| ID Source | ID |
|---|---|
| PubMed CID | 6450551 |
| CHEMBL ID | 1289926 |
| CHEBI ID | 66910 |
| CHEBI ID | 94568 |
| SCHEMBL ID | 172918 |
| SCHEMBL ID | 22930506 |
| MeSH ID | M0489638 |
| Synonym |
|---|
| AC-1539 |
| ag 013736 |
| ag013736 |
| HY-10065 |
| AB01274739-01 |
| inlyta (tn) |
| 319460-85-0 |
| D03218 |
| axitinib (jan/usan) |
| n-methyl-2-({3-[(e)-2-(pyridin-2-yl)ethenyl]-1h-indazol-6-yl}sulfanyl)benzamide |
| bdbm25117 |
| AG-13736 , |
| inlyta |
| axitinib , |
| ag-013736 |
| n-methyl-2-[[3-[(e)-2-pyridin-2-ylethenyl]-1h-indazol-6-yl]sulfanyl]benzamide |
| NCGC00241108-01 |
| chebi:66910 , |
| nsc-757441 |
| CHEMBL1289926 |
| cas-319460-85-0 |
| dtxcid8028975 |
| dtxsid3049049 , |
| tox21_113597 |
| S1005 , |
| BCP9000345 |
| nsc757441 |
| (e)-n-methyl-2-((3-(2-(pyridin-2-yl)vinyl)-1h-indazol-6-yl)thio)benzamide |
| c9lvq0yuxg , |
| benzamide, n-methyl-2-((3-((e)-2-(2-pyridinyl)ethenyl)-1h-indazol-6-yl)thio)- |
| axitinib [usan:inn:jan] |
| unii-c9lvq0yuxg |
| benzamide, n-methyl-2-((3-((1e)-2-(2-pyridinyl)ethenyl)-1h-indazo)-6-yl)thio)- |
| n-methyl-2-((3-((1e)-2-(pyridin-2-yl)ethenyl)-1h-indazol-6-yl)sulfanyl)benzamide |
| nsc 757441 |
| benzamide, n-methyl-2-[[3-[(1e)-2-(2-pyridinyl)ethenyl]-1h-indazol-6-yl]thio]- |
| AM20090673 |
| BCPP000372 |
| axitinib,ag-013736 |
| (e)-n-methyl-2-(3-(2-(pyridin-2-yl)vinyl)-1h-indazol-6-ylthio)benzamide |
| axitinib [jan] |
| axitinib [mi] |
| axitinib [inn] |
| axitinib [usan] |
| axitinib [mart.] |
| n-methyl-2((3-((1e0-2-(pyridin-2-yl)ethenyl)-1h-inazol-6-ylsufanyl)benzamide |
| axitinib [orange book] |
| benzamide, n-methyl-2-((3-((1e)-2-(2-pyridinyl)ethenyl)-1h-indazol-6-yl)thio)- |
| axitinib [vandf] |
| n-methyl-2-(3-((e)-2-pyridin-2-yl-vinyl)-1h-indazol-6-ylsulfanyl)-benzamide |
| axitinib [who-dd] |
| axitinibum |
| n-methyl-2-({3-[(e)-2-(pyridin-2-yl)vinyl]-1h-indazol-6-yl}sulfanyl)benzamide |
| CS-0116 |
| AKOS015902898 |
| gtpl5659 |
| BRD-K29905972-001-01-4 |
| smr002530046 |
| MLS006010164 |
| SCHEMBL172918 |
| NCGC00241108-04 |
| 4AG8 |
| 4AGC |
| tox21_113597_1 |
| n-methyl-2-[[3-[(e)-2-(2-pyridyl)vinyl]-1h-indazol-6-yl]sulfanyl]benzamide |
| J-502064 |
| Q-200662 |
| n-methyl-[[3[(1e)-2-(2-pyridinyl)ethenyl]-1h-indazol-6-yl]thio]-benzamide |
| axitinib (ag 013736) |
| AB01274739_02 |
| mfcd09837898 |
| EX-A337 |
| ag-013736;axitinib |
| SR-01000941566-1 |
| sr-01000941566 |
| CHEBI:94568 |
| KS-1448 |
| axitinib, >=98% (hplc) |
| NCGC00241108-06 |
| SW219464-1 |
| DB06626 |
| n-methyl-2-({3-[(e)-2-pyridin-2-ylethenyl]-2h-indazol-6-yl}sulfanyl)benzamide |
| Q4830631 |
| n-methyl-2-[[3-[2-(2-pyridinyl)ethenyl]-1h-indazol-6-yl]thio]benzamide |
| Z2216885372 |
| BCP01371 |
| BRD-K29905972-001-02-2 |
| CCG-264772 |
| nsc799341 |
| nsc-799341 |
| ag13736 |
| SCHEMBL22930506 |
| n-methyl-2-[[3-[(e)-2-(2-pyridyl)vinyl]-2h-indazol-6-yl]sulfanyl]benzamide |
| 1528729-60-3 |
| EN300-26869010 |
| n-methyl-2-({3-[(1e)-2-(pyridin-2-yl)ethenyl]-1h-indazol-6-yl}sulfanyl)benzamide |
| axitinib (mart.) |
| n-methyl-2-((3-((e)-2-(pyridin-2-yl)vinyl)-1h-indazol-6-yl)sulfanyl)benzamide |
| l01xe17 |
| n-methyl-2-((3-((e)-2-(pyridin-2-yl)ethenyl)-1h-indazol-6-yl)sulfanyl)benzamide |
| n-methyl-2-((3-((1e)-2-(pyridin-2-yl)ethen-1-yl)-1h-indazol-6-yl)sulfanyl)benzamide |
| n-methyl-2-((3-(2-(pyridin-2-yl)vinyl)-1h-indazol-6-yl)thio)benzamide |
Axitinib (AXI) is a tyrosine kinase inhibitor, currently under investigation in an international phase II/III trial including thymic neuroendocrine tumors. It is a potent inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3.
Axitinib has shown activity in metastatic renal cell carcinoma (mRCC) in a large phase III clinical trial and was approved in patients who failed first-line therapy. It represents an additional treatment option for patients with advanced thyroid cancer.
Axitinib alone could inhibit cell proliferation and retard tumor growth through inducing cell cycle arrest at G2/M phase, cell senescence, cell apoptosis, and antiangiogenesis. The drug can cause retinal vein occlusions, and clinicians, both oncologists, and ophthalmologists should be aware of this rare but potentially blinding side effect.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Axitinib can cause retinal vein occlusions, and clinicians, both oncologists, and ophthalmologists need to be aware of this rare but potentially blinding side effect." | ( Bilateral Central Retinal Vein Occlusion Associated with Axitinib Therapy: A Case Report. Dutta Majumder, P; Ganvir, A; Goyal, S; Pyare, R; Rao, C, 2023) | 2.6 |
| "Axitinib does not inhibit CYP3A4/5, CYP1A2, CYP2C8, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or UGT1A1 at concentrations" | ( Clinical pharmacology of axitinib. Chen, Y; Garrett, M; Hee, B; Klamerus, KJ; Pithavala, YK; Tortorici, MA, 2013) | 1.41 |
| "Axitinib alone could inhibit cell proliferation and retard tumor growth through inducing cell cycle arrest at G2/M phase, cell senescence, cell apoptosis, and antiangiogenesis in vitro and in vivo. " | ( Axitinib alone or in combination with chemotherapeutic drugs exerts potent antitumor activity against human gastric cancer cells in vitro and in vivo. Gao, J; Ge, S; He, Q; Li, Y; Peng, Z; Shen, L; Wang, T, 2014) | 3.29 |
| "Axitinib did not inhibit hepatic activation of cyclophosphamide or export of its activated metabolite, 4-hydroxy-cyclophosphamide (4-OH-CPA), to extrahepatic tissues; rather, axitinib selectively decreased 9L tumor uptake of 4-OH-CPA by 30% to 40%." | ( Modulation of the antitumor activity of metronomic cyclophosphamide by the angiogenesis inhibitor axitinib. Ma, J; Waxman, DJ, 2008) | 1.28 |
Axitinib treatment after nivolumab treatment failure can be beneficial for some patients with metastatic RCC. Pre-treatment with axitinib increased acute endothelial cell apoptosis following SDRT.
Axitinib therapy after the immune checkpoint inhibitor nivolumab showed good efficacy with a moderate risk of adverse events. The common all-causality adverse events (all grades) in Japanese patients were dysphonia (68%), hypertension (64%), hand-foot syndrome (64%) and diarrhea (56%) for axitinib.
Axitinib was rapidly absorbed, with a median plasma Tmax of 2. The data demonstrated that axitinib can be characterized as not sensitive to ethnic factors.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Rifampin expectedly decreased AUCinf and Cmax of axitinib (geometric mean reduced by 79 and 71%, respectively)." | ( Effect of rifampin on the pharmacokinetics of Axitinib (AG-013736) in Japanese and Caucasian healthy volunteers. Garrett, M; Hee, B; Klamerus, KJ; Kuruganti, U; Ni, G; Pithavala, YK; Toh, M; Tortorici, M, 2010) | 0.87 |
| " This study evaluated changes in axitinib plasma pharmacokinetic parameters and assessed safety and tolerability in healthy subjects, following axitinib co-administration with the potent CYP3A inhibitor ketoconazole." | ( Effect of ketoconazole on the pharmacokinetics of axitinib in healthy volunteers. Garrett, M; Hee, B; Klamerus, KJ; Mount, J; Pithavala, YK; Rahavendran, SV; Sarapa, N; Selaru, P; Tong, W, 2012) | 0.91 |
| " Axitinib was administered as 5-, 7-, and 10-mg doses under fed conditions in study periods 1, 2, and 3, respectively, followed by pharmacokinetic assessments and safety monitoring." | ( A Phase I study to evaluate the pharmacokinetics of axitinib (AG-13736) in healthy Chinese volunteers. Chen, Y; Hu, P; Jiang, J; Lu, L; Ni, G; Pithavala, YK; Tortorici, MA; Zhang, J, 2011) | 1.53 |
| " The potential contribution of polymorphisms in genes encoding these enzymes and transporters to axitinib pharmacokinetic variability was assessed." | ( Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Brennan, M; Chen, Y; Liu, YC; Pithavala, Y; Tortorici, M; Williams, JA, 2012) | 0.81 |
| " None of the polymorphisms analysed was a statistically significant predictor of axitinib pharmacokinetic variability." | ( Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Brennan, M; Chen, Y; Liu, YC; Pithavala, Y; Tortorici, M; Williams, JA, 2012) | 0.82 |
| " The pharmacokinetic (PK) properties of axitinib may provide a selective treatment effect while minimizing adverse reactions and enhancing safety." | ( Pharmacokinetic evaluation of axitinib. B Cohen, R; Olszanski, AJ; Patson, B, 2012) | 0.93 |
| "This article provides a comprehensive and critical review of the PK properties of axitinib as they relate to safety and tolerability, as well as potential pharmacodynamic and efficacy parameters." | ( Pharmacokinetic evaluation of axitinib. B Cohen, R; Olszanski, AJ; Patson, B, 2012) | 0.89 |
| "For Form IV FCIR, compared with overnight fasting, axitinib plasma exposure [area under the concentration curve (AUC)] was decreased 23 % when administered with food." | ( Evaluation of the effect of food on the pharmacokinetics of axitinib in healthy volunteers. Chen, Y; Garrett, M; Hee, B; Klamerus, KJ; LaBadie, RR; Mount, J; Ni, G; Pithavala, YK; Selaru, P; Toh, M; Tortorici, MA, 2012) | 0.87 |
| " Axitinib population pharmacokinetic and pharmacokinetic/pharmacodynamic relationships were evaluated." | ( Axitinib in metastatic renal cell carcinoma: results of a pharmacokinetic and pharmacodynamic analysis. Dutcher, JP; Garrett, M; Kim, S; Motzer, RJ; Pithavala, YK; Poland, B; Rini, BI; Rixe, O; Stadler, WM; Tarazi, J; Wilding, G, 2013) | 2.74 |
| "Plasma concentration-time data from 337 healthy volunteers in 10 phase I studies were analyzed, using non-linear mixed effects modelling (nonmem) to estimate population pharmacokinetic parameters and evaluate relationships between parameters and food, formulation, demographic factors, measures of renal and hepatic function and metabolic genotypes (UGT1A1*28 and CYP2C19)." | ( Population pharmacokinetic analysis of axitinib in healthy volunteers. Amantea, MA; Brennan, M; Garrett, M; Hee, B; Pithavala, YK; Poland, B, 2014) | 0.67 |
| " Secondary endpoints included progression-free survival (PFS), overall survival (OS), safety, pharmacokinetic parameters, and patient-reported outcomes assessed with the MD Anderson Symptom Inventory questionnaire." | ( Treatment of advanced thyroid cancer with axitinib: Phase 2 study with pharmacokinetic/pharmacodynamic and quality-of-life assessments. Agate, L; Boucher, A; Bycott, P; Chen, C; Cohen, EE; Ingrosso, A; Jarzab, B; Kane, MA; Kim, S; Licitra, L; Locati, LD; Ou, SH; Pithavala, YK; Qin, S; Wirth, LJ, 2014) | 0.67 |
| " Boxplots of maximum observed plasma concentration (C max) and area under the plasma concentration-time curve (AUC) of data from these tumor populations was compared to C max and AUC from the final population pharmacokinetic model developed for metastatic renal cell carcinoma (mRCC) to compare axitinib pharmacokinetics across different tumor types." | ( Pharmacokinetics of single-agent axitinib across multiple solid tumor types. Cohen, EE; Fruehauf, JP; Garrett, M; Kim, S; Pithavala, YK; Ruiz-Garcia, A; Tortorici, MA, 2014) | 0.86 |
| " The final analysis indicated that the pharmacokinetic model for mRCC was able to successfully describe axitinib pharmacokinetics in patients with NSCLC, thyroid cancer, and melanoma." | ( Pharmacokinetics of single-agent axitinib across multiple solid tumor types. Cohen, EE; Fruehauf, JP; Garrett, M; Kim, S; Pithavala, YK; Ruiz-Garcia, A; Tortorici, MA, 2014) | 0.9 |
| " Ambulatory BP monitoring (ABPM) and pharmacokinetic data were collected in a randomised, double-blind phase II study of axitinib with or without dose titration in previously untreated patients with metastatic renal cell carcinoma." | ( Population pharmacokinetic-pharmacodynamic modelling of 24-h diastolic ambulatory blood pressure changes mediated by axitinib in patients with metastatic renal cell carcinoma. Bair, AH; Chen, Y; Mugundu, GM; Pithavala, YK; Rini, BI, 2015) | 0.83 |
| "We employed a three-stage modelling approach, which included development of (1) a baseline 24-h ABPM model, (2) a pharmacokinetic model from serial and sparse pharmacokinetic data, and (3) an indirect-response, maximum-effect (Emax) model to evaluate the exposure-driven effect of axitinib on dBP." | ( Population pharmacokinetic-pharmacodynamic modelling of 24-h diastolic ambulatory blood pressure changes mediated by axitinib in patients with metastatic renal cell carcinoma. Bair, AH; Chen, Y; Mugundu, GM; Pithavala, YK; Rini, BI, 2015) | 0.8 |
| " Upon review, the data demonstrated that axitinib can be characterized as not sensitive to ethnic factors based on its pharmacokinetic and pharmacodynamic properties." | ( Axitinib plasma pharmacokinetics and ethnic differences. Chen, Y; Garrett, M; LaBadie, RR; Pithavala, YK; Suzuki, A; Tortorici, MA; Umeyama, Y, 2015) | 2.13 |
| " Plasma VEGF and axitinib pharmacokinetic levels were also assessed at specified time points." | ( Pharmacodynamic study of axitinib in patients with advanced malignancies assessed with (18)F-3'deoxy-3'fluoro-L-thymidine positron emission tomography/computed tomography. Bruce, JY; Carmichael, LL; Eickhoff, JC; Heideman, JL; Jeraj, R; Kolesar, JM; Liu, G; Perlman, SB; Scully, PC, 2015) | 1.06 |
| "Effect of renal function (baseline creatinine clearance [CrCL]) on axitinib clearance was evaluated in a population pharmacokinetic model in 207 patients with advanced solid tumors who received a standard axitinib starting dose, and in 383 healthy volunteers." | ( Effect of Renal Impairment on the Pharmacokinetics and Safety of Axitinib. Chen, Y; Dutcher, JP; Garrett, M; Motzer, RJ; Pithavala, YK; Rini, BI; Rixe, O; Stadler, WM; Tarazi, J; Wilding, G, 2016) | 0.91 |
| " The population pharmacokinetic model adequately predicted axitinib clearance in individuals with severe renal impairment or end-stage renal disease." | ( Effect of Renal Impairment on the Pharmacokinetics and Safety of Axitinib. Chen, Y; Dutcher, JP; Garrett, M; Motzer, RJ; Pithavala, YK; Rini, BI; Rixe, O; Stadler, WM; Tarazi, J; Wilding, G, 2016) | 0.92 |
Axitinib is well tolerated in combination with FOLFOX, FOLFIRI, or FOL FOX plus 2 mg/kg bevacizumab. The primary endpoint was MTD of axitinib in combinationWith RT. AxitinIB combined with 5-fluorouracil (5-FU) had synergistic inhibitory effect.
We did a multicentre, phase 2 trial of axitinib given on an individualised dosing algorithm. Results confirmed that drug release from the axit inib nanowafer is more effective in inhibiting CNV compared to the topical eye drop treatment.
| 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. |
| vascular endothelial growth factor receptor antagonist | An antagonist at the vascular endothelial growth factor receptor. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| indazoles | |
| pyridines | Any organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives. |
| aryl sulfide | Any organic sulfide in which the sulfur is attached to at least one aromatic group. |
| benzamides | |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 0.6906 | 0.0072 | 15.7588 | 89.3584 | AID1224835; AID624030 |
| acetylcholinesterase | Homo sapiens (human) | Potency | 27.5404 | 0.0025 | 41.7960 | 15,848.9004 | AID1347398 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 0.3218 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 26.8325 | 0.1737 | 34.3047 | 61.8120 | AID1346924 |
| PPM1D protein | Homo sapiens (human) | Potency | 16.5388 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 26.8325 | 0.1737 | 34.3047 | 61.8120 | AID1346924 |
| TDP1 protein | Homo sapiens (human) | Potency | 3.4390 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 11.8832 | 0.0007 | 14.5928 | 83.7951 | AID1259369 |
| AR protein | Homo sapiens (human) | Potency | 5.3593 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID743042; AID743053; AID743054 |
| caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 1.8834 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 33.4915 | 0.0006 | 57.9133 | 22,387.1992 | AID1259377; AID1259378 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 0.4422 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224839; AID1224893 |
| progesterone receptor | Homo sapiens (human) | Potency | 16.7855 | 0.0004 | 17.9460 | 75.1148 | AID1346795 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 0.3090 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 0.1107 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 4.1822 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 1.2085 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 4.4732 | 0.3758 | 27.4851 | 61.6524 | AID743217; AID743220 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 0.3758 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 4.0095 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID1259383; AID743069; AID743075; AID743077; AID743078; AID743079; AID743080; AID743091 |
| G | Vesicular stomatitis virus | Potency | 3.4671 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 34.6713 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 12.6815 | 0.0010 | 24.5048 | 61.6448 | AID743212; AID743215; AID743227 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 13.3322 | 0.0010 | 19.4141 | 70.9645 | AID743191 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 19.3574 | 0.0237 | 23.2282 | 63.5986 | AID743222; AID743223 |
| caspase-3 | Homo sapiens (human) | Potency | 1.8834 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 3.0198 | 0.0007 | 23.0674 | 1,258.9301 | AID743085; AID743122 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 0.5956 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 49.1940 | 0.0391 | 47.5451 | 146.8240 | AID1224845 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 0.9439 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| histone deacetylase 9 isoform 3 | Homo sapiens (human) | Potency | 1.3126 | 0.0376 | 17.0823 | 61.1927 | AID1259364; AID1259388 |
| tyrosine-protein kinase Yes | Homo sapiens (human) | Potency | 0.6884 | 0.0000 | 5.0182 | 79.2586 | AID686947 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 3.9074 | 0.0006 | 27.2152 | 1,122.0200 | AID743202; AID743219 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 0.0668 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
| Interferon beta | Homo sapiens (human) | Potency | 13.2709 | 0.0033 | 9.1582 | 39.8107 | AID1347411; AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 3.4671 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 0.8748 | 0.0023 | 19.5956 | 74.0614 | AID651631; AID720552 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 0.0668 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 19.9526 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 3.4671 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 0.3551 | 0.0119 | 17.9420 | 71.5630 | AID651632; AID720516 |
| Ataxin-2 | Homo sapiens (human) | Potency | 0.2371 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 3.4671 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID624995 | Binding constant for CSF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625125 | Binding constant for CLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624934 | Binding constant for FLT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625100 | Binding constant for NLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424986 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID625099 | Binding constant for TAOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1510860 | Inhibition of VEGFR2 (unknown origin) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma. |
| AID1584971 | Antiproliferative activity in human KU812 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| AID624968 | Binding constant for DRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625077 | Binding constant for DAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624831 | Binding constant for CHEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624774 | Binding constant for QSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624914 | Binding constant for WEE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424897 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624776 | Binding constant for PCTK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624779 | Binding constant for BTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1510861 | Inhibition of VEGFR1 (unknown origin) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma. |
| AID625025 | Binding constant for MAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624856 | Binding constant for GSK3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624970 | Binding constant for CDK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624726 | Binding constant for HIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1215234 | Drug level in brain of Abcb1a/1b;Abcg2 (-/-) FVB mouse at 10 mg/kg, po after 4 hrs by liquid chromatography-tandem mass spectrometry relative to wild type FVB mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID1612810 | Inhibition of ABL1 (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID625060 | Binding constant for CAMKK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424500 | Inhibition of VEGFR3 (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Recent developments in small molecule therapies for renal cell carcinoma. |
| 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. |
| 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. |
| 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. |
| AID624804 | Binding constant for ERBB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1215213 | Relative brain accumulation index, ratio of drug level in brain after 1 hr to AUC (0 to 1 hr) in Abcb1a/1b;Abcg2 (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID624949 | Binding constant for CSNK1G3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624816 | Binding constant for HPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1565280 | Antiangiogenic activity in transgenic fli1a:EGFP-tagged zebrafish embryo assessed as reduction in intersegmental vessel sprouting at 0.1 to 1 uM administered from 24 hrs post fertilization and measured after 72 hrs by fluorescence microscopy relative to c | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model. |
| 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. |
| AID624805 | Binding constant for RSK3(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1215240 | Drug transport in MDCK2 cells expressing human ABCG2 assessed as transporter-mediated efflux ratio at 1 uM after 1 to 4 hrs | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID625013 | Binding constant for LCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624748 | Binding constant for EPHA6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1584947 | Inhibition of BCR/ABL H369P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID624894 | Binding constant for MEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425030 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624811 | Binding constant for PAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425094 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624711 | Binding constant for STK35 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624994 | Binding constant for AKT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1585050 | Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID625017 | Binding constant for TIE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425086 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID625141 | Binding constant for RIOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625057 | Binding constant for TYRO3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215227 | Drug level in brain of Abcb1a/1b (-/-) FVB mouse at 10 mg/kg, po after 1 hr by liquid chromatography-tandem mass spectrometry relative to wild type FVB mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID625097 | Binding constant for TNNI3K kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215248 | Drug transport in MDCK2 cells expressing human ABCC2 assessed as transporter-mediated drug transport at 1 uM after 1 to 4 hrs | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID624903 | Binding constant for SRPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624786 | Binding constant for KIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624760 | Binding constant for PFPK5(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1612817 | Inhibition of SRC (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID625105 | Binding constant for EPHB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625004 | Binding constant for EGFR(L858R,T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1575473 | Cell cycle arrest in human CCRF-CEM cells at 100 nM after 24 hrs by propidium iodide staining based FACS analysis | 2019 | Journal of natural products, 01-25, Volume: 82, Issue:1 | Bifunctional Duocarmycin Analogues as Inhibitors of Protein Tyrosine Kinases. |
| 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. |
| AID624724 | Binding constant for TAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624825 | Binding constant for BMPR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425056 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID624902 | Binding constant for MEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625098 | Binding constant for IRAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624751 | Binding constant for PIP5K1C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624900 | Binding constant for RSK1(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625085 | Binding constant for ULK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215252 | AUC (0 to 1 hr) in Abcb1a/1b;Abcg2 (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID624702 | Binding constant for BRSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424902 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624916 | Binding constant for ULK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624727 | Binding constant for FYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625038 | Binding constant for PIK3CA(E542K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424926 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624729 | Binding constant for FAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1584951 | Inhibition of BCR/ABL M351T mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| AID624723 | Binding constant for CSNK1A1L kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425054 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID624801 | Binding constant for MAP3K15 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624993 | Binding constant for ABL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624962 | Binding constant for ASK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624832 | Binding constant for IKK-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624922 | Binding constant for CAMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624971 | Binding constant for DAPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624822 | Binding constant for CDKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424942 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1215237 | Drug transport in MDCK2 cells expressing human ABCB1 assessed as transporter-mediated efflux ratio at 1 uM after 1 to 4 hrs in presence of 5 uM ABCB1/ABCG2 inhibitor elacridar | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID1584945 | Inhibition of BCR/ABL F317L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| AID624744 | Binding constant for ZAP70 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215253 | Drug level in brain of Abcg2 (-/-) FVB mouse at 10 mg/kg, po after 1 hr by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID1215233 | Drug level in brain of Abcb1a/1b (-/-) FVB mouse at 10 mg/kg, po after 4 hrs by liquid chromatography-tandem mass spectrometry relative to wild type FVB mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID624835 | Binding constant for ERN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425050 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1612826 | Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID624988 | Binding constant for ABL1(T315I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1585047 | Inhibition of inactive wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 hrs by ADP-G | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| AID625041 | Binding constant for PIK3CA(H1047L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424999 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID624743 | Binding constant for LTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624851 | Binding constant for ERBB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625138 | Binding constant for STK33 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1215219 | Drug level in brain of Abcg2 (-/-) FVB mouse at 10 mg/kg, po after 4 hrs by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID762237 | Antiproliferative activity against human HCC1954 cells assessed as growth inhibition after 5 days by SRB assay | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. |
| AID624732 | Binding constant for PYK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624815 | Binding constant for ERBB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624789 | Binding constant for KIT(D816V) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624710 | Binding constant for SRMS kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624788 | Binding constant for KIT(D816H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425204 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1689138 | Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones. |
| AID1508897 | Inhibition of TEL fused c-KIT V559A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| AID624877 | Binding constant for PIK3C2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624728 | Binding constant for NIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625133 | Binding constant for CDC2L2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425087 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID625084 | Binding constant for HUNK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624848 | Binding constant for CSNK2A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624803 | Binding constant for CHEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624845 | Binding constant for CDK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625135 | Binding constant for ADCK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1612813 | Inhibition of CSK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID624878 | Binding constant for PIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1612812 | Inhibition of BTK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID1689135 | Cytotoxicity against human HCT-116 p53 mutant cells assessed as inhibition of cell growth after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones. |
| AID625117 | Binding constant for PAK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624767 | Binding constant for MERTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424958 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624750 | Binding constant for PRP4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425097 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624808 | Binding constant for TRKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624758 | Binding constant for RIPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625036 | Binding constant for PIK3CA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215245 | Relative brain accumulation index, ratio of drug level in brain after 4 hrs to AUC (0 to 4 hrs) in Abcb1a/1b (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry relative to wild type FVB mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID1508898 | Inhibition of TEL fused c-KIT V559G mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| AID624981 | Binding constant for ABL1(F317L)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624768 | Binding constant for SRPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625007 | Binding constant for EGFR(T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215244 | Relative brain accumulation index, ratio of drug level in brain after 4 hrs to AUC (0 to 4 hrs) in Abcg2 (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry relative to wild type FVB mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID1425135 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624755 | Binding constant for ZAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625137 | Binding constant for MEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215258 | Relative brain accumulation index, ratio of drug level in brain after 1 hr to AUC (0 to 1 hr) in Abcg2 (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| 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. |
| 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. |
| AID762240 | Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition after 5 days by SRB assay | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. |
| AID624920 | Binding constant for MRCKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624809 | Binding constant for MYLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1215254 | Drug level in brain of Abcb1a/1b (-/-) FVB mouse at 10 mg/kg, po after 1 hr by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID625089 | Binding constant for AAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1584975 | Antiproliferative activity in human OCI-AML2 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID625014 | Binding constant for PRKCE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215236 | Efflux ratio in wild type MDCK2 cells at 1 uM after 1 to 4 hrs | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID624925 | Binding constant for RIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625112 | Binding constant for YANK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624861 | Binding constant for LIMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425076 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624715 | Binding constant for ERK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1565243 | Selectivity index, ratio of IC50 for cytotoxicity against HEK293T cells to IC50 for cytotoxicity against human HT-29 cells | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model. |
| AID624953 | Binding constant for EPHA7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625058 | Binding constant for VRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624709 | Binding constant for MYLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624875 | Binding constant for PDGFRB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424892 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624795 | Binding constant for MET(M1250T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425142 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624913 | Binding constant for TYK2(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425128 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1215212 | Relative brain accumulation index, ratio of drug level in brain after 1 hr to AUC (0 to 1 hr) in Abcb1a/1b (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID624790 | Binding constant for KIT(L576P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625086 | Binding constant for SLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625011 | Binding constant for FGR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624918 | Binding constant for DYRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625002 | Binding constant for EGFR(L747-T751del,Sins) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624800 | Binding constant for IGF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425144 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID625015 | Binding constant for ROCK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1508903 | Inhibition of TEL fused c-KIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| 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. |
| AID624996 | Binding constant for EGFR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425203 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1565239 | Cytotoxicity against human PC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model. |
| AID624917 | Binding constant for MST3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425121 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1510862 | Inhibition of VEGFR3 (unknown origin) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma. |
| AID1508896 | Inhibition of TEL fused c-KIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| 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. |
| AID625010 | Binding constant for FER kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624876 | Binding constant for PDPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624855 | Binding constant for FRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624775 | Binding constant for STK16 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1575474 | Cell cycle arrest in human CEM/ADR5000 cells at 100 nM after 24 hrs by propidium iodide staining based FACS analysis | 2019 | Journal of natural products, 01-25, Volume: 82, Issue:1 | Bifunctional Duocarmycin Analogues as Inhibitors of Protein Tyrosine Kinases. |
| AID624806 | Binding constant for RPS6KA4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624879 | Binding constant for PIK3CG kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID625091 | Binding constant for MAST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624717 | Binding constant for JNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215228 | Drug level in brain of Abcb1a/1b;Abcg2 (-/-) FVB mouse at 10 mg/kg, po after 1 hr by liquid chromatography-tandem mass spectrometry relative to wild type FVB mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID624939 | Binding constant for FLT3(N841I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624978 | Binding constant for ABL1(E255K)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1508902 | Inhibition of TEL fused c-KIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| AID624912 | Binding constant for TYK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID762239 | Antiproliferative activity against human SKBR3 cells assessed as growth inhibition after 5 days by SRB assay | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. |
| AID624992 | Binding constant for ABL1-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625069 | Binding constant for TLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625139 | Binding constant for SNARK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425168 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624737 | Binding constant for EPHA5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424980 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID1508904 | Inhibition of TEL fused c-KIT D816H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| AID624927 | Binding constant for RPS6KA4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624706 | Binding constant for MLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425111 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425103 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624954 | Binding constant for EPHB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1584949 | Inhibition of BCR/ABL Y253F mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID624746 | Binding constant for WEE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624818 | Binding constant for ULK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624765 | Binding constant for TRKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425196 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID625126 | Binding constant for TAOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624847 | Binding constant for CSNK1E kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1584944 | Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| 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. |
| AID624924 | Binding constant for RIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625111 | Binding constant for RIOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1478069 | Inhibition of human VEGFR2 | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1 | Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID625029 | Binding constant for BRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624955 | Binding constant for EPHB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625087 | Binding constant for MELK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624871 | Binding constant for PAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624985 | Binding constant for ABL1(M351T)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625109 | Binding constant for BIKE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624761 | Binding constant for CDC2L5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625083 | Binding constant for LATS2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624866 | Binding constant for MLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424979 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1612830 | Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID624826 | Binding constant for BMPR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624745 | Binding constant for PKN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1565246 | Selectivity index, ratio of IC50 for cytotoxicity against HEK293T cells to IC50 for cytotoxicity against human U87MG cells | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model. |
| AID1425012 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID625073 | Binding constant for SGK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425013 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424501 | Antitumor activity in renal cell carcinoma patient with previous cytokine therapies assessed as progression free survival | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Recent developments in small molecule therapies for renal cell carcinoma. |
| AID1215232 | Drug level in brain of Abcg2 (-/-) FVB mouse at 10 mg/kg, po after 4 hrs by liquid chromatography-tandem mass spectrometry relative to wild type FVB mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID1424898 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424989 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624944 | Binding constant for ALK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625012 | Binding constant for GAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1689134 | Cytotoxicity against multidrug resistant human KB-V1 cells assessed as inhibition of cell growth after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones. |
| AID624901 | Binding constant for RSK1(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID625001 | Binding constant for EGFR(L747-S752del, P753S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1215242 | Drug transport in MDCK2 cells expressing human ABCG2 assessed as transporter-mediated efflux ratio at 1 uM after 1 to 4 hrs in presence of 5 uM ABCB1/ABCG2 inhibitor elacridar | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| 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. |
| 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. |
| AID624941 | Binding constant for CDKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625101 | Binding constant for TAOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625006 | Binding constant for EGFR(S752-I759del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624952 | Binding constant for EPHA4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425117 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1612811 | Inhibition of BRK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID625030 | Binding constant for LOK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425134 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624712 | Binding constant for DYRK1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1508893 | Inhibition of wild type TEL fused c-KIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| AID624736 | Binding constant for RPS6KA5(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625113 | Binding constant for MARK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624882 | Binding constant for PKAC-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1565241 | Cytotoxicity against human U87MG cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model. |
| AID624787 | Binding constant for KIT(A829P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424939 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624823 | Binding constant for MKNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624778 | Binding constant for ACVRL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625121 | Binding constant for RET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID762241 | Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 5 days by SRB assay | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. |
| AID624733 | Binding constant for SIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625106 | Binding constant for MARK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624752 | Binding constant for SNRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624813 | Binding constant for MINK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424917 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID625140 | Binding constant for MARK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624945 | Binding constant for BMPR1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624926 | Binding constant for RIOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424967 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1508905 | Inhibition of TEL fused c-KIT D820E mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| AID624764 | Binding constant for CLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424499 | Inhibition of VEGFR2 (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Recent developments in small molecule therapies for renal cell carcinoma. |
| AID624868 | Binding constant for MST1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424502 | Antitumor activity in renal cell carcinoma patient with previous sunitinib treatment assessed as progression free survival | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Recent developments in small molecule therapies for renal cell carcinoma. |
| 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. |
| AID624784 | Binding constant for INSR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215223 | AUC (0 to 4 hrs) in FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID624714 | Binding constant for p38-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625070 | Binding constant for PFTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625023 | Binding constant for HIPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624873 | Binding constant for PAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625071 | Binding constant for STK39 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1178626 | Cytotoxicity against human MDA-MB-468 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents. |
| AID624834 | Binding constant for DAPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625110 | Binding constant for TRPM6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624938 | Binding constant for FLT3(K663Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1584941 | Inhibition of BCR/ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID625130 | Binding constant for FGFR4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424978 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624730 | Binding constant for CAMK2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624936 | Binding constant for FLT3(D835Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625119 | Binding constant for CAMK1G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624872 | Binding constant for PAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624956 | Binding constant for EPHB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425089 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID624857 | Binding constant for HCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625107 | Binding constant for DMPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625088 | Binding constant for ARK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424991 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624940 | Binding constant for FLT3(R834Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1201534 | Inhibition of PLK-4 (unknown origin) | 2015 | European journal of medicinal chemistry, 05-05, Volume: 95 | Drug discovery using spirooxindole cores: Success and Challenges [corrected]. |
| AID624881 | Binding constant for PKAC-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1565238 | Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model. |
| AID624771 | Binding constant for TLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1612814 | Inhibition of Fyn A (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID624889 | Binding constant for JNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625050 | Binding constant for PKN2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624725 | Binding constant for NEK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625055 | Binding constant for MST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624833 | Binding constant for CSNK1G2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425169 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1689133 | Cytotoxicity against human HDfa cells assessed as inhibition of cell growth after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones. |
| 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. |
| AID625068 | Binding constant for NEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625120 | Binding constant for EPHA8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624742 | Binding constant for NEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624957 | Binding constant for EPHB6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625040 | Binding constant for PIK3CA(E545K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625118 | Binding constant for CAMK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624819 | Binding constant for ACVR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1508907 | Inhibition of TEL fused c-KIT A829P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| AID624841 | Binding constant for BLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625090 | Binding constant for ICK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625142 | Binding constant for TSSK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625043 | Binding constant for PIK3CA(I800L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625082 | Binding constant for RSK4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624799 | Binding constant for TIE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1584974 | Antiproliferative activity in human HL60 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID624885 | Binding constant for ERK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624731 | Binding constant for CAMK2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1612815 | Inhibition of LCK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID624791 | Binding constant for KIT(V559D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624898 | Binding constant for GRK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624812 | Binding constant for SBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624785 | Binding constant for JAK3(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1508908 | Binding affinity to c-KIT (unknown origin) | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| AID1178637 | Cytotoxicity against human SKBR3 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents. |
| 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. |
| AID625123 | Binding constant for RET(V804L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215247 | Drug transport in MDCK2 cells expressing mouse ABCC2 assessed as transporter-mediated drug transport at 1 uM after 1 to 4 hrs | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| 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. |
| AID625049 | Binding constant for PRKCH kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624766 | Binding constant for p38-gamma kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624864 | Binding constant for CTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425113 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1584948 | Inhibition of BCR/ABL Q252H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID625027 | Binding constant for MAP3K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1508906 | Inhibition of TEL fused c-KIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| 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. |
| AID625062 | Binding constant for MAP3K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624892 | Binding constant for p38-delta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625021 | Binding constant for LIMK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424981 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID625108 | Binding constant for MKNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625080 | Binding constant for EIF2AK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1584946 | Inhibition of BCR/ABL F317I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID1565242 | Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model. |
| AID624783 | Binding constant for FGFR3(G697C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624718 | Binding constant for PFTAIRE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624763 | Binding constant for RIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215226 | Drug level in brain of Abcg2 (-/-) FVB mouse at 10 mg/kg, po after 1 hr by liquid chromatography-tandem mass spectrometry relative to wild type FVB mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID1612816 | Inhibition of Lyn B (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| 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. |
| 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. |
| AID625034 | Binding constant for PDGFRA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624740 | Binding constant for LRRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624757 | Binding constant for PKMYT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424928 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID624798 | Binding constant for LKB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID762206 | Inhibition of human PLK4 | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. |
| AID625008 | Binding constant for EPHA1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215216 | Relative brain accumulation index, ratio of drug level in brain after 4 hrs to AUC (0 to 4 hrs) in FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| 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. |
| AID1215221 | AUC (0 to 4 hrs) in Abcb1a/1b;Abcg2 (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID625037 | Binding constant for PIK3CA(C420R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424498 | Inhibition of VEGFR1 (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Recent developments in small molecule therapies for renal cell carcinoma. |
| AID1565276 | Inhibition of recombinant human N-terminal GST-tagged VEGFR2 (805 to 1356 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 45 mins by kinase-Glo luminescent assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model. |
| AID625022 | Binding constant for MUSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624908 | Binding constant for TEC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625016 | Binding constant for SRC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1584970 | Antiproliferative activity in human K562 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| 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. |
| AID1178636 | Cytotoxicity against human MDA-MB-231 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents. |
| AID624870 | Binding constant for NEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624951 | Binding constant for EPHA2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625079 | Binding constant for NEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625056 | Binding constant for TESK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215214 | Relative brain accumulation index, ratio of drug level in brain after 4 hrs to AUC (0 to 4 hrs) in Abcb1a/1b (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| 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. |
| AID1584976 | Antiproliferative activity in human U937 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| AID624719 | Binding constant for GRK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624884 | Binding constant for PRKD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624734 | Binding constant for YANK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625019 | Binding constant for AKT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215231 | Relative brain accumulation index, ratio of drug level in brain after 1 hr to AUC (0 to 1 hr) in Abcb1a/1b;Abcg2 (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry relative to wild type FVB mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID624858 | Binding constant for JAK1(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425037 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624756 | Binding constant for MAP4K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624930 | Binding constant for TNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1689136 | Cytotoxicity against wild type human HCT-116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones. |
| AID624780 | Binding constant for CDK4-cyclinD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625066 | Binding constant for IRAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624972 | Binding constant for MTOR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625042 | Binding constant for PIK3CA(H1047Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624910 | Binding constant for TTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425125 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425187 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID1584972 | Antiproliferative activity in human MEG01 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID624969 | Binding constant for ROCK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624965 | Binding constant for LZK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624793 | Binding constant for KIT(V559D,V654A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625081 | Binding constant for RSK4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625072 | Binding constant for TBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624932 | Binding constant for CLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624708 | Binding constant for CDC2L1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624964 | Binding constant for DYRK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424976 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID624854 | Binding constant for FLT4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425209 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID762238 | Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 5 days by SRB assay | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. |
| AID624703 | Binding constant for MAPKAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624852 | Binding constant for FES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID625048 | Binding constant for PRKCD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624769 | Binding constant for AURKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624961 | Binding constant for TGFBR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424908 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID625045 | Binding constant for PIK3CA(Q546K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1412778 | Antiproliferative activity against VEGF-stimulated human HepG2 cells after 48 hrs by CCK8 assay | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Discovery of novel picolinamide-based derivatives as novel VEGFR-2 kinase inhibitors: synthesis, |
| AID1612829 | Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID625093 | Binding constant for TNIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624874 | Binding constant for PCTK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1508901 | Inhibition of TEL fused c-KIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| AID625102 | Binding constant for PRKD2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425108 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID1575475 | Cell cycle arrest in human Jurkat cells at 100 nM after 24 hrs by propidium iodide staining based FACS analysis | 2019 | Journal of natural products, 01-25, Volume: 82, Issue:1 | Bifunctional Duocarmycin Analogues as Inhibitors of Protein Tyrosine Kinases. |
| 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. |
| AID1215239 | Drug transport in MDCK2 cells expressing human ABCB1 assessed as transporter-mediated efflux ratio at 1 uM after 1 to 4 hrs | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| 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. |
| AID1508899 | Inhibition of TEL fused c-KIT L576P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| 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. |
| AID1424936 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1425080 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624770 | Binding constant for CAMK2D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625033 | Binding constant for PCTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624802 | Binding constant for PIM3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625116 | Binding constant for ADCK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424995 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID624929 | Binding constant for BRSK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625096 | Binding constant for STK36 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| AID624749 | Binding constant for CASK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625061 | Binding constant for MAP4K5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624893 | Binding constant for MEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1584950 | Inhibition of BCR/ABL V299L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID625005 | Binding constant for EGFR(L861Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215246 | Relative brain accumulation index, ratio of drug level in brain after 4 hrs to AUC (0 to 4 hrs) in Abcb1a/1b;Abcg2 (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry relative to wild type FVB mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID1565245 | Selectivity index, ratio of IC50 for cytotoxicity against HEK293T cells to IC50 for cytotoxicity against human A549 cells | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model. |
| AID624960 | Binding constant for RSK2(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624937 | Binding constant for FLT3(ITD) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215255 | Drug level in brain of Abcb1a/1b;Abcg2 (-/-) FVB mouse at 10 mg/kg, po after 1 hr by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| 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. |
| 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. |
| AID624942 | Binding constant for DRAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624991 | Binding constant for ABL1-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624958 | Binding constant for PIK3C2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624984 | Binding constant for ABL1(H396P)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624923 | Binding constant for MAPKAPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425120 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424957 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624720 | Binding constant for HIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1875855 | Effect on angiogenic activity in 24 hrs post-fertilized fil1/EGFP transgenic zebrafish embryo assessed as subintestinal vessel area at 100 nM measured after 48 hrs by fluorescence microscopy (Rvb = 100%) | |||
| AID625059 | Binding constant for YSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625095 | Binding constant for SIK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624849 | Binding constant for CSNK2A2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625018 | Binding constant for YES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624950 | Binding constant for DMPK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625128 | Binding constant for CSNK1G1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215238 | Drug transport in MDCK2 cells at 1 uM after 1 to 4 hrs in presence of 5 uM ABCB1/ABCG2 inhibitor elacridar | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID624904 | Binding constant for NEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625028 | Binding constant for ASK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1178625 | Cytotoxicity against human MCF7 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents. |
| AID1575476 | Cell cycle arrest in human A549 cells at 100 nM after 24 hrs by propidium iodide staining based FACS analysis | 2019 | Journal of natural products, 01-25, Volume: 82, Issue:1 | Bifunctional Duocarmycin Analogues as Inhibitors of Protein Tyrosine Kinases. |
| AID624883 | Binding constant for PRKCI kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424998 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1565240 | Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model. |
| AID624850 | Binding constant for DDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624979 | Binding constant for ABL1(F317I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624905 | Binding constant for CDKL5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215257 | Relative brain accumulation index, ratio of drug level in brain after 1 hr to AUC (0 to 1 hr) in FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID625124 | Binding constant for RET(V804M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624975 | Binding constant for PLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624886 | Binding constant for ERK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625143 | Binding constant for CAMKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624869 | Binding constant for NEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624713 | Binding constant for ERK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624722 | Binding constant for MKK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624974 | Binding constant for PIK3CD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624839 | Binding constant for AKT2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625092 | Binding constant for NDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624887 | Binding constant for ERK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425159 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID624983 | Binding constant for ABL1(H396P)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1425015 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624946 | Binding constant for BRAF kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624963 | Binding constant for LATS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624777 | Binding constant for DDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424901 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1215251 | AUC (0 to 1 hr) in Abcb1a/1b (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID624762 | Binding constant for DLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624859 | Binding constant for JAK1(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215225 | Relative brain accumulation index, ratio of drug level in brain after 4 hrs to AUC (0 to 4 hrs) in Abcb1a/1b;Abcg2 (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID624973 | Binding constant for JAK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215215 | Relative brain accumulation index, ratio of drug level in brain after 4 hrs to AUC (0 to 4 hrs) in Abcg2 (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID1612828 | Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| 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. |
| AID624911 | Binding constant for TXK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624753 | Binding constant for PKNB(M.tuberculosis) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624827 | Binding constant for CAMK2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624817 | Binding constant for MYO3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424930 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1584943 | Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID625131 | Binding constant for FGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624840 | Binding constant for AXL kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624998 | Binding constant for EGFR(G719C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624880 | Binding constant for PIK4CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| AID624860 | Binding constant for VEGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425185 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624895 | Binding constant for MEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425007 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID625053 | Binding constant for PRKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624999 | Binding constant for EGFR(G719S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624986 | Binding constant for ABL1(Q252H)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624862 | Binding constant for LYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1689137 | Cytotoxicity against human 518A2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones. |
| AID1215243 | Drug transport in MDCK2 cells expressing mouse ABCG2 assessed as transporter-mediated efflux ratio at 1 uM after 1 to 4 hrs in presence of 5 uM ABCB1/ABCG2 inhibitor elacridar | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID1424959 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624977 | Binding constant for OSR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424985 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID1565244 | Selectivity index, ratio of IC50 for cytotoxicity against HEK293T cells to IC50 for cytotoxicity against human PC3 cells | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model. |
| AID624821 | Binding constant for YANK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425181 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID624980 | Binding constant for ABL1(F317I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424966 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID625063 | Binding constant for PLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625136 | Binding constant for YSK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424896 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID625032 | Binding constant for TRKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425206 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624820 | Binding constant for ACVR2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624935 | Binding constant for FLT3(D835H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425063 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID624705 | Binding constant for MYLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425026 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624735 | Binding constant for ANKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425123 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID625020 | Binding constant for ITK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624773 | Binding constant for AMPK-alpha1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215217 | Drug level in brain of Abcb1a/1b;Abcg2 (-/-) FVB mouse at 10 mg/kg, po after 4 hrs by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| 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. |
| AID625075 | Binding constant for INSRR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624921 | Binding constant for MAP4K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425124 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624754 | Binding constant for NEK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625132 | Binding constant for FGFR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624738 | Binding constant for MLCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425177 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID624853 | Binding constant for FLT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID538338 | Inhibition of recombinant VEGFR2 after 1 hr by fluorescence polarization assay | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors. |
| AID1584973 | Antiproliferative activity in human MEC1 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID1412777 | Antiproliferative activity against VEGF-stimulated human A549 cells after 48 hrs by CCK8 assay | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Discovery of novel picolinamide-based derivatives as novel VEGFR-2 kinase inhibitors: synthesis, |
| AID624948 | Binding constant for CSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625074 | Binding constant for IKK-epsilon kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID625046 | Binding constant for PIK3CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625067 | Binding constant for NDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425051 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1215222 | AUC (0 to 4 hrs) in Abcb1a/1b (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID624966 | Binding constant for DCAMKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424931 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID625031 | Binding constant for MRCKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625115 | Binding constant for PAK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624836 | Binding constant for IKK-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624907 | Binding constant for SYK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625078 | Binding constant for SRPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624989 | Binding constant for ABL1(T315I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625134 | Binding constant for PIP5K2C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1412779 | Selectivity ratio of IC50 for VEGF-stimulated human HepG2 cells to IC50 for VEGF-stimulated human A549 cells | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Discovery of novel picolinamide-based derivatives as novel VEGFR-2 kinase inhibitors: synthesis, |
| AID624906 | Binding constant for S6K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624947 | Binding constant for BRAF(V600E) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425150 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624888 | Binding constant for ERK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID762243 | Inhibition of PLK3 (unknown origin) by FRET-based homogeneous assay | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. |
| AID625035 | Binding constant for PHKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624915 | Binding constant for PIP5K2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1584939 | Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID625051 | Binding constant for PRKCQ kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425017 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1215256 | Drug level in brain of FVB mouse at 10 mg/kg, po after 1 hr by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID624897 | Binding constant for RAF1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425157 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624899 | Binding constant for ROS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625039 | Binding constant for PIK3CA(E545A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624739 | Binding constant for GRK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625054 | Binding constant for MST2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624865 | Binding constant for MAP3K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625026 | Binding constant for MAP3K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624810 | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625052 | Binding constant for PRKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1584977 | Antiproliferative activity in CHO cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID624959 | Binding constant for MAP4K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624844 | Binding constant for CDK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624891 | Binding constant for JNK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624814 | Binding constant for DCAMKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425119 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624716 | Binding constant for CSNK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624781 | Binding constant for CDK4-cyclinD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624721 | Binding constant for MEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625127 | Binding constant for RSK3(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1425138 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1215250 | AUC (0 to 1 hr) in Abcg2 (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID625009 | Binding constant for EPHA3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625044 | Binding constant for PIK3CA(M1043I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624747 | Binding constant for SgK110 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424990 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID625129 | Binding constant for HIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425047 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID1425031 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1584940 | Inhibition of wild type BCR/ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID625104 | Binding constant for MYO3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID762246 | Inhibition of N-terminal GST-tagged human PLK4 (1 to 391 amino acids) expressed in Escherichia coli using TMB as substrate after 30 mins by indirect ELISA assay | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. |
| AID1215220 | Drug level in brain of FVB mouse at 10 mg/kg, po after 4 hrs by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID625064 | Binding constant for PIM2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1215235 | Drug transport in MDCK2 cells at 1 uM after 1 to 4 hrs in presence of 5 uM ABCB1 inhibitor zosuquidar | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| 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. |
| 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. |
| 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. |
| AID624759 | Binding constant for PFCDPK1(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624707 | Binding constant for DCAMKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624997 | Binding constant for EGFR(E746-A750del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1612827 | Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID624794 | Binding constant for MET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624933 | Binding constant for PLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624807 | Binding constant for TNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425105 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624829 | Binding constant for CDK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625103 | Binding constant for MST4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624796 | Binding constant for MET(Y1235D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424949 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624830 | Binding constant for CDK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624967 | Binding constant for RPS6KA5(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624828 | Binding constant for CDK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625114 | Binding constant for GSK3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624782 | Binding constant for FGFR3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1508900 | Inhibition of TEL fused c-KIT V654A/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| AID624772 | Binding constant for AURKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424947 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID624909 | Binding constant for TGFBR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1178617 | Inhibition of human N-terminal GST-tagged PLK4 (1 to 391 residues) expressed in Escherichia coli incubated for 30 mins by ELISA method | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents. |
| AID625122 | Binding constant for RET(M918T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624931 | Binding constant for CLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624846 | Binding constant for CSNK1A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624838 | Binding constant for ACVR2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624987 | Binding constant for ABL1(Q252H)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215230 | Relative brain accumulation index, ratio of drug level in brain after 1 hr to AUC (0 to 1 hr) in Abcb1a/1b (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry relative to wild type FVB mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| 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. |
| AID624943 | Binding constant for ACVR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1178616 | Inhibition of PLK4 (unknown origin) | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents. |
| AID1425006 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID624976 | Binding constant for PRKX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1508909 | Binding affinity to c-KIT V559D/T670I double mutant (unknown origin) | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| AID624867 | Binding constant for MLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215218 | Drug level in brain of Abcb1a/1b (-/-) FVB mouse at 10 mg/kg, po after 4 hrs by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| 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. |
| 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. |
| AID624792 | Binding constant for KIT(V559D,T670I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624982 | Binding constant for ABL1(F317L)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1575477 | Cell cycle arrest in human MIAPaCa2 cells at 100 nM after 24 hrs by propidium iodide staining based FACS analysis | 2019 | Journal of natural products, 01-25, Volume: 82, Issue:1 | Bifunctional Duocarmycin Analogues as Inhibitors of Protein Tyrosine Kinases. |
| AID624797 | Binding constant for PHKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624863 | Binding constant for MARK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215241 | Drug transport in MDCK2 cells expressing mouse ABCG2 assessed as transporter-mediated efflux ratio at 1 uM after 1 to 4 hrs | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID625047 | Binding constant for AMPK-alpha2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624843 | Binding constant for CAMK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID762244 | Inhibition of PLK1 (unknown origin) by FRET-based homogeneous assay | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. |
| 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. |
| 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. |
| AID624896 | Binding constant for PRKR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625076 | Binding constant for PLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1585049 | Inhibition of inactive wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| 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. |
| 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. |
| AID624837 | Binding constant for IRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624704 | Binding constant for NEK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1425016 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| 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. |
| AID625065 | Binding constant for CIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425043 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624919 | Binding constant for AURKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624842 | Binding constant for BMX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425082 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID1508892 | Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| AID762245 | Inhibition of PLK2 (unknown origin) by FRET-based homogeneous assay | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. |
| 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. |
| AID1585048 | Inhibition of active wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID624928 | Binding constant for CDKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425008 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624824 | Binding constant for PIP5K1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625024 | Binding constant for PRKD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624990 | Binding constant for ABL1(Y253F)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1508894 | Inhibition of TEL fused c-KIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of ( E)- N |
| AID1215229 | Relative brain accumulation index, ratio of drug level in brain after 1 hr to AUC (0 to 1 hr) in Abcg2 (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry relative to wild type FVB mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| AID625094 | Binding constant for CDK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625000 | Binding constant for EGFR(L747-E749del, A750P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1215224 | AUC (0 to 4 hrs) in Abcg2 (-/-) FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| 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. |
| 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. |
| AID625003 | Binding constant for EGFR(L858R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624890 | Binding constant for p38-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1215249 | AUC (0 to 1 hr) in FVB mouse plasma at 10 mg/kg, po by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5 | Differential impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on axitinib brain accumulation and oral plasma pharmacokinetics. |
| 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. |
| AID624741 | Binding constant for LRRK2(G2019S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1798514 | PLK Kinase Assay from Article 10.1021/bi7008745: \\Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.\\ | 2007 | Biochemistry, Aug-21, Volume: 46, Issue:33 | Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity. |
| AID1801713 | Competition Binding Assays from Article 10.1021/acschembio.5b01063: \\Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors.\\ | 2016 | ACS chemical biology, 05-20, Volume: 11, Issue:5 | Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors. |
| AID1801133 | KinEASE-STK Assay from Article 10.1021/cb500908d: \\Identification and further development of potent TBK1 inhibitors.\\ | 2015 | ACS chemical biology, Jan-16, Volume: 10, Issue:1 | Identification and further development of potent TBK1 inhibitors. |
| 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. |
| AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Identification of potent Yes1 kinase inhibitors using a library screening approach. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| 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. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| 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. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| 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. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1345858 | Human polo like kinase 4 (Polo-like kinase (PLK) family) | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. |
| AID1345506 | Human kinase insert domain receptor (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family) | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors. |
| AID1345506 | Human kinase insert domain receptor (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family) | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2012 | Proceedings of the National Academy of Sciences of the United States of America, Nov-06, Volume: 109, Issue:45 | Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| [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 | 51 (6.84) | 29.6817 |
| 2010's | 463 (62.06) | 24.3611 |
| 2020's | 232 (31.10) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (71.76) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 145 (18.95%) | 5.53% |
| Reviews | 125 (16.34%) | 6.00% |
| Case Studies | 79 (10.33%) | 4.05% |
| Observational | 9 (1.18%) | 0.25% |
| Other | 407 (53.20%) | 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 | ||
|---|---|---|---|---|---|---|---|
| Multi-center Phase II Open-label Study of Bavituximab, Axitinib, and Avelumab in Advanced Hepatocellular Carcinoma [NCT05249569] | Phase 2 | 1 participants (Actual) | Interventional | 2022-11-04 | Terminated(stopped due to Sponsor pulled support for one of the study drugs.) | ||
| A Phase II Study of Transarterial Chemoembolisation and Axitinib for the Treatment of Unresectable Hepatocellular Carcinoma [NCT01352728] | Phase 2 | 50 participants (Actual) | Interventional | 2011-05-18 | Completed | ||
| An Observational Chart Review Study to Describe the Real-world Outcomes and Use of Avelumab in Combination With Axitinib for Treatment of Patients With Advanced Renal Cell Carcinoma in the United Kingdom. [NCT05394493] | 130 participants (Actual) | Observational | 2021-06-11 | Completed | |||
| Retrospective, Multicenter, Observational Study to Evaluate Current Treatment Outcomes in Japanese Patients With Metastatic Renal Cell Carcinoma Treated With Avelumab Plus Axitinib as a First-line Therapy [NCT05012865] | 48 participants (Actual) | Observational | 2021-09-14 | Completed | |||
| A Phase 1b/2 Open Label Umbrella Study of Sasanlimab Combined With Anti-Cancer Therapies Targeting Multiple Molecular Mechanisms in Participants With Non-Small Cell Lung Cancer (NSCLC) [NCT04585815] | Phase 1/Phase 2 | 34 participants (Actual) | Interventional | 2020-11-10 | Active, not recruiting | ||
| Phase II Study of Axitinib Intensification Plus Nivolumab Compared to Nivolumab Alone After Induction With Nivolumab Plus Ipilimumab in mRCC Patients Without Previous Complete Response (AxIn Study). [NCT05817903] | Phase 2 | 118 participants (Anticipated) | Interventional | 2023-04-18 | Recruiting | ||
| A Phase I/II Study of PI3Kγδ Inhibitor Duvelisib in Combination With Nivolumab in Patients With Advanced Unresectable Melanoma Who Have Progressed on Anti-PD1 Therapy [NCT04688658] | Phase 1/Phase 2 | 42 participants (Anticipated) | Interventional | 2021-07-21 | Recruiting | ||
| A RANDOMIZED PHASE 2 STUDY OF THE ANTI-ANGIOGENESIS AGENT AG-013736 IN COMBINATION WITH GEMCITABINE IN PATIENTS WITH CHEMOTHERAPY-NAIVE ADVANCED PANCREATIC CANCER PRECEDED BY A PHASE 1 PORTION [NCT00219557] | Phase 2 | 111 participants (Actual) | Interventional | 2005-07-05 | Completed | ||
| An Expanded Access Program to Axitinib is Available for Patients With Advanced Forms of Kidney Cancer (Ductal; Papillary; Chromophobic; Oncocytic), Confirmed Mutations in VHL, PBRM1 / BAP1, SETD2, VEGF), for Whom Standard Systemic Therapy Has Failed or Pr [NCT05941637] | 0 participants | Expanded Access | Available | ||||
| Phase I Clinical Trials Investigating the Potential Efficacy of Axitinib in Patients With a BRCA 1/2 Mutations Independent of HER2 Expression With Progression After Previous Treatment [NCT05904730] | Phase 1 | 30 participants (Anticipated) | Interventional | 2023-07-11 | Enrolling by invitation | ||
| A Phase II/III Clinical Study to Evaluate the Efficacy and Safety of Fruquintinib in Combination With Sintilimab Versus Axitinib or Everolimus as Second-line Treatment for Locally Advanced or Metastatic Renal Cell Carcinoma [NCT05522231] | Phase 2/Phase 3 | 264 participants (Anticipated) | Interventional | 2022-10-27 | Recruiting | ||
| NAXIVA- Phase II Neoadjuvant Study of Axitinib for Reducing Extent of Venous Tumour Thrombus in Clear Cell Renal Cell Cancer With Venous Invasion [NCT03494816] | Phase 2 | 24 participants (Actual) | Interventional | 2017-12-15 | Completed | ||
| AXEL: Axitinib-Avelumab Combination in Recurrent or Metastatic Nasopharyngeal Cancer: a Multicenter Phase 2 Trial [NCT04562441] | Phase 2 | 43 participants (Anticipated) | Interventional | 2021-05-06 | Active, not recruiting | ||
| Phase I Study of the Combination of Axitinib (AX) Plus Everolimus (EV) in Patients With Malignant Advanced Solid Tumors [NCT01334073] | Phase 1 | 19 participants (Actual) | Interventional | 2011-03-31 | Completed | ||
| An Open-Label, Multi-Center, Phase 2 Clinical Study to Evaluate Efficacy, Safety, and Tolerability of KN046 in Combination With Axitinib in Subjects With Advanced Non-Small Cell Lung Cancer [NCT05420220] | Phase 2 | 54 participants (Anticipated) | Interventional | 2022-07-15 | Enrolling by invitation | ||
| A Phase Ib/II Study of Talazoparib and Axitinib in Metastatic Renal Cell Carcinoma [NCT04337970] | Phase 1/Phase 2 | 23 participants (Actual) | Interventional | 2020-04-06 | Active, not recruiting | ||
| Phase 2 Trial Of AG-013736 As First-Line Treatment For Patients With Squamous Non-Small Cell Lung Cancer Receiving Treatment With Cisplatin And Gemcitabine [NCT00735904] | Phase 2 | 38 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
| Neoadjuvant Pembrolizumab and Axitinib in Renal Cell Carcinoma With Associated Inferior Vena Cava Tumor Thrombus (NEOPAX) [NCT05969496] | Phase 2 | 17 participants (Anticipated) | Interventional | 2023-12-14 | Recruiting | ||
| A Monocentric, Single-arm, Open, Phase II Clinical Study on the Efficacy and Safety of Toripalimab Combined With Axitinib as Neoadjuvant Therapy in Patients With Localized Mucosal Melanoma [NCT04180995] | Phase 2 | 30 participants (Anticipated) | Interventional | 2019-08-06 | Recruiting | ||
| Phase 2 Study of the Anti-Angiogenesis Agent AG-013736 as Second- or Later- Line Treatment in Patients With Advanced Non-Small Cell Lung Cancer [NCT00094094] | Phase 2 | 32 participants (Actual) | Interventional | 2005-02-28 | Completed | ||
| A Phase 1 Study of the VEGF Receptor Tyrosine Kinase Inhibitor Axitinib (INLYTA, IND# TBD) in Children With Recurrent or Refractory Solid Tumors [NCT02164838] | Phase 1 | 51 participants (Anticipated) | Interventional | 2014-09-30 | Completed | ||
| A Pivotal Phase 2 Study Of The Anti-Angiogenesis Agent AG-013736 In Patients With 131I-Refractory Metastatic Or Unresectable Locally-Advanced Thyroid Cancer [NCT00389441] | Phase 2 | 52 participants (Actual) | Interventional | 2006-12-31 | Completed | ||
| Phase 2 Study Of AG-013736 In Patients With Poor Prognosis Acute Myeloid Leukemia (AML) Or Myelodysplastic Syndrome (MDS) [NCT00071006] | Phase 2 | 12 participants (Actual) | Interventional | 2003-09-30 | Completed | ||
| Phase 2 Study Of The Anti-Angiogenesis Agent AG-013736 In Patients With Metastatic Melanoma [NCT00094107] | Phase 2 | 32 participants (Actual) | Interventional | 2004-12-31 | Completed | ||
| Targeting of Renal Cell Cancer With Specific Inhibitors: A Model for Selective Adaptive Medicine Based on Molecular Alterations [NCT02560012] | Phase 2 | 4 participants (Actual) | Interventional | 2016-01-04 | Terminated(stopped due to Loss of laboratory performing molecular analysis) | ||
| A PHASE 1, OPEN-LABEL, MULTI-CENTER, DOSE-FINDING, PHARMACOKINETIC, SAFETY AND TOLERABILITY STUDY OF PF 07265807 IN PARTICIPANTS WITH SELECTED ADVANCED OR METASTATIC SOLID TUMOR MALIGNANCIES [NCT04458259] | Phase 1 | 67 participants (Actual) | Interventional | 2020-09-24 | Active, not recruiting | ||
| Phase II Clinical Trial on the Combination of Avelumab and Axitinib for the Treatment of Patients With Recurrent Glioblastoma [NCT03291314] | Phase 2 | 52 participants (Actual) | Interventional | 2017-05-03 | Completed | ||
| Phase II Study of Toripalimab Combined With Axitinib as Neoadjuvant Therapy in Patients With Non-metastatic Locally Advanced Nonmetastatic Clear Cell Renal Cell Carcinoma [NCT04118855] | Phase 2 | 20 participants (Actual) | Interventional | 2020-03-01 | Completed | ||
| An Open Label Continuation Study of TRC105 Therapy for Patients Who Have Completed a Prior TRC105 Trial and Are Judged by the Investigator to Have the Potential to Benefit From Continued TRC105 Therapy [NCT02354612] | 0 participants | Expanded Access | No longer available | ||||
| A Phase III Randomized, Open-label Study to Evaluate Efficacy and Safety of Pembrolizumab (MK-3475) in Combination With Axitinib Versus Sunitinib Monotherapy as a First-line Treatment for Locally Advanced or Metastatic Renal Cell Carcinoma (mRCC) (KEYNOTE [NCT02853331] | Phase 3 | 861 participants (Actual) | Interventional | 2016-09-16 | Active, not recruiting | ||
| OASIS: Open-label, Dose-escalation, Phase 1/2a Study of the Safety and Tolerability of Suprachoroidally Administered CLS-AX Following Intravitreal Anti-VEGF Therapy in Subjects With Neovascular Age-related Macular Degeneration [NCT04626128] | Phase 1/Phase 2 | 27 participants (Actual) | Interventional | 2020-12-15 | Completed | ||
| A Multicenter, NI, Retrospective, Observational Study Evaluating Real-World Treatment Outcomes in Japanese Patients With Metastatic Renal Cell Carcinoma (mRCC) Treated With Avelumab Plus Axitinib as First-line Therapy: J-DART2 [NCT05650164] | 171 participants (Actual) | Observational | 2023-01-25 | Active, not recruiting | |||
| A Phase I Multi-center Study to Evaluate the Safety ,Tolerability and Efficacy of LBL-007 Combined With Toripalimab or LBL-007 Combined With Toripalimab and Axitinib Tablets in the Treatment of Unresectable or Metastatic Melanoma [NCT04640545] | Phase 1 | 88 participants (Anticipated) | Interventional | 2020-05-12 | Recruiting | ||
| A Multi-Center, Open Label, Randomized Phase 2 Study of AGS-16C3F vs. Axitinib in Metastatic Renal Cell Carcinoma [NCT02639182] | Phase 2 | 133 participants (Actual) | Interventional | 2016-05-03 | Completed | ||
| A Single-center, Non-randomized Controlled, Single-arm, Phase II Clinical Trial of Pembrolizumab and Axitinib as Neoadjuvant Therapy for Locally Advanced Non-metastatic Clear Cell Renal Cell Carcinoma [NCT04995016] | Phase 2 | 18 participants (Anticipated) | Interventional | 2021-08-20 | Not yet recruiting | ||
| A Prospective Observational Study of Molecular Classification and Circulating Tumor DNA Dynamic Monitoring to Explore Related Factors That Predict the Efficacy of Single Targeted Therapy or Combined With Immunotherapy for Metastatic Renal Cell Carcinoma [NCT05816642] | 500 participants (Anticipated) | Interventional | 2022-08-01 | Recruiting | |||
| A Dutch National Study on Behalf of the CPCT to Facilitate Patient Access to Commercially Available, Targeted Anti-cancer Drugs to Determine the Potential Efficacy in Treatment of Advanced Cancers With a Known Molecular Profile [NCT02925234] | Phase 2 | 1,550 participants (Anticipated) | Interventional | 2016-08-31 | Recruiting | ||
| A Prospective Clinical Study on the Safety and Effectiveness of Tislelizumab Combined With Axitinib for Neoadjuvant Treatment of Clear Cell Renal Cell Carcinoma [NCT05172440] | Phase 2 | 20 participants (Anticipated) | Interventional | 2021-12-09 | Active, not recruiting | ||
| Phase 2 Study of the Anti-Angiogenesis Agent AG-013736 in Patients With Metastatic Thyroid Cancer Who Are Refractory to or Not Suitable Candidates for 131 I Treatment [NCT00094055] | Phase 2 | 60 participants (Actual) | Interventional | 2004-09-30 | Completed | ||
| A Phase 1/2 Study of INCB099280 in Combination With Axitinib in Adults With Advanced Solid Tumors [NCT05949632] | Phase 1/Phase 2 | 145 participants (Anticipated) | Interventional | 2023-12-15 | Not yet recruiting | ||
| A Randomized Phase I/II Study of Standard Chemotherapy (Cisplatin and Pemetrexed) With or Without Axitinib in Patients With Malignant Mesothelioma: Interim Biopsy Analysis to Determine Efficacy [NCT01211275] | Phase 1/Phase 2 | 32 participants (Actual) | Interventional | 2009-05-22 | Completed | ||
| A Phase 1b, Open-label Study to Evaluate the Safety, Tolerability, Pharmacokinetics, Immunogenicity, and Antitumor Activity of MEDI5752 in Combination With Axitinib in Subjects With Advanced Renal Cell Carcinoma [NCT04522323] | Phase 1 | 179 participants (Anticipated) | Interventional | 2020-08-05 | Recruiting | ||
| Axitinib Plus Toripalimab as Second-line Treatment in Hepatobiliary Malignant Tumors: a Single-arm, Non-randomized, Single-center Phase II Trial [NCT04010071] | Phase 2 | 60 participants (Anticipated) | Interventional | 2020-05-01 | Recruiting | ||
| Retrospective Analysis of Axitinib Treatment Optimization and Management of Selected Immune Related Adverse Events of Checkpoints Inhibitors [NCT04555603] | 0 participants (Actual) | Observational | 2020-09-15 | Withdrawn(stopped due to Failed at data quality assurance process before any analyses would be performed) | |||
| Pre-Surgical Androgen Deprivation Therapy With or Without Axitinib in Previously Untreated Prostate Cancer Patients With Known or Suspected Lymph Node Metastasis [NCT01409200] | Phase 2 | 73 participants (Actual) | Interventional | 2012-03-26 | Active, not recruiting | ||
| A Randomized, Controlled, Multicenter Phase II Clinical Study to Evaluate the Efficacy and Safety of Toripalimab Injection Combined With Axitinib in the First-Line Treatment of Patients With Advanced Mucosal Melanoma [NCT03941795] | Phase 2 | 99 participants (Anticipated) | Interventional | 2019-11-11 | Recruiting | ||
| A Clinicopathological Phase II Study of Axitinib in Patients With Advanced Angiosarcoma and Other Soft Tissue Sarcomas [NCT01140737] | Phase 2 | 145 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
| AN OPEN LABEL, SINGLE ARM PHASE 1B STUDY OF AVELUMAB PLUS AXITINIB AS FIRST LINE TREATMENT IN PATIENTS WITH ADVANCED HEPATOCELLULAR CARCINOMA [NCT03289533] | Phase 1 | 22 participants (Actual) | Interventional | 2017-09-08 | Completed | ||
| A Randomized Phase II Clinical Trial on the Efficacy of Axitinib as a Monotherapy or in Combination With Lomustine for the Treatment of Patients With Recurrent Glioblastoma [NCT01562197] | Phase 2 | 56 participants (Actual) | Interventional | 2014-04-30 | Completed | ||
| A Phase II Trial of Axitinib (AG-013736) After Prior Antiangiogenic Therapy in Advanced Hepatocellular Carcinoma [NCT01334112] | Phase 2 | 30 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
| Avelumab With Axitinib in Persistent or Recurrent Cervical Cancer After Platinum-based Chemotherapy - a Proof-of-concept Study (ALARICE Study) [NCT03826589] | 23 participants (Anticipated) | Interventional | 2019-06-01 | Active, not recruiting | |||
| Phase I/II Study of Seleno-L Methionine (SLM) in Sequential Combination With Fixed Doses and Schedules of Axitinib and Pembrolizumab (SAP) in Locally Advanced and Metastatic Clear Cell Renal Cell Carcinoma (ccRCC) [NCT05363631] | Phase 1/Phase 2 | 55 participants (Anticipated) | Interventional | 2022-09-19 | Recruiting | ||
| Phase 1B Study of Hepatic Chemoembolization Plus Axitinib and Hydroxychlorquine for Liver-Dominant Metastatic Adenocarcinoma Of The Colon And Rectum [NCT04873895] | Phase 1 | 25 participants (Anticipated) | Interventional | 2022-01-24 | Recruiting | ||
| Retrospective Observational Study Of Subjects With Cytokine-Refractory Metastatic Renal Cancer Treated With Axitinib (AG-013736) To Estimate 5-Yr Survival [NCT01056263] | 52 participants (Actual) | Observational | 2010-04-30 | Completed | |||
| A Randomized, Phase II Study Assessing Axitinib as Pre-Surgical Therapy in Patients With High Risk Prostate Cancer [NCT01385059] | Phase 2 | 11 participants (Actual) | Interventional | 2011-10-28 | Completed | ||
| Randomized Phase II Stereotactic Ablative Radiation Therapy (SABR) for Metastatic Unresected Renal Cell Carcinoma (RCC) Receiving Immunotherapy (SAMURAI) [NCT05327686] | Phase 2 | 240 participants (Anticipated) | Interventional | 2022-06-30 | Recruiting | ||
| Phase II Study on Inlyta® (Axitinib) in Recurrent and/or Metastatic Salivary Gland Cancers (SGCs) of the Upper Aerodigestive Tract [NCT02857712] | Phase 2 | 26 participants (Actual) | Interventional | 2014-12-31 | Completed | ||
| An Open Label Phase 1 Study To Evaluate The Pharmacokinetics Of AG-013736 In Healthy Chinese Volunteers [NCT00919204] | Phase 1 | 14 participants (Actual) | Interventional | 2009-08-31 | Completed | ||
| AG-013736 (AXITINIB) FOR THE TREATMENT OF METASTATIC RENAL CELL CANCER [NCT00920816] | Phase 3 | 492 participants (Actual) | Interventional | 2009-08-25 | Completed | ||
| Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR): A Phase II Basket Trial [NCT03297606] | Phase 2 | 720 participants (Anticipated) | Interventional | 2018-03-23 | Recruiting | ||
| Phase II Study on Axitinib in Advanced VEGFR and/or PDGFR Solitary Fibrous Tumor [NCT02261207] | Phase 2 | 17 participants (Actual) | Interventional | 2014-11-30 | Completed | ||
| A Multicenter Randomized Controlled Clinical Study of Neoadjuvant Combination of Axitinib Plus PD-1 Monoclonal Antibody to Improve Disease Free Survival of Patients With Renal Cell Carcinoma [NCT05738694] | Phase 2 | 246 participants (Anticipated) | Interventional | 2023-04-19 | Recruiting | ||
| Biomarker Study of Patients With Metastatic Clear Cell Renal Carcinoma (ccRCC) Undergoing Sequential Therapy With 1st Line Sunitinib and 2nd Line Axitinib [NCT03592199] | Phase 2 | 7 participants (Actual) | Interventional | 2017-12-11 | Active, not recruiting | ||
| Modular Phase 1B Hypothesis-Testing, Biomarker-Driven, Talazoparib Combination Trial (TalaCom) [NCT04693468] | Phase 1 | 111 participants (Anticipated) | Interventional | 2020-12-01 | Recruiting | ||
| A PHASE 2, OPEN LABEL STUDY TO EVALUATE SAFETY AND CLINICAL ACTIVITY OF AVELUMAB (BAVENCIO (REGISTERED)) IN COMBINATION WITH AXITINIB (INLYTA (REGISTERED)) IN PATIENTS WITH ADVANCED OR METASTATIC PREVIOUSLY TREATED NON-SMALL CELL LUNG CANCER OR TREATMENT [NCT03472560] | Phase 2 | 60 participants (Actual) | Interventional | 2018-05-02 | Terminated(stopped due to The study was terminated since there was no need for further safety or efficacy data to be collected. The participants having benefit from the Investigational treatments have been moved to a continuation study (NCT05059522)) | ||
| A Phase II Clinical Trial Examining the Impact Of Neoadjuvant Axitinib On Primary Tumor Response In Patients With Locally Advanced Clear Cell Renal Cell Carcinoma [NCT01263769] | Phase 2 | 39 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
| Phase 2 Study of Axitinib + Ipilimumab in Advanced Melanoma [NCT04996823] | Phase 2 | 25 participants (Anticipated) | Interventional | 2021-08-04 | Recruiting | ||
| Avelumab, Palbociclib and Axitinib in in Treatment Naive Metastatic Clear Cell Renal Cell Carcinoma. [NCT05176288] | Phase 2 | 0 participants (Actual) | Interventional | 2024-05-31 | Withdrawn(stopped due to The overall protocol will be changed in a new amendment, which will be resubmitted under the new IND.) | ||
| A Phase 1 Dose-Finding Study Of The Anti-Angiogenesis Agent, AG-013736, In Combinations Of Paclitaxel/Carboplatin, Weekly Paclitaxel, Docetaxel, Capecitabine, Gemcitabine/Cisplatin and Pemetrexed/Cisplatin In Patients With Advanced Solid Tumors [NCT00454649] | Phase 1 | 102 participants (Actual) | Interventional | 2005-12-31 | Completed | ||
| Randomized, Placebo-Controlled, Double-Blind, Phase 2 Study Of AG-013736 In Combination With Docetaxel Versus Docetaxel Alone In Patients With Metastatic Breast Cancer Preceded By A Phase 1 Evaluation Of The Combination [NCT00076024] | Phase 1/Phase 2 | 174 participants (Actual) | Interventional | 2004-02-29 | Completed | ||
| Pembrolizumab With Axitinib in Recurrent Endometrial Cancer With Deficient Mismatch Repair System Post PD1 Exposure: Phase II Trial [NCT04197219] | Phase 2 | 0 participants (Actual) | Interventional | 2021-02-01 | Withdrawn(stopped due to PI is leaving institution) | ||
| Genomics-Based Target Therapy for Children With Relapsed or Refractory Malignancy [NCT02638428] | Phase 2 | 90 participants (Anticipated) | Interventional | 2015-12-31 | Recruiting | ||
| A Phase I Clinical Trial Evaluating the Safety and Maximum Tolerated Dose of Axitinib in Combination With Radiotherapy for Advanced Hepatocellular Carcinoma (HCC) [NCT02814461] | Phase 1 | 9 participants (Actual) | Interventional | 2015-11-30 | Completed | ||
| Alternating or Combined Therapy With Axitinib and Bosutinib for Patients With Chronic Myeloid Leukemia in Chronic, Accelerated, or Blastic Phases [NCT02782403] | Phase 1 | 4 participants (Actual) | Interventional | 2017-03-20 | Terminated(stopped due to Terminated per PI's request at the time of CR. Study was closed due to low/slow accrual due to other competing studies.) | ||
| Phase 2 Study of Axitinib + PD-1 Blockade in Mucosal Melanoma With Pilot Addition of Stereotactic Body Radiotherapy or Ipilimumab in Select Progressors [NCT05384496] | Phase 2 | 20 participants (Anticipated) | Interventional | 2022-05-17 | Recruiting | ||
| Avelumab Master Protocol: An Open-label Continuation Study for Participants Continuing From Pfizer-sponsored Avelumab Clinical Studies. [NCT05059522] | Phase 3 | 262 participants (Anticipated) | Interventional | 2021-09-29 | Recruiting | ||
| A PHASE 3, MULTINATIONAL, RANDOMIZED, OPEN-LABEL, PARALLEL-ARM STUDY OF AVELUMAB (MSB0010718C) IN COMBINATION WITH AXITINIB (INLYTA(REGISTERED)) VERSUS SUNITINIB (SUTENT(REGISTERED)) MONOTHERAPY IN THE FIRST-LINE TREATMENT OF PATIENTS WITH ADVANCED RENAL [NCT02684006] | Phase 3 | 888 participants (Actual) | Interventional | 2016-03-23 | Active, not recruiting | ||
| International Multicentric Study ARON-1 [NCT05287464] | 1,220 participants (Anticipated) | Observational | 2022-03-10 | Recruiting | |||
| A Phase 2 Clinical Trial of Axitinib and Avelumab in Patients With Recurrent/Metastatic Adenoid Cystic Carcinoma (ACC) [NCT03990571] | Phase 2 | 36 participants (Actual) | Interventional | 2019-07-22 | Completed | ||
| Randomized Phase 2 Trial Of AG013736 Or Bevacizumab In Combination With Paclitaxel And Carboplatin As First Line Treatment For Patients With Advanced Non Small Cell Lung Cancer [NCT00600821] | Phase 2 | 118 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
| A Phase 1 Study Of Axitinib In Combination With Cisplatin And Capecitabine In Patients With Advanced Gastric Cancer [NCT00842244] | Phase 1 | 22 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
| A Phase 1 Study In Patients With Advanced Solid Tumor To Evaluate The Pharmacokinetics And Safety Of AG-013736 At Single Doses Of 5 mg, 7 mg And 10 mg, And At Multiple Doses [NCT00726752] | Phase 1 | 6 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
| A Phase I Open-Label Study In Healthy Volunteers To Compare The Plasma Pharmacokinetics of Polymorph Form XLI AG-013736 In The Fasted And Fed State [NCT00918632] | Phase 1 | 30 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
| Evaluation of the Safety and Efficacy of Axitinib in Metastatic Renal Cell Carcinoma Patients With Favorable Prognostic Factors [NCT02700568] | Phase 2 | 21 participants (Actual) | Interventional | 2016-01-31 | Completed | ||
| Phase I Study To Determine The Maximally Tolerated Dose Of Oral, Daily CP-868,596 And CP-868,596 Plus AG-013736 When Given In Combination With Docetaxel Administered Every 3 Weeks To Patients With Advanced Solid Tumors [NCT00949624] | Phase 1 | 50 participants (Actual) | Interventional | 2005-12-31 | Completed | ||
| A Randomized, Phase 2 Study to Assess the Safety and Efficacy of CRLX101 in Combination With Bevacizumab in Patients With Metastatic Renal Cell Carcinoma (RCC) Versus Standard of Care (SOC) (Investigator's Choice) [NCT02187302] | Phase 2 | 115 participants (Actual) | Interventional | 2014-07-31 | Completed | ||
| Pharmacodynamic Study of Axitinib in Patients With Advanced Solid Malignancies [NCT00859118] | Phase 1 | 30 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
| A Randomized, Phase 2 Study Of FOLFOX Or FOLFIRI With AG-013736 Or Bevacizumab (Avastin) In Patients With Metastatic Colorectal Cancer After Failure Of An Irinotecan Or Oxaliplatin-Containing First-Line Regimen [NCT00615056] | Phase 2 | 171 participants (Actual) | Interventional | 2008-03-31 | Completed | ||
| A Phase II, Single Arm Study of Avelumab In Combination With Axitinib in Patients With Unresectable/Metastatic Gastrointestinal Stromal Tumor After Failure of Standard Therapy - AXAGIST [NCT04258956] | Phase 2 | 58 participants (Anticipated) | Interventional | 2019-04-30 | Recruiting | ||
| A Phase 2, Two-Group, Two-Stage, Open-Label Study of Avelumab in Patients With MSS, MSI-H and POLE-mutated Recurrent or Persistent Endometrial Cancer, Avelumab / Talazoparib in Patients With MSS Recurrent or Persistent Endometrial Cancer, and Avelumab / A [NCT02912572] | Phase 2 | 106 participants (Actual) | Interventional | 2016-11-14 | Active, not recruiting | ||
| PHASE 2 STUDY OF AG-013736 AS SECOND-LINE TREATMENT IN PATIENTS WITH METASTATIC RENAL CELL CANCER [NCT00569946] | Phase 2 | 64 participants (Actual) | Interventional | 2007-12-12 | Completed | ||
| Randomized Phase 2 Study Of Cisplatin/Pemetrexed With Or Without Axitinib (AG-013736) As First-Line Treatment For Patients With Non-Squamous Non-Small Cell Lung Cancer [NCT00768755] | Phase 1/Phase 2 | 180 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
| Treatment Patterns and Outcomes Among Advanced Renal Cell Carcinoma (aRCC) Patients Treated With Cabozantinib or Axitinib Therapy: Non Interventional, Retrospective Study Using Data From Public Health England's Cancer Analysis System [NCT04637204] | 1,540 participants (Actual) | Observational | 2020-11-24 | Completed | |||
| STAR-TOR- REGISTRY FOR THE EVALUATION OF THE SAFETY, TOLERABILITY AND EFFICACY OF TEMSIROLIMUS (TORISEL), SUNITINIB (SUTENT) AND AXITINIB (INLYTA) FOR THE TREATMENT OF SUBJECTS WITH ADVANCED RENAL CELL CARCINOMA (MRCC), MANTLE CELL LYMPHOMA (MCL) AND GAST [NCT00700258] | 1,520 participants (Actual) | Observational | 2008-02-13 | Completed | |||
| Phase 2 Study of CP-868,596 + Docetaxel, AG-013736 + Docetaxel, or CP-868,596 + AG-013736 + Docetaxel and of Docetaxel Alone in Patients With Stage IIIb or IV Non-Small Cell Lung Cancer. [NCT00386555] | Phase 2 | 0 participants (Actual) | Interventional | 2007-05-31 | Withdrawn(stopped due to Study was cancelled before patient enrollment) | ||
| A Phase I Bioequivalence Study To Compare The Plasma Pharmacokinetics Of Five 1-mg And One 5-mg AG-013736 Tablets In Healthy Volunteers [NCT00905814] | Phase 1 | 60 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
| A Randomized, Double-Blind Phase 3 Study Of Gemcitabine Plus AG-013736 Versus Gemcitabine Plus Placebo For The First-Line Treatment Of Patients With Locally Advanced, Unresectable Or Metastatic Pancreatic Cancer. [NCT00471146] | Phase 3 | 630 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
| Randomized Phase II Study of Axitinib in Patients With Recurred or Metastatic Adenoid Cystic Carcinoma [NCT02859012] | Phase 2 | 60 participants (Anticipated) | Interventional | 2016-09-30 | Completed | ||
| Phase 2 Study Of AG-013736 In Patients With Refractory Metastatic Renal Cell Cancer [NCT00282048] | Phase 2 | 62 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
| A Phase 1 Study Of AG-013736 (Axitinib) In Japanese Patients With Advanced Solid Tumors [NCT00447005] | Phase 1 | 12 participants (Actual) | Interventional | 2007-02-28 | Completed | ||
| Treatment Patterns With Targeted Therapies in Metastatic Renal Cell Carcinoma (mRCC) in Sweden - A Retrospective Analysis of Data From National Registries [NCT04669366] | 1,095 participants (Actual) | Observational | 2021-01-20 | Completed | |||
| Phase 1 Umbrella Trial of Erlotinib In Combination With Select Tyrosine Kinase Inhibitors In Adult Patients With Advanced Solid Tumors [NCT06161558] | Phase 1 | 70 participants (Anticipated) | Interventional | 2024-01-03 | Not yet recruiting | ||
| A Phase 1 Clinical Study to Evaluate the Bioavailability of Pembrolizumab Via Subcutaneous Injection of MK-3475A, a Formulation of Pembrolizumab With MK-5180, in Participants With Advanced Solid Tumors [NCT05017012] | Phase 1 | 72 participants (Anticipated) | Interventional | 2021-09-21 | Recruiting | ||
| Phase II Trial of Cadonilimab (AK104) Monotherapy or AK104 Plus Axitinib in Advanced/Metastatic Renal Cell Carcinoma (RCC) [NCT05256472] | Phase 2 | 70 participants (Anticipated) | Interventional | 2023-07-06 | Recruiting | ||
| A Phase II Study of Perioperative Pembrolizumab-Based Therapy in Patients With Locally Advanced or Metastatic Renal Cell Carcinoma Prior to Cytoreductive Nephrectomy or Metastasectomy [NCT04370509] | Phase 2 | 84 participants (Anticipated) | Interventional | 2021-02-09 | Recruiting | ||
| An Open-label, Non-randomized, Multicenter, Two Stage Designed Phase II Study of Axitinib for Downstaging Large Renal Tumors Not Primarily Suitable for Partial Nephrectomy (AXIPAN) [NCT02597322] | Phase 2 | 21 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
| A Randomized Phase 2 Study Of The Anti-Angiogenesis Agent AG-013736 In Combinations With Chemotherapy And Bevacizumab In Patients With Metastatic Colorectal Cancer Preceded By A Phase 1 Portion [NCT00460603] | Phase 1/Phase 2 | 187 participants (Actual) | Interventional | 2006-01-31 | Completed | ||
| AXITINIB (AG-013736) AS SECOND LINE THERAPY FOR METASTATIC RENAL CELL CANCER: AXIS TRIAL [NCT00678392] | Phase 3 | 723 participants (Actual) | Interventional | 2008-09-03 | Completed | ||
| A Two Arm Phase II Trial of Sequential Axitinib and Carboplatin/Paclitaxel in Melanoma With Correlative FLT PET Scans (3'Deoxy-3'-18F-Fluorothymidine Positron Emission Tomography Scans)(CC# 10852) [NCT01174238] | Phase 2 | 40 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
| A Phase 1/2 Trial of X4P-001 as Single Agent and in Combination With Axitinib in Patients With Advanced Renal Cell Carcinoma [NCT02667886] | Phase 1/Phase 2 | 74 participants (Actual) | Interventional | 2016-01-31 | Completed | ||
| A Phase 1 Bioequivalence Study To Compare The Plasma Pharmacokinetics Of AG-013736 Polymorph Form IV Versus Market-Image Polymorph Form XLI Tablets In Healthy Volunteers Under Fed Conditions [NCT01020136] | Phase 1 | 42 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
| Randomized, Double-blind Phase 2 Study Of Axitinib (Ag-013736) With Or Without Dose Titration In Patients With Metastatic Renal Cell Carcinoma [NCT00835978] | Phase 2 | 213 participants (Actual) | Interventional | 2009-08-31 | Completed | ||
| Phase I/II Study of Nivolumab and Axitinib in Patients With Advanced Renal Cell Carcinoma [NCT03172754] | Phase 1/Phase 2 | 98 participants (Anticipated) | Interventional | 2017-06-12 | Recruiting | ||
| A Phase 1 Study To Evaluate The Pharmacokinetics Of AG-013736 In Subjects With Impaired Hepatic Function [NCT00692341] | Phase 1 | 24 participants (Actual) | Interventional | 2008-05-31 | Completed | ||
| CONTINUING ACCESS TO THE TYROSINE KINASE INHIBITOR OF VEGFR-2, AG-013736 (A406) FOR PATIENTS PREVIOUSLY RECEIVING AG-013736 IN CLINICAL TRIALS [NCT00828919] | 52 participants (Actual) | Interventional | 2003-03-07 | Completed | |||
| Clinical Study With Axitinib (AG 013736) In Patients With Metastatic Renal Cell Carcinoma After Failure Of One Prior Systemic First-Line Therapy [NCT01473043] | 0 participants | Expanded Access | 2012-03-31 | No longer available | |||
| Phase II Study of Avelumab Plus Intermittent Axitinib in Previously Untreated Patients With Metastatic Renal Cell Carcinoma (Tide-A Study) [NCT04698213] | Phase 2 | 75 participants (Anticipated) | Interventional | 2020-10-07 | Recruiting | ||
| Phase 2 Study of Axitinib in Patients With Recurrent or Metastatic Nasopharyngeal Carcinoma [NCT01249547] | Phase 2 | 37 participants (Actual) | Interventional | 2010-12-31 | Completed | ||
| A Therapeutic Trial for Safety and Preliminary Efficacy of the Combination of Axitinib and Seleniomethionine (SLM) for Adult Patients With Advanced Metastatic Clear Cell Renal Cell Carcinoma (CCRCC) [NCT02535533] | Phase 1/Phase 2 | 46 participants (Actual) | Interventional | 2016-01-31 | Active, not recruiting | ||
| A MULTICENTER, GLOBAL, RANDOMIZED, DOUBLE-BLIND STUDY OF AXITINIB PLUS BEST SUPPORTIVE CARE VERSUS PLACEBO PLUS BEST SUPPORTIVE CARE IN PATIENTS WITH ADVANCED HEPATOCELLULAR CARCINOMA FOLLOWING FAILURE OF ONE PRIOR ANTIANGIOGENIC THERAPY [NCT01210495] | Phase 2 | 224 participants (Actual) | Interventional | 2010-12-06 | Completed | ||
| Strata PATH™ (Precision Indications for Approved Therapies): A Study Evaluating the Clinical Activity and Safety of Approved Drugs Within Biomarker-Guided Patients With Solid Tumors [NCT05097599] | Phase 2 | 700 participants (Anticipated) | Interventional | 2021-11-19 | Recruiting | ||
| Axitinib as Second-line Treatment for Advanced Hepatocellular Carcinoma [NCT01273662] | Phase 2 | 45 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
| A Prospective, Multicenter, Single-arm Clinical Study of the Efficacy and Safety of Toripalimab in Combination With Axitinib for Postoperative Adjuvant Therapy for Non-clear Renal Cell Carcinoma With High-risk Recurrence Factors [NCT05768464] | Phase 2 | 30 participants (Anticipated) | Interventional | 2023-02-01 | Recruiting | ||
| A Phase II Study of Axitinib as Maintenance Treatment for Patients With Metastatic Colorectal Carcinoma [NCT01483638] | Phase 2 | 84 participants (Actual) | Interventional | 2012-02-29 | Terminated(stopped due to The trial was prematurely closed due to lack of accrual) | ||
| Assessment of the Tumor Vascular Effects of the Pan-vegfr Tyrosine Kinase Inhibitor Axitinib Using Dynamic Contrast-enhanced Ultrasonography (Dce-us) in Patients With Refractory Metastatic Colorectal Cancer [NCT01486251] | 27 participants (Actual) | Interventional | 2011-09-30 | Completed | |||
| A Phase III, Randomized, Open-label, Active Controlled, Multicenter Study on Toripalimab Combined With Axitinib Versus Sunitinib Monotheraphy as a First-Line Treatment for Unresectable or Metastatic Renal Cell Carcinoma (RCC) [NCT04394975] | Phase 3 | 421 participants (Actual) | Interventional | 2020-08-20 | Active, not recruiting | ||
| A Phase II Trial of Concurrent Axitinib and Pembrolizumab in Subjects With Advanced Alveolar Soft Part Sarcoma (ASPS) and Other Soft Tissue Sarcomas (STS) [NCT02636725] | Phase 2 | 33 participants (Actual) | Interventional | 2016-04-19 | Completed | ||
| A Phase II/III Randomized Double-blind Study of Sandostatin LAR in Combination With Axitinib Versus Sandostatin LAR With Placebo in Patients With Advanced G1-G2 Neuroendocrine Tumours (WHO 2010) of Non-pancreatic Origin [NCT01744249] | Phase 2/Phase 3 | 255 participants (Anticipated) | Interventional | 2011-11-30 | Active, not recruiting | ||
| A Randomized Open Label Phase II Study of Immune Checkpoint Inhibitor Combinations With Axitinib in Patients With Previously Untreated Locally Advanced Unresectable or Metastatic Renal Cell Carcinoma [NCT05805501] | Phase 2 | 210 participants (Anticipated) | Interventional | 2023-04-21 | Recruiting | ||
| Predictive Markers of Response in a Phase II Trial of Axitinib in Advanced Melanoma [NCT01533948] | Phase 2 | 25 participants (Actual) | Interventional | 2012-01-31 | Terminated(stopped due to low accrual) | ||
| Phase II Trial of Neoadjuvant Immune-based Combinations in Patients Undergoing Nephrectomy for Locally Advanced ccRCC [NCT06114940] | Phase 2 | 32 participants (Anticipated) | Interventional | 2022-12-20 | Recruiting | ||
| ODYSSEY: A Phase 2b Study of Suprachoroidally Administered CLS-AX in Participants With Neovascular Age-Related Macular Degeneration [NCT05891548] | Phase 2 | 60 participants (Anticipated) | Interventional | 2023-05-31 | Active, not recruiting | ||
| A Study of AK104 Plus Axitinib in Advanced/Metastatic Special Pathological Subtypes of Renal Cell Carcinoma [NCT05808608] | Phase 1/Phase 2 | 33 participants (Anticipated) | Interventional | 2023-09-30 | Not yet recruiting | ||
| Phase I Study of Axitinib and Temsirolimus in Solid Tumors [NCT01529138] | Phase 1 | 13 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
| Pharmacodynamic Study Using FLT-PET/CT in Patients With Prostate and Other Solid Malignancies Treated With an Interrupted High-dose Axitinib Schedule [NCT01540526] | Phase 1 | 24 participants (Actual) | Interventional | 2012-03-31 | Completed | ||
| ProTarget - A Danish Nationwide Clinical Trial on Targeted Cancer Treatment Based on Genomic Profiling [NCT04341181] | Phase 2 | 300 participants (Anticipated) | Interventional | 2020-08-24 | Recruiting | ||
| Phase II Trial Evaluating Axitinib (AG-013736) In Patients With Unresectable, Recurrent Or Metastatic Head And Neck Cancer [NCT01469546] | Phase 2 | 42 participants (Actual) | Interventional | 2012-01-31 | Completed | ||
| Toripalimab Combined With Axitinib as Neoadjuvant Therapy for Advanced/Metastatic Non-clear Cell Renal Cell Carcinoma [NCT04385654] | Phase 2 | 40 participants (Anticipated) | Interventional | 2020-06-30 | Not yet recruiting | ||
| A Phase II Study of Axitinib (AG-013736) in Patients With Progressive, Recurrent/Metastatic Adenoid Cystic Carcinoma [NCT01558661] | Phase 2 | 33 participants (Actual) | Interventional | 2012-03-31 | Completed | ||
| Study on the Efficacy and Safety of KN046 Combined With Acitinib as a Neoadjuvant Therapy in Resectable Stage IB-IIIB Non-small Cell Lung Cancer (NSCLC) Patients [NCT06020352] | Phase 2/Phase 3 | 20 participants (Anticipated) | Interventional | 2023-08-25 | Recruiting | ||
| A Phase 2 Randomized, Double-Blind Study of Dalantercept and Axitinib Compared to Placebo and Axitinib in Patients With Advanced Renal Cell Carcinoma [NCT01727336] | Phase 2 | 160 participants (Actual) | Interventional | 2012-12-31 | Terminated(stopped due to The study was terminated by the sponsor following unblinding of the Progression Free Survival endpoint.) | ||
| Phase I Clinical Trial of Nasal Spray in Treating Patients With Recurrent Glioblastoma, Gliosarcoma, Glioma [NCT03275558] | Phase 1 | 0 participants (Actual) | Interventional | 2018-07-17 | Withdrawn(stopped due to Study halted prior to enrollment of first participant. (It has been determined on 2018 May 15 that the NCT03275558 study will be stopped by sponsor decision)) | ||
| A-PREDICT: A Phase II Study Of Axitinib In Metastatic Renal Cell Cancer in Patients Unsuitable for Nephrectomy [NCT01693822] | Phase 2 | 99 participants (Anticipated) | Interventional | 2012-10-31 | Active, not recruiting | ||
| A Real World Retrospective Database Study of Patients Diagnosed With Metastatic and/or Advanced Renal Cell Carcinoma and Treated With Sunitinib and/or Axitinib in a Specialist United Kingdom Oncology Centre [NCT04033991] | 684 participants (Actual) | Observational | 2019-09-27 | Completed | |||
| A Phase II Study of Axitinib in Advanced Carcinoid Tumors [NCT01435122] | Phase 2 | 30 participants (Actual) | Interventional | 2011-10-25 | Completed | ||
| Multicenter Phase II Study of Axitinib +/- Pembrolizumab in First Line Treatment for Patients With Locally Advanced or Metastatic Papillary Renal Cell Carcinoma (PRCC) [NCT05096390] | Phase 2 | 72 participants (Anticipated) | Interventional | 2022-01-25 | Recruiting | ||
| A Phase II Study of Axitinib in Metastatic Non-clear Cell Renal Cell Carcinoma Patients Previously Treated With Temsirolimus [NCT01798446] | Phase 2 | 41 participants (Actual) | Interventional | 2013-02-28 | Completed | ||
| A Single-arm, Single-center, Phase II Clinical Study to Investigate the Efficacy and Safety of JS001 Combined With Axitinib in the Treatment of Advanced Non-small Cell Lung Cancer (NSCLC) With Negative Driving Gene After First-line Chemotherapy [NCT04459663] | Phase 2 | 50 participants (Anticipated) | Interventional | 2020-08-31 | Not yet recruiting | ||
| NEXT: Subsequent Exposure to Tyrosine Kinase Inhibition (TKI) at Recurrence After Adjuvant Therapy in Renal Cell Carcinoma (RCC) [NCT01649180] | Phase 2 | 3 participants (Actual) | Interventional | 2012-07-31 | Terminated(stopped due to Closed due to prolonged enrollment timelines) | ||
| A Phase II Trial of Single Agent Axitinib as Maintenance Therapy for Patients With First Line Metastatic Colorectal Cancer (mCRC) [NCT01490866] | Phase 2 | 70 participants (Actual) | Interventional | 2012-01-31 | Completed | ||
| Phase I, Open-Label, Multicenter, Dose-Escalation Study Of The Tyrosine Kinase Inhibitor Of VEGFR-2, AG013736, In Patients With Advanced Solid Tumors [NCT01469052] | Phase 1 | 36 participants (Actual) | Interventional | 2002-11-30 | Completed | ||
| A Phase 1B, Open-Label, Dose Escalation Study To Evaluate Safety, Pharmacokinetics And Pharmacodynamics Of Crizotinib (PF-02341066) Plus VEGF Inhibitor Combinations In Patients With Advanced Solid Tumors. [NCT01441388] | Phase 1 | 0 participants (Actual) | Interventional | 2011-12-31 | Withdrawn(stopped due to Business/Operational issues) | ||
| Phase II Study of Axitinib (AG-013736) With Evaluation of the VEGF-Pathway in Metastatic, Recurrent or Primary Unresectable Adrenocortical Cancer [NCT01255137] | Phase 2 | 13 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
| Phase 2 Study of the Anti-Angiogenesis Agent Axitinib (AG-013736) in Patients With Stage III Malignant Melanoma [NCT01321437] | Phase 2 | 11 participants (Actual) | Interventional | 2011-12-31 | Completed | ||
| Multicenter Phase II Study of Axitinib in First Line Treatment for Patients With Locally Advanced or Metastatic Papillary Renal Cell Carcinoma (PRCC) [NCT02489695] | Phase 2 | 44 participants (Actual) | Interventional | 2015-10-31 | Completed | ||
| A Single-center, Non-randomized Controlled, Single-arm, Phase II Clinical Trial of Sintilimab in Combination With Axitinib in the Treatment of Advanced Renal Cell Carcinoma [NCT04958473] | Phase 2 | 40 participants (Anticipated) | Interventional | 2021-08-01 | Not yet recruiting | ||
| "PADRES (Prior Axitinib as a Determinant of Outcome of REnal Surgery)" [NCT03438708] | Phase 2 | 50 participants (Anticipated) | Interventional | 2018-03-05 | Recruiting | ||
| Optimizing Pembrolizumab Therapy With Timing and Intensification With Axitinib in Metastatic Renal Cell Cancer: A Response Adapted Study (OPTIMAX) [NCT05263609] | Phase 2 | 0 participants (Actual) | Interventional | 2022-06-30 | Withdrawn(stopped due to PI left University) | ||
| A PHASE 1B, OPEN-LABEL, DOSE-FINDING STUDY TO EVALUATE SAFETY, PHARMACOKINETICS AND PHARMACODYNAMICS OF AVELUMAB (MSB0010718C) IN COMBINATION WITH AXITINIB (AG-013736) IN PATIENTS WITH PREVIOUSLY UNTREATED ADVANCED RENAL CELL CANCER [NCT02493751] | Phase 1 | 55 participants (Actual) | Interventional | 2015-10-26 | Completed | ||
| A Randomized Phase 2 Trial of Axitinib and TRC105 Versus Axitinib Alone (Including a lead-in Phase 1B Dose Escalation Portion) in Patients With Advanced or Metastatic Renal Cell Carcinoma [NCT01806064] | Phase 1/Phase 2 | 173 participants (Actual) | Interventional | 2013-03-08 | Terminated(stopped due to The study did not meet endpoint.) | ||
| A Phase II Trial of Nivolumab Plus Axitinib in Patients With Anti-PD1 Refractory Advanced Melanoma [NCT04493203] | Phase 2 | 31 participants (Anticipated) | Interventional | 2020-12-18 | Recruiting | ||
| Phase II Expansion Trial Evaluating Axitinib in Patients With Unresectable Recurrent, or Metastatic Head and Neck Cancer Utilizing Choi Response Criteria Phase [NCT02762513] | Phase 2 | 29 participants (Actual) | Interventional | 2016-08-30 | Completed | ||
| Phase II Randomized Double Blind Trial of PF-04518600, an OX40 Antibody, in Combination With Axitinib Versus Axitinib in Immune-Checkpoint Inhibitor Exposed Patients With Metastatic Renal Cell Carcinoma [NCT03092856] | Phase 2 | 62 participants (Actual) | Interventional | 2017-07-19 | Active, not recruiting | ||
| Extension Study to Evaluate the Long-term Outcomes of Subjects Following CLS-AX Administration for Age-related Macular Degeneration in the CLS-AX CLS1002-101 Study [NCT05131646] | 15 participants (Actual) | Observational | 2021-10-08 | Completed | |||
| A Phase II Study of the Efficacy and Safety of Axitinib Given on an Individualized Schedule for Metastatic Renal Cell Cancer After Treatment With Pd-1 or Pd-L1 Inhibitors [NCT02579811] | Phase 2 | 40 participants (Actual) | Interventional | 2015-12-30 | Completed | ||
| A PHASE 1B, OPEN LABEL, DOSE ESCALATION STUDY TO EVALUATE SAFETY, PHARMACOKINETICS AND PHARMACODYNAMICS OF AXITINIB (AG-013736) IN COMBINATION WITH CRIZOTINIB (PF-02341066) IN PATIENTS WITH ADVANCED SOLID TUMORS [NCT01999972] | Phase 1 | 50 participants (Actual) | Interventional | 2014-02-26 | Completed | ||
| Safety and Efficacy Study of Oncolytic Virus（Intratumoral Injection）in Combination With HX-008（Intravenous Injection）and Axitinib in Melanoma Patients With Liver Metastasis Who Lack or Become Refractory to Standard Treatment [NCT05070221] | Phase 1 | 30 participants (Anticipated) | Interventional | 2021-10-01 | Not yet recruiting | ||
| A Phase II Double Blind, Randomised Controlled Trial of VEGF Inhibitor Axitinib Monotherapy With Early Dynamic Contrast Enhanced Ultrasound Monitoring in Chemorefractory Third Line Metastatic Colorectal Cancer [NCT04355156] | Phase 2 | 52 participants (Actual) | Interventional | 2012-09-17 | Completed | ||
| A Proof of Concept Study to Explore Safety and Efficacy of Tri-therapy Approach in Advanced/Metastatic NSCLC and Retrospectively Assess the Ability of Integrated Genomics and Transcriptomics to Match Patients to the Combination [NCT03386929] | Phase 1/Phase 2 | 15 participants (Actual) | Interventional | 2017-11-29 | Terminated(stopped due to The SPRING trial had to be early terminated at the end of the Phase 1 portion of the study due to the absence of funding necessary for the performance of the Phase 2.) | ||
| Phase II Study of Axitinib (AG-013736) With Evaluation of the VEGF-pathway in Metastatic, Recurrent or Primary Unresectable Pheochromocytoma/Paraganglioma [NCT03839498] | Phase 2 | 25 participants (Anticipated) | Interventional | 2019-01-22 | Recruiting | ||
| A Phase II Window Study of Front-line Axitinib Followed by Axitinib and Radiation for Elderly Patients With Glioblastoma Multiforme (GBM) [NCT01508117] | Phase 2 | 1 participants (Actual) | Interventional | 2011-08-31 | Terminated(stopped due to transferred study sponsor) | ||
| Phase II Study of Axitinib (AG-013736) With Evaluation of the VEGF-pathway in Metastatic, Recurrent or Primary Unresectable Pheochromocytoma/Paraganglioma [NCT01967576] | Phase 2 | 14 participants (Actual) | Interventional | 2013-10-19 | Completed | ||
| A PHASE II TRIAL OF PF-04856884 (CVX-060), A SELECTIVE ANGIOPOIETIN-2 (ANG-2) INHIBITOR IN COMBINATION WITH AG-013736 (AXITINIB) IN PATIENTS WITH PREVIOUSLY TREATED METASTATIC RENAL CELL CARCINOMA [NCT01441414] | Phase 2 | 18 participants (Actual) | Interventional | 2011-11-21 | Terminated(stopped due to See termination reason in detailed description.) | ||
| Adjuvant Axitinib Treatment of Renal Cancer: A Randomized Double-blind Phase 3 Study of Adjuvant Axitinib vs. Placebo in Subjects at High Risk of Recurrent RCC [NCT01599754] | Phase 3 | 724 participants (Actual) | Interventional | 2012-04-30 | Terminated(stopped due to Primary endpoint did not reach statistical significance) | ||
| A PHASE 1B, OPEN LABEL, DOSE FINDING STUDY TO EVALUATE SAFETY, PHARMACOKINETICS AND PHARMACODYNAMICS OF AXITINIB (AG-013736) IN COMBINATION WITH PEMBROLIZUMAB (MK-3475) IN PATIENTS WITH ADVANCED RENAL CELL CANCER [NCT02133742] | Phase 1 | 52 participants (Actual) | Interventional | 2014-09-16 | Completed | ||
| Safety, Tolerability and Efficacy of Vaginal Suppositories for Treatment of the Endometriosis [NCT03481842] | Phase 1/Phase 2 | 0 participants (Actual) | Interventional | 2021-10-10 | Withdrawn(stopped due to Change in study design and sponsor) | ||
| A Panel-Based Chart Review Study to Examine the Effects of Axitinib Dose Reduction and Interruption for Adverse Event Management Among Patients Receiving First-Line Axitinib in Combination With Immune-Oncology Drugs for the Treatment of Advanced Renal Cel [NCT04682587] | 481 participants (Actual) | Observational | 2021-02-24 | Completed | |||
| A Phase 1 Study to Compare Bempegaldesleukin Combined With Nivolumab and Tyrosine Kinase Inhibitor (TKI) to Nivolumab and TKI Alone in Participants With Previously Untreated Advanced or Metastatic Renal Cell Carcinoma (mRCC) (PIVOT IO 011) [NCT04540705] | Phase 1 | 30 participants (Actual) | Interventional | 2020-09-11 | Active, not recruiting | ||
| A Randomized Phase 2 Trial of Axitinib/Nivolumab Combination Therapy vs. Single Agent Nivolumab for the Treatment of TFE/Translocation Renal Cell Carcinoma (tRCC) Across All Age Groups [NCT03595124] | Phase 2 | 40 participants (Anticipated) | Interventional | 2019-01-08 | Active, not recruiting | ||
| Neoadjuvant AXITINIB and AVELUMAB for Patients With Localized Clear-cell RCC and a Moderate to High Risk [NCT03341845] | Phase 2 | 40 participants (Anticipated) | Interventional | 2018-03-28 | Recruiting | ||
| Single-arm Phase II Clinical Trial to Evaluate the Initial Efficacy and Safety of Sintilimab Injection Combined With Inlyta in Fumarate Hydratase- Deficient Renal Cell Carcinoma [NCT04387500] | Phase 2 | 41 participants (Anticipated) | Interventional | 2021-07-01 | Recruiting | ||
| Phase II Study of Axitinib in Patients With Neurofibromatosis Type 2 and Progressive Vestibular Schwannomas [NCT02129647] | Phase 2 | 13 participants (Actual) | Interventional | 2014-04-30 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||