| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| 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. |
| AID1677972 | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
| Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase. |
| 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. |
| AID1425112 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID1452945 | Antiproliferative activity against human 1205 Lu cells harboring BRAF V600E mutant after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, and identification of a novel napthalamide-isoselenocyanate compound NISC-6 as a dual Topoisomerase-IIα and Akt pathway inhibitor, and evaluation of its anti-melanoma activity. |
| AID1380308 | Inhibition of N-terminal His-tagged BRAF V600E mutant (unknown origin) expressed in baculovirus infected insect cells co-expressing CDC37 using biotinylated-MEK as substrate by AlphaScreen assay | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Current Insights of BRAF Inhibitors in Cancer. |
| 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. |
| AID1534639 | Inhibition of BRAF (unknown origin) | | | |
| 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. |
| AID1298902 | Cytotoxicity against human HCT116 cells harboring wild type B-Raf assessed as growth inhibition after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
| Design and synthesis of N-(4-aminopyridin-2-yl)amides as B-Raf(V600E) inhibitors. |
| 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. |
| 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. |
| AID1298019 | Inhibition of wild type B-Raf in human MIAPaCa2 cells assessed as induction of ERK phosphorylation preincubated for 1 hr by Western blot method relative to control | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
| Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling. |
| AID1534637 | Antiproliferative activity against human SW579 cells after 72 hrs by Cell-Titer Glo assay | | | |
| AID1298899 | Selectivity ratio of IC50 for recombinant wild type full length human GST-tagged B-Raf to IC50 for recombinant human N-terminal GST-tagged B-Raf V600E mutant | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
| Design and synthesis of N-(4-aminopyridin-2-yl)amides as B-Raf(V600E) inhibitors. |
| AID1753609 | Binding affinity to wild-type human partial length MAP4K5 (M1 to P297 residues) expressed in bacterial expression system assessed as residual binding level at 100 nM by Kinomescan method relative to control | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design and synthesis of 1H-pyrazolo[3,4-b]pyridines targeting mitogen-activated protein kinase kinase 4 (MKK4) - A promising target for liver regeneration. |
| 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. |
| AID1127859 | Cytotoxicity against human M238 cells expressing B-raf V600E mutant | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
| Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis. |
| AID1226865 | Inhibition of recombinant BRAF V600E mutant (unknown origin) assessed as ADP formation measured for 5 hrs by pyruvate kinase/lactate dehydrogenase coupled assay in presence of ATP, MEK1, NADH | 2015 | Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
| Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. |
| AID1226868 | Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay | 2015 | Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
| Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. |
| 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. |
| 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. |
| AID642947 | Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human A375 cells after 1 hr by fluorescence analysis | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
| Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors. |
| AID1588982 | Induction of apoptosis in human MCF7 cells assessed as late necrotic cells level at 4 uM incubated for 12 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 6.88%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| 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. |
| 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. |
| AID1186994 | Cytotoxicity against human HepG2 cells assessed as cell viability at 1 uM after 24 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
| Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
| 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. |
| 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. |
| 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. |
| AID1561559 | Binding affinity to DNA-tagged BRAF (unknown origin) by KINOMEscan assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Discovery of Selective Small Molecule Degraders of BRAF-V600E. |
| AID677926 | Inhibition of BRAF V600E mutant at 1 uM by ELISA | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Combining pharmacophore, docking and substructure search approaches to identify and optimize novel B-RafV600E inhibitors. |
| 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. |
| AID1316702 | Cytotoxicity against human 293T cells assessed as cell growth inhibition after 24 hrs by MTT assay | | | |
| AID1533157 | Inhibition of recombinant human full length GST-tagged BRAF expressed in baculovirus expression system | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
| Privileged Structures and Polypharmacology within and between Protein Families. |
| 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. |
| AID1298017 | Inhibition of B-Raf V600E mutant in human A375 cells assessed as ERK phosphorylation preincubated for 1 hr by Western blot method | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
| Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling. |
| 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. |
| 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. |
| AID1229274 | Antiproliferative activity against human SK-MEL-1 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5
| N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors. |
| AID701670 | Inhibition of B-Raf in presence of 100 uM ATP | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Conformation-specific effects of Raf kinase inhibitors. |
| 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. |
| AID1424938 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1396139 | Induction of N-terminal 6x-His-tagged BRAF V600E mutant (unknown origin) dimer formation expressed in baculovirus infected Sf9 insect cells co-expressing mouse p50cdc37 at 15 uM by sedimentation velocity method | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
| N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide (TAK632) Promotes Inhibition of BRAF through the Induction of Inhibited Dimers. |
| AID1588972 | Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells level at 4 uM incubated for 24 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 6.37%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| AID1755761 | Binding affinity to wild type full length human MKK7 (M1 to R419 residues) expressed in mammalian expression system assessed as residual activity at 100 nM measured by Kinomescan assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | From off-to on-target: New BRAF-inhibitor-template-derived compounds selectively targeting mitogen activated protein kinase kinase 4 (MKK4). |
| AID1549742 | Inhibition of B-raf (unknown origin) at 10 uM | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Synthesis of novel 7-azaindole derivatives containing pyridin-3-ylmethyl dithiocarbamate moiety as potent PKM2 activators and PKM2 nucleus translocation inhibitors. |
| AID1127862 | Cytotoxicity against human SK-MEL-28 cells expressing B-raf V600E mutant | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
| Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis. |
| AID1480961 | Antiproliferative activity human A375 cells after 72 hrs by cell titer-glo luminescence assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of derivatives based on pyrimidine scaffold as potent Pan-Raf inhibitors to overcome resistance. |
| 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. |
| AID1570014 | Inhibition of BRAF V600E in human A375 cells assessed as reduction in ERK phosphorylation incubated for 1 hr by immunoblot analysis | 2019 | ACS medicinal chemistry letters, Jul-11, Volume: 10, Issue:7
| Rigidification Dramatically Improves Inhibitor Selectivity for RAF Kinases. |
| 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. |
| AID1229277 | Antiproliferative activity against human NZM20 cells expressing B-Raf V600E mutant isolated from New Zealand metastatic melanoma patient incubated for 68 hrs by SRB assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5
| N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors. |
| AID1425064 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID1486184 | Inhibition of N-terminal GST-tagged recombinant human full-length ZAK expressed in baculovirus infected Sf9 insect cells using MBP as substrate after 30 mins by ADP-Glo assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors. |
| AID1393533 | Inhibition of BCR-ABL (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Effects of rigidity on the selectivity of protein kinase inhibitors. |
| AID701666 | Inhibition of C-Raf in presence of 100 uM ATP | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Conformation-specific effects of Raf kinase inhibitors. |
| 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. |
| AID1425021 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1588979 | Induction of apoptosis in human MCF7 cells assessed as viable cells level at 4 uM incubated for 12 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 89%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| AID1588967 | Induction of apoptosis in human MCF7 cells assessed as viable cells level at 2 uM incubated for 24 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 82%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| 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. |
| 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. |
| AID1452941 | Antiproliferative activity against human UACC-903 cells harboring BRAF V600E mutant after 24 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, and identification of a novel napthalamide-isoselenocyanate compound NISC-6 as a dual Topoisomerase-IIα and Akt pathway inhibitor, and evaluation of its anti-melanoma activity. |
| AID1452946 | Antiproliferative activity against human 1205 Lu cells harboring BRAF V600E mutant after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, and identification of a novel napthalamide-isoselenocyanate compound NISC-6 as a dual Topoisomerase-IIα and Akt pathway inhibitor, and evaluation of its anti-melanoma activity. |
| 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. |
| AID1445054 | Activation of CRAF in human Calu6 cells assessed as increase in MEK phosphorylation at 3 uM after 2 hrs by FRET assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers. |
| 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. |
| 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. |
| AID1452952 | Antiproliferative activity against human CHL-1 cells harboring wild type BRAF after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, and identification of a novel napthalamide-isoselenocyanate compound NISC-6 as a dual Topoisomerase-IIα and Akt pathway inhibitor, and evaluation of its anti-melanoma activity. |
| 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. |
| AID1755764 | Binding affinity to GST tagged mouse MKK4 expressed in Escherichia coli expression system measured by Kinomescan assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | From off-to on-target: New BRAF-inhibitor-template-derived compounds selectively targeting mitogen activated protein kinase kinase 4 (MKK4). |
| AID1226871 | Antiproliferative activity against human A375 cells after 72 hrs by resazurin assay | 2015 | Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
| Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. |
| AID1722370 | Inhibition of BRAF V600E mutant (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
| Modification of imidazothiazole derivatives gives promising activity in B-Raf kinase enzyme inhibition; synthesis, in vitro studies and molecular docking. |
| AID1588975 | Induction of apoptosis in human MCF7 cells assessed as viable cells level at 8 uM incubated for 24 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 82%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| 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. |
| 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. |
| 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. |
| AID1889297 | Aqueous solubility of the compound in FaSSIF at pH 6.5 measured by dissolution tester | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Dose Number as a Tool to Guide Lead Optimization for Orally Bioavailable Compounds in Drug Discovery. |
| AID1229270 | Antiproliferative activity against human SK-MEL-2 cells expressing wild type B-Raf incubated for 68 hrs by MTT assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5
| N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors. |
| AID1588970 | Induction of apoptosis in human MCF7 cells assessed as late necrotic cells level at 2 uM incubated for 24 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 1.49%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| 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. |
| AID642945 | Inhibition of full length human B-Raf V600E mutant expressed in baculovirus infected insect cells assessed as [gamma-33P]incorporation into MEK after 60 mins by scintillation counting | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
| Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors. |
| AID1425197 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1677971 | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) at 20uM using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
| Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase. |
| AID1416481 | Inhibition of B-Raf V600E mutant (unknown origin) at 10 uM using fluorescein-MAP2K1 as substrate after 1 hr by electrophoretic assay relative to control | 2017 | MedChemComm, Sep-01, Volume: 8, Issue:9
| Integrating docking scores and key interaction profiles to improve the accuracy of molecular docking: towards novel B-Raf |
| 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. |
| 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. |
| AID1720834 | Selectivity index, ratio for IC50 for human T75 cells to IC50 for human A2058 cells | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
| Structure-activity relationship study of cytotoxic neolignan derivatives using multivariate analysis and computation-aided drug design. |
| AID1845374 | Inhibition of human BRAF V600E mutant using MEK1 as substrate in presence of ATP | 2021 | Bioorganic & medicinal chemistry, 01-01, Volume: 29 | Evaluation of imidazo[2,1-b]thiazole-based anticancer agents in one decade (2011-2020): Current status and future prospects. |
| AID1588977 | Induction of apoptosis in human MCF7 cells assessed as late apoptotic cells level at 8 uM incubated for 24 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 10.1%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
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| The target landscape of clinical kinase drugs. |
| 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. |
| AID701674 | Antiproliferative activity against human HCT116 cells expressing wild type b-Raf and KRAS mutant | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Conformation-specific effects of Raf kinase inhibitors. |
| AID1662637 | Inhibition of BRAF (unknown origin) | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
| Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting |
| AID1706952 | Inhibition of colony formation of human VACO432 cells at 2 uM refreshed every 3 to 4 days by crystal violet staining based assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement. |
| AID1316701 | Antiproliferative activity against human WM1361 cells assessed as cell growth inhibition after 24 hrs by MTT assay | | | |
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| The target landscape of clinical kinase drugs. |
| AID1863530 | Binding affinity to BRAF (unknown origin) assessed as percent of control at 100 nM by Kinomescan method relative to control | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Scaffold modified Vemurafenib analogues as highly selective mitogen activated protein kinase kinase 4 (MKK4) inhibitors. |
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| The target landscape of clinical kinase drugs. |
| AID1425184 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1588989 | Induction of apoptosis in human MCF7 cells assessed as late apoptotic cells level at 4 uM incubated for 36 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 3.1%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| AID1405212 | Antitumor activity against human A375 cells xenografted in nude mouse assessed as tumor weight at 5 mg/kg, ip administered every second day for 14 days and measured on day 15 | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAF |
| 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. |
| 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. |
| 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. |
| AID1298018 | Selectivity index, ratio of EC50 for wild type B-Raf in human MIAPaCa2 cells to IC50 for B-Raf V600E mutant in human A375 cells | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
| Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling. |
| AID1753610 | Binding affinity to wild-type human partial length MKK4 (S84 to D399 residues) expressed in mammalian expression system assessed as residual binding level at 100 nM by Kinomescan method relative to control | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design and synthesis of 1H-pyrazolo[3,4-b]pyridines targeting mitogen-activated protein kinase kinase 4 (MKK4) - A promising target for liver regeneration. |
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| The target landscape of clinical kinase drugs. |
| AID1301359 | Antiproliferative activity against human WM266.4 cells assessed as cell viability after 24 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Design, biological evaluation and 3D QSAR studies of novel dioxin-containing triaryl pyrazoline derivatives as potential B-Raf inhibitors. |
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| The target landscape of clinical kinase drugs. |
| AID1424995 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID1405141 | Antiproliferative activity against human WM266.4 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAF |
| AID1823644 | Inhibition of Pan-Raf in human A-375 cells assessed as reduction in MEK phosphorylation at 5 uM measured after 24 hrs by immunoblot assay | 2021 | Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
| Discovery of New Imidazo[2,1- |
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| The target landscape of clinical kinase drugs. |
| AID1534636 | Antiproliferative activity against human HepG2 cells after 72 hrs by Cell-Titer Glo assay | | | |
| AID1276994 | Inhibition of wild-type B-Raf (unknown origin) using MEK1 K97M as substrate preincubated for 90 mins followed by substrate addition measured after 1 hr by fluorescence polarization assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Design and synthesis of new imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrazine derivatives with antiproliferative activity against melanoma cells. |
| AID1720832 | Cytotoxicity against human A2058 cells | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
| Structure-activity relationship study of cytotoxic neolignan derivatives using multivariate analysis and computation-aided drug design. |
| AID1405139 | Inhibition of recombinant human full length GST-tagged wild type BRAF expressed in baculovirus expression system using recombinant human full length N-terminal His-tagged MEK1 as substrate preincubated for 1 hr followed by substrate addition measured afte | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAF |
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| 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. |
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| The target landscape of clinical kinase drugs. |
| AID1280917 | Inhibition of B-Raf/C-Raf in human A549 cells assessed as effect on Her3 levels at five times IC50 value after 12 to 24 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Novobiocin Analogues That Inhibit the MAPK Pathway. |
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| The target landscape of clinical kinase drugs. |
| AID1425060 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1630167 | Cytotoxicity against vemurafenib-resistant human A375 R5C3 cells assessed as cell viability at 5 uM after 48 hrs by trypan blue exclusion assay relative to control | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery and Optimization of N-(4-(3-Aminophenyl)thiazol-2-yl)acetamide as a Novel Scaffold Active against Sensitive and Resistant Cancer Cells. |
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| 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. |
| 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. |
| AID1298898 | Inhibition of recombinant wild type full length human GST-tagged B-Raf expressed in baculovirus expression system using Z'-LYTE Ser/Thr3 peptide as substrate incubated for 1 hr by FRET-based Z'-LYTE assay | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
| Design and synthesis of N-(4-aminopyridin-2-yl)amides as B-Raf(V600E) inhibitors. |
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| The target landscape of clinical kinase drugs. |
| AID1128934 | Antiproliferative activity against vemurafenib-resistant human SK-MEL-28-PR30 cells harboring BRAF V600E mutant and EGFR after 68 hrs by MTS assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib. |
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| The target landscape of clinical kinase drugs. |
| AID1535428 | Inhibition of B-Raf (unknown origin) | 2019 | Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
| The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton. |
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| The target landscape of clinical kinase drugs. |
| 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. |
| AID1186996 | Cytotoxicity against human HepG2 cells assessed as cell viability at 100 uM after 24 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
| Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
| AID701672 | Antitumor activity against B-Raf V600E mutation harboring metastatic melanoma cells in human | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Conformation-specific effects of Raf kinase inhibitors. |
| AID1569154 | Cytotoxicity against human A375 cells harboring BRAF V600E mutant assessed as reduction in cell viability at 10 uM incubated for 24 hrs by MTS assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Light-controlled inhibition of BRAFV600E kinase. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
| 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. |
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| The target landscape of clinical kinase drugs. |
| AID749995 | Inhibition of BRAF V600E mutant (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| Synthetic approaches to the 2011 new drugs. |
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| The target landscape of clinical kinase drugs. |
| AID1226872 | Antiproliferative activity against human HCT116 cells after 67 hrs by resazurin assay | 2015 | Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
| Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. |
| AID1128954 | Inhibition of MAPK-mediated ERK phosphorylation at Thr202/Tyr204 in human SK-MEL-28-PR30 cells at 1 uM after 48 hrs by Western blotting analysis | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib. |
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| The target landscape of clinical kinase drugs. |
| AID1755760 | Binding affinity to GST tagged mouse MKK4 expressed in Escherichia coli expression system assessed as residual activity at 100 nM measured by Kinomescan assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | From off-to on-target: New BRAF-inhibitor-template-derived compounds selectively targeting mitogen activated protein kinase kinase 4 (MKK4). |
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| The target landscape of clinical kinase drugs. |
| AID1588968 | Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells level at 2 uM incubated for 24 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 6.37%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| AID1869917 | Antitumor activity against human A-375 cells implanted in BALB/c mouse assessed as suppression of tumor growth at 20 mg/kg, ip measured once every two days for 14 days | | | |
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| The target landscape of clinical kinase drugs. |
| AID1588974 | Induction of apoptosis in human MCF7 cells assessed as late necrotic cells level at 4 uM incubated for 24 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 1.49%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| AID1393534 | Inhibition of BRAF V600E mutant in human A375 cells assessed as reduction in cell proliferation incubated for 96 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Effects of rigidity on the selectivity of protein kinase inhibitors. |
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| The target landscape of clinical kinase drugs. |
| AID1229272 | Antiproliferative activity against human NZM40 cells expressing wild type B-Raf isolated from New Zealand metastatic melanoma patient incubated for 68 hrs by SRB assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5
| N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors. |
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| 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. |
| AID1452942 | Antiproliferative activity against human UACC-903 cells harboring BRAF V600E mutant after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, and identification of a novel napthalamide-isoselenocyanate compound NISC-6 as a dual Topoisomerase-IIα and Akt pathway inhibitor, and evaluation of its anti-melanoma activity. |
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| The target landscape of clinical kinase drugs. |
| AID1425086 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID1174654 | Antiproliferative activity against human A375 cells after 72 hrs by CCK8 assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Design, synthesis and biological evaluation of bis-aryl ureas and amides based on 2-amino-3-purinylpyridine scaffold as DFG-out B-Raf kinase inhibitors. |
| AID1588973 | Induction of apoptosis in human MCF7 cells assessed as late apoptotic cells level at 4 uM incubated for 24 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 10.1%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1128931 | Inhibition of BRAF V600E mutant (unknown origin) after 1 to 1.5 hrs by FRET-based Z'-Lyte assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1549740 | Cytotoxicity against mouse C2C12 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Synthesis of novel 7-azaindole derivatives containing pyridin-3-ylmethyl dithiocarbamate moiety as potent PKM2 activators and PKM2 nucleus translocation inhibitors. |
| AID1486185 | Inhibition of recombinant human B-RAF V600E mutant using Ser/Thr3 as substrate after 1 hr by FRET-based Z'-Lyte assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1298014 | Inhibition of wild type B-Raf (unknown origin) assessed as MEK1 phosphorylation using MEK1-Avitag as substrate after 1 hr by HTRF assay | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
| Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling. |
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| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1226870 | Inhibition of KDR (unknown origin) | 2015 | Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
| Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. |
| AID1869925 | Antitumor activity against human A-375 cells implanted in BALB/c mouse assessed as shrinkage of tumor tissue at 20 mg/kg, ip measured once every two days for 14 days | | | |
| AID1569161 | Inhibition of human recombinant BRAF V600E mutant using MEK1 as substrate measured after 1 hr by Western blot analysis | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Light-controlled inhibition of BRAFV600E kinase. |
| AID1570011 | Inhibition of CRAF (unknown origin) at 1 uM relative to control | 2019 | ACS medicinal chemistry letters, Jul-11, Volume: 10, Issue:7
| Rigidification Dramatically Improves Inhibitor Selectivity for RAF Kinases. |
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| The target landscape of clinical kinase drugs. |
| AID1424944 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| 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. |
| AID1588984 | Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells level at 4 uM incubated for 24 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 1.06%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| 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. |
| AID1480963 | Antiproliferative activity human HepG2 cells after 72 hrs by cell titer-glo luminescence assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of derivatives based on pyrimidine scaffold as potent Pan-Raf inhibitors to overcome resistance. |
| AID1480955 | Antiproliferative activity human COLO205 cells after 72 hrs by cell titer-glo luminescence assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of derivatives based on pyrimidine scaffold as potent Pan-Raf inhibitors to overcome resistance. |
| AID1533155 | Displacement of 6-amino-9-(2-((4-((2-((6-((5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-methylphenyl)carbamoyl)quinolin-2-yl)oxy)ethyl)amino)-4-oxobutyl)(methyl)carbamoyl)phenyl)-3-imino-3H-xanthene-4,5-disulfonic acid from pirin (unknown origin) b | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
| Privileged Structures and Polypharmacology within and between Protein Families. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1630170 | Cytotoxicity against vemurafenib-resistant human A375 RIV cells assessed as cell viability at 5 uM after 48 hrs by trypan blue exclusion assay relative to control | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery and Optimization of N-(4-(3-Aminophenyl)thiazol-2-yl)acetamide as a Novel Scaffold Active against Sensitive and Resistant Cancer Cells. |
| AID1229271 | Antiproliferative activity against human NZM09 cells expressing wild type B-Raf isolated from New Zealand metastatic melanoma patient incubated for 68 hrs by SRB assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5
| N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors. |
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| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1127857 | Cytotoxicity against human M14 cells expressing NRAS G12C mutant | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
| Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis. |
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| 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. |
| 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. |
| AID1247129 | Inhibition of wild type C-RAF (unknown origin) | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Recent progress on MAP kinase pathway inhibitors. |
| AID1561574 | Cytotoxicity in human A375 cells assessed as reduction in cell viability by Cell-titer-Lumi assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Discovery of Selective Small Molecule Degraders of BRAF-V600E. |
| AID1416480 | Inhibition of B-Raf V600E mutant (unknown origin) using fluorescein-MAP2K1 as substrate after 1 hr by electrophoretic assay | 2017 | MedChemComm, Sep-01, Volume: 8, Issue:9
| Integrating docking scores and key interaction profiles to improve the accuracy of molecular docking: towards novel B-Raf |
| AID1317115 | Antiproliferative activity against human SK-MEL-28 cells harboring BRAF V600E mutant assessed as concentration required for total growth inhibition measured after 48 hrs resazurin assay | 2016 | ACS medicinal chemistry letters, Oct-13, Volume: 7, Issue:10
| Photoinduced Conversion of Antimelanoma Agent Dabrafenib to a Novel Fluorescent BRAF |
| AID1316699 | Antiproliferative activity against human A375 cells assessed as cell growth inhibition after 24 hrs by MTT assay | | | |
| 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. |
| 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. |
| 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. |
| AID1226912 | Competitive binding affinity to CRAF in human A375 cells after 15 mins in presence of ATP analogue | 2015 | Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
| Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. |
| AID1425213 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID1534635 | Antiproliferative activity against human MV4-11 cells after 72 hrs by Cell-Titer Glo assay | | | |
| 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. |
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| 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. |
| 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. |
| AID1393537 | Inhibition of BRAF V600E mutant in human A375 cells assessed as decrease in ERK phosphorylation at > 1 uM after 1 hr by immunoblotting assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Effects of rigidity on the selectivity of protein kinase inhibitors. |
| 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. |
| AID1226867 | Inhibition of wild type CRAF (unknown origin) assessed as ADP formation measured for 5 hrs by pyruvate kinase/lactate dehydrogenase coupled assay in presence of ATP, MEK1, PEP, NADH | 2015 | Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
| Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. |
| AID1298016 | Inhibition of wild type B-Raf in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation preincubated for 1 hr by Western blot method | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
| Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling. |
| AID1425041 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1424917 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1677973 | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with high 200 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
| Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase. |
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| The target landscape of clinical kinase drugs. |
| AID1128953 | Inhibition of MAPK-mediated ERK phosphorylation at Thr202/Tyr204 in human SK-MEL-28-PR30 cells at 1 uM after 24 hrs by Western blotting analysis | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib. |
| AID1055888 | Cytotoxicity against human A375 cells after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, , Volume: 70 | Overman rearrangement and Pomeranz-Fritsch reaction for the synthesis of benzoazepinoisoquinolones to discover novel antitumor agents. |
| AID1480962 | Antiproliferative activity human SK-MEL-2 cells after 72 hrs by cell titer-glo luminescence assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of derivatives based on pyrimidine scaffold as potent Pan-Raf inhibitors to overcome resistance. |
| AID1226866 | Inhibition of wild type BRAF (unknown origin) assessed as ADP formation measured for 5 hrs by pyruvate kinase/lactate dehydrogenase coupled assay in presence of ATP, MEK1, NADH | 2015 | Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
| Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. |
| AID1588990 | Induction of apoptosis in human MCF7 cells assessed as late necrotic cells level at 4 uM incubated for 36 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 6.88%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| AID1393536 | Inhibition of BRAF V600E mutant in human A375 cells assessed as decrease in MEK phosphorylation at > 1 uM after 1 hr by immunoblotting assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Effects of rigidity on the selectivity of protein kinase inhibitors. |
| AID1445096 | Stimulation of BRAF-CRAF dimerization in human HCT116 cells by luciferase complementation assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers. |
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| Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
| AID1630164 | Cytotoxicity against vemurafenib-sensitive human A375 cells assessed as cell viability at 5 uM after 48 hrs by trypan blue exclusion assay relative to control | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery and Optimization of N-(4-(3-Aminophenyl)thiazol-2-yl)acetamide as a Novel Scaffold Active against Sensitive and Resistant Cancer Cells. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
| AID1588987 | Induction of apoptosis in human MCF7 cells assessed as viable cells level at 4 uM incubated for 36 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 89%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. |
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| The target landscape of clinical kinase drugs. |
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| Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling. |
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| The target landscape of clinical kinase drugs. |
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| Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| Discovery of New Imidazo[2,1- |
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| The target landscape of clinical kinase drugs. |
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| N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| Rigidification Dramatically Improves Inhibitor Selectivity for RAF Kinases. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
| AID1588976 | Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells level at 8 uM incubated for 24 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 6.37%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
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| The target landscape of clinical kinase drugs. |
| AID1166975 | Antiproliferative activity against human A375 cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
| Design, synthesis and biological evaluation of novel 5-phenyl-1H-pyrazole derivatives as potential BRAF(V600E) inhibitors. |
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| The target landscape of clinical kinase drugs. |
| AID1570010 | Inhibition of BRAF (unknown origin) at 1 uM relative to control | 2019 | ACS medicinal chemistry letters, Jul-11, Volume: 10, Issue:7
| Rigidification Dramatically Improves Inhibitor Selectivity for RAF Kinases. |
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| The target landscape of clinical kinase drugs. |
| AID1276995 | Inhibition of B-Raf V600E mutant (unknown origin) using MEK1 K97M as substrate preincubated for 90 mins followed by substrate addition measured after 1 hr by fluorescence polarization assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Design and synthesis of new imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrazine derivatives with antiproliferative activity against melanoma cells. |
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| Small molecule inhibitors of BRAF in clinical trials. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen. |
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| 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. |
| AID1316700 | Antiproliferative activity against human WM266.4 cells harboring BRAF V600E mutant assessed as cell growth inhibition after 24 hrs by MTT assay | | | |
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| The target landscape of clinical kinase drugs. |
| AID1452944 | Antiproliferative activity against human 1205 Lu cells harboring BRAF V600E mutant after 24 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, and identification of a novel napthalamide-isoselenocyanate compound NISC-6 as a dual Topoisomerase-IIα and Akt pathway inhibitor, and evaluation of its anti-melanoma activity. |
| AID1677975 | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using high 10 uM hFX-CP as substrate mixture with 10 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
| Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase. |
| AID1494019 | Cytotoxicity against human UACC-903 cells assessed as cell viability at 25 uM after 48 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design and synthesis of novel thiobarbituric acid derivatives targeting both wild-type and BRAF-mutated melanoma cells. |
| AID1405140 | Antiproliferative activity against human A375 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAF |
| AID1588969 | Induction of apoptosis in human MCF7 cells assessed as late apoptotic cells level at 2 uM incubated for 24 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 10.1%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| 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. |
| 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. |
| AID1534632 | Antiproliferative activity against human A375 cells after 72 hrs by Cell-Titer Glo assay | | | |
| 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. |
| AID1753611 | Binding affinity to wild-type human full length MKK7 (M1 to R419 residues) expressed in mammalian expression system assessed as residual binding level at 100 nM by Kinomescan method relative to control | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design and synthesis of 1H-pyrazolo[3,4-b]pyridines targeting mitogen-activated protein kinase kinase 4 (MKK4) - A promising target for liver regeneration. |
| AID1863532 | Binding affinity to MKK4 (unknown origin) assessed as percent of control at 100 nM by Kinomescan method relative to control | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Scaffold modified Vemurafenib analogues as highly selective mitogen activated protein kinase kinase 4 (MKK4) inhibitors. |
| 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. |
| AID1494018 | Antiproliferative activity against human CHL-1 cells harboring wild type BRAF after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design and synthesis of novel thiobarbituric acid derivatives targeting both wild-type and BRAF-mutated melanoma cells. |
| AID1534640 | Inhibition of cRAF (unknown origin) | | | |
| 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. |
| AID1276993 | Antiproliferative activity against human A375P cells expressing BRAF V600E mutant after 72 hrs by CellTiter-Glo assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Design and synthesis of new imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrazine derivatives with antiproliferative activity against melanoma cells. |
| AID1174655 | Inhibition of B-raf V600E mutant in human A375 cells assessed as reduction in ERK1/2 phosphorylation incubated for 90 mins by Western blotting method | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | Design, synthesis and biological evaluation of bis-aryl ureas and amides based on 2-amino-3-purinylpyridine scaffold as DFG-out B-Raf kinase inhibitors. |
| AID1186991 | Cytotoxicity against human HepG2 cells assessed as cell viability at 1 uM after 4 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
| Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
| 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. |
| AID701676 | Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Conformation-specific effects of Raf kinase inhibitors. |
| 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. |
| AID1127863 | Cytotoxicity against human M263 cells expressing B-raf V600E mutant | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
| Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis. |
| 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. |
| 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. |
| AID1755763 | Binding affinity to wild type partial length human ZAK (M1 to L331) expressed in bacterial expression system assessed as residual activity at 100 nM measured by Kinomescan assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | From off-to on-target: New BRAF-inhibitor-template-derived compounds selectively targeting mitogen activated protein kinase kinase 4 (MKK4). |
| AID1317118 | Growth inhibition of human SK-MEL-28 cells harboring BRAF V600E mutant preincubated for 1 hr followed by irradiation of 1.13 kW/m2 UV-light for 5 mins measured after 48 hrs resazurin assay | 2016 | ACS medicinal chemistry letters, Oct-13, Volume: 7, Issue:10
| Photoinduced Conversion of Antimelanoma Agent Dabrafenib to a Novel Fluorescent BRAF |
| AID1229267 | Antiproliferative activity against human COLO205 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5
| N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1186993 | Cytotoxicity against human HepG2 cells assessed as cell viability at 100 uM after 4 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
| Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
| 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. |
| AID1534634 | Antiproliferative activity against human HT-29 cells after 72 hrs by Cell-Titer Glo assay | | | |
| AID1486220 | Inhibition of human ZAK (5 to 309 residues) expressed in baculovirus infected Sf9 insect cells using ZAKtide as substrate after 1 hr by mass spectrometry | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors. |
| AID1561575 | Cytotoxicity in human HT-29 cells assessed as reduction in cell viability by Cell-titer-Lumi assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Discovery of Selective Small Molecule Degraders of BRAF-V600E. |
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| The target landscape of clinical kinase drugs. |
| AID1707081 | Antiproliferative activity against human HT-29 cells incubated for 3 days by WST8 assay | | | |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1452947 | Antiproliferative activity against human A375M cells harboring BRAF V600E mutant after 24 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, and identification of a novel napthalamide-isoselenocyanate compound NISC-6 as a dual Topoisomerase-IIα and Akt pathway inhibitor, and evaluation of its anti-melanoma activity. |
| AID749994 | Inhibition of wild type BRAF (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| Synthetic approaches to the 2011 new drugs. |
| AID1229269 | Antiproliferative activity against human LoVo cells expressing wild type B-Raf incubated for 68 hrs by MTT assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5
| N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors. |
| 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. |
| AID1396129 | Induction of N-terminal 6x-His-tagged BRAF (unknown origin) dimer formation expressed in baculovirus infected Sf9 insect cells co-expressing mouse p50cdc37 at 200 uM measured after trypsin digestion for 30 mins by coomassie blue staining-based SDS-PAGE me | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
| N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide (TAK632) Promotes Inhibition of BRAF through the Induction of Inhibited Dimers. |
| AID1588980 | Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells level at 4 uM incubated for 12 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 1.06%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| AID1128932 | Inhibition of EGFR (unknown origin) after 1 to 1.5 hrs by FRET-based Z'-Lyte assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib. |
| AID1534638 | Inhibition of ARaf (unknown origin) | | | |
| 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. |
| AID1452943 | Antiproliferative activity against human UACC-903 cells harboring BRAF V600E mutant after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, and identification of a novel napthalamide-isoselenocyanate compound NISC-6 as a dual Topoisomerase-IIα and Akt pathway inhibitor, and evaluation of its anti-melanoma activity. |
| 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. |
| AID642946 | Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human MALME-3M cells after 1 hr by fluorescence analysis | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
| Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors. |
| 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. |
| 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. |
| 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. |
| AID1588988 | Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells level at 4 uM incubated for 36 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 1.06%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| 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. |
| AID1823650 | Antitumor activity against human A-375 cells xenografted in BALB/c nude mouse assessed as tumor weight at 50 mg/kg/day, ip administered for 21 days (Rvb = 3.15g) | 2021 | Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
| Discovery of New Imidazo[2,1- |
| AID1486186 | Inhibition of wild type GST-tagged recombinant human full-length B-RAF expressed in baculovirus expression system using Ser/Thr3 as substrate after 1 hr by FRET-based Z'-Lyte assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
| Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors. |
| AID1226962 | Paradoxical activation of RAS/RAF/MEK signaling pathway in human HCT116 cells expressing wild type BRAF assessed as ERK phosphorylation at 0.34 to 20000 nM | 2015 | Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
| Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. |
| 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. |
| AID1127858 | Cytotoxicity against human M262 cells expressing B-raf V600E mutant | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
| Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis. |
| 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. |
| 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. |
| AID677925 | Inhibition of BRAF V600E mutant at 10 uM by ELISA | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Combining pharmacophore, docking and substructure search approaches to identify and optimize novel B-RafV600E inhibitors. |
| AID1534633 | Antiproliferative activity against human SK-MEL-2 cells after 72 hrs by Cell-Titer Glo assay | | | |
| AID1588983 | Induction of apoptosis in human MCF7 cells assessed as viable cells level at 4 uM incubated for 24 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 89%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| 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. |
| AID1280929 | Effect on B-Raf level in human A549 cells at five times IC50 value after 12 to 24 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Novobiocin Analogues That Inhibit the MAPK Pathway. |
| AID1229275 | Antiproliferative activity against human SK-MEL-28 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5
| N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors. |
| AID1298013 | Selectivity index, ratio of IC50 for wild type B-Raf (unknown origin) to IC50 for B-Raf V600E mutant (unknown origin) | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
| Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling. |
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| The target landscape of clinical kinase drugs. |
| AID1405143 | Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAF |
| 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. |
| AID1226873 | Inhibition of MEK (unknown origin) | 2015 | Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
| Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. |
| AID1424982 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1128933 | Antiproliferative activity against human SK-MEL-28 cells harboring BRAF V600E mutant after 68 hrs by MTS assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib. |
| 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. |
| AID1755759 | Binding affinity to wild type partial length human MAP4K5 (M1 to P297) expressed in Bacterial expression system assessed as residual activity at 100 nM measured by Kinomescan assay relative to control | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | From off-to on-target: New BRAF-inhibitor-template-derived compounds selectively targeting mitogen activated protein kinase kinase 4 (MKK4). |
| 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. |
| AID1229278 | Antiproliferative activity against human NZM07 cells expressing B-Raf V600E mutant isolated from New Zealand metastatic melanoma patient incubated for 68 hrs by SRB assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5
| N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors. |
| 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. |
| 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. |
| AID1405138 | Inhibition of mouse full length GST-tagged BRAF V600E mutant using recombinant human full length N-terminal His-tagged MEK1 as substrate preincubated for 1 hr followed by substrate addition measured after 25 mins | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAF |
| 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. |
| AID1166974 | Antiproliferative activity against human WM266.4 cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| Novel pyrazoline derivatives as bi-inhibitor of COX-2 and B-Raf in treating cervical carcinoma. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| Privileged Structures and Polypharmacology within and between Protein Families. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
| AID1588971 | Induction of apoptosis in human MCF7 cells assessed as viable cells level at 4 uM incubated for 24 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 82%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| Design and synthesis of N-(4-aminopyridin-2-yl)amides as B-Raf(V600E) inhibitors. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
| AID1677974 | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and high 20 uM FAS incubated for 35 mins by MS analysis | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
| Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
| AID1380311 | Cytotoxicity against human SK-MEL-32 cells | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Current Insights of BRAF Inhibitors in Cancer. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
| AID1706959 | Inhibition of ERK phosphorylation in human VACO432 cells at 2 uM incubated for 24 to 48 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
| AID1823652 | Antitumor activity against human A-375 cells xenografted in BALB/c nude mouse assessed as tumor size at 50 mg/kg/day, ip administered for 21 days (Rvb = 400 mm3) | 2021 | Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
| Discovery of New Imidazo[2,1- |
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| The target landscape of clinical kinase drugs. |
| AID1226910 | Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogue | 2015 | Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
| Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| Non-kinase targets of protein kinase inhibitors. |
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| Combining pharmacophore, docking and substructure search approaches to identify and optimize novel B-RafV600E inhibitors. |
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| The target landscape of clinical kinase drugs. |
| AID1425157 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1229266 | Inhibition of human recombinant B-Raf V600E mutant by FRET-based Z'-lyte assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5
| N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
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| The target landscape of clinical kinase drugs. |
| AID1424946 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1316698 | Inhibition of human recombinant GST-tagged BRAF catalytic domain (416 to 766 residues) V600E mutant expressed in baculovirus expression system preincubated for 1 hr followed by human full length recombinant N-terminal His-tagged MEK1 substrate addition me | | | |
| 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. |
| AID1380310 | Inhibition of BRAF V600E mutant in human A375 cells assessed as reduction in ERK phosphorylation by AlphaScreen assay | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
| Current Insights of BRAF Inhibitors in Cancer. |
| AID1424920 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1588981 | Induction of apoptosis in human MCF7 cells assessed as late apoptotic cells level at 4 uM incubated for 12 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 3.1%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| AID1889303 | Permeability in human Caco-2 cells | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Dose Number as a Tool to Guide Lead Optimization for Orally Bioavailable Compounds in Drug Discovery. |
| 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. |
| 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. |
| 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. |
| AID1720833 | Cytotoxicity against human T75 cells | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
| Structure-activity relationship study of cytotoxic neolignan derivatives using multivariate analysis and computation-aided drug design. |
| 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. |
| 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. |
| AID1753607 | Binding affinity to wild-type human partial length BRAF (S429 to E741 residues) expressed in mammalian expression system assessed as residual binding level at 100 nM by Kinomescan method relative to control | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Design and synthesis of 1H-pyrazolo[3,4-b]pyridines targeting mitogen-activated protein kinase kinase 4 (MKK4) - A promising target for liver regeneration. |
| AID1337182 | Stabilization of FECH in human K562 cells after 1 hr by thermal shift assay | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6
| Non-kinase targets of protein kinase inhibitors. |
| 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. |
| AID1393531 | Inhibition of ABL (unknown origin) by phosphocellulose paper disk assay | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Effects of rigidity on the selectivity of protein kinase inhibitors. |
| AID1588978 | Induction of apoptosis in human MCF7 cells assessed as late necrotic cells level at 8 uM incubated for 24 hrs by Annexin V-FITC/PI double staining based flow cytometry analysis (Rvb = 1.49%) | 2019 | Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
| Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors. |
| 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. |
| 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. |
| 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. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| 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. |
| AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| 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. |
| AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
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| Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors. |
| AID1345813 | Human Raf-1 proto-oncogene, serine/threonine kinase (RAF family) | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Conformation-specific effects of Raf kinase inhibitors. |
| AID1345687 | Human B-Raf proto-oncogene, serine/threonine kinase (RAF family) | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Conformation-specific effects of Raf kinase inhibitors. |
| AID1345813 | Human Raf-1 proto-oncogene, serine/threonine kinase (RAF family) | 2015 | Cancer cell, Sep-14, Volume: 28, Issue:3
| Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2010 | Nature, Sep-30, Volume: 467, Issue:7315
| Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |