ID Source | ID |
---|---|
PubMed CID | 11167602 |
CHEMBL ID | 1946170 |
CHEBI ID | 68647 |
CHEBI ID | 68646 |
SCHEMBL ID | 432230 |
MeSH ID | M0558795 |
Synonym |
---|
HY-10331 |
bay73-4506 hydrochloride |
CAS:835621-07-3;REGORAFENIB HYDROCHLORIDE |
regorafenib (bay 73-4506) |
bay 73-4506 , |
regorafenib;1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea |
A25020 |
regorafenib , |
bay-73-4506 |
bay73-4506 |
bdbm50363397 |
stivarga (tn) |
D10138 |
regorafenib (usan/inn) |
stivarga |
4-(4-(((4-chloro-3-(trifluoromethyl)phenyl)carbamoyl}amino)-3-fluorophenoxy)-n-methylpyridine-2-carboxamide |
24t2a1doyb , |
regorafenibum |
unii-24t2a1doyb |
4-(4-(((4-chloro-3-(trifluoromethyl)phenyl)carbamoyl)amino)-3-fluorophenoxy)-n-methylpyridine-2-carboxamide |
regorafenib [usan:inn] |
BCP9000384 |
755037-03-7 |
4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-n-methylpyridine-2-carboxamide |
AKOS015951107 |
FT-0674338 |
BCPP000352 |
regorafenib anhydrous |
CHEMBL1946170 , |
bay-734506 |
chebi:68647 , |
regorafenib,bay 73-4506 |
NCGC00263138-01 |
unii-mgn125fs9d |
4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-n-methylpicolinamide |
regorafenib [inn] |
regorafenib [mi] |
regorafenib [who-dd] |
regorafenib [vandf] |
CHEBI:68646 , |
CS-0170 |
S1178 |
gtpl5891 |
4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-n-methylpyridine-2-carboxamide |
DB08896 |
SCHEMBL432230 |
smr004701370 |
MLS006010303 |
2-pyridinecarboxamide, 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-n-methyl- |
AM81251 |
4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide |
DTXSID60226441 , |
c21h15clf4n4o3 |
AC-31116 |
AC-25075 |
AB01565826_02 |
DTXSID70144349 , |
835621-08-4 |
mfcd16038047 |
EX-A058 |
fluoro-sorafenib |
SR-01000941571-1 |
sr-01000941571 |
HMS3654K16 |
NCGC00263138-13 |
SW218097-2 |
regorafenib (bay73-4506,fluoro-sorafenib) |
BCP02105 |
Q3891664 |
AS-16304 |
R0142 |
BRD-K16730910-001-02-4 |
SB16819 |
HMS3672E15 |
2-pyridinecarboxamide,4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-n-methyl- |
CCG-269571 |
NCGC00263138-19 |
regorafenib crystalline form i |
4-[4-({[4-chloro-3-(trifluoromethy)phenyl]carbamoyl}amino)-3-fluorophenoxy]-1-methylpyridine-2-carboxamide |
nsc800865 |
nsc-800865 |
nsc763932 |
nsc-763932 |
BKD17855 |
regorafenib-13c-d3 |
755037-03-7 (anhydrous); 1019206-88-2 (hydrate) |
regorafenib (usp-rs) |
dtxcid60148932 |
dtxcid8066840 |
l01xe21 |
regorafenib (usp monograph) |
755037-03-7 , regorafenib |
Z2235801830 |
Regorafenib is an oral tyrosine kinase inhibitor (TKI) approved to treat refractory metastatic colorectal cancer (mCRC) It is a multikinase inhibitor that targets CAFs and suppresses tumor growth.
Regorafenib (RGF) has a great success in the treatment of colorectal cancer, gastrointestinal stromal tumours and hepatocellular carcinoma by inhibiting angiogenic,Stromal and oncogenic kinases. Regorafinib has an important clinical antitumour effect in non-adipocytic soft tissue sarcomas, improving progression-free survival.
Regorafenib has been approved among the treatment options for patients with advanced stage colorectal cancer (CRC), hepatocellular carcinoma (HCC), and gastrointestinal stromal tumors (GIST) The starting dose has been controversial in recent studies.
Regorafenib may enhance antitumor immunity through modulation of macrophage polarization, independent of its anti-angiogenic effects. It also promotes reprogramming and maturation of hair cells in both normal and neomycin-damaged cochlear explants.
Regorafenib was the treatment for 22.2% of patients and 77.8% received trifluridine/tipiracil. Regorafinib is a new treatment standard in patients who already received chemotherapy for metastatic colorectal cancer.
Diarrhea is one of the most frequently observed adverse reactions associated with regorafenib. The most common clinically significant grade 3 or higher adverse events were arterial hypertension and hand and foot skin reaction. Safety analysis showed that regoracenib performed better in reducing grade ≥ 3 adverse events than cetuximab and conatumumab.
Regorafenib had acceptable tolerability and minor pharmacokinetic interactions in combination with standard doses of cisplatin and pemetrexed. There was no significant change in time to maximum concentration or terminal half-life between single dosing and 21-day continuous dosing. No significant differences in the plasma concentrations of unbound regoracenib were observed between the two rat groups.
The in vitro and in vivo anti-tumor activity of pimasertib, a selective MEK 1/2 inhibitor, alone or in combination with a PI3K inhibitor (PI3Ki), a mTOR inhibitor (everolimus), or with multi-targeted kinase inhibitors was tested. We report a case of early diffuse bilateral lung metastasis after LT beyond the Milan transplantation criteria that achieved 1-year tumor-free remission survival with sirolimus combined with regorafenib.
The results of cytotoxicity assay and pharmacokinetics study in rats showed that the regorafenib-lentinan nanosuspensions reduced the toxicity and enhanced the in vitro anticancer activity. Poor site-specific delivery and bioavailability significantly restrict the efficient permeability to brain lesions and compromise its treatment efficacy.
There was no significant change in time to maximum concentration or terminal half-life of regorafenib and its active metabolites M2 and M5 between single dosing and 21-day continuous dosing. It also suggested that individualised dosing in patients with mCRC might result in better clinical outcomes. Total peak plasma drug concentrations were comparable to those in humans.
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. |
hepatotoxic agent | A role played by a chemical compound exihibiting itself through the ability to induce damage to the liver in animals. |
[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 |
---|---|
aromatic ether | Any ether in which the oxygen is attached to at least one aryl substituent. |
pyridinecarboxamide | A member of the class of pyridines that is a substituted pyridine in which at least one of the substituents is a carboxamide or N-substituted caraboxamide group. |
monochlorobenzenes | Any member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine. |
(trifluoromethyl)benzenes | An organofluorine compound that is (trifluoromethyl)benzene and derivatives arising from substitution of one or more of the phenyl hydrogens. |
monofluorobenzenes | Any member of the class of fluorobenzenes containing a mono- or poly-substituted benzene ring carrying a single fluorine substitutent. |
phenylureas | Any member of the class of ureas in which at least one of the nitrogens of the urea moiety is substituted by a phenyl or substituted phenyl group. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Fumarate hydratase | Homo sapiens (human) | Potency | 37.2212 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
PPM1D protein | Homo sapiens (human) | Potency | 23.3617 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 26.8370 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
EWS/FLI fusion protein | Homo sapiens (human) | Potency | 20.9310 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
G | Vesicular stomatitis virus | Potency | 9.5221 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 26.8370 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
polyprotein | Zika virus | Potency | 37.2212 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
tyrosine-protein kinase Yes | Homo sapiens (human) | Potency | 4.8732 | 0.0000 | 5.0182 | 79.2586 | AID686947 |
Interferon beta | Homo sapiens (human) | Potency | 19.9018 | 0.0033 | 9.1582 | 39.8107 | AID1347411; AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 9.5221 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 11.3469 | 0.0096 | 10.5250 | 35.4813 | AID1479145; AID1479148 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 9.5221 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 9.5221 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Bone morphogenetic protein receptor type-1B | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.1413 | 3.7000 | AID1424922 |
Membrane-associated progesterone receptor component 1 | Homo sapiens (human) | Kd | 30.0000 | 0.2040 | 0.2040 | 0.2040 | AID1425109 |
Serine/threonine-protein kinase PLK4 | Homo sapiens (human) | Kd | 30.0000 | 0.0008 | 1.5144 | 9.0000 | AID1425121 |
ATP-dependent RNA helicase DDX3X | Homo sapiens (human) | Kd | 30.0000 | 0.4350 | 0.4350 | 0.4350 | AID1424975 |
Pyridoxal kinase | Homo sapiens (human) | Kd | 30.0000 | 0.2860 | 5.0765 | 16.4040 | AID1425106 |
Citron Rho-interacting kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0330 | 3.0646 | 48.8760 | AID1424954 |
Serine/threonine-protein kinase Chk1 | Homo sapiens (human) | Kd | 30.0000 | 0.0028 | 1.4744 | 8.7000 | AID1424953 |
Aurora kinase A | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.7342 | 9.3000 | AID1424917 |
Cyclin-G-associated kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 0.9086 | 28.6510 | AID1425009 |
Ephrin type-B receptor 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 1.0768 | 9.0000 | AID1424995 |
Peroxisomal acyl-coenzyme A oxidase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0260 | 1.3140 | 2.6020 | AID1424896 |
Receptor-interacting serine/threonine-protein kinase 2 | Homo sapiens (human) | Kd | 0.7670 | 0.0020 | 1.6212 | 11.4330 | AID1425155 |
Mitotic checkpoint serine/threonine-protein kinase BUB1 | Homo sapiens (human) | Kd | 30.0000 | 0.0940 | 1.3910 | 3.5070 | AID1424926 |
Dynamin-like 120 kDa protein, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0170 | 0.3610 | 0.7050 | AID1425097 |
Eukaryotic translation initiation factor 5B | Homo sapiens (human) | Kd | 30.0000 | 0.2320 | 0.2320 | 0.2320 | AID1424986 |
Rho-associated protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 2.7105 | 56.0660 | AID1425158 |
Serine/threonine-protein kinase ULK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0008 | 1.8410 | 23.2730 | AID1425208 |
Serine/threonine-protein kinase/endoribonuclease IRE1 | Homo sapiens (human) | Kd | 30.0000 | 0.0057 | 2.0095 | 12.2010 | AID1424997 |
Ribosomal protein S6 kinase alpha-5 | Homo sapiens (human) | Kd | 30.0000 | 0.0170 | 1.9737 | 29.9570 | AID1425162 |
U5 small nuclear ribonucleoprotein 200 kDa helicase | Homo sapiens (human) | Kd | 30.0000 | 1.3820 | 1.3820 | 1.3820 | AID1425174 |
Ribosomal protein S6 kinase alpha-4 | Homo sapiens (human) | Kd | 30.0000 | 0.0120 | 1.6396 | 7.2000 | AID1425161 |
Serine/threonine-protein kinase 16 | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 1.2483 | 9.9690 | AID1425179 |
Serine/threonine-protein kinase 10 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 2.9234 | 57.4530 | AID1425177 |
Serine/threonine-protein kinase D3 | Homo sapiens (human) | Kd | 30.0000 | 0.0089 | 2.2738 | 23.3410 | AID1425137 |
Structural maintenance of chromosomes protein 2 | Homo sapiens (human) | Kd | 30.0000 | 0.2090 | 0.6575 | 1.1060 | AID1425173 |
Mitogen-activated protein kinase kinase kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 1.5781 | 8.0000 | AID1425050 |
Mitogen-activated protein kinase kinase kinase kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0082 | 2.3645 | 62.7720 | AID1425054 |
Serine/threonine-protein kinase LATS1 | Homo sapiens (human) | Kd | 30.0000 | 0.0140 | 1.8393 | 10.7330 | AID1425033 |
Serine/threonine-protein kinase PAK 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0027 | 2.5694 | 30.3710 | AID1425100 |
Tyrosine-protein kinase ABL1 | Homo sapiens (human) | Kd | 0.7530 | 0.0000 | 1.0411 | 13.4530 | AID1424890 |
Epidermal growth factor receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 1.3514 | 20.8270 | AID1424983 |
High affinity nerve growth factor receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.3484 | 9.2000 | AID1425094 |
Guanine nucleotide-binding protein G(i) subunit alpha-2 | Homo sapiens (human) | Kd | 30.0000 | 0.1840 | 0.1840 | 0.1840 | AID1425011 |
ADP/ATP translocase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.4510 | 0.4510 | 0.4510 | AID1425169 |
Protein kinase C beta type | Homo sapiens (human) | Kd | 30.0000 | 0.0013 | 2.7081 | 26.3240 | AID1425130 |
Insulin receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 1.0823 | 7.9060 | AID1425026 |
Tyrosine-protein kinase Lck | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1174 | 24.2210 | AID1425034 |
Tyrosine-protein kinase Fyn | Homo sapiens (human) | Kd | 30.0000 | 0.0008 | 1.4238 | 8.4000 | AID1425008 |
Cyclin-dependent kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.2880 | 1.4952 | 3.0490 | AID1424937 |
Glycogen phosphorylase, liver form | Homo sapiens (human) | Kd | 30.0000 | 2.1210 | 2.1210 | 2.1210 | AID1425146 |
Tyrosine-protein kinase Fes/Fps | Homo sapiens (human) | Kd | 30.0000 | 0.0048 | 1.0986 | 7.4000 | AID1425003 |
Adenine phosphoribosyltransferase | Homo sapiens (human) | Kd | 30.0000 | 0.0290 | 0.0290 | 0.0290 | AID1424914 |
Tyrosine-protein kinase Yes | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.3708 | 17.1520 | AID1425212 |
Tyrosine-protein kinase Lyn | Homo sapiens (human) | Kd | 30.0000 | 0.0006 | 1.0485 | 5.7000 | AID1425037 |
Proto-oncogene tyrosine-protein kinase receptor Ret | Homo sapiens (human) | Kd | 0.1260 | 0.0007 | 0.8642 | 27.5420 | AID1425154 |
Insulin-like growth factor 1 receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.9211 | 19.2170 | AID1425022 |
Signal recognition particle receptor subunit alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 0.0080 | 0.0080 | AID1425176 |
Cytochrome c1, heme protein, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.2020 | 0.2020 | 0.2020 | AID1424969 |
Hepatocyte growth factor receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.6297 | 8.5000 | AID1425076 |
Tyrosine-protein kinase HCK | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 2.0343 | 15.9930 | AID1425017 |
Platelet-derived growth factor receptor beta | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 1.0050 | 11.1070 | AID1425104 |
Tyrosine-protein kinase Fgr | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.0721 | 7.8000 | AID1425005 |
Serine/threonine-protein kinase A-Raf | Homo sapiens (human) | Kd | 30.0000 | 0.0470 | 9.6832 | 33.6550 | AID1424915 |
Glycogen phosphorylase, brain form | Homo sapiens (human) | Kd | 30.0000 | 3.5690 | 3.5690 | 3.5690 | AID1425145 |
Breakpoint cluster region protein | Homo sapiens (human) | Kd | 0.7390 | 0.0030 | 1.2196 | 17.3640 | AID1424919 |
Serine/threonine-protein kinase pim-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.1393 | 19.3160 | AID1425111 |
Fibroblast growth factor receptor 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.5581 | 6.2000 | AID1425004 |
DNA topoisomerase 2-alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0640 | 0.2750 | 0.4860 | AID1425202 |
Cyclin-dependent kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0033 | 1.6050 | 8.6000 | AID1424946 |
ADP/ATP translocase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 0.2505 | 0.4950 | AID1425170 |
Proto-oncogene tyrosine-protein kinase Src | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.5077 | 9.6000 | AID1425175 |
cAMP-dependent protein kinase type II-alpha regulatory subunit | Homo sapiens (human) | Kd | 30.0000 | 0.0520 | 1.7535 | 3.4550 | AID1425128 |
Serine/threonine-protein kinase B-raf | Homo sapiens (human) | Kd | 3.1250 | 0.0002 | 1.6258 | 26.0180 | AID1424924 |
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 2.0569 | 9.5000 | AID1425110 |
Ribosyldihydronicotinamide dehydrogenase [quinone] | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 6.7556 | 88.9030 | AID1425093 |
Tyrosine-protein kinase Fer | Homo sapiens (human) | Kd | 30.0000 | 0.0014 | 1.3604 | 8.8000 | AID1425002 |
Protein kinase C alpha type | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.7922 | 21.3520 | AID1425129 |
cAMP-dependent protein kinase catalytic subunit alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0039 | 2.9479 | 23.2450 | AID1425123 |
General transcription and DNA repair factor IIH helicase subunit XPD | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.6906 | 12.0220 | AID1424996 |
Casein kinase II subunit alpha' | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 2.5309 | 28.8720 | AID1424968 |
Ras-related protein Rab-6A | Homo sapiens (human) | Kd | 30.0000 | 0.0330 | 0.0330 | 0.0330 | AID1425150 |
Ephrin type-A receptor 1 | Homo sapiens (human) | Kd | 0.0070 | 0.0041 | 1.8000 | 9.8000 | AID1424987 |
Multifunctional protein ADE2 | Homo sapiens (human) | Kd | 30.0000 | 5.4810 | 5.4810 | 5.4810 | AID1425098 |
cAMP-dependent protein kinase catalytic subunit gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 8.5577 | 49.2780 | AID1425125 |
cAMP-dependent protein kinase catalytic subunit beta | Homo sapiens (human) | Kd | 30.0000 | 0.0130 | 0.7408 | 4.1000 | AID1425124 |
Ferrochelatase, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.2430 | 6.4343 | 67.9140 | AID1425001 |
Glycine receptor subunit alpha-1 | Homo sapiens (human) | EC50 (µMol) | 1.8000 | 0.3200 | 1.4577 | 4.2000 | AID1203550 |
Ribosomal protein S6 kinase beta-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0013 | 1.1805 | 4.8000 | AID1425164 |
Tyrosine-protein kinase JAK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0016 | 1.2166 | 7.8000 | AID1425030 |
Cyclin-dependent kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.5179 | 10.4870 | AID1424944 |
Beta-adrenergic receptor kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 5.5791 | 22.4940 | AID1424908 |
Probable ATP-dependent RNA helicase DDX6 | Homo sapiens (human) | Kd | 30.0000 | 4.1030 | 4.1030 | 4.1030 | AID1424977 |
Mitogen-activated protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.4300 | 5.2743 | 9.8000 | AID1425061 |
MAP/microtubule affinity-regulating kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 3.9689 | 58.2400 | AID1425069 |
Deoxycytidine kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0120 | 1.0875 | 2.1630 | AID1424970 |
Mitogen-activated protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 2.7441 | 7.3000 | AID1425056 |
Ephrin type-A receptor 2 | Homo sapiens (human) | Kd | 0.8505 | 0.0009 | 1.0752 | 8.1980 | AID1424988; AID1802323 |
Ephrin type-B receptor 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0004 | 3.1536 | 53.1980 | AID1424992 |
Non-receptor tyrosine-protein kinase TYK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.5575 | 8.7000 | AID1425207 |
UMP-CMP kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0045 | 0.0060 | AID1424959 |
Phosphatidylethanolamine-binding protein 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0030 | 0.0030 | AID1425107 |
Wee1-like protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0014 | 3.5389 | 65.1580 | AID1425210 |
Heme oxygenase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.1190 | 0.1190 | 0.1190 | AID1425018 |
DnaJ homolog subfamily A member 1 | Homo sapiens (human) | Kd | 30.0000 | 0.9620 | 0.9620 | 0.9620 | AID1424980 |
RAC-alpha serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0006 | 1.0621 | 4.4000 | AID1424910 |
RAC-beta serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0021 | 1.6196 | 8.7000 | AID1424911 |
Dual specificity protein kinase TTK | Homo sapiens (human) | Kd | 3.9230 | 0.0065 | 1.6269 | 8.5000 | AID1425205 |
DNA replication licensing factor MCM4 | Homo sapiens (human) | Kd | 30.0000 | 0.6290 | 0.6290 | 0.6290 | AID1425072 |
Myosin-10 | Homo sapiens (human) | Kd | 30.0000 | 0.2290 | 0.4935 | 0.7580 | AID1425079 |
Dual specificity mitogen-activated protein kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0039 | 1.6429 | 9.6000 | AID1425039 |
Receptor-type tyrosine-protein kinase FLT3 | Homo sapiens (human) | Kd | 0.5620 | 0.0002 | 0.9559 | 9.9000 | AID1425006 |
Bone morphogenetic protein receptor type-1A | Homo sapiens (human) | Kd | 30.0000 | 0.0600 | 1.5010 | 7.0000 | AID1424921 |
Activin receptor type-1B | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 1.5110 | 15.2580 | AID1424901 |
TGF-beta receptor type-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 2.2785 | 9.6000 | AID1425196 |
TGF-beta receptor type-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0800 | 1.8351 | 6.9000 | AID1425197 |
Electron transfer flavoprotein subunit beta | Homo sapiens (human) | Kd | 30.0000 | 0.0120 | 0.0120 | 0.0120 | AID1424999 |
Tyrosine-protein kinase CSK | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 3.4578 | 39.5530 | AID1424960 |
Glycine--tRNA ligase | Homo sapiens (human) | Kd | 30.0000 | 0.0400 | 0.0400 | 0.0400 | AID1425010 |
Protein kinase C iota type | Homo sapiens (human) | Kd | 30.0000 | 0.0260 | 9.3316 | 51.0180 | AID1425133 |
Exosome RNA helicase MTR4 | Homo sapiens (human) | Kd | 30.0000 | 2.6070 | 2.6070 | 2.6070 | AID1425168 |
Tyrosine-protein kinase Tec | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.0095 | 8.7000 | AID1425193 |
Tyrosine-protein kinase ABL2 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1249 | 14.9240 | AID1424891 |
Tyrosine-protein kinase FRK | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.2424 | 10.8370 | AID1425007 |
G protein-coupled receptor kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 1.1890 | 1.4020 | 1.6150 | AID1425012 |
Tyrosine-protein kinase SYK | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 2.0052 | 9.2260 | AID1425188 |
26S proteasome regulatory subunit 6B | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 0.0050 | 0.0050 | AID1425141 |
Mitogen-activated protein kinase 8 | Homo sapiens (human) | Kd | 30.0000 | 0.0110 | 2.0965 | 26.0590 | AID1425063 |
Mitogen-activated protein kinase 9 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.4596 | 8.1000 | AID1425064 |
Dual specificity mitogen-activated protein kinase kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 2.0462 | 6.6000 | AID1425040 |
Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha | Homo sapiens (human) | Kd | 30.0000 | 0.2080 | 3.6125 | 7.0170 | AID1425113 |
Casein kinase I isoform alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 2.5756 | 19.3520 | AID1424961 |
Casein kinase I isoform delta | Homo sapiens (human) | Kd | 30.0000 | 0.0150 | 2.2270 | 18.3960 | AID1424962 |
MAP kinase-activated protein kinase 2 | Homo sapiens (human) | Kd | 0.6820 | 0.0003 | 2.0274 | 14.7420 | AID1425065 |
Elongation factor Tu, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.4640 | 0.4640 | 0.4640 | AID1425206 |
Choline-phosphate cytidylyltransferase A | Homo sapiens (human) | Kd | 30.0000 | 0.0410 | 0.0410 | 0.0410 | AID1425103 |
Cysteine--tRNA ligase, cytoplasmic | Homo sapiens (human) | Kd | 30.0000 | 0.0120 | 0.3320 | 0.6520 | AID1424932 |
Casein kinase I isoform epsilon | Homo sapiens (human) | Kd | 30.0000 | 0.0130 | 1.4086 | 12.4090 | AID1424963 |
Very long-chain specific acyl-CoA dehydrogenase, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 1.6890 | 1.6890 | 1.6890 | AID1424894 |
Dual specificity protein kinase CLK1 | Homo sapiens (human) | Kd | 2.1070 | 0.0020 | 1.8791 | 29.8810 | AID1424955 |
Dual specificity protein kinase CLK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.1384 | 6.5000 | AID1424956 |
Dual specificity protein kinase CLK3 | Homo sapiens (human) | Kd | 30.0000 | 0.0100 | 2.4499 | 9.0000 | AID1424957 |
Glycogen synthase kinase-3 alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 2.4754 | 22.5430 | AID1425013 |
Glycogen synthase kinase-3 beta | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.0057 | 6.1680 | AID1425014 |
Cyclin-dependent kinase 7 | Homo sapiens (human) | Kd | 30.0000 | 0.0025 | 1.6783 | 7.7000 | AID1424949 |
Cyclin-dependent kinase 9 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.6166 | 9.9010 | AID1424950 |
Ras-related protein Rab-27A | Homo sapiens (human) | Kd | 30.0000 | 4.4930 | 4.4930 | 4.4930 | AID1425149 |
Interleukin-1 receptor-associated kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0061 | 1.5252 | 8.5000 | AID1425027 |
Ribosomal protein S6 kinase alpha-3 | Homo sapiens (human) | Kd | 30.0000 | 0.0170 | 2.8896 | 37.6050 | AID1425160 |
Serine/threonine-protein kinase Nek2 | Homo sapiens (human) | Kd | 30.0000 | 0.1100 | 1.5649 | 6.5000 | AID1425086 |
Serine/threonine-protein kinase Nek3 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 5.9368 | 38.0880 | AID1425087 |
Dual specificity mitogen-activated protein kinase kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0034 | 2.3943 | 6.5000 | AID1425043 |
Serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.5711 | 5.0000 | AID1425120 |
LIM domain kinase 1 | Homo sapiens (human) | Kd | 0.6160 | 0.0260 | 1.7840 | 21.0890 | AID1425035 |
LIM domain kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0570 | 4.9717 | 52.0560 | AID1425036 |
Mitogen-activated protein kinase 10 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.6354 | 5.9000 | AID1425057 |
Tyrosine--tRNA ligase, cytoplasmic | Homo sapiens (human) | Kd | 30.0000 | 3.3160 | 3.3160 | 3.3160 | AID1425211 |
5'-AMP-activated protein kinase subunit gamma-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 1.4681 | 10.2120 | AID1425126 |
Ephrin type-B receptor 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0069 | 2.1713 | 6.4100 | AID1424993 |
Ephrin type-A receptor 5 | Homo sapiens (human) | Kd | 1.1230 | 0.0002 | 1.2100 | 5.9000 | AID1424990 |
Ephrin type-B receptor 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 2.1678 | 26.3990 | AID1424994 |
Ephrin type-A receptor 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0012 | 3.1525 | 43.9420 | AID1424989 |
Adenylate kinase 2, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 1.0360 | 1.0360 | 1.0360 | AID1424909 |
Adenosine kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0130 | 1.8368 | 3.4930 | AID1424907 |
Ras-related protein Rab-10 | Homo sapiens (human) | Kd | 30.0000 | 1.3480 | 1.3480 | 1.3480 | AID1425148 |
Actin-related protein 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0360 | 2.7735 | 5.5110 | AID1424899 |
Actin-related protein 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 0.0040 | 0.0040 | AID1424898 |
GTP-binding nuclear protein Ran | Homo sapiens (human) | Kd | 30.0000 | 0.7590 | 0.7590 | 0.7590 | AID1425153 |
Casein kinase I isoform gamma-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0460 | 1.4506 | 6.6000 | AID1424965 |
Cyclin-dependent kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 3.0602 | 63.6140 | AID1424945 |
Cyclin-dependent kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0320 | 1.2007 | 3.3560 | AID1424948 |
Cyclin-dependent-like kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0430 | 1.3757 | 8.3000 | AID1424947 |
Cyclin-dependent kinase 16 | Homo sapiens (human) | Kd | 30.0000 | 0.0011 | 1.5855 | 10.0000 | AID1424941 |
Cyclin-dependent kinase 17 | Homo sapiens (human) | Kd | 0.7190 | 0.0010 | 0.8233 | 5.6000 | AID1424942 |
ATP-dependent 6-phosphofructokinase, platelet type | Homo sapiens (human) | Kd | 30.0000 | 0.9830 | 0.9830 | 0.9830 | AID1425108 |
Dual specificity mitogen-activated protein kinase kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1386 | 8.7730 | AID1425038 |
DNA topoisomerase 2-beta | Homo sapiens (human) | Kd | 30.0000 | 0.1480 | 1.2270 | 2.5970 | AID1425203 |
Protein kinase C theta type | Homo sapiens (human) | Kd | 30.0000 | 0.0007 | 1.6140 | 7.2000 | AID1425134 |
Activin receptor type-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 1.4853 | 16.1210 | AID1424900 |
Macrophage-stimulating protein receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 2.0718 | 8.4000 | AID1425078 |
Focal adhesion kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.2255 | 13.0390 | AID1425142 |
Protein kinase C delta type | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1261 | 9.2060 | AID1425131 |
Tyrosine-protein kinase BTK | Homo sapiens (human) | Kd | 30.0000 | 0.0006 | 1.5299 | 10.1530 | AID1424925 |
Activated CDC42 kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.7138 | 9.6000 | AID1425201 |
Epithelial discoidin domain-containing receptor 1 | Homo sapiens (human) | Kd | 0.3580 | 0.0002 | 1.6314 | 71.4840 | AID1424972 |
Mitogen-activated protein kinase kinase kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0031 | 1.4681 | 14.0430 | AID1425052 |
Serine/threonine-protein kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.7120 | 25.9020 | AID1425185 |
5'-AMP-activated protein kinase catalytic subunit alpha-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0037 | 1.8913 | 15.3890 | AID1425122 |
Dual specificity mitogen-activated protein kinase kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 2.6590 | 65.6770 | AID1425042 |
Mitogen-activated protein kinase 7 | Homo sapiens (human) | Kd | 30.0000 | 0.0420 | 2.0073 | 9.9000 | AID1425062 |
Serine/threonine-protein kinase PAK 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0031 | 2.3045 | 6.0000 | AID1425099 |
Serine/threonine-protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.8602 | 17.5260 | AID1425182 |
Mitogen-activated protein kinase kinase kinase 1 | Homo sapiens (human) | Kd | 0.4650 | 0.0970 | 2.5995 | 12.4730 | AID1425044 |
Integrin-linked protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0200 | 0.4603 | 1.3290 | AID1425024 |
Rho-associated protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.7555 | 13.4620 | AID1425157 |
Non-receptor tyrosine-protein kinase TNK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0018 | 1.0064 | 11.2690 | AID1425200 |
Calcium/calmodulin-dependent protein kinase type II subunit gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.0209 | 7.8000 | AID1424929 |
Calcium/calmodulin-dependent protein kinase type II subunit delta | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.5044 | 20.3010 | AID1424928 |
Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 2.1016 | 40.2910 | AID1424981 |
Activin receptor type-2B | Homo sapiens (human) | Kd | 30.0000 | 0.0076 | 2.7328 | 9.9000 | AID1424902 |
Bone morphogenetic protein receptor type-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0190 | 2.5917 | 14.3770 | AID1424923 |
Protein-tyrosine kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0043 | 1.7430 | 9.0000 | AID1425144 |
cGMP-dependent protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0016 | 0.7072 | 3.8000 | AID1425138 |
Cyclin-dependent kinase 13 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.2571 | 4.5180 | AID1424940 |
Inhibitor of nuclear factor kappa-B kinase subunit epsilon | Homo sapiens (human) | Kd | 30.0000 | 0.0051 | 1.1093 | 8.3000 | AID1425023 |
Protein-tyrosine kinase 2-beta | Homo sapiens (human) | Kd | 30.0000 | 0.0011 | 1.9450 | 30.4140 | AID1425143 |
Maternal embryonic leucine zipper kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0049 | 2.2835 | 29.9330 | AID1425074 |
Structural maintenance of chromosomes protein 1A | Homo sapiens (human) | Kd | 30.0000 | 0.3650 | 0.3650 | 0.3650 | AID1425172 |
Chromodomain-helicase-DNA-binding protein 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0030 | 0.0030 | AID1424952 |
Peroxisomal acyl-coenzyme A oxidase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0140 | 0.1425 | 0.2710 | AID1424895 |
Cyclin-dependent kinase 10 | Homo sapiens (human) | Kd | 30.0000 | 0.0090 | 0.0090 | 0.0090 | AID1424938 |
Delta(24)-sterol reductase | Homo sapiens (human) | Kd | 30.0000 | 0.4320 | 0.4320 | 0.4320 | AID1424978 |
Ribosomal protein S6 kinase alpha-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0280 | 2.5286 | 22.7260 | AID1425159 |
Myosin light chain kinase, smooth muscle | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 1.2088 | 7.9000 | AID1425081 |
Mitogen-activated protein kinase 11 | Homo sapiens (human) | Kd | 1.9110 | 0.0001 | 0.4610 | 3.7430 | AID1425058 |
Serine/threonine-protein kinase STK11 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.9949 | 5.9000 | AID1425178 |
Serine/threonine-protein kinase N1 | Homo sapiens (human) | Kd | 30.0000 | 0.0013 | 3.1729 | 49.8130 | AID1425117 |
Serine/threonine-protein kinase N2 | Homo sapiens (human) | Kd | 30.0000 | 0.0018 | 1.7527 | 9.9000 | AID1425118 |
Mitogen-activated protein kinase 14 | Homo sapiens (human) | Kd | 0.7050 | 0.0000 | 0.5036 | 8.5000 | AID1425059 |
Calcium/calmodulin-dependent protein kinase type IV | Homo sapiens (human) | Kd | 30.0000 | 0.0300 | 1.9215 | 5.4600 | AID1424930 |
Mitogen-activated protein kinase kinase kinase 11 | Homo sapiens (human) | Kd | 30.0000 | 0.0110 | 1.5639 | 17.9840 | AID1425045 |
Discoidin domain-containing receptor 2 | Homo sapiens (human) | Kd | 0.4210 | 0.0030 | 1.9888 | 42.2800 | AID1424973 |
AP2-associated protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0012 | 1.3707 | 13.7110 | AID1424889 |
Myosin light chain kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.6184 | 10.4240 | AID1425082 |
Rab-like protein 3 | Homo sapiens (human) | Kd | 30.0000 | 4.8300 | 4.8300 | 4.8300 | AID1425151 |
Serine/threonine-protein kinase MRCK alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0570 | 4.5547 | 14.0200 | AID1424933 |
Serine/threonine-protein kinase MRCK gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0370 | 1.9625 | 9.5000 | AID1424935 |
Acyl-CoA dehydrogenase family member 10 | Homo sapiens (human) | Kd | 30.0000 | 0.0780 | 1.6997 | 3.9570 | AID1424892 |
Serine/threonine-protein kinase N3 | Homo sapiens (human) | Kd | 30.0000 | 0.0990 | 0.7365 | 1.3740 | AID1425119 |
Serine/threonine-protein kinase ULK3 | Homo sapiens (human) | Kd | 30.0000 | 0.0012 | 1.3350 | 9.9000 | AID1425209 |
Uncharacterized protein FLJ45252 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 1.2292 | 9.3110 | AID1425147 |
Acyl-CoA dehydrogenase family member 11 | Homo sapiens (human) | Kd | 30.0000 | 1.9160 | 3.0730 | 4.1470 | AID1424893 |
Serine/threonine-protein kinase/endoribonuclease IRE2 | Homo sapiens (human) | Kd | 30.0000 | 0.1160 | 0.7604 | 1.5000 | AID1424998 |
Serine/threonine-protein kinase MARK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 1.8425 | 11.1030 | AID1425068 |
ATP-dependent RNA helicase DHX30 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 0.0060 | 0.0060 | AID1424979 |
Serine/threonine-protein kinase TAO1 | Homo sapiens (human) | Kd | 30.0000 | 0.0004 | 2.1612 | 18.7570 | AID1425189 |
STE20-related kinase adapter protein alpha | Homo sapiens (human) | Kd | 30.0000 | 0.3160 | 1.7208 | 3.6720 | AID1425186 |
AarF domain-containing protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0230 | 3.1137 | 22.7470 | AID1424904 |
Mitogen-activated protein kinase kinase kinase kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0051 | 1.6413 | 15.4350 | AID1425053 |
MAP kinase-activated protein kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 1.1241 | 3.1180 | AID1425067 |
Atypical kinase COQ8A, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0940 | 5.1673 | 65.3020 | AID1424905 |
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 2.7522 | 8.8000 | AID1425115 |
Mitogen-activated protein kinase 15 | Homo sapiens (human) | Kd | 30.0000 | 0.0049 | 0.6880 | 4.5000 | AID1425060 |
Serine/threonine-protein kinase Nek9 | Homo sapiens (human) | Kd | 30.0000 | 0.0160 | 2.7428 | 19.6170 | AID1425089 |
Serine/threonine-protein kinase Nek7 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 3.6719 | 8.7000 | AID1425088 |
ATP-dependent RNA helicase DDX1 | Homo sapiens (human) | Kd | 30.0000 | 0.0860 | 0.0860 | 0.0860 | AID1424974 |
Mitogen-activated protein kinase kinase kinase kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 0.9378 | 5.5000 | AID1425051 |
Aurora kinase B | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.0614 | 22.8520 | AID1424918 |
MAP/microtubule affinity-regulating kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0054 | 1.1029 | 4.9000 | AID1425070 |
Serine/threonine-protein kinase Nek1 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 2.4294 | 8.3000 | AID1425085 |
PAS domain-containing serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 1.0670 | 1.0670 | 1.0670 | AID1425102 |
Calcium/calmodulin-dependent protein kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 3.2331 | 52.8470 | AID1424931 |
EKC/KEOPS complex subunit TP53RK | Homo sapiens (human) | Kd | 30.0000 | 0.3110 | 1.9519 | 3.8400 | AID1425204 |
Dual specificity testis-specific protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 0.0020 | 0.0020 | AID1425195 |
Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0440 | 0.9285 | 2.9000 | AID1425116 |
Mitogen-activated protein kinase kinase kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0700 | 6.5647 | 50.5360 | AID1425049 |
Mitogen-activated protein kinase kinase kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 1.5331 | 9.9000 | AID1425047 |
Eukaryotic translation initiation factor 2-alpha kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0580 | 1.9224 | 4.8360 | AID1424984 |
Nucleolar GTP-binding protein 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0090 | 4.1035 | 8.1980 | AID1425016 |
Serine/threonine-protein kinase D2 | Homo sapiens (human) | Kd | 30.0000 | 0.0081 | 2.3723 | 25.0190 | AID1425136 |
NUAK family SNF1-like kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.6774 | 4.6000 | AID1425095 |
RNA cytidine acetyltransferase | Homo sapiens (human) | Kd | 30.0000 | 1.2400 | 1.2400 | 1.2400 | AID1425083 |
Serine/threonine-protein kinase SIK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0011 | 1.8165 | 41.7950 | AID1425166 |
STE20-like serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 3.8573 | 99.2320 | AID1425171 |
Serine/threonine-protein kinase TAO3 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 2.7131 | 14.1960 | AID1425191 |
dCTP pyrophosphatase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.5730 | 1.7403 | 3.0540 | AID1424971 |
Dual specificity protein kinase CLK4 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.4122 | 8.3000 | AID1424958 |
Casein kinase I isoform gamma-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0530 | 2.0622 | 5.7000 | AID1424964 |
Phenylalanine--tRNA ligase beta subunit | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0045 | 0.0060 | AID1425000 |
Isoleucine--tRNA ligase, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0110 | 0.0110 | 0.0110 | AID1425020 |
BMP-2-inducible protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0022 | 2.4097 | 56.0320 | AID1424920 |
Obg-like ATPase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0050 | 0.0070 | AID1425096 |
Interleukin-1 receptor-associated kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 3.4719 | 34.1450 | AID1425029 |
Mitogen-activated protein kinase kinase kinase 20 | Homo sapiens (human) | Kd | 0.2740 | 0.0023 | 1.7034 | 13.6380 | AID1425213 |
Cyclin-dependent kinase 12 | Homo sapiens (human) | Kd | 30.0000 | 0.0320 | 1.8032 | 5.6350 | AID1424939 |
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13 | Homo sapiens (human) | Kd | 30.0000 | 3.9200 | 3.9200 | 3.9200 | AID1425084 |
Serine/threonine-protein kinase pim-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0019 | 0.8415 | 5.0000 | AID1425112 |
Serine/threonine-protein kinase 26 | Homo sapiens (human) | Kd | 30.0000 | 0.0074 | 1.7380 | 8.3000 | AID1425181 |
Succinate--CoA ligase [ADP-forming] subunit beta, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 0.0070 | 0.0070 | AID1425187 |
Serine/threonine-protein kinase NLK | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 1.0226 | 4.4000 | AID1425090 |
5'-AMP-activated protein kinase subunit gamma-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 1.1581 | 9.1280 | AID1425127 |
Serine/threonine-protein kinase TBK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.7674 | 49.6010 | AID1425192 |
Septin-9 | Homo sapiens (human) | Kd | 30.0000 | 0.0100 | 0.2430 | 0.6350 | AID1425165 |
Ribosomal protein S6 kinase alpha-6 | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 2.4153 | 23.7620 | AID1425163 |
TRAF2 and NCK-interacting protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0047 | 1.3935 | 10.0000 | AID1425199 |
Serine/threonine-protein kinase TAO2 | Homo sapiens (human) | Kd | 30.0000 | 0.0100 | 2.0176 | 12.9420 | AID1425190 |
Long-chain-fatty-acid--CoA ligase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 0.6353 | 1.6900 | AID1424897 |
Serine/threonine-protein kinase ICK | Homo sapiens (human) | Kd | 30.0000 | 0.0007 | 1.4717 | 9.3000 | AID1425021 |
RAC-gamma serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0025 | 1.7646 | 6.2000 | AID1424912 |
Serine/threonine-protein kinase SIK3 | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.5086 | 10.3180 | AID1425167 |
Mitogen-activated protein kinase kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0024 | 1.3298 | 6.9000 | AID1425046 |
Mitogen-activated protein kinase kinase kinase kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.9494 | 50.2140 | AID1425055 |
Receptor-interacting serine/threonine-protein kinase 3 | Homo sapiens (human) | Kd | 0.3680 | 0.0110 | 1.4797 | 6.7000 | AID1425156 |
Serine/threonine-protein kinase MRCK beta | Homo sapiens (human) | Kd | 30.0000 | 0.0340 | 3.6252 | 50.0050 | AID1424934 |
Interleukin-1 receptor-associated kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.7137 | 25.5810 | AID1425028 |
Serine/threonine-protein kinase 24 | Homo sapiens (human) | Kd | 30.0000 | 0.0065 | 0.8920 | 4.0840 | AID1425180 |
Casein kinase I isoform gamma-3 | Homo sapiens (human) | Kd | 30.0000 | 0.0970 | 2.3978 | 8.7000 | AID1424966 |
Mitogen-activated protein kinase kinase kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0390 | 2.3970 | 8.4000 | AID1425048 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
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. |
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. |
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. |
AID1581237 | Inhibition of human c-KIT A loop exon 18 A829P single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
AID1703972 | Antiproliferative activity against human HT-29 cells assessed as dead cells by measuring green fluorescent cells for 48 to 72 hrs by IncuCyte live-cell imaging assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
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. |
AID1387026 | Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
AID1719859 | Inhibition of human PDGFRAlpha assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1581259 | Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining based assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
AID1465755 | Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
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. |
AID1719909 | Inhibition of human C-Raf assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1581229 | Inhibition of human c-KIT A loop exon 17 D816V single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
AID1600255 | Inhibition of VEGFR1 (unknown origin) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors. |
AID1649983 | Antitumor activity against human HCT116 cells xenografted in BALB/c mouse assessed as reduction in tumor growth at 12 mg/kg, ip treated for every other day relative to control | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction. |
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. |
AID1719910 | Inhibition of mouse ARG assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
AID1581258 | Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as cell growth inhibition after 144 hrs by methylene blue staining based assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
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. |
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. |
AID1581215 | Inhibition of wild type recombinant GST-tagged FLT3 (Y567 to S993 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using Her2 peptide as substrate measured after 4 hrs in presence of ATP by Kinase-Glo Plus reagent-based lumine | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
AID1520195 | Inhibition of UGT1A in rat hepatocytes assessed as decrease in bilirubin monoglucuronide level at 10 uM preincubated for 2 mins followed by UDPGA addition measured after 45 mins by HPLC analysis relative to control | 2019 | MedChemComm, Jan-01, Volume: 10, Issue:1 | Efforts in redesigning the antileukemic drug 6-thiopurine: decreasing toxic side effects while maintaining efficacy. |
AID1386990 | Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant and T670I mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
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. |
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. |
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. |
AID1600259 | Inhibition of BRAF (unknown origin) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors. |
AID1424926 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1719850 | Inhibition of mouse ARG assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1850318 | Down-regulation of MLKL expression in human T24 cells at 7.5 to 10 uM measured after 16 hrs by Western blot analysis | |||
AID1873224 | Inhibition of ABCG2 (unknown origin) expressed in human S1M180 cells mediated [3H]-mitoxantrone efflux assessed as intracellular [3H]-mitoxantrone level 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. |
AID1895657 | Inhibition of BRAF V600E (409 to 765 residues) (unknown origin) by HTRF assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16 | Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
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. |
AID1719844 | Inhibition of human PTK5 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1581243 | Inhibition of human c-KIT A loop exon 11/17 V560G/N822K double mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
AID1719906 | Inhibition of human EphA2 assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1703964 | Inhibition of c-Met (unknown origin) at 1 uM using FAM-labelled peptide and ATP incubated for 10 mins by mobility shift assay relative to control | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
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. |
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. |
AID1301726 | Antiproliferative activity against human HT-29 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. |
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. |
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. |
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. |
AID1895664 | Inhibition of c-kit (unknown origin) by HTRF assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16 | Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
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. |
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. |
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. |
AID1719851 | Inhibition of human FMS assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1876095 | Cytotoxicity against human A549 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. |
AID1424938 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
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. |
AID1465756 | Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
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. |
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. |
AID1719854 | Inhibition of human HIPK2 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1425102 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1386988 | Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
AID1719834 | Inhibition of human PDGFRbeta assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1510861 | Inhibition of VEGFR1 (unknown origin) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma. |
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. |
AID1581214 | Inhibition of recombinant N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) (unknown origin) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr) 4:1 as substrate measured after 150 mins in presence of | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
AID1387022 | Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
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. |
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. |
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. |
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. |
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. |
AID1465758 | Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
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. |
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. |
AID1895658 | Inhibition of RET (unknown origin) by HTRF assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16 | Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
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. |
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. |
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. |
AID1719899 | Inhibition of human MAP4K5 assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1719858 | Inhibition of human MNK2 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1424935 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
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. |
AID1703982 | Cell cycle arrest in human HT-29 cells assessed as accumulation in G0/G1 phase at 3 ug/ml incubated for 48 hrs by propidium iodide base flow cytometry analysis (Rvb = 71.6%) | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
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. |
AID1719893 | Inhibition of human RAF1 assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1719901 | Inhibition of human TRKB assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1719911 | Inhibition of human FMS assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1387033 | Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
AID1719852 | Inhibition of human DDR1 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1850361 | AUMC in Sprague-Dawley rat at 12 mg/kg, IG measured HPLC analysis | |||
AID1425145 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
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. |
AID1387030 | Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
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. |
AID1719840 | Inhibition of mouse BLK assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1387027 | Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
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. |
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. |
AID1387025 | Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
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. |
AID1719896 | Inhibition of mouse Abl assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1719857 | Inhibition of human LOK assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1850288 | Antiproliferative activity against human T24 cells measured after 48 hrs by MTT assay | |||
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. |
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. |
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. |
AID1581226 | Inhibition of human c-KIT A loop exon 17 D816H single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
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. |
AID1649962 | Inhibition of cell adhesion of human HCT116 cells assessed as cell adhesion to fibronectin at 1 uM after 24 hrs by MTT/ELISA method (Rvb = 78%) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction. |
AID1301725 | Antiproliferative activity against human A549 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. |
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. |
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. |
AID1203550 | Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents after 1 to 4 days by two-electrode voltage clamp assay | 2015 | Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7 | Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain. |
AID1425168 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID1719898 | Inhibition of human HIPK4 assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
AID1719887 | Inhibition of human HIPK3 assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1581216 | Antiproliferative activity against human GISTT1 cells harboring heterozygous deletion mutation at C-kit exon 11 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
AID1703974 | Antiproliferative activity aganist human FHC at 10 ug/ml measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
AID1424956 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1425202 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1703975 | Cytotoxicity aganist human FHC at 10 ug/ml measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
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. |
AID756127 | Inhibition of human recombinant soluble epoxide hydrolase assessed as cyano(6-methoxy-naphthalen-2-yl)methyl trans-[(3-phenyloxyran-2-yl)methyl] carbonate conversion to 6-methoxy-2-naphthaldehyde preincubated for 5 mins prior to substrate addition by fluo | 2013 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13 | Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors. |
AID1850315 | Down-regulation of RIPK1 expression in human T24 cells at 7.5 to 10 uM measured after 16 hrs by Western blot analysis | |||
AID1719839 | Inhibition of human MAP4K5 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1719831 | Inhibition of human VEGFR1 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1465750 | Inhibition of wild type KIT (unknown origin) using biotinylated poly-Glu-Tyr as substrate preincubated for 30 mins followed by substrate addition in presence of ATP by TR-FRET assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
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. |
AID1581221 | Inhibition of human c-KIT ATP binding domain exon 13 V654A single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
AID1895659 | Inhibition of BRAF (unknown origin) by HTRF assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16 | Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
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. |
AID1387045 | Antitumor activity against mouse BA/F3 cells expressing Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) allografted in CB17 SCID mouse assessed as inhibition of tumor growth at 100 mg/kg, po qd measured on last day of dosing | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
AID1719908 | Inhibition of human ABL assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1719836 | Inhibition of mouse Abl assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1387023 | Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
AID1703965 | Inhibition of Ron (unknown origin) at 0.5 uM using FAM-labelled peptide and ATP incubated for 10 mins by mobility shift assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
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. |
AID1895663 | Inhibition of FGFR1 (unknown origin) by HTRF assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16 | Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
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. |
AID1424922 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID1719883 | Inhibition of human C-Raf assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1600176 | Inhibition of human N-terminal GST tagged VEGFR-2 expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate in presence of ATP by Kinase-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors. |
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. |
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. |
AID1387037 | Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
AID1649961 | Inhibition of cell adhesion of human HCT116 cells assessed as cell adhesion to fibronectin at 2 uM after 24 hrs by MTT/ELISA method (Rvb = 78%) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction. |
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. |
AID1581222 | Inhibition of human c-KIT ATP binding domain exon 13 K642E single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
AID1719867 | Inhibition of human RAF1 assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1387035 | Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
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. |
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. |
AID1850363 | Absorption rate constant in Sprague-Dawley rat at 12 mg/kg, IG measured HPLC analysis | |||
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. |
AID1581220 | Inhibition of human c-KIT ATP binding domain exon 13 V654A single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
AID1850287 | Antiproliferative activity against human MGC-803 cells measured after 48 hrs by MTT assay | |||
AID1719848 | Inhibition of human ABL assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID756110 | Ratio of compound IC50 to sorafenib IC50 for human recombinant soluble epoxide hydrolase | 2013 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13 | Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors. |
AID1876046 | Antiviral activity against influenza A virus H3N2 | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
AID1905552 | Inhibition of human RET kinase using IGF1Rtide as substrate incubated for 40 mins and measured by ADP-Glo assay | |||
AID1581228 | Inhibition of human c-KIT A loop exon 17 D816V single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
AID1850359 | AUC (0 to 48 hrs) in Sprague-Dawley rat at 12 mg/kg, IG measured HPLC analysis | |||
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. |
AID1719902 | Inhibition of human TRKC assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
AID1425151 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1581234 | Inhibition of human c-KIT A loop exon 17 Y823D single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
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. |
AID1719903 | Inhibition of human LYN assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
AID1895660 | Inhibition of VEGFR1 (unknown origin) by HTRF assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16 | Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
AID1703984 | Cell cycle arrest in human HT-29 cells assessed as accumulation in G2/M phase at 3 ug/ml incubated for 48 hrs by propidium iodide base flow cytometry analysis (Rvb = 2.4%) | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
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. |
AID1850357 | Tmax in Sprague-Dawley rat at 12 mg/kg, IG measured HPLC analysis | |||
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. |
AID1850320 | Down-regulation of p-RIPK3 expression in human T24 cells at 7.5 to 10 uM measured after 16 hrs by Western blot analysis | |||
AID1203551 | Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents at 10 uM after 1 to 4 days by two-electrode voltage clamp assay relative to control | 2015 | Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7 | Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain. |
AID1876093 | Inhibition of VEGFR 2 (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. |
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. |
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. |
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. |
AID1387024 | Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
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. |
AID1719914 | Inhibition of human HIPK2 assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
AID1575641 | Inhibition of Streptococcus pyogenes UDPGDH expressed in Escherichia coli/rat liver microsome UGT-1A assessed as reduction in BMG production at 10 uM by HPLC analysis | 2019 | MedChemComm, May-01, Volume: 10, Issue:5 | New methods to assess 6-thiopurine toxicity and expanding its therapeutic application to pancreatic cancer |
AID1850316 | Down-regulation of RIPK2 expression in human T24 cells at 7.5 to 10 uM measured after 16 hrs by Western blot analysis | |||
AID1719846 | Inhibition of human EphA2 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
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. |
AID1387032 | Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
AID1719837 | Inhibition of human ZAK assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1719842 | Inhibition of human TRKC assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
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. |
AID1649985 | Antitumor activity against human HCT116 cells xenografted in BALB/c mouse assessed as tumor weight at 12 mg/kg, ip treated for every other day (Rvb = 0.782g) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction. |
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. |
AID1719889 | Inhibition of human MuSK assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1581219 | Inhibition of human c-KIT JM domain exon 11 V560G single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1465757 | Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
AID1719828 | Inhibition of human c-Kit assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1649979 | Inhibition of cell adhesion of human HCT116 cells assessed as cell adhesion to laminin at 2 uM after 24 hrs by MTT/ELISA method (Rvb = 82%) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction. |
AID1581230 | Inhibition of human c-KIT A loop exon 17 D820E single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
AID1424957 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
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. |
AID1387036 | Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
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. |
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. |
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. |
AID1600179 | Inhibition of FGFR1 (unknown origin) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors. |
AID1703966 | Inhibition of c-Met (unknown origin) using FAM-labelled peptide and ATP incubated for 10 mins by mobility shift assay relative to control | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
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. |
AID1719904 | Inhibition of human PTK5 assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1703968 | Anticancer activity against human HT-29 cells assessed as inhibition of cell proliferation by MTT assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
AID1719832 | Inhibition of human RAF1 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1719838 | Inhibition of human HIPK4 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1387028 | Inhibition of Kit exon 11 deletion (557 to 558 residues) and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
AID1424958 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID1850367 | Half-life in Sprague-Dawley rat at 12 mg/kg, IG measured HPLC analysis | |||
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. |
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. |
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. |
AID1581218 | Inhibition of human c-KIT JM domain exon 11 V560G single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
AID1203549 | Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents at 1 uM after 1 to 4 days by two-electrode voltage clamp assay relative to control | 2015 | Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7 | Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain. |
AID1719888 | Inhibition of human HIPK2 assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1719915 | Inhibition of human MuSK assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1850319 | Down-regulation of p-RIPK1 expression in human T24 cells at 7.5 to 10 uM measured after 16 hrs by Western blot analysis | |||
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. |
AID1719869 | Inhibition of human p38alpha assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1425084 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
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. |
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. |
AID1719833 | Inhibition of human VEGFR2 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1600258 | Inhibition of GST-tagged TIE2 (unknown origin) using biotin-Ahx-EPKDDAYPLYSDFG peptide as substrate by HTRF method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors. |
AID1719856 | Inhibition of human FLT3 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1719875 | Inhibition of human TRKB assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1649946 | Cytotoxicity against human NCM460 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction. |
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. |
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. |
AID1719874 | Inhibition of mouse BLK assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
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. |
AID1703969 | Antiproliferative activity against human HT-29 cells assessed as dead cells by measuring green fluorescent cells at 5 ug/mL for 72 hrs by IncuCyte live-cell imaging assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
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. |
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. |
AID1424895 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1581242 | Inhibition of human c-KIT A loop exon 11/17 V560G/N822K double mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
AID1895662 | Inhibition of VEGFR3 (unknown origin) by HTRF assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16 | Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
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. |
AID1581225 | Inhibition of human c-KIT ATP binding domain exon 14 T670I single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
AID1649960 | Inhibition of cell adhesion of human HCT116 cells assessed as cell adhesion to fibronectin at 4 uM after 24 hrs by MTT/ELISA method (Rvb = 78%) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction. |
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. |
AID1719872 | Inhibition of human HIPK4 assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1719865 | Inhibition of human RET assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1465754 | Cytotoxicity against human GIST48B cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
AID1581233 | Inhibition of human c-KIT A loop exon 17 D820Y single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
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. |
AID1386987 | Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
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. |
AID1719881 | Inhibition of human B-Raf assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
AID1600177 | Inhibition of human wild type BRAF by Kinase-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors. |
AID1425205 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1386989 | Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
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. |
AID1719878 | Inhibition of human PTK5 assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
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. |
AID1581239 | Inhibition of human c-KIT A loop exon 11/13 V559D/V654A double mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
AID1719900 | Inhibition of mouse BLK assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1719913 | Inhibition of human HIPK3 assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
AID1719879 | Inhibition of human EphA8 assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
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. |
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. |
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. |
AID1581223 | Inhibition of human c-KIT ATP binding domain exon 13 K642E single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
AID1520185 | Inhibition of UGT1A in rat hepatocytes assessed as decrease in bilirubin monoglucuronide level at 10 uM after 45 mins in presence of UDPGA by HPLC analysis | 2019 | MedChemComm, Jan-01, Volume: 10, Issue:1 | Efforts in redesigning the antileukemic drug 6-thiopurine: decreasing toxic side effects while maintaining efficacy. |
AID1719912 | Inhibition of human DDR1 assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1719868 | Inhibition of human VEGFR2 assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
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. |
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. |
AID1510860 | Inhibition of VEGFR2 (unknown origin) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma. |
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. |
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. |
AID1633238 | Inhibition of VEGFR2 (unknown origin) | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis and docking study of novel picolinamide derivatives as anticancer agents and VEGFR-2 inhibitors. |
AID1425107 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1581240 | Inhibition of human c-KIT A loop exon 11/17 V560G/D816V double mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
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. |
AID1387034 | Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
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. |
AID1581231 | Inhibition of human c-KIT A loop exon 17 D820E single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
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. |
AID1425113 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID643995 | Inhibition of B-Raf V600E mutant | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Small molecule inhibitors of BRAF in clinical trials. |
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. |
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. |
AID1703983 | Cell cycle arrest in human HT-29 cells assessed as accumulation in S phase at 3 ug/ml incubated for 48 hrs by propidium iodide base flow cytometry analysis (Rvb = 22.4%) | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
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. |
AID1719884 | Inhibition of mouse ARG assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1520196 | Inhibition of UGT1A in rat hepatocytes assessed as decrease in bilirubin diglucuronide level at 10 uM after 45 mins in presence of UDPGA by HPLC analysis | 2019 | MedChemComm, Jan-01, Volume: 10, Issue:1 | Efforts in redesigning the antileukemic drug 6-thiopurine: decreasing toxic side effects while maintaining efficacy. |
AID1719891 | Inhibition of human RET assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1719866 | Inhibition of human VEGFR1 assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1719892 | Inhibition of human VEGFR1 assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1895661 | Inhibition of VEGFR2 (unknown origin) by HTRF assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16 | Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
AID1719853 | Inhibition of human HIPK3 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1719895 | Inhibition of human p38alpha assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID756116 | Inhibition of full length recombinant c-RAF (unknown origin) using MEK1 as substrate after 1 hr by luminescence assay | 2013 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13 | Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors. |
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. |
AID1424898 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
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. |
AID1301724 | Antiangiogenic activity in HRMEC 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. |
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. |
AID1581241 | Inhibition of human c-KIT A loop exon 11/17 V560G/D816V double mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
AID1719864 | Inhibition of human VEGFR3 assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1850365 | Clearance in Sprague-Dawley rat at 12 mg/kg, IG measured HPLC analysis | |||
AID1719876 | Inhibition of human TRKC assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1425079 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
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. |
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. |
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. |
AID1719870 | Inhibition of mouse Abl assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1600256 | Inhibition of mouse VEGFR-2 (785 to 1376 residues) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors. |
AID1649942 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction. |
AID1649980 | Inhibition of cell adhesion of human HCT116 cells assessed as cell adhesion to laminin at 4 uM after 24 hrs by MTT/ELISA method (Rvb = 82%) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction. |
AID1850289 | Antiproliferative activity against human HCV-29 cells measured after 48 hrs by MTT assay | |||
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. |
AID1387029 | Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
AID1425180 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
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. |
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. |
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. |
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. |
AID1703973 | Antiproliferative activity against human HT-29 cells assessed as dead cells by measuring green fluorescent cells at 1 to 3 ug/mL by IncuCyte live-cell imaging assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
AID1703993 | Cytotoxicity aganist human FHC at 0.19 ug/ml measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
AID1424979 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1719873 | Inhibition of human MAP4K5 assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1387053 | Antitumor activity against mouse BA/F3 cells expressing Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) allografted in CB17 SCID mouse assessed as tumor regression at 100 mg/kg, po qd measured on last day of dosing | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
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. |
AID1719860 | Inhibition of human p70S6K assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
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. |
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. |
AID1649940 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction. |
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. |
AID1600182 | Inhibition of RAF1 (unknown origin) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors. |
AID1719871 | Inhibition of human ZAK assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1719847 | Inhibition of human B-Raf assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1719855 | Inhibition of human MuSK assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
AID1719890 | Inhibition of human VEGFR3 assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1719862 | Inhibition of human LIMK1 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1895656 | Inhibition of RAF1 (305 to 648 residues) (unknown origin) by HTRF assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16 | Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
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. |
AID1719861 | Inhibition of human TAO1 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1424976 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1719897 | Inhibition of human ZAK assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1719843 | Inhibition of human LYN assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1520194 | Inhibition of UGT1A in rat hepatocytes assessed as decrease in bilirubin diglucuronide level at 10 uM preincubated for 2 mins followed by UDPGA addition measured after 45 mins by HPLC analysis relative to control | 2019 | MedChemComm, Jan-01, Volume: 10, Issue:1 | Efforts in redesigning the antileukemic drug 6-thiopurine: decreasing toxic side effects while maintaining efficacy. |
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. |
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. |
AID1850321 | Down-regulation of p-MLKL expression in human T24 cells at 7.5 to 10 uM measured after 16 hrs by Western blot analysis | |||
AID643994 | Inhibition of wild-type B-Raf | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Small molecule inhibitors of BRAF in clinical trials. |
AID1719849 | Inhibition of human C-Raf assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
AID1386991 | Inhibition of KDR (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1719863 | Inhibition of human CDKL2 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
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. |
AID1581238 | Inhibition of human c-KIT A loop exon 11/13 V559D/V654A double mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
AID1581232 | Inhibition of human c-KIT A loop exon 17 D820Y single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
AID1850286 | Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay | |||
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. |
AID1719886 | Inhibition of human DDR1 assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
AID1581326 | Antitumor activity against patient-derived human GS5107 cells harboring exon 13(K642E)/exon 17 (N822K) double mutant. xenografted in NOD/SCID mouse assessed as tumor growth inhibition at 30 mg/kg, po administered 5 days a week for 2 weeks measured after d | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
AID1719905 | Inhibition of human EphA8 assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1719830 | Inhibition of human RET assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1719882 | Inhibition of human ABL assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
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. |
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. |
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. |
AID1387031 | Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19 | Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
AID1465753 | Inhibition of KIT D816H mutant (unknown origin) using biotinylated poly-Glu-Tyr as substrate preincubated for 30 mins followed by substrate addition in presence of ATP by TR-FRET assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
AID1581224 | Inhibition of human c-KIT ATP binding domain exon 14 T670I single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
AID1719880 | Inhibition of human EphA2 assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1581235 | Inhibition of human c-KIT A loop exon 17 Y823D single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
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. |
AID1719845 | Inhibition of human EphA8 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
AID1465771 | Intrinsic clearance in mouse liver microsomes at 3 uM after 60 mins by LC-MS analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
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. |
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. |
AID1719829 | Inhibition of human VEGFR3 assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1719894 | Inhibition of human VEGFR2 assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
AID1703967 | Inhibition of Ron (unknown origin) using FAM-labelled peptide and ATP incubated for 10 mins by mobility shift assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
AID1850317 | Down-regulation of RIPK3 expression in human T24 cells at 7.5 to 10 uM measured after 16 hrs by Western blot analysis | |||
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. |
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. |
AID1719841 | Inhibition of human TRKB assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1649943 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction. |
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. |
AID1850369 | MRT (0 to 48 hrs) in Sprague-Dawley rat at 12 mg/kg, IG measured HPLC analysis | |||
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1719885 | Inhibition of human FMS assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1600257 | Inhibition of mouse VEGFR-3 (818 to 1363 residues) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors. |
AID1649944 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction. |
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. |
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. |
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. |
AID1425094 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
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. |
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. |
AID1649978 | Inhibition of cell adhesion of human HCT116 cells assessed as cell adhesion to laminin at 1 uM after 24 hrs by MTT/ELISA method (Rvb = 82%) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction. |
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. |
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. |
AID1581260 | Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
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. |
AID1600254 | Inhibition of PDGFR beta (561 to 1106 residues) (unknown origin) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors. |
AID1581217 | Antiproliferative activity against human MOLM13 harboring FLT3-ITD mutant assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
AID1581227 | Inhibition of human c-KIT A loop exon 17 D816H single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
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. |
AID1649941 | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction. |
AID1581236 | Inhibition of human c-KIT A loop exon 18 A829P single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
AID1719907 | Inhibition of human B-Raf assessed as remaining enzyme activity at 0.01 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
AID1465751 | Inhibition of KIT V559D/T670I double mutant (unknown origin) using biotinylated poly-Glu-Tyr as substrate preincubated for 30 mins followed by substrate addition in presence of ATP by TR-FRET assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
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. |
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. |
AID1850290 | Selectivity index, ratio IC50 for antiproliferative activity against human HCV-29 cells over IC50 for antiproliferative activity against human T24 cells | |||
AID1719835 | Inhibition of human p38alpha assessed as remaining enzyme activity at 1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
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. |
AID1649945 | Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction. |
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. |
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. |
AID1895665 | Inhibition of Tie-2 (unknown origin) by HTRF assay | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16 | Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
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. |
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. |
AID1575640 | Inhibition of Streptococcus pyogenes UDPGDH expressed in Escherichia coli/rat liver microsome UGT-1A assessed as reduction in BDG production at 10 uM by HPLC analysis | 2019 | MedChemComm, May-01, Volume: 10, Issue:5 | New methods to assess 6-thiopurine toxicity and expanding its therapeutic application to pancreatic cancer |
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. |
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. |
AID1703970 | Cytotoxicity against human HT-29 cells assessed as reduction in cell viability at 5 ug/mL by MTT assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
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. |
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. |
AID1703971 | Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 36 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer. |
AID1850355 | Cmax in Sprague-Dawley rat at 12 mg/kg, IG measured HPLC analysis | |||
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. |
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. |
AID1719877 | Inhibition of human LYN assessed as remaining enzyme activity at 0.1 uM | 2020 | Journal of medicinal chemistry, 08-27, Volume: 63, Issue:16 | Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. |
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. |
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. |
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. |
AID1465752 | Inhibition of KIT V559D/V654A double mutant (unknown origin) using biotinylated poly-Glu-Tyr as substrate preincubated for 30 mins followed by substrate addition in presence of ATP by TR-FRET assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Identification of potent Yes1 kinase inhibitors using a library screening approach. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1345687 | Human B-Raf proto-oncogene, serine/threonine kinase (RAF family) | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Small molecule inhibitors of BRAF in clinical trials. |
AID1345506 | Human kinase insert domain receptor (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family) | 2011 | International journal of cancer, Jul-01, Volume: 129, Issue:1 | Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 508 (59.07) | 24.3611 |
2020's | 352 (40.93) | 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 (71.93) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 122 (13.80%) | 5.53% |
Reviews | 162 (18.33%) | 6.00% |
Case Studies | 79 (8.94%) | 4.05% |
Observational | 25 (2.83%) | 0.25% |
Other | 496 (56.11%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |