ID Source | ID |
---|---|
PubMed CID | 123631 |
CHEMBL ID | 939 |
CHEBI ID | 49668 |
SCHEMBL ID | 7866 |
MeSH ID | M0444984 |
Synonym |
---|
AC-1556 |
4-quinazolinamine, n-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-4-morpholin)propoxy)- |
4-quinazolinamine, n-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(4-morpholinyl)propoxy)- |
ccris 9011 |
zd 1839 |
gefitinib [usan] |
cid_123631 |
bdbm5447 |
n-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine |
zd1839 |
iressa , |
n-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]quinazolin-4-amine |
chembl939 , |
HY-50895 |
AB01273954-01 |
AB01273954-03 |
AB01273954-02 |
184475-35-2 |
g-4408 |
gefitinib , |
n-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine |
nsc715055 |
zd-1839 |
n-(3-chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine |
NCHEMBIO866-COMP14 |
4-quinazolinamine, n-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]- |
gefitini; iressa |
K00240 |
3-chloro-4-fluoro-n-[(4z)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4(1h)-ylidene]aniline |
IRE , |
BCB03_000781 |
n-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(4-morpholinyl)propoxy)-4-quinazolinamine |
4-(3'-chloro-4'-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline |
NCGC00159455-02 |
NCGC00159455-03 |
DB00317 |
iressa (astrazeneca) |
nsc-715055 |
gefitinib (jan/usan/inn) |
D01977 |
iressa (tn) |
KBIOSS_002241 |
CU-00000000396-1 , |
6-(3-morpholinopropoxy)-n-(3-chloro-4-fluorophenyl)-7-methoxyquinazolin-4-amine |
irressat |
CHEBI:49668 , |
gefitinibum |
HMS2089B19 |
AKOS000280752 |
iressa(tm) |
n-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine |
n-(3-chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine |
nsc-759856 |
EC-000.2409 |
KINOME_3321 |
KINOME_3322 |
STK621310 |
NCGC00159455-06 |
NCGC00159455-04 |
NCGC00159455-05 |
cas-184475-35-2 |
tox21_111683 |
dtxcid6021034 |
dtxsid8041034 , |
A812870 |
nsc759856 |
pharmakon1600-01502274 |
GEFITINIB - IRESSA |
c22h24clfn4o3 |
BCP9000718 |
gefitinib [usan:inn:ban] |
s65743jhbs , |
nsc 759856 |
unii-s65743jhbs |
HMS3244N21 |
HMS3244M22 |
HMS3244M21 |
BCPP000221 |
smr002204119 |
MLS003899193 |
gefitinib,zd-1839,iressa |
FT-0602325 |
NCGC00159455-08 |
AB20814 |
gefitinib [orange book] |
gefitinib [inn] |
gefitinib [jan] |
gefitinib [ema epar] |
gefitinib [who-dd] |
gefitinib [mi] |
gefitinib [ep monograph] |
gefitinib [vandf] |
gefitinib [mart.] |
CS-0124 |
S1025 |
gtpl4941 |
CCG-220642 |
AM20090619 |
SCHEMBL7866 |
NCGC00159455-09 |
tox21_111683_1 |
KS-1204 |
4-(3'-chloro-4'-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)-quinazoline |
Q-201149 |
gefitinib (zd1839) |
AB01273954_04 |
mfcd04307832 |
gefitinib (iressa) , |
(3-chloro-4-fluoro-phenyl)-[7-methoxy-6-(3-morpholin-4-yl-propoxy)-quinazolin-4-yl]-amine |
SR-00000000262-2 |
sr-00000000262 |
HMS3654A07 |
gefitinib for system suitability, europepharmacopoeia (ep) reference standard |
gefitinib, europepharmacopoeia (ep) reference standard |
gefitinib, >=98% (hplc) |
SR-00000000262-3 |
NCGC00159455-14 |
HMS3714A05 |
4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-(3-morpholinopropoxy)quinazoline |
SY002154 |
SW199108-4 |
Q417824 |
Z1546610485 |
HMS3677H08 |
BCP01365 |
HMS3413H08 |
HMS3295A21 |
HMS3748E17 |
nsc-800105 |
nsc800105 |
CS-0622782 |
HY-50895G |
gefitinib (gmp) |
EN300-123024 |
BG164498 |
gefitinib (mart.) |
gefitinib (ep monograph) |
l01xe02 |
G0546 |
Gefitinib is an inhibitor of epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) commonly used to suppress tumour growth. It is a widely used therapeutic drug for non-small cell lung cancer (NSCLC)
Gefitinib has an anti-migratory effect on MDA-MB231 that results in anAnti-proliferative effect. Has a modest activity in previously treated patients with advanced non-small cell lung cancer (NSCLC)
Gefitinib has been shown to inhibit cell survival and growth signaling pathways such as the extracellular signal-regulated kinase 1/2 pathway and the Akt pathway, as a consequence of the inactivation of EGFR. The drug has been approved for the treatment of patients with non-small cell lung cancer.
Gefitinib has lower anti-tumor activity on A549 lung cancer cells when co-cultured with HFL-1 fibroblasts. Gefit inib can inhibit ABCG2-mediated PpIX efflux from malignant brain tumor cells to increase the intracellular Ppix.
The gefitinib + anlotinib treatment exerted a synergistic antitumor effect by downregulating the activation of VEGFR2 and downstream effectors, Akt and ERK. Gefit inib treatment for bone metastases in patients harboring EGFR mutation resulted in a beneficial osteosclerotic change in most patients.
Gefitinib (GEF) is a multi-targeted tyrosine kinase inhibitor with anti-cancer properties. Few cases of cardiotoxicity has been reported as a significant side effect associated with GEF treatment.
We studied the combination of bexarotene and gefitinib in the third-line treatment of advanced non-small-cell lung cancer to examine pharmacokinetic interactions and establish the maximum tolerated dose. The potential for drug interactions between gef itinib and cytotoxic agents was evaluated through pharmacokinetics assessments.
Osimertinib, rather than gefitinib combined with anti-PD-L1 treatment could lead to lung injury in an EGFR mutated tumor-bearing mouse model.
Gefitinib (Iressa, ZD 1839) is an orally bioavailable small molecule that selectively inhibits epidermal growth factor receptor(EGFR) tyrosine kinase activity. Resveratrol and Gefit inib are adjunct therapies for various cancers. Both have been limited by low solubility, low cellular uptake, and bioavailability issues.
Gefitinib and sirolimus were administered on a continuous daily dosing schedule. At 200 days suppressed small intestinal tumourigenesis more effectively than either treatment alone (median small intestinal adenoma volume (47 mm(3) (comb) vs 248’mm( 3) (AZ12253801), P=0.5).
Role | Description |
---|---|
antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
epidermal growth factor receptor antagonist | An antagonist at the epidermal growth factor receptor. |
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Class | Description |
---|---|
quinazolines | Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives. |
morpholines | Any compound containing morpholine as part of its structure. |
aromatic ether | Any ether in which the oxygen is attached to at least one aryl substituent. |
monochlorobenzenes | Any member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine. |
monofluorobenzenes | Any member of the class of fluorobenzenes containing a mono- or poly-substituted benzene ring carrying a single fluorine substitutent. |
secondary amino compound | A compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups. |
tertiary amino compound | A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Pathway | Proteins | Compounds |
---|---|---|
Gefitinib Action Pathway | 1 | 1 |
EGFR tyrosine kinase inhibitor resistance | 0 | 3 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
acetylcholinesterase | Homo sapiens (human) | Potency | 36.7865 | 0.0025 | 41.7960 | 15,848.9004 | AID1347395; AID1347398 |
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 12.3572 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
Fumarate hydratase | Homo sapiens (human) | Potency | 29.6535 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
TDP1 protein | Homo sapiens (human) | Potency | 5.3091 | 0.0008 | 11.3822 | 44.6684 | AID686979 |
GLI family zinc finger 3 | Homo sapiens (human) | Potency | 14.1467 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 32.4648 | 0.1800 | 13.5574 | 39.8107 | AID1460; AID1468 |
AR protein | Homo sapiens (human) | Potency | 26.5854 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID743042; AID743054 |
caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 33.4915 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 7.4978 | 0.0006 | 57.9133 | 22,387.1992 | AID1259377; AID1259378 |
nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 3.7197 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224893 |
progesterone receptor | Homo sapiens (human) | Potency | 27.3116 | 0.0004 | 17.9460 | 75.1148 | AID1346784; AID1346795 |
EWS/FLI fusion protein | Homo sapiens (human) | Potency | 30.5401 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 22.8506 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 5.6804 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 16.7780 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224848; AID1224849; AID1259401; AID1259403 |
farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 26.6011 | 0.3758 | 27.4851 | 61.6524 | AID743217 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 28.1838 | 0.0054 | 28.0263 | 1,258.9301 | AID1346985 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 25.6844 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID743069; AID743078; AID743079; AID743091 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 4.8975 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
polyprotein | Zika virus | Potency | 29.6535 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
caspase-3 | Homo sapiens (human) | Potency | 33.4915 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 11.0878 | 0.0007 | 23.0674 | 1,258.9301 | AID743085; AID743122 |
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 0.5308 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
Caspase-7 | Cricetulus griseus (Chinese hamster) | Potency | 33.4915 | 0.0067 | 23.4960 | 68.5896 | AID1346980 |
vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 89.1251 | 0.3548 | 28.0659 | 89.1251 | AID504847 |
potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 35.4813 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
caspase-3 | Cricetulus griseus (Chinese hamster) | Potency | 33.4915 | 0.0067 | 23.4960 | 68.5896 | AID1346980 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 9.3434 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
epidermal growth factor receptor isoform a precursor | Homo sapiens (human) | Potency | 0.3761 | 0.0008 | 0.4819 | 3.5481 | AID1727; AID1729; AID1731 |
tyrosine-protein kinase Yes | Homo sapiens (human) | Potency | 1.5512 | 0.0000 | 5.0182 | 79.2586 | AID686947 |
nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 4.7304 | 0.0006 | 27.2152 | 1,122.0200 | AID743219 |
geminin | Homo sapiens (human) | Potency | 21.5957 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 36.1254 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
lamin isoform A-delta10 | Homo sapiens (human) | Potency | 0.0008 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 19.9526 | 0.3162 | 12.7657 | 31.6228 | AID881 |
Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 33.4915 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 26.6032 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 33.4915 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 19.9526 | 0.0063 | 8.2350 | 39.8107 | AID881 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 12.5893 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
AID1798634 | Fluorescence Binding Assay from Article 10.1073/pnas.0709662105: \\The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP.\\ | 2008 | Proceedings of the National Academy of Sciences of the United States of America, Feb-12, Volume: 105, Issue:6 | The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. |
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. |
AID1798633 | Fluorescence Binding Assay from Article 10.1016/j.ccr.2006.12.017: \\Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity.\\ | 2007 | Cancer cell, Mar, Volume: 11, Issue:3 | Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity. |
AID1802936 | EGFR Tyrosine Kinase Activity Assay from Article 10.3109/14756360903169485: \\Quinazoline-urea, new protein kinase inhibitors in treatment of prostate cancer.\\ | 2010 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 25, Issue:2 | Quinazoline-urea, new protein kinase inhibitors in treatment of prostate cancer. |
AID1801080 | In vitro EGFR TK Inhibition Assays from Article 10.1111/cbdd.12383: \\Synthesis and evaluation of salicylanilide derivatives as potential epidermal growth factor receptor inhibitors.\\ | 2015 | Chemical biology & drug design, Mar, Volume: 85, Issue:3 | Synthesis and evaluation of salicylanilide derivatives as potential epidermal growth factor receptor inhibitors. |
AID1795774 | Kinase Inhibition Assay from Article 10.1016/j.bmcl.2003.10.010: \\Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.\\ | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1 | Synthesis and SAR of potent EGFR/erbB2 dual inhibitors. |
AID1802937 | VEGFR-2 Tyrosine Kinase Activity Assay from Article 10.3109/14756360903169485: \\Quinazoline-urea, new protein kinase inhibitors in treatment of prostate cancer.\\ | 2010 | Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 25, Issue:2 | Quinazoline-urea, new protein kinase inhibitors in treatment of prostate cancer. |
AID625075 | Binding constant for INSRR 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. |
AID624804 | Binding constant for ERBB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624914 | Binding constant for WEE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1441914 | Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
AID624794 | Binding constant for MET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256639 | Average Binding Constant for PHkg1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID1712166 | Growth inhibition of human Non-small cell lung cancer cell line incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
AID748061 | Antitumor activity against gefitinib-resistant human NCI-H1975 cells harboring EGFR L858R/T90M double mutant xenografted in athymic BALB/c nude mouse assessed as tumor growth inhibition at 16 mg/kg, ip qd administered for 14 days measured every other day | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID1443511 | Growth inhibition of human MDA-MB-231 cells | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
AID1305368 | Antitumor activity against human PC9 cells harboring EGFR exon19 deletion activating mutant xenografted in mouse at 6.25 mg/kg/day, po qd for 7 days | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Utilization of Structure-Based Design to Identify Novel, Irreversible Inhibitors of EGFR Harboring the T790M Mutation. |
AID624997 | Binding constant for EGFR(E746-A750del) 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. |
AID435157 | Binding constant for EGFR(G719C) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624829 | Binding constant for CDK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256605 | Average Binding Constant for STK17B; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID1585920 | Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID1712105 | Growth inhibition of human Hs-578T cells incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
AID1378277 | Inhibition of EGFR in human A549 cells assessed as reduction in EGF-induced Akt phosphorylation at S473 residue at 25 uM preincubated for 2 hrs followed by EGF stimulation for 10 mins by Western blot analysis | |||
AID624935 | Binding constant for FLT3(D835H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1762240 | Inhibition of EGFR (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 41 | Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer cell lines. |
AID1870649 | Growth inhibition of human NCI-H3255 cells harbouring EGFR L858R mutant incubated for 72 hrs by CCK8 assay | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. |
AID1442477 | MRT (0 to infinity) in Sprague-Dawley rat plasma at 10 mg/kg, po measured after 24 hrs by UPLC analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of an Orally Selective Inhibitor of Signal Transducer and Activator of Transcription 3 Using Advanced Multiple Ligand Simultaneous Docking. |
AID624780 | Binding constant for CDK4-cyclinD1 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. |
AID1224766 | Delta TM value showing the stabilisation of CK1G3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID489609 | Inhibition of human EGFR autophosphorylation expressed in Sf9 cells DELFIA assay | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Synthesis and antiproliferative activity of indolizine derivatives incorporating a cyclopropylcarbonyl group against Hep-G2 cancer cell line. |
AID1353466 | Inhibition of EGF-induced EGFR activation in human A549 cells assessed as reduction in Akt phosphorylation at S473 residue at 5 uM preincubated for 2 hrs followed by EGF stimulation measured after 10 mins by Western blot analysis | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | 6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells. |
AID1712104 | Growth inhibition of human MDA-MB-231/ATCC cells incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
AID451988 | Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1 | Novel lead for potent inhibitors of breast cancer resistance protein (BCRP). |
AID256629 | Average Binding Constant for HCK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID1742796 | Cytotoxicity against human HCV-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Synthesis and in vitro anti-bladder cancer activity evaluation of quinazolinyl-arylurea derivatives. |
AID1224777 | Delta TM value showing the stabilisation of MST4(1) produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1250371 | Fraction unbound in Han Wistar rat brain at 5 uM by equilibrium dialysis method | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20 | Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
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AID1586912 | Cytotoxicity against human A549 cells after 72 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1 | Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors. |
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AID1877685 | Cytotoxicity against human L02 cells by CCK8 assay | 2022 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 57 | Shikonin N-benzyl matrinic acid ester derivatives as novel telomerase inhibitors with potent activity against lung cancer cell lines. |
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AID1810183 | Cytotoxicity against human HCC827 cells assessed as reduction in cell viability at 20 nM after 72 hrs in presence of pro-HGF by crystal violet staining based assay | 2021 | Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24 | Macrocyclic Inhibitors of HGF-Activating Serine Proteases Overcome Resistance to Receptor Tyrosine Kinase Inhibitors and Block Lung Cancer Progression. |
AID1876266 | Binding affinity to GAK (unknown origin) assessed as dissociation constant | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID666831 | Cytotoxicity against human SGC7901 cells after 72 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and biological evaluation of novel 2-(2-arylmethylene)hydrazinyl-4-aminoquinazoline derivatives as potent antitumor agents. |
AID1532910 | Toxicity in human A549 cells xenografted BALB/c nude mouse assessed as effect on body weight at 30 mg/kg, ig administered every 2 days for 19 days | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold. |
AID624926 | Binding constant for RIOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1562603 | Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay | |||
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AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1715114 | Inhibition of EPHA6 (unknown origin) at 1 uM relative to control | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
AID1742795 | Antiproliferative activity against human T-24 cells assessed as reduction in cell viability measured upto 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | Synthesis and in vitro anti-bladder cancer activity evaluation of quinazolinyl-arylurea derivatives. |
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. |
AID1702618 | Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth by MTT assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance. |
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AID748092 | Cytotoxicity against gefitinib-sensitive human HCC827 cells harboring EGFR E746_A740 deletion mutant assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID1425088 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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AID624812 | Binding constant for SBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435807 | Binding constant for MARK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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AID457038 | Inhibition of EGFR autophosphorylation in human NCI-H1975 cells up to 10 uM by Western blot | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion. |
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AID256594 | Average Binding Constant for BMX; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
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AID1855769 | Inhibition of recombinant human EGFR incubated for 40 to 45 mins and measured after 15 mins by Kinase-Glo Max assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | New thiazole-based derivatives as EGFR/HER2 and DHFR inhibitors: Synthesis, molecular modeling simulations and anticancer activity. |
AID435555 | Binding constant for PRKR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624999 | Binding constant for EGFR(G719S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1768070 | Antiproliferative activity against human WI-26 AV4 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Investigation of 3-sulfamoyl coumarins against cancer-related IX and XII isoforms of human carbonic anhydrase as well as cancer cells leads to the discovery of 2-oxo-2H-benzo[h]chromene-3-sulfonamide - A new caspase-activating proapoptotic agent. |
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. |
AID1690748 | Induction of DNA damage in human A549 cells at 0.1 to 10 uM after 2 hrs by comet assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Comparative analysis of the dual EGFR-DNA targeting and growth inhibitory properties of 6-mono-alkylamino- and 6,6-dialkylaminoquinazoline-based type II combi-molecules. |
AID1224805 | Delta TM value showing the stabilisation of VRK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
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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. |
AID1582385 | Inhibition of EGFR L858R in human H3255 cells assessed as reduction in EGFR autophosphorylation at 1 uM treated 8 hrs post serum starvation measured after 16 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders. |
AID624821 | Binding constant for YANK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID269265 | Inhibition of EGFR-mediated polyGAT phosphorylation at 0.001 uM | 2006 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15 | 5-benzylidene-hydantoins as new EGFR inhibitors with antiproliferative activity. |
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. |
AID1712171 | Growth inhibition of human Panel renal (Carcinoma cell lines) incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
AID1586913 | Thermodynamic solubility of the compound in pH 7.4 phosphate buffered saline measured after 24 hrs by UV-HPLC analysis | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1 | Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors. |
AID435310 | Binding constant for FLT3(ITD) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative 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. |
AID1760621 | Antitumor activity against human NCI-H1975 cells xenografted in BALB/c nude mouse assessed as reduction in tumor growth at 60 mg/kg, ig administered once daily for 3 weeks | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer. |
AID69565 | Inhibition of EGF-stimulated epidermal growth factor receptor phosphorylation at 0.1 ug/mL | 2004 | Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9 | Synthesis and biological evaluation of benzamides and benzamidines: structural requirement of a pyrimidine ring for inhibition of EGFR tyrosine kinase. |
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. |
AID1617468 | Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki | 2019 | Journal of natural products, 11-22, Volume: 82, Issue:11 | Discovery of an Oleanolic Acid/Hederagenin-Nitric Oxide Donor Hybrid as an EGFR Tyrosine Kinase Inhibitor for Non-Small-Cell Lung Cancer. |
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. |
AID435660 | Binding constant for full-length MELK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1532892 | Inhibition of wild type human N-terminal His-tagged HER2 cytoplasmic domain (676 to 1255 residues) expressed in baculovirus expression system after 1 hr in presence of ULight-labeled peptide substrate and ATP by LANCE ultra kinase assay | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold. |
AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID1403041 | Induction of apoptosis in human A549 cells assessed as late apoptotic cells after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.11%) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of anilino-furo[2,3-d]pyrimidine derivatives as dual inhibitors of EGFR/HER2 tyrosine kinase and their anticancer activity. |
AID1768129 | Antifibrotic activity in C57BL mouse model of BLM-induced lung fibrosis assessed as HYP level at 60 mg/kg (Rvb = 5.31 +/- 0.79 ug/mg) | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Synthesis and biological evaluation of selenogefitinib for reducing bleomycin-induced pulmonary fibrosis. |
AID1443499 | Inhibition of NF-kappaB in human MDA-MB-231 cells assessed as decrease in CBP/p300 level in NF-kappaB transcriptional complex in cell nuclear extracts at 2.5 to 15 uM incubated for 12 hrs by ELISA | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
AID435661 | Binding constant for full-length MKNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1676529 | Inhibition of HER2-G776delinsVC mutant (unknown origin) expressed in human H1781 cells assessed as reduction in HER2 induced cell viability after 96 hrs by CellTiter-Glo assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
AID1637535 | Antiproliferative activity against human MCF7 cells after 48 hrs in presence of 10% FBS by MTT method | 2016 | Bioorganic & medicinal chemistry, 10-01, Volume: 24, Issue:19 | Discovery of N-(benzyloxy)-1,3-diphenyl-1H-pyrazole-4-carboxamide derivatives as potential antiproliferative agents by inhibiting MEK. |
AID1224774 | Delta TM value showing the stabilisation of p38beta produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1443520 | Solubility in water | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
AID1499601 | Inhibition of recombinant human His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells at 0.001 uM using Tyr66-biotinylated PTP1B peptide as substrate preincubated for 5 mins followed by substrate addition measured after 1 hr by ELISA relative to c | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Development of a series of novel 4-anlinoquinazoline derivatives possessing quinazoline skeleton: Design, synthesis, EGFR kinase inhibitory efficacy, and evaluation of anticancer activities in vitro. |
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AID625010 | Binding constant for FER kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1473928 | AUC in human at 250 to 500 mg, po QD after 24 hrs | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID1712093 | Growth inhibition of human UACC-62 cells incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
AID489615 | Antiproliferative activity against human A375 cells after 48 hrs by MTT assay | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Synthesis and preliminary biological evaluation of novel taspine derivatives as anticancer agents. |
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. |
AID410944 | Inhibition of ERBb2 by HTRF assay | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1 | Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors. |
AID589577 | Inhibition of human EGFR-mediated poly(Glu4Tyr) phosphorylation after 1 hr | 2011 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7 | Impact of aryloxy-linked quinazolines: a novel series of selective VEGFR-2 receptor tyrosine kinase inhibitors. |
AID488728 | Induction of apoptosis in human MIAPaCa2 cells at 5 to 10 uM after 48 hrs by propidium iodide staining-based FACS analysis | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Design and synthesis of novel Gefitinib analogues with improved anti-tumor activity. |
AID1224798 | Delta TM value showing the stabilisation of DRAK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
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. |
AID1896793 | Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID256611 | Average Binding Constant for RIPK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624855 | Binding constant for FRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID271143 | Inhibition of tumor volume in human LoVo cell xenografted in nude mouse at 50 mg/kg, po | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18 | Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics. |
AID1896772 | Inhibition of wild type EGFR (unknown origin) preincubated with compound 30 mins followed ATP addition incubated for 30 mins by HTRF KinEASE TK assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1702617 | Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance. |
AID295769 | Inhibition of human VEGFR2 in presence of 1 uM ATP | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2. |
AID1443456 | Inhibition of TNFalpha-stimulated NF-kappaB (unknown origin) expressed in human U937 cells incubated for 3 hrs followed by TNFalpha stimulation measured after 2.5 hrs by luciferase reporter gene assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
AID625050 | Binding constant for PKN2 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. |
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. |
AID436047 | Binding constant for full-length PRKX | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1460601 | Growth inhibition of Staphylococcus aureus SAK2378 up to 100 ug/ml by broth microdilution assay | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors. |
AID1574931 | Inhibition of human C-terminal His6-tagged ERBB2 (676 to end residues) expressed in baculovirus infected sf21 cells using poly(Glu, Tyr) 4:1 as substrate | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
AID435284 | Binding constant for DCAMKL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1168675 | Cytotoxicity against human BFTC905 cells assessed as reduction in cell viability at 20 to 80 uM after 24 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22 | Optimization of gefitinib analogues with potent anticancer activity. |
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AID436033 | Binding constant for PIK3CA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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AID435937 | Binding constant for TESK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1391277 | Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors. |
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AID435532 | Binding constant for MST3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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AID1312556 | Inhibition of ErbB2 (unknown origin) | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design, synthesis, anti-tumor activity, and molecular modeling of quinazoline and pyrido[2,3-d]pyrimidine derivatives targeting epidermal growth factor receptor. |
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AID1689696 | Inhibition of NFkappaB p65 in human RPMI-8226 cells incubated for 2 hrs by ELISA | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | 1,2,3-Triazole-Chalcone hybrids: Synthesis, in vitro cytotoxic activity and mechanistic investigation of apoptosis induction in multiple myeloma RPMI-8226. |
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AID1756975 | Induction of apoptosis in human NCI-H1975 cells assessed as late apoptotic cells at 2 uM incubated for 24 hrs by annexin V-FITC and propidium iodide based flow cytometry analysis (Rvb = 4.98 %) | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. |
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AID1464635 | Cytotoxicity against human A549 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 27, Issue:20 | Synthesis and evaluation of the NSCLC anti-cancer activity and physical properties of 4-aryl-N-phenylpyrimidin-2-amines. |
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AID624744 | Binding constant for ZAP70 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID1817355 | Protac activity at VHL/EGFR in human NCI-H1299 cells assessed as induction of EGFR degradation at up to 15 uM incubated for 36 hrs by Western blot analysis | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP. |
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AID1904133 | Reversal of BCRP-mediated multidrug resistance in dog MDCK-II-BCRP cells assessed as fold reduction in mitoxantrone IC50 at 5 uM measured after 48 hrs by MTT assay relative to mitoxantrone IC50 alone | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel. |
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AID1896773 | Inhibition of EGFR (unknown origin) Del19 mutant preincubated with compound 30 mins followed ATP addition incubated for 30 mins by HTRF KinEASE TK assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
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AID1460603 | Growth inhibition of Staphylococcus aureus SA1199B up to 100 ug/ml by broth microdilution assay | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors. |
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AID1499598 | Inhibition of recombinant human His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells at 0.000001 uM using Tyr66-biotinylated PTP1B peptide as substrate preincubated for 5 mins followed by substrate addition measured after 1 hr by ELISA relative t | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Development of a series of novel 4-anlinoquinazoline derivatives possessing quinazoline skeleton: Design, synthesis, EGFR kinase inhibitory efficacy, and evaluation of anticancer activities in vitro. |
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AID435395 | Binding constant for CDC2L1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256592 | Average Binding Constant for LIMK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435800 | Binding constant for FYN kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1896803 | Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
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AID624759 | Binding constant for PFCDPK1(P.falciparum) 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. |
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AID1443470 | Growth inhibition of HUVEC after 48 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
AID1545393 | Antiproliferative activity against human MCF7 by MTT assay | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances. |
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AID625074 | Binding constant for IKK-epsilon kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1443451 | Inhibition of IL-1beta-stimulated nuclear translocation of GFP-tagged NF-kappaB-p65 (unknown origin) expressed in CHO cells at 15 uM preincubated with IL-1beta for 30 mins followed by compound addition by fluorescence assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
AID435934 | Binding constant for PLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224761 | Delta TM value showing the stabilisation of CLK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
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AID1609535 | Antitumour activity against human HCT116 cells xenografted in BALB/c nude mouse assessed as reduction in tumour growth at 10 mg/kg, ip administered daily for 18 days started from 2 days after tumor cell inoculation by digital caliper method | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design and synthesis of novel artemisinin derivatives with potent activities against colorectal cancer in vitro and in vivo. |
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AID1712167 | Growth inhibition of human Panel colon (Carcinoma cell lines) incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
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AID589578 | Inhibition of recombinant human VEGFR-2-mediated poly(Glu4Tyr) phosphorylation after 1 hr | 2011 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7 | Impact of aryloxy-linked quinazolines: a novel series of selective VEGFR-2 receptor tyrosine kinase inhibitors. |
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AID624876 | Binding constant for PDPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1315992 | Stability in rat hepatocytes assessed as length of time required to give 50% loss of parent compound at 1 uM by mass spectrometric analysis | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family. |
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AID1589893 | Growth inhibition of human MOLT4 cells incubated for 48 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors. |
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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. |
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AID1724875 | Antiproliferative activity against EGFR/C-RAF knockdown human H-PDAC-M-X3 cells harboring K-RAS G12D/TP53 H179Y mutant xenografted in mouse tumor model assessed as inhibition of cell proliferation by MTT assay in presence of gefitinib | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10 | Complete Regression of Carcinoma via Combined C-RAF and EGFR Targeted Therapy. |
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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. |
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AID1068998 | Cytotoxicity against human NCI-N87 cells expressing HER2 after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 1: erlotinib analogs. |
AID1278392 | Inhibition of wild type recombinant human EGFR assessed as reduction in autophosphorylation of cytoplasmic domain by Z'-Lyte assay | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | Novel 4-anilinoquinazoline derivatives featuring an 1-adamantyl moiety as potent EGFR inhibitors with enhanced activity against NSCLC cell lines. |
AID1873220 | Inhibition of ABCG2 (unknown origin) expressing human PC-6/SN2-5 cells assessed as increase in topotecan accumulation for 15 mins by flow cytometry | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators. |
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. |
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AID1283994 | Antiproliferative activity against human NCI-H358 cells assessed as viable cells after 48 hrs by CCK8 assay | 2016 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6 | Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors. |
AID771345 | Inhibition of wild type human EGFR tyrosine kinase assessed as Ulight-CAGAGAIETDKEYYTVKD phosphorylation after 15 mins by time-resolved fluorometry | 2013 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 23, Issue:19 | Long-lasting inhibition of EGFR autophosphorylation in A549 tumor cells by intracellular accumulation of non-covalent inhibitors. |
AID624923 | Binding constant for MAPKAPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435183 | Binding constant for PLK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1676530 | Inhibition of C-terminal His6-tagged HER2-A775_G776insYVMA mutant (703 to 1029 residues) (unknown origin) expressed in Sf9 insect cells using TK as substrate preincubated for 30 mins followed by substrate addition and measured after 40 mins in presence of | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
AID761600 | Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors. |
AID457035 | Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion. |
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. |
AID1460154 | Cytotoxicity against human MCF7 cells assessed as cell viability at 3 uM after 48 hrs by MTT assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3 | Design, synthesis, and biological evaluation of novel 1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-3-carboxamide analogs in MCF-7 and MDA-MB-468 breast cancer cell lines. |
AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1712082 | Growth inhibition of human NCI-H522 cells incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
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AID1443992 | Total Cmax in human administered as single dose | 2014 | Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3 | Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump. |
AID1378275 | Inhibition of EGF-induced EGFR phosphorylation at Y1086-residue in human A549 cells at 25 uM preincubated for 2 hrs followed by EGF stimulation for 10 mins by Western blot analysis | |||
AID1715112 | Inhibition of ARG (unknown origin) at 1 uM relative to control | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
AID295768 | Ratio of IC50 for EGFR in presence of 1 mM ATP to IC50 for EGFR in presence of 1 uM ATP | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2. |
AID1439616 | Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7 | Synthesis and in vitro biological evaluation of novel quinazoline derivatives. |
AID625043 | Binding constant for PIK3CA(I800L) 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. |
AID748091 | Inhibition of wild type EGFR (unknown origin) after 1.5 hrs by FRET-based Z'Lyte assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
AID371183 | Inhibition of human EGFR | 2008 | European journal of medicinal chemistry, Jul, Volume: 43, Issue:7 | Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors. |
AID625080 | Binding constant for EIF2AK1 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. |
AID1712090 | Growth inhibition of human LOX IMVI cells incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
AID1585969 | Ratio of drug uptake in human A549 cells at 1 uM measured after 1 hr to drug uptake in human A549 cells at 1 uM incubated for 1 hr followed by compound washout and measured after 8 hrs | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Balancing reactivity and antitumor activity: heteroarylthioacetamide derivatives as potent and time-dependent inhibitors of EGFR. |
AID624822 | Binding constant for CDKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID619792 | Cytotoxicity against human DLD1 cells assessed as cell viability at 10 uM after 3 days by colorimetric MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Synthesis and pharmacological evaluations of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as a new class of anti-cancer agents. |
AID456589 | Inhibition of EGF-induced EGFR phosphorylation in human A431 cells pretreated for 1 hrs followed by EGF-stimulation by immunoblot analysis | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2 | Enhancement of EGFR tyrosine kinase inhibition by C-C multiple bonds-containing anilinoquinazolines. |
AID1717443 | Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay | |||
AID1266269 | Inhibition of VEGFR-2 (unknown origin) assessed as ATP level by luminescence analysis | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2 | Combination of 4-anilinoquinazoline, arylurea and tertiary amine moiety to discover novel anticancer agents. |
AID256583 | Average Binding Constant for CAMKK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID1439619 | Inhibition of wild type recombinant EGFR (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7 | Synthesis and in vitro biological evaluation of novel quinazoline derivatives. |
AID1768130 | Antifibrotic activity in C57BL mouse model of BLM-induced lung fibrosis assessed as MDA content at 60 mg/kg measured after 14 days (Rvb = 9.93 +/- 1.41 nmol/ml) | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Synthesis and biological evaluation of selenogefitinib for reducing bleomycin-induced pulmonary fibrosis. |
AID271146 | AUC in nude mouse xenografted with human LoVo cell at 50 mg/kg, po | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18 | Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics. |
AID1460162 | Inhibition of EGFR phosphorylation in gefitinib-resistant human MDA-MB-468 cells at 10 uM after 6 hrs by Western blot method | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3 | Design, synthesis, and biological evaluation of novel 1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-3-carboxamide analogs in MCF-7 and MDA-MB-468 breast cancer cell lines. |
AID1224773 | Delta TM value showing the stabilisation of ASK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1250365 | Inhibition of EGFR exon19 deletion mutant phosphorylation in human PC9 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20 | Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
AID271149 | Cmax in nude mouse xenografted with human LoVo cell at 50 mg/kg, po | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18 | Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics. |
AID1715120 | Inhibition of DDR1 (unknown origin) at 1 uM relative to control | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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. |
AID256636 | Average Binding Constant for JNK3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID1904124 | Inhibition of BCRP (unknown origin) | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel. |
AID761599 | Antiproliferative activity against wild type EGFR/k-Ras dependent human A549 cells after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors. |
AID771342 | Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured at 1 hr by Western blot analysis | 2013 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 23, Issue:19 | Long-lasting inhibition of EGFR autophosphorylation in A549 tumor cells by intracellular accumulation of non-covalent inhibitors. |
AID435808 | Binding constant for full-length MEK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625045 | Binding constant for PIK3CA(Q546K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1264284 | Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant. |
AID310063 | Inhibition of EGFR | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22 | Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors. |
AID435534 | Binding constant for NEK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID1224785 | Delta TM value showing the stabilisation of PDK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID449028 | Inhibition of EGFR-mediated poly(L-glutamic acid L-tyrosine) phosphorylation | 2009 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18 | Design and synthesis of new stabilized combi-triazenes for targeting solid tumors expressing the epidermal growth factor receptor (EGFR) or its closest homologue HER2. |
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. |
AID436009 | Binding constant for full-length CAMK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1600796 | Cytotoxicity against human MCF10A cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19 | New amide linked dimeric 1,2,3-triazoles bearing aryloxy scaffolds as a potent antiproliferative agents and EGFR tyrosine kinase phosphorylation inhibitors. |
AID1378273 | Inhibition of recombinant human C-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA | |||
AID1432782 | Induction of ROS generation in human NCI-H1975 cells harboring EGFR L858R/T790M double mutant at 15 to 60 uM after 4 hrs by DCFH-DA staining based flow cytometry | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6 | Novel conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents. |
AID1896774 | Inhibition of EGFR (unknown origin) L858R mutant preincubated with compound 30 mins followed ATP addition incubated for 30 mins by HTRF KinEASE TK assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID436055 | Binding constant for full-length YANK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID761598 | Antiproliferative activity against human HCC827 cells expressing EGFR E746_A750 deletion mutant after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors. |
AID435690 | Binding constant for RPS6KA1(Kin.Dom.1 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID1222793 | Dissociation constant, pKa of the compound | 2013 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5 | Which metabolites circulate? |
AID1473930 | Ratio of drug concentration at steady state in human at 250 to 500 mg, po QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID449029 | Growth inhibition of mouse NIH/3T3 cells expressing erB2 gene | 2009 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18 | Design and synthesis of new stabilized combi-triazenes for targeting solid tumors expressing the epidermal growth factor receptor (EGFR) or its closest homologue HER2. |
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. |
AID625030 | Binding constant for LOK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1407100 | Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity. |
AID1712172 | Growth inhibition of human Panel prostate (Carcinoma cell lines) incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
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. |
AID625096 | Binding constant for STK36 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. |
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. |
AID624719 | Binding constant for GRK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435149 | Binding constant for AMPK-alpha2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435167 | Binding constant for KIT(V559D) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256600 | Average Binding Constant for EPHA8; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID1432771 | Antiproliferative activity against EGFR over-expressing human A431 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6 | Novel conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents. |
AID624769 | Binding constant for AURKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1399721 | Antitumor activity against human NCI-H460 cells xenografted in nude mouse assessed as inhibition of tumor volume at 100 mg/kg, po qd for 14 consecutive days relative to control | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
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. |
AID271134 | Free drug level in mouse plasma at 50 mg/kg, po at 4 hrs | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18 | Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics. |
AID91107 | Inhibition of human epidermal growth factor receptor-2 autophosphorylation | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20 | Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents. |
AID745324 | Cytotoxicity against human HCT116 cells after 72 hrs by WST-8 assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Design and synthesis of novel 4-benzothiazole amino quinazolines Dasatinib derivatives as potential anti-tumor agents. |
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. |
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. |
AID1168678 | Cytotoxicity against human A549 cells assessed as cell viability at 40 uM after 24 hrs by MTT assay (Rvb = 100%) | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22 | Optimization of gefitinib analogues with potent anticancer activity. |
AID256643 | Average Binding Constant for CAMK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435295 | Binding constant for MAP4K3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1824043 | Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as inhibition in cell viability after 72 hrs by CCK-8 assay | |||
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. |
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. |
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. |
AID1378293 | Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as reduction in EGF-induced STAT3 phosphorylation at 25 uM preincubated for 2 hrs followed by EGF stimulation for 10 mins by Western blot analysis | |||
AID435438 | Binding constant for full-length p38-gamma | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1315991 | Stability in human liver microsomes assessed as length of time required to give 50% loss of parent compound at 5 uM by mass spectrometric analysis | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family. |
AID624964 | Binding constant for DYRK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624965 | Binding constant for LZK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624768 | Binding constant for SRPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256621 | Average Binding Constant for CAMK2A; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624941 | Binding constant for CDKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID1443479 | Inhibition of SIK2 (unknown origin) at 0.5 uM | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
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AID1250383 | AUC (0 to 7 hrs) in Han Wistar rat CSF at 20 mg/kg, po measured after 0.5 to 24 hrs by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20 | Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
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AID1532104 | Growth inhibition of MDCK2 cells harboring GFP-fused human ABCG2 after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Synthesis and biological evaluation of quinazoline derivatives - A SAR study of novel inhibitors of ABCG2. |
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AID1704490 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Antiproliferative effect of mitochondria-targeting allobetulin 1,2,3-triazolium salt derivatives and their mechanism of inducing apoptosis of cancer cells. |
AID1595626 | Antiproliferative activity against human CH22 cells measured after 72 hrs by alamar blue assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma. |
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. |
AID1712079 | Growth inhibition of human NCI-H23 cells incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
AID1756963 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. |
AID1768071 | Antiproliferative activity against human WI-26 AV4 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Investigation of 3-sulfamoyl coumarins against cancer-related IX and XII isoforms of human carbonic anhydrase as well as cancer cells leads to the discovery of 2-oxo-2H-benzo[h]chromene-3-sulfonamide - A new caspase-activating proapoptotic agent. |
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AID1466879 | Growth inhibition of human Hs578T cells at 4 uM after 48 hrs by sulforhodamine assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Discovery of novel substituted benzo-anellated 4-benzylamino pyrrolopyrimidines as dual EGFR and VEGFR2 inhibitors. |
AID1529996 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24 | Dihydropyrazothiazole derivatives as potential MMP-2/MMP-8 inhibitors for cancer therapy. |
AID435559 | Binding constant for SNARK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1443498 | Inhibition of NF-kappaB-p65 binding to NF-kappaB response element oligonucleotide in nuclear extracts of 12 hrs compound pre-treated human MDA-MB-231 cells at 2.5 to 15 uM by ELISA | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
AID435828 | Binding constant for full-length PIP5K2B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625019 | Binding constant for AKT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256587 | Average Binding Constant for ACK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID1128933 | Antiproliferative activity against human SK-MEL-28 cells harboring BRAF V600E mutant after 68 hrs by MTS assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib. |
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AID624871 | Binding constant for PAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID477295 | Octanol-water partition coefficient, log P of the compound | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | QSPR modeling of octanol/water partition coefficient of antineoplastic agents by balance of correlations. |
AID1690729 | Growth inhibition of human NCI-H1975 cells incubated for 5 days by SRB assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Comparative analysis of the dual EGFR-DNA targeting and growth inhibitory properties of 6-mono-alkylamino- and 6,6-dialkylaminoquinazoline-based type II combi-molecules. |
AID624961 | Binding constant for TGFBR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435531 | Binding constant for MKNK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID507080 | Inhibition of recombinant HCK by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
AID624847 | Binding constant for CSNK1E kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435405 | Binding constant for ERK8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative 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. |
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. |
AID745321 | Cytotoxicity against human U937 cells after 72 hrs by WST-8 assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Design and synthesis of novel 4-benzothiazole amino quinazolines Dasatinib derivatives as potential anti-tumor agents. |
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AID295765 | Inhibition of human EGFR in presence of 1 mM ATP | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2. |
AID1632289 | Cytotoxicity against human Calu cells overexpressing HER2 assessed as growth inhibition after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19 | Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 2: Gefitinib analogs. |
AID435171 | Binding constant for NEK9 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative 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. |
AID435293 | Binding constant for JNK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256572 | Average Binding Constant for STK36; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624730 | Binding constant for CAMK2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID1129574 | Antiproliferative activity against human BEAS2B cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
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AID256669 | Average Binding Constant for ABL1(M351T); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID1586918 | Cytotoxicity against human FHS cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1 | Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors. |
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. |
AID625026 | Binding constant for MAP3K1 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. |
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AID1896804 | Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
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AID625099 | Binding constant for TAOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
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AID1768131 | Antifibrotic activity in C57BL mouse model of BLM-induced lung fibrosis assessed as IL-4 level in blood at 60 mg/kg measured after 14 days by flow cytometry (Rvb = 2.72 +/- 0.14 pg/ml) | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Synthesis and biological evaluation of selenogefitinib for reducing bleomycin-induced pulmonary fibrosis. |
AID625038 | Binding constant for PIK3CA(E542K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1264283 | Antiproliferative activity against human A549 cells harboring wild type EGFR/k-Ras mutation after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant. |
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. |
AID1442475 | AUMC (0 to infinity) in Sprague-Dawley rat plasma at 10 mg/kg, po measured after 24 hrs by UPLC analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of an Orally Selective Inhibitor of Signal Transducer and Activator of Transcription 3 Using Advanced Multiple Ligand Simultaneous Docking. |
AID1163075 | Safety index, ratio of IC50 for human MCF10A cells to EC50 for human ER-negative MCF7 cells | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Thioaryl naphthylmethanone oxime ether analogs as novel anticancer agents. |
AID1724870 | Antiproliferative activity against EGFR/C-RAF knockdown human PDAC003T cells harboring K-RAS G12D/TP53 Q136P mutant xenografted in mouse tumor model assessed as inhibition of cell proliferation by MTT assay in presence of gefitinib | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10 | Complete Regression of Carcinoma via Combined C-RAF and EGFR Targeted Therapy. |
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AID256613 | Average Binding Constant for Aurora2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435164 | Binding constant for IGF1R kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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AID256645 | Average Binding Constant for JAK2 (Kin.Dom. 2); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435326 | Binding constant for TYRO3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative 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. |
AID1756966 | Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. |
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AID1240079 | Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | The discovery of oxazolones-grafted spirooxindoles via three-component diversity oriented synthesis and their preliminary biological evaluation. |
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AID1562645 | Inhibition of EGF-induced EGFR phosphorylation at Y1068 in human A549 cells at 10 uM preincubated for 2 hrs followed by EGF treatment and measured after 10 mins by Western blot analysis | |||
AID1470945 | Antiproliferative activity against human HCC827 cells harboring EGFR del E746 to A750 mutant assessed as decrease in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10 | C-2 (E)-4-(Styryl)aniline substituted diphenylpyrimidine derivatives (Sty-DPPYs) as specific kinase inhibitors targeting clinical resistance related EGFR |
AID1473929 | Drug concentration at steady state in human at 250 to 500 mg, po QD after 24 hrs | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
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AID1330926 | Inhibition of HDAC1 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis | 2017 | Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1 | Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy. |
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AID1265456 | Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 10 uM by propidium iodide staining based flow cytometric analysis (Rvb = 12.77 +/- 1.55%) | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Design, synthesis, and biological evaluation of novel quinazolinyl-diaryl urea derivatives as potential anticancer agents. |
AID436045 | Binding constant for PRKD1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1532114 | Non-competitive inhibition of GFP-fused human ABCG2 expressed in MDCK2 cells up to 3160 nM using varying levels of Hoechst 33342 as substrate preincubated for 30 mins followed by Hoechst 33342 addition by Lineweaver-Burk plot analysis | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Synthesis and biological evaluation of quinazoline derivatives - A SAR study of novel inhibitors of ABCG2. |
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. |
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AID1589078 | Anti-tubercular activity against Mycobacterium tuberculosis H37Rv expressing LuxABCDE assessed as relative luminescence by measuring ratio of RLU (test compound)/RLU(no compound) at 5 uM by luminescence based assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines. |
AID1460599 | Inhibition of NorA in Staphylococcus aureus SA1199B harboring GrlA A116E mutant assessed as inhibition of ethidium bromide efflux after 5 mins by fluorometric method | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors. |
AID1589891 | Growth inhibition of human NCI-H460 cells incubated for 48 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors. |
AID1442462 | AUMC (0 to t) in Sprague-Dawley rat plasma at 1 mg/kg, iv measured after 24 hrs by UPLC analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of an Orally Selective Inhibitor of Signal Transducer and Activator of Transcription 3 Using Advanced Multiple Ligand Simultaneous Docking. |
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AID624928 | Binding constant for CDKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID1250381 | AUC (0 to 7 hrs) in Han Wistar rat brain at 20 mg/kg, po measured after 0.5 to 24 hrs by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20 | Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
AID745318 | Inhibition of human recombinant SRC at 10 uM relative to control | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Design and synthesis of novel 4-benzothiazole amino quinazolines Dasatinib derivatives as potential anti-tumor agents. |
AID624962 | Binding constant for ASK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1244850 | Inhibition of epidermal growth factor receptor kinase (unknown origin) using [33P]-ATP after 20 to 30 mins by radiometric assay | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Molecular design and synthesis of certain new quinoline derivatives having potential anticancer activity. |
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AID625084 | Binding constant for HUNK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID1673304 | Binding affinity to T7-tagged GAK (unknown origin) expressed in Escherichia coli BL21 incubated for 1 hr | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14 | Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK). |
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AID1499560 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Development of a series of novel 4-anlinoquinazoline derivatives possessing quinazoline skeleton: Design, synthesis, EGFR kinase inhibitory efficacy, and evaluation of anticancer activities in vitro. |
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AID394729 | Cytotoxicity against human K562 cells after 96 hrs by MTT assay | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | 2,3-Disubstituted 8-arylamino-3H-imidazo[4,5-g]quinazolines: a novel class of antitumor agents. |
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AID1586911 | Inhibition of human EGFR using poly[Glu:Tyr] (4:1) as substrate measured after 20 mins in presence of [gamma33P]ATP by filter-binding assay | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1 | Acrylamide Functional Group Incorporation Improves Drug-like Properties: An Example with EGFR Inhibitors. |
AID1399725 | Toxicity in nude mouse xenografted with human NCI-H460 cells assessed as death at 25 to 100 mg/kg, po qd for 14 consecutive days | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
AID435663 | Binding constant for full-length MST4 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435777 | Binding constant for ABL2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1760623 | Toxicity in BALB/c nude mouse xenografted with human NCI-H1975 cells assessed as body weight loss at 60 mg/kg, ig administered once daily for 3 weeks | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer. |
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AID1321930 | Antiproliferative activity against NHBE cells after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Synthesis and biological evaluation of azole-diphenylpyrimidine derivatives (AzDPPYs) as potent T790M mutant form of epidermal growth factor receptor inhibitors. |
AID624925 | Binding constant for RIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1265432 | Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 10 uM by propidium iodide staining based flow cytometric analysis (Rvb = 63.82 +/- 2.66%) | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Design, synthesis, and biological evaluation of novel quinazolinyl-diaryl urea derivatives as potential anticancer agents. |
AID1600798 | Inhibition of EGFR in human MCF7 cells assessed as reduction in EGFR phosphorylation at 10 uM incubated for 48 hrs by Western blot analysis | 2019 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19 | New amide linked dimeric 1,2,3-triazoles bearing aryloxy scaffolds as a potent antiproliferative agents and EGFR tyrosine kinase phosphorylation inhibitors. |
AID619785 | Cytotoxicity against human A549 cells assessed as cell viability at 1 uM after 3 days by colorimetric MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Synthesis and pharmacological evaluations of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as a new class of anti-cancer agents. |
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AID1637534 | Antiproliferative activity against human HeLa cells after 48 hrs in presence of 10% FBS by MTT method | 2016 | Bioorganic & medicinal chemistry, 10-01, Volume: 24, Issue:19 | Discovery of N-(benzyloxy)-1,3-diphenyl-1H-pyrazole-4-carboxamide derivatives as potential antiproliferative agents by inhibiting MEK. |
AID624854 | Binding constant for FLT4 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. |
AID537735 | Binding affinity to Candida albicans CaMdr1p expressed in yeast AD1-8u | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans. |
AID624817 | Binding constant for MYO3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1309514 | Inhibition of EGFR T790M mutant (unknown origin) preincubated for 5 mins followed by ATP addition for 30 mins by HTRF assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | 6-Oxooxazolidine-quinazolines as noncovalent inhibitors with the potential to target mutant forms of EGFR. |
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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. |
AID624874 | Binding constant for PCTK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1585924 | Selectivity index, ratio of IC50 for human A431 cells harboring wild-type EGFR to IC50 for human NCI-H1975 cells harboring EGFR T790M/L858R double mutant | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID436021 | Binding constant for LATS2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID780347 | Inhibition of EGFR in shed membrane vesicles of human A431 cells using poly-Glu-Tyr as substrate after 30 mins by ELISA | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Discovery of 2-aryl-8-hydroxy (or methoxy)-isoquinolin-1(2H)-ones as novel EGFR inhibitor by scaffold hopping. |
AID624757 | Binding constant for PKMYT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID624726 | Binding constant for HIPK1 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. |
AID624824 | Binding constant for PIP5K1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID256604 | Average Binding Constant for STK10; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
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. |
AID1306587 | Inhibition of EGFR in human PC9 cells assessed as reduction in Akt phosphorylation at 10 uM after 6 hrs by Western blot analysis | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives. |
AID1609531 | Antiproliferative activity against human WM266.4 cells assessed as inhibition of cell viability after 48 hrs by MTS assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design and synthesis of novel artemisinin derivatives with potent activities against colorectal cancer in vitro and in vivo. |
AID1768068 | Antiproliferative activity against human A-431 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Investigation of 3-sulfamoyl coumarins against cancer-related IX and XII isoforms of human carbonic anhydrase as well as cancer cells leads to the discovery of 2-oxo-2H-benzo[h]chromene-3-sulfonamide - A new caspase-activating proapoptotic agent. |
AID644745 | Inhibition of EGFR at 10 uM after 50 mins by HTRF assay | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Synthesis and biological evaluation of quinazoline and quinoline bearing 2,2,6,6-tetramethylpiperidine-N-oxyl as potential epidermal growth factor receptor(EGFR) tyrosine kinase inhibitors and EPR bio-probe agents. |
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AID1667573 | Antiproliferative activity against human Calu3 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9 | Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold. |
AID435677 | Binding constant for LOK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256562 | Average Binding Constant for PAK4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID436011 | Binding constant for full-length CLK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID436007 | Binding constant for AXL kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID662599 | Antiproliferative activity against human A549 cells expressing wild type EGFR coexpressing k-Ras mutant after 72 hrs by MTS assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6 | Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID624733 | Binding constant for SIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625103 | Binding constant for MST4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1589889 | Growth inhibition of human A549 cells incubated for 48 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors. |
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. |
AID624851 | Binding constant for ERBB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1532906 | Cytotoxicity against mouse L929 cells assessed as cell growth inhibition at 1 uM after 72 hrs by MTT assay relative to control | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold. |
AID624922 | Binding constant for CAMK1 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. |
AID625118 | Binding constant for CAMK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1432774 | Antiproliferative activity against human HL7702 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6 | Novel conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents. |
AID624704 | Binding constant for NEK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1712096 | Growth inhibition of human OVCAR-4 cells incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
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AID1224800 | Delta TM value showing the stabilisation of MST4 (2) produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
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AID1617467 | Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k | 2019 | Journal of natural products, 11-22, Volume: 82, Issue:11 | Discovery of an Oleanolic Acid/Hederagenin-Nitric Oxide Donor Hybrid as an EGFR Tyrosine Kinase Inhibitor for Non-Small-Cell Lung Cancer. |
AID1265424 | Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 10 uM after 48 hrs by Annexin-V/Propidium iodide dual staining based flow cytometric analysis (Rvb = 3.53 +/- 0.89%) | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Design, synthesis, and biological evaluation of novel quinazolinyl-diaryl urea derivatives as potential anticancer agents. |
AID435776 | Binding constant for ABL1(Y253F) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256609 | Average Binding Constant for AAK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID625011 | Binding constant for FGR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID271154 | Terminal half life in human | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18 | Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics. |
AID1532907 | Cytotoxicity against mouse L929 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold. |
AID1425015 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435786 | Binding constant for full-length CLK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1057947 | Cytotoxicity against MDCK cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24 | Investigation of quinazolines as inhibitors of breast cancer resistance protein (ABCG2). |
AID624749 | Binding constant for CASK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID1595618 | Binding affinity to wild-type human partial length EGFR (R669 to V1011 residues) expressed in bacterial expression system by Kinomescan method | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma. |
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AID625072 | Binding constant for TBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435904 | Binding constant for full-length CSK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624873 | Binding constant for PAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256635 | Average Binding Constant for CAMK2D; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID1236609 | Antiproliferative activity against human gefitinib-resistant NCI-H1975 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Synthesis and biological evaluation of diarylthiazole derivatives as antimitotic and antivascular agents with potent antitumor activity. |
AID765703 | Cytotoxicity against human A549 cells after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Design and synthesis of novel quinazoline nitrogen mustard derivatives as potential therapeutic agents for cancer. |
AID625113 | Binding constant for MARK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1824044 | Antiproliferative activity against human HCC827 cells expressing EGFR del119 mutant assessed as inhibition in cell viability after 72 hrs by CCK8 assay | |||
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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. |
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AID1904170 | Inhibition of P-gp in human K562/A02 cells assessed as rescue of intracellular Rhodamine 123 accumulation at 5 uM incubated for 5 to 120 mins and measured by flow cytometry analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel. |
AID256640 | Average Binding Constant for PTK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID1894146 | Inhibition of EGFR in human A-431 cells membrane | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application. |
AID410946 | Antiproliferative activity against human BT474 cells overexpressing ERBb2 after 3 days by methylene blue staining | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1 | Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors. |
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AID1768125 | Cytotoxicity against human HBE cells assessed as inhibition of cell growth measured by CCK8 assay | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Synthesis and biological evaluation of selenogefitinib for reducing bleomycin-induced pulmonary fibrosis. |
AID1738680 | Cytotoxicity against human L0-2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR |
AID674792 | Inhibition of SRC at >100 uM | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Novel oxazolo[4,5-g]quinazolin-2(1H)-ones: dual inhibitors of EGFR and Src protein tyrosine kinases. |
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AID1585921 | Selectivity index, ratio of IC50 for wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells to IC50 for human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
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AID1545394 | Antiproliferative activity against human HepG2 cells by MTT assay | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances. |
AID624989 | Binding constant for ABL1(T315I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID1403033 | Antitumor activity against mouse EAC cells implanted in albino mouse assessed as increase in caspase-3 expression in tumor at 10 mg/kg, po once daily for 8 consecutive days by immunohistochemical analysis relative to control | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of anilino-furo[2,3-d]pyrimidine derivatives as dual inhibitors of EGFR/HER2 tyrosine kinase and their anticancer activity. |
AID1589077 | Anti-tubercular activity against Mycobacterium tuberculosis H37Rv expressing LuxABCDE assessed as relative luminescence by measuring ratio of RLU (test compound)/RLU(no compound) at 2.5 uM by luminescence based assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines. |
AID1876267 | Binding affinity to AAK1 (unknown origin) assessed as dissociation constant | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
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AID436053 | Binding constant for full-length STK33 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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AID1442460 | Apparent volume of distribution in Sprague-Dawley rat plasma at 1 mg/kg, iv measured after 24 hrs by UPLC analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of an Orally Selective Inhibitor of Signal Transducer and Activator of Transcription 3 Using Advanced Multiple Ligand Simultaneous Docking. |
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AID435794 | Binding constant for EPHA3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624862 | Binding constant for LYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1525111 | Cytotoxicity against human PLC/PRF/5 cells assessed as reduction in cell viability by MTT assay | 2019 | Journal of natural products, 05-24, Volume: 82, Issue:5 | Strepantibins A-C: Hexokinase II Inhibitors from a Mud Dauber Wasp Associated Streptomyces sp. |
AID708800 | Cytotoxicity against human A431 cells incubated for 72 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations. |
AID1391276 | Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors. |
AID1460602 | Growth inhibition of Staphylococcus aureus SA1199 up to 100 ug/ml by broth microdilution assay | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors. |
AID1632285 | Cytotoxicity against human NCI-N87 cells overexpressing HER2 assessed as growth inhibition after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19 | Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 2: Gefitinib analogs. |
AID625061 | Binding constant for MAP4K5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625068 | Binding constant for NEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID1167183 | Antitumor activity against human A431 cells xenografted in SCID mouse assessed as tumor growth inhibition at 6.25 mg/kg/day, po qd for 7 days relative to control | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. |
AID1762238 | Cytotoxicity against human A549 cells incubated for 2 to 4 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 41 | Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer cell lines. |
AID1442478 | Anticancer activity against human MDA-MB-231 cells xenografted in BALB/c nude mouse assessed as reduction in tumor volume at 40 mg/kg, po qd | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of an Orally Selective Inhibitor of Signal Transducer and Activator of Transcription 3 Using Advanced Multiple Ligand Simultaneous Docking. |
AID1751265 | Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 08-01, Volume: 43 | Design, synthesis and biological evaluation of novel 2,4-disubstituted quinazoline derivatives targeting H1975 cells via EGFR-PI3K signaling pathway. |
AID1595407 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | 2,4-Disubstituted quinazolines targeting breast cancer cells via EGFR-PI3K. |
AID1129575 | Antiproliferative activity against human 16HBE cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID624849 | Binding constant for CSNK2A2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624977 | Binding constant for OSR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID624796 | Binding constant for MET(Y1235D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1068982 | Inhibition of EGFR (unknown origin) after 10 mins | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 1: erlotinib analogs. |
AID624908 | Binding constant for TEC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625104 | Binding constant for MYO3A 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. |
AID625016 | Binding constant for SRC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID624835 | Binding constant for ERN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1616593 | Antitumor activity against human HCC827 cells xenografted in athymic NU-Fox1nu nude mouse assessed as inhibition of tumor growth at 20 mg/kg, po dosed via gavage for 5 days/week for 2 consecutive weeks relative to control | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
AID662597 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTS assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6 | Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant. |
AID1460600 | Growth inhibition of Staphylococcus aureus SA1902 up to 100 ug/ml by broth microdilution assay | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors. |
AID1693246 | Inhibition of EGFR in human A431 cell line assessed as reduction in EGF-induced EGFR autophosphorylation by measuring relative pEGFR at 3 uM measured upto 24 hrs by ELISA method in relative to control | 2021 | Bioorganic & medicinal chemistry, 01-01, Volume: 29 | Development of a novel acetyl glucose-modified gefitinib derivative to enhance the radiosensitizing effect. |
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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. |
AID435659 | Binding constant for full-length MARK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID295770 | Inhibition of human VEGFR2 in presence of 1 uM ATP at <10000 nM | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2. |
AID435409 | Binding constant for full-length JNK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224764 | Delta TM value showing the stabilisation of CK1G1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624802 | Binding constant for PIM3 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. |
AID625057 | Binding constant for TYRO3 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. |
AID1715796 | Inhibition of recombinant human N-terminal GST tagged EGFR (669 to 1210 residues) expressed in insect expression system using peptide as substrate incubated for 2 hrs followed by substrate addition and measured after 30 mins by TR-FRET assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
AID1562644 | Inhibition of EGF-induced EGFR phosphorylation at Tyr-residue in human A549 cells at 10 uM preincubated for 2 hrs followed by EGF treatment and measured after 10 mins by Western blot analysis | |||
AID1129586 | Induction of NO production in human NCI-H1975 cells harboring EGFR L858R/T790M mutant at 100 uM incubated for 150 mins | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID624985 | Binding constant for ABL1(M351T)-phosphorylated 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. |
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. |
AID1321929 | Antiproliferative activity against human A549 cells harboring K-ras mutation after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Synthesis and biological evaluation of azole-diphenylpyrimidine derivatives (AzDPPYs) as potent T790M mutant form of epidermal growth factor receptor inhibitors. |
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. |
AID1904127 | Cytotoxicity against human K562/A02 cells after 48 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel. |
AID484275 | Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in presence of 0.01% Triton X-100 | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10 | Colloid formation by drugs in simulated intestinal fluid. |
AID1224770 | Delta TM value showing the stabilisation of JAK1~B produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1306588 | Inhibition of EGFR Del19/T790M double mutant in human PC9/GR4 cells assessed as reduction in Akt phosphorylation at 10 uM after 6 hrs by Western blot analysis | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives. |
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AID777423 | Inhibition of wild type EGFR in human A431 cells assessed as growth inhibition after 48 hrs by MTT assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10 | Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting EGFR. |
AID1278396 | Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant assessed as reduction in cell viability after 72 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | Novel 4-anilinoquinazoline derivatives featuring an 1-adamantyl moiety as potent EGFR inhibitors with enhanced activity against NSCLC cell lines. |
AID435908 | Binding constant for EPHA2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435204 | Binding constant for WEE1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID1574929 | Inhibition of human N-terminal GST-tagged EGFR kinase domain (696 to end residues) expressed in baculovirus infected sf21 cells using poly(Glu, Tyr) 4:1 as substrate | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
AID624987 | Binding constant for ABL1(Q252H)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1399720 | Antitumor activity against human NCI-H460 cells xenografted in nude mouse assessed as inhibition of tumor volume at 50 mg/kg, po qd for 14 consecutive days relative to control | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
AID624880 | Binding constant for PIK4CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256564 | Average Binding Constant for MAP3K4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID456588 | Inhibition of recombinant EGFR by ELISA | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2 | Enhancement of EGFR tyrosine kinase inhibition by C-C multiple bonds-containing anilinoquinazolines. |
AID625037 | Binding constant for PIK3CA(C420R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID644746 | Inhibition of EGFR after 50 mins by HTRF assay | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Synthesis and biological evaluation of quinazoline and quinoline bearing 2,2,6,6-tetramethylpiperidine-N-oxyl as potential epidermal growth factor receptor(EGFR) tyrosine kinase inhibitors and EPR bio-probe agents. |
AID428425 | Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Synthesis and in vitro antitumor activities of novel 4-anilinoquinazoline derivatives. |
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. |
AID435188 | Binding constant for PAK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1712092 | Growth inhibition of human UACC-257 cells incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
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. |
AID624949 | Binding constant for CSNK1G3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1309511 | Antiproliferative activity against human NCI-H1975 cells expressing L858R/T790M mutant EGFR after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | 6-Oxooxazolidine-quinazolines as noncovalent inhibitors with the potential to target mutant forms of EGFR. |
AID435201 | Binding constant for TRKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID625029 | Binding constant for BRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1068994 | Cytotoxicity against human Calu3 cells expressing HER2 after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 1: erlotinib analogs. |
AID394884 | Cell cycle arrest in human K562 cells assessed as accumulation at G2/M phase at 10 umol/L after 24 hrs by FACS relative to untreated control | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | 2,3-Disubstituted 8-arylamino-3H-imidazo[4,5-g]quinazolines: a novel class of antitumor agents. |
AID1353464 | Inhibition of EGF-induced EGFR phosphorylation at Y1086 residue in human A549 cells at 5 uM preincubated for 2 hrs followed by EGF stimulation measured after 10 mins by Western blot analysis | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | 6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells. |
AID435785 | Binding constant for full-length CDK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256627 | Average Binding Constant for RPS6KA2 (Kin.Dom. 1); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624904 | Binding constant for NEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435413 | Binding constant for MLCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID1880626 | Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR assessed as cell growth inhibition at 1 uM | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12 | Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras. |
AID1129592 | Inhibition of ERK phosphorylation in human H1975 cells harboring EGFR L858R/T790M mutant at 1 uM by Western blotting analysis | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
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AID1128932 | Inhibition of EGFR (unknown origin) after 1 to 1.5 hrs by FRET-based Z'-Lyte assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib. |
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AID624836 | Binding constant for IKK-beta 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. |
AID624774 | Binding constant for QSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625088 | Binding constant for ARK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID1870650 | Growth inhibition of human A549 cells expressing EGFR incubated for 72 hrs by CCK8 assay | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. |
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AID1617466 | Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay | 2019 | Journal of natural products, 11-22, Volume: 82, Issue:11 | Discovery of an Oleanolic Acid/Hederagenin-Nitric Oxide Donor Hybrid as an EGFR Tyrosine Kinase Inhibitor for Non-Small-Cell Lung Cancer. |
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AID1916783 | Cytotoxicity against human NCI-H1299 cells assessed as cell growth inhibition incubated for 48 hrs by SRB assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery. |
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AID1877681 | Antiproliferative activity against human HeLa cells by CCK8 assay | 2022 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 57 | Shikonin N-benzyl matrinic acid ester derivatives as novel telomerase inhibitors with potent activity against lung cancer cell lines. |
AID625035 | Binding constant for PHKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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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. |
AID1240085 | Cytotoxicity against human HuH7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | The discovery of oxazolones-grafted spirooxindoles via three-component diversity oriented synthesis and their preliminary biological evaluation. |
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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. |
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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. |
AID435327 | Binding constant for VEGFR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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AID625089 | Binding constant for AAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID1712106 | Growth inhibition of human MDA-MB-468 cells incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
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AID624886 | Binding constant for ERK4 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. |
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. |
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. |
AID1174872 | Cytotoxicity against human HT-29 cells after 72 hrs under normoxia conditions by SRB assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Design, synthesis and biological evaluation of 6-(nitroimidazole-1H-alkyloxyl)-4-anilinoquinazolines as efficient EGFR inhibitors exerting cytotoxic effects both under normoxia and hypoxia. |
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AID435899 | Binding constant for AKT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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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. |
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AID1896794 | Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
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AID394731 | Cytotoxicity against human MOLT4 cells after 96 hrs by MTT assay | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | 2,3-Disubstituted 8-arylamino-3H-imidazo[4,5-g]quinazolines: a novel class of antitumor agents. |
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AID1649878 | Growth inhibition of human 22Rv1 cells after 5 days by SRB assay | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | Design and Synthesis of a Trifunctional Molecular System "Programmed" to Block Epidermal Growth Factor Receptor Tyrosine Kinase, Induce High Levels of DNA Damage, and Inhibit the DNA Repair Enzyme (Poly(ADP-ribose) Polymerase) in Prostate Cancer Cells. |
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AID1715119 | Inhibition of LOK (unknown origin) at 1 uM relative to control | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
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AID1904172 | Effect on P-gp expression in human K562/A02 cells at 5 uM measured by Western blot analysis | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel. |
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AID1585971 | Inhibition of recombinant human GST-tagged EGFR (668 to 1210 residues) T790M/L858R double mutant expressed in baculovirus expression system preincubated for 5 hrs followed by kinase tracer 199 addition by TR-FRET assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Balancing reactivity and antitumor activity: heteroarylthioacetamide derivatives as potent and time-dependent inhibitors of EGFR. |
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AID1250372 | Ratio of unbound AUC (0 to 24 hrs) in brain to blood of Han Wistar rat at 20 mg/kg, po by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20 | Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
AID1514365 | Cytotoxicity against EGFR over-expressing human MDA-MB-468 cells assessed as cell viability at 10 uM after 48 hrs by MTT assay relative to control | 2019 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1 | Discovery and SAR studies of novel 2-anilinopyrimidine-based selective inhibitors against triple-negative breast cancer cell line MDA-MB-468. |
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AID435158 | Binding constant for EPHA5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1654031 | Antifibrotic activity against bleomycin-induced pulmonary fibrosis C57BL/6J mouse model assessed as reduction in lung coefficient at 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. |
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AID1330925 | Inhibition of HER2 (unknown origin) assessed as remaining ATP level measured after 15 mins by luminescence analysis | 2017 | Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1 | Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy. |
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AID1224772 | Delta TM value showing the stabilisation of MAP2K6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624737 | Binding constant for EPHA5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1687591 | Antiproliferative activity against human NCI-H1975 cells measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Design, synthesis and biological evaluation of new Axl kinase inhibitors containing 1,3,4-oxadiazole acetamide moiety as novel linker. |
AID1460605 | Synergistic antibacterial activity against Staphylococcus aureus SA1199 in presence of CPX by checkerboard assay | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors. |
AID624887 | Binding constant for ERK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1443469 | Growth inhibition of CHOK1 cells after 48 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
AID625027 | Binding constant for MAP3K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1129591 | Inhibition of Akt phosphorylation in human H1975 cells harboring EGFR L858R/T790M mutant at 1 uM by Western blotting analysis | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. |
AID1652807 | Antitumor activity against mouse LLC cells allografted in C57BL/6J mouse assessed as inhibition of tumor growth at 5 mg/kg, ip dosed every 3 days for 17 days starting from 2 days after inoculation relative to control | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13 | Evaluation of Manassantin A Tetrahydrofuran Core Region Analogues and Cooperative Therapeutic Effects with EGFR Inhibition. |
AID435203 | Binding constant for TTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256560 | Average Binding Constant for FGR; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID488716 | Inhibition of HER2 at 10 uM | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Design and synthesis of novel Gefitinib analogues with improved anti-tumor activity. |
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AID1439618 | Cytotoxicity against human A431 cells assessed as decrease in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7 | Synthesis and in vitro biological evaluation of novel quinazoline derivatives. |
AID457044 | Cytotoxicity against human SW620 cells after 72 hrs by MTT assay | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion. |
AID625107 | Binding constant for DMPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID1877687 | Antiproliferative activity against human H460 cells by CCK8 assay | 2022 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 57 | Shikonin N-benzyl matrinic acid ester derivatives as novel telomerase inhibitors with potent activity against lung cancer cell lines. |
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. |
AID1712103 | Growth inhibition of human MCF7 cells incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
AID295773 | Ratio of IC50 for VEGFR2 in presence of 1 mM ATP to IC50 for VEGFR2 in presence of 1 uM ATP | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2. |
AID435439 | Binding constant for PAK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID599781 | Antiproliferative activity against human MDA-MB-468 cells after 120 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. |
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. |
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. |
AID451987 | Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1 | Novel lead for potent inhibitors of breast cancer resistance protein (BCRP). |
AID1916784 | Inhibition of EGFR (unknown origin) incubated for 1 hr in presence of ATP by Kinase-Glo Plus luminescence kinase assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery. |
AID435556 | Binding constant for RAF1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1163076 | Safety index, ratio of IC50 for human MCF10A cells to EC50 for human ER-positive MDA-MB-231 cells | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Thioaryl naphthylmethanone oxime ether analogs as novel anticancer agents. |
AID1198995 | Antiproliferative activity against mouse B16F10 cells after 24 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9 | Design, synthesis, biological evaluation and molecular modeling of dihydropyrazole sulfonamide derivatives as potential COX-1/COX-2 inhibitors. |
AID1265418 | Induction of apoptosis in human A549 cells assessed as viable cells at 10 uM after 48 hrs by Annexin-V-FITC/Propidium iodide staining based flow cytometric analysis (Rvb = 92.46 +/- 4.23%) | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Design, synthesis, and biological evaluation of novel quinazolinyl-diaryl urea derivatives as potential anticancer agents. |
AID1315993 | Stability in human hepatocytes assessed as length of time required to give 50% loss of parent compound at 1 uM by mass spectrometric analysis | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family. |
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AID435654 | Binding constant for full-length ERK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID666830 | Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and biological evaluation of novel 2-(2-arylmethylene)hydrazinyl-4-aminoquinazoline derivatives as potent antitumor agents. |
AID624778 | Binding constant for ACVRL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436004 | Binding constant for ACVR2A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative 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. |
AID1389963 | Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by MTT assay | |||
AID256582 | Average Binding Constant for NEK9; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID625102 | Binding constant for PRKD2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1312564 | Inhibition of cytoplasmic GST-tagged human recombinant EGFR expressed in baculovirus system by z-lyte assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design, synthesis, anti-tumor activity, and molecular modeling of quinazoline and pyrido[2,3-d]pyrimidine derivatives targeting epidermal growth factor receptor. |
AID435936 | Binding constant for full-length SRPK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1264287 | Inhibition of human recombinant EGFR T790M/delE746_A750 double mutant preincubated for 10 mins followed by FAM-labeled peptide/ATP addition measured after 1 hr by mobility shift assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant. |
AID619791 | Cytotoxicity against human MV4-11 cells assessed as cell viability at 10 uM after 3 days by colorimetric MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Synthesis and pharmacological evaluations of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as a new class of anti-cancer agents. |
AID1904122 | Inhibition of EGFR (unknown origin) | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel. |
AID625136 | Binding constant for YSK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID1562622 | Induction of apoptosis in human A549 cells assessed as necrotic cells at 20 uM incubated for 48 hrs by annexin V -FITC and PI staining based flow cytometric analysis (Rvb = 0.27%) | |||
AID256670 | Average Binding Constant for ABL1(T315I); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID1443481 | Inhibition of STK10 (unknown origin) at 0.5 uM | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
AID1585928 | Antiproliferative activity against NHBE cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID624933 | Binding constant for PLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224799 | Delta TM value showing the stabilisation of NDR1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID436043 | Binding constant for PKMYT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224776 | Delta TM value showing the stabilisation of ERK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1877684 | Antiproliferative activity against human A549 cells by CCK8 assay | 2022 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 57 | Shikonin N-benzyl matrinic acid ester derivatives as novel telomerase inhibitors with potent activity against lung cancer cell lines. |
AID1545469 | Inhibition of EGFR (unknown origin) | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry. |
AID1771675 | Inhibition of wild type EGFR (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate incubated for 1 hr by TR-FRET assay | |||
AID1424906 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1250385 | AUC (0 to 7 hrs) in Han Wistar rat blood at 20 mg/kg, po measured after 0.5 to 24 hrs by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20 | Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
AID624974 | Binding constant for PIK3CD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424193 | Inhibition of wild type N-terminal GST tagged human recombinant EGFR (695 to end amino acids) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) Peptide substrate by ADP-Glo assay | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Synthesis and biological evaluation of morpholine-substituted diphenylpyrimidine derivatives (Mor-DPPYs) as potent EGFR T790M inhibitors with improved activity toward the gefitinib-resistant non-small cell lung cancers (NSCLC). |
AID1425099 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424197 | Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Synthesis and biological evaluation of morpholine-substituted diphenylpyrimidine derivatives (Mor-DPPYs) as potent EGFR T790M inhibitors with improved activity toward the gefitinib-resistant non-small cell lung cancers (NSCLC). |
AID1353465 | Inhibition of EGF-induced EGFR phosphorylation at Y992 residue in human A549 cells at 5 uM preincubated for 2 hrs followed by EGF stimulation measured after 10 mins by Western blot analysis | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | 6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells. |
AID435150 | Binding constant for ARK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID435168 | Binding constant for LTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID456904 | Inhibition of EGFR expressed in Sf9 cells assessed as inhibition of receptor autophosphorylation by DELFIA time resolved fluorimetry | 2010 | Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3 | Design, synthesis and biological evaluation of chrysin long-chain derivatives as potential anticancer agents. |
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. |
AID625143 | Binding constant for CAMKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1768132 | Antifibrotic activity in C57BL mouse model of BLM-induced lung fibrosis assessed as IL-6 level in blood at 60 mg/kg measured after 14 days by flow cytometry (Rvb = 2.36 +/- 0.16 pg/ml) | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Synthesis and biological evaluation of selenogefitinib for reducing bleomycin-induced pulmonary fibrosis. |
AID435398 | Binding constant for DAPK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624971 | Binding constant for DAPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435445 | Binding constant for ZAP70 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID624711 | Binding constant for STK35 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID435410 | Binding constant for KIT kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1442465 | MRT (0 to infinity) in Sprague-Dawley rat plasma at 1 mg/kg, iv measured after 24 hrs by UPLC analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of an Orally Selective Inhibitor of Signal Transducer and Activator of Transcription 3 Using Advanced Multiple Ligand Simultaneous Docking. |
AID1875898 | Antiviral activity against vaccinia virus infected in human HepG2 cells assessed as reduction in plaque formation | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID271130 | Clearance in Wistar rat at 2 mg/kg, iv and 10 mg/kg, po | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18 | Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics. |
AID1638772 | Binding affinity to GAK (unknown origin) | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK). |
AID1432776 | Inhibition of recombinant human GST-tagged EGFR L858R mutant cytoplasmic domain (695-end residues) expressed in insect cells by Z'-Lyte assay | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6 | Novel conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents. |
AID435163 | Binding constant for full-length GSK3B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1266264 | Antiproliferative activity against human A431 cells after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2 | Combination of 4-anilinoquinazoline, arylurea and tertiary amine moiety to discover novel anticancer agents. |
AID1432773 | Antiproliferative activity against human HCC827 cells harboring EGFR E746_A750 deletion mutant after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6 | Novel conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents. |
AID1876083 | Antiviral activity against VACV | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID624720 | Binding constant for HIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435781 | Binding constant for full-length BMX | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID394883 | Cell cycle arrest in human K562 cells assessed as accumulation at S phase at 10 umol/L after 24 hrs by FACS relative to untreated control | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | 2,3-Disubstituted 8-arylamino-3H-imidazo[4,5-g]quinazolines: a novel class of antitumor agents. |
AID624760 | Binding constant for PFPK5(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID708803 | Cytotoxicity against human PC9 cells incubated for 72 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations. |
AID1904130 | Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM by measuring adriamycin IC50 after 48 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel. |
AID256631 | Average Binding Constant for FLT4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID745322 | Cytotoxicity against human A549 cells after 72 hrs by WST-8 assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Design and synthesis of novel 4-benzothiazole amino quinazolines Dasatinib derivatives as potential anti-tumor agents. |
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. |
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. |
AID1057953 | Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation treated 30 mins before Hoechst 33342 addition measured up to 120 mins by fluorescence assay | 2013 | Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24 | Investigation of quinazolines as inhibitors of breast cancer resistance protein (ABCG2). |
AID1712099 | Growth inhibition of human RXF 393 cells incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
AID1877686 | Antiproliferative activity against human Calu-3 cells by CCK8 assay | 2022 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 57 | Shikonin N-benzyl matrinic acid ester derivatives as novel telomerase inhibitors with potent activity against lung cancer cell lines. |
AID260903 | Inhibition of ligand stimulated erbB2 autophosphorylation in T24 NIH cells | 2006 | Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4 | Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors. |
AID1762237 | Cytotoxicity against human PCS-800-011 cells | 2021 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 41 | Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer cell lines. |
AID624937 | Binding constant for FLT3(ITD) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID708801 | Cytotoxicity against human Calu3 cells incubated for 72 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations. |
AID1715121 | Inhibition of EGFR (unknown origin) at 1 uM relative to control | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
AID1321928 | Antiproliferative activity against wild type human A431 cells after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Synthesis and biological evaluation of azole-diphenylpyrimidine derivatives (AzDPPYs) as potent T790M mutant form of epidermal growth factor receptor inhibitors. |
AID435802 | Binding constant for KIT(V559D,V654A) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1532893 | Inhibition of human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 residues) T790M mutant expressed in baculovirus expression system after 1 hr in presence of ULight-labeled peptide substrate and ATP by LANCE ultra kinase assay | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold. |
AID1425096 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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AID1443482 | Inhibition of ERBB2 (unknown origin) at 0.5 uM | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
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AID1460609 | Inhibition of NorA in Staphylococcus aureus SA1199B harboring GrlA A116E mutant assessed as potentiation of CPX-induced antibacterial activity by measuring fold reduction in CPX MIC at 6.25 to 12.5 ug/ml by checkerboard assay | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors. |
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. |
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AID435926 | Binding constant for PDGFRB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID771340 | Cellular uptake in human A549 cells incubated for 1 hr followed by compound washout measured at 1 hr by HPLC-MS/MS analysis | 2013 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 23, Issue:19 | Long-lasting inhibition of EGFR autophosphorylation in A549 tumor cells by intracellular accumulation of non-covalent inhibitors. |
AID624801 | Binding constant for MAP3K15 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435678 | Binding constant for MUSK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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AID507423 | Inhibition of recombinant INSR by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
AID435165 | Binding constant for JAK1(Kin.Dom.1/JH2 - pseudokinase) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1582383 | Induction of EGFR L858R degradation in human H3255 cells at 1 uM treated 8 hrs post serum starvation measured after 16 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders. |
AID1585970 | Inhibition of recombinant human wild type GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus expression system after 1 hr by kinase tracer 199 based TR-FRET assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Balancing reactivity and antitumor activity: heteroarylthioacetamide derivatives as potent and time-dependent inhibitors of EGFR. |
AID295771 | Inhibition of human VEGFR2 in presence of 1 mM ATP | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2. |
AID435286 | Binding constant for EPHA7 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224756 | Delta TM value showing the stabilisation of CAMKK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
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. |
AID435823 | Binding constant for full-length PAK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624771 | Binding constant for TLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436020 | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1589076 | Anti-tubercular activity against Mycobacterium tuberculosis H37Rv expressing LuxABCDE assessed as relative luminescence by measuring ratio of RLU (test compound)/RLU(no compound) at 1.25 uM by luminescence based assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines. |
AID435274 | Binding constant for ACVR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1545414 | Antiproliferative activity against human MCF7 after 18 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances. |
AID1265405 | Antiproliferative activity against human HepG2 cells by MTT assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Design, synthesis, and biological evaluation of novel quinazolinyl-diaryl urea derivatives as potential anticancer agents. |
AID435400 | Binding constant for DDR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative 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. |
AID435651 | Binding constant for DCAMKL2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435180 | Binding constant for MAPKAPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624748 | Binding constant for EPHA6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424363 | Binding affinity to human EGFR assessed as residence time | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors. |
AID1443513 | Antitumor activity against human MDA-MB-231 cells xenografted in NMRI nu/nu mouse at 25 mg/kg, sc administered 5 days post tumor cell inoculation treated for 14 days followed by treatment pause for 6 days followed by treatment continuation on every second | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
AID1724874 | Antiproliferative activity against EGFR/C-RAF knockdown human Panc198 cells harboring K-RAS G12D/TP53 D208V mutant xenografted in mouse tumor model assessed as inhibition of cell proliferation by MTT assay in presence of gefitinib | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10 | Complete Regression of Carcinoma via Combined C-RAF and EGFR Targeted Therapy. |
AID1265460 | Induction of apoptosis in human A549 cells assessed as increase in ROS production at 10 uM after 12 hrs by DCF staining based luminescence spectrometric analysis | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Design, synthesis, and biological evaluation of novel quinazolinyl-diaryl urea derivatives as potential anticancer agents. |
AID1265426 | Induction of apoptosis in human A549 cells assessed as necrotic cells at 10 uM after 48 hrs by Annexin-V/Propidium iodide dual staining based flow cytometric analysis (Rvb = 2.57 +/- 0.39%) | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Design, synthesis, and biological evaluation of novel quinazolinyl-diaryl urea derivatives as potential anticancer agents. |
AID256647 | Average Binding Constant for SYK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID436016 | Binding constant for full-length ERK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256571 | Average Binding Constant for BIKE; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID624763 | Binding constant for RIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID1399705 | Toxicity in nude mouse xenografted with human NCI-H460 cells assessed as body weight at 100 mg/kg, po qd for 14 consecutive days (Rvb = 20.6 +/- 1.5 g) | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
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. |
AID1511362 | Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20 | Novel promising 4-anilinoquinazoline-based derivatives as multi-target RTKs inhibitors: Design, molecular docking, synthesis, and antitumor activities in vitro and vivo. |
AID435775 | Binding constant for ABL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1240081 | Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | The discovery of oxazolones-grafted spirooxindoles via three-component diversity oriented synthesis and their preliminary biological evaluation. |
AID436018 | Binding constant for FLT4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435778 | Binding constant for full-length ADCK4 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID624722 | Binding constant for MKK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID745317 | Inhibition of human recombinant ABL at 10 uM relative to control | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Design and synthesis of novel 4-benzothiazole amino quinazolines Dasatinib derivatives as potential anti-tumor agents. |
AID1443480 | Inhibition of MNK1 (unknown origin) at 0.5 uM | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
AID1565417 | Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | 1,2,4-Oxadiazole derivatives targeting EGFR and c-Met degradation in TKI resistant NSCLC. |
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. |
AID1595628 | Antiproliferative activity against human UCH14 cells measured after 72 hrs by alamar blue assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma. |
AID1525109 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay | 2019 | Journal of natural products, 05-24, Volume: 82, Issue:5 | Strepantibins A-C: Hexokinase II Inhibitors from a Mud Dauber Wasp Associated Streptomyces sp. |
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AID1712088 | Growth inhibition of human SNB-75 cells incubated for 48 hrs by sulforhodamine B assay | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Novel 5-substituted-2-anilinoquinolines with 3-(morpholino or 4-methylpiperazin-1-yl)propoxy moiety as broad spectrum antiproliferative agents: Synthesis, cell based assays and kinase screening. |
AID1595617 | Antiproliferative activity against human UCH2 cells measured after 72 hrs by alamar blue assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma. |
AID1562608 | Antiproliferative activity against human SW480 cells incubated for 72 hrs by MTT assay | |||
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. |
AID1649879 | Growth inhibition of human PC3 cells after 5 days by SRB assay | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | Design and Synthesis of a Trifunctional Molecular System "Programmed" to Block Epidermal Growth Factor Receptor Tyrosine Kinase, Induce High Levels of DNA Damage, and Inhibit the DNA Repair Enzyme (Poly(ADP-ribose) Polymerase) in Prostate Cancer Cells. |
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. |
AID1894147 | Antiproliferative activity against EGF-stimulated human KB cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application. |
AID624968 | Binding constant for DRAK1 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. |
AID435312 | Binding constant for MET kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative 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. |
AID1306586 | Inhibition of EGFR Del19/T790M double mutant phosphorylation in human PC9/GR4 cells at 10 uM after 6 hrs by Western blot analysis | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives. |
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AID1402963 | Inhibition of EGFR (unknown origin) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of anilino-furo[2,3-d]pyrimidine derivatives as dual inhibitors of EGFR/HER2 tyrosine kinase and their anticancer activity. |
AID1177586 | Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability | 2014 | Journal of natural products, Aug-22, Volume: 77, Issue:8 | Brocazines A-F, Cytotoxic Bisthiodiketopiperazine Derivatives from Penicillium brocae MA-231, an Endophytic Fungus Derived from the Marine Mangrove Plant Avicennia marina. |
AID1353454 | Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | 6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells. |
AID1689707 | Induction of ROS accumulation in human RPMI-8226 cells incubated for 2 hrs by ELISA (Rvb = 26.06 +/- 1.45 pg/ml) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | 1,2,3-Triazole-Chalcone hybrids: Synthesis, in vitro cytotoxic activity and mechanistic investigation of apoptosis induction in multiple myeloma RPMI-8226. |
AID1391278 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors. |
AID1690749 | Inhibition of EGFR (unknown origin) using poly (Glu,Tyr) 4:1 as substrate incubated for 8 mins in presence of ATP by colorimetric analysis | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Comparative analysis of the dual EGFR-DNA targeting and growth inhibitory properties of 6-mono-alkylamino- and 6,6-dialkylaminoquinazoline-based type II combi-molecules. |
AID1443485 | Inhibition of ERBB4 (unknown origin) at 0.5 uM | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
AID1756968 | Inhibition of recombinant human N-terminal GST-tagged EGFR T790M mutant (669 to 1210 residues) expressed in baculovirus expression system using peptide as substrate incubated for 2 hrs followed by substrate addition and measured after 30 mins by TR-FRET a | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. |
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. |
AID624709 | Binding constant for MYLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1353459 | Inhibition of recombinant human N-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | 6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells. |
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. |
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AID256614 | Average Binding Constant for YES; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435191 | Binding constant for full-length RIOK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID256597 | Average Binding Constant for CLK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID1389970 | Inhibition of VEGFR2 (unknown origin) using peptide substrate after 60 mins by HTRF assay | |||
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AID1896769 | Inhibition of wild type EGFR (unknown origin) assessed as percent of control activity at 1 uM by radiometric protein kinase-reaction biology assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1224779 | Delta TM value showing the stabilisation of NEK6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID456903 | Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3 | Design, synthesis and biological evaluation of chrysin long-chain derivatives as potential anticancer agents. |
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. |
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. |
AID765701 | Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Design and synthesis of novel quinazoline nitrogen mustard derivatives as potential therapeutic agents for cancer. |
AID624856 | Binding constant for GSK3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID256637 | Average Binding Constant for JNK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3 | A small molecule-kinase interaction map for clinical kinase inhibitors. |
AID435323 | Binding constant for RET(M918T) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID633730 | Cytotoxicity against serum-starved human BT474 cells at 10 uM after 48 hrs by Cell Titer-Glo luminescent assay | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Identification of new aminoacid amides containing the imidazo[2,1-b]benzothiazol-2-ylphenyl moiety as inhibitors of tumorigenesis by oncogenic Met signaling. |
AID435929 | Binding constant for PAK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1439617 | Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7 | Synthesis and in vitro biological evaluation of novel quinazoline derivatives. |
AID1470863 | Inhibition of recombinant human N-terminal GST-tagged EGFR T790M mutant (668 to 1210 residues) expressed in baculovirus expression system preincubated for 5 mins with substrate followed by ATP addition measued after 30 mins by HTRF method | 2017 | Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10 | Design and synthesis of quinazolinones as EGFR inhibitors to overcome EGFR resistance obstacle. |
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. |
AID1585923 | Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID435192 | Binding constant for ROS1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative 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. |
AID1264285 | Cytotoxicity against human HT-29 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant. |
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. |
AID624870 | Binding constant for NEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624789 | Binding constant for KIT(D816V) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID1656984 | Inhibition of EGFR2 (unknown origin) | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | Acetylene Group, Friend or Foe in Medicinal Chemistry. |
AID1432775 | Inhibition of recombinant human GST-tagged EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system by Z'-Lyte assay | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6 | Novel conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents. |
AID1443519 | Inhibition of IL-1beta-stimulated nuclear translocation of GFP-tagged NF-kappaB-p65 (unknown origin) expressed in CHO cells at 15 uM preincubated with IL-1beta for 30 mins followed by compound addition in presence of Pluronic F127 by fluorescence assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
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AID1562641 | Induction of cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 20 uM incubated for 48 hrs by PI staining based flow cytometric analysis (Rvb = 14.36%) | |||
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AID1756973 | Induction of apoptosis in human NCI-H1975 cells assessed as viable cells at 2 uM incubated for 24 hrs by annexin V-FITC and propidium iodide based flow cytometry analysis (Rvb = 93.2 %) | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. |
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AID1609530 | Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 48 hrs by MTS assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design and synthesis of novel artemisinin derivatives with potent activities against colorectal cancer in vitro and in vivo. |
AID1532904 | Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 8 uM after 72 hrs by FITC-annexin V/propidium iodide-double staining based flow cytometry (Rvb = 6.59%) | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold. |
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AID435662 | Binding constant for MST2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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AID435799 | Binding constant for FLT3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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AID1585968 | Drug uptake in human A549 cells at 1 uM incubated for 1 hr followed by compound washout and measured after 8 hrs by LC-MS analysis | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Balancing reactivity and antitumor activity: heteroarylthioacetamide derivatives as potent and time-dependent inhibitors of EGFR. |
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AID624753 | Binding constant for PKNB(M.tuberculosis) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID1562649 | Inhibition of EGF-induced EGFR phosphorylation at Y992 in human A431 cells at 5 uM preincubated for 2 hrs followed by EGF treatment and measured after 10 mins by Western blot analysis | |||
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AID1508627 | Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
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. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
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. |
AID1508628 | Confirmatory 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. |
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. |
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. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
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. |
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. |
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. |
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. |
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. |
AID1508629 | Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID493040 | Navigating the Kinome | 2011 | Nature chemical biology, Apr, Volume: 7, Issue:4 | Navigating the kinome. |
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. |
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. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1345502 | Human epidermal growth factor receptor (Type I RTKs: ErbB (epidermal growth factor) receptor family) | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2. |
AID1345502 | Human epidermal growth factor receptor (Type I RTKs: ErbB (epidermal growth factor) receptor family) | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
[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 | 1905 (37.38) | 29.6817 |
2010's | 2559 (50.22) | 24.3611 |
2020's | 632 (12.40) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (66.95) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 566 (10.82%) | 5.53% |
Reviews | 688 (13.15%) | 6.00% |
Case Studies | 461 (8.81%) | 4.05% |
Observational | 19 (0.36%) | 0.25% |
Other | 3,497 (66.85%) | 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 Randomized, Controlled Phase III Trial to Evaluate the Efficacy of Elortinib vs Gefitinib in Advanced Non-small-cell Lung Cancer With EGFR Exon 19 or 21 Mutations [NCT01024413] | Phase 3 | 256 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
A Phase I, Open-Label, Multicentre Study to Assess the Safety, Tolerability, Pharmacokinetics and Preliminary Anti-tumour Activity of Gefitinib in Combination With MEDI4736 (Anti PD-L1) in Subjects With Non-Small Cell Lung Cancer(NSCLC) [NCT02088112] | Phase 1 | 56 participants (Actual) | Interventional | 2014-03-24 | Completed | ||
A Randomized, Phase III Trial of Prophylactic Cranial Irradiation (PCI) in Patients With Advanced Non-small Cell Lung Cancer (NSCLC) Who Are Effective on Erlotinib or Gefitinib(RT1001) [NCT01158170] | Phase 3 | 200 participants (Anticipated) | Interventional | 2010-06-30 | Recruiting | ||
Paclitaxel/Carboplatin (PC) Followed by Gefitinib or Paclitaxel/Carboplatin (PC) in Advanced Non-small Cell Lung Cancer (NSCLC): Randomized Phase II Study [NCT01196234] | Phase 2 | 84 participants (Actual) | Interventional | 2009-12-31 | Completed | ||
A Randomized, Open-label, Controlled, Multi-Center Phase II/III Study to Assess the Efficacy and Safety of AZD3759 vs. a Standard of Care EGFR TKI, as First Line Treatment to EGFR Mutation Positive Advanced NSCLC With CNS Metastases [NCT03653546] | Phase 2/Phase 3 | 492 participants (Actual) | Interventional | 2018-10-29 | Completed | ||
A Prospective, Single-arm, Multicenter Study of Anlotinib Hydrochloride Combined With First-generation EGFR TKIs as Second-line Treatment in Acquired (Non-T790M Mutation) Resistance Advanced Non-small Cell Lung Cancer [NCT03766490] | 66 participants (Anticipated) | Interventional | 2019-03-30 | Not yet recruiting | |||
A Single-arm, Phase II Study of Preoperative Gefitinib for Stage II-IIIa NSCLC With Activating EGFR Mutation [NCT01833572] | Phase 2 | 36 participants (Actual) | Interventional | 2013-05-31 | Completed | ||
A Randomized, Double-blind, Positive-controlled, Multi-center Phase III Clinical Study of Evaluating Alflutinib Mesylate Versus Gefitinib as First-line Therapy in Patients With Locally Advanced or Metastatic Non-Small-Cell Lung Cancer (NSCLC) With EGFR-se [NCT03787992] | Phase 3 | 358 participants (Actual) | Interventional | 2019-05-30 | Active, not recruiting | ||
A Phase Ib/II Multicenter, Randomized, Open Label Trial to Compare Tepotinib (MSC2156119J) Combined With Gefitinib Versus Chemotherapy as Second-Line Treatment in Subjects With MET Positive, Locally Advanced or Metastatic NSCLC Harboring EGFR Mutation and [NCT01982955] | Phase 1/Phase 2 | 88 participants (Actual) | Interventional | 2013-12-23 | Completed | ||
Oral Navelbine Carboplatin Versus Gefitinib Neoadjuvant Therapy for Resectable EGFR Mutation Positive Stage Ⅱ-ⅢA NSCLC, Prospective, Randomized, Multicenter, Phase Ⅲ Clinical Trial [NCT03203590] | Phase 3 | 590 participants (Anticipated) | Interventional | 2017-09-30 | Not yet recruiting | ||
Randomized to Assess the Efficacy of Whole Brain Radiation Therapy (WBRT) With Concomitant Gefitinib Followed by Maintenance Gefitinib, and Gefitinib Alone, in Lung Cancer Patients With Brain Metastasis [NCT01363557] | 1 participants (Actual) | Interventional | 2012-03-31 | Terminated(stopped due to Decision of Sponsor) | |||
A Phase III, Multi Center, Randomized, Placebo Controlled Study to Evaluate the Efficacy of the Combination Gefitinib With Thalidomide in Patients With Locally Advanced and Metastatic Non-Small-Cell-Lung-Cancer With EGFR Mutation [NCT02387086] | Phase 2/Phase 3 | 380 participants (Anticipated) | Interventional | 2015-05-31 | Not yet recruiting | ||
A Phase III Randomized, Controlled, Double-Blind, Multicenter Clinical Trial to Evaluate the Efficacy and Safety of HS-10296 Versus Gefitinib as First-Line Therapy for Locally Advanced or Metastatic NSCLC With EGFR Sensitizing Mutations [NCT03849768] | Phase 3 | 429 participants (Actual) | Interventional | 2019-02-01 | Active, not recruiting | ||
A Phase II Trial of Gefitinib Monotherapy in Pretreated Patients With Advanced Non-small Cell Lung Cancer Not Harboring Active EGFR Mutations [NCT01312337] | Phase 2 | 92 participants (Anticipated) | Interventional | 2010-09-30 | Recruiting | ||
A Phase I/II Study of MK-3475 (SCH900475) in Combination With Chemotherapy or Immunotherapy in Patients With Locally Advanced or Metastatic Non-Small Cell Lung Carcinoma [NCT02039674] | Phase 1/Phase 2 | 267 participants (Actual) | Interventional | 2014-02-21 | Completed | ||
Combination of Chemotherapy and Gefitinib as First-line Treatment of Patients With Advanced Lung Adenocarcinoma and Sensitive EGFR Mutations: a Randomised Controlled Trial [NCT02148380] | 121 participants (Actual) | Interventional | 2014-05-31 | Completed | |||
Pilot Neoadjuvant Study of ZD1839 (IRESSA®) as Single Agent Preoperative Therapy for Clinical Stage 1A and 1B (T1-2N0), II (T1-2N1, T3N0) and Selected IIIA (T3N1) Non-Small Cell Lung Cancer (NSCLC) With Molecular Correlates [NCT00104728] | 42 participants (Actual) | Interventional | 2004-10-31 | Terminated(stopped due to Early Stopping Rule: Would not meet interim analysis goal to proceed with enrollment) | |||
A Phase I/II Trial of Fixed Doses of Daily Gefitinib With Escalating Doses of Daily RAD001 in Advanced Non-Small Cell Lung Cancer [NCT00096486] | Phase 1/Phase 2 | 74 participants (Actual) | Interventional | 2004-05-31 | Completed | ||
A Phase III, Double-blind, Randomised Study to Assess the Safety and Efficacy of AZD9291 Versus a Standard of Care Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor as First Line Treatment in Patients With Epidermal Growth Factor Receptor Mutatio [NCT02296125] | Phase 3 | 674 participants (Actual) | Interventional | 2014-12-03 | Active, not recruiting | ||
Evaluation of the Efficacy of Domestic Gefitinib Tablets in the Treatment of Locally Advanced or Metastatic Non-small Cell Lung Cancer Patients Using a Multicenter, Randomized, Positive Drug Gefitinib Pharmacodynamics and Pharmacodynamics [NCT03264794] | Phase 4 | 100 participants (Anticipated) | Interventional | 2017-08-31 | Not yet recruiting | ||
ARCHER 1050: A RANDOMIZED, OPEN-LABEL, PHASE 3, EFFICACY AND SAFETY STUDY OF DACOMITINIB (PF-00299804) VERSUS GEFITINIB FOR THE FIRST LINE TREATMENT OF LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER IN SUBJECTS WITH EPIDERMAL GROWTH FACTOR RECE [NCT01774721] | Phase 3 | 452 participants (Actual) | Interventional | 2013-05-09 | Completed | ||
Observational Clinical Trial of Adjuvant Chemotherapy for Non-squamous Cell Carcinoma of Non-small Cell Lung Cancer [NCT03656393] | Phase 3 | 48 participants (Anticipated) | Interventional | 2018-08-31 | Recruiting | ||
The Continuation of Gefitinib Treatment Beyond Progression in Non-small Cell Lung Cancer Patients With EGFR Mutation: A Phase II Single Arm Prospective Study [NCT03399669] | Phase 2 | 100 participants (Anticipated) | Interventional | 2015-02-17 | Active, not recruiting | ||
Dose Climbing Trial of Anlotinib Plus Gefitinib in the First-line Treatment of Advanced Gene Positive Non-squamous Non-small Cell Lung Cancer [NCT03602027] | 9 participants (Anticipated) | Interventional | 2018-08-01 | Not yet recruiting | |||
An Open-label, Multi-centre Study to Evaluate Efficacy and Safety of Gefitinib as the First-line Treatment for Locally Advanced (IIIB), Metastatic (IV) or Recurrent Pulmonary Adenocarcinoma Patients With Epidermal Growth Factor Receptor (EGFR) Mutation. [NCT00344773] | Phase 2 | 46 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
N-of-1 Trial of Actionable Target Identification in Metastatic Cancer for Palliative Systemic Therapy [NCT02142036] | Phase 2 | 50 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
Single-dose, Open-label, Randomized, 2-way Crossover Bioequivalence Study of Gefitinib Tablets Under Fasting Conditions in Chinese Healthy Male Subjects [NCT03050164] | Phase 1 | 38 participants (Actual) | Interventional | 2016-09-08 | Completed | ||
A Biomarker-directed Phase 2 Platform Study in Patients With Advanced Non-Small Lung Cancer Whose Disease Has Progressed on First-Line Osimertinib Therapy. [NCT03944772] | Phase 2 | 250 participants (Anticipated) | Interventional | 2019-06-25 | Active, not recruiting | ||
A Phase II Study of 250-mg ZD1839 Monotherapy in Recurrent or Metastatic or Both Recurrent and Metastatic Squamous Cell Carcinoma [NCT01185158] | Phase 2 | 46 participants (Actual) | Interventional | 2002-05-31 | Completed | ||
Pemetrexed Disodium and Cisplatin Chemotherapy Combined With Synchronous Gefitinib vs Chemotherapy Alone as Adjuvent Therapy in Patient With Stage II-IIIA, Epidermal Growth Factor Receptor Mutant Expressing Lung Adenocarcinoma [NCT02518802] | Phase 3 | 220 participants (Anticipated) | Interventional | 2015-01-31 | Recruiting | ||
A Phase 1/2 Safety And Pharmacokinetic Study Of SU011248 In Combination With Gefitinib (Iressa) In Patients With Metastatic Renal Cell Carcinoma [NCT00113529] | Phase 1/Phase 2 | 42 participants (Actual) | Interventional | 2004-10-31 | Completed | ||
A Randomized Phase II Trial of Combination Anastrozole (NSC #719344) Plus ZD1839 (Iressa, NSC #715055, IND #61187) and of Combination Fulvestrant (NSC #719276) Plus ZD1839 in the Treatment of Postmenopausal Women With Hormone Receptor-Positive Metastatic [NCT00057941] | Phase 2 | 148 participants (Actual) | Interventional | 2003-09-30 | Completed | ||
A Randomized, Open-label, Phase III Study of Single Agent Nazartinib Versus Investigator's Choice (Erlotinib or Gefitinib) as First-Line Treatment in Patients With Locally Advanced or Metastatic Non-Small Cell Lung Cancer Harboring EGFR Activating Mutatio [NCT03529084] | Phase 3 | 0 participants (Actual) | Interventional | 2018-07-24 | Withdrawn(stopped due to Decision by Sponsor not to continue with the trial.) | ||
A Phase Ib Trial of Gefitinib (EGFR Tyrosine Kinase Inhibitor, Iressa™) in Combination With BKM120, an Oral Pan-class I PI3K Inhibitor in Patients With Advanced Non-Small Cell Lung Cancer, With Enrichment for Patients Whose Tumours Harbour Molecular Alter [NCT01570296] | Phase 1 | 38 participants (Actual) | Interventional | 2011-10-03 | Completed | ||
An Open-label Phase II Trial of Gefitinib and Berberine in Patients With Advanced Non-small Cell Lung Cancer and Activating EGFR Mutations [NCT03486496] | Phase 2 | 50 participants (Anticipated) | Interventional | 2018-06-05 | Not yet recruiting | ||
An Multicenter,Phase II Trial of EGFR-TKIs Combine With Anlotinib as First-line Treatment for Patients With Advanced EGFR Mutation-positive NSCLC [NCT03720873] | Phase 2 | 90 participants (Anticipated) | Interventional | 2018-10-31 | Recruiting | ||
Phase 2 Study of Gefitinib Compared With Pemetrexed/Cisplatin in Advanced Non-Small [NCT01192243] | Phase 2 | 68 participants (Anticipated) | Interventional | 2009-12-31 | Recruiting | ||
Exploratory Study of Drug Sensitivity Prediction Software (IRCR-DReSS) With Patient-derived Tumor Cells of Metastatic Gastric Cancer [NCT03170180] | Phase 2 | 66 participants (Actual) | Interventional | 2017-03-01 | Completed | ||
A Open-label, One-arm Trial of Gefitinib Combined With Radiotherapy as Adjuvant Therapy in Completely Resected Patients With Pathological Stage IIIA-N2 Non-small Cell Lung Cancer Harbouring Sensitive Mutations of EGFR [NCT03381430] | 50 participants (Anticipated) | Interventional | 2018-06-30 | Not yet recruiting | |||
β-elemene Combine With EGFR-TKI for Advanced EGFR-TKI-resistant Non-Small Cell Lung Cancer [NCT03123484] | Phase 2 | 80 participants (Anticipated) | Interventional | 2017-04-30 | Not yet recruiting | ||
A Phase II Study of Gefitinib Combined With Radiotherapy in Elderly Patients With Esophageal [NCT01291823] | Phase 2 | 70 participants (Anticipated) | Interventional | 2010-12-31 | Recruiting | ||
A Randomized Controlled, Double-blind, Multicenter, Phase III Clinical Study to Compare Efficacy and Safety of Abivertinib Maleate Versus First-line Standard Therapy EGFR-TKI in Patients With Advanced NSCLC With Sensitive EGFR Mutation [NCT03856697] | Phase 3 | 406 participants (Anticipated) | Interventional | 2019-03-31 | Not yet recruiting | ||
A Randomized Ph 3 Study Comparing First-Line Pemetrexed/Cisplatin Followed by Gefitinib With Gefitinib Alone in East Asian Never Smoker or Light Ex-Smoker Patients With Locally Advanced or Metastatic Nonsquamous NSCLC [NCT01017874] | Phase 3 | 236 participants (Actual) | Interventional | 2009-11-30 | Completed | ||
Phase 1 Pharmacokinetic (PK) and Pharmacodynamic (PD) Study of the Combination of Cetuximab (C-225), a Chimeric Monoclonal Antibody Against the Epidermal Growth Factor Receptor (EGFR), and Gefitinib (ZD1839), a Selective EGFR Tyrosine Kinase Inhibitor, in [NCT00820417] | Phase 1 | 63 participants (Actual) | Interventional | 2004-06-30 | Completed | ||
A Multicenter, Randomized,Double-Blind Study of Gefitinib in Combination With Apatinib or Placebo in Previously Untreated Patients With EGFR Mutation-Positive Advanced Non-squamous Non-Small-Cell Lung Cancer [NCT02824458] | Phase 3 | 246 participants (Anticipated) | Interventional | 2016-06-30 | Recruiting | ||
A Phase III Study of IRESSA in Combination With Intravesical BCG Versus Intravesical BCG Alone in High Risk Superficial Transitional Cell Carcinoma of the Bladder [NCT00352079] | Phase 3 | 41 participants (Actual) | Interventional | 2007-01-04 | Terminated(stopped due to terminated due to poor accrual) | ||
EGFR-TKI With Chemotherapy as First Line Treatment in Stage IIIB/IV NSCLC Patients With Both EGFR Mutation and BIM Deletion Polymorphism [NCT02859077] | Phase 3 | 100 participants (Anticipated) | Interventional | 2016-08-31 | Not yet recruiting | ||
Phase I of Vorinostat-Iressa Combined Therapy on Resistance by BIM Polymorphysim in EGFR Mutant Lung Cancer [NCT02151721] | Phase 1 | 12 participants (Actual) | Interventional | 2014-06-01 | Active, not recruiting | ||
Phase I Study of Cisplatin And ZD1839 (IRESSA®) in Combination With Concomitant Re-Irradiation in Patients With Loco-Regional Recurrent Squamous Cell Cancer of the Head and Neck [NCT00185835] | Phase 1 | 10 participants (Actual) | Interventional | 2002-06-30 | Completed | ||
A Phase 1/2 Study of Osimertinib in Combination With Gefitinib in EGFR Inhibitor naïve Advanced EGFR Mutant Lung Cancer [NCT03122717] | Phase 1/Phase 2 | 48 participants (Actual) | Interventional | 2017-05-09 | Active, not recruiting | ||
Phase II Trial of Adding UFUR to Non-small-cell Lung Cancer Patients Treated With Iressa [NCT01037998] | Phase 2 | 115 participants (Actual) | Interventional | 2005-11-30 | Completed | ||
A Phase 1b/2 Study of AV-299 (Formerly SCH 900105) in Combination With Gefitinib in Asian Subjects With Non-Small Cell Lung Cancer (P06162) [NCT01039948] | Phase 1/Phase 2 | 203 participants (Actual) | Interventional | 2009-12-31 | Completed | ||
"A Phase 2 Trial of Pemetrexed and Cisplatin Followed Sequentially by Gefitinib Versus Pemetrexed and Cisplatin in Asian Never Smoker Patients With Advanced Non-Small Cell Lung Cancer" [NCT00409006] | Phase 2 | 70 participants (Actual) | Interventional | 2007-02-28 | Completed | ||
A Phase II Study of ZD1839 (Iressa), Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor, in Treatment of Recurrent or Metastatic Squamous Cell Carcinoma of the Skin [NCT00054691] | Phase 2 | 40 participants (Actual) | Interventional | 2004-05-31 | Completed | ||
A Phase III Prospective Randomized, Double-Blind, Placebo-Controlled Trial of the Epidermal Growth Factor Receptor Antagonist, ZD1839 (IRESSA) in Completely Resected Primary Stage IB, II and IIIA Non-Small Cell Lung Cancer [NCT00049543] | Phase 3 | 503 participants (Actual) | Interventional | 2002-09-30 | Completed | ||
A Phase II With a Lead in Phase I Study to Examine the Tolerability, Safety Profile and Efficacy of Hydroxychloroquine and Gefitinib in Advanced Non-Small Cell Lung Cancer [NCT00809237] | Phase 1/Phase 2 | 71 participants (Anticipated) | Interventional | 2008-11-30 | Recruiting | ||
Phase I/II Trial of Gefitinib and Radiation in Pediatric Patients Newly Diagnosed With Brain Stem Tumors or Incompletely Resected Supratentorial Malignant Gliomas With Phase II Limited to Brain Stem Tumors [NCT00042991] | Phase 1/Phase 2 | 69 participants (Actual) | Interventional | 2002-07-31 | Completed | ||
A Phase II Study of ZD1839 and Radiation in Patients With Squamous Cell Carcinoma of the Skin [NCT00126555] | Phase 2 | 23 participants (Actual) | Interventional | 2005-03-31 | Completed | ||
Phase II, Open-Label Trial to Assess the Activity of ZD1839 (IRESSA TM) in Patients With Recurrent Prostate Cancer Who Have Rising Serum PSA Levels Despite Serum Testosterone < 50mg/dl [NCT00635856] | Phase 2 | 100 participants (Anticipated) | Interventional | 2001-05-31 | Completed | ||
A Phase II Trial of Hypofractionated Radiotherapy for Limited Metastatic NSCLC Harboring Sensitizing EGFR Mutations After First Line TKI Therapy [NCT02788058] | Phase 2 | 76 participants (Anticipated) | Interventional | 2016-05-31 | Not yet recruiting | ||
Whole Brain Radiotherapy Concurrent With EGFR-TKI Versus EGFR-TKI Alone in the Treatment of Non-small Cell Lung Cancer Patients With Brain Metastasis [NCT02714010] | Phase 3 | 601 participants (Anticipated) | Interventional | 2015-08-31 | Recruiting | ||
A PreSurgical Study to Evaluate Molecular Alterations That Occur in Human Breast Cancer Tissue and Normal Skin After Short Term Exposure to ZD1839 (IRESSA) and to Correlate These Alterations With Pharmacokinetic Parameters. [NCT00637026] | Phase 2 | 65 participants (Anticipated) | Interventional | 2003-07-31 | Completed | ||
A Phase II Trial to Assess the Efficacy of IRESSA™ (Gefitinib) 500 mg/Day in Patients With Breast Cancer Who Have Failed Tamoxifen or Have an Oestrogen Receptor Negative Tumour and Would be Considered for Systemic Therapy [NCT00632723] | Phase 2 | 54 participants (Actual) | Interventional | 2001-04-30 | Completed | ||
A Multicentre, Open-label, Randomised, Controlled Study of Molecularly Precision Target Therapy Based on Tumor Molecular Profiling With GEMOX in Advanced or Recurrent Extrahepatic Cholangiocarcinoma and Gallbladder Carcinoma [NCT02836847] | Phase 2 | 152 participants (Anticipated) | Interventional | 2016-07-31 | Recruiting | ||
A Phase III, Double-blind, Randomised Study of SH-1028 Tablets Versus Gefiitinib as First Line Treatment in Patients With Epidermal Growth Factor Receptor Mutation Positive, Locally Advanced or Metastatic Non Small Cell Lung Cancer [NCT04239833] | Phase 3 | 240 participants (Anticipated) | Interventional | 2020-01-31 | Not yet recruiting | ||
An International Phase 4 Field Study for Analyzing the Psychometric Properties of the Updated Module on Assessing Quality of Life of Patients With Lung Cancer (EORTC QLQ-LC29) [NCT02745691] | 523 participants (Actual) | Observational | 2016-04-01 | Completed | |||
A Phase 2 Study of EGF816 and Gefitinib in TKI-naïve EGFR-mutant Non-Small Cell Lung Cancer [NCT03292133] | Phase 2 | 11 participants (Actual) | Interventional | 2017-10-31 | Active, not recruiting | ||
A Phase II Stdy of ZD 1839 in Recurrent and/or Metastatic Squamous Cell Carcinoma of the Head and Neck [NCT00015964] | Phase 2 | 51 participants (Actual) | Interventional | 2001-03-31 | Completed | ||
Multicentre, Open Label, Extension Study of Treatment With Gefitinib(IRESSA™) for Patients Completing Other Gefitinib Clinical Studies Who May Benefit From Gefitinib Treatment [NCT00683306] | 0 participants | Expanded Access | Approved for marketing | ||||
Phase II Multi-centre Randomized Controlled Study of Gefitinib 500mg Versus 250mg in Patients With NSCLC With Stable Disease After a Month Treatment of Gefitinib 250mg [NCT01017679] | Phase 2 | 96 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
A Phase III, Randomized, Double-blind Study to Assess the Efficacy and Safety of Lazertinib Versus Gefitinib as the First-line Treatment in Patients With Epidermal Growth Factor Receptor Sensitizing Mutation Positive, Locally Advanced or Metastatic Non-Sm [NCT04248829] | Phase 3 | 393 participants (Actual) | Interventional | 2020-02-13 | Active, not recruiting | ||
A Placebo-Controlled, Multicentre, Randomised, Parallel Group, Trial to Assess the Efficacy, Safety and Tolerability of Gefitinib (Iressa® 250mg) as Maintenance Therapy in Locally Advanced or Metastatic (StageIIIB/IV) Non Small Cell Lung Cancer (NSCLC) Ch [NCT00770588] | Phase 4 | 296 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
Evaluation of ZD1839 (NSC #715055) for Advanced Transitional Cell Carcinoma of the Urothelium, Phase II [NCT00014144] | Phase 2 | 31 participants (Actual) | Interventional | 2001-02-28 | Completed | ||
A Phase II Trial of Gefitinib in Squamous NSCLC Patients Who Failed First-Line Chemotherapy [NCT01485809] | Phase 2 | 36 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
Conventional Postoperative Radiotherapy (Standard Fractionation) Plus Iressa or Hyperfractionated Radiotherapy Plus Cisplatin and Iressa for Advanced Head & Neck Cancer: A Phase I Pilot Trial [NCT00681967] | Phase 1 | 30 participants (Actual) | Interventional | 2004-02-29 | Completed | ||
PROGRESS: PRe-Operative Gefitinib in Resectable EGFR Mutation Positive Lung Cancer With Sector Sequencing for Biomarker Discovery [NCT02804776] | Phase 2 | 15 participants (Actual) | Interventional | 2015-01-27 | Completed | ||
An International Expanded Access Clinical Programme With ZD1839 (IRESSA) for Patients With Advanced Non-small Cell Lung Cancer(NSCLC) and Patients With Recurrent or Metastatic or Both Recurrent and Metastatic Squamous Cell Carcinoma of the Head and Neck ( [NCT00684385] | 0 participants | Expanded Access | Approved for marketing | ||||
Can Epidermal Growth Factor Receptor - Tyrosine Kinase Inhibitor Improve the Postoperative Survivorship for Inoperable Non-small Cell Lung Cancer With Spinal Metastasis of the Thoracic and Lumbar Spine?- A Retrospective Comparison With Platinum-based Chem [NCT02740894] | 100 participants (Actual) | Observational | 2016-02-29 | Completed | |||
A Randomized, Open-label Trial of Gefitinib Versus Combination of Vinorelbine Plus Platinum as Adjuvant Treatment in Pathological Stage II-IIIA(N1-N2) Non-small Cell Lung Cancer With EGFR Mutation [NCT01405079] | Phase 3 | 222 participants (Actual) | Interventional | 2011-09-19 | Active, not recruiting | ||
Tyrosine Kinase Inhibitors in DyplAsia of Lung Epithelium [NCT01405846] | Phase 2 | 32 participants (Actual) | Interventional | 2011-12-31 | Terminated(stopped due to Futility) | ||
Phase 2 Randomized, Controlled, Open-label Study of Pemetrexed Versus Gefitinib in Patients With Locally Advanced or Metastatic Non Small Cell Lung Cancer Who Have Previously Received Platinum-Based Chemotherapy Without EGFR Mutations [NCT00891579] | Phase 2 | 161 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
Phase II Study of EGFR Status Based Gefitinib Neoadjuvant Therapy in NSCLC Patients [NCT00986284] | Phase 2 | 102 participants (Actual) | Interventional | 2009-09-30 | Suspended(stopped due to Lack of patients and some progressed disease soon after surgery) | ||
A Randomized Phase II Study Of ZD1839 (IRESSA) In Patients With Hormone Refractory Prostate Cancer [NCT00025116] | Phase 2 | 40 participants (Actual) | Interventional | 2001-04-24 | Completed | ||
An Open-label, Phase II Trial of ZD1839 (IRESSA) in Patients With Malignant Mesothelioma [NCT00787410] | Phase 2 | 23 participants (Actual) | Interventional | 2003-09-30 | Completed | ||
A Phase II Trial of Hypofractionated Radiotherapy Combined With Thymosin for Metastatic NSCLC Patients Who Showed Stable Disease After First Line TKI Therapy [NCT02787447] | Phase 2 | 46 participants (Anticipated) | Interventional | 2016-05-31 | Recruiting | ||
Multi-Centre, Open-Label Extension Trial of Treatment With ZD1839 (Iressa) in Patients Who Have Been Treated in Other ZD1839 Clinical Trials and May Benefit From Continued Monotherapy ZD 1839. [NCT00635973] | Phase 3 | 100 participants (Anticipated) | Interventional | 2000-02-29 | Completed | ||
Multicentric Randomized Phase III Study Comparing Gefitinib Versus Platinum-Based Chemotherapy In EGFR Fish Positive NSCLC Patients (Range) [NCT00807066] | Phase 3 | 1 participants (Actual) | Interventional | 2008-11-30 | Completed | ||
A Phase I Study of Cetuximab in Combination With Gefitinib in Patients With Advanced/Metastatic Non-Small Cell Lung Cancer [NCT00162318] | Phase 1 | 30 participants | Interventional | 2005-03-31 | Completed | ||
A Phase III, Multi-center, Randomized Trial of Pemetrexed and Gefitinib in Never-smoker and Adenocarcinoma Patients With Non-small Cell Lung Cancer Previously Treated With Platinum-based Chemotherapy [NCT01066195] | Phase 3 | 129 participants (Anticipated) | Interventional | 2008-05-31 | Enrolling by invitation | ||
PD-1 Immune Checkpoint Inhibitors and Immune-Related Adverse Events: a Cohort Study [NCT04115410] | 4,724 participants (Anticipated) | Observational | 2020-07-01 | Not yet recruiting | |||
Third-line Treatment of Gefitinib in NSCLC Patients Who Had Received First-line Gefitinib With EGFR 19del/L858R Mutation and Tumor Progression After the Second-line Chemotherapy: a Single-arm, Prospective and Multi-center Study [NCT01933347] | Phase 2 | 46 participants (Actual) | Interventional | 2014-04-07 | Completed | ||
A Randomized, Phase III Trial of Prophylactic Cranial Irradiation (PCI) in Patients With Advanced Non-small Cell Lung Cancer (NSCLC) Who Are Nonprogressive on Gefitinib or Erlotinib [NCT00955695] | Phase 3 | 242 participants (Anticipated) | Interventional | 2009-05-31 | Not yet recruiting | ||
Phase I, Open-label, Safety, Tolerability and Preliminary Efficacy Study of Tremelimumab in Combination With Gefitinib in EGFR Mutant NSCLC Patients [NCT02040064] | Phase 1 | 27 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
A Randomized, Double Blind, Phase III Comparative Trial of 2 Doses of ZD1839 (IRESSA) in Combination With Gemcitabine and Cisplatin Versus Placebo in Combination With Gemcitabine and Cisplatin in Chemotherapy Naive Patients With Advanced (Stage III or IV) [NCT00006048] | Phase 3 | 0 participants | Interventional | 2000-05-31 | Active, not recruiting | ||
A Trial of ZD1839 (Iressa) in Patients With Advanced Renal Cell Carcinoma [NCT00012337] | Phase 2 | 0 participants | Interventional | 2001-01-31 | Completed | ||
Phase II Study Of ZD1839 (NSC 715055) In Newly Diagnosed Patients With Glioblastoma (Grade 4 Astrocytoma) [NCT00014170] | Phase 2 | 92 participants (Actual) | Interventional | 2001-03-31 | Completed | ||
Safety and Efficacy of Anlotinib Hydrochloride Combined With Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors (EGFR TKIs) in Treating Advanced Non-small-cell Lung Cancer (NSCLC) Patients With Acquired Resistance to EGFR TKIs [NCT04007835] | 120 participants (Anticipated) | Interventional | 2019-07-31 | Not yet recruiting | |||
CARISSA Trial - Multicenter Randomized Phase II Trial Comparing Post-operative Radiotherapy and Cisplatin Alone or in Combination With the EGFR Inhibitor ZD 1839 (Iressa) in Upper Aerodigestive Tract Carcinomas [NCT00169221] | Phase 2 | 54 participants (Actual) | Interventional | 2005-09-30 | Terminated(stopped due to Toxicity in an independent study IMEX. The trial was subsequently terminated (54 pts instead of 140) despite safety analyses showing no excess of toxicity) | ||
Clinical Study of Yiqi-yangyin-jiedu Decoction Combined With Gefitinib in Advanced Pulmonary Adenocarcinoma Patients With Activating EGFR Mutation [NCT02929693] | Phase 3 | 198 participants (Anticipated) | Interventional | 2016-10-31 | Enrolling by invitation | ||
A Phase 2 Randomised, Double-Blind, Placebo-Controlled, Multicentre Comparative Study of Gefitinib 250 mg or 500 mg (IRESSA™) Given Either Continuously or Concomitantly With Cisplatin Plus Radiotherapy for the Treatment of Patients With Previously Untreat [NCT00229723] | Phase 2 | 224 participants (Actual) | Interventional | 2004-11-30 | Completed | ||
Paclitaxel/Carboplatin Combined With Intermittent Gefitinib in Patients With Untreated Advanced Non-small Cell Lung Cancer: A Phase Ⅱa Trial [NCT01024712] | Phase 2 | 26 participants (Anticipated) | Interventional | 2009-05-31 | Recruiting | ||
Phase II Study of Skin Toxicity Dosing of IRESSA (Gefitinib) as Monotherapy in Recurrent and/or Metastatic Squamous Cell Carcinoma of the Head and Neck [NCT00519077] | Phase 2 | 44 participants (Actual) | Interventional | 2005-03-31 | Completed | ||
Phase II Study of Taxotere® (Docetaxel) + ZD1839 (IRESSA®) in Previously Untreated Elderly Patients (≥70 Years Old) With Stage III-b (With Malignant Pleural Effusion [MPE+]) or Stage IV Non-Small Cell Lung Cancer (NSCLC) [NCT00231465] | Phase 2 | 44 participants (Actual) | Interventional | 2003-07-31 | Completed | ||
Open Label, Randomised, Parallel Group, Multicentre, Ph III Study To Assess Efficacy, Safety & Tolerability Of Gefitinib (IRESSA™) Versus Carboplatin/Paclitaxel DC As 1st-Line Treatment In Selected Patients With Stage IIIB / IV NSCLC In Asia [NCT00322452] | Phase 3 | 1,329 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
A Phase II Study of ZD 1839 (IRESSA®) in Patients With Advanced Thyroid Cancer [NCT00095836] | Phase 2 | 27 participants (Actual) | Interventional | 2003-03-31 | Completed | ||
Phase II Study in Operable Adenocarcinoma of the Esophagus to Measure Response Rate and Toxicity of Preoperative Combined Modality Paclitaxel (Taxol®, Bristol-Myers Squibb), Cisplatin (Platinol®, Abbott Laboratories), ZD1839 (IRESSA®) and Radiotherapy Fol [NCT00493025] | Phase 2 | 19 participants (Actual) | Interventional | 2005-04-30 | Terminated(stopped due to Closed due to early stopping rule-Low accrual) | ||
A Phase I/II Study of Weekly Topotecan and Gefitinib (Iressa) in Patients With Platinum-Resistant Ovarian, Peritoneal, of Fallopian Tube Cancer [NCT00317772] | Phase 1/Phase 2 | 19 participants (Actual) | Interventional | 2004-09-02 | Completed | ||
A Phase I Study of ZD1839 (Iressa) and Hypofractionated Thoracic Radiotherapy With Stereotactic Body Frame Immobilization for Patients With Advanced Non-Small Cell Lung Cancer [NCT00328562] | Phase 1 | 13 participants (Actual) | Interventional | 2003-12-31 | Completed | ||
A Randomized, Open-Label Phase II Study Of ZD1839 (IRESSA™) Versus Gemcitabine And Carboplatin In Chemotherapy-Naive Patients With Advanced (Stage IIIB OR IV) Non-Small Cell Lung Cancer And ECOG Performance Status 2 [NCT00264498] | Phase 2 | 38 participants (Actual) | Interventional | 2004-10-31 | Completed | ||
A Phase II Trial of ZD1839 (IRESSA®) for Patients With Recurrent or Metastatic Cancer of the Esophagus or Gastroesophageal Junction [NCT00268346] | Phase 2 | 58 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
Ph II Trial of Induction Chemotherapy With Carboplatin and Paclitaxel, Followed by Concurrent Chemotherapy/Radiation Therapy With ZD1839 (IRESSA), 5-FU, Hydroxyurea, and Twice-Daily Radiation, Followed by Adjuvant ZD1839 Monotherapy in Patients With Local [NCT01185171] | Phase 2 | 70 participants (Actual) | Interventional | 2003-01-27 | Completed | ||
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 | ||
Phase II of Gefitinib (IRESSA) Administered as First-line Treatment in Patients With Non-resectable Pneumonic-type Adenocarcinoma (P-ADC) [NCT00198380] | Phase 2 | 90 participants (Actual) | Interventional | 2005-04-30 | Completed | ||
A Phase III Randomised, Stratified, Parallel-Group, Multi-Centre, Comparative Study of ZD1839 (Iressa®) 250 Mg and 500 Mg Versus Methotrexate for Previously Treated Patients With Squamous Cell Carcinoma of the Head and Neck [NCT00206219] | Phase 3 | 477 participants | Interventional | 2003-11-30 | Completed | ||
A Phase II, Open Label Study of Gefitinib (IRESSA) in Treatment-Naïve Subjects With Stage IIIB or IV Non-Small Cell Lung Cancer and Somatic Activating Mutations in the Epidermal Growth Factor Receptor [NCT00411047] | Phase 2 | 34 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
Arimidex/Faslodex/Iressa Study: A Phase II Trial of Primary Systemic Therapy Using a Combination of Arimidex, Faslodex and Iressa (Gefitinib) in Postmenopausal Women With Hormone Receptor Positive Breast Cancer [NCT00206414] | Phase 2 | 15 participants (Actual) | Interventional | 2003-01-31 | Terminated(stopped due to Difficulty accruing subjects the study accrual was closed) | ||
A Randomized, Placebo-Controlled, Double-Blind Phase 2b Study of Raltitrexed (Tomudex) and ZD1839 (Iressa) Versus Raltitrexed Alone as Second Line Chemotherapy in Subjects With Colorectal Carcinoma [NCT00234429] | Phase 2/Phase 3 | 74 participants | Interventional | 2003-11-30 | Completed | ||
A Phase III, Double-Blind, Randomised Study Comparing ZD1839 (IressaTM) Versus Placebo As Maintenance Therapy In Subjects With Locally Advanced Stage III Non-Small Cell Lung Cancer (NSCLC) After Combined Modality Therapy [NCT00234468] | Phase 3 | 490 participants (Anticipated) | Interventional | 2004-01-31 | Terminated(stopped due to Closed due to insufficient recruitment) | ||
Whole Brain Radiotherapy in Combination With Gefitinib (Iressa) or Temozolomide (Temodal) for Brain Metastases From Non-Small Lung Cancer (NSCLC) A Randomized Phase II Trial [NCT00238251] | Phase 2 | 59 participants (Actual) | Interventional | 2005-05-31 | Completed | ||
A Study Of Nasopharyngeal Carcinoma (NPC) Treated With Celecoxib And ZD1839 [NCT00212108] | Phase 1/Phase 2 | 22 participants (Actual) | Interventional | 2003-11-30 | Completed | ||
UpSwinG: Real World Study on TKI Activity in Uncommon Mutations and Sequencing Giotrif® [NCT04179890] | 462 participants (Actual) | Observational | 2019-12-17 | Completed | |||
A Randomized, Open-label Phase II Trial of Erlotinib 100mg Daily Versus Gefitinib 250mg Daily in Patients With Advanced Non-small Cell Lung Cancer Who Harbor EGFR Mutations. [NCT01955421] | Phase 2 | 224 participants (Anticipated) | Interventional | 2013-07-31 | Recruiting | ||
An Open,Multi Center Trial to Evaluate the Efficacy and Safety of High-Dose,Pulsatile Erlotinib/Gefitinib for Advanced Non-Small Cell Lung Cancer Patients After Failure of Standard Dose EGFR-TKIs [NCT01965275] | Phase 2 | 20 participants (Anticipated) | Interventional | 2013-10-31 | Recruiting | ||
A Prospective Clinical Study of Lenvatinib Combined With Gefitinib in the Treatment of Lenvatinib-resistant Hepatocellular Carcinoma [NCT04642547] | 30 participants (Actual) | Interventional | 2020-12-02 | Completed | |||
A Pilot Study of Genomic Sequencing Guided Individualized Therapy in Gastrointestinal Cancers [NCT02013089] | 50 participants (Anticipated) | Interventional | 2013-12-31 | Recruiting | |||
Iressa Re-challenge in Advanced NSCLC EGFR Mutated Patients Who Responded to an EGFR-TKI Used as First-line or Previous Treatment (NVALT 16) [NCT02025218] | Phase 2 | 21 participants (Actual) | Interventional | 2014-01-31 | Terminated | ||
A Phase I Study of Intravenous (IV) Calcitriol in Combination With ZD1839 (IRESSA®) in Refractory Solid Tumors [NCT00084708] | Phase 1 | 53 participants (Actual) | Interventional | 2002-11-30 | Completed | ||
A Phase I/II Pilot Study of Bioimmunotherapy With IRESSA (Gefitinib) and Pegylated Interferon Alpha-2a for Patients With Unresectable/Metastatic Squamous Cell Carcinoma of the Skin [NCT00423397] | Phase 1/Phase 2 | 16 participants (Anticipated) | Interventional | 2006-09-30 | Active, not recruiting | ||
A Randomized, Double-Blind, Phase III Comparative Trial of 2 Doses of ZD1839 (IRESSA) in Combination With Paclitaxel and Carboplatin Versus Placebo in Combination With Paclitaxel and Carboplatin in Chemotherapy-Naive Patients With Advanced (Stage III or I [NCT00006049] | Phase 3 | 0 participants | Interventional | 2000-05-31 | Active, not recruiting | ||
Tyrosine-kinase Inhibitor (TKI) With or Without SBRT in Newly Diagnosed EGFRm Advanced Staged Lung Adenocarcinoma [NCT02893332] | Phase 3 | 200 participants (Anticipated) | Interventional | 2016-01-15 | Terminated(stopped due to After interim analysis, IRB recommend termination.) | ||
Real World Study to Evaluate the Efficacy and Resistant Mechanism of Erlotinib/Gefitinib Combined With Bevacizumab in First Line EGFR Mutation Positive Advanced Non-aquamous Non-small Cell Lung Cancer [NCT03647592] | 30 participants (Anticipated) | Observational | 2018-06-01 | Recruiting | |||
A Phase IV, Multicenter, Non-randomized, Open-labeled Study to Evaluate the Efficacy of Gefitinib (IRESSA®) as a Second-line Therapy in NSCLC Patients [NCT00608868] | Phase 4 | 156 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
A Randomized/Open Label/Parallel Group/Multicenter/Phase IV Study to Assess Safety/Tolerability/Efficacy of Oral Gefitinib 250 mg Versus IV Docetaxel 60 mg/m2 in Patients With Locally Advanced or Metastatic NSCL Cancer of Adenocarcinoma Histology Previous [NCT00536107] | Phase 4 | 14 participants (Actual) | Interventional | 2007-10-31 | Terminated | ||
ZD-1839 (Iressa®) With Concurrent Docetaxel and Conformal Three Dimensional Thoracic Radiation Followed by Consolidative Docetaxel and ZD-1839 for Patients With Stage III Non Small Cell Lung Cancer: A Phase I Study [NCT00310154] | Phase 1 | 45 participants (Anticipated) | Interventional | 2003-11-30 | Completed | ||
A Phase II Trial of Neoadjuvant Gefitinib Therapy Based on Mutation Study in Biopsy- Proven Stage IIIA N2 Non-Squamous Non-Small Cell Lung Cancer [NCT00616499] | Phase 2 | 35 participants (Anticipated) | Interventional | 2006-11-30 | Recruiting | ||
A Phase II Study of Gefitinib in Benefited Patients With Asymptomatic Brain Metastasis Advanced Non-Small Cell Lung Cancer by Chemotherapy [NCT00614809] | Phase 2 | 45 participants (Anticipated) | Interventional | 2007-12-31 | Active, not recruiting | ||
An Open Label, Multicentre, Single Arm Study to Characterise the Efficacy, Safety and Tolerability of Gefitinib 250 mg (IRESSA™) as First Line Treatment in Caucasian Patients, Who Have Epidermal Growth Factor Receptor (EGFR) Mutation Positive Locally Adva [NCT01203917] | Phase 4 | 1,060 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
Comparing Whole Brain Radiation With Hypofractionated Stereotactic RadioSurgery (HFSRS) in Patients With NSCL Brain Metastases [NCT02882984] | Phase 3 | 325 participants (Anticipated) | Interventional | 2015-03-31 | Recruiting | ||
A Phase II Trial of Radiation Therapy Combined With Iressa in Patients With Locally Advanced Non-small Cell Lung Cancer With Harboring Active EGFR Mutations [NCT01391260] | Phase 2 | 30 participants (Anticipated) | Interventional | 2011-07-31 | Recruiting | ||
Multicenter Phase III Study of Gefitinib Mono-therapy or Gefitinib Combined With Chemotherapy in Patients With Brain Metastases From Non-small Cell Lung Cancer Harboring EGFR Mutation [NCT01951469] | Phase 3 | 160 participants (Anticipated) | Interventional | 2016-01-31 | Recruiting | ||
Randomized Phase II Study of Gefitinib Plus Nimotuzumab Versus Gefitinib in Patients With Advanced Non-small Cell Lung Cancer: Dual-agent Molecular Targeting of EGFR (DATE) [NCT01498562] | Phase 2 | 160 participants (Actual) | Interventional | 2011-12-31 | Completed | ||
A Phase I/II Trial of Induction Chemotherapy Plus Gefitinib (Iressa) Followed by Concurrent Chemotherapy, Radiation Therapy, and Gefitinib (Iressa) For Patients With Locally Advanced Squamous Carcinoma of the Head and Neck [NCT00193284] | Phase 2 | 50 participants | Interventional | 2003-10-31 | Completed | ||
A Phase I/II Study of Capecitabine (XELODA®, Roche) Plus Oxaliplatin (Eloxatin®, Sanofi) Plus ZD 1893 (IRESSA®) in the Treatment of Metastatic Colorectal Cancer [NCT00087334] | Phase 1/Phase 2 | 10 participants (Actual) | Interventional | 2004-01-31 | Terminated(stopped due to Withdrawn due to poor/low accrual) | ||
A Randomized Phase III Study of Follow Up With or Without Adjuvant Gefitinib (Iressa™) Following Chemotherapy in Patients With Advanced Non-Small Cell Lung Cancer [NCT00091156] | Phase 3 | 598 participants (Anticipated) | Interventional | 2004-05-31 | Terminated(stopped due to low accrual) | ||
ZD1839 (IRESSA®) With Oxaliplatin and Radiotherapy for Esophageal Carcinoma. A Phase I/II Study With Biologic Correlates [NCT00093652] | Phase 1/Phase 2 | 0 participants | Interventional | 2003-05-31 | Terminated | ||
A Phase II Study of ZD1839 (Iressa)in Chemotherapy Refractory Germ Cell Tumors Expressing Epidermal Growth Factor Receptor (EGFR) [NCT00198159] | Phase 2 | 21 participants | Interventional | 2002-09-30 | Terminated | ||
Randomized Phase 2 Study of 3 Therapeutic Modalities in PS 2/3 Patients With NSCLC Stage IIIB/IV [NCT00198393] | Phase 2 | 126 participants (Actual) | Interventional | 2004-11-30 | Completed | ||
Phase II Trial to Correlate Radiographic Response Induced By Gefitinib With Mutations in the Protein-Tyrosine Kinase Domain of the EGF Receptor Gene in Patients With NSCLC [NCT00588445] | Phase 2 | 65 participants (Actual) | Interventional | 2004-06-30 | Completed | ||
A Randomized,Double-blind,Multicenter Phase III Trial to Evaluate the Safety and Efficacy of Icotinib and Gefitinib in Advanced NSCLC Patients Previously Treated With Chemotherapy [NCT01040780] | Phase 3 | 399 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
Phase II Trial of Chronic Oral ZD1839 (Iressa®) (NSC-715055) in Both Previously-Untreated and Previously-Treated Patients With Selected Stage IIIB and IV Bronchioloalveolar Carcinoma (BAC) [NCT00029003] | Phase 2 | 90 participants (Actual) | Interventional | 2001-12-31 | Completed | ||
A Phase II Study of ZD1839 (Iressa) Plus Anastrozole (Arimidex) in Patients With Relapsed Ovarian Cancer [NCT00181688] | Phase 2 | 35 participants | Interventional | 2003-10-31 | Completed | ||
Bevacizumab Plus EGFR Tyrosine Kinase Inhibitors in Chinese Patients With Stage IIIB-IV EGFR-mutant Non-small Cell Lung Cancer: a Prospective,Multicenter, Non-interventional,Real-world Study [NCT04575415] | 272 participants (Anticipated) | Observational | 2020-10-07 | Recruiting | |||
Multicenter Phase II Trial of Gefitinib (Iressa™) First Line Therapy Followed by Chemotherapy in Advanced Non-Small Cell Lung Cancer (NSCLC) [NCT00217698] | Phase 2 | 63 participants (Actual) | Interventional | 2003-11-30 | Completed | ||
A Phase II Trial of ZD1839 (Iressa) in Patients With Nonresectable Adrenocortical Carcinoma (ACC) [NCT00215202] | Phase 2 | 16 participants (Actual) | Interventional | 2004-08-31 | Completed | ||
A Phase II, Randomized, Placebo Controlled Study to Evaluate the Efficacy of the Combination of Gefitinib and Metformin in Patients With Locally Advanced and Metastatic Non-Small-Cell-Lung-Cancer [NCT01864681] | Phase 2 | 224 participants (Actual) | Interventional | 2013-05-31 | Completed | ||
An Open-label, Randomized, Controlled Study of Gefitinib Plus Autologous Cytokine-Induced Killer Cell Immunotherapy(CIK)Versus Gefitinib Alone As Second Or Third-Line Treatment in Patients With Advanced Adenocarcinoma Non-Small Cell Lung Cancer [NCT01871480] | Phase 2 | 50 participants (Anticipated) | Interventional | 2013-05-31 | Terminated | ||
A Randomized, Double-blind, Positive Controlled Phase III Study to Evaluate the Efficacy and Safety of BPI-7711 Capsule in Locally Advanced or Recurrent/Metastatic Treatment-naïve Non-small Cell Lung Cancer Patients With EGFR Mutation [NCT03866499] | Phase 3 | 369 participants (Actual) | Interventional | 2021-04-30 | Active, not recruiting | ||
First Line Bio-immunotherapy With Thymosin Alpha 1 in Patients With Sensitizing EGFR Mutation Positive Non Small Cell Lung Cancer Who Are Taking Standard of Care Therapy [NCT02906163] | Phase 1/Phase 2 | 188 participants (Anticipated) | Interventional | 2016-10-31 | Not yet recruiting | ||
Phase II Trial of ZD1839 (IRESSA®) and Pegylated Interferon Alfa 2b (PEG-Intron™) in Unresectable or Metastatic Renal Cell Carcinoma [NCT00467077] | Phase 2 | 21 participants (Actual) | Interventional | 2004-09-30 | Terminated(stopped due to Protocol was closed due to slow accrual.) | ||
Randomized Phase II Trail Comparing Gefitinib Plus Simvastatin and Gefitinib Alone in Patients With Previously Treated Advanced Non-Small Cell Lung Cancer (NSCLC) [NCT00452244] | Phase 2 | 110 participants (Actual) | Interventional | 2006-05-31 | Completed | ||
A Randomized Phase III Study of Gefitinib (IRESSATM) Versus Standard Chemotherapy (Gemcitabine Plus Cisplatin) as First-line Treatment for in Never Smokers Advance or Metastatic Adenocarcinoma of Lung [NCT00455936] | Phase 3 | 315 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
Phase I Study of Iressa and CRT/IMRT in Chinese Patients With IIIB/IV NSCLC After Failure of Platinum-Based Chemotherapy [NCT00497250] | Phase 1 | 32 participants (Anticipated) | Interventional | 2007-07-31 | Recruiting | ||
A Randomized, Open Label, Parallel Group, Regional, Multicenter, Phase III Study of Oral Gefitinib (IRESSA®) Versus Intravenous Docetaxel (TAXOTERE®) in Patients With Locally Advanced or Metastatic Recurrent Non Small Cell Lung Cancer Who Have Previously [NCT00478049] | Phase 3 | 163 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
Chemotherapy Plus Gefitinib Versus Gefitinib Alone as First-line Treatment for Patients With Advanced Lung Adenocarcinoma and Sensitive EGFR Mutations: a Randomized Controlled Trial [NCT02951637] | Phase 2 | 300 participants (Anticipated) | Interventional | 2016-12-31 | Not yet recruiting | ||
A Dose Finding Study (Phase I) of the Combination of ZD1839 (Iressa®) and an Oral Formulation of Irinotecan (Camptosar™) in Children With Refractory Solid Tumors [NCT00132158] | Phase 1 | 19 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
Combination of Gefitinib With Chemotherapy or Anti-angiogenesis as 1st Line Treatment in Advanced NSCLC Patients Detected With Bim Deletion or Low EGFR Activating Mutation Abundance [NCT02930954] | Phase 2 | 180 participants (Anticipated) | Interventional | 2016-11-30 | Not yet recruiting | ||
A Randomized, Controlled, Open-label, Prospective Trial of S-1 Plus Gefitinib Versus Gefitinib Monotherapy for First-line Treatment of Advanced Non-squamous Non-small Cell Lung Cancer With EGFR-sensitive Mutation [NCT03457337] | Phase 2 | 200 participants (Anticipated) | Interventional | 2018-03-28 | Recruiting | ||
A Phase IB/II, Open Label, Multicenter Study of INC280 Administered Orally in Combination With Gefitinib in Adult Patients With EGFR Mutated, c-MET-amplified Non-small Cell Lung Cancer Who Have Progressed After EGFR Inhibitor Treatment [NCT01610336] | Phase 2 | 161 participants (Actual) | Interventional | 2012-04-05 | Completed | ||
A Multi-center, Open-label, Fixed-sequence Study of Effect of Gefitinib on the Pharmacokinetics of Apatinib Mesylate in Non-squamous, Non-small-cell Lung Cancer Patients [NCT04390984] | Phase 1 | 22 participants (Anticipated) | Interventional | 2020-05-26 | Recruiting | ||
An Open-Label, Phase II Trial Of 250 mg ZD1839 (IRESSA™) In Prostate Cancer Patients With Early Biochemical Failure Post Prostatectomy [NCT00265070] | Phase 2 | 80 participants (Actual) | Interventional | 2003-01-31 | Completed | ||
An Open-label, Multi-center, Global, Rollover Study for Patients Who Have Previously Been Treated With Capmatinib (INC280) as Monotherapy or in Combination in a Novartis Sponsored Trial. [NCT03040973] | Phase 2 | 40 participants (Anticipated) | Interventional | 2017-07-04 | Recruiting | ||
Phase II Study of Iressa in Relapsed and Refractory Small Cell Lung Cancer [NCT00298688] | Phase 2 | 56 participants | Interventional | 2004-09-30 | Completed | ||
A Randomised, Non-Comparative, Multicentre, Phase II, Parallel-Group Trial Of ZD1839 (Iressa™) In Combination With 5 Fluorouracil, Leucovorin And Cpt-11 (Irinotecan) In Patients With Metastatic Colorectal Cancer [NCT00233623] | Phase 2 | 190 participants | Interventional | 2004-07-31 | Withdrawn | ||
A Phase II Trial to Evaluate the Combination of ZD1839 (Iressa) and Fulvestrant (Faslodex®) in Patients With Advanced or Metastatic Breast Cancer [NCT00234403] | Phase 2 | 60 participants | Interventional | 2004-05-31 | Completed | ||
A Phase II, Multicentre, Non-Comparative, Open-Label Study To Evaluate The Efficacy And Tolerability Of ZD1839 (Iressa™) In Asymptomatic Radio-Naive Patients With Brain Metastases From Non-Small Cell Lung Carcinoma (NSCLC) Who Have Relapsed Following Prio [NCT00234442] | Phase 2 | 47 participants | Interventional | 2004-07-31 | Terminated(stopped due to Closed due to insufficient recruitment.) | ||
Phase II Multicenter, Double-Blind, Randomized Trial Comparing Anastrozole (ZD1033, Arimidex™)-Placebo to the Combination Anastrozole-ZD1839 (Gefitinib, IRESSA™) in Postmenopausal Patients With Estrogen Receptor (ER) and/or Progesterone Receptor (PgR) Met [NCT00077025] | Phase 2 | 174 participants (Anticipated) | Interventional | 2004-01-31 | Completed | ||
A Phase 2 Trial to Evaluate ZD1839 (IRESSA) in Combination With Cisplatin & Radiotherapy in Patients With Advanced Head & Neck Carcinoma (Unresectable &Inoperable) [NCT00242749] | Phase 2 | 47 participants | Interventional | 2002-12-31 | Completed | ||
A Phase I/II, Multicentre Clinical Study Of ZD1839 (Iressa™) In Combination With Capecitabine (Xeloda™) In Subjects With Advanced Colorectal Carcinoma After Failure Of First-Line Chemotherapy [NCT00242788] | Phase 1/Phase 2 | 40 participants | Interventional | 2004-02-29 | Completed | ||
A Phase II, Randomised, Double-Blind, Placebocontrolled Study To Investigate The Effects Of ZD1839 (IRESSA™) On Cell Proliferation In Oestrogen And Progesterone Receptor Negative Breast Cancer Prior To Surgery [NCT00252811] | Phase 2 | 60 participants | Interventional | 2004-02-29 | Withdrawn | ||
Phase II, Placebo Controlled, Parallel Group, Double Blind, Randomised, Multicentre Trial Comparing the Anastrozole (Arimidex®) Placebo Combination to the Anastrozole - ZD1839 (Iressa™) Combination as Neoadjuvant Treatment in Postmenopausal Women With Sta [NCT00255463] | Phase 2 | 185 participants | Interventional | 2004-01-31 | Completed | ||
A Randomised, Open Label, Parallel Group, Multi-Centre, Phase II Study of Progression Free Survival Comparing ZD1839 (IRESSA™) (250 MG Tablet) Versus Vinorelbine (30 MG/M2 Infusion) in Chemonaive, Elderly Patients With Locally Advanced (Stage IIIB) or Met [NCT00256711] | Phase 2 | 192 participants | Interventional | 2004-07-31 | Completed | ||
Phase I/II Study of Induction Gefitinib and Concurrent Radiotherapy in Patients With Previously Untreated, Medically Inoperable Stage I or II Non-Small Cell Lung Cancer [NCT00268255] | Phase 1/Phase 2 | 0 participants (Actual) | Interventional | Withdrawn(stopped due to Study never moved forward with accrual.) | |||
A Randomized, Open-Label, Parallel Group, International, Multicenter, Phase III Study of Oral ZD1839 (IRESSA®) Versus Intravenous Docetaxel (TAXOTERE®) in Patients With Locally Advanced or Metastatic Recurrent Non-Small Cell Lung Cancer Who Have Previousl [NCT00076388] | Phase 3 | 1,440 participants | Interventional | 2004-02-29 | Completed | ||
A Pilot Study of Adjuvant Therapy of Gefitinib (Iressa, ZD1839) in Patients With Resectable Hepatocellular Carcinoma [NCT00282100] | Phase 2 | 40 participants (Anticipated) | Interventional | 2005-12-31 | Active, not recruiting | ||
A Phase I/II Study to Evaluate Safety and Efficacy in Patients Who Have Resectable Esophageal Cancer and Are Treated With Neoadjuvant Cisplatin, Irinotecan (CPT-11) ZD1839 (IRESSA), and Radiotherapy Followed by Surgical Resection [NCT00290719] | Phase 1 | 6 participants (Actual) | Interventional | 2005-11-30 | Terminated(stopped due to low enrollment) | ||
EGFR Pathway Modulation In Patients With Ductal Carcinoma In Situ Of The Breast [NCT00082667] | Phase 2 | 1 participants (Actual) | Interventional | 2002-10-31 | Terminated(stopped due to PI left VICC) | ||
A Pilot Phase I Dose Escalation Study Of The EGFR Tyrosine Kinase Inhibitor Gefitinib (Iressa) Combined With Paclitaxel (Taxol) And External Beam Radiation Therapy In Patients With Advanced Squamous Cell Carcinoma Of The Head And Neck (SCCHN) [NCT00083057] | Phase 1 | 30 participants (Anticipated) | Interventional | 2004-05-31 | Completed | ||
A Phase IIIb Randomized, Double-Blind Study Comparing Maintenance ZD1839 (IRESSA®) or Placebo Following Completion of Front Line, Platinum-Based, Double Chemotherapy in Subjects With Advanced or Metastatic Non-Small Cell Lung Cancer [NCT00090675] | Phase 3 | 0 participants (Actual) | Interventional | 2006-01-31 | Withdrawn(stopped due to No patients randomised) | ||
A Randomised Phase II Study: Treatment With Daily p.o. Iressa™ (ZD1839) or Placebo in Combination With Weekly IV Infusion of Docetaxel in Patients With Metastatic Breast Cancer [NCT00319618] | Phase 2 | 66 participants | Interventional | 2003-06-30 | Completed | ||
A Pilot Feasibility Study to Evaluate the Efficacy of ZD1839 (IRESSA) in Eliminating Chemo- and Hormone- Resistant Cytokeratin-Positive Tumour Cells Circulating in the Blood of Women With Breast Cancer [NCT00428896] | Phase 2 | 24 participants (Actual) | Interventional | 2005-04-30 | Completed | ||
A Phase I/II Trial of ZD1839 (Iressa®) and Rapamycin (Rapamune) in Patients With Advanced Non Small Cell Lung Cancer [NCT00098462] | Phase 1/Phase 2 | 0 participants (Actual) | Interventional | 2004-10-31 | Withdrawn(stopped due to Withdrawn as study never opened) | ||
Neuroblastoma Protocol 2005: Therapy for Children With Advanced Stage High-Risk Neuroblastoma [NCT00135135] | Phase 2 | 23 participants (Actual) | Interventional | 2005-08-31 | Completed | ||
A Randomized Phase III Trial of Chemotherapy Alone Versus Chemotherapy Followed by Gefitinib in Stage IIIB/IV Non-Small Cell Lung Cancer [NCT00144066] | Phase 3 | 600 participants | Interventional | 2003-01-31 | Completed | ||
A Phase I, Open-Label, Dose Escalation Study Evaluating High-Dose Gefitinib (IRESSA®) on Weekly and Twice Weekly Schedules in Subjects With Solid Malignancies That Are Locally Advanced, Recurrent or Metastatic [NCT00127829] | Phase 1 | 66 participants (Anticipated) | Interventional | 2005-07-31 | Completed | ||
Phase I Study of High Dose Gefitinib (Iressa) for the Treatment of Carcinomatous Meningitis in Adult Patients With Non-Small Cell Lung Cancer and Known or Suspected EGFR Mutations [NCT00372515] | Phase 1 | 7 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
A Phase I Open-Label Study to Assess the Safety, Tolerability and PK of Ascending Multiple Oral Doses of AZD2171 When co-Administered With Fixed Multiple Oral Doses of ZD1839 (250mg or 500mg Once Daily) in Patients With Advanced Cancer [NCT00502060] | Phase 1 | 65 participants (Anticipated) | Interventional | 2004-08-31 | Completed | ||
Synergistic Real-World Study and Evidence-based Medicine Evaluation of Elemene Combined With Tyrosine Kinase Inhibitors(TKIs)in the Treatment of Advanced Non-small Cell Lung Cancer (NSCLC): Prospective Study [NCT04401059] | Phase 4 | 744 participants (Anticipated) | Interventional | 2020-11-09 | Recruiting | ||
A Randomized Phase II Trial of Gefitinib With Anlotinib in Advanced Non-squamous NSCLC Patients With Uncleared Plasma ctDNA EGFRm After First-line Treatment With Gefitinib [NCT04358562] | Phase 2 | 240 participants (Anticipated) | Interventional | 2020-05-01 | Not yet recruiting | ||
EGFR-TKI With/Without Chemotherapy in NSCLC Patients With Both EGFR Mutation and BIM Deletion Polymorphism [NCT03002844] | Phase 2 | 50 participants (Anticipated) | Interventional | 2016-12-31 | Not yet recruiting | ||
Phase I-II Study of ZD1839 (IRESSA®), Cisplatin, and External-Beam Radiation Therapy in Patients With Locally Advanced, Non-Metastatic, Squamous Cell Carcinoma of the Head and Neck [NCT00195078] | Phase 1/Phase 2 | 29 participants (Anticipated) | Interventional | 2004-04-30 | Terminated | ||
A Phase Ib, Multi-center, Open Label Study of Ningetinib (CT053PTSA) in Combination With Gefitinib in Stage IIIB or IV NSCLC Patients With EGFR Mutation and T790M Negative Who Have Progressed After EGFR TKI Therapy [NCT03758287] | Phase 1/Phase 2 | 158 participants (Anticipated) | Interventional | 2016-11-30 | Active, not recruiting | ||
Phase II Study of Gefitinib and Docetaxel as Salvage Therapy in Advanced Pancreatic Carcinoma [NCT00177242] | Phase 2 | 45 participants | Interventional | 2004-09-30 | Completed | ||
An Open, Single.Centre, Phase I/II Study of ZD1839 (Iressa) in Combination With 5-Fluorouracil, Leucovorin and Radiotherapy in Subjects With Resectable Gastric Cancer [NCT00237900] | Phase 1/Phase 2 | 34 participants | Interventional | 2003-07-31 | Terminated | ||
A Phase II Exploratory, Multicentre, Open-label, Non-comparative Study of ZD1839 (Iressa™) and Radiotherapy in the Treatment of Patients With Glioblastoma Multiforme [NCT00238797] | Phase 2 | 36 participants | Interventional | 2003-02-28 | Completed | ||
A Phase I/II Trial of ZD1839 (Iressa) Given Concurrently With Cisplatin and Radiotherapy in Patients With Locally Advanced Head and Neck Cancer [NCT00239304] | Phase 1/Phase 2 | 40 participants | Interventional | 2003-06-30 | Completed | ||
Randomised Placebo-controlled Phase II Trial of Preoperative Therapy With Gefitinib (Iressa®/ZD1839) and Epirubicin-Cyclophosphamide in Patients With Primary Operable (T2-T3) Oestrogen Receptor Negative Breast Cancer [NCT00239343] | Phase 2 | 160 participants (Anticipated) | Interventional | 2004-10-31 | Completed | ||
A Phase I Trial to Evaluate ZD1839(Iressa™) and Concurrent Chemo-Radiation in Patients With Locally Advanced Non Small Cell Lung Cancer [NCT00252798] | Phase 1 | 44 participants | Interventional | 2002-07-31 | Completed | ||
Study of Chinese Medicine Plus Targeted Therapy Maintenance Versus Targeted Therapy Maintenance in Advanced Pulmonary Adenocarcinoma: A Randomized Double-blind Controlled Clinical Trial [NCT02889692] | Phase 3 | 23 participants (Actual) | Interventional | 2013-03-31 | Completed | ||
Multicenter, Randomized, Phase Ib/IIb Study to Evaluate the Efficacy and Tolerability of Gefitinib in Combination With Olaparib (AZD2281) Versus Gefitinib Alone, in Patients With EGFR Mutation Positive Advanced Non-small-cell Lung Cancer [NCT01513174] | Phase 1/Phase 2 | 186 participants (Actual) | Interventional | 2011-08-31 | Completed | ||
A Randomized, Controlled Phase II Clinical Trial of Apatinib in Combination With EGFR-TKI Versus EGFR-TKI for Non-squamous, Non-small Cell Lung Cancer(NSCLC) With T790M-negative After the Failure of EGFR-TKI Therapy [NCT03389256] | Phase 2 | 144 participants (Anticipated) | Interventional | 2018-12-30 | Not yet recruiting | ||
Phase II Randomised Clinical Trial Evaluating an EGFR Tyrosine Kinase Inhibitor (EGFR-TKI) Versus an EGFR-TKI Combined With an Anti-oestrogen Treatment (Fulvestrant) in Women With Advanced Stage Non-squamous Lung Cancer [NCT01556191] | Phase 2 | 379 participants (Actual) | Interventional | 2012-05-15 | Completed | ||
A Phase II Study Of Maintenance ZD1839 (IRESSA) In Patients With Locally Advanced Esophageal Cancer After Treatment Given With Curative Intent [NCT00100945] | Phase 2 | 70 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
Phase II Study With Gefitinib (Sequentially) Following Gemcitabine/Cisplatin as Induction Regimen for Patients With Stage IIIA N2 NSCLC [NCT00103051] | Phase 2 | 0 participants | Interventional | 2004-12-31 | Completed | ||
A Phase I/II Trial of Herceptin and ZD1839 (Iressa, NSC #715055, IND#61187) in Patients With Metastatic Breast Cancer That Overexpresses HER2/Neu (erbB-2) [NCT00024154] | Phase 2 | 132 participants (Actual) | Interventional | 2002-02-28 | Completed | ||
A Phase II Study Of ZD 1839 (NSC 715055, IND 61187) In Patients With Malignant Mesothelioma [NCT00025207] | Phase 2 | 40 participants (Actual) | Interventional | 2001-09-30 | Completed | ||
ZD1839 FOR Treatment Of Recurrent Or Progressive Malignant Astrocytoma Or Glioblastoma And Recurrent Or Progressive Meningioma: A Phase II Study With A Phase I Component For Patients Receiving EIAEDs [NCT00025675] | Phase 2 | 105 participants (Actual) | Interventional | 2001-10-09 | Completed | ||
A Phase I/ Randomized Phase II Trial Of Oxaliplatin (NSC #266046) With Or Without ZD 1839 (NSC # 715055) In Patients With Advanced Colorectal Carcinoma [NCT00026299] | Phase 1/Phase 2 | 14 participants (Actual) | Interventional | 2001-09-30 | Completed | ||
A Phase I Study Of ZD 1839 And Temozolomide For The Treatment Of Gliomas [NCT00027625] | Phase 1 | 0 participants | Interventional | 2002-01-28 | Completed | ||
An Expanded Access Clinical Program With ZD1839 (IRESSA®) for Patients With Advanced Non-small Cell Lung Cancer (NSCLC) [NCT00034879] | Phase 3 | 0 participants | Interventional | 2000-08-31 | Completed | ||
A Phase II Trial Of IRESSA (NSC 715055, IND 61187) In Combination With 5-FU/LV/ CPT-11 In Patients With Advanced Or Recurrent Colorectal Cancer [NCT00052585] | Phase 2 | 50 participants (Actual) | Interventional | 2002-10-31 | Terminated(stopped due to Administratively complete.) | ||
A Phase II, Randomized Double-blind, 2-part, Multicenter Study to Compare the Efficacy of ZD6474 With the Efficacy of ZD1839 (Iressa™) in Subjects With Locally Advanced or Metastatic (IIIB/IV) Non-small Cell Lung Cancer After Failure of First-line Platinu [NCT00059722] | Phase 2 | 160 participants | Interventional | 2003-05-31 | Completed | ||
Parallel Phase II Trials of ZD1839 (Iressa) Alone or Weekly Carboplatin and Paclitaxel Followed by ZD1839 (Iressa) (Oncologists Must Choose) for Metastatic Non-Small Cell Lung Cancer in Patients > or = 65 Years of Age [NCT00062062] | Phase 2 | 65 participants (Actual) | Interventional | 2004-10-31 | Completed | ||
Single Agent ZD-1839 (NSC-715055, IND-61187) in Patients With Advanced Head and Neck Carcinoma or Non-Small Cell Lung Cancer Aged 75 Years and Older (and in a Cohort of Patients 50 Years Old and Younger) [NCT00068497] | 40 participants (Anticipated) | Interventional | 2003-08-31 | Completed | |||
Phase II Study of the Combination of ZD1839 (Iressa) and Celecoxib in Patients With Platinum Refractory Non-Small Cell Lung Cance [NCT00068653] | Phase 2 | 27 participants (Actual) | Interventional | 2003-06-30 | Completed | ||
A Phase II Trial of ZD1839 (Iressa®) in Metastatic Neuroendocrine Tumors [NCT00075439] | Phase 2 | 90 participants (Anticipated) | Interventional | 2003-12-31 | Completed | ||
ZD1839 (IRESSA) In Tamoxifen-Resistant Metastatic Breast Cancer [NCT00080743] | Phase 2 | 2 participants (Actual) | Interventional | 2004-01-31 | Completed | ||
A Phase II Study of Docetaxel in Combination With ZD 1839 (IRESSA) in Previously Treated Patients With Metastatic Pancreatic Cancer [NCT00137761] | Phase 2 | 32 participants (Actual) | Interventional | 2004-10-31 | Completed | ||
A Phase II Study Of ZD1839 (NSC #715055) In Renal Cell Carcinoma Stage IV And Renal Cell Carcinoma Recurrent [NCT00014183] | Phase 2 | 0 participants | Interventional | 2001-01-31 | Completed | ||
A Phase II Study of ZD 1839 (NSC 715055) for Patients With First Relapse Glioblastoma Multiforme [NCT00016991] | Phase 2 | 0 participants | Interventional | 2001-06-30 | Completed | ||
A Phase III Trial of Cisplatin/Etoposide/Radiotherapy With Consolidation Docetaxel Followed by Maintenance Therapy With ZD1839 (NSC-715055) or Placebo in Patients With Inoperable Locally Advanced Stage III Non-Small Cell Lung Cancer [NCT00020709] | Phase 3 | 840 participants (Actual) | Interventional | 2001-06-30 | Completed | ||
A Randomized Phase II Trial of Two Dose Levels of ZD1839 (Iressa) (NSC 715055, IND 61187) in Patients With Recurrent Colorectal Adenocarcinoma [NCT00025350] | Phase 2 | 0 participants | Interventional | 2001-10-31 | Completed | ||
A Phase I Study Of ZD1839 (Iressa) In Combination With Irinotecan, Leucovorin, And 5-Fluorouracil In Previously Untreated, Stage IV Colorectal Cancer [NCT00026364] | Phase 1 | 22 participants (Actual) | Interventional | 2001-11-30 | Completed | ||
A Phase II Trial of ZD 1839 (IRESSA) (NSC #715055) in the Treatment of Persistent or Recurrent Endometrial Carcinoma [NCT00027690] | Phase 2 | 56 participants (Actual) | Interventional | 2002-06-30 | Completed | ||
A Phase I Trial of ZD1839 With Capecitabine in Patients With Advanced Solid Tumors (Formerly a Phase I Trial of ZD1839 With Capecitabine and Celecoxib) [NCT00039390] | Phase 1 | 41 participants (Actual) | Interventional | 2002-04-30 | Completed | ||
ZD1839 (NSC #715055, IND #61187) With Induction Paclitaxel And Carboplatin Followed By Either Radiation Or Concomitant Radiation With Weekly Paclitaxel And Carboplatin In Stage III Non-Small Cell Lung Cancer, A Phase II Study [NCT00040794] | Phase 2 | 144 participants (Actual) | Interventional | 2002-05-31 | Completed | ||
Phase II Study Of Cisplatin, Gemcitabine, And ZD 1839 (IRESSA) (IND #61187; NSC 715055) For The Treatment Of Advanced Urothelial Tract Carcinoma [NCT00041106] | Phase 2 | 50 participants (Actual) | Interventional | 2002-05-31 | Completed | ||
A Phase II And Biologic Correlative Study Investigating ARIMIDEX In Combination With IRESSA (ZD1839) In Post-Menopausal Patients With Estrogen Receptor-Positive Metastatic Breast Carcinoma Who Have Previously Failed Hormonal Therapy [NCT00049062] | Phase 2 | 0 participants | Interventional | 2002-09-30 | Completed | ||
A Phase II Trial of ZD1839 (Iressa) (NSC# 715055) in the Treatment of Persistent or Recurrent Epithelial Ovarian or Primary Peritoneal Carcinoma [NCT00023699] | Phase 2 | 0 participants | Interventional | 2001-08-31 | Completed | ||
A Phase II Study of ZD 1839 (Iressa) in Recurrent or Metastatic Squamous Cell Cancer of the Head and Neck [NCT00024089] | Phase 2 | 60 participants (Actual) | Interventional | 2001-07-31 | Completed | ||
A Study of ZD1839 (Iressa) in Combination With Oxaliplatin, 5-Fluorouracil (5-FU) and Leucovorin (LV) in Advanced Solid Malignancies (Phase I) and Advanced Colorectal Cancers (Phase II) [NCT00025142] | Phase 2 | 0 participants | Interventional | 2001-07-31 | Completed | ||
A Phase II Clinical, Biological and Pharmacological Study of ZD1839 in Patients With Advanced Colorectal Carcinoma Refractory to 5-Fluorouracil (5-FU) and Irinotecan Chemotherapy [NCT00030524] | Phase 2 | 0 participants | Interventional | 2002-01-31 | Completed | ||
A Phase I Study Of ZD 1839 In Combination With Radiation And Chemotherapy In Locally Advanced Squamous Cell Carcinoma Of The Head And Neck [NCT00033449] | Phase 1 | 30 participants (Actual) | Interventional | 2002-02-28 | Terminated(stopped due to Administratively complete.) | ||
An IDBBC Single Arm Phase II Trial Evaluating The Activity Of Iressa (ZD1839) In Metastatic Breast Cancer Patients Pretreated With An Antiestrogen And A Non-Steroidal Aromatase Inhibitor (Anastrozole Or Letrozole) [NCT00066339] | Phase 2 | 44 participants (Actual) | Interventional | 2003-05-31 | Completed | ||
An EORTC Randomized, Double Blind, Placebo-Controlled, Phase II Multi-Center Trial Of Anastrozole (Arimidex) In Combination With ZD 1839 (Iressa) Or Placebo In Patients With Advanced Breast Cancer [NCT00066378] | Phase 2 | 71 participants (Actual) | Interventional | 2003-05-31 | Completed | ||
A Phase II Study of ZD1839 (Iressa, Gefitinib, NSC 715055) in Advanced Unresectable Hepatocellular Carcinoma [NCT00071994] | Phase 2 | 59 participants (Actual) | Interventional | 2004-02-29 | Completed | ||
A Phase I Study Of ZD1839 (Iressa TM), An Oral Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor, In Children With Refractory Solid Tumors [NCT00040781] | Phase 1 | 45 participants (Actual) | Interventional | 2002-06-30 | Completed | ||
A Pilot Trial of Daily Oral ZD1839 (Iressa) With Standard Doses of Carboplatin and Paclitaxel in Patients With Advanced Non-Small Cell Lung Cancer [NCT00005806] | Phase 1 | 0 participants | Interventional | 1999-09-30 | Completed | ||
A Phase II Study of Cisplatin and Irinotecan Induction Chemotherapy, Followed by ZD 1839 (IRESSA) in Adult Patients With Surgically Unresectable and/or Metastatic Esophageal or Gastric Carcinomas [NCT00215995] | Phase 2 | 21 participants (Actual) | Interventional | 2003-07-31 | Completed | ||
A Phase II Study of Iressa (Gefitinib), in Patients With Relapsed or Refractory Acute Myelogenous Leukemia and in Older Patients With Newly Diagnosed Acute Myelogenous Leukemia [NCT00130702] | Phase 2 | 18 participants (Actual) | Interventional | 2005-08-31 | Completed | ||
Phase 3 Randomized Study of TLK286 (Telcyta) Versus Gefitinib (Iressa) as Third-Line Therapy in Locally Advanced or Metastatic Non-Small Cell Lung Cancer [NCT00080340] | Phase 3 | 520 participants | Interventional | Completed | |||
Phase II Pilot Study of Clinical Activity and Proteomic Pathway Profiling of the EGFR Inhibitor, ZD1839 (Iressa; Gefitinib), in Patients With Epithelial Ovarian Cancer or Cervical Cancer [NCT00049556] | Phase 2 | 0 participants | Interventional | 2002-10-31 | Completed | ||
A Phase 2, Multi-Center Trial of ZD1839 (IRESSA) in Combination With Docetaxel as First-Line Treatment in Patients With Advanced Breast Cancer [NCT00052169] | Phase 2 | 33 participants (Actual) | Interventional | 2003-01-31 | Completed | ||
A Phase I/II Study of an Oral Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor (EGFR-TKI), ZD 1839 (Iressa), [NSC #715055] With Radiation Therapy in Glioblastoma Multiforme [NCT00052208] | Phase 1/Phase 2 | 158 participants (Actual) | Interventional | 2002-03-31 | Completed | ||
Phase II Study Of Iressa (ZD 1839) In Locally Advanced And/Or Metastatic Synovial Sarcoma Expressing HER1/EGFR1 [NCT00052754] | Phase 2 | 48 participants (Actual) | Interventional | 2002-10-31 | Completed | ||
A Phase II Study to Evaluate the Efficacy and Safety of Iressa as a First-Line Treatment in Chemonaive Patients With Inoperable Non-Small Cell Lung Cancer (NSCLC) [NCT00173875] | Phase 2 | 108 participants (Actual) | Interventional | 2005-03-31 | Completed | ||
A Phase I Study of ZD1839 (Iressa) in Combination With Irinotecan (Camptosar or CPT-11) and Vincristine in Pediatric Patients With Refractory Solid Tumors [NCT00186979] | Phase 1 | 34 participants (Actual) | Interventional | 2003-05-31 | Completed | ||
Phase II Study Of Single Agent Gefitinib (Iressa) In Patients With Clinical Stage I Non-Small Cell Lung Cancer (NSCLC) Proceeding To Mediastinoscopy And Surgery [NCT00188617] | Phase 2 | 35 participants (Actual) | Interventional | 2005-01-31 | Completed | ||
A Phase II Study of ZD1839 and Tamoxifen in Patients With Epithelial Ovarian Carcinoma, Cancer of the Fallopian Tube or the Peritoneum Refractory to Platinum- and Taxane-based Therapy [NCT00189358] | Phase 2 | 0 participants | Interventional | Completed | |||
Phase II Trial of Single Agent ZD1839 (Iressa) in Poor Performance Status Patients With Previously Untreated Advanced Non-Small Cell Lung Cancer [NCT00193336] | Phase 2 | 60 participants | Interventional | 2003-03-31 | Completed | ||
A Phase II Study of ZD1839 (Iressa), Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor, in Combination With Docetaxel in Patients With Recurrent or Metastatic Advanced Non-Small Cell Lung Cancer [NCT00048087] | Phase 2 | 0 participants (Actual) | Interventional | 2002-08-31 | Withdrawn(stopped due to Slow accrual.) | ||
A Phase I Dose Escalation of ZD1839 (Iressa®) (Days 1 and 2) and Docetaxel (Day 3) Every 3 Weeks in Patients With an Advanced Solid Tumor [NCT00084786] | Phase 1 | 0 participants | Interventional | 2004-03-31 | Completed | ||
Neoadjuvant Chemoradiotherapy (Gemcitabine/Cisplatin and Taxotere) With or Without Co-Administration of ZD 1839 (Iressa) for Stage IIIA (N2) and Selective Stage IIIB Non-Small Cell Lung Cancer: Phase I-II Study [NCT00062270] | Phase 1/Phase 2 | 0 participants | Interventional | 2003-05-31 | Completed | ||
Efficacy and Safety of Precision Therapy in Refractory Tumor (Long March Pathway) [NCT03239015] | Phase 2 | 300 participants (Anticipated) | Interventional | 2017-01-01 | Recruiting | ||
Phase II Trial of Weekly Docetaxel (Taxotere) Vs. Weekly Docetaxel in Combination With ZD1839 (Iressa®) As Consolidation Therapy For Metastatic Urothelial Cancer Following Maximal Response To Multi-Agent Chemotherapy [NCT00479089] | Phase 2 | 50 participants (Actual) | Interventional | 2004-02-29 | Terminated(stopped due to Study halted due to drug sponsor decision to not continue.) | ||
Bone Metastasis on the Survival of Gefitinib Effective Patients With Non-small Cell Lung Cancer [NCT03157310] | 265 participants (Actual) | Interventional | 2009-05-01 | Completed | |||
A Phase I Study of ZD1839 (Iressa) and Palliative Thoracic Radiotherapy in Patients With Non-small Cell Lung Cancer [NCT00255489] | Phase 1 | 36 participants | Interventional | 2004-05-31 | Completed | ||
Phase II Study of Iressa With/Without Concurrent Chemoradiotherapy in Patients With Advanced Non-Nasopharyngeal Head and Neck Carcinoma and to Study the Effect of Iressa™ (ZD1839) on Tumour Gene Expression Profiles ® [NCT00228488] | Phase 2 | 60 participants | Interventional | 2004-06-30 | Completed | ||
A Phase II Randomised, Double-Blind, Stratified, Multi-Centre Trial Comparing the Nolvadex 20 Mg And Placebo Combination To The Nolvadex 20 Mg and ZD1839 (IRESSA™) 250 MG Combination In Patients With Metastatic Breast Cancer And Estrogen Receptor (ER) and [NCT00229697] | Phase 2 | 317 participants (Actual) | Interventional | 2003-10-31 | Completed | ||
A Phase II Safety, Efficacy, and Feasibility Study of Neoadjuvant ZD1839 (IRESSA) in Resectable Esophageal Cancer [NCT00258297] | Phase 2 | 30 participants (Anticipated) | Interventional | 2004-04-30 | Terminated(stopped due to Withdrawn for lack of funding and accrual) | ||
A 2 Part Phase 2 Trial to Evaluate ZD1839 (Iressa™) & Radiotherapy in Patients w/Locally Advanced Inoperable Squamous Cell Carcinoma of the Head & Neck [NCT00233636] | Phase 2 | 28 participants | Interventional | 2003-07-31 | Withdrawn | ||
A Trial to Evaluate ZD1839 (IRESSA) in Combination With Radiotherapy & Gemcitabine as First-Line Treatment in Patients With Locally Advanced Pancreatic Cancer [NCT00234416] | Phase 1/Phase 2 | 45 participants | Interventional | 2002-08-31 | Completed | ||
A Phase I/II Study of ZD1839 (Iressa) Given Concurrently With Radiotherapy in Patients With Non-Metastatic Prostate Cancer [NCT00239291] | Phase 1/Phase 2 | 42 participants (Actual) | Interventional | 2003-01-31 | Completed | ||
An Open Label, Non-Comparative, Phase II Study of ZD1839 (Iressa) as First-Line Treatment in Subjects With Relapsed Prostate Cancer Following Radical Prostatectomy or Radiotherapy [NCT00241475] | Phase 2 | 30 participants | Interventional | 2003-12-31 | Completed | ||
A Phase II Study to Evaluate the Safety and Efficacy of the Combination of ZD1839 (IRESSA™), Docetaxel and Cisplatin in Subjects With Recurrent and/or Metastatic Head and Neck Cancer [NCT00242762] | Phase 2 | 36 participants | Interventional | 2003-07-31 | Completed | ||
A Double Blind,Placebo Controlled,Parallel Group,Multicentre,Randomised,Phase Iii Survival Study Comparing ZD1839 (IRESSA™)(250mg Tablet) Plus Best Supportive Care Versus Placebo Plus Best Supportive Care In Patients With Advanced NSCLC Who Have Received [NCT00242801] | Phase 3 | 1,692 participants | Interventional | 2003-07-31 | Completed | ||
Phase II Trial of Neoadjuvant Docetaxel and ZD 1839 (Iressa) Followed by Radical Prostatectomy in Patients With High Risk, Locally Advanced Prostate Cancer [NCT00242918] | Phase 2 | 29 participants | Interventional | 2003-05-31 | Completed | ||
An Open Randomised Phase II Study Of Gemcitabine Plus Cisplatin +/- Concomitant or Sequential ZD1839 in Patients With Advanced or Metastatic Transitional Cell Carcinoma of the Urothelium [NCT00246974] | Phase 2 | 125 participants (Anticipated) | Interventional | 2003-05-31 | Completed | ||
A Multicentre, Randomised, Double-Blind, Non-Comparative Phase II Trial Of ZD1839 (Iressa™) And Placebo In Combination With Chemotherapy With Docetaxel As First-Line Treatment In Patients With Metastatic Breast Cancer [NCT00247481] | Phase 2 | 77 participants | Interventional | 2002-09-30 | Completed | ||
A Multicentre, Randomised, Open-Label, Parallel-Group, Phase III Post-Marketing Clinical Study to Compare the Overall Survival Between Gefitinib and Docetaxel in Patients With Advanced or Metastatic (Stage IIIB/IV), or Recurrent Non-Small Cell Lung Cancer [NCT00252707] | Phase 3 | 484 participants (Anticipated) | Interventional | 2003-09-30 | Completed | ||
A Randomised Phase II Study to Investigate the Feasibility and Benefits of Combining ZD1839 and Cisplatin/5FU, as Induction Therapy, in Patients With Locally and Advanced Squamous Cell Carcinoma of the Head and Neck [NCT00255476] | Phase 2 | 64 participants | Interventional | 2004-02-29 | Completed | ||
A Phase 1 Study of LY2875358 in Japanese Patients With Advanced Malignancies [NCT01602289] | Phase 1 | 17 participants (Actual) | Interventional | 2012-06-30 | Completed | ||
A Phase II Multicentre Randomised, Parallel Group, Double-Blind, Placebo-Controlled Study of ZD1839 (IRESSATM) (250MG Tablet) Plus Best Supportive Care (BSC) Versus Placebo Plus BSC in Chemotherapy-Naive Patients With Advanced (Stage IIIB or IV) Non-Small [NCT00259064] | Phase 2/Phase 3 | 216 participants (Actual) | Interventional | 2004-09-30 | Completed | ||
A Phase II Study of Second-Line Therapy With Irinotecan or Gefitinib in Docetaxel Pretreated Patients With Non-Small Cell Lung Cancer: a New Treatment Strategy According to Clinical Predictors for Response [NCT00319800] | Phase 2 | 50 participants | Interventional | 2006-02-28 | Active, not recruiting | ||
A Phase II Open-Label Multicentre Study Of The Efficacy Of ZD1839 (IRESSA™) In Combination With Irradiation Followed By Chemotherapy In Patients With Inoperable Stage III Non Small Cell Lung Cancer [NCT00333294] | Phase 2 | 50 participants | Interventional | 2004-09-30 | Completed | ||
A Randomized Placebo-controlled Phase II Study of Intercalated Administration of Pemetrexed/Cisplatin With Iressa® (Gefitinib) or Placebo as First-line Treatment of Stage IIIB/IV Lung Adenocarcinoma in Never-smokers [NCT01502202] | Phase 2 | 162 participants (Anticipated) | Interventional | 2012-03-31 | Recruiting | ||
First Line Gefitinib Treatment for Advanced Non-small Cell Lung Cancer (NSCLC) by the FDG-PET Metabolic Response [NCT01510990] | Phase 2 | 60 participants (Anticipated) | Interventional | 2012-04-30 | Recruiting | ||
Phase Ⅱ Study of Gefitinib in Triple-negative,EGFR Positive Metastatic Breast Cancer [NCT01732276] | Phase 2 | 50 participants (Anticipated) | Interventional | 2013-01-31 | Not yet recruiting | ||
Study of Chinese Medicine Plus EGFR-TKI Versus EGFR-TKI in Advanced Pulmonary Adenocarcinoma: a Randomized Double-blind Controlled Clinical Trial [NCT01745302] | 470 participants (Anticipated) | Observational | 2011-11-30 | Enrolling by invitation | |||
A Phase Ⅱ Randomized Controlled Trial to Compare Chemotherapy Sequenced by EGFR-TKIs and Chemotherapy Combined With EGFR-TKIs for Advanced or Metastatic NSCLC Patients Failed to EGFR-TKIs Therapy [NCT01746277] | Phase 2 | 60 participants (Anticipated) | Interventional | 2012-10-31 | Recruiting | ||
A Phase Ⅱ Randomized Clinical Trial Comparing Vinorelbine-ifosfamide With Gefitinib as Third-line Treatment in Advanced EGFR Gene Mutation Negative Non-small Cell Lung Cancer Patients [NCT01749072] | Phase 2 | 120 participants (Anticipated) | Interventional | 2012-12-31 | Recruiting | ||
A Phase Ⅱ Randomized Controlled Trial to Compare Gefitinib With Docetaxel as Second-line Therapy for Advanced or Metastatic Non-squamous NSCLC Patients With Wild-type EGFR [NCT01755923] | Phase 2 | 60 participants (Anticipated) | Interventional | 2012-12-31 | Recruiting | ||
Random Open Exploratory Clinical Research of Sequential Gefitinib With Pemetrexed/Platinum Compare With Pemetrexed/Platinum Treatment for Advanced Non-small Cell Lung Cancer Exploratory Clinical Research [NCT01769066] | Phase 2/Phase 3 | 117 participants (Actual) | Interventional | 2009-12-31 | Completed | ||
Detection of Resistance Genes From Serially Collected Plasma DNA in Non-small Cell Lung Cancer Patients Harboring EGFR Activating Mutation Who Are Being Treated With EGFR TKIs [NCT01776684] | 200 participants (Anticipated) | Interventional | 2012-06-30 | Recruiting | |||
Randomized Phase II Study of Pemetrexed Versus Gefitinib in Previously Treated Patients With Advanced Non-small Cell Lung Cancer [NCT01783834] | Phase 2 | 95 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
A Multi-center Phase II Randomized Study of Customized Neoadjuvant Therapy Versus Standard Chemotherapy in Non-small Cell Lung Cancer (NSLC) Patients With Resectable Stage IIIA (N2) Disease (CONTEST-TRIAL) [NCT01784549] | Phase 2 | 168 participants (Anticipated) | Interventional | 2012-07-31 | Recruiting | ||
Intercalating and Maintenance Use of Iressa vs. Chemotherapy in Selected Advanced NSCLC: a Randomised Study [NCT01404260] | Phase 3 | 219 participants (Actual) | Interventional | 2011-06-30 | Completed | ||
A Multicenter, Randomized, Double-Blind Study of Gefitinib in Combination With Anlotinib or Placebo in Previously Untreated Patients With EGFR Mutation-Positive Advanced Non-Small-Cell Lung Cancer [NCT04028778] | Phase 3 | 310 participants (Anticipated) | Interventional | 2019-04-10 | Recruiting | ||
A Phase Ib, Open-label, Multi-centre Study to Assess the Safety, Tolerability, Pharmacokinetics, and Preliminary Anti-tumour Activity of Volitinib in Combination With Gefitinib in Patients With Epidermal Growth Factor Receptor-mutated Non-small Cell Lung [NCT02374645] | Phase 1 | 64 participants (Actual) | Interventional | 2015-04-30 | Completed | ||
A Randomized, Open-label, Multiple-centre Study of Intercalating and Maintenance Gefitinib in Combination With Chemotherapy for Advanced NSCLC With EGFR Mutation Positive [NCT02299765] | Phase 4 | 61 participants (Actual) | Interventional | 2014-12-31 | Terminated(stopped due to the research data is not statistically significant) | ||
Gefitinib Alone or With Concomitant Whole Brain Radiotherapy for Patients Harboring an EGFR Mutation With Multiple Brain Metastases From Non-Small-cell Lung Cancer: a Phase II/III Randomized Controlled Trial [NCT02338011] | Phase 2/Phase 3 | 210 participants (Anticipated) | Interventional | 2014-11-30 | Recruiting | ||
[NCT02447419] | Phase 2 | 16 participants (Actual) | Interventional | 2014-12-03 | Completed | ||
A Phase IIa, Open-Label, Multi-Center, Multi-Cohort, Immune-Modulated Study of Selected Small Molecules (Gefitinib, AZD9291, or Selumetinib + Docetaxel) or a 1st Immune-Mediated Therapy (IMT; Tremelimumab) With a Sequential Switch to a 2nd IMT (MEDI4736) [NCT02179671] | Phase 2 | 32 participants (Actual) | Interventional | 2014-07-25 | Completed | ||
Phase III Randomized, Placebo Controlled, Trial of Docetaxel Versus Docetaxel Plus ZD1839 (Iressa, Gefitinib) in Performance Status 2 or Previously Treated Patients With Recurrent or Metastatic Head and Neck Cancer [NCT00088907] | Phase 3 | 270 participants (Actual) | Interventional | 2004-08-31 | Terminated(stopped due to It was unlikely that the primary endpoint would be reached based on the fifth interim analysis results.) | ||
APPLE Trial: Feasibility and Activity of AZD9291 (Osimertinib) Treatment on Positive PLasma T790M in EGFR Mutant NSCLC Patients [NCT02856893] | Phase 2 | 156 participants (Anticipated) | Interventional | 2017-10-10 | Active, not recruiting | ||
Retreatment of Gefitinib in the Patients With Non-small Cell Lung Cancer (NSCLC) Previously Responded to Gefitinib A Single Arm, Open Label, Phase II Study [NCT00824746] | Phase 2 | 23 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
A Randomised Phase 2 Trial of Pemetrexed and Gefitinib Versus Gefitinib as First Line Treatment for Patients With Stage IV Non-Squamous Non-Small Cell Lung Cancer With Activating Epidermal Growth Factor Receptor Mutations [NCT01469000] | Phase 2 | 195 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
LUX-Lung 7: A Randomised, Open-label Phase IIb Trial of Afatinib Versus Gefitinib as First-line Treatment of Patients With EGFR Mutation Positive Advanced Adenocarcinoma of the Lung [NCT01466660] | Phase 2 | 319 participants (Actual) | Interventional | 2011-12-13 | Completed | ||
Phase I/II Trial of ZD1839 (Iressa®), Trastuzumab (Herceptin®), and Docetaxel (Taxotere®) in Patients With erbB-2 (HER-2) Overexpressing, Stage IV Breast Carcinoma [NCT00086957] | Phase 1/Phase 2 | 31 participants (Actual) | Interventional | 2004-01-31 | Completed | ||
An Open Label, Randomized, Multicenter, Phase II Study to Compare Efficacy and Safety of Gefitinib/ Pemetrexed With Pemetrexed Alone as Maintenance Therapy in Patients With Advanced (Stage IV) EGFR Mutation Negative or T790M Single Mutation Nonsquamous NS [NCT01579630] | Phase 2/Phase 3 | 52 participants (Actual) | Interventional | 2011-03-31 | Active, not recruiting | ||
A Randomized Placebo Controlled Study to Assess the Rate of PSA Decrease, Anatomical & Metabolic Changes in the Prostate Determined by MRI/3D-MRS & Histological Changes by Biopsy in Subjects With Locally Advanced Prostate Carcinoma Treated With Either Cas [NCT00319787] | Phase 2 | 102 participants | Interventional | 2003-12-31 | Completed | ||
A Phase II Open Label, Multicentre, Single Arm Study to Characterise the Efficacy, Safety and Tolerability of Gefitinib 250 mg (IRESSA) as 3rd Line Treatment Re-challenge in Patients, Who Have Epidermal Growth Factor Receptor (EGFR) Mutation Positive Loca [NCT01530334] | Phase 2 | 61 participants (Actual) | Interventional | 2012-07-31 | Completed | ||
Fruquintinib in Combination With Gefitinib as First-line Therapy in Patients With Advanced Non-squamous Non-small-cell Lung Cancer Harboring Activating EGFR Mutations : a Single-arm, Multicenter, Phase II Study [NCT02976116] | Phase 2 | 50 participants (Actual) | Interventional | 2016-12-31 | Completed | ||
A Phase III,Double-Blind, Randomised Study to Assess the Efficacy and Safety of ASK120067 Versus Gefitinib as First-Line Treatment in Patients With Epidermal Growth Factor Receptor Mutation Positive, Locally Advanced or Metastatic Non-Small Cell Lung Canc [NCT04143607] | Phase 3 | 334 participants (Anticipated) | Interventional | 2019-07-23 | Recruiting | ||
A Phase Ib, Open Label, Multi-center Study to Characterize the Safety, Tolerability and Preliminary Efficacy of EGF816 in Combination With Selected Targeted Agents in EGFR Mutant NSCLC [NCT03333343] | Phase 1 | 105 participants (Actual) | Interventional | 2018-01-29 | Active, not recruiting | ||
Bevacizumab Combined With Gefitinib in the Treatment of Advanced NSCLC Clinical Study of L858R Positive Mutation Patients [NCT04425187] | Phase 2 | 120 participants (Anticipated) | Interventional | 2020-06-08 | Recruiting | ||
A Phase III Randomised, Double Blind, Placebo Controlled, Parallel, Multicentre Study to Assess the Efficacy and Safety of Continuing IRESSA 250 mg in Addition to Chemotherapy Versus Chemotherapy Alone in Patients Who Have Epidermal Growth Factor Receptor [NCT01544179] | Phase 3 | 265 participants (Actual) | Interventional | 2012-03-15 | Completed | ||
Targeted Therapy With Gefitinib in Patients With USP8-mutated Cushing's Disease [NCT02484755] | Phase 2 | 6 participants (Anticipated) | Interventional | 2015-06-30 | Recruiting | ||
Induction Therapy With Gefitinib Followed by Taxane Platinum Chemotherapy and Intercalated Gefitinib in NSCLC Stages II-IIIB With Activating EGFR Mutation - A Single Arm Phase II Trial. [NCT02326285] | Phase 2/Phase 3 | 1 participants (Actual) | Interventional | 2015-11-30 | Terminated(stopped due to Due to low patient enrollment was stopped. Only one patient could be enrolled. 37 patients were pre-screened, but not into the inclusion criteria (wt-EGFR)) | ||
Effect of Metformin in Combination With Tyrosine Kinase Inhibitors (TKI) on Clinical, Biochemical and Nutritional in Patients With Non-Small Cell Lung Carcinoma (NSCLC): Randomized Clinical Trial [NCT03071705] | 120 participants (Anticipated) | Interventional | 2016-03-31 | Recruiting | |||
Randomised, Controlled Study Comparing Chemotherapy Plus Intercalated EGFR-Tyrosine Kinase Inhibitors Combination Therapy With EGFR-Tyrosine Kinase Inhibitors Alone Therapy as First-line Treatment for Patients With Non-Small-Cell Lung Cancer [NCT02031601] | Phase 4 | 250 participants (Anticipated) | Interventional | 2014-01-31 | Recruiting | ||
Multicenter Open-label, Long-term Safety Trial of Treatment Extension With ZD1839 in Patients Who Have Been Treated in Other ZD1839 Clinical Trials. [NCT00357734] | Phase 3 | 14 participants (Actual) | Interventional | 2005-01-31 | Completed | ||
Phase II Study of ZD1839 (Iressa®), Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor in Patients With Advanced, Recurrent or Metastatic Salivary Gland Cancer (IRUSIRES0198) [NCT00509002] | Phase 2 | 37 participants (Actual) | Interventional | 2004-05-31 | Completed | ||
A Phase II Study Evaluating the Efficacy of Iressa Plus Etoposide in Patients With Advanced Hormone Refractory Prostate Cancer [NCT00483561] | Phase 2 | 26 participants (Actual) | Interventional | 2004-01-31 | Terminated(stopped due to PI left UNMC) | ||
A Phase I/II Trial to Assess the Tolerability of RAD 001 With Gefitinib in Patients With Glioblastoma Multiforme and Prostate Cancer and Efficacy in Patients With Castrate Metastatic Prostate Cancer [NCT00085566] | Phase 1/Phase 2 | 61 participants (Actual) | Interventional | 2004-03-31 | Completed | ||
Single-dose, Open-label, Randomized, 2-way Crossover Bioequivalence Study of Gefitinib Tablets Under Fed Conditions in Chinese Healthy Male Subjects [NCT03050177] | Phase 1 | 38 participants (Actual) | Interventional | 2016-09-01 | Completed | ||
A Study of Apatinib Combine With EGFR-TKI for Advanced EGFR-TKI-resistant Non-Small Cell Lung Cancer [NCT03050411] | Phase 1 | 30 participants (Anticipated) | Interventional | 2016-05-31 | Recruiting | ||
An Open-label, Randomized Phase 3 Efficacy Study of ASP8273 vs Erlotinib or Gefitinib in First-line Treatment of Patients With Stage IIIB/IV Non-small Cell Lung Cancer Tumors With EGFR Activating Mutations [NCT02588261] | Phase 3 | 530 participants (Actual) | Interventional | 2016-02-11 | Terminated(stopped due to Following recommendation by SOLAR Study IDMC, Astellas closed enrollment in ASP8273 studies) | ||
Multi-Center, Randomized, Double-Blind Phase II Study Comparing Cediranib (AZD2171) Plus Gefitinib (Iressa, ZD1839) With Cediranib Plus Placebo in Subjects With Recurrent/Progressive Glioblastoma (DORIC Trial) [NCT01310855] | Phase 2 | 38 participants (Actual) | Interventional | 2011-05-31 | Terminated(stopped due to closed to recruitment early due to AstraZeneca not developing cediranib further) | ||
A Multicenter Phase II Trial of Neoadjuvant Gefitinib Followed by Surgery, Followed by Adjuvant Gefitinib in Patients With Unresectable Stage III Non-Small Cell Lung Cancer Harboring Activating Epidermal Growth Factor Receptor Mutations. [NCT02347839] | Phase 2 | 37 participants (Anticipated) | Interventional | 2016-01-31 | Recruiting | ||
The Phase Three Trials of Pemetrexed/Cisplatin Intercalating Gefitinib vs Pemetrexed/Cisplatin Treating EGFR Wild NSCLC(Non Squamous Cell Carcinoma) [NCT03374280] | Phase 2 | 178 participants (Anticipated) | Interventional | 2016-12-01 | Recruiting | ||
A Phase III, Randomized, Multi-center Study to Determine the Efficacy of the Intercalating Combination Treatment of Chemotherapy and Gefitinib or Chemotherapy as Adjuvant Treatment in NSCLC With Common EGFR Mutations. [NCT03381066] | Phase 3 | 225 participants (Anticipated) | Interventional | 2018-04-10 | Recruiting | ||
Gefitinib Versus Combination of Gefitinib With Chemotherapy or Anti-angiogenesis as 1st Line Treatment in Advanced NSCLC Patients Detected With Bim Deletion or Low EGFR Activating Mutation Abundance:A Randomized, Multicentre, Phase II Study [NCT03267654] | Phase 2 | 100 participants (Anticipated) | Interventional | 2017-10-12 | Recruiting | ||
Randomized, Phase II Study With Gefitinib Plus Vinorelbine Versus Gefitinib Alone in Patients Affected by Non-small Cell Lung Cancer (NSCLC) With Activating Mutations of EGFR [NCT02319577] | Phase 2 | 80 participants (Anticipated) | Interventional | 2012-03-31 | Recruiting | ||
A Phase 1 Open-label Prospective Cohort Trial of Curcumin Plus Tyrosine Kinase Inhibitors for Epidermal Growth Factor Receptor (EGFR)-Mutant Advanced Non-small Cell Lung Cancer [NCT02321293] | Phase 1 | 20 participants (Anticipated) | Interventional | 2015-08-31 | Recruiting | ||
Blood Detection of EGFR Mutation For Iressa Treatment [NCT02282267] | 188 participants (Actual) | Interventional | 2014-10-31 | Active, not recruiting | |||
A Multicenter, Randomized, Double-Blind Study of Erlotinib in Combination With Ramucirumab or Placebo in Previously Untreated Patients With EGFR Mutation-Positive Metastatic Non-Small Cell Lung Cancer [NCT02411448] | Phase 3 | 545 participants (Actual) | Interventional | 2015-05-06 | Active, not recruiting | ||
Drug Treatment Patterns and Effects for Metastatic Non-small Cell Lung Cancer Patients In NORway (DELINOR) [NCT05834348] | 20,605 participants (Anticipated) | Observational | 2023-06-26 | Recruiting | |||
A Multicenter, Open-Label Phase 1 Study of DS-1205c in Combination With Gefitinib in Subjects With Metastatic or Unresectable EGFR-Mutant Non-Small Cell Lung Cancer [NCT03599518] | Phase 1 | 20 participants (Actual) | Interventional | 2018-09-21 | Terminated(stopped due to This study was terminated based on a business decision by the Sponsor.) | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |