N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source
dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).
ID Source | ID |
---|---|
PubMed CID | 3062316 |
CHEMBL ID | 1421 |
CHEBI ID | 49375 |
SCHEMBL ID | 8226 |
MeSH ID | M0470497 |
Synonym |
---|
n-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide |
unii-x78ug0a0rn |
x78ug0a0rn , |
dasatinib [usan:inn] |
HY-10181 |
c22h26cln7o2s |
AB01273956-01 |
AB01273956-02 |
sprycel |
nsc-732517 |
dasatinib , |
bms-354825 |
1n1 , |
D03658 |
302962-49-8 |
dasatinib (jan/inn) |
n-(2-chloro-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide |
BCB03_000715 |
NCGC00181129-01 |
anhydrous dasatinib |
dasatinib anhydrous |
bms dasatinib |
dasatinib (anh.) |
dasatinib (anhydrous) |
anh. dasatinib |
DB01254 |
5-thiazolecarboxamide, monohydrate |
nsc732517 |
d-3307 |
sprycel (bristol meyers) |
bms354825 |
5-thiazolecarboxamide, n-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)-1-piperazinyl)-2-methyl-4-pyrimidinyl)amino)- |
bms 354825 |
n-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide |
2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)-n-(2-chloro-6-methylphenyl)thiazole-5-carboxamide |
chembl1421 , |
cid_3062316 |
n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide |
bdbm13216 |
dasatinibum |
CHEBI:49375 , |
nsc-759877 |
bms-354825 hydrate |
EC-000.2122 |
FT-0650671 |
n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide |
KINOME_3650 |
n-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide |
NCGC00181129-02 |
NCGC00181129-05 |
NCGC00181129-03 |
cas-302962-49-8 |
dtxsid4040979 , |
dtxcid2020979 |
tox21_112736 |
nsc759877 |
BCP9000589 |
pharmakon1600-01502275 |
dasatinib (bms-354825) , |
MLS004774145 |
DASATINIB - BMS-354825 |
HMS3265C19 |
HMS3244A06 |
HMS3265C20 |
HMS2043N05 |
HMS3265D19 |
HMS3244A05 |
HMS3265D20 |
HMS3244B05 |
BCPP000263 |
302962-49-8 pound not863127-77-9 |
dasatinib,bms-354825 |
MLS003915609 |
smr002529551 |
CS-0100 |
S1021 |
AKOS015902363 |
AM20080877 |
5-thiazolecarboxamide, n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]- |
BRD-K49328571-001-07-7 |
bms 35482513 |
gtpl5678 |
bms 345825 |
dasatinib [who-dd] |
dasatinib [mi] |
dasatinib [inn] |
MLS006010904 |
ZBNZXTGUTAYRHI-UHFFFAOYSA-N |
SCHEMBL8226 |
tox21_112736_1 |
NCGC00181129-06 |
n-(2-chloro-6-methyl-phenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methyl-pyrimidin-4-yl]amino]thiazole-5-carboxamide |
mfcd11046566 |
Q-101345 |
AC-22749 |
AB01273956_03 |
EX-A401 |
GS-6548 |
SR-00000000554-5 |
sr-00000000554 |
HMS3654K05 |
NCGC00181129-12 |
SW208076-5 |
NCGC00181129-07 |
Q419940 |
BCP01797 |
BRD-K49328571-001-05-1 |
SB17284 |
n-(2-chloro-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl}amino)-1,3-thiazole-5-carboxamide |
AR-270/43507994 |
n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide |
HMS3744C11 |
CCG-264779 |
NCGC00181129-14 |
nsc-800087 |
nsc800087 |
NCGC00481571-01 |
NCGC00181129-22 |
EN300-123025 |
D5949 |
PA-3062316 |
dtxcid50157977 |
l01xe06 |
Z1546610486 |
Dasatinib is a small-molecule kinase inhibitor used for the treatment of imatinib-resistant chronic myelogenous leukemia (CML) Dasatinib has been recently studied for its anti-fibrotic effects in a variety of fibrous diseases.
Dasatinib has an acceptable tolerability profile; it is associated with myelosuppression. Dasatinib 100 mg QD has a favorable safety profile and maintains a similar degree of activity as the previously reported twice-daily dosing schedules.
Dasatinib monotherapy has demonstrated modest clinical activity in chronic myeloid leukemia in lymphoid blastic phase (CML-LBP) Dasatinib has superior preclinical activity in comparison with other tyrosine kinase inhibitors against cells with most common KIT mutation, exon 11.
Dasatinib can enhance the efficacy of paclitaxel or gemcitabine by reducing the cell viability and inhibiting the cell proliferation. Dasatinib is known to cause adverse pulmonary events such as chylothorax.
Treatment with dasatinib caused a decrease in src-phosphorylation and inhibition of downstream pathways, including AKT and ERK1/2 in all cell lines tested. Only the MCF7-TAMR showed a concomitant decrease in markers of cell cycle progression.
Ponatinib and dasatinib seemed to be both safe for the clinical application of Ph-positive CNSL. Pleural effusion is a frequent side effect in patients during d asatinib treatment. Liver dysfunction is a common side effect associated with the treatment of dasasinib.
Dasatinib is a second-generation tyrosine kinase inhibitor of BCR-ABL 1. It is used for first-line treatment of Philadelphia chromosome-positive chronic myeloid leukemia (CML)
Cyclosporine had an additive or synergistic effect on T-cell proliferation when combined with dasatinib and imatinib. In xenografts derived from these two cell lines, d asatinib did not improve the efficacy of cetuximab combined with radiotherapy.
Dasatinib is an orally bioavailable potent inhibitor of multiple tyrosine kinases, including ABL and SRC. It is indicated for the treatment of chronic myeloid leukemia and Philadelphia-positive acute lymphoblastic leukemia.
Intermittent dosing of dasatinib with a once daily regimen has been shown to reduce side effects while preserving clinical efficacy in early and advanced phase chronic myeloid leukemia (CML)
Role | Description |
---|---|
antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
tyrosine kinase inhibitor | Any protein kinase inhibitor that interferes with the action of tyrosine kinase. |
anticoronaviral agent | Any antiviral agent which inhibits the activity of coronaviruses. |
[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 |
---|---|
aminopyrimidine | A member of the class of pyrimidines that is pyrimidine substituted by at least one amino group and its derivatives. |
1,3-thiazoles | |
monocarboxylic acid amide | A carboxamide derived from a monocarboxylic acid. |
N-arylpiperazine | |
N-(2-hydroxyethyl)piperazine | |
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. |
organochlorine compound | An organochlorine compound is a compound containing at least one carbon-chlorine bond. |
[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 |
---|---|---|
Dasatinib Inhibition of BCR-ABL | 19 | 1 |
Acute myeloid leukemia | 0 | 9 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
acetylcholinesterase | Homo sapiens (human) | Potency | 7.2474 | 0.0025 | 41.7960 | 15,848.9004 | AID1347395; AID1347398 |
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 1.0008 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
Fumarate hydratase | Homo sapiens (human) | Potency | 37.2212 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
GALC protein | Homo sapiens (human) | Potency | 0.7079 | 28.1838 | 28.1838 | 28.1838 | AID1159614 |
GLS protein | Homo sapiens (human) | Potency | 15.8489 | 0.3548 | 7.9355 | 39.8107 | AID624170 |
PPM1D protein | Homo sapiens (human) | Potency | 0.0587 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
TDP1 protein | Homo sapiens (human) | Potency | 2.8212 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
GLI family zinc finger 3 | Homo sapiens (human) | Potency | 0.1153 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
AR protein | Homo sapiens (human) | Potency | 14.2904 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID743035; AID743036; AID743042; AID743054; AID743063 |
Smad3 | Homo sapiens (human) | Potency | 1.2589 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
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 | 23.7101 | 0.0006 | 57.9133 | 22,387.1992 | AID1259378 |
nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 10.4375 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224893 |
progesterone receptor | Homo sapiens (human) | Potency | 13.3332 | 0.0004 | 17.9460 | 75.1148 | AID1346795 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 15.4871 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
EWS/FLI fusion protein | Homo sapiens (human) | Potency | 15.9901 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 9.5322 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692; AID720719 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 8.6389 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 2.6832 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 3.9665 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403 |
farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 16.7842 | 0.3758 | 27.4851 | 61.6524 | AID743217 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 0.5925 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982; AID1346985 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 13.1909 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID743069; AID743075; AID743079; AID743080; AID743091 |
polyprotein | Zika virus | Potency | 37.2212 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
67.9K protein | Vaccinia virus | Potency | 8.2852 | 0.0001 | 8.4406 | 100.0000 | AID720579; AID720580 |
peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 0.4730 | 0.0010 | 24.5048 | 61.6448 | AID743215 |
peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 14.9589 | 0.0010 | 19.4141 | 70.9645 | AID743191 |
vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 12.4187 | 0.0237 | 23.2282 | 63.5986 | AID743222; AID743223; AID743241 |
caspase-3 | Homo sapiens (human) | Potency | 33.4915 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 1.1883 | 0.0007 | 23.0674 | 1,258.9301 | AID743085 |
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 1.3333 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 26.6032 | 0.0016 | 28.0151 | 77.1139 | AID1259385; AID1259395 |
nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 0.1000 | 9.1916 | 31.6228 | AID1346983 |
Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 42.2497 | 0.0391 | 47.5451 | 146.8240 | AID1224845; AID1224896 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 17.1895 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
huntingtin isoform 2 | Homo sapiens (human) | Potency | 35.4813 | 0.0006 | 18.4198 | 1,122.0200 | AID1688 |
serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 4.3310 | 0.0037 | 8.6189 | 23.2809 | AID651784; AID651789; AID651793 |
tyrosine-protein kinase Yes | Homo sapiens (human) | Potency | 0.0024 | 0.0000 | 5.0182 | 79.2586 | AID686947 |
nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 25.1131 | 0.0006 | 27.2152 | 1,122.0200 | AID743219 |
geminin | Homo sapiens (human) | Potency | 17.8132 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 6.0596 | 0.0056 | 12.3677 | 36.1254 | AID624032; AID624044 |
Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 10.5909 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
Interferon beta | Homo sapiens (human) | Potency | 0.0735 | 0.0033 | 9.1582 | 39.8107 | AID1347407; AID1347411 |
Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 0.0944 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 10.5909 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 17.8095 | 0.0119 | 17.9420 | 71.5630 | AID651632; AID720516 |
Ataxin-2 | Homo sapiens (human) | Potency | 18.8336 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Neuronal proto-oncogene tyrosine-protein kinase Src | Mus musculus (house mouse) | Activity | 0.0910 | 0.0910 | 0.0910 | 0.0910 | AID1749280 |
Protein cereblon | Homo sapiens (human) | DC50 | 10.0000 | 0.0080 | 0.4835 | 2.1000 | AID1772713 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1345861 | Human SRC proto-oncogene, non-receptor tyrosine kinase (Src family) | 2005 | Cancer research, Jun-01, Volume: 65, Issue:11 | In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. |
AID1345848 | Human SIK family kinase 3 (QIK subfamily) | 2015 | The Biochemical journal, Jan-15, Volume: 465, Issue:2 | The clinically approved drugs dasatinib and bosutinib induce anti-inflammatory macrophages by inhibiting the salt-inducible kinases. |
AID1345890 | Human salt inducible kinase 2 (QIK subfamily) | 2015 | The Biochemical journal, Jan-15, Volume: 465, Issue:2 | The clinically approved drugs dasatinib and bosutinib induce anti-inflammatory macrophages by inhibiting the salt-inducible kinases. |
AID1345606 | Human ABL proto-oncogene 1, non-receptor tyrosine kinase (Abl family) | 2013 | Genes to cells : devoted to molecular & cellular mechanisms, Feb, Volume: 18, Issue:2 | Activity-based kinase profiling of approved tyrosine kinase inhibitors. |
AID1345829 | Human salt inducible kinase 1 (QIK subfamily) | 2015 | The Biochemical journal, Jan-15, Volume: 465, Issue:2 | The clinically approved drugs dasatinib and bosutinib induce anti-inflammatory macrophages by inhibiting the salt-inducible kinases. |
AID1802639 | LanthaScreen Eu Kinase Activity Assay from Article 10.1111/cbdd.12863: \\Synthesis and biological evaluation of novel dasatinib analogues as potent DDR1 and DDR2 kinase inhibitors.\\ | 2017 | Chemical biology & drug design, 03, Volume: 89, Issue:3 | Synthesis and biological evaluation of novel dasatinib analogues as potent DDR1 and DDR2 kinase inhibitors. |
AID1797044 | Kinase Assay and Binding Constant Measurement from Article 10.1073/pnas.0504952102: \\Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.\\ | 2005 | Proceedings of the National Academy of Sciences of the United States of America, Aug-02, Volume: 102, Issue:31 | Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. |
AID1799403 | Tyrosine Kinase Inhibition Assay from Article 10.1038/nchembio.162: \\A new screening assay for allosteric inhibitors of cSrc.\\ | 2009 | Nature chemical biology, Jun, Volume: 5, Issue:6 | A new screening assay for allosteric inhibitors of cSrc. |
AID1804127 | No assay is provided from Article 10.1002/med.21724: \\The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.\\ | 2021 | Medicinal research reviews, 01, Volume: 41, Issue:1 | The recent outbreaks of human coronaviruses: A medicinal chemistry perspective. |
AID1799177 | Kinetics Assay for IC50 Determination from Article 10.1021/jm9002928: \\Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc.\\ | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. |
AID1799404 | Serine/Threonine Kinase Inhibition Assay from Article 10.1038/nchembio.162: \\A new screening assay for allosteric inhibitors of cSrc.\\ | 2009 | Nature chemical biology, Jun, Volume: 5, Issue:6 | A new screening assay for allosteric inhibitors of cSrc. |
AID1802324 | HotSpot Kinase Activity Assay from Article 10.1021/acschembio.6b00709: \\Chemical Proteomics and Structural Biology Define EPHA2 Inhibition by Clinical Kinase Drugs.\\ | 2016 | ACS chemical biology, 12-16, Volume: 11, Issue:12 | Chemical Proteomics and Structural Biology Define EPHA2 Inhibition by Clinical Kinase Drugs. |
AID1802323 | Kinobeads Competition Assay from Article 10.1021/acschembio.6b00709: \\Chemical Proteomics and Structural Biology Define EPHA2 Inhibition by Clinical Kinase Drugs.\\ | 2016 | ACS chemical biology, 12-16, Volume: 11, Issue:12 | Chemical Proteomics and Structural Biology Define EPHA2 Inhibition by Clinical Kinase Drugs. |
AID1802640 | FRET-Based Z'-Lyte Assay from Article 10.1111/cbdd.12863: \\Synthesis and biological evaluation of novel dasatinib analogues as potent DDR1 and DDR2 kinase inhibitors.\\ | 2017 | Chemical biology & drug design, 03, Volume: 89, Issue:3 | Synthesis and biological evaluation of novel dasatinib analogues as potent DDR1 and DDR2 kinase inhibitors. |
AID1799577 | Kinase Assay from Article 10.1111/j.1747-0285.2007.00556.x: \\Crystal structure of the T315I mutant of AbI kinase.\\ | 2007 | Chemical biology & drug design, Sep, Volume: 70, Issue:3 | Crystal structure of the T315I mutant of AbI kinase. |
AID1797004 | Lck Kinase Inhibition Assay from Article 10.1021/jm060727j: \\2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-met | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatin |
AID1801731 | Kinome-Wide Inhibitor Profiling from Article 10.1021/acschembio.5b01018: \\Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.\\ | 2016 | ACS chemical biology, 05-20, Volume: 11, Issue:5 | Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity. |
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. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
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. |
AID627338 | Inhibition of LCK using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
AID1425182 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 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. |
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. |
AID1612815 | Inhibition of LCK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID435152 | Binding constant for CAMK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID507684 | Inhibition of cKIT D816V mutant | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID1817039 | Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT assay | |||
AID329191 | Inhibition of TAP-tagged Btk T474I mutant | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
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AID303305 | Inhibition of Abl kinase | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib. |
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AID435831 | Binding constant for RPS6KA5(Kin.Dom.1 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625121 | Binding constant for RET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1439891 | Antiproliferative activity against human K562 cells | 2017 | ACS medicinal chemistry letters, Apr-13, Volume: 8, Issue:4 | RITA Mimics: Synthesis and Mechanistic Evaluation of Asymmetric Linked Trithiazoles. |
AID1425126 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1774078 | Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 4 uM incubated for 1 week by absorbance method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
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AID271973 | Inhibition of FGFR1 | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatin |
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AID435410 | Binding constant for KIT kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625097 | Binding constant for TNNI3K kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424953 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1764401 | Ratio of drug concentration in brain to plasma of P-gp knock out Sprague-Dawley rat | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
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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. |
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AID507074 | Inhibition of recombinant PI3Kdelta 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. |
AID435281 | Binding constant for full-length CSNK1A1L | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID729551 | Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells at 10 uM by TR-FRET based binding assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay. |
AID624868 | Binding constant for MST1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624745 | Binding constant for PKN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID507680 | Inhibition of ABL T315I mutant | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID709933 | Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
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. |
AID1425030 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435911 | Binding constant for MEK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID718818 | Inhibition of Abl at 100 uM | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening. |
AID435407 | Binding constant for FLT3(D835Y) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1473869 | Ratio of drug concentration at steady state in patient with advanced phase CML and Ph+ ALL at 100 mg, po BID after 12 hrs to IC50 for human MRP4 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. |
AID435279 | Binding constant for full-length CDK9 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID360790 | Antiviral activity against Dengue virus 2 infected in human Huh7 cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
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. |
AID435545 | Binding constant for NEK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435563 | Binding constant for TNIK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID282238 | Inhibition of FGFR1 kinase | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID625091 | Binding constant for MAST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425164 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435694 | Binding constant for TNK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID735399 | Cytotoxicity against human LXFA 983L cells after 4 days by propidium iodide staining | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography. |
AID1206297 | Antiinvasive activity against human MDA-MB-231 cells at 0.1 uM after 24 hrs by transwell assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 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). |
AID625114 | Binding constant for GSK3A 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. |
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. |
AID624912 | Binding constant for TYK2(JH1domain-catalytic) 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. |
AID1473865 | Drug concentration at steady state in patient with advanced phase CML and Ph+ ALL at 100 mg, po BID after 12 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. |
AID1616470 | Protac activity against VHL/BCR-ABL in human K562 cells assessed as induction of BCR-ABL degradation at 20 times IC50 incubated for 12 hrs followed by drug wash-out and incubation in drug-free medium up to 72 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. |
AID1224792 | Delta TM value showing the stabilisation of RIOK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435930 | Binding constant for PHKG2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1424990 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID677647 | Antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as inhibition of network formation at 1.8 to 15 uM after 72 hrs | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17 | A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model: from in silico screening to cyclodextrin formulation. |
AID1764399 | Unbound plasma concentration in P-gp knock out Sprague-Dawley rat at 5 mg/ml/kg, po measured upto 4 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
AID625127 | Binding constant for RSK3(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435534 | Binding constant for NEK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID724977 | Inhibition of human recombinant ABL1 G250E mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID1915580 | Cytotoxicity against human K562 cells | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID625141 | Binding constant for RIOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624995 | Binding constant for CSF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625095 | Binding constant for SIK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624881 | Binding constant for PKAC-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1186126 | Antiproliferative activity against human GXF251L cells after 4 days by modified propidium iodide assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Pyrrolo[3,2-b]quinoxaline derivatives as types I1/2 and II Eph tyrosine kinase inhibitors: structure-based design, synthesis, and in vivo validation. |
AID435934 | Binding constant for PLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID435646 | Binding constant for BLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624844 | Binding constant for CDK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624737 | Binding constant for EPHA5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625008 | Binding constant for EPHA1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425062 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID458676 | Inhibition of CSF1-stimulated human FMS autophosphorylation expressed in growth factor dependent mouse FDC-P1 cells relative to control by Western blot | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Colony stimulating factor-1 receptor as a target for small molecule inhibitors. |
AID498533 | Antiproliferative activity against human CML cells | 2009 | Nature chemical biology, Mar, Volume: 5, Issue:3 | A pulse at the heart of targeted therapy. |
AID1224765 | Delta TM value showing the stabilisation of CK1G2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624726 | Binding constant for HIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID282248 | Inhibition of PKCalpha | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID415074 | Inhibition of VEGFR2 | 2009 | Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8 | Structure-based virtual screening of Src kinase inhibitors. |
AID1424995 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624920 | Binding constant for MRCKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1205061 | Inhibition of ACK1 kinase (unknown origin) | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Development of novel ACK1/TNK2 inhibitors using a fragment-based approach. |
AID435779 | Binding constant for ALK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID282266 | Toxicity in nude mouse | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID627293 | Inhibition of c-Src using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
AID463628 | Inhibition of Src | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4 | Selectively nonselective kinase inhibition: striking the right balance. |
AID625118 | Binding constant for CAMK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424949 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID640177 | Cytotoxicity against human K562 cells after 72 hrs by WST-8 reagent based MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Design, synthesis, and in vitro antiproliferative activity of novel Dasatinib derivatives. |
AID1734864 | Inhibition of Fra1 phosphorylation in human MDA-MB-231 cells at 0.03 to 0.3 uM incubated for 20 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
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AID1224781 | Delta TM value showing the stabilisation of PAK4 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435402 | Binding constant for EGFR(G719S) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1242627 | Inhibition of c-Kit (unknown origin) using biotinylated HER2 peptide as substrate at 0.003 uM by time resolved fluorescence method | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors. |
AID624963 | Binding constant for LATS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425110 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID735396 | Cytotoxicity against human RXF 393NL cells after 4 days by propidium iodide staining | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography. |
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AID1886532 | Vasculo-toxicity in human HMVEC cells assessed as reduction in vascular structure integrity by measuring AUC measured after 6 hrs by calcein AM dye based fluorescence assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
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. |
AID435198 | Binding constant for TIE1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1424947 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID436053 | Binding constant for full-length STK33 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1207363 | Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells expressing hKvLQT1/hminK measured using IonWorks Quattro automated patch clamp platform | |||
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AID1876318 | Antiviral activity against MERS-CoV infected in 1 hr pretreated african green monkey Vero E6 cells measured after 48 hrs by fluorescence based plate reader method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy. |
AID624754 | Binding constant for NEK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624916 | Binding constant for ULK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID1873218 | Inhibition of ABCG2 (unknown origin) expressed in human K562 cells assessed as extrusion of Hoechst 33342 using Hoechst 33342 as substrate 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. |
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AID1424932 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1774076 | Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli at 400 uM incubated for 1 hr in presence of 75 uM ANS by fluorescence method (Rvb = 91 +/- 0.92%) | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID360778 | Antiviral activity against Modoc virus M544 infected in african green monkey Vero cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
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AID625004 | Binding constant for EGFR(L858R,T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624945 | Binding constant for BMPR1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625038 | Binding constant for PIK3CA(E542K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID435785 | Binding constant for full-length CDK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative 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. |
AID624845 | Binding constant for CDK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID375156 | Antiproliferative activity against human PC3 cells assessed as reduction of cell count at 100 nM after 5 hrs | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. |
AID436033 | Binding constant for PIK3CA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1246523 | Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for human K562 cells | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID1425074 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435280 | Binding constant for CSF1R kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1240469 | Inhibition of Bcr-Abl T315I mutant (unknown origin) using Tyr2 peptide substrate after 2 hrs by FRET-based Z'-lyte assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. |
AID329198 | Inhibition of basal TNFalpha release in human U937 cells at 2 uM after 1 hr by ELISA | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID1424943 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1616418 | Protac activity against VHL/BCR-ABL in human K562 cells assessed as induction of BCR-ABL degradation at 100 nM by Western blot analysis | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. |
AID1425192 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID282222 | Antiproliferative activity against human PC3 cells after 72 hrs | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
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. |
AID624893 | Binding constant for MEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625043 | Binding constant for PIK3CA(I800L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424924 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435798 | Binding constant for FGR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID671741 | Inhibition of human BTK by enzymatic assay | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
AID1425174 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1421413 | Inhibition of recombinant human Erbb4 at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
AID1424896 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507073 | Inhibition of recombinant PI3Kbeta 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. |
AID624802 | Binding constant for PIM3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624836 | Binding constant for IKK-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1207457 | Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform | |||
AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 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. |
AID1425146 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID638912 | Inhibition of c-Kit at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
AID271968 | Inhibition of Yes | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatin |
AID732825 | Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. |
AID624873 | Binding constant for PAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224748 | Delta TM value showing the stabilisation of AMPKA2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624976 | Binding constant for PRKX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID435275 | Binding constant for BIKE kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1573074 | Antiproliferative activity against human HCT116 cells | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID624781 | Binding constant for CDK4-cyclinD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435937 | Binding constant for TESK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID724665 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
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. |
AID329181 | Binding affinity to Btk from human K562 cells extract by LC-MSMS | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID624740 | Binding constant for LRRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1734825 | Induction of apoptosis in human MDA-MB-231 cells assessed as early apoptotic cells at 0.1 uM incubated for 24 hrs by annexin V-FITC and propidium iodide staining based flow cytometry analysis (Rvb = 2 %) | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
AID1373718 | Inhibition of colony formation in human MCF7 cells at 7.5 uM incubated for 10 days by crystal violet staining based plate cloning test | 2018 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4 | Design and synthesis of novel dasatinib derivatives as inhibitors of leukemia stem cells. |
AID1310140 | Antimigratory activity in human MDA-MB-231 cells assessed as reduction in cell motility at 10 nM at 6 hrs by microscopy based scratch-wound cell migration assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID1396666 | Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay | |||
AID767460 | Inhibition of CSF1R (unknown origin) | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Selectivity data: assessment, predictions, concordance, and implications. |
AID624915 | Binding constant for PIP5K2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224749 | Delta TM value showing the stabilisation of CAMK1D produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1425040 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID271971 | Inhibition of Her1 | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatin |
AID1876319 | Antiviral activity against SARS-CoV in 2 hrs pretreated african green monkey Vero E6 cells measured after 48 hrs by CellTireGlo luminescent cell viability assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy. |
AID624770 | Binding constant for CAMK2D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1857476 | Inhibition of LIMK1/LIMK2 in human SH-SY5Y cells assessed as effect on phospho cofilin serine 3 phosphorylation incubated for 2 hr by AlphaLISA SureFire assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20 | Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
AID624769 | Binding constant for AURKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1450952 | Selectivity ratio of Kd for recombinant human N-terminal His6-tagged Wee1 kinase domain (291 to 575 residues) to Kd for recombinant human N-terminal His6-tagged Wee2 kinase domain (202 to 492 residues) | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors. |
AID1573088 | Antiproliferative activity against human GL261 cells | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID1310129 | Inhibition of human PDGFRalpha using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID435149 | Binding constant for AMPK-alpha2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1450947 | Binding affinity to recombinant human N-terminal His6-tagged Myt1 kinase domain (75 to 361 residues) by isothermal titration calorimetry | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors. |
AID1772713 | PROTAC activity at CRBN/Bcr-Abl in human K562 cells assessed as degrading activity by Western blotting analysis | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation. |
AID625140 | Binding constant for MARK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435654 | Binding constant for full-length ERK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1286541 | Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID1424910 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435151 | Binding constant for CAMK1G kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1424939 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1206292 | Induction of apoptosis in human MDA-MB-231 cells assessed as viable cells at 0.3 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 94.4%) | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID1207489 | Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform | |||
AID435900 | Binding constant for AKT3 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. |
AID624813 | Binding constant for MINK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625142 | Binding constant for TSSK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425103 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435411 | Binding constant for KIT(D816V) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID329192 | Inhibition of LPS-induced Btk autophosphorylation on Tyr223 in human U937 cells after 1 hr | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID1206294 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G0/G1 phase at 0.3 uM after 24 to 48 hrs by flow cytometric analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID625053 | Binding constant for PRKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435676 | Binding constant for LCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1186996 | Cytotoxicity against human HepG2 cells assessed as cell viability at 100 uM after 24 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
AID624750 | Binding constant for PRP4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1724049 | Inhibition of Src (unknown origin) | 2020 | Bioorganic & medicinal chemistry, 09-15, Volume: 28, Issue:18 | Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors. |
AID1310168 | Half life in nude mouse at 10 mg/kg, iv via oral gavage | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID1734720 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
AID435806 | Binding constant for MAPKAPK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1286553 | Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID329189 | Inhibition of LPS-induced Btk autophosphorylation on Tyr223 in human U937 cells at >= 100 nM after 1 hr | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID624866 | Binding constant for MLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1301837 | Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
AID1425116 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435559 | Binding constant for SNARK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1764402 | Unbound brain-to-plasma concentration ratio in P-gp knock out Sprague-Dawley rat | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
AID435293 | Binding constant for JNK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1612830 | Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID1409089 | Inhibition of human ABL at 100 uM | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
AID624784 | Binding constant for INSR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625073 | Binding constant for SGK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424972 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID329202 | Inhibition of antigen-induced histamine release in wild-type BMMCs at 1 uM after 30 mins | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID435652 | Binding constant for EGFR(L747-E749del, A750P) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID282262 | Clearance in Sprague-Dawley rat at 10 mg/kg, iv | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1450955 | Binding affinity to recombinant human N-terminal His6-tagged Myt1 kinase domain (75 to 361 residues) assessed as change in melting temperature at 50 uM by differential scanning fluorimetry | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors. |
AID507704 | Inhibition of FES at 10 mM | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID592838 | Inhibition of c-SRC | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8 | Synthesis and pharmacological evaluation of thieno[2,3-b]pyridine derivatives as novel c-Src inhibitors. |
AID435278 | Binding constant for full-length CDK7 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625050 | Binding constant for PKN2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624882 | Binding constant for PKAC-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID718820 | Inhibition of EPHA2 at 100 uM | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening. |
AID1425014 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625009 | Binding constant for EPHA3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435677 | Binding constant for LOK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1310134 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 5 days by PrestoBlue assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID360781 | Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID436017 | Binding constant for ERK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID282232 | Inhibition of yes kinase | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID625291 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal | 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). |
AID435394 | Binding constant for CAMK2B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID463631 | Inhibition of Bcr-Abl Y253F mutant | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4 | Selectively nonselective kinase inhibition: striking the right balance. |
AID625096 | Binding constant for STK36 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID329193 | Inhibition of LPS-induced Btk T474I autophosphorylation on Tyr223 in human U937 cells after 1 hr | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID625012 | Binding constant for GAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1734721 | Antiproliferative activity against human MDA-MB-435 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
AID435163 | Binding constant for full-length GSK3B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID724650 | Inhibition of BCR-ABL T315I mutant in mouse BA/F3 cells after 4 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID1515661 | Binding affinity to wild-type human partial length TNK2 (S159 to D474 residues) expressed in bacterial expression system by TR-FRET assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Controlling cellular distribution of drugs with permeability modifying moieties. |
AID624911 | Binding constant for TXK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1331474 | Inhibition of recombinant human Abl T315I mutant using abtide as substrate by [gamma-32P]ATP based assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Novel pyrazolo[3,4-d]pyrimidines as dual Src-Abl inhibitors active against mutant form of Abl and the leukemia K-562 cell line. |
AID640176 | Growth inhibition of human U937 cells at 10 uM after 72 hrs by WST-8 reagent based MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Design, synthesis, and in vitro antiproliferative activity of novel Dasatinib derivatives. |
AID435326 | Binding constant for TYRO3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435780 | Binding constant for BMPR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624858 | Binding constant for JAK1(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625046 | Binding constant for PIK3CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1386050 | Inhibition of wild type BCR-ABL1 (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
AID1425005 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435558 | Binding constant for RPS6KA3(Kin.Dom.1 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624951 | Binding constant for EPHA2 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. |
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. |
AID624988 | Binding constant for ABL1(T315I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID638914 | Inhibition of PDGFRbeta at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
AID1425153 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1409088 | Inhibition of human c-Src at 100 uM | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
AID624827 | Binding constant for CAMK2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID282236 | Inhibition of Her1 kinase | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1424986 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1315387 | Cytotoxicity against human A549 cells assessed as reduction in cell viability after 96 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Part-1: Design, synthesis and biological evaluation of novel bromo-pyrimidine analogs as tyrosine kinase inhibitors. |
AID624733 | Binding constant for SIK 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. |
AID436013 | Binding constant for DMPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624931 | Binding constant for CLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1315386 | Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 96 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Part-1: Design, synthesis and biological evaluation of novel bromo-pyrimidine analogs as tyrosine kinase inhibitors. |
AID435935 | Binding constant for RIPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1240468 | Inhibition of wild type Bcr-Abl (unknown origin) using Tyr2 peptide substrate after 2 hrs by FRET-based Z'-lyte assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. |
AID1612812 | Inhibition of BTK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID507422 | Inhibition of recombinant Ret 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. |
AID1886531 | Inhibition of ABL1 T315I mutant (unknown origin) | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
AID1424992 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625109 | Binding constant for BIKE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1817043 | Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | |||
AID1425150 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1186994 | Cytotoxicity against human HepG2 cells assessed as cell viability at 1 uM after 24 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
AID435529 | Binding constant for LATS1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624994 | Binding constant for AKT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624961 | Binding constant for TGFBR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224807 | Delta TM value showing the stabilisation of YSK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID436012 | Binding constant for full-length CSNK2A1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224758 | Delta TM value showing the stabilisation of CDK6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435822 | Binding constant for MEK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624792 | Binding constant for KIT(V559D,T670I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224755 | Delta TM value showing the stabilisation of CAMK4 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435655 | Binding constant for ERK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625115 | Binding constant for PAK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625107 | Binding constant for DMPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1876247 | Antiviral activity against DENV infected in 180 mins pretreated african green monkey Vero cells incubated for 1 to 72 hrs | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID624830 | Binding constant for CDK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID735397 | Cytotoxicity against human PRXF DU145 cells after 4 days by propidium iodide staining | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography. |
AID624957 | Binding constant for EPHB6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224795 | Delta TM value showing the stabilisation of SLK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435532 | Binding constant for MST3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1386085 | Inhibition of BCR-ABL1 Q252H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
AID624905 | Binding constant for CDKL5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425075 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424998 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1240405 | Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. |
AID710011 | Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
AID1425022 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425128 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1224778 | Delta TM value showing the stabilisation of NEK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624953 | Binding constant for EPHA7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625117 | Binding constant for PAK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624888 | Binding constant for ERK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624761 | Binding constant for CDC2L5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625080 | Binding constant for EIF2AK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624703 | Binding constant for MAPKAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID638922 | Inhibition of RON at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
AID1616472 | Protac activity against VHL/BCR-ABL in human K562 cells assessed as reduction in BCR-ABL-mediated STAT5 phosphorylation at 20 times IC50 incubated for 12 hrs followed by drug wash-out and incubation in drug-free medium up to 72 hrs by Western blot analysi | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. |
AID507682 | Inhibition of mouse BLK | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID1425082 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624829 | Binding constant for CDK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1612826 | Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID1310175 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability at 0.03 to 300 uM after 5 days by PrestoBlue assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
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. |
AID375154 | Inhibition of human DU145 cell adhesion at 100 nM after 5 hrs by light microscopy | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. |
AID624820 | Binding constant for ACVR2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
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. |
AID1246518 | Cytotoxicity against human K562 cells assessed as reduction in cell viability | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID435276 | Binding constant for BMPR1A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625055 | Binding constant for MST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424978 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625129 | Binding constant for HIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424960 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1421417 | Inhibition of recombinant human ABL at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
AID507683 | Inhibition of cKIT | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID1425196 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425118 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
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. |
AID625143 | Binding constant for CAMKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425186 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID303309 | Growth inhibition of human M07e cells after 48 hrs by [3H]thymidine uptake assay | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib. |
AID435321 | Binding constant for PRKCQ kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID624930 | Binding constant for TNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624985 | Binding constant for ABL1(M351T)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624885 | Binding constant for ERK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1573085 | Antiproliferative activity against human LN18 cells | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID724675 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID1205872 | Angiostatic activity in human ECRF24 cells assessed as inhibition of cell migration after 7 hrs by laser scanner cytometry based wound closure assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Improved angiostatic activity of dasatinib by modulation with hydrophobic chains. |
AID1425176 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1612822 | Inhibition of Fyn A (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID1734827 | Antimigratory activity against human MDA-MB-231 cells assessed as inhibition of cell migration at 0.3 uM incubated for 20 hrs by wound healing assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
AID1450945 | Binding affinity to recombinant human N-terminal His6-tagged Wee1 kinase domain (291 to 575 residues) expressed in Escherichia coli BL21 (DE3) by isothermal titration calorimetry | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors. |
AID1425011 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624869 | Binding constant for NEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424988 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID375152 | Inhibition of human PC3 cell adhesion at 100 nM after 5 hrs by light microscopy | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. |
AID282251 | Inhibition of PKCzeta | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID624753 | Binding constant for PKNB(M.tuberculosis) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425063 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1695245 | Growth inhibition of human Ri1 cells incubated for 72 hrs | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Understanding the mechanism of action of pyrrolo[3,2- |
AID435322 | Binding constant for PRKG2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624834 | Binding constant for DAPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID1053271 | Inhibition of ACE (unknown origin) assessed as 3-Hydroxybutyril-glycil-glycil-glycine conversion to 3-hydroxybutyric acid at 500 uM after 60 mins by WST assay relative to control | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching. |
AID435162 | Binding constant for FLT3(N841I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624839 | Binding constant for AKT2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID360775 | Antiviral activity against Dengue virus 1 Hawaii infected in african green monkey Vero cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
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). |
AID498532 | Cmax in chronic myeloid leukemia patient | 2009 | Nature chemical biology, Mar, Volume: 5, Issue:3 | A pulse at the heart of targeted therapy. |
AID625029 | Binding constant for BRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625135 | Binding constant for ADCK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1515656 | Binding affinity to wild-type human partial length LCK (R207 to P509 residues) expressed in bacterial expression system by TR-FRET assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Controlling cellular distribution of drugs with permeability modifying moieties. |
AID435931 | Binding constant for PIM1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID638920 | Inhibition of EPH-B2 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
AID282265 | Antitumor activity against human K562 xenograft in nude mouse at 50 mg/kg, po for 10 days in 5 day on and 2 day off schedule | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1772722 | PROTAC activity at CRBN/Bcr-Abl in human K562 cells assessed as reduction in Bcr-Abl level after 16 hrs by Western blotting analysis | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation. |
AID507075 | Inhibition of recombinant PI3Kgamma 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. |
AID435518 | Binding constant for AURKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435821 | Binding constant for GAK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1246519 | Cytotoxicity against imatinib resistant human IR-K562 cells assessed as reduction in cell viability | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID1206281 | Induction of apoptosis in human MDA-MB-231 cells assessed as early apoptotic cells at 0.3 uM after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 1.58%) | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID1739051 | Binding affinity to human CSF1R | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone. |
AID760519 | Cytotoxicity against human HMEC after 72 hrs by WST1 assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1823816 | Inhibition of CSF1R (unknown origin) by enzymatic assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration. |
AID435329 | Binding constant for YSK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435433 | Binding constant for full-length MST1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1616414 | Protac activity against VHL/BCR-ABL in human K562 cells assessed as induction of BCR-ABL degradation at 10 uM by Western blot analysis | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. |
AID1286552 | Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID1515646 | Ratio of drug concentration in unbound HEK293 cell to media | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Controlling cellular distribution of drugs with permeability modifying moieties. |
AID627290 | Inhibition of RSK2 using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
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. |
AID435804 | Binding constant for LYN kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1893830 | Binding affinity to Src (unknown origin) assessed as inhibition constant | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-Aminothiazole: A privileged scaffold for the discovery of anti-cancer agents. |
AID1286561 | Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID1205868 | Cytotoxicity against human ECRF24 cells after 72 hrs by MTT assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Improved angiostatic activity of dasatinib by modulation with hydrophobic chains. |
AID435678 | Binding constant for MUSK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435801 | Binding constant for full-length GSK3A | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID507701 | Inhibition of TIE2 at 10 mM | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID435190 | Binding constant for full-length PIP5K1A | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625098 | Binding constant for IRAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424907 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624751 | Binding constant for PIP5K1C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1515660 | Binding affinity to wild-type human partial length SIK (M1 to Y304 residues) expressed in bacterial expression system by TR-FRET assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Controlling cellular distribution of drugs with permeability modifying moieties. |
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. |
AID625123 | Binding constant for RET(V804L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625125 | Binding constant for CLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425171 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1202518 | Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Design and optimization of hybrid of 2,4-diaminopyrimidine and arylthiazole scaffold as anticancer cell proliferation and migration agents. |
AID1310136 | Inhibition of FAK phosphorylation at tyrosine 861 in human MDA-MB-231 cells at 3 to 100 nM preincubated for 1.5 hrs followed by serum stimulation for 1 hr by Western blot analysis | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID1425101 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425198 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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). |
AID1734822 | Induction of apoptosis in human MDA-MB-231 cells assessed as necrotic cells at 0.1 uM incubated for 24 hrs by annexin V-FITC and propidium iodide staining based flow cytometry analysis (Rvb = 0.2 %) | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
AID624996 | Binding constant for EGFR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID724671 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID435560 | Binding constant for SNF1LK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative 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). |
AID1424905 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1504524 | Inhibition of MAPK p38 (unknown origin) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis and biological evaluation of novel benzimidazole amidines as potent multi-target inhibitors for the treatment of non-small cell lung cancer. |
AID1182700 | Antiproliferative activity against human HMC-1.2 cells carrying V560G, D816V mutant assessed as cell growth inhibition by MTT assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Development and biological evaluation of potent and selective c-KIT(D816V) inhibitors. |
AID1425002 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624843 | Binding constant for CAMK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625010 | Binding constant for FER kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425206 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424962 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435561 | Binding constant for SRMS kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID282257 | Cmax in Sprague-Dawley rat at 10 mg/kg, po | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID624755 | Binding constant for ZAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435188 | Binding constant for PAK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID282252 | Cmax in Sprague-Dawley rat at 10 mg/kg, iv | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1857473 | Inhibition of PAK mediated recombinant LIMK2 phosphorylation (347 to 659 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 180 mins by RapidFire Mass Spectrometry kinase assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20 | Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 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). |
AID624759 | Binding constant for PFCDPK1(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID760499 | Cytotoxicity against human KM12 cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID624812 | Binding constant for SBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424891 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1421415 | Inhibition of recombinant human c-SRC at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
AID624842 | Binding constant for BMX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1175325 | Inhibition of c-Src (unknown origin) at 100 uM | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3β (GSK-3β) with cellular activity of promoting glucose uptake. |
AID1449628 | Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12 | Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification. |
AID625116 | Binding constant for ADCK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435829 | Binding constant for RPS6KA1(Kin.Dom.2 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1695243 | Growth inhibition of human MEC-1 cells incubated for 72 hrs | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Understanding the mechanism of action of pyrrolo[3,2- |
AID435169 | Binding constant for full-length MEK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1286588 | Inhibition of BCR/ABL in human KU812 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID1224787 | Delta TM value showing the stabilisation of PIM2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID724676 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 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). |
AID624710 | Binding constant for SRMS kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1734724 | Antitumor activity against human MDA-MB-231 cells xenografted in SCID mouse assessed as tumor growth inhibition at 40 mg/kg, po qd for 21 days and measured every 3 days | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
AID435796 | Binding constant for ERBB2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624936 | Binding constant for FLT3(D835Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436049 | Binding constant for PTK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID507703 | Inhibition of EGFR T790M mutant at 10 mM | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID624791 | Binding constant for KIT(V559D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID282255 | Mean residence time in Sprague-Dawley rat at 10 mg/kg, iv | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID435323 | Binding constant for RET(M918T) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425136 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1224769 | Delta TM value showing the stabilisation of GSK3B produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID625047 | Binding constant for AMPK-alpha2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID443957 | Cytotoxicity against Philadelphia chromosome positive human ALL3 cells by Alamar Blue fluorescent assay | 2009 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24 | Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors. |
AID1424928 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435199 | Binding constant for TLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1373722 | Toxicity in Kunming mouse assessed as survival rat at 200 mg/kg, po dosed once for 2 weeks | 2018 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4 | Design and synthesis of novel dasatinib derivatives as inhibitors of leukemia stem cells. |
AID435201 | Binding constant for TRKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435319 | Binding constant for PKN1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID282244 | Inhibition of FAK | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1425086 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1224763 | Delta TM value showing the stabilisation of CLK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID507077 | Inhibition of DNA-PK 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. |
AID625087 | Binding constant for MELK 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. |
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. |
AID1573072 | Antiproliferative activity against human H460 cells | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID329200 | Inhibition of antigen-induced IL6 secretion in mouse mast cells at 1 uM after 24 hrs by ELISA | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID435800 | Binding constant for FYN kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID303306 | Inhibition of Src | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib. |
AID625016 | Binding constant for SRC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624850 | Binding constant for DDR1 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. |
AID745320 | Inhibition of EGFR (unknown origin) 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. |
AID435408 | Binding constant for INSR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624891 | Binding constant for JNK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1206304 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of colony formation at >0.01 uM after 12 days by crystal violet staining-based assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID1612821 | Inhibition of CSK (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
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. |
AID624918 | Binding constant for DYRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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). |
AID498534 | Half life in chronic myeloid leukemia patient | 2009 | Nature chemical biology, Mar, Volume: 5, Issue:3 | A pulse at the heart of targeted therapy. |
AID1515651 | Binding affinity to wild-type human partial length SRC (L240 to L536 residues) expressed in bacterial expression system by TR-FRET assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Controlling cellular distribution of drugs with permeability modifying moieties. |
AID624722 | Binding constant for MKK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435924 | Binding constant for MARK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1631451 | Antiviral activity against Dengue virus 2 NGC infected in human HuH7 cells assessed as reduction in viral titer after 24 hrs | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | The Medicinal Chemistry of Dengue Virus. |
AID1875895 | Antiviral activity against pseudo typed HCV infected in human Huh-7.5.1 cells assessed as inhibition of viral infection | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1375356 | Antitumor activity against human K562 cells overexpressing GFP-fussed full length mouse eIF4E xenografted in SCID mouse assessed as tumor growth inhibition at 2.5 mg/kg, po qd administered via gavage for 5 days on 2 days off per cycle for 2 cycles relativ | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 | Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia. |
AID435830 | Binding constant for RPS6KA2(Kin.Dom.2 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625108 | Binding constant for MKNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625082 | Binding constant for RSK4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID724664 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID271950 | Inhibition of Src in presence of ATP | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatin |
AID435290 | Binding constant for FGFR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1612818 | Inhibition of ABL1 (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID360789 | Inhibition of Dengue virus 2 assembly in african green monkey Vero cells assessed as virus-induced membrane structures at 2.5 uM after 4 days postinfection by electron microscopy | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID1283286 | Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | Structure-Activity Relationship Study of Rakicidins: Overcoming Chronic Myeloid Leukemia Resistance to Imatinib with 4-Methylester-Rakicidin A. |
AID1186991 | Cytotoxicity against human HepG2 cells assessed as cell viability at 1 uM after 4 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 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. |
AID624975 | Binding constant for PLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1286626 | Binding affinity to SRC (unknown origin) | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID1424890 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1310135 | Inhibition of SRC phosphorylation at tyrosine 416 in human MDA-MB-231 cells at 3 to 100 nM preincubated for 1.5 hrs followed by serum stimulation for 1 hr by Western blot analysis | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID1425098 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID375148 | Inhibition of cSrc in human PC3 cells assessed as reduction of phosphorylated FAK Y576/Y577 level at 100 nM after 5 hrs by immunoblot | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. |
AID624914 | Binding constant for WEE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624704 | Binding constant for NEK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435519 | Binding constant for AURKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID724649 | Inhibition of BCR-ABL T315I mutant-mediated CRK1 phosphorylation in mouse BA/F3 cells after 4 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID458665 | Inhibition of mouse GM-CSF-stimulated cell proliferation of growth factor dependent mouse FDC-P1 cells expressing human FMS after 48 hrs by resazurin dye reduction assay | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Colony stimulating factor-1 receptor as a target for small molecule inhibitors. |
AID1206283 | Induction of apoptosis in human MDA-MB-231 cells assessed as viable cells at 0.3 uM after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 95.5%) | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID624879 | Binding constant for PIK3CG kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425121 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1315389 | Cytotoxicity against human K562 cells assessed as reduction in cell viability after 96 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Part-1: Design, synthesis and biological evaluation of novel bromo-pyrimidine analogs as tyrosine kinase inhibitors. |
AID435556 | Binding constant for RAF1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624766 | Binding constant for p38-gamma kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1612819 | Inhibition of BRK (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID435193 | Binding constant for RPS6KA6(Kin.Dom.1 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435286 | Binding constant for EPHA7 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425105 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624862 | Binding constant for LYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435409 | Binding constant for full-length JNK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID624856 | Binding constant for GSK3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID282237 | Inhibition of Her2 kinase | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
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. |
AID1425127 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1224754 | Delta TM value showing the stabilisation of CAMK2G produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435940 | Binding constant for full-length TSSK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625077 | Binding constant for DAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID1473866 | Ratio of drug concentration at steady state in patient with chronic phase CML at 70 to 90 mg, po BID after 12 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. |
AID435805 | Binding constant for MAP4K5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1616413 | Growth inhibition of human K562 cells incubated for 2 days by CCK8 assay | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. |
AID624823 | Binding constant for MKNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425144 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1515654 | Binding affinity to wild-type human partial length DDR1 (R565 to V876 residues) expressed in bacterial expression system by TR-FRET assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Controlling cellular distribution of drugs with permeability modifying moieties. |
AID624786 | Binding constant for KIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624919 | Binding constant for AURKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1875892 | Antiviral activity against MERS-CoV infected in 1 hr pretreated African green monkey Vero E6 cells ssessed as inhibition of cytopathic effect incubated for 48 hrs by plate reader method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1886527 | Cytotoxicity against human iPSC-CM cells assessed as reduction in contractile alterations or amplitude in cell voltage by VF2.1.Cl dye based assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
AID1206216 | Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID435799 | Binding constant for FLT3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624727 | Binding constant for FYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424917 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1315388 | Cytotoxicity against human U937 cells assessed as reduction in cell viability after 96 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Part-1: Design, synthesis and biological evaluation of novel bromo-pyrimidine analogs as tyrosine kinase inhibitors. |
AID282246 | Inhibition of IR kinase | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
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. |
AID624965 | Binding constant for LZK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID360776 | Antiviral activity against Dengue virus 3 H87 infected in african green monkey Vero cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID1310171 | Antimigratory activity in Tg(brn3c:mGFP) zebrafish neuromasts at 1 to 10 uM treated for 20 to 48 hrs post fertilization measured at 72 hrs post fertilization by fluorescent microscopy | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID1246527 | Resistance index, ratio of IC50 for imatinib resistant human IR-K562 cells to IC50 for human K562 cells | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID282249 | Inhibition of PKCdelta | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID282239 | Inhibition of MEK | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID455986 | Permeability across human Caco-2 cells | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain. |
AID1612824 | Inhibition of Lyn B (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID624950 | Binding constant for DMPK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424999 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID436052 | Binding constant for full-length SNF1LK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425067 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1301849 | Hematotoxicity in human PHA/IL2-stimulated PBMC | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
AID1242619 | Inhibition of DDR1 (unknown origin) at 0.0015 uM after 1 hr by time resolved fluorescence method | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors. |
AID625037 | Binding constant for PIK3CA(C420R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1515659 | Binding affinity to wild-type human partial length RIPK2 (M1 to K310 residues) expressed in bacterial expression system by TR-FRET assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Controlling cellular distribution of drugs with permeability modifying moieties. |
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AID732826 | Antiproliferative activity against human T47D cells after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. |
AID1875939 | Antiviral activity against DENV infected in human Huh-7 cells assessed as inhibition of viral replication | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID282240 | Inhibition of VEGFR2 kinase | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1141140 | Binding affinity to wild type DDR2 (unknown origin) by FLiK assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Identification of type II and III DDR2 inhibitors. |
AID732831 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. |
AID458666 | Selectivity index, ratio of IC50 for mouse GM-CSF-stimulated proliferation of mouse FDC-P1 cells expressing human FMS to IC50 for human FMS-mediated mouse FDC-P1 cells proliferation in presence of human CSF1 | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Colony stimulating factor-1 receptor as a target for small molecule inhibitors. |
AID435936 | Binding constant for full-length SRPK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID732828 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. |
AID638917 | Inhibition of ErbB2 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
AID435443 | Binding constant for TXK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1141136 | Inhibition of wild type DDR2 (unknown origin) preincubated for 30 mins before substrate addition by FRET assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Identification of type II and III DDR2 inhibitors. |
AID435555 | Binding constant for PRKR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425178 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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AID735398 | Cytotoxicity against human PAXF 1657L cells after 4 days by propidium iodide staining | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography. |
AID1654861 | Antiviral activity against HCV genotype 2a pseudoparticle infected in human Huh7.5 cells assessed as reduction in viral replication at 2 to 4 uM | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | 2-((4-Arylpiperazin-1-yl)methyl)benzonitrile Derivatives as Orally Available Inhibitors of Hepatitis C Virus with a Novel Mechanism of Action. |
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. |
AID435896 | Binding constant for AAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1424965 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID724975 | Inhibition of human recombinant ABL1 M351T mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID1424967 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1286563 | Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
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AID624721 | Binding constant for MEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436022 | Binding constant for full-length MEK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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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. |
AID435662 | Binding constant for MST2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID360787 | Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID1205944 | Binding affinity to human GAK fused to T7 bacteriophage expressed in Escherichia coli BL21 after 1 hr by qPCR analysis | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8 | Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents. |
AID435528 | Binding constant for IRAK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624889 | Binding constant for JNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID1764400 | Unbound brain concentration in P-gp knock out Sprague-Dawley rat at 5 mg/ml/kg, po measured upto 4 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
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. |
AID624764 | Binding constant for CLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1256162 | Cytotoxicity against human K562 cells expressing Bcr-Abl assessed as growth inhibition after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Expanding the structural diversity of Bcr-Abl inhibitors: Dibenzoylpiperazin incorporated with 1H-indazol-3-amine. |
AID436032 | Binding constant for MYO3B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID360788 | Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID435516 | Binding constant for ADCK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224786 | Delta TM value showing the stabilisation of PIM1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1875893 | Antiviral activity against SARS-CoV infected in 2 hrs pretreated African green monkey Vero E6 cells assessed as inhibition of cytopathic effect incubated for 48 hrs by celltitre-glo luminescent assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID435148 | Binding constant for AMPK-alpha1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1424908 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435932 | Binding constant for PKAC-alpha kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625072 | Binding constant for TBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID282234 | Inhibition of PDGFRbeta | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1450946 | Binding affinity to recombinant human N-terminal His6-tagged Wee2 kinase domain (202 to 492 residues) expressed in Escherichia coli BL21 (DE3) by isothermal titration calorimetry | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors. |
AID624990 | Binding constant for ABL1(Y253F)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1893833 | Oral bioavailability in rat relative to control | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-Aminothiazole: A privileged scaffold for the discovery of anti-cancer agents. |
AID435328 | Binding constant for YES kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625112 | Binding constant for YANK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435933 | Binding constant for PKN2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1424919 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1373713 | Inhibition of human BCR/ABL V299L mutant | 2018 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4 | Design and synthesis of novel dasatinib derivatives as inhibitors of leukemia stem cells. |
AID1424951 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1573061 | Antiproliferative activity against human K562 cells | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID624706 | Binding constant for MLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID1301834 | Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
AID638921 | Inhibition of c-Met at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
AID1695244 | Growth inhibition of human PCL12 cells incubated for 72 hrs | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Understanding the mechanism of action of pyrrolo[3,2- |
AID1207551 | Inhibition of long-lasting type calcium current (hICa) in Chinese Hamster Ovary (CHO) cells expressing hCav1.2 measured using IonWorks Quattro automated patch clamp platform | |||
AID624934 | Binding constant for FLT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624960 | Binding constant for RSK2(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507424 | Inhibition of recombinant PDGFR 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. |
AID1425204 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1310146 | Cardiotoxicity in wild-type zebrafish embryos at >10 uM treated for 4 hrs measured after 48 hrs by fluorescent microscopy | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID625001 | Binding constant for EGFR(L747-S752del, P753S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1141137 | Inhibition of DDR2 T654M mutant (unknown origin) preincubated for 30 mins before substrate addition by FRET assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Identification of type II and III DDR2 inhibitors. |
AID282253 | AUC (total) in Sprague-Dawley rat at 10 mg/kg, iv | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1424904 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1286555 | Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID436048 | Binding constant for full-length PTK2B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625054 | Binding constant for MST2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1246525 | Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for human THP1 cells | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID435524 | Binding constant for full-length CSNK1D | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1772712 | Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation. |
AID507079 | Inhibition of recombinant c-Abl 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. |
AID625056 | Binding constant for TESK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435514 | Binding constant for ABL1(M351T) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1876062 | Inhibition of c-Abl (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID745323 | Cytotoxicity against human K562 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. |
AID625011 | Binding constant for FGR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424959 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1224768 | Delta TM value showing the stabilisation of DMPK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID375143 | Activity of human N-terminal His-tagged p38alpha expressed in Escherichia coli BL21 (DE3) | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. |
AID624884 | Binding constant for PRKD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625015 | Binding constant for ROCK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435795 | Binding constant for EPHA4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1283290 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | Structure-Activity Relationship Study of Rakicidins: Overcoming Chronic Myeloid Leukemia Resistance to Imatinib with 4-Methylester-Rakicidin A. |
AID303308 | Growth inhibition of human M07ep210 cells after 48 hrs by [3H]thymidine uptake assay | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib. |
AID625086 | Binding constant for SLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID1189756 | Induction of apoptosis in human SH-SY5Y cells assessed as accumulation of hypodiploid cells at 0.1 uM after 24 hrs by propidium iodide staining-based cytofluorimetry | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | Combining X-ray crystallography and molecular modeling toward the optimization of pyrazolo[3,4-d]pyrimidines as potent c-Src inhibitors active in vivo against neuroblastoma. |
AID435659 | Binding constant for full-length MARK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1386087 | Inhibition of BCR-ABL1 E255K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
AID435675 | Binding constant for KIT(V559D,T670I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625000 | Binding constant for EGFR(L747-E749del, A750P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID625021 | Binding constant for LIMK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435192 | Binding constant for ROS1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID1206301 | Inhibition of ERK phosphorylation in human MDA-MB-231 cells at 0.001 to 1 uM after 20 hrs by Western blot analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID1425133 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1573086 | Antiproliferative activity against human SK-N-FI cells | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID1176842 | Inhibition of c-SRC (unknown origin) at 1 uM by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization. |
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AID1186123 | Antiproliferative activity against human RXF 393NL cells after 4 days by modified propidium iodide assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Pyrrolo[3,2-b]quinoxaline derivatives as types I1/2 and II Eph tyrosine kinase inhibitors: structure-based design, synthesis, and in vivo validation. |
AID724648 | Inhibition of BCR-ABL T315I mutant-mediated STAT5 phosphorylation in mouse BA/F3 cells after 4 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID760498 | Cytotoxicity against human U251 cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID709935 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
AID1425029 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424912 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624999 | Binding constant for EGFR(G719S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID463630 | Inhibition of wild type Bcr-Abl | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4 | Selectively nonselective kinase inhibition: striking the right balance. |
AID624825 | Binding constant for BMPR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624713 | Binding constant for ERK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID761478 | Inhibition of Yes1 (unknown origin) assessed as kinase-dependent enzymatic production of ADP from ATP using coupled luminescence-based reaction by ADP-Glo kinase assay | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Identification of potent Yes1 kinase inhibitors using a library screening approach. |
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. |
AID282263 | Oral bioavailability in Sprague-Dawley rat at 10 mg/kg, po | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID724672 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID624874 | Binding constant for PCTK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625036 | Binding constant for PIK3CA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435289 | Binding constant for ERK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID507076 | Inhibition of recombinant mTOR 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. |
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. |
AID625067 | Binding constant for NDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1616471 | Protac activity against VHL/BCR-ABL in human K562 cells assessed as reduction in BCR-ABL phosphorylation at 20 times IC50 incubated for 12 hrs followed by drug wash-out and incubation in drug-free medium up to 72 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. |
AID435663 | Binding constant for full-length MST4 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625126 | Binding constant for TAOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1286559 | Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID435166 | Binding constant for full-length JNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative 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. |
AID435292 | Binding constant for ITK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1186128 | Antiproliferative activity against human PRXF DU145 cells after 4 days by modified propidium iodide assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Pyrrolo[3,2-b]quinoxaline derivatives as types I1/2 and II Eph tyrosine kinase inhibitors: structure-based design, synthesis, and in vivo validation. |
AID732855 | Inhibition of c-KIT (unknown origin) using Ser/Thr 6 peptide as substrate incubated for 1 hr prior to substrate addition measured after 2 hrs by FRET assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. |
AID1425173 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625131 | Binding constant for FGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624896 | Binding constant for PRKR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1286554 | Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID624796 | Binding constant for MET(Y1235D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624742 | Binding constant for NEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1242637 | Antiproliferative activity against human NCI-H2286 cells expressing DDR2 mutant after 72 hrs by alamar blue assay | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors. |
AID435910 | Binding constant for MAP4K4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID436015 | Binding constant for EPHA6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1310130 | Inhibition of human RET using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID638919 | Inhibition of EPH-A2 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
AID625119 | Binding constant for CAMK1G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625041 | Binding constant for PIK3CA(H1047L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1186993 | Cytotoxicity against human HepG2 cells assessed as cell viability at 100 uM after 4 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
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. |
AID1246521 | Cytotoxicity against human U937 cells assessed as reduction in cell viability | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID624758 | Binding constant for RIPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID627131 | Inhibition of Aurora A using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
AID1612811 | Inhibition of BRK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID435647 | Binding constant for CAMK2D kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425114 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425157 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435157 | Binding constant for EGFR(G719C) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1386086 | Inhibition of BCR-ABL1 Y253H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
AID624991 | Binding constant for ABL1-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID638924 | Inhibition of FGFR1 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
AID624831 | Binding constant for CHEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425052 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID705593 | Time dependent inhibition of CYP3A4 in human liver microsomes | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. |
AID1612903 | Inhibition of DDR2 (unknown origin) using poly (Glu, Tyr) 4:1 substrate after 60 mins by ELISA | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
AID435941 | Binding constant for ZAK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1310149 | Solubility of the compound in water at pH 2.6 | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID360770 | Inhibition of EPHA2 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID599957 | Binding affinity to human KIT incubated for 1 hr by kinase binding assay | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. |
AID1875894 | Antiviral activity against pseudo typed HCV infected in human Huh-7.5.1 cells assessed as prevention of pseudo particle entry | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1425211 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1616469 | Induction of cell death in human K562 cells assessed as reduction in cell viability at 20 times IC50 incubated for 12 hrs followed by drug wash-out and incubation in drug-free medium up to 144 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. |
AID625022 | Binding constant for MUSK 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. |
AID1224783 | Delta TM value showing the stabilisation of PAK6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1373714 | Growth inhibition of human K562 cells | 2018 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4 | Design and synthesis of novel dasatinib derivatives as inhibitors of leukemia stem cells. |
AID1425213 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID1425149 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID638915 | Inhibition of RET at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
AID625093 | Binding constant for TNIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625059 | Binding constant for YSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425141 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624822 | Binding constant for CDKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID732856 | Inhibition of BCR/ABL (unknown origin) using tyrosine 2 peptide as substrate incubated for 1 hr prior to substrate addition measured after 2 hrs by FRET assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) 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. |
AID625045 | Binding constant for PIK3CA(Q546K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1186125 | Antiproliferative activity against human LXFA 983L cells after 4 days by modified propidium iodide assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Pyrrolo[3,2-b]quinoxaline derivatives as types I1/2 and II Eph tyrosine kinase inhibitors: structure-based design, synthesis, and in vivo validation. |
AID498730 | Binding affinity to p38alpha | 2009 | Nature chemical biology, Jun, Volume: 5, Issue:6 | A new screening assay for allosteric inhibitors of cSrc. |
AID375142 | Activity of wild type chicken c N-terminal His-tagged Src expressed in Escherichia coli BL21 (DE3) | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. |
AID624941 | Binding constant for CDKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624747 | Binding constant for SgK110 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1771926 | Binding affinity to non-phosphorylated ABL1 (unknown origin) assessed as change in melting temperature by SYPRO orange dye based DSF assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Design and Development of a Chemical Probe for Pseudokinase Ca |
AID435277 | Binding constant for full-length CDK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435776 | Binding constant for ABL1(Y253F) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435782 | Binding constant for BRSK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1310133 | Selectivity ratio of IC50 for human ABL to IC50 for C-terminal His-tagged full length human SRC expressed in insect cells | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID360780 | Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID435312 | Binding constant for MET kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224752 | Delta TM value showing the stabilisation of CAMK2B produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435150 | Binding constant for ARK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224774 | Delta TM value showing the stabilisation of p38beta produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID625104 | Binding constant for MYO3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425200 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1876249 | Antiviral activity against HIV-1 in U87/CD4/CCR5 cells expressing HIV-1-envelope-protein assessed as decreased cell-cell fusion at 300 nM | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID435688 | Binding constant for full-length PCTK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625136 | Binding constant for YSK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID724666 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID1310137 | Increase in total SRC in human MDA-MB-231 cells preincubated for 1.5 hrs followed by serum stimulation for 1 hr by Western blot analysis | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID621337 | Inhibition of LCK | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors. |
AID624814 | Binding constant for DCAMKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1857470 | Inhibition of recombinant LIMK1 (330 to 637 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 105 mins by RapidFire Mass Spectrometry kinase assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20 | Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
AID507689 | Inhibition of EGFR | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID271946 | Inhibition of human Lck in presence of ATP | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatin |
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AID435533 | Binding constant for NEK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435191 | Binding constant for full-length RIOK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1573073 | Antiproliferative activity against human NCI-H226 cells | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID435171 | Binding constant for NEK9 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624940 | Binding constant for FLT3(R834Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624795 | Binding constant for MET(M1250T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1612814 | Inhibition of Fyn A (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID435645 | Binding constant for ACVRL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1817045 | Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | |||
AID624921 | Binding constant for MAP4K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425037 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID360784 | Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID435310 | Binding constant for FLT3(ITD) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435546 | Binding constant for PRKG1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425016 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507430 | Inhibition of AXL at 10 mM | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID621336 | Inhibition of AurB | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors. |
AID1573075 | Antiproliferative activity against human SW620 cells | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID624962 | Binding constant for ASK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507702 | Inhibition of IRAK4 at 10 mM | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID1876230 | Antiviral activity against DENV infected in 180 mins pretreated human C6/36 cells incubated for 1 to 72 hrs | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID435181 | Binding constant for full-length p38-alpha | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425137 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625070 | Binding constant for PFTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1695218 | Growth inhibition of human SU-DHL-2 cells incubated for 72 hrs | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Understanding the mechanism of action of pyrrolo[3,2- |
AID625019 | Binding constant for AKT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID724668 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID624735 | Binding constant for ANKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1757412 | Inhibition of ABL (unknown origin) at 1 uM by ELISA | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors. |
AID624707 | Binding constant for DCAMKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID435832 | Binding constant for SLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435438 | Binding constant for full-length p38-gamma | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1207517 | Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay | |||
AID624715 | Binding constant for ERK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624880 | Binding constant for PIK4CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID435808 | Binding constant for full-length MEK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625110 | Binding constant for TRPM6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1286625 | Binding affinity to P38-alpha (unknown origin) | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID1425115 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624857 | Binding constant for HCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425083 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1612810 | Inhibition of ABL1 (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID435395 | Binding constant for CDC2L1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624974 | Binding constant for PIK3CD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID739095 | Inhibition of Bcr-Abl T315I mutant (unknown origin) phosphorylation transfected in mouse Ba/F3 cells after 1 hr by Western blot analysis | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant. |
AID625030 | Binding constant for LOK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435440 | Binding constant for PIM2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID724981 | Inhibition of human recombinant wild type ABL1 expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID435826 | Binding constant for full-length PCTK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1310172 | Cardiotoxicity in wild-type zebrafish embryos assessed as heart enlargement at 1 to 10 uM treated for 4 hrs measured after 48 hrs by fluorescent microscopy | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID624804 | Binding constant for ERBB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID638913 | Inhibition of PDGFRalpha at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
AID625052 | Binding constant for PRKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1202713 | Inhibition of DDR2 (unknown origin) assessed as reduction in collagen-induced DDR2 activation | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8 | Small molecule discoidin domain receptor kinase inhibitors and potential medical applications. |
AID625134 | Binding constant for PIP5K2C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID625078 | Binding constant for SRPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435792 | Binding constant for EGFR(S752-I759del) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1876063 | Antiviral activity against MERS-CoV | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1425023 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 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). |
AID282261 | Mean residence time in Sprague-Dawley rat at 10 mg/kg, po | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID436044 | Binding constant for PLK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID458668 | Inhibition of CSF1-stimulated human FMS autophosphorylation expressed in growth factor dependent mouse FDC-P1 cells assessed as phosphorylated receptor level at 2.5 nM relative to control by Western blot | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Colony stimulating factor-1 receptor as a target for small molecule inhibitors. |
AID624935 | Binding constant for FLT3(D835H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID282256 | Volume of distribution in Sprague-Dawley rat at 10 mg/kg, iv | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID624964 | Binding constant for DYRK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625035 | Binding constant for PHKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID732857 | Inhibition of DDR2 (unknown origin) using fluorescein-labeled poly GAT as substrate incubated for 1 hr prior to substrate addition measured after 1 hr by TR-FRET assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. |
AID329199 | Inhibition of LPS-induced TNFalpha release in human U937 cells at 2 uM after 1 hr by ELISA | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID1224793 | Delta TM value showing the stabilisation of RSK2a produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID724678 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID435160 | Binding constant for FER kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID435525 | Binding constant for EGFR(L858R) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1876284 | Inhibition of LCK (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID1206299 | Inhibition of Src in human MDA-MB-231 cells assessed as reduction of FAK phosphorylation at >0.03 uM after 20 hrs by Western blot analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID360777 | Antiviral activity against Dengue virus 4 H241 infected in african green monkey Vero cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID1774079 | Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 10 uM incubated for 1 week by absorbance method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID624723 | Binding constant for CSNK1A1L kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624933 | Binding constant for PLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID1206215 | Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID435523 | Binding constant for CIT kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1757413 | Inhibition of EphA2 (unknown origin) at 1 uM by ELISA | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors. |
AID1286571 | Antiproliferative activity against human CHL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID1424925 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435901 | Binding constant for BRAF kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID329186 | Inhibition of recombinant Tec kinase | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID1053270 | Inhibition of ACE (unknown origin) assessed as 3-Hydroxybutyril-glycil-glycil-glycine conversion to 3-hydroxybutyric acid after 60 mins by WST assay | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching. |
AID1425195 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1734835 | Inhibition of Src in human MDA-MB-231 cells assessed as inhibition of FAK phosphorylation at 0.03 to 0.3 uM incubated for 20 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
AID624954 | Binding constant for EPHB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1854085 | Inhibition of BCR-ABL phosphorylation in human K562 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | The progress of small-molecules and degraders against BCR-ABL for the treatment of CML. |
AID435515 | Binding constant for ABL1(Q252H) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435551 | Binding constant for full-length p38-beta | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1424948 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1224801 | Delta TM value showing the stabilisation of MST1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1386091 | Inhibition of BCR-ABL1 E459K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
AID624811 | Binding constant for PAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625092 | Binding constant for NDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435666 | Binding constant for full-length NEK7 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624860 | Binding constant for VEGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID435400 | Binding constant for DDR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID329194 | Inhibition of LPS-induced Btk autophosphorylation of tyrosine in human Namalwa cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID435794 | Binding constant for EPHA3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1734824 | Induction of apoptosis in human MDA-MB-231 cells assessed as live cells at 0.1 uM incubated for 24 hrs by annexin V-FITC and propidium iodide staining based flow cytometry analysis (Rvb = 96.95 %) | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
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. |
AID435788 | Binding constant for CLK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624952 | Binding constant for EPHA4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624782 | Binding constant for FGFR3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID463629 | Inhibition of Lck | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4 | Selectively nonselective kinase inhibition: striking the right balance. |
AID436024 | Binding constant for MRCKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1473863 | AUC in patient with advanced phase CML and Ph+ ALL at 100 mg, po BID after 12 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. |
AID271972 | Inhibition of Her2 | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatin |
AID621334 | Inhibition of BRK pretreated for 30 mins by microplate reader | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors. |
AID1515645 | Permeability of compound in 5% DMSO after 7 hrs by PAMPA | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Controlling cellular distribution of drugs with permeability modifying moieties. |
AID624997 | Binding constant for EGFR(E746-A750del) 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. |
AID624772 | Binding constant for AURKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424952 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625033 | Binding constant for PCTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625027 | Binding constant for MAP3K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436051 | Binding constant for RPS6KA5(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625061 | Binding constant for MAP4K5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1207335 | Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform | |||
AID1310150 | Solubility of the compound in water at pH 7 | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID1573066 | Inhibition of wild type BCR/ABL (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell growth | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID435790 | Binding constant for DRAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624871 | Binding constant for PAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224802 | Delta TM value showing the stabilisation of TNIK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1424991 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435786 | Binding constant for full-length CLK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624929 | Binding constant for BRSK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425111 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435834 | Binding constant for YANK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435441 | Binding constant for RPS6KA4(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1424892 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424889 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1734863 | Inhibition of ERK phosphorylation in human MDA-MB-231 cells at 0.03 to 0.3 uM incubated for 20 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
AID709938 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
AID1516991 | Inhibition of recombinant Nanoluc-tagged p38alpha (unknown origin) expressed in HEK293 cells incubated for 2 to 3 mins by NanoBRET assay | |||
AID625085 | Binding constant for ULK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1256160 | Inhibition of wild type Bcr-Abl (unknown origin) by ADP-Glo assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Expanding the structural diversity of Bcr-Abl inhibitors: Dibenzoylpiperazin incorporated with 1H-indazol-3-amine. |
AID1425024 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624854 | Binding constant for FLT4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1886524 | Growth inhibition of human K562 cells expressing BCR-ABL T315I mutant measured after 48 hrs by alamarblue assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
AID435650 | Binding constant for full-length CSNK1E | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625289 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease | 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). |
AID282260 | Half life in Sprague-Dawley rat at 10 mg/kg, po | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID282221 | Antiproliferative activity against human K562 cells after 72 hrs | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID624841 | Binding constant for BLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625013 | Binding constant for LCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625120 | Binding constant for EPHA8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625076 | Binding constant for PLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435777 | Binding constant for ABL2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID507688 | Inhibition of cRAF | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID1224794 | Delta TM value showing the stabilisation of RSK2b produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1734823 | Induction of apoptosis in human MDA-MB-231 cells assessed as late apoptotic cells at 0.1 uM incubated for 24 hrs by annexin V-FITC and propidium iodide staining based flow cytometry analysis (Rvb = 0.85 %) | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
AID625122 | Binding constant for RET(M918T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435182 | Binding constant for full-length PKAC-beta | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624734 | Binding constant for YANK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1857471 | Inhibition of recombinant LIMK2 (347 to 659 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 180 mins by RapidFire Mass Spectrometry kinase assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20 | Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
AID435158 | Binding constant for EPHA5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative 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. |
AID435552 | Binding constant for PIK3CA(E545K) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID709991 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
AID1424997 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID282254 | Half life in Sprague-Dawley rat at 10 mg/kg, iv | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1425097 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID724978 | Inhibition of human recombinant ABL1 Q252H mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID1224760 | Delta TM value showing the stabilisation of CHEK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID724674 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID624903 | Binding constant for SRPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1893831 | Binding affinity to Abl (unknown origin) assessed as inhibition constant | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-Aminothiazole: A privileged scaffold for the discovery of anti-cancer agents. |
AID638911 | Inhibition of KDR at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
AID435168 | Binding constant for LTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1424893 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624711 | Binding constant for STK35 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID329197 | Decrease in LPS-induced TNFalpha release in human U937 cells after 1 hr by ELISA | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
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. |
AID1386090 | Inhibition of BCR-ABL1 F359V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
AID1425109 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID760495 | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1857472 | Inhibition of PAK mediated recombinant LIMK1 phosphorylation (330 to 637 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 105 mins by RapidFire Mass Spectrometry kinase assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20 | Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
AID1315391 | Inhibition of BRC/ABL1 (unknown origin) after 40 mins by ADP-Glo assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Part-1: Design, synthesis and biological evaluation of novel bromo-pyrimidine analogs as tyrosine kinase inhibitors. |
AID1310125 | Inhibition of human ABL using EAIYAAPFAKKK as substrate in presence of [gamma-33P]ATP | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
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. |
AID1515652 | Binding affinity to wild-type human full length BTK (M1 to S659 residues) expressed in mammalian expression system by TR-FRET assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Controlling cellular distribution of drugs with permeability modifying moieties. |
AID1242638 | Antiproliferative activity against human HCC366 cells expressing DDR2 mutant after 72 hrs by alamar blue assay | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors. |
AID436047 | Binding constant for full-length PRKX | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1421419 | Inhibition of recombinant human IGF1R at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
AID624789 | Binding constant for KIT(D816V) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1315390 | Cytotoxicity against human L02 cells assessed as reduction in cell viability after 96 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Part-1: Design, synthesis and biological evaluation of novel bromo-pyrimidine analogs as tyrosine kinase inhibitors. |
AID1206291 | Induction of apoptosis in human MDA-MB-231 cells assessed as late apoptotic cells at 0.3 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 4.25%) | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID435828 | Binding constant for full-length PIP5K2B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1573084 | Antiproliferative activity against human SW1088 cells | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID282247 | Inhibition of MK2 | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1425140 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1814382 | Inhibition of c-SRC (unknown origin) at 100 uM incubated for 60 mins by ELISA relative to control | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia. |
AID435908 | Binding constant for EPHA2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425188 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1612820 | Inhibition of BTK (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID282258 | Tmax in in Sprague-Dawley rat at 10 mg/kg, po | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID360783 | Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID1425051 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID1310147 | Toxicity in wild-type zebrafish embryos assessed as mortality at >10 uM treated for 4 hrs measured after 48 hrs by fluorescent microscopy | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID624909 | Binding constant for TGFBR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436008 | Binding constant for full-length BTK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624818 | Binding constant for ULK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435827 | Binding constant for PDGFRA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625014 | Binding constant for PRKCE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID1734726 | Toxicity in SCID mouse xenografted with MDA-MB-231 cells assessed as change in body weight at 40 mg/kg, po qd for 21 days and measured every 3 days | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
AID1774077 | Binding affinity to TTR V3OM mutant (unknown origin) expressed in Escherichia coli incubated for 60 mins by tryptophan intrinsic fluorescence method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1425038 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID271945 | Inhibition of murine Lck in presence of ATP | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatin |
AID1425019 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID761477 | Inhibition of Yes1 (unknown origin) by [gamma-33P]-ATP radiolabeled enzyme activity assay | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Identification of potent Yes1 kinase inhibitors using a library screening approach. |
AID1425080 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1202712 | Inhibition of DDR1b (unknown origin) assessed as reduction in collagen-induced DDR1b activation | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8 | Small molecule discoidin domain receptor kinase inhibitors and potential medical applications. |
AID436054 | Binding constant for TLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624956 | Binding constant for EPHB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID1246524 | Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for imatinib resistant human IR-K562 cells | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID1425081 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624790 | Binding constant for KIT(L576P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224803 | Delta TM value showing the stabilisation of PBK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID282225 | AUC (0-4 hrs) in BALB/c mouse at 50 mg/kg, po after 4 hrs | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID435413 | Binding constant for MLCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1450954 | Binding affinity to recombinant human N-terminal His6-tagged Wee2 kinase domain (202 to 492 residues) expressed in Escherichia coli BL21 (DE3) assessed as change in melting temperature at 50 uM by differential scanning fluorimetry | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors. |
AID435531 | Binding constant for MKNK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1301836 | Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
AID282264 | Antitumor activity against human K562 xenograft in nude mouse at 5 mg/kg, po for 10 days in 5 day on and 2 day off schedule | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID624895 | Binding constant for MEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425194 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425162 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425069 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624917 | Binding constant for MST3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID724673 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID1425181 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1409082 | Inhibition of human EPHA2 at 100 uM | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
AID1425000 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624776 | Binding constant for PCTK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1506674 | Binding affinity to SRC (unknown origin) assessed as on rate constant | |||
AID1425007 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624902 | Binding constant for MEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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AID435161 | Binding constant for FES kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1424921 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1515657 | Binding affinity to PDGFRalpha V561D mutant (unknown origin) by TR-FRET assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Controlling cellular distribution of drugs with permeability modifying moieties. |
AID435905 | Binding constant for full-length CSNK1G3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1310128 | Inhibition of human mTOR using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID625139 | Binding constant for SNARK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1286551 | Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
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AID1695219 | Growth inhibition of human MAVER-1 cells incubated for 72 hrs | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Understanding the mechanism of action of pyrrolo[3,2- |
AID458669 | Inhibition of CSF1-stimulated human FMS autophosphorylation expressed in growth factor dependent mouse FDC-P1 cells assessed as phosphorylated receptor level at 0.25 nM relative to control by Western blot | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Colony stimulating factor-1 receptor as a target for small molecule inhibitors. |
AID724976 | Inhibition of human recombinant ABL1 H396P mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID329196 | Decrease in basal TNFalpha release in human U937 cells after 1 hr by ELISA | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID303307 | Growth inhibition of human K562 cells after 48 hrs by [3H]thymidine uptake assay | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib. |
AID624992 | Binding constant for ABL1-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1573062 | Antiproliferative activity against human K562R cells | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID1206214 | Inhibition of human Src | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID1473868 | Ratio of drug concentration at steady state patient with chronic phase CML at 70 to 90 mg, po BID after 12 hrs to IC50 for human MRP4 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. |
AID624809 | Binding constant for MYLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624849 | Binding constant for CSNK2A2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625007 | Binding constant for EGFR(T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID760491 | Cytotoxicity against human SW620 cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID435429 | Binding constant for FLT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624756 | Binding constant for MAP4K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224750 | Delta TM value showing the stabilisation of CAMK1G produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1425156 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625133 | Binding constant for CDC2L2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID282243 | Inhibition of AKT | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID375138 | Inhibition of wild type chicken N-terminal His-tagged cSrc expressed in Escherichia coli BL21 (DE3) | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. |
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. |
AID1425119 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID271951 | Inhibition of Bcr-Abl in presence of ATP | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatin |
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. |
AID625066 | Binding constant for IRAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507695 | Inhibition of PDGFRa | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID709996 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
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. |
AID375191 | Inhibition of cSrc in human DU145 cells assessed as effect on total FAK level at 100 nM after 5 hrs by immunoblot | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. |
AID709993 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
AID507696 | Inhibition of RIPK2 | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID624978 | Binding constant for ABL1(E255K)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435564 | Binding constant for TRKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435320 | Binding constant for PRKCE kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1424940 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424923 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1659069 | Antiproliferative activity against human K562 cells incubated for 3 days by CCK8 assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects. |
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. |
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. |
AID625048 | Binding constant for PRKCD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID732830 | Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. |
AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 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). |
AID1734865 | Inhibition of Fra1 expression in human MDA-MB-231 cells at 0.03 to 0.3 uM incubated for 20 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
AID625138 | Binding constant for STK33 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624865 | Binding constant for MAP3K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID329203 | Inhibition of antigen-induced histamine release in Tec-deficient BMMC at 1 uM after 30 mins | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID1206302 | Effect on AKT phosphorylation in human MDA-MB-231 cells at 0.001 to 1 uM after 20 hrs by Western blot analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID1424954 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435291 | Binding constant for FGFR3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624922 | Binding constant for CAMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435146 | Binding constant for ABL1(H396P) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425185 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425068 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID463632 | Inhibition of Bcr-Abl T315I mutant | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4 | Selectively nonselective kinase inhibition: striking the right balance. |
AID625064 | Binding constant for PIM2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID360771 | Inhibition of p38 MAPK | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID1424894 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID458667 | Inhibition of CSF1-stimulated human FMS autophosphorylation expressed in growth factor dependent mouse FDC-P1 cells assessed as phosphorylated receptor level at 25 nM relative to control by Western blot | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Colony stimulating factor-1 receptor as a target for small molecule inhibitors. |
AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
AID624906 | Binding constant for S6K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive 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. |
AID507082 | Inhibition of recombinant c-Src T338I mutant 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. |
AID1425012 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1612817 | Inhibition of SRC (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID1424955 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624859 | Binding constant for JAK1(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1650167 | Inhibition of ABL1 in human HEK293T cells assessed as reduction in cell viability at 1 uM measured after 48 hrs relative to control | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Generation of highly potent DYRK1A-dependent inducers of human β-Cell replication via Multi-Dimensional compound optimization. |
AID1424909 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1573068 | Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell growth | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID624910 | Binding constant for TTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624835 | Binding constant for ERN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624725 | Binding constant for NEK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435693 | Binding constant for TGFBR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1386088 | Inhibition of BCR-ABL1 E255V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
AID1613018 | Antiproliferative activity against human NCI-H2286 cells harboring DDR2 mutation after 72 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
AID624851 | Binding constant for ERBB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435197 | Binding constant for TEC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435691 | Binding constant for SgK085 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624775 | Binding constant for STK16 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624785 | Binding constant for JAK3(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624840 | Binding constant for AXL kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID724979 | Inhibition of human recombinant ABL1 E255K mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID1425036 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1224790 | Delta TM value showing the stabilisation of PLK4 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID498727 | Inhibition of wild type cSrc | 2009 | Nature chemical biology, Jun, Volume: 5, Issue:6 | A new screening assay for allosteric inhibitors of cSrc. |
AID625032 | Binding constant for TRKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1205870 | Antiangiogenic activity in chicken embryo chorioallantoic membrane model assessed as inhibition of vasculature formation at 20 uM, iv dosed for 3 consecutive days by FITC-dextran fluorescence angiography | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Improved angiostatic activity of dasatinib by modulation with hydrophobic chains. |
AID1425095 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625024 | Binding constant for PRKD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID724667 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
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. |
AID1515662 | Antiproliferative activity against human K562 cells assessed as reduction in cell viability by measuring ATP level incubated for 3 days by Celltiter-Glo assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Controlling cellular distribution of drugs with permeability modifying moieties. |
AID624939 | Binding constant for FLT3(N841I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435823 | Binding constant for full-length PAK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624968 | Binding constant for DRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425049 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435200 | Binding constant for full-length TNNI3K | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1396667 | Inhibition of N-[3',6'-dihydroxy-3-oxo-3H-spiro(2-benzofuran-1,9'-xanthen)-5-yl]-N'-[2-(4-{4-[N-(2-chloro-6-methylphenyl)-5-carboxamido]-thiazol-2-yl})-amino-2-methyl-pyrimid-6-yl)piperazinyl]-ethyl]thiourea binding to human PKMYT1 kinase doamin expressed | |||
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. |
AID435396 | Binding constant for CHEK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624821 | Binding constant for YANK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435897 | Binding constant for ABL1(T315I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1454437 | Displacement of CAT-1 from catalytic site of N-terminal His6-tagged ABL (83 to 534 residues) (unknown origin) expressed in Escherichia coli co-expressing Protein Tyrosine Phosphatase 1b at 25 uM by 19F NMR spectroscopy based dual-site competition assay | 2017 | ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6 | |
AID435287 | Binding constant for EPHA8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1876260 | Inhibition of Abl (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID435658 | Binding constant for JAK2(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1260957 | Inhibition of recombinant EphA2 kinase domain (unknown origin) at 1 uM after 30 mins by ELISA | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Δ(5)-Cholenoyl-amino acids as selective and orally available antagonists of the Eph-ephrin system. |
AID1425018 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID282224 | Antiproliferative activity against human WiDr cells after 72 hrs | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1424941 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID360774 | Antiviral activity against Dengue virus 2 infected in african green monkey Vero cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID507694 | Inhibition of LIMK1 | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID624983 | Binding constant for ABL1(H396P)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425032 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507083 | Inhibition of recombinant VEGFR2 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. |
AID1857475 | Inhibition of recombinant LIMK2(unknown origin) expressed in HEK293 cells using NanoGlo substrate incubated for 2 hrs followed by substrate addition by NanoBRET assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20 | Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
AID624937 | Binding constant for FLT3(ITD) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425120 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624800 | Binding constant for IGF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424900 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435404 | Binding constant for EPHB4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624719 | Binding constant for GRK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1612813 | Inhibition of CSK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID624870 | Binding constant for NEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624793 | Binding constant for KIT(V559D,V654A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1286564 | Inhibition of BCR/ABL p210-T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID1473862 | AUC in patient with chronic phase CML at 70 to 90 mg, po BID after 12 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. |
AID1206290 | Induction of apoptosis in human MDA-MB-231 cells assessed as early apoptotic cells at 0.3 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 1.05%) | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID1424920 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624947 | Binding constant for BRAF(V600E) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425045 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624798 | Binding constant for LKB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435403 | Binding constant for EPHB1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID360779 | Antiviral activity against Poliovirus 1 infected in african green monkey Vero cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID1206296 | Antimigratory activity against human MDA-MB-231 cells at 0.03 to 0.3 uM after 20 hrs by wound healing assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID1425035 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1205873 | Angiostatic activity in human ECRF24 cells assessed as inhibition of cell migration at 50 uM after 7 hrs by laser scanner cytometry based wound closure assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Improved angiostatic activity of dasatinib by modulation with hydrophobic chains. |
AID435195 | Binding constant for SRC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1301835 | Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
AID1424934 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1460608 | Inhibition of Staphylococcus aureus SAK2378 norA assessed as potentiation of CPX-induced antibacterial activity by measuring fold reduction in CPX MIC at 12.5 to 25 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. |
AID435553 | Binding constant for PRKCD kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID745319 | Cytotoxicity against human NCI-H661 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. |
AID282235 | Inhibition of p38 kinase | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID282229 | Inhibition of Bcr-Abl kinase | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1817044 | Cytotoxicity against human KU812 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | |||
AID435401 | Binding constant for full-length DRAK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID360785 | Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID724984 | Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID624987 | Binding constant for ABL1(Q252H)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625005 | Binding constant for EGFR(L861Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624867 | Binding constant for MLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID709995 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
AID1301838 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
AID625040 | Binding constant for PIK3CA(E545K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID724677 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID624787 | Binding constant for KIT(A829P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID745325 | Cytotoxicity against human DLD1 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. |
AID435899 | Binding constant for AKT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID360786 | Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID435445 | Binding constant for ZAP70 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224791 | Delta TM value showing the stabilisation of PRKACA produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1425148 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425187 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625094 | Binding constant for CDK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624705 | Binding constant for MYLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624883 | Binding constant for PRKCI kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID638910 | Inhibition of Flt-1 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
AID435526 | Binding constant for FGFR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425039 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1886523 | Growth inhibition of human K562 cells measured after 48 hrs by alamarblue assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
AID1425003 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID329183 | Binding affinity to Itk from human K562 cells extract by LC-MSMS | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID507085 | Inhibition of recombinant EphB4R 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. |
AID435517 | Binding constant for AKT2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625044 | Binding constant for PIK3CA(M1043I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1573083 | Antiproliferative activity against human SK-N-MC cells | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID329187 | Inhibition of recombinant Itk | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID1573082 | Antiproliferative activity against human DaOY cells | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID1612823 | Inhibition of LCK (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID282259 | AUC (total) in Sprague-Dawley rat at 10 mg/kg, po | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1186995 | Cytotoxicity against human HepG2 cells assessed as cell viability at 10 uM after 24 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
AID1613039 | Inhibition of DDR2 I638F mutant phosphorylation in human NCI-H2286 cells at 100 nM after 2 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
AID435170 | Binding constant for MYO3A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435789 | Binding constant for full-length CSNK2A2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID724974 | Inhibition of human recombinant ABL1 Y253F mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID435398 | Binding constant for DAPK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625006 | Binding constant for EGFR(S752-I759del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624808 | Binding constant for TRKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1772723 | PROTAC activity at CRBN/Bcr-Abl in human K562 cells assessed as reduction in c-Abl level after 16 hrs by Western blotting analysis | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation. |
AID624828 | Binding constant for CDK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID1301839 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
AID1515658 | Binding affinity to wild-type human partial length PDGFRB (V582 to Y1009 residues) expressed in bacterial expression system by TR-FRET assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Controlling cellular distribution of drugs with permeability modifying moieties. |
AID624748 | Binding constant for EPHA6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435783 | Binding constant for full-length BRSK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1176843 | Inhibition of ABL (unknown origin) at 1 uM by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization. |
AID435285 | Binding constant for DMPK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID739091 | Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated CrkL level after 1 hr by Western blot analysis | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant. |
AID625068 | Binding constant for NEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1613037 | Antitumor activity against human NCI-H2286 cells xenografted in SCID mouse assessed as tumor growth inhibition at 50 mg/kg, po qd for 10 consecutive days relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
AID624717 | Binding constant for JNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424996 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624926 | Binding constant for RIOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1814383 | Inhibition of ABL (unknown origin) at 100 uM incubated for 60 mins by ELISA relative to control | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia. |
AID624925 | Binding constant for RIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425170 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624894 | Binding constant for MEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435442 | Binding constant for SYK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID732858 | Inhibition of DDR1 (unknown origin) using fluorescein-labeled poly GAT as substrate incubated for 1 hr prior to substrate addition measured after 1 hr by TR-FRET assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. |
AID624875 | Binding constant for PDGFRB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625003 | Binding constant for EGFR(L858R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID458664 | Inhibition of human FMS expressed in growth factor dependent mouse FDC-P1 cells assessed as inhibition of FMS-mediated cell proliferation in presence human CSF1 after 48 hrs by resazurin dye reduction assay | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Colony stimulating factor-1 receptor as a target for small molecule inhibitors. |
AID624946 | Binding constant for BRAF 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. |
AID1425147 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID709937 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
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. |
AID1425043 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1286558 | Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID435196 | Binding constant for full-length SRPK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1616455 | Antitumor activity against luciferse expressing human K562 cells xenografted in NOD/SCID mouse assessed as attenuation of tumor progression at 5 mg/kg, ip QD for 12 days by serial volumetric analysis | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. |
AID435311 | Binding constant for HCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative 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. |
AID435803 | Binding constant for full-length LIMK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435775 | Binding constant for ABL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID735400 | Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography. |
AID624898 | Binding constant for GRK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624779 | Binding constant for BTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435294 | Binding constant for full-length LIMK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625034 | Binding constant for PDGFRA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436046 | Binding constant for PRKD2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1186992 | Cytotoxicity against human HepG2 cells assessed as cell viability at 10 uM after 4 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
AID625051 | Binding constant for PRKCQ kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1310127 | Inhibition of human KIT using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID1386089 | Inhibition of BCR-ABL1 E355G mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
AID436005 | Binding constant for ANKK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435906 | Binding constant for EGFR(L747-T751del,Sins) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435205 | Selectivity for ABL1 as proportion of 290 kinases in screen with similar potency; non-selective = 1 highly selective = 0 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624810 | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID435296 | Binding constant for MARK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435415 | Binding constant for MYLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID732829 | Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. |
AID1425078 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435664 | Binding constant for MYLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435282 | Binding constant for full-length CSNK1G2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435802 | Binding constant for KIT(V559D,V654A) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1817042 | Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay | |||
AID1186124 | Antiproliferative activity against human CXF 1103L cells after 4 days by modified propidium iodide assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Pyrrolo[3,2-b]quinoxaline derivatives as types I1/2 and II Eph tyrosine kinase inhibitors: structure-based design, synthesis, and in vivo validation. |
AID625042 | Binding constant for PIK3CA(H1047Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID329190 | Inhibition of TAP-tagged wild-type Btk | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID435147 | Binding constant for ACVR2B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425210 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435689 | Binding constant for full-length PFTK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID729593 | Inhibition of EPHA2 (unknown origin) at 100 uM after 60 mins by ELISA relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Design, synthesis and biological evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
AID624771 | Binding constant for TLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1734813 | Inhibition of colony formation in human MDA-MB-231 cells at 0.1 uM treated for 12 days by crystal violet staining based visual analysis | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
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. |
AID624886 | Binding constant for ERK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1373715 | Growth inhibition of human HL60 cells | 2018 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4 | Design and synthesis of novel dasatinib derivatives as inhibitors of leukemia stem cells. |
AID435781 | Binding constant for full-length BMX | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1817046 | Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | |||
AID624973 | Binding constant for JAK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224751 | Delta TM value showing the stabilisation of CAMK2A produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624797 | Binding constant for PHKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224797 | Delta TM value showing the stabilisation of MPSK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1425058 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435154 | Binding constant for DDR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID735401 | Cytotoxicity against human CXF 1103L cells after 4 days by propidium iodide staining | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography. |
AID435651 | Binding constant for DCAMKL2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624716 | Binding constant for CSNK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625023 | Binding constant for HIPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID638916 | Inhibition of EGFR at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
AID435430 | Binding constant for INSRR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624982 | Binding constant for ABL1(F317L)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425053 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1206308 | Antitumor activity against human MDA-MB-231 cells xenografted in SCID mouse assessed as tumor growth inhibition at 40 mg/kg/day administered for 18 days measured every 3 days during compound dosing | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID435907 | Binding constant for EGFR(L861Q) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624794 | Binding constant for MET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1421420 | Inhibition of recombinant human EPHA2 at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
AID625071 | Binding constant for STK39 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425020 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID507084 | Inhibition of recombinant EGFR 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. |
AID329182 | Binding affinity to Tec kinase from human K562 cells extract by LC-MSMS | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID435324 | Binding constant for full-length RIOK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1424926 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624816 | Binding constant for HPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224764 | Delta TM value showing the stabilisation of CK1G1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624846 | Binding constant for CSNK1A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435925 | Binding constant for PCTK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1246526 | Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for human U937 cells | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID1893832 | Clearance in rat relative to hepatic blood flow | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-Aminothiazole: A privileged scaffold for the discovery of anti-cancer agents. |
AID625057 | Binding constant for TYRO3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID282250 | Inhibition of PKCtau | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID624724 | Binding constant for TAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1484897 | Inhibition of EPH-A2 (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 1 hr by ELISA relative to control | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer. |
AID436014 | Binding constant for full-length DYRK1B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624899 | Binding constant for ROS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID1659072 | Protac activity at Cereblon/BCR/ABL T315I mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in BCR-ABL T315I mutant driven cell viability incubated for 3 days by CCK8 assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects. |
AID1425025 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625100 | Binding constant for NLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435444 | Binding constant for TYK2(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624837 | Binding constant for IRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224806 | Delta TM value showing the stabilisation of VRK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
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. |
AID1876248 | Antiviral activity against DENV infected in 180 mins pretreated human Huh-7 cells incubated for 1 to 72 hrs | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID1286565 | Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID624959 | Binding constant for MAP4K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1612829 | Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID435203 | Binding constant for TTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1310131 | Inhibition of C-terminal His-tagged full length human SRC expressed in insect cells preincubated for 20 mins using poly[Glu,Tyr]4:1 as substrate measured after 5 to 120 mins in presence of [gamma-33P]ATP by Kinome assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID507081 | Inhibition of recombinant c-Src 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. |
AID1425143 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID507072 | Inhibition of recombinant PI3Kalpha 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. |
AID1854086 | Inhibition of SRC (unknown origin) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | The progress of small-molecules and degraders against BCR-ABL for the treatment of CML. |
AID435557 | Binding constant for RIPK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1386084 | Inhibition of BCR-ABL1 G250H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
AID435903 | Binding constant for CDK8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624993 | Binding constant for ABL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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). |
AID1224762 | Delta TM value showing the stabilisation of CLK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID599959 | Binding affinity to human KIT D816V mutant incubated for 1 hr by kinase binding assay | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. |
AID624765 | Binding constant for TRKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624838 | Binding constant for ACVR2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624927 | Binding constant for RPS6KA4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID729550 | Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells by TR-FRET based binding assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay. |
AID1424911 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435204 | Binding constant for WEE1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1206282 | Induction of apoptosis in human MDA-MB-231 cells assessed as late apoptotic cells at 0.3 uM after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 2.67%) | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID1425047 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1331472 | Inhibition of recombinant human Src using KVEKIGEGTYGVVYK as substrate by [gamma-32P]ATP based assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Novel pyrazolo[3,4-d]pyrimidines as dual Src-Abl inhibitors active against mutant form of Abl and the leukemia K-562 cell line. |
AID1224804 | Delta TM value showing the stabilisation of VRK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID507691 | Inhibition of EPHB2 | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID1286568 | Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID1425076 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID435938 | Binding constant for TGFBR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435283 | Binding constant for DAPK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625069 | Binding constant for TLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624819 | Binding constant for ACVR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435189 | Binding constant for full-length PDPK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1168646 | Antiviral activity against Dengue virus assessed as inhibition of viral RNA replication | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | A perspective on targeting non-structural proteins to combat neglected tropical diseases: Dengue, West Nile and Chikungunya viruses. |
AID1246522 | Cytotoxicity against HEK293 cells assessed as reduction in cell viability | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID624887 | Binding constant for ERK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435909 | Binding constant for full-length LKB1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID627289 | Inhibition of RSK1 using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
AID1286569 | Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID624969 | Binding constant for ROCK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224771 | Delta TM value showing the stabilisation of MEK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID498728 | Binding affinity to wild type cSrc by fluorescence based binding assay | 2009 | Nature chemical biology, Jun, Volume: 5, Issue:6 | A new screening assay for allosteric inhibitors of cSrc. |
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. |
AID625017 | Binding constant for TIE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435432 | Binding constant for MLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425056 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1450953 | Binding affinity to recombinant human N-terminal His6-tagged Wee1 kinase domain (291 to 575 residues) expressed in Escherichia coli BL21 (DE3) assessed as change in melting temperature at 50 uM by differential scanning fluorimetry | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors. |
AID625063 | Binding constant for PLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507687 | Inhibition of cKIT V654A mutant | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
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. |
AID1764398 | Substrate activity at P-gp (unknown origin) assessed as net efflux ratio | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
AID360769 | Inhibition of c-Kit | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID1202517 | Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay | 2015 | European journal of medicinal chemistry, , Volume: 96 | Design and optimization of hybrid of 2,4-diaminopyrimidine and arylthiazole scaffold as anticancer cell proliferation and migration agents. |
AID282223 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1207423 | Inhibition of transient outward potassium current (Ito) current in Chinese Hamster Ovary (CHO) K1 cells expressing human Kv4.3 measured using IonWorks Quattro automated patch clamp platform | |||
AID1616432 | Induction of ternary complex formation between VHL and BCR-ABL (unknown origin) using recombinant ABL kinase domain and recombinant VHL/EloB/EloC by SEC-MALS analysis | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. |
AID435284 | Binding constant for DCAMKL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624826 | Binding constant for BMPR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624730 | Binding constant for CAMK2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624861 | Binding constant for LIMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1612828 | Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID435554 | Binding constant for PRKD3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
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. |
AID436055 | Binding constant for full-length YANK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID282230 | Inhibition of src kinase | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID724669 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID435687 | Binding constant for PAK7/PAK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1774075 | Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli assessed as ANS saturation ratio at 400 uM incubated for 1 hr in presence of 7.5 uM ANS by fluorescence method (Rvb = 56 +/- 2.3%) | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID375150 | Inhibition of cSrc in human DU145 cells assessed as reduction of phosphorylated FAK Y576/Y577 level at 100 nM after 5 hrs by immunoblot | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. |
AID360767 | Antiviral activity against Dengue virus infected in african green monkey Vero cells administered after viral challenge after 3 days by viral plaque assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID1425028 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624773 | Binding constant for AMPK-alpha1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435898 | Binding constant for ACVR1B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID729592 | Inhibition of ABL (unknown origin) at 100 uM after 60 mins by ELISA relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Design, synthesis and biological evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
AID507421 | Inhibition of recombinant CK1 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. |
AID435327 | Binding constant for VEGFR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID709997 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
AID435521 | Binding constant for CAMKK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID507700 | Inhibition of TXK | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID1734836 | Increase in cleaved caspase-3 level in human MDA-MB-231 cells at 0.03 to 0.3 uM incubated for 20 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
AID624932 | Binding constant for CLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1659071 | Antiproliferative activity against wild type mouse BA/F3 cells incubated for 3 days by CCK8 assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects. |
AID435667 | Binding constant for full-length NLK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1424983 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435414 | Binding constant for MLK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1573063 | Antiproliferative activity against human MOLT4 cells | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID435797 | Binding constant for ERBB4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1424966 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1286566 | Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID1425165 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID436010 | Binding constant for full-length CDK5 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425061 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID436023 | Binding constant for MERTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625025 | Binding constant for MAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1484899 | Inhibition of c-Src (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 1 hr by ELISA relative to control | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer. |
AID709990 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
AID329184 | Inhibition of recombinant Btk | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID1425093 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624943 | Binding constant for ACVR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625130 | Binding constant for FGFR4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435288 | Binding constant for EPHB2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1424984 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID282242 | Inhibition of IKK | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID271947 | Inhibition of anti CD3/anti CD28-induced T cell proliferation | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatin |
AID624944 | Binding constant for ALK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435318 | Binding constant for PAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624872 | Binding constant for PAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625060 | Binding constant for CAMKK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625137 | Binding constant for MEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
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. |
AID624958 | Binding constant for PIK3C2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624984 | Binding constant for ABL1(H396P)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425077 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
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. |
AID1695242 | Growth inhibition of human Jeko-1 cells incubated for 72 hrs | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Understanding the mechanism of action of pyrrolo[3,2- |
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. |
AID1286557 | Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID435661 | Binding constant for full-length MKNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435295 | Binding constant for MAP4K3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625102 | Binding constant for PRKD2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425021 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435674 | Binding constant for JAK3(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624746 | Binding constant for WEE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624852 | Binding constant for FES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID282226 | Cmax in BALB/c mouse at 50 mg/kg, po after 4 hrs | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID436045 | Binding constant for PRKD1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1734841 | Antitumor activity against human MDA-MB-435 cells xenografted in SCID mouse assessed as tumor growth inhibition at 40 mg/kg, po QD for 21 days and measured every 3 days | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
AID435155 | Binding constant for full-length DLK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1206303 | Inhibition of Src phosphorylation in human MDA-MB-231 cells at 0.001 to 1 uM after 20 hrs by Western blot analysis | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID1425106 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435399 | Binding constant for DCAMKL3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID677651 | Antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as inhibition of network formation at 0.15 uM after 72 hrs | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17 | A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model: from in silico screening to cyclodextrin formulation. |
AID624989 | Binding constant for ABL1(T315I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1331469 | Inhibition of wild type recombinant human Abl assessed as residual activity at 100 uM using abtide as substrate by [gamma-32P]ATP based assay relative to control | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Novel pyrazolo[3,4-d]pyrimidines as dual Src-Abl inhibitors active against mutant form of Abl and the leukemia K-562 cell line. |
AID1310132 | Inhibition of human YES using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P] ATP | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID1224788 | Delta TM value showing the stabilisation of PIM3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID625106 | Binding constant for MARK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 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). |
AID435153 | Binding constant for full-length DAPK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID282227 | Plasma concentration in BALB/c mouse at 50 mg/kg, po after 4 hrs | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID624728 | Binding constant for NIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436042 | Binding constant for full-length PHKG1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624752 | Binding constant for SNRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625099 | Binding constant for TAOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1331475 | Cytotoxicity against human K562 cells assessed as decrease in cell viability by MTT assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Novel pyrazolo[3,4-d]pyrimidines as dual Src-Abl inhibitors active against mutant form of Abl and the leukemia K-562 cell line. |
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. |
AID375146 | Inhibition of cSrc in human DU145 cells assessed as reduction of phosphorylated Src Y416 level at 100 nM after 5 hrs by immunoblot | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. |
AID375144 | Inhibition of cSrc in human PC3 cells assessed as reduction of phosphorylated Src Y416 level at 100 nM after 5 hrs by immunoblot | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. |
AID625105 | Binding constant for EPHB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624708 | Binding constant for CDC2L1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435412 | Binding constant for MAP3K5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624949 | Binding constant for CSNK1G3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1876064 | Cytotoxicity against African green monkey Vero E6 cells | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1425001 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624876 | Binding constant for PDPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425209 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1654860 | Antiviral activity against HCV genotype 1b pseudoparticle infected in human Huh7.5 cells assessed as reduction in viral replication at 2 to 4 uM | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | 2-((4-Arylpiperazin-1-yl)methyl)benzonitrile Derivatives as Orally Available Inhibitors of Hepatitis C Virus with a Novel Mechanism of Action. |
AID507426 | Inhibition of TRKB at 10 mM | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID624972 | Binding constant for MTOR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435530 | Binding constant for MAP3K4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435397 | Binding constant for CSNK1G1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID415072 | Inhibition of EGFR | 2009 | Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8 | Structure-based virtual screening of Src kinase inhibitors. |
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. |
AID760493 | Cytotoxicity against human HCT116 cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1224759 | Delta TM value showing the stabilisation of CDKL1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624900 | Binding constant for RSK1(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID507685 | Inhibition of cKIT D816H mutant | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID1224757 | Delta TM value showing the stabilisation of CDK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624864 | Binding constant for CTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424980 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1460604 | Synergistic antibacterial activity against Staphylococcus aureus SAK1902 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. |
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. |
AID1425125 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435406 | Binding constant for FLT3(D835H) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1876282 | Inhibition of SRC (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID435297 | Binding constant for MLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435660 | Binding constant for full-length MELK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625065 | Binding constant for CIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1915579 | Inhibition of Bcr-Abl (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID624738 | Binding constant for MLCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624832 | Binding constant for IKK-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID271954 | Inhibition of p38 kinase | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatin |
AID1424933 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624980 | Binding constant for ABL1(F317I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425050 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1141134 | Binding affinity to human acrylodan-labeled N-terminal His-tagged DDR2 (558 to 855 aa) by FLiK assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Identification of type II and III DDR2 inhibitors. |
AID1734834 | Inhibition of Src in human MDA-MB-231 cells assessed as reduction in phosphorylation of SRC at 0.03 to 0.3 uM incubated for 20 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
AID1573087 | Antiproliferative activity against human U87 cells | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID435657 | Binding constant for full-length IKK-epsilon | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1256161 | Inhibition of Bcr-Abl T315I mutant (unknown origin) by ADP-Glo assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Expanding the structural diversity of Bcr-Abl inhibitors: Dibenzoylpiperazin incorporated with 1H-indazol-3-amine. |
AID1425123 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625124 | Binding constant for RET(V804M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1286570 | Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID1425100 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435939 | Binding constant for TIE2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1331473 | Inhibition of wild type recombinant human Abl using abtide as substrate by [gamma-32P]ATP based assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Novel pyrazolo[3,4-d]pyrimidines as dual Src-Abl inhibitors active against mutant form of Abl and the leukemia K-562 cell line. |
AID1473867 | Ratio of drug concentration at steady state in patient with advanced phase CML and Ph+ ALL at 100 mg, po BID after 12 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. |
AID624799 | Binding constant for TIE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624777 | Binding constant for DDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1205867 | Cytotoxicity against human A2780 cells after 72 hrs by MTT assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Improved angiostatic activity of dasatinib by modulation with hydrophobic chains. |
AID624924 | Binding constant for RIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1473864 | Drug concentration at steady state in patient with chronic phase CML at 70 to 90 mg, po BID after 12 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. |
AID624712 | Binding constant for DYRK1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224789 | Delta TM value showing the stabilisation of PLK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID435562 | Binding constant for STK36 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435194 | Binding constant for RPS6KA6(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID436007 | Binding constant for AXL kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624923 | Binding constant for MAPKAPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID709992 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
AID1424981 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425166 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425193 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624966 | Binding constant for DCAMKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435274 | Binding constant for ACVR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435692 | Binding constant for STK16 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624928 | Binding constant for CDKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624801 | Binding constant for MAP3K15 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435648 | Binding constant for CAMKK2 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. |
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. |
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. |
AID1460598 | Inhibition of NorA in Staphylococcus aureus SA1199B harboring GrlA A116E mutant assessed as inhibition of ethidium bromide efflux at 50 uM measured after 5 mins by fluorometric method relative to control | 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. |
AID435912 | Binding constant for MRCKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624763 | Binding constant for RIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224753 | Delta TM value showing the stabilisation of CAMK2D produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
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. |
AID624807 | Binding constant for TNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624762 | Binding constant for DLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID760492 | Cytotoxicity against human MALME-3M cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID435434 | Binding constant for RET kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425131 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625111 | Binding constant for RIOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625084 | Binding constant for HUNK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID732824 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. |
AID375139 | Inhibition of chicken N-terminal His-tagged cSrc T338M mutant expressed in Escherichia coli BL21 (DE3) | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. |
AID625074 | Binding constant for IKK-epsilon kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1301840 | Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
AID625132 | Binding constant for FGFR1 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. |
AID435926 | Binding constant for PDGFRB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative 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. |
AID640178 | Cytotoxicity against human U937 cells after 72 hrs by WST-8 reagent based MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Design, synthesis, and in vitro antiproliferative activity of novel Dasatinib derivatives. |
AID625020 | Binding constant for ITK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435325 | Binding constant for RPS6KA4(Kin.Dom.1 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435653 | Binding constant for EGFR(L747-S752del, P753S) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625113 | Binding constant for MARK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1875917 | Antiviral activity against SARS-CoV | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID271970 | Inhibition of Cdk2 | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatin |
AID624783 | Binding constant for FGFR3(G697C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435787 | Binding constant for CLK2 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. |
AID435393 | Binding constant for CAMK1D kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID625062 | Binding constant for MAP3K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID329188 | Reduction of LPS-induced Btk autophosphorylation on Tyr223 in human U937 cells at 30 nM after 1 hr | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID638923 | Inhibition of IGF1R at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
AID1229717 | Antiviral activity against DENV by CPE-reduction assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12 | Discovery of Multitarget Antivirals Acting on Both the Dengue Virus NS5-NS3 Interaction and the Host Src/Fyn Kinases. |
AID1425175 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1515650 | Binding affinity to ABL (unknown origin) by TR-FRET assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Controlling cellular distribution of drugs with permeability modifying moieties. |
AID507425 | Inhibition of TRKA at 10 mM | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID1454442 | Displacement of CAT-1 from catalytic site of N-terminal His6-tagged ABL T315I mutant (unknown origin) at 25 uM by 19F NMR spectroscopy based dual-site competition assay | 2017 | ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6 | |
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. |
AID1857474 | Inhibition of recombinant LIMK1(unknown origin) expressed in HEK293 cells using NanoGlo substrate incubated for 2 hrs followed by substrate addition by NanoBRET assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20 | Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. |
AID1286556 | Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID624741 | Binding constant for LRRK2(G2019S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID415071 | Inhibition of Src kinase | 2009 | Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8 | Structure-based virtual screening of Src kinase inhibitors. |
AID624955 | Binding constant for EPHB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424968 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1176844 | Inhibition of EPHA2 (unknown origin) at 1 uM by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization. |
AID282245 | Inhibition of IGF1R kinase | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID624815 | Binding constant for ERBB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625090 | Binding constant for ICK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435431 | Binding constant for MAP4K1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1373716 | Growth inhibition of human KG1a cells | 2018 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4 | Design and synthesis of novel dasatinib derivatives as inhibitors of leukemia stem cells. |
AID1425190 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435929 | Binding constant for PAK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624833 | Binding constant for CSNK1G2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1873492 | Inhibition of N-terminal 6His-tagged SARS-CoV2 nsp3 Mac1 (200 to 380 residues) expressed in Escherichia coli BL21 (DE3) | 2022 | Bioorganic & medicinal chemistry, 08-01, Volume: 67 | Design, synthesis and evaluation of inhibitors of the SARS-CoV-2 nsp3 macrodomain. |
AID1224780 | Delta TM value showing the stabilisation of OSR1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID436019 | Binding constant for FRK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624848 | Binding constant for CSNK2A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425085 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425112 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID732827 | Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. |
AID1224775 | Delta TM value showing the stabilisation of ERK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID624780 | Binding constant for CDK4-cyclinD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID329195 | Inhibition of Itk F435T mutant | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID624998 | Binding constant for EGFR(G719C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1886530 | Inhibition of ABL1 (unknown origin) | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
AID1573067 | Inhibition of BCR/ABL E225K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell growth | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID435156 | Binding constant for EGFR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624714 | Binding constant for p38-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID436043 | Binding constant for PKMYT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624948 | Binding constant for CSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435793 | Binding constant for EPHA1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435902 | Binding constant for BRAF(V600E) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1573065 | Antiproliferative activity against human Jurkat cells | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). |
AID625039 | Binding constant for PIK3CA(E545A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425048 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID360768 | Inhibition of PDGFR | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID624877 | Binding constant for PIK3C2B 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. |
AID624938 | Binding constant for FLT3(K663Q) 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. |
AID436034 | Binding constant for PRKCH kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624778 | Binding constant for ACVRL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1283298 | Resistance index, ratio IC50 for mouse BA/F3 cells expressing BCR-ABL T315I mutant to IC50 for human K562 cells | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | Structure-Activity Relationship Study of Rakicidins: Overcoming Chronic Myeloid Leukemia Resistance to Imatinib with 4-Methylester-Rakicidin A. |
AID1242622 | Inhibition of c-Src (unknown origin) using biotinylated HER2 peptide as substrate at 0.003 uM by time resolved fluorescence method | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors. |
AID436016 | Binding constant for full-length ERK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425057 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID329201 | Inhibition of antigen-induced histamine release in human basophils at 1 uM after 30 mins | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID435649 | Binding constant for CDC2L2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1186127 | Antiproliferative activity against human PAXF 1657L cells after 4 days by modified propidium iodide assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Pyrrolo[3,2-b]quinoxaline derivatives as types I1/2 and II Eph tyrosine kinase inhibitors: structure-based design, synthesis, and in vivo validation. |
AID1386051 | Inhibition of BCR-ABL1 T315I mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
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. |
AID624970 | Binding constant for CDK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID724985 | Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID624890 | Binding constant for p38-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1240407 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. |
AID1286567 | Antiproliferative activity against human MOLM14 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
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. |
AID1425117 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID739092 | Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated STAT5 level after 1 hr by Western blot analysis | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant. |
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. |
AID624824 | Binding constant for PIP5K1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424950 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1865204 | Binding affinity to P38alpha (unknown origin) measured at 0.51 to 10 uM after 360 secs by SPR analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18 | A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
AID1886534 | Vasculo-toxicity in human HMVEC cells assessed as reduction in vascular structure integrity at 10 uM measured after 6 hrs by calcein AM dye based fluorescence assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
AID435833 | Binding constant for full-length TNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624863 | Binding constant for MARK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
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. |
AID1424993 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624732 | Binding constant for PYK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435679 | Binding constant for PIM3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1224782 | Delta TM value showing the stabilisation of PAK5 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1425142 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID625083 | Binding constant for LATS2 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. |
AID1286550 | Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID435184 | Binding constant for PTK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
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. |
AID435405 | Binding constant for ERK8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1373719 | Inhibition of cell migration of mouse B16-BL6 cells at 8.13 uM incubated for 24 to 48 hrs by cell wound scratch assay | 2018 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4 | Design and synthesis of novel dasatinib derivatives as inhibitors of leukemia stem cells. |
AID1515653 | Binding affinity to wild-type human partial length CSF1R (I564 to S939 residues) expressed in bacterial expression system by TR-FRET assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Controlling cellular distribution of drugs with permeability modifying moieties. |
AID435656 | Binding constant for FGFR4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1876283 | Binding affinity to Fyn (unknown origin) assessed as dissociation constant | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID1724048 | Inhibition of ABL (unknown origin) | 2020 | Bioorganic & medicinal chemistry, 09-15, Volume: 28, Issue:18 | Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors. |
AID436006 | Binding constant for full-length AURKC | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425159 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID760494 | Cytotoxicity against human Hs578T cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
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. |
AID282228 | Protein binding in human serum at 10 uM | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1425163 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425065 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624817 | Binding constant for MYO3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625049 | Binding constant for PRKCH kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1515655 | Binding affinity to wild-type human partial length FYN (T243 to L534 residues) expressed in bacterial expression system by TR-FRET assay | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Controlling cellular distribution of drugs with permeability modifying moieties. |
AID1425089 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624855 | Binding constant for FRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424929 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1207734 | Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits | 2013 | Scientific reports, , Volume: 3 | MICE models: superior to the HERG model in predicting Torsade de Pointes. |
AID271967 | Inhibition of Fyn | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatin |
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. |
AID624907 | Binding constant for SYK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425207 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624803 | Binding constant for CHEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID329185 | Inhibition of recombinant Abl kinase | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
AID624892 | Binding constant for p38-delta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1207303 | Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform | |||
AID1207395 | Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells transfected with KCNQ1 / Kv1.7 / KvLQT1 and KCNE1/minK measured using IonWorks automated patch clamp platform | |||
AID1424975 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1772740 | Antitumor activity against human K562 cells xenografted in NOD-SCID mouse assessed as tumor growth inhibition at 5 mg/kg, ip administered daily 10 days | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation. |
AID624897 | Binding constant for RAF1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID724980 | Inhibition of human recombinant ABL1 T315I mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID1724050 | Inhibition of c-kit (unknown origin) | 2020 | Bioorganic & medicinal chemistry, 09-15, Volume: 28, Issue:18 | Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors. |
AID760501 | Cytotoxicity against human NCI60 cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1425044 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624853 | Binding constant for FLT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435522 | Binding constant for CDK11 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435439 | Binding constant for PAK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435164 | Binding constant for IGF1R kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425087 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435520 | Binding constant for CAMK2A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425033 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624878 | Binding constant for PIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID638918 | Inhibition of c-Src at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
AID709936 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 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). |
AID1424914 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID624720 | Binding constant for HIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1424897 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID436050 | Binding constant for RPS6KA2(Kin.Dom.1 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
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. |
AID1242616 | Inhibition of DDR2 (unknown origin) after 1 hr by time resolved fluorescence method | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors. |
AID1224796 | Delta TM value showing the stabilisation of LOK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1734838 | Inhibition of MEK phosphorylation in human MDA-MB-231 cells at 0.03 to 0.3 uM incubated for 20 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer. |
AID435159 | Binding constant for EPHB3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425046 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID360773 | Antiviral activity against Dengue virus 2 infected in asian tiger mosquito C6/36 cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
AID624749 | Binding constant for CASK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1823809 | Inhibition of NanoLuc-fused CSF1R (unknown origin) expressed in HEK293 cells incubated for 2 hrs by NanoBRET assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration. |
AID1616468 | Growth inhibition of human K562 cells assessed as reduction in cell density at 20 times IC50 incubated for 12 hrs followed by drug wash-out and incubation in drug-free medium up to 144 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. |
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. |
AID625031 | Binding constant for MRCKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425203 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1899933 | Inhibition of from NanoLuc-fused Fyn (unknown origin) transfected in HEK293 cells using tracer K4 incubated for 1 hr by NanoBRET assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | ARN25068, a versatile starting point towards triple GSK-3β/FYN/DYRK1A inhibitors to tackle tau-related neurological disorders. |
AID1286562 | Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID625128 | Binding constant for CSNK1G1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425161 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1424963 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435665 | Binding constant for NEK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624847 | Binding constant for CSNK1E kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID724670 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID625079 | Binding constant for NEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624736 | Binding constant for RPS6KA5(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1286589 | Inhibition of BCR/ABL in human MEG01 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID1286543 | Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID624942 | Binding constant for DRAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1224767 | Delta TM value showing the stabilisation of DAPK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
AID1286587 | Inhibition of BCR/ABL in human K562 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
AID1246520 | Cytotoxicity against human THP1 cells assessed as reduction in cell viability | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19 | Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
AID435527 | Binding constant for FGFR3(G697C) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID677650 | Antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as inhibition of cell growth at 0.15 uM after 72 hrs | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17 | A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model: from in silico screening to cyclodextrin formulation. |
AID624718 | Binding constant for PFTAIRE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1915581 | Cytotoxicity against human DU-145 cells | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID624731 | Binding constant for CAMK2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID729552 | Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells at 5 uM by TR-FRET based binding assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay. |
AID625028 | Binding constant for ASK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID625089 | Binding constant for AAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435784 | Binding constant for CAMK2G kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID282231 | Inhibition of lck inase | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
AID1310126 | Inhibition of human FYN using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
AID507686 | Inhibition of cKIT V560G mutant | 2009 | Leukemia, Mar, Volume: 23, Issue:3 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
AID436025 | Binding constant for NDR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID435202 | Binding constant for TRKC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1612825 | Inhibition of SRC (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID436011 | Binding constant for full-length CLK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1612816 | Inhibition of Lyn B (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
AID1425154 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1876259 | Antiviral activity against SARS-CoV infected in african green monkey Vero E6 cells measured after 50 hrs by cell-titre glo assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID624788 | Binding constant for KIT(D816H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1425108 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1205869 | Cytotoxicity against human HEK293 cells after 72 hrs by MTT assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Improved angiostatic activity of dasatinib by modulation with hydrophobic chains. |
AID436009 | Binding constant for full-length CAMK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID624760 | Binding constant for PFPK5(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID1814378 | Inhibition of EPHA2 (unknown origin) at 100 uM incubated for 60 mins by ELISA relative to control | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia. |
AID435778 | Binding constant for full-length ADCK4 | 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. |
AID1425172 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID436018 | Binding constant for FLT4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1425160 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID760496 | Cytotoxicity against human DU145 cells after 48 hrs by SRB assay | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Development of a chimeric c-Src kinase and HDAC inhibitor. |
AID1424987 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID435644 | Binding constant for ABL1(E255K) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID1207275 | Inhibition of long-lasting type calcium current (ICaL) in HEK293 cells (alpha1C/beta2a/alpha2delta1) cells measured using IonWorks Barracuda automated patch clamp platform | |||
AID625101 | Binding constant for TAOK3 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. |
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. |
AID624739 | Binding constant for GRK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624744 | Binding constant for ZAP70 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID624702 | Binding constant for BRSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID624757 | Binding constant for PKMYT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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. |
AID625075 | Binding constant for INSRR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
AID435791 | Binding constant for EGFR(E746-A750del) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
AID640175 | Growth inhibition of human K562 cells at 10 uM after 72 hrs by WST-8 reagent based MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Design, synthesis, and in vitro antiproliferative activity of novel Dasatinib derivatives. |
AID710013 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
AID1508591 | NCATS Rat Liver Microsome Stability Profiling | 2020 | Scientific reports, 11-26, Volume: 10, Issue:1 | Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models. |
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. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
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. |
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. |
AID1508612 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Highly predictive and interpretable models for PAMPA permeability. |
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. |
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. |
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. |
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. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
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. |
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. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
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. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
AID493040 | Navigating the Kinome | 2011 | Nature chemical biology, Apr, Volume: 7, Issue:4 | Navigating the kinome. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
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. |
AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
AID1347140 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability 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. |
AID1347139 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability 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. |
AID1347141 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability 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. |
AID1347137 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability 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. |
AID1347136 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability 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. |
AID1347138 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D caspase 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. |
AID1347135 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability 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. |
AID1347163 | 384 well plate NINDS AMC confirmatory qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347169 | Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347149 | Furin counterscreen qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347156 | DAPI mCherry counterscreen qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1645848 | NCATS Kinetic Aqueous Solubility Profiling | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14 | Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity. |
AID1347151 | Optimization of GU AMC 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. |
AID1347168 | HepG2 cells viability qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347150 | Optimization screen NINDS AMC qHTS for Zika virus inhibitors: Linked 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. |
AID1347164 | 384 well plate NINDS Rhodamine confirmatory qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347167 | Vero cells viability qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347158 | ZIKV-mCherry secondary 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. |
AID1347155 | Optimization screen NINDS Rhodamine qHTS for Zika virus inhibitors: Linked 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. |
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. |
AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
[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 | 411 (15.44) | 29.6817 |
2010's | 1638 (61.53) | 24.3611 |
2020's | 613 (23.03) | 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 (82.92) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 216 (7.98%) | 5.53% |
Reviews | 347 (12.82%) | 6.00% |
Case Studies | 400 (14.78%) | 4.05% |
Observational | 24 (0.89%) | 0.25% |
Other | 1,720 (63.54%) | 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 | ||
---|---|---|---|---|---|---|---|
The Safety and Clinical Efficacy of Dasatinib Plus Human CD19/CD22 Bispecific CAR-T Cell Therapy for Elderly Subjects With Ph-positive Acute Lymphoblastic Leukemia [NCT05523661] | Phase 1 | 15 participants (Anticipated) | Interventional | 2021-03-01 | Recruiting | ||
A Study Using Molecular Guided Therapy With Induction Chemotherapy Followed by a Randomized Controlled Trial of Standard Immunotherapy With or Without DFMO Followed by DFMO Maintenance for Subjects With Newly Diagnosed High-Risk Neuroblastoma [NCT02559778] | Phase 2 | 500 participants (Anticipated) | Interventional | 2015-09-30 | Recruiting | ||
Dasatinib Combination for Chronic Lymphocytic Leukemia Patients With Chemo Refractory Disease [NCT01051115] | Phase 2 | 35 participants (Anticipated) | Interventional | 2008-10-31 | Recruiting | ||
A Multicenter, Open-label, Phase Ii Study of Dasatinib in Combination With Melphalan and Prednisone (D-MP) in Advanced, Relapsed / Refractory Multiple Myeloma Patients [NCT01116128] | Phase 2 | 8 participants (Actual) | Interventional | 2008-02-29 | Terminated(stopped due to difficulty in enrolling patients) | ||
Phase II Study of Dasatinib (BMS-354825) for Advanced Estrogen/Progesterone Receptor-Positive or Her2/Neu-Positive Breast Cancer [NCT00371345] | Phase 2 | 92 participants (Actual) | Interventional | 2006-12-31 | Completed | ||
Treatment With Second Generation TYROSINE KINASE INHIBITORS (2G TKI) Post Imatinib Failure: Factors Predicting Response and Predictive Value of Response [NCT01188278] | 173 participants (Actual) | Observational | 2010-07-31 | Completed | |||
Comparison of Biomarker Modulation by Inhibition of EGFR and/or Src Family Kinases Using Erlotinib and Dasatinib in Head and Neck Lung Cancers [NCT00779389] | Phase 1 | 58 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
Molecular Analysis for Therapy Choice (MATCH) [NCT02465060] | Phase 2 | 6,452 participants (Anticipated) | Interventional | 2015-08-17 | Active, not recruiting | ||
Continuing Treatment for Subjects Who Have Participated on a Prior Protocol Investigating Dasatinib [NCT02297139] | Phase 2 | 17 participants (Actual) | Interventional | 2015-07-31 | Completed | ||
A Multicenter, Open-Label, Randomized, Phase II Trial of Adjuvant Dasatinib Plus Gemcitabine Versus Single-Agent Gemcitabine in Patients With Resected Pancreatic Adenocarcinoma [NCT01234935] | Phase 2 | 8 participants (Actual) | Interventional | 2011-01-13 | Completed | ||
Phase I/II Study of Dasatinib and Osimertinib (AZD9291) in Patients With Advanced Non-small Cell Lung Cancer With EGFR Mutations [NCT02954523] | Phase 1/Phase 2 | 10 participants (Actual) | Interventional | 2016-10-31 | Active, not recruiting | ||
Low-dose Dasatinib as First-line Treatment for Chronic Myeloid Leukemia [NCT03216070] | Phase 4 | 12 participants (Anticipated) | Interventional | 2016-04-01 | Recruiting | ||
Phase II Clinical Trial to Evaluate the Safety and Feasibility of Senolytic Therapy in Alzheimer's Disease [NCT04685590] | Phase 2 | 48 participants (Anticipated) | Interventional | 2021-12-22 | Recruiting | ||
Phase II Short-term Adjuvant Therapy and Biomarker Studies With Targeted Agents in Women With Estrogen Receptor Negative Breast Cancer [NCT01471106] | Phase 2 | 26 participants (Actual) | Interventional | 2014-01-21 | Active, not recruiting | ||
Effectiveness of Dasatinib(Sprycel®) in Adult Patients With Chronic Myeloid Leukemia in China: A Multicenter, Registry Study [NCT02389972] | 128 participants (Actual) | Observational | 2013-04-11 | Completed | |||
A Phase II Study of Dose-Adjusted Etoposide, Prednisone, Vincristine, Cyclophosphamide, and Doxorubicin (DA-EPOCH) as Front-Line Therapy for Adults With Acute Lymphoblastic Leukemia/Lymphoma [NCT03023046] | Phase 2 | 54 participants (Actual) | Interventional | 2017-02-23 | Completed | ||
Persistence Of Major Molecular Remission In Chronic Myeloid Leukemia After A Second Stop Of Tki Treatment In Patients Who Failed An Initial Stop Attempt: A Multicenter Prospective Trial [NCT03573596] | Phase 2 | 134 participants (Anticipated) | Interventional | 2018-02-01 | Recruiting | ||
Dasatinib Combined With Multi-agents Chemotherapy in Relapsed t(8;21) Acute Myeloid Leukemia With KIT D816 Mutation [NCT03560908] | Phase 1 | 0 participants (Actual) | Interventional | 2018-07-01 | Withdrawn(stopped due to No enough eligable participants enrolled) | ||
Phase II Study of Adding the Anti-PD-1 Pembrolizumab to Tyrosine Kinase Inhibitors in Patients With Chronic Myeloid Leukemia and Persistently Detectable Minimal Residual Disease [NCT03516279] | Phase 2 | 40 participants (Anticipated) | Interventional | 2019-06-26 | Recruiting | ||
Phase Ib Study of Nivolumab and Dasatinib in Patients With Relapsed/Refractory Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia (Ph+ ALL) [NCT02819804] | Phase 1 | 1 participants (Actual) | Interventional | 2017-08-17 | Terminated(stopped due to Due to funding and accrual issues) | ||
A Study of Complete Molecular Response for Chronic Myeloid Leukemia in Chronic Phase Patients, Treated With Dasatinib [NCT01342679] | Phase 2 | 21 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
Ancillary Observational Study of Post-Frontline Sequential Treatment of Adult Philadelphia Chromosome-Positive (Ph+) Acute Lymphoblastic Leukemia (ALL) Patients With Dasatinib and the Bispecific Monoclonal Antibody Blinatumomab [NCT03318770] | 60 participants (Anticipated) | Observational | 2019-05-10 | Recruiting | |||
Multicenter, Non-randomized Phase II Pilot Study to Assess the Efficacy and Safety of Dasatinib After Allogeneic Stem Cell Transplantation in Patients With de Novo Philadelphia Positive (Bcr-abl +) Acute Lymphoblastic Leukemia [NCT01310010] | Phase 2 | 30 participants (Anticipated) | Interventional | 2010-04-30 | Completed | ||
Dose Individualization of Antineoplastic Drugs and Anti-Infective Drug in Children With Hematoplastic Disease [NCT03844360] | Phase 4 | 1,500 participants (Anticipated) | Interventional | 2016-01-31 | Recruiting | ||
Effect of Omega-3 Fatty Acid, Eicosapentaenoic Acid, and Its Metabolites in Combination With Tyrosine Kinase Inhibitors in Chronic Myeloid Leukemia in Stable Chronic Phase [NCT04006847] | Phase 1/Phase 2 | 1 participants (Actual) | Interventional | 2020-09-14 | Terminated(stopped due to Product complaint) | ||
A Phase II Study of Punctual, Cyclic, and Intensive Chemotherapy With Liposomal Cytarabine (Depocyt®) CNS Prophylaxis for Adults With Acute Lymphoblastic Leukemia and Lymphoblastic Lymphoma [NCT02043587] | Phase 2 | 31 participants (Actual) | Interventional | 2014-01-31 | Terminated(stopped due to Original investigator for the trial has left) | ||
A Randomized Two-by-Two, Multicenter, Open-Label Phase III Study of BMS-354825 Administered Orally at a Dose of 50 mg or 70 mg Twice Daily or 100 mg or 140 mg Once Daily in Subjects With Chronic Phase Philadelphia Chromosome or BCR-ABL Positive Chronic My [NCT00123474] | Phase 3 | 724 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
Phase II Studies of Two Different Schedules of Dasatinib (NSC-732517) in Bone Metastasis Predominant Metastatic Breast Cancer [NCT00410813] | Phase 2 | 85 participants (Actual) | Interventional | 2007-03-31 | Completed | ||
A Prospective Phase II Clinical Trial Evaluating the Efficacy and the Safety of Tyrosine Kinase Inhibitors Withdrawal After a Previous Two-step Dose Reduction in Patients With Chronic Myeloid Leukemia in Deep Molecular Remission [NCT04147533] | Phase 2 | 150 participants (Anticipated) | Interventional | 2020-06-16 | Active, not recruiting | ||
A Phase II Study of BMS-354825 in Subjects With Lymphoid Blast Phase Chronic Myeloid Leukemia or Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia Resistant to or Intolerant of Imatinib Mesylate [NCT00101595] | Phase 2 | 96 participants (Actual) | Interventional | 2005-01-31 | Completed | ||
A Phase 1 Study of Gemcitabine, Dasatinib and Erlotinib in Patients With Advanced Pancreatic Carcinoma [NCT01660971] | Phase 1 | 19 participants (Actual) | Interventional | 2012-07-30 | Active, not recruiting | ||
A Phase II Study of Dasatinib Therapy in Children and Adolescents With Newly Diagnosed Chronic Phase Chronic Myelogenous Leukemia or With Ph+ Leukemias Resistant or Intolerant to Imatinib [NCT00777036] | Phase 2 | 130 participants (Actual) | Interventional | 2009-03-20 | Active, not recruiting | ||
A Phase 2 Multi-Center, Historically Controlled Study of Dasatinib Added to Standard Chemotherapy in Pediatric Patients With Newly Diagnosed Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia [NCT01460160] | Phase 2 | 106 participants (Actual) | Interventional | 2012-04-13 | Completed | ||
Phase II Study of Combination of Hyper-CVAD and Dasatinib (NSC-732517) With or Without Allogeneic Stem Cell Transplant in Patients With Philadelphia (Ph) Chromosome Positive and/or BCR-ABL Positive Acute Lymphoblastic Leukemia (ALL) (A BMT Study) [NCT00792948] | Phase 2 | 97 participants (Actual) | Interventional | 2009-09-01 | Active, not recruiting | ||
PICAASO / CA180-722: Psma Intensity Can be Altered by Androgen and Phospho-SrC Obstruction [NCT04925648] | Phase 2 | 22 participants (Anticipated) | Interventional | 2021-10-18 | Recruiting | ||
Extension Study of a Study to Evaluate Efficacy and Safety of Imatinib (Glinib®) 600mg/Day Depending on Early Molecular Response in Newly Diagnosed Patients With Chronic Myeloid Leukemia in Chronic Phase [NCT02421926] | 0 participants (Actual) | Observational | 2014-10-31 | Withdrawn | |||
A Phase IV, Open-label, Multicenter Study of Dasatinib in Chronic-Phase Chronic Myeloid Leukemia (CP-CML) Patients With Chronic, Low-grade Non-Hematologic Toxicity to Imatinib [NCT01660906] | Phase 4 | 39 participants (Actual) | Interventional | 2012-12-31 | Completed | ||
A Phase 2, Randomized, Open Label, Pivotal Study to Evaluate the Efficacy and Safety of HQP1351 in CML CP Patients Who Are Resistant and/or Intolerant to First- and Second-Generation Tyrosine Kinase Inhibitors [NCT04126681] | Phase 2 | 144 participants (Actual) | Interventional | 2019-10-21 | Active, not recruiting | ||
Senescence, Frailty, and Mesenchymal Stem Cell Functionality in Chronic Kidney Disease: Effect of Senolytic Agents [NCT02848131] | Phase 2 | 30 participants (Anticipated) | Interventional | 2016-07-31 | Enrolling by invitation | ||
A Phase II Study of Dasatinib (Sprycel®) (NSC #732517) as Primary Therapy Followed by Transplantation for Adults >/= 18 Years With Newly Diagnosed Ph+ Acute Lymphoblastic Leukemia by CALGB, ECOG and SWOG [NCT01256398] | Phase 2 | 66 participants (Actual) | Interventional | 2010-12-14 | Completed | ||
Single Nuclei RNA-sequencing to Map Adipose Cellular Populations and Senescent Cells in Older Subjects [NCT05653258] | Phase 2/Phase 3 | 160 participants (Anticipated) | Interventional | 2023-09-30 | Not yet recruiting | ||
Phase II Trial of Tislelizumab, an Anti-PD-1 Monoclonal Antibody, in Combination With Dasatinib and Quercetin, as a Novel Neoadjuvant Pre-Surgical Therapy for Head and Neck Squamous Cell Carcinoma [NCT05724329] | Phase 2 | 24 participants (Anticipated) | Interventional | 2023-02-05 | Recruiting | ||
A Phase I, Multicenter, Open-label Study of Oral ABL001 in Patients With Chronic Myelogenous Leukemia (CML) or Philadelphia Chromosome-positive Acute Lymphoblastic Leukemia (Ph+ ALL) [NCT02081378] | Phase 1 | 326 participants (Actual) | Interventional | 2014-04-24 | Completed | ||
A Phase I/II Study of BMS-354825 in Subjects With Imatinib Resistant or Intolerant Philadelphia Chromosome Positive Chronic Myelogenous Leukemia and Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia Who Are Resistant or Intolerant to Treatment [NCT00337454] | Phase 1/Phase 2 | 48 participants | Interventional | 2005-07-31 | Completed | ||
Explore the Synergy of Combination TKI Therapy - A Pilot Study to Evaluate the Effect of Imatinib on Dasatinib Pharmacokinetics in Healthy Volunteers [NCT02129166] | Phase 1 | 0 participants (Actual) | Interventional | 2014-09-30 | Withdrawn(stopped due to PI resigned) | ||
A Phase I/II Trial of the Insulin-Like Growth Factor 1 Receptor (IGF-1R) Antibody AMG479 (Ganitumab) in Combination With the Src Family Kinase (SFK) Inhibitor Dasatinib in Patients With Embryonal and Alveolar Rhabdomyosarcoma [NCT03041701] | Phase 1/Phase 2 | 14 participants (Actual) | Interventional | 2017-07-07 | Terminated(stopped due to The pharmaceutical company discontinued availability of the drug and we were forced to close the study before phase II was completed. Only one participant was enrolled on phase II.) | ||
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 | ||
Biomarker and Tumor Cell Culture-Driven Pilot Trial for Treatment of Recurrent Glioblastoma [NCT05432518] | Early Phase 1 | 10 participants (Anticipated) | Interventional | 2023-06-27 | Recruiting | ||
Phase-III Randomized Study to Optimize TKIs Multiple Approaches - (OPTkIMA) - and Quality of Life (QoL) in Elderly Patients (≥60 Years) With Ph+ Chronic Myeloid Leukemia (CML) and MR3.0 / MR4.0 Stable Molecular Response [NCT02326311] | Phase 3 | 502 participants (Anticipated) | Interventional | 2015-06-10 | Recruiting | ||
Phase II Study of Combination of Hyper-CVAD and Dasatinib in Patients With Philadelphia (Ph) Chromosome Positive and/or BCR-ABL Positive Acute Lymphoblastic Leukemia (ALL) [NCT00390793] | Phase 2 | 107 participants (Actual) | Interventional | 2006-09-28 | Active, not recruiting | ||
Asciminib as Initial Therapy for Patients With Chronic Myeloid Leukemia in Chronic Phase With Addition of Lower Dose Tyrosine Kinas Inhibitors for Patients With Chronic Myeloid Leukemia Who do Not Achieve a Deep Molecular Remission [NCT05143840] | Phase 2 | 8 participants (Anticipated) | Interventional | 2022-04-22 | Recruiting | ||
A Phase 2, Fast Real Time Assessment of Combination Therapies in Immuno-Oncology Study in Subjects With Advanced Non-Small Cell Lung Cancer (FRACTION-Lung) [NCT02750514] | Phase 2 | 295 participants (Actual) | Interventional | 2016-05-09 | Terminated(stopped due to The standard of care for the patient population changed and we were unable to accrue any longer.) | ||
Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) Trial: PRIME [NCT03878524] | Phase 1 | 2 participants (Actual) | Interventional | 2020-04-01 | Active, not recruiting | ||
KISS Study: A Phase II Study of Dasatinib Followed by Imatinib in Newly Diagnosed, Previously Untreated Patients With Chronic Phase CML [NCT03193281] | Phase 2 | 91 participants (Actual) | Interventional | 2017-07-17 | Active, not recruiting | ||
Randomized Phase III Study of Intensive Chemotherapy With or Without Dasatinib (Sprycel™) in Adult Patients With Newly Diagnosed Core-Binding Factor Acute Myeloid Leukemia (CBF-AML) [NCT02013648] | Phase 3 | 203 participants (Anticipated) | Interventional | 2014-07-31 | Active, not recruiting | ||
Combination of Autophagy Selective Therapeutics (COAST) in Advanced Solid Tumors or Relapsed Prostate Cancer, A Phase I/II Trial [NCT05036226] | Phase 1/Phase 2 | 76 participants (Anticipated) | Interventional | 2022-03-03 | Recruiting | ||
A Phase I Trial of Dasatinib (Src Inhibitor), Bevacizumab (Anti-VEGF Monoclonal Antibody) and Metronomic Paclitaxel + or - Methylnaltrexone in Patients With Advanced Malignancies [NCT01015222] | Phase 1 | 122 participants (Actual) | Interventional | 2009-11-30 | Completed | ||
Treatment-free Remission Accomplished With Dasatinib in Patients With CML [NCT02268370] | Phase 2 | 131 participants (Actual) | Interventional | 2014-10-31 | Active, not recruiting | ||
Phase II Trial of Dasatinib in Patients With Recurrent Glioblastoma Multiforme [NCT00423735] | Phase 2 | 64 participants (Actual) | Interventional | 2007-01-24 | Completed | ||
An Open-Label, One-Arm, Multi-Site Trial of Precision Diagnosis Directing Target Total Therapy for Adult Ph-like Acute Lymphoblastic Leukemia [NCT03564470] | Phase 2/Phase 3 | 120 participants (Anticipated) | Interventional | 2016-02-14 | Recruiting | ||
A Randomized Phase II Study of Ruxolitinib (NSC-752295) in Combination With BCR-ABL Tyrosine Kinase Inhibitors in Chronic Myeloid Leukemia (CML) Patients With Molecular Evidence of Disease [NCT03654768] | Phase 2 | 84 participants (Anticipated) | Interventional | 2018-10-24 | Active, not recruiting | ||
A Phase I Study of Palbociclib in Combination With Chemotherapy in Pediatric Patients With Relapsed or Refractory Acute Lymphoblastic Leukemia [NCT03515200] | Phase 1 | 12 participants (Actual) | Interventional | 2018-04-20 | Terminated(stopped due to Due to departure of PI from St. Jude) | ||
A Pilot Study of Oral Dasatinib in Subjects With MDS and Excess Marrow Blasts [NCT00624585] | 18 participants (Actual) | Interventional | 2008-02-29 | Completed | |||
A Phase I Study of the Combination of Gemcitabine Plus Dasatinib in Patients With Refractory Solid Tumors With an Expanded Cohort in Advanced Pancreatic Cancer [NCT00598091] | Phase 1 | 30 participants (Actual) | Interventional | 2007-04-30 | Terminated(stopped due to Low accrual, unable to meet endpoint in timely manner) | ||
A Bioequivalence Study Between the Generic Dasatinib Tablet and Reference Product in Vivo [NCT05640804] | Phase 1 | 56 participants (Actual) | Interventional | 2018-09-09 | Completed | ||
A Phase I/II Study of Dasatinib in Relapsed or Refractory Non-Hodgkin's Lymphoma (NHL) (BMS Protocol 180129) [NCT00550615] | Phase 1/Phase 2 | 38 participants (Actual) | Interventional | 2007-09-17 | Completed | ||
Dasatinib (BMS-354825) Combined With SMO Inhibitor (BMS-833923; XL139) in CML With Resistance or Suboptimal Response to a Prior TKI [NCT01218477] | Phase 1/Phase 2 | 33 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
The Life After Stopping Tyrosine Kinase Inhibitors Study (The LAST Study) [NCT02269267] | Phase 2 | 173 participants (Actual) | Interventional | 2014-12-18 | Completed | ||
SEN-SURVIVORS: An Open-Label Intervention Trial to Reduce Senescence and Improve Frailty in Adult Survivors of Childhood Cancer [NCT04733534] | Phase 2 | 60 participants (Anticipated) | Interventional | 2022-06-06 | Recruiting | ||
Prospective Pilot Trial to Assess a Multimodal Molecular Targeted Therapy in Children, Adolescent and Young Adults With Relapsed or Refractory High-grade Pineoblastoma [NCT02596828] | Phase 2 | 4 participants (Actual) | Interventional | 2016-04-30 | Completed | ||
A Phase I/II Study of Dasatinib and Rituximab for Relapsed/Refractory Chronic Lymphocytic Leukemia [NCT00949988] | Phase 1/Phase 2 | 3 participants (Actual) | Interventional | 2009-05-31 | Terminated(stopped due to Three subjects were enrolled and all three subjects withdrew.) | ||
Long-Term Safety and Efficacy of Dasatinib (BMS-354825) in Chronic Myelogenous Leukemia or Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia in Subjects Who Experienced Clinical Benefit on Protocol CA180-002 [NCT00978731] | Phase 1 | 46 participants (Actual) | Interventional | 2005-12-31 | Completed | ||
BMS CA180157: A Phase I Combination Study of Dasatinib Plus Vorinostat in Accelerated Phase, Chronic Phase Refractory to Second Line Therapy or Blast Crisis Chronic Myelogenous Leukemia (CML), and in Philadelphia Chromosome Positive Acute Lymphoblastic Le [NCT00816283] | Phase 1 | 5 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
Frequency and Severity of Pleural Effusion Associated With the Use of Dasatinib in Patients With Chronic Myeloid Leukemia. A Descriptive, Mexican Multicenter Study [NCT02546791] | 101 participants (Actual) | Observational | 2015-07-22 | Completed | |||
An Open-Label, Multi-Center, Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of RO7283420 as a Single Agent in Hematologic and Molecular Relapsed/Refractory Acute Myeloid Leukemia [NCT04580121] | Phase 1 | 59 participants (Actual) | Interventional | 2020-11-04 | Completed | ||
A Phase Ib Adaptive Study Dasatinib for the Prevention of Oxaliplatin-Induced Neuropathy in Patients With Metastatic Gastrointestinal Cancer Receiving FOLFOX Chemotherapy With or Without Bevacizumab [NCT04164069] | Phase 1 | 9 participants (Anticipated) | Interventional | 2020-09-02 | Active, not recruiting | ||
Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR): A Phase II Basket Trial [NCT03297606] | Phase 2 | 720 participants (Anticipated) | Interventional | 2018-03-23 | Recruiting | ||
Study of Dasatinib (BMS-354825) in Subjects With Chronic Myelogenous Leukemia With Accelerated or Myeloid or Lymphoid Blast Phase or Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia Who Are Resistant to or Intolerant of Imatinib Mesylate [NCT00298987] | Phase 2 | 400 participants (Anticipated) | Interventional | 2006-02-28 | Completed | ||
A Pilot Study of Neoadjuvant Dasatinib Followed by Radical Cystectomy for Transitional Cell Carcinoma of the Bladder [NCT00706641] | 25 participants (Actual) | Interventional | 2008-06-30 | Completed | |||
[NCT00454753] | 0 participants | Expanded Access | No longer available | ||||
Phase I/II Study of Dasatinib in Combination With Zoledronic Acid for the Treatment of Breast Cancer With Bone Metastasis [NCT00566618] | Phase 1/Phase 2 | 31 participants (Actual) | Interventional | 2007-11-01 | Completed | ||
Targeting Cellular Senescence With Senolytics to Improve Skeletal Health in Older Humans: A Phase 2, Single-Center, 20-week, Open-Label, Randomized Controlled Trial. [NCT04313634] | Phase 2 | 120 participants (Anticipated) | Interventional | 2020-06-09 | Active, not recruiting | ||
An Open-Label, Multicenter, Phase II Study to Assess Dasatinib in Patients With Core Binding Factors Acute Myelogenous Leukemia Refractory to Conventional Chemotherapy or in Molecular Relapse. Intergroupe Français Des leucémie aiguë myéloblastique [NCT02113319] | Phase 2 | 27 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
Safety and Impact of Dasatinib on Viral Persistence and Inflammation in People With HIV Under Antiretroviral Treatment [NCT05780073] | Phase 2 | 60 participants (Anticipated) | Interventional | 2023-10-16 | Recruiting | ||
Maximal Androgen Depletion Followed by Randomization of Maximal Androgen Ablation With Molecular Targeted Therapies [NCT01254864] | Phase 2 | 190 participants (Actual) | Interventional | 2011-03-16 | Completed | ||
Senolytics To Alleviate Mobility Issues and Neurological Impairment in Aging [NCT05422885] | Phase 1/Phase 2 | 12 participants (Actual) | Interventional | 2022-05-20 | Active, not recruiting | ||
A Phase I Study of Dasatinib With Bortezomib (Velcade®) and Dexamethasone in Subjects With Relapsed or Refractory Multiple Myeloma [NCT00560352] | Phase 1 | 16 participants (Actual) | Interventional | 2008-02-29 | Terminated | ||
Phase I Study of Induction Therapy With Cytarabine, High-Dose Mitoxantrone and Dasatinib for Patients With Philadelphia-Chromosome Positive (Ph+) Acute Lymphoblastic Leukemia (ALL): ALL-6 Protocol [NCT00940524] | Phase 1 | 7 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
A Phase II Study of Blinatumomab and POMP (Prednisone, Vincristine, Methotrexate, 6-Mercaptopurine) for Patients ≥ 65 Years of Age With Newly Diagnosed Philadelphia-Chromosome Negative (Ph-) Acute Lymphoblastic Leukemia (ALL) and of Dasatinib, Prednisone [NCT02143414] | Phase 2 | 53 participants (Actual) | Interventional | 2015-06-30 | Active, not recruiting | ||
A Phase II Trial of Dasatinib in Advanced Sarcomas [NCT00464620] | Phase 2 | 366 participants (Actual) | Interventional | 2007-05-31 | Completed | ||
A Randomized Two-Arm, Multicenter, Open-Label Phase III Study of BMS-354825 Administered Orally at a Dose of 70 mg Twice Daily or 140 mg Once Daily in Subjects With Chronic Myeloid Leukemia in Accelerated Phase or in Myeloid or Lymphoid Blast Phase or Wit [NCT00123487] | Phase 3 | 638 participants (Actual) | Interventional | 2005-06-30 | Completed | ||
A Phase II Study of Dasatinib (NSC 732517) in Previously-Treated Patients With Metastatic Colorectal Cancer [NCT00504153] | Phase 2 | 19 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
Phase I/II Study of Dasatinib and Docetaxel in Metastatic Hormone Refractory Prostate Cancer [NCT00439270] | Phase 1/Phase 2 | 49 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
Total Therapy Study XVI for Newly Diagnosed Patients With Acute Lymphoblastic Leukemia [NCT00549848] | Phase 3 | 600 participants (Actual) | Interventional | 2007-10-29 | Completed | ||
A Randomized, Multicenter, Open-label Phase II Study of Dasatinib (BMS-354825) Administered Orally at a Dose of 50mg Twice Daily or 100mg Once Daily in Subjects With Chronic Phase Philadelphia Chromosome Positive Chronic Myeloid Leukemia Who Are Resistant [NCT00482703] | Phase 1/Phase 2 | 23 participants (Actual) | Interventional | 2007-05-31 | Completed | ||
Multicenter, Open-Label, Single Arm Phase II Clinical Trial of Dasatinib in the Treatment of Systemic Mastocytosis [NCT00979160] | Phase 2 | 30 participants (Anticipated) | Interventional | 2009-11-30 | Not yet recruiting | ||
A Phase 2 Trial of Dasatinib in Patients With Lung Adenocarcinoma With Acquired Resistance to Erlotinib or Gefitinib [NCT00570401] | Phase 2 | 22 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
Phase II Study of Dasatinib (BMS-354825) for Advanced 'Triple-negative' Breast Cancer [NCT00371254] | Phase 2 | 55 participants (Actual) | Interventional | 2006-12-31 | Completed | ||
Phase I Study of Dasatinib (BMS-354825) and Capecitabine for Advanced Breast Cancer [NCT00452673] | Phase 1 | 52 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
A Phase II Trial of Genomic Guided Therapy With Dasatinib or Nilutamide in Metastatic Castration-Resistant Prostate Cancer [NCT00918385] | Phase 2 | 57 participants (Actual) | Interventional | 2009-05-31 | Terminated(stopped due to Permanent closure of trial to further accrual based on IDE disapproval) | ||
A Phase 2 Study of Dasatinib in Advanced Melanoma [NCT00436605] | Phase 2 | 39 participants (Actual) | Interventional | 2006-12-31 | Completed | ||
A Phase I/II Trial of Dasatinib in Combination With Trastuzumab and Paclitaxel in the First Line Treatment of Her2-Positive Metastatic Breast Cancer (MBC) Patients [NCT01306942] | Phase 1/Phase 2 | 37 participants (Actual) | Interventional | 2011-07-31 | Completed | ||
Randomized Phase II of Lomustine Versus Lomustine-Dasatinib in Patients With Recurrent Glioblastoma [NCT00948389] | Phase 1/Phase 2 | 28 participants (Actual) | Interventional | 2009-10-31 | Terminated(stopped due to Inability to meet protocol objectives) | ||
A Prospective, Single-arm, Multi-center Clinical Trial Evaluating the Efficacy and Safety of Dasatinib in RefrActory MetAstatic Gastrointestinal Stromal Tumor [NCT02776878] | 57 participants (Anticipated) | Interventional | 2016-05-31 | Recruiting | |||
Phase II Efficacy and Safety Study of Dasatinib in Patients With Chronic and Accelerated Phase Chronic Myeloid Leukemia Relapsing After Allogeneic Blood or Bone Marrow Transplantation [NCT00895297] | Phase 2 | 50 participants (Anticipated) | Interventional | 2010-02-28 | Terminated(stopped due to Slow recruitment. No safety concerns during this study.) | ||
D-ALBA Front-Line Sequential Treatment of Adult Philadelphia Chromosome Positive (Ph+) Acute Lymphoblastic Leukemia (ALL) Patients With Dasatinib and the Bispecific Monoclonal Antibody Blinatumomab [NCT02744768] | Phase 2 | 60 participants (Anticipated) | Interventional | 2017-05-31 | Recruiting | ||
Genomics-Based Target Therapy for Children With Relapsed or Refractory Malignancy [NCT02638428] | Phase 2 | 90 participants (Anticipated) | Interventional | 2015-12-31 | Recruiting | ||
A Phase Ib Feasibility Study of Personalized Kinase Inhibitor Therapy Combined With Induction in Acute Leukemias Who Exhibit In Vitro Kinase Inhibitor Sensitivity [NCT02779283] | Phase 1 | 7 participants (Actual) | Interventional | 2016-01-13 | Completed | ||
Randomized, Open-Label, Phase II, Multicenter, Multi-Country Study to Evaluate Safety and Efficacy of Dasatinib 50 mg in First-Line Treatment of Early Chronic Phase Chronic Myeloid Leukemia [NCT03625388] | Phase 2 | 56 participants (Actual) | Interventional | 2018-11-05 | Completed | ||
Phase II Study of Dasatinib in Non Small Cell Lung Cancer [NCT00459342] | Phase 2 | 35 participants (Actual) | Interventional | 2007-03-31 | Completed | ||
A Phase II Trial of Dasatinib (BMS-354825) in Advanced Hepatocellular Carcinoma [NCT00459108] | Phase 2 | 25 participants (Actual) | Interventional | 2007-04-30 | Terminated(stopped due to Halted early for futility.) | ||
Pilot Study to Test the Safety and Efficacy of Metformin, Dasatinib, Rapamycin and Nutritional Supplements (Bio-quercetin; Bio-fisetin; Glucosamine; Nicotinamide Riboside; Trans-resveratrol) in Reducing Clinical Measures of Aging in Older Adults [NCT04994561] | Phase 1 | 0 participants (Actual) | Interventional | 2022-06-30 | Withdrawn(stopped due to Study was withdrawn) | ||
Front-line Treatment of BCR-ABL+ Chronic Myeloid Leukemia (CML) With Dasatinib. An Observational Multicentric Study. [NCT01761890] | 147 participants (Actual) | Observational | 2014-01-28 | Active, not recruiting | |||
A Phase 1 Study of ABL001 in Combination With Dasatinib, Prednisone, and Blinatumomab in Patients With BCR-ABL Positive (BCR-ABL+) B-cell Acute Lymphoblastic Leukemia (B-ALL) and Chronic Myeloid Leukemia (CML) [NCT03595917] | Phase 1 | 40 participants (Anticipated) | Interventional | 2018-07-24 | Recruiting | ||
Phase II Trial of Dasatinib (BMS 354825) for Recurrent or Metastatic c-KIT Expressing Adenoid Cystic Carcinoma and Non-adenoid Cystic Malignant Salivary Tumors [NCT00859937] | Phase 2 | 55 participants (Actual) | Interventional | 2009-03-16 | Completed | ||
A Randomized, Double-Blind, Multi-Center Phase II Trial of Exemestane (Aromasin®) Plus Dasatinib Versus Exemestane Plus Placebo in Advanced Estrogen Receptor-Positive Breast Cancer After Disease Progression on a Non-Steroidal Aromatase Inhibitor (NSAI) [NCT00767520] | Phase 2 | 155 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
A Preoperative Biological Trial of Cetuximab, Dasatinib or the Combination in Colorectal Cancer Patients With Resectable Liver Metastases [NCT00835679] | Early Phase 1 | 9 participants (Actual) | Interventional | 2009-12-31 | Terminated | ||
A Phase I-II Study of Dasatinib in Combination With Weekly Paclitaxel for Patients With Metastatic Breast Carcinoma [NCT00820170] | Phase 1/Phase 2 | 55 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
A Phase II Evaluation of Dasatinib (Sprycel®, NSC #732517) in the Treatment of Persistent or Recurrent Epithelial Ovarian, Fallopian Tube, or Primary Peritoneal Carcinoma [NCT00671788] | Phase 2 | 35 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
A Prospective Study on Early Conversion of Dasatinib in CML-CP Patients Who Have Not Early Molecular Response on Imatinib [NCT04136015] | 200 participants (Anticipated) | Observational | 2019-10-22 | Enrolling by invitation | |||
Dasatinib in Combination With Chemotherapy for Relapsed or Refractory Core Binding Factor Acute Myeloid Leukemia: A Phase I Study (AflacLL1401) [NCT02680951] | Phase 1 | 0 participants (Actual) | Interventional | 2015-12-31 | Withdrawn(stopped due to Withdrawn due to lack of participants.) | ||
SENolytics to Improve Osteoporosis Therapy: a Randomised Controlled Clinical Trial The SENIOR Trial [NCT06018467] | Phase 2 | 120 participants (Anticipated) | Interventional | 2023-09-06 | Recruiting | ||
A Phase I Study of Ixabepilone Combined With Dasatinib in Patients With Solid Tumors [NCT00717704] | Phase 1 | 19 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
Open-label, Non-randomized, Two-treatment, Single-period, Single Dose, Drug-drug Interaction Study to Evaluate the Effects of Omeprazole 40mg on the Pharmacokinetics of SPRYCEL® 100 mg Film-coated Tablets (Dasatinib) in Adult Human Subjects [NCT06145217] | Phase 1 | 18 participants (Actual) | Interventional | 2023-08-22 | Completed | ||
A Phase I Study of Dasatinib, Cetuximab and Radiation With or Without Cisplatin in Locally Advanced Squamous Cell Carcinoma of Head and Neck (HNSCC) [NCT00882583] | Phase 1 | 22 participants (Actual) | Interventional | 2009-07-31 | Terminated(stopped due to Low accrual) | ||
A Phase I Study of Capecitabine, Oxaliplatin, Bevacizumab, and Dasatinib for Patients With Advanced Solid Tumors With Expanded Cohort of Patients With Previously Untreated Metastatic Colorectal Cancer. [NCT00920868] | Phase 1 | 22 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
A Phase I Trial of A SRC Kinase Inhibitor, Dasatinib,in Combination With Paclitaxel and Carboplatin in Patients With Advanced or Recurrent Ovarian, Peritoneal, and Tubal Cancer [NCT00672295] | Phase 1 | 11 participants (Actual) | Interventional | 2007-08-31 | Completed | ||
Randomized Phase II Trial of Letrozole With or Without Dasatinib as First and Second-line Treatment for Hormone Receptor-positive, HER2-negative Post-menopausal Breast Cancer That is Unresectable, Locally Recurrent or Metastatic [NCT00696072] | Phase 2 | 120 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
Phase I/II Trial of Dasatinib (Sprycel) With Radiation Therapy and Concomitant and Adjuvant Temozolomide in Patients With Newly-Diagnosed Glioblastoma [NCT00895960] | Phase 1 | 16 participants (Actual) | Interventional | 2009-05-07 | Terminated(stopped due to Sponsor withdrew support; Study did not progress to Phase II.) | ||
Phase II Study of Dasatinib in Advanced Non-small Cell Lung Cancer With Ex Vivo and In Vivo Assessment of Tumor Target Modulation [NCT00858403] | Phase 2 | 7 participants (Actual) | Interventional | 2009-03-31 | Terminated(stopped due to Slow Accrual) | ||
Phase I Pharmacokinetic Study of Dasatinib (BMS-354825) (NSC-732517) in Patients With Advanced Malignancies and Varying Levels of Liver Dysfunction [NCT00608361] | Phase 1 | 80 participants (Actual) | Interventional | 2008-10-31 | Completed | ||
A Phase I/II Study of Combination Dasatinib and Lenalidomide in Purine Analogue-Failed Chronic Lymphocytic Leukemia [NCT00829647] | Phase 1/Phase 2 | 0 participants (Actual) | Interventional | 2009-01-31 | Withdrawn(stopped due to Unable to enroll) | ||
Phase I Study of Dasatinib Plus Erlotinib in Recurrent Malignant Glioma [NCT00609999] | Phase 1 | 47 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
Randomized, Open Label Study of Dasatinib (100mg qd) vs. High-Dose Imatinib (600mg) in Patients With Chronic Phase CML Who Have Had Suboptimal Response After 3-18 Months of Therapy With Imatinib (400mg) [NCT00854841] | 0 participants | Expanded Access | Available | ||||
Phase II Study Assessing Safety and Clinical Activity of the Combination of ASTX727 With Dasatinib in Patients With Newly Diagnosed Chronic Myeloid Leukemia in Chronic Phase (CML-CP) [NCT05007873] | Phase 2 | 70 participants (Anticipated) | Interventional | 2021-10-21 | Recruiting | ||
Safety, Tolerance and Antiretroviral Activity of Dasatinib: a Pilot Clinical Trial in Patients With Recent HIV-1 Infection [NCT05527418] | Phase 2 | 24 participants (Anticipated) | Interventional | 2023-11-30 | Not yet recruiting | ||
A Pre-Surgical Study to Evaluate Molecular Changes That Occur in Human Breast Cancer Tissue After Short Term Exposure to Dasatinib and To Correlate These Alterations With Pharmacokinetics Parameters [NCT01410708] | Phase 2 | 0 participants (Actual) | Interventional | Withdrawn | |||
Preliminary Evaluation of TKI Exposure-response Relationships in Real World Patients (RWPs) With Chronic Myelogenous Leukemia (CML) [NCT03885830] | 45 participants (Actual) | Observational | 2019-06-20 | Completed | |||
Open-Label, Multicenter Phase Ib/IIa Study For the Evaluation of Dasatinib (Sprycel™) Following Induction and Consolida-tion Therapy as Well as in Maintenance Therapy in Patients With Newly Diagnosed Core Binding Factor (CBF) Acute Myeloid Leukemia (AML) [NCT00850382] | Phase 1/Phase 2 | 89 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
Phase I Study of the Combination of Vandetanib and Dasatinib Administered During and After Radiation Therapy in Children With Diffuse Intrinsic Pontine Glioma [NCT00996723] | Phase 1 | 25 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
A Phase 1, Open-label, Dose-escalation Study of Dasatinib and All-Trans Retinoic Acid for Relapsed/Refractory and/or Elderly Patients With Acute Myelogenous Leukemia or Myelodysplastic Syndrome [NCT00892190] | Phase 1 | 9 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
A Phase II Study of Biological Response to Dasatinib Treatment in Patients With Acral Lentiginous, Mucosal, or Chronic Sun-damaged Melanoma [NCT01092728] | Phase 2 | 19 participants (Actual) | Interventional | 2011-03-31 | Terminated(stopped due to Slow accrual.) | ||
A Phase II Study of Neoadjuvant Dasatinib Plus LHRH Analogue Therapy in High-Risk Localized Prostate Cancer [NCT00860158] | Phase 2 | 1 participants (Actual) | Interventional | 2009-03-31 | Terminated(stopped due to Slow accrual; closed by funder) | ||
A Phase 1 Study of Combining Ibrutinib, Dasatinib and Prednisone in Patients 60 Years or Older With Philadelphia Chromosome-positive Acute Lymphoblastic Leukemia [NCT02815059] | Phase 1 | 0 participants (Actual) | Interventional | 2016-09-28 | Withdrawn(stopped due to Termination of Investigator Initiated Studies using Ibrutinib) | ||
The Combination of Lower Dosage of Chemotherapy With Tyrosine Kinase Inhibitor to Treat Newly Diagnosed ph+ Acute Lymphoblastic Leukemia Patients [NCT02690922] | Phase 4 | 40 participants (Anticipated) | Interventional | 2016-03-31 | Not yet recruiting | ||
A Phase I-II, Randomization, Open-Label Clinical Trial of Fulvestrant Versus the Combination of Fulvestrant, MK-0646, and Dasatinib as First-Line Therapy for Metastatic Hormone Receptor-Positive HER2-Negative Breast Cancer [NCT00903006] | Phase 1/Phase 2 | 11 participants (Actual) | Interventional | 2009-11-30 | Terminated(stopped due to Low Accrual) | ||
The Effect of Omeprazole on the Pharmacokinetics of Dasatinib (BMS-354825) in Healthy Subjects [NCT00655746] | Phase 1 | 14 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
A Phase I Single Arm Dose Escalation Study of the Combination of Dasatinib (Sprycel®) With Lenalidomide (Revlimid®) and Dexamethasone in Subjects With Relapsed and/ or Refractory Multiple Myeloma [NCT00560391] | Phase 1 | 35 participants (Actual) | Interventional | 2008-05-31 | Completed | ||
Intensified Tyrosine Kinase Inhibitor Therapy (Dasatinib NSC# 732517) in Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia (ALL) [NCT00720109] | Phase 2/Phase 3 | 63 participants (Actual) | Interventional | 2008-07-14 | Completed | ||
A Study to Document the Long-Term Safety and Efficacy of BMS-354825 in Subjects With Imatinib Resistant or Intolerant Chronic Myelogenous Leukemia and Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia Who Are Resistant or Intolerant to Previou [NCT01030718] | Phase 1/Phase 2 | 54 participants (Actual) | Interventional | 2006-01-31 | Completed | ||
Phase II Randomized Trial of Fulvestrant With or Without Dasatinib in Men and Postmenopausal Women Who Have Hormone Receptor-positive Advanced Breast Cancer Previously Treated With an Aromatase Inhibitor [NCT00754325] | Phase 2 | 100 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
A Randomized Double-Blind Phase 3 Trial Comparing Docetaxel Combined With Dasatinib to Docetaxel Combined With Placebo in Castration-Resistant Prostate Cancer [NCT00744497] | Phase 3 | 1,930 participants (Actual) | Interventional | 2008-10-31 | Completed | ||
A Phase II Trial of DCTD-Sponsored Dasatinib in Recurrent/Persistent Ovary, Fallopian Tube, Primary Peritoneal, and Endometrial Clear Cell Carcinoma Characterized for the Retention or Loss of BAF250a Expression [NCT02059265] | Phase 2 | 35 participants (Actual) | Interventional | 2014-02-14 | Terminated(stopped due to Interim monitoring) | ||
Phase I Study to Evaluate the Safety of Zileuton (Zyflo®) in Combination With Dasatinib (Sprycel®) in Patients With Chronic Myelogenous Leukemia [NCT02047149] | Phase 1 | 2 participants (Actual) | Interventional | 2014-01-31 | Terminated(stopped due to Low accrual) | ||
A Phase II Study of Dasatinib in Patients With Imatinib Resistant or Intolerant Chronic Myeloid Leukemia [NCT00866736] | Phase 2 | 65 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
A Phase 2 Study of Dasatinib in Head and Neck Squamous Cell Carcinoma [NCT00507767] | Phase 2 | 15 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
A Phase I Dose-Escalation Study of Erlotinib in Combination With Dasatinib in Subjects With Advanced Cancer. Companion Study to Umbrella Protocol 2007-0638. [NCT00895128] | Phase 1 | 65 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
A Phase II Study to Determine the Activity of Dasatinib Administered Orally (PO) at a Dose of 100 mg Once Daily (QD) in Chronic Phase Chronic Myelogenous Leukemia (CML), at a Dose of 70 mg Twice Daily (BID) in Advanced Phase Chronic Myelogenous Leukemia ( [NCT00529763] | Phase 2 | 121 participants (Actual) | Interventional | 2007-11-17 | Completed | ||
Safety And Efficacy Of Tyrosine Kinase Inhibitor Cessation For Chronic Myeloid Leukemia Patients With Stable Molecular Response In A Real World Population [NCT04626024] | Phase 2 | 100 participants (Anticipated) | Interventional | 2020-12-22 | Recruiting | ||
A Phase I Study of BMS-354825 in Patients With Solid Tumors [NCT00339144] | Phase 1 | 16 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
An Open-label, Randomized Study of Dasatinib vs High-dose (800-mg) Imatinib in the Treatment of Subjects With Chronic Phase Chronic Myeloid Leukemia Who Have Had a Suboptimal Response After at Least 3 Months of Therapy With 400 mg Imatinib [NCT00320190] | Phase 2 | 52 participants (Actual) | Interventional | 2006-08-31 | Terminated(stopped due to Terminated due to slow participant accrual) | ||
An Open-Label, Randomized, Multicenter Phase III Trial of Dasatinib (SPRYCEL®) vs. Standard Dose Imatinib (400 mg) in the Treatment of Subjects With Newly Diagnosed Chronic Phase Philadelphia Chromosome Positive Chronic Myeloid Leukemia [NCT00481247] | Phase 3 | 547 participants (Actual) | Interventional | 2007-09-30 | Completed | ||
PhaseⅡClinical Trial of Dasatinib for Patients With Newly Diagnosed Chronic Myeloid Leukemia in Chronic Phase and Stop Therapy After Achieving Complete Molecular Response for Cure D-NewS [NCT01887561] | Phase 2 | 100 participants (Anticipated) | Interventional | 2012-11-30 | Recruiting | ||
A PROSPECTIVE RANDOMIZED PHASE II STUDY EVALUATING THE OPTIMIZATION OF THE RESIDUAL PLASMATIC LEVEL OF DASATINIB (SPRYCEL®) IN PATIENTS NEWLY DIAGNOSED WITH CHRONIC PHASE CHRONIC MYELOGENOUS LEUKAEMIA (CP-CML). [NCT01916785] | Phase 2 | 289 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
Therapy of Early Chronic Phase Chronic Myelogenous Leukemia (CML) With Dasatinib (BMS-354825) [NCT00254423] | Phase 2 | 156 participants (Actual) | Interventional | 2005-11-08 | Active, not recruiting | ||
An Open Label, Non-Randomized, Two-Treatment, Single-Period, Single-Dose, Drug-Drug Interaction Study to Evaluate the Effects of Omeprazole on the Pharmacokinetics of XS004 (Dasatinib) 90 mg Film-Coated Tablets in Healthy Adult Subjects Under Fasting Cond [NCT05433896] | Phase 1 | 17 participants (Actual) | Interventional | 2020-11-01 | Completed | ||
Dasatinib First-Line Treatment in Gastrointestinal Stromal Tumors. A Multi Center Phase II Trial [NCT00568750] | Phase 2 | 47 participants (Actual) | Interventional | 2008-01-22 | Completed | ||
A Phase II Trial of Dasatinib in KIT-Positive Patients With Unresectable Locally Advanced or Stage IV Mucosal, Acral and Vulvovaginal Melanomas [NCT00700882] | Phase 2 | 81 participants (Actual) | Interventional | 2009-07-02 | Completed | ||
The Feasibility of Selecting Patient-Specific Biologically Targeted Therapy With Sorafenib, Everolimus, Erlotinib or Dasatinib for Pediatric Patients With Refractory Or Recurrent Brain Tumors [NCT02015728] | 20 participants (Anticipated) | Interventional | 2013-12-31 | Active, not recruiting | |||
Phase I-II Study of Ruxolitinib (INCB18424) for Patients With Chronic Myeloid Leukemia (CML) With Minimal Residual Disease While on Therapy With Tyrosine Kinase Inhibitors [NCT01751425] | Phase 1 | 8 participants (Actual) | Interventional | 2013-07-24 | Terminated(stopped due to Per PI Request. 2) No additional benefit was noted with the addition of Ruxolitinib.) | ||
Clinical Trial for the Safety and Efficacy of CD19/BCMA-targeted CAR-T Cells Combined With Dasatinib for Patients With Relapsed and/or Refractory B-cell Acute Lymphoblastic Leukemia, B-cell Non-Hodgkin's Lymphoma and Multiple Myeloma [NCT04603872] | Early Phase 1 | 120 participants (Anticipated) | Interventional | 2020-11-01 | Recruiting | ||
Phase II Study of Dasatinib (BMS-354825) in Patients With Metastatic Adenocarcinoma of the Pancreas [NCT00474812] | Phase 2 | 51 participants (Actual) | Interventional | 2007-05-31 | Completed | ||
A Phase II Study of Dasatinib (NSC #732517) in Patients With Chemo-Sensitive Relapsed Small Cell Lung Cancer [NCT00470054] | Phase 2 | 44 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
Phase I Study of Dasatinib in Recipients of Allogeneic Stem Cell Transplantation for Hematologic Malignancies. [NCT01643603] | Phase 1 | 5 participants (Actual) | Interventional | 2012-05-31 | Terminated(stopped due to Study terminated due to slow accrual.) | ||
Phase I Study of the Combination of Crizotinib and Dasatinib in Pediatric Research Participants With Diffuse Pontine Glioma (DIPG) and High-Grade Glioma (HGG) [NCT01644773] | Phase 1 | 36 participants (Actual) | Interventional | 2012-11-27 | Completed | ||
Phase II Trial of Dasatinib With Fludarabine and Rituximab in Relapsed and Refractory Chronic Lymphocytic Leukemia and Small Lymphocytic Lymphoma [NCT01173679] | Phase 2 | 10 participants (Actual) | Interventional | 2010-07-31 | Terminated(stopped due to Slow accrual) | ||
An Open-Label, Randomized, Multicenter Phase 2 Trial of Dasatinib (SPRYCEL®) vs. Dasatinib Plus Smoothened Antagonist (BMS-833923) in the Treatment of Subjects With Newly Diagnosed Chronic Phase Philadelphia Chromosome Positive Chronic Myeloid Leukemia (C [NCT01357655] | Phase 2 | 70 participants (Actual) | Interventional | 2011-09-30 | Terminated(stopped due to No participants enrolled in this trial could receive the SMO antagonist as a recommended phase 2 dose was not determined by a different, concurrently-run trial.) | ||
Pilot Study to Investigate the Safety and Feasibility of Senolytic Therapy to Modulate Progression of Alzheimer's Disease (SToMP-AD) [NCT04063124] | Phase 1/Phase 2 | 5 participants (Actual) | Interventional | 2020-02-14 | Completed | ||
Phase 1 Trial of Dasatinib and Bendamustine in Chronic Lymphocytic Leukemia [NCT00872976] | Phase 1 | 0 participants (Actual) | Interventional | 2009-05-31 | Withdrawn(stopped due to Business Objectives Changed) | ||
A Phase 2 Multicenter Study of First-line Dasatinib Plus Conventional Chemotherapy in Adults With Newly Diagnosed Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia [NCT01004497] | Phase 2 | 51 participants (Actual) | Interventional | 2010-03-31 | Completed | ||
Clinical Research for Azacitidine Combined With Low-dose Dasatinib in Maintenance Therapy of Acute Myeloid Leukemia [NCT05042531] | 30 participants (Anticipated) | Interventional | 2021-11-13 | Recruiting | |||
Phase I-II Study of Dasatinib and Erlotinib in Non-Small Cell Lung Cancer [NCT00826449] | Phase 1/Phase 2 | 53 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
Phase I Trial of the Combination of Dasatinib and Lapatinib [NCT00662636] | Phase 1 | 27 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
Assessment of Metabolic Outcomes Among Patients With Chronic Myelogenous Leukemia (CML) Initiating Therapy With a Tyrosine Kinase Inhibitor (TKI) [NCT02733445] | 2,650 participants (Actual) | Observational | 2015-12-31 | Completed | |||
An Open Label Phase II Study to Evaluate the Efficacy and Safety of Induction and Consolidation Therapy With Dasatinib in Combination With Chemotherapy in Patients Aged 55 Years and Over With Philadelphia Chromosome Positive (Ph+ or BCR-ABL+) Acute Lympho [NCT02888990] | Phase 2 | 71 participants (Actual) | Interventional | 2007-08-31 | Completed | ||
Phase I/Randomized Phase II Trial of Either Dasatinib or Placebo Combined With Standard Chemo-Radiotherapy for Newly Diagnosed Glioblastoma Multiforme (GBM) [NCT00869401] | Phase 1/Phase 2 | 217 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
A Biologic Efficacy Study of Dasatinib, a Multi-Targeted Tyrosine Kinase, in Locally Advanced Triple-Negative Breast Cancer Patients Developing Effective Therapies for Er-Negative Breast Cancer Using Genomics and Proteomics: Project 3 [NCT00817531] | Phase 2 | 22 participants (Actual) | Interventional | 2008-12-31 | Terminated(stopped due to terminated due to futility after interim analysis) | ||
Phase I/Randomized Phase II Double Blind Study of Either Dasatinib or Placebo Combined With Bevacizumab in Recurrent Glioblastoma [NCT00892177] | Phase 2 | 144 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
Multicenter, Open-label, Non-randomized Phase II Trial of Dasatinib in Patients With Chronic Myeloid Leukemia in Chronic Phase (CP-CML) Who Meet Criteria for Late Suboptimal Response After Prior Imatinib Treatment [NCT01802450] | Phase 2 | 18 participants (Actual) | Interventional | 2013-03-31 | Active, not recruiting | ||
Retrospective, Non-interventional Study to Evaluate Chronic Myeloid Leukemia Treatment Landscape and Real-life Treatment Outcomes in Hungary: Analysis of National Health Insurance Fund Database [NCT05286528] | 1,484 participants (Actual) | Observational | 2020-11-18 | Completed | |||
Effects of Gastric pH on the Pharmacokinetics of Dasatinib in Healthy Volunteers [NCT01398046] | Phase 1 | 10 participants (Actual) | Interventional | 2011-08-31 | Completed | ||
Exploiting Synergy in Chronic Myelogenous Leukemia: A Phase Ib Evaluation of Dasatinib Plus Cyclosporine in Patients With Ph+ Leukemia (ESCAPE1b) [NCT01426334] | Phase 1 | 4 participants (Actual) | Interventional | 2011-09-30 | Terminated | ||
An Open-Label, Randomized, Multicenter Phase II Trial Comparing the Depletion of Malignant Stem Cells With Dasatinib vs. Imatinib in Patients With Newly Diagnosed Chronic Phase Chronic Myeloid [NCT00852566] | Phase 2 | 46 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
Phase II Study of Dasatinib in Previously Treated Patients With Advanced Non-Small Cell Lung Cancer (NSCLC) [NCT00787267] | Phase 2 | 37 participants (Actual) | Interventional | 2008-09-30 | Terminated(stopped due to Poor accrual) | ||
Targeted Removal of Pro-Inflammatory Cells: An Open Label Human Pilot Study in Idiopathic Pulmonary Fibrosis [NCT02874989] | Phase 1 | 26 participants (Actual) | Interventional | 2016-12-16 | Completed | ||
Prospective Non-randomized Stratified Study of REduction And DIscontinuation Treatment of TKI (Imatinib, Nilotinib, Dasatinib and Bosutinib) in Adults With Ph+ Chronic Myeloid Leukemia With Stable Deep Molecular Response [NCT04578847] | Phase 2 | 100 participants (Anticipated) | Interventional | 2020-01-15 | Active, not recruiting | ||
Discontinuation of Dasatinib in Patients With Chronic Myeloid Leukemia in Chronic Phase Who Have Maintained Complete Molecular Remission for Two Years; Dasatinib Stop Trial [NCT01627132] | Phase 2 | 50 participants (Anticipated) | Interventional | 2012-02-29 | Recruiting | ||
[NCT01872442] | Phase 2 | 0 participants | Interventional | 2013-10-15 | Completed | ||
Dasatinib Plus Quercetin for Accelerated Aging in Mental Disorders [NCT05838560] | Phase 2 | 40 participants (Anticipated) | Interventional | 2023-07-01 | Recruiting | ||
An Open Label, Multi-center Asciminib Roll-over Study to Assess Long-term Safety in Patients Who Have Completed a Novartis Sponsored Asciminib Study and Are Judged by the Investigator to Benefit From Continued Treatment [NCT04877522] | Phase 4 | 347 participants (Anticipated) | Interventional | 2022-08-30 | Recruiting | ||
Placebo-controlled Double-blind Trial of Dasatinib Added to Gemcitabine for Subjects With Locally-advanced Pancreatic Cancer [NCT01395017] | Phase 2 | 202 participants (Actual) | Interventional | 2011-06-30 | Completed | ||
Phase II Study Evaluating The Safety And Response To Neoadjuvant Dasatinib In Early Stage Non-Small Cell Lung Cancer (NSCLC). [NCT00564876] | Phase 2 | 2 participants (Actual) | Interventional | 2007-11-30 | Terminated(stopped due to Lack of accrual, study closed.) | ||
A Phase II, Non-Randomized Study of the Use of Desatinib (Sprycel) in Treating Patients With Polycythemia Vera (PV) BMS Protocol Number: CA180-104 [NCT00538980] | Phase 2 | 10 participants (Actual) | Interventional | 2007-04-30 | Terminated(stopped due to This study was terminated due to lack of efficacy.) | ||
Single-Dose Pharmacokinetics of Dasatinib in Subjects With Hepatic Impairment Compared to Healthy Adult Subjects [NCT00382668] | 40 participants (Anticipated) | Observational | 2006-10-31 | Completed | |||
A Safety and Efficacy Study of Adding Low Dose Pegylated IFN-alpha 2B to Standard Dose Dasatinib in Patients With Newly Diagnosed Chronic Phase Myeloid Leukemia [NCT01725204] | Phase 2 | 40 participants (Actual) | Interventional | 2012-09-30 | Completed | ||
Phase I Trial Evaluating the Epidermal Growth Factor Receptor Inhibitor Erlotinib in Combination With the SRC Kinase Inhibitor Dasatinib for Patients With Recurrent Non-small Cell Lung Cancer (NSCLC) [NCT00444015] | Phase 1 | 34 participants (Actual) | Interventional | 2007-03-31 | Completed | ||
Dasatinib in Chronic Myelogenous Leukemia or Philadelphia Chromosome Positive Acute Lymphoblastic Leukemic Subjects Who Are Experiencing Clinical Benefit on Current START or CA180-039 Protocols: Long Term Safety and Efficacy Analysis [NCT00982488] | Phase 2 | 238 participants (Actual) | Interventional | 2007-10-31 | Completed | ||
A Phase I Dose Escalation of MK0457 in Combination With Dasatinib in Patients With Chronic Myelogenous Leukemia and Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia [NCT00500006] | Phase 1 | 3 participants (Actual) | Interventional | 2007-10-31 | Terminated | ||
Allogeneic Nonmyeloablative Hematopoietic Stem Cell Transplant for Patients With BCR-ABL Tyrosine Kinase Inhibitor Responsive Ph+ Acute Leukemia ? A Multi-center Trial [NCT00036738] | Phase 2 | 28 participants (Actual) | Interventional | 2001-07-13 | Completed | ||
A Phase Ib/IIa Single-arm, Open-label Clinical Trial to Evaluate the Safety, Pharmacokinetics, and Efficacy of BP1001 (a Liposomal Grb2 Antisense Oligonucleotide) in Combination With Dasatinib in Patients With Philadelphia Chromosome Positive (Ph+) Chroni [NCT02923986] | Phase 1/Phase 2 | 0 participants (Actual) | Interventional | 2017-09-01 | Withdrawn(stopped due to No enrollment) | ||
A Randomized International Phase 3 Trial of Imatinib and Chemotherapy With or Without Blinatumomab in Patients With Newly-Diagnosed Philadelphia Chromosome-Positive or Philadelphia Chromosome-Like ABL-Class B-Cell Acute Lymphoblastic Leukemia [NCT06124157] | Phase 3 | 680 participants (Anticipated) | Interventional | 2024-01-22 | Not yet recruiting | ||
A Phase I Study of Dasatinib in Combination With Bevacizumab in Advanced Solid Tumors [NCT01445509] | Phase 1 | 50 participants (Actual) | Interventional | 2008-12-29 | Completed | ||
A Phase 0 Pharmacodynamic Study of Dasatinib in Women With Newly Diagnosed Endometrial Cancer [NCT01482728] | Early Phase 1 | 12 participants (Actual) | Interventional | 2012-01-31 | Completed | ||
An Open-Label, Multicenter, Phase 1b/2 Study of the Safety and Efficacy of KRT-232 Combined With a Tyrosine Kinase Inhibitor (TKI) in Patients With Relapsed or Refractory Ph+ Chronic Myeloid Leukemia (CML) [NCT04835584] | Phase 1/Phase 2 | 109 participants (Anticipated) | Interventional | 2021-05-07 | Recruiting | ||
A Phase I Dose-Escalation Study of BMS-354825 in Patients With Refractory Solid Tumors [NCT00099606] | Phase 1 | 60 participants | Interventional | 2004-07-31 | Completed | ||
Phase I Study of BMS-354825 in Patients With Chronic Accelerated, or Blast Phase Chronic Myelogenous Leukemia or Philadelphia Positive Acute Lymphoblastic Leukemia [NCT00103701] | Phase 1 | 0 participants | Interventional | 2003-11-30 | Completed | ||
A Dose-Finding Phase Ib Study of the Oral BCL-2 Inhibitor Venetoclax (ABT-199) in Combination With Standard Induction Therapy, Dasatinib, Prednisone, (and Rituximab in CD20+ Patients) in Adult Patients With Newly Diagnosed and Relapsed Philadelphia Chromo [NCT04872790] | Phase 1 | 20 participants (Anticipated) | Interventional | 2022-09-02 | Recruiting | ||
A Phase 2 Study of Dasatinib in Combination With Everolimus for Children With Gliomas Harboring PDGFR Alterations [NCT03352427] | Phase 2 | 3 participants (Actual) | Interventional | 2017-12-06 | Terminated(stopped due to Low accrual) | ||
Long-Term Safety and Efficacy of Dasatinib (BMS-354825) in Subjects Who Experienced Clinical Benefit on Protocol CA 180-002 [NCT00345826] | Phase 1 | 19 participants (Actual) | Interventional | 2005-11-30 | Completed | ||
A Randomized Multi-Center Open Label Study of BMS-354825 vs Imatinib Mesylate (Gleevec®) 800 mg/d in Subjects With Chronic Phase Philadelphia Chromosome-Positive Chronic Myeloid Leukemia Who Have Disease That is Resistant to Iamtinib at a Dose of 400-600 [NCT00112775] | Phase 2 | 0 participants | Interventional | 2005-03-31 | Active, not recruiting | ||
A Randomized Multi-Center Open Label Study of BMS-354825 vs. Imatinib Mesylate (Gleevec) 800 mg/d in Subjects With Chronic Phase Philadelphia Chromosome-Positive Chronic Myeloid Leukemia Who Have Disease That is Resistant to Imatinib at a Dose at 400 - 60 [NCT00103844] | Phase 2 | 150 participants (Actual) | Interventional | 2005-02-28 | Completed | ||
A Phase II Clinical Trial of Dasatinib in Patients With Metastatic Pancreatic Cancer [NCT00544908] | Phase 2 | 7 participants (Actual) | Interventional | 2007-09-30 | Terminated(stopped due to Toxicity) | ||
Phase II Trial of Dasatinib in Advanced (Stage IIIB/IV) Squamous Cell Lung Cancer [NCT01491633] | Phase 2 | 5 participants (Actual) | Interventional | 2011-09-30 | Terminated(stopped due to Safety issues/concerns per DF/HCC PI) | ||
A Phase I Trial of Dasatinib (PDGFR and SRC Inhibitor), Temsirolimus, and Cyclophosphamide in Patients With Advanced Solid Tumors [NCT02389309] | Phase 1 | 14 participants (Actual) | Interventional | 2015-10-05 | Active, not recruiting | ||
Phase II Trial of Cetuximab and Dasatinib in Patients With Cetuximab-resistant, Metastatic and/or Recurrent Squamous Cell Carcinoma of the Head and Neck and Low Serum IL-6 [NCT01488318] | Phase 2 | 21 participants (Actual) | Interventional | 2011-09-30 | Terminated(stopped due to PI leaving the institution) | ||
A Phase III, Multi-center, Open-label, Randomized Study of Oral Asciminib Versus Investigator Selected TKI in Patients With Newly Diagnosed Philadelphia Chromosome Positive Chronic Myelogenous Leukemia in Chronic Phase [NCT04971226] | Phase 3 | 405 participants (Actual) | Interventional | 2021-10-06 | Active, not recruiting | ||
A Phase I-II Study of the Combination of Ruxolitinib or Dasatinib With Chemotherapy in Patients With Philadelphia Chromosome (Ph)-Like Acute Lymphoblastic Leukemia (ALL) [NCT02420717] | Phase 2 | 11 participants (Actual) | Interventional | 2015-07-15 | Terminated(stopped due to Study was closed early due to low accrual and lack of response.) | ||
A Phase III Randomized Trial of Steroids + Tyrosine Kinase Inhibitor (TKI) Induction With Chemotherapy or Blinatumomab for Newly Diagnosed BCR-ABL-Positive Acute Lymphoblastic Leukemia (ALL) in Adults [NCT04530565] | Phase 3 | 348 participants (Anticipated) | Interventional | 2021-01-25 | Recruiting | ||
A Phase II, Single-Institution, Single-Arm, Open-Label Study to Evaluate the Safety and Efficacy of a Single Agent Dasatinib (Sprycel) in Subjects With Relapsed or Refractory Diffuse Large B-Cell Lymphoma [NCT00918463] | Phase 2 | 2 participants (Actual) | Interventional | 2009-06-30 | Terminated(stopped due to The study was terminated early due to lack of accrual.) | ||
PD-1 Combined With Dasatinib for as Third-line Treatment for ARID1A Mutation Advanced NSCLC [NCT04284202] | Phase 2 | 30 participants (Anticipated) | Interventional | 2020-03-01 | Not yet recruiting | ||
Phase I Open-Labeled Trial of Gemcitabine and Dasatinib in Advanced Solid Tumors [NCT00429234] | Phase 1 | 54 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
A Multi-Arm Complete Phase 1 Trial of Valproic Acid-Based 2-Agent Oral Regimens for Patients With Advanced Solid Tumor [NCT00495872] | Phase 1 | 204 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
Dual Inhibition of EGFR and c-Src by Cetuximab and Dasatinib Combined With FOLFOX Chemotherapy in Metastatic Colorectal Cancer (CA180048) [NCT00501410] | Phase 1 | 86 participants (Actual) | Interventional | 2007-04-23 | Completed | ||
The Efficacy and Safety of Switching to Flumatinib Versus Dasatinib After Imatinib-related Low-grade Adverse Events in Patients With Chronic Myeloid Leukemia in Chronic Phase: an Randomized Controlled Trial. [NCT04933526] | Phase 4 | 118 participants (Anticipated) | Interventional | 2021-07-01 | Recruiting | ||
Phase Ib/II Study of EPA-Based EphA2 Targeted Therapy for Patients With Metastatic Triple-Negative Inflammatory Breast Cancer [NCT05198843] | Phase 1/Phase 2 | 18 participants (Anticipated) | Interventional | 2022-11-08 | Recruiting | ||
Phase I Study of Cetuximab Plus Dasatinib (BMS-354825) in Advanced Solid Malignancies [NCT00388427] | Phase 1 | 31 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
Cytochrome P450 Inhibition With Ketoconazole to Decrease Dosage and Costs of Dasatinib for Chronic Myelogenous Leukemia [NCT05638763] | Phase 2 | 15 participants (Anticipated) | Interventional | 2024-11-30 | Recruiting | ||
A Phase I Dose-Escalation Study To Determine The Safety, Pharmacokinetics, And Pharmacodynamics Of BMS-354825 In The Treatment Of Patients With Chronic Phase Chronic Myelogenous Leukemia Who Have Hematologic Resistance To Imatinib Mesylate (Gleevec [NCT00064233] | Phase 1 | 42 participants (Actual) | Interventional | 2003-11-30 | Completed | ||
Phase I Study to Evaluate the Effect of Ketoconazole on the Pharmacokinetics of Dasatinib and the Effect of Dasatinib on Pharmacodynamic Markers in Patients With Advanced Solid Tumors [NCT00162214] | Phase 1 | 60 participants | Interventional | 2005-08-31 | Terminated | ||
A Phase II Study of Dasatinib in the Treatment of Relapsed or Plateau Phase Multiple Myeloma [NCT00429949] | Phase 2 | 21 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
A Phase II Study of Dasatinib (NSC #732517) in Patients With Previously Treated Malignant Mesothelioma [NCT00509041] | Phase 2 | 46 participants (Actual) | Interventional | 2007-08-31 | Completed | ||
Therapy of Early Chronic Phase Chronic Myelogenous Leukemia (CML) With Dasatinib and Venetoclax: A Phase II Study [NCT02689440] | Phase 2 | 155 participants (Actual) | Interventional | 2016-02-19 | Active, not recruiting | ||
A Randomized Controlled Study of Dasatinib Combined With Reduced Intensive Consolidation Chemotherapy in Newly Diagosed Philadelphia Chromesome Positive Adult Lymphoblastic Leukemia [NCT05026229] | 60 participants (Anticipated) | Interventional | 2021-09-06 | Recruiting | |||
Dasatinib Versus Nilotinib as Upfront Therapy for Treatment Naïve Chronic Myeloid Leukemia Chronic Phase [NCT03079505] | Phase 3 | 10 participants (Actual) | Interventional | 2017-08-03 | Terminated(stopped due to Protocol Deviation) | ||
The Efficiency of CAMS-2016 Trial for the Newly Diagnosed Pediatric Acute Myeloid Leukemia: A Prospective Single Centre Trial From China [NCT03173612] | 132 participants (Anticipated) | Interventional | 2016-08-31 | Recruiting | |||
An Open Label Study to Evaluate the Safety of Dasatinib in the Treatment of Scleroderma Pulmonary Interstitial Fibrosis [NCT00764309] | Phase 1/Phase 2 | 47 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
A Phase II Proof-of-Concept Trial to Study Kinase Inhibition in Relapsed/Refractory Acute Leukemias: Using a Comprehensive In Vitro Kinase Inhibitor Panel to Select Individualized, Targeted Therapies [NCT01620216] | Phase 2 | 12 participants (Actual) | Interventional | 2012-05-11 | Terminated(stopped due to Unable to recruit enough eligible subjects) | ||
Phase II Study of 5-Fluorouracil, Oxaliplatin Plus Dasatinib (FOLFOX-D) in First-line Metastatic Pancreatic Adenocarcinoma [NCT01652976] | Phase 2 | 44 participants (Actual) | Interventional | 2012-07-31 | Completed | ||
A Phase II Study Using a BFM Regimen Plus Tyrosine Kinase Inhibitor in Adult Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia [NCT04845035] | Phase 2 | 23 participants (Anticipated) | Interventional | 2024-01-31 | Recruiting | ||
Phase II Study of Blinatumomab and Concurrent Oral Tyrosine Kinase Inhibitor Therapy as Consolidation and Maintenance Therapy for Patients With Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia Following Chemotherapy-Sparing Induction [NCT04329325] | Phase 2 | 17 participants (Actual) | Interventional | 2020-03-30 | Active, not recruiting | ||
A Randomized Phase 2 Pilot Study of Type I-Polarized Autologous Dendritic Cell Vaccines Incorporating Tumor Blood Vessel Antigen (TBVA)-Derived Peptides in Combination With Dasatinib in Patients With Metastatic Melanoma [NCT01876212] | Phase 2 | 15 participants (Actual) | Interventional | 2014-05-16 | Completed | ||
Study to Investigate Outcome of Individualized Treatment Based on Pharmacogenomic Profiling & Ex Vivo Drug Sensitivity Testing of Patient-derived Organoids in Patients With Metastatic Colorectal Cancer [NCT05725200] | Phase 2 | 40 participants (Anticipated) | Interventional | 2022-09-27 | Recruiting | ||
Phase I Study of Dasatinib in Combination With Ipilimumab for Patients With Advanced Gastrointestinal Stromal Tumor and Other Sarcomas [NCT01643278] | Phase 1 | 29 participants (Actual) | Interventional | 2012-07-31 | Completed | ||
A Randomized Phase II Trial of Dasatinib Plus Abiraterone Compared to Abiraterone Alone for Metastatic, Castration-Resistant Prostate Cancer Prior to Chemotherapy [NCT01685125] | Phase 2 | 96 participants (Anticipated) | Interventional | 2012-09-30 | Active, not recruiting | ||
Phase I Study of Dasatinib in Recipients of Autologous Stem Cell Transplantation for Hematologic Malignancies. [NCT01609816] | Phase 1 | 8 participants (Actual) | Interventional | 2015-02-12 | Terminated(stopped due to Low accrual. No Analyses were performed) | ||
An Open-label, Neoadjuvant Phase 2 Study Comparing the Effects of AR Inhibition With and Without SRC or MEK Inhibition on the Development of EMT in Prostate Cancer [NCT01990196] | Phase 2 | 45 participants (Actual) | Interventional | 2014-09-23 | Active, not recruiting | ||
A Phase I Study of BMS-354825 (Dasatinib) in Children With Recurrent/Refractory Solid Tumors or Imatinib Resistant Ph+ Leukemia (BMS Trial CA180038) [NCT00316953] | Phase 1 | 48 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
Hematopoietic Stem Cell Transplant Survivors Study (HTSS Study) [NCT02652052] | 10 participants (Anticipated) | Interventional | 2016-03-01 | Recruiting | |||
Pilot Study on the Determination of Intratumoral Concentrations of Kinase Inhibitors in Patients With Advanced Solid Malignancies. [NCT01636908] | 43 participants (Actual) | Interventional | 2011-08-31 | Completed | |||
A Phase I Trial of Dasatinib in Combination With Crizotinib in Patients With Advanced Malignancies [NCT01744652] | Phase 1 | 62 participants (Actual) | Interventional | 2013-03-31 | Completed | ||
Open-Label Single Arm Phase 2 Study Evaluating Dasatinib Therapy Discontinuation In Patients With Chronic Phase Chronic Myeloid Leukemia (CP-CML) With Stable Complete Molecular Response (CMR) DASFREE [NCT01850004] | Phase 2 | 84 participants (Actual) | Interventional | 2014-01-22 | Completed | ||
A Phase II Trial of Dasatinib to Treat Women With Stage IV or Inoperable Stage III Advanced Breast Cancer [NCT00546104] | Phase 2 | 31 participants (Actual) | Interventional | 2007-10-31 | Completed | ||
Dasatinib in Patients With Waldenström Macroglobulinemia (WM) Progressing on Ibrutinib [NCT04115059] | Phase 1 | 6 participants (Anticipated) | Interventional | 2019-11-04 | Recruiting | ||
Phase II Individualized Therapies Selection Study for Patients With Metastatic Colorectal Carcinoma According to the Genomic Expression Profile in Tumor Samples. [NCT01703910] | Phase 2 | 29 participants (Actual) | Interventional | 2012-11-30 | Completed | ||
A Phase II Randomized Double-Blind Trial of Dasatinib Modulation of Hyperinflammation in Moderate and Severe Patients With COVID-19 [NCT04830735] | Phase 2 | 0 participants (Actual) | Interventional | 2022-08-05 | Withdrawn(stopped due to PI decided not to pursue study) | ||
Phase II Trial of Dasatinib in Subjects With Advanced Cancers Harboring DDR2 Mutation or Inactivating B-RAF Mutation [NCT01514864] | Phase 2 | 19 participants (Actual) | Interventional | 2012-05-31 | Terminated(stopped due to Lack of efficacy and slow accrual) | ||
Therapy of Chronic Lymphocytic Leukemia With Dasatinib (BMS-354825) [NCT00364286] | Phase 2 | 17 participants (Actual) | Interventional | 2006-08-31 | Completed | ||
A Randomized Proof-of-concept Phase II Trial Comparing Therapy Based on Tumor Molecular Profiling Versus Conventional Therapy in Patients With Refractory Cancer. [NCT01771458] | Phase 2 | 742 participants (Actual) | Interventional | 2012-10-31 | Active, not recruiting | ||
A Trial of De-escalation and Stopping Treatment in Chronic Myeloid Leukaemia Patients With Excellent Responses to Tyrosine Kinase Inhibitor Therapy [NCT01804985] | Phase 2 | 168 participants (Anticipated) | Interventional | 2013-12-31 | Active, not recruiting | ||
Phase I Trial Evaluating Safety and Tolerability of the Irreversible Epidermal Growth Factor Receptor Inhibitor Afatinib (BIBW 2992) in Combination With the SRC Kinase Inhibitor Dasatinib for Patients With Non-small Cell Lung Cancer (NSCLC) [NCT01999985] | Phase 1 | 25 participants (Actual) | Interventional | 2013-12-31 | Completed | ||
Evaluation of DASATINIB Monotherapy in Acute Myeloid Leukemia Patients Refractory to VENETOCLAX-AZACITIDINE [NCT06055621] | Phase 2 | 35 participants (Anticipated) | Interventional | 2023-12-31 | Not yet recruiting | ||
International Proof of Concept Therapeutic Stratification Trial of Molecular Anomalies in Relapsed or Refractory HEMatological Malignancies in Children, Sub-protocol B Dasatinib + Venetoclax + Dexamethasone + Cyclophosphamide and Cytarabine in Pediatric P [NCT05751044] | Phase 1/Phase 2 | 26 participants (Anticipated) | Interventional | 2023-10-01 | Not yet recruiting | ||
Pilot and Translational Study of Dasatinib (NSC#732517) Paclitaxel and Carboplatin in Women With Advanced Stage and Recurrent Endometrial Cancer [NCT01440998] | Phase 1 | 18 participants (Actual) | Interventional | 2011-09-20 | Completed | ||
RAVEN: A Phase I/II Trial Treating Relapsed Acute Lymphoblastic Leukemia With Venetoclax and Navitoclax [NCT05192889] | Phase 1/Phase 2 | 90 participants (Anticipated) | Interventional | 2022-08-25 | Recruiting | ||
Phase I Trial Adding Ruxolitinib to a Combination of Dasatinib Plus Dexamethasone in Remission Induction Therapy in Newly Diagnosed Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia Patients Aged 40 Years or Older. [NCT02494882] | Phase 1 | 12 participants (Actual) | Interventional | 2015-06-29 | Active, not recruiting | ||
A Phase III, Prospective Randomised Comparison of Imatinib (STI571, Glivec/Gleevec) 400mg Daily Versus Dasatinib 100mg in Patients With Newly-diagnosed Chronic Phase Chronic Myeloid Leukaemia [NCT01460693] | Phase 3 | 814 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
Prospective, Open Label, Randomized Phase II Trial to Assess a Multimodal Molecular Targeted Therapy in Children, Adolescent and Young Adults With Relapsed or Refractory High-risk Neuroblastoma [NCT01467986] | Phase 2 | 130 participants (Actual) | Interventional | 2013-08-31 | Completed | ||
A Phase II Multicenter Study on the Treatment of Adult de Novo Philadelphia Chromosome Positive (Ph+) Acute Lymphoblastic Leukemia (ALL) With the Protein Tyrosine Kinase Inhibitor BMS-354825. EudraCT Number 2005-005107-42. [NCT00391989] | Phase 2 | 53 participants (Actual) | Interventional | 2006-09-30 | Completed | ||
Dasatinib and Quercetin, a Combination of Senolytics to Treat Fibrotic Non-alcoholic Fatty Liver Disease - the TRUTH Study [NCT05506488] | Phase 1/Phase 2 | 30 participants (Anticipated) | Interventional | 2023-03-01 | Recruiting | ||
Phase II Trial of Dasatinib in Patients With Isocitrate Dehydrogenase (IDH)-Mutant Advanced Intrahepatic Cholangiocarcinoma [NCT02428855] | Phase 2 | 8 participants (Actual) | Interventional | 2015-04-30 | Completed | ||
A Umbrella Study in Relapsed/Refractory Peripheral T-cell Lymphoma Guided by Molecular Subtypes [NCT05559008] | Phase 1/Phase 2 | 116 participants (Anticipated) | Interventional | 2022-09-30 | Recruiting | ||
MATCH Treatment Subprotocol X: Phase II Study of Dasatinib in Patients With Tumors With DDR2 Mutations [NCT04439305] | Phase 2 | 0 participants (Actual) | Interventional | 2016-02-25 | Withdrawn(stopped due to zero accrual) | ||
An Open Label, Randomized (2:1) Phase IIb Study of Dasatinib Versus Imatinib in Patients With Chronic Phase Chronic Myeloid Leukemia Who Have Not Achieved an Optimal Response to 3 Months of Therapy With 400 mg Imatinib [NCT01593254] | Phase 2 | 262 participants (Actual) | Interventional | 2012-09-12 | Completed | ||
A Phase II Study to Determine the Activity of BMS-354825 in Subjects With Chronic Phase Philadelphia Chromosome-Positive Chronic Myeloid Leukemia Who Have Disease That is Resistant to High Dose Imatinib Mesylate (Gleevec) or Who Are Intolerant of Imatinib [NCT00101660] | Phase 2 | 387 participants (Actual) | Interventional | 2005-02-28 | Completed | ||
A Phase II Study of BMS-354825 in Subjects With Myeloid Blast Phase Chronic Myeloid Leukemia Resistant to or Intolerant of Imatinib Mesylate [NCT00101816] | Phase 2 | 124 participants (Actual) | Interventional | 2004-12-31 | Completed | ||
A Phase II Study of a Chemotherapy-Free Induction Regimen for Ph+ Acute Lymphoblastic Leukemia (ALL) Incorporating Inotuzumab Ozogamicin (InO) [NCT04747912] | Phase 2 | 25 participants (Anticipated) | Interventional | 2021-03-02 | Recruiting | ||
Treatment Optimization for Patients With Chronic Myeloid Leukemia (CML) With Treatment naïve Disease (1st Line) and Patients With Resistance or Intolerance Against Alternative Abl-Kinase Inhibitors (≥2nd Line) [NCT02890784] | Phase 3 | 291 participants (Actual) | Interventional | 2016-08-31 | Completed | ||
A Phase II Study of BMS-354825 in Subjects With Accelerated Phase Chronic Myeloid Leukemia Resistant to or Intolerant of Imatinib Mesylate [NCT00101647] | Phase 2 | 197 participants (Actual) | Interventional | 2004-12-31 | Completed | ||
The Safety and Effectivness of Quercetin and Dasatinib on the Epigenetic Aging Rates in Healthy Individuals [NCT04946383] | Phase 2 | 25 participants (Anticipated) | Interventional | 2020-12-16 | Active, not recruiting | ||
Open Label Phase II Study to Evaluate the Safety of Standard Induction and Consolidation Therapy in Combination With Dasatinib in Newly Diagnosed Adult Patients With Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia (PH+ALL) [NCT01724879] | Phase 2 | 19 participants (Actual) | Interventional | 2011-11-30 | Completed | ||
Dasatinib With Ifosfamide, Carboplatin, Etoposide: A Pediatric Phase I/II Trial [NCT00788125] | Phase 1/Phase 2 | 7 participants (Actual) | Interventional | 2008-09-03 | Terminated(stopped due to Terminated early due a shift in resources after lackluster performance of the drug.) | ||
ALSENLITE: An Open-Label Pilot Study of Senolytics for Alzheimer's Disease [NCT04785300] | Phase 1/Phase 2 | 20 participants (Anticipated) | Interventional | 2022-07-06 | Enrolling by invitation | ||
Phase 1b Study of Brexucabtagene Autoleucel Plus Dasatinib in Adults With Acute Lymphoblastic Leukemia [NCT05993949] | Phase 1 | 20 participants (Anticipated) | Interventional | 2023-10-02 | Recruiting | ||
An Open-Label Randomized Phase III Study of Dasatinib vs. High-Dose (600 mg) Imatinib Mesylate in the Treatment of Subjects With Chronic Phase Philadelphia Chromosome-Positive Chronic Myeloid Leukemia Who Are Imatinib Failures or Who Have Had a Suboptimal [NCT00362466] | Phase 3 | 3 participants (Actual) | Interventional | 2007-04-30 | Terminated(stopped due to Insufficient Enrollment) | ||
An Open Label, Balanced, Randomized, Two-Treatment, Two-Sequence, Four-Period, Full Replicate, Crossover, Single Dose, Oral Comparative Bioavailability Study of XS004 (Dasatinib) 100 mg Film-Coated Tablets, Formulation G of Xspray Pharma AB, Sweden, and S [NCT05439408] | Phase 1 | 110 participants (Actual) | Interventional | 2021-06-07 | Completed | ||
A Phase II Study of Dasatinib (BMS-354825) in Subjects With Chronic or Advanced Phase Chronic Myelogenous Leukemia or Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia Who Are Resistant or Intolerant to Imatinib [NCT00349518] | Phase 2/Phase 3 | 0 participants (Actual) | Interventional | 2006-12-31 | Withdrawn | ||
A Phase I Dose Escalation Study of the Combination of Dasatinib (BMS-354825) and Imatinib in Subjects With Chronic Myeloid Leukemia in Chronic Phase [NCT00324077] | Phase 1 | 0 participants (Actual) | Interventional | 2006-08-31 | Withdrawn(stopped due to Insufficient Enrollment) | ||
A Phase 2 Randomized Study of Cediranib (AZD2171) Alone Compared With the Combination of Cediranib (AZD2171) Plus BMS-354825 (Dasatinib, Sprycel) in Docetaxel Resistant, Castration Resistant Prostate Cancer [NCT01260688] | Phase 2 | 22 participants (Actual) | Interventional | 2010-10-31 | Completed | ||
A Phase II Study of Dasatinib in Chronic Lymphocytic Leukemia in Patients Who Exhibit in Vitro Dasatinib Sensitivity [NCT01441882] | Phase 2 | 19 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
Phase I Trial of Induction Dasatinib Therapy in Patients With Resectable Malignant Pleural Mesothelioma [NCT00652574] | Phase 1 | 56 participants (Actual) | Interventional | 2008-03-12 | Completed | ||
Apatinib Mesylate Versus Standard Second-line TKI in the Treatment of Advanced Gastrointestinal Stromal Tumors: a Randomized, Open, Controlled, Single-center Clinical Study [NCT05751733] | 258 participants (Anticipated) | Interventional | 2023-02-01 | Recruiting | |||
A Phase II Study of Induction (Daunorubicin/Cytarabine) and Consolidation (High-Dose Cytarabine) Chemotherapy Plus Dasatinib (NSC #732517) and Continuation Therapy With Dasatinib Alone in Newly Diagnosed Patients With Core Binding Factor Acute Myeloid Leu [NCT01238211] | Phase 2 | 61 participants (Actual) | Interventional | 2010-12-14 | Completed | ||
Therapy of Myeloid Metaplasia-Myelofibrosis, Atypical Chronic Myeloid or Myelomonocytic Leukemia, C-Kit Positive Acute Myeloid Leukemia (AML) or High-Risk Myelodysplastic Syndrome (AML-MDS), Hypereosinophilic Syndrome, Polycythemia Vera, and Mastocytosis [NCT00255346] | Phase 2 | 68 participants (Actual) | Interventional | 2005-11-15 | Completed | ||
An Open-Label, Phase I/II Study of Two Different Schedules of Dasatinib (Sprycel) and Decitabine (Dacogen) Used in Combination for Patients With Accelerated or Blastic Phase Chronic Myelogenous Leukemia (Protocol CA180357) [NCT01498445] | Phase 1/Phase 2 | 32 participants (Actual) | Interventional | 2012-06-12 | Terminated(stopped due to The study was terminated early during the phase II portion of the study due to slow enrollment.) | ||
A Phase I Study of Dasatinib, Androgen Deprivation Therapy and Radiation For Intermediate and High Risk Prostate Cancer [NCT01826838] | Phase 1 | 0 participants (Actual) | Interventional | 2013-01-31 | Withdrawn(stopped due to Lack of patients) | ||
Observation of the Effect of Chemotherapy Combined With Tyrosinase Inhibitor on the Reactivation of CMV and EBV in Patients With Acute Lymphoblastic Leukemia [NCT03331211] | 100 participants (Anticipated) | Observational [Patient Registry] | 2017-11-01 | Recruiting | |||
Efficacy and Safety of Dasatinib 70 mg as First-Line Treatment for Newly Diagnosed Chronic-Phase Chronic Myeloid Leukemia (CML-CP) [NCT04155411] | Phase 4 | 65 participants (Anticipated) | Interventional | 2019-12-01 | Recruiting | ||
First-Line Dasatinib or Nilotinib Followed by Response Guided Switch to Imatinib in Newly Diagnosed Chronic Phase Chronic Myeloid Leukemia [NCT02709083] | Phase 2 | 7 participants (Actual) | Interventional | 2016-10-31 | Terminated(stopped due to Original principal investigator left institution) | ||
A Phase 1A Dose Escalation and Phase 1B Expansion Study to Evaluate the Safety and Tolerability of ETC-1907206 in Combination With Dasatinib in Advanced Haematologic Malignancies [NCT03414450] | Phase 1 | 0 participants (Actual) | Interventional | 2018-04-25 | Withdrawn(stopped due to Withdrawal requested by D3) | ||
A Randomized Controlled Study of Tyrosine Kinase Inhibitor Maintenance Therapy Following Allogeneic Hematopoietic Stem Cell Transplantation in Newly Diagnosed Philadelphia Chromesome Positive Adult Acute Lymphoblastic Leukemia [NCT05024357] | 80 participants (Anticipated) | Interventional | 2021-09-06 | Recruiting | |||
Open-label, Randomized, 3-period, 3-treatment Crossover, Bioequivalence Study Comparing Dasatinib (BMS-354825) Liquid Formulation and the Dispersed Tablet Formulation Relative to the Reference Tablet Formulation in Health Subjects [NCT01392703] | Phase 1 | 141 participants (Actual) | Interventional | 2011-07-31 | Completed | ||
Frontline Asciminib Combination in Chronic Phase CML [NCT03906292] | Phase 2 | 125 participants (Actual) | Interventional | 2019-08-19 | Active, not recruiting | ||
Dasatinib Plus Multi-agent Chemotherapy for New Diagnosed Philadelphia Chromosome-positive Acute Lymphoblastic Leukemia [NCT02523976] | Phase 2 | 30 participants (Actual) | Interventional | 2015-08-01 | Completed | ||
Phase I Study of SRC/ABL Tyrosine Kinase Inhibitor Dasatinib [BMS-354825] in Children and Adolescents With Relapsed or Refractory Leukemia, Protocol ITCC 005 [NCT00306202] | Phase 1 | 63 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
A Phase 2 Study of Dasatinib in Patients With Transplant and Non-Transplant Related Unresectable or Metastatic Cutaneous Squamous Cell Carcinoma and RAI Stage 0-1 Chronic Lymphocytic Leukemia [NCT00563290] | Phase 2 | 7 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
Total Therapy XVII for Newly Diagnosed Patients With Acute Lymphoblastic Leukemia and Lymphoma [NCT03117751] | Phase 2/Phase 3 | 790 participants (Actual) | Interventional | 2017-03-29 | Active, not recruiting | ||
A Phase III Randomized Trial for Newly Diagnosed High Risk B-Lymphoblastic Leukemia (B-ALL) Including a Stratum Evaluating Dasatinib (NSC#732517) in Patients With Ph-like Tyrosine Kinase Inhibitor (TKI) Sensitive Mutations [NCT02883049] | Phase 3 | 5,937 participants (Actual) | Interventional | 2012-02-29 | Active, not recruiting | ||
BMS CA180-097: A Phase II Trial of Dasatinib (Sprycel®) in Subjects With Hormone-refractory Prostate Cancer, Previously Treated With Chemotherapy [NCT00570700] | Phase 2 | 38 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
Personalized Treatment Selection for Metastatic Breast Cancer [NCT00780676] | Phase 2 | 97 participants (Actual) | Interventional | 2009-06-30 | Terminated(stopped due to Closed early for futility.) | ||
A Phase I Study of Dasatinib With Concurrent Chemoradiation for Stage III NSCLC Principal Investigator: Howard Safran, MD. [NCT00787852] | Phase 1 | 11 participants (Actual) | Interventional | 2009-03-31 | Terminated(stopped due to for efficacy and safety reasons) | ||
Phase I/II Trial of Dasatinib Plus Ixabepilone in 2nd or 3rd Line Metastatic Breast Cancer [NCT00924352] | Phase 1/Phase 2 | 56 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
Efficacy and Safety of Dasatinib in the First-line Treatment of Newly Diagnosed Chronic-Phase Chronic Myeloid Leukemia (CML-CP) [NCT04925141] | Phase 4 | 62 participants (Actual) | Interventional | 2016-05-10 | Completed | ||
Window of Opportunity Study of Dasatinib in Operable Triple Negative Breast Cancers With Nuclear Epidermal Growth Factor Receptor (nEGFR) [NCT02720185] | Phase 2 | 5 participants (Actual) | Interventional | 2017-05-03 | Terminated(stopped due to Study terminated early due to COVID-19 related slow enrollment and funding) | ||
Phase II Study of Dasatinib (BMS-354825) for Androgen-deprived Progressive Prostate Cancer [NCT00385580] | Phase 2 | 94 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
Phase II Study of Dasatinib (BMS-354825) in Relapsed Chronic Lymphocytic Leukemia [NCT00438854] | Phase 2 | 15 participants (Actual) | Interventional | 2006-12-31 | Completed | ||
A Phase I/II Study of Dasatinib and Dacarbazine in Patients With Metastatic Melanoma [NCT00597038] | Phase 1/Phase 2 | 50 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
Biological Medicine for Diffuse Intrinsic Pontine Glioma (DIPG) Eradication [NCT02233049] | Phase 2 | 250 participants (Anticipated) | Interventional | 2014-10-31 | Recruiting | ||
Bioequivalence Studies of Dasatinib 100 mg Tablets in Healthy Colombian Subjects in Postprandial Condition [NCT05944783] | Phase 4 | 46 participants (Anticipated) | Interventional | 2023-11-01 | Not yet recruiting | ||
Treatment of Newly Diagnosed Acute Lymphoblastic Leukemia in Children and Adolescents [NCT03020030] | Phase 3 | 560 participants (Actual) | Interventional | 2017-03-03 | Active, not recruiting | ||
A Phase IIb Study of Molecular Responses to Imatinib, at Standard or Increased Doses, or Dasatinib (BMS-354825) (NSC-732517) for Previously Untreated Patients With Chronic Myelogenous Leukemia (CML) in Chronic Phase [NCT00070499] | Phase 2 | 406 participants (Actual) | Interventional | 2004-08-15 | Active, not recruiting | ||
A Phase 1B Dose Escalation Study to Investigate the Safety, Tolerability and Preliminary Efficacy for the Combination Dasatinib (BMS-354825) Plus Nivolumab (BMS-936558) in Patients Chronic Myeloid Leukemia (CML) [NCT02011945] | Phase 1 | 35 participants (Actual) | Interventional | 2014-02-07 | Completed | ||
Phase I/II Study of the Combination of Dasatinib With Chemotherapy for High Risk Acute Myeloid Leukemia (AML) Patients [NCT01876953] | Phase 1/Phase 2 | 20 participants (Actual) | Interventional | 2013-09-13 | Terminated(stopped due to Due to the budget issues, the study discontinued at Phase II.) | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |