Inhibition of bFGF-induced apoptosis in HUVEC assessed as increase of cleaved caspase 3 level treated 2 hrs before bFGF challenge by Western blotting | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID397062 | Antiangiogenic activity against human FADU cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID397083 | Induction of apoptosis in HMSEC assessed as caspase-3 cleavage | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID624941 | Binding constant for CDKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID761354 | Inhibition of PDGFRbeta (unknown origin) using poly (Glu, Tyr)4:1 as substrate by ELISA | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Naphthalimides exhibit in vitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs). |
AID624968 | Binding constant for DRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624886 | Binding constant for ERK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424926 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507207 | Antiangiogenic activity in HUVEC assessed as inhibition of bFGF-induced cell proliferation by [3H]thymidine incorporation assay | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID507195 | Inhibition of human insulin receptor | 2008 | Cancer research, Jun-15, Volume: 68, Issue:12 | BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
AID624870 | Binding constant for NEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425204 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425006 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624850 | Binding constant for DDR1 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. |
AID1425212 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624945 | Binding constant for BMPR1A 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. |
AID624827 | Binding constant for CAMK2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424918 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424994 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID397037 | Inhibition of human VEGFR2 expressed in Sf9 cells | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). |
AID1424954 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624865 | Binding constant for MAP3K3 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. |
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. |
AID1425030 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424993 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425011 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624768 | Binding constant for SRPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1699271 | In-vivo inhibition of CHIT1 in bleomycin-induced C57BL/6N mouse model of pulmonary fibrosis assessed as reduction in chitinolytic activity in plasma at 100 mg/kg, po qd administered from 7th day post-bleomycin challenge and measured 24 hrs post last dose | |||
AID624824 | Binding constant for PIP5K1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425002 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425185 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624898 | Binding constant for GRK1 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. |
AID1801713 | Competition Binding Assays from Article 10.1021/acschembio.5b01063: \\Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors.\\ | 2016 | ACS chemical biology, 05-20, Volume: 11, Issue:5 | Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase 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. |
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. |
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. |
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. |
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. |
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. |
AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
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. |
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. |
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. |
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. |
AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
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. |
AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
AID1508612 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Highly predictive and interpretable models for PAMPA permeability. |
AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
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. |
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. |
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. |
AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
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. |
AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
AID1508591 | NCATS Rat Liver Microsome Stability Profiling | 2020 | Scientific reports, 11-26, Volume: 10, Issue:1 | Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models. |
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. |
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. |
AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
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. |
AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
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. |
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. |
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. |
AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
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. |
AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
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. |
AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
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. |
AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
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. |
AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
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. |
AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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. |
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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 5 (0.61) | 29.6817 |
2010's | 481 (59.02) | 24.3611 |
2020's | 329 (40.37) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 133 (15.72%) | 5.53% |
Reviews | 185 (21.87%) | 6.00% |
Case Studies | 46 (5.44%) | 4.05% |
Observational | 11 (1.30%) | 0.25% |
Other | 471 (55.67%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
A Phase II Study of BIBF1120 in Recurrent and Platinum-Sensitive Small Cell Lung Cancer (SCLC)[NCT02152059] | Phase 2 | 0 participants (Actual) | Interventional | 2014-07-31 | Withdrawn(stopped due to contract issues) | ||
An Open-label, Fixed-sequence Drug-drug Interaction Study in Healthy Subjects to Evaluate the Effect of GLPG4716 on the Pharmacokinetics of Nintedanib and Pirfenidone[NCT04971746] | Phase 1 | 58 participants (Actual) | Interventional | 2021-07-19 | Completed | ||
A Phase I-II Clinical Trial of Pegylated Liposomal Doxorubicin (Doxil®) in Combination With BIBF 1120 in Patients With Ovarian Cancer: Hoosier Oncology Group GYN10-149[NCT01485874] | Phase 1 | 11 participants (Actual) | Interventional | 2011-11-30 | Terminated(stopped due to Funding withdrawn due to drug unavailability) | ||
BARIS - BIBF1120 and RAD001 in Solid Tumors. A Phase I Trial to Evaluate the Safety and Tolerability of Combined BIBF 1120 and RAD001 in Solid Tumors and to Determine the Maximum Tolerated Dose (MTD) of the Combination[NCT01349296] | Phase 1 | 18 participants (Actual) | Interventional | 2012-07-31 | Completed | ||
Post-marketing Surveillance of Ofev Capsules in Chronic Fibrosing Interstitial Lung Diseases With a Progressive Phenotype in Japan[NCT04559581] | 425 participants (Actual) | Observational | 2020-09-28 | Active, not recruiting | |||
Pragmatic Management of Progressive Disease in Idiopathic Pulmonary Fibrosis: a Randomized Trial[NCT03939520] | Phase 4 | 378 participants (Anticipated) | Interventional | 2020-06-11 | Recruiting | ||
Study of Pulmonary Rehabilitation In Nintedanib Treated Patients With IPF: Improvements in Activity, Exercise Endurance Time, and QoL[NCT03717012] | Phase 4 | 19 participants (Actual) | Interventional | 2018-11-15 | Terminated(stopped due to The trial was terminated prematurely due to difficulties with recruitment because of the COVID-19 pandemic.) | ||
Non-Interventional Study (NIS) Collecting Experiences For IPF in Taiwan[NCT03242759] | 101 participants (Actual) | Observational | 2017-08-17 | Completed | |||
A Double Blind, Randomized, Placebo-controlled Trial Evaluating the Efficacy and Safety of Nintedanib Over 52 Weeks in Patients With Progressive Fibrosing Interstitial Lung Disease (PF-ILD)[NCT02999178] | Phase 3 | 663 participants (Actual) | Interventional | 2017-01-17 | Completed | ||
Efficacy of Nintedanib Per os as a Treatment for Epistaxis in HHT Disease. A National, Randomized, Multicentre Phase II Study[NCT03954782] | Phase 2 | 61 participants (Actual) | Interventional | 2020-06-22 | Completed | ||
"A Prospective, Observational Study on the Correlations Between Change in Lung Function and Change in Cough and Dyspnoea in Patients With Connective Tissue Disease-associated Progressive Fibrosing INTErstitial luNg diseaSE (CTD Associated PF-ILD) Treated [NCT05503030] | 120 participants (Anticipated) | Observational | 2022-11-01 | Recruiting | |||
TRICC-C: A Multicenter, Randomized, Phase II Trial: BIBF 1120 vs. Placebo in Patients Receiving Oxaliplatin Plus Fluorouracil and Leucovorin (mFOLFOX6) for Advanced, Chemorefractory Metastatic Colorectal Cancer (mCRC)[NCT01362361] | Phase 2 | 54 participants (Actual) | Interventional | 2011-06-30 | Completed | ||
Phase I Dose Escalation Trial to Determine the Maximum Tolerated Dose of BIBF 1120 in Combination With Carboplatin and Pegylated Liposomal Doxorubicin (PLD) in Patients With a First, Second or Third Platinum Sensitive Relapse of Advanced Epithelial Ovaria[NCT01314105] | Phase 1 | 19 participants (Actual) | Interventional | 2011-03-31 | Completed | ||
Multi-center Open-label Expanded Access Program of Oral Nintedanib 150 mg Twice Daily in Patients With Idiopathic Pulmonary Fibrosis[NCT02171156] | 0 participants | Expanded Access | Approved for marketing | ||||
Safety and Pharmacokinetics/Bioavailability of a Single Dose of 150 mg BIBF 1120 Administered as Soft Gelatine Capsules With and Without Food to Healthy Male Volunteers in an Open, Randomised, Intra-individual Crossover Comparison Design[NCT02182076] | Phase 1 | 15 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
Metabolism and Pharmacokinetics of [14C]-BIBF 1120 After Administration of Single Doses of 100 mg [14C]-BIBF 1120 Oral Solution in Healthy Male Volunteers[NCT02182154] | Phase 1 | 8 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
A Phase I Open Label Dose Escalation Study of Continuous Oral Treatment With BIBF 1120 Together With Paclitaxel and Carboplatin in Patients With Advanced Stage Non-small-cell Lung Cancer[NCT02182232] | Phase 1 | 33 participants (Actual) | Interventional | 2005-06-30 | Completed | ||
Phase II Study of BIBF 1120 in Recurrent Glioblastoma Multiforme[NCT01251484] | Phase 2 | 25 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
A Phase I Open Label Dose Escalation Study of Oral Treatment With BIBF 1120 in Combination With Standard Treatment of Paclitaxel and Carboplatin in Patients With Advanced Gynaecological Malignancies[NCT02182245] | Phase 1 | 22 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
A Multi-centre 3-arm Randomised Phase II Trial of BIBF 1120 Versus BIBW 2992 Versus Sequential Administration of BIBF 1120 and BIBW 2992 in Patients With Hormone-resistant Prostate Cancer[NCT00706628] | Phase 2 | 87 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
An Open-label Extension Trial of the Long Term Safety of Nintedanib in Patients With Progressive Fibrosing Interstitial Lung Disease (PF-ILD)[NCT03820726] | Phase 3 | 435 participants (Actual) | Interventional | 2019-04-16 | Completed | ||
An Open-label, Dose Escalation Phase I Study of the Safety and Tolerability of BIBF 1120 in Combination With Carboplatin and Pegylated Liposomal Doxorubicin (PLD) in Japanese Patients With a First, Second or Third Platinum-sensitive Relapse of Advanced Ep[NCT01329549] | Phase 1 | 2 participants (Actual) | Interventional | 2011-04-30 | Terminated | ||
Real-World Medication Adherence Trajectories to Nintedanib Among Idiopathic Pulmonary Fibrosis Patients[NCT05022784] | 1,500 participants (Actual) | Observational | 2021-08-23 | Completed | |||
Relative Bioavailability of 100 mg Nintedanib (Ofev®) Given as Four Capsules of 25 mg Compared to One Capsule of 100 mg Following Oral Administration in Healthy Male Subjects (an Open-label, Randomised, Single-dose, Two-period, Two-sequence Crossover Stud[NCT04938453] | Phase 1 | 20 participants (Actual) | Interventional | 2021-07-14 | Completed | ||
Multi-center Open-label Expanded Access Program of Oral Nintedanib 150 mg Twice Daily in Patients With Idiopathic Pulmonary Fibrosis[NCT02230982] | 0 participants | Expanded Access | No longer available | ||||
Safety of Nintedanib in Real World in China: a Non-interventional Study Based on Idiopathic Pulmonary (Interstitial) Fibrosis Registry China Study (PORTRAY) Data[NCT05676112] | 800 participants (Anticipated) | Observational | 2023-12-29 | Not yet recruiting | |||
Tolerability and Safety of Nintedanib in Myositis Associated Interstitial Lung Disease: a Pilot Study[NCT05335278] | 25 participants (Anticipated) | Interventional | 2021-06-01 | Recruiting | |||
A Single-centre, Open-label, Fixed-sequence Trial to Evaluate the Impact of C21 on the Exposure of CYP1A2, CYP2C9, CYP3A4 and P-gp Substrates in Healthy Volunteers[NCT05830799] | Phase 1 | 18 participants (Actual) | Interventional | 2023-03-29 | Completed | ||
LUME-Colon 2: An Open-label Randomized Phase II Study to Assess the Efficacy and Safety of Nintedanib Alone or in Combination With Capecitabine for Patients With Refractory Metastatic Colorectal Cancer[NCT02780700] | Phase 2 | 1 participants (Actual) | Interventional | 2016-07-05 | Terminated(stopped due to Substance discontinued) | ||
A Double-blind, Randomised Phase II Study to Determine Efficacy and Safety of Oral Treatment With BIBF 1120 ES 250 mg Twice Daily Versus 150 mg Twice Daily in Patients Suffering From Advanced Non-small-cell Lung Cancer[NCT02182050] | Phase 2 | 73 participants (Actual) | Interventional | 2005-08-31 | Completed | ||
A Phase I Open-label Dose-escalation Study of Continuous Twice-daily Oral Treatment With BIBF 1120 in Japanese Patients With Advanced Solid Tumours[NCT02182128] | Phase 1 | 24 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
A Phase I Open Label Dose Escalation Study of Continuous Once-daily or Twice Daily Oral Treatment With BIBF 1120 in Patients With Advanced Solid Tumours[NCT02182206] | Phase 1 | 50 participants (Actual) | Interventional | 2003-06-30 | Completed | ||
Phase II Evaluation of BIBF 1120 in the Treatment of Bevacizumab-Resistant, Persistent, or Recurrent Epithelial Ovarian, Fallopian Tube, or Primary Peritoneal Carcinoma[NCT01669798] | Phase 2 | 32 participants (Actual) | Interventional | 2013-02-28 | Completed | ||
INSTAGE: A 24-week, Double-blind, Randomized, Parallel-group Study Evaluating the Efficacy and Safety of Oral Nintedanib Co-administered With Oral Sildenafil, Compared to Treatment With Nintedanib Alone, in Patients With Idiopathic Pulmonary Fibrosis (IPF[NCT02802345] | Phase 3 | 274 participants (Actual) | Interventional | 2016-06-30 | Completed | ||
A Phase I Open Label Study of Continuous Oral Treatment With BIBF 1120 Together With Pemetrexed in Previously Treated Patients With Non-small Cell Lung Cancer[NCT02182102] | Phase 1 | 26 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
Safety and Tolerability of Single Rising Doses of 1 mg, 3 mg, 10 mg and 20 mg of BIBF 1120 as Intravenous Infusion (Single-blind, Placebocontrolled at Each Dose Group) and Absolute Bioavailability of 100 mg BIBF 1120 as Soft Gelatine Capsule (Intra-indivi[NCT02182258] | Phase 1 | 30 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
A Phase II Evaluation of BIBF 1120 in the Treatment of Recurrent or Persistent Endometrial Carcinoma[NCT01225887] | Phase 2 | 37 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
A Randomised Phase II Study Of Nintedanib (BIBF1120) Compared To Chemotherapy in Patients With Recurrent Clear Cell Carcinoma Of The Ovary Or Endometrium[NCT02866370] | Phase 2 | 120 participants (Anticipated) | Interventional | 2015-04-30 | Recruiting | ||
A Multicenter, Open Label, Phase I /Randomised Phase II Study to Evaluate Safety, Pharmacokinetics and Efficacy of BIBF 1120 in Comparison With Oral Sorafenib for Advanced Hepatocellular Carcinoma Patients.[NCT01004003] | Phase 2 | 125 participants (Actual) | Interventional | 2009-10-22 | Completed | ||
The Effect of Multiple Oral Doses of BI 1015550 on the Pharmacokinetics of Nintedanib and Pirfenidone Administered Single Dose to Healthy Male Subjects (Open-label, Two-period, Fixed-sequence Crossover Trial)[NCT06070610] | Phase 1 | 14 participants (Actual) | Interventional | 2023-11-08 | Completed | ||
Safety and Relative Bioavailability of a Single Dose of 150 mg BIBF 1120 Administered as Soft Gelatine Capsules Charge 1 Compared to BIBF 1120 Soft Gelatine Capsules Charge 2 Compared to BIBF 1120 Administered as Drinking Solution Following Oral Administr[NCT02182193] | Phase 1 | 54 participants (Actual) | Interventional | 2006-09-30 | Completed | ||
Post-marketing Surveillance on Long Term Use of Ofev Capsules in Systemic Scleroderma Associated Interstitial Lung Disease (SSc-ILD) in Japan[NCT04325217] | 550 participants (Anticipated) | Observational | 2020-04-15 | Recruiting | |||
A Phase 1, Single-Center, Fixed Sequence, Drug-Drug Interaction Study of ENV-101 (Taladegib) on Nintedanib Pharmacokinetics in Healthy Subjects[NCT05817240] | Phase 1 | 21 participants (Actual) | Interventional | 2023-05-03 | Completed | ||
Prospective Observational Investigation of Possible Correlations Between Change in FVC and Change in Cough or Dyspnea Scores Using the Living With Pulmonary Fibrosis Questionnaire (L-PF) Between Baseline and After Approximately 52 Weeks of Nintedanib Trea[NCT04702893] | 108 participants (Actual) | Observational | 2021-05-28 | Active, not recruiting | |||
Phase II Monocentric Randomized Study on Efficacy of Nintedanib for Treatment of Epistaxis in Hereditary Hemorrhagic Telangiectasia (HHT) Patients[NCT04976036] | Phase 2 | 48 participants (Anticipated) | Interventional | 2022-05-05 | Recruiting | ||
An Open Label Randomized Phase II Study of Oral Treatment With BIBF 1120 250 mg Twice Daily Versus 150 mg Twice Daily in Patients Suffering From Hormone Refractory Prostate Cancer After Progression With Docetaxel Based Regimen[NCT02182063] | Phase 2 | 81 participants (Actual) | Interventional | 2005-11-30 | Completed | ||
An Open Label Dose Escalation Study of BIBF 1120 Administered Orally for Four Weeks in Patients With Relapsed or Refractory Multiple Myeloma With Repeated Administration in Patients With Clinical Benefit[NCT02182141] | Phase 1 | 17 participants (Actual) | Interventional | 2003-04-30 | Completed | ||
A Phase I Open Label Dose Escalation Study of Continuous (Except on the Days of Chemotherapy Infusion) Oral Treatment With BIBF 1120 Together With Docetaxel and Prednisone in Patients With Hormone Refractory Prostate Cancer[NCT02182219] | Phase 1 | 21 participants (Actual) | Interventional | 2005-11-30 | Completed | ||
Nintedanib Plus Standard of Care Immunosuppression Versus Standard of Care Immunosuppression Alone in Patients With Progressive Fibrotic Myositis Associated - Interstitial Lung Disease: A Randomized, Double-Blind, Exploratory Trial[NCT05799755] | Phase 4 | 134 participants (Anticipated) | Interventional | 2023-08-01 | Recruiting | ||
Nintedanib as Maintenance Treatment of Pleural Malignant Mesothelioma (NEMO): a Randomized Double Blinded Phase II Study of the EORTC Lung Cancer Group[NCT02863055] | Phase 2 | 37 participants (Actual) | Interventional | 2018-02-04 | Active, not recruiting | ||
Multicenter Phase II Trial of Nintedanib (Vargatef®) Plus Docetaxel in Second Line of Treatment in Patients With no Squamous Non Small Cell Lung Cancer Refractory to First Line Chemotherapy[NCT02531737] | Phase 2 | 59 participants (Actual) | Interventional | 2015-09-30 | Completed | ||
A 12 Month, Double Blind, Randomized, Placebo-controlled Trial Evaluating the Effect of BIBF 1120 Administered at Oral Doses of 50 mg qd, 50 mg Bid, 100 mg Bid and 150 mg Bid on Forced Vital Capacity Decline During One Year, in Patients With Idiopathic Pu[NCT00514683] | Phase 2 | 432 participants (Actual) | Interventional | 2007-08-31 | Completed | ||
Phase II Trial of BIBF1120 (Nintedanib) in Patients With Recurrent or Metastatic Salivary Gland Cancer of the Head and Neck : a Multicentre Phase II Study[NCT02558387] | Phase 2 | 20 participants (Actual) | Interventional | 2014-11-30 | Active, not recruiting | ||
Phase I Dose Escalation Study of Nintedanib Plus Bevacizumab in Advanced Solid Tumors[NCT02835833] | Phase 1 | 21 participants (Actual) | Interventional | 2016-06-09 | Completed | ||
Randomized Double Blind Placebo-controlled Phase II Trial of Vargatef® (Nintedanib) in Addition to First Line Chemotherapy With Interval Debulking Surgery in Patients With Adenocarcinoma of the Ovary, the Fallopian Tube or Serous Adenocarcinoma of the Per[NCT01583322] | Phase 2 | 188 participants (Actual) | Interventional | 2012-06-30 | Completed | ||
Phase Ib, Open Label, Combination Study of Nintedanib With 5-Azacitidine in Acute Myeloid Leukemia Characterized by HOX Gene Overexpression, That Are Not Candidates of Intensive Chemotherapy[NCT03513484] | Phase 1 | 44 participants (Anticipated) | Interventional | 2018-11-14 | Active, not recruiting | ||
An Open Label, Randomised Study in Healthy Participants to Investigate the Effect of AZD5055 on the Pharmacokinetics of Nintedanib.[NCT05644600] | Phase 1 | 18 participants (Actual) | Interventional | 2023-05-26 | Terminated(stopped due to The study was terminated as no drug-drug interactions were observed in Part-A of the study and therefore Part-B of the study was not required as per protocol.) | ||
Multicenter, Randomized, Double-blind, Phase III Trial to Investigate the Efficacy and Safety of Oral BIBF 1120 Plus Standard Pemetrexed Therapy Compared to Placebo Plus Standard Pemetrexed Therapy in Patients With Stage IIIB/IV or Recurrent Non Small Cel[NCT00806819] | Phase 3 | 718 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
Phase II Double-Blind, Randomized, Placebo Controlled Study to Evaluate the Efficacy and Safety of Nintedanib (BIBF 1120) + Prednisone Taper in Patients With Radiation Pneumonitis[NCT02496585] | Phase 2 | 33 participants (Anticipated) | Interventional | 2015-07-31 | Active, not recruiting | ||
Multicentre, Randomised, Double-blind, Phase III Trial to Investigate the Efficacy and Safety of Oral BIBF 1120 Plus Standard Docetaxel Therapy Compared to Placebo Plus Standard Docetaxel Therapy in Patients With Stage IIIB/IV or Recurrent Non Small Cell [NCT00805194] | Phase 3 | 1,314 participants (Actual) | Interventional | 2008-12-03 | Completed | ||
A Combination Phase I Open Label Dose Escalation Study of Concomitant Administration of BIBW 2992 With BIBF 1120 in Patients With Advanced Solid Tumors[NCT00730821] | Phase 1 | 28 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
A Phase II Open Label, Roll Over Study of the Long Term Tolerability, Safety and Efficacy of Oral BIBF 1120 in Patients With Idiopathic Pulmonary Fibrosis[NCT01170065] | Phase 2 | 198 participants (Actual) | Interventional | 2010-06-25 | Completed | ||
Nintedanib Plus mFOLFOX6 for Previously Untreated Metastatic Esophagogastric Adenocarcinoma (MEGAN): A Randomized, Placebo-controlled, Triple-blind Phase II Study[NCT02856867] | Phase 2 | 0 participants (Actual) | Interventional | 2016-12-31 | Withdrawn | ||
Prospective Observational Investigation of Possible Correlations Between Change in FVC and Change in Cough or Dyspnea Scores Using the Living With Pulmonary Fibrosis Questionnaire (L-PF) Between Baseline and After Approximately 52 Weeks of Nintedanib Trea[NCT05151640] | 123 participants (Anticipated) | Observational | 2022-09-26 | Recruiting | |||
The Special Drug Use-results Survey (All-Case Surveillance) of Ofev® Capsules in Patients With Idiopathic Pulmonary Fibrosis (IPF) in Japan[NCT02607722] | 10,117 participants (Actual) | Observational | 2015-08-31 | Completed | |||
A Randomised Placebo-Controlled Phase II Study of Continuous Maintenance Treatment With BIBF 1120 Following Chemotherapy in Patients With Relapsed Ovarian Cancer[NCT00710762] | Phase 2 | 89 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
A Phase 1, Open-Label, Non-Randomized, Fixed Sequence Study to Evaluate the Steady-state Pharmacokinetics of BLD-0409, Nintedanib and Pirfenidone When Administered Concurrently in Healthy Volunteers[NCT04939467] | Phase 1 | 86 participants (Actual) | Interventional | 2021-10-15 | Completed | ||
Economic Burden Associated With Nintedanib Non-adherence Among Medicare Beneficiaries With IPF[NCT05870956] | 1,798 participants (Actual) | Observational | 2023-05-16 | Completed | |||
Extension Study to Establish Safety, Pharmacokinetics and Efficacy of BIBF 1120 in Patients With Previous Clinical Benefit From BIBF 1120[NCT00715403] | Phase 1 | 41 participants (Actual) | Interventional | 2004-10-31 | Completed | ||
A Double-blind, Randomised, Placebo-controlled (Within a Dose Group) Study to Evaluate Safety and Pharmacokinetics of Multiple Rising Doses of BIBF 1120 at 50 mg Bid (14 Days), 100 mg Bid (14 Days), and 150 mg Bid (28 Days) p.o., on Top of Standard Medica[NCT01136174] | Phase 2 | 50 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
Nintedanib Plus Usual Transplant Care Compared to Usual Transplant Care Alone After Single Lung Transplantation in Patients With Idiopathic Pulmonary Fibrosis: a Pilot Randomized Controlled Trial[NCT03562416] | Phase 2 | 1 participants (Actual) | Interventional | 2019-07-05 | Terminated(stopped due to Low enrollment) | ||
A Phase II Trial of Weekly Alternating Sequential Administration of BIBF 1120 and BIBW 2992 in Patients With Advanced Colorectal Cancer[NCT00801294] | Phase 2 | 46 participants (Actual) | Interventional | 2006-07-01 | Completed | ||
Phase I Study of Induction Cisplatin, Docetaxel, and Nintedanib for Stage IB-IIIA Non-Small Cell Lung Cancers Amenable for Surgical Resection[NCT02225405] | Phase 1 | 26 participants (Actual) | Interventional | 2015-04-03 | Active, not recruiting | ||
Multicenter, Randomised, Double-blind Phase III Trial to Investigate the Efficacy and Safety of BIBF 1120 in Combination With Carboplatin and Paclitaxel Compared to Placebo Plus Carboplatin and Paclitaxel in Patients With Advanced Ovarian Cancer[NCT01015118] | Phase 3 | 1,366 participants (Actual) | Interventional | 2009-11-17 | Completed | ||
Public-interest Multicenter Umbrella Trial Based on Genetic Analysis in Korean Head and Neck Cancer and Esophageal Cancer Patient - Part 1 (HNSCC)][NCT03292250] | Phase 2 | 180 participants (Actual) | Interventional | 2017-09-10 | Completed | ||
A Single Center, Open Label Study to Evaluate Drug-drug Interactions Between HEC585 and Pirfenidone or Nintedanib in Healthy Volunteers[NCT05383131] | Phase 1 | 33 participants (Actual) | Interventional | 2021-06-23 | Completed | ||
The Nintedanib in Progressive Pneumoconiosis Study (NiPPS): a Collaborative NSW Treatment Trial[NCT04161014] | Phase 2 | 100 participants (Anticipated) | Interventional | 2020-10-09 | Recruiting | ||
A Phase I/Phase II Study of Nintedanib Plus EGFR TKI In EGFR-mutated Non-small Cell Lung Cancer Patients[NCT06071013] | Phase 1/Phase 2 | 20 participants (Anticipated) | Interventional | 2023-09-28 | Not yet recruiting | ||
An Open Label Dose Escalation Study of BIBF 1120 Administered Orally for Four Weeks in Patients With Advanced Solid Tumours With Repeated Administration in Patients With Clinical Benefit[NCT01951846] | Phase 1 | 61 participants (Actual) | Interventional | 2002-11-30 | Completed | ||
Phase I Dose Escalation Study of Concomitant BIBF 1120 and BIBW 2992 in Patients With Advanced Solid Tumours.[NCT00998296] | Phase 1 | 70 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
Expanded Access Program of OFEV® (Nintedanib) in Children and Adolescents (6- to 17-year-old) With Clinically Significant Fibrosing Interstitial Lung Disease (ILD)[NCT05624281] | 0 participants | Expanded Access | Temporarily not available | ||||
Investigating Trends in Quality of Life in Patients With Idiopathic Pulmonary Fibrosis (IPF) Under Treatment With Nintedanib[NCT03710824] | 180 participants (Actual) | Observational | 2019-02-28 | Completed | |||
An Open-label Trial of the Long-term Safety and Tolerability of Nintedanib Per os, on Top of Standard of Care, Over at Least 2 Years, in Children and Adolescents With Clinically Significant Fibrosing Interstitial Lung Disease (InPedILD®-ON)[NCT05285982] | Phase 3 | 60 participants (Anticipated) | Interventional | 2022-04-04 | Recruiting | ||
Dose Ranging Study of Oral Epigallocatechin-3-gallate (EGCG) Given Daily for 12 Weeks to Patients With Idiopathic Pulmonary Fibrosis (IPF) Evaluating Safety, PK Interactions With Standard of Care Drugs, and Biomarkers of Drug Effect[NCT05195918] | Phase 1 | 50 participants (Anticipated) | Interventional | 2023-08-24 | Recruiting | ||
ENGOT-EN1/FANDANGO: A Randomized Phase II Trial of First-line Combination Chemotherapy With Nintedanib / Placebo for Patients With Advanced or Recurrent Endometrial Cancer[NCT02730416] | Phase 2 | 146 participants (Actual) | Interventional | 2016-12-12 | Completed | ||
Assessment of the Dose Reduction and Discontinuation Associated With Anti-Fibrotic Medications in Patients With Idiopathic Pulmonary Fibrosis[NCT05779007] | 2,778 participants (Actual) | Observational | 2023-04-18 | Completed | |||
A 52 Weeks, Double Blind, Randomized, Placebo-controlled Trial Evaluating the Effect of Oral BIBF 1120, 150 mg Twice Daily, on Annual Forced Vital Capacity Decline, in Patients With Idiopathic Pulmonary Fibrosis (IPF)[NCT01335477] | Phase 3 | 551 participants (Actual) | Interventional | 2011-05-31 | Completed | ||
A 52 Weeks, Double Blind, Randomized, Placebo-controlled Trial Evaluating the Effect of Oral BIBF 1120, 150 mg Twice Daily, on Annual Forced Vital Capacity Decline, in Patients With Idiopathic Pulmonary Fibrosis (IPF)[NCT01335464] | Phase 3 | 515 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
LUME-Lung 3: A Phase I/II Study of Continuous Oral Treatment With BIBF 1120 Added to Standard Gemcitabine/Cisplatin Therapy in First Line NSCLC Patients With Squamous Cell Histology[NCT01346540] | Phase 1 | 16 participants (Actual) | Interventional | 2011-04-14 | Completed | ||
Nintedanib Plus Letrozole in Postmenopausal Women With Breast Cancer: Clinical Trial Phase 0/1 Safety and Pharmacodynamics[NCT02619162] | Phase 1 | 25 participants (Actual) | Interventional | 2015-07-31 | Completed | ||
An Open Label Phase I Dose Escalation Trial of Intravenous BI 6727 in Combination With Oral BIBF 1120 in Patients With Advanced Solid Tumours With Repeated Administration in Patients With Clinical Benefit[NCT01022853] | Phase 1 | 30 participants (Actual) | Interventional | 2009-12-31 | Completed | ||
A Randomised, Open Label, Parallel Group Phase II Study Comparing the Efficacy and Tolerability of BIBF 1120 Versus Sunitinib in Previously Untreated Patients With Renal Cell Cancer[NCT01024920] | Phase 2 | 99 participants (Actual) | Interventional | 2009-12-16 | Completed | ||
A Phase I/II Study of Continuous, Concomitant Oral Treatment With BIBF 1120 and Pemetrexed - a Phase I, Open-label, Dose-escalation Study & a Phase II, 2 Arm, Randomized, Double-blind, Placebo-controlled Study in Japanese Patients With Stage IIIB/IV or Re[NCT00979576] | Phase 1 | 19 participants (Actual) | Interventional | 2009-10-31 | Terminated | ||
A Phase I Study of Continuous, Concomitant Oral Treatment With BIBF 1120 and Docetaxel - a Phase I, Open-label, Dose-escalation Study in Japanese Patients With Stage IIIB/IV or Recurrent Non-small-cell Lung Cancer After Failure of Chemotherapy[NCT00876460] | Phase 1 | 43 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
"A Phase II Multicenter Study Comparing the Efficacy of the Oral Angiogenesis Inhibitor Nintedanib With the Intravenous Cytotoxic Compound Ifosfamide for Treatment of Patients With Advanced Metastatic Soft Tissue Sarcoma After Failure of Systemic Non-oxaz[NCT02808247] | Phase 2 | 80 participants (Actual) | Interventional | 2017-07-07 | Terminated(stopped due to Exceed of pre-specified number of failures in the experimental arm) | ||
A Phase I Study for Formulation Selection and Subsequent Optimization of Two Different Oral Formulations of Nintedanib in Healthy Male Subjects (Open-label, Randomised, Single-dose Study in Three Parts)[NCT05262751] | Phase 1 | 21 participants (Actual) | Interventional | 2022-03-28 | Completed | ||
"Nintedanib for the Treatment of SARS-Cov-2 Induced Pulmonary Fibrosis"[NCT04541680] | Phase 3 | 250 participants (Anticipated) | Interventional | 2020-10-29 | Recruiting | ||
A Phase I-II Study of BIBF 1120 and FOLFOX Compared to Bevacizumab and FOLFOX in First Line Metastatic Colorectal Cancer Patients[NCT00904839] | Phase 2 | 128 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
A 12-week, Double Blind, Randomised, Placebo Controlled, Parallel Group Trial Followed by a Single Active Arm Phase of 40 Weeks Evaluating the Effect of Oral Nintedanib 150 mg Twice Daily on Change in Biomarkers of Extracellular Matrix (ECM) Turnover in P[NCT02788474] | Phase 4 | 347 participants (Actual) | Interventional | 2016-06-09 | Completed | ||
A Single-arm, Open Label, Multi-center Phase I/II Trial to Assess the Safety and Efficacy of BIBF 1120 Added to Low-dose Cytarabine in Elderly Patients With AML Unfit for an Intensive Induction Therapy[NCT01488344] | Phase 1/Phase 2 | 140 participants (Anticipated) | Interventional | 2012-03-31 | Active, not recruiting | ||
A Multicentre, Retrospective Chart Review Study to Describe the Clinical Profile of Idiopathic Pulmonary Fibrosis (IPF) Patients Treated With Nintedanib (OFEV®) in Real-world Practice in Spain.[NCT03281200] | 172 participants (Actual) | Observational | 2017-10-24 | Completed | |||
A Double Blind, Randomized, Placebo-controlled Trial Evaluating the Efficacy and Safety of Nintedanib Over 52 Weeks in Chinese Patients With Chronic Fibrosing ILDs With a Progressive Phenotype[NCT05065190] | Phase 3 | 81 participants (Actual) | Interventional | 2021-11-25 | Active, not recruiting | ||
A Phase 1b and Pharmacodynamic Study of Nintedanib Monotherapy for Advanced Pancreatic Cancer[NCT02902484] | Phase 1/Phase 2 | 14 participants (Actual) | Interventional | 2017-09-07 | Active, not recruiting | ||
A Phase I-II Randomized Trial of a Combination of Nintedanib/Placebo in Combination With Induction Chemotherapy for Patients With Refractory or First Relapse Acute Myeloid Leukemia[NCT02665143] | Phase 2 | 25 participants (Actual) | Interventional | 2016-07-21 | Completed | ||
An Open-label Extension Trial of the Long Term Safety of Oral BIBF 1120 in Patients With Idiopathic Pulmonary Fibrosis (IPF)[NCT01619085] | Phase 3 | 752 participants (Actual) | Interventional | 2012-06-06 | Completed | ||
Multicenter Phase 2 Study of Nintedanib for Patients With Advanced Carcinoid Tumors[NCT02399215] | Phase 2 | 32 participants (Actual) | Interventional | 2015-05-15 | Completed | ||
An Exploratory Multicenter, Open-Label, Single Arm Study of the Safety and Tolerability of Pirfenidone (Esbriet®) in Combination With Nintedanib (Ofev®) in Patients With Idiopathic Pulmonary Fibrosis[NCT02598193] | Phase 4 | 89 participants (Actual) | Interventional | 2016-01-14 | Completed | ||
Phase Ib Trial Of Pembrolizumab And Nintedanib[NCT02856425] | Phase 1 | 221 participants (Anticipated) | Interventional | 2016-11-10 | Recruiting | ||
LCI-GI-APX-NIN-001: Nintedanib in Metastatic Appendiceal Carcinoma[NCT03287947] | Phase 2 | 5 participants (Actual) | Interventional | 2017-11-10 | Terminated(stopped due to Low enrollment) | ||
Phase II Trial of Triple Receptor Tyrosine Kinase Receptor Inhibitor BIBF 1120 in Recurrent High-Grade Gliomas[NCT01380782] | Phase 2 | 37 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
Nintedanib in Patients With Bronchiolitis Obliterans Syndrome Following Hematopoietic Stem Cell Transplantation (HSCT)- a Multicentre Phase II Trial[NCT03805477] | Phase 2 | 20 participants (Anticipated) | Interventional | 2019-03-20 | Recruiting | ||
Bioequivalence of 1 Soft Gelatine Capsule Containing 200 mg Nintedanib Compared to 2 Soft Gelatine Capsules Containing 100 mg Nintedanib Following Oral Administration in Healthy Male Subjects[NCT02572752] | Phase 1 | 70 participants (Actual) | Interventional | 2015-08-31 | Completed | ||
A Phase II Trial of BIBF1120 in Patients With Advanced FGFR3 Mutated, FGFR3 Overexpressed, or FGFR3 Wild Type Urothelial Carcinoma of Urinary Bladder, Urethra, Ureter, and Renal Pelvis and Who Have Failed Platinum-based Chemotherapy[NCT02278978] | Phase 2 | 129 participants (Anticipated) | Interventional | 2014-10-31 | Active, not recruiting | ||
An Open Label Phase I Dose Escalation Trial of Oral BIBF 1120 in Combination With Intravenous Carboplatin and Vinorelbine in Elderly Patients With Advanced Non-Small Cell Lung Cancer - Stage IV[NCT01683682] | Phase 1 | 8 participants (Actual) | Interventional | 2013-04-30 | Completed | ||
An Open Label Phase I Dose Escalation Trial of Oral BIBF 1120 in Combination With Intravenous Vinorelbine in Elderly Patients With Advanced Non Small Lung Cell Cancer - Stage IV[NCT01684111] | Phase 1 | 7 participants (Actual) | Interventional | 2013-06-30 | Completed | ||
A Phase II Randomized Study of Docetaxel With or Without NINTEDANIB (BIBF-1120) in Patient Receiving a First or Second-line of Chemotherapy for HER Negative Metastatic or Locally Recurrent Breast Cancer[NCT01658462] | Phase 2 | 51 participants (Actual) | Interventional | 2013-05-31 | Completed | ||
A Phase I/II, Randomized, Open-label, Multi-centre Study of BIBF1120 + Reirradiation (R-RT) Versus Reirradiation in the Treatment of Patients With First or Second Progression of Glioblastoma[NCT01666600] | Phase 1/Phase 2 | 63 participants (Actual) | Interventional | 2012-08-31 | Terminated(stopped due to Interim Analysis for Feasibility) | ||
Phase I/II Study of Nivolumab and Ipilimumab Combined With Nintedanib in Non Small Cell Lung Cancer[NCT03377023] | Phase 1/Phase 2 | 68 participants (Actual) | Interventional | 2018-02-02 | Active, not recruiting | ||
Relative Bioavailability of Nintedanib Given Alone and in Combination With Ketoconazole at Steady State in Healthy Male Volunteers (an Open-label, Randomised, Two-way Cross-over Clinical Phase I Study)[NCT01679613] | Phase 1 | 34 participants (Actual) | Interventional | 2012-09-30 | Completed | ||
A Phase II Study Exploring the Safety and Efficacy of Nintedanib (BIBF1120) as Second Line Therapy for Patients With Either Differentiated or Medullary Thyroid Cancer Progressing After First Line Therapy.[NCT01788982] | Phase 2 | 100 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
A Phase II Study of BIBF1120 (Nintedanib) for Patients With Metastatic HER2-Negative Inflammatory Breast Cancer (IBC)[NCT02389764] | Phase 2 | 10 participants (Actual) | Interventional | 2015-06-22 | Terminated(stopped due to Slow Accrual) | ||
Characteristics of IPF Patients Initiating Nintedanib, Pirfenidone or no Antifibrotic Treatment in the US[NCT03958071] | 13,264 participants (Actual) | Observational | 2019-02-01 | Completed | |||
An Open Label Phase I Safety run-in Trial of Oral Nintedanib Plus Docetaxel Therapy in Japanese Patients With Locally Advanced or Metastatic Adenocarcinoma Subtype Non-small Cell Lung Cancer After Failure of Platinum-based First Line Chemotherapy[NCT02300298] | Phase 1 | 10 participants (Actual) | Interventional | 2014-12-24 | Completed | ||
A Phase II Study Of BIBF 1120 as Second-line Treatment for Patients With Small Cell Lung Cancer[NCT01441297] | Phase 2 | 24 participants (Actual) | Interventional | 2011-12-31 | Completed | ||
A Phase I Trial to Investigate the Effect of Nintedanib on the Pharmacokinetics of a Combination of Ethinylestradiol and Levonorgestrel in Female Patients With Systemic Sclerosis Associated Interstitial Lung Disease (SSc-ILD)[NCT03675581] | Phase 1 | 17 participants (Actual) | Interventional | 2018-11-08 | Completed | ||
"BGOG-cx1/ENGOT-cx1: Randomized Double-blind Phase II Study Comparing 3-weekly Carboplatin + Paclitaxel With or Without Concomitant and Maintenance Nintedanib (NINTEDANIB) in Advanced or Recurrent Cervical Carcinoma."[NCT02009579] | Phase 2 | 120 participants (Actual) | Interventional | 2014-03-31 | Active, not recruiting | ||
A Multicenter, Open Label, Phase I/Randomized II Study to Evaluate Safety, Pharmacokinetics and Efficacy of BIBF 1120 in Comparison With Sorafenib for Advanced Hepatocellular Carcinoma Patients in Asia.[NCT00987935] | Phase 2 | 134 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
Feasibility and Safety of Nintedanib in Combination With Nivolumab in Pretreated Patients With Advanced or Metastatic NSCLC of Adenocarcinoma Histology - An AIO Phase Ib Trial[NCT04046614] | Phase 1/Phase 2 | 56 participants (Actual) | Interventional | 2018-05-25 | Active, not recruiting | ||
Efficacy and Safety of Nintedanib Ethanesulfonate Soft Capsule in the Treatment of Pulmonary Fibrosis in Patients With Moderate to Severe COVID-9(COVID 19) : a Single-center, Randomized, Placebo-controlled Study[NCT04338802] | Phase 2 | 96 participants (Anticipated) | Interventional | 2020-04-02 | Not yet recruiting | ||
A Twelve Week, Open-label, Randomised, Parallel-group Study Evaluating Safety, Tolerability and Pharmacokinetics (PK) of Oral Nintedanib in Combination With Oral Pirfenidone, Compared to Treatment With Nintedanib Alone, in Patients With Idiopathic Pulmona[NCT02579603] | Phase 4 | 105 participants (Actual) | Interventional | 2015-10-16 | Completed | ||
Phase II, Randomised, Placebo Controlled, Multicentre, Feasibility Study of Low Dose (Metronomic) Cyclophosphamide With and Without Nintedanib (BIBF 1120) in Advanced Ovarian Cancer[NCT01610869] | Phase 2 | 117 participants (Actual) | Interventional | 2014-08-31 | Completed | ||
A Phase I/II Study of Nintedanib and Capecitabine in Refractory Metastatic Colorectal Cancer[NCT02393755] | Phase 1/Phase 2 | 42 participants (Actual) | Interventional | 2015-05-08 | Completed | ||
A Six Month Double Blind Randomized Placebo Controlled Trial Followed by Each Arm Being Converted to Oral Nintedanib 150 mg Twice Daily Comparing the Effect on High Resolution Computerized Tomography Quantitative Lung Fibrosis Score, Lung Function, Six Mi[NCT01979952] | Phase 3 | 113 participants (Actual) | Interventional | 2013-11-26 | Completed | ||
A Phase II Randomized, Double-Blind, Placebo-Controlled Study Evaluating Nintedanib Versus Placebo as Prophylaxis Against Radiation Pneumonitis in Patients With Unresectable NSCLC Undergoing Chemoradiation Therapy[NCT02452463] | Phase 2 | 8 participants (Actual) | Interventional | 2015-06-29 | Terminated(stopped due to low accrual) | ||
FGFR1 Amplification as A Predictor of Efficacy in A Biomarker-Driven Phase II Study of BIBF 1120 in Advanced Squamous Cell Lung Cancer Patients Who Have Failed Up to Two Prior Chemotherapeutic Regimens[NCT01948141] | Phase 2 | 6 participants (Actual) | Interventional | 2014-01-30 | Completed | ||
Influence of Bosentan on the Pharmacokinetics of Nintedanib in Healthy Male Subjects[NCT02667704] | Phase 1 | 13 participants (Actual) | Interventional | 2016-02-29 | Completed | ||
A Phase I Trial to Investigate the Effect of Nintedanib on the Pharmacokinetics of a Combination of Ethinylestradiol and Levonorgestrel in Patients With Non-small Cell Lung Cancer[NCT02751385] | Phase 1 | 2 participants (Actual) | Interventional | 2016-05-20 | Terminated(stopped due to Terminated- Study halted due to low recruitment.) | ||
A Double Blind, Randomised, Placebo-controlled Trial to Evaluate the Dose-exposure and Safety of Nintedanib Per os on Top of Standard of Care for 24 Weeks, Followed by Open Label Treatment With Nintedanib of Variable Duration, in Children and Adolescents [NCT04093024] | Phase 3 | 39 participants (Actual) | Interventional | 2019-12-03 | Completed | ||
Prospective Clinical Study of Nintedanib to Inhibit Endometrial Fibrosis to Prevent Recurrence of Uterine Adhesions[NCT05635071] | Phase 2/Phase 3 | 90 participants (Anticipated) | Interventional | 2023-12-01 | Not yet recruiting | ||
Investigation of Drug-drug Interaction Between Nintedanib and Pirfenidone in Patients With IPF (an Open Label, Multiple-dose, Two Group Study)[NCT02606877] | Phase 4 | 37 participants (Actual) | Interventional | 2016-04-19 | Completed | ||
A Double-blind, Randomised, Placebo Controlled Phase III Study of Nintedanib Plus Best Supportive Care (BSC) Versus Placebo Plus BSC in Patients With Metastatic Colorectal Cancer Refractory to Standard Therapies.[NCT02149108] | Phase 3 | 768 participants (Actual) | Interventional | 2014-09-25 | Completed | ||
An Open Label Phase I of Oral Nintedanib Plus Weekly Docetaxel Therapy in Patients With Locally Advanced or Metastatic Lung Adenocarcinoma After Failure of Platinum -Based First Line Chemotherapy[NCT02668393] | Phase 1 | 14 participants (Actual) | Interventional | 2016-03-07 | Completed | ||
Pharmacokinetics, Safety and Tolerability of Nintedanib Single Oral Dose in Male and Female Patients With Different Degrees of Hepatic Impairment (Child-Pugh Classification A and B) as Compared With Nintedanib Administration to Male and Female Healthy Sub[NCT02191865] | Phase 1 | 33 participants (Actual) | Interventional | 2014-07-31 | Completed | ||
A Double Blind, Randomised, Placebo-controlled Trial Evaluating Efficacy and Safety of Oral Nintedanib Treatment for at Least 52 Weeks in Patients With Systemic Sclerosis Associated Interstitial Lung Disease (SSc-ILD)[NCT02597933] | Phase 3 | 580 participants (Actual) | Interventional | 2015-11-12 | Completed | ||
A Multi-center, Randomised, Double-blind Trial of Nintedanib in Lung Transplant (LTx) Recipients With Bronchiolitis Obliterans Syndrome (BOS) Grade 0p-1-2[NCT03283007] | Phase 3 | 80 participants (Anticipated) | Interventional | 2019-10-30 | Recruiting | ||
An Open Label, Dose Escalation Phase I Study to Evaluate the Safety and Tolerability of Continuous Twice-daily Oral Treatment of Nintedanib in Japanese Patients With Hepatocellular Carcinoma.[NCT01594125] | Phase 1 | 30 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
Relative Bioavailability of a Single Oral Dose of Nintedanib Given Alone and in Combination With Multiple Oral Doses of Rifampicin in Healthy Male Volunteers (an Open-label, Two-period, Fixed Sequence Phase I Trial)[NCT01770392] | Phase 1 | 26 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
A Phase 2, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety and Efficacy of FG-3019 in Patients With Idiopathic Pulmonary Fibrosis[NCT01890265] | Phase 2 | 160 participants (Actual) | Interventional | 2013-07-30 | Completed | ||
"An Open Label, 2-part, One-sequence, 3-period Study to Evaluate Drug-drug Interactions Between DWN12088 and Pirfenidone or Nintedanib in Healthy Volunteers"[NCT04888715] | Phase 1 | 48 participants (Actual) | Interventional | 2021-07-23 | Completed | ||
A Study of the Efficacy and Safety of Pirfenidone vs. Nintedanib in the Treatment of Fibrotic Lung Disease After Coronavirus Disease-19 Pneumonia[NCT04856111] | Phase 4 | 48 participants (Anticipated) | Interventional | 2021-03-17 | Active, not recruiting | ||
A Double Blind, Randomized, Placebo-controlled Trial Evaluating the Efficacy and Safety of Nintedanib Over 52 Weeks in Patients With Progressive Fibrosing Coal Mine Dust-Induced Interstitial Lung Disease (PF-CMD-ILD)[NCT05067517] | Phase 3 | 160 participants (Anticipated) | Interventional | 2021-11-30 | Not yet recruiting | ||
Early Nintedanib Deployment in COVID-19 Interstitial Lung Disease[NCT04619680] | Phase 4 | 103 participants (Actual) | Interventional | 2020-11-18 | Active, not recruiting | ||
LUME-Meso: Double Blind, Randomised, Multicentre, Phase II/III Study of Nintedanib in Combination With Pemetrexed / Cisplatin Followed by Continuing Nintedanib Monotherapy Versus Placebo in Combination With Pemetrexed / Cisplatin Followed by Continuing Pl[NCT01907100] | Phase 2/Phase 3 | 545 participants (Actual) | Interventional | 2013-09-19 | Terminated | ||
A Phase II Open Label, Follow up Study to Investigate the Long Term Tolerability and Safety of Oral BIBF 1120 on Top of Pirfenidone in Japanese Patients With Idiopathic Pulmonary Fibrosis[NCT01417156] | Phase 2 | 20 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
A Pilot Study of Nintedanib for LymphAngioleioMyomatosis (LAM)[NCT03062943] | Phase 2 | 30 participants (Actual) | Interventional | 2016-12-06 | Completed | ||
Phase I/II,Multicenter,Randomized,Double-blind,Placebo-controlled Trial Evaluating the Efficacy and Safety of Nintedanib/Vargatef in Combination With Paclitaxel Chemotherapy for Treatment of Patients With BRAF Wildtype Metastatic Melanoma[NCT02308553] | Phase 1/Phase 2 | 33 participants (Actual) | Interventional | 2015-03-17 | Completed | ||
An Open-label Extension Trial of the Long Term Safety of Nintedanib in Patients With 'Systemic Sclerosis Associated Interstitial Lung Disease' (SSc-ILD)[NCT03313180] | Phase 3 | 444 participants (Actual) | Interventional | 2017-11-27 | Completed | ||
Phase II Trial of Nintedanib in Patients With Advanced Esophagogastric Cancer[NCT02234596] | Phase 2 | 34 participants (Actual) | Interventional | 2014-09-04 | Completed | ||
Multicentre, Randomised, Double-blind, Phase III Trial to Investigate the Efficacy and Safety of Oral Nintedanib Plus Docetaxel Therapy Compared to Placebo Plus Docetaxel Therapy in Patients With Stage IIIB/IV or Recurrent, Adenocarcinoma Subtype Non-smal[NCT02231164] | Phase 3 | 12 participants (Actual) | Interventional | 2014-10-31 | Terminated | ||
A Phase II Trial of BIBF 1120 (Nintedanib) in Recurrent Malignant Pleural Mesothelioma[NCT02568449] | Phase 2 | 20 participants (Actual) | Interventional | 2016-03-15 | Completed | ||
Medical Need Program With Ofev® (Nintedanib) for the Treatment of Adult Patients With Non-IPF (Idiopathic Pulmonary Fibrosis) Chronic Fibrosing Interstitial Lung Diseases (ILDs) With a Progressive Phenotype (PF-ILD's)[NCT04739150] | 0 participants | Expanded Access | No longer available | ||||
A Phase 1, Four-part, Fixed-sequence, Open-label Study to Evaluate the Effect of Multiple Doses of CC-90001 on the Pharmacokinetics of Omeprazole, Midazolam, Warfarin, Rosuvastatin, Metformin, Digoxin, and Nintedanib in Healthy Adult Subjects[NCT03363815] | Phase 1 | 56 participants (Actual) | Interventional | 2017-12-04 | Completed | ||
A Phase I Trial of Combination Nab-Paclitaxel and Nintedanib or Nab-paclitaxel and Placebo in Relapsed Non-Small Cell Lung Cancer Adenocarcinoma[NCT03361319] | Phase 1/Phase 2 | 0 participants (Actual) | Interventional | 2020-07-31 | Withdrawn(stopped due to Withdrawal of financial support from funder) | ||
A Pilot Study of Nintedanib in Molecularly Selected Patients With Advanced Non-Small Cell Lung Cancer (NSCLC)[NCT02299141] | Phase 2 | 20 participants (Actual) | Interventional | 2015-05-07 | Active, not recruiting | ||
A Regulatory Required Non-interventional Study to Monitor the Safety and Effectiveness of Ofev(Nintedanib 150mg/100mg BID) in Korean Patients[NCT04525547] | 70 participants (Actual) | Observational | 2021-01-13 | Completed | |||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |