| 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. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
| Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | | | |
| 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. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| 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. |
| 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. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
| Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1646075 | Inhibition of human JNK2 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID625025 | Binding constant for MAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256633 | Average Binding Constant for PRKACA; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435393 | Binding constant for CAMK1D kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624773 | Binding constant for AMPK-alpha1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624926 | Binding constant for RIOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID673353 | Hepatotoxicity in Crlj:CD1(ICR) mouse assessed as change in plasma total bilirubin level at 500 to 1000 mg/kg, po administered for 5 consecutive days measured 24 hrs post final dosing | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
| Design and synthesis of novel p38α MAP kinase inhibitors: discovery of pyrazole-benzyl ureas bearing 2-molpholinopyrimidine moiety. |
| AID256616 | Average Binding Constant for CDK5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID256578 | Average Binding Constant for SLK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435523 | Binding constant for CIT kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435442 | Binding constant for SYK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435907 | Binding constant for EGFR(L861Q) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625075 | Binding constant for INSRR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636911 | Inhibition of AKT3 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624985 | Binding constant for ABL1(M351T)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID436010 | Binding constant for full-length CDK5 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624957 | Binding constant for EPHB6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435290 | Binding constant for FGFR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624855 | Binding constant for FRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435320 | Binding constant for PRKCE kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435398 | Binding constant for DAPK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625063 | Binding constant for PLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624872 | Binding constant for PAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624911 | Binding constant for TXK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625082 | Binding constant for RSK4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256561 | Average Binding Constant for BTK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435692 | Binding constant for STK16 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625036 | Binding constant for PIK3CA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625113 | Binding constant for MARK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1141134 | Binding affinity to human acrylodan-labeled N-terminal His-tagged DDR2 (558 to 855 aa) by FLiK assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Identification of type II and III DDR2 inhibitors. |
| AID636918 | Inhibition of BLK | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624834 | Binding constant for DAPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256587 | Average Binding Constant for ACK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID339965 | Inhibition of human JNK3 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
| AID215434 | Tested for inhibition of Tumor necrosis factor, alpha in THP cells | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). |
| AID624770 | Binding constant for CAMK2D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1451486 | Binding affinity to wild type human biotin labelled p38 alpha (9 to 352 residues) expressed in sf21 insect cells assessed as dissociation half life by SPR analysis | | | |
| AID435169 | Binding constant for full-length MEK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636432 | Inhibition of ERK2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624922 | Binding constant for CAMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624977 | Binding constant for OSR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435190 | Binding constant for full-length PIP5K1A | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624987 | Binding constant for ABL1(Q252H)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624943 | Binding constant for ACVR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624735 | Binding constant for ANKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435439 | Binding constant for PAK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435188 | Binding constant for PAK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624788 | Binding constant for KIT(D816H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435153 | Binding constant for full-length DAPK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625017 | Binding constant for TIE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624853 | Binding constant for FLT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID341052 | Inhibition of p38alpha phosphorylation in IL-1-alpha-stimulated HLF cells | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID624960 | Binding constant for RSK2(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624897 | Binding constant for RAF1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1451483 | Binding affinity to wild type biotin labelled human p38 alpha (9 to 352 residues) expressed in sf21 insect cells assessed as association rate constant by SPR analysis | | | |
| AID341207 | Inhibition of SLK | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID624864 | Binding constant for CTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435552 | Binding constant for PIK3CA(E545K) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435556 | Binding constant for RAF1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435157 | Binding constant for EGFR(G719C) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID513132 | Inhibition of p38V kinase stie 3 delta 296-301 mutant | 2006 | Nature chemical biology, Jul, Volume: 2, Issue:7
| Rational design of inhibitors that bind to inactive kinase conformations. |
| AID624854 | Binding constant for FLT4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636455 | Inhibition of IRAK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624847 | Binding constant for CSNK1E kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256660 | Average Binding Constant for KIT; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625051 | Binding constant for PRKCQ kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435659 | Binding constant for full-length MARK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435441 | Binding constant for RPS6KA4(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256589 | Average Binding Constant for EPHA4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435545 | Binding constant for NEK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID296934 | Bioavailability in Sprague-Dawley rat at 10 mg/kg, po | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| Discovery and optimization of p38 inhibitors via computer-assisted drug design. |
| AID24441 | Partition coefficient (logP) | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). |
| AID435834 | Binding constant for YANK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625101 | Binding constant for TAOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID127260 | Binding affinity for Mitogen-activated protein kinase p38 alpha | 2003 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 13, Issue:18
| The kinetics of binding to p38MAP kinase by analogues of BIRB 796. |
| AID435788 | Binding constant for CLK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435906 | Binding constant for EGFR(L747-T751del,Sins) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1646079 | Inhibition of human MRCKbeta | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID625053 | Binding constant for PRKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624925 | Binding constant for RIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624865 | Binding constant for MAP3K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435195 | Binding constant for SRC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624979 | Binding constant for ABL1(F317I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435667 | Binding constant for full-length NLK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435256 | Percentage p38-gamma MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID625027 | Binding constant for MAP3K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1706574 | Inhibition of EPHA2 (unknown origin) assessed as change in melting temperature at 10 uM by DSF assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Selective targeting of the αC and DFG-out pocket in p38 MAPK. |
| AID435821 | Binding constant for GAK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624761 | Binding constant for CDC2L5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624824 | Binding constant for PIP5K1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256592 | Average Binding Constant for LIMK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625020 | Binding constant for ITK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID308410 | Inhibition of LPS-induced TNFalpha production in THP1 cells | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site. |
| AID1286659 | Inhibition of CYP2C19 (unknown origin) at 30 uM | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma. |
| AID436049 | Binding constant for PTK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435154 | Binding constant for DDR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID701485 | Antiinflammatory activity in po dosed rat assessed as inhibition of LPS-induced TNFalpha production administered 4 hrs prior to LPS-challenge measured after 1 to 1.5 hrs by ELISA relative to vehicle-treated control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID636429 | Inhibition of EPHB4 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624970 | Binding constant for CDK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1706571 | Inhibition of AURKB (unknown origin) assessed as change in melting temperature at 10 uM by DSF assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Selective targeting of the αC and DFG-out pocket in p38 MAPK. |
| AID624991 | Binding constant for ABL1-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID436037 | Percentage MAPKAPK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636433 | Inhibition of FAK | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435830 | Binding constant for RPS6KA2(Kin.Dom.2 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624902 | Binding constant for MEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435327 | Binding constant for VEGFR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624807 | Binding constant for TNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435407 | Binding constant for FLT3(D835Y) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636480 | Inhibition of P38beta2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435402 | Binding constant for EGFR(G719S) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624945 | Binding constant for BMPR1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624908 | Binding constant for TEC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256635 | Average Binding Constant for CAMK2D; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1286660 | Inhibition of CYP2D6 (unknown origin) at 30 uM | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma. |
| AID436053 | Binding constant for full-length STK33 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435165 | Binding constant for JAK1(Kin.Dom.1/JH2 - pseudokinase) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435688 | Binding constant for full-length PCTK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435554 | Binding constant for PRKD3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624923 | Binding constant for MAPKAPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435808 | Binding constant for full-length MEK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID166200 | Selectivity against RAF proto-oncogene serine/threonine-protein kinase (c-Raf-1) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID436023 | Binding constant for MERTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435541 | Percentage PKA activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636472 | Inhibition of MLK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435295 | Binding constant for MAP4K3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID339971 | Inhibition of human PKBalpha at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
| AID625142 | Binding constant for TSSK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624796 | Binding constant for MET(Y1235D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435373 | Percentage PKCzeta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID625134 | Binding constant for PIP5K2C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435644 | Binding constant for ABL1(E255K) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625102 | Binding constant for PRKD2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624832 | Binding constant for IKK-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1065372 | Inhibition of human p38-MAPK | 2014 | Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
| KLIFS: a knowledge-based structural database to navigate kinase-ligand interaction space. |
| AID435260 | Percentage RSK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID256669 | Average Binding Constant for ABL1(M351T); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID256649 | Average Binding Constant for CSK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435409 | Binding constant for full-length JNK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1646062 | Inhibition of human CDK5 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID636453 | Inhibition of IKK-beta | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435325 | Binding constant for RPS6KA4(Kin.Dom.1 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1202715 | Binding affinity to DDR2 (unknown origin) | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| Small molecule discoidin domain receptor kinase inhibitors and potential medical applications. |
| AID512564 | Inhibition of p38alpha | 2005 | Chemistry & biology, Jun, Volume: 12, Issue:6
| Features of selective kinase inhibitors. |
| AID1646070 | Inhibition of human p38gamma | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID435278 | Binding constant for full-length CDK7 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID341050 | Inhibition of human recombinant p38alpha-mediated ATF2 phosphorylation by TR-FRET assay | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID636459 | Inhibition of JAK3 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435555 | Binding constant for PRKR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435932 | Binding constant for PKAC-alpha kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636524 | Inhibition of TBK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625095 | Binding constant for SIK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID353464 | Binding affinity to p38alpha assessed as melting temperature of enzyme-inhibitor complex by thermal denaturation assay | 2009 | Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
| Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors. |
| AID435294 | Binding constant for full-length LIMK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625127 | Binding constant for RSK3(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435807 | Binding constant for MARK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624753 | Binding constant for PKNB(M.tuberculosis) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435370 | Percentage p38beta MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID256621 | Average Binding Constant for CAMK2A; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435300 | Percentage PAK6 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID322017 | Inhibition of LPS-induced TNFalpha production in human THP1 cells | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors. |
| AID435658 | Binding constant for JAK2(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624899 | Binding constant for ROS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256675 | Average Binding Constant for PTK6; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID629189 | Antiinflammatory activity in po dosed rat assessed as inhibition of LPS-induced rise in plasma TNFalpha level administered 1 hr prior to LPS-challenge measured 1.5 hrs post-challenge by ELISA | 2011 | Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
| 1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase. |
| AID624750 | Binding constant for PRP4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624898 | Binding constant for GRK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID224298 | Selectivity against p59 Fyn tyrosine kinase | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID624907 | Binding constant for SYK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256564 | Average Binding Constant for MAP3K4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625030 | Binding constant for LOK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID445088 | Inhibition of p38alpha active form expressed in Escherichia coli BL21(DE3) cells by HTRF assay | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Displacement assay for the detection of stabilizers of inactive kinase conformations. |
| AID71176 | Selectivity against Extracellular signal-regulated kinase 1 (Erk-1) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID636520 | Inhibition of SGK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435182 | Binding constant for full-length PKAC-beta | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435501 | Percentage SmMLCK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID625001 | Binding constant for EGFR(L747-S752del, P753S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID292893 | Metabolic stability in human liver microsomes at 1 uM after 40 mins | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
| Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry. |
| AID436047 | Binding constant for full-length PRKX | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625068 | Binding constant for NEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID353468 | Inhibition of LPS-induced endotoxemia in mouse assessed as inhibition of TNFalpha production at 3 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
| Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors. |
| AID636912 | Inhibition of ALK | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435293 | Binding constant for JNK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636436 | Inhibition of FGFR1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID1646088 | Inhibition of human TRKC | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID256569 | Average Binding Constant for PAK7/PAK5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID256637 | Average Binding Constant for JNK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624769 | Binding constant for AURKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625143 | Binding constant for CAMKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435557 | Binding constant for RIPK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636440 | Inhibition of FGR | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID256645 | Average Binding Constant for JAK2 (Kin.Dom. 2); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435375 | Percentage RSK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636445 | Inhibition of FYN | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435782 | Binding constant for BRSK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636444 | Inhibition of FMS | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435780 | Binding constant for BMPR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435905 | Binding constant for full-length CSNK1G3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID717757 | Inhibition of human recombinant C-terminal His-tagged PYK2 using ATP as substrate incubated for 1 hr prior to substrate addition | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
| Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors. |
| AID625013 | Binding constant for LCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636475 | Inhibition of MST1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID341051 | Inhibition of HSP27 phosphorylation in IL-1-alpha-stimulated HLF cells | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID435559 | Binding constant for SNARK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436012 | Binding constant for full-length CSNK2A1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624930 | Binding constant for TNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435924 | Binding constant for MARK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625074 | Binding constant for IKK-epsilon kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435171 | Binding constant for NEK9 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625046 | Binding constant for PIK3CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256599 | Average Binding Constant for TTK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435430 | Binding constant for INSRR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435786 | Binding constant for full-length CLK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435180 | Binding constant for MAPKAPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636413 | Inhibition of c-MET | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435661 | Binding constant for full-length MKNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625139 | Binding constant for SNARK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435926 | Binding constant for PDGFRB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624790 | Binding constant for KIT(L576P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624938 | Binding constant for FLT3(K663Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256671 | Average Binding Constant for ABL1(Y253F); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435560 | Binding constant for SNF1LK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625061 | Binding constant for MAP4K5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625002 | Binding constant for EGFR(L747-T751del,Sins) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625033 | Binding constant for PCTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256577 | Average Binding Constant for CLK4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID319703 | Inhibition of JNK2a | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| Structure-based design and subsequent optimization of 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) inhibitors of p38 MAP kinase. |
| AID624774 | Binding constant for QSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624863 | Binding constant for MARK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435803 | Binding constant for full-length LIMK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435528 | Binding constant for IRAK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636917 | Inhibition of AXL | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624828 | Binding constant for CDK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435396 | Binding constant for CHEK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636443 | Inhibition of FLT4 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID636515 | Inhibition of ROCK-1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID8971 | Tested for plasma level after 90 min of 10 mg/kg dose administered in mice | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). |
| AID256634 | Average Binding Constant for CSNK1G2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625123 | Binding constant for RET(V804L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624830 | Binding constant for CDK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624895 | Binding constant for MEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636509 | Inhibition of PLK2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435987 | Percentage PRK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID435962 | Percentage CDK2-cyclinA activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636458 | Inhibition of JAK2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435292 | Binding constant for ITK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435797 | Binding constant for ERBB4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435518 | Binding constant for AURKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID29537 | Maximum time (Tmax) was measured after oral dosing at 10 mg/kg in male cynomolgus monkey (100% PEG400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID435312 | Binding constant for MET kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436020 | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435801 | Binding constant for full-length GSK3A | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624851 | Binding constant for ERBB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625045 | Binding constant for PIK3CA(Q546K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624876 | Binding constant for PDPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636510 | Inhibition of PLK3 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID636531 | Inhibition of ZAP70 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID673364 | Antiinflammatory activity in BALB/c mouse model of endotoxic shock assessed as inhibition of LPS-induced TNFalpha production at 50 mg/kg, po administered 30 mins before LPS challenge measured after 60 mins by ELISA | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
| Design and synthesis of novel p38α MAP kinase inhibitors: discovery of pyrazole-benzyl ureas bearing 2-molpholinopyrimidine moiety. |
| AID435551 | Binding constant for full-length p38-beta | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1646061 | Inhibition of human BLK | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID636470 | Inhibition of MARK2/PAR-1Balpha | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435704 | Percentage Aurora B activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID624893 | Binding constant for MEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID224149 | Selectivity against p56 Lck tyrosine kinase | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID624712 | Binding constant for DYRK1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1706573 | Inhibition of STK10 (unknown origin) assessed as change in melting temperature at 10 uM by DSF assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Selective targeting of the αC and DFG-out pocket in p38 MAPK. |
| AID516347 | Binding affinity to full-length GST-tagged p38alpha after 2.5 hrs by TR-FRET competition binding assay | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19
| Biochemical and biophysical characterization of unique switch pocket inhibitors of p38α. |
| AID1451484 | Binding affinity to wild type human biotin labelled p38 alpha (9 to 352 residues) expressed in sf21 insect cells assessed as dissociation rate constant by SPR analysis | | | |
| AID435931 | Binding constant for PIM1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624919 | Binding constant for AURKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435202 | Binding constant for TRKC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID322019 | Inhibition of human p38-alpha kinase phosphorylation | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors. |
| AID436072 | Percentage CK1delta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID435934 | Binding constant for PLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID127261 | Rate of dissociation from Mitogen-activated protein kinase p38 alpha | 2003 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 13, Issue:18
| The kinetics of binding to p38MAP kinase by analogues of BIRB 796. |
| AID339969 | Inhibition of human PKA at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
| AID435900 | Binding constant for AKT3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435515 | Binding constant for ABL1(Q252H) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636522 | Inhibition of SYK | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625137 | Binding constant for MEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435158 | Binding constant for EPHA5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID639972 | Inhibition of N-terminus His-tagged human p38alpha expressed in Escherichia coli BL21 DE3 using GST-tagged ATF2 as substrate after 90 mins by HTRF assay | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Structure-based design, synthesis and biological evaluation of N-pyrazole, N'-thiazole urea inhibitors of MAP kinase p38α. |
| AID435800 | Binding constant for FYN kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256618 | Average Binding Constant for PHkg2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID436084 | Percentage GAK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID501376 | Binding affinity to JNK2 | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors. |
| AID624952 | Binding constant for EPHA4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256596 | Average Binding Constant for CLK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624989 | Binding constant for ABL1(T315I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435151 | Binding constant for CAMK1G kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID25722 | Area under curve was measured after intravenous dosing at 1 mg/kg in female BALB/c mice (70% PEG 400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID624818 | Binding constant for ULK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624975 | Binding constant for PLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625055 | Binding constant for MST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625087 | Binding constant for MELK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435534 | Binding constant for NEK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624886 | Binding constant for ERK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624904 | Binding constant for NEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1646087 | Inhibition of human TRKB | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID435318 | Binding constant for PAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435939 | Binding constant for TIE2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625086 | Binding constant for SLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636466 | Inhibition of MAPKAPK2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624996 | Binding constant for EGFR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625089 | Binding constant for AAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624910 | Binding constant for TTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435427 | Percentage PKBalpha activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636467 | Inhibition of MAPKAPK3 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624831 | Binding constant for CHEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624745 | Binding constant for PKN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID341201 | Inhibition of p38beta/gamma | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID636425 | Inhibition of EPHA5 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625108 | Binding constant for MKNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624713 | Binding constant for ERK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435647 | Binding constant for CAMK2D kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624838 | Binding constant for ACVR2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256605 | Average Binding Constant for STK17B; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435783 | Binding constant for full-length BRSK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624950 | Binding constant for DMPK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625103 | Binding constant for MST4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636517 | Inhibition of RON | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435676 | Binding constant for LCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636523 | Inhibition of TAK1-TAB1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435912 | Binding constant for MRCKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID29536 | Maximum time (Tmax) was measured after oral dosing at 10 mg/kg in female BALB/c mice(100% PEG400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID625038 | Binding constant for PIK3CA(E542K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256611 | Average Binding Constant for RIPK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435938 | Binding constant for TGFBR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256584 | Average Binding Constant for CAMK1D; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435408 | Binding constant for INSR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435199 | Binding constant for TLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256586 | Average Binding Constant for STK4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435339 | Percentage CaMKKbeta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID435706 | Percentage BRSK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID624868 | Binding constant for MST1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624826 | Binding constant for BMPR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636508 | Inhibition of PLK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435756 | Percentage Src activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID624833 | Binding constant for CSNK1G2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID296933 | Cmax in Sprague-Dawley rat at 10 mg/kg, po | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| Discovery and optimization of p38 inhibitors via computer-assisted drug design. |
| AID435696 | Selectivity for p38-alpha as proportion of 290 kinases in screen with similar potency; non-selective = 1 highly selective = 0 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID26484 | Bioavailability was measured after oral dosing at 10 mg/kg in male cynomolgus monkey (100% PEG400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID292892 | Inhibition of MAPK p38 | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
| Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry. |
| AID624870 | Binding constant for NEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1646069 | Inhibition of human EPHB2 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID624840 | Binding constant for AXL kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256644 | Average Binding Constant for CSNK1E; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID296927 | Inhibition of LPS-induced TNFalpha production in human whole blood | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| Discovery and optimization of p38 inhibitors via computer-assisted drug design. |
| AID624927 | Binding constant for RPS6KA4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636469 | Inhibition of MARK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624785 | Binding constant for JAK3(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID209654 | Selectivity against Syk protein tyrosine kinase | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID624966 | Binding constant for DCAMKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1646082 | Inhibition of human SLK | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID497107 | Inhibition of human recombinant full-length N-terminal GST-tagged p38alpha expressed in Escherichia coli by radiometric kinase assay | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
| The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796. |
| AID624784 | Binding constant for INSR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636456 | Inhibition of IRAK4 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID256639 | Average Binding Constant for PHkg1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435461 | Percentage CK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID435826 | Binding constant for full-length PCTK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435781 | Binding constant for full-length BMX | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436050 | Binding constant for RPS6KA2(Kin.Dom.1 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256590 | Average Binding Constant for EPHB1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435681 | Percentage MAPKAPK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID1646083 | Inhibition of human STK10 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID1646080 | Inhibition of human PTK2beta | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID636422 | Inhibition of EPHA2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435896 | Binding constant for AAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435669 | Percentage PDK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID436018 | Binding constant for FLT4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID339968 | Inhibition of human SAPK4/p38delta at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
| AID624971 | Binding constant for DAPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636512 | Inhibition of PYK2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID436004 | Binding constant for ACVR2A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625023 | Binding constant for HIPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636500 | Inhibition of PKCdelta | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID636404 | Inhibition of CDK2/cyclin E | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624993 | Binding constant for ABL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625043 | Binding constant for PIK3CA(I800L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435937 | Binding constant for TESK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1623456 | Inhibition of ABCB1 in human A2780/ADR cells assessed as potentiation of daunorubicin-induced cytotoxicity measured after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Novel chalcone and flavone derivatives as selective and dual inhibitors of the transport proteins ABCB1 and ABCG2. |
| AID624936 | Binding constant for FLT3(D835Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID292888 | Partition coefficient, log P of the compound | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
| Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry. |
| AID1646084 | Inhibition of human TIE1 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID624877 | Binding constant for PIK3C2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624889 | Binding constant for JNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1646068 | Inhibition of human EPHA8 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID436052 | Binding constant for full-length SNF1LK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436086 | Percentage HIPK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID435901 | Binding constant for BRAF kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625040 | Binding constant for PIK3CA(E545K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256591 | Average Binding Constant for EPHA5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435524 | Binding constant for full-length CSNK1D | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435378 | Percentage S6K1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID625035 | Binding constant for PHKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435147 | Binding constant for ACVR2B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435794 | Binding constant for EPHA3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435656 | Binding constant for FGFR4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID319701 | Apparent permeability across human Caco-2 cells | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| Structure-based design and subsequent optimization of 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) inhibitors of p38 MAP kinase. |
| AID624903 | Binding constant for SRPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636482 | Inhibition of P38gamma | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625032 | Binding constant for TRKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435910 | Binding constant for MAP4K4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435546 | Binding constant for PRKG1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435678 | Binding constant for MUSK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256677 | Average Binding Constant for STK38L; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624972 | Binding constant for MTOR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435432 | Binding constant for MLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435522 | Binding constant for CDK11 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435674 | Binding constant for JAK3(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1286661 | Inhibition of CYP3A4 (unknown origin) at 30 uM | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma. |
| AID435561 | Binding constant for SRMS kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435802 | Binding constant for KIT(V559D,V654A) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256576 | Average Binding Constant for MKNK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435311 | Binding constant for HCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435406 | Binding constant for FLT3(D835H) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435734 | Percentage NEK6 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID624759 | Binding constant for PFCDPK1(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624787 | Binding constant for KIT(A829P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624836 | Binding constant for IKK-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636499 | Inhibition of PKCbeta2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435819 | Percentage PKBbeta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID624718 | Binding constant for PFTAIRE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID436006 | Binding constant for full-length AURKC | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625003 | Binding constant for EGFR(L858R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435321 | Binding constant for PRKCQ kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625128 | Binding constant for CSNK1G1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1706568 | Inhibition of p38alpha (unknown origin) assessed as change in melting temperature at 10 uM by DSF assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Selective targeting of the αC and DFG-out pocket in p38 MAPK. |
| AID636428 | Inhibition of EPHB3 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID215435 | Tested for inhibition of Tumor necrosis factor, alpha in human whole blood | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). |
| AID624737 | Binding constant for EPHA5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435161 | Binding constant for FES kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436083 | Percentage ERK8 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID353465 | Inhibition of LPS-induced TNFalpha production in human THP1 cells | 2009 | Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
| Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors. |
| AID435415 | Binding constant for MYLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625016 | Binding constant for SRC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636402 | Inhibition of CDK1/cyclin B | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624941 | Binding constant for CDKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435779 | Binding constant for ALK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256623 | Average Binding Constant for MYLK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624703 | Binding constant for MAPKAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636490 | Inhibition of PDGFRalpha | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID636487 | Inhibition of PAK5 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID445090 | Inhibition of JNK2 active form by HTRF assay | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Displacement assay for the detection of stabilizers of inactive kinase conformations. |
| AID256588 | Average Binding Constant for PCTK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID636526 | Inhibition of TRKA | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID256606 | Average Binding Constant for STK16; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435196 | Binding constant for full-length SRPK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435200 | Binding constant for full-length TNNI3K | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624732 | Binding constant for PYK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625024 | Binding constant for PRKD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435250 | Percentage MSK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID624802 | Binding constant for PIM3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624776 | Binding constant for PCTK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435123 | Percentage NEK7 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID435805 | Binding constant for MAP4K5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624929 | Binding constant for BRSK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624804 | Binding constant for ERBB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636488 | Inhibition of PAK6 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435723 | Percentage GSK3-beta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID435322 | Binding constant for PRKG2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624857 | Binding constant for HCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435558 | Binding constant for RPS6KA3(Kin.Dom.1 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636408 | Inhibition of CHK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435727 | Percentage JNK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636457 | Inhibition of IRR | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID339974 | Inhibition of human LCK at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
| AID636446 | Inhibition of GRK5 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625467 | Antiinflammatory activity in rat assessed as inhibition of LPS-induced TNFalpha production plasma administered orally 1 hr prior to LPS challenge measured after 1.5 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
| Indolin-2-one p38α inhibitors III: bioisosteric amide replacement. |
| AID624707 | Binding constant for DCAMKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256638 | Average Binding Constant for PRKAA1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625129 | Binding constant for HIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID28297 | Maximum plasma conc. was measured after oral dosing at 10 mg/kg in female BALB/c mice(100% PEG400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID624947 | Binding constant for BRAF(V600E) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625007 | Binding constant for EGFR(T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636909 | Inhibition of AKT1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625005 | Binding constant for EGFR(L861Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID341206 | Inhibition of JNK1 | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID625124 | Binding constant for RET(V804M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625073 | Binding constant for SGK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636502 | Inhibition of PKCeta | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624964 | Binding constant for DYRK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435649 | Binding constant for CDC2L2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436011 | Binding constant for full-length CLK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID339972 | Inhibition of human GSK3-beta at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
| AID636421 | Inhibition of EPHA1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624990 | Binding constant for ABL1(Y253F)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624706 | Binding constant for MLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624721 | Binding constant for MEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435204 | Binding constant for WEE1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625106 | Binding constant for MARK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624789 | Binding constant for KIT(D816V) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435338 | Percentage CaMK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID256597 | Average Binding Constant for CLK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435940 | Binding constant for full-length TSSK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID127252 | Dissociation constant at Tref against human Mitogen-activated protein kinase p38 alpha | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Thermal denaturation: a method to rank slow binding, high-affinity P38alpha MAP kinase inhibitors. |
| AID435411 | Binding constant for KIT(D816V) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636431 | Inhibition of ERK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID256581 | Average Binding Constant for CAMK1G; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID436025 | Binding constant for NDR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624702 | Binding constant for BRSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636405 | Inhibition of CDK5/p25 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624755 | Binding constant for ZAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435197 | Binding constant for TEC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636454 | Inhibition of IR | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435902 | Binding constant for BRAF(V600E) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435395 | Binding constant for CDC2L1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1286662 | Inhibition of CYP2C9 (unknown origin) at 30 uM | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma. |
| AID624726 | Binding constant for HIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625126 | Binding constant for TAOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636426 | Inhibition of EPHB1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435621 | Percentage p38alpha MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID625054 | Binding constant for MST2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624835 | Binding constant for ERN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435323 | Binding constant for RET(M918T) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435675 | Binding constant for KIT(V559D,T670I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256563 | Average Binding Constant for ULK3 m; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID436014 | Binding constant for full-length DYRK1B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625048 | Binding constant for PRKCD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625029 | Binding constant for BRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636519 | Inhibition of RSK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435521 | Binding constant for CAMKK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435201 | Binding constant for TRKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435438 | Binding constant for full-length p38-gamma | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435666 | Binding constant for full-length NEK7 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625136 | Binding constant for YSK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625058 | Binding constant for VRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256595 | Average Binding Constant for CLK3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1706575 | Inhibition of C-terminal NanoLuc-fused full length human MAPK14 expressed in HEK293T cells after 2 hrs by NanoBRET assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Selective targeting of the αC and DFG-out pocket in p38 MAPK. |
| AID624896 | Binding constant for PRKR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256608 | Average Binding Constant for MARK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435329 | Binding constant for YSK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1706570 | Inhibition of BRAF (unknown origin) assessed as change in melting temperature at 10 uM by DSF assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Selective targeting of the αC and DFG-out pocket in p38 MAPK. |
| AID699610 | Antiinflammatory activity in po dosed C57BL/6 mouse assessed as decrease in LPS-induced serum TNFalpha level administered 30 mins prior to LPS challenge measured 60 mins post LPS challenge by ELISA | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach. |
| AID436005 | Binding constant for ANKK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625085 | Binding constant for ULK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256603 | Average Binding Constant for FER; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID292890 | Distribution coefficient, log D at pH 6.5 | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
| Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry. |
| AID624733 | Binding constant for SIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624819 | Binding constant for ACVR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID599959 | Binding affinity to human KIT D816V mutant incubated for 1 hr by kinase binding assay | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
| Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. |
| AID256614 | Average Binding Constant for YES; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625072 | Binding constant for TBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435176 | Percentage PIM2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID435865 | Percentage MKK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID624782 | Binding constant for FGFR3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636452 | Inhibition of IGF-1R | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624962 | Binding constant for ASK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636505 | Inhibition of PKD2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID636923 | Inhibition of BTK | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID256632 | Average Binding Constant for CDK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625004 | Binding constant for EGFR(L858R,T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1645935 | Inhibition of human p38beta | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID624968 | Binding constant for DRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435443 | Binding constant for TXK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436076 | Percentage DYRK1A activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636465 | Inhibition of LYN | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID636504 | Inhibition of PKCtheta | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID163168 | Selectivity against Protein kinase C alpha, Protein kinase C beta, Protein kinase C gamma | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID636471 | Inhibition of MINK | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435790 | Binding constant for DRAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435319 | Binding constant for PKN1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624729 | Binding constant for FAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624734 | Binding constant for YANK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624743 | Binding constant for LTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625000 | Binding constant for EGFR(L747-E749del, A750P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID341195 | Inhibition of cRAF | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID435283 | Binding constant for DAPK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435530 | Binding constant for MAP3K4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1646089 | Inhibition of human ZAK | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID636532 | Inhibition of ZIPK | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID427502 | Antiinflammatory activity in adjuvant-induced arthritis Wistar rat model assessed as inhibition of contralateral paw volume at 10 mg/kg, po administered on day 11 post inoculation once daily for 7 days relative to vehicle control | 2009 | Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
| Design, synthesis, and structure-activity relationships of aminopyridine N-oxides, a novel scaffold for the potent and selective inhibition of p38 mitogen activated protein kinase. |
| AID501375 | Inhibition of p38alpha | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors. |
| AID624815 | Binding constant for ERBB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435527 | Binding constant for FGFR3(G697C) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1460598 | Inhibition of NorA in Staphylococcus aureus SA1199B harboring GrlA A116E mutant assessed as inhibition of ethidium bromide efflux at 50 uM measured after 5 mins by fluorometric method relative to control | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
| Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors. |
| AID624961 | Binding constant for TGFBR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435793 | Binding constant for EPHA1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435563 | Binding constant for TNIK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624720 | Binding constant for HIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID296930 | Inhibition of LPS-induced TNFalpha production in BALB/c mouse at 10 mg/kg, po | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| Discovery and optimization of p38 inhibitors via computer-assisted drug design. |
| AID624878 | Binding constant for PIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256619 | Average Binding Constant for RPS6KA3 (Kin.Dom. 1); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624999 | Binding constant for EGFR(G719S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435284 | Binding constant for DCAMKL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435814 | Percentage PIM3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID275050 | Inhibition of p38 alpha | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
| Design, synthesis, and biological evaluation of phenylamino-substituted 6,11-dihydro-dibenzo[b,e]oxepin-11-ones and dibenzo[a,d]cycloheptan-5-ones: novel p38 MAP kinase inhibitors. |
| AID625118 | Binding constant for CAMK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624767 | Binding constant for MERTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256571 | Average Binding Constant for BIKE; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435164 | Binding constant for IGF1R kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436048 | Binding constant for full-length PTK2B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624822 | Binding constant for CDKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID516348 | Binding affinity to full-length GST-tagged p38alpha by surface plasmon resonance assay | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19
| Biochemical and biophysical characterization of unique switch pocket inhibitors of p38α. |
| AID256657 | Average Binding Constant for LCK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624860 | Binding constant for VEGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID436033 | Binding constant for PIK3CA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624988 | Binding constant for ABL1(T315I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625091 | Binding constant for MAST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID721303 | Binding affinity to p38alpha MAP kinase (unknown origin) by FLiK assay | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| Dibenzosuberones as p38 mitogen-activated protein kinase inhibitors with low ATP competitiveness and outstanding whole blood activity. |
| AID625008 | Binding constant for EPHA1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624892 | Binding constant for p38-delta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624814 | Binding constant for DCAMKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624805 | Binding constant for RSK3(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID341193 | Binding affinity to human unphosphorylated p38alpha by surface plasmon resonance | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID435691 | Binding constant for SgK085 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625080 | Binding constant for EIF2AK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624719 | Binding constant for GRK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1646085 | Inhibition of human TIE2 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID256560 | Average Binding Constant for FGR; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625117 | Binding constant for PAK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636420 | Inhibition of EGFR | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624741 | Binding constant for LRRK2(G2019S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID292891 | Distribution coefficient, log D at pH 7.4 | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
| Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry. |
| AID636921 | Inhibition of BRK | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625077 | Binding constant for DAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624942 | Binding constant for DRAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256617 | Average Binding Constant for TEK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID636915 | Inhibition of ASK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624880 | Binding constant for PIK4CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636407 | Inhibition of CDK9/cyclin T1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624901 | Binding constant for RSK1(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435163 | Binding constant for full-length GSK3B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256654 | Average Binding Constant for FGFR2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID436045 | Binding constant for PRKD1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436036 | Percentage Lck activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID435223 | Percentage CSK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID339959 | Inhibition of human c-RAF at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
| AID624856 | Binding constant for GSK3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625088 | Binding constant for ARK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1141140 | Binding affinity to wild type DDR2 (unknown origin) by FLiK assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Identification of type II and III DDR2 inhibitors. |
| AID636521 | Inhibition of STK33 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID636462 | Inhibition of JNK3 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435434 | Binding constant for RET kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256630 | Average Binding Constant for FYN; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435718 | Percentage EF2K activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636430 | Inhibition of ERBB4 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID256624 | Average Binding Constant for FGFR3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624924 | Binding constant for RIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID513134 | Inhibition of c-Raf kinase | 2006 | Nature chemical biology, Jul, Volume: 2, Issue:7
| Rational design of inhibitors that bind to inactive kinase conformations. |
| AID256665 | Average Binding Constant for ABL1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624885 | Binding constant for ERK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624730 | Binding constant for CAMK2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1646074 | Inhibition of human JNK1 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID624763 | Binding constant for RIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435792 | Binding constant for EGFR(S752-I759del) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624746 | Binding constant for WEE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624731 | Binding constant for CAMK2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624760 | Binding constant for PFPK5(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1141136 | Inhibition of wild type DDR2 (unknown origin) preincubated for 30 mins before substrate addition by FRET assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Identification of type II and III DDR2 inhibitors. |
| AID624752 | Binding constant for SNRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625056 | Binding constant for TESK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624948 | Binding constant for CSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636530 | Inhibition of YES | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435650 | Binding constant for full-length CSNK1E | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636919 | Inhibition of BMX | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435520 | Binding constant for CAMK2A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256567 | Average Binding Constant for EPHA6; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID767465 | Inhibition of MAPK14 (unknown origin) | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Selectivity data: assessment, predictions, concordance, and implications. |
| AID1646066 | Inhibition of human EPHA3 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID625011 | Binding constant for FGR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435787 | Binding constant for CLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435796 | Binding constant for ERBB2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435679 | Binding constant for PIM3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435728 | Percentage JNK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID625050 | Binding constant for PKN2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636486 | Inhibition of PAK4 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435233 | Percentage HIPK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636901 | Inhibition of ABL2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID256610 | Average Binding Constant for Aurora3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435280 | Binding constant for CSF1R kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624742 | Binding constant for NEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624778 | Binding constant for ACVRL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636474 | Inhibition of MSK2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625065 | Binding constant for CIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624801 | Binding constant for MAP3K15 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256651 | Average Binding Constant for DAPK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624823 | Binding constant for MKNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID436017 | Binding constant for ERK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624992 | Binding constant for ABL1-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625138 | Binding constant for STK33 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625059 | Binding constant for YSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624757 | Binding constant for PKMYT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625034 | Binding constant for PDGFRA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435403 | Binding constant for EPHB1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624883 | Binding constant for PRKCI kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256575 | Average Binding Constant for NEK6; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624715 | Binding constant for ERK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1286657 | Inhibition of human recombinant p38 alpha assessed as phosphorylation of MAPKAP-K2 preincubated for 2 hrs followed by FRET peptide and MAPKAP-K2 addition measured after 1 hr by Z-LYTE assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma. |
| AID624983 | Binding constant for ABL1(H396P)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636417 | Inhibition of DAPK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435904 | Binding constant for full-length CSK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID341199 | Inhibition of LCK | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID636913 | Inhibition of ALK4 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435203 | Binding constant for TTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256573 | Average Binding Constant for PAK6; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435454 | Percentage CaMKKalpha activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID436008 | Binding constant for full-length BTK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435374 | Percentage PLK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID127269 | Thermal denaturation temperature (Tm) of the inhibitor and murine pMitogen-activated protein kinase p38 alpha complex | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). |
| AID436034 | Binding constant for PRKCH kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636411 | Inhibition of CK2alpha | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624793 | Binding constant for KIT(V559D,V654A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435433 | Binding constant for full-length MST1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624879 | Binding constant for PIK3CG kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624809 | Binding constant for MYLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256674 | Average Binding Constant for PKMYT1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624915 | Binding constant for PIP5K2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID215449 | Tested for inhibition of Tumor necrosis factor, alpha in LPS-stimulated mice at a dose of 30 mg/kg | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). |
| AID435804 | Binding constant for LYN kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624995 | Binding constant for CSF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625006 | Binding constant for EGFR(S752-I759del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435445 | Binding constant for ZAP70 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1730913 | Inhibition of human GSK-3beta using Ser/Thr 6 peptide as substrate preincubated for 60 mins followed by ATP and substrate addition and measured after 45 mins by Z'lyte assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| Structure-Based Design of Potent Selective Nanomolar Type-II Inhibitors of Glycogen Synthase Kinase-3β. |
| AID624933 | Binding constant for PLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624862 | Binding constant for LYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435822 | Binding constant for MEK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435828 | Binding constant for full-length PIP5K2B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256574 | Average Binding Constant for STK3_m; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624844 | Binding constant for CDK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256647 | Average Binding Constant for SYK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435282 | Binding constant for full-length CSNK1G2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256653 | Average Binding Constant for FGFR1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624932 | Binding constant for CLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435933 | Binding constant for PKN2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID292896 | Suppression of lipopolysaccharide-induced TNFalpha release in mouse at 10 mg/kg, po after 120 mins | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
| Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry. |
| AID624791 | Binding constant for KIT(V559D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624974 | Binding constant for PIK3CD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435613 | Percentage MNK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID625042 | Binding constant for PIK3CA(H1047Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1141137 | Inhibition of DDR2 T654M mutant (unknown origin) preincubated for 30 mins before substrate addition by FRET assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Identification of type II and III DDR2 inhibitors. |
| AID625026 | Binding constant for MAP3K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625037 | Binding constant for PIK3CA(C420R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1706572 | Inhibition of SLK (unknown origin) assessed as change in melting temperature at 10 uM by DSF assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Selective targeting of the αC and DFG-out pocket in p38 MAPK. |
| AID636473 | Inhibition of MSK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625090 | Binding constant for ICK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID341192 | Ratio of IC50 for LPS-stimulated TNFalpha release in human PBMC to Ki for human p38alpha | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID353470 | Binding affinity to p38alpha assessed as half life dissociation | 2009 | Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
| Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors. |
| AID435281 | Binding constant for full-length CSNK1A1L | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636922 | Inhibition of BRSK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID1646071 | Inhibition of human FLT1 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID624931 | Binding constant for CLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435315 | Percentage MARK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID624946 | Binding constant for BRAF kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624861 | Binding constant for LIMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435677 | Binding constant for LOK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435326 | Binding constant for TYRO3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435731 | Percentage MNK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID435785 | Binding constant for full-length CDK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625131 | Binding constant for FGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435228 | Percentage ERK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID435194 | Binding constant for RPS6KA6(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID339973 | Inhibition of human ROCK2 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
| AID27883 | Plasma clearance (CL) was measured after intravenous dosing at 1 mg/kg in female BALB/c mice(70% PEG400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID256598 | Average Binding Constant for FRK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID256646 | Average Binding Constant for JAK1 (Kin.Dom. 1); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID339967 | Inhibition of human SAPK3/p38gamma at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
| AID436019 | Binding constant for FRK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636503 | Inhibition of PKCmu | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435652 | Binding constant for EGFR(L747-E749del, A750P) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435908 | Binding constant for EPHA2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624867 | Binding constant for MLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624800 | Binding constant for IGF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625028 | Binding constant for ASK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256663 | Average Binding Constant for INSR; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624728 | Binding constant for NIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID436071 | Percentage CHK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID624748 | Binding constant for EPHA6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625067 | Binding constant for NDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435517 | Binding constant for AKT2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624905 | Binding constant for CDKL5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435155 | Binding constant for full-length DLK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636400 | Inhibition of CAMK2beta | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624786 | Binding constant for KIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435526 | Binding constant for FGFR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636451 | Inhibition of HIPK3 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625076 | Binding constant for PLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435440 | Binding constant for PIM2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID319696 | Binding affinity to mitogen-activated protein kinase p38 by thermal denaturation assay | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| Structure-based design and subsequent optimization of 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) inhibitors of p38 MAP kinase. |
| AID256562 | Average Binding Constant for PAK4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624900 | Binding constant for RSK1(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435799 | Binding constant for FLT3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624811 | Binding constant for PAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625066 | Binding constant for IRAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624953 | Binding constant for EPHA7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624816 | Binding constant for HPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256667 | Average Binding Constant for ABL1(E255K); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435404 | Binding constant for EPHB4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435444 | Binding constant for TYK2(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID513135 | Inhibition of Lck kinase | 2006 | Nature chemical biology, Jul, Volume: 2, Issue:7
| Rational design of inhibitors that bind to inactive kinase conformations. |
| AID435664 | Binding constant for MYLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435159 | Binding constant for EPHB3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436044 | Binding constant for PLK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636506 | Inhibition of PKG1alpha | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID319700 | Solubility at pH 7.4 | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| Structure-based design and subsequent optimization of 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) inhibitors of p38 MAP kinase. |
| AID435654 | Binding constant for full-length ERK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625047 | Binding constant for AMPK-alpha2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624839 | Binding constant for AKT2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID339955 | Inhibition of human SAPK2b/p38--beta-2 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
| AID624994 | Binding constant for AKT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435690 | Binding constant for RPS6KA1(Kin.Dom.1 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435184 | Binding constant for PTK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624937 | Binding constant for FLT3(ITD) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1409768 | Inhibition of sodium arsenate activated N-terminal GST-tagged Brugia malayi MPK1 expressed in HEK293F cells using FAM-p38tide as substrate by IMAP assay | 2018 | ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
| Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis. |
| AID427501 | Antiinflammatory activity in po dosed rat assessed as inhibition of LPS-induced TNFalpha release in plasma administered 1 hr prior to LPS challenge measured after 1.5 hrs by ELISA | 2009 | Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
| Design, synthesis, and structure-activity relationships of aminopyridine N-oxides, a novel scaffold for the potent and selective inhibition of p38 mitogen activated protein kinase. |
| AID30170 | Vss was measured after intravenous dosing at 1 mg/kg in male cynomolgus monkey (70% PEG400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID341203 | Inhibition of JNK2 | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID624944 | Binding constant for ALK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636920 | Inhibition of BRAF (V599E) | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID636501 | Inhibition of PKCgamma | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435883 | Percentage SGK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID353469 | Binding affinity to p38alpha by exchange curve binding kinetic analysis | 2009 | Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
| Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors. |
| AID436032 | Binding constant for MYO3B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID27885 | Plasma clearance was measured after intravenous dosing at 1 mg/kg in male cynomolgus monkey (70% PEG400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID256629 | Average Binding Constant for HCK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID636460 | Inhibition of JNK1alpha1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435660 | Binding constant for full-length MELK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435225 | Percentage DYRK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID1202714 | Binding affinity to DDR1 (unknown origin) | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| Small molecule discoidin domain receptor kinase inhibitors and potential medical applications. |
| AID1286654 | Inhibition of HCK (unknown origin) preincubated for 2 hrs followed by FRET peptide addition measured after 1 hr by Z-LYTE assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma. |
| AID625109 | Binding constant for BIKE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624725 | Binding constant for NEK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625015 | Binding constant for ROCK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624980 | Binding constant for ABL1(F317I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID445089 | Displacement of N,N'-(2,2'-(3,3'-disulfanediylbis(2,5-dioxopyrrolidine-3,1-diyl))bis(ethane-2,1-diyl))bis(2-(3-(3-tert-butyl-5-(3-naphthalen-1-ylureido)-1H-pyrazol-1-yl)phenylamino)acetamide) from inactive form of JNK2 by enzyme fragment complementation a | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Displacement assay for the detection of stabilizers of inactive kinase conformations. |
| AID435156 | Binding constant for EGFR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID673366 | Inhibition of human recombinant P38alpha-mediated ATF2 phosphorylation after 1 hr | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
| Design and synthesis of novel p38α MAP kinase inhibitors: discovery of pyrazole-benzyl ureas bearing 2-molpholinopyrimidine moiety. |
| AID625083 | Binding constant for LATS2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624873 | Binding constant for PAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625081 | Binding constant for RSK4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435979 | Percentage MST2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636442 | Inhibition of FLT3 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID256607 | Average Binding Constant for STK18; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1646077 | Inhibition of human KIT | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID256604 | Average Binding Constant for STK10; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435286 | Binding constant for EPHA7 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435400 | Binding constant for DDR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID30169 | Vss was measured after intravenous dosing at 1 mg/kg in female BALB/c mice(70% PEG400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID624951 | Binding constant for EPHA2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1730914 | Inhibition of Ustilago maydis GSK-3beta using Ser/Thr 6 peptide as substrate preincubated for 60 mins followed by ATP and substrate addition and measured after 45 mins by Z'lyte assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| Structure-Based Design of Potent Selective Nanomolar Type-II Inhibitors of Glycogen Synthase Kinase-3β. |
| AID339961 | Inhibition of human MAPK2/ERK2 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
| AID625019 | Binding constant for AKT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID164782 | Selectivity against Protein kinase A (PKA) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID625121 | Binding constant for RET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID70050 | Selectivity against Epidermal growth factor receptor | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID435277 | Binding constant for full-length CDK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624874 | Binding constant for PCTK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625141 | Binding constant for RIOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID29077 | Half life was measured after intravenous dosing at 1 mg/kg in female BALB/c mice(70% PEG400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID624738 | Binding constant for MLCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256652 | Average Binding Constant for CAMK2B; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435183 | Binding constant for PLK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624779 | Binding constant for BTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636447 | Inhibition of GRK6 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624705 | Binding constant for MYLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435881 | Percentage ROCK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID256673 | Average Binding Constant for PAK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625125 | Binding constant for CLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636441 | Inhibition of FLT1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625010 | Binding constant for FER kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625133 | Binding constant for CDC2L2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID501377 | Binding affinity to JNK3 | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors. |
| AID624758 | Binding constant for RIPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256565 | Average Binding Constant for MAP4K5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID636914 | Inhibition of ARK5 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625014 | Binding constant for PRKCE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256641 | Average Binding Constant for ABL2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624799 | Binding constant for TIE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625070 | Binding constant for PFTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624812 | Binding constant for SBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624795 | Binding constant for MET(M1250T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624765 | Binding constant for TRKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625057 | Binding constant for TYRO3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435791 | Binding constant for EGFR(E746-A750del) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435198 | Binding constant for TIE1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID353466 | Inhibition of LPS-induced TNFalpha production in human whole blood | 2009 | Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
| Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors. |
| AID624739 | Binding constant for GRK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435529 | Binding constant for LATS1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625049 | Binding constant for PRKCH kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID341208 | Inhibition of TEK | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID436051 | Binding constant for RPS6KA5(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID339964 | Inhibition of human JNK2alpha2 at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
| AID256615 | Average Binding Constant for p38-gamma; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624973 | Binding constant for JAK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624976 | Binding constant for PRKX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636449 | Inhibition of HCK | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID341209 | Inhibition of TNIK | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID636485 | Inhibition of PAK3 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435431 | Binding constant for MAP4K1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624740 | Binding constant for LRRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID322018 | Inhibition of human p38-alpha kinase | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors. |
| AID256583 | Average Binding Constant for CAMKK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID256594 | Average Binding Constant for BMX; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625092 | Binding constant for NDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID249742 | In vivo threshold minimum effective dose for inhibition of bone erosion and cartilage destruction in rat after oral bid dosing for 14 days | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
| Design of potent and selective 2-aminobenzimidazole-based p38alpha MAP kinase inhibitors with excellent in vivo efficacy. |
| AID624846 | Binding constant for CSNK1A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624959 | Binding constant for MAP4K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1706569 | Inhibition of p38beta (unknown origin) assessed as change in melting temperature at 10 uM by DSF assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Selective targeting of the αC and DFG-out pocket in p38 MAPK. |
| AID636492 | Inhibition of PDK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624858 | Binding constant for JAK1(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435148 | Binding constant for AMPK-alpha1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625104 | Binding constant for MYO3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624736 | Binding constant for RPS6KA5(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435827 | Binding constant for PDGFRA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435291 | Binding constant for FGFR3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435399 | Binding constant for DCAMKL3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435899 | Binding constant for AKT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636401 | Inhibition of CAMK2delta | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624921 | Binding constant for MAP4K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636498 | Inhibition of PKCbeta1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID256601 | Average Binding Constant for EPHA3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435287 | Binding constant for EPHA8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256582 | Average Binding Constant for NEK9; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID639673 | Binding affinity to p38alpha MAPK by surface plasmon resonance method | 2011 | Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
| Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease. |
| AID624744 | Binding constant for ZAP70 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625084 | Binding constant for HUNK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435328 | Binding constant for YES kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435275 | Binding constant for BIKE kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435854 | Percentage IKK-beta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID25725 | Area under curve was measured after oral dosing at 10 mg/kg in male cynomolgus monkey (100% PEG400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID624891 | Binding constant for JNK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435317 | Percentage PIM1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID625078 | Binding constant for SRPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID93317 | Selectivity against I-kappa-B-kinase beta | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID435935 | Binding constant for RIPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625044 | Binding constant for PIK3CA(M1043I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID436042 | Binding constant for full-length PHKG1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625071 | Binding constant for STK39 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624850 | Binding constant for DDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435645 | Binding constant for ACVRL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624934 | Binding constant for FLT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435562 | Binding constant for STK36 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID313711 | Inhibition of LPS-induced TNFalpha release in BALB/c mouse at 50 mg/kg | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
| Novel heterocycle-substituted pyrimidines as inhibitors of NF-kappaB transcription regulation related to TNF-alpha cytokine release. |
| AID435687 | Binding constant for PAK7/PAK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436043 | Binding constant for PKMYT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436015 | Binding constant for EPHA6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624869 | Binding constant for NEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636481 | Inhibition of P38delta | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624954 | Binding constant for EPHB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1646078 | Inhibition of human MAP4K4 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID435532 | Binding constant for MST3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID319702 | Protein binding in human plasma | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| Structure-based design and subsequent optimization of 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) inhibitors of p38 MAP kinase. |
| AID341205 | Inhibition of FYN | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID625114 | Binding constant for GSK3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435653 | Binding constant for EGFR(L747-S752del, P753S) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID497610 | Inhibition of human recombinant full-length GST-tagged B-Raf by radiometric kinase assay | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
| The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796. |
| AID636419 | Inhibition of DRAK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID636496 | Inhibition of PKA | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID26483 | Bioavailability was measured after oral dosing at 10 mg/kg in female BALB/c mice(100% PEG400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID256602 | Average Binding Constant for EPHA2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435713 | Percentage CHK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID435694 | Binding constant for TNK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624928 | Binding constant for CDKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID339970 | Inhibition of human PKCalpha at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
| AID625094 | Binding constant for CDK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256613 | Average Binding Constant for Aurora2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624913 | Binding constant for TYK2(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID497611 | Inhibition of mouse recombinant N-terminal His6-tagged Abl by radiometric kinase assay | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
| The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796. |
| AID624751 | Binding constant for PIP5K1C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625012 | Binding constant for GAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256570 | Average Binding Constant for PIM2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435514 | Binding constant for ABL1(M351T) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624890 | Binding constant for p38-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID220435 | Selectivity against Zeta-chain (TCR) associated protein kinase 70 kDa (ZAP70) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID624764 | Binding constant for CLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624829 | Binding constant for CDK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256572 | Average Binding Constant for STK36; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID256648 | Average Binding Constant for RPS6KA5 (Kin.Dom 1); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID256661 | Average Binding Constant for PDGFRB; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID636434 | Inhibition of FER | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID1646081 | Inhibition of human RET | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID435829 | Binding constant for RPS6KA1(Kin.Dom.2 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435162 | Binding constant for FLT3(N841I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435657 | Binding constant for full-length IKK-epsilon | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1286656 | Antiinflammatory activity in differentiated human U937 cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 2 hrs followed by LPS-stimulation for 4 hrs by sandwich ELISA relative to vehicle-treated control | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma. |
| AID624998 | Binding constant for EGFR(G719C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID81724 | Selectivity against HER2 kinase | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID436055 | Binding constant for full-length YANK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636437 | Inhibition of FGFR2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID256655 | Average Binding Constant for CSNK1G1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435655 | Binding constant for ERK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624727 | Binding constant for FYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624949 | Binding constant for CSNK1G3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624825 | Binding constant for BMPR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256662 | Average Binding Constant for ERBB2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID636528 | Inhibition of TSSK2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID436024 | Binding constant for MRCKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624806 | Binding constant for RPS6KA4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1646063 | Inhibition of human CDK8 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID435663 | Binding constant for full-length MST4 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624914 | Binding constant for WEE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636424 | Inhibition of EPHA4 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624849 | Binding constant for CSNK2A2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636525 | Inhibition of TIE2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625018 | Binding constant for YES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624845 | Binding constant for CDK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256628 | Average Binding Constant for LYN; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624820 | Binding constant for ACVR2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID25723 | Area under curve was measured after intravenous dosing at 1 mg/kg in male cynomolgus monkey (70% PEG400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID624916 | Binding constant for ULK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435215 | Percentage AMPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID308411 | Inhibition of LPS-induced TNFalpha production in human whole blood | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site. |
| AID435167 | Binding constant for KIT(V559D) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435784 | Binding constant for CAMK2G kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435189 | Binding constant for full-length PDPK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624986 | Binding constant for ABL1(Q252H)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID127251 | Dissociation constant at Tm against human Mitogen-activated protein kinase p38 alpha (fluorescence exchange curve) | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Thermal denaturation: a method to rank slow binding, high-affinity P38alpha MAP kinase inhibitors. |
| AID435519 | Binding constant for AURKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624909 | Binding constant for TGFBR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID639674 | Antiinflammatory activity in LPS-stimulated human isolated PBMC assessed as inhibition of TNFalpha production preincubated for 1 hr prior to LPS-challenge by ELISA | 2011 | Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
| Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease. |
| AID625064 | Binding constant for PIM2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636910 | Inhibition of AKT2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID639971 | Binding affinity to N-terminus His-tagged human p38alpha expressed in Escherichia coli BL21 DE3 after 5 hrs by fluorescence analysis | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Structure-based design, synthesis and biological evaluation of N-pyrazole, N'-thiazole urea inhibitors of MAP kinase p38α. |
| AID625100 | Binding constant for NLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624808 | Binding constant for TRKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID445087 | Displacement of N,N'-(2,2'-(3,3'-disulfanediylbis(2,5-dioxopyrrolidine-3,1-diyl))bis(ethane-2,1-diyl))bis(2-(3-(3-tert-butyl-5-(3-naphthalen-1-ylureido)-1H-pyrazol-1-yl)phenylamino)acetamide) from inactive form of p38alpha expressed in Escherichia coli BL | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Displacement assay for the detection of stabilizers of inactive kinase conformations. |
| AID625115 | Binding constant for PAK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636479 | Inhibition of P38alpha | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624704 | Binding constant for NEK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256658 | Average Binding Constant for p38-beta; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID636483 | Inhibition of p70S6K | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624783 | Binding constant for FGFR3(G697C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435738 | Percentage p38delta MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636916 | Inhibition of aurora A | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435847 | Percentage DYRK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID624884 | Binding constant for PRKD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256670 | Average Binding Constant for ABL1(T315I); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624756 | Binding constant for MAP4K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435925 | Binding constant for PCTK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624710 | Binding constant for SRMS kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID277018 | Inhibition of Jnk2alpha2 | 2006 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
| Discovery and design of benzimidazolone based inhibitors of p38 MAP kinase. |
| AID8973 | Tested for plasma level after 90 min of 30 mg/kg dose administered in mice | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). |
| AID1286666 | Antiinflammatory activity in Balb/c mouse assessed as inhibition of neutrophil accumulation in bronchoalveolar lavage fluid at 0.2 mg/mL, it preincubated for 2 to 18 hrs followed by LPS challenge for 30 mins measured after 8 hrs by Neubaur hemocytometer | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma. |
| AID639747 | Binding affinity to p38alpha MAPK assessed as half life by surface plasmon resonance method | 2011 | Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
| Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease. |
| AID256668 | Average Binding Constant for ABL1(H396P); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435689 | Binding constant for full-length PFTK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636448 | Inhibition of GSK3-beta | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624875 | Binding constant for PDGFRB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435310 | Binding constant for FLT3(ITD) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID701484 | Antiinflammatory activity in po dosed Lewis rat assessed as suppression of Mycobacterium tuberculosis adjuvant-induced paw edema administered QD from days 15 to 24 post adjuvant-challenge measured on day 25 relative to vehicle-treated control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor. |
| AID256593 | Average Binding Constant for NEK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625110 | Binding constant for TRPM6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID127268 | Kd value and murine Mitogen-activated protein kinase p38 alpha complex was calculated | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). |
| AID636477 | Inhibition of NEK3 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625052 | Binding constant for PRKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID28117 | Maximum conc. (Cmax) was measured after oral dosing at 10 mg/kg in male cynomolgus monkey (100% PEG400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
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| A quantitative analysis of kinase inhibitor selectivity. |
| AID435789 | Binding constant for full-length CSNK2A2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256626 | Average Binding Constant for NTRK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID256580 | Average Binding Constant for CAMKK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID292894 | Suppression of lipopolysaccharide-induced TNFalpha release in mouse at 10 mg/kg, po after 30 mins | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
| Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry. |
| AID624817 | Binding constant for MYO3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1177340 | Inhibition of EphB4 (unknown origin) by FRET-based enzymatic assay in presence of 30 uM ATP | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1
| Structural Analysis of the Binding of Type I, I1/2, and II Inhibitors to Eph Tyrosine Kinases. |
| AID435417 | Percentage PAK4 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID624821 | Binding constant for YANK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256642 | Average Binding Constant for VEGFR2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435493 | Percentage PKD1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636518 | Inhibition of ROS | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435842 | Percentage Aurora C activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID673365 | Antiinflammatory activity in human whole blood cells assessed as inhibition of LPS-induced TNFalpha production after 4 hrs by time-resolved fluorescence assay | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
| Design and synthesis of novel p38α MAP kinase inhibitors: discovery of pyrazole-benzyl ureas bearing 2-molpholinopyrimidine moiety. |
| AID624714 | Binding constant for p38-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625140 | Binding constant for MARK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID127262 | Rate of association to Mitogen-activated protein kinase p38 alpha | 2003 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 13, Issue:18
| The kinetics of binding to p38MAP kinase by analogues of BIRB 796. |
| AID625093 | Binding constant for TNIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625062 | Binding constant for MAP3K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624841 | Binding constant for BLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624813 | Binding constant for MINK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435867 | Percentage NEK2a activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID256566 | Average Binding Constant for TNIK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435516 | Binding constant for ADCK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624843 | Binding constant for CAMK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636415 | Inhibition of CSK | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID1451481 | Binding affinity to wild type human biotin labelled p38 alpha (9 to 352 residues) expressed in sf21 insect cells SPR analysis | | | |
| AID435274 | Binding constant for ACVR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435160 | Binding constant for FER kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625069 | Binding constant for TLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435795 | Binding constant for EPHA4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435525 | Binding constant for EGFR(L858R) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256676 | Average Binding Constant for SRC; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435823 | Binding constant for full-length PAK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256666 | Average Binding Constant for ABL1(Q252H); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID673352 | Hepatotoxicity in Crlj:CD1(ICR) mouse assessed as change in plasma direct bilirubin level at 500 to 1000 mg/kg, po administered for 5 consecutive days measured 24 hrs post final dosing | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
| Design and synthesis of novel p38α MAP kinase inhibitors: discovery of pyrazole-benzyl ureas bearing 2-molpholinopyrimidine moiety. |
| AID624935 | Binding constant for FLT3(D835H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625060 | Binding constant for CAMKK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID495022 | Inhibition of phospho-p38 alpha activity by ELISA | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
| Optimization of alpha-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site. |
| AID636516 | Inhibition of ROCK-2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624827 | Binding constant for CAMK2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID127249 | Dissociation constant at Tm against human Mitogen-activated protein kinase p38 alpha | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Thermal denaturation: a method to rank slow binding, high-affinity P38alpha MAP kinase inhibitors. |
| AID624981 | Binding constant for ABL1(F317L)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435168 | Binding constant for LTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636416 | Inhibition of c-SRC | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625096 | Binding constant for STK36 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256672 | Average Binding Constant for CAMK2G; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435276 | Binding constant for BMPR1A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435238 | Percentage JNK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636495 | Inhibition of PIM2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624810 | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435911 | Binding constant for MEK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625122 | Binding constant for RET(M918T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID308420 | Protein binding in human plasma by equilibrium dialysis | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site. |
| AID624762 | Binding constant for DLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256640 | Average Binding Constant for PTK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624906 | Binding constant for S6K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID341053 | Ratio of IC50 for HSP27 phosphorylation to IC50 for p38alpha phosphorylation in IL-1-alpha-stimulated HLF cells | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID435777 | Binding constant for ABL2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID219489 | Selectivity against c-Jun N-terminal kinase 2-alpha 2 protein kinase | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID636409 | Inhibition of CHK2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625097 | Binding constant for TNNI3K kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435778 | Binding constant for full-length ADCK4 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1646076 | Inhibition of human JNK3 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID1451485 | Binding affinity to wild type human biotin labelled p38 alpha (9 to 352 residues) expressed in sf21 insect cells assessed as residence time by SPR analysis | | | |
| AID636427 | Inhibition of EPHB2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID636511 | Inhibition of PRKX | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435418 | Percentage PAK5 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID435192 | Binding constant for ROS1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID209191 | Inhibition of LPS-induced tumor necrosis factor-alpha (TNF-alpha) production in THP-1 cells | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID256636 | Average Binding Constant for JNK3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624969 | Binding constant for ROCK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435531 | Binding constant for MKNK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624798 | Binding constant for LKB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256622 | Average Binding Constant for JNK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435279 | Binding constant for full-length CDK9 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435288 | Binding constant for EPHB2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624918 | Binding constant for DYRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624917 | Binding constant for MST3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID215446 | Tested for inhibition of Tumor necrosis factor, alpha in LPS-stimulated mice at a dose of 10 mg/kg | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). |
| AID624724 | Binding constant for TAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID308413 | Inhibition of LPS-induced TNFalpha production in mouse at 10 mg/kg after 1 hr | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site. |
| AID513136 | Inhibition of Fyn kinase | 2006 | Nature chemical biology, Jul, Volume: 2, Issue:7
| Rational design of inhibitors that bind to inactive kinase conformations. |
| AID625022 | Binding constant for MUSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435410 | Binding constant for KIT kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256609 | Average Binding Constant for AAK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624708 | Binding constant for CDC2L1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624958 | Binding constant for PIK3C2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256631 | Average Binding Constant for FLT4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID636450 | Inhibition of HIPK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435903 | Binding constant for CDK8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256568 | Average Binding Constant for STK17A; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID636412 | Inhibition of c-KIT (D816V) | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID636403 | Inhibition of CDK2/cyclin A | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID436007 | Binding constant for AXL kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624920 | Binding constant for MRCKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636514 | Inhibition of RIPK2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID29098 | Half-life was measured after intravenous dosing at 1 mg/kg in male cynomolgus monkey (70% PEG400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID624709 | Binding constant for MYLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435820 | Percentage PKCalpha activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID624754 | Binding constant for NEK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID495020 | Inhibition of p38 alpha activity by ELISA | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
| Optimization of alpha-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site. |
| AID319698 | Inhibition of LPS-stimulated TNFalpha production in human whole blood | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| Structure-based design and subsequent optimization of 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) inhibitors of p38 MAP kinase. |
| AID624956 | Binding constant for EPHB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435405 | Binding constant for ERK8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624984 | Binding constant for ABL1(H396P)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624881 | Binding constant for PKAC-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1646064 | Inhibition of human DDR1 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID636410 | Inhibition of CK1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435413 | Binding constant for MLCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625132 | Binding constant for FGFR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435191 | Binding constant for full-length RIOK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID251720 | Inhibition of TNF-alpha production in rat joint after oral administration at 3 mg/Kg | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
| Design of potent and selective 2-aminobenzimidazole-based p38alpha MAP kinase inhibitors with excellent in vivo efficacy. |
| AID292889 | Distribution coefficient, log D at pH 6.0 | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
| Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry. |
| AID435146 | Binding constant for ABL1(H396P) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636406 | Inhibition of CDK5/p35 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624882 | Binding constant for PKAC-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435553 | Binding constant for PRKCD kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1286664 | Antiinflammatory activity in tobaco smoke-induced A/J mouse steroid refractory inflammation model assessed as inhibition of neutrophil accumulation in bronchoalveolar lavage fluid at 0.04 mg/mL, in bid administered for 3 days measured 96 hrs after last to | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma. |
| AID624888 | Binding constant for ERK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256579 | Average Binding Constant for MAP3K5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435909 | Binding constant for full-length LKB1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435152 | Binding constant for CAMK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256620 | Average Binding Constant for FLT3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID256559 | Average Binding Constant for EPHB4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID636507 | Inhibition of PKG1beta | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624965 | Binding constant for LZK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256664 | Average Binding Constant for EGFR; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435285 | Binding constant for DMPK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624871 | Binding constant for PAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624771 | Binding constant for TLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435412 | Binding constant for MAP3K5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625112 | Binding constant for YANK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624781 | Binding constant for CDK4-cyclinD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435665 | Binding constant for NEK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID339962 | Inhibition of human JNK1-alpha-1/SAPK1c at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
| AID636438 | Inhibition of FGFR3 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID436021 | Binding constant for LATS2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624982 | Binding constant for ABL1(F317L)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435496 | Percentage RIP2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID625041 | Binding constant for PIK3CA(H1047L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625079 | Binding constant for NEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624797 | Binding constant for PHKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435193 | Binding constant for RPS6KA6(Kin.Dom.1 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624859 | Binding constant for JAK1(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625119 | Binding constant for CAMK1G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435296 | Binding constant for MARK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID127075 | Binding affinity against human Mitogen-activated protein kinase p38 kinase evaluated by exchange curve | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID636900 | Inhibition of ABL1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID1646072 | Inhibition of human FRK | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID625111 | Binding constant for RIOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435747 | Percentage PRAK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636489 | Inhibition of PASK | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625107 | Binding constant for DMPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435324 | Binding constant for full-length RIOK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435401 | Binding constant for full-length DRAK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625098 | Binding constant for IRAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435429 | Binding constant for FLT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435181 | Binding constant for full-length p38-alpha | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625105 | Binding constant for EPHB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID599957 | Binding affinity to human KIT incubated for 1 hr by kinase binding assay | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
| Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. |
| AID436054 | Binding constant for TLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636491 | Inhibition of PDGFRbeta | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624772 | Binding constant for AURKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624955 | Binding constant for EPHB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435832 | Binding constant for SLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625130 | Binding constant for FGFR4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID341204 | Inhibition of JNK3 | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID256585 | Average Binding Constant for EPHA7; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID339966 | Inhibition of human SAPK2a/p38-alpha at 10 uM | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. |
| AID624887 | Binding constant for ERK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624749 | Binding constant for CASK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624912 | Binding constant for TYK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636478 | Inhibition of NLK | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435930 | Binding constant for PHKG2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435806 | Binding constant for MAPKAPK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435897 | Binding constant for ABL1(T315I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1646067 | Inhibition of human EPHA7 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID624716 | Binding constant for CSNK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636464 | Inhibition of LCK | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID624939 | Binding constant for FLT3(N841I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435929 | Binding constant for PAK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID249740 | In vivo threshold minimum effective dose for inhibition of rat paw-swelling after oral bid dosing for 14 days | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
| Design of potent and selective 2-aminobenzimidazole-based p38alpha MAP kinase inhibitors with excellent in vivo efficacy. |
| AID435662 | Binding constant for MST2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1646086 | Inhibition of human TNIK | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID624963 | Binding constant for LATS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624711 | Binding constant for STK35 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636418 | Inhibition of DDR2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID636513 | Inhibition of RET | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID513133 | Inhibition of JNK2alpha2 kinase | 2006 | Nature chemical biology, Jul, Volume: 2, Issue:7
| Rational design of inhibitors that bind to inactive kinase conformations. |
| AID435170 | Binding constant for MYO3A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624894 | Binding constant for MEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID341049 | Displacement of rhodamine-green labeled (2-(6-amino-3-imino-3H-xanthen-9-yl)-5-{[({4-[4-(4-Cl-3-hydroxyphenyl)-5-(4-pyridinyl)-1H-imidazol-2yl]phenyl}methyl)amino]carbonyl}benzoic acid from human p38alpha by fluorescence polarization | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID435693 | Binding constant for TGFBR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624775 | Binding constant for STK16 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624842 | Binding constant for BMX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625021 | Binding constant for LIMK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636494 | Inhibition of PIM1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID256656 | Average Binding Constant for p38-alpha; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624766 | Binding constant for p38-gamma kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256600 | Average Binding Constant for EPHA8; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624723 | Binding constant for CSNK1A1L kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256659 | Average Binding Constant for DAPK3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624852 | Binding constant for FES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID436013 | Binding constant for DMPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435651 | Binding constant for DCAMKL2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624803 | Binding constant for CHEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID308412 | Lipophilicity, log D at pH 7.4 | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site. |
| AID624792 | Binding constant for KIT(V559D,T670I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636461 | Inhibition of JNK2alpha2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435646 | Binding constant for BLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636439 | Inhibition of FGFR4 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435564 | Binding constant for TRKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID673354 | Hepatotoxicity in Crlj:CD1(ICR) mouse assessed as change in plasma AST level at 500 to 1000 mg/kg, po administered for 5 consecutive days measured 24 hrs post final dosing | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
| Design and synthesis of novel p38α MAP kinase inhibitors: discovery of pyrazole-benzyl ureas bearing 2-molpholinopyrimidine moiety. |
| AID256643 | Average Binding Constant for CAMK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624997 | Binding constant for EGFR(E746-A750del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435394 | Binding constant for CAMK2B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435533 | Binding constant for NEK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624768 | Binding constant for SRPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1380351 | Inhibition of p38alpha (unknown origin) | 2018 | Journal of medicinal chemistry, 08-09, Volume: 61, Issue:15
| Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations. |
| AID435936 | Binding constant for full-length SRPK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435648 | Binding constant for CAMKK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625031 | Binding constant for MRCKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435898 | Binding constant for ACVR1B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436046 | Binding constant for PRKD2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625099 | Binding constant for TAOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624722 | Binding constant for MKK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID436022 | Binding constant for full-length MEK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624794 | Binding constant for MET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID296932 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| Discovery and optimization of p38 inhibitors via computer-assisted drug design. |
| AID624940 | Binding constant for FLT3(R834Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256612 | Average Binding Constant for GAK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID636476 | Inhibition of MST2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID636484 | Inhibition of PAK2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625009 | Binding constant for EPHA3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624747 | Binding constant for SgK110 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624866 | Binding constant for MLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624777 | Binding constant for DDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435397 | Binding constant for CSNK1G1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435414 | Binding constant for MLK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636497 | Inhibition of PKCalpha | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID256627 | Average Binding Constant for RPS6KA2 (Kin.Dom. 1); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID636493 | Inhibition of PHKgamma2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435363 | Percentage MELK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636527 | Inhibition of TRKB | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435831 | Binding constant for RPS6KA5(Kin.Dom.1 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624837 | Binding constant for IRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID629190 | Antiarthritic activity in po dosed adjuvant-induced Wistar rat arthritis model assessed as change in paw volume administered once daily for 7 days by plethysmometry | 2011 | Journal of medicinal chemistry, Nov-24, Volume: 54, Issue:22
| 1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase. |
| AID625116 | Binding constant for ADCK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625135 | Binding constant for ADCK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636435 | Inhibition of FES | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID636468 | Inhibition of MAPKAPK5 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID625039 | Binding constant for PIK3CA(E545A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435941 | Binding constant for ZAK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1646073 | Inhibition of human NTRK1 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID1646065 | Inhibition of human DDR2 | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
| AID624848 | Binding constant for CSNK2A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435297 | Binding constant for MLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435539 | Percentage PHK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID636529 | Inhibition of WNK2 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435798 | Binding constant for FGR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436016 | Binding constant for full-length ERK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624967 | Binding constant for RPS6KA5(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435149 | Binding constant for AMPK-alpha2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435776 | Binding constant for ABL1(Y253F) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435150 | Binding constant for ARK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435775 | Binding constant for ABL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256625 | Average Binding Constant for PAK3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID341054 | Inhibition of LPS-stimulated TNFalpha release in human PBMC by ELISA | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes. |
| AID435289 | Binding constant for ERK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID636414 | Inhibition of COT1 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435166 | Binding constant for full-length JNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1286658 | Antiinflammatory activity in differentiated human U937 cells assessed as inhibition of LPS-induced of CXCL8 production preincubated for 2 hrs followed by LPS-stimulation for 4 hrs by sandwich ELISA relative to vehicle-treated control | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma. |
| AID435833 | Binding constant for full-length TNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256650 | Average Binding Constant for PIM1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID636423 | Inhibition of EPHA3 | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID1286655 | Inhibition of human recombinant p38 gamma assessed as phosphorylation of MAPKAP-K2 preincubated for 2 hrs followed by FRET peptide and MAPKAP-K2 addition measured after 1 hr by Z-LYTE assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma. |
| AID624978 | Binding constant for ABL1(E255K)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID636463 | Inhibition of KDR | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID435350 | Percentage ERK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID435995 | Percentage SRPK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3
| The selectivity of protein kinase inhibitors: a further update. |
| AID25724 | Area under curve was measured after oral dosing at 10 mg/kg in female BALB/c mice(100% PEG400) | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
| Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
| AID624717 | Binding constant for JNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625120 | Binding constant for EPHA8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624780 | Binding constant for CDK4-cyclinD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID319697 | Inhibition of LPS-stimulated TNFalpha production in human THP1 cells | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| Structure-based design and subsequent optimization of 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) inhibitors of p38 MAP kinase. |
| 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. |
| AID493040 | Navigating the Kinome | 2011 | Nature chemical biology, Apr, Volume: 7, Issue:4
| Navigating the kinome. |
| AID1797314 | Fluorescence Exchange Curve Assay from Article 10.1038/nsb770: \\Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site.\\ | 2002 | Nature structural biology, Apr, Volume: 9, Issue:4
| Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. |
| AID1797044 | Kinase Assay and Binding Constant Measurement from Article 10.1073/pnas.0504952102: \\Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.\\ | 2005 | Proceedings of the National Academy of Sciences of the United States of America, Aug-02, Volume: 102, Issue:31
| Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. |
| AID1797315 | Fluorescence Exchange Curve Assay from Article 10.1021/jm030120s: \\Thermal denaturation: a method to rank slow binding, high-affinity P38alpha MAP kinase inhibitors.\\ | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Thermal denaturation: a method to rank slow binding, high-affinity P38alpha MAP kinase inhibitors. |
| AID1799755 | Inhibition Assay from Article 10.1021/cb300128b: \\Targeting GSK3 from Ustilago maydis: Type-II Kinase Inhibitors as Potential Antifungals.\\ | 2012 | ACS chemical biology, Jul-20, Volume: 7, Issue:7
| Targeting GSK3 from Ustilago maydis: type-II kinase inhibitors as potential antifungals. |
| AID1797317 | UV-Thermal Melt from Article 10.1021/jm030121k: \\Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796).\\ | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). |
| AID1345304 | Human mitogen-activated protein kinase 14 (p38 subfamily) | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1345697 | Human mitogen-activated protein kinase 12 (p38 subfamily) | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID1345334 | Human mitogen-activated protein kinase 11 (p38 subfamily) | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID1345384 | Human mitogen-activated protein kinase 13 (p38 subfamily) | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID1345304 | Human mitogen-activated protein kinase 14 (p38 subfamily) | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2002 | Nature structural biology, Apr, Volume: 9, Issue:4
| Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. |
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2002 | Nature structural biology, Apr, Volume: 9, Issue:4
| Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |