ID Source | ID |
---|---|
PubMed CID | 24826799 |
CHEMBL ID | 1171837 |
CHEBI ID | 78543 |
SCHEMBL ID | 589260 |
MeSH ID | M0558593 |
Synonym |
---|
HY-12047 |
ponatinib (ap24534) |
0li , |
3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzam ide |
FT-0660376 |
bdbm50322535 |
3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide |
3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-n-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide |
ap24534 |
ponatinib , |
ap-24534 |
chebi:78543 , |
CHEMBL1171837 , |
ap 24534 |
ap24534,ponatinib |
ponatinib (usan/inn) |
D09950 |
hsdb 8184 |
benzamide, 3-(2-imidazo(1,2-b)pyridazin-3-ylethynyl)-4-methyl-n-(4-((4-methyl-1- piperazinyl)methyl)-3-(trifluoromethyl)phenyl)- |
4340891kfs , |
3-(2-(imidazo(1,2-b)pyridazin-3-yl)ethynyl)-4-methyl-n-(4-((4-methylpiperazin-1- yl)methyl)-3-(trifluoromethyl)phenyl)benzamide |
unii-4340891kfs |
ponatinib [usan:inn] |
BCP9000307 |
3-(2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl)-4-methyl-n-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide |
AKOS015995214 |
943319-70-8 |
BCPP000397 |
NCGC00263152-02 |
NCGC00263152-01 |
PB34916 |
ponatinib [who-dd] |
ponatinib [mi] |
ponatinib [vandf] |
ponatinib [usan] |
ponatinib [inn] |
3-(2-(imidazo(1,2-b)pyridazin-3-yl)ethynyl)-4-methyl-n-(4-((4-methylpiperazin-y-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide |
CS-0204 |
3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide |
gtpl5890 |
BRD-K44227013-001-02-3 |
3-(2-imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide |
SCHEMBL589260 |
DB08901 |
smr004701274 |
MLS006010166 |
AM81261 |
benzamide, 3-(2-imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]- |
ponatinibum |
3-(2-imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]benzamide |
3-(2-imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-benzamide |
AC-26973 |
AB01565847_03 |
mfcd17215203 |
DTXSID50241426 , |
EX-A067 |
HMS3654H16 |
NCGC00263152-14 |
SW218091-2 |
3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzam |
943319-70-8 (free base) |
3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide. |
S1490 |
AS-19133 |
BCP02037 |
Q198728 |
HMS3295I23 |
CCG-264900 |
NCGC00263152-12 |
ponatinib, free base |
ponatinib;3-(2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl)-4-methyl-n-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide |
A24930 |
nsc758487 |
nsc800855 |
nsc-758487 |
nsc-800855 |
3-(2-{imidazo[1,2-b]pyridazin-3-yl}ethynyl)-4-methyl-n-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide |
EN300-6733072 |
3-(2-(imidazo(1,2-b)pyridazin-3-yl)ethynyl)-4-methyl-n-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide |
benzamide, 3-(2-imidazo(1,2-b)pyridazin-3-ylethynyl)-4-methyl-n-(4-((4-methyl-1-piperazinyl)methyl)-3-(trifluoromethyl)phenyl) |
l01xe24 |
dtxcid50163917 |
benzamide, 3-(2-imidazo(1,2-b)pyridazin-3-ylethynyl)-4-methyl-n-(4-((4-methyl-1-piperazinyl)methyl)-3-(trifluoromethyl)phenyl)- |
3-(imidazo(1,2-b)pyridazin-3-ylethynyl)-4-methyl-n-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide |
Z1828098700 |
Ponatinib (PON) is a key drug for patients with second tyrosine kinase inhibitor (TKI)-resistant/intolerant Philadelphia chromosome-positive leukemia. Ponatinib is a third-generation, rationally-designed TKI with clinically meaningful activity in this difficult-to-treat population.
Ponatinib (P) has been used for the treatment of chronic myeloid leukemia (CML) It is known that inhibition of BCR-ABL fusion protein by p onatinib induces apoptosis of CML cells. Ponatinib has shown efficacy in patients with refractory chronicMyeloid leukaemia.
Excerpt | Reference | Relevance |
---|---|---|
"Ponatinib was found to inhibit the kinase activity of KIT G560V and KIT D816V in the human mast cell leukemia cell line HMC-1." | ( Synergistic growth-inhibitory effects of ponatinib and midostaurin (PKC412) on neoplastic mast cells carrying KIT D816V. Blatt, K; Gleixner, KV; Hadzijusufovic, E; Peter, B; Radia, D; Reiter, A; Suppan, V; Valent, P, 2013) | 1.38 |
Ponatinib maintenance treatment might show superior survival for Ph-positive CNSL patients with or without the T315I mutation. Ponatinib treatment significantly increased plasma VEGF, soluble (s)VEGFR1, sVEG FR2, sTIE2, interferon gamma (IFNγ) and tumor necrosis factor alpha (TNF-α)
Ponatinib dose intensity is associated with increased incidence of adverse effects (AEs), including vascular events. Ponatinib and dasatinib seemed to be both safe for the clinical application of Ph-positive CNSL.
Rifampin decreased maximum plasma concentration (Cmax ) and area under the plasma concentration-time curve (AUC) by 42%, 59%, and 63%, respectively, with no effect on time to Cmax. Two major BBB efflux transporters, P-glycoprotein (P-gp) and breast cancer resistance protein (Bcrp), cooperate to modulate the brain exposure of ponatinib.
Excerpt | Reference | Relevance |
---|---|---|
" Mixed-model analyses of variance (anova) were performed on natural log-transformed PK parameters Cmax and AUC0-∞." | ( Effects of food on the pharmacokinetics of ponatinib in healthy subjects. Dorer, DJ; Haluska, F; Narasimhan, NI; Niland, K; Sonnichsen, D, 2013) | 0.65 |
" All limits of the 90% CIs of the estimated geometric mean ratios for Cmax and all AUC comparisons fell within the 80%-125% margins." | ( Effects of food on the pharmacokinetics of ponatinib in healthy subjects. Dorer, DJ; Haluska, F; Narasimhan, NI; Niland, K; Sonnichsen, D, 2013) | 0.65 |
" Mean elimination half-life was extended in subjects with hepatic impairment (43-47 vs 36 h)." | ( Evaluation of pharmacokinetics and safety of ponatinib in subjects with chronic hepatic impairment and matched healthy subjects. Davis, J; Dorer, DJ; Marbury, TC; Narasimhan, NI; Sonnichsen, D; Turner, CD, 2014) | 0.66 |
" Rifampin decreased maximum plasma concentration (Cmax ) and area under the plasma concentration-time curve (AUC) from time zero to time of last measurable concentration (AUC0-t ) and from time zero to infinity (AUC0-∞ ) of ponatinib by 42%, 59%, and 63%, respectively, with no effect on time to Cmax ." | ( Evaluation of the effect of multiple doses of rifampin on the pharmacokinetics and safety of ponatinib in healthy subjects. Davis, J; Dorer, DJ; Narasimhan, NI; Sonnichsen, D; Turner, CD, 2015) | 0.82 |
" In vivo pharmacokinetic studies in wild-type and transporter knockout mice showed that two major BBB efflux transporters, P-glycoprotein (P-gp) and breast cancer resistance protein (Bcrp), cooperate to modulate the brain exposure of ponatinib." | ( Pharmacokinetic Assessment of Cooperative Efflux of the Multitargeted Kinase Inhibitor Ponatinib Across the Blood-Brain Barrier. Elmquist, WF; Kim, M; Laramy, JK; Parrish, KE; Sarkaria, JN, 2018) | 0.89 |
" We report a population pharmacokinetic model-based analysis for ponatinib and its application to inform dose selection for pediatric development." | ( Population Pharmacokinetics of Ponatinib in Healthy Adult Volunteers and Patients With Hematologic Malignancies and Model-Informed Dose Selection for Pediatric Development. Diderichsen, PM; Gupta, N; Hanley, MJ; Narasimhan, N; Srivastava, S; Venkatakrishnan, K, 2022) | 1.25 |
"This study aimed to investigate the drug-drug interactions of ponatinib with strong, moderate, or weak CYP3A4 inhibitors/inducers by developing physiologically based pharmacokinetic (PBPK) models." | ( Physiologically based pharmacokinetic modeling of ponatinib to describe drug-drug interactions in patients with cancer. Hanada, K; Morita, TO, 2022) | 1.21 |
The study aimed to investigate the drug-drug interactions of ponatinib with strong, moderate, or weak CYP3A4 inhibitors/inducers by developing physiologically based pharmacokinetic (PBPK) models. The PBPK model predicted a significant drug interaction when p onatinib was combined with a strong CYP 3A4 inducer.
Ponatinib (AP24534) is a novel orally bioavailable TKI against T315I Bcr-Abl. It is not clear whether ponatinIB is effective against T674I FIP1L1-PDGFRα. A high ponarinib bioavailability was noted; therefore, we administered it 15 mg/3d to avoid adverse events due to high exposure.
Daily oral dosing of ponatinib (10-30 mg/kg) to mice reduced tumor growth and inhibited signaling in all three tumor models examined. Ponatinib is associated with an increased risk of arterial occlusive events (AOEs)
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. |
[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 |
---|---|
N-methylpiperazine | |
benzamides | |
acetylenic compound | Any organic molecule containing a C#C bond. |
imidazopyridazine | An organic heterobicyclic compound that consists of an imidazole ring ortho-fused to a pyridazine ring. |
(trifluoromethyl)benzenes | An organofluorine compound that is (trifluoromethyl)benzene and derivatives arising from substitution of one or more of the phenyl hydrogens. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Pathway | Proteins | Compounds |
---|---|---|
Ponatinib Inhibition of BCR-ABL | 19 | 1 |
Ponatinib Pathway, Pharmacokinetics/Pharmacodynamics | 6 | 4 |
Acute myeloid leukemia | 0 | 9 |
Endometrial cancer | 0 | 4 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Fumarate hydratase | Homo sapiens (human) | Potency | 11.7704 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
PPM1D protein | Homo sapiens (human) | Potency | 4.1544 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 15.0916 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
EWS/FLI fusion protein | Homo sapiens (human) | Potency | 5.4355 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
G | Vesicular stomatitis virus | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 16.9330 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
polyprotein | Zika virus | Potency | 11.7704 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
tyrosine-protein kinase Yes | Homo sapiens (human) | Potency | 0.0012 | 0.0000 | 5.0182 | 79.2586 | AID686947; AID686948 |
Interferon beta | Homo sapiens (human) | Potency | 6.1127 | 0.0033 | 9.1582 | 39.8107 | AID1347411; AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 3.5481 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 11.9877 | 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 |
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 | 1.8620 | 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 | 0.0830 | 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 |
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 kinase 4 | Homo sapiens (human) | Kd | 0.3070 | 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) | EC50 (µMol) | 0.0036 | 0.0000 | 0.0345 | 0.1400 | AID1301834; AID1301835; AID1659072 |
Tyrosine-protein kinase ABL1 | Homo sapiens (human) | Kd | 0.0125 | 0.0000 | 1.0411 | 13.4530 | AID1424890; AID1801731; AID1801733 |
Proto-oncogene tyrosine-protein kinase Src | Gallus gallus (chicken) | Kd | 0.0007 | 0.0000 | 0.0315 | 0.2960 | AID1801731; AID1801733 |
Epidermal growth factor receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 1.3514 | 20.8270 | AID1424983 |
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 | 0.0240 | 0.0002 | 1.1174 | 24.2210 | AID1425034 |
Tyrosine-protein kinase Fyn | Homo sapiens (human) | Kd | 0.0360 | 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 | 0.2180 | 0.0003 | 1.3708 | 17.1520 | AID1425212 |
Tyrosine-protein kinase Lyn | Homo sapiens (human) | Kd | 0.0270 | 0.0006 | 1.0485 | 5.7000 | AID1425037 |
Proto-oncogene tyrosine-protein kinase receptor Ret | Homo sapiens (human) | Kd | 0.0250 | 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 | 0.0820 | 0.0003 | 2.0343 | 15.9930 | AID1425017 |
Platelet-derived growth factor receptor beta | Homo sapiens (human) | Kd | 3.2850 | 0.0001 | 1.0050 | 11.1070 | AID1425104 |
Tyrosine-protein kinase Fgr | Homo sapiens (human) | Kd | 0.0380 | 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 |
Mast/stem cell growth factor receptor Kit | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 0.8159 | 9.8000 | AID1425032 |
Glycogen phosphorylase, brain form | Homo sapiens (human) | Kd | 30.0000 | 3.5690 | 3.5690 | 3.5690 | AID1425145 |
Breakpoint cluster region protein | Homo sapiens (human) | EC50 (µMol) | 0.0036 | 0.0000 | 0.0393 | 0.1400 | AID1301834; AID1301835; AID1659072 |
Breakpoint cluster region protein | Homo sapiens (human) | Kd | 0.0500 | 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 | 0.3670 | 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 | 1.1940 | 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 | 1.1400 | 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 |
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 | 0.0170 | 0.0009 | 1.0752 | 8.1980 | AID1424988; AID1802323 |
Ephrin type-B receptor 2 | Homo sapiens (human) | Kd | 1.8570 | 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 |
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 | 30.0000 | 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 | 0.0070 | 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 |
Serine/threonine-protein kinase receptor R3 | Homo sapiens (human) | Kd | 30.0000 | 0.0029 | 1.9936 | 9.5000 | AID1424903 |
TGF-beta receptor type-2 | Homo sapiens (human) | Kd | 1.7790 | 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 | 0.3150 | 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 | 0.0200 | 0.0002 | 1.1249 | 14.9240 | AID1424891 |
Tyrosine-protein kinase FRK | Homo sapiens (human) | Kd | 0.0940 | 0.0003 | 1.2424 | 10.8370 | AID1425007 |
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 | 8.0250 | 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 |
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 | 0.4680 | 0.0003 | 2.0274 | 14.7420 | AID1425065 |
Elongation factor Tu, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.4640 | 0.4640 | 0.4640 | AID1425206 |
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 | 30.0000 | 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 |
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 | 0.6910 | 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 | 30.0000 | 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 | 0.5470 | 0.0069 | 2.1713 | 6.4100 | AID1424993 |
Ephrin type-A receptor 5 | Homo sapiens (human) | Kd | 0.0080 | 0.0002 | 1.2100 | 5.9000 | AID1424990 |
Ephrin type-B receptor 4 | Homo sapiens (human) | Kd | 1.4930 | 0.0003 | 2.1678 | 26.3990 | AID1424994 |
Ephrin type-A receptor 4 | Homo sapiens (human) | Kd | 17.1520 | 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 | 1.7290 | 0.0011 | 1.5855 | 10.0000 | AID1424941 |
Cyclin-dependent kinase 17 | Homo sapiens (human) | Kd | 0.3350 | 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 |
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 | 1.8410 | 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 | 0.0180 | 0.0002 | 1.6314 | 71.4840 | AID1424972 |
Mitogen-activated protein kinase kinase kinase kinase 2 | Homo sapiens (human) | Kd | 0.0410 | 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 | 2.9520 | 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 | 0.4930 | 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 | 0.0840 | 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 |
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 | 0.2950 | 0.0011 | 1.9450 | 30.4140 | AID1425143 |
Maternal embryonic leucine zipper kinase | Homo sapiens (human) | Kd | 2.9870 | 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 |
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 |
Dual specificity testis-specific protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0330 | 1.7568 | 5.6000 | AID1425194 |
Myosin light chain kinase, smooth muscle | Homo sapiens (human) | Kd | 0.0990 | 0.0030 | 1.2088 | 7.9000 | AID1425081 |
Mitogen-activated protein kinase 11 | Homo sapiens (human) | Kd | 1.0120 | 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 | 0.1540 | 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 | 0.0870 | 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 |
Uncharacterized aarF domain-containing protein kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.2020 | 0.4990 | 0.7960 | AID1424906 |
Putative heat shock protein HSP 90-beta 2 | Homo sapiens (human) | Kd | 30.0000 | 2.5660 | 2.5660 | 2.5660 | AID1425019 |
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 ULK3 | Homo sapiens (human) | Kd | 1.7200 | 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 |
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 |
ATP-dependent RNA helicase DDX1 | Homo sapiens (human) | Kd | 0.0860 | 0.0860 | 0.0860 | 0.0860 | AID1424974 |
Mitogen-activated protein kinase kinase kinase kinase 1 | Homo sapiens (human) | Kd | 0.7690 | 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 | 1.7660 | 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 |
Protein cereblon | Homo sapiens (human) | EC50 (µMol) | 0.0106 | 0.0090 | 0.0365 | 0.0870 | AID1659072 |
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 |
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 | 2.1360 | 0.0002 | 2.7131 | 14.1960 | AID1425191 |
dCTP pyrophosphatase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.5730 | 1.7403 | 3.0540 | AID1424971 |
Casein kinase I isoform gamma-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0530 | 2.0622 | 5.7000 | AID1424964 |
Serine/threonine-protein kinase PAK 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0004 | 1.9194 | 9.7000 | AID1425101 |
Phenylalanine--tRNA ligase beta subunit | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0045 | 0.0060 | AID1425000 |
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 | 2.1900 | 0.0017 | 3.4719 | 34.1450 | AID1425029 |
Mitogen-activated protein kinase kinase kinase 20 | Homo sapiens (human) | Kd | 0.0410 | 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 | 0.3850 | 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 |
Thyroid hormone receptor-associated protein 3 | Homo sapiens (human) | Kd | 30.0000 | 2.7460 | 2.7460 | 2.7460 | AID1425198 |
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 | 0.0230 | 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 |
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] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Fibroblast growth factor receptor 1 | Homo sapiens (human) | INH | 0.0007 | 0.0007 | 0.0007 | 0.0007 | AID1814374 |
Vascular endothelial growth factor receptor 2 | Homo sapiens (human) | INH | 0.0017 | 0.0008 | 0.0032 | 0.0070 | AID1814373 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1345914 | Human ret proto-oncogene (Type XIV RTKs: RET) | 2013 | Molecular and cellular endocrinology, Sep-05, Volume: 377, Issue:1-2 | Ponatinib is a potent inhibitor of wild-type and drug-resistant gatekeeper mutant RET kinase. |
AID1345673 | Human cyclin dependent kinase 19 (CDK8 subfamily) | 2015 | Nature chemical biology, Dec, Volume: 11, Issue:12 | A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. |
AID1345661 | Human cyclin dependent kinase 8 (CDK8 subfamily) | 2015 | Nature chemical biology, Dec, Volume: 11, Issue:12 | A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. |
AID1345606 | Human ABL proto-oncogene 1, non-receptor tyrosine kinase (Abl family) | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID1817050 | Inhibition of BCR-ABL phosphorylation at tyrosine 245 residue in mouse BaF3 cells at upto 1000 nM measured after 4 hrs by Western blot analysis | |||
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. |
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. |
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. |
AID1716357 | Binding affinity to Nluc-tagged YSK4 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID491314 | Plasma concentration in CD rat at 30 mg/kg, po after 24 hrs by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID491290 | Antiproliferative activity against mouse BA/F3 cells after 3 days by MTS assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID739098 | Cytotoxicity against mouse BA/F3 cells after 48 hrs by XTT assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant. |
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. |
AID1648806 | Inhibition of LCK (unknown origin) assessed as residual activity at 10 uM incubated for 5 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay relative to control | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
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. |
AID1673956 | Inhibition of wild type human ABL using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
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. |
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. |
AID1301840 | Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
AID1435462 | Inhibition of recombinant RET V840M mutant (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
AID491304 | AUC (0 to 24 hrs) in CD rat at 10 mg/kg, po by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID1435450 | Inhibition of recombinant EGFR (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
AID1283290 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | Structure-Activity Relationship Study of Rakicidins: Overcoming Chronic Myeloid Leukemia Resistance to Imatinib with 4-Methylester-Rakicidin A. |
AID1659085 | Toxicity in HUVEC assessed as inhibition of tube formation at 200 nM incubated for 20 hrs by optical microscopy based matrigel-based assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects. |
AID1601504 | Inhibition of human FGFR2 using poly[Glu:Tyr] (4:1) substrate and ATP and [gamma33P]-ATP | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6 | Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects. |
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. |
AID1424903 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID1817091 | Inhibition of human ABL T315I mutant using EAIYAAPFAKKK as substrate at 10 nM incubated for 30 mins followed by 33P-ATP addition and measured after 2 hrs by liquid scintillation counter method relative to control | |||
AID1779906 | Therapeutic index, ratio of CC50 for rat RBL2H3 cells to IC50 for Antiallergic activity against anti-DNP-IgE sensitized rat RBL-2H3 cells | |||
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. |
AID491288 | Antiproliferative activity against mouse BA/F3 cells expressing wild type ABL after 3 days by MTS assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID1716405 | Binding affinity to human FGFR1 using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1895695 | Inhibition of PDGFR (unknown origin) by kinase hotspot 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. |
AID1886533 | Cytotoxicity against HEK293 cells assessed as reduction in cell viability measured after 48 hrs by alamar blue assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
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. |
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. |
AID1659069 | Antiproliferative activity against human K562 cells incubated for 3 days by CCK8 assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects. |
AID1659071 | Antiproliferative activity against wild type mouse BA/F3 cells incubated for 3 days by CCK8 assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects. |
AID1435449 | Inhibition of recombinant VEGFR1 (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
AID1425002 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID491325 | Selectivity for human ABL over CDK2/Cyclin E | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID1895689 | Inhibition of BCR-ABL (unknown origin) by kinase hotspot 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. |
AID1817043 | Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | |||
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. |
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. |
AID1814374 | Inhibition of FGFR1 (unknown origin) at 100 uM incubated for 60 mins by ELISA relative to control | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia. |
AID1716387 | Binding affinity to Nluc-tagged PDGFRalpha (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
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. |
AID1328572 | Inhibition of CCDC6/RET (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23 | Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitors. |
AID1435459 | Antiproliferative activity against mouse BAF3 cells expressing TEL-KDR fusion protein after 72 hrs by CCK8/SRB assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
AID1886529 | Inhibition of recombinant human full-length His-tagged ABL1 T315I mutant cytoplasmic domain expressed in baculovirus infected insect cells using Tyr 02 as substrate measured after 1 hr by Z'-lyte assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
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. |
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. |
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. |
AID1716378 | Binding affinity to Nluc-tagged JAK1 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1673951 | Inhibition of wild type human ABL H396P mutant using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
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. |
AID491333 | Inhibition of human ABL F317V mutant after 2 hrs by TR-FRET assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
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. |
AID1817079 | Inhibition of human ABL Y253F mutant using EAIYAAPFAKKK as substrate assessed as residual activity at 10 nM incubated for 30 mins followed by 33P-ATP addition and measured after 2 hrs by liquid scintillation counter method relative to control | |||
AID491306 | Cmax in CD rat at 30 mg/kg, po by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID1817077 | Half life in ICR mouse at 15 mg/kg, po measured upto 24 hrs by LC/MS/MS analysis | |||
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. |
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. |
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. |
AID1301837 | Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
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. |
AID491324 | Inhibition of recombinant Aurora kinase by Hotspot assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID491343 | Antiproliferative activity against mouse BA/F3 cells expressing ABL F255V mutant after 3 days by MTS assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID1425132 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
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. |
AID1779216 | Cytotoxicity against imatinib mesylate resistant wild-type human KBM5 cells expressing T315I mutant assessed as cell growth inhibition measured after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia. |
AID724975 | Inhibition of human recombinant ABL1 M351T mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
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. |
AID1716375 | Binding affinity to Nluc-tagged YES (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1435453 | Inhibition of recombinant c-Src (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
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. |
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. |
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. |
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. |
AID1817090 | Inhibition of human ABL T315I mutant using EAIYAAPFAKKK as substrate assessed as residual activity at 10 nM incubated for 30 mins followed by 33P-ATP addition and measured after 2 hrs by liquid scintillation counter method relative to control | |||
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. |
AID1409096 | Inhibition of human FGFR1 | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
AID1386091 | Inhibition of BCR-ABL1 E459K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
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. |
AID1716399 | Binding affinity to human FYN using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
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. |
AID1409095 | Inhibition of human KDR | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
AID1465772 | Intrinsic clearance in human 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. |
AID1465775 | Protein binding in human plasma at 5 uM after 6 hrs by equilibrium dialysis method | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
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. |
AID1533737 | Inhibition of FGFR-1 (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Type IIA - Type IIB protein tyrosine kinase inhibitors hybridization as an efficient approach for potent multikinase inhibitor development: Design, synthesis, anti-proliferative activity, multikinase inhibitory activity and molecular modeling of novel ind |
AID1779214 | Cytotoxicity against Bcr-Abl expressing human KU812 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia. |
AID491328 | Selectivity for human ABL over IGF1R | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID1716379 | Binding affinity to Nluc-tagged FYN (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1716371 | Binding affinity to Nluc-tagged CSK (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
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. |
AID724977 | Inhibition of human recombinant ABL1 G250E mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID491286 | Inhibition of wild type human ABL after 1 hr by TR-FRET assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID759167 | Inhibition of wild-type cKIT (unknown origin)-mediated phosphorylation of biotinylated poly-Glu-Tyr preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
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. |
AID1386088 | Inhibition of BCR-ABL1 E255V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
AID1673953 | Inhibition of wild type human ABL Y253F mutant using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
AID1435446 | Inhibition of recombinant FGFR3 (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
AID1425144 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
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. |
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. |
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. |
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. |
AID1817044 | Cytotoxicity against human KU812 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | |||
AID491293 | Inhibition of ABL T315I mutant autophosphorylation | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID1240405 | Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. |
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. |
AID1878098 | Inhibition of ABL (unknown origin) | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia. |
AID1817049 | Inhibition of BCR-ABL phosphorylation at tyrosine 245 residue in human K562 cells at upto 1000 nM measured after 4 hrs by Western blot analysis | |||
AID1817067 | Tmax in ICR mouse at 15 mg/kg, po measured upto 24 hrs by LC/MS/MS analysis | |||
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. |
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. |
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. |
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. |
AID1817080 | Clearance in ICR mouse at 5 mg/kg, iv measured upto 24 hrs by LC/MS/MS analysis | |||
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. |
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. |
AID1716363 | Binding affinity to Nluc-tagged MAP4K5 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1716365 | Binding affinity to Nluc-tagged MAP3K5 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1204917 | Inhibition of RET (unknown origin) | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer. |
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. |
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. |
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. |
AID1283298 | Resistance index, ratio IC50 for mouse BA/F3 cells expressing BCR-ABL T315I mutant to IC50 for human K562 cells | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | Structure-Activity Relationship Study of Rakicidins: Overcoming Chronic Myeloid Leukemia Resistance to Imatinib with 4-Methylester-Rakicidin A. |
AID1895692 | Inhibition of KIT (unknown origin) by kinase hotspot 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. |
AID1856829 | Inhibition of RIP1 (1 to 375 residues) (unknown origin) assessed as substrate phosphorylation using MBP and ATP as substrate at 10 uM preincubated for 15 mins followed by substrate addition and measured after 90 mins by ADP-Glo luminescence assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Discovery of a New Class of Uracil Derivatives as Potential Mixed Lineage Kinase Domain-like Protein (MLKL) Inhibitors. |
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. |
AID1817073 | AUC (0 to infinity) in ICR mouse at 15 mg/kg, po measured upto 24 hrs by LC/MS/MS analysis | |||
AID491295 | Clearance in CD rat at 5 mg/kg, iv by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID1817071 | AUC (0 to t) in ICR mouse at 15 mg/kg, po measured upto 24 hrs by LC/MS/MS 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. |
AID491305 | AUC (0 to 24 hrs) in CD rat at 5 mg/kg, po by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
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. |
AID491332 | Inhibition of human ABL F317L mutant after 2 hrs by TR-FRET assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
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. |
AID1431281 | Inhibition of recombinant human FGFR1 using substrate KKKSPGEYVNIEFG in presence of [33-P]ATP by kinase hotspot assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. |
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. |
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. |
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. |
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. |
AID491341 | Antiproliferative activity against mouse BA/F3 cells expressing ABL Y253H mutant after 3 days by MTS assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID1817059 | Inhibition of hERG | |||
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. |
AID1206215 | Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
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. |
AID1435454 | Inhibition of recombinant ABL (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
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. |
AID1856830 | Inhibition of RIP1 (1 to 375 residues) (unknown origin) assessed as substrate phosphorylation using MBP and ATP as substrate at 1 uM preincubated for 15 mins followed by substrate addition and measured after 90 mins by ADP-Glo luminescence assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Discovery of a New Class of Uracil Derivatives as Potential Mixed Lineage Kinase Domain-like Protein (MLKL) Inhibitors. |
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. |
AID1817047 | Cytotoxicity against human K562 cells assessed as induction of cell death | |||
AID1659079 | Antiproliferative activity against human HUVEC incubated for 3 days by CCK8 assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects. |
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. |
AID1435442 | Inhibition of recombinant FGFR1 (unknown origin) using poly (Glu, Tyr) 4:1 after 60 mins by ELISA method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
AID1659080 | Inhibition of human ABL T315I mutant using EAIYAAPFAKKK substrate and [gamma-33P]-ATP incubated for 40 mins by scintillation counting method | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects. |
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. |
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. |
AID739097 | Cytotoxicity against human K562 cells | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant. |
AID1716377 | Binding affinity to Nluc-tagged FRK (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1611096 | Inhibition of VEGFR2 (unknown origin) at 1 uM using poly (Glu,Tyr) 4:1 as substrate measured after 1 hr in presence of ATP by spectrophotometric analysis relative to control | 2019 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23 | Discovery of arylamide-5-anilinoquinazoline-8-nitro derivatives as VEGFR-2 kinase inhibitors: Synthesis, in vitro biological evaluation and molecular docking. |
AID601429 | Inhibition of human ABL T315I mutant using [EAIYAAPFAKKK] peptide substrate after 2 hrs by TR-FRET assay | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. |
AID739102 | Cytotoxicity against mouse BA/F3 cells transfected with wild type Bcr-Abl after 48 hrs by XTT assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant. |
AID1580373 | Inhibition of recombinant human His-tagged RIPK2 (8 to 317 residues) incubated for 1 hr by ADP-Glo assay | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. |
AID1601505 | Inhibition of human FGFR3 using poly[Glu:Tyr] (4:1) substrate and ATP and [gamma33P]-ATP | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6 | Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects. |
AID491311 | Half life in CD rat at 5 mg/kg, po by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
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. |
AID1648810 | Inhibition of MAP4K3 (unknown origin) assessed as residual activity at 10 uM incubated for 5 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay relative to control | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
AID1465777 | Efflux ratio of apparent permeability across basolateral to apical over apical to basolateral side in human Caco2 cells at 10 uM after 2 hrs by LC-MS/MS | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
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. |
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. |
AID1716390 | Binding affinity to human JAK2 using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1895691 | Inhibition of FLT3 (unknown origin) by kinase hotspot 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. |
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. |
AID1425194 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
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. |
AID1204922 | Inhibition of RET (unknown origin) V804 mutant | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer. |
AID1817038 | Inhibition of human ABL G250E mutant using EAIYAAPFAKKK as substrate assessed as residual activity at 10 nM incubated for 30 mins followed by 33P-ATP addition and measured after 2 hrs by liquid scintillation counter method relative to control | |||
AID1716352 | Binding affinity to Nluc-tagged RIPK2 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
AID1817083 | Inhibition of human ABL1 using EAIYAAPFAKKK as substrate assessed as residual activity at 10 nM incubated for 30 mins followed by 33P-ATP addition and measured after 2 hrs by liquid scintillation counter method relative to control | |||
AID1386084 | Inhibition of BCR-ABL1 G250H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
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. |
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. |
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. |
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. |
AID1817070 | Cmax in ICR mouse at 5 mg/kg, iv measured upto 24 hrs by LC/MS/MS analysis | |||
AID1435448 | Inhibition of recombinant RET (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
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. |
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. |
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. |
AID1905553 | Inhibition of full-length RET kinase expressed in human HEK293 cells and measured by NanoBRET assay | |||
AID1580376 | Anti-neprotic activity in human Jurkat cells assessed as reduction in TNF-induced necroptosis incubated for 24 hrs by cell titer glo-based luminescence assay | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. |
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. |
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. |
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. |
AID491318 | Inhibition of recombinant FLT3 by Hotspot assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID491302 | Oral bioavailability in CD rat at 15 mg/kg by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID1716388 | Binding affinity to MAPK14 (unknown origin) | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
AID1716366 | Binding affinity to Nluc-tagged PRKACA (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1716392 | Binding affinity to human LCK using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID491289 | Antiproliferative activity against mouse BA/F3 cells expressing ABL T315I mutant after 3 days by MTS assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID1240468 | Inhibition of wild type Bcr-Abl (unknown origin) using Tyr2 peptide substrate after 2 hrs by FRET-based Z'-lyte assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. |
AID491322 | Inhibition of recombinant PDGFRalpha by Hotspot assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID1371339 | Inhibition of human RIPK2 expressed in Sf9 cells after 1 hr by ADP-Glo assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8 | Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins. |
AID1435443 | Inhibition of recombinant KDR (unknown origin) using poly (Glu, Tyr) 4:1 after 60 mins by ELISA method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
AID1386089 | Inhibition of BCR-ABL1 E355G mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
AID759137 | Growth inhibition of human LMS676 cells at 0.1 to 0.8 uM after 72 hrs by SRB assay relative to control | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
AID1854094 | Inhibition of recombinant VEGFR2 (unknown origin) in presence of [33P]-ATP by kinase hotspot assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | The progress of small-molecules and degraders against BCR-ABL for the treatment of CML. |
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. |
AID759158 | Inhibition of KIT in human GISTT1 cells assessed as growth inhibition after 72 hrs by SRB assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
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. |
AID1814373 | Inhibition of KDR (unknown origin) at 100 uM incubated for 60 mins by ELISA relative to control | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11 | Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia. |
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. |
AID491300 | Tmax in CD rat at 15 mg/kg, po by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
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. |
AID1737427 | Inhibition of FLT3 (unknown origin) | |||
AID759165 | Inhibition of cKIT V559D/T670I double mutant (unknown origin)-mediated phosphorylation of biotinylated poly-Glu-Tyr preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
AID1611098 | Antiproliferative activity against human HUVEC cells expressing VEGFR2 assessed as cell growth inhibition measured after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23 | Discovery of arylamide-5-anilinoquinazoline-8-nitro derivatives as VEGFR-2 kinase inhibitors: Synthesis, in vitro biological evaluation and molecular docking. |
AID491301 | Half life in CD rat at 15 mg/kg, po by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID1817076 | MRT in ICR mouse at 5 mg/kg, iv measured upto 24 hrs by LC/MS/MS analysis | |||
AID1386090 | Inhibition of BCR-ABL1 F359V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
AID1659082 | Inhibition of human c-SRC using poly(Glu,Tyr)4:1 substrate and [gamma-33P]-ATP incubated for 40 mins by scintillation counting method | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects. |
AID1886524 | Growth inhibition of human K562 cells expressing BCR-ABL T315I mutant measured after 48 hrs by alamarblue assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
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. |
AID1580374 | Inhibition of recombinant GST-tagged RIPK3 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 4 hrs by ADP-Glo assay | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. |
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. |
AID491319 | Inhibition of recombinant FGFR by Hotspot assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID1648809 | Inhibition of VEGFR (unknown origin) assessed as residual activity at 10 uM incubated for 5 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay relative to control | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
AID1454442 | Displacement of CAT-1 from catalytic site of N-terminal His6-tagged ABL T315I mutant (unknown origin) at 25 uM by 19F NMR spectroscopy based dual-site competition assay | 2017 | ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6 | |
AID1454437 | Displacement of CAT-1 from catalytic site of N-terminal His6-tagged ABL (83 to 534 residues) (unknown origin) expressed in Escherichia coli co-expressing Protein Tyrosine Phosphatase 1b at 25 uM by 19F NMR spectroscopy based dual-site competition assay | 2017 | ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6 | |
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. |
AID1716368 | Binding affinity to Nluc-tagged JAK2 JH2 catalytic domain (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
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. |
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. |
AID491310 | Half life in CD rat at 10 mg/kg, po by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID491339 | Antiproliferative activity against mouse BA/F3 cells expressing ABL F317L mutant after 3 days by MTS assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
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. |
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. |
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. |
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. |
AID1716351 | Binding affinity to Nluc-tagged MEK5 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
AID1435479 | Antitumor activity against FGFR2-amplified human SNU16 cells xenografted in nude mouse assessed as tumor growth inhibition at 30 mg/kg, po qd administered for 18 days and measured on day 18 post last dose relative to vehicle-treated control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
AID1716380 | Binding affinity to Nluc-tagged ABL1 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1716386 | Binding affinity to Nluc-tagged EPHA1 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID759170 | Inhibition of chicken wild-type cSRC (251 to 533)-mediated phosphorylation of biotinylated poly-Glu-Tyr expressed in Escherichia coli BL21(DE3) preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
AID1716360 | Binding affinity to Nluc-tagged CAMK2G (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1648807 | Inhibition of EPHB4 (unknown origin) assessed as residual activity at 10 uM incubated for 5 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay relative to control | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
AID1817075 | MRT in ICR mouse at 15 mg/kg, po measured upto 24 hrs by LC/MS/MS analysis | |||
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. |
AID1435457 | Antiproliferative activity against FGFR3-amplified human RT112 cells after 72 hrs by CCK8/SRB assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
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. |
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. |
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. |
AID1876282 | Inhibition of SRC (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID1673955 | Inhibition of wild type human ABL T315I mutant using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
AID1611099 | Antiproliferative activity against human HepG2 cells expressing VEGFR2 assessed as cell growth inhibition measured after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23 | Discovery of arylamide-5-anilinoquinazoline-8-nitro derivatives as VEGFR-2 kinase inhibitors: Synthesis, in vitro biological evaluation and molecular docking. |
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. |
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. |
AID1854091 | Inhibition of recombinant wild type Abl (unknown origin) in presence of [33P]-ATP by radiometric hotspot assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | The progress of small-molecules and degraders against BCR-ABL for the treatment of CML. |
AID1301838 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
AID1386087 | Inhibition of BCR-ABL1 E255K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
AID1716350 | Binding affinity to Nluc-tagged GRK1 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID491316 | Antitumor activity against mouse BA/F3 cells expressing ABL T315I mutant xenografted in nude mouse assessed as increase in overall survival at 30 mg/kg, po QD for 19 days | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID1601506 | Inhibition of human FGFR4 using poly[Glu:Tyr] (4:1) substrate and ATP and [gamma33P]-ATP | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6 | Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects. |
AID1648802 | Inhibition of PDGFRalpha (unknown origin) assessed as residual activity at 10 uM incubated for 5 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay relative to control | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
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. |
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. |
AID1648797 | Metabolic stability in mouse liver microsomes assessed as half life at 3 uM measured up to 30 mins in presence of NADPH by LS-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
AID1878041 | Inhibition of FLT3 (unknown origin) | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia. |
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. |
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. |
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. |
AID1716384 | Binding affinity to Nluc-tagged FLT1 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
AID1716407 | Binding affinity to human PDGFRalpha using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1716402 | Binding affinity to human IGF1R using KKKSPGEYVNIEFG as substrate by radiometric hotspot kinase assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1431278 | Inhibition of recombinant human ABL using peptide substrate EAIYAAPFAKKK in presence of [33-P]ATP by kinase hotspot assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. |
AID1716361 | Binding affinity to Nluc-tagged STK16 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
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. |
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. |
AID1431279 | Inhibition of recombinant human Lyn using peptide substrate poly[Glu:Tyr] (4:1) in presence of [33-P]ATP by kinase hotspot assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. |
AID1425153 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1611102 | Cytotoxicity against human LO2 cells | 2019 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23 | Discovery of arylamide-5-anilinoquinazoline-8-nitro derivatives as VEGFR-2 kinase inhibitors: Synthesis, in vitro biological evaluation and molecular docking. |
AID1435455 | Antiproliferative activity against FGFR2-amplified human NCI-H1581 cells after 72 hrs by CCK8/SRB assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
AID1896644 | Inhibition of GST tagged recombinant RIPK3 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 4 hrs by ADP-glo assay | 2022 | Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22 | Small-Molecule Receptor-Interacting Protein 1 (RIP1) Inhibitors as Therapeutic Agents for Multifaceted Diseases: Current Medicinal Chemistry Insights and Emerging Opportunities. |
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. |
AID601430 | Antiproliferative activity against mouse BA/F3 cells expressing wild type BCR-ABL | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. |
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. |
AID1386050 | Inhibition of wild type BCR-ABL1 (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
AID491309 | Half life in CD rat at 30 mg/kg, po by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
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. |
AID1779904 | Antiallergic activity against anti-DNP-IgE sensitized rat RBL-2H3 cells assessed as induction of degranulation by measuring beta-hexosaminidase release using P-nitrophenyl-N-acetyl-D-glucosamide as substrate measured after 1 hr by microplate reader | |||
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. |
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. |
AID491298 | Dose normalized AUC (0 to 24 hrs) in CD rat at 15 mg/kg, po by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
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. |
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. |
AID1425019 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID1182700 | Antiproliferative activity against human HMC-1.2 cells carrying V560G, D816V mutant assessed as cell growth inhibition by MTT assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Development and biological evaluation of potent and selective c-KIT(D816V) inhibitors. |
AID1716364 | Binding affinity to Nluc-tagged MAP4K1 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
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. |
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. |
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. |
AID1175334 | Inhibition of FGFR1 (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3β (GSK-3β) with cellular activity of promoting glucose uptake. |
AID1854096 | Inhibition of recombinant SRC (unknown origin) in presence of [33P]-ATP by kinase hotspot assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | The progress of small-molecules and degraders against BCR-ABL for the treatment of CML. |
AID1301835 | Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
AID1716395 | Binding affinity to human YES using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1817051 | Inhibition of BCR-ABL phosphorylation at tyrosine 245 residue in mouse BaF3 cells expressing T315I mutant at up to 1000 nM measured after 4 hrs by Western blot analysis | |||
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. |
AID1817082 | Oral bioavailability in ICR mouse at 15 mg/kg measured upto 24 hrs by LC/MS/MS analysis | |||
AID1716376 | Binding affinity to Nluc-tagged LYN (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1817088 | Inhibition of human ABL M351T mutant using EAIYAAPFAKKK as substrate assessed as residual activity at 10 nM incubated for 30 mins followed by 33P-ATP addition and measured after 2 hrs by liquid scintillation counter method relative to control | |||
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. |
AID1779215 | Cytotoxicity against Imatinib mesylate sensitive wild-type human KBM5 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia. |
AID491296 | Volume of distribution in CD rat at 5 mg/kg, iv by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
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. |
AID1716385 | Binding affinity to Nluc-tagged FGFR1 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1716358 | Binding affinity to Nluc-tagged AAK1 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
AID1716355 | Binding affinity to Nluc-tagged SIK1 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1896643 | Inhibition of GST tagged recombinant RIPK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 4 hrs by ADP-glo assay | 2022 | Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22 | Small-Molecule Receptor-Interacting Protein 1 (RIP1) Inhibitors as Therapeutic Agents for Multifaceted Diseases: Current Medicinal Chemistry Insights and Emerging Opportunities. |
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. |
AID1817045 | Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | |||
AID491307 | Cmax in CD rat at 10 mg/kg, po by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID1716381 | Binding affinity to Nluc-tagged LTK (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1716394 | Binding affinity to human HCK using KVEKIGEGTYGVVYK as substrate by radiometric hotspot kinase assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID491337 | Inhibition of human ABL F359V mutant after 2 hrs by TR-FRET assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
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. |
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. |
AID1648805 | Inhibition of EPHB3 (unknown origin) assessed as residual activity at 10 uM incubated for 5 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay relative to control | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
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. |
AID1817042 | Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay | |||
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. |
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. |
AID759169 | Inhibition of cSRC T338M mutant (unknown origin)-mediated phosphorylation of biotinylated poly-Glu-Tyr preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
AID1435447 | Inhibition of recombinant FGFR4 (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
AID1425126 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID1716393 | Binding affinity to human SRC using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
AID1716372 | Binding affinity to Nluc-tagged LCK (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1817085 | Inhibition of human ABL E255K mutant using EAIYAAPFAKKK as substrate assessed as residual activity at 10 nM incubated for 30 mins followed by 33P-ATP addition and measured after 2 hrs by liquid scintillation counter method relative to control | |||
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. |
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. |
AID759166 | Inhibition of ABL T315I mutant (unknown origin)-mediated phosphorylation of biotinylated poly-Glu-Tyr preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
AID1240469 | Inhibition of Bcr-Abl T315I mutant (unknown origin) using Tyr2 peptide substrate after 2 hrs by FRET-based Z'-lyte assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. |
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. |
AID1206216 | Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
AID1301834 | Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
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. |
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. |
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. |
AID1435444 | Antiproliferative activity against FGFR1-translocated human KG1 cells after 72 hrs by CCK8/SRB assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
AID1425201 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1659083 | Inhibition of human VEGFR2 using MBP substrate and [gamma-33P]-ATP incubated for 40 mins by scintillation counting method | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects. |
AID1716369 | Binding affinity to Nluc-tagged JAK2 JH1 catalytic domain (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
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. |
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. |
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. |
AID1435460 | Antiproliferative activity against mouse BAF3 cells expressing CCDC6-RET fusion protein after 72 hrs by CCK8/SRB assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
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. |
AID1435456 | Antiproliferative activity against FGFR2-amplified human SNU16 cells after 72 hrs by CCK8/SRB assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
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. |
AID1716400 | Binding affinity to LTK (unknown origin) | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
AID491330 | Selectivity for human ABL over c-Met | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID1424906 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1832756 | Antiproliferative activity against T315I mutant expressing human K-562R cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 10-15, Volume: 48 | Design, synthesis, and biological evaluation of novel Bcr-Abl |
AID1716389 | Binding affinity to PRKACA (unknown origin) | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
AID1895694 | Inhibition of VEGFR (unknown origin) by kinase hotspot 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. |
AID491287 | Inhibition of human ABL T315I mutant after 2 hrs by TR-FRET assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID491308 | Cmax in CD rat at 5 mg/kg, po by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID759168 | Inhibition of human wild-type ABL (Ser229 to Gln513)-mediated phosphorylation of biotinylated poly-Glu-Tyr expressed in Escherichia coli BL21(DE3) preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
AID1779905 | Cytotoxicity against rat RBL2H3 cells assessed as cell viability incubated for 24 hrs by CCK-8 assay | |||
AID1240407 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. |
AID1648795 | Metabolic stability in human liver microsomes assessed as half life at 3 uM measured up to 30 mins in presence of NADPH by LS-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
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. |
AID1648798 | Inhibition of human recombinant CYP3A4 expressed in insect cell microsomes in presence of NADPH by fluorescence assay | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
AID1716370 | Binding affinity to Nluc-tagged JAK2 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1425101 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1283286 | Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | Structure-Activity Relationship Study of Rakicidins: Overcoming Chronic Myeloid Leukemia Resistance to Imatinib with 4-Methylester-Rakicidin A. |
AID1301839 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
AID1580375 | Inhibition of Abl (unknown origin) incubated for 1 hr by ADP-Glo assay | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. |
AID491340 | Antiproliferative activity against mouse BA/F3 cells expressing ABL F317V mutant after 3 days by MTS assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID1886523 | Growth inhibition of human K562 cells measured after 48 hrs by alamarblue assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
AID1873223 | Inhibition of ABCG2 (unknown origin) expressed in human MCF7 cells membrane mediated [125I]iodoarylazidoprazosin photolabelling for 5 mins by radiometric scintillation analysis | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators. |
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. |
AID1659078 | Antiproliferative activity against rat H9C2 cells incubated for 3 days by CCK8 assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects. |
AID1716401 | Binding affinity to human ABL1 using EAIYAAPFAKKK as substrate by radiometric hotspot kinase assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
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. |
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. |
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. |
AID1817074 | AUC (0 to infinity) in ICR mouse at 5 mg/kg, iv measured upto 24 hrs by LC/MS/MS analysis | |||
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. |
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. |
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. |
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. |
AID491317 | Toxicity in nude mouse xenografted with mouse BA/F3 cells expressing ABL T315I mutant at 10 mg/kg, po QD for 19 days | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID1856832 | Inhibition of full length RIP3 (unknown origin) assessed as substrate phosphorylation using MBP and ATP as substrate at 1 uM preincubated for 15 mins followed by substrate addition and measured after 90 mins by ADP-Glo luminescence assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Discovery of a New Class of Uracil Derivatives as Potential Mixed Lineage Kinase Domain-like Protein (MLKL) Inhibitors. |
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. |
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. |
AID724979 | Inhibition of human recombinant ABL1 E255K mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
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. |
AID1648799 | Inhibition of human ERG incubated for 4 hrs by competitive fluorescence tracer binding based assay | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
AID1386085 | Inhibition of BCR-ABL1 Q252H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
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. |
AID1328571 | Inhibition of RET (unknown origin) using poly[Glu:Tyr] (4:1) as substrate after 60 mins by ELISA | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23 | Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitors. |
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. |
AID1895693 | Inhibition of FGFR (unknown origin) by kinase hotspot 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. |
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. |
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. |
AID1817081 | Volume of distribution at steady state in ICR mouse at 5 mg/kg, iv measured upto 24 hrs by LC/MS/MS analysis | |||
AID1854095 | Inhibition of recombinant FGFR1 (unknown origin) in presence of [33P]-ATP by kinase hotspot assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | The progress of small-molecules and degraders against BCR-ABL for the treatment of CML. |
AID491315 | Antitumor activity against mouse BA/F3 cells expressing ABL T315I mutant xenografted in nude mouse assessed as increase in overall survival at 10 mg/kg, po QD for 19 days | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID1895688 | Inhibition of RET (unknown origin) by kinase hotspot 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. |
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. |
AID1611100 | Antiproliferative activity against human A549 cells expressing EGFR assessed as cell growth inhibition measured after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23 | Discovery of arylamide-5-anilinoquinazoline-8-nitro derivatives as VEGFR-2 kinase inhibitors: Synthesis, in vitro biological evaluation and molecular docking. |
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. |
AID1435461 | Antiproliferative activity against mouse BAF3 cells expressing CCDC6-RET V840M mutant after 72 hrs by CCK8/SRB assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
AID1673952 | Inhibition of wild type human ABL M351T mutant using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
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. |
AID1601503 | Inhibition of human FGFR1 using poly[Glu:Tyr] (4:1) substrate and ATP and [gamma33P]-ATP | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6 | Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects. |
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. |
AID1435445 | Inhibition of recombinant FGFR2 (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
AID759136 | Growth inhibition of human MPNST cells at 0.1 to 0.8 uM after 72 hrs by SRB assay relative to control | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
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. |
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. |
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. |
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. |
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. |
AID1673954 | Inhibition of wild type human ABL Q252H mutant using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
AID1648804 | Inhibition of EPHB2 (unknown origin) assessed as residual activity at 10 uM incubated for 5 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay relative to control | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
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. |
AID1648808 | Inhibition of NEK6 (unknown origin) assessed as residual activity at 10 uM incubated for 5 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay relative to control | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
AID491342 | Antiproliferative activity against mouse BA/F3 cells expressing ABL F255K mutant after 3 days by MTS assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID1611101 | Antiproliferative activity against human MDA-MB-231 cells expressing EGFR assessed as cell growth inhibition measured after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23 | Discovery of arylamide-5-anilinoquinazoline-8-nitro derivatives as VEGFR-2 kinase inhibitors: Synthesis, in vitro biological evaluation and molecular docking. |
AID1435452 | Inhibition of recombinant PDGFRbeta (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
AID1833212 | Reversible covalent binding affinity to recombinant His-tagged human FGFR4 expressed in baculovirus expression system assessed as recovery of kinase activity preincubated for 120 mins followed by dialysis of protein for 3 days by MALDI-TOF MS analysis rel | 2021 | Bioorganic & medicinal chemistry, 11-15, Volume: 50 | Characterization of an aromatic trifluoromethyl ketone as a new warhead for covalently reversible kinase inhibitor design. |
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. |
AID491335 | Inhibition of human ABL F255K mutant after 2 hrs by TR-FRET assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID491331 | Inhibition of human ABL T315A mutant after 2 hrs by TR-FRET assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID491320 | Inhibition of recombinant VEGFR by Hotspot assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID1206214 | Inhibition of human Src | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9 | Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer. |
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. |
AID1425198 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID1856831 | Inhibition of full length RIP3 (unknown origin) assessed as substrate phosphorylation using MBP and ATP as substrate at 10 uM preincubated for 15 mins followed by substrate addition and measured after 90 mins by ADP-Glo luminescence assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Discovery of a New Class of Uracil Derivatives as Potential Mixed Lineage Kinase Domain-like Protein (MLKL) Inhibitors. |
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. |
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. |
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. |
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. |
AID491292 | Inhibition of ABL autophosphorylation | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID491312 | Plasma concentration in CD rat at 30 mg/kg, po after 2 hrs by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID491313 | Plasma concentration in CD rat at 30 mg/kg, po after 6 hrs by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID601432 | Antiproliferative activity against BCR-ABL-negative parental mouse BA/F3 cells | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. |
AID1301836 | Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
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. |
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. |
AID1716367 | Binding affinity to Nluc-tagged MAPK14 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
AID1484901 | Inhibition of KDR (unknown origin) using poly (Glu, Tyr) 4:1 as substrate at after 1 hr by ELISA | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer. |
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. |
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. |
AID1854092 | Inhibition of recombinant Abl-T315I mutant (unknown origin) in presence of [33P]-ATP by kinase hotspot assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | The progress of small-molecules and degraders against BCR-ABL for the treatment of CML. |
AID1865233 | Binding affinity to P38alpha (unknown origin) measured at 0.05 to 333.33 nM after 600 secs by SPR analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18 | A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
AID1896641 | Anti-necroptic activity in TNF alpha stimulated FADD-deficient human Jurkat T cells incubated for 24 hrs by celltiter-glo luminescent cell viability assay | 2022 | Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22 | Small-Molecule Receptor-Interacting Protein 1 (RIP1) Inhibitors as Therapeutic Agents for Multifaceted Diseases: Current Medicinal Chemistry Insights and Emerging Opportunities. |
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. |
AID1386086 | Inhibition of BCR-ABL1 Y253H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
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. |
AID1854093 | Inhibition of recombinant PDGFRalpha (unknown origin) in presence of [33P]-ATP by kinase hotspot assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | The progress of small-molecules and degraders against BCR-ABL for the treatment of CML. |
AID1817086 | Inhibition of human ABL F317I mutant using EAIYAAPFAKKK as substrate assessed as residual activity at 10 nM incubated for 30 mins followed by 33P-ATP addition and measured after 2 hrs by liquid scintillation counter method relative to control | |||
AID1895696 | Inhibition of RET V804M (unknown origin) in presence of ATP by SDS-PAGE analysis | 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. |
AID724980 | Inhibition of human recombinant ABL1 T315I mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
AID1817041 | Inhibition of cell proliferation in mouse BaF3 cells expressing BCR-ABL T315I mutant assessed as cell viability at 100 uM measured after 48 hrs by trypan blue based assay (RVB=100%) | |||
AID1580372 | Inhibition of recombinant GST-tagged RIPK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 4 hrs by ADP-Glo assay | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. |
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. |
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. |
AID1886527 | Cytotoxicity against human iPSC-CM cells assessed as reduction in contractile alterations or amplitude in cell voltage by VF2.1.Cl dye based assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
AID1716362 | Binding affinity to Nluc-tagged STK4 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1648801 | Inhibition of DDR2 (unknown origin) assessed as residual activity at 10 uM incubated for 5 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay relative to control | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
AID724974 | Inhibition of human recombinant ABL1 Y253F mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
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. |
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. |
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. |
AID1716403 | Binding affinity to DDR1 (unknown origin) at 5 uM | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
AID1905552 | Inhibition of human RET kinase using IGF1Rtide as substrate incubated for 40 mins and measured by ADP-Glo assay | |||
AID1817089 | Inhibition of human ABL Q252H mutant using EAIYAAPFAKKK as substrate assessed as residual activity at 10 nM incubated for 30 mins followed by 33P-ATP addition and measured after 2 hrs by liquid scintillation counter method relative to control | |||
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. |
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. |
AID1465776 | Protein binding in mouse plasma at 5 uM after 6 hrs by equilibrium dialysis method | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
AID1716397 | Binding affinity to human FRK using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
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. |
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. |
AID1648803 | Inhibition of SRC (unknown origin) assessed as residual activity at 10 uM incubated for 5 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay relative to control | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
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. |
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. |
AID724976 | Inhibition of human recombinant ABL1 H396P mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
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. |
AID1716373 | Binding affinity to Nluc-tagged SRC (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID739394 | Inhibition of breakpoint cluster region-Abelson tyrosine kinase T315I mutant (unknown origin) using [gamma-33P]ATP as substrate by radiometric kinase assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant. |
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. |
AID724981 | Inhibition of human recombinant wild type ABL1 expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
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. |
AID724978 | Inhibition of human recombinant ABL1 Q252H mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
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. |
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. |
AID1817055 | Antitumor activity against mouse BaF3 cells expressing BCR-ABL T315I mutant xenografted in BALB/c-nu mouse assessed as tumor growth inhibition at 5 mg/kg, po administered once daily for 15 days relative to control | |||
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. |
AID1716404 | Binding affinity to FLT1 (unknown origin) | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
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. |
AID1716374 | Binding affinity to Nluc-tagged HCK (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1156109 | Inhibition of VEGFR2 (unknown origin) using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2014 | ACS medicinal chemistry letters, Jun-12, Volume: 5, Issue:6 | Discovery of Anilinopyrimidines as Dual Inhibitors of c-Met and VEGFR-2: Synthesis, SAR, and Cellular Activity. |
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. |
AID1611097 | Inhibition of EGFR (unknown origin) at 1 uM using poly (Glu,Tyr) 4:1 as substrate measured after 1 hr in presence of ATP by spectrophotometric analysis relative to control | 2019 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23 | Discovery of arylamide-5-anilinoquinazoline-8-nitro derivatives as VEGFR-2 kinase inhibitors: Synthesis, in vitro biological evaluation and molecular docking. |
AID1716354 | Binding affinity to Nluc-tagged SLK (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1659081 | Inhibition of human LYN using poly(Glu,Tyr)4:1 substrate and [gamma-33P]-ATP incubated for 40 mins by scintillation counting method | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects. |
AID491327 | Selectivity for human ABL over FAK | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID1328573 | Inhibition of CCDC6/RET V804M mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23 | Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitors. |
AID491323 | Inhibition of recombinant PDGFRbeta by Hotspot assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID1886528 | Inhibition of recombinant human full-length His-tagged ABL1 cytoplasmic domain expressed in baculovirus expression system using Tyr 02 as substrate measured after 1 hr by Z'-lyte assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
AID1817068 | Tmax in ICR mouse at 5 mg/kg, iv measured upto 24 hrs by LC/MS/MS analysis | |||
AID491338 | Antiproliferative activity against mouse BA/F3 cells expressing ABL T315A mutant after 3 days by MTS assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID1386051 | Inhibition of BCR-ABL1 T315I mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
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. |
AID491299 | Cmax in CD rat at 15 mg/kg, po by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID1779907 | Inhibition of human recombinant CSF1R using ATP/Ulight-TK peptide incubated for 15 mins | |||
AID1817072 | AUC (0 to t) in ICR mouse at 5 mg/kg, iv measured upto 24 hrs by LC/MS/MS analysis | |||
AID1878093 | Inhibition of TrkA (unknown origin) | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia. |
AID1175333 | Inhibition of KDR (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3β (GSK-3β) with cellular activity of promoting glucose uptake. |
AID1435451 | Inhibition of recombinant PDGFRalpha (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
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. |
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. |
AID1716396 | Binding affinity to LYN (unknown origin) | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
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. |
AID491336 | Inhibition of human ABL F255V mutant after 2 hrs by TR-FRET assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
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. |
AID1431280 | Inhibition of recombinant human VEGFR2 using substrate poly[Glu:Tyr] (4:1) in presence of [33-P]ATP by kinase hotspot assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. |
AID1860259 | Antiproliferative activity against human K-562R cells expressing Bcr-Abl T315I mutant assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | |||
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. |
AID1648800 | Inhibition of ABL1 (unknown origin) assessed as residual activity at 10 uM incubated for 5 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay relative to control | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
AID491344 | Antiproliferative activity against mouse BA/F3 cells expressing ABL F359V mutant after 3 days by MTS assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID1409614 | Overall antiviral activity against SARS-CoV-2 (isolate France/IDF0372/2020) in the Vero E6 cell line at 48 h based on three assays 1) detection of viral RNA by qRT-PCR (targeting the N-gene), 2) plaque assay using lysate 3 days after addition of compound | 2020 | Nature, 07, Volume: 583, Issue:7816 | A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
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. |
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. |
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. |
AID491334 | Inhibition of human ABL Y253H mutant after 2 hrs by TR-FRET assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID759138 | Growth inhibition of human LPS141 cells at 0.1 to 0.8 uM after 72 hrs by SRB assay relative to control | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
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. |
AID1817078 | Half life in ICR mouse at 5 mg/kg, iv measured upto 24 hrs by LC/MS/MS analysis | |||
AID491326 | Selectivity for human ABL over EGFR | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
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. |
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. |
AID1659072 | Protac activity at Cereblon/BCR/ABL T315I mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in BCR-ABL T315I mutant driven cell viability incubated for 3 days by CCK8 assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects. |
AID1817046 | Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | |||
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. |
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. |
AID1425032 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID759134 | Growth inhibition of human LPS141 cells at 0.001 to 10 uM after 72 hrs by SRB assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
AID1817069 | Cmax in ICR mouse at 15 mg/kg, po measured upto 24 hrs by LC/MS/MS analysis | |||
AID1435458 | Antiproliferative activity against mouse BAF3 cells expressing TEL-FGFR4 fusion protein after 72 hrs by CCK8/SRB assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
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. |
AID1817039 | Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT assay | |||
AID1716391 | Binding affinity to human CSK using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1716359 | Binding affinity to Nluc-tagged PIM1 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1716356 | Binding affinity to Nluc-tagged PKN1 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1817087 | Inhibition of human ABL H396P mutant using EAIYAAPFAKKK as substrate assessed as residual activity at 10 nM incubated for 30 mins followed by 33P-ATP addition and measured after 2 hrs by liquid scintillation counter method relative to control | |||
AID1716398 | Binding affinity to human JAK1 using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID601431 | Antiproliferative activity against mouse BA/F3 cells expressing ABL T315I mutant | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. |
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. |
AID491297 | Half life in CD rat at 5 mg/kg, iv by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID491321 | Inhibition of recombinant c-Kit by Hotspot assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
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. |
AID491329 | Selectivity for human ABL over JAK2 | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID759135 | Growth inhibition of human LMS676 cells at 0.001 to 10 uM after 72 hrs by SRB assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
AID759155 | Growth inhibition of human GIST48B cells after 72 hrs by SRB assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
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. |
AID1856828 | Anti-necroptic activity in human HT-29 cells assessed as inhibition of TSZ (TNFalpha, Smac mimetic and z-VAD-FMK) induced necroptosis incubated for 24 hrs by celltiter-glo luminescent cell viability assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Discovery of a New Class of Uracil Derivatives as Potential Mixed Lineage Kinase Domain-like Protein (MLKL) Inhibitors. |
AID1716382 | Binding affinity to Nluc-tagged IGF1R (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1881789 | Inhibition of MNK2 (unknown origin) at 123 nM | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Update on the Development of MNK Inhibitors as Therapeutic Agents. |
AID1716406 | Binding affinity to human EPHA1 using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
AID1817040 | Inhibition of cell proliferation in human K562 assessed as cell viability at 100 uM measured after 48 hrs by trypan blue based assay (RVB=100%) | |||
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. |
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. |
AID1895690 | Inhibition of SRC (unknown origin) by kinase hotspot 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. |
AID1886532 | Vasculo-toxicity in human HMVEC cells assessed as reduction in vascular structure integrity by measuring AUC measured after 6 hrs by calcein AM dye based fluorescence assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
AID1716383 | Binding affinity to Nluc-tagged DDR1 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
AID1648793 | Inhibition of human ABL1 assessed as residual activity using EAIYAAPFAKKK as substrate by [gamma-33P]-ATP assay | 2020 | ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4 | Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease. |
AID491303 | AUC (0 to 24 hrs) in CD rat at 30 mg/kg, po by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th |
AID759133 | Growth inhibition of human MPNST cells at 0.001 to 10 uM after 72 hrs by SRB assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
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. |
AID1716353 | Binding affinity to Nluc-tagged IRAK4 (unknown origin) expressed in HeLa cells assessed as change in melting temperature incubated for 30 to 60 mins by NaLTSA assay | 2018 | ACS medicinal chemistry letters, Jun-14, Volume: 9, Issue:6 | Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift. |
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. |
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. |
AID759157 | Inhibition of KIT T670I mutant in human GISTT1 cells assessed as growth inhibition after 72 hrs by SRB assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
AID601428 | Inhibition of wild type human ABL using [EAIYAAPFAKKK] peptide substrate after 1 hr by TR-FRET assay | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. |
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. |
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. |
AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
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. |
AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
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. |
AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Identification of potent Yes1 kinase inhibitors using a library screening approach. |
AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
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. |
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. |
AID1802324 | HotSpot Kinase Activity Assay from Article 10.1021/acschembio.6b00709: \\Chemical Proteomics and Structural Biology Define EPHA2 Inhibition by Clinical Kinase Drugs.\\ | 2016 | ACS chemical biology, 12-16, Volume: 11, Issue:12 | Chemical Proteomics and Structural Biology Define EPHA2 Inhibition by Clinical Kinase Drugs. |
AID1799755 | Inhibition Assay from Article 10.1021/cb300128b: \\Targeting GSK3 from Ustilago maydis: Type-II Kinase Inhibitors as Potential Antifungals.\\ | 2012 | ACS chemical biology, Jul-20, Volume: 7, Issue:7 | Targeting GSK3 from Ustilago maydis: type-II kinase inhibitors as potential antifungals. |
AID1801733 | Kinome-Wide Inhibitor Profiling for Phosphorylated c-Abl from Article 10.1021/acschembio.5b01018: \\Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.\\ | 2016 | ACS chemical biology, 05-20, Volume: 11, Issue:5 | Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity. |
AID1802830 | LRRK2 Kinase Assay from Article 10.1074/jbc.M113.537811: \\The Parkinson disease-linked LRRK2 protein mutation I2020T stabilizes an active state conformation leading to increased kinase activity.\\ | 2014 | The Journal of biological chemistry, May-09, Volume: 289, Issue:19 | The Parkinson disease-linked LRRK2 protein mutation I2020T stabilizes an active state conformation leading to increased kinase activity. |
AID1801731 | Kinome-Wide Inhibitor Profiling from Article 10.1021/acschembio.5b01018: \\Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.\\ | 2016 | ACS chemical biology, 05-20, Volume: 11, Issue:5 | Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity. |
[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 | 1 (0.19) | 29.6817 |
2010's | 333 (63.19) | 24.3611 |
2020's | 193 (36.62) | 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 (67.13) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 34 (6.32%) | 5.53% |
Reviews | 72 (13.38%) | 6.00% |
Case Studies | 81 (15.06%) | 4.05% |
Observational | 6 (1.12%) | 0.25% |
Other | 345 (64.13%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
OPEN LABEL PHASE 2 STUDY ON THE EFFICACY AND TOLERANCE OF A COMBINATION OF PONATINIB AND 5-AZACITIDINE IN CHRONIC MYELOGENOUS LEUKAEMIA IN ACCELERATED PHASE OR IN MYELOID BLAST CRISIS - PONAZA TRIAL [NCT03895671] | Phase 2 | 40 participants (Anticipated) | Interventional | 2019-06-19 | Recruiting | ||
Newly Diagnosed Adult Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia (Ph+ ALL). Sequential Treatment With Ponatinib and the Bispecific Monoclonal Antibody Blinatumomab vs Chemotherapy and Imatinib [NCT04722848] | Phase 3 | 236 participants (Anticipated) | Interventional | 2021-09-08 | Recruiting | ||
Ponatinib for the Management of Minimal Residual Disease (MRD) and Hematologic Relapse in Adult Ph+ Acute Lymphoblastic Leukemia (Ph+ ALL) Patients [NCT04475731] | Phase 2 | 67 participants (Anticipated) | Interventional | 2021-05-04 | Recruiting | ||
A Pivotal Phase 1/2, Single-Arm, Open-label Study to Evaluate the Safety and Efficacy of Ponatinib With Chemotherapy in Pediatric Patients With Philadelphia Chromosome-Positive (Ph+) Acute Lymphoblastic Leukemia (ALL) Who Have Relapsed or Are Resistant or [NCT04501614] | Phase 1/Phase 2 | 68 participants (Anticipated) | Interventional | 2021-02-24 | Recruiting | ||
A Phase 1/2 Multi-center, Open-label Study of Ponatinib in Japanese Patients With Chronic Myeloid Leukemia (CML) Who Have Failed Dasatinib or Nilotinib or Ph+ Acute Lymphoblastic Leukemia (ALL) Who Have Failed Prior Tyrosine Kinase Inhibitors (TKIs) [NCT01667133] | Phase 1/Phase 2 | 35 participants (Actual) | Interventional | 2012-08-31 | Completed | ||
Ponatinib Plus Reduced-intensity Chemotherapy in the First-line Treatment of Adult Patients With Ph-positive Acute Lymphoblastic Leukemia [NCT04554459] | Phase 2 | 32 participants (Anticipated) | Interventional | 2021-02-16 | Active, not recruiting | ||
A Phase II Study of the Combination of Decitabine, Venetoclax, and Ponatinib in Patients With Philadelphia Chromosome-Positive Acute Myeloid Leukemia or Myeloid Blast Phase Chronic Myelogenous Leukemia [NCT04188405] | Phase 2 | 30 participants (Anticipated) | Interventional | 2020-05-17 | Recruiting | ||
A Randomized, Open-label, Phase 2 Trial of Ponatinib in Patients With Resistant Chronic Phase Chronic Myeloid Leukemia to Characterize the Efficacy and Safety of a Range of Doses [NCT02467270] | Phase 2 | 283 participants (Actual) | Interventional | 2015-06-30 | Active, not recruiting | ||
Phase II Study of Ponatinib for Advanced Cancers With Genomic Alterations in Fibroblastic Growth Factor Receptor (FGFR) and Other Genomic Targets (KIT, PDGFRá, RET FLT3, ABL1) [NCT02272998] | Phase 2 | 22 participants (Actual) | Interventional | 2015-02-24 | Active, not recruiting | ||
"Phase 2 Study of Ponatinib (Iclusig) for Prevention of Relapse After Allogeneic Stem Cell Transplantation (Allo-SCT) in FLT3-ITD AML Patients: the PONALLO Trial." [NCT03690115] | Phase 2 | 24 participants (Actual) | Interventional | 2019-12-02 | Active, not recruiting | ||
A Phase I/II Study of the Combination of Venetoclax, Ponatinib and Corticosteroids in Patients With Relapsed or Refractory Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia and Lymphoid Blast Phase Chronic Myelogenous Leukemia [NCT03576547] | Phase 1/Phase 2 | 11 participants (Actual) | Interventional | 2018-06-26 | Active, not recruiting | ||
Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) Trial: PRIME [NCT03878524] | Phase 1 | 2 participants (Actual) | Interventional | 2020-04-01 | Active, not recruiting | ||
Ponatinib as Second Line Therapy for Patients With Chronic Myeloid Leukemia in Chronic Phase Resistant or Intolerant to Imatinib, Dasatinib or Nilotinib [NCT01746836] | Phase 2 | 50 participants (Anticipated) | Interventional | 2013-01-17 | Recruiting | ||
Ponatinib as Initial Therapy for Patients With Chronic Myeloid Leukemia in Accelerated Phase [NCT01570868] | Phase 2 | 51 participants (Actual) | Interventional | 2012-04-30 | Terminated(stopped due to Closed due to slow accrual) | ||
Phase II Study of Combination of Hyper-CVAD and Ponatinib in Patients With Philadelphia (PH) Chromosome Positive and/or BCR-ABL Positive Acute Lymphoblastic Leukemia (ALL) [NCT01424982] | Phase 2 | 88 participants (Actual) | Interventional | 2011-10-05 | Active, not recruiting | ||
Combination of Ponatinib Plus Chemotherapy As Frontline Treatment For Patients With BCR/ABL1-Like Acute Lymphoblastic Leukemia (BCR/ABL1-Like ALL) [NCT05306301] | Phase 2 | 32 participants (Anticipated) | Interventional | 2022-10-05 | Recruiting | ||
A Phase 1 Dose Escalation Trial to Determine the Safety, Tolerability and Maximum Tolerated Dose of Oral AP24534 in Patients With Refractory or Advanced Chronic Myelogenous Leukemia and Other Hematologic Malignancies [NCT00660920] | Phase 1 | 81 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
Phase II Study of the Sequential Combination of Low-Intensity Chemotherapy and Ponatinib Followed by Blinatumomab and Ponatinib in Patients With Philadelphia Chromosome (Ph)-Positive and/or BCR-ABL Positive Acute Lymphoblastic Leukemia (ALL) [NCT03147612] | Phase 2 | 21 participants (Actual) | Interventional | 2018-02-08 | Active, not recruiting | ||
The Rome Trial From Histology to Target: the Road to Personalize Target Therapy and Immunotherapy [NCT04591431] | Phase 2 | 400 participants (Actual) | Interventional | 2020-10-07 | Active, not recruiting | ||
Phase I/II, Dose-Escalation Study of Ponatinib, a FLT3 Inhibitor, With and Without Combination of 5-Azacytidine, in Patients With FLT3-Mutated Acute Myeloid Leukemia (AML) [NCT02829840] | Phase 1/Phase 2 | 0 participants (Actual) | Interventional | 2016-09-30 | Withdrawn | ||
A Phase II Study of the Combination of Ponatinib With Mini-hyper CVD Chemotherapy and Venetoclax in Patients With Relapsed or Refractory T-cell Acute Lymphoblastic Leukemia [NCT05268003] | Phase 2 | 20 participants (Anticipated) | Interventional | 2022-06-07 | Recruiting | ||
Phase II Study of the Combination of Blinatumomab and Ponatinib in Patients With Philadelphia Chromosome (Ph)-Positive and/or BCR-ABL Positive Acute Lymphoblastic Leukemia (ALL) [NCT03263572] | Phase 2 | 90 participants (Anticipated) | Interventional | 2017-11-29 | Recruiting | ||
A Phase Ib Feasibility Study of Personalized Kinase Inhibitor Therapy Combined With Induction in Acute Leukemias Who Exhibit In Vitro Kinase Inhibitor Sensitivity [NCT02779283] | Phase 1 | 7 participants (Actual) | Interventional | 2016-01-13 | Completed | ||
A Multicentre, Open-label Phase II Trial Evaluating the Safety and Efficacy of Ponatinib Induction Followed by Imatinib Maintenance in Adult Patients With Chronic Myelogenous Leukemia in Chronic Phase (CML-CP) ≤ 65 Years [NCT04070443] | Phase 2 | 170 participants (Anticipated) | Interventional | 2019-11-13 | Active, not recruiting | ||
Optimizing Ponatinib USe (OPUS). A GIMEMA Phase 2 Study of the Activity and Risk Profile of Ponatinib, 30 mg Once Daily, in Chronic Myeloid Leukemia (CML) Chronic Phase (CP) Patients Resistant to Imatinib [NCT02398825] | Phase 2 | 16 participants (Actual) | Interventional | 2016-06-23 | Active, not recruiting | ||
An Open-Label, Single-Arm, Phase 1/2 Study Evaluating the Safety and Efficacy of Ponatinib for the Treatment of Recurrent or Refractory Leukemias, Lymphomas or Solid Tumors in Pediatric Participants [NCT03934372] | Phase 1/Phase 2 | 60 participants (Anticipated) | Interventional | 2020-01-29 | Recruiting | ||
Multicenter, Open-Label, Single Arm, Phase II Exploratory Study to Evaluate the Effect of a One-Year Consolidation Treatment With Ponatinib 15 mg on Treatment Free-Remission Rate in Patients With Philadelphia-Positive Chronic Myeloid Leukemia, Who Had Pre [NCT04043676] | Phase 2 | 40 participants (Anticipated) | Interventional | 2019-04-30 | Recruiting | ||
Ponatinib Survey: Retrospective Evaluation of CML Patients in the National Compassionate Program According to the 648/96 Decree [NCT02448095] | 38 participants (Actual) | Observational | 2015-12-22 | Terminated(stopped due to lack of interest) | |||
An Open Label, 3-arm, Randomised Phase II Study to Compare the Safety and Efficacy of Ponatinib in Combination With Either Chemotherapy or Blinatumomab With Imatinib Plus Chemotherapy as Front-line Therapy for Patients Aged 55 Years and Over With Philadel [NCT04688983] | Phase 2 | 180 participants (Anticipated) | Interventional | 2021-01-31 | Not yet recruiting | ||
Cardiovascular Assessment of Ponatinib as Third Line Treatment Option in Chronic Phase Chronic Myeloid Leukemia After Failure of Imatinib and Bosutinib (CarPAs) [NCT04709731] | Phase 2 | 50 participants (Anticipated) | Interventional | 2021-02-01 | Not yet recruiting | ||
A Pilot Evaluation of Ponatinib (AP24534), a Potent Oral Pan-FGFR Inhibitor, in the Treatment of FGFR Mutation Positive Recurrent or Persistent Endometrial Carcinoma: a Multi-Institutional Study [NCT01888562] | 0 participants (Actual) | Interventional | 2016-01-31 | Withdrawn(stopped due to Could not obtain an IDE on the FGFR2 assay) | |||
A Phase 1 Trial of Trametinib and Ponatinib in Patients With KRAS Mutant Advanced Non-Small Cell Lung Cancer [NCT03704688] | Phase 1/Phase 2 | 12 participants (Actual) | Interventional | 2018-10-09 | Completed | ||
A Pivotal Phase 2 Trial of Ponatinib (AP24534) in Patients With Refractory Chronic Myeloid Leukemia and Ph+ Acute Lymphoblastic Leukemia [NCT01207440] | Phase 2 | 449 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
"Post-Marketing Surveillance of Safety and Effectiveness of Iclusig® Tablets in Korean Patients With CML or Ph+ ALL Under the Risk Management Plan" [NCT03709017] | 50 participants (Anticipated) | Observational | 2018-08-07 | Active, not recruiting | |||
Retrospective, Non-interventional Study to Evaluate Chronic Myeloid Leukemia Treatment Landscape and Real-life Treatment Outcomes in Hungary: Analysis of National Health Insurance Fund Database [NCT05286528] | 1,484 participants (Actual) | Observational | 2020-11-18 | Completed | |||
Multicenter, Open-Label, Single Arm, Phase II Exploratory Study to Evaluate the Reinduction and Second Stop of TKI With Ponatinib in CML in Molecular Response (ResToP) [NCT04160546] | Phase 2 | 80 participants (Anticipated) | Interventional | 2020-01-17 | Active, not recruiting | ||
Overall Survival With Ponatinib Versus Allogeneic Stem Cell Transplant in Philadelphia-positive Leukemias With the T315I Mutation [NCT02981784] | 184 participants (Actual) | Observational | 2000-01-31 | Completed | |||
A Phase II, Open-Label Study of Ponatinib, A Multi-Targeted Oral Tyrosine Kinase Inhibitor, in Advanced Non-Small Cell Lung Cancer Harboring RET Translocations [NCT01813734] | Phase 2 | 9 participants (Actual) | Interventional | 2013-09-30 | Completed | ||
A Phase III Randomized Trial of Steroids + Tyrosine Kinase Inhibitor (TKI) Induction With Chemotherapy or Blinatumomab for Newly Diagnosed BCR-ABL-Positive Acute Lymphoblastic Leukemia (ALL) in Adults [NCT04530565] | Phase 3 | 348 participants (Anticipated) | Interventional | 2021-01-25 | Recruiting | ||
Treatment Plan for the Compassionate Use of Ponatinib (AP24534) in Patients With Imatinib-, Dasatinib-, and Nilotinib- Resistant/Intolerant Philadelphia Chromosome Positive Leukemias. [NCT01549548] | 0 participants | Expanded Access | No longer available | ||||
Phase 2 Trial of Ponatinib in Patients With Metastatic and/or Unresectable Gastrointestinal Stromal Tumor (GIST) Following Failure or Intolerance of Prior Therapy With Imatinib [NCT03171389] | Phase 2 | 81 participants (Anticipated) | Interventional | 2017-03-22 | Recruiting | ||
A Phase 3 Randomized,Open-Label Study of Ponatinib Versus Imatinib in Adult Patients With Newly Diagnosed Chronic Myeloid Leukemia in Chronic Phase [NCT01650805] | Phase 3 | 307 participants (Actual) | Interventional | 2012-06-30 | Terminated(stopped due to Study terminated based on evaluation of safety data.) | ||
A Phase II Proof-of-Concept Trial to Study Kinase Inhibition in Relapsed/Refractory Acute Leukemias: Using a Comprehensive In Vitro Kinase Inhibitor Panel to Select Individualized, Targeted Therapies [NCT01620216] | Phase 2 | 12 participants (Actual) | Interventional | 2012-05-11 | Terminated(stopped due to Unable to recruit enough eligible subjects) | ||
A Phase II Study Using a BFM Regimen Plus Tyrosine Kinase Inhibitor in Adult Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia [NCT04845035] | Phase 2 | 23 participants (Anticipated) | Interventional | 2024-01-31 | Recruiting | ||
Treatment Protocol for Newky Diagnosed Adult Ph-Chromosome Positive (BCR::ABL1) Acute Lymphoblastic Leukemia (LALPh2022) [NCT06175702] | 150 participants (Anticipated) | Observational | 2023-12-25 | Not yet recruiting | |||
Pilot Study of Ponatinib in Biliary Cancer Patients With FGFR2 Fusions [NCT02265341] | Phase 2 | 12 participants (Actual) | Interventional | 2014-12-31 | Completed | ||
A Phase II Study of a Chemotherapy-Free Induction Regimen for Ph+ Acute Lymphoblastic Leukemia (ALL) Incorporating Inotuzumab Ozogamicin (InO) [NCT04747912] | Phase 2 | 25 participants (Anticipated) | Interventional | 2021-03-02 | Recruiting | ||
Phase 2 Clinical Trial With Ponatinib as a Second Line Therapy for Patients With Chronic Myeloid Leukemia in Chronic Phase Resistant or Intolerant to Prior First Line Tyrosine Kinase Inhibitor Treatment [NCT03807479] | Phase 2 | 18 participants (Actual) | Interventional | 2018-12-11 | Terminated(stopped due to less recruting) | ||
Phase II Study of Ponatinib in Advanced Lung and Head and Neck Cancers With FGFR Kinase Alterations [NCT01761747] | Phase 2/Phase 3 | 3 participants (Actual) | Interventional | 2013-01-31 | Terminated(stopped due to FDA hold and toxicity associated with study drug) | ||
A Randomized, Open-label Study of Ponatinib Versus Nilotinib in Patients With Chronic Myeloid Leukemia in Chronic Phase Following Resistance to Imatinib [NCT02627677] | Phase 3 | 44 participants (Actual) | Interventional | 2015-12-31 | Terminated(stopped due to The study was stopped due to operational feasibility and not due to any safety concerns) | ||
Expanded Access Program of Ponatinib (AP24534) for Patients With Refractory Chronic Myeloid Leukemia or Ph+ Acute Lymphoblastic Leukemia [NCT01592136] | 0 participants | Expanded Access | Approved for marketing | ||||
A Phase II Study of Ponatinib in Cohorts of Patients With Lung Cancer Preselected Using Different Candidate Predictive Biomarkers [NCT01935336] | Phase 2 | 171 participants (Actual) | Interventional | 2013-09-24 | Completed | ||
A Study of Ponatinib in Advanced or Metastatic Medullary Thyroid Cancer (MTC) [NCT03838692] | Phase 2 | 0 participants (Actual) | Interventional | 2019-07-26 | Withdrawn(stopped due to Closed by sponsor) | ||
Observation of the Effect of Chemotherapy Combined With Tyrosinase Inhibitor on the Reactivation of CMV and EBV in Patients With Acute Lymphoblastic Leukemia [NCT03331211] | 100 participants (Anticipated) | Observational [Patient Registry] | 2017-11-01 | Recruiting | |||
A Phase I - II Study to Assess Safety and Efficacy of the Combination of Ponatinib With High or Intermediate-Dose Cytarabine as Consolidation Therapy for Patients With Intermediate-Risk Cytogenetic FLT3-ITD AML iIn First Complete Remission [NCT02428543] | Phase 1/Phase 2 | 49 participants (Actual) | Interventional | 2013-07-31 | Active, not recruiting | ||
Front-line Treatment of Philadelphia Positive/BCR-ABL Positive Acute Lymphoblastic Leukemia With Ponatinib, a New Potent Tyrosine Kinase Inhibitor. [NCT01641107] | Phase 2 | 44 participants (Actual) | Interventional | 2014-12-04 | Completed | ||
Concurrent Ponatinib With Chemotherapy for Young Adults With Newly Diagnosed Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia [NCT02776605] | Phase 2 | 30 participants (Actual) | Interventional | 2016-06-30 | Active, not recruiting | ||
A Phase II Study of Ponatinib in Advanced or Metastatic Medullary Thyroid Cancer [NCT01838642] | Phase 2 | 3 participants (Actual) | Interventional | 2013-03-31 | Terminated(stopped due to Recruiting halted prematurely and will not resume. New study to open soon.) | ||
Phase 2 Trial of Ponatinib in Patients With Metastatic and/or Unresectable Gastrointestinal Stromal Tumor Following Failure of Prior Tyrosine Kinase Inhibitor Therapy [NCT01874665] | Phase 2 | 45 participants (Actual) | Interventional | 2013-06-05 | Completed | ||
A Multicentre, Randomized Trial in Adults With de Novo Philadelphia-Chromosome Positive Acute Lymphoblastic Leukemia to Assess the Efficacy of Ponatinib Versus Imatinib in Combination With Low-intensity Chemotherapy, to Compare End of Therapy With Indicat [NCT06061094] | Phase 2 | 220 participants (Anticipated) | Interventional | 2023-07-14 | Recruiting | ||
A Phase II Multi-center, Randomized, Open-label Study of Ponatinib in Chinese Patients With Chronic Myeloid Leukemia Who Have Failed Prior TKIs or With T315I Mutation, or Ph+ALL Who Have Failed Prior TKIs or With T315I Mutation [NCT04233346] | Phase 2 | 90 participants (Anticipated) | Interventional | 2020-07-09 | Active, not recruiting | ||
A Phase 3, Randomized, Open-label, Multicenter Study Comparing Ponatinib Versus Imatinib, Administered in Combination With Reduced-Intensity Chemotherapy, in Patients With Newly Diagnosed Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia (Ph+ [NCT03589326] | Phase 3 | 245 participants (Actual) | Interventional | 2018-10-04 | Active, not recruiting | ||
Phase II Trial of Ponatinib in Patients With Bevacizumab-Refractory Glioblastoma [NCT02478164] | Phase 2 | 17 participants (Actual) | Interventional | 2015-07-13 | Completed | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |